YASMIN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for YASMIN (YASMIN).
Combination of ethinyl estradiol and drospirenone suppresses gonadotropins, inhibiting ovulation. Drospirenone has antimineralocorticoid activity, reducing water retention, and antiandrogenic activity.
| Metabolism | Ethinyl estradiol is primarily metabolized by CYP3A4; drospirenone is metabolized by CYP3A4 and also undergoes reduction and sulfate conjugation. |
| Excretion | Approximately 40% renal and 60% fecal after oral administration; metabolites are excreted as glucuronide and sulfate conjugates. |
| Half-life | Terminal elimination half-life is approximately 30 hours for drospirenone; steady-state concentration is achieved after 10 days of daily dosing. |
| Protein binding | Drospirenone is 95-97% bound to serum proteins, primarily to albumin but not to sex hormone-binding globulin (SHBG) or corticosteroid-binding globulin (CBG). |
| Volume of Distribution | Apparent volume of distribution is approximately 4 L/kg for drospirenone, indicating extensive tissue distribution. |
| Bioavailability | Oral bioavailability of drospirenone is approximately 76% due to first-pass metabolism. |
| Onset of Action | Oral: Onset of contraceptive effect occurs within 7 days of continuous dosing if initiated on day 1 of menstrual cycle; immediate effect if started on first day of menses. |
| Duration of Action | Duration of contraceptive effect lasts 24 hours; requires daily dosing. Withdrawal bleeding typically occurs during the 7-day placebo interval. |
| Brand Substitutes | Rasmin 0.03 mg/3 mg Tablet, Janya 0.03 mg/3 mg Tablet, Terobiz 0.03mg/3mg Tablet, Yanci Tablet, Drosmac Tablet |
One tablet (ethinyl estradiol 0.03 mg / drospirenone 3 mg) orally once daily for 21 days, followed by 7 days of placebo.
| Dosage form | TABLET |
| Renal impairment | Contraindicated in patients with severe renal insufficiency (GFR < 30 mL/min) or acute renal failure. No dose adjustment required for mild to moderate impairment (GFR 30-89 mL/min). |
| Liver impairment | Contraindicated in patients with severe hepatic disease (Child-Pugh class C) or liver tumors. Use with caution in mild to moderate impairment (Child-Pugh A or B); monitor liver function. |
| Pediatric use | Not indicated for use in postmenarchal pediatric patients for contraception; safety and efficacy established only for moderate acne vulgaris in girls ≥14 years. Dose: one tablet daily for 21 days followed by 7 days placebo. |
| Geriatric use | Not indicated for use in postmenopausal women; contraindicated in women over 35 years who smoke due to increased cardiovascular risk. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for YASMIN (YASMIN).
| Breastfeeding | Excreted in breast milk in small amounts (ethinyl estradiol M/P ratio ~0.4; drospirenone M/P ratio not established). May reduce milk production and quality. Use in breastfeeding is not recommended, especially in early postpartum period. Alternative contraception advised. |
| Teratogenic Risk | YASMIN (drospirenone/ethinyl estradiol) is contraindicated in pregnancy. First trimester: no increased risk of major birth defects from inadvertent use, but theoretical risk due to hormonal effects. Second and third trimesters: associated with fetal harm, including cardiovascular and genitourinary anomalies from continued use; not indicated for use in pregnancy. |
■ FDA Black Box Warning
Cigarette smoking increases the risk of serious cardiovascular events from combination oral contraceptives. This risk increases with age (especially in women over 35 years) and with the number of cigarettes smoked. Women who use combination hormonal contraceptives should be strongly advised not to smoke.
| Serious Effects |
["Thrombophlebitis or thromboembolic disorders","Cerebrovascular or coronary artery disease","Known or suspected pregnancy","Undiagnosed abnormal uterine bleeding","Breast cancer or other estrogen- or progestin-sensitive cancer","Hepatic adenoma or carcinoma, or active liver disease","Renal insufficiency (creatinine clearance <50 mL/min)","Adrenal insufficiency","Use with hepatitis C drug combinations containing ombitasvir/paritaprevir/ritonavir with or without dasabuvir"]
| Precautions | ["Thrombotic disorders and cardiovascular events","Hyperkalemia risk due to drospirenone's antimineralocorticoid effect, especially in patients with renal, hepatic, or adrenal insufficiency","Liver disease","Elevated blood pressure","Gallbladder disease","Carbohydrate and lipid metabolic effects","Headache/migraine","Bleeding irregularities"] |
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| Fetal Monitoring | If inadvertent use in pregnancy occurs, monitor fetal growth and development via ultrasound. No specific monitoring required otherwise, as drug should be discontinued immediately upon pregnancy diagnosis. Assess for signs of thrombosis, hypertension, and hepatic effects if exposure continues. |
| Fertility Effects | YASMIN is used as an oral contraceptive and reversibly suppresses ovulation. After discontinuation, return to fertility may be delayed by up to 3 cycles. No permanent effect on fertility. |