Nabilone (United States: Not available): Drug information

For additional information see "Nabilone (United States: Not available): Patient drug information" and "Nabilone (United States: Not available): Pediatric drug information"

For abbreviations, symbols, and age group definitions show table

Brand Names: Canada

ACT Nabilone [DSC];
Cesamet;
PMS-Nabilone;
RAN-Nabilone [DSC];
TEVA-Nabilone

Pharmacologic Category

Antiemetic

Dosing: Adult

Chemotherapy-induced nausea and vomiting

Chemotherapy-induced nausea and vomiting (severe): Note: Nabilone may be offered for refractory or breakthrough nausea and vomiting (which occurs despite optimal prophylaxis) in patients who have already received a trial of olanzapine (Ref).

Oral: Initial: 1 to 2 mg twice daily; begin with the lower dose in the range and adjust dose based on response and/or tolerance; begin the evening prior to chemotherapy, then administer the second dose 1 to 3 hours before chemotherapy; continue for up to 24 hours after the last chemotherapy dose. Maximum: 6 mg/day divided in 3 doses.

Dosing: Kidney Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).

Dosing: Liver Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling (has not been studied); use with extreme caution in patients with severe impairment.

Dosing: Older Adult

Refer to adult dosing. Use the lower end of the dosing range (to minimize adverse events).

Dosing: Pediatric

(For additional information see "Nabilone (United States: Not available): Pediatric drug information")

Dosage guidance:

Dosage form information: Product only available in Canada.

Chemotherapy-induced nausea and vomiting, prevention

Chemotherapy-induced nausea and vomiting (CINV), prevention: Note: Nabilone is not recommended for prevention of CINV in the most current clinical practice guidelines due to lack of proven efficacy and safety (Ref); poor symptom control was also reported in a retrospective review of pediatric patients (n=110; median age: 14 years [range: 1.1 to 18 years]) receiving prophylaxis for acute CINV where 52.3% of patients achieved complete control; rate is similar to that reported previously with 5HT3 monotherapy (Ref):

Children ≥3 years and Adolescents: Very limited data available, efficacy results variable (Ref): Oral:

<18 kg: 0.5 mg twice daily.

18 to 30 kg: 1 mg twice daily.

>30 kg: 1 mg 3 times daily.

Dosing: Kidney Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).

Dosing: Liver Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

>10%:

Gastrointestinal: Xerostomia (22%)

Nervous system: Abnormal sensory symptoms (12%), ataxia (13%), depression (14%), drowsiness (66%), mood elevation (psychological high: 39%), vertigo (59%)

Ophthalmic: Blurred vision (13%)

1% to 10%:

Cardiovascular: Orthostatic hypotension (5%)

Gastrointestinal: Anorexia (8%)

Nervous system: Asthenia (8%), euphoria (4%), hallucination (2%), headache (7%)

<1%:

Cardiovascular: Syncope, tachycardia

Nervous system: Altered time perception, confusion, dissociative reaction, dysphoria, nightmares, psychotic reaction, seizure, tremor

Postmarketing:

Cardiovascular: Chest pain, hypotension

Gastrointestinal: Constipation, nausea, oral paresthesia, vomiting

Hematologic & oncologic: Leukopenia

Hypersensitivity: Facial edema

Nervous system: Anxiety, ataxia, central nervous system depression, central nervous system stimulation, changes in thinking, depersonalization, dizziness, emotional lability, insomnia, psychosis, stupor

Ophthalmic: Visual disturbance

Contraindications

Hypersensitivity to nabilone, marijuana, other cannabinoids, or any component of the formulation; history of psychotic reactions.

Warnings/Precautions

Concerns related to adverse effects:

• Cardiovascular effects: May cause tachycardia and/or orthostatic hypotension; use with caution in patients with cardiovascular disease.

• CNS effects: May impair physical or mental abilities; patients must be cautioned about performing tasks that require mental alertness (eg, operating machinery, driving). Dizziness, drowsiness, ataxia, depression, hallucinations, and psychosis have been reported; psychiatric adverse reactions may persist for up to 3 days after discontinuing treatment. Use with extreme caution in persons with a history of nonpsychotic emotional disorders.

