Loratadin

General characteristics. Structure:

Active ingredient: 10 mg of a loratadin.

 Excipients: cellulose microcrystallic, sugar milk (lactose), sodium carboxymethylstarch (sodium salt of a glikolyat of starch), calcium  stearate.

Antihistaminic drug which possesses antiallergic, antipruritic, antiexudative action. Reduces permeability of capillaries, edematization of fabrics warns, removes spasms of smooth muscles.

Pharmacological properties:

Pharmacodynamics. H1 blocker - histamine receptors (long action). Inhibits release of a histamine and C4 leukotriene from mast cells. Prevents development and facilitates the course of allergic reactions.

The antiallergic effect develops in 30 min., reaches a maximum in 8-12 h and lasts 24 h. Action duration is promoted considerably by an active metabolite дезлоратадин. Does not influence the central nervous system and does not cause accustoming (since does not get through a blood-brain barrier).

Pharmacokinetics. It is quickly and completely soaked up in digestive tract. The maximum concentration in a blood plasma is reached in 1,3-2,5 h; meal slows down it on 1 h. The maximum concentration 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 P450 CYP3A4 cytochrome and to a lesser extent CYP2D6.

Equilibrium concentration of a loratadin and metabolite in plasma are reached for the 5th days of introduction.
Does not get through a blood-brain barrier.

Elimination half-life of a loratadin - 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 h) and 11-38 h (17,5 h). At alcoholic damage of a liver the elimination half-life increases with increase in 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 edema, pruritic dermatosis; pseudo-allergic reactions, allergic reactions to stings of insects.

Route of administration and doses:

Inside. To children from 2 to 6 years (with body weight less than 30 kg): 1/2 tablets (5 mg) of 1 times a day.

To children of 6 years (with body weight more than 30 kg) and the adult: on 1 tablet of 1 times a day.

At patients with a liver and/or renal failure (clearance of creatinine <30 ml/min.) drug is used every other day on 10 mg.

People of advanced age do not have need for reduction of a dose.

Features of use:

During treatment it is necessary to abstain from occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

The undesirable phenomena which are listed below at use of a loratadin met frequency of ³2% and approximately with the same frequency, as at use from placebo ("baby's dummy").

At adults: a headache, fatigue, dryness in a mouth, drowsiness, gastrointestinal frustration (nausea, gastritis), and also allergic reactions in the form of rash. Besides, there were rare messages on an anaphylaxis, an alopecia, abnormal liver function, heartbeat, tachycardia.

At children seldom: headache, nervousness, sedative action.

Interaction with other medicines:

Erythromycin, Cimetidinum, кетоконазол increase concentration of a loratadin in a blood plasma, without causing clinical manifestations and without influencing an ECG.

Inductors of a microsomal oxidation (Phenytoinum, ethanol, barbiturates, зиксорин, rifampicin, phenylbutazone, tricyclic   antidepressants) reduce efficiency of a loratadin.

Contraindications:

Hypersensitivity, pregnancy, the lactation period, children's age (up to 2 years).

With care — a liver and/or renal failure (clearance of creatinine <30 ml/min.).

Overdose:

Symptoms: drowsiness, tachycardia, headache.

Treatment: induction of vomiting, gastric lavage, reception of absorbent carbon.

Storage conditions:

Period of validity: 2 years. Not to use after the expiry date specified on packaging. In the dry, protected from light place at a temperature not over 25 ºС.

Issue conditions:

Without recipe

Packaging:

Tablets of 10 mg. On 10 tablets in  a blister strip packaging or to bank polymeric. 1 planimetric packaging or bank together with   the application instruction in a pack cardboard.