Antiproliferative effect of oil refineries. Current therapy for osteoarthritis Selective COX blockers 2

ON THE HELP OF THE PRACTICAL LIKAR

© Karateev A.E., 2014 UDC 615.276.036.06

Selective Ingibitori Cyclooxygenase-2 І "STOCKED" of non-steroidal anti-inflammatory drugs: TWO METHODS OF PROPHYLACTICS Likarsky USKLADNEN

A. Karateev

FSBI "Scientific-Preceding Institute of Rheumatology IM. V.A. Nasonova "RAMS, Moscow

Non-steroidal anti-inflammatory drugs (NPZP) are an indispensable tool for the control of severe and chronic pain. The stench is widespread in case of ailments of the support-arm apparatus, as well as for pain relief from injuries and prompt engagement... Unfortunately, non-steroidal anti-fatigue can give a number of class-specific side effects, in front of feeding on the shlunkovo-intestinal tract (QCT) and heart-vascular system (CVS). We will be able to see accelerated treatment є NPZP-gastropathy, which manifests itself by the development of the slurry path і / abo two-fingered intestines(Duodenal ulcer), bleeding, perforation and damage to the passage of the shlunkovo-intestinal tract. Prevention of NPZP-gastropathy spiral on 2 main methods: transition to new, more non-baked preparations abo the sign of non-steroidal anti-pyrexia at once with strained anti-inflammatory drugs.

Zastosuvannya koksibiv yak method of prevention of shlunkovo ​​intestinal acceleration. The main reason "coxibiv" (from the English abbreviation COX) is the concentration of the activity of cyclooxygenase (COX) - the vibration of the infused COX: in therapeutic doses, the stench is practically unrecognizable in the form of the COX ... The price of a change in the negative injection of the oil refineries on the reduced potential of the mucous membrane of the intestinal tract and the change in the efficiency of the ear.

In Russia, the family of coxibs is represented by two drugs - celecoxib and etoricoxib, which have undergone a serious reconsideration to prove that they are better than nonselective COX-2 (n-NPZP) inhibitors.

Bezpeka celecoxib is approved for 2 large-scale randomized controls (PCI) - CLASS and SUCCESS-1. First of all, they have celecoxib (800 mg / dobu), as well as drugs for oral administration - diclofenac (150 mg / dobu) and ibuprofen (2400 mg / dobu), boules were diagnosed for 6 ms for about 8000 we have rheumatoid arthritis (RA) and osteoar- thrombus (OA). Low doses of aspirin - NDA (325 mg / day and mensh) could be recognized for the witnesses, which was taken in the bag by about 20% of the participants. summarily se-

Reasonable shlunkovo-intestinal deterioration was observed in 0.76% of ailments, when celecoxib was eliminated, and in 1.45% of patients in the active control group. The test was statistically unreliable, protestable in individuals who did not eliminate NDA: 0.44% versus 1.27% (p< 0,05). В 3-месячное РКИ SUCCESS-1 были включены только больные ОА, которые получали целекоксиб в дозе 200 или 400 мг (n = 8800), а также диклофенак (100 мг) или напроксен (1000 мг) (n = 4394). НДА применяли гораздо реже (7,1%), поэтому результаты были однозначны: желудочно-кишечные кровотечения и перфорации язв были выявлены у 2 и 7 больных (р = 0,008).

Low risk of intestinal and intestinal acceleration in case of vicorian celecoxib, in addition to metaanalysis of 31 PCI (total 39 605 ailments): non-safety of intestinal and intestinal acceleration in case of total intake of 2% % altogether).

Celecoxib passages showed 2 PCI (3 і 6 mіs, n = 1059), in which the dynamics of the endoscopic picture of the upper endoscopic picture of the upper intestinal tract was injected on the same drug (400 mg), naproxen (1000 mg) and ). As a result of the twisting of the slurry / DPK, the winery was found in 4 і 25% (p = 0.001) і 4 і 15% (p = 0.001) apparently.

The remaining hour, when assessing the negative infusion of oil refineries on the small intestine, more and more respect is given to the development of the pathology of the small intestine due to the development of the penetration and chronic inflammation, due to the components of the penetrating chemical diseases in the intestinal tract. The process of acceleration can be manifested by important bleeding, perforation and stricture; however, the most characteristic of this sign is subclinical blood loss, which leads to the development of chronic hypersensitivity anemia (ZDA). The rest of the camp of patients, changing Kisnev's capacity of blood and strength to new age, is the reason for the development of the risk of cardiovascular disasters.

Complex pіdhіd before the assessment of shlunkovo-intestinal acceleration buv vikoristany G. Singh і spіvavt.,

They conducted a meta-analysis of 52 PCI (n = 51,048), in which celecoxib was administered with placebo and n-NPZP. In total, the incidence of shlunkovo-intestinal bleeding, perforation, twisting of the shlunka and duodenum, as well as ZDA, was 1.8%. The whole indicator is not significant in the case of a placebo (1.2%), ale on a lower level, and in the case of vicorian n-refractory (5.3%, p< 0,0001) .

The total assessment of the oil refinery injected on the pipe was carried out in РСІ CONDOR. In the course of the last 4481 ailments of the RA abo OA with a high risk of NPZP-gastropathy, which is not the infection of Helicobacter pylori, with a stretch of 6 msec celecoxib (400 mg) or diclofenac (150 mg / dobu) and / dobrazole) (20 mg / dobu) and omeprazole. The number of serous intestinal slimes was significantly higher in case of vicious combination of diclofenac and omeprazole-la was significantly higher; % and 6% of illnesses, according to the case (р< 0,001) .

Another one of the advantages of celecoxib for the small intestine was the robot J. Goldstein and spivavt. , It is based on the method of video capsule endoscopy. During the course of a trial, 356 volunteers took two sessions of celecoxib (400 mg), naproxen (1000 mg) in addition to omeprazole (20 mg) or placebo. There were no problems in the flow to the mill of the upper intestinal tract between the groups; In the celecoxib group, the number of patients with small intestinal mucosa was significantly lower than in the naproxen group (16 and 55%, p< 0,001), хотя и больше, чем в группе плацебо (7%) .

GI-REASONS has become a new customer of the celecoxib transfer, in the course of a safe preparation, it was evaluated in 4035 OA patients, who were treated for 6 msec. The control was laid by 4032 ailments of OA, yakim buli

Celecoxib H. pylori -

Small. 1. The frequency of serous intestinal and intestinal acceleration, including a decrease in the hemoglobin level of more than 20 g / l, for a 6-month intake of celecoxib and traditional oil refineries, in the presence of H.

special n-refinery. The peculiarities of the robotics chain were the field of detection of H. pylori (the microorganism was detected in approximately 33.6% of the participants), they introduced vikoristovuvati proton pump inhibitors (IPP) and the blockers of H2-receptors were removed by 22.8%. viklyuchennya to the reception of the NDA. The main criterion for non-baking was the frequency of shlunkovo-intestinal acceleration, including the decrease in hemoglobin level by 2 g / dl, as it is possible to tie the mucous membrane of the shlunkovo-intestinal tract. The clinically significant slurry-intestinal acceleration in vicorian celecoxib was significantly higher (1.3% and 2.4% apparently, p< 0,001) (рис. 1).

Prior to GI-REASONS, yak і CONDOR, we clearly supported the greater safety of celecoxib in the case of traditional oil refineries, including in situations that simulate a real classroom practice.

Etorikoksib, yak i celecoxib, bv of devices for the advancement of the safety of the therapy of oil refineries. Having become on this year's day the point of development of the concept of selective ingibitoriv COG-2: the spivid activity of engaging concentration COG-1 / COG-2 for those who are close - 6 to become close in an hour

First, the last time they were unambiguously pidtverzhuvali a high level of safety without etorikoksibu. So, metaanalysis of PCI, completed before 2003, in which etoricoxib and n-NPZP were infused (n = 5441), showing a significantly lower frequency of unsafe shlunkovo-intestinal acceleration in the case of a new drug. The lateral frequency of bleeding, perforation and clinically twisting bends on the etore-koksibi (60-120 mg) aphrodisiac was 1.24%, with vicious drugs in porous (diclofenac, naproxen, ibuprofen) - 2.48% (p< 0,001) .

Serious proof of the greater safety of etoricoxib was 2 large-scale 12-mile PCI (n = 742 and n = 680), in which the frequency of development of endoscopic virazoks of the upper viddili in the cerebrospinal tract in patients with ailments was assessed. (2400 mg), naproxen (1000 mg) or placebo. The acceleration rate for the smallest intake of etoricoxib was indicated in 8.1 and 7.4% of the ailments, i.e., Bolsh lower in 2 times higher, lower in the case of n-refractory treatment (17 and 25.3%, p< 0,001), хотя и чаще, чем при использовании плацебо (1,9 и 1,4%) .

Reading the line of proofs of the Etore-Koksibi pass, however, the bullet was destroyed after the publication of the results of MEDAL, which was the best on the current day of the RSI refinery. With a clear message, I’ll tell you that etorikoksib is not great for the CCC, not the traditional oil refinery plant. Having become a MEDAL member, 34 701 patients from OA and RA were treated with etoricoxib (60 or 90 mg) or diclofenac (150 mg / dobu) for a stretch of at least 1.5 times. With a great deal of ailment, if it was obvious, the demonstration could be victorious IPP and NDA. Ito-

The main result of these problems is that the number of cardiovascular accidents (including fatal outcomes) with vicorian etoricoxib and diclofenac is practically the same.

In addition to the data on the frequency of serious shlunkovo-intestinal acceleration steel for MIDAL organizers is an unacceptable surprise. I want the total frequency in case of vikorystanny etoricoksibu bula is one hundred percent lower, less in case of stasis diclofenac (1 and 1.4%, p< 0,001), число эпизодов желудочно-кишечных кровотечений оказалось фактически равным - 0,3 и 0,32 эпизода на 100 пациентов в год. При этом одинаковая частота желудочно-кишечных кровотечений наблюдалась независимо от сопутствующего приема НДА и ИПП . Столь же трудно объяснить другой результат MEDAL. Оказалось, что частота побочных эффектов в дистальных отделах ЖКТ (таких, как кишечное кровотечение) при приеме эторикоксиба и ди-клофенака практически не различалась - 0,32 и 0,38 эпизода на 100 пациентов в год .

On the other hand, it is impossible to say that the results of MEDAL will increase the strength of those who are in front of them, while the stench of thought will be heard, but we do not see all aspects of the development of the intestinal-intestinal acceleration, which may be associated with the end of all non-steroidal pathogenetic officials, Which do not mean when їх is apparently short-term victorian.

In such a rank, let us talk about the value of reducing the risk of serious intestinal shlunkovalny and increasing the tolerance of coxibs (celecoxib and etoricoxib) in some cases of n-refinery. Prove that celecoxib is more accurate; the drug has shown itself to be safe not only in the upper, but in the lower parts of the intestinal tract.

Low rhizic shlunkovo-intestinal accelerated with vikorystanny celecoxib is given to populational dosages. In the end of 2012, there were published reports of meta-analyzes of 28 epidemiological robots (victors from 1980 to 2011), in which the development of slurry-intestinal acceleration was assessed during victorian growth of oil refineries. Celecoxib demonstrating the least significant recession (RR) of the intestinal shlunkovalny - 1.45; nebezpeka bula is clearly visible in case of vicorian ibuprofen (1.84), diclofenac (3.34), meloxicam (3.47), nimesulide (3.83), ketoprofen (3.92), naproxen (4.1) and indomethacin ( 4.14). The same low rhizic of shlunkovo-intestinal accelerated, as in celecoxib, the authoritative last name was given for one of the representatives of traditional oil refineries - aceclofenac (1.43).

Celecoxib with all its merits, however, is far from ideal. With the presence of a high risik (zokrema, in patients, who are not very quick to go, or take NDA), there is a possibility of a serious reduction in the intestinal tract. We have a plan for Velmi

shows є dan F. Chen і spivavt. ... 441 patients with rheumatic illnesses became a participant of the whole pre-sluggishness, in those who had a history of severe bleeding from the paths of the upper intestinal tract, which were diagnosed at the bottom of the refinery. For a successful fight against H. pylori, all ailments were treated with celecoxib (400 mg / dob) for 12 msec, either without additional prophylaxis, or in combination with esomeprazole (20 mg). During the period, the relapse of bleeding veins was prevented in 8.9% of the ailments who received only celecoxib, and in one of the patients who took celecoxib with esomeprazole.

