triazolam (Rx)

>10%

Drowsiness (14%)

1-10%

Headache (5-10%)

Dizziness (5-10%)

Nervousness (5-10%)

Ataxia (4-5%)

Lightheadedness (4-5%)

N/V (4-5%)

<1%

Anterogade amnesia

Paradoxical reactions

Travelers amnesia-especially if combined with EtOH

Confusion

Cramps

Fatigue

Memory impairment

Depression

Visual disturbance

Xerostomia

Anterograde amnesia

Dreaming/nightmares

Confusion

Contraindications

Documented hypersensitivity

Acute alcohol intoxication

Myasthenia gravis (allowable in limited circumstances)

Narrow angle glaucoma (questionable)

Severe respiratory depression

Depressed neuroses, psychotic reactions

IV use in shock, coma, depressed respiration, patients who recently received other respiratory depressants

Medications that significantly impair oxidative metabolism mediated by cytochrome P450 3A (CYP 3A) including ketoconazole, itraconazole, nefazodone, and several HIV protease inhibitors

Caution

Use caution in COPD, sleep apnea, renal/hepatic disease, open-angle glaucoma (questionable), impaired gag reflex, depression, suicide ideation

Anterograde amnesia may occur

Hypersensitivity reactions reported

Sleep related activities (sleep driving, sleep-cooking, sleep-eating etc) may occur

Hyperactive aggressive behavior may occur

May impair ability to perform hazardous tasks

Failure of insomnia to remit after 7 - 10 days of treatment may indicate presence of primary psychiatric and/or medical illness that should be evaluated

Increase in daytime anxiety may occur; consider therapy discontinuation if this occurs

Use caution and consider appropriate dose reduction when used concomitantly with weak or moderate CYP450 3A inhibitors

Use caution in patients with history of drug abuse or acute alcoholism; tolerance, psychological and physical dependence may occur with prolonged use

Therapy can cause drowsiness and a decreased level of consciousness; patients, particularly the elderly, are at higher risk of falls

Pregnancy Category: X

Lactation: Avoid if breastfeeding

Minor tranquilizers should be avoided in 1st trimester of pregnancy due to increased risk of congenital malformations

Maternal use shortly before delivery is associated with floppy infant syndrome (good and consistent evidence)

Prenatal benzodiazepine exposure slightly increased oral cleft risk (limited or inconsistent evidence)

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Depresses all levels of CNS (eg, limbic and reticular formation), possibly by increasing membrane permeability to chloride ions, which in turn increases the inhibitory activity of GABA on neuronal excitability.

Pharmacokinetics

Half-Life: 1.5-5.5 hr

Peak plasma time: 0.5-2 hr

Onset of action: 15-30 min

Vd: 0.8-1.8 L/kg

Protein binding: 89%

Duration: 6-7 hr

Peak plasma concentration: 1-6 ng/mL

Metabolism: CYP3A4, glucuronic acid conjugation

Metabolites: Inactive metabolites

Excretion: Urine