Nabilone

Medical uses

Nabilone is used to treat nausea and vomiting in people under chemotherapy.

Nabilone has shown modest effectiveness in relieving fibromyalgia. A 2011 systematic review of cannabinoids for chronic pain determined there was evidence of safety and modest efficacy for some conditions.

The main settings that have seen published clinical trials of nabilone include movement disorders such as parkinsonism, chronic pain, dystonia and spasticity neurological disorders, multiple sclerosis, and the nausea of cancer chemotherapy. Nabilone is also effective in the treatment of inflammatory bowel disease, especially ulcerative colitis.

In one study of current daily users of cannabis, oral nabilone at 4, 6, and 8 mg produced sustained and dose-dependent mood elevation and psychomotor slowing comparable to 10 or 20 mg oral dronabinol (THC). Nabilone had a slower onset of peak action and a greater dose-dependence of effects, which the investigators attributed to greater bioavailability.

A study comparing nabilone with metoclopramide, conducted before the development of modern 5-HT3 antagonist anti-emetics such as ondansetron, revealed that patients taking cisplatin chemotherapy preferred metoclopramide, while patients taking carboplatin preferred nabilone to control nausea and vomiting.

Nabilone is sometimes used for nightmares in post-traumatic stress disorder, but there have not been studies longer than nine weeks, so effects of longer-term use are not known. Nabilone has also been used for medication overuse headache.

Side effects

In the treatment of fibromyalgia, adverse effects limit the useful dose. Adverse effects of nabilone include, but are not limited to: dizziness/vertigo, euphoria, drowsiness, dry mouth, ataxia, sleep disturbance, headache, nausea, disorientation, depersonalization, hallucinations, and asthenia.

Pharmacology

Pharmacodynamics

Nabilone is a partial agonist of the cannabinoid CB1 and CB2 receptors. Nabilone binds with both higher affinity and greater efficacy than THC.

Pharmacokinetics

Nabilone is given in 1 or 2 mg doses multiple times a day up to a total of 6 mg. It is completely absorbed from oral administration and highly plasma protein bound. Multiple cytochrome P450 enzymes extensively metabolize nabilone to various metabolites that have not been fully characterized.

Chemistry

Nabilone is a racemic mixture consisting of (S,S)-(+)- and (R,R)-(−)-isomers.

History

Nabilone was originally developed by Eli Lilly and Company; and was first approved by Health Canada in 1981; shortly followed by its approval in Mexico, the United Kingdom, and Germany. Lilly received FDA approval in 1985 to market it, but withdrew that approval in 1989 for commercial reasons. Valeant Pharmaceuticals acquired the rights from Lilly in 2004. and then succeeded in 2006.

In 2007, Valeant acquired the United Kingdom and European Union rights to market nabilone from Cambridge Laboratories.

Nabilone was approved in Austria to treat chemotherapy-induced nausea in 2013; it was already approved in Spain for the same indication and was legal in Belgium to treat glaucoma, spasticity in multiple sclerosis, wasting due to AIDS, and chronic pain.

References

References

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9. (September 2013). "Subjective, cognitive and cardiovascular dose-effect profile of nabilone and dronabinol in marijuana smokers". Addiction Biology.
10. (April 1988). "A randomized trial of oral nabilone and prochlorperazine compared to intravenous metoclopramide and dexamethasone in the treatment of nausea and vomiting induced by chemotherapy regimens containing cisplatin or cisplatin analogues". European Journal of Cancer & Clinical Oncology.
11. (November 2015). "Cannabinoids for nausea and vomiting in adults with cancer receiving chemotherapy". The Cochrane Database of Systematic Reviews.
12. (July 2025). ["Long-term Nabilone Use: A Review of the Clinical Effectiveness and Safety"](https://www.ncbi.nlm.nih.gov/pubmedhealth/PMH0079568/ }}{{dead link). CADTH Rapid Response Reports.
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16. (2017-01-01). "The Synthetic Analog of Δ9-Tetrahydrocannabinol (THC): Nabilone. Pharmacology and Clinical Application". Academic Press.
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