Oral Progestins in Hormonal Contraception: Importance and Future Perspectives of a New Progestin Only-Pill Containing 4 mg Drospirenone

Abstract

Hormonal contraceptives are an effective and safe method for preventing pregnancy. Progestins used in contraception are either components of combined hormonal contraceptives (tablets, patches or vaginal rings) or are used as a single active ingredient in progestin mono-preparations (the progestin-only pill (POP), implants, intrauterine systems or depot preparations). Progestins are highly effective in long-term contraception when used properly, and have a very good safety profile with very few contraindications. A new oestrogen-free ovulation inhibitor (POP) has recently been authorised in the USA and the EU. This progestin mono-preparation contains 4 mg of drospirenone (DRSP), which has anti-gonadotropic, anti-mineralocorticoidic and anti-androgenic properties. The hormone administration regimen of 24 days followed by a 4-day hormone-free period was chosen to improve bleeding control and to maintain oestradiol concentrations at early follicular-phase levels, preventing oestrogen deficiency. Clinical trials have demonstrated a high contraceptive effectiveness, a very low risk of cardiovascular side effects and a favourable menstrual bleeding pattern. Due to the long half-life of DRSP (30 – 34 hours), the effectiveness of the preparation is maintained even if a woman forgets to take a pill on a single occasion. Studies involving deliberate 24-hour delays in taking a pill have demonstrated that ovulation inhibition is maintained if a single pill is missed. Following a summary of the current status of oestrogen-free contraception, this review article will describe the clinical development programme of the 4 mg DRSP mono-preparation and the resulting data on the effectiveness and safety of this new oestrogen-free oral hormonal contraceptive.

Safety of Progestogen Hormonal Contraceptive Methods during Lactation: An Overview

“…Thus, no adverse effects on neonates and/or breastfed infants are expected with 4 mg drospirenone. Notably, the 24 + 4 day regimen of 4 mg drospirenone demonstrates high safety, and a high acceptance rate that is documented with a low incidence of treatment discontinuation due to unacceptable changes in bleeding profiles [ 22 , 24 , 35 ]. DRSP ( n = 71) used postpartum statistically reduces the risk of postpartum depression compared to the control group ( n = 78), as assessed by the Edinburgh Postpartum Depression Scale at 12 and 24 weeks postpartum, particularly in women with individual steroid sensitivity [ 36 ].…”

Venous Thromboembolism Issues in Women

“…Moreover, DRSP has antigonadotropic, antimineralocorticoidic, and antiandrogenic properties. 33 Whereas the intake of CHCs containing DRSP is associated with a sixfold increased incidence of VTE, no cases of VTE and no changes in hemostaseological factors (i.e., APC resistance, protein C, antithrombin, factor VII, factor VIII, D-dimer levels) were observed in more than 2,500 women and over 25,000 cycles in DRSP users. 34 Venous Thromboembolism Issues in Women Linnemann et al 293…”

Slynd: does a drospirenone progestogen-only pill offer an advantage?

“…A new pack is started the day after the last tablet of the previous pack. The regimen of 24 days of progestogen followed by a 4-day hormone-free period was chosen in an attempt ‘to improve bleeding control and to maintain oestradiol concentrations at early follicular phase levels, preventing oestrogen deficiency’ 12…”