Estazolam

Pronunciation

Pronunciation: ess-TAZZ-OH-lam
Class: Benzodiazepine

Trade Names

Estazolam
- Tablets 1 mg
- Tablets 2 mg

Pharmacology

Potentiates action of GABA, an inhibitory neurotransmitter, resulting in increased neuronal inhibition and CNS depression, especially in limbic system and reticular formation.

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Pharmacokinetics

Distribution

Plasma protein binding is 93%.

Metabolism

Extensively metabolized (4-hydroxy estazolam is the major metabolite).

Elimination

Metabolites primarily excreted in the urine with less than 5% of an administered dose excreted unchanged in the urine. Only 4% of the dose appears in the feces. Mean elimination t ½ varies from 10 to 24 h.

Indications and Usage

Short-term management of insomnia characterized by difficulty in falling asleep, frequent nocturnal awakenings, and/or early morning awakenings.

Contraindications

Pregnancy; hypersensitivity to benzodiazepines.

Dosage and Administration

Adults

PO Start with 1 mg at bedtime; however, some patients may need a 2 mg dose.

General Advice

  • Administer prescribed dose 30 min before bedtime.
  • Administer prescribed dose without regard to meals but administer with food if GI upset occurs.

Storage/Stability

Store tablets at controlled room temperature (below 86°F).

Drug Interactions

Alcohol, anticonvulsants, antihistamines, barbiturates, MAOIs, narcotics, phenothiazines, psychotropic drugs

May potentiate the CNS depressant effects of estazolam.

Azole antifungal agents (eg, ketoconazole), cimetidine, disulfiram, oral contraceptives, protease inhibitors (eg, indinavir)

Estazolam plasma levels may be elevated, increasing the pharmacologic and adverse effects.

Digoxin

May increase serum digoxin concentrations.

Rifamycins (eg, rifampin)

Estazolam plasma levels may be reduced, decreasing the pharmacologic effects.

Theophyllines

May antagonize sedative effects of estazolam.

Laboratory Test Interactions

None well documented.

Adverse Reactions

CNS

Somnolence (42%); hypokinesia (8%); dizziness (7%); abnormal coordination (4%); hangover (3%); confusion (2%); abnormal thinking (2%); anxiety (at least 1%).

Dermatologic

Pruritus (1%); Stevens-Johnson syndrome (postmarketing).

GI

Constipation, dry mouth (at least 1%).

Hematologic

Agranulocytosis (postmarketing).

Miscellaneous

Asthenia (11%); lower extremity pain (3%); photosensitivity (postmarketing).

Precautions

Monitor

Response to therapy

Frequently assess patient for response to treatment. Notify health care provider if condition does not appear to be improve or worsens.

Review therapy

Ensure that therapy is periodically reviewed to determine if it needs to be continued without change or if a dose change (eg, increase, decrease, discontinuation) is indicated.


Pregnancy

Category X .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

Use with caution in small or debilitated elderly patients.

Amnesia

As with other benzodiazepines, amnesia may occur.

Debilitated patients

Increased adverse reactions; start with lowest dose.

Depression

Use with caution in patients exhibiting signs and symptoms of depression. Suicidal tendencies may be present in such patients. The least amount of drug that is feasible should be dispensed.

Paradoxical reactions

Paradoxical reactions (eg, excitement, agitation) may occur.

Respiratory depression

Patients with compromised respiratory function may be at increased risk of respiratory depression.

Withdrawal

Signs and symptoms may occur following rapid or abrupt discontinuation. If treatment is to be discontinued or the dose reduced after prolonged therapy, gradually taper the dose. Monitor patient for withdrawal symptoms (eg, increased anxiety, tremor, muscle or abdominal cramps, sweating). If significant withdrawal symptoms develop, reinstitute previous dosing schedule and attempt a less rapid tapering regimen after patient has stabilized.

Overdosage

Symptoms

Somnolence, respiratory depression, confusion, impaired coordination, slurred speech, coma.

Patient Information

  • Advise patient or caregiver to read the patient information leaflet before starting therapy and with each refill.
  • Advise patient that medication may be started at a low dose and then gradually increased as tolerated until maximum benefit is obtained.
  • Caution patient that medication may be habit forming and to take as prescribed and not to stop taking or change the dose unless advised by health care provider.
  • Advise patient to take prescribed dose at bedtime with or without food but to take with food if stomach upset occurs.
  • Advise patient that if medication needs to be discontinued, it will be slowly withdrawn unless safety concerns (eg, rash) require a more rapid withdrawal.
  • Instruct patient to avoid alcoholic beverages and other depressants while taking this medication.
  • Instruct patient to contact health care provider if sleep disorder does not appear to be getting better, is getting worse, or if bothersome adverse reactions (eg, drowsiness, memory impairment) occur.
  • Advise patient that drug may cause drowsiness or impair judgment, thinking, or reflexes and to use caution while driving or performing other tasks requiring mental alertness until tolerance is determined. Caution patient that there may be residual daytime effects on performance from the dose taken the night before.
  • Advise women of childbearing potential to use effective contraception while using this medication.

Copyright © 2009 Wolters Kluwer Health.

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