Drospirenone

Hormonal Contraceptiveprescriptionoral · inferred

Fourth-generation progestin derived from 17-alpha-spirolactone. Unique among OC progestins in retaining meaningful antimineralocorticoid (spironolactone-like, ~1/8 potency) and antiandrogenic activity with no estrogenic, glucocorticoid, or androgenic effects. Component of Yaz, Yasmin, Beyaz (with EE + folate). Can raise serum potassium (caution in CKD, with ACE inhibitors, ARBs, spironolactone). Long terminal half-life (~30h) supports once-daily dosing. Higher VTE risk than second-generation progestins.

Projected serum levels — 3 mg, once daily

Drospirenone

Maintenance only With loading dose

Maintenance schedule: 3 mg once daily (oral).

Loading schedule: 7.1 mg on day 1, then 3 mg once daily — reaching therapeutic levels sooner.

Modeled steady state after ~3 days: peak ≈ 5.2 mg, trough ≈ 3.1 mg body load. Population-based estimate over 15 days for a 3 mg dose at a 70 kg reference body mass — the interactive app scales curves to your doses, timing, and body mass.

Key facts

Category: Hormonal Contraceptive
Route modeled: Oral
Model confidence: inferred
Half-life: 31 h
Common dose: 3 mg
Suggested maximum: 4 mg/day
Reference dose range: 1.5–4 mg (single dose)
Suggested cadence: once daily
Validated against: 3 mg oral — Cmax 0.040 mg/L at 1.5 h

Documented interactions

danger
Carbamazepine (Tegretol) + Drospirenone CYP induction
Carbamazepine (Tegretol) inducer of CYP3A4 predicted to change Drospirenone AUC by ~0.49x
danger
Combined OC (Drospirenone / Ethinyl Estradiol) + Drospirenone Stacked effects
Combined OC (Drospirenone / Ethinyl Estradiol) and Drospirenone both push the androgen receptor, mineralocorticoid receptor, and progesterone receptor in the same direction.
danger
Depo-Provera (DMPA Injection) + Drospirenone Stacked effects
Depo-Provera (DMPA Injection) and Drospirenone both push the glucocorticoid receptor, mineralocorticoid receptor, and progesterone receptor in the same direction.
danger
Efavirenz (Sustiva) + Drospirenone CYP induction
Efavirenz (Sustiva) inducer of CYP3A4 predicted to change Drospirenone AUC by ~0.35x
danger
Levothyroxine (Synthroid) + Drospirenone Protein binding
Drospirenone may displace Levothyroxine (Synthroid) from plasma protein binding sites, transiently raising free drug concentration. This drug has a narrow therapeutic index; free concentration…
danger
Micronized Progesterone (Oral) + Drospirenone Stacked effects
Drospirenone and Micronized Progesterone (Oral) both push the androgen receptor, mineralocorticoid receptor, and progesterone receptor in the same direction.

Serum checks 225 modeled interaction pairings for drospirenone across your whole stack — absorption conflicts, enzyme inhibition, and nutrient depletion included.

Research behind this entry

Drospirenone: a novel progestin with antimineralocorticoid and antiandrogenic activity Krattenmacher R · Contraception, 2000 DOI
Definitive preclinical and clinical PK/PD review establishing drospirenone as a spironolactone-derived progestin with unique antimineralocorticoid/antiandrogenic profile, oral F ~76%, terminal t1/2 ~30h.
Pharmacokinetics of drospirenone and ethinylestradiol in Caucasian and Japanese women Blode H et al. · European Journal of Contraception and Reproductive Health Care, 2001 DOI
Single- and multiple-dose PK study confirming oral F 76%, protein binding 97%, minor CYP3A4 metabolism, predominant non-CYP reductive clearance.
Hormonal contraception and risk of venous thromboembolism: national follow-up study Lidegaard O et al. · BMJ, 2011 DOI
Danish registry cohort (1.6M women) finding drospirenone-containing COCs carried ~2x VTE risk vs LNG-containing COCs.

3 published studies referenced in the app, each with a plain-language summary.