ETIZOLAM

brands

Class

• Neuroscience-based Nomenclature: GABA Positive Allosteric Modulator (GABA-PAM) Thienodiazepine Derivative (closely related to benzodiazepines but structurally distinct)

ETIZOLAM commonly prescribed for

(Bold for FDA approved)

How ETIZOLAM 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

• Inhibits excessive neuronal activity in the amygdala, which is central to anxiety regulation, providing therapeutic effects in anxiety and panic disorders.

• Its effect on GABA-A receptors in the cerebral cortex and brainstem contributes to its hypnotic properties, making it effective for insomnia and other sleep disturbances.

How long until ETIZOLAM works

• While immediate relief is common, consistent dosing over several days may be required to achieve stable and sustained therapeutic benefits.

Notable Side Effects

• Sedation, fatigue, dizziness, ataxia, confusion, memory impairment

• Depression, irritability, nervousness

• Weakness, dry mouth, blurred vision

• Nausea, constipation

• (Rare) Hallucinations, mania

• (Rare) Hypotension, palpitations

• (Uncommon) Rash, itching

• (Uncommon) Headaches, sleep disturbances

Life Threatening Side Effects

• Respiratory Depression: Especially with CNS depressants or overdose

• Hepatic/Renal Dysfunction: Liver toxicity, kidney issues

• Blood Disorders: Leukopenia, thrombocytopenia (rare)

• Seizures: In overdose or withdrawal situations

weight gain

unusual

sedation

not usual

What to do about ETIZOLAM side effects

• Wait

• Wait

• Wait

• Lower the dose

• Take largest dose at bedtime to avoid sedative effects during the day

• Switch to another agent

usual dosage range

• Anxiety: 0.5–1 mg/day, typically in 2–3 divided doses

• Panic Disorders: 1–2 mg/day, divided into 2–3 doses

• Insomnia: 0.25–0.5 mg at bedtime

Dosage Forms

• Tablets: 0.25 mg, 0.5 mg, 1 mg

long term use

• Risk of dependence, particularly for treatment periods longer than 12 weeks and especially in patients with past or current polysubstance abuse.

habit forming

• Etizolam is a Schedule IV drug

• Patients may develop dependence and/or tolerance with long-term use

Renal Impairment

• Dose should be reduced

Hepatic Impairment

• Dose should be reduced

Cardiac Impairment

• Etizolam have been used to treat anxiety associated with acute myocardial infarction

Elderly

• Should receive lower doses and be monitored

Children and Adolescents

• Safety and efficacy not established in panic disorder

• For anxiety, children and adolescents should generally receive lower doses and be more closely monitored

• Long-term effects of etizolam in children/adolescents are unknow

Pregnancy

• Possible increased risk of birth defects when benzodiazepines are taken during pregnancy

• Because of the potential risks, Etizolam is not generally recommended as treatment for anxiety during pregnancy, especially during first trimester

• Drug should be tapered if discontinued

• 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

• Seizures, even mild seizures, may cause harm to the embryo/fetus

Breast Feeding

• Some drug is found in mother’s breast milk

• Recommended either to discontinue drug or bottle feed

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