Selective inhibition of human cyclo-oxygenase-2 by meloxicam

Churchill, Laurie; Graham, Anne G.; Shih, C-K.; Pauletti, Daniel; Farina, Peter R.; Grob, Peter M.

doi:10.1007/bf02735467

Cited by 82 publications

(42 citation statements)

References 16 publications

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“…The 5-methyl group on the thiazolyl ring of meloxicam can enter the side pocket at the active site of COX-2. Meloxicam has a 100-fold selectivity in favor of COX-2 in microsomal preparations of human recombinant enzymes (Churchill et al, 1996;Pairet et al, 1998) and a 10-fold selectivity for COX-2 in the human whole blood assay (Patrignani et al, 1997;Warner et al, 1999); however, in the modified William Harvey whole blood assay, a 25-fold selectivity for COX-2 over COX-1 has been reported (Warner et al, 1999).…”

Section: A Treatment Of Inflammatory Diseasesmentioning

confidence: 99%

Cyclooxygenase Isozymes: The Biology of Prostaglandin Synthesis and Inhibition

2004

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Section: A Treatment Of Inflammatory Diseasesmentioning

confidence: 99%

Cyclooxygenase Isozymes: The Biology of Prostaglandin Synthesis and Inhibition

2004

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“…Meloxicam is a new enolic acid derivative developed for the treatment of rheumatoid arthritis and osteoarthritis. Its selective inhibition of the COX-2 enzyme has been demonstrated in the microsomal assay [25]. The data regarding the safety of meloxicam as an alternative treatment in patients with ASA hypersensitivity are currently limited [17,18,19,26,27,28].…”

Section: Discussionmentioning

confidence: 99%

Safety of Meloxicam in Aspirin-Hypersensitive Patients with Asthma and/or Nasal Polyps

Bavbek

Dursun²,

Dursun³

et al. 2006

Int Arch Allergy Immunol

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Background: The anti-inflammatory actions of acetylsalicylic acid (ASA)/non-steroidal anti-inflammatory drugs (NSAIDs) are thought to be due to inhibition of COX-2, whereas the side effects such as gastric damage and aspirin-induced asthma are mediated through inhibition of COX-1. Therefore, a new class of drugs with COX-2 selectivity may be well tolerated by patients with ASA/NSAIDs hypersensitivity. Objective: We investigated whether subjects with asthma and/or nasal polyps (NP) and analgesic intolerance proven by oral ASA provocation test tolerated the selective COX-2 inhibitor, meloxicam. Methods: All subjects were first challenged with ASA using a 2-day, single-blind, placebo-controlled oral provocation test. Thereafter, the subjects showing positive response to ASA provocation underwent a single-blind, placebo-controlled challenge with a cumulative dose of 7.5 mg of meloxicam on 2 separate days. One and three fourths of the divided doses of placebo and the active drug were given at 1-hour intervals. Clinical symptoms, lung function, and blood pressure were monitored during these challenge protocols. Results: Twenty-one patients with asthma and/or NP (10 males and 11 females; mean age: 38.4 ± 2.9 years) who reacted to ASA challenges were enrolled in the study. Response to ASA provocation was rhinitis + bronchospasm in 13, and extrabronchial reactions in 8 (isolated rhinitis in 3) patients. Mean PD₂₀ was 163.4 ± 39.9 mg ASA among patients who reacted with bronchospasm to ASA. Only 1 patient reacted to meloxicam challenge at a cumulative dose of 7.5 mg. Conclusion: This study indicates that 7.5 mg of meloxicam is a safe alternative treatment for ASA-hypersensitive asthma and/or NP patients with proven hypersensitivity via oral ASA challenges.

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“…Meloxicam selectively inhibits cyclooxygenase-2 leading to inhibition of prostaglandin synthesis, which is induced by inflammatory stimuli in pathophysio-doi:10.5455/vetworld.2013.516-520 logical conditions rather than cyclooxy-genase-1 which chromatography (HPLC) system. Waters HPLC system is responsible for physiological processes [5,7]. It has consisting of a Degasser, two pumps A and B (Waters also potential analgesic and antipyretic activities [8].In 515 HPLC pump), an injecter, C-18 symmetry column contrast with other NSAIDs, it has neither acute nor (particle size 5 µm;4.6mm ×250mm), Waters 2487 chronic gastrointestinal toxicity but has high intrinsic dual ë absorbance detector and a screen was used.…”

Section: Introductionmentioning

confidence: 99%

Pharmacokinetic studies of meloxicam after its intravenous administration in local goat (Capra hircus) of Assam

Wani¹,

Roy²,

Ashraf³

et al. 2013

Vet World

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Aim: The aim of the present study was to determine the meloxicam concentrations in the plasma of goats at different time intervals after its administration by IV route and data were used to determine the different pharmacokinetic parameters and the bioavailability of meloxicam in goats. Materials and Methods:The present study was conducted on 12 to 18 months old, five adult male local goats (Capra hircus) of Assam, with body weight ranging between 10 to 18 kg. All goats were clinically sound and healthy and reared at Goat Research station, Burnihat, Assam. A single dose of meloxicam was administered intravenously into the jugular vein of goats at the rate of 1 mg/kg body weight. Blood samples were analyzed with the help of high performance liquid chromatography (HPLC) system.Results:After single intravenous administration of meloxicam at the dose rate of 1mg/kg, the mean peak plasma level of the drug was 6.538±0.1189 µg/ml at 2 min. The mean elimination half life (t ) and mean distribution half life (t ) were Conclusion:After calculating various pharmacokinetic determinants, dosage regimens were computed for meloxicam in goats, based on minimum effective therapeutic plasma concentration of 0.7 µg/ml.To maintain the minimum effective concentration of 0.7 µg/ml in plasma for 25 hours following iv administration of meloxicam,an initial loading dose of 1.1 mg/kg body weight followed by a maintenance dose of 1mg/kg body weight/day is recommended.

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Selective inhibition of human cyclo-oxygenase-2 by meloxicam

Cited by 82 publications

References 16 publications

Cyclooxygenase Isozymes: The Biology of Prostaglandin Synthesis and Inhibition

Cyclooxygenase Isozymes: The Biology of Prostaglandin Synthesis and Inhibition

Safety of Meloxicam in Aspirin-Hypersensitive Patients with Asthma and/or Nasal Polyps

Pharmacokinetic studies of meloxicam after its intravenous administration in local goat (Capra hircus) of Assam

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