triazolam
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triazolam
[tri-a´zo-lam]triazolam
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.
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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.