Xlorfenamin

When ATH:
R06AB04

Pharmacological action

Gistaminovыh blocker H1-receptors, It has antiserotoninovoe, antihistamine, weak anticholinergic, sedation. Reduces the severity of allergic reactions, mediated through the action of histamine, reduces the permeability of capillaries, constricts blood vessels, eliminates swelling and congestion of the nasal mucosa, nasopharynx and paranasal sinuses; reduces local exudative manifestations, suppresses the symptoms of allergic rhinitis: chikhaniye, rhinorrhea, itchy eyes, nose. Valid – through 20-30 m, duration – 4-4.5 no.

Pharmacokinetics

Once inside chlorphenamine relatively slowly absorbed from the gastrointestinal tract. Cmax achieved through 2.5-6 no. Bioavailability is low – 25-50%. Treated effect “first pass” through the liver. Plasma protein binding – about 70%. Chlorphenamine is widely distributed in the organs and tissues of the body, CNS penetration.

Intensively metabolized in the liver with the formation of desmethyl- and didesmetilhlorfenamina. Unchanged drug and its metabolites are excreted primarily in the urine. Urinary incontinence depends on pH and flow rate of urine. The feces are determined only trace amounts chlorphenamine.

Chlorphenamine characterized by considerable interindividual variability of pharmacokinetic parameters: T1/2 It varies between 2 to 43 no.

In children, there is a faster absorption of chlorphenamine, a higher clearance and a shorter T1/2.

Testimony

As part of the combined drugs with allergic rhinitis, rinosinusopatii, vasomotor rhinitis, hay fever; infectious diseases and SARS, accompanied by rhinitis, rhinorrhea, sinusiti, rinofaringitom.

Dosage regimen

Individual, depending upon the dosage form.

Side effect

CNS: sedation (It may disappear after a few days of treatment), weakness, drowsiness, dystaxia; when used in high doses in children and possible paradoxical reactions, due to the stimulating effect on the central nervous system.

From the hematopoietic system: in a few cases – agranulocytosis, thrombocytopenia, pancytopenia, aplasticheskaya anemia.

Other: in a few cases – exfoliative dermatitis; possible manifestations of anticholinergic action (dry mouth, reduced secretion of the mucous membrane of the respiratory tract), double vision, strangury, constipation,

Contraindications

Hypersensitivity to chlorphenamine.

Cautions

Effects on ability to drive vehicles and management mechanisms

During treatment, patients should avoid driving vehicles and other activities, require high concentration and speed of psychomotor reactions.

Drug Interactions

Chlorphenamine phenytoin may interfere with the metabolism in the liver, which leads to an increase in its concentration in blood plasma.

In an application with drugs, having anticholinergic activity increases the risk of anticholinergic effects.

Ethanol enhances the sedative effect chlorphenamine.

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