Cesamet


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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.

nabilone

(na-bi-lone) ,

Cesamet

(trade name)

Classification

Therapeutic: antiemetics
Pharmacologic: cannabinoids

Indications

Treatment of nausea and vomiting due to chemotherapy that has not responded to other conventional antiemetics.

Action

Antiemetic action may be due to interaction with cannabinoid receptor system in the brain.

Therapeutic effects

Decreased nausea and vomiting due to emetogenic chemotherapy.

Pharmacokinetics

Absorption: Completely absorbed following oral administration.
Distribution: unknownnown.
Protein Binding: Highly protein bound.
Metabolism and Excretion: Highly metabolized with extensive first pass hepatic metabolism; metabolites excreted in feces (67%) and urine (22%).
Half-life: 2 hr.

Time/action profile

ROUTEONSETPEAKDURATION
POunknown1–3 hr8–12 hr*
*Psychoactive effects may persist for 72 hr.

Contraindications/Precautions

Contraindicated in: Hypersensitivity; Obstetric: Lactation.
Use Cautiously in: History of substance abuse or mental illness/psychiatric disorder; Geriatric: Increased risk of hypotension, tachycardia and psychoactive effects in patients >65 yr; Obstetric: Use in pregnancy only if maternal benefit outweighs fetal risk; Pediatric: Safe use in children <18 yr not established; increased risk of psychoactive reactions.

Adverse Reactions/Side Effects

Central nervous system

  • concentration difficulty (most frequent)
  • drowsiness (most frequent)
  • euphoria (most frequent)
  • sleep disturbance (most frequent)
  • vertigo (most frequent)
  • altered mental state
  • anxiety
  • depression
  • detachment
  • disorientation
  • headache
  • panic
  • paranoia
  • psychotomimetic reactions

Cardiovascular

  • hypotension (most frequent)
  • tachycardia

Gastrointestinal

  • dry mouth (most frequent)
  • increased appetite
  • nausea

Neurologic

  • ataxia (most frequent)
  • physical dependence
  • psychological dependence

Interactions

Drug-Drug interaction

↑ risk of CNS depression with other CNS depressants including alcohol, antihistamines, barbiturates, benzodiazepines, buspirone, lithium, muscle relaxants, opioids, sedative/hypnotics or other other CNS depressants .↑ risk of hypertension, tachycardia and cardiotoxicity with amphetamines, cocaine, and other sympathomimetic agents.↑ risk of tachycardia or drowsiness with atropine, scopolamine, antihistamines, or other anticholinergics.↑ risk of tachycardia, hypertension, drowsiness with tricyclic antidepressants.May displace, be displaced by or otherwise interfere with other highly protein-bound drugs.May cause reversible hypomanic reaction with disulfiram or fluoxetine.May ↓ clearance and ↑ effects of barbiturates..May ↑ clearance and ↓ effects of theophylline. Cross-tolerance and potentiation of effects may occur with opioids.Naltrexone may enhance effects.Alcohol may ↑ mood effects.

Route/Dosage

Oral (Adults) 1 or 2 mg twice daily; initial dose should be given 1 to 3 hrs prior to chemotherapy. May be given as 1 or 2 mg the night before. Not to exceed 6 mg/day (2 mg three times daily). May be used during entire course of each cycle of chemotherapy and for 48 hrs after the last dose if needed.

Availability

Capsules: 1 mg

Nursing implications

Nursing assessment

  • Monitor patient closely for altered mental status. Patient should remain under the supervision of a responsible adult, especially during initiation of therapy and dose adjustments. Adverse psychiatric reactions may persist for 48–72 hrs following cessation of treatment.
  • Monitor vital signs periodically during therapy. May cause tachycardia and orthostatic hypotension.
  • Lab Test Considerations: May cause anemia.

Potential Nursing Diagnoses

Nausea (Indications)
Risk for injury (Side Effects)

Implementation

  • Start with lowest dose and increase as needed to minimize side effects.
  • Oral: Administer 1–3 hr before chemotherapeutic regimen is administered. May also be administered the night before chemotherapy Administer 2 or 3 times daily during entire course of each cycle of chemotherapy and, if needed, for 48 hr after last dose of each cycle of chemotherapy.

Patient/Family Teaching

  • Instruct patient to take nabilone as directed. Do not take more than recommended.
  • Causes difficulty concentrating, drowsiness, euphoria and other mental changes. Caution patient to avoid driving and other activities requiring alertness until response to nabilone is known.
  • Caution patient to avoid taking alcohol, sedatives, hypnotics, CNS depressants, and other psychoactive substances concurrently with nabilone.
  • Advise patient to notify health care professional prior to taking any Rx, OTC, or herbal product.

Evaluation/Desired Outcomes

  • Decrease in nausea and vomiting during emetogenic chemotherapy.

Cesamet

a trademark for nabilone.
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References in periodicals archive ?
On February 22, 2007, Valeant announced the submission of an Investigational New Drug application to test Cesamet as a treatment for chemotherapy-induced neuropathic pain.
Moreover, two FDA-approved drugs are based on cannabinoids - Marinol and Cesamet.
Comment: Cesamet was approved in the United States in 1985, but Eli Lilly & Co.