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Azelastine hydrochloride structure

Azelastine hydrochloride

Azelastine hydrochloride, with the chemical formula C22H24ClN3O and CAS registry number 79307-93-0, is a compound used primarily as a nasal spray for the treatment of allergic rhinitis. It belongs to the class of antihistamines and works by blocking the effects of histamine, a substance in the body that causes allergy symptoms. Azelastine hydrochloride is known for its ability to relieve symptoms such as sneezing, itching, runny nose, and nasal congestion. It is also used in combination with fluticasone propionate for the treatment of seasonal allergic rhinitis. This compound is typically administered as a nasal spray and is generally well-tolerated, with common side effects including bitter taste, headache, and nasal irritation. Azelastine hydrochloride is an important medication in the management of allergic rhinitis, providing relief for individuals suffering from nasal allergies.
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1. Names and Identifiers
1.1 Name
Azelastine hydrochloride
1.2 Synonyms
4-[(4-chlorophenyl)methyl]-2-(1-methylazepan-4-yl)-phthalazin-1-one hydrochloride; 4-[(4-Chlorophenyl)methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1(2H)-phthalazinone Hydrochloride; a5610; AZELASTINE HCL; azeptin; e-0659; w-2979m;
1.3 CAS No.
79307-93-0
1.5 EINECS
620-469-0
1.6 Molecular Formula
C22H25Cl2N3O
1.7 Inchi
InChI=1/C22H24ClN3O.ClH/c1-25-13-4-5-18(12-14-25)26-22(27)20-7-3-2-6-19(20)21(24-26)15-16-8-10-17(23)11-9-16;/h2-3,6-11,18H,4-5,12-15H2,1H3;1H
1.8 InChkey
YEJAJYAHJQIWNU-UHFFFAOYNA-N
1.9 Canonical Smiles
Cl[H].CN1CCCC(CC1)N1N=C(CC2=CC=C(Cl)C=C2)C2=C(C=CC=C2)C1=O
1.10 Isomers Smiles
CN1CCCC(CC1)N2C(=O)C3=CC=CC=C3C(=N2)CC4=CC=C(C=C4)Cl.Cl
2. Properties
2.1 StorageTemp
Inert atmosphere,Store in freezer, under -20°C
3. Use and Manufacturing
3.1 Description

Azelastine hydrochloride, with the chemical formula C22H24ClN3O, has the CAS number 79307-93-0. It is a white or almost white crystalline powder. Azelastine hydrochloride has no characteristic odor. Its basic structure consists of a hydrochloride salt of azelastine, which is an antihistamine. This compound is freely soluble in water and in methanol, slightly soluble in ethanol, and practically insoluble in ether. Azelastine hydrochloride is stable under normal conditions of use and storage. It is not reactive with common materials and is not considered to be a fire hazard. However, it may be irritating to the eyes, skin, and respiratory system. It is recommended to handle this compound with care and use appropriate protective measures.

Applicable Fields

Allergy Treatment: Azelastine hydrochloride is commonly used in the treatment of allergies. Its mechanism of action involves blocking the effects of histamine, a substance in the body that causes allergic symptoms such as itching, sneezing, and runny nose. Azelastine hydrochloride helps relieve these symptoms by reducing the release of histamine and other chemicals in the body.

Nasal Congestion: This compound is also used to relieve nasal congestion associated with seasonal allergies and allergic rhinitis. It works by reducing the swelling and inflammation in the nasal passages, allowing for easier breathing and relieving congestion.

Storage

Conditions: Store in a cool and dry place.

4. MSDS

2.Hazard identification

2.1 Classification of the substance or mixture

no data available

2.2 GHS label elements, including precautionary statements

Pictogram(s) no data available
Signal word

no data available

Hazard statement(s)

no data available

Precautionary statement(s)
Prevention

no data available

Response

no data available

Storage

no data available

Disposal

no data available

2.3 Other hazards which do not result in classification

no data available

5.Other Information
Merck
14,906
Target
Value
Description
Azelastine hydrochloride is an orally effective antihistamine useful in the treatment of asthma and nasal allergy. It appears to inhibit release of histamine, in addition to antagonizing its action.
Chemical Properties
White or almost white, crystalline powder.
Originator
Asta-Werke(Degussa) (W. Germany)
Uses
Orally active H1-hystamine receptor antagonist. Antihistaminic
Definition
ChEBI: The hydrochloride salt of azelastine.
Brand name
Astelin (Medpointe); Optivar (Medpointe);AZEPTIN.
General Description
(±)-4-[(4-chlorophenyl)methyl]-2-(hexahydro-l-methyl-1H-azepin-4-yl)-l-(2H)-phthalazinone monohydrochloride (Optivar), is a whitecrystalline powder that is sparingly soluble in water,methanol, and propylene glycol and slightly soluble inethanol, octanol, and glycerine. The commercial preparationis available as a 0.05% sterile ophthalmic solution fortopical administration to the eyes. Each milliliter of azelastinesolution contains 0.5-mg azelastine hydrochlorideequivalent to 0.457 mg of azelastine base, the preservativebenzalkonium chloride (0.125 mg), and inactive ingredientsincluding disodium edetate dihydrate, hydroxypropylmethylcellulose,sorbitol solution, sodium hydroxide, andwater for injection. The solution has a pH of approximately5.0 to 6.5 and an osmolality of approximately 271to 312 mOsm/L.
The recommended dose of azelastine solution is 1 dropinstilled into each affected eye twice a day. This drugproduct is for ocular administration only and not for injectionor oral use. Absorption of azelastine following ocularadministration is relatively low (less than 1 ng/rnL).Absorbed drug undergoes extensive oxidative N-demethylationby CYP, and the parent drug and metabolite are eliminatedprimarily in the feces. The most frequently reportedadverse reactions are transient eye burning or stinging,headaches, and bitter taste. Azelastine solution should beused with caution during pregnancy or while nursing, becauseits safety has not been studied under these circumstances.
Biochem/physiol Actions
H1 histamine receptor antagonist; NF-kB activator.
Safety Profile
Poison by ingestion andintravenous routes. An experimental teratogen. Otherexperimental reproductive effects. When heated todecomposition it emits toxic fumes of NOx and HCl.
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7. Related Questions
What is Azelastine Hydrochloride and How Does it Benefit Patients with Chronic Rhinitis? Introduction Azelastine hydrochloride is an intranasal antihistamine used for seasonal allergic rhinitis (SAR) and nonallergic vasomotor rhinitis (VMR). Approximately 60 million people in the US suff..
What are the benefits and instructions for using Azelastine hydrochloride?Azelastine hydrochloride is an antihistamine with multiple mechanisms of action and can also inhibit the release of inflammatory mediators from mast cells. There are several formulations and specifica..
Does Azelastine Hydrochloride Provide Relief for Allergic Rhinitis?Azelastine hydrochloride (azelastine) nasal spray is an H1 receptor antagonist commonly used to treat allergic rhinitis and alleviate symptoms. However, the effects of azelastine on nasal mucosal cong..
How to prepare Azelastine hydrochloride?Background and overview[1] The chemical formula of Azelastine hydrochloride is 4-(4-chlorobenzyl)-2-(hexahydro-1-methyl-1H-azepine-4-yl)-1-(2H)-phthalazine hydrochloride , was developed by Germany's A..
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