KESTÏN
Active material: Eʙastin
When ATH: R06AX22
CCF: Gistaminovыh blocker H1-receptors. Allergy medication
ICD-10 codes (testimony): J30.1, J30.3, L50
When CSF: 13.01.01.02
Manufacturer: NYCOMED DENMARK ApS (Denmark)
Pharmaceutical form, composition and packaging
◊ Pills, coated white or nearly white, round, Engraved “E20” on one side.
| 1 tab. | |
| eʙastin | 20 mg |
Excipients: magnesium stearate, microcrystalline cellulose, pregelatinized corn starch, lactose monohydrate (177 mg), sodium croscarmellose, gipromelloza, Titanium dioxide, macrogol 6000 (polyethylene glycol 6000).
10 PC. – blisters (1) – packs cardboard.
10 PC. – blisters (2) – packs cardboard.
Pharmacological action
Gistaminovыh blocker H1-long-acting receptor. It prevents histamine-induced spasms of smooth muscle and increased vascular permeability. After oral administration expressed antiallergic action is developed through 1 h and lasts for 48 no. After a 5-day course of treatment Kestin® antihistaminic activity is maintained for 72 h due to the action of the active metabolites.
The drug does not cause significant sedation and anticholinergic. There was no influence Kestin® the duration of the QT interval on the ECG, even at a dose of 80 mg.
Pharmacokinetics
Absorption and distribution
After taking the drug inside Ebastine is rapidly absorbed from the gastrointestinal tract and is almost completely biotransformed in the liver to the active metabolite karebastina. Reception with food accelerates absorption of fat (plasma concentration is increased to 50%).
After receiving a single dose of the drug 10 mg Cmax karebastina plasma achieved through 2.6-4 h and is 80-100 ng / ml. When taken daily at a dose of the drug 10 mg Css achieved through 3-5 days and is 130-160 ng / ml.
Do not cross the BBB.
Linking blood plasma ebastine and karebastina is over 95%.
While taking the drug at the same time eating karebastina level in the blood increases 1.6-2 times, however, this does not alter the time to reach Cmax metabolite and has no effect on the clinical effects Kestin®.
Metabolism and excretion
T1/2 karebastina is from 15 to 19 no. 66% the active substance is excreted as urine conjugates.
Pharmacokinetics in special clinical situations
In elderly patients the pharmacokinetic parameters did not significantly change.
In patients with renal insufficiency T1/2 increases to 23-26 no, and in liver failure - to 27 no, However, the concentration of the drug when taken in doses 10 mg / day does not exceed the therapeutic value.
Testimony
- Seasonal allergic rhinitis and / or year-round (caused by household, pollen, epidermal, food, Drug allergens);
- Urticaria (caused incl. household, pollen, epidermal, food, insektnыmi, Drug allergens, exposure to the sun, cold).
Dosage regimen
Adults and children over 15 years the drug is prescribed for 10-20 mg (1/2-1 tab.) 1 time / day, regardless of the meal.
Children aged 12 to 15 years – by 10 mg (1/2 tab.) 1 time / day.
In patients with impaired liver function daily dose should not exceed 10 mg.
Side effect
CNS: perhaps – headache; rarely – drowsiness, insomnia.
From the digestive system: perhaps – dry mouth; rarely – dyspepsia, nausea, stomach ache.
Other: rarely – sinusitis, rhinitis, asthenic syndrome.
Contraindications
- Pregnancy;
- Lactation (breast-feeding);
- Childhood and adolescence up 12 years;
- Hypersensitivity to the drug.
FROM caution prescribers with renal and / or hepatic insufficiency, with an increase in the QT interval on an electrocardiogram, if hypokalemia.
Pregnancy and lactation
Kestïn® contraindicated during pregnancy because of the lack of reliable clinical data, confirming the safety of the drug.
Do not take Kestin® during breastfeeding due to a lack of data on the allocation of the active substance in breast milk.
Cautions
Use in Pediatrics
In children aged 6 to 12 years preferred use of the drug in the form of a syrup or tablet form 10 mg (by 5 mg / day).
Effects on ability to drive vehicles and management mechanisms
The drug does not affect the patients' ability to drive vehicles and operating machinery.
Overdose
Treatment: There is no specific antidote. Recommend gastric lavage, medical supervision; if necessary, symptomatic therapy.
Drug Interactions
Do not appoint Kestin® simultaneously with ketoconazole and erythromycin because of the increased risk of prolonging the QT interval.
There were no clinically significant drug interactions Kestin® theophylline, nepryamыmy anticoagulants, cimetidine, diazepamom, ethanol and drugs etanolosoderzhaschimi.
Conditions of supply of pharmacies
The drug is resolved to application as an agent Valium holidays.
Conditions and terms
List B. The drug should be stored in a dark and inaccessible to children at temperature not above 30 ° C. Shelf life – 3 year.
