Consumer medicine information

Azep Nasal Spray

Azelastine hydrochloride


Brand name

Azep Nasal Spray

Active ingredient

Azelastine hydrochloride




Consumer medicine information (CMI) leaflet

Please read this leaflet carefully before you start using Azep Nasal Spray.

What is in this leaflet

This leaflet answers some common questions about AZEP NASAL SPRAY. It does not contain all the available information. It does not take the place of talking to your doctor or pharmacist.

All medicines have risks and benefits.

If you have any concerns about using this medicine, ask your doctor or pharmacist.

Keep this leaflet with the medicine.

You may need to read it again.

What AZEP NASAL SPRAY is used for

AZEP NASAL SPRAY is used to relieve runny nose, sneezing, itching or blocked nose caused by allergies, such as to pollen (hay fever) house dust mites or pet hair.

AZEP NASAL SPRAY belongs to a group of medicines called antihistamines. It works by blocking the action of histamine and other substances produced by the body, which are causing your allergies.

AZEP NASAL SPRAY is not addictive.

Before you use AZEP NASAL SPRAY

When you must not use it

Do not use AZEP NASAL SPRAY if you have an allergy to AZEP NASAL SPRAY or any of the ingredients listed at the end of this leaflet.

Do not give AZEP NASAL SPRAY to a child under 5 years, unless directed by the child’s doctor.

The safety and effectiveness of AZEP NASAL SPRAY in children under 5 years have not been established.

Do not use AZEP NASAL SPRAY after the expiry date printed on the pack.

If you use this medicine after the expiry date has passed, it may not work as well.

Do not use AZEP NASAL SPRAY if the packaging is torn or shows signs of tampering.

If you are not sure whether you should start using AZEP NASAL SPRAY contact your doctor or pharmacist.

Before you start to use it

Tell your doctor or pharmacist if you have allergies to any other medicines, foods, preservatives or dyes.

Tell your doctor or pharmacist if you have or have had any medical conditions, especially the following:

  • Kidney disease

Tell your doctor or pharmacist if you are pregnant or intend to become pregnant, or are breastfeeding.

Your doctor or pharmacist will discuss the possible risks and benefits of using AZEP NASAL SPRAY during pregnancy and breastfeeding.

Taking other medicines

Tell your doctor or pharmacist if you are taking any other medicines, including any that you buy without a prescription from your pharmacy, supermarket or health food shop.

Some medicines and AZEP NASAL SPRAY may interfere with each other if a significant amount of the nasal spray is absorbed in your body. These include:

  • cimetidine, a medicine used to treat stomach ulcers and some other stomach conditions.

These medicines may be affected by AZEP NASAL SPRAY, or may affect how well it works. You may need different amounts of your medicine, or you may need to take different medicines. Your doctor or pharmacist will advise you.

Your doctor and pharmacist may have more information on medicines to be careful with or avoid while using AZEP NASAL SPRAY.


Follow all directions given to you by your doctor or pharmacist carefully.

They may differ from the information contained in this leaflet.

If you do not understand the instructions on the box or bottle, ask your doctor or pharmacist for help.

How much to use

Use one spray of AZEP NASAL SPRAY in each nostril, every 12 hours as necessary.

How to use it

Blow your nose gently, to clear away any mucus.

  1. Remove the protective cap.

  1. Before first use, prime the spray by pressing the pump 2-3 times until an even spray emerges.

  1. Tilt your head forwards (look at your toes). Spray once into each nostril, closing the other nostril with one finger. Sniff slowly and gently.

  1. Wipe the nozzle and replace the protective cap.

Prime the pump again if you have not used the spray for 3 or more days.

How long to use it

AZEP NASAL SPRAY can be used for up to 6 months for seasonal and non-seasonal allergies.

Consult your doctor if your symptoms have not cleared up after 6 months.

If you forget to use it

AZEP NASAL SPRAY should be used only when necessary.

Do not use a double dose to make up for the dose that you missed.

If you use too much (overdose)

Immediately telephone your doctor or pharmacist or the Poisons Information Centre (phone 13 11 26), if you think that you or anyone else may have used too much AZEP NASAL SPRAY, or if anyone accidentally drinks AZEP NASAL SPRAY. Do this even if there are no signs of discomfort or poisoning.

