Source: Υπουργείο Υγείας (CY) Revision Year: 2020 Publisher: GlaxoSmithKline Καταναλωτικά Προϊόντα Υγείας Ελλάς Μονοπρόσωπη Ανώνυμη Εταιρεία, διακριτικός τίτλος «GSK CH Ελλάς Μονοπρόσωπη Α.Ε.», 274 Kifissias Ave. , Halandri, 152 32 Athens, Greece Tel.: 210 6882100 ...
ATC Code: R06AB03
Pharmacotherapeutic group: Antihistamine (histamine H1-receptor antagonist)
Dimetindene is an antihistamine drug which belongs to the alkylamine group. Dimethindene maleate is a histamine H1-receptor antagonist which has a high binding affinity for these receptors and it also inhibits in vivo and in vitro the histamine effects induced by these receptors. Dimethindene has mild anticholinergic and sedative action.
It considerably reduces the hyper permeability of the capillaries, which are associated with immediate hypersensitivity reactions. As an antagonist of H1-receptors, dimetindene does not affect the histamine induced increase in gastric secretion.
In addition, dimethindene maleate has shown some evidence of antikinin and a weak anticholinergic activity.
In association with H2-antihistamines, dimethindene maleate suppresses virtually all circulatory effects of histamine.
In a histamine skin weal and flare study, the effect on skin reactions of a single dose of 4 mg dimethindene as drops was still measurable up to 24 hours post-administration.
The systemic bioavailability of dimethindene from drops is approximately 70%. Peak serum concentrations of dimethindene are reached within two hours after administration of oral solution The apparent half-life of elimination is about six hours.
At concentrations ranging from 0.09mg/ml to 2mg/ml, approximately 90% of dimethindene is bound to human plasma proteins.
Metabolic reactions include hydroxylation and methoxylation of the compound.
Dimethindene and its metabolites are eliminated by both the biliary and urinary routes. 5-10% of the administered dose is eliminated unmetabolized in the urine and the bile.
Preclinical data on the active substance reveal no special hazard for humans based on conventional studies of safety pharmacology, repeated dose toxicity genotoxicity, carcinogenic potential and reproduction toxicity.
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