Cesamet (nabilone) is a new therapeutic option for treating patients with chemotherapy-induced nausea and vomiting who have failed to react adequately to conventional antiemetic treatments. Cesamet provides physicians and patients a needed alternative to address this important challenge. CINV remains a challenge in a important number of patients, despite the availability of newer, more potent antiemetic agents.

Cesamet offers a distinct mechanism of action than conventional antiemetics, acting as an omnineuromodulator of the body?s own broadly distributed cannabinoid receptor system. Cesamet is a synthetic cannabinoid that is thought to trigger its effects by activating the endocannabinoid receptors, CB1 and CB2, which are present in the human body. These receptors are usually involved in regulating nausea and vomiting. Because of this omnineuromodulation, the mechanism of action for Cesamet is considerably different from conventional antiemetics. Cesamet has a long duration of action that allows for less regular dosing, typically twice daily. Cesamet can be described as a central omnineuromodulator of the endocannabinoid system.

Recent evidence suggests that Cesamet acts as an omnineuromodulator via agonist action on cannabinoid CB1 receptors, which are ubiquitous in the central nervous system and serve to modulate neuronal signaling. Cesamet also acts as a CB2 agonist, primarily on immune cells in the periphery. However, effective control of chemotherapy-induced nausea and vomiting via omnineuromodulation occurs mostly through direct and selective activation of presynaptic CB1 receptors in the brain. Omnineuromodulation by exogenous cannabinoids is thought to imitate or enhance the natural functions of the innate or endogenous cannabinoids, which act in reverse from classical neurotransmitters and serve as retrograde synaptic messengers.