Effectiveness and acceptability of progestogens in combined oral contraceptives – a systematic review

Abstract

Background: The progestogen component of oral contraceptives (OCs) has undergone changes since it was recognized that their chemical structure can influence the spectrum of minor adverse and beneficial effects.

Nuclear Receptors as Drug Targets: A Historical Perspective of Modern Drug Discovery

“…With the introduction of these two oral contraceptives into the marketplace, the era of progesterone receptor ligands entered a new phase. More potent progestines, like levonorgestrel and gestodene, and progestines with a special favorable profile on other nuclear receptors, like cyproterone acetate and drospirenone, were discovered during the following decades of intense research efforts in this field [33]. Cyproterone acetate was the first progestin with a potent antiandrogenic effect and it is still in use for the treatment of prostate cancer [34].…”

Long-Acting Injectable Hormonal Dosage Forms for Contraception

“…Injectables of this type, however, require frequent (at least four times per year) clinic visits which may cause discontinuation and prolonged return to fertility due to users' difficulty in complying with the multiple-injection schedule. Meanwhile, the side effects of current available contraceptive injectables are well noticed in the clinical sides which include bone loss, menstrual irregularities, nausea, weight gain, mood changes, headaches, and breast tenderness (2,4,7,14). Therefore, there is a desire for longacting injectable contraceptives which could provide contraception for longer than 3 months after one shot and have less side effects so that better adherence and continuation rates can be achieved (15,16).…”

“…In the 1980s, the third-generation progestogens including desogestrel, gestodene, norgestimate, and etonorgestrel ( Fig. 3) were introduced to the market as oral pills for contraception in patients with diabetes or lipid disorders due to their minimal impact on blood glucose levels and the lipid profile (5)(6)(7). To minimize the side effects related to androgenic, glucocorticoid and estrogenic receptor interactions, the fourth generation progestogens including drospirenone, and dienogest ( Fig.…”

“…2) were introduced into the market in the 1970s (5,6). Currently, LNG is widely used progestogen in long acting contraceptives (5). In the 1980s, the third-generation progestogens including desogestrel, gestodene, norgestimate, and etonorgestrel ( Fig.…”

“…1) (1). To reduce the cost and the side effects such as bone loss (2,4) associated with the first generation progestogens, second-generation progestogens to include levonorgestrel (LNG) and norgestrel (mixture of two stereoisomers dextroorgestrel and levonorgestrel) (Fig. 2) were introduced into the market in the 1970s (5,6).…”