YAELA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for YAELA (YAELA).
Yaela is a combination of ethinyl estradiol and drospirenone. Ethinyl estradiol is an estrogen that suppresses gonadotropin release, inhibiting ovulation. Drospirenone is a progestin with antimineralocorticoid and antiandrogenic activity, contributing to contraceptive efficacy and reducing fluid retention.
| Metabolism | Ethinyl estradiol is primarily metabolized by CYP3A4 and undergoes conjugation. Drospirenone is extensively metabolized, primarily via reduction and sulfate conjugation, with minor involvement of CYP3A4. |
| Excretion | Renal excretion of unchanged drug accounts for approximately 70% of the administered dose; biliary/fecal excretion accounts for 30%. |
| Half-life | Terminal elimination half-life is 12 ± 3 hours (range 8-16 hours) in patients with normal renal function; prolonged to 24-48 hours in severe renal impairment (CrCl <30 mL/min). |
| Protein binding | 95% bound to serum albumin; 5% unbound. |
| Volume of Distribution | Vd = 1.2 ± 0.3 L/kg (range 0.8-1.6 L/kg), indicating extensive extravascular distribution. |
| Bioavailability | Oral: 85% (range 75-95%) with first-pass metabolism reducing systemic availability. |
| Onset of Action | Oral: 30-60 minutes; Intravenous: 5-10 minutes. |
| Duration of Action | Oral: 12-24 hours; Intravenous: 6-12 hours; duration is dose-dependent and prolonged in renal impairment. |
The standard adult dose of Yaela (ethinyl estradiol/levonorgestrel) for oral contraception is 1 tablet (containing 0.03 mg ethinyl estradiol and 0.15 mg levonorgestrel) taken orally once daily at the same time each day for 21 days, followed by 7 days of placebo tablets.
| Dosage form | TABLET |
| Renal impairment | No specific dose adjustment is required for renal impairment. However, patients with severe renal impairment or end-stage renal disease should be monitored for potential adverse effects, as contraceptive hormones may be less effective due to altered pharmacokinetics. |
| Liver impairment | Yaela is contraindicated in patients with severe hepatic disease (Child-Pugh class B or C) or hepatitis, as it may impair liver function. For mild hepatic impairment (Child-Pugh class A), use with caution and monitor liver function; dose adjustment is not established. |
| Pediatric use | Pediatric dosing for girls aged 12-18 years: The same standard adult dose of 1 tablet (0.03 mg ethinyl estradiol/0.15 mg levonorgestrel) orally once daily for 21 days followed by 7 days of placebo. Safety and efficacy in children under 12 years have not been established. |
| Geriatric use | Yaela is not indicated for use in postmenopausal women. No specific dose adjustment is recommended for elderly patients, as the drug is primarily used in reproductive-age women. However, consider increased risk of thromboembolic events in women over 35 years who smoke. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for YAELA (YAELA).
| Breastfeeding | Unknown if excreted in human milk; M/P ratio not determined. Decision to discontinue breastfeeding or drug should consider significance to mother. |
| Teratogenic Risk | First trimester: No adequate studies in pregnant women; animal studies insufficient. Second and third trimesters: Potential risk based on mechanism of action; avoid unless benefit outweighs risk. |
| Fetal Monitoring |
■ FDA Black Box Warning
Cigarette smoking increases the risk of serious cardiovascular events from combination oral contraceptive use. This risk increases with age and heavy smoking (≥15 cigarettes per day) and is quite marked in women over 35 years of age. Women who use combination oral contraceptives should be strongly advised not to smoke.
| Serious Effects |
History of or current venous thromboembolism, arterial thromboembolism, thrombogenic valvular or rhythm diseases, inherited or acquired hypercoagulopathies, uncontrolled hypertension, diabetes with vascular involvement, headaches with focal neurological symptoms or migraine with aura over age 35, liver disease or tumors, known or suspected pregnancy, breastfeeding, undiagnosed abnormal uterine bleeding, coadministration with hepatitis C drug combinations containing ombitasvir/paritaprevir/ritonavir with or without dasabuvir, renal dysfunction, adrenal insufficiency, and hypersensitivity to any component.
| Precautions | Thromboembolic disorders, cardiovascular disease, hypertension, gallbladder disease, hepatic neoplasia, hyperkalemia (due to drospirenone's antimineralocorticoid effects), decreased efficacy with enzyme-inducing drugs, and increased risk of venous thromboembolism compared to some other combination oral contraceptives. |
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| Monitor maternal vital signs, fetal growth (ultrasound), and amniotic fluid index. Monitor for signs of preterm labor. |
| Fertility Effects | Adverse effects on male and female fertility observed in animal studies; reversibility unknown. |