By Helmut Buschmann; Gregor Bahrenberg; et al
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Additional info for Analgesics : from chemistry and pharmacology to clinical application
Today this compound serves as a pharmacological tool. A continuous effort was made in chemical research to develop a second generation of COX-2 inhibitors, structurally different from existing ones, that would show very high COX-2 selectivity, a suitable pharmacokinetic profile and in vivo efficacy in animal models. , 2001). 2 h to > 72 h). In addition, pharmacokinetic studies in rats showed that the clearance of DFP was significantly increased upon multiple dosing. The basis of these pharmacokinetic behaviors was Investigated through in vitro metabolic studies.
5 (1) Young etal. , 1980) is a nonsteroidal anti-inflammatory drug used in the treatment of mild to moderate pain including osteoarthritis, rheumatoid arthritis and primary dysmenorrhoea. It is used as base or lysine- or arginine-salt for oral or parenteral application. Diflunisal shows weak inhibition of both, COX-1 and COX2 in a whole blood assay. Peak plasma concentrations are reached within 2 to 3 h after oral dosing. Diflunisal is heavily bound to plasma protein (>99 %), has a long elimination half-life (8-12 h) and non-linear kinetics.
1996) Cl glucuronidation and sulphatation Scheme 12: Metabolic pathway of diclofenac. Diclofenac Is used mainly as the sodium salt orally or parenterally (75-150 mg/day) and as an ophthalmic solution. Topical formulations may contain the dJethylammonium or epolamine salt. Diclofenac is combined with misoprostol to reduce gastrointestinal effects, which are the main side-effects. , 1999): The diazotation of 2,4-difluoroanaline with isoamyl nitrite and condensation with anisole gives 4-(2,4difluorophenyl)anisole, which is hydrolyzed with HI in refluxing acetic acid yielding 4-(2,4-difluorophenyl)phenol.
Analgesics : from chemistry and pharmacology to clinical application by Helmut Buschmann; Gregor Bahrenberg; et al