![]() ![]() Hepatic CYP3A4 activity appears in the liver during the first weeks of life it is thus lower in neonate than adult liver, resulting in reduced midazolam clearance (Cl) in neonates. Finally, this metabolite is glucuronidated before excretion into urine. Midazolam is mainly eliminated by hydroxylation to form 1-hydroxymidazolam by CYP3A4 and CYP3A5 enzymes. Bioavailability of midazolam is about 50% when absorbed directly through either oral or nasal mucosa. In adults, the half-life ( 1/2) of midazolam is 1.9 hours, which is 22-fold shorter than that of diazepam. Midazolam, which was approved for clinical use in 1976, acts as a sedative-hypnotic, is used in the treatment of refractory seizures, and induces anaesthesia. Benzodiazepines act at receptors by binding directly to a specific site that is distinct from that of GABA binding. receptors are responsible for most inhibitory neurotransmission in the central nervous system. Midazolam exerts most of its effects by interacting with inhibitory neurotransmitter receptors directly activated by GABA. Antianxiety properties are related to increasing the glycine inhibitory neurotransmitter. The sedative and anticonvulsant properties of midazolam are related to GABA accumulation and occupation of benzodiazepine receptors. Midazolam is one of the most widely used sedatives in the “neonatal intensive care unit”. It has anxiolytic, muscle relaxant, and anticonvulsant activity, now most widely used to generate anterograde amnesia and to stop prolonged seizures in children. Midazolam is a short-acting benzodiazepine with rapid onset of action. In conclusion, midazolam is a safe and effective drug which is employed as a sedative, as antiepileptic agent, for infants who are refractory to standard antiepileptic therapy, and as an anaesthetic. Respiratory depression and hypotension appear in a limited percentage of infants following intravenous infusion of midazolam. The adverse effects of midazolam in neonates are scarce: pain, tenderness, and thrombophlebitis may occur. ![]() ECMO therapy increases t 1/2, Cl, and Vd of midazolam several times. Disease affects the pharmacokinetics of midazolam in neonates multiple organ failure reduces the Cl of midazolam and mechanical ventilation prolongs the t 1/2 of this drug. Midazolam is usually administered intravenously when minimal sedation is required, intranasal administration of midazolam is employed. Information of midazolam as an anaesthetic in infants are very little. ![]() Midazolam acts as a sedative, as an antiepileptic, for those infants who are refractory to standard antiepileptic therapy, and as an anaesthetic. Midazolam is hydroxylated by CYP3A4 and CYP3A5 the activities of these enzymes surge in the liver in the first weeks of life and thus the metabolic rate of midazolam is lower in neonates than in adults. The volume of distribution (Vd) is 1.1 L/kg both in neonates and adults. In healthy neonates the half-life ( t 1/2) and the clearance (Cl) are 3.3-fold longer and 3.7-fold smaller, respectively, than in adults. This brief review describes midazolam's potential role in rapid tranquillisation via these routes, and discusses the risks and benefits of these options in order to help readers consider their places in regular clinical practice, particularly in light of the shortage of lorazepam injection.Midazolam is a benzodiazepine with rapid onset of action and short duration of effect. Healthcare providers who include IM midazolam in their rapid tranquillisation guidelines or policies need to ensure that clinicians using it have the necessary knowledge, skills and competencies surrounding its use including clinical sequelae and the use of the ‘antidote’ flumazenil. The absorption of intramuscular midazolam is erratic and it has an unpredictable propensity for causing profound oversedation. It has recently become available in a new formulation specifically designed for buccal administration, and is also available as a solution for injection. It is not available for oral administration as this route of administration leads to poor bioavailability. Midazolam is a short acting benzodiazepine. Benzodiazepines are mainstay medicines in rapid tranquillisation.
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