Indications
Drospirenone is a progestin that females use as an oral contraceptive.
⚠️ Always consult a registered physician before taking any medicine.
Pharmacology
Drospirenone is a progestin. It is used by females of reproductive potential to prevent pregnancy. As an oral contraceptive, it lowers the risk of becoming pregnant mainly by suppressing ovulation. Drospirenone is a spironolactone analogue and has anti-mineralocorticoid activity.
Absorption: After single oral doses from 1 to 10 mg, the pharmacokinetics of drospirenone are dose-proportional. Maximum plasma concentrations (Cmax) of about 27 ng/ml are reached roughly 2 to 6 hours after a single dose. During a treatment cycle, maximum steady-state serum concentrations of about 41 ng/ml are reached after about 10 days of treatment. Taking drospirenone with food has no influence on how much is absorbed.
Distribution: Between 95% and 97% of drospirenone is bound to serum albumin. It does not bind to sex hormone binding globulin (SHBG) or corticosteroid-binding globulin (CBG). The apparent volume of distribution is approximately 4 L/kg.
Metabolism: Drospirenone is extensively metabolized after oral administration. The two main metabolites found in human plasma are the acid form of drospirenone, which is generated when the lactone ring opens, and 4,5-dihydro drospirenone-3-sulfate, which is formed by reduction and then sulfation. Neither metabolite was shown to be pharmacologically active. Drospirenone also undergoes oxidative metabolism catalyzed by CYP3A4.
Excretion: Serum concentrations of drospirenone show a terminal disposition phase half-life of approximately 30 hours, after both single and multiple dose regimens. Excretion was nearly complete after ten days, and the amounts excreted were slightly higher in feces than in urine. Because drospirenone was extensively metabolized, only trace amounts of unchanged drospirenone were found in urine and feces.
Pregnancy & Breastfeeding
Studies and meta-analyses show little or no increased risk of birth defects in children born to women who take an oral progestin by mistake in early pregnancy. If pregnancy occurs, stop the medicine, because there is no reason to use hormonal contraceptives during pregnancy.
Only negligible amounts of Drospirenone pass into breast milk. So at therapeutic doses, no effects are expected in breastfed newborns or infants. In general, no adverse effects have been found on milk production, or on the health, growth or development of the infant, with the use of POPs.
⚠️ Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.
Side Effects & Interactions
Side Effects
No side-effect data recorded yet.