IOPIDINE SOLUTION

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Active ingredient:
APRACLONIDINE (APRACLONIDINE HYDROCHLORIDE)
Available from:
NOVARTIS PHARMACEUTICALS CANADA INC
ATC code:
S01EA03
INN (International Name):
APRACLONIDINE
Dosage:
1%
Pharmaceutical form:
SOLUTION
Composition:
APRACLONIDINE (APRACLONIDINE HYDROCHLORIDE) 1%
Administration route:
OPHTHALMIC
Units in package:
0.1MLX2
Prescription type:
Prescription
Therapeutic area:
EENT DRUGS, MISCELLANEOUS
Product summary:
Active ingredient group (AIG) number: 0122471001; AHFS: 52:92.00
Authorization status:
APPROVED
Authorization number:
00888354
Authorization date:
2017-11-22

Documents in other languages

IOPIDINE Product Monograph

Page 1 of 29

PRODUCT MONOGRAPH

INCLUDING PATIENT MEDICATION INFORMATION

IOPIDINE

®

Apraclonidine Ophthalmic Solution, USP

0.5% w/v and 1% w/v (as apraclonidine hydrochloride)

S01EA03 Ophthalmologicals: Antiglaucoma Preparations and Miotics

Novartis Pharmaceuticals Canada Inc.

385 Bouchard Blvd.

Dorval, Quebec

H9S 1A9

www.novartis.ca

Date of Preparation:

February 15, 1994

Date of Revision:

February 8, 2018

Submission Control No:

IOPIDINE is a registered trademark

IOPIDINE Product Monograph

Page 2 of 29

Table of Contents

PART I: HEALTH PROFESSIONAL INFORMATION .........................................................3

SUMMARY PRODUCT INFORMATION ........................................................................3

INDICATIONS AND CLINICAL USE ..............................................................................3

CONTRAINDICATIONS ...................................................................................................4

WARNINGS AND PRECAUTIONS ..................................................................................4

ADVERSE REACTIONS ....................................................................................................6

DRUG INTERACTIONS ..................................................................................................10

DRUG INTERACTIONS ..................................................................................................10

DOSAGE AND ADMINISTRATION ..............................................................................11

OVERDOSAGE ................................................................................................................11

ACTION AND CLINICAL PHARMACOLOGY ............................................................12

STORAGE AND STABILITY ..........................................................................................12

DOSAGE FORMS, COMPOSITION AND PACKAGING .............................................13

PART II: SCIENTIFIC INFORMATION ...............................................................................14

PHARMACEUTICAL INFORMATION ..........................................................................14

CLINICAL TRIALS ..........................................................................................................14

DETAILED PHARMACOLOGY .....................................................................................16

TOXICOLOGY .................................................................................................................18

REFERENCES ..................................................................................................................19

PART III: PATIENT MEDICATION INFORMATION ........................................................20

PART III: PATIENT MEDICATION INFORMATION ........................................................24

IOPIDINE

®

Product Monograph

Page 3 of 29

IOPIDINE

®

Apraclonidine Ophthalmic Solution, USP

PART I: HEALTH PROFESSIONAL INFORMATION

SUMMARY PRODUCT INFORMATION

Route of

Administration

Dosage Form / Strength

Clinically Relevant Nonmedicinal

Ingredients

Ophthalmic

(topical)

Ophthalmic solution/

apraclonidine 0.5% w/v and 1%

w/v (as apraclonidine

hydrochloride)

Benzalkonium chloride as preservative.

For a complete listing see Dosage

Forms, Composition and Packaging

section.

INDICATIONS AND CLINICAL USE

IOPIDINE

®

1%

IOPIDINE

1% (apraclonidine ophthalmic solution) is indicated for the control or prevention of

postsurgical elevations in intraocular pressure (IOP) that occur in patients after anterior segment

laser ophthalmic surgery including argon laser trabeculoplasty, argon

laser iridotomy and

neodymium:yttrium aluminum garnet (Nd:YAG) laser posterior capsulotomy.

IOPIDINE

®

0.5%

IOPIDINE 0.5% (apraclonidine ophthalmic solution) is indicated for adjunctive use in lowering

intraocular pressure (IOP) and may be used as a short-term therapy in glaucoma patients on

maximally tolerated medical therapy who require an additional IOP reduction.

The largest body of clinical data regarding the efficacy of apraclonidine as an adjunctive drug

has been obtained in patients using timolol as the primary therapy. Apraclonidine has also been

found to be effective in combination with topical betaxolol, carbachol, dipivefrin, echothiophate,

epinephrine, levobunolol and pilocarpine and systemic acetazolamide and methazolamide.

The addition of IOPIDINE 0.5% to patients already using two aqueous suppressing drugs (i.e.

beta-blocker plus carbonic anhydrase inhibitor) as part of their maximally tolerated medical

therapy

provide

much

additional

benefit.

Since

IOPIDINE

0.5%

aqueous

suppressing drug, the addition of a third aqueous suppressant may not significantly reduce IOP.

IOPIDINE Product Monograph

Page 4 of 29

Geriatrics (> 65 years of age):

IOPIDINE, 1% and 0.5%, is not recommended for use in the elderly as the safety and efficacy of

IOPIDINE, 1% or 0.5%, have not been established in this population (see

WARNINGS AND

PRECAUTIONS, Special Populations, Geriatrics

Pediatrics (< 18 years of age):

IOPIDINE, 1% and 0.5%, is contraindicated for use in children as the safety and efficacy of

IOPIDINE, 1% or 0.5%, have not been established in this population (see

WARNINGS AND

PRECAUTIONS, Special Populations, Pediatrics

CONTRAINDICATIONS

IOPIDINE, 1% and 0.5%, is contraindicated in patients who are:

Hypersensitive to this drug or to any ingredient in the formulation or component of the

container. For a complete listing, see the

DOSAGE FORMS, COMPOSITION AND

PACKAGING

section of the product monograph.

Hypersensitive to clonidine.

Receiving monoamine oxidase inhibitors (MAOIs).

