EROLIN®
Active material: Loratadine
When ATH: R06AX13
CCF: Gistaminovыh blocker H1-receptors. Allergy medication
ICD-10 codes (testimony): H10.1, J30.1, J30.3, L20.8, L23, L24, L28.0, L29, L30.0, L50
When CSF: 13.01.01.02
Manufacturer: EGIS PHARMACEUTICALS Plc (Hungary)
Pharmaceutical form, composition and packaging
◊ Pills white or nearly white, round, flat, chamfered, Engraved “E 531” on one side and Valium – another.
| 1 tab. | |
| loratadine | 10 mg |
Excipients: lactose monohydrate, microcrystalline cellulose, Colloidal anhydrous silica, pre-gelatinized starch, magnesium stearate.
5 PC. – blisters (1) – packs cardboard.
10 PC. – blisters (1) – packs cardboard.
10 PC. – blisters (3) – packs cardboard.
◊ Syrup pale yellow, clear, uniform, with a characteristic fruity odor; without deposit and mechanical impurities.
| 5 ml | |
| loratadine | 5 mg |
Excipients: Sodium benzoate, sucrose (3 g 5 ml), propylene glycol, glycerol, Citric acid anhydrous, vanilla flavor AB-710, Strawberry flavor 22754-00, Purified water.
120 ml – vials of dark glass (1) complete with a scoop – packs cardboard.
Pharmacological action
Electoral tricyclic histamine H1-long-acting receptor. Has antiallergic, antipruritic and antiexudative action.
It inhibits the release of histamine and leukotriene C4 from mast cells.
It prevents the development and facilitates the allergic reactions. Decreases capillary permeability, prevents the development of edema, relieves spasms of smooth muscles.
No effect on the central nervous system and is not addictive (tk. It does not penetrate the BBB).
The onset of action observed after 30 m, maximum effect is observed after 8-12 no. The duration of action after a single oral dose of 24 no.
Pharmacokinetics
Absorption
After oral administration, loratadine is rapidly absorbed from the gastrointestinal tract. Tmax is 1.3-2.5 h and increased at mealtime 1 no.
Distribution and metabolism
Plasma protein binding – 97%. Css loratadine and its metabolite in plasma are reached on the 5 day reception.
It is metabolized in the liver to the active metabolite descarboethoxyloratadine with the participation of CYP3A4, and to a lesser extent – CYP2D6. Do not cross the BBB.
Deduction
T1/2 loratadine – 3-20 no (average 8.4), aktivnogo metabolite – 8.8-92 no (average 28 no). Excreted by the kidneys and the bile.
Pharmacokinetics in special clinical situations
In patients with chronic renal insufficiency pharmacokinetics practically unchanged.
In elderly patients withmax in the blood plasma is increased by 50%, T1/2 loratadine and of the active metabolite increased up to 6.7-37 no (average 18.2 no) and 11-38 no (average 17.5 no).
In alcoholic liver disease Cmax in plasma and T1/2 loratadine and of the active metabolite increased proportionally to the severity of the disease.
Testimony
For adults
- Seasonal and perennial allergic rhinitis;
- Allergic conjunctivitis;
- Idiopathic chronic urticaria;
- Pruritic dermatoses;
- Pseudoallergy reaction, caused by the release of histamine;
- An allergic reaction to insect bites.
For children over 2 years
- Seasonal allergic rhinitis and conjunctivitis;
- Allergic skin reactions (incl. idiopathic urticaria).
Dosage regimen
Tablets should be taken before meals, do not chew, drink liquid.
Adults and children weighing more than 30 kg the drug is prescribed in a dose 10 mg (1 tab. or 10 ml syrup) 1 time / day.
Children aged 2 to 12 years from body weight <30 kg – 5 mg / day (1/2 tab. or 5 ml syrup).
Children aged 2 to 6 years should appoint Erolin® in the form of a syrup, as swallowing pills can be difficult for them. The usual dose is on 5 mg (5 ml syrup) in one day. With good tolerability of the drug dose can be gradually increase.
