Overview of COX-2 in inflammation: from the biology to the clinic

Pairet, M.; Ryn, Joanne van; Distel, Manuel

doi:10.1007/978-3-0348-8747-2_1

Cited by 5 publications

(6 citation statements)

References 159 publications

(152 reference statements)

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“…The activity of nimesulide against canine COX‐1 and COX‐2 was evaluated using a whole blood assay which is considered as the most clinically relevant in vitro test approach (Pairet et al, 1999). The results of the present experiment confirm that nimesulide with a ratio of IC 50 COX‐1–COX‐2 of 13 has some selectivity for COX‐2 in the dog as in other species (Famaey, 1997).…”

Section: Discussionmentioning

confidence: 99%

Pharmacokinetic profile andin vitroselective cyclooxygenase‐2 inhibition by nimesulide in the dog

Toutain

Cester

Haak

et al. 2001

Vet Pharm & Therapeutics

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The pharmacokinetic properties and in vitro potency of nimesulide, a nonsteroidal anti-inflammatory drug (NSAID) were investigated in 8 or 10 dogs after intravenous (i.v.), intramuscular (i.m.) and oral (single and multiple dose) administrations at the nominal dose of 5 mg/kg. After i.v. administration, the plasma clearance was 15.3 +/- 4.2 mL/kg/h, the steady-state volume of distribution was low (0.18 +/- 0.011 L/kg) and the elimination half-life was 8.5 +/- 2.1 h. After i.m. administration, the terminal half-life was 14.0 +/- 5.3 h indicating a slow process of absorption with a maximum plasma concentration (6.1 +/- 1.5 microg/mL) at 10.9 +/- 2.1 h postadministration and the systemic bioavailability was 69 +/- 22%. After oral administration in fasted dogs, the maximal plasma concentration (10.1 +/- 2.7 microg/mL) was observed 6.1 +/- 1.6 h after drug administration, the plasma half-life was 6.2 +/- 1.9 h and the mean bioavailability was 47 +/- 12%. After daily oral administrations for 5 days, the average plasma concentration during the fifth dosage interval was 8.1 +/- 2.9 microg/mL and the overall bioavailability was 58 +/- 16%. The mean accumulation ratio was 1.27 +/- 0.4. In vitro nimesulide inhibitory potencies for cyclooxygenase (COX)-1 and COX-2 isoenzymes were determined using a whole blood assay. Canine clotting blood was used to test for inhibition of COX-1 activity and whole blood stimulated by lipopolysaccharide (LPS) was used to test for inhibition of COX-2 activity. The inhibitory concentration (IC50) for inhibition of COX-2 and COX-1 were 1.6 +/- 0.4 microM (0.49 +/- 0.12 microg/mL) and 20.3 +/- 2.8 microM (6.3 +/- 0.86 microg/mL) giving a nimesulide COX-1/COX-2 ratio of 12.99 +/- 3.41. It was concluded that at the currently recommended dosage regimen (5 mg/kg), the plasma concentration totally inhibits COX-2 and partly inhibits COX-1 isoenzyme.

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Section: Discussionmentioning

confidence: 99%

Pharmacokinetic profile andin vitroselective cyclooxygenase‐2 inhibition by nimesulide in the dog

Toutain

Cester

Haak

et al. 2001

Vet Pharm & Therapeutics

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“…COX-1 is the constitutive isoenzyme found under physiological conditions in most tissues, a so-called ''housekeeping'' enzyme, while COX-2 expression is induced, particularly during inflammatory processes [4]. It has been proposed that COX-2 inhibition is the relevant target for the anti-inflammatory effects of nonsteroidal anti-inflammatory drugs, whereas inhibition of COX-1 is responsible for the gastric and renal side effects of non-steroidal anti-inflammatory drugs [3][4][5].…”

Section: Introductionmentioning

confidence: 99%

Experimental models used to investigate the differential inhibition of cyclooxygenase-1 and cyclooxygenase-2 by non-steroidal anti-inflammatory drugs

Pairet

Ryn

1998

Inflamm. res.

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Numerous in vitro assays have been developed for testing and comparing the relative inhibitory activities of non-steroidal anti-inflammatory drugs against cyclooxygenase (COX)-1 and COX-2. Despite variability among these systems, which precludes direct comparison of data, analysis of the ratio of inhibition of COX-1 to COX-2 by non-steroidal anti-inflammatory drugs, suggests inhibitors can be classified based on their COX selectivity. Standard non-steroidal anti-inflammatory drugs can be considered nonselective; compounds such as meloxicam and nimesulide can be classified as COX-2 preferential; and compounds such as SC 58125 and L-754,337 are selective for COX-2. Although in vitro systems are important for characterizing COX-1 and COX-2 inhibitory activity, the clinical relevance of these data should be considered carefully. The level of inhibition of COX-1 and COX-2, in vivo at a given dose in patients, cannot be predicted from in vitro data alone. The pharmacokinetic properties of each compound, including plasma levels, distribution and binding to plasma proteins, have to be taken into account. Human pharmacology studies concentrating on the inhibition of prostanoid synthesis in target tissues are of paramount importance in determining the clinical relevance of COX-2 selectivity.

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“…This is in addition of repairing of different tissues and facilitating contraction of wounds. 42,43 Chitosan helps in blocks nerve endings reducing pain and natural blood clotting. Chitosan will gradually degrade to release N-acetyl-β-D-glucosamine, which initiates fibroblast proliferation, and stimulates increased level of natural hyaluronic acid synthesis at the wound site and helps in ordered collagen deposition.…”

Section: Wound Dressingmentioning

confidence: 99%

Radiation synthesis and modification of biopolymers and polymeric composites for biomedical applications

Ghaffar

2023

Polymers and Polymer Composites

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Recently the replacing of the petrochemical origin polymers with biopolymers and biocomposites which are environmental biodegradable polymers became a growing interest. The use of gamma radiation for synthesis and produce further modification of the biopolymers and biocomposites found to be suitable for biomedical application due to none using of toxic additives. Moreover, the radiation technique is the combining of preparation and sterilization in a one technological step thus, reducing time of the production and lower the costs. The use of gamma radiation technique in biomedical application is growing rapidly in controlled drug delivery, injectable materials, wound dressing, tissue engineering, immobilized enzymes and biosensors.

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Overview of COX-2 in inflammation: from the biology to the clinic

Cited by 5 publications

References 159 publications

Pharmacokinetic profile andin vitroselective cyclooxygenase‐2 inhibition by nimesulide in the dog

Pharmacokinetic profile andin vitroselective cyclooxygenase‐2 inhibition by nimesulide in the dog

Experimental models used to investigate the differential inhibition of cyclooxygenase-1 and cyclooxygenase-2 by non-steroidal anti-inflammatory drugs

Radiation synthesis and modification of biopolymers and polymeric composites for biomedical applications

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