IOPIDINE,

0.5%,

contraindicated

children

(see

WARNINGS

AND

PRECAUTIONS

Special Populations

Pediatrics

WARNINGS AND PRECAUTIONS

General

NOT FOR INJECTION. Topical ophthalmic use only.

IOPIDINE, 1% and 0.5%, is a potent depressor of intraocular pressure (IOP); therefore, patients

may develop exaggerated reductions in IOP and should be closely monitored.

IOPIDINE 0.5%:

In most patients, a loss of effect occurs over time. This appears to be an individual occurrence

with a variable time of onset and should be closely monitored.

Use of IOPIDINE 0.5% can lead to an allergic-like reaction characterized wholly or in part by

the symptoms of hyperemia, pruritus, discomfort, tearing, foreign body sensation, and edema of

the lids and conjunctiva. If ocular allergic-like symptoms occur, IOPIDINE 0.5% therapy should

be discontinued. The allergic-like reaction associated with apraclonidine use may be masked by

seasonal allergic conjunctivitis.

Effects on ability to drive and use machinery:

IOPIDINE, 1% and 0.5%, can cause dizziness and somnolence. Patients who engage in mental

activities requiring mental alertness should be warned of the potential for a decrease in mental

IOPIDINE

®

Product Monograph

Page 5 of 29

alertness, especially when using IOPIDINE 0.5%. Patients should be advised not to drive or

operate machinery.

Cardiovascular

Caution

should

exercised

patients

with

severe

cardiovascular

disease,

including

hypertension. The possibility of a vasovagal attack should be considered and caution should be

exercised in patients with a history of such episodes.

Caution should also be exercised in patients with coronary insufficiency, recent myocardial

infarction, cerebrovascular disease, Raynaud’s disease or thromboanginitis obliterans.

Hepatic

IOPIDINE 0.5%:

Close monitoring of patients with impaired liver function is advised as the systemic dosage form

of clonidine is partly metabolized in the liver.

Ophthalmologic

IOPIDINE 0.5%:

Contact with soft contact lenses should be avoided. IOPIDINE 0.5% contains the preservative

benzalkonium chloride, which may cause eye irritation and is known to discolour soft contact

lenses. Patients must be instructed to remove contact lenses prior to application of IOPIDINE

0.5% and wait at least 15 minutes before re-insertion.

Psychiatric

IOPIDINE

0.5%:

Caution and monitoring of depressed patients are advised since apraclonidine has been

associated with depression.

Renal

IOPIDINE 0.5%:

Close monitoring of patients with impaired renal function is advised if they are candidates for

topical IOPIDINE 0.5% therapy. While systemic absorption of apraclonidine following topical

administration is low (see

DETAILED PHARMACOLOGY, Pharmacokinetics

), structurally-

related clonidine does undergo a significant increase in half-life in patients with severe renal

impairment.

Sexual Function/Reproduction

Human clinical

studies have not been performed to evaluate the effect of

topical

ocular

administration of IOPIDINE, 1% or 0.5%, on fertility. Reproduction and fertility studies in rats

showed no adverse effect on male or female fertility at doses 5 to 10 times the maximum

recommended human dose.

Special Populations

Pregnant Women:

IOPIDINE, 1% and 0.5%, is not recommended for use during pregnancy.

The safety of IOPIDINE, 1% and 0.5%, has not been evaluated in adequate and well controlled

IOPIDINE Product Monograph

Page 6 of 29

studies in pregnant women. Animal studies have shown that apraclonidine can have direct

embryocidal effects in rabbits (see

TOXICOLOGY, Reproduction and Teratology

Nursing Women:

Breastfeeding should be discontinued while using IOPIDINE, 1% and 0.5%.

It is not known if topically applied IOPIDINE, 1% or 0.5%, is excreted in human milk. However,

systemic clonidine can be found in mother's milk.

Geriatrics (> 65 years of age):

IOPIDINE, 1% and 0.5%, is not recommended for use in the elderly as the safety and efficacy of

IOPIDINE, 1% or 0.5%, have not been established in this population.

Pediatrics (< 18 years of age)

: IOPIDINE, 1% and 0.5%, is contraindicated for use in children

(see

CONTRAINDICATIONS

Adverse

reactions

including

lethargy,

bradycardia

decreased oxygen saturation have been reported in neonates and infants under 1 year of age even

when

single

dose

IOPIDINE,

0.5%,

administered

(see

ADVERSE

REACTIONS, Pediatric Population

ADVERSE REACTIONS

Adverse Drug Reaction Overview

The most commonly reported adverse events for IOPIDINE 1% in the use of laser surgery are

upper lid elevation (1.3%), conjunctival blanching (0.4%) and mydriasis (0.4%).

The most commonly reported adverse events for IOPIDINE 0.5% leading to discontinuation

include

hyperemia,

pruritus,

discomfort,

tearing,

mouth,

edema

foreign

body

sensation.

Clinical Trial Adverse Drug Reactions

Because clinical trials are conducted under very specific conditions the adverse reaction rates

observed in the clinical trials may not reflect the rates observed in practice and should not be

compared to the rates in the clinical trials of another drug. Adverse drug reaction information

from clinical trials is useful for identifying drug-related adverse events and for approximating

rates

IOPIDINE

®

Product Monograph

Page 7 of 29

IOPIDINE 1%:

The following adverse events were reported in association with the use of IOPIDINE 1% in laser

surgery: upper lid elevation (1.3%), conjunctival blanching (0.4%) and mydriasis (0.4%).

The following adverse events were observed in investigational non-laser surgery studies in which

IOPIDINE 1% was administered once or twice daily for up to 28 days

Cardiovascular disorders:

bradycardia, orthostatic episode, palpitations, vasovagal attack;

Central nervous system disorders:

decreased libido, dream disturbances, insomnia, irritability;

Eye disorders:

allergic response, blurred or dimmed vision, burning, conjunctival blanching,

conjunctival microhemorrhage, discomfort, dryness, foreign body sensation, hypotony, itching,

mydriasis, upper lid elevation;

Gastrointestinal disorders:

abdominal pain, diarrhea, discomfort, emesis stomach;

Other disorders:

body heat sensation, chest heaviness or burning, clammy or sweaty palms, dry

mouth, extremity pain or numbness, fatigue, headache, head cold sensation, increased pharyngeal

secretion, nasal burning or dryness, paresthesia, pruritus not associated with rash, shortness of

breath, taste abnormalities.

