Azelastine hydrochloride 0.5 MG/ML Ophthalmic Solution
Generic Name: AZELASTINE HYDROCHLORIDE
Brand Name: Azelastine Hydrochloride
- Substance Name(s):
- AZELASTINE HYDROCHLORIDE
WARNINGS
Azelastine hydrochloride ophthalmic solution is for ocular use only and not for injection or oral use.
DESCRIPTION
Azelastine hydrochloride ophthalmic solution, 0.05% is a sterile ophthalmic solution containing azelastine hydrochloride, a relatively selective H 1 -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 22 H 24 CIN 3 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.
chemical structure
HOW SUPPLIED
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.
Storage 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].
GERIATRIC USE
Geriatric Use No overall differences in safety or effectiveness have been observed between elderly and younger adult patients.
INDICATIONS AND USAGE
Azelastine hydrochloride ophthalmic solution is indicated for the treatment of itching of the eye associated with allergic conjunctivitis.
PEDIATRIC USE
Pediatric Use Safety and effectiveness in pediatric patients below the age of 3 have not been established.
PREGNANCY
Pregnancy Teratogenic Effects: Pregnancy Category C.
Azelastine hydrochloride has been shown to be embryotoxic, fetotoxic, and teratogenic (external and skeletal abnormalities) in mice at an oral dose of 68.6 mg/kg/day (57,000 times the recommended ocular human use level).
At an oral dose of 30 mg/kg/day (25,000 times the recommended ocular human use level), delayed ossification (undeveloped metacarpus) and the incidence of 14 th rib were increased in rats.
At 68.6 mg/kg/day (57,000 times the maximum recommended ocular human use level) azelastine hydrochloride caused resorption and fetotoxic effects in rats.
The relevance to humans of these skeletal findings noted at only high drug exposure levels is unknown.
There are no adequate and well-controlled studies in pregnant women.
Azelastine hydrochloride ophthalmic solution should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
NUSRING MOTHERS
Nursing Mothers It is not known whether azelastine hydrochloride is excreted in human milk.
Because many drugs are excreted in human milk, caution should be exercised when azelastine hydrochloride ophthalmic solution is administered to a nursing woman.
INFORMATION FOR PATIENTS
Information for Patients To prevent contaminating the dropper tip and solution, care should be taken not to touch any surface, the eyelids or surrounding areas with the dropper tip of the bottle.
Keep bottle tightly closed when not in use.
This product is sterile when packaged.
Patients should be advised not to wear a contact lens if their eye is red.
Azelastine hydrochloride ophthalmic solution should not be used to treat contact lens related irritation.
The preservative in azelastine hydrochloride ophthalmic solution, benzalkonium chloride, may be absorbed by soft contact lenses.
Patients who wear soft contact lenses and whose eyes are not red , should be instructed to wait at least ten minutes after instilling azelastine hydrochloride ophthalmic solution before they insert their contact lenses.
DOSAGE AND ADMINISTRATION
The recommended dose is one drop instilled into each affected eye twice a day.