Clinical Pharmacology of New Histamine H1 Receptor Antagonists

@article{Simons1999ClinicalPO,
  title={Clinical Pharmacology of New Histamine H1 Receptor Antagonists},
  author={F. Estelle R. Simons and Keith J. Simons},
  journal={Clinical Pharmacokinetics},
  year={1999},
  volume={36},
  pages={329-352}
}
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… Expand
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Ebastine appears to be a safe, effective and well-tolerated second-generation antihistamine in the treatment of allergic rhinitis and chronic idiopathic urticaria. Expand
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Cardiotoxicity of new antihistamines and cisapride.
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References

SHOWING 1-10 OF 132 REFERENCES
H1-Receptor Antagonists
TLDR
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. Expand
Loratadine. A reappraisal of its pharmacological properties and therapeutic use in allergic disorders.
TLDR
Loratadine, with its attributes of once daily administration, fast onset of action and essentially nonsedating properties, would appear to be an appropriate first-line agent for the treatment of allergic rhinitis or urticaria. Expand
Comparison of the effects of single doses of the new H1-receptor antagonists loratadine and terfenadine versus placebo in children.
TLDR
This bioassay has been found to be ideal for determining the onset of action, potency, and duration of action of HIreceptor antagonists in children and to correlate with suppression of the symptoms of rhinoconjunctivitis. Expand
Pharmacokinetic-Pharmacodynamic Relationships of H1-Antihistamines
TLDR
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. Expand
Pharmacokinetics of the H1-receptor antagonist ebastine and its active metabolite carebastine in healthy subjects.
TLDR
Results strongly suggest that carebastine is responsible for the antihistamine activity after administration of ebastine. Expand
Pharmacokinetics and pharmacodynamics of ebastine in children.
TLDR
It is concluded that ebastine, an effective H1-receptor antagonist with a prompt onset of action and a long duration of action, is suitable for once-daily administration to children. Expand
Effect of the H2-antagonist cimetidine on the pharmacokinetics and pharmacodynamics of the H1-antagonists hydroxyzine and cetirizine in patients with chronic urticaria.
TLDR
Co-administration of hydroxyZine with cimetidine resulted in significantly increased serum hydroxyzine concentrations and increased wheal and flare suppression, thus confirming the rationale for a trial of concomitant administration of these medications in some patients with chronic urticaria unresponsive to treatment with an H1-antagonist alone. Expand
The in vivo potency and selectivity of azelastine as an H1 histamine-receptor antagonist in human airways and skin.
TLDR
The GM potency ratios derived from the PC20 values obtained for each patient indicated that the three increasing doses of azelastine displaced the histamine dose-response curve to the right by factors of 12.8, 54.4, and 50.2. Expand
Cetirizine : A Reappraisal of its Pharmacological Properties and Therapeutic Use in Selected Allergic Disorders.
TLDR
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. Expand
Effect of azelastine on bronchoconstriction induced by histamine and leukotriene C4 in patients with extrinsic asthma.
TLDR
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. Expand
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