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Nabilone

Pronunciation

(NA bi lone)

Dosage Forms

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

Capsule, Oral:

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

Brand Names: U.S.

  • Cesamet

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

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

Note: The Pediatric Oncology Group of Ontario (POGO) Guideline for the Prevention of Acute Chemotherapy-Induced Nausea and Vomiting in Pediatric Cancer Patients: A Focused Update no longer recommends the use of nabilone for prevention of acute nausea and vomiting (Patel 2017).

Nausea and vomiting (refractory) associated with cancer chemotherapy (off-label population) (Dupuis 2003; Dupuis 2013): Children and Adolescents: Oral:

<18 kg: 0.5 mg every 12 hours

18 to 30 kg: 1 mg every 12 hours

>30 kg: 1 mg every 8 to 12 hours

Maximum dose: 0.06 mg/kg/day

Dosing: Renal Impairment

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

Dosing: Hepatic Impairment

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

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

CNS Depressants: Nabilone may enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Cocaine: 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: Blood Pressure Lowering Agents may enhance the hypotensive effect of Levodopa. 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

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 Risk Factor

C

Pregnancy Considerations

Adverse events have been observed in animal reproduction studies.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience loss of strength and energy, feeling high, dry mouth, lack of appetite, increased appetite, headache, or insomnia. Have patient report immediately to prescriber signs of depression (suicidal ideation, anxiety, emotional instability, or confusion), confusion, severe dizziness, passing out, behavioral changes, mood changes, tachycardia, hallucinations, memory impairment, difficulty focusing, severe fatigue, severe change in balance, or vision changes (HCAHPS).

• Educate patient about signs of a significant reaction (eg, 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. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

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