The Pharmacokinetics of Rectal Midazolam for Premedication in Children

Saint-Maurice, C; Meistelman, Claude; Rey, Elisabeth; Esteve, Cristina; Lauture, D. De; Olivé, G

doi:10.1097/00000542-198611000-00019

Cited by 120 publications

(38 citation statements)

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“…Saint-Maurice et al (1986) demonstrated therapeutically effective serum concentrations, a rapid time to peak serum concentrations (16 min) and a terminal elimination half-life similar to that observed after parenteral dosing following the rectal administration of 0.3 mg/kg diluted to 5.0ml with normal saline, in children. These data suggest that rectal administration of midazolam may be the preferable route when the drug is used as a premedication for the induction of anaesthesia in children.…”

Section: Rectal Administrationmentioning

confidence: 60%

Clinical Pharmacokinetics in Infants and Children A Reappraisal

Kearns

Reed

1989

Clinical Pharmacokinetics

174

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A significant increase in the knowledge base in paediatric clinical pharmacology has occurred over the past 2 decades and has largely been the result of important scientific and sociological advancements pertaining to paediatric therapeutics. Although the data on drug disposition in infants and children have increased considerably over the past few years, pharmacokinetic-pharmacodynamic interactions, particularly the effect of development on pharmacodynamics, remain poorly understood.The impact of developmental physiology on drug absorption, distribution, metabolism and elimination in infants and children is reviewed and contrasted to the determinants of clinical pharmacokinetics in neonates. The most notable differences in drug disposition between in/ants and children when compared with neonates and young adults centre around alterations in body water and serum protein composition and the affinity/capacity for hepatic biotransformation of xenobiotics.As opposed to examining the effect of age on the disposition of specific compounds, the differences in developmental pharmacology are highlighted by the review of important and/or emerging pharmacokinetic-pharmacodynamic controversies in infants and children. These include the issues of altered drug distribution and metabolism in cysticjibrosis, pharmacokinetic determinants of successful antimicrobial therapy in bacterial meningitis and the pharmacokinetic determinants of immunosuppression treatment with cyclosporin. The pharmacological differences which are characteristic of development in both infants and children are also reviewed by examination of considerations for clinical pharmacokinetic evaluations such as specific routes and techniques for both drug administration and determination of sampling strategies.Clinical pharmacokinetics will continue to function as a bridge between the generation of new information and the practical application of this knowledge. Consequently, pharmacokinetics provides a pharmacological tool for use in research and clinical care. The clinical application of this tool is examined by a review of the pertinent assumptions and limitations, as well as useful mathematical techniques for use in paediatric patients. Additionally, 'non-traditional' uses of clinical pharmacokinetics (forensic application and use to evaluate organ function) in infants and children are discussed as are considerations for research use of clinical pharmacokinetic data.

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Section: Rectal Administrationmentioning

confidence: 60%

Clinical Pharmacokinetics in Infants and Children A Reappraisal

Kearns

Reed

1989

Clinical Pharmacokinetics

174

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“…Midazolam has been shown to be rapidly absorbed from the rectum in children 35 36. However, no efficacy data have been published.…”

Section: How Should the Drug Be Given?mentioning

confidence: 99%

Benzodiazepines for prolonged seizures

Anderson

2010

Archives of Disease in Childhood - Education and Practice

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“…A satisfactory preanaesthetic level of sedation has been obtained by rectal application of midazolam in children (Saint-Maurice et al, 1986).…”

Section: Introductionmentioning

confidence: 97%

Pharmacokinetics of midazolam and alpha‐hydroxy‐midazolam following rectal and intravenous administration.

Clausen

Wolff

et al. 1988

Brit J Clinical Pharma

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1 In an open cross-over trial, plasma concentrations of midazolam were measured in eight healthy male volunteers following administration of 0.3 mg kg-' body weight given by the rectal and intravenous routes.2 Maximumplasma concentrations of 92-156 ng ml-' (mean 118 ng ml-) were recorded from 20 to 50 min (mean 31 min) after rectal application. The rectal bioavailability was 40-65% (mean 52%) and the terminal half-life was 114-305 min (mean 161 min). 3 A substantial first-pass hepatic effect was observed following rectal administration. 4 No systemic or local intolerance was noted. 5 In conclusion, the rectal route of administration provides a rapid and reliable absorption of midazolam.

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The Pharmacokinetics of Rectal Midazolam for Premedication in Children

Cited by 120 publications

References 0 publications

Clinical Pharmacokinetics in Infants and Children A Reappraisal

Clinical Pharmacokinetics in Infants and Children A Reappraisal

Benzodiazepines for prolonged seizures

Pharmacokinetics of midazolam and alpha‐hydroxy‐midazolam following rectal and intravenous administration.

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