What Is Ebastine?

Ebastine (Ebastine) alias Kesting; Eba stop; Sike stop; Ebastel; Kestine, chemical name is 1- (4-tert-butylphenyl) -4- [4- (diphenylmethoxy) Group) -1-piperidinyl] -1-butanone is a non-hygroscopic, white crystalline powder. Molecular formula: C32H39NO2, molecular weight: 469.65800, melting point: 80-82 ° C. Its antihistamine activity is competitive at low concentrations and non-competitive at high concentrations. It is used clinically for allergic diseases, including allergic rhinitis in children, year-round rhinitis in adults, seasonal rhinitis, hay fever and chronic urticaria. ^[1-3]

Drug Name: Ebastine
Alias: Kaisting; Eba stop; Sike stop; Ebastel; Kestine
Foreign name: Ebastine
Main indications: Allergic rhinitis with or without allergic conjunctivitis
Dosage: Detailed below

Adverse reactions: Lethargy, headache, etc.
Main medication contraindications: Patients who are allergic to ebastine or any of the ingredients in the tablet
Dosage form: Tablets 0.5mg, 1mg; nasal spray
Drug type: chemical
CAS: 90729-43-4

Ebastine Basic Information

Chinese name

Chinese alias: Abbastine;

5-amino-tetrazole monohydrate;

1- (4-tert-butylphenyl) -4- [4- (diphenylmethoxy) -1-piperidinyl] -1-butanone;

1- [4- (1,1-dimethylethyl) phenyl] -4- [4- (diphenylmethoxy) -1-piperidinyl] -1-butanone;

English name: 4- (4-benzhydryloxypiperidin-1-yl) -1- (4-tert-butylphenyl) butan-1-one

English alias: Ebastinum [Latin];

carebastine;

4-diphenylmethoxy-1- [3- (4-tert-butylbenzoyl) propyl] -piperidine;

LAS W-090;

Estivan;

Ebastine;

ebastine;

[14C] -Ebastine;

Ebastina [Spanish];

Kestine;

Ebastel;

Ebastin;

CAS number: 90729-43-4 ^[1]

Molecular formula: C32H39NO2

Molecular weight: 469.65800

Chemical Structure:

Exact mass: 469.29800

PSA: 29.54000

LogP: 7.15550 ^[1]

Ebastine physical and chemical properties

Density: 1.09 g / cm3

Melting point: 80-82 ° C

Boiling point: 596.3ºC at 760 mmHg

Flash point: 314.5ºC

Refractive index: 1.59

Storage conditions: Room temp ^[1]

Ebastine Safety Information

RTECS number: EL8140000 ^[1]

Ebastine production method

Alkylation of 4-piperidinol with compound (I) gives compound (II). The alkylation with dityl bromide yields ebastine. ^[1]

Overview of basic information about ebastine drugs

Ebastine drug name

Chinese name: Ebastine

English name: Ebastine

Alias: Kai Siting; Aiba Park; Sike Park; Ebastel; Kestine ^[3]

Classification by basting

Respiratory Drugs> Asthma Drugs> Airway Dilators ^[3]

Ebastine dosage form

0.5mg, 1mg;

2. Nasal spray: 0.1%. ^[3]

Ebastine pharmacological effects

Ebastine is highly selective for H1 receptors and has no central inhibitory effect. Compared with terfenadine, ebastine has a strong and long-lasting effect. Ebastine has a protective effect on histamine-induced bronchospasm. Animal experiments have confirmed that its protective effect is 4.5 times that of terfenadine and 2.9 times that of aspartazol. It does not accumulate after continuous administration. Its metabolite Carebestine protects histamine-induced bronchospasm three times more than the original drug. Ebastine has the effect of antagonizing leukotriene C4, can inhibit the bronchospasm induced by leukotriene C4, and has an anticholinergic effect. Can inhibit experimental wheezing and nasal allergies. ^[3]

