nabilone


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Related to nabilone: Cesamet, Marinol

nabilone

Cesamet

Pharmacologic class: Synthetic cannabinoid

Therapeutic class: Antiemetic

Controlled substance schedule II

Pregnancy risk category C

Action

Unclear. Drug has complex effects on CNS, including relaxation, drowsiness, and euphoria; antiemetic effect may result from interaction with cannabinoid receptor system in neural tissues.

Availability

Capsules: 1 mg

Indications and dosages

Nausea and vomiting associated with cancer chemotherapy in patients who respond inadequately to conventional antiemetics

Adults: 1 to 2 mg P.O. twice daily; give initial dose 1 to 3 hours before chemotherapy. Maximum daily dose, 6 mg given in divided doses three times daily.

Contraindications

• Hypersensitivity to drug or other cannabinoids

Precautions

Use cautiously in:

• hepatic or renal impairment, hypertension, cardiac disease, QT interval prolongation, psychiatric disorders (current or previous)

• history of substance abuse

• concurrent use of sedatives, hypnotics, other psychoactive drugs, or CNS depressants

• concurrent alcohol use

• pregnant or breastfeeding patients

• elderly patients

• children (safety and efficacy not established).

Administration

• On day of chemotherapy, give 1 to 3 hours before chemotherapeutic drug is administered.

• To minimize adverse reactions, give recommended lower starting dosage and increase dosage as necessary.

• Know that drug may be given two or three times daily during entire course of each chemotherapy cycle and, if needed, for 48 hours after last dose of each chemotherapy cycle.

Adverse reactions

CNS: drowsiness, euphoria, dysphoria, inebriated feeling, mood swings, irritability, fatigue, malaise, ataxia, headache, poor concentration, disorientation, anxiety, depersonalization, depersonalization syndrome, speech disorder or disturbance, insomnia, abnormal dreams, vertigo, light-headedness, dizziness, orthostatic dizziness, twitching, depression, confusion, asthenia, sedation, hallucinations, paresthesia, memory disturbance, perception disturbance, seizures, dystonia, numbness, akathisia, tremor, incoordination, toxic psychosis, paranoia, apathy, thought disorder, panic disorder, withdrawal, nervousness, phobic neurosis, emotional disorder, hyperactivity, hypotonia, sinus headache

CV: orthostatic hypotension

EENT: visual disturbances, pharyngitis, nasal congestion, dry throat, dry nose, nosebleed, voice change, thick tongue sensation

GI: nausea, dry mouth

GU: increased or decreased urination, urinary retention, urinary frequency

Metabolic: thirst

Musculoskeletal: muscle pain, back pain, neck pain, joint pain

Respiratory: dyspnea, wheezing, cough

Skin: excessive sweating, pruritus, rash, photosensitivity

Other: taste changes, increased appetite, fever, hot flashes, chills, unspecified pain, bacterial infection, chest pain, allergic reaction

Interactions

Drug-drug. Amitriptyline, amoxapine, desipramine, other tricyclics: additive tachycardia, hypertension, drowsiness

Amphetamines, cocaine, other sympathomimetics: additive hypertension, tachycardia, possible cardiotoxicity

Anticholinergics, antihistamines, tri-cyclic antidepressants: increased tachycardia and hypertension

Antihistamines, atropine, scopolamine, other anticholinergics: additive or superadditive tachycardia, drowsiness

Antihistamines, barbiturates, benzodiazepines, buspirone, lithium, muscle relaxants, opioids, other CNS depressants: additive drowsiness and CNS depression

Antipyrine, barbiturates: decreased clearance of these drugs

Disulfiram, fluoxetine: reversible hypomanic reaction

Opioids: cross-tolerance and mutual potentiation

Naltrexone: enhanced nabilone effects

Theophylline: increased theophylline metabolism

Drug-behaviors. Alcohol use: increased positive mood effects, increased CNS depression

Sun exposure: increased risk of skin reactions

Patient monitoring

• Ensure that patient remains under supervision of responsible adult, especially during initial use and dosage adjustments.

