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Azelastine hydrochloride

Azelastine hydrochloride structure

CAS No:
79307-93-0
Formula:
C22H24ClN3O.ClH
Chemical Name:
Azelastine hydrochloride
Synonyms:
1(2H)-Phthalazinone,4-[(4-chlorophenyl)methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)-,hydrochloride (1:1);1(2H)-Phthalazinone,4-[(4-chlorophenyl)methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)-,monohydrochloride;Azelastine hydrochloride;A 5610;Azeptin;E 0659;Allergodil;Astelin;Rhinolast;W 2979M;Optivar;Astepro;Zalastine;Azelast
Categories:
Active Pharmaceutical Ingredients > Antiallergic Drugs

Description

Azelastine HCl is a potent, second-generation, selective, histamine antagonist.Target: Histamine ReceptorAzelastine is a selective H(1)-receptor antagonist that inhibits histamine release and interferes with activation of several other mediators of allergic inflammation. Azelastine can inhibit CHMCs activation and release of IL-6, tryptase, and histamine. On an equimolar basis, azelastine was a more potent inhibitor than olopatadine [1]. Topical azelastine progressively improved itching

Azelastine hydrochloride is the hydrochloride salt of azelastine. It has a role as a platelet aggregation inhibitor, a bronchodilator agent, an anti-asthmatic drug, an anti-allergic agent, a H1-receptor antagonist and an EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor. It contains an azelastine.

Azelastine hydrochloride Basic Attributes

Molecular Weight：

418.35900

Exact Mass：

417.13700

EC Number：

253-720-4

NSC Number：

758971

DSSTox ID：

DTXSID2045945

HScode：

2933992600

Characteristics

PSA：

38.13000

XLogP3：

5.03740

Appearance：

white crystalline powder

Density：

1.25 g/cm3

Melting Point：

225-229 °C

Boiling Point：

533.9ºC at 760 mmHg

Flash Point：

276.7ºC

Storage Conditions：

-20ºC Freezer

Toxicity：

LD50 in male, female mice, male, female rats (mg/kg): 36.5, 35.5, 26.9, 30.3 i.v.; 56.4, 42.8, 43.2, 46.6 i.p.; 63.0, 54.2, 66.5, 59.6 s.c.; 124, 139, 310, 417 orally (Zechel)

Collision Cross Section：

192.7 Å² [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

Safety Information

Transport codes：

NONH for all modes of transport

hazard class code：

Marks：

Stability/Shelf Life：

Incompatible with strong oxidizing agents.

Precautionary statement(s)：

P301 + P312 + P330

Hazard Statements：

H302

Drug Information

Drug Indication：

Treatment of allergic rhinitis, Treatment of rhino-conjuctivitis

MeSH：

A class of non-sedating drugs that bind to but do not activate histamine receptors (DRUG INVERSE AGONISM), thereby blocking the actions of histamine or histamine agonists. These antihistamines represent a heterogenous group of compounds with differing chemical structures, adverse effects, distribution, and metabolism. Compared to the early (first generation) antihistamines, these non-sedating antihistamines have greater receptor specificity, lower penetration of BLOOD-BRAIN BARRIER, and are less likely to cause drowsiness or psychomotor impairment. (See all compounds classified as Histamine H1 Antagonists, Non-Sedating.)|Compounds that bind to and inhibit that enzymatic activity of LIPOXYGENASES. Included under this category are inhibitors that are specific for lipoxygenase subtypes and act to reduce the production of LEUKOTRIENES. (See all compounds classified as Lipoxygenase Inhibitors.)|Agents that are used to treat allergic reactions. Most of these drugs act by preventing the release of inflammatory mediators or inhibiting the actions of released mediators on their target cells. (From AMA Drug Evaluations Annual, 1994, p475) (See all compounds classified as Anti-Allergic Agents.)|Agents that cause an increase in the expansion of a bronchus or bronchial tubes. (See all compounds classified as Bronchodilator Agents.)

MeSH Entry Terms：

4-((4-chlorophenyl)methyl)-2- (hexahydro-1-methyl-1H-azepin-4-yl)-1(2H)- phthalazinone HCl

Azelastine hydrochloride Use and Manufacturing

Uses

Orally active H1-hystamine receptor antagonist. Antihistaminic Pharmacological effects: Azelastine hydrochloride and its main metabolites are histamine H1 receptor antagonists, which have antihistamine effects. 2. Toxicological research: Genotoxicity: Ames test, DNA damage repair test, mouse lymphocyte positive mutation test, mouse micronucleus test and rat bone marrow chromosome aberration test have not found genetic toxicity.

Use Classification：

Human Drugs -> EU pediatric investigation plans|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:418.4
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:3
Rotatable Bond Count:3
Exact Mass:417.1374678
Monoisotopic Mass:417.1374678
Topological Polar Surface Area:35.9
Heavy Atom Count:28
Complexity:558
Undefined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

Drug Function and Efficacy

It is a new structural derivative of 2,3-phthalazinone, a potential long-acting antiallergic compound with the characteristics of H1 receptor antagonist. Animal experimental data show that high concentrations of azelastine hydrochloride can prevent the synthesis and release of certain chemical mediators in allergic reactions (such as leukotrienes, histamine, 5-hydroxytryptamine) and can prevent the upregulation of I-CAMI and the migration of eosinophils to play a wide range of anti-inflammatory effects. When administered by nasal spray, no local toxicity or organ-specific toxicity was detected at the maximum dose allowed.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Azelastine hydrochloride nasal spray
Ingredients	Azelastine hydrochloride. Molecular weight: C22H24ClN3O
Indication	This product is prohibited when drinking alcohol or using central nervous system depressants, otherwise it will aggravate central nervous system depression. Oral administration of azelastine hydrochloride (4 mg twice a day) and oral administration of cimetidine (150 mg twice a day) can increase the bioavailability of azelastine hydrochloride by 65%. Oral administration of azelastine hydrochloride and erythromycin (500 mg 3 times a day for 7 consecutive days) and ketoconazole (200 mg twice a day for 7 consecutive days) respectively. Erythromycin has no effect on the pharmacokinetics and QT interval of azelastine hydrochloride. Ketoconazole has no effect on the QT interval, but interferes with the determination of blood concentrations of azelastine hydrochloride. (See the instructions inside the package for details)
Specifications	10ml:10mg

Azelastine Hydrochloride
Manufacturer	Guizhou Yunfeng Pharmaceutical Co., Ltd.

Azelastine Hydrochloride Eye Drops
Specifications	6 ml: 3 mg

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Registered Holders

KOREA UNITED PHARMACEUTICALS INC

United States
Active
ZYDUS LIFESCIENCES LTD

United States
Active
CURIA Italy SRL

United States
Active

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