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Nabilone

Last updated on October 6, 2021

NabiloneDrug Approvals

(British Approved Name, US Adopted Name, rINN)

Synonyms: Compound 109514; Lilly-109514; Nabilon; Nabilona; Nabiloni; Nabilonum
BAN: Nabilone
USAN: Nabilone
INN: Nabilone [rINN (en)]
INN: Nabilona [rINN (es)]
INN: Nabilone [rINN (fr)]
INN: Nabilonum [rINN (la)]
INN: Набилон [rINN (ru)]
Chemical name: (±)-(6aR,10aR)-3-(1,1-Dimethylheptyl)-6a,7,8,9,10,10a-hexahydro-1-hydroxy-6,6-dimethyl-6H-benzo[c]chromen-9-one
Molecular formula: C24H36O3 =372.5
CAS: 51022-71-0
ATC code: A04AD11
Read code: y0288

Adverse Effects

Nabilone may produce adverse effects similar to those of cannabis. The most common adverse effects are drowsiness, vertigo, and dry mouth. Neurological effects have included ataxia, confusion, disorientation, dizziness, euphoria, dysphoria, hallucinations, psychosis, depression, headache, decreased concentration, blurred vision, sleep disturbances, decreased coordination, and tremors. Adverse cardiovascular reactions including hypotension, orthostatic hypotension, and tachycardia have occurred. Gastrointestinal disturbances, decreased appetite, and abdominal pain have also been reported.

Precautions

Nabilone is extensively metabolised and largely excreted in bile, and therefore is not recommended in patients with severe hepatic impairment. It should be used with caution in patients with a history of psychiatric disorders or depression, or those with hypertension or heart disease.

Because of the possibility of CNS depression, patients should be warned not to drive or operate machinery.

The possibility of dependence similar to that of cannabis should be borne in mind.

Interactions

Nabilone has been shown to have an additive CNS depressant effect when given with alcohol, codeine, diazepam, or other CNS depressants.

Pharmacokinetics

Nabilone is well absorbed from the gastrointestinal tract and is rapidly and extensively metabolised one or more of the metabolites may be active. The major excretory pathway is the biliary system about 65% of a dose is excreted in the faeces and about 20% in the urine. The elimination half-life of nabilone is about 2 hours, but the half-life of its combined metabolites is about 35 hours after an oral dose.

Uses and Administration

Nabilone, a synthetic cannabinoid with antiemetic properties, is used for the control of nausea and vomiting associated with cancer chemotherapy in patients who have failed to respond adequately to conventional antiemetics.

The usual initial oral dose for adults is 1 mg twice daily, increased to 2 mg twice daily if necessary. The first dose should be given the evening before starting chemotherapy, and the second dose 1 to 3 hours before the first dose of antineoplastic. Nabilone may be given throughout each cycle of chemotherapy and for 48 hours after the last dose of chemotherapy, if required. The dose of nabilone should not exceed 6 mg daily, given in 3 divided dos-

Multiple sclerosis

There is a report of reduction in spasticity and nocturia, and improvement in mood and well-being, in a patient with multiple sclerosis who received nabilone 1 mg every second day. A subsequent small crossover study in patients with chronic upper motor neurone syndrome found that oral nabilone 1 mg daily reduced spasticity-related pain in this group. There are also anecdotal reports of improvement in symptoms in patients with multiple sclerosis who took cannabis, however, a review considered evidence of effectiveness to be lacking.

Proprietary Preparations

Argentina: Cesamet

Canada: Cesamet

Ireland: Cesamet

USA: Cesamet.

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