Disease-related concerns:

• Hepatic impairment: Use with extreme caution in patients with severe liver impairment.

Concurrent drug therapy issues:

• CNS depressants: Effects may be potentiated when used with other psychoactive drugs, sedatives, hypnotics, and/or ethanol.

Special populations:

• Older adult: Use with caution in older adult patients; may cause postural hypotension and elevate heart rate (standing and supine).

Product Availability

Not available in the United States.

Pricing: US

Capsules (Cesamet Oral)

1 mg (per each): $47.04

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Dosage Forms: Canada

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Capsule, Oral:

Cesamet: 0.25 mg [contains fd&c blue #1 (brilliant blue), fd&c red #40 (allura red ac dye), quinoline yellow (d&c yellow #10)]

Cesamet: 0.5 mg [contains fd&c red #40 (allura red ac dye), quinoline yellow (d&c yellow #10)]

Cesamet: 1 mg [contains fd&c blue #2 (indigotine,indigo carmine)]

Generic: 0.25 mg, 0.5 mg, 1 mg

Controlled Substance

CDSA II

Administration: Adult

Oral: The initial dose should be administered the night before chemotherapy and the second dose should be administered 1 to 3 hours before chemotherapy.

Administration: Pediatric

Oral: In pediatric trials, initial dose given 8 to 12 hours prior to chemotherapy, followed by scheduled dosing 2 or 3 times daily (based on weight) (Ref). One small study (n=22; ages: 8 months to 17 years) described opening capsules and dividing the powder if necessary to obtain the correct dose (Ref).

Use: Labeled Indications

Note: Not approved in the United States.

Chemotherapy-associated nausea and vomiting, severe: Treatment of severe nausea and vomiting associated with cancer chemotherapy in patients ≥18 years of age.

Metabolism/Transport Effects

None known.

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.

Agents with Clinically Relevant Anticholinergic Effects: May increase tachycardic effects of Cannabinoid-Containing Products. Risk C: Monitor

Alcohol (Ethyl): Nabilone may increase CNS depressant effects of Alcohol (Ethyl). Risk X: Avoid

Alfuzosin: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Alizapride: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Amifostine: Blood Pressure Lowering Agents may increase hypotensive effects of Amifostine. Management: When used at chemotherapy doses, hold blood pressure lowering medications for 24 hours before amifostine administration. If blood pressure lowering therapy cannot be held, do not administer amifostine. Use caution with radiotherapy doses of amifostine. Risk D: Consider Therapy Modification

Amisulpride (Oral): May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Amisulpride (Oral): May increase hypotensive effects of Hypotension-Associated Agents. Risk C: Monitor

Antipsychotic Agents (Second Generation [Atypical]): Blood Pressure Lowering Agents may increase hypotensive effects of Antipsychotic Agents (Second Generation [Atypical]). Risk C: Monitor

Arginine: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Articaine: May increase CNS depressant effects of CNS Depressants. Management: Consider reducing the dose of articaine if possible when used in patients who are also receiving CNS depressants. Monitor for excessive CNS depressant effects with any combined use. Risk D: Consider Therapy Modification

Azelastine (Nasal): May increase CNS depressant effects of CNS Depressants. Risk X: Avoid

Barbiturates: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Benperidol: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Benperidol: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Blonanserin: CNS Depressants may increase CNS depressant effects of Blonanserin. Management: Use caution if coadministering blonanserin and CNS depressants; dose reduction of the other CNS depressant may be required. Strong CNS depressants should not be coadministered with blonanserin. Risk D: Consider Therapy Modification

Blood Pressure Lowering Agents: May increase hypotensive effects of Hypotension-Associated Agents. Risk C: Monitor

Brimonidine (Topical): May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Brimonidine (Topical): May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Bromopride: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Bromperidol: May decrease hypotensive effects of Blood Pressure Lowering Agents. Blood Pressure Lowering Agents may increase hypotensive effects of Bromperidol. Risk X: Avoid

Bromperidol: May increase CNS depressant effects of CNS Depressants. Risk X: Avoid

Buclizine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

BusPIRone: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Cannabinoid-Containing Products: CNS Depressants may increase CNS depressant effects of Cannabinoid-Containing Products. Risk C: Monitor

