Drug intelligence / Profile preview

nabiximols + fluconazole

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

Overview

Nabiximols + fluconazole refers to the co-administration of **nabiximols** (a standardized *Cannabis sativa* extract containing a near 1:1 ratio of tetrahydrocannabinol (THC) and cannabidiol (CBD)) with **fluconazole** (a triazole antifungal agent and potent inhibitor of CYP2C9/3A4). Nabiximols, typically marketed as Sativex, is delivered as an oromucosal spray and is indicated for symptomatic relief of spasticity in multiple sclerosis, neuropathic pain, and advanced cancer pain. Nabiximols acts primarily via the **cannabinoid receptors CB1 and CB2**, modulating pain and neuroinflammatory processes. Fluconazole, in this context, is of interest because it inhibits the metabolism of THC and CBD by blocking key cytochrome P450 enzymes, leading to **increased plasma concentrations** of nabiximols' active components and their metabolites. This combination may increase the efficacy and/or toxicity of nabiximols due to elevated exposure, and should be used with caution.

Brand names
SativexDiflucan
Other names
nabiximolsdelta-9-tetrahydrocannabinol and cannabidiol oromucosal spraydelta9-tetrahydrocannabinol and cannabidiol oromucosal spraydelta 9-tetrahydrocannabinol and cannabidiol oromucosal sprayTHC/CBD oromucosal sprayfluconazole
02

Targets

CNR1 (Cannabinoid receptor 1)CYP2C9 (Cytochrome P450 family 2 subfamily C member 9)CYP51A1 (Sterol 14α-demethylase)CYP3A4 (Cytochrome P450 3A4)

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