Estazolam
- Atc Codes:N05CD04
- CAS Codes:29975-16-4
- PHARMGKB ID:29975-16-4
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
France: Nuctalon; Italy: Esilgan; Lithuania: Estazolam TC; Poland: Estazolam; Portugal: Kainever.
North America
USA: Estazolam.
Latin America
Brazil: Noctal; Mexico: Tasedan.
Asia
Japan: Estazolam, Eurodin.
Drug combinations
Chemistry
Estazolam: C~16~H~11~ClN~4~. Mw: 294.74. (1) 4H-[1,2,4]Triazolo[4,3-a][1,4]benzodiazepine, 8-chloro-6-phenyl-; (2) 8-Chloro-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepine. CAS-29975-16-4 (1990).
Pharmacologic Category
Anxiolytics, Sedatives, and Hypnotics; Benzodiazepines. (ATC-Code: N05CD04).
Mechanism of action
Binds to stereospecific benzodiazepine receptors on the postsynaptic GABA neuron at several sites within the CNS, 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.
Therapeutic use
Short-term management of insomnia.
Pregnancy and lactiation implications
Contraindicated during pregnancy or lactation.
Unlabeled use
Contraindications
Hypersensitivity to estazolam or any component of the formulation (cross-sensitivity with other benzodiazepines may exist). Pregnancy.
Warnings and precautions
Benzodiazepines have been associated with anterograde amnesia. May cause CNS depression. Use of hypnotic/sedative agents for sleep has been associated with hypersensitivity reactions including anaphylaxis as well as angioedema. Paradoxical reactions, including hyperactive or aggressive behavior, reported with benzodiazepines, particularly in adolescent/pediatric or psychiatric patients. Increased risk for sleep-related activities. Use caution in depression, particularly if suicidal risk may be present, in history of drug abuse or acute alcoholism (potential for drug dependency exists), in hepatic or renal impairment, in impaired gag reflux, and in respiratory disease. Use with caution in patients receiving other CNS depressants or psychoactive medication (effects with other sedative drugs or ethanol may be potentiated). High potential for CYP-mediated interactions. Use with caution in debilitated patients, and in the elderly (risk of falls and traumatic injury). Use with extreme caution in patients at risk of falls. Does not have analgesic, antidepressant, or antipsychotic properties. Rebound or withdrawal symptoms may occur following abrupt discontinuation or large decreases in dose. Flumazenil may cause withdrawal in patients receiving long-term benzodiazepine therapy.