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Sterile, clear colourless aqueous solution containing azelastine hydrochloride 0.05 % w/v. Each drop contains azelastine hydrochloride 0.015 mg.
Azelastine, a phthalazinone derivative of novel structure is classified as a potent long-acting anti-allergic compound with particularly strong, selective H1 antagonist properties. An additional anti-inflammatory effect could be detected after topical ocular administration (higher local concentrations).
Data from in vivo pre-clinical and in vitro studies show that azelastine inhibits the synthesis or release of the chemical mediators known to be involved in early and late stage allergic reactions e.g. leukotriene, histamine, PAF inhibitors and serotonin.
To date, long term ECG evaluations of patients treated with high oral doses of azelastine, have shown that in multiple dose studies, there is no clinically significant effect of azelastine on the corrected QT (QTc) interval.
No association of azelastine with ventricular arrhythmia or torsades de pointes was observed in over 3700 patients treated with oral azelastine.
Following oral administration azelastine is rapidly absorbed showing an absolute bioavailability of 81%. Food has no influence on absorption. The volume of distribution is high indicating distribution predominantly into the periphery. The level of protein binding is relatively low (80 to 90%, a level too low to give concern over drug displacement reactions).
Plasma elimination half lives after a single dose of azelastine are approximately 20 hours for azelastine and about 45 hours for the therapeutically active metabolite N-desmethylazelastine. Excretion occurs mainly via the faeces. The sustained excretion of small amounts of the dose in the faeces suggests that some enterohepatic circulation may take place.
After repeated ocular application of EYEZEP eye drops (up to one drop in each eye, four times daily), Cmax steady state plasma levels of azelastine hydrochloride were very low and were detected at or below the limit of quantification.
Symptomatic treatment and prevention of seasonal allergic conjunctivitis in adults and children 4 years and older.
The usual dosage for adults and children 4 years or older is one drop into each eye twice daily that can be increased, if necessary, to four times daily.
If pollen exposure is anticipated EYEZEP eye drops should be administered prophylactically, prior to the exposure.
Treatment should be continued as long as required for relief of symptoms.
Proven allergy to any of the components of EYEZEP eye drops.
As with other ophthalmic solutions, EYEZEP eye drops is not recommended for use whilst wearing contact lenses.
EYEZEP eye drops are not intended for treatment of eye infections.
Azelastine hydrochloride displayed no sensitising potential in the guinea pig. Azelastine demonstrated no genotoxic potential in a battery of in vitro and in vivo tests, nor any carcinogenic potential in rats or mice.
In male and female rats, azelastine at oral doses greater than 30 mg/kg/day caused a dose-related decrease in the fertility index; no substance-related alterations were found in the reproductive organs of males or females during chronic toxicity studies, however.
Embryotoxic and teratogenic effects in rats, mice and rabbits occurred only at maternal toxic doses (for example, skeletal malformations were observed in rats and rabbits at doses of 50 mg/kg/day).
There is insufficient information available to establish the safety of azelastine in human pregnancy. At high oral doses azelastine has shown to induce adverse effects (foetal death, growth retardation and skeletal malformation) in experimental animals. Local ocular application will result in minimal systemic exposure (picogram range). However, caution should be exercised when using EYEZEP eye drops during pregnancy.
Azelastine is excreted into the milk in low quantities. For that reason EYEZEP eye drops is not recommended during lactation.
Azelastine is presumed to be safe or unlikely to produce an effect on the ability to drive or use machinery. Patients with seasonal allergic conjunctivitis are likely to experience watery and itchy eyes which may affect vision. The mild, transient irritation which can be experienced after application of EYEZEP eye drops is unlikely to affect vision to any greater extent.
Occasionally, a mild, transient irritation in the eye after application of EYEZEP eye drops is experienced. Less frequently reported is a bitter taste.
No specific interaction studies with EYEZEP eye drops have been performed.
Interaction studies at high oral doses have been performed however they bear no relevance to EYEZEP eye drops, as systemic levels, after administration of the eye drops, are in the picogram range.
No specific reactions after ocular overdosage are known, and with the ocular route of administration, overdosage reactions are not anticipated.
There is no experience with the administration of toxic doses of azelastine hydrochloride in humans. In the case of overdose or intoxication, disturbances of the central nervous system are to be expected based on the results of animal experiments. Treatment of these disorders must be symptomatic. There is no known antidote.
Shelf life 36 months. Store below 30 °C. Do not use for longer than 4 weeks after first opening.
Prescription Medicine
6 ml in a dropper bottle.
Azelastine hydrochloride is hydrochloride salt of 4-(4-chlorobenzyl)-2-(1-methylperhydroazepin-4-yl)-1(2H)-phtalazinone. It has a molecular formula and weight of C22H27Cl2N3O and 420.38 respectively.
Other ingredients of EYEZEP eye drops are: sorbitol, disodium edeteate, hydroxypropyl methylcellulose, benzalkonium chloride and water for injection.
Douglas Pharmaceuticals Ltd
PO Box 45 027
AUCKLAND 1230
Telephone: (09) 835 0660
28 July 2004