IOPIDINE Product Monograph

Page 8 of 29

IOPIDINE 0.5%:

Table 1

-

Treatment-related adverse reactions (incidence rate ≥ 2.0%) in placebo-controlled clinical

studies of IOPIDINE 0.5%

Coded Adverse

Event

SINGLE THERAPY

N=183

ADJUNCTIVE +

MAXIMAL THERAPY

N=152

PLACEBO

N=160

N

%

N

%

N

%

Ocular

Pruritus

13.1

Discomfort

10.4

Hyperemia

16.4

Tearing

Dry Eye

Foreign Body

Sensation

Lid Edema

Blanching

Blurred Vision

Conjunctivitis

Nonocular

Body as a Whole

Headache

Asthenia

Central Nervous

System

Somnolence

Dizziness

Digestive

Dry Mouth

21.3

10.0

Constipation

Respiratory

Dry Nose

Rhinitis

Special Senses

Taste Perversion

N = sample size

Use of IOPIDINE 0.5% can lead to an allergic-like reaction characterized wholly or in part by

the symptoms of hyperemia, pruritus, discomfort, tearing, foreign body sensation, and edema of

the lids and conjunctiva.

The overall discontinuation rate in clinical studies with IOPIDINE 0.5% was 16%. The most

commonly reported events leading to discontinuation included (in decreasing order of frequency)

hyperemia, pruritus, discomfort, tearing, dry mouth, lid edema, and foreign body sensation.

IOPIDINE

®

Product Monograph

Page 9 of 29

The following adverse reactions (incidence) were reported in clinical studies of IOPIDINE 0.5%

as being related to therapy:

Ocular:

Hyperemia (11.9%), pruritus (11.3%), discomfort (7.2%), tearing (4.8%), foreign body

sensation (2.7%), lid edema (2.4%), dry eye (2.1%), blurred vision (1.8%), blanching (1.5%),

conjunctivitis (1.5%), lid margin crusting (1.2%).

Body as a whole:

Headache (2.7%), asthenia (2.1%).

Central nervous system:

Somnolence (1.2%), dizziness (1.2%).

Digestive system:

Dry mouth (12.8%), constipation (1.5%).

Respiratory system:

Dry nose (3.3%), rhinitis (1.2%).

Special senses:

Taste perversion (3.6%).

Less Common Clinical Trial Adverse Drug Reactions (<1%)

Ocular:

Conjunctival edema (0.9%), discharge (0.9%), abnormal vision (0.9%), pain (0.6%), lid

disorder

(0.6%),

edema

(0.6%),

erythema

(0.6%),

irritation

(0.3%),

keratitis

(0.3%),

blepharitis (0.3%), blepharoconjunctivitis (0.3%), photophobia (0.3%), conjunctival follicles

(0.3%), scleritis (0.3%), keratopathy (0.3%), lid scales (0.3%), corneal infiltrate (0.3%), corneal

staining (0.3%).

Body as a whole:

Chest pain (0.6%), abnormal coordination (0.3%), malaise (0.3%).

Cardiovascular:

Peripheral edema (0.3%), arrhythmia. Although no reports of bradycardia

related to 0.5% Apraclonidine Hydrochloride Ophthalmic Solution were available from clinical

studies, the possibility of its occurrence based on apraclonidine's alpha 2 agonist effect should be

considered.

Central nervous system:

Depression (0.6%), nervousness (0.6%), insomnia (0.3%), paresthesia

(0.3%).

Digestive system:

Nausea (0.6%).

Musculoskeletal system:

Myalgia (0.3%).

Respiratory system:

Dyspnea (0.3%), pharyngitis (0.3%).

Skin:

Contact dermatitis (0.3%), dermatitis (0.3%).

Special senses:

Parosmia (0.3%).

IOPIDINE Product Monograph

Page 10 of 29

Post-Market Adverse Drug Reactions

IOPIDINE 1%:

The following adverse reactions were seen either in subsequent clinical trials or via spontaneous

post-market reporting:

Eye disorders:

conjunctival vascular disorder, eyelid retraction, ocular hyperemia, punctate

keratitis;

Gastrointestinal disorders:

nausea;

Nervous system disorders:

dizziness postural, presyncope, syncope;

Vascular disorders:

hypertension, hypotension.

Immune system disorders:

hypersensitivity

IOPIDINE 0.5%:

The following adverse reactions were seen either in subsequent clinical trials or via spontaneous

post-market reporting:

Eye disorders:

blepharospasm, conjunctival vascular disorders, eyelid ptosis, mydriasis, visual

acuity reduced;

General disorders and administration site conditions:

fatigue, irritability;

Respiratory, thoracic and mediastinal disorders:

rhinorrhea, throat irritation;

Vascular disorders:

vasodilation.

Immune system disorders:

hypersensitivity

Pediatric Population

IOPIDINE, 1% and 0.5%, is contraindicated for use in children. Adverse reactions including

lethargy, bradycardia and decreased oxygen saturation have been reported in neonates and

infants under 1 year of age even when a single dose of apraclonidine was administered.

DRUG INTERACTIONS

Overview

IOPIDINE, 1% and 0.5%, is contraindicated in patients receiving monoamine oxidase inhibitors

(MAOIs).

There is the potential for interactions with CNS depressants, tricyclic antidepressants, beta-

blockets, antihypertensives and cardiac glycosides.

Drug-Drug Interactions

IOPIDINE, 1% and 0.5%, is contraindicated in patients receiving monoamine oxidase inhibitors

(MAOIs). Alpha-antagonists, including apraclonidine, could potentiate the centrally mediated

effects of MAOIs, in particular the side effects of orthostatic hypotension. Concomitant use of

alpha-antagonists and MAOIs could produce a profound synergistic hypotensive effect and cause

cardiovascular collapse in sensitive patients.

