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nabilone (Cesamet)

 

Classes: Antiemetic Agents

Dosing and uses of Cesamet (nabilone)

 

Adult dosage forms and strengths

capsule: Schedule II

  • 1mg

 

Chemotherapy-Induced Nausea/Vomiting

1-2 mg PO q8-12hr

 

Renal Impairment

Dose adjustment not necessary

 

Administration

Give 1-3 hours before chemotherapy

May give one dose the night before chemotherapy

May continue 24 hours after chemotherapy

No more than 6 mg/day

 

Pediatric dosage forms and strengths

capsule: Schedule II

  • 1mg

 

Chemotherapy-Induced Nausea/Vomiting (Off-label)

>4 years

  • <18 kg: 0.5 mg PO q12hr
  • 18-30 kg: 1 mg PO q12hr
  • >30 kg: 1 mg PO q8hr

 

Geriatric dosage forms and strengths

 

Chemotherapy-induced nausea/vomiting

1-2 mg PO q8-12hr; not to exceed 6 mg divided q8hr

 

Cesamet (nabilone) adverse (side) effects

>10%

Vertigo (52%)

Drowsiness (52%)

Dry mouth (36%)

Ataxia (14%)

Visual disturbance (13%)

Blurred vision (12.8%)

Concentration difficulties (12%)

Euphoria (11%)

Sleep disturbance (11%)

 

1-10%

Depersonalization

Disorientation

Dysphoria

Headache

Hypotension

Nausea

 

Warnings

Contraindications

Hypersensitivity to cannabinoids

History of psychotic reactions

 

Cautions

Severe liver impairment

Give only to patients in whom conventional antiemetics have failed

Emotionally disturbed patients (non-psychotic)

Concomitant use of alcohol or other psychoactive substances can potentiate psychotropic effects

May cause tachycardia and orthostatic hypotension

May impair ability to drive or perform hazardous tasks

 

Pregnancy and lactation

Pregnancy category: C

Lactation: not recommended

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Cesamet (nabilone)

Mechanism of action

Cannabinoid antiemetic may act in the central nervous system by acting on cannabinoid receptors

 

Pharmacokinetics

Excretion: Feces (65%; primarily bile); urine (20%)

Half-life elimination: 2 hr (parent compound); 35 hr (metabolites)

Peak plasma time: 2 hr

Distribution: 12.5 L/kg

Metabolism: Direct enzymatic oxidation and possibly CYP450 enzymes