The main shortcomings of celecoxib and etorikok-Siba є belonging to the highly selective ingibitoriv COG-2 - the same type of oil refinery, which can be used for the production of antibiotics, but it is not sterile.

Thus, the results of the previous MEDAL, if they did not show an increase in the number of cardiovascular catastrophes with vicoristanna etoricoxib, showed a virally negative inflow to the pro-progressive arterial hypertension... In addition, the population of recent and meta-analyzes of PCI indicate about a hundred of cardiovascular rhizic, tied to the use of a drug.

It means that many experts are using celecoxib on the list of all coxibs to make it safe for CCC. The whole fact has been confirmed by a series of populational doslejens, which are seen in a kind of systematic survey (including metaanalysis) P. McGettigan and D. Henry. Authors evaluated the data of 30 days of admission control, which included 184 946 ailments with cardiovascular acceleration, and 21 cohort adolescents (in total there were 2.7 million patients), with vicorystann_ celecoxib, sklav 1.17 (1.08-1.27); The number of trochi is higher, lower on tlі naproxen 1.09 (1.02-1.16), and so it is with the consumption of ibuprofen - 1.18 (1.11-1.25). In case of vicious non-steroidal anti-pyretic contamination, the indicator appeared to be girshim for - 1.20 (1.07-1.33) for meloxicam, 1.30 (1.19-1.41) for indomethacin, 1.40 (1.27- 1.55) for diclofenac and 2.05 (1.45-2.88) for etoricoxib.

It is not possible, however, to ignore a number of serious preliminaries, which may lead to celecoxib, which can cause cardiovascular disasters. So, in 2011 S. Trelle i spivavt. The results of a meta-analysis of 31 PCI (a total of 116 429 ailments) were published, in which they were vaccinated without bake celecoxib, Etore-coxibi, lumirocoxib and rofecoxib; served as control n-NPZP, as well as placebo. Criteria for assessing the development of myocardial infarction, stroke and death in cases of cardiovascular accidents. As a matter of fact, prior to any given risk, the development of myocardial infarction on aphids

when taking celecoxib appears to be visible, not when taking etoricoxib (OR 1.35 і 0.75), and also drugs in oral administration - diclofenac (0.82) and naproxen (0.82), ale lower, lower in ibuprofen (1.61) ... Naygolovnishe, in case of vicorian celecoxib, there is an increase in the risk of a lethal result (2.07), especially in the case of proxency (0.98). True, the wine is usually lower, lower with vicorian ibuprofen (2.39) and lower, lower with stasis diclofenac (3.98) and etoricoxib (4.07).

The rate of thromboembolism is shown in the part of the PCI. So, in the presumed food of the prescriptive SUCCESS-1 in the ailments, when celecoxib was eliminated, there were 10 types of myocardial infarction (0.55 per 100 patients / rocks), and in the case of naproxen, and 100 diclofenacs (0 ); Not sure (p = 0.11). In pre-admission GI-REASONS, the frequency of cardiovascular acceleration on thyroid celecoxib and n-NPZP did not increase: 0.4% 0.3%, zealous revascularization (4 types).

Another indication of the potent negative infusion of celecoxib into the heart-vascular system was the scale of the population of G. Gislason and co-ed. ... The author was responsible for the accumulation of the presence of the oil refinery plant and the risk of death of the ailments, who had suffered myocardial infarction. 58,432 patients became the group before they became patients, who completed a successful course of treatment for the first myocardial infarction in the period from 1995 to 2002, Nadal 9773 patients had myocardial infarction again, and 16 573 patients. Having shown the conduct of analyzes, the acceptance of any oil refineries is associated with the hundredth risk of death of patients. In case of vicorian celecoxib, nebezpeka appeared to be the best (with a vignette of rofecoxib) - HR 2.57; for diclofenac tsey the index of clavs is 2.40, and for ibuprofen it is 1.50.

This rank, obviously, is celecoxib for the current day - the gold standard of gastrointestinal tolerance. Protecting the vicarystannya celecoxibu to the problems of a non-baked vicoristannya oil refinery plant, obviously, is not brought up.

A combination of non-selective non-steroidal anti-inflammatory drugs and anti-inflammatory drugs has been fixed. Another method for the prevention of NPZP-gastropathy is the administration of gastroprotectors, who have been shown to purify the intestinal tract from negative inheritances from non-steroidal anti-festering diseases. The first of them became a synthetic analogue of PGE2 misoprostol, which has absorbed the unpleasant traces of blockade of COX-1, and then, having passed the development of the intestinal shlunkovyh, tied with the priyoma of non-steroidal anti-firing devices. The main proof of its effectiveness was the 12th anniversary of the RSI MUCOSA, participants in the boule of 8843 patients from the RA

zoprostol (200 mcg 4 times per dobu) or placebo. Misoprostol significantly reduced the risk of shlunko-intestinal acceleration: for example, bleeding and perforation in the group of active therapy for the disease in 0.76% of patients, in the control group - in 1.5% (p< 0,05) .

On the basis of a gastroprotective basis, the “stolen” NPZP, such as arthritis-tech, should be given 50 mg of diclofenac sodium and 200 mcg of misoprostol.

It's a pity, misoprostol is not very tolerable: it often suffers from dyspepsia and diarrhea. Victory efficiencies and an inaccurate scheme of storing them, they have simply surrounded it in real practice, especially when there have appeared selective engaging in COG-2 and a cob of a wide victorian IPP.

IPP shvidko gained popularity in the capacity of two and three gastroprotectors. A series of large-scale PCI clearly confirmed its effectiveness in the treatment and prevention of NPZP-gastropathy, but not least, the problem of NPZP-gastropathy did not become an increase in the type of therapy and one of the main reasons for the major - lack of it.

Unfortunately, there is a significant part of the ailments, which may be a serious factor in the risk of shlunkovo-intestinal acceleration, and at the same time regularly vicious oil refineries, do not take the signs of gastroprotective drugs. It can be tied with a singular lack of hand for ailments ("take two pills to replace one"), for the benefit of treatment, as well as for reasons of motivation in this case, if the Tektor, why don't my shlunnits hurt? "). In addition, the kidnapped children can simply forget and miss out on the prodigious efforts.

The problem of the kindness of the robot of the American scientists J. Goldstein and the spivavt. They evaluated the sickness before gastroprotective therapy in a cohort of 144,203 ailments for rheumatic illnesses, who took NPZP. IPP or H2-blockers are strictly recommended. 1.8% of ailments in conjunction with a serious rhizic of the intestinal and shlunkovyh accelerated, however, as vyavilosya, mayzhe tretina (32%) of the patients were victoriously took gastroprotectors irregularly or did not call them. First, it called to the most unacceptable inheritances: a rhizic of shlunkov-intestinal bleeding in individuals who did not receive gastroprotective therapy, which was 2.5 times more common, but not in ailments, they neatly displayed the sign of a doctor.

The key to the finalization of the addiction of the sickness of the sick can be the use of combined drugs, to avenge non-steroidal anti-fatigue and anti-trauma problems. The revival of the idea of ​​the "stolen oil refinery" appeared 20 years later after the stem of Artro-tech, and the main reason for this was the decrease in interest to selective COG-2 Ingibitors in the case of "crises of coxibs".

The current main official, who is surrounded by victorian oil refineries, is rich in experts who do not meddle in the pathology of the intestinal tract, but rather for cardiovascular disasters. aje effective technique The increase in cardiovascular surgery, tied to the oil refinery plant, is, unfortunately, not broken up until now. One effective method for the prevention of thromboembolic acceleration is a sign of anti-thrombotic activity, such as NDA, which rapidly increases the amount of slunk-intestinal acceleration.

If I want the negative inflow on the CCC to be applied to the number of class-specific side effects of the oil refinery, the middle є of the preparation, for some risiks the development of the rapid development is low. Tse traditional (nonselective) oil refineries, and the known leader of the middle of them, according to the data of the number of populational and key people, naproxen. The drug is followed by ibuprofen and ketoprofen, which can also be used to achieve a low frequency of cardiovascular acceleration.

The very same preparations are the most thoroughly vikoristovuvati for the establishment of combined use. Yak gastroprotection is the most acceptable IPP: the stench is effective, handy at the victorian and well tolerated. True, the IPP can give a powerful bit of an effect, such as a frequency adjustment intestinal infections, Out-of-pocket pneumonia, a change in the metabolism of bedbugs-dagrel and methotrexate. In addition, in the last few years, it is necessary to discuss nutrition about a possible negative infusion of an intravenous injection into the progression of postmenopausal osteoporosis and an increase in the risk of osteoporotic fractures. At the same time, the efficiency for the improvement of the inconsistent shlunkovo-intestinal accelerated completely compensates for the relatively low risk of possible side effects, which can be affected by the IPPs themselves.

The idea of ​​a one-hour consumption of "cardiopausible" n-NPZP and IPP, which caused negative inheritance of the first drug on the slunk-intestinal tract, was realized in the case of a fixed formulation of the combination of naproxene and anemia.

In order to confirm the decrease in the frequency of the intestinal-intestinal acceleration with vicoristannі of a new drug, bulo viconano 2 large-scale 6-month PCI (n = 854). In cich robots, a test of the FKNE was carried out and an extraordinary intestinal-rozchinny naproxen was carried out. According to the recognized results, the frequency of slings and DPKs, which occurred on the bottom of the FKNE, dropped in the first preliminarily 4.6%, and in the other - 8.1%. Among the ailments, who were trimmed only on proxies, the twists appeared in a few times (28.2 and 30% apparently, p< 0,001). При этом у пациентов, получавших ФКНЭ в сочетании с НДА, язвы желудка развились лишь у 3%, а у получавших напроксен вместе с НДА - у 28,4% (р < 0,001) .

The total tolerance of the new drug, as a larger world, begins with the development of dyspepsia, so it itself became more beautiful. The number of witnesses through secondary slurry-intestinal defects in ailments who took FKNE, fell 3.2 і 4.8%, in those who took naproxen only - 12% і 11.9% (р< 0,001) .

Another stage of vivchennya perevag FKNE was the second step with celecoxib - a drug that, as it is meant to be, is rightfully used by the best non-baked in the middle of all oil refineries for the development of secondary slurry-intestinal effects.

The test of FKNE and celecoxib was carried out within the framework of two identical 12-stage PCIs (n = 619 and n = 610). Pre-juvenile groups were stored by patients with OA, yakim boules of FKNE (1 tablet 2 times per dobu), celecoxib (200 mg / dobu) or placebo. new drug did not submit for the effectiveness of the drug. Too much portability, then it was more beautiful (not correct) with vicorian combined drug. Thus, the number of vidmins through the intestinal shlunkovalnennogo on the first dose of FKNE, celecoxib and placebo dropped in the first preliminaries 1.2, 1.6 and 2.4%, and in the other - 0.8, 3.7 and 2.5% ...

One hour with FKNE, having blown one more light drug combinations Take revenge on ketoprofen (in doses of 100, 150 and 200 mg) in conjunction with omeprazole. As a whole, the project can be assessed as promising due to the fact that ketoprofen is an effective analgesic, and lykarska form With confidence in the vivilny of the dialectical speech, we allow you to take it 1 time for the dob, the protesting classmates have been shown to be safe for a new drug, still feigned, so it is easy to judge about its dignity.

The only alternative to IPP yak gastroprotector is the H2-receptor blocker famotidine. The proof of its effectiveness was 6-month PCI, in every 285 ailments, taking non-steroidal anti-fumes, taking famotidine (80 mg, 40 mg) or placebo. Until the end of the period, the number of slink / WPC bends was 10, 17 and 33% altogether. Tsya growth, however, proved to be a reliable deprivation for famotidine at a dose of 80 mg (^< 0,05) .

By all appearances, there are no great PCI, in which the direct preparation of famotidine and IPP was carried out for the prevention of NPZP-gastropathy. To protect the efficiency, it is possible to follow the results of the E N і spіvavt. ... Doslidzhuvan to the group got 311 ailments ischemic ailment heart, the combination of NDA and clopid-Grelya was designated as a yakim; In addition, during the development of severe coronary syndrome, a course of enoxyparin abo thrombolisis was carried out. For the prophylaxis of slunk-intestinal acceleration for the entire term of the antiplatelet therapy (from 4 to 52 cases), famotidine (40 mg / dobu) or esomeprazole (20 mg / dobu) was prescribed. As a result,

in the case of naproxen in the case of ibuprofen with esomeprazole and famotidine

Small. 2. The results of 6-month clinical trials of fixed combination of NPZP and gastroprotectors: naproxen 500 mg in addition with esomeprazole 20 mg 2 times per dose (n = 854) and ibuprofen 800 mg per dose 26.6 mg per dose = one thousand three hundred and fifty-two).

intestinal bleeding developed in 9 ailments, when famotidine was eliminated (6.1%), and in 1 (0.6%) patient, who took esomeprazole ^< 0,001) .

