The common adverse effects associated with midazolam use are hiccoughs, cough, nausea, and vomiting. Midazolam has both hydrophilic and lipophilic properties, depending upon the pH. Age-related deficits, hepatic, and renal insufficiency, also affect the pharmacokinetics of midazolam. Almost all the pharmacologic effects, including sedation, anxiolysis, anterograde amnesia, and anticonvulsant effect, can are explainable through its action on GABA receptors. Midazolam acts on glycine receptors and produces a muscle-relaxing effect. The anticonvulsant activity of midazolam is related to the excess GABA action on motor circuits in the brain. Occupation of both the receptors cause membrane hyperpolarization and neuronal inhibition. It increases the frequency of chloride channel opening. Two separate receptors for GABA and benzodiazepine couple to a common chloride channel. The mechanism of action of midazolam indirect and is related to GABA accumulation and its affinity to the benzodiazepine receptors. Midazolam metabolism occurs via hepatic CYP450 enzymes and glucuronide conjugation. Midazolam has poor oral absorption and has an elimination half-life of 1.5 to 2.5 hours. Midazolam converts into its active metabolite alpha-1 hydroxy midazolam, which contributes to 10% of drug action. Midazolam is an adjunct medication to regional and local anesthesia for a wide range of diagnostic and therapeutic procedures and has greater patient and physician acceptance. Midazolam can be used for anxiolysis and hypnosis during the maintenance phase of general anesthesia and is also superior to thiopental in the maintenance of anesthesia because of the less need for adjunct medications. Because of its easy mode of administration through the buccal and intranasal routes, it is a viable option in children to manage seizures. For its use in anesthesia, the response to the induction dose is more variable compared to thiopental. Midazolam has a high rate of tolerance, and the dose can be increased to maintain the therapeutic effect.
Because of its water-soluble nature, midazolam has a rapid onset of action and can be used to manage status epilepticus when intravenous administration of other medications is not feasible. Intravenous midazolam is used for the induction of anesthesia and also in the management of acute seizures.
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