Changing convention in combination oral contraceptives: estradiol and nomegestrol acetate in a monophasic 24/4 regimen

Abstract

Initial oral contraceptive regimens were characterised by high doses of ethinylestradiol (EE) and a progestogen in a 21-day regimen that either included seven additional hormone-free tablets or simply the 21 days of combination hormonal tablets. These regimens were developed to ensure high contraceptive effectiveness, regular and predictable withdrawal bleeding episodes to mimic a menstrual cycle, and minimal unscheduled vaginal bleeding. However, these regimens were associated with adverse tolerability and safety issues resulting from the dose and characteristics of their hormonal components. Attempts to ameliorate these adverse issues included the development of lower-dose EE regimens, the incorporation of new progestogens, multiphasic regimens, and reduced hormone-free interval regimens. However, the EE component has remained a constant until the recent approval of combination oral contraceptives with an estrogen component other than EE. The development and introduction of an estradiol-based oral contraceptive regimen is presented in this review.

Estetrol‐Drospirenone combination oral contraceptive: a clinical study of contraceptive efficacy, bleeding pattern and safety in Europe and Russia

“… 3 , 4 Over the past few decades, the EE dose has been reduced to improve the safety and risk profiles. More recently, COCs with natural estrogen derivatives, estradiol or estradiol valerate, have been developed, 5 , 6 with the prospect of decreasing cardiovascular risk.…”

▼Zoely: a new combined oral contraceptive

“…It is postulated that combined oral contraceptives (COCs) containing synthetic estradiol, which is structurally identical to endogenous oestrogen,3 are potentially safer and better tolerated than those containing ethinylestradiol, the synthetic oestrogen most commonly used in COCs 4. The progestogen in Zoely is nomegestrol acetate, which is structurally related to progesterone,5 in contrast to the majority of progestogens in COCs that are derived from 19-nortestosterone6 and associated with androgenic effects 7. It is suggested that nomegestrol acetate, with its greater specificity for progesterone receptors, may minimise the potential for androgenic, oestrogenic and glucocorticoid effects 7.…”

Saudi Women Information About Two Selected Contraceptive Methods in Riyadh

“…The introduction of oral contraceptives in the 1960s represents one of the significant advances in women's health, impacting women and society from a medical, social and political viewpoint. While, the overall health benefits of contraception and oral contraception have been well documented [3,4,5]. The oral contraceptive pill (OCP) provides very effective reversible contraception/ and has an excellent overall safety and tolerability profile.…”