triazolam

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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

/tri·a·zo·lam/ (tri-a´zo-lam) a benzodiazepine used as a sedative and hypnotic in the treatment of insomnia.

triazolam

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

triazolam

[tri·az′əlam]
a benzodiazepine hypnotic agent. This drug was withdrawn from the market in the United Kingdom; it continues to be available in the United States. Its prototype is lorazepam.
indication It is prescribed in the short-term treatment of insomnia.
contraindications Known sensitivity to this drug or to other benzodiazepines or concurrent use of drugs that block CYP3A4 (e.g., ketoconazole) prohibits its use. It is not given to pregnant women, lactating mothers, or patients younger than 18 years.
adverse effects Among the most serious adverse effects are anterograde amnesia, paradoxical reactions, tachycardia, depression, confusion or memory impairment, and visual disturbances.

triazolam

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