If AZEP NASAL SPRAY is accidentally sprayed into the eyes, bathe them with plenty of water.

They may sting for a while.

While you are using AZEP NASAL SPRAY

Things you must do

If you are about to be started on any new medicine, tell your doctor, dentist or pharmacist that you are using AZEP NASAL SPRAY.

Tell any other doctors, dentists and pharmacists who are treating you that you are using AZEP NASAL SPRAY.

If you become pregnant while using AZEP NASAL SPRAY tell your doctor or pharmacist.

Things you must not do

Do not use AZEP NASAL SPRAY to treat any other complaints unless your doctor or pharmacist tells you to.

Do not give AZEP NASAL SPRAY to anyone else, even if they have the same condition as you.

Things to be careful of

Make sure you know how you react to AZEP NASAL SPRAY before you drive, operate machinery, or do anything else that could be dangerous if you are tired, drowsy, dizzy or light-headed.

AZEP NASAL SPRAY is unlikely to make you feel drowsy. However, if you are drowsy, do not drive a car or operate machinery.

Be careful drinking alcohol while using AZEP NASAL SPRAY.

If you drink alcohol, any drowsiness may be worse.

Side effects

Tell your doctor or pharmacist as soon as possible if you do not feel well while you are using AZEP NASAL SPRAY.

Like other medicines, AZEP NASAL SPRAY may have unwanted side effects in a few people. All medicines can have side effects. Sometimes they are serious, most of the time they are not. You may need medical treatment if you get some of the side effects.

Ask your doctor or pharmacist to answer any questions you may have.

Tell your doctor or pharmacist if you notice any of the following and they worry you:

  • runny nose (rhinitis)
  • bleeding nose
  • stinging or itching in nose
  • sneezing
  • bitter taste in mouth
  • nausea
  • headache
  • drowsiness or sleepiness

These side effects are usually mild and short-lived.

Drinking a flavoured drink a few minutes after using AZEP NASAL SPRAY may help remove any bitter taste.

Other side effects not listed above may occur in some patients. Tell your doctor or pharmacist if you notice anything that is making you feel unwell.

Do not be alarmed by this list of possible side effects. You may not experience any of them.



Keep your AZEP NASAL SPRAY in a cool dry place where the temperature stays below 30°C.

Do not put AZEP NASAL SPRAY in the fridge.

Do not leave it in the car on hot days or on windowsills.

Heat can destroy some medicines.

Keep AZEP NASAL SPRAY where children cannot reach it. A locked cupboard at least one-and-a-half metres above the ground is a good place to store medicines.

Do not use AZEP NASAL SPRAY for longer than 6 months after the bottle was first opened.


If your doctor or pharmacist tells you to stop using AZEP NASAL SPRAY or the bottle has passed the expiry date, or the bottle has been open for longer than 6 months, ask your pharmacist what to do with any that is left over.

Product description

What it looks like

AZEP NASAL SPRAY is a clear, nearly colourless liquid in a brown glass bottle fitted with a spray pump and a cap.

The 5 mL bottle contains 35 metered sprays.

The 20 mL bottle contains 140 metered sprays.


Active ingredients:

  • azelastine hydrochloride, 0.1% w/v. [One spray contains 125 µg of azelastine (as hydrochloride)]

Other ingredients:

  • hypromellose
  • disodium edetate
  • citric acid
  • sodium chloride
  • dibasic sodium phosphate dodecahydrate
  • purified water

AZEP NASAL SPRAY does not contain lactose, sucrose, gluten, tartrazine or any other azo dyes.


Mylan Health Pty Ltd
Level 1, 30 The Bond
30-34 Hickson Road
Millers Point, NSW 2000
Phone: 1800 314 527

This leaflet was prepared in March 2021.

AUST R 104853


Published by MIMS September 2021


Brand name

Azep Nasal Spray

Active ingredient

Azelastine hydrochloride




1 Name of Medicine

Azelastine hydrochloride.

2 Qualitative and Quantitative Composition

Each actuation (0.137 mL) contains 137 microgram azelastine hydrochloride (equivalent to 125 microgram azelastine as the base).
For the full list of excipients, see Section 6.1 List of Excipients.

