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. |
| Molecular Weight | 246.27 |
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 | Contraindicated due to risk of teratogenicity (neural tube defects, congenital heart defects). |
| 2nd trimester | Contraindicated due to risk of fetal harm; no established safe dose. |
| 3rd trimester | Contraindicated due to risk of neonatal hemorrhage and fetal nephrotoxicity. |
Clinical note
Comprehensive clinical and safety monograph for YAELA (YAELA).
| Placental transfer | Crosses placenta extensively (fetal concentrations approach maternal levels). |
| Breastfeeding | Excreted into breast milk; may cause adverse effects in nursing infants such as bleeding and renal impairment. Avoid breastfeeding while on therapy. |
| Lactation Rating |
■ 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 |
PregnancyHypersensitivity to drug or excipientsActive peptic ulcer diseaseSevere hepatic impairment
| 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. |
| Food/Dietary | Take with food to reduce gastrointestinal upset. Avoid grapefruit and grapefruit juice as they may increase drug levels. No specific dietary restrictions otherwise. |
Loading safety data…
| L5 (Contraindicated) |
| 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 | 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. |
| Clinical Pearls | YAELA is a novel oral anticoagulant, a direct factor Xa inhibitor with rapid onset. No routine coagulation monitoring required. Use with caution in renal impairment (CrCl <15 mL/min contraindicated). Reversal agent andexanet alfa available. Avoid concurrent use with strong dual CYP3A4 and P-gp inhibitors. |
| Patient Advice | Take exactly as prescribed, at the same time each day. · If a dose is missed, take as soon as remembered on the same day; do not double dose. · Do not stop taking without consulting your doctor; risk of clot formation. · Monitor for signs of bleeding: unusual bruising, prolonged bleeding, dark stools, pink urine. · Seek immediate medical attention for severe bleeding or head injury. · Inform all healthcare providers that you are taking YAELA before any surgery or procedure. · Avoid aspirin, NSAIDs, and other anticoagulants unless prescribed. |