Classifications: anxiolytic; sedative-hypnotic; benzodiazepine; Therapeutic: antianxiety; sedative-hypnotic
Pregnancy Category: X
Controlled Substance: Schedule IV
1 mg, 2 mg tablets
Benzodiazepine whose effects (anxiolytic, sedative, hypnotic, skeletal muscle relaxant) are mediated by the inhibitory neurotransmitter
gamma-aminobutyric acid (GABA). GABA acts at the thalamic, hypothalamic, and limbic levels of CNS.
Benzodiazepines generally decrease the number of awakenings from sleep. Stage 2 sleep is increased with all benzodiazepines.
Estazolam shortens stages 3 and 4 (slow-wave sleep), and REM sleep is shortened. The total sleep time, however, is increased.
Short-term management of insomnia.
Known sensitivity to benzodiazepines; acute closed-angle glaucoma, primary depressive disorders or psychosis; abrupt discontinuation;
children <18 y; coma, shock, acute alcohol intoxication; pregnancy (category X), lactation.
Renal and hepatic impairment, renal failure; organic brain syndrome, alcoholism, benzodiazepine dependence, suicidal ideations,
CNS depression, seizure disorder, status epilepticus; substance abuse; shock, coma; dementia, mania, psychosis; myasthenia
gravis, Parkinson's disease; sleep apnea; open-angle glaucoma, GI disorders, older adult and debilitated patients; limited
pulmonary reserve, pulmonary disease, COPD.
Route & Dosage
Adult: PO 1 mg h.s. may increase up to 2 mg if necessary (some debilitated older adult patients should start with 0.5 mg h.s.)
- For older adult patients in good health, a 1 mg dose is indicated; reduce initial dose to 0.5 mg for debilitated or small
older adult patients.
- Dosage reduction also may be needed in the presence of hepatic impairment.
Adverse Effects (≥1%)CNS:
Headache, dizziness, impaired coordination, hypokinesia, somnolence,
hangover, weakness. CV:
Palpitations, arrhythmias, syncope (all rare). Hematologic:
. GI: Constipation
, xerostomia, anorexia, flatulence, vomiting. Musculoskeletal: Arthritis
, arthralgia, myalgia, muscle spasm.
may decrease metabolism of estazolam and increase its effects; alcohol
and other cns depressants
may increase drowsiness; CYP3A4 inhibitors (ketoconazole, itraconazole, nefazodone, diltiazem, fluvoxamine, cimetidine, isoniazid, erythromycin)
can increase concentrations and toxicity of estazolam; carbamazepine, phenytoin, rifampin, barbiturates
may decrease estazolam concentrations. Food: Grapefruit juice
>1 quart may increase toxicity. Herbal: Kava, valerian
may potentiate sedation.
Rapidly absorbed from GI tract. Onset:
2030 min. Peak:
2 h. Distribution:
Crosses rapidly into brain; crosses placenta; distributed into breast milk. Metabolism:
Extensively in liver. Elimination:
In urine. Half-Life:
Assessment & Drug Effects
- Monitor for improvement in S&S of insomnia.
- Assess for excess CNS depression or daytime sedation.
- Assess for safety, especially with older adult or debilitated patients, as dizziness and impaired coordination are known adverse
Patient & Family Education
- Learn adverse effects and report those experienced to the physician.
- Avoid using this drug in combination with other CNS depressant drugs or alcohol.
- Do not drive or engage in other potentially hazardous activities until response to drug is known.