-
The Journal of Emergency Medicine 1997Midazolam is a familiar agent commonly used in the emergency department to provide sedation prior to procedures such as laceration repair and reduction of dislocations.... (Review)
Review
Midazolam is a familiar agent commonly used in the emergency department to provide sedation prior to procedures such as laceration repair and reduction of dislocations. Midazolam is also effective in the treatment of generalized seizures, status epilepticus, and behavioral emergencies, particularly when intravenous access is not available. Midazolam is often employed as an induction agent for rapid sequence endotracheal intubation. Midazolam has a rapid onset of action following intravenous, intramuscular, oral, nasal, and rectal administration. Only 50% of an orally administered dose reaches the systemic circulation due to extensive first-pass metabolism. Midazolam is metabolized by the cytochrome P450 enzyme system to several metabolites including an active metabolite, alpha-hydroxymidazolam. Cytochrome P450 inhibitors such as cimetidine can profoundly reduce the metabolism of midazolam. Midazolam has a half-life of approximately 1 h, but this half-life may be prolonged in patients with renal or hepatic dysfunction. Midazolam has been associated with respiratory depression and cardiac arrest when used in combination with an opioid, particularly in the elderly, although all ages are at risk for respiratory depression. Midazolam is relatively free of side effects when used alone and offers several advantages over traditional pharmacological agents such as chloral hydrate and the combination of meperidine, chlorpromazine, and promethazine. Hiccups, cough, nausea, and vomiting are the most commonly reported adverse effects. Many of the adverse effects associated with midazolam can be reversed rapidly by the administration of flumazenil, a competitive benzodiazepine receptor antagonist. Midazolam is a safe and effective agent for providing sedation in the emergency department.
Topics: Conscious Sedation; Drug Interactions; Emergency Service, Hospital; Humans; Hypnotics and Sedatives; Metabolic Clearance Rate; Midazolam; Tissue Distribution
PubMed: 9258787
DOI: 10.1016/s0736-4679(97)00022-x -
European Journal of Heart Failure Oct 2022Benzodiazepines have been used as safe anxiolytic drugs for decades and some authors have suggested they could be an alternative for morphine for treating acute... (Randomized Controlled Trial)
Randomized Controlled Trial
AIMS
Benzodiazepines have been used as safe anxiolytic drugs for decades and some authors have suggested they could be an alternative for morphine for treating acute cardiogenic pulmonary oedema (ACPE). We compared the efficacy and safety of midazolam and morphine in patients with ACPE.
METHODS AND RESULTS
A randomized, multicentre, open-label, blinded endpoint clinical trial was performed in seven Spanish emergency departments (EDs). Patients >18 years old clinically diagnosed with ACPE and with dyspnoea and anxiety were randomized (1:1) at ED arrival to receive either intravenous midazolam or morphine. Efficacy was assessed by in-hospital all-cause mortality (primary endpoint). Safety was assessed through serious adverse event (SAE) reporting, and the composite endpoint included 30-day mortality and SAE. Analyses were made on an intention-to-treat basis. The trial was stopped early after a planned interim analysis by the safety monitoring committee. At that time, 111 patients had been randomized: 55 to midazolam and 56 to morphine. There were no significant differences in the primary endpoint (in-hospital mortality for midazolam vs. morphine 12.7% vs. 17.9%; risk ratio[RR] 0.71, 95% confidence interval [CI] 0.29-1.74; p = 0.60). SAE were less common with midazolam versus morphine (18.2% vs. 42.9%; RR 0.42, 95% CI 0.22-0.80; p = 0.007), as were the composite endpoint (23.6% vs. 44.6%; RR 0.53, 95% CI 0.30-0.92; p = 0.03).
CONCLUSION
Although the number of patients was too small to draw final conclusions and there were no significant differences in mortality between midazolam and morphine, a significantly higher rate of SAEs was found in the morphine group.
Topics: Humans; Adolescent; Midazolam; Morphine; Pulmonary Edema; Heart Failure; Hospital Mortality
PubMed: 35780488
DOI: 10.1002/ejhf.2602 -
Physiological Research Sep 2020Midazolam is a short acting sedative with small number of adverse effects. Administered orally, it is currently the most common form of conscious sedation in children....
