Pharmacotherapeutic group: anti-allergic agent – H1-histamine receptor blocker
ATC code: R06AX13
Pharmacological properties
Pharmacodynamics
H1-histamine receptor blocker (long action). Inhibits the release of histamine and leukotriene C4 from mast cells. Prevents the development and facilitates the course of allergic reactions. It has anti-allergic, antipruritic, antiexudative action. Reduces capillary permeability, prevents the development of tissue edema, relieves spasms of smooth muscles. Anti-allergic effect develops in 30 minutes, reaches its maximum in 8-12 hours and lasts for 24 hours. It does not affect central nervous system (as it does not penetrate through the blood-brain barrier) and is not addictive.
Pharmacokinetics
Fast and fully absorbed in the gastrointestinal tract. Time of reaching maximum concentration in blood plasma after drug intake is 1.3-2.5 hours; it is delayed by 1 hour with food intake. Maximum drug concentration in blood plasma is increased by 50% in elderly people, with alcoholic liver damage – with increase of disease severity. Binding with plasma proteins is 97%. It is metabolized in the liver with the formation of the active metabolite dekarboethoxyloratadine with the participation of cytochrome isoenzymes CYP3A4 and, to a lesser extent, CYP2D6. Equilibrium concentrations of loratadine and metabolite in plasma are reached by 5 days of administration. It does not penetrate the blood-brain barrier. Half-life of loratadine is 3-20 hours (on the average 8.4 hours), active metabolite – 8.8-92 hours (on the average 28 hours); for elderly patients – 6.7-37 hours (on the average 18.2 hours) and 11-38 hours (17.5 hours), respectively. In alcoholic liver damage the half-life increases in proportion to the severity of the disease.
Excreted by the kidneys and with bile. In patients with chronic renal failure and during hemodialysis pharmacokinetics practically does not change.
Indications
Active ingredient
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How to take, the dosage
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Synopsis
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Similarities
Weight | 0.015 kg |
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Shelf life | 5 years. Do not use after the expiration date. |
Conditions of storage | In a dry place at a temperature not exceeding 25 oC. Keep out of reach of children. |
Manufacturer | Akrihin HFC JSC, Russia |
Medication form | pills |
Brand | Akrihin HFC JSC |
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