Histamine antagonists; Histamine receptor antagonists; Histamine receptor blocker
DefinitionThis section has been translated automatically.
Drugs that prevent or attenuate the histamine effect in allergic reactions by an antagonism at the histamine receptor or have a comparable antihistaminic effect:
- Sedative H1 antagonists (1st generation): clemastine, dexchloropheniramine, dimetindene, hydroxyzine, ketotifen, meclizine, promethazine, etc.
- Non-sedating H1 antagonists (2nd generation): Azelastine, Cetirizine, Desloratadine, Ebastine, Fexofenadine, Levocetirizine, Loratadine, Mequitazine, Mizolastine, Terfenadine, etc.
- Serotonin antagonists: Cyproheptadine and Ketotifen.
- Leukotriene antagonists: montelukast.
Pharmacodynamics (Effect)This section has been translated automatically.
Competitive antagonism at the H1 receptor: leads to relaxation of the vascular muscles, reduction of vascular permeability and attenuation of itching.
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Dosage and method of useThis section has been translated automatically.
The dosages are recommended according to the manufacturer's instructions. In general clinical applications and smaller studies in chronic therapy-resistant chronic urticaria as well as in pruritus sine materia, antihistaminic high-dose chemistries in monotherapy with desloratadine (4-fold standard therapy), in double or triple combination therapies with levocetericin/exofenadine, levocetericin/exofenadin/azelastine (double dose in each case) proved to be significantly more successful than standard dosed monotherapy.
Note(s)This section has been translated automatically.
Cave! Astemizole and terfenadine have now been withdrawn from the market in some countries due to cardiac side effects (torsade-de-pointes arrhythmias).
LiteratureThis section has been translated automatically.
- del Cuvillo A et al (2006) Comparative pharmacology of the H1 antihistamines. J Invest Allergol Clin Immunol 16: 3-12
- Schulz S et al (2009) Antipruritic efficacy of a high-dose antihistamine therapy. Dermatologist 60: 564-568