Drospirenone
Drospirenone is a fourth-generation progestogen with anti-mineralocorticoid and anti-androgen activity. It is widely used in combined oral contraceptives (Yaz, Yasmin) and in a progestogen-only pill (Slynd), often preferred for premenstrual symptoms and acne.
- Chemical formula
- C24H30O3
- CAS number
- 67392-87-4
- ATC code
- G03AA12
- Molecular weight
- 366.49 g/mol
- Drug class
- Progestogen with anti-mineralocorticoid and anti-androgen activity
- Also known as
- Yaz, Yasmin, Slynd
What is it?
Drospirenone is a synthetic progestogen approved in 2000, structurally derived from spironolactone rather than from older progestogen scaffolds. It is most commonly marketed in combined oral contraceptives Yasmin and Yaz (with ethinylestradiol) and in the progestogen-only pill Slynd. Authorised generics of these combinations are widely available. The molecule represents a distinct fourth-generation progestogen profile with both contraceptive and dermatological/symptomatic applications.
Mechanism of action
Drospirenone activates progesterone receptors to suppress ovulation and produce the contraceptive effect when combined with an estrogen. Its anti-mineralocorticoid activity (similar to spironolactone) reduces water retention and blood pressure changes typical of older progestogens, and its anti-androgen activity reduces sebum production and hair-follicle androgen response — useful for acne and hirsutism. The molecule does not have meaningful glucocorticoid or estrogenic activity.
Pharmacokinetics
Drospirenone is well absorbed after oral administration with bioavailability of approximately 76%. Peak plasma concentrations occur 1–2 hours post-dose. The terminal half-life is around 30 hours, supporting once-daily dosing. Metabolism produces several inactive metabolites; minimal CYP3A4 involvement makes drug interactions less prominent than with some older progestogens. Excretion is approximately equal between urine and faeces.
Indications
Drospirenone in combination with ethinylestradiol is approved as combined oral contraception, treatment of moderate acne in women requesting contraception, and treatment of premenstrual dysphoric disorder. As a progestogen-only pill (Slynd), drospirenone alone is approved for contraception in patients who cannot use estrogen. According to clinical guidelines, drospirenone-containing pills are often preferred for women with premenstrual symptoms or hormonal acne.
Safety profile
Common adverse effects include menstrual irregularities, breast tenderness, headache, mood changes and nausea, mostly in the first 2–3 cycles. The clinically important risks are venous thromboembolism (slightly higher than with older progestogens like levonorgestrel) and hyperkalaemia (from anti-mineralocorticoid activity, especially with concurrent ACE inhibitors, NSAIDs or renal impairment). According to the prescribing information, baseline and periodic potassium monitoring is sensible in users with risk factors.
Products containing this ingredient
Frequently asked questions
Why is drospirenone preferred for acne or PMDD? ▾
Drospirenone has anti-androgen activity that reduces sebum production and the hormonal driver of acne. Its anti-mineralocorticoid effect reduces water retention and bloating that some women experience on other contraceptive pills. According to clinical guidelines, drospirenone-containing combined pills are a reasonable first choice when these symptoms are part of the picture.
Does drospirenone increase blood clot risk more than older pills? ▾
Some evidence suggests a slightly higher venous thromboembolism risk with drospirenone-containing combined pills than with levonorgestrel-containing pills. The absolute risk remains low for most women. According to current contraception guidelines, the small increment matters most for women with prior thrombosis, smoking after 35, or other clotting risk factors.
What is the difference between Yaz and Yasmin? ▾
Both contain drospirenone with ethinylestradiol, but Yaz uses a 24/4 regimen (24 active pills + 4 placebo) with lower estrogen dose, while Yasmin uses a 21/7 regimen with slightly higher estrogen dose. Yaz is more commonly chosen for premenstrual symptoms because of the shorter pill-free interval and lower estrogen exposure.
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