Midazolam is a short acting sedative with small number of adverse effects. Administered orally, it is currently the most common form of conscious sedation in children. The objective of this paper is to describe effect of midazolam administered to children during dental treatment on their vital signs, and to monitor changes in children's behavior. We described values of vital signs and behavior in 418 sedations conducted in 272 children between 1-12 years of age. To achieve the following results, we used data from 272 all first-time sedations. After administration of midazolam arterial blood pressure and blood oxygen saturation decreased by values which were not clinically significant. The heart rate increased, with values staying within the limits of physiological range. The speed of onset of midazolam's clinical effects depends on age and dose. The lower age and dose correlated with the higher behavior score. The effectiveness of midazolam treatment is 97.8 %. Unwillingness of child to receive midazolam is predictor for disruptive behavior during sedation. 1.8 % of all sedation cases showed paradoxical reactions. The administration of midazolam in dose of 0.5 mg per 1 kg of child's body weight is safe and could be recommended for dental treatment in pediatric dentistry.
Topics: Administration, Oral; Child; Child Behavior; Child, Preschool; Conscious Sedation; Dentistry; Female; Humans; Hypnotics and Sedatives; Infant; Male; Midazolam; Vital Signs
PubMed: 33094628
DOI: 10.33549/physiolres.934511 -
European Review For Medical and... 2006Benzodiazepines have been involved during the years in the prevention and treatment of Post-Operative Nausea and Vomiting (PONV). Midazolam, a short acting... (Review)
Review
Benzodiazepines have been involved during the years in the prevention and treatment of Post-Operative Nausea and Vomiting (PONV). Midazolam, a short acting benzodiazepine widely used as a premedicant before surgery, for induction of anaesthesia, and for conscious sedation, has been particularly studied, sometimes with conflicting results. This paper will discuss the possible mechanisms of action of midazolam in PONV management and its fields of application (adults and children undergoing surgery, treatment of persistent postoperative emesis), as far as potentialities of other non-traditional anti-emetics, maybe ready to get out the arena of case reports, and the need of further studies on postoperative anti-emetics in their efficacy in treating established PONV.
Topics: Adult; Animals; Antiemetics; Child; Humans; Midazolam; Postoperative Nausea and Vomiting; Premedication; Randomized Controlled Trials as Topic
PubMed: 16875045
DOI: No ID Found -
Lancet (London, England) Jul 1988
Review
Topics: Adult; Aged; Cardiovascular Diseases; Flumazenil; Humans; Midazolam; Respiratory Insufficiency
PubMed: 2899192
DOI: No ID Found -
The American Journal of Hospice &... 1993
-
Neurotoxicity Research Jun 2022Central nervous system (CNS) dysfunction induced by sepsis and pathogenic microbial infections is reported to be closely associated with increased permeability of the...
Central nervous system (CNS) dysfunction induced by sepsis and pathogenic microbial infections is reported to be closely associated with increased permeability of the blood-brain barrier (BBB), which is mainly mediated by the stimulation of lipopolysaccharide (LPS) on inflammatory signaling. Midazolam is a novel sedative acting on the benzodiazepine receptor, which is recently reported to exert a neuroprotective effect by inhibiting inflammation. The present study will explore the potential repair capacity of Midazolam on LPS-induced damage to the BBB. The in vivo mice model was established by intraperitoneal injection of LPS, while the in vitro model was constructed by stimulating endothelial cells utilizing LPS. We found that the increased malondialdehyde (MDA) level and reduced superoxide dismutase (SOD) activity in the brain cortices, promoted serum concentration of inflammatory factors, and elevated BBB permeability were found in the LPS group, all of which were dramatically reversed by 1 mg/kg and 2 mg/kg Midazolam. Interestingly, Midazolam increased the expression of the tight junction protein zonula occludens-1 (ZO-1). In LPS-challenged in vitro human brain microvascular endothelial cells (HBMECs), the increased concentration of inflammatory factors, reduced trans-endothelial electrical resistance (TEER) level, elevated relative value of trans-endothelial permeability, and downregulated ZO-1 were observed, all of which were pronouncedly alleviated by Midazolam, accompanied by the inhibition on the Ras homolog family member A/ Rho-kinase 2 (RhoA/ROCK-2) pathway. Furthermore, the regulatory effects of Midazolam on ZO-1 expression and the endothelial monolayer permeability in LPS-challenged HBMECs were abolished by the overexpression of RhoA. Collectively, our data imply that Midazolam ameliorated the impairment of the BBB against LPS by regulating the RhoA/ROCK2 pathway.
