estazolam

Absorption: Well absorbed following oral administration.

Distribution: Highly lipid-soluble. Crosses the blood-brain barrier.

Protein Binding: 93%.

Metabolism/Excretion: Mostly metabolized by the liver; metabolites do not have CNS depressant activity.

Half-Life: 10–24 hr.

Time/Action Profile ⬆ ⬇

(hypnotic activity)

ROUTE	ONSET	PEAK‡	DURATION
PO	15–30 min	2 hr	6–8 hr

‡Plasma level.

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity to estazolam or other benzodiazepines;
Lactation: Lactation.

Use Cautiously in:

Renal impairment;
Hepatic impairment;
History of depression;
History of drug abuse or suicide attempt;
OB: Use late in pregnancy can result in sedation (respiratory depression, lethargy, hypotonia) and/or withdrawal symptoms (hyperreflexia, irritability, restlessness, tremors, inconsolable crying, and feeding difficulties) in neonates;
Pedi: Safety and effectiveness not established in children;
Geri: Appears on Beers list. risk of cognitive impairment, delirium, falls, fractures, and motor vehicle accidents. Avoid use in older adults.

Adv. Reactions/Side Effects ⬆ ⬇

CV: chest pain

EENT: pharyngitis

GI: abdominal pain, dyspepsia, nausea

MS: back pain, lower extremity pain, stiffness

Neuro: drowsiness, headache, weakness, abnormal coordination, abnormal dreams, abnormal thinking, behavior changes, confusion, depression, dizziness, hallucinations, hypokinesia, hangover, malaise, nervousness, sleep-driving

Misc: ANAPHYLAXIS, physical dependence, psychological dependence

Interactions ⬆ ⬇

Drug-drug:

Additive CNS depression with alcohol, antihistamines, antidepressants, MAO inhibitors, other sedative/hypnotics (including benzodiazepines), or opioid analgesics.
Cimetidine or hormonal contraceptives may ↓ metabolism and ↑ effects of estazolam.
May ↓ efficacy of levodopa.
Rifampin or cigarette smoking ↑ metabolism and ↓ effectiveness.
Theophylline may antagonize the effectiveness of estazolam.

Drug-Natural Products:

Concomitant use of kava, valerian, chamomile, or hops can ↑ CNS depression.
See sedative interactions.
St. John's wort may affect estazolam levels and effectiveness; avoid use.

Route/Dosage ⬆ ⬇

PO (Adults ): 1 mg at bedtime; some patients may require 2 mg (range 0.5–2 mg). Debilitated or small elderly patients: may initiate at 0.5 mg, ↑ as needed.

Availability ⬆ ⬇

(Generic available)

Tablets: 1 mg; 2 mg

Assessment ⬆ ⬇

Assess sleep patterns prior to and periodically during therapy.
Prolonged therapy may lead to psychological or physical dependence. Restrict amount of drug available to patient, especially if patient is depressed, suicidal, or has a history of addiction.
Assess risk for addiction, abuse, or misuse prior to administration.

Implementation ⬆ ⬇

PO: Administer at bedtime.
Supervise ambulation and transfer of patients following administration. Remove cigarettes. Side rails should be raised and call bell within reach at all times.
Gradually taper to discontinue or reduce the dose to reduce risk of withdrawal reactions (mild dysphoria, insomnia, abdominal and muscle cramps, vomiting, sweating, tremors, convulsions). If patient develops withdrawal symptoms, pause taper or increase dose to previous tapered dose level; decrease dose more slowly. Some patients may require longer tapering period (weeks to >12 mo).

Patient/Family Teaching ⬆ ⬇

Advise patient to take medication as directed. Discuss the importance of preparing environment for sleep (dark room, quiet, avoidance of nicotine and caffeine). Gradual discontinuation may be required following prolonged therapy. May cause disturbed sleep for the first 2 nights following discontinuation.
May cause daytime drowsiness. Caution patient to avoid driving and other activities requiring alertness until response to medication is known. Inform patient to notify health care professional if sleep-related behaviors, (may include sleep-driving—driving while not fully awake after ingestion of a sedative-hypnotic product, with no memory of the event) occur.
Advise patient that estazolam is a drug with known abuse potential. Protect it from theft, and never give to anyone other than the individual for whom it was prescribed. Store out of sight and reach of children, and in a location not accessible by others.
Caution patients to avoid taking alcohol or other CNS depressants, including opioids, concurrently with this medication, may lead to overdose.
Rep: Advise females to avoid breastfeeding. Monitor infants exposed to estazolam during 2nd and 3rd trimester or immediately prior to or during childbirth for sedation (respiratory depression, lethargy, hypotonia) and/or flaccidity and symptoms of withdrawal (hypertonia, hyperreflexia, hypoventilation, irritability, tremors, diarrhea, vomiting). Inform women who take estazolam during pregnancy about the National Pregnancy Registry for Other Psychiatric Medications to monitor pregnancy outcomes in women exposed to estazolam during pregnancy. Enroll patient by calling 1-866-961-2388 or visiting online at https://womensmentalhealth.org/clinical-and-research-programs/pregnancyregistry/othermedications/.

Evaluation/Desired Outcomes ⬆ ⬇

Improvement in sleep pattern.

US Brand Names ⬆ ⬇

Contr. Subst. Schedule ⬆ ⬇

Code ⬆

NDC Code

0591- Actavis Pharma, Inc.
- 0591-0744- Estazolam
  - 0591-0744-01- 100 TABLET in 1 BOTTLE, PLASTIC (0591-0744-01)

0591- Actavis Pharma, Inc.
- 0591-0745- Estazolam
  - 0591-0745-01- 100 TABLET in 1 BOTTLE, PLASTIC (0591-0745-01)

51862- Mayne Pharma
- 51862-069- Estazolam
  - 51862-069-01- 100 TABLET in 1 BOTTLE (51862-069-01)

51862- Mayne Pharma
- 51862-070- Estazolam
  - 51862-070-01- 100 TABLET in 1 BOTTLE (51862-070-01)

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