Erolin - instructions for use, dose, side effects, contraindications

Active substance - loratadine 10 mg in 1 tablet, excipients: lactose monohydrate, microcrystalline cellulose, pregelatinized starch, silicon dioxide colloidal anhydrous, magnesium stearate.

Description:

Round, flat pills with a bevel, engraved "E 531" on one side and risky on the other side, white or almost white.

Pharmacotherapeutic group:Antiallergic - H1 histamine receptor blocker

ATX: & nbsp

R.06.A.X Other antihistamines for systemic use

R.06.A.X.13 Loratadin

Pharmacodynamics:

Loratadin is a long-acting selective tricyclic blocker of peripheral histamine H1receptors. Its clinical feature is the absence of sedative action and anticholinergic properties. Long-term administration of loratadine does not lead to a change in vital functions, parameters of laboratory studies, mental state.

Prevents development and facilitates the course of allergic reactions. It has antiallergic, antipruritic, antiexudative action. Reduces the permeability of capillaries, prevents the development of edema of tissues, relieves spasms of smooth muscles.

Inhibits the release of histamine and leukotriene C4 from mast cells.

With a long study of direct toxic effects or specific effects associated with the use of the drug, it is not revealed.

In this case, the onset of action is observed after 1-3 hours, the maximum effect reaches 8-12 hours.The duration of action after a single dose of the drug inside is 24 to 48 hours.

Pharmacokinetics:

Suction

After oral administration, it is rapidly absorbed from the gastrointestinal tract. It does not penetrate the hemato-encephalic barrier and has a weak affinity for histamine receptors in the brain.

Effect of food on absorption: when taking the drug after eating, the area under the concentration-time curve (AUC) and time to reach the maximum concentration (T_m_Oh) for loratadine and its active metabolite are increasing.

With a single appointment a day reaches the state of equilibrium concentration on day 5. When administered at a dosage range of 10 to 40 mg per day, the pharmacokinetic parameters of the parent compound and its active metabolite are dose independent.

Metabolism

Virtually completely metabolized in the liver under the influence of isoenzyme CYP 3A4. In the presence of inhibitors of this enzyme system, loratadine can be metabolized by isoenzyme CYP 2D6. As a result of intensive metabolism, the "first pass" through the liver produces an active metabolite - descarbotoxytoloratadine. This, more active than the original compound, the metabolite is inactivated subsequently by conjugation.

Distribution

The binding of loratadine to plasma proteins is 97%, whereas the binding of its active metabolite with proteins is 73-77%. More intensively binds to peripheral histamine H1receptors than with the central nervous system receptors.

Loratadine and its active metabolite penetrate the placental barrier.

Excretion

The half-life (T1 / 2) is 12-15 hours. In the elderly, as well as in patients with chronic liver disease, the half-life increases. 24 hours after the appointment of the drug, 27% of the administered dose is excreted by the kidneys in conjugated form. When the drug is prescribed for 10 days, 40% and 42% of the total amount administered is excreted by the kidneys and through the intestine, respectively. Loratadin and its active metabolite is excreted in breast milk.

In patients with chronic renal failure, pharmacokinetics practically does not change.

Indications:

Adults

- seasonal and year-round allergic rhinitis; allergic conjunctivitis; idiopathic chronic urticaria;

- itching dermatoses;

pseudoallergic reactions caused by the release of histamine; allergic reactions to insect bites.

Children over 3 years old

- seasonal allergic rhinitis and conjunctivitis;

- allergic skin reactions, for example, idiopathic urticaria.

Contraindications:

- hypersensitivity to the active or any other component of the drug;

- pregnancy and / or lactation period (see the section "Pregnancy and lactation period");

- Children under 3 years old (for this dosage form).

Carefully:Severe violations of liver function, renal failure (glomerular filtration rate (GFR) <30 ml / min).

Pregnancy and lactation:The use of Erolin during pregnancy is only possible if the intended benefit to the mother exceeds the potential risk to the fetus. The drug is excreted in breast milk, so when taking the drug during lactation should resolve the issue of ending breastfeeding.

Dosing and Administration:

Adults:

Tablets should be taken before meals, not chewed, and washed down with liquid.