The possibility of an additive or potentiating effect with CNS depressants (alcohol, barbiturates,

opiates, sedatives, anesthetics) should be borne in mind.

IOPIDINE

®

Product Monograph

Page 11 of 29

Tricyclic

antidepressants

have

been

reported

blunt

hypotensive

effect

systemic

clonidine. It is not known whether the concurrent use of these agents with apraclonidine can lead

to a reduction in IOP lowering effect. No data on the level of circulating catecholamines after

apraclonidine withdrawal are available. Caution, however, is advised in patients taking tricyclic

antidepressants which can affect the metabolism and uptake of circulating amines.

Since apraclonidine may reduce pulse and blood pressure, caution in using drugs such as beta-

blockers

(ophthalmic

systemic),

antihypertensives,

cardiac

glycosides

advised.

Patients using cardiovascular drugs concurrently with apraclonidine should have pulse and blood

pressures frequently monitored. Caution should be exercised with simultaneous use of clonidine

and other similar pharmacologic agents.

IOPIDINE 0.5%:

No specific drug interactions with topical glaucoma drugs (betaxolol, carbachol, dipivefrin,

echothiopate,

epinephrine,

levobunolol,

pilocarpine,

timolol)

systemic

medications

(acetazolamide, methazolamide) were identified in clinical studies with IOPIDINE 0.5%.

DOSAGE AND ADMINISTRATION

Recommended Dose and Dose Adjustment

IOPIDINE 1%:

One drop of IOPIDINE 1% should be instilled in the scheduled operative eye one hour before

initiating anterior segment laser surgery and a second drop should be instilled in the same eye

immediately upon completion of the laser surgical procedure. Use a separate container for each

single drop dose and discard each container after use.

IOPIDINE 0.5%:

One to two drops of IOPIDINE 0.5% should be instilled in the affected eye(s) two or three times

daily. Since IOPIDINE 0.5% will be used with other ocular glaucoma therapies, an approximate

5 minute interval between instillation of each medication should be practised to prevent washout

of the previous dose.

Missed Dose

IOPIDINE 0.5%:

If a dose is missed, a single drop should be applied as soon as possible before reverting to the

regular dose. Do not use a double dose to make up for a missed dose.

OVERDOSAGE

Overdose is unlikely with topical ocular instillation, as the volume of exposure is limited by the

capacity of the cul-de-sac. The small volume packaging and unique design of the DROP-

TAINER

limit the potential for accidental overdosage by ingestion.

IOPIDINE Product Monograph

Page 12 of 29

Signs of toxicity of apraclonidine in animals include lethargy, decreased activity, loss of appetite,

hypothermia,

decreased

motility

constipation.

Following

oral

administration

apraclonidine to monkeys, plasma levels 100 times greater than those seen in human plasma

level studies were associated with moderate signs of toxicity, including lethargy, hypoactivity,

and loss of appetite; no significant target organ toxicities were found. Acute oral toxicity studies

in rats and mice resulted in LD

values of 64 and 5 mg/kg, respectively. While higher doses

usually caused deaths within 24 hours, lower doses often resulted in delayed deaths.

While no instances of human ingestion of IOPIDINE, 1% and 0.5%, are known, overdose with

the oral form of clonidine has been reported to cause hypotension, transient hypertension,

asthenia, vomiting, irritability, diminished or absent reflexes, lethargy, somnolence, sedation or

coma, pallor, hypothermia, bradycardia, conduction defects, arrhythmias, dryness of the mouth,

miosis, apnea, respiratory depression, hypoventilation, and seizure, particularly in children.

Treatment of an oral overdose includes supportive and symptomatic therapy; a patent airway

should be maintained. Gastric lavage, IV fluids, atropine, dopamine, tolazoline, furosemide and

diazoxide have been reported to be useful in treating the systemic symptoms associated with oral

clonidine overdose. Hemodialysis is of limited value, since a maximum of 5% of circulating drug

is removed.

An ocular overdose can be flushed from the eye(s) with lukewarm water.

For management of a suspected drug overdose, contact your regional Poison Control Centre.

ACTION AND CLINICAL PHARMACOLOGY

Apraclonidine is a relatively selective alpha adrenergic agonist and does not have significant

membrane stabilizing (local anaesthetic) activity. When instilled into the eye, apraclonidine has

the action of reducing intraocular pressure (IOP). Aqueous fluorophotometry studies in humans

demonstrate that apraclonidine's predominant mechanism of action is reduction of aqueous flow

via stimulation of the alpha-adrenergic system.

Apraclonidine is a partial agonist for alpha 1 and alpha 2 adrenergic receptors. The affinity of

apraclonidine for alpha 2 receptors, as measured by competitive radioligand binding studies, is

much higher than its affinity toward alpha 1 receptors.

onset

action

apraclonidine

usually

noted

within

hour

following

administration. The maximum IOP reduction usually occurs three to five hours after application

of a single dose.

STORAGE AND STABILITY

Store between 2-30

C (36 – 86

F). Do not freeze. Protect from light. Keep out of the reach and

sight of children.

IOPIDINE

®

Product Monograph

Page 13 of 29

DOSAGE FORMS, COMPOSITION AND PACKAGING

IOPIDINE 1%:

IOPIDINE 1% is a sterile isotonic aqueous solution containing:

Medicinal ingredient:

apraclonidine hydrochloride 1.15% equivalent to 1% apraclonidine base

Preservative:

benzalkonium chloride 0.01%

Non-medicinal

ingredients:

sodium

chloride,

sodium

acetate,

sodium

hydroxide

and/or

hydrochloric acid (to adjust pH) and purified water.

IOPIDINE 1% is supplied as follows: 0.1 mL in plastic ophthalmic dispensers, packaged two per

pouch. These dispensers are enclosed in a foil overwrap as an added barrier to evaporation.

IOPIDINE 0.5%:

IOPIDINE 0.5% is a sterile isotonic aqueous solution containing:

Medicinal ingredient:

apraclonidine hydrochloride 0.575% equivalent to 0.5% apraclonidine

base

Preservative:

benzalkonium chloride 0.01%

Non-medicinal

ingredients:

sodium

chloride,

sodium

acetate,

sodium

hydroxide

and/or

hydrochloric acid (to adjust pH) and purified water.