Cetirizine (Systemic): May increase CNS depressant effects of CNS Depressants. Management: Consider avoiding this combination if possible. If required, monitor for excessive sedation or CNS depression, limit the dose and duration of combination therapy, and consider CNS depressant dose reductions. Risk D: Consider Therapy Modification

Chlorphenesin Carbamate: May increase adverse/toxic effects of CNS Depressants. Risk C: Monitor

CNS Depressants: May increase CNS depressant effects of Cannabinoid-Containing Products. Risk C: Monitor

CNS Depressants: Nabilone may increase CNS depressant effects of CNS Depressants. Risk X: Avoid

Diazoxide: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Difelikefalin: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Dihydralazine: CNS Depressants may increase hypotensive effects of Dihydralazine. Risk C: Monitor

Dimethindene (Topical): May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Dothiepin: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

DroPERidol: May increase CNS depressant effects of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (eg, opioids, barbiturates) with concomitant use. Risk D: Consider Therapy Modification

DULoxetine: Blood Pressure Lowering Agents may increase hypotensive effects of DULoxetine. Risk C: Monitor

Emedastine (Systemic): May increase CNS depressant effects of CNS Depressants. Management: Consider avoiding this combination if possible. If required, monitor for excessive sedation or CNS depression, limit the dose and duration of combination therapy, and consider CNS depressant dose reductions. Risk C: Monitor

Entacapone: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Flunarizine: CNS Depressants may increase CNS depressant effects of Flunarizine. Risk X: Avoid

Herbal Products with Blood Pressure Lowering Effects: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Hypotension-Associated Agents: Blood Pressure Lowering Agents may increase hypotensive effects of Hypotension-Associated Agents. Risk C: Monitor

Ixabepilone: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Kava Kava: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Ketotifen (Systemic): May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Kratom: May increase CNS depressant effects of CNS Depressants. Risk X: Avoid

Levocetirizine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Levodopa-Foslevodopa: Blood Pressure Lowering Agents may increase hypotensive effects of Levodopa-Foslevodopa. Risk C: Monitor

Lisuride: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Lofexidine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Lormetazepam: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Magnesium Sulfate: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Mequitazine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Metergoline: May decrease antihypertensive effects of Blood Pressure Lowering Agents. Blood Pressure Lowering Agents may increase orthostatic hypotensive effects of Metergoline. Risk C: Monitor

Metergoline: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Metoclopramide: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

MetyroSINE: CNS Depressants may increase sedative effects of MetyroSINE. Risk C: Monitor

Minocycline (Systemic): May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Molsidomine: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Moxonidine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Naftopidil: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Nicergoline: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Nicorandil: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Nitroprusside: Blood Pressure Lowering Agents may increase hypotensive effects of Nitroprusside. Risk C: Monitor

Noscapine: CNS Depressants may increase adverse/toxic effects of Noscapine. Risk X: Avoid

Obinutuzumab: May increase hypotensive effects of Blood Pressure Lowering Agents. Management: Consider temporarily withholding blood pressure lowering medications beginning 12 hours prior to obinutuzumab infusion and continuing until 1 hour after the end of the infusion. Risk D: Consider Therapy Modification

Olopatadine (Nasal): May increase CNS depressant effects of CNS Depressants. Risk X: Avoid

Opicapone: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Opioid Agonists: CNS Depressants may increase CNS depressant effects of Opioid Agonists. Management: Avoid concomitant use of opioid agonists and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Risk D: Consider Therapy Modification

Opipramol: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Orphenadrine: CNS Depressants may increase CNS depressant effects of Orphenadrine. Risk X: Avoid

Oxomemazine: May increase CNS depressant effects of CNS Depressants. Risk X: Avoid

Paraldehyde: CNS Depressants may increase CNS depressant effects of Paraldehyde. Risk X: Avoid

Pentoxifylline: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Periciazine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Phosphodiesterase 5 Inhibitors: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Pipamperone: May increase adverse/toxic effects of CNS Depressants. Risk C: Monitor

Piribedil: CNS Depressants may increase CNS depressant effects of Piribedil. Risk C: Monitor