In such a rank, famotidine is readily used by the IPP from a prophylactic efficacy that is quickly knitted with the use of NDA. Obviously, NPZP-gastropathy, the situation is not very clear, it is unlikely that famotidine is associated with perevagi. At the same time, a number of experts vvazayut an important experience of famotidine in the rapidity of the power of the IPP, and smut, a negative influx on the metabolism of clopidagrel, the most important component of complex antiplatelet therapy.

Not long ago, the original drug Duexis® appeared on the US pharmacological market, to revenge 800 mg of ibuprofen and 26.6 mg of famotidine. The drug should be taken 3 times for dobu, i.e. the maximum dosage is transferred to ibuprofen - 2400 mg, in addition to a high dose of fa-motidin - 80 mg / dobu.

Not long ago, published data on 6-month old PCI REDUCE-1 and 2 (all one thousand three hundred and fifty two ailments), so that the drug was tested. It means that, in the case of the FKNE vip tests, the patients in the cich pre-adolescent chick-intestinal rhizomes have a lot of problems with the lower ones: the middle age is 55 years, the average age is 15% - 6,2% anamnesis - 6,2%. According to the given data, the number of slurry lines on the combined preparation was 12.5%, in the control - 20.7%, and the DPK line was 1.1% and 5.1%.

If there is a difference in the frequency of virazoks, it is obvious that protests with vicorian combination of ibuprofen and famotid in the stench were more frequent than with vicorian FKNE (Fig. 2). If I want to do so, I’m not called eligible, but I’m obviously asking for it, some of the robots are more likely to be motivated, some of the characteristics of the ailments.

An important part of the duexis can be included in the warehouse of ibuprofen. Є vagomi dana,

What about those who change the anti-thrombotic effect of NDA, which is shown to some patients with high cardiovascular disease. Negative interaction with NDA can quite interfere with the possibility of storing the combination of ibuprofen and famotidine in patients with a kidney disease, and even more of them may be involved in the treatment of the cardiovascular anti-vascular system.

I would like to see the concept of combined drugs in the dungeon of cicava, in her case, she has a minus. So, the preparation is not manual for short courses, or in the regime for vimoga. For example, the intestinal solution of naproxen in the FKNE warehouse will be repaired in 3 years after receiving a treatment, and hence, the drug should be used to control chronic pain, but not for an urgent purchase.

Our problem is related to the fact that IPP and famo-din will prevent the loss of the upper viddil in the slunk-intestinal tract, which does not flow into the development of the refinery-enteropathy. And tsya pathology, as it is shown, it can be even more serious of clinical significance.

The breadth of the pathology chain demonstrates the results of M. Doherty's robots and spivavt. ... The authors evaluated the efficacy of ibuprofen and paracetamol (in monotherapy or in combination) in 892 patients with OA. Participants in the last few weeks put 4 groups: in the 1st buv the signs of paracetamol (1 g), in the 2nd - ibuprofen (400 mg), in the 3rd - paracetamol (0.5 g) and ibuprofen (200 mg), in 4 th - paracetamol (1 g) and ibuprofen (400 mg); All the ills were taken 3 times. At the same time, after 3 m / s, the decrease in hemoglobin level by 1 g / l was determined in 20.3, 19.6, 28.1 and 38.4% of the ailments.

It can be seen that in the case of vicorian ibuprofen at a dose of less than 1200 mg / day in a dermal patient, the development of subclinical intestinal blood loss was indicated. And vikorystannya duexis transferring is trivial with 2400 mg of ibuprofen!

Likewise, there can be problems, but it’s possible for me to take naproxen: I’ve also shown a quote from J. Goldstein’s prescription and spivavt. In a large number of volunteers, who took naproxen with ome-prazol for 2 years, it meant the appearance of erosive changes in the mucous membrane of the small intestine.

At the same hour, the real critical information is allowed to assess the meaning of this medical problems... At the end of the day, it’s worthwhile, J. Goldstein and spivavt. They introduced the injection of oil refineries into the small intestine mill, and were among the organizers of 6-month old PCI (n = 854), in which they used the FKNE bake and snake naproxen. With a lot of clues about the development of anemia among the participants of the cich doslidzhen it is not. Similarly, there were no serious problems with the pathology of the small intestine in patients who were treated with FKNE, with celecoxib. So, in total, in two PCI (n = +1229) on a 3-month intake of the combination of naproxen and esomeprazole, the decrease in hemoglobin level is more than

Reconciliation and shortcomings of coxibs and fixed combination of n-refineries and gastroprotectors, as well as for the prevention of refractory-gastropathy

exponent

Coxibi (celecoxib, etoricoxib)

n-NPZP + gastroprotectors (Vimovo ™, Duexis®, Axorid®) *

perevagi

shortcomings

Tsilova group of patients

Shvidka diya

Reducing the risk of development of pathology in the distal pathology of the slunk-intestinal tract, including chronic blood loss associated with NPZP-enteropathy (brought to celecoxib)

Greater high risk of development of cardiovascular-them accelerated in porous with n-oil refineries (using naproxen and ibuprofen): Combination of NDA for development of rapid development of slurry-intestinal

Young children with chronic pain and chronically ill, bureaucrats can develop the development of shlunkovo-intestinal acceleration, without a concomitant pathology of the CVS

Low frequency of acceleration from the side of the upper viddil_ in the shlunkovo-intestinal tract

Low frequency of development of the slurry paths when combining with aspirin

Beautiful portability based on traditional oil refineries

Going to the warehouse of combined drugs in n-oil refineries is not safe in the plan for the development of cardiovascular disasters (especially naproxen)

Do not come for pain relief (Vimovo ™)

Do not underestimate the development of pathology of the distal pathology in the shlunkovo-intestinal tract

Possibility of development of side effects associated with a gastroprotective drug ** Can reduce the antithrombotic effect of aspirin (ibuprofen)

Patients of a senior with chronic pain associated with rheumatic illnesses, with rhiziks, the development of intestinal and cardiovascular diseases

Note. * - Duexis® and Axorid® preparations are not registered in Russia; ** - IPP can increase the development of intestinal infections, pneumonia, change the effectiveness of the clopidogrel, and in case of trivial (bagatory) priyomy, the risk of progression of postmenopausal osteoporosis.

by 20 g / l, it was indicated that it was deprived of 3 patients (in the middle they took celecoxib from one). In REDUCE-1 and 2, it was indicated that the decrease in hemoglobin by 20 g / l was less than 2 per second - an offense in patients who took the drug off the combination.

At the end of the day, it means that the prevention of severe intestinal and intestinal acceleration in patients who require an amount of non-steroidal anti-fatigue diseases is not easy to establish, but it is not easy to find the retardation of individual factors. In the Danish hour in the arsenal of the Russian lykar

Karateev Andriy Evgenovich - dr honey... sciences, head. lab. [Email protected]

LITERATURE (REFERENCES)

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3. Singh G., Fort J., Goldstein J. et al. Celecoxib versus naproxen and diclofenac in osteoarthritis patients: SUCCESS-1 study. Am. J. Med. 2006; 119: 255-66.

4. Moore R., Derry S., Makinson G., McQuay H. Tolerability and adverse events in clinical trials of celecoxib in osteoarthritis and rheumatoid arthritis: systemic review and meta-analysis on information from company clinical reports. Arthr. Res. Ther. 2005; 7: 644-65.

5. Simon L., Weaver A., ​​Graham D. Anti-inflammatory and upper gastrointestinal effects of celecoxib in rheumatoid arthritis: a randomized control trial. J. A. M. A. 1999; 282; 1921-8.

6. Emery P., Zeidler H., Kvien T. et al. Celecoxib versus diclofenac in long-term management of rheumatoid arthritis: randomized doubleblind comparison. Lancet. 1999; 354: 2106-11.

є 2 two tools for the development of non-alcoholic refinery therapy: selective reactions of COX-2 (coxibi) and a combination of n-proxene and esomeprazole. Quite a few preparations may be perevagi and incomplete (div. Table), an analysis of which allows you to see the whole group of patients, some of which will be most docile. If you don't see any competitors - it will be better, coxibi and Vimovo ™ will add one to one, expanding the ability to treat chronic pain.

7. Sands G., Shell B., Zhang R. Adverse events in patients with blood loss: a pooled analysis of 51 clinical studies from the celecoxib clinical trial database. Open Rheumatol. J. 2012; 6: 44-9.

8. Singh G., Agrawal N., Makinson G. et al. Safety without borders: upper and lower gastrointestinal safety of celecoxib in a pooled analysis of 52 prospective, randomized, double-blinded, parallel-group clinical trials. EULAR-2010 THU0437.

9. Chan F., Lanas A., Scheiman J. et al. Celecoxib versus omeprazole and diclofenac in patients with osteoarthritis and rheumatoid arthritis (CONDOR): a randomized trial. Lancet. 2010 rock; 376: 173-9.

10. Goldstein J., Eisen G., Lewis B. et al. Video capsule endoscopy to prospectively assess small bowel injury with celecoxib, naproxen plus omeprazole, and placebo. Clin. Gastroenterol. Hepatol. 2005: Dodati 3-13.

11. Cryer B., Li C., Simon L. et al. GI-REASONS: A Novel 6-Month, Prospective, Randomized, Open-Label, Blinded Endpoint (PROBE) Trial. Am. J. Gastroenterol. 2012; 108 (3): 392-400.

12. Schwartz J., Dallob A., Larson P. et al. Comparative inhibitory activity of etoricoxib, celecoxib, and diclofenac on COX-2 versus COX-1 in healthy subjects. J. Clin. Pharmacol. 2008, 48 (6): 745-54.

13. Ramey D., Watson D., Yu C. et al. The incidence of upper gastrointestinal adverse events in clinical trials of etoricoxib vs. non-selec-

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14. Hunt R., Harper S., Watson D. et al. The gastrointestinal safety of the COX-2 selective inhibitor etoricoxib assessed by both endoscopy and analysis of upper gastrointestinal events. Am. J. Gastroenterol. 2003 98 (8): 1725-33.

15. Cannon C., Curtis S., FitzGerald G. et al. Cardiovascular outcomes with etoricoxib and diclofenac in patients with osteoarthritis and rheumatoid arthritis in the Multinational Etoricoxib and Diclofenac Arthritis Long-term (MEDAL) program: a randomized comparison. Lancet. 2006; 368 (9549): 1771-81.

16. Laine L., Curtis S. P., Cryer B. et al. Assessment of upper gastrointestinal safety of etoricoxib and diclofenac in patients with osteoarthritis and rheumatoid arthritis in the Multinational Etoricoxib and Di-clofenac Arthritis Long-term (MEDAL) program: a randomized comparison. Lancet. 2007; 369: 465-73.

17. Laine L., Curtis S., Langman M. et al. Lower gastrointestinal events in a double-blind trial of the cyclo-oxygenase-2 selective inhibitor etoricoxib and the traditional nonsteroidal anti-inflammatory drug diclofenac. Gastroenterology. 2008; 135 (5): 1517-25.

18. Castellsague J., Riera-Guardia N., Calingaert B. et al. Individual NSAIDs and upper gastrointestinal complications: a systematic review and meta-analysis of observational studies (the SOS project). Drug. Saf. 2012; 35 (12): 1127-46.

19. Chan F., Wong V., Suen B. et al. Combination of a cyclo-oxygenase-2 inhibitor and a proton-pump inhibitor for prevention of recurrent ulcer bleeding in patients at very high risk: a double-blind, randomized trial. Lancet. 2007; 369: 1621-6.

20. McGettigan P., Henry D. Cardiovascular risk with non-steroidal anti-inflammatory drugs: a systematic review of population-based controlled observational studies. PLoSMed. 2011 rock; 8 (9): e1001098.

21. Trelle S., Reichenbach S., Wandel S. et al. Cardiovascular safety of non-steroidal anti-inflammatory drugs: network meta-analysis. Br. Med. J. 2011 rock; 342: 70-86.

