ESTAZOLAM

ESTAZOLAM
(es-ta-zo'lam)
Classifications: anxiolytic; sedative-hypnotic; benzodiazepine;
Therapeutic: antianxiety
; sedative-hypnotic
Prototype: Lorazepam
Pregnancy Category: X
Controlled Substance: Schedule IV

Availability

1 mg, 2 mg tablets

Action

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.

Therapeutic Effect

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.

Uses

Short-term management of insomnia.

Contraindications

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.

Cautious Use

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

Insomnia
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.)

Administration

Oral
  • 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: Leukopenia, agranulocytosis. GI: Constipation, xerostomia, anorexia, flatulence, vomiting. Musculoskeletal: Arthritis, arthralgia, myalgia, muscle spasm.

Interactions

Drug: Cimetidine 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.

Pharmacokinetics

Absorption: Rapidly absorbed from GI tract. Onset: 20–30 min. Peak: 2 h. Distribution: Crosses rapidly into brain; crosses placenta; distributed into breast milk. Metabolism: Extensively in liver. Elimination: In urine. Half-Life: 10–24 h.

Nursing Implications

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 effects.

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.

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

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