Efficacy and Tolerability of Meloxicam, a COX-2 Preferential Nonsteroidal Anti-Inflammatory Drug

Abstract

Meloxicam is an enolcarboxamide with preferential COX-2 inhibitory activity. In vitro studies with human tissues have confirmed the high affinity of meloxicam for COX-2, whereas COX-1 was inhibited only at the highest concentrations (ratio of 50% inhibitory concentration for COX-2 : COX-1 = 0.09 in whole blood assays).Meloxicam has a bioavailability of 89% after oral administration, is strongly bound to plasma proteins, and its half-life is 20-24 hours. It readily penetrates into synovial fluid, reaching 45-57% of plasma concentrations. Meloxicam pharmacokinetics are not significantly altered in elderly patients or in those with mild renal/hepatic impairment.The efficacy and tolerability of meloxicam in the treatment of pain and inflammation associated with rheumatic and musculoskeletal disorders has been evaluated in numerous studies comparing meloxicam 7.5-15 mg/day (up to 22.5 mg/day in ankylosing spondylitis), administered for 2 weeks to 12 months, with placebo or other nonsteroidal anti-inflammatory drugs (NSAIDs). Overall, the efficacy of meloxicam was significantly superior to that of placebo and similar to that of other NSAIDs, whereas the incidence of adverse events (especially gastrointestinal) was lower than with other NSAIDs. Intramuscular meloxicam provided faster pain relief than the oral drug in patients with rheumatoid arthritis. Meloxicam also appears to be effective in the prevention of postoperative pain, as shown in patients undergoing abdominal hysterectomy or inguinal hernia repair. Meloxicam may also have a cardioprotective role: in patients with acute coronary syndrome without ST-segment elevation, a lower incidence of cardiovascular events was observed in those who received meloxicam plus aspirin and heparin versus aspirin and heparin alone, both during coronary care stay and at 90-day follow-up.Meloxicam has demonstrated a favourable tolerability profile in large-scale comparative trials, where its gastrointestinal tolerability was superior to that of nonselective NSAIDs. In particular, meloxicam 7.5 mg/day was associated with a lower incidence of gastrointestinal adverse events compared with diclofenac (13% vs 19%; p < 0.001) or piroxicam (10.3% vs 15.4%; p < 0.001). This was confirmed by a prescription-event monitoring study that found a relatively low

Comparison of Pain Score in Osteoarthritis Patients Treated With a Combination of Diacerein and Meloxicam and Meloxicam Alone

“…A significant reduction effect in pain intensity after 4 w follow-up in this study was supported by the results of the other literature, which said that effects of diacerein appear 2-4 w after therapy, and were significant after 4-8 w [20]. Meloxicam reaches significant effects as an analgesic in 2 nd -4 th w [27].…”

“…One of the NSAIDs that can be used is meloxicam that showed benefit in overcoming the pain of OA and rheumathoid disorder [23][24][25][26]. Meloxicam has a long halflife (20-24 h) so the using frequency was lower and easier for patients [27]. Based on the above, pain outcomes of OA patients receiving combination therapy of diacerein and meloxicam, and meloxicam alone were compared in this study.…”

Prospects for using injectable meloxicam (Amelotex®) in patients with osteoarthrosis

“…Так, данные проспективного исследования больных ОА и ревматоидным артритом (РА) продемонстрировали, что относительный риск (ОР) развития инфаркта миокарда при со-вместном приеме аспирина и мелоксикама составил 0,53 (0,26-1,10), что оказалось намного ниже, чем при параллель-ном приеме аспирина с другими, особенно неселективными, НПВП [15]. Интересно, что, несмотря на селективность в от-ношении ЦОГ 2, мелоксикам существенно снижает уровень ТхВ2 (примерно на 50%) и ТхА2, причем это снижение намного значительнее, чем при использовании коксибов, и ниже, но со-поставимо с ингибированием синтеза тромбоксанов у неселек-тивных НПВП [16][17][18]. Так, риск развития цереброваскуляр-ных тромбозов при приеме целекоксиба выше, чем при ис-пользовании мелоксикама: ОР 1,66 (1,10; 2,51).…”

The place of meloxicam in the series of modern non-steroidal anti-inflammatory drugs

“…It is convenient for use and promotes strict treatment compliance; it is especially important in cases of prolonged therapy of severe rheumatologic diseases. Another advantageous and distinguishing feature of meloxicam is its compatibility with antacids, acetylsalicylic acid, methotrexate, warfarin, furosemide -the drugs most commonly taken by the patients of the middle and old age suffering not only from rheumatologic diseases, but also from cardiovascular system diseases, disorders of water-salt metabolism, hypercoagulation syndrome [5,29,32]. For today the original drug of meloxicam -"Movalis®" (Beringher Ingelhime, Germany) is represented at the Ukrainian pharmaceutical market only in two dosage forms (solution for injection and tablets).…”