22. Gislason G., Jacobsen S., Rasmussen J. et al. Risk of death or rein-farction associated with the use of selective cyclooxygenase-2 inhibitors and nonselective nonsteroidal antiinflammatory drugs after acute myocardial infarction. Circulation. 2006; 113 (25): 2906-13.

23. Silverstein F., Graham D., Senior J. et al. Misoprostol reduces serious gastrointestinal complications in patients with rheumatoid arthritis receiving nonsteroidal anti-inflammatory drugs. A randomized, double-blind, placebo-controlled trial. Ann. Intern. Med. 1995; 123: 241-9.

24. Acevedo E., Castaneda O., Ugaz M. et al. Tolerability profiles of rofecoxib (Vioxx) and Arthrotec. A comparison of six weeks treatment in patients with osteoarthritis. Scand. J. Rheumatol. 2001; 30: 19-24.

25. Saccar C. The pharmacology of esomeprazole and its role in gastric acid related diseases. Exp. Opin. Drug Metab. Toxicol. 2009 rock; 5 (9): 1113-24.

26. Lanas A., Polo-Tomás M., Roncales P. et al. Prescription of and adherence to non-steroidal anti-inflammatory drugs and gastroprotec-tive agents in at-risk gastrointestinal patients. Am. J. Gastroenterol. 2012; 107 (5): 707-14.

27. Goldstein J., Howard K., Walton S. et al. Impact of adherence to concomitant gastroprotective therapy on nonsteroidal-related gastro-duodenal ulcer complications. Clin. Gastroenterol. Hepatol. 2006; 4 (11): 1337-45.

28. Burmester G., Lanas A., Biasucci L. et al. The appropriate use of non-steroidal anti-inflammatory drugs in rheumatic disease: opin-

ions of a multidisciplinary European expert panel. Ann. Rheum. Dis. 2011, 70 (5): 818-22.

29. Leonard J., Marshall J., Moayyedi P. Systematic review of the risk of enteric infection in patients taking acid suppression. Am. J. Gastroenterol. 2007; 102 (9): 2047-56.

30. Giuliano C., Wilhelm S., Kale-Pradhan P. Are proton pump inhibitors associated with the development of community-acquired pneumonia? A meta-analysis. Exp. Rev. Clin. Pharmacol. 2012; 5 (3): 337-44.

31. Drepper M., Spahr L., Frossard J. Clopidogrel and proton pump inhibitors - where do we stand in-2012? World J. Gastroenterol. 2012; 18 (18): 2161-71.

32. Bezabeh S., Mackey A., Kluetz P. et al. Accumulating evidence for a drug-drug interaction between methotrexate and proton pump inhibitors. Oncologist. 2012; 17 (4): 550-4.

33. Ngamruengphong S., Leontiadis G., Radhi S. et al. Proton pump inhibitors and risk of fracture: a systematic review and meta-analysis of observational studies. Am. J. Gastroenterol. 2011 rock; 106 (7): 1209-18.

34. Roberts D., Miner P. Safety aspects and rational use of a naproxen + esomeprazole combination in the treatment of rheumatoid disease. Drug. Health Patient Saf. 2011 rock; 3: 1-8.

35. Goldstein J., Hochberg M., Fort J. et al. Clinical trial: the incidence of NSAID-associated endoscopic gastric ulcers in patients treated with PN 400 (naproxen plus esomeprazole magnesium) vs. enteric-coated naproxen alone. Aliment. Pharmacol. Ther. 2010 32 (3): 401-13.

36. Hochberg M., Fort J., Svensson O. et al. Fixed-dose combination of enteric-coated naproxen and immediate-release esomeprazole has comparable efficacy to celecoxib for knee osteoarthritis: two randomized trials. Curr. Med. Res. Opin. 2011 rock; 27 (6): 1243-53.

37. Gigante A., Tagarro I. Non-steroidal anti-inflammatory drugs and gastroprotection with proton pump inhibitors: a focus on ketoprofen / omeprazole. Clin. Drug Invest. 2012; 32 (4): 221-33.

38. Taha A., Hudon N., Hawkey C. et al. Famotidine for the prevention of gastric and duodenal ulcers caused by nonsteroidal antiinflammatory drugs. N. Engl. J. Med. 1996; 334: 1435-9.

39. Ng F., Tunggal P., Chu W. et al. Esomeprazole compared with fa-motidine in the prevention of upper gastrointestinal bleeding in patients with acute coronary syndrome or myocardial infarction Am. J. Gastroenterol. 2012; 107 (3): 389-96.

40. Humphries T. Famotidine: a notable lack of drug interactions. Scand. J. Gastroenterol. 1987; 22 (Suppl. 134): 55-60.

41. Bello A. Duexis® (ibuprofen 800 mg, famotidine 26.6 mg): a new approach to gastroprotection for patients with chronic pain and inflammation who require treatment with a nonsteroidal anti-inflammatory drug. Ther. Adv. Musculoskelet. Dis. 2012; 4 (5): 327-39.

42. Laine L., Kivitz A., Belo A. et al. Double-Blind Randomized Trials of Single-Tablet Ibuprofen / High-Dose Famotidine vs. Ibuprofen Alone for Reduction of Gastric and Duodenal Ulcers. Am. J. Gastroenterol. 2012; 107: 379-86.

43. Patel T., Goldberg K. Use of aspirin and ibuprofen compared with aspirin alone and the risk of myocardial infarction. Arch. Intern. Med. 2004; 164: 852-6.

44. Singh G., Graham D., Wang H. et al. Concominant aspirin use reduces the risk of acute myocardial infarction in users of cyclooxy-genase-2 selective and some non-selective nonsteroidal anti-inflammatory drugs. Ann. Rheum. Dis. 2006; 65 (Suppl. II): 61 (0P0024).

45. Doherty M., Hawkey C., Goulder M. et al. A randomized controlled trial of ibuprofen, paracetamol or a combination tablet of ibuprofen / paracetamol in community-derived people with knee pain Ann. Rheum. Dis. 2011 rock; 70 (9): 1534-41.

Non-steroidal antiapalny drugs of the new generation without over-use of the most popular drugs in the US.

There are a lot of zhodnoy medical galusies, even though the representative of this group does not have bi prescriptions in the standard of treatment.

The stench of great efficiency, albeit, at the same time, the supply in large regions is surrounded by a list of recipes, so as an independent reception of this group lykarsky zasobiv you can bring Skoda.

You can be added to non-steroidal anti-inflammatory drugs (NSAIDs)

Representatives of this group of trochas are more than 30, however, they are widely spread around 10 licars.

To a group of non-steroidal anti-pyretic agents, lycars are introduced, as they ingest the enzyme cyclooxygenase, and take part in the synthesis of markers ignited: prostaglandins, thromboxanes and prostacyclines. The speech takes a part in the process of temperature alleviation and pain syndrome. There are three types of cyclooxygenase enzyme (isoform), both of which may function.

Cyclooxygenase type 1 - constantly present in the body, won’t get lost in the synthesis of prostaglandins and similar rechovins, to seize the slings, nyrki, and also regulate the processes of microcirculation.

Cyclooxygenase type 2 - to establish itself in the body when ignited, present permanently. Synthesis of speech, which take a part in the processes of firing and dividing the client.

Cyclooxygenase type 3 - the receptor of the given enzyme is importantly located in the nervous system, the third isoform takes part in the processes of temperature alteration and plays a role in the appearance of pain syndrome.

As a matter of fact, before є 3 types of enzyme, use 3 groups of non-steroidal anti-fiery substances.

1. Selective (vibrating) blockers COG 1 - the most popular representative of all refineries - aspirin.
2. Non-selective (vibration) blockers of COX 1 and COX 2 - a large number of refineries: diclofenac, indomethacin, ketoprofen, ketorolac, proproxicam.
3. Selective reactions of COX 2 -nimesulide, meloxicam, rofecoxib, celecoxib.
4. Selective reactions of COX 3 - paracetamol, analgin.

Selective COG 1 and nonselective COG 1, 2 є “old” generations of this group of Likarsk people. Aspirin is widely used in small doses in antiplatelet mats (blood-thinning mats) in the prevention of heart-vascular disasters.

Іngіbіtori COG 3 okremoyu group, moreover, it means that analgin (metamіzol sodium) is not circulated to the extent of storage in large regions, in our land permits to storage. And paracetamol is widely used as a disease-resistant drug in Europe and the United States.

New generation of ingibitorіv COG, mechanizm dії

Ingibitori COG 2 is a non-steroidal preparation of the so-called "new" generation, the stench is in the main and vikoristovyuyu in the practice of a bitter liquor.

Іngіbіtori COG 2 to be distributed to:

• Preparations for overloading COX 2 - nimesulide, meloxicam. The stench still may cause a slight reaction to COG 1, especially when it is trivial.
• Highly selective ingibitori COX 2 - celecoxib, rofecoxib.

Mechanism of the Department of Ingibitoriv COG 2 (nimesulid, meloxicam)

In the process of firing up the isoform of cyclooxygenase 2, when the ingibitor COX 2 is taken, it quickly gets wet from the grass tract, 89% of the speech is consumed in the roof. When consumed in the roof, the drug substitutes for receptors, such as receptors for COX 2, so the number of ignition markers (prostaglandins) is changed.

In addition to blocking these receptors, it is also often possible to compete with the substitution of COX 1 receptors, especially in the case of trivial intake of drugs in the whole group, or in case of transposition of the therapeutic dose.

A special feature of the group is a decrease in selectivity in case of trivial intake or intake of a drug at high doses. There is an increase in the frequency of side effects, which is why COG 1 can be manifested in the minds of the minds - the fallowing ones.

Mechanism of the Visokovibirkovo Ingibitoriv COX 2 (celecoxib, rofecoxib)

When it gets into the body, the drug gets wet from the herbal tract, drinking into the systemic bloodstream, competitively with the COX 2 receptor block. Standard therapeutic concentrations do not have COX 1.

What is the origin of the “old” drugs from the “new” drugs?

On vіdmіnu od selectively іngіbіtorіv COX 1 i nonselective іngіbіtorіv COX 1 i 2 selektivnі i visokoselektivnі іngіbіtori іzoformi cyclooxygenase 2 in protsesі lіkuvannya not postupayutsya for efektivnіstyu "old" pokolіnnyu and frequency urazhennya travnoї system in Vier Razi nizhche in porіvnyannі of nonselective іngіbіtorami, y deyakikh, for example, celecoxib, in seme development.

There is also a reason for the diagnosis of COX 1

In case of stagnation of ingibitoriv COX 2, there is an increase in bronchospasm, loss of bronchial asthma or heart failure. It is also indicated that there is a great deal of harmless reception from a person who has been kidnapped.

Today the refinery Ingibitori COG 2 is being developed from the other side - in the role of powerful anti-splinters. In laboratory tests, celecoxib has shown anti-inflammatory and anti-swelling effect.

References and indications for the victorious selection of selective ingibitoriv COG 2

Shown for reception of Ingibitorіv oil refinery is even greater. In the official instructions for the storage of a group of drugs in the main predominance rіznі ailing slopes and spinal stumps, so that there is a great deal of pain in the field and the most common cause of pain syndrome.

showing

• Pain syndrome.
• Injury of loafs: rheumatoid arthritis, arthritis, osteoarthritis, trauma, gout, etc.
• Pain syndrome in neurological practice.
• Tooth bill.
• Menstrual beats.
• Head bill.
• In the quality of the disease in the period of operation.

Prototype

Submit all indications drugs given group:

• "Aspirinova triada": bronchial asthma, intolerance to aspirin, polyposis of the nose and nasal sinuses;
• virazkovі urazhennya herbal tract in zagostrennі;
• hemorrhagic in the brain;
• severe heart failure;
• severe nirkov lack of;
• hemophilia;
• the period of the coronary artery bypass surgery;
• vagina and lactation;
• drug addiction and alcoholism.

Features victorian іngіbіtorіv COG 2

I want a side effect from this group of drugs in significantly less bends, less when nonselective COGs are stuck, all there are more side effects of blocking COG 2 є. To that, the reception of the COG 2 is guilty through, shonaymenhe, for the second time, when there is a malfunctioning defect in either the case of the intestinal tract, then the reception of the antihypertenant of the COG 2 .), and the priyom on the doba is guilty of a two-fold booty.

It is admittedly a trivial use of a given group of drugs, a protest of memory, so that the development of non-essential effects is directly proportional to the triviality of therapy.

