Consumer medicine information

APO-Olopatadine Eye Drops

Olopatadine

BRAND INFORMATION

Brand name

APO-Olopatadine

Active ingredient

Olopatadine

Schedule

S4

 

Consumer medicine information (CMI) leaflet

Please read this leaflet carefully before you start using APO-Olopatadine Eye Drops.

What is in this leaflet

Read this leaflet carefully before taking your medicine.

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

The information in this leaflet was last updated on the date listed on the last page. More recent information on this medicine may be available.

Ask your doctor or pharmacist:

  • if there is anything you do not understand in this leaflet,
  • if you are worried about taking your medicine, or
  • to obtain the most up-to-date information.

You can also download the most up to date leaflet from www.apotex.com.au.

All medicines have risks and benefits. Your doctor has weighed the risks of you using this medicine against the benefits they expect it will have for you.

Pharmaceutical companies cannot give you medical advice or an individual diagnosis.

Keep this leaflet with your medicine. You may want to read it again.

What this medicine is used for

The name of your medicine is APO-Olopatadine eye drops. It contains the active ingredient olopatadine hydrochloride.

It is used to treat allergic conjunctivitis, which is inflammation of the eye due to pollens that cause an allergic response to give watery, itchy and/or red eyes.

Before prescribing olopatadine for you or your child, your doctor will have examined the eye and decided that olopatadine is the right medicine.

Ask your doctor if you have any questions about why this medicine has been prescribed for you. Your doctor may have prescribed this medicine for another reason.

This medicine is available only with a doctor's prescription.

How it works

Olopatadine belongs to the group of medicines called antihistamines and also to the group of medicines called anti-allergics.

There is no evidence that this medicine is addictive.

Use in children

This medicine should not be used in children under age 3 years.

Safety and effectiveness has not been established.

Before you use this medicine

When you must not take it

Do not take this medicine if:

  • You are hypersensitive to, or have had an allergic reaction to, olopatadine or any of the ingredients listed at the end of this leaflet.
    Symptoms of an allergic reaction may include: cough, shortness of breath, wheezing or difficulty breathing; swelling of the face, lips, tongue, throat or other parts of the body; rash, itching or hives on the skin; fainting; or hay fever-like symptoms.
    If you think you are having an allergic reaction, do not take any more of the medicine and contact your doctor immediately or go to the Accident and Emergency department at the nearest hospital.
  • The expiry date (EXP) printed on the pack has passed.
  • The packaging is torn, shows signs of tampering or it does not look quite right.

Do not put the eye drops into your eye(s) while you are wearing soft contact lenses.

The preservative in olopatadine eye drops (benzalkonium chloride) may be deposited in soft contact lenses. You can put your soft contact lenses into your eyes 15 minutes after you have used olopatadine eye drops.

Before you start to take it

Before you start taking this medicine, tell your doctor if:

  1. You or your child has allergies to:
  • any other medicines
  • any other substances, such as foods, preservatives or dyes.
  1. You or your child have or have had any medical conditions.
  2. You are currently pregnant or you plan to become pregnant. Do not take this medicine whilst pregnant until you and your doctor have discussed the risks and benefits involved.
  3. You are currently breastfeeding or you plan to breastfeed. Do not take this medicine whilst breastfeeding until you and your doctor have discussed the risks and benefits involved.
  4. You are planning to have surgery or an anaesthetic.
  5. You are taking or are planning to take any other medicines. This includes vitamins and supplements that are available from your pharmacy, supermarket or health food shop. This is particularly important if you are currently using any other type of eye drops.

How to use this medicine

Follow carefully all directions given to you by your doctor. Their instructions may be different to the information in this leaflet.

How much to use

Your doctor will tell you how much of this medicine you should take. This will depend on your condition and whether you are taking any other medicines.

The usual dose of olopatadine is one or two drops in the affected eye(s) twice each day. The dosing instructions will be printed on the label your pharmacist puts on the bottle or carton.

