LEVLITE
Clinical safety rating
cautionComprehensive clinical and safety monograph for LEVLITE (LEVLITE).
Levonorgestrel is a progestin that suppresses ovulation by inhibiting gonadotropin release (LH and FSH) and alters cervical mucus, endometrial thickness, and tubal motility.
| Metabolism | Hepatic via CYP3A4; reduced to inactive metabolites; excreted in urine and feces. |
| Excretion | Renal: ~50% (30% as unchanged drug, 20% as metabolites); Fecal: ~40%; Biliary: minor |
| Half-life | Terminal elimination half-life: 21-28 hours; clinical context: permits once-daily dosing |
| Protein binding | Levonorgestrel: ~99% bound to sex hormone-binding globulin (SHBG) and albumin; Ethinyl estradiol: ~98% bound to albumin |
| Volume of Distribution | Levonorgestrel: 1.8 L/kg; Ethinyl estradiol: 2.5 L/kg; clinical meaning: extensive tissue distribution |
| Bioavailability | Oral: ~100% for both levonorgestrel and ethinyl estradiol (high bioavailability due to minimal first-pass metabolism) |
| Onset of Action | Oral: 1-2 hours (serum progesterone elevation); peak effect: 48-72 hours for ovulation inhibition |
| Duration of Action | 21-day cycle (active pills) with 7-day hormone-free interval; clinical note: sustained suppression of gonadotropins during active phase |
| Molecular Weight | 1209.4 |
One tablet (levonorgestrel 0.1 mg, ethinyl estradiol 0.02 mg) orally once daily for 21 days, followed by 7 placebo tablets.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment. Not studied in severe renal impairment (GFR <30 mL/min); use with caution. |
| Liver impairment | Contraindicated in severe hepatic disease (Child-Pugh Class C). For mild to moderate impairment (Child-Pugh A/B), use with caution and monitor liver function. |
| Pediatric use | Not indicated for use in postmenarchal pediatric patients; safety and efficacy not established in prepubertal children. |
| Geriatric use | Not indicated for use in postmenopausal women; no specific geriatric dosing studies available. |
| 1st trimester | Contraindicated due to risk of fetal masculinization of female fetuses and potential teratogenic effects. |
| 2nd trimester | Contraindicated due to continued risk of fetal harm including clitoromegaly, labial fusion, and potential virilization. |
| 3rd trimester | Contraindicated; may cause fetal harm such as ambiguous genitalia in female fetuses and potential long-term effects. |
Clinical note
Comprehensive clinical and safety monograph for LEVLITE (LEVLITE).
| Placental transfer | Yes, leuprolide crosses the placenta. Evidence from animal studies and limited human data. |
| Breastfeeding | Excreted in breast milk; potential for adverse effects in nursing infants including virilization. Use only if clearly needed and with caution. |
| Lactation Rating | L3 (Moderately Safe) |
| Teratogenic Risk | FDA Pregnancy Category X. Ethinyl estradiol and levonorgestrel are contraindicated in pregnancy due to risk of fetal harm, including cardiovascular defects and limb reduction defects from first-trimester exposure. Second and third trimester exposure may be associated with genitourinary abnormalities and masculinization of female fetuses. |
| Fetal Monitoring | Not indicated during pregnancy as product is contraindicated. If exposure occurs, monitor fetus with high-resolution ultrasound and echocardiography. In postpartum use, monitor infant for jaundice, weight gain, and developmental milestones. |
| Fertility Effects | Suppresses ovulation; reversible upon discontinuation. No permanent adverse effects on fertility. Return to baseline fertility typically occurs within 1-3 cycles after cessation. |
■ FDA Black Box Warning
Cigarette smoking increases risk of serious cardiovascular events. Women over 35 who smoke should not use combination hormonal contraceptives.
| Serious Effects |
PregnancyUndiagnosed abnormal vaginal bleedingHypersensitivity to leuprolide acetate or GnRH agonists
| Precautions | Thrombotic disorders, Hepatic disease, Hypertension, Diabetes, Gallbladder disease, Depression, Ectopic pregnancy risk (emergency contraception), Reduced efficacy with CYP3A4 inducers |
| Food/Dietary | No known significant food interactions. Grapefruit and grapefruit juice do not interact with ethinyl estradiol or levonorgestrel. However, a high-fat meal may increase absorption of some oral contraceptives; consistency in taking with or without food is recommended. |
| Clinical Pearls | LEVLITE is a combination oral contraceptive containing ethinyl estradiol and levonorgestrel. Use with caution in women with migraines with aura due to increased stroke risk. Smoking increases cardiovascular risk, especially in women over 35. Monitor blood pressure at baseline and periodically. Consider alternative contraception in women with uncontrolled hypertension or history of venous thromboembolism. |
| Patient Advice | Take one pill daily at the same time each day. · If you miss a pill, follow the package instructions or consult your healthcare provider. · Do not smoke while taking this medication, as it increases the risk of blood clots and heart problems. · Use barrier contraception if you also take certain antibiotics or anticonvulsants. · Common side effects include nausea, headache, and breast tenderness, which often improve after a few months. · Seek immediate medical help for symptoms of a blood clot: leg pain/swelling, sudden chest pain, or trouble breathing. |
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