Quazepam

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Genes that may be involved
  • Substrate of
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

North America

USA: Doral.

Asia

Japan: Doral, Quazepam.

Drug combinations

Chemistry

Quazepam: C~17~H~11~ClF~4~N~2~S. Mw: 386.79. (1) 2H-1,4-Benzodiazepine-2-thione, 7-chloro-5-(2-fluorophenyl)-1,3-dihydro-1-(2,2,2-trifluoroethyl)-; (2) 7-Chloro-5-(o-fluorophenyl)-1,3-dihydro-1-(2,2,2-trifluoroethyl)-2H-1,4-benzodiazepine-2-thione. CAS-36735-22-5 (1976).

Pharmacologic Category

Anxiolytics, Sedatives, and Hypnotics; Benzodiazepines. (ATC-Code: N05CD10).

Mechanism of action

Binds to stereospecific benzodiazepine receptors on postsynaptic GABA neuron at several sites within CNS (limbic system, reticular formation). Enhances inhibitory effect of GABA on neuronal excitability by increasing neuronal membrane permeability to chloride ions, resulting in hyperpolarization and stabilization.

Therapeutic use

Insomnia.

Pregnancy and lactiation implications

Increased risk of congenital malformations following exposure to other benzodiazepines during the 1^st^ trimester. Withdrawal symptoms in neonate and neonatal flaccidity reported. Use during pregnancy contraindicated. Not recommended in nursing women.

Unlabeled use

Contraindications

Hypersensitivity to quazepam, other benzodiazepines, or any component of the formulation. Sleep apnea. Pregnancy. Use in narrow-angle glaucoma with other benzodiazepines.

Warnings and precautions

Benzodiazepines associated with anterograde amnesia. May cause CNS depression. Use with caution in patients receiving other CNS depressants or psychoactive medication (effects may be potentiated). Use of hypnotic/sedative agents for sleep associated with hypersensitivity reactions. Paradoxical reactions (hyperactive or aggressive behavior) reported, particularly in adolescent/pediatric or psychiatric patients. Increased risk for hazardous sleep-related activities. Use caution in depression (particularly if suicidal risk exists), in history of drug abuse or acute alcoholism (risk of drug dependency), and in hepatic/renal/respiratory impairment. Use with caution in impaired gag reflux, in debilitated patients, and in the elderly (risk of falls and traumatic injury). 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.

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