Do not stop taking your medicine or change your dosage without first checking with your doctor.

How to use it

It is important to use olopatadine exactly as your doctor has told you. If you use it less often than you should, it may not work as well and the eye problem may not improve. Using it more often than you should, may not improve the eye problem any faster and may cause increased side effects.

If you are wearing soft contact lenses, remove them before putting the drops in your eye.

Follow these steps to use the eye drops:

  1. Wash your hands thoroughly.
  2. Shake the bottle.
  3. Remove the cap from the bottle.
  4. Hold the bottle upside down in one hand between your thumb and middle finger.
  5. While tilting your head back, gently pull down the lower eyelid of your eye to form a pouch/pocket.
  6. Place the tip of the bottle close to your eye. Do not let it touch your eye.
  7. Release one drop into the pouch/pocket formed between the eye and eyelid by gently tapping or pressing the base of the bottle with your forefinger.
  8. Close your eye. Do not blink or rub your eye.
  9. While your eye is closed, place your index finger against the inside corner of your eye and press against your nose for about two minutes. This will help to stop the medicine from draining through the tear duct to the nose and throat, from where it can be absorbed into other parts of the body. This will also reduce the unpleasant taste sensation that some people experience when using these drops.
  10. If necessary, repeat the above steps for the other eye.
  11. Your eyelids can only hold less than one drop at a time, so it is normal for a small amount of the eye drop to spill onto your cheek. You should wipe away any spillage with a tissue.
  12. Replace the cap on the bottle, closing it tightly.
  13. Wash your hands again with soap and water to remove any residue.

You may feel a slight burning sensation in the eye(s) shortly after using olopatadine eye drops. If this persists, or is very uncomfortable, contact your doctor.

Do not touch the tip of the dropper tip with your fingers, to the eye or any other surface. This will prevent the eye drops becoming dirty or contaminated.

When to use it

Take this medicine at the same time each day. Taking it at the same time each day will have the best effect and will also help you remember when to take it.

It does not matter if you take it before, with or after food.

How long to use it for

Continue taking your medicine for as long as your doctor tells you.

If you use olopatadine longer than your doctor tells you, the chance of side effects may increase.

If you are unsure about when or how to stop using olopatadine you should talk to your doctor.

Make sure you have enough to last over weekends and holidays.

If you forget to use it

If it is almost time to take your next dose, skip the missed dose and take your next dose at the usual time. Otherwise, take it as soon as you remember and then go back to taking your medicine as you would normally.

Do not take a double dose to make up for missed doses. This may increase the chance of you experiencing side effects.

If you have trouble remembering to take your medicine, ask your pharmacist for some hints to help you remember.

If you or your child take too much (overdose)

If you think that you or your child have swallowed it or anyone else may have taken too much of this medicine, immediately telephone your doctor or the Poisons Information Centre (Tel: 13 11 26 in Australia) for advice. Alternatively, go to the Accident and Emergency department at your nearest hospital.

Do this even if there are no signs of discomfort or poisoning. You may need urgent medical attention.

While you are using this medicine

Things you must do

Tell your doctor that you or your child is taking this medicine if:

  • if you feel that this medicine is not helping the eye problem
  • if for any reason, you have not used this medicine exactly as prescribed. Otherwise your doctor may think that it was not effective and change the treatment unnecessarily
  • you are about to be started on any new medicine
  • you are pregnant or are planning to become pregnant
  • you are breastfeeding or are planning to breastfeed
  • you are about to have any blood tests
  • you are going to have surgery or an anaesthetic or are going into hospital.

Go to your doctor regularly for a check-up.

Tell any other doctors, dentists and pharmacists who are treating you that you take this medicine.

Things you must not do

Do not:

  • Give this medicine to anyone else, even if their symptoms seem similar to yours.
  • Take your medicine to treat any other condition unless your doctor tells you to.
  • Stop taking your medicine, or change the dosage, without first checking with your doctor.
  • Let children handle this medicine.

