ESTAZOLAM

brands

Class

• Neuroscience-based Nomenclature: GABA positive allosteric modulator (GABA-PAM)
• Benzodiazepine (hypnotic)

ESTAZOLAM commonly prescribed for

(Bold for FDA approved)

How ESTAZOLAM works

• Binds to benzodiazepine receptors at the GABA-A ligand-gated chloride channel complex

• Enhances the inhibitory effects of GABA

• Boosts chloride conductance through GABA-regulated channels

• Inhibitory actions in sleep centers may provide sedative hypnotic effects

How long until ESTAZOLAM works

• Generally takes effect in less than an hour

Notable Side Effects

• Sedation, fatigue, depression

• Dizziness, ataxia, slurred speech, weakness

• Forgetfulness, confusion

• Hyperexcitability, nervousness

• Rare hallucinations, mania

• Rare hypotension

• Hypersalivation, dry mouth

• Rebound insomnia when withdrawing from long-term treatment

Life Threatening Side Effects

• Respiratory depression, especially when taken with CNS depressants in overdose

• Rare hepatic dysfunction, renal dysfunction, blood dyscrasias

weight gain

unusual

sedation

common

What to do about ESTAZOLAM side effects

• Wait

• To avoid problems with memory, take estazolam only if planning to have a full night’s sleep

• Lower the dose

• Switch to a shorter-acting sedative hypnotic

• Switch to a non-benzodiazepine hypnotic

• Administer flumazenil if side effects are severe or life-threatening

usual dosage range

• 1–2 mg/day at bedtime

Dosage Forms

• Tablet 1 mg scored, 2 mg scored

long term use

• Not generally intended for long-term use

• Evidence of efficacy up to 12 weeks

habit forming

• Estazolam is a Schedule IV drug

• Some patients may develop dependence and/or tolerance; risk may be greater with higher doses

• History of drug addiction may increase risk of dependence

Renal Impairment

• Drug should be used with caution

Hepatic Impairment

• Drug should be used with caution

Cardiac Impairment

• Benzodiazepines have been used to treat insomnia associated with acute myocardial infarction

Elderly

• No dose adjustment in healthy patients

• Debilitated patients: recommended initial dose of 0.5 mg/day

Children and Adolescents

• Safety and efficacy have not been established

• Long-term effects of estazolam in children/ adolescents are unknown

• Should generally receive lower doses and be more closely monitored

Pregnancy

• Contraindicated for use in pregnancy

• Effective June 30, 2015, the FDA requires changes to the content and format of pregnancy and lactation information in prescription drug labels, including the elimination of the pregnancy letter categories; the Pregnancy and Lactation Labeling Rule (PLLR or final rule) applies only to prescription drugs and will be phased in gradually for drugs approved on or after June 30, 2001

• Infants whose mothers received a benzodiazepine late in pregnancy may experience withdrawal effects

• Neonatal flaccidity has been reported in infants whose mothers took a benzodiazepine during pregnancy

Breast Feeding

• Unknown if estazolam is secreted in human breast milk, but all psychotropics are assumed to be secreted in breast milk

• Recommended either to discontinue drug or bottle feed

• Effects on infant have been observed and include feeding difficulties, sedation, and weight loss