|Trade names||Cesamet, Canemes|
|Drug class||Synthetic cannabinoid|
|Main uses||Chemotherapy-induced nausea and vomiting|
|Side effects||Sleepiness, dry mouth, dizziness, feeling high, poor coordination, headache|
|By mouth (capsules)|
|Typical dose||1 to 2 mg BID|
|Bioavailability||20% after first-pass by the liver|
|Protein binding||similar to THC (±97%)|
|Elimination half-life||2 hours, with metabolites around 35 hours|
|Chemical and physical data|
|Molar mass||372.549 g·mol−1|
|3D model (JSmol)|
Nabilone, sold under the brand name Cesamet among others, is a medication used for chemotherapy-induced nausea and vomiting. Some evidence supports modest effectiveness for fibromyalgia and multiple sclerosis. It is taken by mouth.
Common side effects include sleepiness, dry mouth, dizziness, feeling high, poor coordination, and headache. Other side effects may include fast heart rate, abuse, and psychosis. Safety in pregnancy is unclear. It is a synthetic cannabinoid which effects similar to tetrahydrocannabinol (THC), the primary psychoactive compound found in Cannabis.
Nabilone was approved for medical use in the United States in 1985. In the United Kingdom 20 pills of 1 mg costs the NHS about £200 as of 2021. This amount in the United States costs about 820 USD. In the United States it is a schedule II controlled substance.
Nabilone has shown modest effectiveness in relieving fibromyalgia. A 2011 review of cannabinoids for chronic pain determined there was evidence of safety and modest efficacy for some conditions.
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.
It is started at 1 mg twice per day and may be increased to 2 mg twice per day.
Nabilone can increase – rather than decrease – postoperative pain. In the treatment of fibromyalgia, adverse effects limit the useful dose. Side effects of nabilone include, but are not limited to: dizziness/vertigo, euphoria, drowsiness, dry mouth, ataxia, sleep disturbance, dysphoria, headache, nausea, disorientation, depersonalization, and asthenia.
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.
Nabilone was originally developed by Eli Lilly and Company; 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. Valeant tried and failed to get the medication approved in 2005 and then succeeded in 2006.
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.
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