If the itching or pain in the eye does not diminish or increases, or severe pain is experienced in the eye, contact your doctor immediately.

Ask your doctor if you are concerned about the length of time that you or your child has been using this medicine.

Things to be careful of

Be careful when driving or operating machinery until you know how this medicine affects you.

Possible side effects

Tell your doctor as soon as possible if you or your child does not feel well while you are taking olopatadine or if you have any questions or concerns.

Do not be alarmed by the following lists of side effects. You may not experience any of them. All medicines can have side effects. Sometimes they are serious but most of the time they are not.

Olopatadine eye drops are generally well tolerated. Reactions that affect the eyes have been reported.

Tell your doctor if you notice any of the following:

  • Swelling of the eyelid or front part of the eye
  • Eye pain
  • Blurred vision
  • Feeling like there is something in the eye
  • Increased tearing
  • Dry eye
  • Red eye/eyelids
  • Itching
  • Crusty eyelids
  • Increased sensitivity to sunlight

Tell your doctor as soon as possible if you notice any of the following.

These may be serious side effects and you may need medical attention:

  • Headache
  • Weakness
  • Dizziness
  • Changes to sensation of taste
  • Dry nose
  • Dry mouth
  • Red, sore and inflamed skin rash
  • Nausea

Other side effects not listed above may occur in some patients.

Allergic reactions

If you think you are having an allergic reaction to olopatadine, do not take any more of this medicine and tell your doctor immediately or go to the Accident and Emergency department at your nearest hospital.

Symptoms of an allergic reaction may include some or all of the following:

  • cough, shortness of breath, wheezing or difficulty breathing
  • swelling of the face, lips, tongue, throat or other parts of the body
  • rash, itching or hives on the skin
  • fainting
  • hay fever-like symptoms.

Storage and disposal

Storage

Keep your medicine in its original packaging until it is time to take it.

If you take your medicine out of its original packaging it may not keep well.

Do not refrigerate this medicine.

Keep your medicine in a cool dry place where the temperature will stay below 25°C.

Do not store your medicine, or any other medicine, in the bathroom or near a sink. Do not leave it on a window sill or in the car. Heat and dampness can destroy some medicines.

Keep this medicine 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.

Disposal

Discard each bottle of olopatadine 4 weeks after it has been opened. Write the date the bottle was opened on the label to remind you when to discard the bottle.

If your doctor tells you to stop taking this medicine or it has passed its expiry date, your pharmacist can dispose of the remaining medicine safely.

Product description

What APO-Olopatadine Eye Drops looks like

1 mg/mL (0.1%) Eye Drops: Clear, colourless solution.

5 mL bottle.

Ingredients

Each eye drop contains 1 mg/mL olopatadine as the active ingredient.

It also contains the following inactive ingredients:

  • sodium chloride
  • dibasic sodium phosphate
  • benzalkonium chloride (as preservative)
  • water for injections
  • hydrochloric acid
  • sodium hydroxide

This medicine is gluten-free, lactose-free, sucrose-free, tartrazine-free and free of other azo dyes.

Australian Registration Numbers

APO-Olopatadine 1 mg/mL (0.1%) bottle: AUST R 241497.

Sponsor

Apotex Pty Ltd
16 Giffnock Avenue
Macquarie Park NSW 2113
Tel: (02) 8877 8333
Web: www1.apotex.com.au

APO is a registered trade mark of Apotex Inc.

This leaflet was last updated in October 2020.

Published by MIMS November 2020

BRAND INFORMATION

Brand name

APO-Olopatadine

Active ingredient

Olopatadine

Schedule

S4

 

1 Name of Medicine

Olopatadine hydrochloride.

2 Qualitative and Quantitative Composition

Olopatadine eye drops are a sterile, isotonic, preserved solution for topical application to the eye. The solution is buffered to a pH of approximately 7 so that it is within the physiological range of the ocular surface fluid.
It is available as a 1 mg/mL (0.1%) strength, present as 1.11 mg/mL olopatadine hydrochloride.
For the full list of excipients, see Section 6.1 List of Excipients.