• Monitor vital signs for orthostatic hypotension and tachycardia.

Check for adverse CNS reactions. Report significant depression, paranoid reaction, or emotional lability. Be aware that adverse psychiatric reactions can last for 48 to 72 hours after treatment ends.

• Monitor for excessive use, abuse, or misuse of drug.

• Monitor patient's nutritional and hydration status.

Patient teaching

• Instruct patient to take drug on day of chemotherapy 1 to 3 hours before chemotherapeutic drug is scheduled.

• Teach patient about significant CNS side effects (especially mood changes) and cardiovascular side effects. Stress importance of taking drug only as prescribed and needed.

• Inform patient that drug may cause additive CNS depression if used with alcohol or other CNS depressants (such as sleeping pills, tranquilizers, or anxiolytics).

Advise patient, family member, or caregiver to immediately report depression, suicidal thoughts, paranoid reactions, and other serious CNS reactions.

• Caution patient to avoid driving and other hazardous activities until drug effects are known.

• Instruct breastfeeding patient not to use drug while breastfeeding.

• As appropriate, review all other significant adverse reactions and interactions, especially those related to the drugs and behaviors mentioned above.

nab·i·lone

(nab'i-lōn),
A synthetic cannabinoid used to treat nausea and vomiting associated with cancer chemotherapy.

nabilone

(năb′ə-lōn′)
n.
A synthetic cannabinoid, C24H36N3, used to treat nausea and vomiting associated with cancer chemotherapy and to treat anorexia in patients with AIDS.
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References in periodicals archive ?
Nabilone was evaluated in 16 trials; dronabinol was utilized in 13 trials; and IM levonantradol, a synthetic cannabinoid analog of dronabinol, was used in 1 trial.
In studies examining the endocannabinoid-based drug "Nabilone" on pain outcomes in fibromyalgia, the statistically significant effects were outweighed when side effects were taken into consideration (78-80).
The cannabinoid drugs used were: delta-9-tetrahydrocannabinol (THC) (11 studies), THC + cannabidiol (two studies), cannabidiol (one study), dronabinol (five studies), nabilone (11 studies), levonantradol (two studies), GW842166 (one study), and dexabinol (one study).
Although some evidence suggests cannabis-based drugs, including dronabinol and nabilone, may have therapeutic benefits for some patients with life-limiting conditions (Philipsen et al 2014; Green and De-Vries 2010), medicinal cannabis in emesis control is a very new treatment option available for Australians.
In 2001, a systematic review of 30 RCTs with a total of 1366 patients looked at how cannabinoids--including oral dronabinol, oral nabilone, and intramuscular levonantradol, a synthetic drug that does not have FDA approval--compared with placebo or other antiemetics.
Synthetic cannabinoids include dronabinol (Marinol[R]) and nabilone (Cesamet[R]).
Nabilone is a synthetic derivative of [[DELTA].sup.9]-THC with a slightly modified molecular structure.
Nevertheless, in the past, dronabinol (Marinol[TM]) a synthetic THC and nabilone (Cesamet[TM]) a synthetic THC-mimetic received FDA approval as appetite stimulants and treatments for chemotherapy induced nausea and vomiting (CINV).
One recent study found that over 70% of their sample of patients with PTSD experienced considerable reduction in nightmare intensity or total cessation of nightmares after taking nabilone, an endocannabinoid receptor agonist (Fraser, 2009).
Another cannabinoid, nabilone, is approved in Canada, Mexico, the United Kingdom, and the United States.
Giagnoni, "Antiinflammatory action of endocannabinoid palmitoylethanolamide and the synthetic cannabinoid nabilone in a model of acute inflammation in the rat," British Journal of Pharmacology, vol.
The most commonly prescribed cannabinoid-based medicines are dronabinol (marketed as Marinol[R] since 1986, Abbott Products Inc.) and nabilone (marketed as Cesamet[R] since 1981, Valeant Pharmaceuticals International).