Erolin

General characteristics. Structure:

Active agent: лоратадин 10 mg
excipients: lactoses monohydrate; MKTs; starch gelated; silicon dioxide colloid anhydrous; magnesium stearate  

in piece blister 5, 7 or 10; in a pack cardboard 1 (5 and 7 pieces) or 1 and 3 (10 pieces) the blister.

Syrup of 1 ml
Active agent: лоратадин 1 mg
excipients: Natrium benzoicum; sucrose; propylene glycol; glycerin; anhydrous citric acid; AV-710 vanillin; aroma strawberry 22754-00; the water distilled  

in bottles of dark glass on 120 ml, complete with a measured spoon; in a pack a cardboard 1 set.
Description of a dosage form

Tablets: round flat tablets in the form of a disk with a facet, with an engraving of "E531" on one party and the dividing line — on another, white or almost white color.
Syrup: the transparent sweet homogeneous syrup which is slightly painted in yellow color with a characteristic fruit smell and taste.

Pharmacological properties:

Pharmacological action - antihistaminic, antiallergic, anti-exudative, antipruritic. Selectively blocks peripheral H1 - histamine receptors. Badly gets through GEB and has weak affinity to histamine receptors of a brain. Inhibits release of a histamine and C4 leukotriene from mast cells. Reduces permeability of capillaries, edematization of fabrics warns, removes spasms of smooth muscles. Has no sedative effect and has no holinoblokiruyushchy properties. Differs in high safety (even long appointment does not lead to change of physiological functions, laboratory indicators, the mental status and EEG). At the long studying of direct toxic impact or specific effects connected with administration of drug it is not revealed.

Pharmacokinetics. After intake it is quickly soaked up from a GIT. At administration of drug after food of AUC and Tmax of a loratadin and its active metabolite increase. At reception of 1 times a day equilibrium concentration is reached by 5th day. At reception in the range of doses from 10 to 40 mg a day pharmacokinetic parameters of a loratadin and its metabolite do not depend on a dose. It is almost completely metabolized in a liver under the influence of CYP3A4 isoenzyme. In the presence of inhibitors of this fermental system лоратадин it can be metabolized by CYP2D6 isoenzyme. As a result of intensive metabolism at "the first passing" through a liver more active is formed, than initial connection, a metabolite — дескарбоэтоксилоратадин which is inactivated in the subsequent by conjugation. Linkng with proteins makes 97% (an active metabolite — 73–77%). Loratadin and active metabolite pass through a placental barrier, get into breast milk. T1/2 of a loratadin at healthy patients — 12–15 h, T1/2 increases at elderly people, and also at patients with chronic diseases of a liver. During 24 h 27% of the general dose it is removed by kidneys in the conjugated form. At purpose of drug within 10 days of 40% also 42% — with a stake are removed with urine. At patients with a chronic renal failure the pharmacokinetics practically does not change.

Pharmacodynamics. Prevents development and facilitates the course of allergic reactions. The beginning of action is noted in 1–3 h, the effect reaches a maximum in 8–12 h, action duration after a single dose inside makes 24–48 h.

Indications to use:

Adult: allergic rhinitis (seasonal and year-round), allergic conjunctivitis, chronic idiopathic small tortoiseshell, pruritic dermatosis; tablets (in addition) — the pseudo-allergic reactions caused by release of a histamine, allergic reactions to stings of insects.
To children 2 years are more senior: seasonal allergic rhinitis and conjunctivitis, allergic skin reactions (for example idiopathic small tortoiseshell).

Route of administration and doses:

Inside. To adults and teenagers 12 years — 10 mg (1 tab. or 10 ml of syrup) in day are more senior.
Patients with insufficiency have functions of a liver or with a renal failure (speed of glomerular filtering <30 ml/min.) the dose is selected individually. An initial dose — usually 5 mg (1/2 tab. or 5 ml of syrup) every day or 10 mg (1 tab. or 10 ml of syrup), but every other day.
At elderly patients 60 years possibly more frequent development of side effects therefore it is necessary to be careful at appointment in the doses recommended to adults with normal function of kidneys are more senior.
Erolin is not recommended to children up to 2 years.
To children aged from 2 up to 12 years Erolin appoint according to body weight: at body weight less than 30 kg — 5 mg (1/2 tab. or 5 ml of syrup) in day, at body weight more than 30 kg — 10 mg (1 tab. or 10 ml of syrup) in day.

Precautionary measures

Erolin's tablets should be applied with care at heavy abnormal liver functions.
Duration of treatment by Erolin needs to be controlled individually.
Erolin does not cause sedation and does not influence the speed of psychomotor reactions. Nevertheless, as well as at treatment by any antihistaminic drug, patients have to be careful at occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of reactions. At the first reception of Erolin by the patient it is necessary to pay attention to a possibility of development of side effects (for example drowsiness) which can affect ability to drive the car or mechanical devices (it is necessary to refrain from performance of similar work before disappearance of side effects).

Side effects:

Erolin, as a rule, is well had. Frequency of manifestation of side effects at use of drug for adults and children is comparable with placebo. Side effects depend on individual sensitivity of the patient, have short character and completely disappear after drug withdrawal.
At adults were noted: a headache, drowsiness, fatigue, dryness in a mouth, nausea, vomiting, increase in appetite, unpleasant feelings in a stomach, allergic reactions in the form of rash; there are rare messages on an anaphylaxis, an alopecia, abnormal liver function, heartbeat, tachycardia.
At children were seldom noted: headache, nervousness, sedative action, asthmatic breath, feeling of fatigue, hyperkinesia, abdominal pain, conjunctivitis, dysphonia, febricula.

Interaction with other medicines:

It is necessary to be careful at possible combined use of Erolin:
- with erythromycin, Cimetidinum or ketokonazoly — increase in concentration of a loratadin and its metabolites in a blood plasma is possible. Concentration of Cimetidinum and ketokonazol in a blood plasma at the same time remains invariable whereas the content of erythromycin decreases by 15%;
- with inhibitors of enzymes of a liver (guanidine, флуконазол, fluoxetine) — there is no enough observations about safety of similar combinations.
Inductors of a microsomal oxidation (Phenytoinum, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) can reduce efficiency.
Loratadin does not strengthen effect of alcohol on TsNS.

Contraindications:

Hypersensitivity, pregnancy and feeding by a breast (see. "Use at pregnancy and feeding by a breast"), children's age up to 2 years.

Use at pregnancy and feeding by a breast

Use at pregnancy is possible only if the estimated advantage for mother exceeds potential risk for a fruit. In the period of a lactation it is necessary to resolve an issue of the breastfeeding termination (gets into breast milk).

Overdose:

Symptoms: after reception of 40-180 mg of a loratadin drowsiness, tachycardia, a headache were observed.
Treatment: it is necessary to begin a symptomatic and maintenance therapy as soon as possible. The patient who is in consciousness — vomitives. Use of drugs of an ipecacuanha is shown even if there is spontaneous vomiting. After gastric emptying — use of absorbent carbon and a large amount of liquid. If attempts to cause vomiting are unsuccessful or if there are contraindications, it is necessary to wash out a stomach via the probe. The specific antidote is absent.

Storage conditions:

Period of validity 4 years. List B.: At a temperature of 15-25 °C.

Issue conditions:

According to the recipe

Packaging:

In bottles of dark glass on 120 ml, complete with a measured spoon; in a pack a cardboard 1 set.