1. Name Of The Medicinal Product
Rhinolast® Nasal Spray
2. Qualitative And Quantitative Composition
Azelastine Hydrochloride 0.1% w/v
3. Pharmaceutical Form
Nasal spray
4. Clinical Particulars
4.1 Therapeutic Indications
For the treatment of both seasonal allergic rhinitis (e.g. hayfever)
and perennial allergic rhinitis.
4.2 Posology And Method Of Administration
Route of application is topical - nasal mucosa.
Adults
One application (0.14 ml) in each nostril twice daily (0.56 mg of azelastine hydrochloride).
Elderly
There have been no specific studies in the elderly.
Children
For children aged 5 years and older, one application (0.14 ml) in each nostril twice daily (0.56 mg of azelastine hydrochloride).
4.3 Contraindications
Proven allergy against azelastine hydrochloride.
4.4 Special Warnings And Precautions For Use
None.
4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction
No specific interactions have been studied.
4.6 Pregnancy And Lactation
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.
4.7 Effects On Ability To Drive And Use Machines
None.
4.8 Undesirable Effects
In rare cases, a mild, transient irritation of the inflamed nasal mucosa may occur, with symptoms such as stinging, itching, sneezing and epistaxis.
More frequently a substance-specific bitter taste may be experienced after administration (often due to incorrect method of application, namely tilting the head too far backwards during administration) which, in rare cases, may lead to nausea.
4.9 Overdose
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.
5. Pharmacological Properties
5.1 Pharmacodynamic Properties
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.
5.2 Pharmacokinetic Properties
After repeated nasal application (0.14 mg) into each nostril twice daily, the plasma levels of azelastine were about 0.26 ng/ml. The levels of the active metabolite desmethylazelastine were detected at or below the lower limit of quantification (0.12 ng/ml).
After repeated oral administration, the mean Cmax steady state plasma levels were determined giving 3.9 ng/ml for azelastine and 1.86 ng/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 suggest that some enterohepatic circulation may take place.
5.3 Preclinical Safety Data
Nothing relevant.
6. Pharmaceutical Particulars
6.1 List Of Excipients
Hypromellose, disodium edetate, , citric acid anhydrous, disodium phosphate dodecahydrate, sodium chloride, purified water.
6.2 Incompatibilities
None.
6.3 Shelf Life
Three years unopened.
6.4 Special Precautions For Storage
Do not store below 8°C. Do not refrigerate.
6.5 Nature And Contents Of Container
Polyethylene bottle with polypropylene cap and polyethylene seal containing either 10 ml or 20 ml.
Glass bottle with screw closure and polypropylene seal containing 10 ml, 20 ml or 22 ml.
Glass bottle with pump attached containing 10 ml, 20 ml or 22 ml.
10 ml glass bottle with pump attached, containing 5 ml aqueous solution.
10 ml polyethylene bottle with polypropylene cap and polyethylene seal, containing 5 ml aqueous solution.
6.6 Special Precautions For Disposal And Other Handling
For separate bottle and pump
Open the bottle by unscrewing the cap. Place the spray pump nozzle in the bottle and screw the pump onto 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.
Discard product six months after first opening.
7. Marketing Authorisation Holder
Meda Pharmaceuticals Ltd
249 West George Street
Glasgow
G2 4RB
Trading as:
Meda Pharmaceuticals Ltd
Skyway House
Parsonage Road
Takeley
Bishop's Stortford
CM22 6PU
UK
8. Marketing Authorisation Number(S)
PL 15142/0037
9. Date Of First Authorisation/Renewal Of The Authorisation
14th August 2009
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