Loratadin

General characteristics. Structure:

Active ingredient: 10 mg of a loratadin in 1 tablet.

Loratadin renders antihistaminic, antiallergic, anti-exudative, antipruritic action.

Pharmacological properties:

Pharmacodynamics. Selectively blocks H1 - histamine receptors and prevents action of a histamine on smooth muscles and vessels. Reduces permeability of capillaries, exudation, reduces an itch and an erythema.

The antiallergic effect begins to develop in 30 minutes after administration of drug inside, reaches a maximum in 8 — 12 hours and remains within not less than 24 hours. Loratadin does not influence the central nervous system, has no anticholinergic and sedative effect. Does not exert impact on QT interval on an ECG. Has weak bronchodilatory effect.

Pharmacokinetics. After intake it is quickly soaked up. Smakh of a loratadin in blood is created through 1,3chasa, its active metabolite (deskarboetoksiloratadin) – in 2,5 hours. Meal does not exert considerably impact on pharmacokinetics, (AUC of a loratadin can increase by 40%, and its active metabolite – for 15%), but Smakh for 1 hour slows down achievement time (it is recommended to accept drug after food). At concentration in plasma 2,5-100ngml of linkng with proteins makes 97% (an active metabolite of 73-77% at the level of 0,5-100 ng/ml).

Equilibrium concentration of a loratadin and its metabolite are reached by 5 days. It biotransformirutsya intensively in a liver by system of P450 cytochrome (preferential by means of CYP3A4 and to a lesser extent CYP2D6) with formation of an active metabolite. Within 24 hours about 30% of the general dose are removed with urine in the form of hydroxylated metabolites and/or conjugates. In 10 days about 80% in the form of metabolites are removed equally with urine (40%) and a stake (40%). T1/2 for a loratadin makes 3-20 hours (on average 8,4 hours), its active metabolite 8,8-92 hours (on average 28 hours). At alcoholic damage of a liver and at elderly people of T1/2 increases. The volume of distribution of a loratadin - 119l/kg, Cl-142-202ml/min/kg.

Within 24 hours of 27% of a loratadin it is removed with urine in the form of hydroxylated metabolites. Loratadin and his active metabolite easily gets into breast milk and through a placental barrier, creating in concentration milk equivalent to level in plasma. After reception in a dose of 40 mkg about 0,03% of drug in 48 hours get to mother's milk.

Indications to use:

Loratadin apply at allergic rhinitises (seasonal and year-round), allergic conjunctivitis, a pollinosis, a chronic idiopathic small tortoiseshell, a pruritic dermatosis (contact allergodermatita, chronic eczema), a Quincke's disease. Drug is used also at bronchial asthma (as supportive application), at allergic reactions to stings of insects, pseudo-allergic reactions to gistaminoliberator.

Route of administration and doses:

Drug is accepted inside. To adults and children 12 years are more senior appoint 10 mg (1 tablet) once a day. To children from 2 to 12 years of 5 mg (1/2 tablets) of 1 times a day. If the body weight of the child makes more than 30 kg, appoint 10 mg of 1 times a day.

Features of use:

Loratadin does not influence the speed of psychomotor reactions and does not cause sedation. However because of a possibility of development of side effects (drowsiness, fatigue, disturbance of concentration of attention, dizziness) during treatment drug is not recommended to be managed motor transport and other potentially dangerous types of activity demanding the increased concentration of attention and bystry psychomotor reaction.

Side effects:

Drug is rather well transferred. In rare instances dryness in a mouth, nausea, vomiting, gastritis, increased fatigue, a headache, drowsiness, disturbance of concentration of attention, dizziness, skin rash, an abnormal liver function can be observed.

Children have a nervousness, excitability or sedation. In isolated cases nervousness, a depression, a hyperkinesia, a tremor, paresthesia, a hypesthesia, a vision disorder, a slezootdeleniya, conjunctivitis, a nictitating spasm, eye and ears pain, a sonitus, spasms are possible. At persons with an abnormal liver function лоратадин can reduce clearance of creatinine, in isolated cases jaundice, hepatitis, a liver necrosis can develop.

Interaction with other medicines:

At simultaneous use of drug with ketokonazoly, erythromycin (CYP3A4 inhibitors), Cimetidinum (CYP3A4 and CYP2D6 inhibitor) notes increase in concentration of a loratadin in a blood plasma, however without any clinical manifestations. At the same time concentration of a ketokonazol and Cimetidinum in a blood plasma does not change whereas concentration of erythromycin decreases by 15%.

At a concomitant use with inductors of a microsomal oxidation (ethanol, Phenytoinum, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) efficiency of a loratadin decreases. Effect of alcohol on TsNS does not potentiate.

There are no data on safe use of a loratadin together with inhibitors of enzymes of a liver (guanidine, флукозанол, fluoxetine) therefore to apply with care.

Contraindications:

Hypersensitivity to drug.

Drug use is not recommended to children under 2 years.

Loratadin is allocated with breast milk, at purpose of drug it is necessary to resolve an issue of the breastfeeding termination.

Safety of use of a loratadin for pregnant women is not established therefore it is necessary to appoint drug only if the estimated advantage for mother exceeds potential risk for a fruit.

Overdose:

Symptoms: at overdose development of drowsiness, tachycardia, headache is possible.

Treatment: there is no specific antidote. It is necessary to cause vomiting, using ipecacuanha syrup with the subsequent gastric lavage and/or use of absorbent carbon.

Issue conditions:

According to the recipe

Packaging:

Tablets on 10 mg, on 10 tablets in a blister strip packaging; on the 2nd blister strip packagings in a pack.