Drug reference

Nabilone

Cannabinoid · Antiemetic

Also known as CESAMET

CannabinoidAntiemeticATC A04AD11

CDSCO approvedSchedule XATC A04AD11

EXCRETION

—

not curated

INTERACTIONS

4 major

SEVERE in our sources

PREGNANCY

Avoid unless essential.

FDA category + note

Top interactionssee all 12 →

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Mechanism

Nabilone is a synthetic cannabinoid with a mode of action similar to that of dronabinol. It exerts complex effects on the central nervous system, including a prominent central sympathomimetic activity.

Indications

Nausea and vomiting caused by cytotoxic chemotherapy, unresponsive to conventional antiemetics (preferably in hospital setting, under close medical supervision)Add-on treatment for chemotherapy-induced nausea and vomiting unresponsive to optimised conventional antiemeticschemotherapy-induced nausea and vomiting in patients who have not responded to conventional antiemeticsCannabis use disorder (under investigation as substitution therapy)Prophylactic agent in patients receiving cancer chemotherapy (when other antiemetic medications are not effective)Cancer chemotherapy induced vomitingantiemetic

Dosing

Adult: BY MOUTH: Initially 1 mg twice daily, increased if necessary to 2 mg twice daily throughout each cycle of cytotoxic therapy and, if necessary, for 48 hours after the last dose of each cycle. The first dose should be taken the night before initiation of cytotoxic treatment and the second dose 1–3 hours before the first dose of cytotoxic drug. Daily dose maximum should be given in 3 divided doses.
Pediatric: Nabilone is not approved for pediatric use.
Hepatic adjustment: Avoid in severe impairment (primarily biliary excretion).
Max dose: 6 mg per day

Pharmacokinetics

Onset

Within an hour

Peak effect

Within 2 hours

Half-life

~2 hours for the parent compound and 35 hours for metabolites

Bioavailability

high absorption from the gut (~96% absorption into bloodstream)

Metabolism

subject to high first-pass metabolism. Pharmacokinetics remain relatively linear over a dose range of 1 to 4 mg. Metabolism is primarily hepatic and likely involves several CYPs and hydroxylation sites on the dimethyl-heptyl side chain and formation of carboxylic analogues, similar to THC.…

Excretion

Metabolites are excreted primarily via the biliary-fecal route (60%), with approximately 25% excreted in the urine.

Contraindications

Severe hepatic impairment
Elderly patients (caution advised)
Heart disease (caution advised)
History of psychiatric disorder (caution advised)
Hypertension (caution advised)
History of substance abuse (caution advised)

Side effects

Common

Abdominal painAppetite decreasedConcentration impairedConfusionDepressionDizzinessDrowsinessDrug use disordersDry mouthEuphoric moodFeeling of relaxationHallucinationHeadacheHypotensionMovement disordersNauseaPsychosisSleep disorderTachycardiaTremorVertigoVisual impairmentincreased anxietynervousnesspanicsedationimpairments in normative cognitive function (particularly at doses ≥5 mg)mild tachycardiapostural hypotension (at doses of 2.5 to 5 mg and above)Significant CNS actions (in more than 10% of patients)Cardiovascular effectsGI effectsHallucinogenic effectsPsychomotor effects

Serious

Adverse effects on mental state can persist for 48–72 hours after stopping
Paranoid reactions
Thinking abnormalities
Abstinence syndrome (irritability, insomnia, and restlessness) upon abrupt withdrawal
hallucinations
delusions