Loratadine is an antihistaminergic drug with a tricyclic structure and a selective peripheral H-1-receptor activity [1]. Desloratadine is its primary active metabolite and is a non-sedating, long-acting histamine antagonist. After oral administration, desloratadine selectively blocks peripheral histamine H1-receptors
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چکیده
Loratadine is an antihistaminergic drug with a tricyclic structure and a selective peripheral H-1-receptor activity [1]. Desloratadine is its primary active metabolite and is a non-sedating, long-acting histamine antagonist. After oral administration, desloratadine selectively blocks peripheral histamine H1-receptors because the substance is excluded from entry to the central nervous system [2]. The antihistaminergic activity of desloratadine is 2.5 4 times as great as loratadine [3]. Loratadine and desloratadine have been approved for the Dutch market since 031989 and 01-2001, respectively [1]. Both drugs are indicated for the relief of symptoms associated with allergic rhinitis and chronic idiopathic urticaria [1,2]. Loratadine is marketed as an over-the-counter drug. Desloratadine is available on prescription. The Dutch SmPC of desloratadine mentions seizures as an adverse reaction: in the Dutch SmPC this is incorrectly and confusingly mentioned as “aanvallen”. No further information is given about the severity or incidence of this reaction [2]. In the Dutch SmPC of loratadine convulsions or seizures are not mentioned. The current observation describes the association between loratadine, desloratadine and convulsions.
منابع مشابه
Antihistaminic, Anti-Inflammatory, and Antiallergic Properties of the Nonsedating Second-Generation Antihistamine Desloratadine: A Review of the Evidence
The allergy cascade presents widespread inflammatory and proinflammatory activation, robust cytokine and chemokine signaling, and heterogeneous immune and endothelial responses that lead ultimately to the manifestations of allergic reaction. Histamine, a small peptide with inherent vasoactive properties, is released from granules contained within mast cells, basophils, lymphocytes, and other re...
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BACKGROUND The FDA recently moved loratadine (Claritin) from prescription only status to over-the-counter (OTC). In response to the availability of an OTC non-sedating antihistamine, many managed care organizations are reevaluating which if any prescription antihistamines should remain on formulary. From a managed care perspective, determining which of the remaining prescription antihistamines ...
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BACKGROUND The first generation antihistamines, such as diphenhydramine, are fairly potent muscarinic antagonists in addition to being H1 selective antihistamines. The antimuscarinic action is often not desirable since it is in part responsible for the drying of secretions in the airways and the sedative effect. We therefore examined a number of antihistamines for antimuscarinic effects on ion ...
متن کاملSynthesis of 3-hydroxy desloratadine, the hydroxyl metabolite of loratadine
The structure of a major active metabolite of the nonsedating antihistamine loratadine was confirmed by synthesis. The metabolite 3 was prepared from 3-methyl pyridine in twelve steps.
متن کاملA retrospective, open-label analysis of the population pharmacokinetics of a single 10-mg dose of loratadine in healthy white Jordanian male volunteers.
BACKGROUND Loratadine is a long-acting tricyclic antihistamine with selective peripheral histamine H(1)-receptor antagonist activity. Loratadine 10-mg tablets have been reported to be rapidly absorbed after once-daily administration for 10 days in healthy adult subjects, with a T(max) of 1.3 hours for loratadine and 2.5 hours for its major active metabolite, descarboethoxyloratadine. The t(1/2)...
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تاریخ انتشار 2009