Note: Cesamet has been discontinued in the United States for >1 year.
Nausea and vomiting (refractory) associated with cancer chemotherapy: Oral: Initial: 1 to 2 mg twice daily; begin with the lower dose in the range and increase if needed; may administer 2 or 3 times per day during the entire chemotherapy course; continue for up to 48 hours after the last chemotherapy dose. Maximum: 6 mg/day divided in 3 doses. A dose of 1 to 2 mg the night before chemotherapy may also be of benefit. 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 (ASCO [Hesketh 2020]).
There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
(For additional information see "Nabilone (United States: Not available): Pediatric drug information")
Note: Cesamet has been discontinued in the United States for >1 year.
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 (POGO [Patel 2017]); 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 (Polito 2018):
Children ≥3 years and Adolescents: Very limited data available, efficacy results variable (Chan 1987): Oral:
<18 kg: 0.5 mg twice daily.
18 to 30 kg: 1 mg twice daily.
>30 kg: 1 mg 3 times daily.
There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
Refer to adult dosing. Use the lower end of the dosing range (to minimize adverse events).
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Capsule, Oral:
Cesamet: 1 mg [DSC] [contains fd&c blue #2 (indigotine)]
No
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)]
Generic: 0.25 mg, 0.5 mg, 1 mg
Cesamet has been discontinued in the United States for >1 year.
C-II
Oral: The initial dose (on day 1 of chemotherapy) should be given 1 to 3 hours before chemotherapy. Administer orally 2 to 3 times daily.
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) (Chan 1987; Dalzell 1986). 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 (Dalzell 1986).
Nausea and vomiting (refractory): Treatment of refractory nausea and vomiting associated with cancer chemotherapy in patients who have failed to adequately respond to conventional antiemetic regimens.
Limitations of use: Due to disturbing psychotomimetic reactions not observed with other antiemetic agents, nabilone should only be used for refractory nausea and vomiting. Nabilone is intended for use under close supervision, particularly during initial use and with dose adjustments. Nabilone is a schedule II controlled substance; schedule II substances have a high potential for abuse; limit prescriptions to the amount necessary for a single chemotherapy cycle (eg, a few days). Nabilone is not intended to be used on as needed basis or as an initial antiemetic agent. Monitor patients receiving nabilone for signs of excessive use, abuse and misuse; patients who may be at increased risk for substance abuse include those with a personal or family history of substance abuse (including drug or alcohol abuse) or mental illness.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
>10%:
Central nervous system: Drowsiness (52% to 66%), dizziness (59%), vertigo (52% to 59%), euphoria (11% to 38%), ataxia (13% to 14%), depression (14%), lack of concentration (12%), sleep disorder (11%)
Gastrointestinal: Xerostomia (22% to 36%)
Ophthalmic: Visual disturbance (13%)
1% to 10%:
Cardiovascular: Hypotension (8%)
Central nervous system: Dysphoria (9%), headache (6% to 7%), sedation (3%), depersonalization (2%), disorientation (2%)
Gastrointestinal: Anorexia (8%), nausea (4%), increased appetite (2%)
Neuromuscular & skeletal: Weakness (8%)
Frequency not defined:
Cardiovascular: Cardiac arrhythmia, cerebrovascular accident, chest pain, flushing, hypertension, orthostatic hypotension, palpitations, syncope, tachycardia
Central nervous system: Abnormal dreams, akathisia, anxiety, apathy, chills, confusion, difficulty thinking, dystonia, emotional disturbance, emotional lability, equilibrium disturbance, fatigue, hallucination, hyperactivity, illusion, insomnia, malaise, memory impairment, nervousness, numbness, pain, psychoneurosis (phobic), panic disorder, paranoia, paresthesia, psychological disorder (withdrawal), psychosis (including toxic), seizure, speech disturbance, stupor, voice disorder
Dermatologic: Anhidrosis, diaphoresis, skin photosensitivity, pruritus, skin rash
Endocrine & metabolic: Hot flash, increased thirst
Gastrointestinal: Abdominal pain, aphthous stomatitis, constipation, diarrhea, dysgeusia, dyspepsia, gastritis, mouth irritation, vomiting
Genitourinary: Altered micturition (decreased/increased), urinary retention
Hematologic & oncologic: Anemia, leukopenia
Hypersensitivity: Hypersensitivity reaction
Infection: Infection
Neuromuscular & skeletal: Arthralgia, back pain, myalgia, neck pain, tremor
Ophthalmic: Amblyopia, eye irritation, mydriasis, photophobia, visual field defect, xerophthalmia
Otic: Tinnitus
Renal: Polyuria
Respiratory: Cough, dyspnea, epistaxis, nasal congestion, pharyngitis, sinus headache, wheezing
Miscellaneous: Fever
Hypersensitivity to nabilone, other cannabinoids, or any component of the formulation
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 which require mental alertness (eg, operating machinery or driving). Dizziness, drowsiness, ataxia, depression, hallucinations, and psychosis have been reported. Use with caution in patients with mania, depression, or schizophrenia; cannabinoid use may reveal symptoms of psychiatric disorders. Careful psychiatric monitoring is recommended; psychiatric adverse reactions may persist for up to 3 days after discontinuing treatment.