Ebastine pharmacokinetics

Ebastine is well absorbed orally, but its plasma concentration is very low or undetectable. Pharmacokinetic studies mainly measure its active metabolite, carebastine. Ebastine takes effect 1 to 2 hours after oral administration, with a tmax of 2.6 to 5.7 hours, which can be maintained for 24 hours, and a plasma protein binding rate of more than 95%. The serum half-life was 13.8 ~ 15.3h. Ebastine has a wide range of first-pass effects and does not accumulate (carebastine). 66% of metabolites are excreted from the urine. In patients with renal insufficiency, the elimination half-life of ebastine can be extended to 23 to 36 hours. In patients with liver insufficiency, the elimination half-life can be extended to 27 hours. Little or no penetration of the blood-cerebrospinal fluid barrier. ^[3]

Ebastine indication

Ebastine can be used for the treatment of allergic rhinitis (allergic rhinitis) and chronic urticaria, 10 mg per day. The effective rate of oral ebastine for 3 months for chronic urticaria is 73%. The patient is well tolerated and can be used as a treatment for chronic urticaria. Because ebastine has a rapid effect, the action time is up to 24 hours, and the central inhibitory effects such as drowsiness are slight, so it can be used as an auxiliary and preventive medicine for the prevention and treatment of allergic asthma. For allergic asthma. ^[3]

Ebastine contraindications

With drowsiness, the driver and dangerous machine operators should be disabled. ^[3]

Ebastine notes

It should be used with caution in pregnant and lactating women. There are no safety data on the use of ebastine in children under 12 years of age. ^[3]

Medication for pregnant and lactating women

Ebastine lacks sufficient validation of women's safety during pregnancy. Animal tests have shown that: Ebastine has no direct or indirect harmful effects on embryo development in early, middle and late pregnancy, and it has not been found to have teratogenic effects in animal tests. No human trials have been conducted. Therefore, ebastine can only be used in pregnant women when absolutely necessary. Whether ebastine is secreted with milk is unclear, so it is contraindicated during lactation. ^[2]

Ebastine medication for children

This product is suitable for children over 2 years old, and the usage and dosage of children over 12 years are the same as adults.
Children 6-11 years old: 5 mg / tablet orally once a day.
Children 2-5 years old: The usual dose is 2.5 mg orally once a day.
Children under 2 years: The safety of this product needs further verification.
Please refer to [Adverse Reactions] for the adverse reactions of children's medication. ^[2]

Ebastine medication for the elderly

There were no statistically significant differences in pharmacokinetics between older subjects and younger adult volunteers.
Dosage adjustment for elderly patients is the same as for adult patients. ^[2]

Ebastine adverse reactions

Visible drowsiness, occasional burnout, the incidence is 3% to 18%; abnormal taste is also more common, the incidence is 2% to 26%; other adverse reactions are rare, such as occasional dry mouth, nausea, numbness of hands, feet Abdominal pain, diarrhea, lack of appetite, facial fever, weight gain, increased transaminase activity, drug rash, etc., the incidence rate is less than 5%.

Ebastine dosage

1. 1-4mg each time, 2 times a day.

2. For patients over 12 years old, spray 2 times per nostril twice a day. Oral: 10 mg each time, once a day. For the prevention and treatment of asthma, 20mg each time, once a night. ^[3]

Interaction of ebastine with other drugs

Ebastine has no effect on various cardiovascular parameters, including QT interval, and even the combination of erythromycin or ketoconazole that can increase the plasma concentration of ebastine did not cause QT interval prolongation. However, as with other antihistamines, caution should be used in patients with known prolonged QT intervals. Ethanol can enhance the central inhibitory effect of ebastine, and it is not advisable to drink alcohol during medication. ^[3]

Ibastine expert review

The long-term efficacy of clinical treatment of chronic urticaria is the same as that of astemizole, terfenadine 120 mg per day or ketotifen 2 mg per day. But astemizole (10mg) started to reduce symptoms more effectively. In the treatment of wind mass, the effective rate of ebastine was 73%, 68% in the terfenadine group, and 52% in the placebo group. The effective rate of ebastine for bronchial asthma is 31.2% more effective, 66.4% more effective; 49.8% more effective for nasal allergies, and 80.2% more effective. Double-blind controlled trials have shown that ebastine is effective. Ebastine is mainly used in the treatment of allergic rhinitis and ophthalmia. It has a lower efficacy in treating asthma and is inferior to other types of anti-asthma drugs. ^[3]