Loratal

General characteristics. Structure:

Active ingredient: 10 mg of a loratadin.

Excipients: lactose, starch corn, magnesium stearate.

Pharmacological properties:

Pharmacodynamics. Лоратал® H1 of histamine receptors of the prolonged action is the selection blocker peripheral. The formed ligand - a receptor complex dissociates slowly, than and long antiallergenic effect of drug speaks. Inhibits release of a histamine and C4 leukotriene from mast cells, suppresses a chemotaxis of eosinophils and aggregation of thrombocytes. Prevents development and facilitates the course of allergic reactions. Shows the complex action including antiallergic anti-exudative and antipruritic activity, reduces permeability of capillaries.

Improvement of a condition of most of patients is observed within the first 30 minutes after reception of Loratala®. The antiallergic effect develops within the first 30 minutes after administration of drug, reaches a maximum within 8 – 12 hours and 24 hours last. Loratadin and his metabolites do not get through a blood-brain barrier. Лоратал® does not influence TsNS, does not show anticholinergic and sedative action, does not influence the speed of psychomotor reactions.

Pharmacokinetics. After intake of Loratala® it is quickly absorbed from digestive tract and it is almost completely metabolized in an organism. The defined concentration of a loratadin are created in a blood plasma in 15 minutes after administration of drug inside. Loratadin well contacts proteins of a blood plasma. The maximum concentration (Cmax) of a loratadin in a blood plasma is reached in 1-1.3 h, and Cmax of the main active metabolite, a deskarboetoksiloratadin - approximately in 2,5 h. Equilibrium concentration of a loratadin and deskarboksietoksiloratadin is reached at most of patients approximately for the 5th day of reception.

At a concomitant use of food and the drug Loratal® system bioavailability of a loratadin and deskarboetoksiloratadin increases approximately by 40% and 15% respectively. Time of achievement of Cmax of a loratadin and deskarboetoksiloratadin at the same time also increases a little (approximately by 1 h), Cmax values of these substances in plasma are left without changes. Loratadin and his metabolites do not get through a blood-brain barrier therefore has no sedative and holinoblokiruyushchy effect on the central nervous system; does not exponentiate effects of alcohol. The pharmacokinetics of drug does not change at elderly people. At a heavy renal failure bioavailability of a loratadin decreases to 60 – 70%, and at alcoholic damage of a liver the elimination half-life of drug increases. The elimination half-life of a loratadin makes 8.4 h (3 – 20 h), a deskarboetoksiloratadin - 28 h (8.8 - 92 h). About 80% of a dose of a loratadin are removed in the form of metabolites with urine and a stake in equal ratios within 10 days. About 27% of a dose are removed with urine within the first days.

Indications to use:

- seasonal and chronic allergic rhinitis;

- seasonal pollinosis;

- allergic konjyuktivit;

- chronic idiopathic small tortoiseshell;

- skin diseases of the allergic nature.

Route of administration and doses:

To adults, patients of advanced age and children 12 years the recommended dose are more senior makes 10 mg once a day.

To children aged from 2 up to 12 years the recommended dose at body weight more than 30 kg on 10 mg of a loratadin once a day, at body weight less than 30 kg on 5 mg of a loratadin (½ tablets) once a day.

Drug is accepted once a day. The maximum single dose for adult-10 mg, a daily dose of-10 mg.

The maximum single dose for children with body weight more than 30 kg-10 mg, a daily dose - 10 mg.

The maximum single dose for children with body weight less than 30 kg-5 of mg, a daily dose - 5 mg.

For patients with abnormal liver functions the initial dose of drug has to make 5 mg of 1 times a day or 10 mg every other day. At a renal failure (clearance of creatinine less than 30 ml/min.) the initial dose of drug has to make 10 mg every other day.

Duration of treatment depends on a clinical picture of a disease.

Features of use:

Лоратал® has no clinically significant sedative effect when using in the recommended doses (on 10 mg of 1 times a day). Лоратал® does not exponentiate effect of alcohol.

Administration of drug of Loratal® should be stopped not later than 48 h before conducting skin tests to avoid distortion of results.

Features of influence of medicine on ability to manage the vehicle or potentially dangerous mechanisms

It is necessary to be careful when driving and potentially dangerous mechanisms.

After the first administration of drug of Loratal® patients should pay attention to a possibility of development of side effects (for example, drowsiness) which can affect ability to manage the vehicle and potentially dangerous mechanisms. Patients need to be warned about danger of performance of the work requiring special attention and speed of psychomotor reactions before disappearance of these side effects.

Side effects:

- dryness of an oral cavity, vomiting, nausea, gastritis, unpleasant feelings in a stomach, it is rare - abnormal liver functions, increase in appetite;

- dizziness, headache, fatigue, drowsiness; at children (seldom) - a headache, nervousness, sedative action, concern, feeling of fatigue, a hyperkinesia;

- skin rash is possible; seldom: anaphylactic reactions; seldom: alopecia;

- seldom: cough, tachycardia; at children: asthmatic breath, dysphonia, febricula;

- arthralgias, mialgiya.

Interaction with other medicines:

At simultaneous use of the drug Loratal® with:

- ketokonazoly, erythromycin or Cimetidinum noted increase in concentration of a loratadin and its metabolite in a blood plasma;

- with ethanol and tranquilizers, potentiation of the oppressing action on the central nervous system is not observed;

- with other blockers of H1 — receptors, barbiturates, benzodiazepines, agonists of opioid receptors, neuroleptics, tricyclic antidepressants, anxiolytics, sedative and hypnagogues, development of dozozavisimy sedation is possible;

With care it is necessary to appoint Loratal® with inhibitors of enzymes of a liver (guanidine, флуконазол, fluoxetine) as there is no enough observations about safety of similar combinations.

Contraindications:

- hypersensitivity to a loratadin or to other components of drug;

- children's age up to 2 years;

- pregnancy and period of a lactation.

Overdose:

Symptoms: at adults: a headache, drowsiness and tachycardia at administration of drug in doses of 40-180 mg considerably exceeding the recommended therapeutic dose of 10 mg. At children with body weight less than 30 kg at administration of drug in a dose more than 10 mg were noted extrapyramidal symptoms and a cardiopalmus.

Treatment: Loratadin is not brought from an organism at a hemodialysis. In case of overdose it is necessary to induce vomiting, to wash out a stomach, to accept absorbent carbon. To patients the symptomatic and maintenance therapy has to be carried out.

Storage conditions:

At a temperature not above 25 °C in the dry, protected from light place. To store in the place, unavailable to children! Period of storage of 5 years. Not to apply after a period of storage.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets place in a blister strip packaging from a film of polyvinyl chloride and printing aluminum foil.

On 1 planimetric packaging together with the instruction on a medical use in the state and Russian languages place in a pack cardboard with the hologram of firm – producer.