Nitrazepam

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

Europe

Austria: Mogadon; Belgium: Mogadon, Nitrazepam; Bulgaria: Radedorm; Cyprus: Nitredon; Denmark: Apodorm, Mogadon, Nitrazepam, Pacisyn; Estonia: Radedorm; Finland: Insomin; France: Mogadon; Germany: Dormalon Nitrazepam, Dormo-Puren, Eatan N, Imeson, Mogadan, Nitrazepam, Novanox, Radedorm; Hungary: Eunoctin; Ireland: Mogadon, Nitrazepam; Italy: Mogadon; Latvia: Radedorm; Lithuania: Eunoctin, Radedorm; Luxembourg: Mogadon; Malta: Mogadon, Nitrazepam, Nitredon; Netherlands: Mogadon, Nitrazepam; Poland: Nitrazepam; Romania: Eunoctin, Nitrazepam; Slovenia: Cerson; Sweden: Apodorm, Mogadon, Nitrazepam; UK: Mogadon, Nitrazepam.

North America

Canada: Mogadon, Nitrazadon, Nitrazepam.

Latin America

Brazil: Nitrapan, Nitrazepam, Nitrazepol.

Asia

Japan: Benzalin, Cysvon, Hirusukamin, Nelbon, Nelurolen, Neuchlonic, Nitrazepam.

Drug combinations

Chemistry

Nitrazepam: C~15~H~11~N~3~O~3~. Mw: 281.27. (1) 2H-1,4-Benzodiazepin-2-one, 1,3-dihydro-7-nitro-5-phenyl-; (2) 1,3-Dihydro-7-nitro-5-phenyl-2H-1,4-benzodiazepin-2-one. CAS-146-22-5 (1966).

Pharmacologic Category

Anxiolytics, Sedatives, and Hypnotics; Benzodiazepines. (ATC-Code: N05CD02).

Mechanism of action

Binds to stereospecific benzodiazepine receptors on postsynaptic GABA neuron at CNS (limbic system, reticular formation). Enhances inhibitory effect of GABA on neuronal excitability by increasing neuronal membrane permeability to chloride ions.

Therapeutic use

Short-term management of insomnia. Myoclonic seizures.

Pregnancy and lactiation implications

Crosses placenta and is associated with increased risks of congenital malformations. Hypotonia, lethargy, feeding problems, and withdrawal symptoms reported with benzodiazepine use near time of delivery. Not recommended. Enters breast milk (not recommended during lactation).

Unlabeled use

Contraindications

Hypersensitivity to nitrazepam or any component of the formulation (cross-sensitivity with other benzodiazepines may exist). Myasthenia gravis. Narrow-angle glaucoma. Severe respiratory insufficiency. Sleep apnea syndrome. Severe hepatic insufficiency.

Warnings and precautions

Nitrazepam may induce anterograde amnesia. Should be used only after evaluation of potential causes of sleep disturbance. Failure of sleep disturbance to resolve after 7-10 days may indicate psychiatric or medical illness. May cause CNS depression, which may impair physical or mental abilities. Paradoxical reactions, including hyperactive or aggressive behavior, reported with benzodiazepines, particularly in adolescent/pediatric or psychiatric patients. Use with caution in depression, particularly if suicidal risk may be present, and in history of drug abuse or acute alcoholism; potential for drug dependency exists. Tolerance, psychological and physical dependence may occur with prolonged use. 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). Use with caution in patients receiving other CNS depressants or psychoactive medication (effects with other sedative drugs or ethanol may be potentiated). Bronchial hypersecretion and excessive salivation/drooling leading to aspiration pneumonia in young and elderly patients may occur rarely. Use with caution in hepatic/renal/respiratory impairment, in debilitated patients, and in the elderly (benzodiazepines associated with falls and traumatic injury). Associated with sudden death in children <5 years of age being treated for seizure disorders. Use should be restricted to children unresponsive to other antiepileptic agents. Does not have analgesic, antidepressant, or antipsychotic properties. Nitrazepam can cause false elevation (about 15%) of clozapine serum levels.

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