Clinical Pharmacology of New Histamine H1 Receptor Antagonists

  title={Clinical Pharmacology of New Histamine H1 Receptor Antagonists},
  author={F. Estelle R. Simons and Keith J. Simons},
  journal={Clinical Pharmacokinetics},
The recently introduced H1 receptor antagonists ebastine, fexofenadine and mizolastine, and the relatively new H1 antagonists acrivastine, astemizole, azelastine, cetirizine, levocabastine and loratadine, are diverse in terms of chemical structure and clinical pharmacology, although they have similar efficacy in the treatment of patients with allergic disorders.Acrivastine is characterised by a short terminal elimination half-life (t1/2,β) [1.7 hours] and an 8-hour duration of action… 

Skin concentrations of H1-receptor antagonists.

The results support the use of fexofenadine and indicate the need to re-examine the role of diphenhydramine in disorders in which the presence and the effects of H1-receptor antagonists in the skin are clinically relevant.

Clinical Pharmacokinetics and Pharmacodynamics of Desloratadine, Fexofenadine and Levocetirizine

Differences among the antihistamines in relation to a lack of significant interaction with drug transporter molecules and somnolence in excess of placebo may provide some advantages for the overall profile of desloratadine compared with fexofenadine and levocetirizine.

Pharmacology and clinical efficacy of desloratadine as an anti-allergic and anti-inflammatory drug

  • D. Agrawal
  • Biology, Medicine
    Expert opinion on investigational drugs
  • 2001
Clinically, desloratadine effectively controls both nasal and non-nasal symptoms of seasonal allergic rhinitis (SAR), including nasal congestion and is effective in the treatment of chronic idiopathic urticaria and improves quality of life and is well-tolerated.

Novel Antihistamines

Ebastine (1,2) is an effective non sedating H 1receptor antagonist marketed for the treatment of allergic rhinitis and urticaria and does not appear to interact with alcohol (ethanol), diazepam or cimetidine.


The therapeutic index of a histamine-1 (H1)antihistamine is the benefit-to-risk ratio of the medication and defines the range of doses and plasma concentrations over which the drug is effective and

A review of the second-generation antihistamine ebastine for the treatment of allergic disorders

Ebastine appears to be a safe, effective and well-tolerated second-generation antihistamine in the treatment of allergic rhinitis and chronic idiopathic urticaria.

Suppression of the early and late cutaneous allergic responses using fexofenadine and montelukast.

  • F. SimonsL. JohnstonX. GuK. Simons
  • Medicine
    Annals of allergy, asthma & immunology : official publication of the American College of Allergy, Asthma, & Immunology
  • 2001

Antipruritic effects of two different 5‐HT3 receptor antagonists and an antihistamine in haemodialysis patients

It is concluded that 5‐HT3 receptor blockers such as tropisetron and ondansetrons and the antihistamine cetirizine do not sufficiently reduce serotonin‐ and histamine‐induced itching in haemodialyis patients.

Cardiotoxicity of new antihistamines and cisapride.

The potential impact of 1st and 2nd generation antihistamines on male fertility

It is reported that the second-generation antihistamine cetirizine hydrochloride has potent and significant effects on male fertility compared with the first-generation H1 antihistamines pheniramine maleate through its changes in prolactin, LH, and FSH levels.



H1-Receptor Antagonists

A benefit-risk ratio or therapeutic index should be developed for each medication in this class of H1-antagonists, and the magnitude of the beneficial effects should be related to the severity of the unwanted effects, especially in the CNS and cardiovascular system.

Pharmacokinetic-Pharmacodynamic Relationships of H1-Antihistamines

This review is mainly devoted to second generation antihistamines that possess a low sedation potential compared with first generation compounds, and it is concluded that this type of approach for therapeutic optimisation is very fruitful and may enable large numbers of clinical studies to be avoided.

Pharmacokinetics of the H1-receptor antagonist ebastine and its active metabolite carebastine in healthy subjects.

Results strongly suggest that carebastine is responsible for the antihistamine activity after administration of ebastine.

Pharmacokinetics and pharmacodynamics of ebastine in children.

The in vivo potency and selectivity of azelastine as an H1 histamine-receptor antagonist in human airways and skin.

Cetirizine : A Reappraisal of its Pharmacological Properties and Therapeutic Use in Selected Allergic Disorders.

Cetirizine 10 mg/day appears to be as effective as conventional dosages of other established antihistamines such as astemizole, hydroxyZine, ketotifen, loratadine or terfenadine in relieving symptoms of these disorders, and is associated with a significantly lower incidence of sedation than hydroxyzine.

Effect of azelastine on bronchoconstriction induced by histamine and leukotriene C4 in patients with extrinsic asthma.

Longer blockade of H1 receptors did not attenuate the response to LTC4, suggesting that histamine and L TC4 act on bronchial smooth muscle through different receptors, suggests that bronchodilator effect was not present after 14 days of treatment.

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.

Cimetidine does not influence the metabolism of the H1-receptor antagonist ebastine to its active metabolite carebastine.

Ebastine is an H1-receptor antagonist with a relative lack of sedating properties and cimetidine coadministration did not induce any effect of ebastine on blood pressure and heart rate or cause sedation.