Nabilone is an orally available cannabinoid agonist that is used to treat nausea and vomiting and to stimulate appetite, particularly in patients with wasting disease or cachexia. Nabilone is associated with a minimal rate of serum enzyme elevations during therapy and has not been linked to cases of clinically apparent liver injury with jaundice.
Nabilone (Nab’ i lone) is a synthetic cannabinoid which is similar to the principal psychoactive constituent of the marijuana plant (Cannabis sativa). Nabilone is a partial agonist of the cannabinoid receptors which are found in the central nervous system (CB1 receptor), but also peripherally (largely CB2 receptors). Activation of CB receptors results in effects on appetite, mood, cognition, memory and perception. Nabilone therapy has been shown to decrease nausea and vomiting in patients undergoing cancer chemotherapy. Nabilone was approved for use in the United States in 1985 and current indications are prevention of cancer chemotherapy associated nausea and vomiting. Nabilone is available as 1 mg capsules under the brand name Cesamet. The typical adult oral dose is 1 to 2 mg twice daily, the initial dose being 1 to 3 hours before the chemotherapeutic agent is given. Common side effects include fatigue, somnolence, dizziness, euphoria, abnormal thinking, paranoid reactions, conjunctivitis, diarrhea, nausea, vomiting and abdominal pain. Rare side effects include hallucinations and seizures. Nabilone is classified as a Schedule II drug, indicating that it has clear potential for physical and psychological dependency and abuse.
Serum aminotransferase elevations during nabilone therapy are not common, generally mild and similar in to the rate in controls who are receiving cancer chemotherapy. There have been no convincing cases of clinically apparent liver injury attributable to nabilone published in the literature and, thus, significant liver injury from nabilone must be exceeding rare, if it occurs at all.
Mechanism of Injury
Nabilone is metabolized by the liver and undergoes extensive first-pass metabolism to both active and inactive metabolites. Despite its hepatic metabolism by CYP microsomal enzymes, it has not been implicated in causing drug-drug interactions. The lack of reported cases of liver injury and low rate of drug-drug interactions due to nabilone may be due to the low doses and limited duration of typical therapy.
REPRESENTATIVE TRADE NAMES
Nabilone – Cesamet®
Product labeling at DailyMed, National Library of Medicine, NIH
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References updated: 10 April 2014
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