temazepam (Rx)

1-10%

Drowsiness (9.1%)

Dizziness (4.5%)

Lethargy (4.5%)

Hangover (2.5%)

Diarrhea (1.7%)

Euphoria (1.5%)

Weakness (1.4%)

Confusion (1.3%)

Vertigo (1.2%)

< 1%

Amnesia

Angioedema

Blood dyscrasias

Sleep-related behavior (eg, sleep driving, sleep cooking, sleep eating)

Ataxia

Contraindications

Documented hypersensitivity

Acute alcohol intoxication

Narrow-angle glaucoma (questionable)

Caution

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

May impair ability to perform hazardous tasks

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

Anterograde amnesia may occur

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

Use in myasthenia gravis is allowed in limited circumstances

Use caution in severe respiratory depression and depressed neuroses, psychotic reactions

Paradoxical hyperactive aggressive behavior reported

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

May cause hyperactive or aggressive behavior

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.

Absorption

Peak plasma time: 2-3 hr

Peak plasma concentration: 260-210 ng/mL

Distribution

Protein bound: 96%

Vd: 1.4 L/kg

Metabolism

Metabolized by CYP3A4 (minor), glucuronic acid conjugation

Metabolites: Inactive

Elimination

Half-life elimination: 9.5-12.4 hr

Excretion: Urine (80-90%)