1985 | J. G. Reves, M.D.,* Robert J. Fragen, M.D.,† H. Ronald Vinik, M.D.,‡ David J. Greenblatt, M.D.,§
Midazolam, an imidazobenzodiazepine derivative, is used as a premedicant, sedative, and anesthetic induction agent. Its unique chemical structure, with a fused imidazole ring, distinguishes it from other benzodiazepines in terms of pharmacological and kinetic properties. Midazolam is water-soluble in acidic form but highly lipophilic in vivo, leading to rapid absorption and entry into brain tissue. It has anxiolytic, hypnotic, anticonvulsant, muscle relaxant, and antegrade amnestic effects, with potency similar to diazepam. Midazolam's anxiolytic effect may be mediated through increased glycine inhibition, while its hypnotic effect involves GABA accumulation and occupation of benzodiazepine receptors. Midazolam also reduces cerebral metabolic rate and blood flow, potentially protecting against cerebral hypoxia. It causes respiratory depression, particularly in patients with chronic obstructive pulmonary disease, and can lead to apnea. Hemodynamic effects include a decrease in blood pressure and an increase in heart rate. Midazolam is rapidly eliminated, with a short duration of action, and is suitable for short-duration anesthesia. It is well-suited for premedication, intravenous sedation, and outpatient procedures due to its rapid onset and lack of significant side effects. Compared to thiopental, midazolam is less rapid-acting but offers advantages in terms of versatility and patient acceptance.Midazolam, an imidazobenzodiazepine derivative, is used as a premedicant, sedative, and anesthetic induction agent. Its unique chemical structure, with a fused imidazole ring, distinguishes it from other benzodiazepines in terms of pharmacological and kinetic properties. Midazolam is water-soluble in acidic form but highly lipophilic in vivo, leading to rapid absorption and entry into brain tissue. It has anxiolytic, hypnotic, anticonvulsant, muscle relaxant, and antegrade amnestic effects, with potency similar to diazepam. Midazolam's anxiolytic effect may be mediated through increased glycine inhibition, while its hypnotic effect involves GABA accumulation and occupation of benzodiazepine receptors. Midazolam also reduces cerebral metabolic rate and blood flow, potentially protecting against cerebral hypoxia. It causes respiratory depression, particularly in patients with chronic obstructive pulmonary disease, and can lead to apnea. Hemodynamic effects include a decrease in blood pressure and an increase in heart rate. Midazolam is rapidly eliminated, with a short duration of action, and is suitable for short-duration anesthesia. It is well-suited for premedication, intravenous sedation, and outpatient procedures due to its rapid onset and lack of significant side effects. Compared to thiopental, midazolam is less rapid-acting but offers advantages in terms of versatility and patient acceptance.