Deyaki representatives of "new" non-steroidal drugs

celecoxib

Tse Visokovibirkovo Ingibitor COG 2. When you take it in the middle it is easy to get wet, reaching the maximum concentration in 3 years in the blood. The drug stagnates when it is consumed, when it is taken at the same time with the fatty one, it will get the liquor wet at the same time.

good luck official instructions, Celecoxib freezes when rheumatoid arthritis, Osteoporosis, psoriatic arthritis, ankylosing spondylitis. The most common side effect is head bill, Dyspepsia. Celecoxib should be taken in a dose of 200 mg x 2 times per day, the maximum allowable dose is 400 mg x 2 times per day.

meloxicam

When you take it all the way through the middle, you get wet from the shlunkovo-intestinal tract, the maximum level is reached after 5 years, when 89% of the drug appears in the plasma. It is well known from the instruction, meloxicam stagnate during ignition processes in the slopes, arthritis, arthrosis, unspecified ailments of the slopes.

The drug is dispensed in the form of a tablet form, an injection drug, rectal testicles. Meloxicam is administered once a day. It is recommended to take the drug every hour. The most frequent neglect of meloxicam is dyspeptic symptoms, headache. With a trivial intake of meloxicam, or the consumption of therapeutic doses, the selectivity changes.

nimesulid

The most frequent selective ingibitor of COX 2. The maximum value is reached in the blood plasma after 1.5 - 2 years from the reception, with an hourly reception and an hour, it will increase significantly. In the indication, before the intake of the given drug, on the view of the representatives of their representatives, there should be included, for reasons of various reasons.

The most frequent non-essential effects: diarrhea, nudota, bluing, adjustment of liver transaminases. The drug is used internally, to remove water-corrosive forms, the maximum amount you can get is a serving 200 mg of nimesulida.

Why should I use a prescription for a prescription?

Zdavalosya, there are fewer side effects, it is possible to take a drive, so why in some pharmacies the whole group is allowed to get a prescription for a liquor? For the skin type, there is evidence that can be displayed only for the skin.

It is not possible to accept a new generation of oil refineries from an insignificant drive, so as in a whole group of unimportant individual side effects, for example - the rapid state of the nation nirkova lack, likarsky hepatitis, etc. ...

The same is true for a great number of people low threshold painful sensitivity, and the stench of a strong pain syndrome And for the group of NAPPs, the organism can no longer function normally without a regular dose of drugs, it can be absorbed through the adaptations of receptors in cyclooxygenase and inhibition of NAPPs.

Likewise, a dweller, not tied to medicine, not able to assess all the risks of a one-hour intake of the drug with інshi likami. For example, the reception of COX 2 blockers reduces the amount of drugs used to reduce the grip. To this self-determination, the vicariousness of the gifts cannot be justified in one way.

Non-steroidal anti-pyretic drugs, which are shortly called oil refineries, or oil refineries (most) are widely stagnated in the world. In the United States, the statistics have blown away all the galuzy of life, they have fucked up, so that the skin of American consumers is given more than 70 million recipes at the refinery. American vip, prick and smear on skins for more than 30 milliard doses of non-steroidal anti-pyretic drugs in rick. It is unlikely that our spyvitchizniki will be seen from them.

With all the popularity, the large number of oil refineries is based on a high level of non-baking and low toxicity. Navi at high doses of acceleration in the region of maloimovirnі. Well, why are you for the miracle?

Non-steroidal anti-flue gasps - there is a large group of people, as they have three effects at once:

• sun-sick;
• fever-lowering;
• to the prototype.

The term "non-steroid" is a reference to steroids, to hormonal drugs, which can also be used as an anti-fatigue.

The power, evidently seen by the refineries of the middle analgesics, is the appearance of the sound in case of trivial consumption.

Excursion to history

The "root" of non-steroidal anti-inflammatory drugs is far away. Hippocrates, is alive at 460-377 rr. until our time, having seen about vicorian measles willow for zebooluvannya. Trochi piznishe, in the 30s BC Celsius confirming his word and stating that the bark of the willow wonderfully pom'yakshu signs of burning.

The riddle about the analgesic bark is coming to a head in 1763. First, in 1827, the chemists were able to see from the willow extract that speech itself, which became famous for the hours of Hippocrates. Active ingredin from verby measles emerged with the glycoside Salicin - an alternator of non-steroidal antiapaline spirits. In 1.5 kg of measles, 30 g of purified salicin were trimmed.

In 1869, for the first time, they were more effective than salicin - salicylic acid... I was unhappy, I won’t be able to slime the slurry, and at the beginning of the day there was an active shout of new speeches. In 1897, the Nimetsky chemist Felix Hoffman and the Bayer company introduced a new era in pharmacology, zoomed in to convert the toxic salicylic acid into acetylsalicylic acid, and I called it Aspirin.

For a long time, aspirin became the first and only representative of the group of non-steroidal anti-fiery animals. Since 1950, pharmacologists have begun to synthesize all new drugs, which are more effective and better than before.

Yak to run an oil refinery?

Non-steroidal anti-fumes help to block the release of words, which are called prostaglandins. The stench is to take a bezposrednyu fate from the development of pain, fever, fever, mazovyh court. Most NPZP nonselectively (nonvibirkovu) block two other enzymes, which are necessary for prostaglandin to virobrate. The stench is called cyclooxygenase - COX-1 and COX-2.

The prototype of the non-steroidal prototype of the fire is rich in what is reasoned:

• changes in the penetration of the vessels and the microcirculation in them;
• Decrease in vivilnennya from the clerk of special speeches, which stimulate fieryness, - mediators fired.

Moreover, the oil refinery is blocking the energy processes in the middle of firing, and by itself amusingly “firing”. Analgetic (zealous) development develops as a result of a change in the ignition process.

serious undersized

It's time to talk about one of the most important minuses of non-steroidal anti-inflammatory drugs. On the right, in the fact that COG-1 has a positive role in viroblastic prostaglandins. Win takes a part in the synthesis of prostaglandin, which is a reversal of mucous slurry under the influence of hydrochloric acid. If you do not vibrate іngіbіtori COG-1 and COG-2 fix the potsyuvati, the stench will increase blocking prostaglandins - і "shkіdlivі", so wicked fired up, і "corisnі", so hijack the slunk. So non-steroidal antiapaline liquors provoke the development of twisted ailments of the slunk and two-fingered intestines, as well as internal bleeding.

Ale the middle of the family of refineries and special preparations. The price of the most efficient tablets, which is the vibrating blocking of COG-2. Cyclooxygenase type 2 is an enzyme that takes care of the fate only in igniting and not having any additional preservation. To that end, the blockade will not be clogged with unacceptable inheritances. Selective COX-2 blockers do not provoke slunk-intestinal problems;

Non-steroidal anti-fumes and fever

NPZP will be absolutely unique in power, as it sees in the middle of the preparations. The stench is nadayut hot-blooded diyu and can be used for licking a feverish woman. It’s bright, as it smells like it’s good quality, it’s later that the temperature rises.

Lichomaniac develops in the form of an increase in prostaglandin E2, which is the name for the swiftness of the shooting neurons (activity) in the boundaries of the hypothalamus. And the hypothalamus itself is a small area in the intermediate brain - and the control of thermoregulation.

Fever-lowering non-steroidal anti-pyretic drugs, which are called antipyretics, and the enzyme COX. It can lead to galvanization of prostaglandin, as a result of galvanization of neuronal activity in the hypothalamus.

Prior to the speech, it was established that the most powerful turns of the heat-resistant powers of Volodya Ibuprofen. Winning has overturned paracetamol as its closest competitor.

Classification of non-steroidal anti-inflammatory drugs

And now, let's try to get back, as we must admit to the non-steroidal anti-fiery spirits.

On the current year, there are dozens of drugs in the whole group, but not all of them are registered in Russia. There are only those types of liquids that can be bought at local pharmacies. The refinery is classified according to its chemical structure and mechanism of development. It’s not easy to read the reader with folding terms, induced by forgiveness of the classifications, in any case, if you want to name them.

Otzhe, the entire list of non-steroidal anti-combustion devices is added to the pod group.

salicylates

The group itself has been nominated, and the history of the refinery has been repaired. Single salicylate, which is stagnant and synonymous, is acetylsalicylic acid, or Aspirin.

Acid propionic acid

Prior to them, one of the most popular non-steroidal antiapalny drugs, zokrema preparations, are mentioned:

• ibuprofen;
• naproxen;
• ketoprofen і deyaki іnshі lіki.

Acid ocetic acid

Not less famous and other-lost ocetic acids: indomethacin, ketorolac, diclofenac, aceclofenac and іnshі.

Selective Ingibitories COG-2

Prior to the safest non-steroidal anti-inflammatory drugs, these new drugs should be administered last generation Alle, only two of them have been registered in Russia. Remember these international names - celecoxib and rofecoxib.

Інші non-steroidal prototypes

The okremі pіdgroup includes piroxicam, meloxicam, mefenamic acid, nimesulide.

Paracetamol is even weakly protivopalny activity. The leading rank in the COG-2 block is in the central nervous system, and it is nada-sick, as well as a low-temperature heat-negative effect.

If the oil refinery is stagnant?

As a rule, oil refineries are used for drinking too much or chronic heat, superfluous pain.

Excessively ill, when stagnant non-steroidal antiapaline drugs:

• arthrosis;
• pomyrnі pain through burning or injuries of soft tissues;
• osteochondrosis;
• b_l across;
• head b_l;
• gostra gout;
• dysmenorrhea (menstrual pain);
• pain in the cysts, wicclicans with metastases;
• pislyaoperating pains;
• I am in pain with Parkinson's ailments;
• fever (increased temperature);
• intestinal imperfection;
• nirkova kolka.

In addition, non-steroidal anti-fiery canals are stagnant for children, some arterial ducts do not curl up for 24 years.

Tsey divovizhniy aspirin!

Aspirin can be easily brought to the preparation, so that the whole light has been preserved. The most extraordinary non-steroidal anti-pyretic tablets, which were used for lowering the temperature and reducing the temperature, demonstrated a non-standard side effect. Viyavilosya, scho, blocking COX-1, aspirin at the same time halmє synthesis of thromboxane A2 - speech, yak zbіlshu sgortania blood. Aspirin is allowed to be injected into the blood viscosity. However, for people with ailments on hypertensive ailments, angina pectoris, ischemic ailments of the heart, and those with heart-vindicated ailments, it is not the case for the sutta. For them, it is more important that aspirin in low doses helps to prevent heart-and-heart catastrophe - infarction and stroke.

Most people recommend taking aspirin to prevent myocardial infarction and insult in cardiological, low doses to people in 45-79 patients and women - 55-79 years old. The dose of aspirin is adjusted according to the drug: as a rule, it should be taken from 100 to 300 mg per dose.

For some rocky ones, they vyavili, but aspirin lowers the development of oncological illnesses and mortality from them. Rectal cancer is especially effective. American patients recommend that their patients take aspirin to prevent the development of colorectal cancer. On ёkhnyu dumka, risik development of side effects in the case of trivial treatment with aspirin is still lower, not oncological. Before we speak, let us be cognizant of the side effects of non-steroidal anti-fiery fires in our neighbors.

Heart rhizics of non-steroidal anti-inflammatory drugs

Aspirin, with its antiaggregant effect, vibrates from a string of siblings in a group. It is important to have a large number of non-steroidal anti-fatigues, including the occasional COG-2 ingibitoria, to promote the development of myocardial infarction and insult. Cardiologists, as well as patients, have recently experienced a heart attack, they need to be reconsidered from the refinery's history. According to the statistics, the growth of unstable angina pectoris has increased by 10 times. It is a good idea to use naproxen from the point of view of the naproxen.

On April 9, 2015, the FDA published an official policy for the FDA. A new person is going to know about the admission of risk of insult and infarction in ailments who are stagnant to nonsteroidal anti-fatigue. Zrozumilo, aspirin is a happy vignatok from the axiomi community.

Injection of non-steroidal anti-combustion on the slunk

Another vidomy side effect of the refinery is shlunkovo-intestinal. We have already spoken, so win the dressing with tight ties pharmacological of all non-vibrating іngіbіtorіv COG-1 and COG-2. However, the oil refinery does not only reduce the level of prostaglandins, and they themselves release the slime of the slurry to the sink. Molecules on their own move aggressively along the way up to the mucous membranes of the intestinal tract.

Nudota, bloating, dyspepsia, diarrhea, fever ailment, including bleeding, may occur on a lingering non-steroidal anti-pyretic disease. The slurry-intestinal side effects of the refinery are developing right away because of the fact that they were consumed by the body: oral in the eyes of the tablets, injections in the eyes and rectal in the eyes of the pigs.

