TRIAZOLAM

TRIAZOLAM (trye-ay'zoe-lam) Halcion Classifications: benzodiazepine; anxiolytic; sedative-hypnotic; Therapeutic: sedative-hypnotic; antianxiety Prototype: Lorazepam Pregnancy Category: X Controlled Substance: Schedule IV

Availability

0.125 mg, 0.25 mg tablets

Action

Benzodiazepine derivative with hypnotic effects with fewer residual daytime effects. Its blockade of cortical and limbic arousal results in hypnotic activity.

Therapeutic Effect

Drug-induced effects on sleep include decreased sleep latency and number of nocturnal awakenings, decreased total nocturnal wake time, and increased duration of sleep.

Uses

Short-term management of insomnia characterized by difficulty in falling asleep, frequent wakeful periods. Following long-term use, tolerance or adaptation may develop.

Contraindications

Hypersensitivity to triazolam and benzodiazepines; pregnancy (category X), lactation; ethanol intoxication; suicidal ideations; concurrent administration with the following medications that impair cytochrome P450 3A (e.g., ketoconazole, itraconazole, and nefazodone).

Cautious Use

Depression; bipolar disorder; dementia; psychosis; myasthenia gravis; Parkinson's disease; older adults and debilitated patients; patients with suicidal tendency; impaired kidney or liver function; chronic pulmonary insufficiency; sleep apnea.

Route & Dosage

Insomnia Adult: PO 0.125–0.25 mg h.s. (max: 0.5 mg/d) Geriatric: PO 0.0625–0.125 mg h.s.

Administration

Oral

• Give immediately before bed; onset of drug action is rapid.
• Do not exceed recommended doses.
• Store at 15°–30° C (59°–86° F).

Adverse Effects (≥1%)

CNS: Drowsiness, light-headedness, headache, dizziness, ataxia, visual disturbances, confusional states, memory impairment, "rebound insomnia," anterograde amnesia, paradoxical reactions, minor changes in EEG patterns. GI: Nausea, vomiting, constipation.

Interactions

Drug: Alcohol, cns depressants, anticonvulsants, nefazodone, benzodiazepines potentiate CNS depression; cimetidine increases triazolam plasma levels, thus increasing its toxicity; may decrease antiparkinsonism effects of levodopa. Herbal: Kava, valerian may potentiate sedation. St. John's wort may decrease efficacy. Food: Grapefruit juice (>1 qt/d) may increase plasma concentrations and adverse effects.

Pharmacokinetics

Absorption: Readily from GI tract. Onset: 15–30 min. Peak: 1–2 h. Duration: 6–8 h. Distribution: Crosses placenta; distributed into breast milk. Elimination: In urine. Half-Life: 2–3 h.

Nursing Implications

Assessment & Drug Effects

• Be aware that signs of developing tolerance or adaptation (with long-term use) include increased daytime anxiety, increased wakefulness during last one third of the night.
• Lab tests: Obtain periodic blood counts, urinalysis, and blood chemistries during long-term use.
• Do not use with addiction-prone patients (drug addicts, alcoholics) unless careful surveillance by health personnel is available. Habituation and dependence can occur.
• Evaluate smoking habit. As with other benzodiazepines, smoking may decrease hypnotic effects.
• Monitor for symptoms of overdosage: Slurred speech, somnolence, confusion, impaired coordination, and coma.

Patient & Family Education

• Do not drive or engage in potentially hazardous activities until response to drug is known.
• Avoid use of alcohol or other CNS depressants while on this drug; they may increase sedative effects.
• Do not stop taking drug suddenly, especially if you are subject to seizures. Withdrawal symptoms may occur and range from mild dysphoria to more serious symptoms (e.g., tremors, abdominal and muscle cramps, convulsions). Consult physician for schedule to discontinue therapy.
• Do not increase dose without physician's advice because of toxic potential of drug.

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Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug