AZELASTINE HYDROCHLORIDE solution/ drops

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

AZELASTINE HYDROCHLORIDE (UNII: 0L591QR10I) (AZELASTINE - UNII:ZQI909440X)

Available from:

Sun Pharmaceutical Industries, Inc.

Administration route:

INTRAOCULAR

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Azelastine hydrochloride ophthalmic solution is indicated for the treatment of itching of the eye associated with allergic conjunctivitis. Azelastine hydrochloride ophthalmic solution is contraindicated in persons with known or suspected hypersensitivity to any of its components.

Product summary:

Azelastine hydrochloride ophthalmic solution, 0.05% is supplied as follows: 6 mL (NDC# 47335-938-90) solution in a translucent 10 mL HDPE container with a LDPE dropper tip, and a white HDPE screw cap. STORE UPRIGHT at 20° to 25°C (68° to 77°F); excursions permitted to 15° to 30°C (59° to 86°F) [see USP Controlled Room Temperature].

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

AZELASTINE HYDROCHLORIDE - AZELASTINE HYDROCHLORIDE SOLUTION/ DROPS
SUN PHARMACEUTICAL INDUSTRIES, INC.
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AZELASTINE HYDROCHLORIDE OPHTHALMIC SOLUTION, 0.05%
DESCRIPTION
Azelastine hydrochloride ophthalmic solution, 0.05% is a sterile
ophthalmic solution containing
azelastine hydrochloride, a relatively selective H -receptor
antagonist for topical administration to the
eyes. Azelastine hydrochloride is a white crystalline powder with a
molecular weight of 418.37.
Azelastine hydrochloride is sparingly soluble in water, methanol and
propylene glycol, and slightly
soluble in ethanol, octanol and glycerine. Azelastine hydrochloride is
a racemic mixture with a melting
point of 225°C. The chemical name for azelastine hydrochloride is
(±)-1-(2H)-phthalazinone,4-[(4-
chlorophenyl) methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)-,
monohydrochloride and is represented
by the following chemical structure:
Empirical chemical structure: C
H CIN O•HCl
Each mL of azelastine hydrochloride ophthalmic solution, 0.05%
contains: ACTIVE: 0.5 mg azelastine
hydrochloride, equivalent to 0.457 mg of azelastine base;
PRESERVATIVE: 0.25 mg benzalkonium chloride
solution (50%) USP-NF; INACTIVES: disodium edetate dihydrate,
hypromellose, sorbitol solution,
sodium hydroxide and water for injection. It has a pH of approximately
5 to 6.5 and an osmolality of
approximately 271 to 312 mOsmol/L.
CLINICAL PHARMACOLOGY
Azelastine hydrochloride is a relatively selective histamine H
antagonist and an inhibitor of the release
of histamine and other mediators from cells (e.g., mast cells)
involved in the allergic response. Based
on in-vitro studies using human cell lines, inhibition of other
mediators involved in allergic reactions
(e.g., leukotrienes and PAF) has been demonstrated with azelastine
hydrochloride. Decreased
chemotaxis and activation of eosinophils has also been demonstrated.
PHARMACOKINETICS AND METABOLISM
1
22
24
3
1
Absorption of azelastine following ocular administration was
relatively low. A study in symptomatic
patients re