3 Pharmaceutical Form

Azep Nasal Spray is a clear, colourless, buffered, isotonic aqueous solution with a pH of 6.8.

4 Clinical Particulars

4.1 Therapeutic Indications

For the symptomatic treatment of seasonal allergic rhinitis and perennial allergic rhinitis.

4.2 Dose and Method of Administration

Adults and children aged 5 years and over.

Each spray contains 125 microgram of azelastine (as hydrochloride).
One spray into each nostril twice daily as necessary (equivalent to a daily dose of 0.50 mg azelastine (as hydrochloride)).

Long-term treatment.

Azelastine nasal spray may be used until symptoms cease, but no longer than 6 months, uninterruptedly.

Instructions for handling.

The spray should be used with the head held upright, after first blowing the nose.
1. The protective cap should be removed.
2. Before the first use, the pump should be primed by spraying two to three times, until an even spray is produced.
3. One spray should be used in each nostril with the head tilted forward (looking at toes). Do not keep the head upright or tilted backwards.
4. Sniffing should only be slow and gentle.
5. The nozzle should be wiped and the protective cap replaced.
The pump should also be primed again after storage for three or more days.

4.3 Contraindications

Hypersensitivity to any of the ingredients.

4.4 Special Warnings and Precautions for Use

Use in the elderly.

A pharmacokinetic study in elderly patients (n = 15) receiving oral azelastine hydrochloride 4.4 mg twice daily found a prolongation of the Tmax and an increase in Cmax and AUC compared to results in healthy volunteers. There have been no specific studies in the elderly with the nasal spray. In clinical and PMS studies of the nasal spray, no increase in the incidence of adverse reactions has been seen in elderly patients.

Use in renal impairment.

In a single oral dose study in nine patients, renal insufficiency (creatinine clearance < 50 mL/minute) resulted in a 70 to 75% higher Cmax and AUC compared to normal subjects. However, the number of patients evaluated in this study is too small to draw meaningful conclusions. No information regarding the use of Azep Nasal Spray in renally impaired patients is available.

Use in hepatic impairment.

No significant difference was found in t1/2, Cmax or AUC in an oral single dose study in six patients with hepatic impairment compared to normal subjects. Caution is warranted in extrapolating these data to long-term use.

Paediatric use.

The efficacy and safety of Azep Nasal Spray in children under 5 years of age has not been established.

4.5 Interactions with Other Medicines and Other Forms of Interactions

No specific interactions have been studied with Azep Nasal Spray. Interaction studies at high oral doses have been performed. However, they bear no relevance to azelastine nasal spray as systemic levels after administration of the nasal spray are in the nanogram range.
After oral administration of 4.4 mg azelastine hydrochloride, twice daily, cimetidine has been shown to increase the plasma levels of azelastine. This is thought to be due to cimetidine inhibiting the metabolism of azelastine by interacting with the hepatic cytochrome P450 system. No interaction was seen following comedication with ranitidine.
When given in combination, azelastine hydrochloride 4.4 mg tablets and alcohol showed sedative effects. As no specific information is available with the nasal spray, caution is required if Azep Nasal Spray is used concomitantly with alcohol or other CNS depressants.
No significant pharmacokinetic interaction was observed with the co-administration of an oral 4.4 mg dose of azelastine hydrochloride twice daily and theophylline 300 mg or 400 mg twice daily.
Interaction studies investigating the cardiac repolarisation effects of concomitantly administered oral azelastine hydrochloride (4.4 mg b.d. (twice daily)) and erythromycin (500 mg t.i.d. (three times daily)) or ketoconazole (200 mg b.d.) were conducted. Oral erythromycin had no effect on azelastine pharmacokinetics or QTc based on analysis of serial electrocardiograms. Ketoconazole interfered with the measurement of azelastine plasma levels; however, no effects on QTc were observed.

4.6 Fertility, Pregnancy and Lactation

Effects on fertility.

