Date of approval.
Date of revision.
Ebastine Tablets Instructions
Please read the instructions carefully and use under the guidance of a physician
Drug Name]
Generic name: Ebastine Tablets
Trade name: Ebastine
English name: Ebastine Tablets
Hanyu Pinyin: Yibasiting Pian
【Composition
Ingredients
The main ingredient of this product is: Ebastine
Its chemical name is: 1-[4-(1,1-dimethylethyl)phenyl]-4-[4-(diphenylmethoxy)-1-piperidinyl]-1-butanone
Chemical structure formula.
Molecular formula: C32H39NO2
Molecular weight: 469.67
Properties
Appearance
This product is white or off-white film-coated tablets, which appear white or off-white after removing the coating.
Indications
It is indicated for allergic rhinitis (seasonal and perennial) with or without allergic conjunctivitis. Symptomatic treatment of chronic idiopathic urticaria.
Specification
Specification
10mg
Dosage and Administration
Take orally.
Adults or children over 12 years old: one or two tablets once a day.
This product is not recommended for use in children under 12 years of age or in patients with swallowing difficulties.
This product can be taken with or without food.
This product must be swallowed whole with a small amount of water.
No dose adjustment is required for elderly patients and patients with renal insufficiency or mild to moderate hepatic insufficiency. The daily dose for patients with severe hepatic insufficiency should not exceed 10 mg.
The duration of treatment may be extended until symptoms disappear.
[Adverse Reactions].
In a pooled analysis of a placebo-controlled clinical trial of 5708 patients treated with epalrestin, the most frequently reported adverse reactions were headache, drowsiness, and dry mouth. Adverse reactions reported in pediatric clinical trials (n = 460) were similar to those observed in adults.
The following table lists adverse reactions in clinical trials and postmarketing use for the following practices: very common (≥1/10), common (≥1/100 to <1/10), occasional (rare) (≥1/1,000 to <1/100), rare (≥1/10,000 to <1/1,000), and very rare (very rare) (<1/ 10,000).
Systemic organ classification very common (³1/10) common
(³1/100 to<1/10) Occasional (rare)
(≥ 1/1,000 to < 1/100) Rare
(³1/10.000 to <1/1.000) Immune system disorders Hypersensitivity reactions (e.g., allergic reactions and angioedema) Metabolic and nutritional disorders Hyperphagia Psychiatric disorders Nervous tension, insomnia Various neurological disorders Headache drowsiness Dizziness, hypoesthesia, taste disturbances
Heart diseases Palpitations, tachycardia Gastrointestinal diseases Dry mouth Vomiting, abdominal pain, nausea, dyspepsia Hepatobiliary diseases Hepatitis, cholestasis, abnormal liver function tests (elevated transaminases, γ-glutamyl transferase, alkaline phosphatase and bilirubin) Skin and subcutaneous tissue diseases Urticaria, rash, dermatitis Reproductive and breast diseases Menstrual disorders Systemic diseases and various reactions at the drug administration site Edema, fatigue Weakness
Foreign literature reports.
The following adverse effects have been reported in less than 1% of children >12 years of age: abdominal pain, dyspepsia, epistaxis, rhinitis, sinusitis, nausea, and insomnia.
Other adverse effects reported in children younger than 12 years of age of less than 1% include: increased appetite, diarrhea, rash, irritability, emotional instability, hyperactivity, taste changes, and weakness.
Contraindications]
Patients who are hypersensitive to epinastine or any of the ingredients in the tablets.
Precautions]
Ibastine should be used with caution in patients with known risk factors for heart disease, such as prolonged QT syndrome on ECG, hypokalemia, and in patients taking drugs with prolonged QT interval or CYP3A4 enzyme inhibitors, such as azole antifungal drugs like ketoconazole and itraconazole and macrolide antibiotics like erythromycin (see [Drug Interactions]).
Pharmacokinetic interactions may also occur when rifampicin is combined with epinastine (see [Drug Interactions]).
Ebastine should be used with caution in patients with severe liver injury (see [Dosage]).
Because epinastine acts after 1 to 3 hours of administration, it is not indicated for monotherapy of acute allergies.
Effects on driving and mechanical ability: A study designed to test the effects of epinastine on driving ability showed no effect if the recommended daily dose was maintained below 30 mg. Based on these data, there was no effect on the ability to drive or operate machinery when ebastine was used correctly. However, for sensitive patients with an abnormal response to epinastine, it is recommended that individual reactions be known before the patient drives or performs complex activities: drowsiness or dizziness may occur (see [ADVERSE REACTIONS]).
This product contains lactose. Patients with hereditary galactose intolerance or glucose-galactose malabsorption should not take this product.
[For pregnant and lactating women].
Fertility
Fertility data related to epalrestin in humans are not available.
Pregnancy
Data on the use of epalrestine in pregnant women are limited. Animal studies have shown no direct or indirect adverse effects with respect to reproductive toxicity. As a precautionary measure, it is best to avoid the use of epinastine during pregnancy.
