Midazolam

Table of contents

  • Brand Names
  • 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
  • Induces
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Midazolam; Belgium: Dormicum, Midazolam; Bulgaria: Dormicum, Midazolam; Cyprus: Dormicum, Midazolam; Czech Republic: Dormicum, Midazolam; Denmark: Dormicum, Midazolam; Estonia: Dormicum, Midazolam; Finland: Dormicum, Midazolam; France: Hypnovel, Midazolam, Versed; Germany: Dormicum, Midacalm, Midazolam; Greece: Dormicum, Dormixal; Hungary: Dormicum, Midazolam; Ireland: Midazolam; Italy: Ipnovel, Midazolam; Latvia: Dormicum, Fulsed, Midazolam; Lithuania: Dormicum, Fulsed, Midazolam; Luxembourg: Dormicum, Midazolam; Malta: Hypnovel, Midazolam; Netherlands: Dormicum, Midazolam; Poland: Dormicum, Midanium, Midazolam, Sopodorm; Portugal: Dormicum, Midazolam, Zolamid; Romania: Dormicum, Midazolam; Slovakia: Dormicum, Midazolam; Slovenia: Dormicum, Midazolam; Spain: Dormicum, Midazolam; Sweden: Dormicum, Midazolam; UK: Hypnovel, Midazolam.

North America

Canada: Midazolam; USA: Midazolam.

Latin America

Argentina: Dalam, Dormicum, Dormid, Drimnorth, Gobbizolam, Midazolam, Rem Chobet; Brazil: Dormire, Dormium, Dormonid, Midazolam; Mexico: Dormicum, Relacum, Zomsol.

Asia

Japan: Dormicum, Midazolam.

Drug combinations

Chemistry

Midazolam Hydrochloride: C~18~H~13~ClFN~3~ HCl. Mw: 362.23. (1) 4H-Imidazo[1,5-a][1,4]benzodiazepine, 8-chloro-6-(2-fluorophenyl)-1-methyl-, monohydrochloride; (2) 8-Chloro-6-(o-fluorophenyl)-1-methyl-4H-imidazo[1,5-a][1,4]benzodiazepine monohydrochloride. CAS-59467-96-8; CAS-59467-70-8 (midazolam)(1981).

Pharmacologic Category

Anxiolytics, Sedatives, and Hypnotics; Benzodiazepines. (ATC-Code: N05CD08).

Mechanism of action

Binds to stereospecific benzodiazepine receptors on postsynaptic GABA neuron. Enhancement of 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

Preoperative sedation; also provides conscious sedation prior to diagnostic or radiographic procedures. Intensive care unit sedation (continuous infusion). Intravenous anesthesia (induction and maintenance).

Pregnancy and lactiation implications

Crosses placenta. Not recommended for use during pregnancy or lactation.

Unlabeled use

Anxiety, status epilepticus.

Contraindications

Hypersensitivity to midazolam or any component of the formulation, including benzyl alcohol (cross-sensitivity with other benzodiazepines may exist). Parenteral form not for intrathecal or epidural injection. Narrow-angle glaucoma. Concurrent use of potent inhibitors of CYP3A4 (amprenavir, atazanavir, or ritonavir). Pregnancy.

Warnings and precautions

Benzodiazepines associated with anterograde amnesia. Might cause CNS depression. Might cause hypotension (might occur more frequently in patients who received opioid analgesics). Paradoxical reactions, including hyperactive or aggressive behavior reported with benzodiazepines, particularly in adolescent/pediatric or psychiatric patients. May cause severe respiratory depression, respiratory arrest, or apnea (use with extreme caution). Use with caution in heart failure, impaired gag reflux, renal impairment, respiratory disease; also in patients receiving other CNS depressants or psychoactive medication. Effects with other sedative drugs or ethanol may be potentiated. Use with caution in debilitated patients and in the elderly. Use with extreme caution in risk of falls, and in obese patients. Parenteral form contains benzyl alcohol. Does not have analgesic, antidepressant, or antipsychotic properties. Does not protect against increases in heart rate or blood pressure during intubation. Use caution when reducing dose or withdrawing therapy.

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