Consumer medicine information

Paladopt 0.1% Eye Drops

Olopatadine

BRAND INFORMATION

Brand name

Paladopt

Active ingredient

Olopatadine

Schedule

S4

 

Consumer medicine information (CMI) leaflet

Please read this leaflet carefully before you start using Paladopt 0.1% Eye Drops.

What is in this leaflet

Read this leaflet carefully before you start to use PALADOPT Eye Drops.

This leaflet has been written to answer some common questions about PALADOPT. It does not contain all of the available information and does not take the place of talking to your doctor or pharmacist.

All medicines have risks and benefits. In deciding to prescribe PALADOPT for you or your child, your doctor has weighed the potential risks and benefits of using this medicine.

The information in this leaflet applies to PALADOPTL only. This information does not apply to similar products, even if they contain the same ingredients.

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

Keep this leaflet with your medicines. You may need it again.

What PALADOPT Eye Drops is used for

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

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

Your doctor may have prescribed PALADOPT for another reason. Ask your doctor if you have any questions about why PALADOPT has been prescribed for you or your child.

PALADOPT is not addictive.

Before you use PALADOPT Eye Drops

When you must not use it

You are allergic to olopatadine or to any other of the ingredients in PALADOPT (these are listed under Product Description).

Some of the symptoms of an allergic reaction may include shortness of breath, wheezing or difficulty breathing; swelling of the face, lips, tongue or other parts of the body; rash, itching or hives on the skin.

Do not use PALADOPT if:

  • the safety seal around the closure and neck area is broken
  • the bottle/packaging shows signs of tampering
  • the expiry date on the bottle/carton has passed.
    If you use this medicine after the expiry date has passed, it may not work.

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

The preservative in PALADOPT 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 PALADOPT Eye Drops.

Do not give PALADOPT to a child under 3 years. The safety and effectiveness of PALADOPT in children under 3 years have not been established.

If you are not sure whether you should start using PALADOPT Eye Drops, talk to your doctor.

Before you start to use it

Let your doctor know if any of the following applies before you or your child start using PALADOPT:

You have:

  • allergies to any other medicines or any substances such as foods, preservatives or dyes
  • any other medical conditions.

If you:

  • Are pregnant or are intending to become pregnant.
    Your doctor will discuss the risks and benefits of using PALADOPT Eye Drops when pregnant.
  • Are breast feeding or intending to breast feed.
    Your doctor will discuss the risks and benefits of using PALADOPT when breast feeding.

If you have not told your doctor about any of the above, tell them before you use PALADOPT Eye Drops.

Using other medicines

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

This is particularly important if you are currently using any other type of eye drops.

Some medicines may affect the way others work. Your doctor or pharmacist will be able to tell you what to do when using PALADOPT with other medicines.

How to use PALADOPT Eye Drops

Carefully follow all directions given to you by your doctor and pharmacist. They may differ from the information contained in this leaflet.

If you are being changed from one medicine to another, follow your doctor’s instructions carefully as to when to stop the medicine and when to start the new eye drops.

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

How much to use

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

How to use it

It is important to use PALADOPT exactly as your doctor or pharmacist 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. Immediately before using a bottle for the first time, break the safety seal around the neck area and throw the loose plastic ring away.
  3. Shake the bottle.
  4. Remove the cap from the bottle.
  5. Hold the bottle upside down in one hand between your thumb and middle finger (see Diagram 1).

  1. While tilting your head back, gently pull down the lower eyelid of your eye to form a pouch/pocket.
  2. Place the tip of the bottle close to your eye. Do not let it touch your eye.
  3. 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 (see Diagrams 2 and 3).

  1. Close your eye. Do not blink or rub your eye.
  2. 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.
  3. If necessary, repeat the above steps for the other eye.
  4. 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.
  5. Replace the cap on the bottle, closing it tightly.
  6. 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 PALADOPT Eye Drops. If this persists, or is very uncomfortable, contact your doctor or pharmacist.

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

How long to use it

Your doctor or pharmacist will tell you how long to use PALADOPT.

Do not take PALADOPT longer than your doctor tells you. If you use PALADOPT longer than your doctor or pharmacist tells you, the chance of side effects may increase.

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

If you forget to use it

If you forget to use PALADOPT you should put the drops that you missed in the eye(s) as soon as you remember and then go back to using them as recommended by your doctor. If it is almost time for the next dose, skip the dose that you missed and continue using them as recommended.

Never take a double dose to make up for the one that you missed.

If you are not sure what to do, contact your doctor or pharmacist.

If you have trouble remembering to use the medicine, ask your pharmacist for some hints.

If you or your child swallow it

Immediately telephone the nearest Poisons Information Centre (in Australia call 13 11 26; in New Zealand call 0800 POISON or 0800 764 766), your doctor or go to Casualty in the nearest Hospital, if you think that you or someone else has swallowed PALADOPT. Do this even if there are no signs of discomfort or poisoning.

While using PALADOPT

Things you must do

Tell all doctors and pharmacists who are treating you or your child that PALADOPT is being used.

If you feel that PALADOPT is not helping the eye problem, tell your doctor or pharmacist.

Tell your doctor if, for any reason, you have not used PALADOPT exactly as prescribed. Otherwise your doctor may think that it was not effective and change the treatment unnecessarily.

You should tell your doctor if you become pregnant while you are using PALADOPT.

Things you must not do

Do not:

  • stop using PALADOPT without first asking your doctor
  • give this medicine to anyone else, even if they appear to have the same condition as you or your child
  • let children handle
  • use PALADOPT to treat other complaints unless you doctor or pharmacist tells you to.