Disease-related concerns:
• Substance abuse: Use with caution in patients with a history of substance abuse; potential for dependency exists. Tolerance, psychological and physical dependence may occur with prolonged use.
Concurrent drug therapy issues:
• CNS depressants: Effects may be potentiated when used with other psychoactive drugs, sedatives and/or ethanol.
Special populations:
• Older adult: Use with caution in the elderly; may cause postural hypotension.
None known.
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 Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Alcohol (Ethyl): Nabilone may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy
Alfuzosin: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Amifostine: Blood Pressure Lowering Agents may enhance the hypotensive effect 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 enhance the hypotensive effect of Hypotension-Associated Agents. Risk C: Monitor therapy
Anticholinergic Agents: May enhance the tachycardic effect of Cannabinoid-Containing Products. Risk C: Monitor therapy
Antipsychotic Agents (Second Generation [Atypical]): Blood Pressure Lowering Agents may enhance the hypotensive effect of Antipsychotic Agents (Second Generation [Atypical]). Risk C: Monitor therapy
Barbiturates: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Benperidol: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Blood Pressure Lowering Agents: May enhance the hypotensive effect of Hypotension-Associated Agents. Risk C: Monitor therapy
Brimonidine (Topical): May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Bromperidol: May diminish the hypotensive effect of Blood Pressure Lowering Agents. Blood Pressure Lowering Agents may enhance the hypotensive effect of Bromperidol. Risk X: Avoid combination
CNS Depressants: May enhance the CNS depressant effect of Cannabinoid-Containing Products. Risk C: Monitor therapy
Cocaine (Topical): May enhance the tachycardic effect of Cannabinoid-Containing Products. Risk C: Monitor therapy
Diazoxide: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
DULoxetine: Blood Pressure Lowering Agents may enhance the hypotensive effect of DULoxetine. Risk C: Monitor therapy
Herbal Products with Blood Pressure Lowering Effects: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Hypotension-Associated Agents: Blood Pressure Lowering Agents may enhance the hypotensive effect of Hypotension-Associated Agents. Risk C: Monitor therapy
Levodopa-Containing Products: Blood Pressure Lowering Agents may enhance the hypotensive effect of Levodopa-Containing Products. Risk C: Monitor therapy
Lormetazepam: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Molsidomine: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Naftopidil: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Nicergoline: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Nicorandil: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Nitroprusside: Blood Pressure Lowering Agents may enhance the hypotensive effect of Nitroprusside. Risk C: Monitor therapy
Obinutuzumab: May enhance the hypotensive effect 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
Pentoxifylline: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Pholcodine: Blood Pressure Lowering Agents may enhance the hypotensive effect of Pholcodine. Risk C: Monitor therapy
Phosphodiesterase 5 Inhibitors: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Prostacyclin Analogues: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Quinagolide: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Sympathomimetics: Cannabinoid-Containing Products may enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy
Tricyclic Antidepressants: May enhance the tachycardic effect of Cannabinoid-Containing Products. Blood pressure raising effects and drowsiness may also be enhanced. Risk C: Monitor therapy
Warfarin: Cannabinoid-Containing Products may increase the serum concentration of Warfarin. Risk C: Monitor therapy
Adverse events have been observed in animal reproduction studies.
Because some cannabinoids are excreted in breast milk, use in breast-feeding is not recommended.
Blood pressure, heart rate; signs and symptoms of excessive use, abuse, or misuse; monitor for neurologic/psychiatric adverse events (eg, dysphoria/euphoria, somnolence, vertigo)
Antiemetic activity may be due to effect on cannabinoid receptors (CB1) within the central nervous system.
Absorption: Rapid and complete
Distribution: ~12.5 L/kg
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%)
Capsules (Cesamet Oral)
1 mg (per each): $47.04
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