ATC Group: R06AX Other antihistamines for systemic use

Acrivastine, a structural analog of triprolidine hydrochloride, exhibits H₁-antihistaminic activity in isolated tissues, animals, and humans, and has sedative effects in humans. The propionic acid derivative of acrivastine is a metabolite in several animal species (as well as in man) and also exhibits H₁-antihistaminic activity.

Antazoline is an antagonist of histamine H1 receptors. It selectively bind to but does not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine.

Astemizole is an antihistamine drug, used to prevent sneezing, runny nose, itching and watering of the eyes, and other allergic symptoms.

Azelastine, a phthalazinone derivative is classified as a potent long-acting anti-allergic compound with selective H₁ antagonist properties. An additional anti-inflammatory effect could be detected after topical ocular administration. Data from in vivo (pre-clinical) and in vitro studies show that azelastine inhibits the synthesis or release of the chemical mediators known to be involved in early and late stage allergic reactions e.g. leukotriene, histamine, PAF and serotonin.

Bilastine is a non-sedating, long-acting histamine antagonist with selective peripheral Η₁ receptor antagonist affinity and no affinity for muscarinic receptors.

Cyproheptadine is a first generation antihistamine which also has anticholinergic and antiserotonergic activities that is used to treat allergic conditions including seasonal rhinitis, conjunctivitis, dermatitits and urticaria.

Desloratadine is a non-sedating, long-acting histamine antagonist with selective peripheral H₁-receptor antagonist activity. After oral administration, desloratadine selectively blocks peripheral histamine Η₁-receptors because the substance is excluded from entry to the central nervous system.

Ebastine has been shown to produce a rapid and long-lasting inhibition of histamine-induced effect and to have a strong affinity towards H₁-receptors.

Epinastine is a topically active, direct H₁-receptor antagonist and an inhibitor of the release of histamine from the mast cell. Epinastine is selective for the histamine H₁-receptor and has affinity for the histamine H₂receptor. Epinastine also possesses affinity for the α₁, α₂, and 5-HT₂–receptors.

Fexofenadine is a non-sedating H₁ antihistamine. Fexofenadine is a pharmacologically active metabolite of terfenadine.

Ketotifen is a histamine H₁-receptor antagonist. In vivo animal studies and in vitro studies suggest the additional activities of mast cell stabilisation and inhibition of infiltration, activation and degranulation of eosinophils.

Loratadine is a tricyclic antihistamine with selective, peripheral H₁-receptor activity. Loratadine has no clinically significant sedative or anticholinergic properties in the majority of the population and when used at the recommended dosage.

Mizolastine possesses antihistamine and antiallergic properties due to a specific and selective antagonism of peripheral histamine H₁ receptors.

Rupatadine is a second-generation antihistamine, long-acting histamine antagonist, with selective peripheral H1-receptor antagonist activity. Some of the metabolites (desloratadine and its hydroxylated metabolites) retain an antihistaminic activity and may partially contribute to the overall efficacy of the drug.