Trade Names:Estazolam- Tablets 1 mg- Tablets 2 mg
Potentiates action of GABA, an inhibitory neurotransmitter, resulting in increased neuronal inhibition and CNS depression, especially in limbic system and reticular formation.
Plasma protein binding is 93%.
Extensively metabolized (4-hydroxy estazolam is the major metabolite).
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.
Short-term management of insomnia characterized by difficulty in falling asleep, frequent nocturnal awakenings, and/or early morning awakenings.
Pregnancy; hypersensitivity to benzodiazepines.
PO Start with 1 mg at bedtime; however, some patients may need a 2 mg dose.
Store tablets at controlled room temperature (below 86°F).
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.
None well documented.
Somnolence (42%); hypokinesia (8%); dizziness (7%); abnormal coordination (4%); hangover (3%); confusion (2%); abnormal thinking (2%); anxiety (at least 1%).
Pruritus (1%); Stevens-Johnson syndrome (postmarketing).
Constipation, dry mouth (at least 1%).
Asthenia (11%); lower extremity pain (3%); photosensitivity (postmarketing).
MonitorResponse 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.
Category X .
Safety and efficacy not established.
Use with caution in small or debilitated elderly patients.
As with other benzodiazepines, amnesia may occur.
Increased adverse reactions; start with lowest dose.
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 (eg, excitement, agitation) may occur.
Patients with compromised respiratory function may be at increased risk of respiratory depression.
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.
Somnolence, respiratory depression, confusion, impaired coordination, slurred speech, coma.
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