IOPIDINE 0.5% is supplied in a 5 mL plastic DROP-TAINER

dispenser.

Tamper evidence is provided by a closure with an extended skirt that locks to the bottle finish on

application and breaks away from the closure on opening. After cap is removed: if tamper

evident snap collar is loose, remove before using product.

IOPIDINE Product Monograph

Page 14 of 29

PART II: SCIENTIFIC INFORMATION

PHARMACEUTICAL INFORMATION

Drug Substance

Proper name: Apraclonidine hydrochloride

Chemical name: 2-[(4-Amino-2,6-dichlorophenyl)imino]imidazolidine

monohydrochloride

Molecular formula and molecular mass: C

HCl; 281.6

Structural formula:

Physicochemical properties: Apraclonidine hydrochloride is a white to off-white powder

and is highly soluble in water.

CLINICAL TRIALS

Laser Surgery Therapy

Optic nerve head damage and visual field loss may result from an acute elevation in intraocular

pressure (IOP) that can occur after surgical procedures. Elevated IOP, whether acute or chronic

in duration, is a major risk factor in the pathogenesis of visual field loss. The higher the peak or

spike of IOP, the greater the likelihood of visual field loss and optic nerve damage especially in

patients with previously compromised optic nerves.

Placebo-controlled clinical studies in patients requiring argon laser trabeculoplasty, argon laser

iridotomy or Nd:YAG laser posterior capsulotomy showed that IOPIDINE

1% apraclonidine

ophthalmic solution) controlled or prevented the postsurgical IOP rise typically observed in

patients after undergoing those procedures. After surgery, the mean IOP was 1.9 to 4.0 mmHg

below the corresponding pre-surgical baseline pressure before IOPIDINE 1% treatment.

With

placebo

treatment,

postsurgical

pressures

were

mmHg

higher

than

their

corresponding pre-surgical baselines. Overall, only 2% of patients treated with IOPIDINE 1%

had severe IOP elevations (spikes ≥ 10 mm Hg) during the first three hours after laser surgery,

whereas 23% of placebo-treated patients responded with severe pressure spikes (

Table 2

). Of the

patients that experienced a pressure spike after surgery, the peak IOP was above the 30 mmHg in

IOPIDINE

®

Product Monograph

Page 15 of 29

most patients (Table 3) and was above 50 mmHg in seven placebo-treated patients and one

IOPIDINE 1% -treated patient.

Table 2: Incidence of Postsurgical Intraocular Pressure Spikes ≥ 10 mmHg Following Laser Surgery

Therapy

Study

Laser Procedure

Treatment

Apraclonidine

Placebo

Overall

0/76

22/79

Overall

3/84

15/84

Trabeculoplasty

0/50

12/51

Trabeculoplasty

2/41

8/42

Iridotomy

0/13

8/19

Iridotomy

0/18

4/19

Posterior

Capsulotomy

Posterior

Capsulotomy

1/25

3/23

N = Number Spikes/Number Eyes

Table 3: Magnitude of Postsurgical Intraocular Pressure in Patients with Severe Pressure Spikes ≥ 10

mmHg Following Laser Surgery Therapy

Treatment

Total Spikes

Maximum Postsurgical Intraocular Pressure (mmHg)

20-29 mmHg

30-39 mmHg

40-49 mmHg

> 50 mmHg

Apraclonidine

Placebo

Glaucoma Therapy:

Dose-response and comparative studies (0.125% - 1.0% apraclonidine) demonstrate that 0.5%

apraclonidine is at the top of the dose/response IOP reduction curve. Based upon the dose

response and efficacy studies, and the incidence of ocular allergic and systemic side effects (see

WARNINGS AND PRECAUTIONS

), IOPIDINE 0.5% is recommended for short term use in

glaucoma patients on maximally tolerated medical therapy who require an additional IOP

reduction.

The utility of IOPIDINE 0.5% is most apparent for those glaucoma patients on maximally

tolerated medical therapy. In such patients, IOPIDINE 0.5% provided further IOP reductions of

2.1 to 3.2 mmHg for three months, even when patients were using a beta-blocker, epinephrine,

pilocarpine, and oral carbonic anhydrase inhibitors, and had undergone laser trabeculoplasty.

Among those patients on maximally tolerated medical therapy whose IOP remained uncontrolled

at 22 mmHg or greater, IOPIDINE 0.5% was particularly effective, providing an additional IOP

reduction of 3.7 to 5.0 mmHg. Filtration surgery was performed in about 15% of patients due to

treatment failure; the average therapy time before surgery was 4.3 months. An additional 19.8%

of patients were discontinued due to adverse events, primarily allergic-like reactions. Thus, in

approximately 67% of the patients, IOPIDINE 0.5% provided substantial control of glaucoma.

IOPIDINE Product Monograph

Page 16 of 29

Adjunctive therapy studies in glaucoma patients demonstrated that IOPIDINE 0.5% dosed BID

for 90 days in patients receiving 0.5% timolol, effectively lowered IOP by an additional 2.5 to

5.0 mmHg. The additional IOP reduction with apraclonidine is more pronounced shortly (3 hrs)

after instillation. IOPIDINE 0.5% as a single therapy dosed TID for 90 days effectively lowered

IOP by 3.9 to 7.9 mmHg in glaucoma patients. Although afternoon IOP reduction is comparable

between a beta-blocker and IOPIDINE 0.5%, a beta-blocker is more effective in reducing

morning IOP than IOPIDINE 0.5%.

The IOP lowering efficacy of IOPIDINE 0.5% is diminished over time in some patients. This

loss of control, or tachyphylaxis, appears to be an individual occurrence with an unpredictable

onset.

Approximately 20% of patients treated with IOPIDINE 0.5% experienced apparent ocular

allergic responses (mean onset time 38.6 days, with a range of 1 to 158 days), which resolved

upon discontinuation of drug therapy.

