Ebastine Powder Raw Material

CAS: 90729-43-4

MF: C32H39NO2

Specification​: 99% min Ebastine

Sample:  Ebastine Powder

Brand: Henrikang

Appearance: White Powder

Storage: Cool Dry Place

Shelf Life: 2 Years

Test Method: HPLC

Ebastine Powder Usage and Synthesis:

Ebastine Powder is an antihistamine drug raw material. Antihistamines are a class of drugs that can compete with histamine for histamine receptors on cells, so that histamine cannot bind to receptors, thereby producing antihistamine effects. According to histamine Different receptor types, antihistamines can be divided into H1 receptor blockers and H2 receptor blockers. Vasodilation and smooth muscle contraction can help relieve or eliminate allergic symptoms caused by the release of endogenous histamine. It is mainly used to prevent and treat skin and mucous membrane allergic diseases, motion sickness and vomiting. Ebastine, cetirizine hydrochloride, loratadine, levocetirizine, and mizolastine are currently several commonly used anti-H1 receptor antihistamines without sedative effect, which belong to anti-allergic drugs. It is characterized by no or little sedative effect on the central nervous system, stronger antihistamine effect, can significantly inhibit the flush and wheal caused by histamine, and does not affect the release of histamine from mast cells.

Pharmacokinetics of Ebastine Powder:
Both Ebastine and its active metabolite, Carebastine, are peripherally selective histamine H1 receptor antagonists, without obvious central nervous system effects and anticholinergic effects. Neither the drug nor its metabolites can cross the blood-brain barrier.
Ebastine has a rapid and long-acting histamine inhibitory effect, and has a super affinity for histamine H1 receptors. When administered orally, ebastine and its metabolites cannot cross the blood-brain barrier. This explains the slight sedative effect of ebastine on the central nervous system observed during the trial. It is used for allergic rhinitis (seasonal and perennial) with or without allergic conjunctivitis, symptomatic treatment of chronic idiopathic urticaria, and eczema, dermatitis, prurigo, pruritus, etc. When ebastine is taken with food at the same time, the blood concentration and its basic active product after metabolism will increase by 1.5-2.0 under the action of certain factors. However, this increase does not affect the time to peak plasma concentration, and taking it with food does not affect the clinical efficacy of ebastine.

Clinical Application of Ebastine Powder:
Clinically, it mainly treats various allergic diseases, such as chronic idiopathic urticaria, seasonal and perennial allergic rhinitis, and skin pruritus. For adults to treat chronic urticaria or allergic rhinitis, po, 10mg, qd; for children, the dose is 5mg, qd. High-dose ebastine 20mg, qd is only used for adults with severe allergic diseases, and better curative effect will be achieved if taken in the morning. Ebastine mainly has anti-allergic effect, belongs to the second-generation antihistamine drug, and is mainly suitable for the treatment of allergic diseases, such as urticaria, eczema, and rhinitis. However, the onset of ebastine is relatively slow, and it takes about 1-3 hours, so ebastine cannot be used if acute allergic symptoms occur. In addition, those who suffer from severe liver failure must reduce the dosage. After taking ebastine, breastfeeding is not allowed, because the milk will contain drug ingredients, so breastfeeding must be stopped. Ebastine needs to be swallowed whole and not chewed, broken or crushed. If a skin allergy test is required during the medication, it must be done 5-7 days after the drug is stopped, otherwise the allergic symptoms may be covered up. The main side effects of ebastine after taking ebastine are headache, drowsiness or dry mouth.