AZELASTINE HYDROCHLORIDE- azelastine hydrochloride solution/ drops
Azelastine Hydrochloride Ophthalmic Solution, 0.05% is sterile ophthalmic solution containing azelastine hydrochloride, relatively selective H1 -receptor antagonist for topical administration to the eyes. Azelastine hydrochloride is white crystalline powder with 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 racemic mixture with 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
mpirical chemical structure: C22 H24 ClN3 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: 0.125 mg benzalkonium chloride; Inactives: disodium edetate dihydrate, hypromellose, sorbitol solution, sodium hydroxide and water for injection. It has pH of approximately 5.0 to 6.5 and an osmolarity of approximately 271 to 312 mOsmol/L.
Azelastine hydrochloride is relatively selective histamine H1 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.
INDICATIONS AND USAGE
Azelastine Hydrochloride Ophthalmic Solution, 0.05% is indicated for the treatment of itching of the eye associated with allergic conjunctivitis.
Azelastine Hydrochloride Ophthalmic Solution, 0.05% is contraindicated in persons with known or suspected hypersensitivity to any of its components.
Azelastine Hydrochloride Ophthalmic Solution, 0.05% is for ocular use only and not for injection or oral use.
info. 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 contact lens if their eye is red. Azelastine Hydrochloride Ophthalmic Solution, 0.05% should not be used to treat contact lens related irritation. The preservative in Azelastine Hydrochloride Ophthalmic Solution, 0.05%, 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, 0.05% before they insert their contact lenses.
Teratogenic Effects: Pregnancy Category C.
Safety and effectiveness in pediatric patients below the age of have not been established.
No overall differences in safety or effectiveness have been observed between elderly and younger adult patients.
In controlled multiple-dose studies where patients were treated for up to 56 days, the most frequently reported adverse reactions were transient eye burning/stinging (approximately 30%), headaches (approximately 15%) and bitter taste (approximately 10%). The occurrence of these events was generally mild.
The following events were reported in 1?10% of patients: asthma, conjunctivitis, dyspnea, eye pain, fatigue, influenza-like symptoms, pharyngitis, pruritus, rhinitis and temporary blurring. Some of these events were similar to the underlying disease being studied.
DOSAGE AND ADMINISTRATION
The recommended dose is one drop instilled into each affected eye twice day.
Azelastine Hydrochloride Ophthalmic Solution, 0.05% is supplied sterile in natural LDPE plastic DROP-TAINER* bottle with natural LDPE dropper tip and white polypropylene cap as follows:
6 mL in mL bottle NDC 61314-308-02
Azelastine Hydrochloride Ophthalmic Solution, 0.05% mL container: STORE UPRIGHT between 2? and 25?C (36? and 77?F).
*DROP-TAINER is registered trademark of Alcon Research, Ltd.