Drug Breakdown: Nabilone

02 December 2024
Volume 6 · Issue 12

Abstract

In this column, Sharon Rees aims to refresh knowledge and interest in some of the commonly used drugs in a series of posts on X. This month she is talking about #nabilone

Day 1: Identification of the psychoactive substance in cannabis (THC) in the 1960s led to analogue development to harness the therapeutic effects. #nabilone was produced in 1980s, but was not available in Europe until mid 2000s. UK use was further delayed until legal changes in 2018

Day 2: An orally active synthetic cannabinoid, #nabilone is licensed in adults for 2nd line nausea & vomiting related to cytotoxic chemotherapy. It is an abusable substance & a Schedule 2 controlled drug. Dosing 1-2mg × 2-3/day during treatment cycle, usually as in-pt. Off-label use as appetite stimulant

Day 3: Good oral absorption/high 1st pass metabolism; cmax 2hrs. Metabolised in liver via direct oxidation (main) & CYP450 reduction. Active metabolite carbinol forms quickly & has extended activity. Major excretion route faeces;25% urine; avoid in severe hepatic impairment. T½ 2-35 hrs

Day 4: Twice as active as tetrahydrocannabinol (THC), #nabilone acts on endogenous cannabinoid system as an agonist at the CB1 receptor in the central nervous system. The mechanism for regulation of the emetic pathway & increased appetite remain unknown

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