Patients dealing with cancer are often on many complicated drug regimens. Cesamet (nabilone) is a synthetic cannabinoid for the treatment of the nausea and vomiting associated with cancer chemotherapy in patients who have failed to respond adequately to conventional antiemetic treatments.¹ Cesamet offers a unique pharmacokinetic profile.

Overview of Available Cannabinoids^1-5

Binding Affinity to Cannabinoid (CB) Receptors⁶

Cannabinoids: CPY450 Activity⁷

• Cesamet is metabolized principally through the cytochrome P450 (CYP450) 2C9 isoenzyme
• Cesamet has no significant inhibitory or inducing effect on any of these isoenzymes
• Cesamet competes with very few medications at the metabolic level (please see accompanying full prescribing information)

*Main metabolizing isoenzyme

Important Safety Information¹

Cesamet, a synthetic cannabinoid similar to the active ingredient found in naturally occurring Cannabis sativa L. [Marijuana; delta-9-tetrahydrocannabinol (delta-9-THC)], is contraindicated in any patient who has a history of hypersensitivity to any cannabinoid. Patients receiving treatment with Cesamet should be specifically warned not to drive, operate machinery, or engage in any hazardous activity while receiving Cesamet.  During controlled clinical trials of Cesamet, virtually all patients experienced at least one adverse reaction. The most commonly encountered events were drowsiness, vertigo, dry mouth, euphoria (feeling “high”), ataxia, headache, and concentration difficulties. Cesamet should not be taken with alcohol, sedatives, hypnotics, or other psychoactive substances because these substances can potentiate the central nervous system (CNS) effects of nabilone. Since Cesamet can elevate supine and standing heart rates and cause postural hypotension, it should be used with caution in the elderly, and in patients with hypertension or heart disease. Cesamet should also be used with caution in patients with current or previous psychiatric disorders, (including manic depressive illness, depression, and schizophrenia) as the symptoms of these disease states may be unmasked by the use of cannabinoids. Cesamet should be used with caution in individuals receiving concomitant therapy with sedatives, hypnotics, or other psychoactive drugs because of the potential for additive or synergistic CNS effects. Cesamet should be used with caution in patients with a history of substance abuse, including alcohol abuse or dependence and marijuana use, since Cesamet contains a similar active compound to marijuana. Cesamet should be used with caution in pregnant patients, nursing mothers, or pediatric patients because it has not been studied in these patient populations.

For complete prescribing details, please see full prescribing information. Click here to download.

References

1. Cesamet™ [package insert]. Valeant Pharmaceuticals International; 2006.
2. Data on File: Protocols 9, 20 and 28. Valeant Pharmaceuticals International.
3. Lemberger L, Rowe H. Clinical pharmacology of nabilone, a cannabinoid derivative. Clin Pharmacol Ther. 1975;18(6):720-726.
4. Einhorn LH, Nagy C, Furnas B, et al. Nabilone: An effective antiemetic in patients receiving cancer chemotherapy. J Clin Pharmacol. 1981;21(suppl):64-69.
5. MARINOL^® [package insert]. Solvay Pharmaceuticals, Inc; 2003.
6. Kalant H. Medicinal use of cannabis: history and current status. Pain Res Manag. 2001;6(2):80-91.
7. Turgeon J, Bartolucci G. Cannabinoids in the treatment of chronic pain. Continuing Education in Neurology & Psychiatry.2003;2(2):1-8.