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Nabilone


General


Pronunciation

(NA bi lone)


Brand Names: U.S.

  • Cesamet

Indications


Use: Labeled Indications

Treatment of refractory nausea and vomiting associated with cancer chemotherapy


Contraindications


Hypersensitivity to nabilone, other cannabinoids, or any component of the formulation


Dosing and Administration


Dosing: Adult

Nausea and vomiting associated with cancer chemotherapy: Oral: 1-2 mg twice daily (maximum: 6 mg divided in 3 doses 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. A dose of 1-2 mg the night before chemotherapy may also be of benefit.


Dosing: Geriatric

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


Dosing: Pediatric

Nausea and vomiting associated with cancer chemotherapy (off-label use; Dupuis, 2003): Oral: Children >4 years:

<18 kg: 0.5 mg every 12 hours

18-30 kg: 1 mg every 12 hours

>30 kg: 1 mg every 8-12 hours


Dosing: Renal Impairment

No dosage adjustment provided in manufacturer 's labeling (has not been studied).


Dosing: Hepatic Impairment

No dosage adjustment provided in manufacturer 's labeling (has not been studied).


Administration

Initial dose should be given 1-3 hours before chemotherapy.


Storage

Store at 25 ‚ °C (77 ‚ °F); excursion permitted to 15 ‚ °C and 30 ‚ °C (59 ‚ °F and 86 ‚ °F).


Dosage Forms/Strengths


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)]


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

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

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

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


Monitoring Parameters

Blood pressure, heart rate; signs and symptoms of excessive use, abuse, or misuse


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%), concentration decreased (12%), sleep disturbance (11%)

Gastrointestinal: Xerostomia (22% to 36%)

Ocular: 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%), appetite increased (2%)

Neuromuscular & skeletal: Weakness (8%)

<1% (Limited to important or life-threatening) and frequency not reported: Abdominal pain, abnormal dreams, akathisia, allergic reaction, amblyopia, anemia, anhydrosis, anxiety, apathy, aphthous ulcer, arrhythmia, back pain, cerebral vascular accident, chest pain, chills, constipation, cough, diaphoresis, diarrhea, dyspepsia, dyspnea, dystonia, emotional disorder, emotional lability, epistaxis, equilibrium dysfunction, eye irritation, fatigue, fever, flushing, gastritis, hallucinations, hot flashes, hyperactivity, hypertension, infection, insomnia, joint pain, leukopenia, lightheadedness, malaise, memory disturbance, mood swings, mouth irritation, muscle pain, nasal congestion, neck pain, nervousness, neurosis (phobic), numbness, orthostatic hypotension, pain, palpitation, panic disorder, paranoia, paresthesia, perception disturbance, pharyngitis, photophobia, photosensitivity, polyuria, pruritus, psychosis (including toxic), pupil dilation, rash, seizure, sinus headache, speech disorder, stupor, syncope, tachycardia, taste perversion, thirst, thought disorder, tinnitus, tremor, urination decreased/increased, urinary retention, visual field defect, voice change, vomiting, wheezing, withdrawal, xerophthalmia


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.


Pregnancy Risk Factor

C


Pregnancy Considerations

Adverse events have been observed in animal reproduction studies.


Actions


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


Patient and Family Education


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, fatigue, dry mouth, or insomnia. Have patient report immediately to prescriber signs of depression (suicidal ideation, anxiety, emotional instability, or illogical thinking), confusion, severe dizziness, passing out, behavioral changes, mood changes, tachycardia, hallucinations, memory impairment, 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 healthcare 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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