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Published on: July 4, 2018
Absorption pharmacokinetics of clonidine nasal drops in children
Nicole Almenrader1, Peter Larsson, Maurizio Passariello
1Department of Anaesthesia and Intensive Care, University Hospital, Policlinico Umberto I, Rome, Italy. n.almenrader@gmail.com
Insights
Clonidine nasal drops show poor and inconsistent absorption in children, making them unsuitable for premedication. This study highlights the variability and delayed absorption of clonidine via the nasal route.
Area of Science:
- Pediatric Anesthesiology
- Pharmacokinetics
- Drug Delivery Systems
Background:
- Clonidine is a commonly used alpha2 agonist for pediatric premedication.
- Established pharmacokinetic data exists for oral, rectal, and intravenous clonidine administration.
- Nasal administration offers a potential alternative route for drug delivery.
Purpose of the Study:
- To investigate the absorption pharmacokinetics of clonidine administered as nasal drops in pediatric patients.
- To evaluate the efficacy and safety of clonidine nasal drops for premedication.
Main Methods:
- A study involving thirteen pediatric patients (ASA I) receiving clonidine (4 mcg x kg(-1)) intranasally post-anesthesia induction.
- Plasma clonidine levels were monitored over 12 hours.
- Analysis utilized liquid chromatography-mass spectrometry and computer-aided curve fitting.
Main Results:
- Clonidine nasal drops exhibited significant interindividual pharmacokinetic variability.
- Absorption was characterized by delays and limitations.
- Key pharmacokinetic parameters included a 95% CI for Cmax of 0.4-0.6 ng x ml(-1) and Tmax of 1.4-3.0 h.
Conclusions:
- Clonidine nasal drops demonstrate erratic absorption from the nasal mucosa in children.
- This route of administration is not recommended for pediatric premedication due to unpredictable absorption.
Background:
The alpha2 agonist clonidine has become a popular drug for premedication in children. Effects and pharmacokinetics after oral, rectal, and intravenous administration are well known. The aim of this study was to investigate the absorption pharmacokinetics of clonidine nasal drops in children.
Methods:
Thirteen ASA I pediatric patients received after induction of anesthesia 4 mcg x kg(-1) of clonidine by the nasal route. Blood samples were taken during a 12-h period and plasma levels of clonidine were analyzed by liquid chromatography-mass spectrometry. Data were calculated by a computer-aided curve-fitting program.
Results:
Plasma pharmacokinetics following administration of clonidine nasal drops showed a considerable interindividual variability and absorption was delayed and limited. A total of 95% confidence intervals for maximum plasma concentration and time to achieve maximum plasma concentration were 0.4-0.6 ng x ml(-1) and 1.4-3.0 h, respectively.
Conclusions:
Clonidine nasal drops are erratically absorbed from the nasal mucosa and, thus, this mode of drug administration is not recommended for premedication purposes.
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