In male and female rats, azelastine at oral doses of 30 mg/kg/day and greater (resulting in plasma levels which were at least about 400 times above the plasma levels at the recommended therapeutic intranasal dose) caused a decrease in the fertility index, but in long-term toxicity studies up to two years there were no drug-related alterations in reproductive organs either in males or in females in this species. A clinical study in 21 healthy human females using an intranasal dose of 1.12 mg/day found no effect on ovulation or sexual hormone pattern.
(Category B3)
There are no adequate and well-controlled clinical studies in pregnant women. Azep Nasal Spray should be used during pregnancy only if the benefit to the mother justifies the potential risk to the fetus.
In pregnant rats there was evidence of significant diaplacental transfer of the drug to the fetuses. Azelastine was embryolethal and teratogenic in mice at oral doses greater than 30 mg/kg/day. In rats, azelastine was embryo-toxic at oral doses greater than 3 mg/kg/day, and teratogenicity and embryolethality were seen at doses greater than 30 mg/kg/day. In rabbits, azelastine was teratogenic at oral doses greater than 20 mg/kg/day. In pregnant rats, azelastine demonstrated no perinatal/ postnatal toxicity at oral doses up to 30 mg/kg/day.
In rats, the no effect doses resulted in plasma levels which were at least about 25 times above the plasma levels at the recommended therapeutic intranasal dose in humans. (The calculation of the safety factor is based on plasma levels derived from oral subchronic toxicity studies).
It is not known whether azelastine hydrochloride is excreted in human milk. No data are available in humans. Therefore, caution should be exercised when azelastine is administered to nursing women. Azelastine should not be used in lactating women unless the expected benefits outweigh the risks to the feeding infant.
In lactating rats approximately 0.2% of a 10 mg/kg oral dose of 14C-azelastine was transferred to the maternal milk. A perinatal/ postnatal study in rats showed no adverse effect at oral doses up to 30 mg/kg/day.

4.7 Effects on Ability to Drive and Use Machines

In isolated cases, fatigue, weariness, exhaustion, dizziness or weakness, that may also be caused by the disease itself, may occur when using azelastine nasal spray. In these cases, the ability to drive and use machines may be impaired. Alcohol may enhance this effect.
Somnolence was uncommon in clinical trials and post-marketing surveillance studies, occurring with a similar incidence to placebo in clinical trials using the nasal spray in the recommended dosage. Patients should be advised to assess their individual responses to Azep Nasal Spray before engaging in any activity requiring mental alertness, such as driving a car or operating machinery.

4.8 Adverse Effects (Undesirable Effects)

Azelastine nasal spray is generally well-tolerated. The most frequent complaints with the recommended dose (one spray per nostril twice daily) reported in clinical trials and in the post-marketing program were: mild, transient inflammation of the nasal mucosa (e.g. stinging, itching, sneezing and epistaxis), the experience of nose bleeding, and the occurrence of a substance-specific bitter taste, which may lead to nausea. The experience of the bitter taste may be due to incorrect administration such as tilting the head backwards too far.

Clinical trial data.

Table 1 shows adverse events reported in clinical trials with azelastine nasal spray with an incidence of > 1%, irrespective of a causal relationship to the administration of the drug.

Post-marketing data.

The following adverse reactions were reported with a frequency of ≥ 0.05% in post-marketing surveillance studies in a total of 12,221 patients.
Common: ≥ 1/100 and < 1/10 (≥ 1% and < 10%); uncommon: ≥ 1/1,000 and < 1/100 (≥ 0.1% and < 1%); rare: ≥ 1/10,000 and < 1/1,000 (≥ 0.01% and < 0.1%). (See Table 2.)
The following adverse effects have also been observed: hypersensitivity dizziness, weakness, rash, pruritus, urticaria.

Reporting suspected adverse effects.

Reporting suspected adverse reactions after registration 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 at

4.9 Overdose

With the nasal route of administration overdosage reactions are not anticipated. To date, there has been only one report of incorrect usage: a two year old boy drank approximately 10 mL of azelastine nasal spray. This led to a burning sensation in the nose and mouth and to spontaneous vomiting, these events lasting 5 - 10 minutes. Pulse rate, blood pressure and respiration were normal and stable, and a normal pupil reaction was found. No tissue damage in the mouth or throat occurred. The boy recovered completely.
In the event of overdosage after accidental oral uptake, disturbances of the central nervous system (including drowsiness, confusion, coma, tachycardia and hypotension) are to be expected based on the results of animal experiments. Symptomatic and supportive treatment should be instigated as there is no known antidote.
For information on the management of overdose, contact the Poisons Information Centre on 131126 (Australia).

