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Published on: October 16, 2013
[Pharmacokinetics of local anesthetics in children]
1Département d'Anesthésie-Réanimation, Hôpital de Bicêtre, Le Kremlin-Bicêtre.
Insights
Children exhibit distinct local anesthetic pharmacokinetics compared to adults, necessitating careful dosing. Factors like protein binding and drug metabolism influence safe administration in pediatric patients.
Area of Science:
- Pharmacology
- Pediatric Anesthesiology
- Drug Metabolism
Context:
- Local anesthetics are widely used in pediatric surgical procedures.
- Significant anatomical and physiological variations exist between pediatric and adult patients.
- Understanding age-related pharmacokinetic differences is crucial for safe and effective anesthesia.
Purpose:
- To elucidate the age-dependent pharmacokinetic profiles of local anesthetics.
- To highlight the implications of these differences for clinical practice in children.
- To provide guidance on the selection and dosing of local anesthetics in pediatric populations.
Summary:
- Children demonstrate faster absorption and potentially higher Cmax of local anesthetics compared to adults.
- Larger volume of distribution, lower Cmax, and longer terminal half-life are observed in pediatric patients.
- Reduced protein binding in infants under 6 months increases the free fraction of drugs, requiring cautious use.
Impact:
- Informs precise dosing strategies for local anesthetics in pediatric patients.
- Highlights the need for individualized treatment based on age and physiological status.
- Contributes to improved patient safety and optimized anesthetic management in children.
Abstract:
Anatomical and physiological differences between children and adults may induce changes in absorption, distribution and elimination of local anesthetics throughout life. Absorption is faster and the Cmax may be higher in children than in adults. In addition, the volume of distribution is larger, and the Cmax is lower and the terminal half-life is longer in children than in adults. The low level of albumin and alpha-1-acid-glycoprotein until 6 months of life, may result in an increase in free fraction of drugs, as it has been demonstrated for bupivacaine. In clinical practice, the decrease in protein binding in infants may lead to careful use before the age of 6 months. It seems preferable to use drugs with moderate protein binding and high hepatic extraction ratio such as lidocaine; the repeated injection of epidural bupivacaine should be careful used because of the longer terminal half-life; maximum dosage regimens are for lidocaine 10 mg.kg-1 and for bupivacaine 2.5 mg.kg-1.
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