Loratadine instuction for use

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pharmachologic effect

The blocker of histamine H1 receptors. Has antiallergic, antipruritic, antiexudative action. Reduces the permeability of capillaries, prevents the development of edema of tissues, reduces the increased contractile activity of smooth muscles, due to the action of histamine.

Pharmacokinetics

When administered orally at a therapeutic dose, loratadine is rapidly absorbed from the gastrointestinal tract and almost completely metabolized in the body. Cmax loratadine in plasma is achieved after 1-1.3 h, the main active metabolite, descarbotoxyloratadine, - after about 2.5 h.
With simultaneous intake of food, the bioavailability of loratadine and descarbonethoxyloratadine increases by approximately 40% and 15%, respectively, the time to reach Cmax increased by about 1 hour, its values ​​for these substances remained unchanged.
The binding with plasma proteins of loratadine is high - about 98%, active metabolite - less pronounced.
On the average, T1 / 2 loratadine is 8.4 h, descarbethoxytoloratadine is 28 h (8.8-92 h).
About 80% of loratadine is excreted in the form of metabolites with urine and feces in equal proportions for 10 days, about 27% - with urine during the first day.

Indications

Seasonal and all-the-year-round allergic rhinitis, conjunctivitis, acute urticaria and Quincke's edema, symptoms of histaminergia caused by the use of histaminoliberates (pseudoallergic syndromes), allergic reactions to insect bites, complex treatment of itching dermatoses (contact allergic dermatitis, chronic eczema).

Contraindications

Pregnancy, lactation, children under 2 years, hypersensitivity to loratadin.

Dosage

Inside adults and children over 12 years of age, as well as with a body weight of more than 30 kg - 10 mg 1 time / day.
Children from 2 to 12 years with a body weight of less than 30 kg - 5 mg 1 time / day.

Side effects

On the part of the digestive system: rarely - dry mouth, nausea, vomiting, gastritis; in some cases - violations of the liver.
From the side of the central nervous system: rarely - increased fatigue, headache, excitability (in children).
From the cardiovascular system: rarely - tachycardia.
Allergic reactions: rarely - skin rash; in isolated cases - anaphylactic reactions.
Dermatological reactions: in some cases - alopecia.

Drug Interactions

With the simultaneous use of loratadine with drugs that inhibit the isoenzymes CYP3A4 and CYP2D6 or are metabolized in the liver with their participation (including cimetidine, erythromycin, ketoconazole, quinidine, fluconazole, fluoxetine), it is possible to change the concentration in blood plasma of loratadine and / or these preparations.
Inducers of microsomal oxidation (phenytoin, ethanol, barbiturates, zixorin, rifampicin, phenylbutazone, tricyclic antidepressants) reduce effectiveness.

special instructions

The use of loratadine can not completely exclude the development of seizures, especially in predisposed patients.
Patients with impaired renal or hepatic function require a correction of the dosing regimen.

Pregnancy and lactemia

Loratadine should not be used during pregnancy and lactation.
In experimental studies on animals, loratadine did not adversely affect the fetus in medium doses, and some fetotoxic effects were observed at high doses.

Application in childhood

Contraindicated in children up to 2 years.

In case of violations of kidney function

Patients with impaired renal or hepatic function require a correction of the dosing regimen.

With violations of liver function

Patients with impaired renal or hepatic function require a correction of the dosing regimen.