TAYTULLA
Clinical safety rating
cautionComprehensive 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. |
| Molecular Weight | 288.42 |
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 | Contraindicated due to risk of female pseudohermaphroditism and other teratogenic effects associated with androgenic activity. |
| 2nd trimester | Contraindicated; potential for virilization of female fetus and other adverse developmental outcomes. |
| 3rd trimester | Contraindicated; risk of clitoromegaly, labioscrotal fusion, and other virilizing effects in female fetuses. |
Clinical note
Comprehensive clinical and safety monograph for TAYTULLA (TAYTULLA).
| Placental transfer | Crosses placenta; demonstrated in animal studies and human case reports. |
| Breastfeeding | Excreted into breast milk; may cause adverse effects in nursing infants, including potential androgenic effects. Not recommended during breastfeeding. |
| Lactation Rating | L5 - Contraindicated |
| 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. |
| 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. |
■ 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 |
PregnancyBreastfeedingKnown or suspected carcinoma of the prostate or male breastSevere hepatic impairmentHypersensitivity to testosterone or any component
| 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. |
| Food/Dietary | No specific food interactions are known. Grapefruit juice may theoretically increase estrogen levels due to CYP3A4 inhibition, but clinical significance is unclear. Avoid excessive alcohol consumption as it may impair liver function and increase VTE risk. |
| Clinical Pearls | TAYTULLA is a combined hormonal contraceptive containing estetrol (E4) and drospirenone. It is the first contraceptive to use estetrol, a native estrogen with selective tissue activity. Its unique pharmacokinetics allow for a 24/4 regimen with a 4-day hormone-free interval. The progestin drospirenone has antimineralocorticoid activity, which can help reduce water retention and may be beneficial in patients with acne or premenstrual dysphoric disorder. Due to the risk of hyperkalemia, monitor serum potassium in patients on concomitant medications that increase potassium levels, such as ACE inhibitors, ARBs, NSAIDs, or potassium-sparing diuretics. The risk of venous thromboembolism (VTE) is present, and patients should be counseled on symptoms. TAYTULLA is contraindicated in patients with a BMI ≥ 35 kg/m² due to increased VTE risk. |
| Patient Advice | Take one tablet daily at the same time, preferably after the evening meal. The pill pack contains 24 active tablets (white) followed by 4 placebo tablets (yellow). · If you miss a white tablet, take it as soon as you remember, even if it means taking two tablets in one day. If you miss a white tablet for more than one day, use backup contraception for the next 7 days. · This medication does not protect against HIV or other sexually transmitted infections. Use condoms for STI protection. · Common side effects include headache, nausea, breast tenderness, and mood changes. Contact your healthcare provider if you experience severe abdominal pain, chest pain, shortness of breath, or leg pain/swelling, which may indicate a blood clot. · Smoking increases the risk of serious cardiovascular side effects. Women over 35 who smoke should not use this medication. · Inform your healthcare provider of all medications you take, especially those that affect potassium levels (e.g., certain blood pressure medications, NSAIDs, potassium supplements). |
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