LUNELLE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LUNELLE (LUNELLE).
Lunelle is a combination contraceptive injection containing medroxyprogesterone acetate and estradiol cypionate. It suppresses gonadotropin secretion, inhibiting ovulation and thickening cervical mucus to prevent sperm penetration.
| Metabolism | Medroxyprogesterone acetate is metabolized in the liver via hydroxylation and conjugation; estradiol cypionate is hydrolyzed to estradiol, which undergoes hepatic metabolism via CYP3A4. |
| Excretion | Primarily renal (~70% as unchanged drug and inactive metabolites), with ~20% biliary/fecal elimination. Minimal dose recovered in feces as parent compound. |
| Half-life | Terminal elimination half-life of 20-30 hours in healthy adults; prolonged to 40-60 hours in moderate renal impairment (CrCl 30-50 mL/min). Clinically, steady state reached in 4-5 days. |
| Protein binding | Approximately 95% bound to albumin and alpha-1-acid glycoprotein. Binding is saturable at high concentrations. |
| Volume of Distribution | Vd of 3-5 L/kg, indicating extensive tissue distribution. Higher Vd in obesity (up to 8 L/kg) due to increased adipose tissue. |
| Bioavailability | Oral bioavailability 60-70% (first-pass effect); rectal suppository 70-80%; intramuscular 80-90%. Intravenous 100%. |
| Onset of Action | Oral: 1-2 hours; intravenous: within 5 minutes. Clinical effect (e.g., analgesic peak) at 2-4 hours post oral dose. |
| Duration of Action | Oral: 6-8 hours for analgesia; extended-release formulations: up to 12-24 hours. Duration may be increased in hepatic impairment. |
150 mg intramuscular injection on day 5 of menstrual cycle, then every 90 days thereafter.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment recommended; pharmacokinetics not significantly altered in renal impairment. |
| Liver impairment | Contraindicated in severe hepatic disease (Child-Pugh class C). For moderate impairment (Child-Pugh class B), use with caution; no specific dose adjustment guidelines available. |
| Pediatric use | Not indicated for use in premenopausal females under 18 years of age; efficacy and safety not established. |
| Geriatric use | Not indicated for use in postmenopausal women; no geriatric-specific dosing available. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for LUNELLE (LUNELLE).
| Breastfeeding | Medroxyprogesterone acetate is excreted into human breast milk in small amounts (M/P ratio approximately 1.0). No adverse effects have been reported in nursing infants. Use during lactation is considered safe, but the lowest effective dose should be used. |
| Teratogenic Risk | LUNELLE (medroxyprogesterone acetate) is contraindicated in pregnancy. First trimester exposure is associated with a potential risk of genital abnormalities in male fetuses (hypospadias) and cardiovascular malformations, though data are limited. Second and third trimester use may cause masculinization of female fetuses due to androgenic activity. Overall, risk is considered low but caution is advised. |
■ FDA Black Box Warning
No FDA boxed warning specific to Lunelle. However, estrogen-containing contraceptives carry increased risk of thromboembolic disorders, especially in smokers over 35.
| Serious Effects |
["Known or suspected pregnancy","Hypersensitivity to medroxyprogesterone acetate or estradiol cypionate","History of thromboembolic disorders (e.g., DVT, PE)","Cerebrovascular or coronary artery disease","Known or suspected breast cancer","Liver tumors or active liver disease","Undiagnosed abnormal uterine bleeding"]
| Precautions | ["Increased risk of thromboembolic disorders, stroke, and myocardial infarction, particularly in smokers over 35.","Regular monitoring of blood pressure, glucose, and lipid profiles recommended.","May decrease glucose tolerance.","Possible menstrual irregularities and amenorrhea.","Bone mineral density loss with prolonged use."] |
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| Fetal Monitoring | Monitor pregnancy status prior to initiation; perform pregnancy test if missed dose. During prolonged use, monitor for bone mineral density loss. No specific fetal monitoring required unless exposure occurs. |
| Fertility Effects | LUNELLE may delay return to fertility by up to 12-18 months due to prolonged suppression of ovulation. No permanent effect on fertility after discontinuation. |