Azelastine hydrochloride

Bezeichnung:Azelastine hydrochloride

CAS-Nr79307-93-0

Englisch Name:Azelastine hydrochloride

CBNumberCB9256008

SummenformelC22H25Cl2N3O

Molgewicht418.36

MOL-Datei79307-93-0.mol

Azelastine hydrochloride physikalisch-chemischer Eigenschaften

Schmelzpunkt	225--2290C
storage temp.	Inert atmosphere,Store in freezer, under -20°C
Löslichkeit	DMSO: >10mg/mL
Aggregatzustand	powder
Farbe	white to off-white
Merck	14,906
Stabilität	Incompatible with strong oxidizing agents.
InChI	InChI=1S/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
InChIKey	YEJAJYAHJQIWNU-UHFFFAOYSA-N
SMILES	C1(=O)C2=C(C=CC=C2)C(CC2=CC=C(Cl)C=C2)=NN1C1CCCN(C)CC1.[H]Cl
CAS Datenbank	79307-93-0(CAS DataBase Reference)

Sicherheit

Kennzeichnung gefährlicher	Xn
R-Sätze:	22
RTECS-Nr.	TH9203900
HS Code	2933992600
Toxizität	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)

Gefahreninformationscode (GHS)

Azelastine hydrochloride Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
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.
Chemische Eigenschaften
White or almost white, crystalline powder.
Originator
Asta-Werke(Degussa) (W. Germany)
Verwenden
Orally active H1-hystamine receptor antagonist. Antihistaminic
Definition
ChEBI: The hydrochloride salt of azelastine.
Trademarks
Astelin (Medpointe); Optivar (Medpointe);AZEPTIN.
Allgemeine Beschreibung
(±)-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.
Sicherheitsprofil
Poison by ingestion andintravenous routes. An experimental teratogen. Otherexperimental reproductive effects. When heated todecomposition it emits toxic fumes of NOx and HCl.

Azelastine hydrochloride Upstream-Materialien And Downstream Produkte

Azelastine hydrochloride Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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