triazolam

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Related to Trazolam: Halcion

triazolam

 [tri-a´zo-lam]
a benzodiazepine used as a sedative and hypnotic in treatment of insomnia; administered orally.

triazolam

Apo-Triazo (CA), Gen-Triazolam (CA), Halcion

Pharmacologic class: Benzodiazepine

Therapeutic class: Sedative-hypnotic

Controlled substance schedule IV

Pregnancy risk category X

Action

Inhibits gamma-aminobutyric acid, a neurotransmitter that activates receptors at limbic, thalamic, and hypothalamic levels of CNS

Availability

Tablets: 0.125 mg, 0.25 mg, 0.5 mg

Indications and dosages

Insomnia

Adults: 0.125 to 0.5 mg P.O. at bedtime p.r.n. After 7 to 10 days, decrease dosage gradually and then discontinue.

Dosage adjustment

• Elderly or debilitated patients

Off-label uses

• Presurgical hypnotic

Contraindications

• Hypersensitivity to drug or other benzodiazepines

• Concurrent use of itraconazole, ketoconazole, or nefazodone

• Pregnancy

Precautions

Use cautiously in:

• hepatic or renal dysfunction, sleep apnea, respiratory compromise, psychosis

• history of suicide attempt or drug abuse

• elderly or debilitated patients

• breastfeeding patients

• children younger than age 18 (safety and efficacy not established).

Administration

• Don't give with grapefruit juice.

Adverse reactions

CNS: dizziness, excessive sedation, hangover, headache, anterograde or traveler's amnesia, confusion, incoordination, lethargy, depression, paradoxical excitation, light-headedness, psychological disturbance, euphoria

GI: nausea, vomiting

Other: physical or psychological drug dependence, drug tolerance, withdrawal symptoms (tremor, abdominal and muscle cramps, vomiting, diaphoresis, dysphoria, perceptual disturbances, insomnia)

Interactions

Drug-drug. Antidepressants, antihistamines, chloral hydrate, opioid analgesics, other psychotropic drugs: additive CNS depression

Cimetidine, disulfiram, fluconazole, hormonal contraceptives, isoniazid, itraconazole, ketoconazole, nefazodone, rifampin, and other drugs that inhibit CYP450-3A4-mediated metabolism: decreased oxidative metabolism and increased action of triazolam

Digoxin: increased digoxin blood level, greater risk of toxicity

Macrolide anti-infectives (such as azithromycin, clarithromycin, erythromycin): increased triazolam bioavailability

Probenecid: rapid onset and prolonged effects of triazolam

Ranitidine: increased triazolam blood level

Theophylline: decreased sedative effect of triazolam

Drug-food. Grapefruit juice: increased triazolam blood level and effects

Drug-herbs. Chamomile, hops, kava, skullcap, valerian: increased CNS depression

Drug-behaviors. Alcohol use: increased CNS depression

Smoking: increased triazolam clearance

Patient monitoring

• Monitor neurologic status. Watch for paradoxical or rebound drug effects.

• Observe for signs of drug hoarding and drug abuse.

Patient teaching

• Tell patient to take at bedtime with a liquid other than grapefruit juice.

• Explain that drug is meant only for short-term use (7 to 10 days).

• Tell patient rebound insomnia may occur for 1 to 2 nights after he discontinues drug.

• Instruct patient to avoid alcohol use and smoking.

• Caution patient to avoid driving and other hazardous activities while under drug's influence.

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

triazolam

(trī-ā′zə-lăm)
n.
A benzodiazepine drug, C17H12Cl2N4, used for short-term treatment of insomnia.

triazolam

Halcion® Pharmacology A sedative-hypnotic benzodiazepine analogue. Adverse effects Drowsiness, ↓ concentration See Benzodiazepine.