Patients with hepatic and renal (CC<30 ml / min) failure appoint 5 mg (1/2 tab. or 5 ml syrup)/day or on 10 mg (1 tab. or 10 ml syrup)/day after day.
Care should be taken when appointing Erolina® elderly patients (senior 60 years) doses, recommended for adults with normal renal function, due to the increased frequency of adverse events.
Side effect
Erolin®, usually, well tolerated.
The frequency of side effects in both age groups the same, both with placebo. Side effects depend on individual sensitivity, are of short duration and completely disappear after drug withdrawal.
In Adult
CNS: headache, fatiguability, drowsiness, increased fatigue.
From the digestive system: dry mouth, nausea, vomiting, increased appetite, discomfort in the stomach, gastritis; rarely – abnormal liver function.
Cardio-vascular system: rarely – palpitations, tachycardia.
Other: allergic reactions such as rashes; rarely – anaphylactic shock, alopecia.
In children
From the central and peripheral nervous system: giperkinezii, fatiguability; rarely – headache, nervousness, sedation.
Contraindications
- Pregnancy;
- Lactation (breast-feeding);
- Children up to age 3 years (for the drug in tablet form);
- Children up to age 2 years (for the preparation in the form of a syrup);
- Hypersensitivity to the drug.
FROM caution use in patients with severe hepatic dysfunction, renal failure (CC <30 ml / min).
Pregnancy and lactation
Application Erolina® Pregnancy may only, if the expected benefit to the mother outweighs the potential risk to the fetus.
Loratadine is excreted in breast milk, therefore, if necessary, use during lactation should stop breastfeeding.
Cautions
Necessary to control the duration Erolina® each patient.
Patients should stop taking the drug at least 4 days before the skin allergy tests in order to avoid false-negative result.
Each tablet formulation Erolin® It contains 63.8 g. lactose, which should be considered when administering the drug to patients with lactase deficiency and rare hereditary diseases (galactose intolerance and malabsorption syndrome glucose / galactose).
IN 5 ml syrup contains 3 g sucrose, that should be considered in the treatment of patients with diabetes mellitus.
Effects on ability to drive and operate machinery
At the beginning of treatment, for individually defined period of time, driving vehicles and works with an increased risk of accidents requires special care because of the risk of side effects such as drowsiness. In the future, the application of Erolina® (as well as other antihistamines) Patients should use caution when driving and operating machinery.
Overdose
Symptoms: drowsiness, tachycardia, headache (after administration 40-180 mg loratadine). In case of overdose should immediately seek medical advice.
Treatment: There are no specific antidotes. Patients, in conscious, should appoint emetics. The use of drugs ipecac shown even if, If vomiting occurs spontaneously. After emptying of the stomach should designate an activated carbon and a large quantity of liquid. If unsuccessful attempt to induce vomiting, or there are contraindications, should be flushed through the stomach probe. Displaying the holding of symptomatic and supportive therapy. After the urgent measures required for patients under medical surveillance.
Drug Interactions
In a joint application Erolina® erythromycin, cimetidine or ketoconazole may increase the concentration of loratadine and its metabolites in blood plasma. Concentration of cimetidine and ketoconazole in plasma remains unchanged, while the content of erythromycin decreases by 15%.
Lack of sufficient number of observations about the safety of Erolina® inhibitors of microsomal liver enzymes (fluconazole, fluoxetine).
Inductors of microsomal oxidation (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) may reduce the effectiveness of Erolina®.
Loratadine does not increase the effect of ethanol on the CNS.
Conditions of supply of pharmacies
The drug is resolved to application as an agent Valium holidays.
Conditions and terms
The drug is in the form of tablets should be stored out of reach of children at or above 25 ° C, in the form of a syrup – 2 ° to 25 ° C.
Shelf life Tablets – 5 years. Shelf life syrup – 3 year.
After opening the bottle syrup usable for 6 months when stored.
