An increase in daytime anxiety may occur after as few as 10 days of continuous use, which may be related to withdrawal reaction in some patients. Anterograde amnesia may occur at a higher rate with triazolam than with other benzodiazepines. Use with caution in elderly or debilitated patients, patients with hepatic disease (including alcoholics), or renal impairment. Use with caution in patients with respiratory disease or impaired gag reflex. Avoid use in patients with sleep apnea.

Causes CNS depression (dose-related) resulting in sedation, dizziness, confusion, or ataxia which may impair physical and mental capabilities. Patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving). Use with caution in patients receiving other CNS depressants or psychoactive agents. Effects with other sedative drugs or ethanol may be potentiated. Benzodiazepines have been associated with falls and traumatic injury and should be used with extreme caution in patients who are at risk of these events (especially the elderly).

Use caution with potent CYP3A4 inhibitors, as they may significantly decreased the clearance of triazolam. Use caution in patients with depression, particularly if suicidal risk may be present. Use with caution in patients with a history of drug dependence. Benzodiazepines have been associated with dependence and acute withdrawal symptoms on discontinuation or reduction in dose. Acute withdrawal, including seizures, may be precipitated after administration of flumazenil to patients receiving long-term benzodiazepine therapy.

Paradoxical reactions, including hyperactive or aggressive behavior have been reported with benzodiazepines, particularly in adolescent/pediatric or psychiatric patients. Does not have analgesic, antidepressant, or antipsychotic properties.

>10%: Central nervous system: Drowsiness, anteriograde amnesia

1% to 10%:

Central nervous system: Headache, dizziness, nervousness, lightheadedness, ataxia

Gastrointestinal: Nausea, vomiting

<1%: Cramps, confusion, depression, euphoria, fatigue, memory impairment, pain, tachycardia, visual disturbance

CNS depressants: Sedative effects and/or respiratory depression may be additive with CNS depressants; includes ethanol, barbiturates, narcotic analgesics, and other sedative agents; monitor for increased effect

CYP3A4 inducers: CYP3A4 inducers may decrease the levels/effects of triazolam. Example inducers include aminoglutethimide, carbamazepine, nafcillin, nevirapine, phenobarbital, phenytoin, and rifamycins.

CYP3A4 inhibitors: May increase the levels/effects of triazolam. Example inhibitors include azole antifungals, ciprofloxacin, clarithromycin, diclofenac, doxycycline, erythromycin, imatinib, isoniazid, nefazodone, nicardipine, propofol, protease inhibitors, quinidine, and verapamil.

Isoniazid: Isoniazid may increase triazolam levels.

Levodopa: Therapeutic effects may be diminished in some patients following the addition of a benzodiazepine; limited/inconsistent data

Oral contraceptives: May decrease the clearance and increase the half-life of triazolam; monitor for increased triazolam effect

Ranitidine: Ranitidine may increase triazolam levels.

Theophylline: May partially antagonize some of the effects of benzodiazepines; monitor for decreased response; may require higher doses for sedation

Ethanol: Avoid ethanol (may increase CNS depression).

Food: Food may decrease the rate of absorption. Triazolam serum concentration may be increased by grapefruit juice; avoid concurrent use.

Herb/Nutraceutical: St John's wort may decrease levels. Avoid valerian, St John's wort, kava kava, gotu kola (may increase CNS depression).

Onset of action: Hypnotic: 15-30 minutes

Duration: 6-7 hours

Distribution: Vd: 0.8-1.8 L/kg

Protein binding: 89%

Metabolism: Extensively hepatic

Half-life elimination: 1.7-5 hours

Excretion: Urine as unchanged drug and metabolites

Children <18 years: Dosage not established

Adults:

Hypnotic: 0.125-0.25 mg at bedtime (maximum dose: 0.5 mg/day)

Preprocedure sedation (dental): 0.25 mg taken the evening before oral surgery; or 0.25 mg 1 hour before procedure

Elderly: Insomnia (short-term use): 0.0625-0.125 mg at bedtime; maximum dose: 0.25 mg/day (see Geriatric Considerations)

Dosing adjustment/comments in hepatic impairment: Reduce dose or avoid use in cirrhosis

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