Estazolam (estazolam)

Dosage of estazolam must be individualized, and the smallest effective dosage should be used (especially in geriatric or debilitated patients). Prolonged administration of estazolam should be avoided.

The usual initial adult dose of estazolam is 1 mg at bedtime, although some adults may require an initial 2-mg dose. In small, debilitated, and/or geriatric patients, an initial dose of 0.5 mg may be appropriate; however, limited evidence suggests that this dose may be only marginally effective in many geriatric patients, and the drug can be initiated in healthy geriatric patients at the 1-mg dose. After individual response has been determined, the dose may be increased gradually to 2 mg if needed. As with other benzodiazepines, abrupt withdrawal of estazolam therapy should be avoided since manifestations of withdrawal, including rebound insomnia, may be precipitated. If estazolam is to be discontinued after prolonged therapy (e.g., 6 weeks), the dosage should be tapered gradually.

Estazolam is administered orally at bedtime.

No dosing information is available for this tab.

No dosing information is available for this tab.

There is no enhanced messaging for this drug.

There are no contraindication interactions for this drug.

There are no severe interactions for this drug.

There are no moderate interactions for this drug.

There is no enhanced messaging for this drug.

There are no contraindication contraindications for this drug.

There are no severe contraindications for this drug.

There are no moderate contraindications for this drug.

There is no enhanced messaging for this drug.

There are no severe adverse reactions for this drug.

There are no less severe adverse reactions for this drug.

A boxed warning has been included in the prescribing information for all benzodiazepines describing the risks of abuse, misuse, addiction, physical dependence, and withdrawal reactions associated with all drugs in this class. Abuse and misuse can result in overdose or death, especially when benzodiazepines are combined with other medicines, such as opioid pain relievers, alcohol, or illicit drugs. Frequent follow-up with patients receiving benzodiazepines is important. Reassess patients regularly to manage their medical conditions and any withdrawal symptoms. Clinicians should assess a patient's risk of abuse, misuse, and addiction. Standardized screening tools are available (https://nida.nih.gov/nidamed-medical-health-professionals/screening-tools- resources/chart-screening-tools). To reduce the risk of acute withdrawal reactions, use a gradual dose taper when reducing the dosage or discontinuing benzodiazepines. Take precautions when benzodiazepines are used in combination with opioid medications.

Estazolam shares the toxic potentials of the benzodiazepines, and the usual precautions of benzodiazepine administration should be observed. (See Cautions in the Benzodiazepines General Statement 28:24.08.)

Hydroxylation of estazolam to form 4-hydroxyestazolam is catalyzed by the hepatic cytochrome P-450 (CYP) 3A isoenzyme, and concomitant use of estazolam with drugs (e.g., some azole antifungals agents, nefazodone, erythromycin, fluvoxamine) that inhibit this isoenzyme system may result in decreased estazolam metabolism and clearance and increased plasma estazolam concentrations. Although specific drug interaction studies are not available, the manufacturer states that caution should be exercised and estazolam dosage adjustment considered during concomitant use of the drug with CYP3A inhibitors (e.g., nefazodone, fluvoxamine, cimetidine, diltiazem, isoniazid, some macrolide antibiotics). Because itraconazole and ketoconazole are very potent CYP3A isoenzyme inhibitors, the manufacturer states that concomitant use of these drugs with estazolam is contraindicated.

For further information about potential interactions between benzodiazepines and drugs and foods affecting hepatic microsomal enzymes, see Drug Interactions in the Benzodiazepines General Statement 28:24.08.

No enhanced messaging available.

Benzodiazepines can cause fetal harm when administered to pregnant women (see Cautions: Pregnancy and Lactation, in the Benzodiazepines General Statement 28:24.08), and those used solely as hypnotics, such as estazolam, are contraindicated during pregnancy. The safety of estazolam during labor or delivery has not been established.

It is not known whether estazolam is distributed into milk in humans; however, estazolam and/or its metabolites are distributed into milk in rats. Because of the potential for serious adverse reactions to estazolam in nursing infants if it were distributed, a decision should be made whether to discontinue nursing or the drug, taking into account the importance of the drug to the woman.

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