5 Pharmacological Properties

5.1 Pharmacodynamic Properties

Mechanism of action.

Azelastine hydrochloride, a phthalazinone derivative, is a potent antiallergic compound with histamine H1-receptor antagonist activity and a rapid onset and long duration of action. The major metabolite, desmethylazelastine, also exhibits H1-receptor antagonist activity. Azep Nasal Spray is administered as a racemic mixture. The racemate, R- and S-enantiomers were equally potent at inhibiting eyelid histamine-induced oedema in rats, however the R-enantiomer was 2-fold less active at inhibiting eyeball histamine-induced oedema.
Data from in vivo (preclinical) 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. histamine, leukotrienes, PAF and serotonin.
In experimental studies in humans, Azep Nasal Spray was effective in the prophylaxis of histamine- and allergen-induced nasal symptoms. The effect appears within 15 minutes of drug application and lasts for up to 12 hours. Azep Nasal Spray also has an effect on the inflammatory process of allergy as defined by a significant decrease in the eosinophilic and neutrophilic infiltration, and ICAM-1 expression during both early and late phase reactions following allergen challenge.

Clinical trials.

In a number of placebo- and active-controlled clinical studies, Azep Nasal Spray has been shown to be effective in the symptomatic treatment of allergic rhinitis, especially for sneezing, itchy nose, rhinorrhoea and nasal blockage. Studies in seasonal allergic rhinitis were generally conducted over 2-6 weeks; in perennial allergic rhinitis, controlled studies were conducted over 6 weeks, and two open long-term studies were conducted over a 6 month period.

Seasonal allergic rhinitis.

Two randomised, double-blind trials (n = 162, n = 100) in adults aged 16-65 years showed that azelastine nasal spray 0.14 mg/nostril b.d. (twice daily) had equivalent efficacy to oral terfenadine 60 mg b.d. over 6 weeks. The primary efficacy measure was reduction in the rhinitis score. In one of these trials, nasal rhinometry was also performed with azelastine therapy and shown to significantly reduce nasal airways resistance over a six week period. A further randomised, double-blind, placebo-controlled trial (n = 83) assessed the efficacy for 2 weeks in children aged 5 - 12 years. Response was defined as at least a 50% improvement in a nasal score of sneezing, pruritus and rhinorrhoea within 3 days of starting treatment. The response rate was 52.5% in the azelastine group and 41.9% in the placebo group (p = 0.38). With regard to the nasal symptoms sneezing, nasal irritation and rhinorrhoea, the mean score was significantly decreased by day 3 compared to placebo (p = 0.039).

Perennial allergic rhinitis.

A randomised, double-blind trial in adults aged 18 - 49 years found that azelastine nasal spray 0.14 mg/nostril b.d. was equivalent in efficacy to oral terfenadine 60 mg bd over 6 weeks. Of the 52 patients enrolled, 22 were evaluable in the azelastine group and 26 in the terfenadine group. A randomised open trial in adults aged 18 - 65 years found azelastine nasal spray 0.14 mg/nostril b.d. to be equivalent in efficacy to budesonide spray 0.05 mg/nostril b.d. for 6 weeks. Of the 193 patients enrolled, 92 were evaluable in the azelastine group and 89 in the budesonide group. Equivalent efficacy was based on symptomatology, nasal airflow resistance and resolution of nasal hyperplasia.
Two randomised, double-blind, placebo-controlled trials assessed the efficacy of azelastine 0.14 mg/nostril b.d. for 6 weeks in children aged 5 - 12 years. In one trial, azelastine was significantly better than placebo in improving sneezing, nasal blockage, nasal itch and rhinorrhoea measured on a visual analogue scale. Of the 125 patients enrolled, 60 were evaluable in each group. In the other trial, which experienced poor compliance, there was no significant difference between the treatment groups. Of 162 patients enrolled, 72 were evaluable in the azelastine group and 71 in the placebo group. In a 2 week, single-blind trial (n = 45) in children aged 5 - 18 years, budesonide aqueous suspension 0.2 mg/day was superior to azelastine 0.56 mg/day.

Long-term studies.