Chim is more than trivially lіkuvannya and chim more than the dosage of oil refineries, thym vishche risik to the development of twisted ailments. In order to increase the efficiency of the diagnosis to the minimum, you can take the lowest effective dose with a stretch of the shortest period.

Recently, it was shown that more than 50% of people use non-steroidal anti-burners, slizova small intestine all the same poshkodzhutsya.

It is obvious that the preparations of a group of non-steroidal anti-pyretic agents are poured onto the slime of the slurry in a different way. So, indomethacin, ketoprofen and piroxicam are most important for the intestine and intestines. And up to the number of the most not-for-great, ibuprofen and diclofenac are introduced.

Okremo would like to say about intestinal-corrosive shells, how to use non-steroidal anti-pyretic tablets. Wyrobniks start dying, so it is also possible to help you to reduce the risk of lowering or lowering the level of niveluvati risik shlunkovo-intestinal accelerated oil refineries. However, the message key practice to show that for the sake of reason such a zajist is not successful. The more effective efficiency of the slime slurry rate decreases the one-hour intake of liquids, which block the hydrochloric acid release. Ingibitories of proton pump - omeprazole, lansoprazole, esomeprazole and іnshі - good food for the preparation of high-quality drugs for a group of non-steroidal anti-apalagines.

Say a word about citramon ...

Tsitramon is a bred brain storm of Radiansk pharmacologists. Far away, since the assortment of our pharmacies is not numbered with thousands of drugs, pharmaceuticals have come up with a miraculous formula for an analgesic-antipyretic. The stinks were given "in one bottle" a complex of non-steroidal anti-pyretic drugs, antipyretics and seasoned with a combination of coffee.

Vinahid viyavivsya deeper in the distance. Kozhne deyucha speech made one dey. Suchasn_ pharmaceuticals have changed the traditional prescriptions, replacing the antipyretic phenacetin with non-baked paracetamol. In addition, from the old version of citramone, they used cocoa and citric acid - citric acid; The drug of the XXI century is to take away aspirin 0.24 g, paracetamol 0.18 g, and coffee 0.03 m and without affecting trophies of changes, everything is so self-help in terms of pain.

However, unaffected by an affordable price and even higher efficiency, Citramon has its majestic skeleton in Shafi. Likars have long been in the process of doing this and have brought me to the bottom of the mucous membrane of the intestinal tract. Seriously, navilki, so in the literature to find the term "tsitramonovaya virazka".

The reason for this obvious aggression is simple: I want to give Aspirin an active drink, which stimulates the production of hydrochloric acid. As a result, the mucous membrane of the slunk was lost without prostaglandin clogging. Moreover, it’s not only when you see it at home, it’s like it and it’s right, but it’s all at once, when the citramon is soaked into the roof.

Dodamo, scho "tsitramonovye" great sizes... Some stinks do not "grow up" to gigantic ones, but take a few stinks in groups in different types of slurry.

The moral of this step is simple: do not try to use citramone, unimpressed on all of your passions. It is also important to have inheritance.

Refinery and ... sex

In 2005, there were a lot of unacceptable side effects of non-steroidal anti-fiery fires in the belongings. The financial events held a pre-session, which showed that the triviality of the oil refinery plant (on 3 months) increased the risk of recurrent dysfunction. Nagadaєmo, as a matter of fact, may be on the view of the ruin of the erection, among the people called the empowerment. Todi urologists and andrologists were interested in no less high-quality experiment: injecting leaks into the sexual function of the assessed only on the presentation of special perceptions of the person and not overturning the faults.

However, in 2011, the authoritative "Journal of Urology" has published the tribute of one more recent report. At the new one, there was also a chime in between the licks of the non-steroidal anti-fiery fires and the destruction of the erectia. Protect, likarі, ryzhuyut, and the residuals are still injected early. And as soon as vchenі is engaged in a fuss of proofs, the choloviks are still more beautifully using non-steroidal protivopalny drugs.

Інші secondary efficiency refineries

With serious inappropriateness, such as blocking up the drink with non-steroidal anti-fiery zasob, we were confused. Let's move on to expand the unfriendly podіyam.

Damaged function of nirok

Acceptance of oil-and-gas production of dressings і from a fairly high level of nirkovy side effects. Prostaglandins take a part in expanded blood vessels in nirk glomeruli, allowing normal filtration in nirkas. If the prostaglandins fall, - and the whole effect is based on the action of non-steroidal anti-firing devices - the robot can never be damaged.

To the most risky of nirk side effects, very well, people are sick because of nirok.

photosensitivity

To achieve often trivial lіkuvannya non-steroidal anti-fiery means of superfluousness. It is worth noting that piroxicam and diclofenac are more due to the unfortunate effect.

People who take antiapaline drugs can react to sleepy changes in their child's heart, and in any case, with their own childish reactions.

hypersensitivity reactions

Non-steroidal anti-fiery "glorified" and allergic reactions. The stench can be manifested by visip, svitlochutlivistyu, sverbіzh, kvіnke quilting and anaphylactic shock. True, the last effect is borne out to the number of children in the region, and this is not the fault of potential patients.

In addition, taking NPZP can lead to headaches, blockages, drowsiness, bronchospasm. Zrіdka ibuprofen wiklikє syndrome of irritated bowels.

Non-steroidal anti-fatigue in case of vaginosis

To deliver often in front of the women of the hospitality of the food supply. What is it possible for mothers to be able to fix oil refineries? It’s a pity it’s dumb.

Unimportant to those preparations of a group of non-steroidal anti-inflammatory drugs, do not affect teratogenic children, so as not to suffer gross vices in the development of a child, we can still smell the naughty one.

So, there are the facts, like talking about the possible completion of the closure of the arterial duct in the fetus, when the mother has taken the refinery for an hour. In addition, deyakі until lіdzhennya show the sound between the reception of the oil refinery and the front canopies.

Protect the drug is still vicious during vaginosis. Napriklad, Aspіrin often priznachayut time of heparin zhіnkam have yakih pid hour vagіtnostі boule viyavlenі antifosfolіpіdnі antitіla. The popularity of endometacin will remain especially popular for the treatment of pathologies of vaginosity by adding old age and endomethacin. Yogo began to be stashed in obstetrics in case of abundant water supply and a threat to the front canopy. However, the French Ministry of Health has seen an official mandate for the protection of non-steroidal anti-fatigues, including aspirin, for a great month of vaginosity.

Refinery: accept chi vіdmovitiya?

If there is a need for a refinery, but if there is a need to see it from them? Let's see all the possible situations.

Refinery in individuals

We also know the strengths and weaknesses of the refinery. And now, let’s spare it, as antiapalny preparations are more beautiful than stasis for pain, as for burning, and as for when temperature and cold.

Acetylsalicylic acid

The first oil refinery, which after pumping light, acetylsalicylic acid, is widely used to accumulate to qix pir. As a rule, її stasis:

• for lowering the temperature of til.

  Beastly respect that acetylsalicylic acid is not recognized for children under 15 years old. It is tied with that, but with a childish feisty on aphids, the drug signifies an increase in the development of Rey's syndrome - birthright pechinki, which do not pose a threat to life.

  matured acetylsalicylic acid and fever-reducing should become 500 mg. The tablets are taken only at an increased temperature.

• as an antiplatelet agent for the prevention of heart-and-vascular disasters. The dose of cardioaspirin can be adjusted from 75 mg to 300 mg per dob.

You can buy acetylsalicylic acid from the fever-lowering dose under the names Aspirin (vyrobnik and owner of the brand name of the nimetska corporation Bayur). Vіtchiznyany enterprises produce even less inexpensive tablets, as they are called - Acetylsalicylic acid. Besides, the French company Bristol Mayers viroblyaє effervescent tablets Upsarin Oops.

Cardioaspirin maє bezlich names and forms of vipusku, including Aspirin Cardio, Aspinat, Aspikor, CardiASK, Trombo ASS and іnshi.

ibuprofen

Ibuprofen is single-use in its own safety and the ability to effectively reduce the temperature and volume, so the preparations on this basis are sold without a prescription. Yak heat-resistant zasib ibuprofen stagnates in that number and for new women. It has been reported that I lower the temperature more beautifully for the other non-steroidal anti-combustion devices.

In addition, ibuprofen is one of the most popular over-the-counter analgesics. Yak antiapalny zasіb wine is recognized not so often, protea drug to reach the popular in rheumatology: it can be used for treating rheumatoid arthritis, osteoarthritis and other sickness slopes.

Prior to the most popular trade names Ibuprofen were introduced by Ibuprom, Nurofen, MIG 200 and MIG 400.

naproxen

Naproksen zaboroneniy until stasuvannya children and adolescents younger than 16 years, and we will grow up, so we suffer from heart failure. Most often, the preparation of non-steroidal anti-pygmy naproxen is stagnant in painfulness in case of headache, toothache, periodical, angular and other types of pain.

In Russian pharmacies, naproxen is sold under the names Nalgezin, Naprobene, Pronaxen, Sanaproks and інshim.

ketoprofen

Ketoprofen preparations give rise to anti-firing activity. Wines are widely used for diseases and for lowering in case of rheumatic diseases. Ketoprofen is used for tablets, ointments, suppositories and injections. Before the number of popular drugs, the line Ketonal is introduced by the Slovak company Lek. Popularity to cure і nіmetsky gel for suglobіv Fastum.

indomethacin

One of the old non-steroidal anti-inflammatory drugs, endomethacin with a cutaneous day in the position. Winning Volodya with modest, sun-loving power and peaceful prototypical activity. In the rest of the rock, I will often call it "endometacin" to sound in obstetrics - it has improved its health to relax the muscles of the uterus.

ketorolac

Uniquely non-steroidal anti-fiery fires, but Volodya turns a sun-sickly soul. Analgesic properties of ketorolac due to the potency of weak narcotic analgesics. On the negative side of the preparation, it is not safe: it can cause bleeding, provoke the sickness of the slunk, as well as pechinka lack. Tomato zastosovuvati ketorolac can be bridged for about an hour.

In pharmacies, ketorolac is sold under the names Ketanov, Ketalgin, Ketorol, Toradol and інshim.

diclofenac

Diclofenac is the most popular non-steroidal anti-inflammatory drug, the "gold standard" in the treatment of osteoarthritis, rheumatism and other lumpy pathologies. Volodya is seen as an anti-fiery and noble power, and that is widely stagnated in rheumatology itself.

Diclofenac can be used in vipusku-free forms: tablets, capsules, ointments, gels, suppositories, ampoules. In addition, the disintegration of the plaster with diclofenac will help you get rid of the trivial diy.

Analogues of diclofenac are even more bagato, and they are too overwhelming if they are not available from them:

• Voltaren is the original drug of the Swiss company Novartis. Become high yak and the same high price;
• Diklak is a line of useful medications in the company Hexal, which are both good and acceptable, and good quality;
• Dikloberl virobnitstva Nimechchini, Berlin Chem company;
• Naklofen - Slovak preparations from the KRKA company.

In addition, there are a lot of inexpensive non-steroidal antiapaline drugs with diclofenac in tablets, ointments and injections.

celecoxib

Suchasny non-steroidal ignition preparation, vibration blocking COX-2. Volodya has a high profile of safety and pro-firing activity. Stomach in case of rheumatoid arthritis and other diseases of the slopes.

Original celecoxib is sold under the name Celebrex (Pfizer company). In addition, in pharmacies, Dilax, Coxib and Celecoxib are more available.

meloxicam

Popular oil refinery, which is used in rheumatology. As a result of being able to get some meats on the herbal tract, that one is often given a pass for the treatment of patients, who may have a history of discomfort or intestines.

I mean meloxicam in tablets, or in a few words. Meloxicam preparations Melbek, Melox, Meloflam, Movalis, Eksen-Sanovel and іnshі.

nimesulid

Most often it is necessary to become stagnant in the quality of a worldly, noble, and innocent - to a heat-resistant. More recently, a child's form was sold in pharmacies for a nimesulid, yaku was used for lowering the temperature, and it was categorically for children younger than 12 years old.

trade name nimesulidu: apon, Nise, Nimesil (original original drug in viglyadі powder for preparing a range for internal consumption) and іnshі.

On the other hand, a couple of rows of mefenamic acid are available. Even if it stagnates because of fever reducing, the protector signifies a step for the effectiveness of the other non-steroidal anti-inflammatory drugs.

