Kestine® [Ebastine]
Almiral S.A.
1771 Items
2019-09-19
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Clinical Pharmacology
Histamine H blocker1- long-acting receptors. Warns histamine-induced smooth muscle spasms and increased vascular permeability.
After taking the drug inside, the pronounced antiallergic action begins after 1 hour and lasts for 48 hours. After a 5-day course of treatment with Kestin®, lyophilized pills with 20 mg of antihistamine activity persist for 72 hours due to the action of the active metabolite.
With prolonged use, a high level of peripheral histamine H blockade is maintained.1receptors without the development of tahifiloxin. The drug does not have a pronounced anticholinergic and sedative effect.
No effect of the drug Kestin® of lyophilized 20 mg pills per QT ECG interval at a dose of 100 mg, 5 times the recommended daily dose (20 mg) was noted.
Pharmacokinetics
Suction
After ingestion, it is rapidly absorbed and almost completely metabolized in the liver, turning into the active metabolite carbastin. After a single dose of 20 mg of the drug, the maximum concentration of carbastine in the blood plasma is reached in 1-3 hours and averages 157 ng / ml. Fatty food accelerates the absorption of carbastine (the concentration in the blood increases by 50%) and presystemic metabolism (formation of carbastine).
Distribution
With daily intake of the drug, the equilibrium concentration is reached after 3-5 days and amounts to 130-160 ng / ml. Binding to plasma proteins Ebastine and Carbastine is more than 95%.
Removal
T1/2 carbastine ranges from 15 to 19 hours. 66% of the drug is excreted in the form of conjugates by the kidneys.
Pharmacokinetics in special clinical situations
In elderly patients, pharmacokinetic parameters do not change significantly.
In renal failure T1/2 increases to 23-26 hours, and with liver failure - up to 27 hours, but the concentration of the drug does not exceed therapeutic values.
Indications
Allergic rhinitis of various etiologies (seasonal and / or year-round).
Urticaria of various etiologies, incl. chronic idiopathic.
Composition
1 tablet soderdit:
Active substances: Ebastine 20 mg.
Excipients: gelatin - 13.00 mg, mannitol - 9.76 mg, aspartame - 2.00 mg, mint flavor - 2.00 mg.
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Dosage and Administration
The drug is intended for resorption in the mouth, regardless of the meal.
Adults, children and teenagers over 15 years old: appoint 20 mg (1 lyophilized tablet) 1 time / day. The course of treatment is determined by the disappearance of the symptoms of the disease.
Elderly patients dose adjustment is not required.
In patients with impaired renal function dose adjustment is not required.
With minor and moderate liver failure the drug can be used in the usual dose. In severe liver dysfunction, the daily dose of Ebastine 10 mg should not be exceeded.
Special precautions when handling the drug
- To avoid damage to the pills, do not remove the tablet from the blister by pressing. Open the package by gently lifting the free edge of the protective film.
- Remove the protective film.
- Gently squeeze the drug, without touching it. Carefully remove the pill and put it on the tongue where it will quickly dissolve. No need to drink water or other liquid. Eating does not affect the effect of the drug.
Adverse reactions
From the nervous system: from 1% to 3.7% - headache, drowsiness; less than 1% - insomnia.
From the digestive system: from 1% to 3.7% - dryness of the oral mucosa; less than 1% - dyspepsia, nausea, abdominal pain.
On the part of the respiratory system: less than 1% - sinusitis, rhinitis.
Other: less than 1% - asthenic syndrome; allergic reactions are possible.
Contraindications
Carefully: use in patients with prolonged QT interval, hypokalemia, with renal and / or liver failure.
Drug interactions
It is not recommended to use Kestin® lyophilized 20 mg pills simultaneously with ketoconazole and erythromycin (an increased risk of prolonged QT interval).
Kestin® freeze-dried pills 20 mg does not interact with theophylline, indirect anticoagulants, cimetidine, diazepam, ethanol and ethanol-containing drugs.
Pregnancy and Lactation
The drug is contraindicated during pregnancy and lactation (breastfeeding).
Special instructions
Ebastine may distort the results of skin allergy tests. Therefore, it is recommended to conduct such tests no earlier than 5-7 days after discontinuation of the drug.
