Cannabinoids for the Treatment of Neuropathic Pain

Are They Safe and Effective?

Tannia Gutierrez; Andrea G Hohmann


Future Neurology. 2011;6(2):129-133. 

In This Article

Abstract and Introduction


The isolation of Δ9-tetrahydrocannabinol (THC), the major psychoactive ingredient in cannabis, set the stage for the discovery of an endogenous cannabinoid (endocannabinoid) transmitter system.[1] Endogenous signaling molecules for this system were subsequently isolated.[2,3] Anandamide[4] and 2-arachidonoylglycerol (2-AG),[2,3] the best characterized endocannabinoids isolated to date, bind to and activate cannabinoid CB1 and CB2 receptors. CB1 is the primary cannabinoid receptor found in the CNS,[5] whereas CB2 is predominantly, but not exclusively, found in the immune system.[6–8] The discovery of cannabinoid receptors allowed researchers to synthesize cannabinoids and characterize their pain-relieving properties. Anandamide and 2-AG are degraded by the enzymes fatty-acid amide hydrolase and monoacylglycerol lipase,[9] respectively. Enzymes catalyzing endocannabinoid breakdown also represent targets for analgesic drug development. This article will briefly summarize the findings of preclinical and clinical studies evaluating the therapeutic and side-effect profile of cannabinoids as pharmacotherapies for neuropathic pain.


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