The overall discontinuation rates in clinical studies with IOPIDINE 0.5% ranged from 14.8% in

single therapy studies to 21.5% in adjunctive therapy studies.

The unpredictable loss of IOP control in some patients and incidence of ocular allergic responses

and systemic side effects may limit the length of use of IOPIDINE 0.5% as a single, or

adjunctive, medication in long term use. However, patients on maximally tolerated medical

therapy still benefit from the additional IOP reduction provided by the short term use of

IOPIDINE 0.5%.

DETAILED PHARMACOLOGY

Pharmacodynamics

Human Studies:

Mechanism of Action:

Apraclonidine is a relatively selective alpha-2 adrenergic agonist and

does not have significant membrane stabilizing (local anaesthetic) activity. When instilled in the

eye, apraclonidine has the action of reducing elevated, as well as normal, intraocular pressure

(IOP), whether or not accompanied by glaucoma.

Aqueous fluorophotometry studies in humans demonstrate that apraclonidine's predominant

mechanism of action is reduction of aqueous flow via stimulation of the alpha-adrenergic system.

Unlike beta-blockers and epinephrine, apraclonidine reduces aqueous flow during the day and

also at night during sleep. Apraclonidine's mechanism of action may account for the additional

IOP reductions observed after instillation of Apraclonidine Ophthalmic Solution in patients

receiving a beta-blocker or receiving maximally tolerated medical therapy.

Cardiovascular:

In a safety study involving 21 healthy volunteers administered 1 drop of 1%

apraclonidine

hydrochloride

ophthalmic

solution

twice

daily

consecutive

days,

clinically significant effects attributable to the drug could be found when blood pressure and

heart rate were measured.

IOPIDINE

®

Product Monograph

Page 17 of 29

Central Nervous System Effects:

A statistically significant decreased IOP was observed in the

contralateral eye of normal volunteers treated unilaterally with 1% apraclonidine hydrochloride

ophthalmic solution. During the seven hour period following treatment, there was a mean

maximum decrease of 6.5 ± 4.3 mmHg in the treated eye (a 37.3% ± 20.4% decrease from pre-

treatment baseline) and a mean maximum decrease of 2.7 ± 3.4 mmHg in the contralateral eye (a

14.9% ± 19% decrease from pre-treatment baseline).

Ocular Effects:

IOPIDINE 0.5% does not produce miosis or myopia commonly associated with

cholinergic agents. The blurred vision and night blindness often observed with standard miotic

therapy are not associated with IOPIDINE 0.5%. Thus patients with central lenticular opacities

avoid the visual impairment caused by a constricted pupil.

Animal Studies:

Blood Flow Effects:

Apraclonidine Ophthalmic Solution, because of its alpha adrenergic

activity, is a vasoconstrictor. Single dose ocular blood flow studies in monkeys, using the

microsphere technique, demonstrated a reduced blood flow for the anterior segment; however, no

reduction in blood flow was observed in the posterior segment of the eye after a topical dose of

0.5%

Apraclonidine

Ophthalmic

Solution.

Chronic

treatment

primates

with

1.5%

Apraclonidine Ophthalmic Solution three times a day for one year did not result in morphologic

effects which would be indicative of vasoconstriction of the anterior or posterior segments of the

eye. Ocular blood flow studies have not been conducted in humans.

Pharmacokinetics:

Human Studies:

The onset of action of apraclonidine can usually be noted within one hour, and the maximum

IOP reduction occurs three to five hours after application. Significant IOP reduction can be

maintained with 0.5% Apraclonidine Ophthalmic Solution; the duration of action in some

patients is less than 12 hours.

Topically

administered

apraclonidine

absorbed

systematically

present

concentrations in the plasma. Studies of 0.5% Apraclonidine Ophthalmic Solution dosed one

drop three times a day in both eyes for 10 days in normal volunteers yielded mean peak and

trough apraclonidine plasma concentrations of 0.9 ng/mL and 0.5 ng/mL, respectively. The half-

life of apraclonidine was calculated to be 8 hours. Protein binding has been measured in human

plasma by ultrafiltration and equilibrium dialysis (3). Both methods indicated the extent of

binding to be low (22-29%). These data are consistent with the low frequency of systemic side

effects observed with apraclonidine in controlled clinical studies.

Animal Studies:

Studies in rabbits with radiolabeled apraclonidine have demonstrated absorption into the eye

after topical ocular administration. In the iris-ciliary body, aqueous humor and lens, maximal

concentrations were reached at approximately 2 hours after dosing (1.4, 0.5, and 0.2 ug

equivalents/gm,

respectively).

half-life

apraclonidine

aqueous

humor

approximately 2 hours. Concentrations of 4.7 ug equivalents/gm were measured in the cornea at

20 minutes post-dose.

IOPIDINE Product Monograph

Page 18 of 29

Following IV administration, the plasma half-life of parent apraclonidine was 9 hours in the

Cynomolgus monkey and 3 hours in the rat. In both species the half-life of radioactivity from

apraclonidine was longer than that of the parent drug. Approximately 10 metabolites were

identified in rat urine and plasma. In both rats and Cynomolgus monkeys, urinary excretion was

the primary route of elimination (65-75% of dose) with the balance eliminated in the feces.

TOXICOLOGY

Acute Toxicity

The oral LD

of the drug ranged from 3 to 8 mg/kg in mice and 38 to 107 mg/kg in rats. The

intravenous LD

of the drug ranged from 6 to 9 mg/kg in mice and 9 to 21 mg/kg in rats. LD

values in these ranges are indicative of a drug with a high degree of toxicity. Mortalities occurred

one (1) to nine (9) days after administration, with systemic signs of toxicity including lethargy,

impaired motor co-ordination and partial loss of consciousness. Bloody tears and/or urine and

hypothermia were observed at extremely high doses (≥ 80 mg/kg).

Long Term Toxicity

Topical ocular administration of two drops of 0.5, 1.0 and 1.5% Apraclonidine Hydrochloride

Ophthalmic Solution to New Zealand albino rabbits three times daily for one month resulted in

sporadic

transient

instances

minimal

corneal

edema

1.5%

group

only.

histopathological changes were noted in the affected eyes.

