No

Benzodiazepine

Short-term management of insomnia

C-IV

X

Hypersensitivity to this drug or any component of its formulation (cross-sensitivity with other benzodiazepines may exist); pregnancy

Use with caution in elderly or debilitated patients, patients with hepatic disease (including alcoholics), or renal impairment. Use with caution in patients with respiratory disease or impaired gag reflex. Avoid use in patients with sleep apnea. As a hypnotic, should be used only after evaluation of potential causes of sleep disturbance. Failure of sleep disturbance to resolve after 7-10 days may indicate psychiatric or medical illness. A worsening of insomnia or the emergence of new abnormalities of thought or behavior may represent unrecognized psychiatric or medical illness and requires immediate and careful evaluation.

Benzodiazepines have been associated with anterograde amnesia. Paradoxical reactions, including hyperactive or aggressive behavior, have been reported with benzodiazepines, particularly in adolescent/pediatric or psychiatric patients. Does not have analgesic, antidepressant, or antipsychotic properties.

Use caution in patients with depression, particularly if suicidal risk may be present. Use with caution in patients with a history of drug dependence. Benzodiazepines have been associated with dependence and acute withdrawal symptoms on discontinuation or reduction in dose. Acute withdrawal, including seizures, may be precipitated in patients after administration of flumazenil to patients receiving long-term benzodiazepine therapy.

>10%:

Central nervous system: Somnolence

Neuromuscular & skeletal: Weakness

1% to 10%:

Cardiovascular: Flushing, palpitations

Central nervous system: Anxiety, confusion, dizziness, hypokinesia, abnormal coordination, hangover, agitation, amnesia, apathy, emotional lability, euphoria, hostility, seizure, sleep disorder, stupor, twitch

Dermatologic: Dermatitis, pruritus, rash, urticaria

Gastrointestinal: Xerostomia, constipation, decreased appetite, flatulence, gastritis, increased appetite, perverse taste

Genitourinary: Frequent urination, menstrual cramps, urinary hesitancy, urinary frequency, vaginal discharge/itching

Neuromuscular & skeletal: Paresthesia

Otic: Photophobia, eye pain, eye swelling

Respiratory: Cough, dyspnea, asthma, rhinitis, sinusitis

Miscellaneous: Diaphoresis

<1%: Myalgia, neck pain, muscle spasm, drug dependence, allergic reactions, chills, fever

Symptoms of overdose include respiratory depression, hypoactive reflexes, unsteady gait, hypotension

Treatment for benzodiazepine overdose is supportive; rarely is mechanical ventilation required; flumazenil has been shown to selectively block the binding of benzodiazepines to CNS receptors, resulting in a reversal of benzodiazepine-induced CNS depression.

Carbamazepine, rifampin, rifabutin may enhance the metabolism of estazolam and decrease its therapeutic effect; consider using an alternative sedative/hypnotic agent

Cimetidine, ciprofloxacin, clarithromycin, clozapine, CNS depressants, diltiazem, disulfiram, digoxin, erythromycin, ethanol, fluconazole, fluoxetine, fluvoxamine, grapefruit juice, isoniazid, itraconazole, ketoconazole, labetalol, levodopa, loxapine, metoprolol, metronidazole, miconazole, nefazodone, omeprazole, phenytoin, rifabutin, rifampin, troleandomycin, valproic acid, verapamil may increase the serum level and/or toxicity of estazolam

Binds to stereospecific benzodiazepine receptors on the postsynaptic GABA neuron at several sites within the central nervous system, including the limbic system, reticular formation. Enhancement of the inhibitory effect of GABA on neuronal excitability results by increased neuronal membrane permeability to chloride ions. This shift in chloride ions results in hyperpolarization (a less excitable state) and stabilization.

Studies have shown that the elderly are more sensitive to the effects of benzodiazepines as compared to younger adults

Duration: Variable

Half-life: 10-24 hours (no significant changes in the elderly)

Peak serum levels: 0.5-1.6 hours

Adults: Oral: 1 mg at bedtime, some patients may require 2 mg; start at doses of 0.5 mg in debilitated or small elderly patients

Alcohol: Additive CNS effect, avoid use

Respiratory and cardiovascular status

No information available to require special precautions

Significant xerostomia occurs in up to 10% of patients. Disappears with cessation of drug therapy.

Use exactly as directed (do not increase dose or frequency or discontinue without consulting prescriber); may cause physical and/or psychological dependence. While using this medication, do not use alcohol or other prescription or OTC medications (especially, pain medications, sedatives, antihistamines, or hypnotics) without consulting prescriber. Maintain adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid intake). You may experience drowsiness, dizziness, or blurred vision (use caution when driving or engaging in tasks requiring alertness until response to drug is known); GI upset (take with water or milk). Report CNS changes (confusion, depression, increased sedation, excitation, headache, abnormal thinking, insomnia, or nightmares), altered voiding patterns or blood in urine, difficulty breathing, chest pain or palpitations, altered gait pattern, or ineffectiveness of medication. Pregnancy/breast-feeding precautions: Inform prescriber if you are pregnant. Do not get pregnant during therapy or for 1 month following therapy. Consult prescriber for instruction on appropriate contraceptive measures. This drug may cause severe fetal defects. Do not breast-feed.

Provide safety measures (ie, side rails, night light, and call button); remove smoking materials from area; supervise ambulation; avoid abrupt discontinuance in patients with prolonged therapy or seizure disorders

Tablet: 1 mg, 2 mg

Busto U, Bendayan R, and Sellers EM, "Clinical Pharmacokinetics of Nonopiate Abuse Drugs," Clin Pharmacokinet, 1989, 16(1):1-26.