Svit refinery is truly hostile to business development. It is unimportant on side effects, the goal is by right to be considered to the number of the most important and necessary, as it is not necessary to substitute, nor to bypass the side. Only to give praise to the unobtrusive pharmacists, who are promoting all the new formulas, and all the more non-baked refineries.

celecoxib (Celecoxib, Celebrex) Celecoxib was developed in the 90s of the 20th century and gave an ear to the whole class of highly specific ingibitoriv COG-2 - "coxibs".

MD: Celecoxib is 375 times the vibrational block of COX-2, in proportion to the COX-1 isoform to the enzyme. Vvazhayut, which is tied to the apparent in the molecules of celecoxib 2 dylyanok, rigidly fixed along the cut: the polar sulfonanilide group of the molecule block hydrophilic cytochrome COX-2, and a part of the ferruginous cytoplasmic channel In connection with this, the COX-1 molecule is not small for the hydrophilic lateral intestine of celecoxib, it is impossible to go to the active center and the links of the COX-1 to the side of the intestinal tract can not be reached. You can only use it when you take high doses of celecoxib (blockade of COX-2 develops even when celecoxib is prescribed at a dose of 0.2 mg / kg or 150-200 mg / day; mg / dobu).

Table 7. Ratio characteristics of the refinery

Note: † - less than the value of COG-1 / COG-2 = -lg[ IC 50 COG-1 /IC 50 COG-2], tim selective for COG-2.

FC: Celecoxib is even more low in water, so the parenteral form of liquor can be dissolved superficially foldably. With oral administration, the bioavailability of celecoxib becomes close to 75%, while it can reduce the absorption rate by 20-30%, or the bioavailability at a further increase and growth by 7-20%. In celecoxib blood, 97% of dressings are with blood cells. For a one-time admission in a dose of 200 mg, the value of the maximum concentration in the blood is 1500 ng / ml and 5 times the cordon of the minimum therapeutic dose (300 ng / ml). Oskilki period of half-life becomes 10-12 years, a decrease in concentration to the minimum therapeutic level is taken in an hour, three more than 2t ½, so that celecoxib can be taken once a day.

Metabolism of celecoxib is opposite to cytochrome P 450 2C9 in the liver (> 90%). Danium cytochrome does not take part in the metabolism of significant amounts of drugs (for example, aminoglycosides, anticonvulsants and oral succumbing diseases), that is, if you do not take drugs too much.

FE: Celecoxib is characterized by antiapalal and analgesic bends. For its efficacy of celecoxib at a dose of 100-400 mg / day, ASA, naproxen and diclofenac are not administered. Quite simply, the anti-firing and analgesic efficacy should not be dose-dependent. At a dose of less than 100 mg / day, the effect is effective during the day, in the range of doses from 100 to 400 mg / day of wine, or further, an adjusted dose from 400 mg / day to 1200 mg / day is practically not to produce until the effect is more stable.

Oskilka celecoxib is practically not poured into COX-1, it does not change the aggregation of platelets and does not lead to the development of antiaggregants.

Shown before zasosuvannya and dosuvannya regimes: Celecoxib zasosovyut for the treatment of chronic igniting lesions of the organs of the support-roc apparatus:

osteoarthritis - 100-400 mg / dob in 1 dose;

rheumatoid arthritis - 200-800 mg / dob in 1-2 doses.

Oskilki є theoretical changes in the possible participation of COX-2 in the processes of carcinogenesis in the colorectal zone, the development of Alzheimer's ailments, then the authors of the author consider celecoxib as a promising one for the prevention of cychitis in young people.

NOT: Due to the high selectivity in terms of the ratio to COG-2 and the preservation of the normal functioning of the physiological form of COG-1 celecoxib is used in more reliable refineries, in some cases with nonselective devices.

Celecoxib is more likely to diagnose malformations on the mucous membrane of the intestinal tract, do not lead to the development of bleeding due to a decrease in platelet aggregation and do not rob the tonometer of the tonometer. Individuals with arterial hypertension do not have a tendency to destabilize the grip.

However, on the cob of hope for the safety of selective COG-2 ingibitors and celecoxib itself, in general, they are aware of the collapse. At the end of the day, it has been established that it is necessary to receive the approval of the coming neobzhannye defects:

Even though celecoxib was already malfunctioning earlier, celecoxib did not develop the development of the vortex mucous shlunkovo-intestinal tract, but it will overwhelm the process of fixing the already extraneous inferior defects. Vvazhayut, well, it is tied to this, that control over the processes of reparation and mitosis of the intestinal tract, the prostaglandin, which is established by the injection of COG-2.

The sulfonanilide group of celecoxib is highly responsive to many allergic reactions and transcends sensitization to sulfanilamide reactions and oral sucrose-related drugs from the group of negligible sulfinis.

1% of people who took celecoxib for a trivial hour developed a state of the art deficiency.

For celecoxib, as well as for nimesulidu in the last CLASS (2000), the status of indukuvati thrombosis development was reported. Yak vvazhayut, the price is informed that the synthesis of thromboxane A 2 is controlled by COX-1, and the synthesis of prostacyclin is controlled by COX-2. Moreover, on the blockade of COX-2 in the body, it is possible to change the level of thromboxane over prostacyclin and the aggregation of thrombocytes in growth, right up to the development of non-fatal myocardial infarction.

It means, however, that it was more recent since it was announced in 2002, but it has not been approved since it was CLASS. To that, nutrition about the infusion of celecoxib on hemostasis is unnecessary and needs to be completed.

The intake of celecoxib in females should be brought up to the development of a circulating bezopliddya (the frequency of such a boole is 2 times, not in the control population of females, who did not take Ingibitori COG-2).

EF: capsules of 100 and 200 mg.

rofecoxib (Rofecoxib, Vioxx) Also, celecoxib should be used before the straining selective ingibitoriv COX-2. The mechanism of rofecoxib is analogous to that of celecoxib, but the role of a blocker of the hydrophobic main channel in the new vicone is the arilfuranose part of the molecule.

F K: Rofecoxib is better absorbed from the intestinal tract, even if the dose is increased. Yak vvazhayut, the price is tied with the peculiarities of the distribution of the lines. On the top of the list of celecoxib, it is better to ring with a bottle (87%), but not less than the first half-life period, but less for celecoxib and to become close to 17 years (which can be added to rofecoxib 1 times). Metabolism of rofecoxib is against the participation of isoforms to cytochrome P 450 3A4, which actively oxidizes liquids in the liver and in the intestine.

FE: Volodya Rofecoxib is good for analgesic, anti-pyretic and antipyretic effects. At the same time, it is possible to add up to the second selective antiplatelet agents COX-2 in the addition of antiaggregant activity.

Constipation and dosage: Rofecoxib vikoristovuyut for the treatment of osteoarthritis and rheumatoid arthritis in a dose of 25 mg / dob once.

NOT: In general, the effects of rofecoxib are similar to those of celecoxib.

PV: tablets of 12.5 and 25 mg.

Suck it up, pour it on the lipoxigenazny way

metabolism of eucosanoids.

Classification:

Ingibitori 5-lipoxygenase: zileuton;

Antagonism of leukotrine cysLT 1 receptors: zafirlukast, montelukast, verlukast, pranlukast, tsіnalukast, іralukast, pobіlukast.

Zileuton (Zileuton, Zyflo) Zileuton was the first to use lykarskiy zasob, which is injected into the function of lipoxygenase pathway to the metabolism of eucosanoids.

M D: In the fired tissue, a part of arachidonic acid, which has established itself in the phospholipids of the membranes of cellini, is metabolized for the lipoxigenase path. At the same time, the enzyme 5-LOG oxidizes arachidonic acid from a combination to 5-hydroperoxyeicosatetraenoic acid, and then hydrolyzes the product to leukotriene A 4 (Div. Scheme 3).

The further metabolism of LTA 4 can be carried out in 2 alternative ways, the vibration of the skin can be found in the type of cell, for a different chemical reaction.

In neutrophils and monocytes, LTB 4 is established due to the participation of acid and hydrolase enzyme. leukotrієnіv protіkayut in the fiery tissues of the bronchial tree. So, in individuals with bronchial asthma, the stench is 5-10 times more intense than in healthy people.

In fabrics-targets, leucotrines are injected onto special membrane receptors and reactions (div. Table 8.):

Table 8. Effectiveness of leukotroin and types of leukotroin receptors.

In such a rank, leukotroeni are responsible for the development of bronchospasm and the attack of bronchial asthma. For the power of the bronchospastic effect, the stench is 1000 times overturned by the histamine (it is not very good for the asthma model in the animals) 20.

Zileuton is reversibly connected to the active center of 5-LOG and the block of synthesis of leukotroins.

FE: Nadaє anti-asthmatic diyu. The reception of zileuton reduces the synthesis of leukotroins and, as a result, the development of bronchospasm, the filling of the mucous membrane of the bronchi changes.

Stagnation and dosage: Zileuton stagnation for the prevention of attacks of bronchial asthma (especially "aspirin" form of asthma, which is triggered by the intake of an oil refinery, which helps to reduce the COH-deposits metabolism of arachidonic acidic acid) To stop the already rooted attack of asthma, the zileuton is not victorious, the spikes in the synthesis of leukotroins is already completed, the stench has triggered the activation of the receptor and launch the fast cells. In such a rank, zileuton is a basic (trivalo) planned asthma therapy.

For the effectiveness of anti-asthmatic diya, Zileuton is used to treat glucocorticosteroids with 2 adrenergic drugs. Long-term zileuton is recommended to be recommended in case of the onset of situations:

In case of bronchial asthma of light persistent interruption, zileuton should be used for monotherapy, as only the basic one.

In case of bronchial asthma of the middle stage of severity of the disease, it is possible to take the supplement to the basic therapy with glucocorticosteroids, as an alternative to  2 -adrenomimetics of the trivalo type (to combine the combination of “GCS +  2-AM”). Vikoristannya zileuton allows one to reduce the additional dose of steroids taken by 20%.

As a rule, zileuton is taken at 600 mg 4 times a day.

NOT: the most significant non-essential effect of zileuton є th hepatotoxicity, as in the meaning of the world it is surrounded by drug consumption.

PV: 600 mg tablets.

zafirlukast (Zafirlukast, Accolate) MD: Zafirlukast connects to cysteinyl cysLT 1-type leukotrinic receptors and blocks. With a whole leukotrieni Z 4, D 4 and E 4, there is no active activation of the receptor and the appearance of an effect on the side of the smooth mucous membranes of the bronchial tubes.

FE: Zafirlukast will override the development of the attack of bronchial asthma, change the swelling of the mucous membrane of the bronchial tubes. It's a pity that asthma attacks have already grown out of the way, because of the activation of leukotroin receptors, the process of rapid bronchial inflammation will start behind the help of internal mediators, in order to lose some of the receptors.

Have Faint pro-fired cytokines are caused by a faint pro-fired cytokine: IL-4.5 and GM-CSF (div. Table 2.), and the processes of chronic firing, such as the malignancy in the bronchial tree, are caused.

For the effective intake of zafirlukast, it is possible to test with the intake of ingestion steroids at a dose of 400-500 mcg / dobu (in beclomethasone equivalent). Moreover, if the patient had previously taken corticosteroids at a dose of up to 400 mcg / day when switching to zafirlukast, it is possible to skasuvati, and if the dose of steroids was 400 mcg / day, then it can be reduced by 200-400 mcg / day.

FC: Zafirlukast is kind enough to get wet when you take it in the middle. A spilny reception with a 40% decrease in the availability of a zafirlukast. The metabolism of liquor is counterproductive in the liver for the participation of cytochrome P 450 2C9. Confirmed in the process of metabolism of hydroxylated kidney in 90 times less active, not just zafirlukast itself. Vivedennya zafirlukasta is 90% healthy. As a result of memory, the reception of zafirlukast is supervised to adapt to the function of cytochromes P 450 (moreover, not only the isoform 2C9, but d 3A4, as it takes a part in the metabolism of the most important lykiv).

Zastosuvannya: Zafirlukast take the rule on the heart in 20 mg 2 times a day, if necessary, the dose can be increased to 40 mg 2 times a day.

Zafirlukast vicoristovuyut for the prevention of asthma attacks in adults and children over 12 years old. With a slight interruption of asthma, zafirlukast vikoristovuyut in viglyad monotherapy,

If you want to go back to the supplement to the ingestion of steroids 21. Slide memory, but the reception of the zafirlukast did not last long after the possibility of asthma attacks.

