Nabilone

Pronunciation

(NA bi lone)

Generic Available

No

Use

Treatment of nausea and vomiting associated with cancer chemotherapy

Restrictions

C-II

Pregnancy Risk Factor

C

Lactation

Excretion in breast milk unknown

Contraindications

Hypersensitivity to nabilone, cannabinoids, tetrahydrocannabinol, or any component of the formulation

Warnings/Precautions

Use with caution in the elderly, those with pre-existing CNS depression, or a history of mental illness.

Adverse Reactions

>10%:

Cardiovascular: Orthostatic hypotension (5% to 42%)

Central nervous system: Dizziness (36%), drowsiness (47% to 65%), vertigo (65%), euphoria (27%), clumsiness

Gastrointestinal: Dry mouth (29%)

1% to 10%:

Central nervous system: Ataxia, depression

Ocular: Blurred vision (13%)

<1%: Changes of mood, confusion, dyspnea, hallucinations, headache, loss of appetite

Overdosage/Toxicology

Symptoms of overdose include nausea, vomiting, disorientation, CNS, respiratory depression, dysphoria, and euphoria. Treatment is supportive and symptomatic.

Drug Interactions

Increased toxicity: CNS depression is potentiated with ethanol and other CNS depressants.

Stability

Store capsules at room temperature.

Mechanism of Action

Unknown; animal studies suggest some activity may involve the chemoreceptor trigger zone.

Pharmacodynamics/Kinetics

Absorption: Rapid

Bioavailability: 95.8%

Distribution: Rapid and extensive to various tissues

Metabolism: To several active metabolites by oxidation and stereospecific reduction

Half-life elimination: Parent compound: 2 hours; Metabolites: 35 hours

Time to peak, serum: Within 2 hours

Excretion: Feces (65%); renal (20%)

Dosage

Refer to individual protocols. Oral:

Children >4 years:

<18 kg: 0.5 mg twice daily

18-30 kg: 1 mg twice daily

>30 kg: 1 mg 3 times/day

Adults: 1-2 mg twice daily (maximum: 6 mg divided in 3 doses daily)

Administration

Oral; I.V. use is reported, but a parenteral formulation is not available in the U.S.

Oncology: Emetic Potential

Very low (<10%)

Dosage Forms

Capsule: 1 mg

References

Ward A and Holmes B, "Nabilone: A Preliminary Review of Its Pharmacological Properties and Therapeutic Use,"Drugs, 1985, 30(2):127-44.

International Brand Names

Cesamet® (IE); Nabilone® (GB)