Comparison of CNS adverse effects between astemizole and chlorpheniramine in children: a randomized, double-blind

A Shanon1, W Feldman, L Leikin

  • 1Department of Pediatrics, Children's Hospital of Eastern Ontario, Ottawa, Canada.

Developmental Pharmacology and Therapeutics
|January 1, 1993
PubMed

Insights

This study found that common antihistamines chlorpheniramine and astemizole had no negative impact on children's cognitive performance or physical side effects. Both medications were well-tolerated, showing no significant adverse effects in children with allergic rhinitis.

Area of Science:

  • Pediatric Allergy and Immunology
  • Clinical Pharmacology
  • Neuroscience

Background:

  • Antihistamines are widely used to manage allergic rhinitis in children.
  • Concerns exist regarding potential central nervous system (CNS) side effects of older antihistamines like chlorpheniramine.
  • Newer antihistamines, such as astemizole, were developed with the aim of reduced CNS effects.

Purpose of the Study:

  • To evaluate and compare the central nervous system (CNS) side effects of chlorpheniramine and astemizole in pediatric patients.
  • To assess the impact of these antihistamines on cognitive functions including attention, memory, and motor skills.

Main Methods:

  • A prospective, randomized, double-blind, cross-over study design was employed.
  • 92 children aged 8-16 with allergic rhinitis participated, receiving either chlorpheniramine or astemizole over 13 weeks with a wash-out period.
  • Cognitive performance was assessed using tests for attention, memory, and motor coordination, alongside monitoring for physical side effects.

Main Results:

  • No significant differences in adverse effects were observed between chlorpheniramine and astemizole, or compared to baseline.
  • Cognitive assessments, including the visual retention test and continuous performance test, showed no significant drug effects.
  • A slight improvement in the visual aural digit span test was noted with astemizole treatment.

Conclusions:

  • The antihistamines chlorpheniramine and astemizole demonstrated no adverse effects on the cognitive performance of children.
  • Both medications were found to be safe and well-tolerated in the pediatric population studied.
  • These findings support the use of these antihistamines in children with allergic rhinitis without significant concern for CNS impairment.
Abstract

Related Concept Videos

Cholinergic Antagonists: Pharmacokinetics01:24

Cholinergic Antagonists: Pharmacokinetics

Cholinergic antagonists—such as antimuscarinics—are available in oral, topical, ocular, parenteral, and inhalational formulations. Most antimuscarinics are oral formulations,  while scopolamine is available as a topical patch, and ipratropium and tiotropium are available as inhalation aerosols or powders. Atropine, tropicamide, and cyclopentolate are topically instilled in the eye. Most antimuscarinics are lipid-soluble and readily absorbed from the gastrointestinal tract and the conjunctiva.
Antiasthma Drugs: Methylxanthines01:24

Antiasthma Drugs: Methylxanthines

Theophylline, a member of the methylxanthine class of bronchodilators, has long been used in asthma management. While its exact mechanism of action is not fully understood, it is believed to have multiple effects on various cellular processes.
Theophylline is thought to inhibit phosphodiesterase enzymes, increasing intracellular levels of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP). This rise in cAMP and cGMP concentrations stimulates cardiac function,...
Antiasthma Drugs: Leukotriene Modifiers01:19

Antiasthma Drugs: Leukotriene Modifiers

Leukotriene modifiers, or cysteinyl leukotriene receptor antagonists, are medications used to manage chronic asthma. These agents target specific inflammatory mediators produced during arachidonic acid metabolism, an essential process in generating inflammation in the body.
Leukotriene modifiers work through two distinct mechanisms:
Antiasthma Drugs: Mast Cell Stabilizers and Anti-IgE Drugs01:25

Antiasthma Drugs: Mast Cell Stabilizers and Anti-IgE Drugs

Asthma is a chronic respiratory condition for which new therapeutic avenues, including anti-inflammatory drugs like mast cell stabilizers and anti-IgE treatments, continue to be developed.
Mast cell stabilizers, such as cromolyn (also known as sodium cromoglycate) and nedocromil (Tilade), are effective drugs in asthma management. These stabilizers hinder histamine release by skillfully obstructing the activation of mast cells and other cellular entities. Notably, they navigate this task without...
Chemotherapy-Induced Nausea and Vomiting: 5-HT3 Receptor Antagonists01:27

Chemotherapy-Induced Nausea and Vomiting: 5-HT3 Receptor Antagonists

5-HT3 receptor antagonists, such as dolasetron, granisetron (Kytril), ondansetron (Zofran), and palonosetron (Axoli), are crucial in managing chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea. These drugs selectively block 5-HT3 receptors in the visceral vagal and spinal afferent nerves, chemoreceptor trigger zone, and the vomiting center. They have a rapid onset of action and can be given as a single dose before chemotherapy. Ondansetron and granisetron, in particular,...
Chemotherapy-Induced Nausea and Vomiting: Dopamine Receptor Antagonists01:29

Chemotherapy-Induced Nausea and Vomiting: Dopamine Receptor Antagonists

Dopamine receptor antagonists, also known as antipsychotic agents, are critical in managing chemotherapy-induced vomiting. These antiemetic agents block dopamine receptors in the chemoreceptor trigger zone (CTZ), inhibiting signal transmission to the vomiting center. Antipsychotic agents encompass phenothiazines (PTZ), butyrophenones, benzamides, and thienobenzodiazepines (Zyprexa), which are utilized for their antiemetic and sedative properties.
Phenothiazines, such as prochlorperazine...