3 Pharmaceutical Form

Eye drops.
Clear, colourless solution.

4 Clinical Particulars

4.1 Therapeutic Indications

Olopatadine eye drops are indicated for the treatment of the signs and symptoms of seasonal allergic conjunctivitis. Treatment may be maintained for up to 14 weeks, if considered necessary.

4.2 Dose and Method of Administration

APO-Olopatadine eye drops are intended for ophthalmic administration.

Dosage.

The recommended therapy is one to two drops in the affected eye(s), twice daily, for up to 14 weeks.

4.3 Contraindications

Olopatadine eye drops are contraindicated in patients hypersensitive to olopatadine hydrochloride or any other component of the preparation (see Section 6.1 List of Excipients).

4.4 Special Warnings and Precautions for Use

Not for injection or oral ingestion.

Instruction to patients.

Olopatadine contains the preservative benzalkonium chloride, which may cause eye irritation and be deposited in or discolour soft (hydrophilic) contact lenses. Avoid contact with soft contact lenses. Patients who wear soft contact lenses should remove their lenses prior to instilling olopatadine eye drops and should not reinsert their lenses until at least 15 minutes after instillation of the eye drops.
To prevent contaminating the dropper tip and solution, care should be taken not to touch the eyelids or surrounding areas with the dropper tip of the bottle. The bottle should be tightly closed when not in use.
Each bottle of olopatadine eye drops is for use in one patient only and should be discarded within 28 days of opening.

Use in the elderly.

No data available.

Paediatric use.

Safety and effectiveness have not been established in children below 3 years of age.

Effects on laboratory tests.

No data available.

4.5 Interactions with Other Medicines and Other Forms of Interactions

Interactions with other medications have not been investigated in vivo. Drug interaction studies on human liver microsomal preparation have shown that olopatadine is not an inhibitor of cytochrome P-450 isozymes 1A2, 2C8/9, 2C19, 2D6, 2E1 or 3A1. Olopatadine eye drops have low drug interaction potential as systemic levels of olopatadine achieved after ocular dosing are negligible and 60-70% of the drug is excreted unchanged in the urine.

4.6 Fertility, Pregnancy and Lactation

Effects on fertility.

There are no human data addressing the effects of topical ocular administration of olopatadine on human fertility. In animal reproductive/fertility studies, olopatadine had no effect on the fertility of male and female rats at oral doses up to 50 mg/kg/day (7,800x the maximum recommended ocular human use level). However, decreases in the fertility index, number of corpora lutea and implantation rate were seen at an oral dose of 400 mg/kg/day.
(Category B1)
Studies in animals with olopatadine have shown reproductive toxicity following systemic administration. Olopatadine was not teratogenic in rats and rabbits at oral doses of 600 mg/kg and 400 mg/kg, respectively (> 90,000x and > 60,000x the maximum recommended ocular human use level, respectively). Given that animal studies are not always predictive of human responses, and that no adequate and well controlled studies in pregnant women have been performed, it should be carefully considered whether the potential benefit to the mother justifies the potential risk to the embryo or foetus.
 Olopatadine has been identified in the milk of nursing rats following oral administration. Rat pups of mothers administered olopatadine orally at greater than 4 mg/kg/day showed (625x, but not at 312x, the maximum recommended ocular human use level demonstrated) reduced body weight gain during the nursing period. It is not known whether topical ocular administration could result in sufficient systemic absorption to produce detectable quantities of olopatadine/metabolites in human breast milk. Patients should be informed that antihistamines may affect the milk production of a nursing mother. Olopatadine eye drops should be used with caution in breastfeeding woman.

4.7 Effects on Ability to Drive and Use Machines

Instillation of eye drops may cause transient blurring of vision or other visual disturbances which may affect the ability to drive or use machines. The patient must wait until vision clears before driving or operating machinery if blurred vision is experienced.

