Dosage Forms
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)]
Pharmacology
Mechanism of Action
Antiemetic activity may be due to effect on cannabinoid receptors (CB1) within the central nervous system.
Pharmacokinetics/Pharmacodynamics
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
Excretion
Feces (~60%); renal (~24%)
Time to Peak
Serum: Within 2 hours
Half-Life Elimination
Parent compound: ~2 hours; Metabolites: ~35 hours
Use: Labeled Indications
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.
Contraindications
Hypersensitivity to nabilone, other cannabinoids, or any component of the formulation
Dosage and Administration
Dosing: Adult
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.
Guideline recommendations: American Society of Clinical Oncology: Nausea or vomiting, refractory or breakthrough: Oral: 1 to 2 mg twice daily on days 1, 2, and 3 (Hesketh 2017)
Dosing: Geriatric
Refer to adult dosing. Use the lower end of the dosing range (to minimize adverse events).
Dosing: Pediatric
Chemotherapy-induced nausea and vomiting, prevention: Limited data available: Note: Use in patients receiving moderate to highly emetogenic chemotherapy in whom corticosteroids are contraindicated (Dupuis, 2013): Oral:
Infants, Children, and Adolescents (Chan, 1997; Dupuis, 2013):
<18 kg: 0.5 mg twice daily
18 to 30 kg: 1 mg twice daily
>30 kg: 1 mg 3 times daily
Administration
The initial dose (on day 1 of chemotherapy) should be given 1 to 3 hours before chemotherapy. Administer orally 2 to 3 times daily.
Storage
Store at 25°C (77°F); excursion permitted to 15°C and 30°C (59°F and 86°F).
Drug Interactions
Alcohol (Ethyl): Nabilone may enhance the CNS depressant effect of Alcohol (Ethyl). Monitor therapy
Alfuzosin: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy
Amifostine: Blood Pressure Lowering Agents may enhance the hypotensive effect of Amifostine. Management: When amifostine is used at chemotherapy doses, blood pressure lowering medications should be withheld for 24 hours prior to amifostine administration. If blood pressure lowering therapy cannot be withheld, amifostine should not be administered. Consider therapy modification
Anticholinergic Agents: May enhance the tachycardic effect of Cannabinoid-Containing Products. Monitor therapy
Benperidol: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy
Blood Pressure Lowering Agents: May enhance the hypotensive effect of Hypotension-Associated Agents. Monitor therapy
Brimonidine (Topical): May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy
Bromperidol: Blood Pressure Lowering Agents may enhance the hypotensive effect of Bromperidol. Bromperidol may diminish the hypotensive effect of Blood Pressure Lowering Agents. Avoid combination
CNS Depressants: Nabilone may enhance the CNS depressant effect of CNS Depressants. Monitor therapy
Cocaine (Topical): May enhance the tachycardic effect of Cannabinoid-Containing Products. Monitor therapy
Diazoxide: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy
DULoxetine: Blood Pressure Lowering Agents may enhance the hypotensive effect of DULoxetine. Monitor therapy
Herbs (Hypotensive Properties): May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy
Hypotension-Associated Agents: Blood Pressure Lowering Agents may enhance the hypotensive effect of Hypotension-Associated Agents. Monitor therapy
Levodopa-Containing Products: Blood Pressure Lowering Agents may enhance the hypotensive effect of Levodopa-Containing Products. Monitor therapy
Lormetazepam: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy
Molsidomine: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy
Naftopidil: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy
Nicergoline: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy
Nicorandil: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy
Nitroprusside: Blood Pressure Lowering Agents may enhance the hypotensive effect of Nitroprusside. 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. Consider therapy modification
Pentoxifylline: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy
Pholcodine: Blood Pressure Lowering Agents may enhance the hypotensive effect of Pholcodine. Monitor therapy
Phosphodiesterase 5 Inhibitors: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy
Prostacyclin Analogues: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy
Quinagolide: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy
Sympathomimetics: Cannabinoid-Containing Products may enhance the tachycardic effect of Sympathomimetics. Monitor therapy
Warfarin: Cannabinoid-Containing Products may increase the serum concentration of Warfarin. Monitor therapy
Adverse Reactions
>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
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 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:
- Elderly: Use with caution in the elderly; may cause postural hypotension.
Monitoring Parameters
Blood pressure, heart rate; signs and symptoms of excessive use, abuse, or misuse; monitor for neurologic/psychiatric adverse events (eg, dysphoria/euphoria, somnolence, vertigo)
Pregnancy
Pregnancy Risk Factor
C
Pregnancy Considerations
Adverse events have been observed in animal reproduction studies.
Patient Education
What is this drug used for?
- It is used to treat upset stomach and throwing up.
Frequently reported side effects of this drug
- Loss of strength and energy
- Difficulty focusing
- Feeling high
- Dry mouth
- Lack of appetite
- Increased appetite
- Headache
- Trouble sleeping
Other side effects of this drug: Talk with your doctor right away if you have any of these signs of:
- Depression like confusion, severe dizziness, passing out, behavioral changes, mood changes, fast heartbeat, sensing things that seem real but are not, trouble with memory, severe fatigue, severe change in balance, or vision changes.
- Signs of a significant reaction like wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat.
Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.
Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine.
