Nabilone

Nabilone, sold under the brand name Cesamet among others, is a synthetic cannabinoid with therapeutic use as an antiemetic and as an adjunct analgesic for neuropathic pain. It mimics tetrahydrocannabinol (THC), the primary psychoactive compound found naturally occurring in Cannabis. The Food and Drug Administration in the United States has indicated nabilone for chemotherapy-induced nausea/vomiting. In other countries, such as Canada, it is widely used as an adjunct therapy for chronic pain management. Numerous trials and case studies have demonstrated modest effectiveness for relieving fibromyalgia and multiple sclerosis.

Medical Uses of Nabilone:

• Treats nausea and vomiting in chemotherapy patients.
• Shows effectiveness in relieving fibromyalgia.
• Clinical trials indicate safety and modest efficacy for chronic pain.
• Effective in treating inflammatory bowel disease, especially ulcerative colitis.
• Published trials cover movement disorders, chronic pain, multiple sclerosis, and cancer chemotherapy nausea.
• Appetite stimulation in AIDS-related anorexia.
• Pain management in fibromyalgia.
• Sleep improvement in PTSD patients.
• Anxiety reduction in patients with anxiety disorders.

Pharmacology of Nabilone:

• Acts as a partial agonist on cannabinoid CB receptors.
• Synthetic cannabinoid similar to THC.
• Given in 1-2mg doses multiple times daily, up to 6mg total.
• Metabolized in the liver.
• Half-life of around 2 hours.
• Potential for drug interactions with CYP3A4 inhibitors.

Side Effects of Nabilone:

• Can increase postoperative pain.
• Adverse effects limit the useful dose in fibromyalgia treatment.
• Include dizziness, euphoria, dry mouth, sleep disturbance, and hallucinations.
• Dizziness and drowsiness.
• Dry mouth and eyes.
• Impaired coordination.
• Euphoria or dysphoria.
• Increased heart rate.

Legal Status and History of Nabilone:

• Schedule II controlled substance in the U.S.
• Approved for medical use in Canada and Europe.
• Restricted availability in some countries.
• Not classified as a narcotic.
• Potential for abuse and dependence.
• Developed by Eli Lilly and approved by Health Canada in 1981.
• Initially withdrawn by Lilly in 1989 but later approved by the FDA in 2006.
• Valeant Pharmaceuticals acquired rights from Lilly in 2004.
• Approved in Austria for chemotherapy-induced nausea in 2013.
• Legal in Belgium for various conditions like glaucoma and chronic pain.

Research and Development of Nabilone:

• Studies on its efficacy in various conditions ongoing.
• Investigated for use in neuropathic pain.
• Potential as an antiemetic in different patient populations.
• Formulation improvements for better bioavailability.
• Exploration of novel delivery methods, such as patches or sprays.

Nabilone Data Sources