4.8 Adverse Effects (Undesirable Effects)

Headaches have been reported at an incidence of 7%. The following adverse experiences have been reported in less than 5% of patients: asthenia, blurred vision, burning or stinging, cold syndrome, dry eye, foreign body sensation, hyperaemia, hypersensitivity, keratitis, lid oedema, nausea, pharyngitis, pruritus, rhinitis, sinusitis and taste perversion. Some of these events are similar to the underlying disease being studied.

Post marketing experience.

The following adverse reactions have been reported during clinical studies with olopatadine eye drops and are classified according to the subsequent convention: 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) and very rare (< 1/10,000). Within each frequency grouping, adverse reactions are presented in order of decreasing seriousness.

Eye disorders.

Uncommon: punctate keratitis, keratitis, eye pain, dry eye, eyelid oedema, eye pruritus, eye discharge, ocular hyperaemia, eyelid margin crusting, ocular discomfort.
Rare: photophobia, vision blurred, erythema of eyelid.

Nervous system disorders.

Uncommon: headache, dysgeusia.
Rare: dizziness.

Respiratory, thoracic and mediastinal disorders.

Uncommon: nasal dryness.

Gastrointestinal disorders.

Rare: dry mouth.

Skin and subcutaneous tissue disorders.

Rare: dermatitis contact.

General disorders and administration site conditions.

Uncommon: fatigue.
Additional adverse reactions identified from post-marketing surveillance include the following. Frequencies cannot be estimated from the available data.

Eye disorders.

Lacrimation increased.

Immune system disorders.

Hypersensitivity.

Gastrointestinal disorders.

Nausea.

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 www.tga.gov.au/reporting-problems and contact Apotex Medical Information Enquiries/Adverse Drug Reaction Reporting on 1800 195 055.

4.9 Overdose

Symptoms.

No specific ocular side effects are known for a topical overdosage of olopatadine eye drops. Results from studies indicated that topical ocular administration resulted in very low systemic concentrations. Multiple oral doses that resulted in plasma concentrations at least 2-3 orders of magnitude greater than those from topical ocular dosing were well tolerated.

Treatment.

A topical overdosage of olopatadine eye drops may be flushed from the eye(s) with warm tap water.
If olopatadine eye drops are accidentally ingested the following information may be useful. A 5 mL bottle contains 5 mg olopatadine. In single dose oral studies, olopatadine was well tolerated up to a dose of 360 mg, with rapid absorption and rapid excretion of the parent drug in the urine. Approximately 84% of the dose was recovered in the urine as parent drug within the first 24 hours.
The most often observed side effect was tiredness usually of a mild to moderate nature, although severe tiredness has been reported.
Due to the characteristics of this preparation, no toxic effects are to be expected with an ocular overdose of this product, nor in the event of accidental ingestion of the contents of one 5 mL bottle.
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.

Olopatadine is an anti-allergic compound which has been demonstrated to stabilize human conjunctival tissue mast cells, preventing the release of histamine and other inflammatory mediators. Olopatadine is a selective histamine H1-antagonist (Ki values for histamine H1, H2 and H3 receptors were 32 nanoM, 100 microM and 79 microM, respectively) that inhibits Type I immediate hypersensitivity reactions. It has been shown to inhibit the release of pro-inflammatory mediators from human conjunctival mast and epithelial cells. Olopatadine has no significant effects on alpha-adrenergic, dopamine and muscarinic Type 1 and 2 receptors.

Clinical trials.