NOT: Zafirlukast has low toxicity. The main effect of this problem (I want to finish it off) is the possibility of developing the Churg-Strauss syndrome. Danish syndrome is a variant of systemic eosinophilic vasculitis, which is a disease in the presence of an autoimmune inflammation of the small cola blood circulation and the following symptoms: an increase in asthma attacks, the appearance of clouds in the tissues of the lung, clouds of inflammation of the lungs

In the last few years, it was established that the greatest risk of development of this syndrome in patients, who, before the cob of therapy with zafirlukast, took glucocorticosteroids at high doses, and for the sign of zafirlukast of raptus. The basis of therapy for Churg-Strauss syndrome is the administration of high doses of glucocorticosteroids systemically (all the way or internally).

In addition, rarely, taking zafirlukast (especially in doses greater than 80 mg / dob) can lead to the development of hepatotoxicity and supernatant exposure to a high level of transaminases in the peripheral blood.

EF: tablets of 0.02 and 0.04.

montelukast (Montelukast, Singulair) Montelukast, behind his mechanism of action and the main pharmacological effects, is nagadu zafirlukast, albeit with a low positive features:

EF: tablets in 10 mg tablets, zhuvaln tablets of 5 or 4 mg.

Lykarsky for the activity of prostaglandins.

Victory in the medical practice of natural prostaglandins is not always possible. It’s tied up with that, that the period of being in the body is numbered with hilin (not more than 10-15 minutes), because of which it stinks and irreversibly waste its activity.

In table 9, there is a summary of the main drugs related to the activity of prostaglandins and their synthetic analogs.

Table 9. Costs based on prostaglandins and synthetic analogs.

anti-gouty

I will gout with a pavuk myself, it burned into the light of people:

Hearing La Fontaine on the light, letting go.

I will not follow him vivishuvati and world,

Naskіlki truths here, і how, і why;

Simultaneously from tim i, to be built, youmu,

Having flattened eyes, in bikes it is possible to change.

I, it became, I do not know in that,

The heat of the people Gout with pavuk.

I.A. Krilov "Gout and Pavuk".

Anti-gout is called likarski zasobi, as zasosovyut for stopping attacks of gout, as well as for those who suffer in the period between attacks.

Gout is a decline in metabolic disease, associated with impaired purine metabolism, accumulation of sech acid in the body and arthritis manifested by repeated attacks, as a result of urate deposition in slopes and cartilages. Sometimes gout is not of a recessive nature and may be linked to the period of an intensive drop of nucleic acids in the body (for example, when there is a drop of swelling, cytostatic therapy or radio therapy).

Non-steroidal antiapalny drugs of the new generation without over-use of the most popular drugs in the US.

Groups of anti-inflammatory drugs

Shown and contraindicated

There are a lot of zhodnoy medical galusies, even though the representative of this group does not have bi prescriptions in the standard of treatment.

The smell of great efficiency, albeit at the same time, the supply in large regions is surrounded by a list of recipes, so as an independent reception of a given group of Likarsk workers can bring a school code.

You can be added to non-steroidal anti-inflammatory drugs (NSAIDs)

Representatives of this group of trochas are more than 30, however, they are widely spread around 10 licars.

To a group of non-steroidal anti-pyretic agents, lycars are introduced, as they ingest the enzyme cyclooxygenase, and take part in the synthesis of markers ignited: prostaglandins, thromboxanes and prostacyclines. The speech takes a part in the process of temperature alleviation and pain syndrome. There are three types of cyclooxygenase enzyme (isoform), both of which may function.

Cyclooxygenase type 1 - constantly present in the body, won’t get lost in the synthesis of prostaglandins and similar rechovins, to seize the slings, nyrki, and also regulate the processes of microcirculation.

Cyclooxygenase type 2 - to establish itself in the body when ignited, present permanently. Synthesis of speech, which take a part in the processes of firing and dividing the client.

Cyclooxygenase type 3 - the receptor of the given enzyme is importantly located in the nervous system, the third isoform takes part in the processes of temperature alteration and plays a role in the appearance of pain syndrome.

As a matter of fact, before є 3 types of enzyme, use 3 groups of non-steroidal anti-fiery substances.

1. Selective (vibrating) blockers COG 1 - the most popular representative of all refineries - aspirin.
2. Non-selective (vibration) blockers of COX 1 and COX 2 - a large number of refineries: diclofenac, indomethacin, ketoprofen, ketorolac, proproxicam.
3. Selective reactions of COX 2 -nimesulide, meloxicam, rofecoxib, celecoxib.
4. Selective reactions of COX 3 - paracetamol, analgin.

Selective COG 1 and nonselective COG 1, 2 є “old” generations of this group of Likarsk people. Aspirin is widely used in small doses in antiplatelet mats (blood-thinning mats) in the prevention of heart-vascular disasters.

Іngіbіtori COG 3 okremoyu group, moreover, it means that analgin (metamіzol sodium) is not circulated to the extent of storage in large regions, in our land permits to storage. And paracetamol is widely used as a disease-resistant drug in Europe and the United States.

New generation of ingibitorіv COG, mechanizm dії

Ingibitori COG 2 is a non-steroidal preparation of the so-called "new" generation, the stench is in the main and vikoristovyuyu in the practice of a bitter liquor.

Іngіbіtori COG 2 to be distributed to:

• Preparations for overloading COX 2 - nimesulide, meloxicam. The stench still may cause a slight reaction to COG 1, especially when it is trivial.
• Highly selective ingibitori COX 2 - celecoxib, rofecoxib.

Mechanism of the Department of Ingibitoriv COG 2 (nimesulid, meloxicam)

In the process of firing up the isoform of cyclooxygenase 2, when the ingibitor COX 2 is taken, it quickly gets wet from the grass tract, 89% of the speech is consumed in the roof. When consumed in the roof, the drug substitutes for receptors, such as receptors for COX 2, so the number of ignition markers (prostaglandins) is changed.

In addition to blocking these receptors, it is also often possible to compete with the substitution of COX 1 receptors, especially in the case of trivial intake of drugs in the whole group, or in case of transposition of the therapeutic dose.

A special feature of the group is a decrease in selectivity in case of trivial intake or intake of a drug at high doses. There is an increase in the frequency of side effects, which is why COG 1 can be manifested in the minds of the minds - the fallowing ones.

Mechanism of the Visokovibirkovo Ingibitoriv COX 2 (celecoxib, rofecoxib)

When it gets into the body, the drug gets wet from the herbal tract, drinking into the systemic bloodstream, competitively with the COX 2 receptor block. Standard therapeutic concentrations do not have COX 1.

Important to the nobility:

Problems with slopes - straight road to invalidity!
Deliver patience bіl in the slopes! Make a note of the revised recipe from the approved drug ...

What is the origin of the “old” drugs from the “new” drugs?

On vіdmіnu od selectively іngіbіtorіv COX 1 i nonselective іngіbіtorіv COX 1 i 2 selektivnі i visokoselektivnі іngіbіtori іzoformi cyclooxygenase 2 in protsesі lіkuvannya not postupayutsya for efektivnіstyu "old" pokolіnnyu and frequency urazhennya travnoї system in Vier Razi nizhche in porіvnyannі of nonselective іngіbіtorami, y deyakikh, for example, celecoxib, in seme development.

There is also a reason for the diagnosis of COX 1

In case of stagnation of ingibitoriv COX 2, there is an increase in bronchospasm, loss of bronchial asthma or heart failure. It is also indicated that there is a great deal of harmless reception from a person who has been kidnapped.

Today the refinery Ingibitori COG 2 is being developed from the other side - in the role of powerful anti-splinters. In laboratory tests, celecoxib has shown anti-inflammatory and anti-swelling effect.

References and indications for the victorious selection of selective ingibitoriv COG 2

Shown for reception of Ingibitorіv oil refinery is even greater. In the official instructions for the storage of the whole group of drugs, the main predominance of the disease of the slopes and the ridge is, as it is more important that the cause of the pain is the most common cause of the pain.

showing

• Pain syndrome.
• Injury of loafs: rheumatoid arthritis, arthritis, osteoarthritis, trauma, gout, etc.
• Pain syndrome in neurological practice.
• Tooth bill.
• Menstrual beats.
• Head bill.
• In the quality of the disease in the period of operation.

Prototype

On the basis of all indications for drug preparations in the group:

• "Aspirinova triada": bronchial asthma, intolerance to aspirin, polyposis of the nose and nasal sinuses;
• virazkovі urazhennya herbal tract in zagostrennі;
• hemorrhagic in the brain;
• severe heart failure;
• severe nirkov lack of;
• hemophilia;
• the period of the coronary artery bypass surgery;
• vagina and lactation;
• drug addiction and alcoholism.

Features victorian іngіbіtorіv COG 2

I want a side effect from this group of drugs in significantly less bends, less when nonselective COGs are stuck, all there are more side effects of blocking COG 2 є. To that, the reception of the COG 2 is guilty through, shonaymenhe, for the second time, when there is a malfunctioning defect in either the case of the intestinal tract, then the reception of the antihypertenant of the COG 2 .), and the priyom on the doba is guilty of a two-fold booty.

It is admittedly a trivial use of a given group of drugs, a protest of memory, so that the development of non-essential effects is directly proportional to the triviality of therapy.

Deyaki representatives of "new" non-steroidal drugs

celecoxib

Tse Visokovibirkovo Ingibitor COG 2. When you take it in the middle it is easy to get wet, reaching the maximum concentration in 3 years in the blood. The drug stagnates when it is consumed, when it is taken at the same time with the fatty one, it will get the liquor wet at the same time.

It is well known from the official instructions, celecoxib is stagnant in rheumatoid arthritis, osteoporosis, psoriatic arthritis, Bekhterev's ailments. The most common side effect is headache, dyspepsia. Celecoxib should be taken in a dose of 200 mg x 2 times per day, the maximum allowable dose is 400 mg x 2 times per day.

meloxicam

When you take it all the way through the middle, you get wet from the shlunkovo-intestinal tract, the maximum level is reached after 5 years, when 89% of the drug appears in the plasma. It is well known from the instruction, meloxicam stagnate during ignition processes in the slopes, arthritis, arthrosis, unspecified ailments of the slopes.

The drug is dispensed in the form of a tablet form, an injection drug, rectal testicles. Meloxicam is administered once a day. It is recommended to take the drug every hour. The most frequent neglect of meloxicam is dyspeptic symptoms, headache. With a trivial intake of meloxicam, or the consumption of therapeutic doses, the selectivity changes.

nimesulid

The most frequent selective ingibitor of COX 2. The maximum value is reached in the blood plasma after 1.5 - 2 years from the reception, with an hourly reception and an hour, it will increase significantly. In the indication, before the intake of the given drug, on the view of the representatives of their representatives, there should be included, for reasons of various reasons.

The most frequent non-essential effects: diarrhea, nudota, bluing, adjustment of liver transaminases. The drug is used internally, to remove water-corrosive forms, the maximum amount you can get is a serving 200 mg of nimesulida.

Why should I use a prescription for a prescription?

Zdavalosya, there are fewer side effects, it is possible to take a drive, so why in some pharmacies the whole group is allowed to get a prescription for a liquor? For the skin type, there is evidence that can be displayed only for the skin.

More in the slopes, come to the end!

Learn about zasib, which is dumb in pharmacies, Ale the zavdyaki, who are already rich in russians vilikuvalis all over the mountains in the slopes and ridges!

Rozpovidak vidomy likar

It is not possible to accept a new generation of oil refineries from an insignificant drive, so as in a whole group of unimportant individual side effects, for example - the rapid state of the nation nirkova lack, likarsky hepatitis, etc. ...

Also in a great number of people there is a low threshold of pain sensitivity, and the stench of painful sensitivities from any minor pain syndrome, and for a group of NPZP, it is called for an hour, the body can no longer function normally without a cycle. inhibition of oil refineries.

Likewise, a dweller, not tied to medicine, not able to assess all the risks of a one-hour intake of the drug with інshi likami. For example, the reception of COX 2 blockers reduces the amount of drugs used to reduce the grip. To this self-determination, the vicariousness of the gifts cannot be justified in one way.

An important fact:
Ail the slopes and wag you will be tied one by one. If it is effective to lower the wagu, then it’s healthy to grow. Tim is bigger, it’s easier to lower it in the middle. Aje z'avivsya zisib, yake ...
Rozpovidak vidomy likar