Diazepam

Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled 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
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Diazepam, Gewacalm, Psychopax, Stesolid, Valium; Belgium: Diazepam, Valium; Bulgaria: Diazepam, Relanium, Valium; Cyprus: Diazepam, Kratium, Remedium, Stesolid; Czech Republic: Apaurin, Diazepam; Denmark: Apozepam, Diazepam, Stesolid, Valaxona, Valium; Estonia: Diazepam, Diazepeks, Seduxen, Valocordin; Finland: Diapam, Diazepam, Medipam, Stesolid, Valium; France: Diazepam, Valium; Germany: Diazep, Diazepam, Faustan, Neurolytril, Stesolid, Valiquid, Valium; Greece: Apollonset, Atarviton, Diazepam, Stedon, Stesolid; Hungary: Diazepam, Seduxen, Stesolid; Ireland: Anxicalm, Diazemuls, Diazepam, Rimapam, Stesolid, Valium; Italy: Ansiolin, Diazemuls, Diazepam, Micronoan, Noan, Tranquirit, Valium; Latvia: Diazepeks, Relium, Seduxen; Lithuania: Apaurin, Diazepeks, Relanium, Relium, Seduxen; Luxembourg: Diazepam, Valium; Malta: Diazepam, Remedium, Stedon, Valium; Netherlands: Diazemuls, Diazepam, Stesolid; Poland: Diazepam, Neorelium, Relanium, Relsed, Valium; Portugal: Bialzepam, Diazepam, Metamidol, Stesolid, Unisedil, Valium; Romania: Calmpose, Diazepam; Slovakia: Apaurin, Diazepam; Slovenia: Apaurin; Spain: Diazepan, Stesolid, Valium; Sweden: Diazepam, Stesolid; UK: Diazemuls, Diazepam, Stesolid.

North America

Canada: Diastat, Diazemuls, Diazepam, Dipam, Valium, Vivol; USA: Diastat, Diazepam, Valium.

Latin America

Argentina: Cuadel, Daiv, Dezepan, Diactal, Diazepam, Dipezona, Fabotranil, Lembrol, Plidan, Rupediz, Saromet, Sicotop, Valium; Brazil: Ansilive, Calmociteno, Compaz, Diazefast, Diazepam, Dienpax, Kiatrium, Menostress, Noan, Uni Diazepax, Valium, Vetansil; Mexico: Alboral, Arzepam, Benzyme, Ifa-Fonal, Laxyl, Ortopsique, Relazepam, Valium, Zepan.

Asia

Japan: Azedipamin, Cellkam, Cercine, Diapax, Diapp, Diazepam, Horizon, Pealkit, Reliezen, Reliver, Serenamin, Serenzin, Sonacon.

Drug combinations

Diazepam and Otilonium Bromide

Diazepam and Sulpiride

Diazepam and Trimebutine

Diazepam, Amitriptyline, and Perphenazine

Diazepam, Metoclopramide, and Simethicone

Diazepam, Cellulase Enzyme, Dehydrocholic Acid, and Pancreatin

Diazepam, Aluminum Glycinate, Dicyclomine, Lidocaine, Magnesium Oxide, and Simethicone

Chemistry

Diazepam: C~16~H~13~ClN~2~O. Mw: 284.74. (1) 2H-1,4-Benzodiazepin-2-one, 7-chloro-1,3-dihydro-1-methyl-5-phenyl-; (2) 7-Chloro-1,3-dihydro-1-methyl-5-phenyl-2H-1,4-benzodiazepin-2-one. CAS-439-14-5 (1963).

Pharmacologic Category

Anticonvulsants; Benzodiazepines. Anxiolytics, Sedatives, and Hypnotics; Benzodiazepines. (ATC-Code: N05BA01).

Mechanism of action

Binds to stereospecific benzodiazepine receptors on the postsynaptic GABA neuron at several sites within the CNS. Enhancement of the inhibitory effect of GABA on neuronal excitability results by increased neuronal membrane permeability to chloride ions, thus resulting in hyperpolarization and stabilization.

Therapeutic use

Management of anxiety disorders, ethanol withdrawal symptoms. Skeletal muscle relaxant. Treatment of convulsive disorders. Also used for the management of refractory epilepsy patients on stable regimens of antiepileptic drugs requiring diazepam to control episodes of increased seizure activity (rectal gel).

Pregnancy and lactiation implications

Crosses the placenta. Associated with fetal malformations. Hypotonia, hypothermia, withdrawal symptoms, respiratory and feeding difficulties reported in the infant following use maternal use. Women should avoid pregnancy while taking this medication and should not breast-feed.

Unlabeled use

Panic disorders. Preoperative sedation, light anesthesia.

Contraindications

Hypersensitivity to diazepam or any component of the formulation (cross-sensitivity with other benzodiazepines may exist). Narrow-angle glaucoma. Avoid use in children <6 months of age (oral). Pregnancy.

Warnings and precautions

Associated with anterograde amnesia. May cause CNS depression or paradoxical reactions (hyperactive or aggressive behavior). Use with caution in depression (particularly in suicidal risk), history of drug abuse or acute alcoholism (risk of drug dependency), hepatic impairment, impaired gag reflux, renal impairment, respiratory disease, debilitated patients (active metabolites with extended half-lives may lead to delayed accumulation and adverse effects), obese patients (may have prolonged action when discontinued), the elderly, or patients at risk of falls. Effects with other sedative drugs or ethanol may be potentiated (use cautiously with other CNS depressants or psychoactive medication). Potential for CYP-mediated interactions. Acute hypotension, muscle weakness, apnea, and cardiac arrest have occurred with parenteral administration. Avoid use of the injection in shock, coma, or acute ethanol intoxication. Intra-arterial injection or extravasation of the parenteral formulation should be avoided. Parenteral formulation contains propylene glycol (risk of toxicity when administered in high dosages). Does not have analgesic, antidepressant, or antipsychotic properties. Withdrawal symptoms may occur following abrupt discontinuation.

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