Influence on the ability to drive vehicles and other mechanisms requiring increased attention concentration
In the event of side effects from the central nervous system, there may be a minimal decrease in the patients' ability to drive vehicles and engage in other potentially hazardous activities that require increased concentration and psychomotor reactions.
Overdosage
Symptoms: moderate effects on the central nervous system (fatigue) and the autonomic nervous system (dry oral mucosa) can occur only at high doses (300-500 mg, which is 15-25 times higher than the therapeutic dose).
Treatment: in case of an overdose, gastric lavage, control of vital body functions, and symptomatic treatment are recommended. There is no special antidote for ebastine.
- Brand name: Kestin
- Active ingredient: Ebastine
- Dosage form: pills lyophilized.
- Manufacturer: Almiral S.A.
- Country of Origin: Spain
Studies and clinical trials of Ebastine (Click to expand)
- Analysis of an aerosol preparation of kameton by the method of gas-liquid chromatography
- Pharmacokinetic–pharmacodynamic analysis of the arrhythmogenic potency of a novel antiallergic agent, ebastine, in rats
- Comparative electrophysiological effects of the second generation antihistamines, astemizole and ebastine, in a canine myocardial infarction model
- Identification of rat faecal metabolites of ebastine by B/E linked scanning liquid secondary ion mass spectrometry
- Optically active analogues of ebastine: Synthesis and effect of chirality on their antihistaminic and antimuscarinic activity
- Effects of antihistamines, ebastine and terfenadine, on electrocardiogram in conscious dogs and cats
- Synthesis of [2H5]-ebastine fumarate and [2H5]-hydroxyebastine
- PI-8Effect of itraconazole and rifampin on the pharmacokinetics and pharmacodynamics of ebastine in relation to CYP2J2*8 genotype
- Simultaneous determination of ebastine and its three metabolites in plasma using liquid chromatography-tandem mass spectrometry
- Biooxidation of methyl group: application to the preparation of alcohol and acid metabolites of terfenadine, ebastine and analogues
- Erratum to “Simultaneous determination of the histamine H1-receptor antagonist ebastine and its two metabolites, carebastine and hydroxyebastine, in human plasma using high-performance liquid chromatography”: [J. Chromatogr. B 757 (2001) 173–179]
- A double-blind, single-dose, crossover comparison of cetirizine, ebastine, epinastine, fexofenadine, terfenadine, and loratadine versus placebo: suppression of histamine-induced wheal and flare response for 24 h in healthy male subjects
- A 12-week, placebo-controlled study of the efficacy and safety of ebastine, 10 and 20 mg once daily, in the treatment of perennial allergic rhinitis
- Duration of the antihistaminic effect after discontinuation of ebastine
- Comparison of cetirizine, ebastine and loratadine in the treatment of immediate mosquito-bite allergy
- Differential cognitive effects of ebastine and (+)-chlorpheniramine in healthy subjects: Correlation between cognitive impairment and plasma drug concentration
- Effects of supratherapeutic doses of ebastine and terfenadine on the QT interval
- Effects of supratherapeutic doses of ebastine and terfenadine on the QT interval
- Neuroimaging of histamine H1-receptor occupancy in human brain by positron emission tomography (PET): A comparative study of ebastine, a second-generation antihistamine, and (+)-chlorpheniramine, a classical antihistamine
- A review of the cardiac systemic side-effects of antihistamines: ebastine
- Ebastine inhibits T cell migration, production of Th2-type cytokines and proinflammatory cytokines
- Validated stability-indicating spectrofluorimetric methods for the determination of ebastine in pharmaceutical preparations
- Validated stability indicating liquid chromatographic determination of ebastine in pharmaceuticals after pre column derivatization: Application to tablets and content uniformity testing
- Placebo controlled comparison of acute effects of ebastine and clemastine on performance and EEG
- Lack of pharmacodynamic and pharmacokinetic interactions of the antihistamine ebastine with ethanol in healthy subjects
- Dose-response relationship of the H1-histamine antagonist, ebastine, against histamine and methacholine-induced bronchoconstriction in patients with asthma
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