Pharmacology of different progestogens: the special case of drospirenone

  title={Pharmacology of different progestogens: the special case of drospirenone},
  author={R{\'e}gine Sitruk-Ware},
  pages={12 - 4}
The pharmacological properties of progestins used in contraception and hormone replacement therapy (HRT) vary, depending upon the molecules from which they are derived. Very small structural changes may induce considerable differences in effects. It is unclear if the currently available progestins are able to bind specifically to the progesterone receptors, PR-A or PR-B. The clinical relevance of more specific binding to one or the other isoforms of the progesterone receptor is still unknown… 

Effects of synthetic gestagens on fish reproduction

The effects of two progestins currently marketed in contraceptive formulations, levonorgestrel (LNG) and drospirenone (DRSP), were investigated in adult fathead minnows following an Organization for Economic Cooperation and Development 21-d fish reproduction screening assay draft protocol with additional end points.

Progestogens used in postmenopausal hormone therapy: differences in their pharmacological properties, intracellular actions, and clinical effects.

Differences in chemical structure, metabolism, pharmacokinetics, affinity, potency, and efficacy via steroid receptors, intracellular action, and biological and clinical effects confirm the absence of a class effect of progestogens.

A review of the cardiovascular and breast actions of drospirenone in preclinical studies

Differences in pharmacological profile among progestins may translate to characteristic divergences in clinical profile, with potential implications for long-term health.

Potential role of progestogens in the control of adipose tissue and salt sensitivity via interaction with the mineralocorticoid receptor

The potential role of the antimineralocorticoid properties of progestogens in the control of body weight, adipose tissue proliferation and salt sensitivity; their therapeutic use in postmenopausal women, as well as in women affected by polycystic ovary syndrome, may open new and unexpected possibilities in the treatment of related metabolic disorders.

Tailoring combination oral contraceptives to the individual woman.

Assisted counseling to raise awareness of the specific characteristics of the different COC options available may optimize adherence and patient acceptability and offer improvements over their predecessors.

Drospirenone: a Latin American perspective for oestrogen-free oral contraception

Considering the increasing prevalence of these comorbidities in Latin America, the 4 mg drospirenone-only pill is suggested as one of the strategies of choice in the region for those women who choose oral contraceptives.

Drospirenone: a novel progestin

Drospirenone-containing contraceptives have similar efficacy and safety profiles to other low-dose oral contraceptives, but seem to offer improved tolerability with regard to weight gain, mood changes, acne and treatment of a severe form of premenstrual syndrome called pre menstrual dysphoric disorder.



Progestogens in hormonal replacement therapy: new molecules, risks, and benefits

Complying with the classic contraindications of HRT and selecting molecules devoid of estrogenic, androgenic, or glucocorticoid effect should allow a larger use of the progestins without any major drawback.

Drospirenone, a progestogen with antimineralocorticoid properties: a short review

  • W. Oelkers
  • Medicine, Biology
    Molecular and Cellular Endocrinology
  • 2004

Drospirenone: a Novel Progestogen with Antimineralocorticoid and Antiandrogenic Activity

Drospirenone exerts potent progestogenic and antigonadotropic activity which was studied in various animal species and efficiently promotes the maintenance of pregnancy in ovariectomized rats, inhibits ovulation in rats and mice and stimulates endometrial transformation in the rabbit.

The pharmacological profile of a novel norpregnance progestin (trimegestone).

Results show trimegestone to have a favorable pharmacological profile with potent progestomimetic activity, and to be not associated with any unwanted pharmacological effects.

Progesterone and progestins

The role of progesterone in sterility contraception and treatment of dysovulation and menopause is described and progestogen derived from testosterone are best adapted to oral contraception although they have some clinical and metabolic side effects.