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:

Fosun Pharma USA 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 72266-141-01) solution in a 10 mL LDPE container with a LDPE dropper tip and a white HDPE screw cap. Storage Store UPRIGHT between 2° and 25°C (36° and 77°F). Rx Only Distributed by: Fosun Pharma USA Inc. Princeton, NJ 08540 Made in India. November 2019 LEA-020311-

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

AZELASTINE HYDROCHLORIDE- AZELASTINE HYDROCHLORIDE SOLUTION/ DROPS
FOSUN PHARMA USA 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: chemical-structure.jpg
Empirical chemical structure: C
H
ClN
O.HCl
Each mL of azelastine hydrochloride ophthalmic solution contains:
Active: 0.5 mg azelastine
hydrochloride, equivalent to 0.457 mg of azelastine base;
Preservative: 0.125 mg benzalkonium
chloride; Inactives: disodium edetate dihydrate, hypromellose,
sorbitol solution, sodium hydroxide and
water for injection. It has a pH of approximately 5.0 to 6.5 and an
osmolarity 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.
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PHARMACOKINETICS AND METABOLISM
Absorption of azelastine following ocular administration was
relatively low. A study in symptomatic
patients receiving one drop of az