Loratadin

General characteristics. Structure:

Active ingredient: 5 mg of a loratadin in 5 ml of syrup.

Excipients: propylene glycol, Natrium benzoicum, food citric acid, sorbite food, the alcohol rectified additive vkusoaromatichesky, the water purified.

Pharmacological properties:

Pharmacodynamics. H1 blocker - histamine receptors (long action). Suppresses release of a histamine and C4 leukotriene from mast cells. Prevents development and facilitates the course of allergic reactions. Possesses antiallergic, antipruritic, antiexudative action. Reduces permeability of capillaries, edematization of fabrics warns.

The antiallergic effect develops in 30 min., reaches a maximum in 8-12 h and lasts 24 h. Does not influence TsNS (since does not get through GEB) and does not cause accustoming.

Pharmacokinetics. It is quickly and completely soaked up in a GIT. Cmax at elderly people increases for 50%, at alcoholic damage of a liver - with increase in disease severity. It is metabolized in a liver with formation of the main metabolite of a dezloratadin with the participation of isoenzymes of CYP3A4 cytochrome and to a lesser extent CYP2D6. Dezloratadin pharmacological is active and makes the significant contribution to clinical effect. Loratadin and дезлоратадин reach the maximum concentration in plasma (Tmax) between 1-1,5 h and 1,5-3,7 hours after administration of drug respectively. Loratadin contacts proteins for 97-99%, дезлоратадин to a lesser extent (73 – 76%).

Css of a loratadin and metabolite in plasma are reached on 5 days of introduction.

Does not get through a blood-brain barrier.

T1/2 of a loratadin is 3 - 20 h (on average 8,4), a dezloratadina - 8,8 - 92 h (on average 28 h); elderly patients respectively have 6,7 - 37 h (on average 18,2 h) and 11 - 38 h (17,5 h). At alcoholic damage of a liver of T1/2 increases in proportion to disease severity.

It is removed by kidneys and with bile.

At patients with a chronic renal failure and when carrying out a hemodialysis the pharmacokinetics practically does not change.

Indications to use:

Allergic rhinitis (seasonal and year-round), conjunctivitis, pollinosis, small tortoiseshell (including chronic idiopathic), Quincke's disease, pruritic dermatosis; the pseudo-allergic reactions caused by release of a histamine; allergic reactions to stings of insects.

Route of administration and doses:

Inside, not less than for 1 h to food. To adults and children 12 years with body weight more than 30 kg - on 10 mg of 1 times a day (2 teaspoons of syrup) are more senior. At a liver failure an initial dose - 5 mg of 1 times a day.

To children aged from 2 up to 12 years with body weight less than 30 kg – 5 mg of 1 times a day (1 teaspoon).

Features of use:

It is recommended to cancel treatment not less than in 1 week prior to conducting skin test on allergens.

Pregnancy and lactation. Safety of use of a loratadin during pregnancy is not established therefore its use is possible only in that case when the estimated advantage for mother exceeds potential risk for a fruit. Loratadin is allocated with breast milk therefore at purpose of drug in the period of a lactation it is necessary to resolve an issue of the breastfeeding termination.

Influence on ability to driving of motor transport and control of mechanisms. During treatment it is necessary to be careful at control of vehicles and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions because of risk of emergence of drowsiness. Further extent of restriction is established individually for each patient.

Side effects:

At adults: headache, dizziness, increased fatigue, tachycardia, increase in appetite, dryness of a mucous membrane of an oral cavity, drowsiness, nausea, gastritis, allergic reactions (rash), anaphylaxis, alopecia, abnormal liver function.

At children: a headache, the increased nervous irritability, sedation.

Interaction with other medicines:

At simultaneous use with ketokonazoly, erythromycin, Cimetidinum note increase in concentration of a loratadin in plasma, however without any clinical manifestations, including electrocardiographic.

Loratadin does not influence effect of ethanol on TsNS.

Contraindications:

Hypersensitivity to medicine components, the lactation period, children's age up to 2 years (because of availability of alcohol as a part of medicine).

With care: liver failure, pregnancy.

Overdose:

Symptoms of overdose are connected with anticholinergic action of a loratadin. In case of overdose are possible: headache, drowsiness, tachycardia.

Treatment: gastric lavage, reception of absorbent carbon, symptomatic and maintenance therapy. The hemodialysis is not effective, about efficiency of peritoneal dialysis information is absent.

Storage conditions:

In the place protected from light, at a temperature from 2 to 30 ºС. To store in the place, unavailable to children. A period of validity - 2 years. Not to apply after the termination of a period of validity.

Issue conditions:

Without recipe

Packaging:

In bottles on 50 ml or 100 ml, in packaging No. 1.