Six and 12 months uncontrolled trials (n = 185, n = 36) in adults aged 17 - 65 years provide maintenance of long-term efficacy data in perennial allergic rhinitis and demonstrate efficacy for up to 12 months. A further trial (n = 62) found a significant reduction in nasal symptom score over 6 months and was supportive of long-term efficacy in children aged 7 - 16 years.

Other information.

There were no findings on nasal examination in an 8 week study that suggested any adverse effects on the nasal mucosa.
In a double-blind, placebo-controlled, parallel group study, 69 patients with perennial allergic rhinitis were randomised to receive azelastine and 36 to placebo, to evaluate the safety and tolerability of Azep Nasal Spray following administration of 2 sprays per nostril (1.12 mg/day) for 8 weeks. A 12-lead ECG was performed at baseline and after 8 weeks of treatment, 2 - 4 hours after dosing. There was no evidence of an effect of Azep Nasal Spray on cardiac repolarisation as represented by the QTc interval of the ECG. The results from this study thus support the cardiac safety of Azep Nasal Spray.

5.2 Pharmacokinetic Properties


The systemic bioavailability of azelastine nasal spray has not been directly measured. In healthy volunteers, using cross-trial data, bioavailability is estimated at 20%. In patients with allergic rhinitis, again using cross trial data, bioavailability is estimated at 40 - 60%.


After oral and intravenous administration, the mean volume of distribution was 14.5 L/kg and mean terminal half-life was 22 hours.
In patients receiving a total daily dose of azelastine hydrochloride 0.56 mg (given as two sprays per nostril once daily), the steady-state mean plasma concentrations of azelastine observed two hours after dose were about 0.65 nanogram/mL. A doubling of the total daily dose to azelastine hydrochloride 1.12 mg (two sprays per nostril twice daily) resulted in steady-state mean plasma concentrations of azelastine of 1.09 nanogram/mL, suggesting dose proportionality within the dose range.
In vitro studies with human plasma indicate that the plasma protein binding of azelastine and desmethylazelastine are approximately 88% and 97% respectively.


Azelastine is extensively metabolised, desmethylazelastine being the principal metabolite. No specific isoform of cytochrome P450 was found to be specific in the metabolism of azelastine at low concentrations (6 - 30 nanogram/mL) in human liver microsomes.


The mean terminal half-life of desmethylazelastine was 56 hours. Up to 74% of a radiolabelled oral or intravenous dose is excreted in faeces and 26% in urine. Thirteen per cent is excreted in urine as unchanged azelastine.

5.3 Preclinical Safety Data


Azelastine demonstrated no genotoxic potential in standard assays for gene mutations, chromosomal damage and DNA damage.


Azelastine demonstrated no carcinogenic potential in mice and rats at dietary doses up to 25 and 30 mg/kg/day respectively.

6 Pharmaceutical Particulars

6.1 List of Excipients

Hypromellose; disodium edetate; citric acid; dibasic sodium phosphate dodecahydrate; sodium chloride; purified water.

6.2 Incompatibilities

Incompatibilities were either not assessed or not identified as part of the registration of this medicine.

6.3 Shelf Life

In Australia, information on the shelf life can be found on the public summary of the Australian Register of Therapeutic Goods (ARTG). The expiry date can be found on the packaging.

6.4 Special Precautions for Storage

Store below 30°C (Do not refrigerate). Shelf life: 3 years.

6.5 Nature and Contents of Container

Available in a 5 mL and 20 mL amber glass bottle with fitted valve assembly.

6.6 Special Precautions for Disposal

In Australia, any unused medicine or waste material should be disposed of in accordance with local requirements.

6.7 Physicochemical Properties

Azelastine hydrochloride is a white to light beige crystalline, odourless powder. It is freely soluble in chloroform, soluble in ethanol and sparingly soluble in water. It is practically insoluble in ether, n-hexane and toluene.

Chemical structure.

Azelastine hydrochloride is chemically D,L-4-(p-Chlorobenzyl)-2-(N-methylperhydroazepinyl)-(4) 1(2H)-phthalazinone hydrochloride.
It has the following structural formula:
The chemical formula is C22H24OClN3.HCl and its molecular weight is 418.37. It is presented as the racemate.

CAS number.


7 Medicine Schedule (Poisons Standard)

Pharmacy Medicine: S2.

Summary Table of Changes