Country: South Africa
Language: English
Source: South African Health Products Regulatory Authority (SAHPRA)
Schering
MIRELLE SCHEDULING STATUS: S3 PROPRIETARY NAME (and dosage form): MIRELLE Tablets COMPOSITION The 28-day pack (Every-Day pack) contains 24 hormonal tablets each with gestodene (17alpha-ethinyl-13-ethyl-17beta- hydroxy-4,15-gonadiene-3-one) 0,06 mg and ethinylestradiol (17alpha-ethinyl-estra-1,3,5(10)-triene-3,17beta-diol) 0,015 mg, plus 4 inactive tablets. PHARMACOLOGICAL CLASSIFICATION A. 18.8 Ovulation controlling agents. PHARMACOLOGICAL ACTION Pharmacodynamics Mirelle is a low-dose monophasic ovulation controlling agent with estrogenic and progestogenic peripheral effects. The mode of action of gestodene in combination with ethinylestradiol includes: * the inhibition of ovulation by suppression of the mid-cycle surge of luteinising hormone; * the suppression of endometrial development thus rendering the endometrium unreceptive to implantation; and * the thickening of cervical mucus so as to constitute a barrier to sperm. Pharmacokinetics • Gestodene Absorption Orally administered gestodene is rapidly and completely absorbed. Peak serum concentrations of 4 ng/ml is reached at about 1 hour after single ingestion. Bioavailability is approximately 99%. Distribution Gestodene is bound to serum albumin and to sex hormone binding globulin (SHBG). Only 1 to 2% of the total serum drug concentration is present as free steroid, 50 to 70% is specifically bound to SHBG. The ethinylestradiol-induced increase in SHBG influences the proportion of gestodene bound to the serum proteins, causing an increase of the SHBG- bound fraction and a decrease of the albumin-bound fraction. The apparent volume of distribution of gestodene is 0,7 to 1,4 L/kg. Metabolism Gestodene is completely metabolised by the known pathways of steroid metabolism. The metabolic clearance rate from the serum is 0,8 to 1,0 ml Read the complete document