The safety of olopatadine eye drops was evaluated in 15 clinical studies in which 1,208 patients were evaluated for safety. These studies included three clinical pharmacology plasma level and tear studies, three comfort studies, five conjunctival antigen challenge studies, an environmental study, an adjunct study to loratadine and two additional safety studies. These 15 studies show no clinically significant change observed in visual acuity, pupil diameter, pupillary response, intraocular pressure, dilated fundus parameters, blood chemistry, haematology, urinalysis, pulse or mean arterial pressure in patients receiving olopatadine eye drops.
Three studies assessed the comfort of olopatadine relative to other agents. Each included 30 subjects. They were single dose crossover studies in which all subjects received all test agents and single-blinded because the subjects themselves reported the comfort of the agents tested. In one study olopatadine 0.1% was compared to ketorolac 0.5%. In the two other studies, olopatadine 0.1% was compared to ketorolac 0.5% and levocabastine 0.05%. The studies showed that olopatadine eye drops 0.1% was significantly more comfortable than ketorolac 0.5% and levocabastine 0.05%.
Results from three pivotal conjunctival antigen challenge studies involving 278 patients demonstrated that, when subjects were challenged with antigen both initially and up to 8 hours after dosing, olopatadine eye drops were significantly more effective than the placebo in preventing chemosis, ocular itching and redness.
Results are also available from a randomized, placebo-controlled environmental study conducted during the ragweed pollen season, involving 159 patients with symptomatic allergic conjunctivitis (SAC), known to be sensitive to ragweed. The trial showed that olopatadine reduces consistently more signs and symptoms than placebo, although these results did not attain statistical significance. Post-hoc analyses showed a correlation of increased pollen counts with increased ocular signs and symptoms of SAC. In the olopatadine group, the slopes of the lines predicting ocular itching, redness and tearing were lower than the slopes for placebo, indicating that olopatadine significantly reduces the effects of pollen levels on ocular redness (p = 0.0413), itching (p = 0.0075) and tearing (p = 0.0059).

5.2 Pharmacokinetic Properties

Following topical ocular administration in humans, olopatadine was shown to have low systemic exposure. Two studies in normal volunteers (totalling 24 subjects) dosed bilaterally with olopatadine 0.15% ophthalmic solution once every 12 hours for two weeks demonstrated plasma concentrations to be generally below the quantitation limit of the assay (< 0.5 nanogram/mL). Samples in which olopatadine was quantifiable were typically found within 2 hours of dosing and ranged 0.5-1.3 nanogram/mL. The half-life in plasma was approximately 8-12 hours and elimination was predominantly through renal excretion. Approximately 60-70% of the dose was recovered in the urine as parent drug. Two metabolites, the mono-desmethyl and the N-oxide, were detected at low concentrations in the urine.

5.3 Preclinical Safety Data

Genotoxicity.

No mutagenic potential was observed when olopatadine was tested in an in vitro bacterial reverse mutation (Ames) test, an in vitro mammalian chromosome aberration assay or an in vivo mouse micronucleus test.

Carcinogenicity.

Long term studies in mice and rats did not provide any evidence of carcinogenicity at oral olopatadine doses up to 500 mg/kg/day and 200 mg/kg/day, respectively (78,000x and 31,000x the maximum recommended ocular human use level, respectively).

6 Pharmaceutical Particulars

6.1 List of Excipients

Sodium chloride, dibasic sodium phosphate, benzalkonium chloride (as preservative), water for injections, hydrochloric acid, sodium hydroxide.

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 25°C.

6.5 Nature and Contents of Container

APO-Olopatadine eye drops.

Bottle (LDPE).
5 mL - AUST R 241497.
APO is a registered trade mark of Apotex Inc.

6.6 Special Precautions for Disposal

In Australia, any unused medicine or waste material should be disposed of by taking to your local pharmacy.

6.7 Physicochemical Properties

Olopatadine hydrochloride, a dibenzoxepine derivative, is a white crystalline, water-soluble powder. It has a melting point of 248°C (decomp).

Chemical structure.


Chemical Name: (Z)-11-[3-(dimethylamino) propylidene]-6-11-dihydrodibenz[b,e]oxepin-2-acetic acid hydrochloride.
Molecular Formula: C21H23NO3.HCl.
Molecular Weight: 373.87.

CAS number.

140462-76-6.

7 Medicine Schedule (Poisons Standard)

S4 - Prescription Only Medicine.

Summary Table of Changes