Pramipexole: CNS Depressants may increase sedative effects of Pramipexole. Risk C: Monitor

Procarbazine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Prostacyclin Analogues: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Quinagolide: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Rilmenidine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Ropeginterferon Alfa-2b: CNS Depressants may increase adverse/toxic effects of Ropeginterferon Alfa-2b. Specifically, the risk of neuropsychiatric adverse effects may be increased. Management: Avoid coadministration of ropeginterferon alfa-2b and other CNS depressants. If this combination cannot be avoided, monitor patients for neuropsychiatric adverse effects (eg, depression, suicidal ideation, aggression, mania). Risk D: Consider Therapy Modification

ROPINIRole: CNS Depressants may increase sedative effects of ROPINIRole. Risk C: Monitor

Rotigotine: CNS Depressants may increase sedative effects of Rotigotine. Risk C: Monitor

Silodosin: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Sympathomimetics: Cannabinoid-Containing Products may increase tachycardic effects of Sympathomimetics. Risk C: Monitor

Thalidomide: CNS Depressants may increase CNS depressant effects of Thalidomide. Risk X: Avoid

Valerian: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Warfarin: Cannabinoid-Containing Products may increase serum concentration of Warfarin. Risk C: Monitor

Pregnancy Considerations

Adverse events have been observed in animal reproduction studies.

Nabilone is a synthetic delta-9-tetrahydrocannabinol (delta-9-THC); THC crosses the placenta (NAP 2017).

Breastfeeding Considerations

It is not known if nabilone is present in breast milk.

Nabilone is a synthetic delta-9-tetrahydrocannabinol (delta-9-THC); THC is present in breast milk (NAP 2017).

Breastfeeding is not recommended by the manufacturer.

Monitoring Parameters

BP, heart rate; monitor for neurologic/psychiatric adverse events (eg, dysphoria/euphoria, somnolence, vertigo).

Mechanism of Action

Nabilone is a synthetic cannabinoid with antiemetic properties. Antiemetic activity may be due to effect on cannabinoid receptors (CB1) within the central nervous system.

Pharmacokinetics (Adult Data Unless Noted)

Absorption: Rapid and complete.

Metabolism: Extensively metabolized to several active metabolites by oxidation and stereospecific enzyme reduction; CYP450 enzymes may also be involved.

Half-life elimination: Parent compound: ~2 hours; Metabolites: ~35 hours.

Time to peak, serum: Within 2 hours.

Excretion: Feces (~60%); renal (~24%).

Brand Names: International

International Brand Names by Country

For country code abbreviations (show table)

(AT) Austria: Canemes;
(DE) Germany: Canemes;
(MX) Mexico: Cesamet

Cesamet (nabilone) [product monograph]. Laval, Quebec, Canada: Bausch Health Canada Inc; May 2019.
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Dalzell AM, Bartlett H, Lilleyman JS. Nabilone: an alternative antiemetic for cancer chemotherapy. Arch Dis Child. 1986;61(5):502-505. [PubMed 3013104]
Hesketh PJ, Kris MG, Basch E, et al. Antiemetics: ASCO guideline update. J Clin Oncol. 2020;38(24):2782-2797. doi:10.1200/JCO.20.01296 [PubMed 32658626]
National Academies of Sciences, Engineering, and Medicine; Health and Medicine Division; Board on Population Health and Public Health Practice; Committee on the Health Effects of Marijuana: An Evidence Review and Research Agenda. The health effects of cannabis and cannabinoids: the current state of evidence and recommendations for research. Washington (DC): National Academies Press (NAP) (US); 2017. [PubMed 28182367]
Patel P, Robinson PD, Thackray J, et al. Guideline for the prevention of acute chemotherapy-induced nausea and vomiting in pediatric cancer patients: a focused update. Pediatr Blood Cancer. 2017;64(10). [PubMed 28453189]
Polito S, MacDonald T, Romanick M, et al. Safety and efficacy of nabilone for acute chemotherapy-induced vomiting prophylaxis in pediatric patients: a multicenter, retrospective review. Pediatr Blood Cancer. 2018;65(12):e27374. [PubMed 30051617]

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Nabilone (United States: Not available): Drug information