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Plasma levels of diazepam after parenteral and rectal administration in children
Insights
Rectal administration of diazepam solution effectively arrests seizures in children, achieving therapeutic plasma levels comparable to intramuscular routes. Suppositories resulted in lower drug concentrations and delayed absorption.
Area of Science:
- Pharmacology
- Pediatric Medicine
- Clinical Chemistry
Background:
- Diazepam is a common anticonvulsant for pediatric seizures.
- Understanding optimal diazepam administration routes in children is crucial for effective seizure management.
- Previous studies have shown variable absorption rates for different diazepam formulations.
Purpose of the Study:
- To compare plasma levels and pharmacokinetic profiles of diazepam following different routes of administration in children.
- To evaluate the efficacy of rectal diazepam solution in achieving therapeutic anticonvulsant plasma concentrations.
- To assess the safety and practicality of rectal diazepam administration for pediatric seizure control.
Main Methods:
- Gas chromatography with capillary samples was used to measure plasma concentrations of diazepam and N-desmethyldiazepam.
- Intravenous, rectal (solution and suppository), and intramuscular administration routes were studied in pediatric patients.
- Plasma level curves were analyzed for absorption and elimination rates.
Main Results:
- Intravenous diazepam showed rapid plasma level decline within the first hour.
- Rectal diazepam solution demonstrated absorption and elimination profiles similar to intramuscular administration.
- Diazepam suppositories yielded significantly lower plasma levels and delayed peak concentrations.
- Recurrent seizures in two children suggested therapeutic plasma levels are between 150-200 mug/liter.
- No significant adverse effects were observed with rectal administration.
Conclusions:
- Rectal administration of diazepam solution is a practical and effective method for arresting convulsions in children.
- This route achieves therapeutic plasma levels comparable to intramuscular administration.
- Diazepam suppositories are less effective due to lower and delayed drug absorption.
Abstract:
Plasma levels of diazepam and N-desmethyldiazepam were investigated in 19 children by a gas chromatographic method permitting the use of capillary sample. Intravenous administration was studied in 3 children and the plasma level curves showed a rapid decline during the first hour. Absorption and elimination after rectal administration of a solution in 16 children were similar to those after intramuscular administration. Diazepam given by suppository to 5 children gave much lower plasma levels and delayed time to peak levels. Recurrence of seizures in 2 children indicated that the anticonvulsants plasma level was of the order of 150 to 200 mug/liter. No significant side effects were observed. Thus rectal administration of a solution of diazepam is a practical method to arrest convulsions in children.