If the patient's allergic symptoms do not decrease within 3 days,the likelihood of further drug intake is reduced.

The usual dose for adults and adolescents over 12 years is 1 tablet (10 mg loratadine) per day.

Children aged 6-12 years:

children weighing less than 30 kg: 1/2 tablet (5 mg) per day, children weighing more than 30 kg: 1 tablet (10 mg) per day.

Children aged 2-6 years are best given Erolin syrup, as it may be difficult to swallow the pill. Assign 5 mg every other day. With good tolerability, the dose can be gradually increased.

Special patient groups:

Patients with hepatic insufficiency or renal insufficiency GSKF <30 ml / min), as well as children older than 6 years: 5 mg (1/2 tablet) per day or 10 mg (1 tablet) every other day.

Side effects:

Erolyn is usually well tolerated. The frequency of side effects when using the drug is the same as with the use of placebo ("dummy").

Side effects, depending on the individual sensitivity of the patient, are of short duration and completely disappear after the drug is discontinued.

In adults There were: headache, fatigue, dry mouth, drowsiness, gastrointestinal disorders (nausea, gastritis), as well as allergic reactions in the form of rashes.In addition, there were rare reports of anaphylaxis, alopecia, impaired liver function, palpitation, tachycardia.

Children rarely noted: headache, nervousness, sedation. As in adults, the frequency of these events was at the same level as when using a placebo ("dummy").

Overdose:

Symptoms: drowsiness, tachycardia, headache.

Treatment: In case of an overdose, immediately consult a doctor.

Specific antidotes are absent. Supportive and symptomatic therapy. Patients who are conscious should be prescribed emetics. The use of pevecacans is indicated even if spontaneous vomiting occurs. After emptying the stomach should be appointed Activated carbon and large quantities of liquid. If attempts to induce vomiting are unsuccessful, or there are contraindications, the stomach should be washed through the probe. After carrying out urgent measures, patients need medical supervision.

Interaction:

Joint application with erythromycin, cimetidine or ketoconazole leads to an increase in the concentration of loratadine and its metabolites in blood plasma.The concentration of cimetidine and ketoconazole in the blood plasma remains unchanged, while the erythromycin content decreases by 15%.

A sufficient number of safety observations on co-administration with liver enzyme inhibitors (fluconazole, fluoxetine) absent.

Inductors of microsomal oxidation (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) may decrease effectiveness.

Loratadine does not enhance the effect of alcohol on the central nervous system.

Special instructions:

The duration of Erolin treatment should be monitored individually. Patients should be advised to stop taking Erolin at least 4 days before the skin allergic tests are performed to avoid their false negative result.

Each Erolin tablet contains 63.8 mg of lactose. This amount should be taken into account when prescribing the drug to patients with lactase deficiency and rare hereditary diseases (galactose intolerance and glucose / galactose absorption disorder syndrome).

Effect on the ability to drive transp. cf. and fur:

At the beginning of the course of treatment, for an individually defined period of time, driving vehicles and performing work with an increased risk of accidents requires special care because of the risk of side effects such as drowsiness. In the future, the degree of restrictions should be set for each patient individually.

Form release / dosage:Tablets 10 mg.

Packaging:

5 tablets in a blister, 1 blister in a cardboard bundle along with instructions for use. 10 tablets in a blister, 1 or 3 blisters in a cardboard pack together with instructions for use.

Storage conditions:

Store at a temperature not exceeding 25 ° C. Keep out of the reach of children.

Shelf life:

5 years. Do not use after the date indicated on the package.

Terms of leave from pharmacies:Without recipe

Registration number:П N013881 / 01

Date of registration:27.02.2008 / 15.01.2015

The owner of the registration certificate:EGIS ZAO Pharmaceutical Plant EGIS ZAO Pharmaceutical Plant Hungary

Manufacturer: & nbsp

EGIS PHARMACEUTICALS, Plc Hungary

Representation: & nbspEGIS ZAO Pharmaceutical Plant EGIS ZAO Pharmaceutical Plant Hungary

Information update date: & nbsp23.06.2016

Illustrated instructions

Instructions

Erolin® (Erolin®)