Summary of Product Characteristics (SmPC) - Rhinolast nasal spray
1 NAME OF THE MEDICINAL PRODUCT
Rhinolast® Nasal Spray
2 QUALITATIVE AND QUANTITATIVE COMPOSITION
Solution containing 0.1% w/v azelastine hydrochloride
One actuation (0.137 ml) contains: 0.137 mg azelastine hydrochloride equivalent to 0.125 mg azelastine.
For the full list of excipients, see section 6.1.
3 PHARMACEUTICAL FORM
Nasal spray
Clear, colourless solution
4 CLINICAL PARTICULARS
4.1 Therapeutic indications
For the treatment of both seasonal allergic rhinitis (e.g. hayfever) and perennial allergic rhinitis in patients aged 6 years and over.
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
No dose adjustment necessary for Rhinolast spray.
Children
For children aged 6 years and older, one application (0.14 ml) in each nostril twice daily (0.56 mg of azelastine hydrochloride).
4.3 Contraindications
Hypersensitivity to the active substance or to any of the excipients listed in section 6.1.
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 Fertility, pregnancy and lactation
Pregnancy
There are no or limited amount of data from the use of azelastine in pregnant women. At high oral doses reproductive toxicity has been seen in animals (see section 5.3). Therefore, caution should be exercised when using azelastine nasal spray during pregnancy.
Breastfeeding
It is unknown whether azelastine/metabolites are excreted in human milk. Therefore, caution should be exercised when azelastine is administered to a nursing woman.
Fertility
Effects on fertility were seen in animal studies (see section 5.3).
4.7 Effects on ability to drive and use machines
Azelastine has minor influence on the ability to drive and use machines.
Rarely, the patient may experience fatigue, dizziness or weakness due to the disease itself, or when using Rhinolast spray. In these cases, the ability to drive and use machines may be impaired. Special attention should be paid to the fact that alcohol may enhance these effects.
4.8 Undesirable effects
Commonly, dysgeusia, a substance-specific unpleasant 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.
Adverse events are listed below by system organ class and frequency. Frequencies are defined as:
Very common (≥ 1/10);
Common (≥ 1/100 to < 1/10);
Uncommon (≥ 1/1,000 to < 1/100);
Rare (≥ 1/10,000 to < 1/1,000);
Very rare (< 1/10,000), not known (cannot be estimated from the available data).
MedDRA system organ class | Common ≥1/100 to <1/10 | Uncommon ≥1/1,000 to <1/100 | Rare ≥1/10,000 to <1/1,000 | Very rare ≤1/10,000 |
| Immune system disorders | Hypersensitivity | |||
| Nervous system disorders | Dysgeusia (bitter/unpleasant taste) | Dizziness* | ||
| Respiratory, thoracic and mediastinal disorders | Nasal discomfort (stinging, itching), Sneezing, Epistaxis | |||
| Gastrointestinal disorders | Nausea | |||
Skin and subcutaneous tissue disorders | Rash, Pruritus, Urticaria | |||
| General disorders | Fatigue*, Weakness* |
* These adverse reactions occur very rarely and may also be caused by the disease itself (see also section 4.7).
Reporting of suspected adverse reactions
Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via the Yellow Card Scheme at: http://www.mhra.gov.uk/yellowcard or search for MHRA Yellow Card in the Google Play or Apple App Store.
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
Pharmacotherapeutic group: Decongestants and other nasal preparations for topical use, Antiallergic agents, excl. corticosteroids. 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.
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
Azelastine hydrochloride displayed no sensitizing 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 3.0 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.
Embryotoxic and teratogenic effects in rats, mice and rabbits (foetal death, growth retardation and an increased incidence of skeletal abnormalities) occurred only at maternal toxic doses (for example in mice and rats at doses of 68.6 mg/kg/day).
Effects in non-clinical studies were observed only at human equivalent doses considered sufficiently in excess of the maximum human exposure indicating little relevance to clinical use.
6 PHARMACEUTICAL PARTICULARS
6.1 List of excipients
Hypromellose, disodium edetate, citric acid, 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 8ºC. Do not refrigerate.
6.5 Nature and contents of container
10 ml or 20 ml polyethylene bottle with polypropylene cap and polyethylene seal.
10 ml or 20 ml or 22ml glass bottle with screw closure and polypropylene seal.
10 ml or 20 ml or 22ml glass bottle with pump attached.
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
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
Cooper Consumer Health B.V.,
Verrijn Stuartweg 60,
1112 AX Diemen,
The Netherlands
8 MARKETING AUTHORISATION NUMBER(S)
PL 60682/0007
9 DATE OF FIRST AUTHORISATION/RENEWAL OF THE
AUTHORISATION
14 May 2002
10 DATE OF REVISION OF THE TEXT
02/09/2025