79307-93-0 Usage
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)
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.
Check Digit Verification of cas no
The CAS Registry Mumber 79307-93-0 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 7,9,3,0 and 7 respectively; the second part has 2 digits, 9 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 79307-93:
(7*7)+(6*9)+(5*3)+(4*0)+(3*7)+(2*9)+(1*3)=160
160 % 10 = 0
So 79307-93-0 is a valid CAS Registry Number.
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/t18-;/m1./s1
79307-93-0Relevant articles and documents
Preparation method of azelastine hydrochloride
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, (2021/07/01)
The invention relates to the technical field of synthesis of raw material medicines, and particularly discloses a preparation method of azelastine hydrochloride. The method comprises the following steps: condensing benzoyl hydrazine and 1-methylhexahydroazepine-4-one serving as raw materials, reducing with sodium borohydride, and reacting to obtain a compound 1; preparing a solid intermediate compound 2 from the compound 1 and organic binary weak acid; hydrolyzing the compound 2, and cyclizing with a compound 3 to form a compound 4; and salifying the compound 4 by hydrochloric acid, and separating water by toluene to obtain a compound 5, namely azelastine hydrochloride. The intermediate compound 2 prepared by the invention is a solid, the stability of the intermediate compound 2 is greatly improved compared with that of hydrochloride obtained in other literatures, the intermediate compound 2 is free of hygroscopicity, the purity can reach 99% or above, the quality risk of subsequent bulk drugs can be greatly reduced, and the process production operation space is larger; and the obtained azelastine hydrochloride does not contain water and meets related quality standards, the yield is increased to 80% or above compared with other literatures, and the purity can reach 99% or above.
Use of combinations comprising non-sedating antihistamines and alpha-adrenergic drugs for the topical treatment of rhinitis/conjunctivitis and cold, cold-like and/or flu symptoms
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, (2008/06/13)
Pharmaceutical combination, applicable topically, containing a non-sedating antihistamine in combination with an α-adrenergic agonist and optionally conventional physiologically acceptable carriers, diluting agents and auxiliaries substances for the prophylaxis and treatment of allergic and/or vasomotoric rhinitis, conjunctivitis, cold, cold-like and/ or flu symptoms are claimed.
