Drug intelligence / Profile preview

nabiximols + rifampicin

Development stage
Unknown
Lead developer
Jazz Pharmaceuticals
Modality
Small Molecules
Administration
Oromucosal, Oral, Intravenous
01

Overview

Nabiximols (marketed as Sativex) is an oromucosal spray containing a standardized 1:1 ratio of delta-9-tetrahydrocannabinol (THC) and cannabidiol (CBD), derived from Cannabis sativa extracts. It acts primarily as a partial agonist at cannabinoid receptors CB1 and CB2. THC is responsible for most of the pharmacological effects via these receptors in the central nervous system and immune cells, while CBD has little activity at cannabinoid receptors but may have neuroprotective properties[5][2]. Nabiximols is indicated for symptom improvement in patients with moderate to severe spasticity due to multiple sclerosis who have not responded adequately to other anti-spasticity medications[6][5]. Rifampicin is a potent inducer of cytochrome P450 enzymes (notably CYP3A4), which can significantly reduce plasma concentrations of both THC and CBD when co-administered with nabiximols[10]. This combination should generally be avoided unless necessary; if used together, careful titration and monitoring are required due to reduced efficacy of nabiximols.

Brand names
SativexRifadinRimactane
Other names
delta-9-tetrahydrocannabinol and cannabidiol oromucosal spray + rifampicin
02

Targets

rpoB (DNA-directed RNA polymerase subunit beta)CNR1 (Cannabinoid receptor 1)

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