Topical ocular administration of 1.5% Apraclonidine Hydrochloride Ophthalmic Solution three

times daily for one year to Cynomolgus monkeys elicited minimal conjunctival congestion and

single instances of transient and sporadic fluorescein staining. No corneal cloudiness, iritis or

lenticular changes were observed.

Reproduction and Teratology

Reproduction and fertility studies in rats showed no adverse effect on male or female fertility at

doses 5 to 10 times the maximum recommended human dose.

Teratogenicity studies with apraclonidine HCl in rabbits and rats at doses up to 3.0 mg/kg/day in

rabbits (60 times the maximum recommended human dose) and 0.3 mg/kg/day in rats (6 times

maximum

recommended

human

dose)

showed

evidence

fetal

malformations.

Embryotoxicity, however, was evident at the high dose level in the rabbit study. Dose-related

maternal toxicity was evident in both the rat and rabbit studies.

Mutagenicity

No evidence of apraclonidine-induced mutagenicity was observed in

in vitro

microbial (Ames

test), mammalian (mouse lymphoma), chromosome aberration, sister chromatid exchange, or

malignant transformation test assays or in an

in vivo

micronucleus assay.

IOPIDINE

®

Product Monograph

Page 19 of 29

Carcinogenicity

There was no significant increase in tumour incidence or type following two years of oral

administration of apraclonidine HCl to rats at dose levels 20 times the maximum recommended

human dose or in mice at dose levels 12 times the maximum recommended human dose.

Other Studies

Two sensitization assays were performed in animals: the Buehler occlusive patch test in guinea

pigs and the guinea pig maximization test (GPMT). While the Buehler test suggested little or no

potential for sensitization, the GPMT revealed a moderate sensitization potential, indicating that

there may be patients who develop a contact sensitization response with repeated use of this

drug.

REFERENCES

Abrams DA, Robin AL, Pollack IP et al. The safety and efficacy of topical 1%

ALO2145 (p-aminoclonidine hydrochloride) in normal volunteers. Arch Ophthalmol

1987;105:1205-1207.

Gharagozloo

Relf

Brubaker

Aqueous

flow

reduced

alpha-adrenergic agonist, apraclonidine hydrochloride (ALO 2145). Ophthalmology

1988;95:1217-1220.

Koskela T, Brubaker RF. Apraclonidine and timolol. Combined effects in previously

untreated normal subjects. Arch Ophthalmol 1991;109:804-806.

Lish AJ, Camras CB, Podos SM. The effect of apraclonidine on intraocular pressure in

glaucoma patients on maximally tolerated medications. J of Glaucoma, 1992, in press

Morrison JC, Robin AL. Adjunctive glaucoma therapy. A comparison of apraclonidine

to dipivefrin when added to timolol maleate. Ophthalmology 1989;96:3-7.

Robin AL, Pollack IP, House B, Enger C. Effects of ALO2145 on intraocular pressure

following argon laser trabeculoplasty. Arch Ophthalmol 1987;105:646-650.

Robin AL, Pollack IP, deFaller JM. Effects of topical ALO2145 (p-aminoclonidine

hydrochloride) on the acute intraocular pressure rise after argon laser iridotomy.

Arch Ophthalmol 1987;105:1208-1211.

Robin AL. Short-term effects of unilateral 1% apraclonidine therapy. Arch Ophthalmol

1988;106:912-915.

IOPIDINE Product Monograph

Page 20 of 29

READ THIS FOR SAFE AND EFFECTIVE USE OF YOUR MEDICINE

PATIENT MEDICATION INFORMATION

IOPIDINE

®

1%

Apraclonidine Ophthalmic Solution, USP

Read this carefully before you start taking

IOPIDINE

®

1%

and each time you get a refill. This

leaflet is a summary and will not tell you everything about this drug. Talk to your healthcare

professional about your medical condition and treatment and ask if there is any new information

about

IOPIDINE 1%

What is IOPIDINE 1%

used for?

Control or prevention of increases in eye pressure (

intraocular pressure

) following

certain types of laser eye surgery.

How does IOPIDINE 1% work?

IOPIDINE 1% contains apraclonidine, an alpha adrenergic agonist. It works by reducing the

production of liquid in the eye as well as by increasing the rate liquid flows out of the eye.

What are the ingredients in IOPIDINE 1%?

Medicinal ingredient:

Apraclonidine 1% w/v (as apraclonidine hydrochloride)

Non-medicinal

ingredients:

Benzalkonium

chloride

(preservative),

sodium

acetate,

sodium

chloride, sodium hydroxide and/or hydrochloric acid (to adjust pH) and purified water

IOPIDINE 1% comes in the following dosage forms:

Eye drop solution in 0.1 mL plastic dispensers packaged 2 per pouch

Do not use IOPIDINE 1% if you are:

Allergic (

hypersensitive

) to apraclonidine or any of the other ingredients in IOPIDINE

1% (see

What are the ingredients in IOPIDINE 1%?

Allergic to clonidine.

Taking monoamine oxidase inhibitors (MAOIs).

IOPIDINE 1% must not be used in children under 18 years of age.

To help avoid side effects and ensure proper use, talk to your healthcare professional

before you take IOPIDINE 1%. Talk about any health conditions or problems you may

have, including if you:

Have or have had any heart conditions or blood circulation problems, such as:

high blood pressure.

a sudden drop in heart rate and blood pressure (

vasovagal attack

not enough blood flow in the arteries (

coronary insufficiency

heart attack or stroke.

lower blood flow to the fingers and/or toes (

Raynaud’s disease

blocked blood vessels in the hands and/or feet (

thromboanginitis obliterans

IOPIDINE

®

Product Monograph

Page 21 of 29

Are pregnant or plan to become pregnant. You should not use IOPIDINE 1% while you

are pregnant.

breastfeeding

plan

breast-feed.

should

breast-feed

while

using

IOPIDINE 1%.

Other warnings you should know about:

You may become dizzy or sleepy after taking IOPIDINE 1%. Do not drive or operate machines

until these symptoms pass.

