Loratadin

General characteristics. Structure:

Acting substance: лоратадин 10 mg

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

Pharmacokinetics. It is quickly and completely soaked up in a GIT. TCmax is 1.3-2.5 h; meal slows down it on 1 h Cmax at elderly people increases for 50%, at alcoholic damage of a liver - with increase in disease severity. Communication with proteins of plasma - 97%. It is metabolized in a liver with formation of an active metabolite of a deskarboetoksiloratadin with the participation of isoenzymes of CYP3A4 cytochrome and to a lesser extent CYP2D6. Css of a loratadin and a metabolite in plasma are reached on 5 days of introduction. Does not get through GEB. T1/2 of a loratadin is 3-20 h (on average 8.4), an active metabolite - 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 HPN 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:

To adults and children with body weight more than 30 kg - on 10 mg of 1 times a day. At a liver failure an initial dose - 5 mg/days. To children from 2 to 12 years with body weight less than 30 kg - 5 mg/days in 1 reception.

Features of use:

During treatment it is necessary to be careful during the driving of motor transport and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

The undesirable phenomena met approximately the same frequency, as at use with placebo. At adults: a headache, increased fatigue, dryness in a mouth, drowsiness, nausea, gastritis, allergic reactions (rash), anaphylaxis, an alopecia, abnormal liver function. At children: a headache, the increased nervous irritability, sedation.

Interaction with other medicines:

CYP3A4 inhibitors (including кетоконазол, erythromycin), CYP3A4 and CYP2D6 inhibitors (Cimetidinum, etc.) increase concentration of a loratadin in blood. Inductors of a microsomal oxidation (Phenytoinum, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) reduce efficiency.

Contraindications:

Hypersensitivity, lactation period.

Overdose:

Symptoms: drowsiness, tachycardia, headache. Treatment: gastric lavage, reception of absorbent carbon.

Storage conditions:

List B. In the dry, protected from light place, at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

tablets of 10 mg (banks polymeric, planimetric strip packagings)