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Nabilone

Medically reviewed by Drugs.com. Last updated on Aug 2, 2020.

Pronunciation

(NA bi lone)

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)]

Brand Names: U.S.

  • Cesamet [DSC]

Pharmacologic Category

  • Antiemetic

Pharmacology

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

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

Dosing: Adult

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.

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 (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.

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 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. Consider therapy modification

Amisulpride (Oral): May enhance the hypotensive effect of Hypotension-Associated Agents. Monitor therapy

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

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

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 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.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Loss of strength and energy

• Dizziness

• Fatigue

• Trouble focusing

• Feeling high

• Dry mouth

• Lack of appetite

• Change in balance

• Increased appetite

• Headache

• Trouble sleeping

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Mood changes

• Behavioral changes

• Confusion

• Severe dizziness

• Passing out

• Fast heartbeat

• Sensing things that seem real but are not

• Vision changes

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, 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 limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.