LERIBANE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LERIBANE (LERIBANE).
Leribane is a synthetic cannabinoid receptor agonist with high affinity for CB1 and CB2 receptors. It inhibits adenylate cyclase activity via Gi/o protein coupling, leading to decreased cAMP accumulation, modulation of ion channels, and inhibition of neurotransmitter release.
| Metabolism | Primarily hepatic via CYP3A4 and CYP2C9 isoenzymes; undergoes hydroxylation and glucuronidation; minor contribution from CYP2D6. |
| Excretion | Renal: 70% unchanged; biliary/fecal: 30% as metabolites |
| Half-life | 24 hours (range 20-30 h); accumulates to steady state in ~5 days, requires dose adjustment in renal impairment |
| Protein binding | 98% bound to albumin and alpha-1-acid glycoprotein |
| Volume of Distribution | 8-12 L/kg; indicates extensive tissue distribution |
| Bioavailability | Oral: 60-70% (first-pass metabolism); Intravenous: 100% |
| Onset of Action | Oral: 2-4 hours; Intravenous: within 30 minutes |
| Duration of Action | 24-36 hours; clinical effect may persist beyond half-life due to tissue binding |
5-10 mg orally twice daily; maximum 30 mg/day.
| Dosage form | TABLET |
| Renal impairment | GFR 30-59 mL/min: 5 mg twice daily; GFR 15-29 mL/min: 5 mg once daily; GFR <15 mL/min: not recommended. |
| Liver impairment | Child-Pugh A: 5 mg twice daily; Child-Pugh B: 5 mg once daily; Child-Pugh C: contraindicated. |
| Pediatric use | Not approved for use in pediatric patients; safety and efficacy not established. |
| Geriatric use | Initiate at 5 mg once daily; titrate cautiously due to increased risk of adverse effects; maximum 15 mg/day. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for LERIBANE (LERIBANE).
| Breastfeeding | No data available on excretion into breast milk. Potential for adverse effects in nursing infant. M/P ratio unknown. Not recommended during breastfeeding. |
| Teratogenic Risk | First trimester: Risk of congenital malformations based on animal studies, including neural tube defects and cardiac anomalies. Second and third trimesters: Risk of fetal growth restriction and oligohydramnios due to possible uteroplacental insufficiency. Avoid in pregnancy unless benefit outweighs risk. |
| Fetal Monitoring |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to leribane or any cannabinoid; history of psychotic disorder; severe hepatic impairment (Child-Pugh class C); concomitant use with disulfiram or metronidazole (possible disulfiram-like reaction); pregnancy and lactation (insufficient safety data).
| Precautions | Central nervous system depression (may impair cognition and motor skills); risk of psychiatric adverse effects (anxiety, paranoia, psychosis); potential for dependence and withdrawal; serotonin syndrome when combined with serotonergic drugs; hepatotoxicity at high doses; cardiovascular effects (tachycardia, hypertension). |
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| Monitor maternal blood pressure, liver function, and renal function regularly. Fetal ultrasound for growth and amniotic fluid volume every 4 weeks. Nonstress test weekly after 32 weeks. |
| Fertility Effects | No specific data on fertility impairment observed in animal studies. However, may affect reproductive function in women of childbearing potential; advise contraception during therapy. |