Drugs 2004; 64 (7): 751-760 ADIS DRUG PROFILE 0012-6667/04/0007-0751/$34.00/0 © 2004 Adis Data Information BV. All rights reserved. Ethinylestradiol/ Chlormadinone Acetate Monique P. Curran and Antona J. Wagstaff Adis International Limited, Auckland, New Zealand Contents Abstract .................................................................................... 751 1. Pharmacodynamic Properties ............................................................. 752 2. Pharmacokinetic Properties ............................................................... 755 3. Clinical Efficacy .......................................................................... 755 4. Tolerability ............................................................................... 757 5. Dosage and Administration ............................................................... 758 6. Current Status ........................................................................... 759 Features and properties of ethinylestradiol/ chlormadinone acetate (EE/CMA) Indications Prevention of pregnancy Mechanism of action Inhibition of ovulation by suppression of gonadotropins (EE and Abstract CMA) Antiandrogenic activity (CMA) ▲ Ethinylestradiol/chlormadinone acetate 0.03/2mg Dosage and administration (EE/CMA) is a combined monophasic contracep- Dosage in clinical trials 0.03/2mg tive pill with antiandrogenic properties. Route of administration Oral ▲ In a large, noncomparative, multicentre trial (≤24 Frequency of administration Once daily for 21 cycles of treatment per woman) and two (6- and days of a 28-day 12-cycle) postmarketing surveillance studies, EE/ cycle CMA was effective in preventing pregnancy. Pharmacokinetic profile (after multiple oral doses of 0.03/ ▲ EE/CMA was significantly more effective than EE/ 2mg in women) levonorgestrel 0.03/0.15 mg/day in treating women Mean peak plasma concentrations (EE/ 130 pg/mL/2 ng/mL CMA) with mild-to-moderate papulopustular acne of the face and related disorders in a randomised, sin- Mean time to peak plasma concentration 1–2h (EE/CMA) gle-blind, multicentre trial. Mean elimination half-life (CMA) 36–39h ▲ EE/CMA was well tolerated in clinical trials and the Adverse events postmarketing surveillance studies. Adverse events Most frequent Breast pain, were those commonly reported with oral contracep- migraine/headache, tives. As expected, the most common menstrual weight gain, disturbances were breakthrough bleeding, spotting gastrointestinal disorder, depression, and amenorrhoea. tiredness