Pajjiż: Afrika t’Isfel
Lingwa: Ingliż
Sors: South African Health Products Regulatory Authority (SAHPRA)
Schering
MELODENE TABLETS SCHEDULING STATUS: S3 PROPRIETARY NAME (and dosage form): MELODENE TABLETS COMPOSITION The 28-day pack (Every-Day pack) contains 21 hormonal tablets each with gestodene (17alpha-ethinyl-13-ethyl-17beta- hydroxy-4,15-gonadiene-3-one) 0,075 mg and ethinylestradiol (17alpha-ethinyl-estra-1,3,5(10)-triene-3,17beta-diol) 0,02 mg, plus 7 non-hormonal tablets. PHARMACOLOGICAL CLASSIFICATION A.18.8 Ovulation controlling agents. PHARMACOLOGICAL ACTION The hormonal components of Melodene inhibit ovulation by suppressing gonadotrophin release. Secondary mechanisms include changes in the cervical mucous (which increases the difficulty of sperm penetration) and changes in the endometrium (which reduce the likelihood of implantation). The pharmacological and biochemical profile of gestodene is very similar to that of progesterone. Due to the high binding affinity and biological activity of gestodene, there is an effective inhibition of ovulation at an exceptionally low dose. Pharmacokinetics Gestodene Orally administered gestodene is rapidly and completely absorbed. Following single ingestion of Melodene, maximum drug serum levels of about 3,5 ng/mL are reached at about 1 hour. Thereafter, gestodene serum levels decreased in two phases. The terminal disposition phase is characterised by a half-life of about 12 hours. For gestodene, an apparent volume of distribution of 0,7 L/kg and a metabolic clearance rate from serum of about 0,8 mL/min/kg were determined. Gestodene is not excreted in unchanged form but as metabolites, which are eliminated with a half-life of about 1 day. Gestodene metabolites are excreted at an urinary to biliary ratio of about 6:4. The biotransformation follows the known pathways of steroid metabolism. No pharmacologically active metabolites are known. Gestodene is bound Aqra d-dokument sħiħ