Introduction of Estradiol valerate/dienogest

Estradiol valerate/dienogest is a 4-phasic oral contraceptive approved for the prevention of pregnancy. The 4-phasic design allows for acceptable cycle control with this hormonal combination. In efficacy trials of estradiol valerate/dienogest in women aged 18-35 years, the Pearl Index ranged from 0.40 to 1.64, a range comparable to that of other combination oral contraceptives.

Menstrual bleeding patterns and cycle control with estradiol valerate/dienogest were comparable to those of a monophasic oral contraceptive containing ethinyl estradiol/levonorgestrel. Estradiol valerate/dienogest differs from other oral contraceptives in that it necessitates more stringent dosing guidelines for maximum contraceptive efficacy. New starts should be on the first day of menses only, and a back-up method of contraception is required for the first 9 days, as compared to 7 days with other oral contraceptives. Back-up contraception is usually required for any pill taken more than 12 hours later than scheduled.

Estradiol valerate/dienogest is an effective oral contraceptive. Because it has more stringent start times and requires a longer duration of backup contraception and stricter adherence, estradiol valerate/dienogest should be reserved for patients who are intolerant of other combination oral contraceptives.

Adverse Effects

In clinical trials, the most frequently reported adverse effects were headache (13.2%), metrorrhagia (8.0%), breast pain or discomfort (6.6%), nausea or vomiting (6.5%), acne (3.9%), and weight gain (2.8%). Adverse reactions led to discontinuation in 11.5% of women, with metrorrhagia, acne, headache/migraine, and weight gain cited as the most common reasons for cessation. Serious adverse effects considered possibly treatment-related were infrequent and included myocardial infarction, deep vein thrombosis, ovarian cyst, uterine leiomyoma, focal nodular hyperplasia of the liver, and autonomic nervous system imbalance.

References:

[1] KAREN L WHALEN  Renee R. Estradiol valerate/dienogest: a novel oral contraceptive.[J]. Annals of Pharmacotherapy, 2011, 45 10: 1256-1261. DOI:10.1345/aph.1Q216.