Read e-book online Analgesics: From Chemistry and Pharmacology to Clinical PDF

By by Helmut Buschmann (Editor), Thomas Christoph (Editor), Elmar Friderichs (Editor), Corinna Maul (Ed

ISBN-10: 3527304037

ISBN-13: 9783527304035

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Etodolac is administered orally (400-1200 mg/day). Peak plasma concentrations are reached within 2 h. Etodolac shows 99 % binding to plasma protein and an elimination half-life of about 7 h (Brooks and Jamali, 1994). Etodolac is metabolized almost completely to the main metabolites 6- or 7-hydroxy-etodolac, acylglucuronide, 8-(1 '-hydroxyethyl)-etodolac and 4-ureidoetodolac. The metabolites and a small quantity of etodolac are excreted in the urine. A small amount of conjugated etodolac is excreted through the biliary tract.

Nevertheless, the FDA has so far rejected claims of reduced side-effect profile of celecoxib. The third generation of COX-2 inhibitors is under development showing an even greater selectivity for COX-2. The fastest-growing product in 2000 was Pharmacia/Pfizer's COX-2 inhibitor, Celebrex (Celecoxib), for osteoarthritis, which was launched in early 1999. 4 billion In sales, up by 65 % from previous year (Table 3). Table 3: The top ten selling drugs In 2000. Product 2000 sales ($ billion) % of global sales % growth (vs.

47 COX selectivity IC50 [pMJ COX-1 COX-2 ratio recomb. 7 (1) Penning etal. (1997) (2) Riendeau et al. (2001) Plasma peak concentrations are achieved within 2 h and the elimination half-life is about 12 h. Within the clinical dose range, there Is high plasma protein binding (-97%). Celecoxib is metabolized primarily via cytochrome P450 2C9 to three inactive main metabolites. It is excreted In faeces (~57%) and urine (~27%) as determined by administration of a single oral dose of radiolabeled drug.

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Analgesics: From Chemistry and Pharmacology to Clinical Application by by Helmut Buschmann (Editor), Thomas Christoph (Editor), Elmar Friderichs (Editor), Corinna Maul (Ed


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