Clinical Pharmacokinetics of H1-Receptor Antagonists (The Antihistamines)

  title={Clinical Pharmacokinetics of H1-Receptor Antagonists (The Antihistamines)},
  author={David M. Paton and Dianne R. Webster},
  journal={Clinical Pharmacokinetics},
SummaryThis article reviews clinical pharmacokinetic data on the H1-receptor antagonists, commonly referred to as the antihistamines. Despite their widespread use over an extendnd period, relatively little pharmacokinetic data are available for many of these drugs.A number of H1-receptor antagonists have been assayed mainly using radioimmunoassay methods. These have also generally measured metabolites to greater or lesser extents. Thus, the interpretation of such data is complex. After oral… 

Pharmacokinetic Optimisation of Histamine H1-Receptor Antagonist Therapy

Information about the pharmacokinetics and pharmacodynamics of second-generation H1-RA, while still incomplete, is now sufficient to permit optimisation of therapy, and areas where more data are required are delineated.

Pharmacokinetic Optimisation of Antiemetic Therapy

Little work has been done on the influence of indicators of systemic disease on the pharmacokinetics of antiemetic drugs, apart from metoclopramide.

Lack of pharmacodynamic and pharmacokinetic interactions of the antihistamine ebastine with ethanol in healthy subjects

It is concluded that treatment with 20 mg ebastine once daily for one week provides steady concentrations of carebastine in plasma without impairment of skilled performance or important interactions with alcohol.

Second-Generation Antihistamines

Evidence does not suggest a primary role for these agents in the management of asthma, but it does support their use for asthmatic patients when there is coexisting allergic rhinitis, dermatitis or urticaria.

Pharmacokinetics of Loratadine in Patients with Renal Insufficiency

The disposition of lor atadine is not significantly altered in patients with severe renal insufficiency nor is hemodialysis an effective means of removing loratadine or descarboethoxylorat adine from the body.

The pharmacology and use of H1-receptor-antagonist drugs.

The second-generation H1-antagonist drugs are supplanting their predecessors in the treatment of allergic rhinoconjunctivitis and chronic urticaria and an even more favorable therapeutic index may be developed with the cloning of the gene encoding the H1 receptor and increased understanding of the precise structural requirements for H 1-receptor activity.

Safety of Antihistamines in Children

The availability of newer generation antihistamine compounds has clearly added to the clinical effectiveness and patient tolerance of a widely prescribed class of drugs and these advances have also been accompanied by improved safety profiles, particularly in the case of third generationAntihistamine overdose.

The pharmacokinetics and pharmacogenetics of the antiemetic cyclizine in palliative care patients.




Clinical Pharmacokinetics of Chlorpheniramine

  • M. Rumore
  • Medicine, Biology
    Drug intelligence & clinical pharmacy
  • 1984
The clinical pharmacokinetics of chlorpheniramine are reviewed and major issues that need further clarification are brought to optimize drug therapy with this antihistamine.

Oxatomide. A review of its pharmacodynamic properties and therapeutic efficacy.

A trial with oxatomide seems a potentially useful alternative in patients with conditions known or thought to be allergic in nature, in whom more established treatments were ineffective or poorly tolerated.

Metabolism of chlorpheniramine maleate in man.

The pharmacokinetics and metabolism of 3 H-chlorpheniramine maleate have been studied in man and it is concluded that the drug underwent an enterohepatic circulation and was extensively metabolized and excreted in the urine as mono- and didesmethyl chlor pheniramine, two unidentified metabolites and small amounts of chlorpheniramines.

Pharmacokinetics of promethazine and its sulphoxide metabolite after intravenous and oral administration to man.

Evidence is presented to support the hypothesis that S-oxidation of promethazine is predominantly an hepatic event and the role of the gut mucosa in S-Oxidation of phenothiazines is critically assessed.

Pharmacokinetics and efficacy of chlorpheniramine in children.

Terfenadine, the first non-sedating antihistamine.

In vitro and ex vivo experiments have shown terfenadine to associate/dissociate with histamine H1-receptors much more slowly than a classical competitive antihistamine, chlorpheniramine, and should prove to have significant clinical advantages for the symptomatic treatment of histamine-associated disorders.

The pharmacokinetics and antihistaminic effects of brompheniramine.

Bioavailability of d-pseudoephedrine and Azatadine from a Repeat Action Tablet Formulation

The data clearly demonstrate the bioequivalence of the repeat action tablets and the conventional tablets of d-pseudoephedrine and azatadine, and show no statistically significant differences in the measured bioavailability parameters.

Metabolic disposition of terfenadine in laboratory animals.

These studies demonstrated that terfenadine was readily absorbed and eliminated, virtually had undergone complete biotransformation and exhibited very low tissue concentrations per se.