País: Sudáfrica
Idioma: inglés
Fuente: South African Health Products Regulatory Authority (SAHPRA)
Donmed
MERCILON® tablets RA 0111 SA S1 (ref 2.0) SCHEDULING STATUS: S3 PROPRIETARY NAME (and dosage form): MERCILON ® tablets COMPOSITION 21 larger white tablets containing 0,15 mg desogestrel and 0,02 mg ethinylestradiol . 7 smaller white tablets that do not contain any active ingredients. List of excipients: colloidal silicon dioxide, lactose, magnesium stearate, potato starch, povidone, stearic acid, dl-alpha- tocopherol. The daily amount of lactose (< 80 mg) is such that women with intolerance to lactose are highly unlikely to experience a problem. PHARMACOLOGICAL CLASSIFICATION A/18.8/Ovulation controlling agents PHARMACOLOGICAL ACTION Mercilon is an oestrogen/ progestogen combination oral contraceptive that inhibits ovulation. Pharmacodynamic properties The contraceptive effect of Mercilon is based on the interaction of various factors, the most important of which are seen as the inhibition of ovulation and the changes in the cervical secretion. Pharmacokinetic properties Desogestrel Absorption Orally administered desogestrel is rapidly and completely absorbed and converted to etonogestrel. Peak serum concentrations of approximately 2 ng/mL are reached at about 1.5 hours after single ingestion. Bioavailability is 62– 81%. Distribution Etonogestrel is bound to serum albumin and to sex hormone binding globulin (SHBG). Only 2–4% of the total serum drug concentrations are present as free steroid, 40-70% are specifically bound to SHBG. The ethinylestradiol-induced increase in SHBG influences the distribution over 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 desogestrel is 1.5 L/kg. Metabolism Etonogestrel is completely metabolised by the known pathways of steroid metabolism. The metabol Leer el documento completo