Things to be careful of

You should not drive or operate any machinery if PALADOPT affects your vision.

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 or pharmacist if you are concerned about the length of time that you or your child have been using PALADOPT.

Side Effects

All medicines can have side effects. Sometimes they are serious, however most of the time they are not. You may need to seek medical treatment if you or your child get some of the side effects.

Tell your doctor as soon as possible if you or your child do not feel well while using PALADOPT.

PALADOPT Eye Drops is generally well tolerated. Reactions that affect the eyes have been reported including:

  • 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

Occasionally some people notice unwanted effects in the rest of their body as a result of using PALADOPT Eye Drops. These effects may include:

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

Tell your doctor immediately and stop using at PALADOPT the first sign of a skin rash or any other sign of allergy (e.g. hives).

Other side effects not listed above may also occur in some patients. Let your doctor know if you observe any unwanted effects while using PALADOPT, even if they do not appear in the list above.

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

After using PALADOPT

Storage

Store PALADOPT in a cool, dry place where the temperature stays below 25°C. Do not leave PALADOPT in the car, in the bathroom or in other warm, damp places. Heat and temperature can destroy some medicines

Do not refrigerate PALADOPT.

Keep PALADOPT, and all other medicines, in a safe place away from children. A locked cupboard at least one and a half meters above the ground is a good place to store medicines.

Disposal

Discard each bottle of PALADOPT 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 using PALADOPT or it has passed it expiry date, ask your pharmacist what to do with any that is left over.

Product Description

What it looks like

PALADOPT is a colourless liquid that comes in a 5 mL dropper bottle.

Ingredients

Active drug:
Olopatadine.

Other ingredients:
Benzalkonium chloride, sodium chloride, sodium phosphate - dibasic, purified water.

Supplier

In Australia, this product is supplied by:

Aspen Pharma Pty Ltd
34-36 Chandos street
St Leonards NSW 2065

AUST R 227798

This leaflet was prepared in November 2015.

Published by MIMS October 2016

BRAND INFORMATION

Brand name

Paladopt

Active ingredient

Olopatadine

Schedule

S4

 

1 Name of Medicine

Olopatadine.

2 Qualitative and Quantitative Composition

Each 1 mL of eye drops contains 1.11 mg of olopatadine hydrochloride (equivalent to 1 mg olopatadine) as the active ingredient.
For the full list of excipients, see Section 6.1 List of Excipients.

3 Pharmaceutical Form

The solution is clear and colourless.

4 Clinical Particulars

4.1 Therapeutic Indications

Paladopt is 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

The recommended therapy is one to two drops of Paladopt in the affected eye(s) twice daily for up to 14 weeks.
Paladopt is for individual patient use only.

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.

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.

Instruction to patients.

Paladopt 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 Paladopt 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 Paladopt should be discarded after 28 days of opening.

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 (7,800 times 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 (> 90,000 and > 60,000 times 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 fetus.
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 (625 times - but not at 312 times - 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. 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 (≥ 0.1% to < 1%): punctate keratitis, keratitis, eye pain, dry eye, eyelid oedema, eye pruritus, eye discharge, ocular hyperaemia, eyelid margin crusting, ocular discomfort.
Rare (≥ 0.01% to < 0.1%): photophobia, vision blurred, erythema of eyelid.

Nervous system disorders.

Uncommon (≥ 0.1% to < 1%): headache, dysgeusia.
Rare (≥ 0.01% to < 0.1%): dizziness.

Respiratory, thoracic and mediastinal disorders.

Uncommon (≥ 0.1% to < 1%): nasal dryness.

Gastrointestinal disorders.

Rare (≥ 0.01% to < 0.1%): dry mouth.

Skin and subcutaneous tissue disorders.

Rare (≥ 0.01% to < 0.1%): dermatitis contact.

General disorders and administration site conditions.

Uncommon (≥ 0.1% to < 1%): 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.

4.9 Overdose

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 to 3 orders of magnitude greater than those from topical ocular dosing were well tolerated.
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. One bottle contains 5 mg of 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 bottle.
For information on the management of overdose, contact the Poisons Information Centre on 13 11 26 (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 eye drops 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 randomised, placebo-controlled environmental study conducted during the ragweed pollen season, involving 159 patients with symptomatic allergic conjunctivitis, known to be sensitive to ragweed. The trial showed that olopatadine eye drops 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 eye drops group, the slopes of the lines predicting ocular itching, redness and tearing were lower than the slopes for placebo, indicating that olopatadine eye drops 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

Absorption.

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 from 0.5 to 1.3 nanogram/mL.

Metabolism.

Two metabolites, the mono-desmethyl and the N-oxide, were detected at low concentrations in the urine.

Excretion.

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.

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 (78,000 and 31,000 times the maximum recommended ocular human use level, respectively).

6 Pharmaceutical Particulars

6.1 List of Excipients

The inactive ingredients in Paladopt are: benzalkonium chloride, dibasic sodium phosphate, hydrochloric acid, sodium chloride, sodium hydroxide, water for injections.

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. Discard 4 weeks after opening.

6.5 Nature and Contents of Container

Container type: Bottle (LDPE).
Pack sizes: 5 mL.
Some strengths, pack sizes and/or pack types may not be marketed.

6.6 Special Precautions for Disposal

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

6.7 Physicochemical Properties

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: 373.88.
Olopatadine hydrochloride, a dibenzoxepine derivative, is a white, crystalline, water-soluble powder. It has a melting point of 248°C (decomposition).
Paladopt is 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.

CAS number.

140462-76-6.

7 Medicine Schedule (Poisons Standard)

S4 (Prescription Only Medicine).

Summary Table of Changes