TAYTULLA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TAYTULLA (TAYTULLA).
Combination of drospirenone, a spironolactone analog with antimineralocorticoid and antiandrogenic activity, and ethinyl estradiol, an estrogen. Suppresses gonadotropins, primarily luteinizing hormone, inhibiting ovulation. Increases cervical mucus viscosity and alters endometrial receptivity.
| Metabolism | Ethinyl estradiol: CYP3A4, sulfation, glucuronidation. Drospirenone: CYP3A4, reduction, sulfation, glucuronidation. |
| Excretion | Renal: ~60% as unchanged drug; Fecal: ~40% as metabolites and unchanged drug. |
| Half-life | Terminal elimination half-life: 30 hours. Provides once-daily dosing with steady-state achieved after 7 days. |
| Protein binding | >=90% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 3.5 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Oral: 87% (immediate-release); TAYTULLA formulation: 79% relative to immediate-release. |
| Onset of Action | Oral: 1 hour after ingestion for initial therapeutic effect; maximal efficacy by 2 hours. |
| Duration of Action | 24 hours for analgesic effect, supporting once-daily dosing; sustained release formulation maintains levels. |
One capsule orally once daily for 24 weeks.
| Dosage form | CAPSULE |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment. Insufficient data for severe impairment (CrCl <30 mL/min); use with caution. |
| Liver impairment | Contraindicated in patients with Child-Pugh Class B or C hepatic impairment. Use with caution in Child-Pugh Class A. |
| Pediatric use | Not approved for use in pediatric patients. |
| Geriatric use | Clinical studies did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects; use with caution due to potential for decreased hepatic, renal, or cardiac function. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TAYTULLA (TAYTULLA).
| Breastfeeding | Drospirenone and ethinyl estradiol are excreted in human milk in small amounts (M/P ratio not established). Use during lactation is not recommended as it may reduce milk production and composition. Alternative contraception should be considered. |
| Teratogenic Risk | TAYTULLA (drospirenone/ethinyl estradiol) is contraindicated in pregnancy. First trimester: No increased risk of major birth defects from inadvertent use, but postmarketing studies show a small increased risk of non-cardiac malformations. Second and third trimesters: Associated with fetal harm including cardiovascular and skeletal malformations, and feminization of male fetuses due to estrogenic effects. |
■ FDA Black Box Warning
Cigarette smoking increases risk of serious cardiovascular events from combination oral contraceptives. Risk increases with age and heavy smoking (≥15 cigarettes/day). Women over 35 who smoke should not use.
| Serious Effects |
Thrombophlebitis or thromboembolic disorders, cerebrovascular or coronary artery disease, known or suspected breast cancer, endometrial carcinoma or other estrogen-dependent neoplasia, undiagnosed abnormal genital bleeding, cholestatic jaundice of pregnancy or jaundice with prior pill use, hepatic adenoma or carcinoma, known or suspected pregnancy, hypersensitivity to any component, uncontrolled hypertension, diabetes with vascular involvement, headaches with focal neurological symptoms, major surgery with prolonged immobilization, heavy smoking and age >35 years.
| Precautions | Thrombotic disorders (DVT, PE, stroke, MI), hypertension, gallbladder disease, hepatic neoplasia, hyperkalemia (especially in patients with renal/hepatic impairment or on potassium-sparing drugs), depression, impaired glucose tolerance, weight gain, fluid retention, irritability, mood changes. |
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| Fetal Monitoring | If inadvertently used during pregnancy, monitor fetal development with ultrasound for congenital anomalies. No routine maternal monitoring required beyond standard prenatal care. |
| Fertility Effects | TAYTULLA is a contraceptive that suppresses ovulation. After discontinuation, fertility typically returns promptly, but there may be a delay in return to normal ovulatory cycles. |