Rhinolast 140 micrograms per Spray, Nasal Spray

Azelastine Hydrochloride 0.1 % w/v.

Each spray actuation delivers 0.14 ml containing 140 micrograms azelastine hydrochloride per spray.

For excipients, see 6.1.

Nasal spray, solution

A clear, colourless, aqueous solution.

For the treatment of both seasonal allergic rhinitis (e.g. Hay fever) and perennial allergic rhinitis.

Adults and children aged 12 years and over

The standard dose is one application (0.14 ml) into each nostril twice daily (0.56 mg of azelastine hydrochloride per day).

For moderate to severe rhinitis (particularly in cases in which nasal blockage is a major presenting symptom), the dose may be increased to two applications into each nostril twice daily (1.12 mg of azelastine hydrochloride per day).

Elderly

There have been no specific studies in the elderly.

Children

For children aged from 5 to 12 years, the dose is one application (0.14 ml) into each nostril twice daily (0.56 mg of azelastine hydrochloride per day).

Method of Administration

For separate bottle and pump

Open the bottle by unscrewing the cap. Place the spray pump nozzle in the bottle and screw the pump into the bottle. Remove the protective cap. Before first using, squeeze down the collar several times until an even spray emerges. The Rhinolast spray is now ready to use.

For attached pump and bottle

Remove the protective cap. Before first using, squeeze down the collar several times until an even spray emerges. The Rhinolast spray is now ready to use.

Proven allergy against azelastine hydrochloride.

See 4.5, 4.6 and 4.7.

No specific interactions have been studied.

At high oral doses in animals, 500 times the proposed oral human daily dose, foetal death, growth retardation and an increased incidence of skeletal abnormalities occurred during reproduction toxicity testing. Due to the nasal route of administration and the low dose administered, minimal systemic exposure can be expected. However as with all medicines caution should be exercised with use during pregnancy and lactation.

None.

Common (1-10%)- A bitter taste may be experienced after administration (often due to incorrect method of application, i.e. tilting the head too far backwards, which may, in rare cases, lead to nausea. This occurs more frequently at the higher dose level.

Uncommon (01-1%) -A mild, transient irritation of the nasal mucosa may cause stinging, itching, sneezing and epistaxis.

Very rarely (< 0.01%)- Hypersensitivity reactions such as rash, pruritus and urticaria.

*Reported for formulations containing benzalkonium chloride.

The results of animal studies show that toxic doses can produce CNS symptoms, e.g. excitation, tremor, convulsions. Should these occur in humans, symptomatic and supportive treatment should be instigated as there is no specific antidote. Gastric lavage is recommended if the overdose is recent.

With the nasal route of administration overdosage reactions are not anticipated.

ATC Code: R01AC03.

Azelastine, a phthalazinone derivative of novel structure, is classified as a potent long acting anti-allergic compound with particularly strong H1 antagonist properties.

Data from animal studies show that where high levels of azelastine are achieved both inhibition and release of chemical mediators (e.g. leukotriene, histamine, serotonin) involved in allergic reaction occurs.

After repeated nasal application (0.14 mg) into each nostril twice daily, the plasma levels of azelastine were about 0.26ng/ml. The levels of the active metabolite desmethylazelastine were detected at or below the lower limit of quantification (0.12ng/ml).

After repeated oral administration, the mean Cmax steady state plasma levels were determined giving 3.9ng/ml for azelastine and 1.86ng/ml for desmethylazelastine after 2.2 mg b.i.d. azelastine which represents the therapeutic oral dose for the treatment of allergic rhinitis.

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 to the peripheral tissues. The level of protein binding is low (80-95%, 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 N-desmethylazelastine (a therapeutically active metabolite). 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.

Nothing relevant.

Hypromellose

Disodium Edetate

Citric Acid Anhydrous

Disodium Phosphate Dodecahydrate

Sodium Chloride

Purified Water

Not applicable.

3 years unopened.

6 months after first opening.

Do not store below 8°C. Do not refrigerate.

Polyethylene bottle with polypropylene cap and polyethylene seal, containing 10ml or 20ml of aqueous solution.

Glass bottle (brown; hydrolytic Type III) with screw closure and polypropylene seal, containing 10ml or 20ml of aqueous solution.

Glass bottle (brown; hydrolytic Type III) with pump attached, containing 10ml or 20ml of aqueous solution.

10ml glass bottle (brown; hydrolytic Type III) with pump attached, containing 5ml of aqueous solution.

10ml polyethylene bottle with polypropylene cap and polyethylene seal, containing 5ml of aqueous solution.

Not all pack sizes may be marketed.

No special requirements.

Meda Health Sales Ireland Ltd. Unit

34/35, Block A,

Dunboyne Business Park Dunboyne

Co. Meath,

PA 1332/15/1

Date of first authorisation: 15 December 1994

Date of last renewal: 15 December 2004

November 2006