Topics: Animals; Blood-Brain Barrier; Capillary Permeability; Endothelial Cells; Humans; Lipopolysaccharides; Mice; Midazolam
PubMed: 35451708
DOI: 10.1007/s12640-022-00508-4 -
Krankenpflege Journal 1996
Topics: Drug Interactions; Humans; Hypnotics and Sedatives; Midazolam; Patient Selection
PubMed: 8850856
DOI: No ID Found -
Clinical Pharmacy Jul 1987The chemistry, pharmacology, pharmacokinetics, clinical efficacy, adverse effects, drug interactions, dosage, and cost and availability of midazolam hydrochloride are... (Review)
Review
The chemistry, pharmacology, pharmacokinetics, clinical efficacy, adverse effects, drug interactions, dosage, and cost and availability of midazolam hydrochloride are reviewed. The anxiolytic, sedative, hypnotic, anticonvulsant, muscle-relaxant, and amnesic properties of midazolam are similar to those of other injectable benzodiazepines. Midazolam is approximately two to four times as potent as diazepam. Midazolam hydrochloride is water soluble (resulting in fewer local adverse reactions after injection), has a rapid onset and short duration of action, and causes relatively mild cardiovascular and respiratory effects. The drug generally is well tolerated. Midazolam is a good premedicant for general or regional anesthesia. Its greatest use will probably be for conscious sedation during surgical or diagnostic procedures performed under local or regional anesthesia. Induction of anesthesia with midazolam alone is somewhat unpredictable; opiate pretreatment makes induction more consistent. Midazolam is a less reliable induction agent than thiopental, but because it produces fewer adverse cardiovascular and respiratory effects than thiopental, midazolam appears to be a safer induction agent for elderly patients or patients with cardiovascular disease. The recommended dose of midazolam for preoperative sedation is 0.07-0.1 mg/kg given by intramuscular injection one hour before surgery. For conscious sedation, 0.1-0.15 mg/kg intravenously in divided doses is usually adequate. Lower doses of midazolam are recommended for elderly or debilitated patients and patients who have severe liver disease. The costs of equipotent doses of midazolam and injectable diazepam are similar. An oral dosage form is under investigation in the United States. Midazolam's pharmacologic and pharmacokinetic profile makes it an attractive alternative to other injectable benzodiazepines used in anesthesia.
Topics: Amnesia; Anesthesia; Anxiety; Cardiovascular System; Humans; Midazolam; Premedication; Respiration
PubMed: 3319363
DOI: No ID Found -
Paediatric Drugs Aug 2012Oromucosal midazolam (Buccolam™) is a benzodiazepine approved for the treatment of pediatric patients with acute, prolonged, convulsive seizures. This article reviews... (Review)
Review
Oromucosal midazolam (Buccolam™) is a benzodiazepine approved for the treatment of pediatric patients with acute, prolonged, convulsive seizures. This article reviews the pharmacologic properties of oromucosal midazolam and its clinical efficacy and tolerability for the treatment of prolonged acute convulsive seizures in pediatric patients aged 3 months to <18 years. Midazolam exerts its action by enhancing the effects of γ-aminobutyric acid (GABA) on GABA(A) receptors, resulting in neural inhibition. Oromucosal midazolam has a rapid onset (<10 minutes; due to rapid absorption across the buccal membrane and high lipophilicity) and short duration of effect (categorized by the short elimination half-life of midazolam and its active metabolite). The oromucosal administration of the drug avoids first-pass hepatic metabolism; as a result, it has a higher bioavailability than oral midazolam. Oromucosal midazolam is at least as effective at seizure cessation as rectal or intravenous diazepam and appears as well tolerated as these diazepam formulations in pediatric patients with acute convulsive seizures (additionally, midazolam has been available for use for decades in various formulations, and is historically well tolerated). Moreover, oromucosal midazolam was associated with a similar or shorter time to response than rectal diazepam. While the time to response was longer with oromucosal midazolam than with intravenous diazepam, the latter took significantly longer to apply than the former, leading to a significantly shorter overall controlling time with oromucosal midazolam. Respiratory depression occurred at a similar rate in recipients of oromucosal midazolam to that observed in recipients of rectal diazepam. Overall, oromucosal midazolam is at least as effective as rectal diazepam and as effective as intravenous diazepam in the treatment of children with prolonged acute convulsive seizures, and is generally well tolerated in this population. It has several advantages over rectal diazepam, the previous gold standard of treatment, such as having a more socially acceptable administration route and having a likely more predictable absorption profile. Oromucosal midazolam is a promising first-line treatment option for children with prolonged acute convulsive seizures, in particular where intravenous access is precluded.
Topics: Administration, Buccal; Adolescent; Anticonvulsants; Child; Child, Preschool; Drug Interactions; Humans; Infant; Midazolam; Seizures
PubMed: 22702742
DOI: 10.2165/11209320-000000000-00000