国: カナダ
言語: 英語
ソース: Health Canada
MISOPROSTOL
AA PHARMA INC
A02BB01
MISOPROSTOL
200MCG
TABLET
MISOPROSTOL 200MCG
ORAL
100/500
Prescription
PROSTAGLANDINS
Active ingredient group (AIG) number: 0116767001; AHFS:
APPROVED
2010-06-02
0 PRODUCT MONOGRAPH MISOPROSTOL MISOPROSTOL TABLETS 100 MCG AND 200 MCG MUCOSAL PROTECTIVE AGENT AA PHARMA INC. DATE OF PREPARATION: 100 KING STREET WEST, SUITE 5700 May 28, 2010 TORONTO, ONTARIO M5X 1C7 CONTROL NUMBER: 138783 1 PRODUCT MONOGRAPH MISOPROSTOL Misoprostol Tablets 100 mcg and 200 mcg THERAPEUTIC CLASSIFICATION Mucosal Protective Agent ACTIONS AND CLINICAL PHARMACOLOGY Misoprostol is a synthetic analogue of prostaglandin E 1 . In animals and man, orally administered misoprostol has both gastric antisecretory and mucosal protective effects. Its antisecretory activity is mediated by misoprostol acid binding to specific prostaglandin receptors on gastric parietal cells. The mechanism of the gastrointestinal mucosal protective effect of misoprostol is not as well understood, but is thought to involve the replacement of prostaglandins following their depletion or inhibition of production, the increasing of mucus production, the increasing of bicarbonate secretion in the duodenum, increased mucosal blood flow, decreased vascular permeability, increased cellular proliferation and migration, and the restoration of the gastric potential difference. Studies conducted in animals and clinical trials in humans have demonstrated that misoprostol can protect the gastric mucosa against various irritants such as alcohol, acetylsalicylic acid, naproxen, tolmetin and sodium taurocholate. Misoprostol is a prodrug for the active de-esterified misoprostol acid. Conversion to misoprostol acid occurs rapidly in the stomach. The misoprostol acid then binds locally to receptors (e.g. on the parietal cells), undergoes additional hydrolysis, is taken up and metabolized by cells lining the stomach or in the liver, or is passed on to the small intestine along with stomach contents. 2 In a recent cross-over study (1995), a single 200 mcg oral dose of misoprostol administered to sixteen fasting, healthy male subjects produced mean C max , AUC (0-24), T max and elimination half-life of misoprostol acid of: 206.5 pg/mL, 141.8 pg.hr/m 完全なドキュメントを読む