Lactation
It is not known whether epinastine is secreted in breast milk. The high protein binding (> 97%) of epinastine and its major metabolite, carristine, suggests that it is not excreted into breast milk. As a precautionary measure, it is best to avoid the use of epinastine during breastfeeding.
[Pediatric Use].
This product is indicated for adults and children over 12 years of age, with the dosage for children over 12 years of age being the same as that for adults.
For adverse reactions in children, please see [Adverse Reactions].
Geriatric use]
There were no statistically significant differences in pharmacokinetics in elderly subjects compared to adult or young volunteers.
The dosage for elderly patients is the same as that for adult patients and no dose adjustment is necessary.
Drug Interactions]
Studies have shown pharmacokinetic and pharmacodynamic interactions when combining epinastine with ketoconazole or erythromycin (both of which are known to prolong the QT interval). This may increase the plasma concentration of epinastine and, to a lesser extent, karestin, but there is no clinically significant pharmacodynamic effect; the QT interval is prolonged by only about 10 ms compared with the two drugs alone. Therefore, ibastine should be used with caution in patients taking concurrent azole antifungals such as ketoconazole or itraconazole and macrolide antibiotics such as erythromycin.
Pharmacokinetic interactions can be observed when ibrastine is administered with rifampicin. These interactions can result in lower plasma concentrations and reduced antihistamine effects.
No interactions have been reported between epinastine and theophylline, warfarin, cimetidine, diazepam, and alcohol.
When epinastine is taken with food, the blood concentration and its post-metabolism basal active product increase by 1.5-2.0 in response to some factor, but this increase does not affect the time to peak blood concentration. Concomitant administration with food does not affect the clinical efficacy of epinastine.
Ebastine affects the effect of skin tests, so skin tests should only be performed 5 to 7 days after discontinuation of ebastine. In addition, the effects of some other antihistamines may be potentiated by the use of epinastine.
Drug overdose
Overdose trials have shown that no clinically significant symptoms occur at doses below 100 mg daily. Ebastine has no specific antidote. Gavage, vital signs monitoring (including ECG) and symptomatic treatment should be performed.
Pharmacology and Toxicology
Ebastine has a rapid and long-lasting antihistamine effect and has a strong affinity for histamine H1 receptors. When administered orally, epinastine and its metabolites do not cross the cerebral blood barrier. This explains why ebastine has only a mild sedative effect on the central nervous system.
Trial data suggest that epinastine is a long-acting, highly selective histamine H1 receptor blocker with no anticholinergic effects.
Preclinical safety data show that epinastine was not found to have toxic effects in routine pharmacological safety test results. Repeated dose testing did not reveal toxicity, reproductive toxicity, potential carcinogenicity, or side effects on reproductive function.
Pharmacokinetics]
After oral administration, epinastine is rapidly absorbed and most of it is initially metabolized in the liver. The product is an active metabolite, Carebastine. After a single oral dose of 10 mg, the maximum blood concentration of the metabolite is 80-100 ng/ml, with a peak time of 2.6-4 hours. The half-life of Carebastine is 15-19 hours, and 66% of ebastine is excreted in the form of bound metabolites, mainly in the urine. Ebastine is administered once daily at 10 mg and reaches its stable blood concentration after 3-5 days, with peak concentrations in the range of 130-160 ng/ml.
Both epinastine and carrestine are highly bound to plasma proteins: >97%.
In patients with mild, moderate and severe renal insufficiency, administered at 20 mg daily, the blood concentrations of epinastine and carristine obtained on days 1 and 5 and the blood concentrations of epinastine and carristine recorded in patients with mild and moderate hepatic insufficiency (20 mg/day), and in patients with severe hepatic insufficiency (10 mg/day) were similar to those of healthy subjects. This suggests that there are no significant changes in the pharmacokinetics of epinastine and its metabolites in patients with varying degrees of hepatic or renal insufficiency.
Storage
Storage】 Store under 30℃ in dry and protected from light.
Package
Package
Aluminum-plastic packaging. 7 tablets/plate×1 plate/box, 7 tablets/plate×2 plates/box, 10 tablets/plate×1 plate/box.
Available
Efficacy
Period】 12 months
【Execution standard
Approval number】
State Drug Administration H20040503
Drug Marketing Licensee
Name: Hangzhou Ao Medicine Pauling Pharmaceutical Co.
Address: No. 668, No. 23 Street, Hangzhou Economic and Technological Development Zone, Zhejiang Province
Postal Code: 310018
Telephone number: (0571) 85318276 85318271
Fax number: (0571) 85318270
Website: www.aoyipollen.com
Manufacturer
Company name: Hangzhou Ao Medical Pauling Pharmaceutical Co.
Address: No. 668, No. 23 Street, Hangzhou Economic and Technological Development Zone, Zhejiang Province
Postal code: 310018
Telephone number: (0571) 85318276 85318271
Fax number: (0571) 85318270
Website: www.aoyipollen.com