DROSPIRENONE

Drospirenone is a synthetic progestin that is an analog to spironolactone. Its molecular weight is 366.5 and its molecular formula is C₂₄H₃₀O₃.

The compound is part of certain birth control formulations. Drospirenone differs from other synthetic progestins in that its pharmacological profile in preclinical studies shows it to be closer to the natural progesterone. As such it has anti-mineralocorticoid properties, counteracts the estrogen-stimulated activity of the renin-angiotensin-aldosterone system, and is not androgenic. With its activities similar to spironolactone it may lead to less water retention and breast tenderness and improved skin appearance (less acne).

Drospirenone is absorbed orally, - about 76% is bioavailable. It is not bound by sex hormone binding globulin or corticosteroid binding globulin, but by other serum proteins. Metabolites have not been shown to be biologically active, show up in urine and feces, and are essentially completely excreted within 10 days.

The compound is part of certain newer oral contraceptive formulations, e.g. Yasmin® contains 3 mg drospirenone and 30 mcg ethinylestradiol per tablet. It is indicated for the prevention of pregnancy in women who elect an oral contraceptive.

The medication is contraindicated in patients with hepatic dysfunction, renal insufficiency, adrenal insufficiency, or in whom the use of oral contraceptives is contraindicated. Because of the anti-mineralocorticoid effects care needs to be exercised when other drugs that may increase potassium levels are taken. Such medications include ACE inhibitors, angiotensin-II receptor agonists, potassium sparing diuretics, potassium supplementation, heparin, aldosterone antagonists, and NSAIDS.

See also

• Progestins
• Oral contraceptive
• Oral contraceptive formulations

External links

• Medline information

References

• Krattenmacher R. Drospirenone: pharmacology and pharmacokinetics of a unique progestogen. Contraception 2000;62:29-38.
• Yasmin product information