CESAMET
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CESAMET (CESAMET).
Nabilone is a synthetic cannabinoid (CB1 receptor agonist) with antiemetic and anxiolytic effects. It binds to central cannabinoid receptors (CB1) in the brain, inhibiting neurotransmitter release and modulating emetic pathways.
| Metabolism | Hepatic, primarily via CYP3A4 and CYP2C9; undergoes first-pass metabolism; multiple metabolites including active 11-hydroxy-nabilone |
| Excretion | Primarily hepatic metabolism with biliary excretion. ~65% eliminated in feces as metabolites, ~20% in urine. Less than 1% excreted unchanged. |
| Half-life | Terminal elimination half-life is approximately 35 hours (range 25–50 hours) in adults. Due to prolonged half-life and active metabolites, steady-state may take 5–7 days; accumulation occurs with repeated dosing. |
| Protein binding | 90–95% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Approximately 2.5–5.5 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Oral bioavailability is approximately 10–20% due to extensive first-pass metabolism. |
| Onset of Action | Oral administration: clinical effect (antiemetic) typically observed within 1–3 hours. |
| Duration of Action | Duration of antiemetic effect is approximately 8–12 hours after a single oral dose. However, due to long half-life, effects may persist longer with repeated dosing. |
1-2 mg orally twice daily; maximum 6 mg/day.
| Dosage form | CAPSULE |
| Renal impairment | No specific dosage adjustment recommended based on GFR; use with caution in severe renal impairment. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: avoid use. |
| Pediatric use | Not approved for use in pediatric patients; safety and efficacy not established. |
| Geriatric use | Start at 1 mg once daily; titrate slowly due to increased sensitivity to adverse effects. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CESAMET (CESAMET).
| Breastfeeding | Nabilone is excreted into breast milk; a specific M/P ratio is not reported. Due to the high lipid solubility and long half-life, significant infant exposure is expected. Breastfeeding is contraindicated due to potential adverse effects on infant neurodevelopment and cannabinoid receptor activation. |
| Teratogenic Risk | Nabilone (Cesamet) is classified as FDA Pregnancy Category C. Animal studies have shown teratogenic effects including skeletal anomalies at doses 0.2-2 times the maximum recommended human dose. There are no adequate and well-controlled studies in pregnant women. First trimester exposure may increase risk of congenital malformations. Second and third trimester exposure may affect fetal growth and neurobehavioral development. Potential risks include low birth weight, preterm birth, and neonatal withdrawal symptoms. |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to nabilone or any cannabinoid","History of seizure disorder","Breastfeeding (excreted in milk)"]
| Precautions | ["Central nervous system depression (drowsiness, dizziness, ataxia)","Psychiatric effects (euphoria, dysphoria, paranoia, hallucinations)","Cognitive and motor impairment (do not drive or operate machinery)","Risk of dependence and withdrawal syndrome","Use with caution in patients with history of psychiatric disorders","May increase heart rate and blood pressure"] |
| Food/Dietary | Take with food or milk to reduce gastrointestinal upset; avoid grapefruit juice as it may alter drug metabolism. |
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| Fetal Monitoring | Monitor maternal vital signs, mental status, and for signs of cannabinoid toxicity (e.g., dizziness, sedation, hypotension). Fetal monitoring should include serial ultrasound for growth assessment and nonstress testing in the third trimester. Monitor neonate for withdrawal symptoms (irritability, jitteriness, poor feeding) and respiratory depression. |
| Fertility Effects | Nabilone may impair fertility in males and females. Animal studies show reduced spermatogenesis and altered estrous cycles. In humans, chronic cannabinoid use is associated with decreased gonadotropin levels, anovulation, reduced sperm count and motility, and menstrual irregularities. |
| Clinical Pearls |
| Titrate slowly to reduce risk of syncope and orthostatic hypotension; monitor for dizziness and sedation; may cause euphoria or dysphoria; use with caution in patients with history of psychiatric disorders; taper to discontinue. |
| Patient Advice | Avoid driving or operating machinery until you know how this drug affects you. · Get up slowly from sitting or lying down to prevent dizziness or fainting. · Avoid alcohol and other sedatives while taking this medication. · Take exactly as prescribed; do not increase dose without consulting your doctor. · Store at room temperature away from moisture and heat. |