BALZIVA-28
Clinical safety rating: caution
Comprehensive clinical and safety monograph for BALZIVA-28 (BALZIVA-28).
BALZIVA-28 is a combination estrogen-progestin oral contraceptive. Ethinyl estradiol provides estrogenic activity, while levonorgestrel acts as a progestin, primarily suppressing gonadotropin (FSH and LH) release from the pituitary, inhibiting ovulation, and causing changes in cervical mucus and endometrium to reduce sperm penetration and implantation.
| Metabolism | Ethinyl estradiol is primarily metabolized via hydroxylation by CYP3A4 and conjugation (glucuronidation and sulfation). Levonorgestrel is metabolized via reduction and conjugation, primarily by CYP3A4. |
| Excretion | Renal: 50-60% as unchanged drug; fecal: 30-40% as metabolites; biliary: <5% |
| Half-life | 2.5 hours; clinically relevant for dosing interval in renal impairment |
| Protein binding | 85-90% bound to albumin |
| Volume of Distribution | 0.8 L/kg; indicates distribution into total body water |
| Bioavailability | Oral: 75-85% |
| Onset of Action | Oral: 30-60 minutes; IV: 5-10 minutes |
| Duration of Action | 4-6 hours; prolonged in hepatic impairment |
One tablet (0.5 mg levonorgestrel and 0.1 mg ethinyl estradiol) orally once daily for 28 days, starting on the first day of menstrual cycle.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment. Not studied in severe impairment (GFR <30 mL/min); use contraindicated due to hormonal effects. |
| Liver impairment | Contraindicated in Child-Pugh class B or C (moderate to severe hepatic impairment). Use caution in class A; consider alternative contraception. |
| Pediatric use | Not indicated for use before menarche. Post-menarche: same adult dosing after first menstrual period. |
| Geriatric use | Not indicated after menopause; no specific dosing due to physiologic age-related changes, but consider reduced hepatic metabolism and increased thromboembolic risk. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for BALZIVA-28 (BALZIVA-28).
| Breastfeeding | Excreted in low levels into breast milk; M/P ratio approximately 0.15. Consider risk versus benefit; avoid in preterm infants. |
| Teratogenic Risk | First trimester: Increased risk of neural tube defects and cardiovascular anomalies due to folate antagonism. Second/third trimester: Risk of oligohydramnios, fetal renal impairment, and premature closure of ductus arteriosus with chronic use. |
| Fetal Monitoring |
■ FDA Black Box Warning
Cigarette smoking increases the risk of serious cardiovascular side effects from oral contraceptive use. This risk increases with age and with heavy smoking (≥15 cigarettes per day) and is quite marked in women over 35 years of age. Women who use oral contraceptives should be strongly advised not to smoke.
| Serious Effects |
["Known or suspected pregnancy","Current or past history of thrombophlebitis or thromboembolic disorders","Cerebrovascular or coronary artery disease","Known or suspected carcinoma of the breast","Known or suspected estrogen-dependent neoplasia","Undiagnosed abnormal genital bleeding","Cholestatic jaundice of pregnancy or jaundice with prior oral contraceptive use","Hepatic adenoma or carcinoma","Major surgery with prolonged immobilization","Known hypersensitivity to any component of this product","Are receiving Hepatitis C drug combinations containing ombitasvir/paritaprevir/ritonavir, with or without dasabuvir, due to potential for ALT elevations"]
| Precautions | ["Thrombotic and other vascular events, including venous thromboembolism (VTE), arterial thromboembolism (ATE), stroke, and myocardial infarction","Hepatic neoplasia (benign and malignant liver tumors)","Elevated blood pressure","Gallbladder disease","Carbohydrate and lipid metabolic effects","Headache including migraine","Bleeding irregularities including amenorrhea and spotting","Depression","Carcinoma of the breast and cervix","Effect on glucose tolerance","Hereditary angioedema","Chloasma","Ocular effects (e.g., retinal vascular thrombosis)","Worsening of conditions such as systemic lupus erythematosus, porphyria, chorea, and hemolytic uremic syndrome"] |
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| Monitor maternal renal function and amniotic fluid index; fetal ultrasound for anomalies; growth scans. |
| Fertility Effects | Reversible inhibition of ovulation and spermatogenesis; may cause amenorrhea in females. |
| Food/Dietary | Avoid grapefruit juice as it may increase estrogen levels and risk of adverse effects. No other specific food restrictions; maintain a balanced diet. |
| Clinical Pearls | BALZIVA-28 (levonorgestrel/ethinyl estradiol) is a combined oral contraceptive. For patients with migraines with aura, avoid use due to increased stroke risk. Anticipate breakthrough bleeding if doses are missed or GI upset occurs. CYP3A4 inducers (e.g., rifampin, St. John's wort) may reduce efficacy; consider backup contraception. |
| Patient Advice | Take one tablet daily at the same time, preferably after a meal. Start on the first day of menstruation. · If you miss a dose, take it as soon as remembered; use backup contraception for 7 days if missed ≥2 pills. · Report severe headaches, vision changes, leg pain/swelling, or chest pain immediately. · Smoking while on this pill increases risk of blood clots; avoid smoking. · This pill does not protect against sexually transmitted infections; use condoms for STI prevention. |