Tell your healthcare professional

about all the medicines you take, including any drugs,

vitamins, minerals, natural supplements or alternative medicines.

The following may interact with IOPIDINE 1%:

Monoamine oxidase inhibitors (MAOIs).

Alcohol.

Antidepressants, including barbiturates and tricyclic antidepressants.

Opiates (class of painkillers).

Sedatives.

Anesthetics.

Beta-blockers (medicines used to treat some heart problems).

Anti-hypertensives (medications used to treat high blood pressure).

Heart

medications,

including

those

used

treat

heart

failure

irregular

heartbeats.

How to take IOPIDINE 1%:

Your doctor or nurse will apply IOPIDINE 1% for you. A separate container will be used for

each single drop. Each container will be discarded after use.

Usual adult dose:

1 drop in the eye scheduled for surgery 1 hour before surgery followed by 1 drop in the same eye

after surgery.

Overdose:

An overdose is unlikely as your doctor or nurse will apply IOPIDINE 1% for you.

If you think you have be given too much IOPIDINE 1%, contact your healthcare professional,

hospital emergency department or regional Poison Control Centre immediately, even if there

are no symptoms.

What are possible side effects from using IOPIDINE 1%?

These are not all the possible side effects you may feel when taking IOPIDINE 1%. If you

experience any side effects not listed here, contact your healthcare professional. Please also see

Warnings and Precautions.

Side effects seen with IOPIDINE 1% used in laser surgery include:

IOPIDINE Product Monograph

Page 22 of 29

Raised upper eyelid or widely opened eyes.

White appearance in the eyes.

Dilated pupils.

Red eye.

Damage to the cornea.

Nausea.

Dizziness when standing.

Feeling faint or fainting.

Low or high blood pressure.

Allergy (hypersensitivity)

If you have a troublesome symptom or side effect that is not listed here or becomes bad enough

to interfere with your daily activities, talk to your healthcare professional.

Reporting Side Effects

You can help improve the safe use of health products for Canadians by reporting serious and

unexpected side effects to Health Canada. Your report may help to identify new side effects

and change the product safety information.

3 ways to report

Online at

MedEffect;

By calling 1-866-234-2345 (toll-free);

By completing a Consumer Side Effect Reporting Form and sending it by:

Fax to 1-866-678-6789 (toll-free), or

Mail to:

Canada Vigilance Program

Health Canada, Postal Locator 1908C

Ottawa, ON

K1A 0K9

Postage paid labels and the Consumer Side Effect Reporting Form are available

at MedEffect.

NOTE: Contact your health professional if you need information about how to manage your

side effects. The Canada Vigilance Program does not provide medical advice.

Storage:

Your doctor or nurse will store IOPIDINE between 2

C and 30

C. Protect from light.

If you want more information about IOPIDINE 1%:

Talk to your healthcare professional

Find the full product monograph that is prepared for healthcare professionals and

includes this Patient Medication Information by visiting the Health Canada website; the

manufacturer’s website www.novartis.ca, or by calling 1-800-363-8883.

This leaflet was prepared by Novartis Pharmaceuticals Canada Inc.

Last Revised: November 28, 2017

IOPIDINE

®

Product Monograph

Page 23 of 29

IOPIDINE is a registered trademark

IOPIDINE Product Monograph

Page 24 of 29

READ THIS FOR SAFE AND EFFECTIVE USE OF YOUR MEDICINE

PATIENT MEDICATION INFORMATION

IOPIDINE

®

0.5%

Apraclonidine Ophthalmic Solution, USP

Read this carefully before you start taking

IOPIDINE

®

0.5%

and each time you get a refill. This

leaflet is a summary and will not tell you everything about this drug. Talk to your healthcare

professional about your medical condition and treatment and ask if there is any new information

about

IOPIDINE 0.5%

What is IOPIDINE 0.5% used for?

IOPIDINE 0.5% is used with other medication to lower high pressure in the eyes. If left

untreated, this high pressure can eventually damage the eyes.

How does IOPIDINE 0.5% work?

IOPIDINE 0.5% contains apraclonidine, an alpha adrenergic agonist. It works by reducing the

production of liquid in the eye as well as by increasing the rate liquid flows out of the eye.

What are the ingredients in IOPIDINE

0.5%?

Medicinal ingredient:

apraclonidine hydrochloride

Non-medicinal

ingredients:

benzalkonium

chloride

(preservative),

sodium

acetate,

sodium

chloride, sodium hydroxide and/or hydrochloric acid (to adjust pH) and purified water

IOPIDINE 0.5% comes in the following dosage forms:

Eye drop solution, 0.5% w/v, in a 5 mL dispenser bottle

Do not use IOPIDINE 0.5% if you are:

Allergic (

hypersensitive

) to apraclonidine or any of the other ingredients in IOPIDINE

0.5% (see

What are the ingredients in IOPIDINE 0.5%?

Allergic to clonidine.

Taking monoamine oxidase inhibitors (MAOIs).

IOPIDINE 0.5% must not be used in children under 18 years of age.

To help avoid side effects and ensure proper use, talk to your healthcare professional

before you take IOPIDINE 0.5%. Talk about any health conditions or problems you may

have, including if you:

Have or have had any heart conditions or blood circulation problems, such as

high blood pressure.

a sudden drop in heart rate and blood pressure (

vasovagal attack

not enought blood flow in the arteries (

coronary insufficiency

heart attack or stroke.

lower blood flow to the fingers and/or toes (

Raynaud’s disease

blocked blood vessels in the hands and/or feet (

thromboanginitis obliterans

IOPIDINE

®

Product Monograph

Page 25 of 29

Have liver or kidney problems.

Are or have been depressed.

Are pregnant or plan to become pregnant. You should not use IOPIDINE 0.5% while you

are pregnant.

breastfeeding

plan

breast-feed.

should

breast-feed

while

using

IOPIDINE 0.5%.

Other warnings you should know about:

Over time, IOPIDINE 0.5% may not work as well. Your doctor should monitor you closely.

If you feel any eye allergy symptoms, such as redness, itching, increased tearing, or swelling,

stop using IOPIDINE 0.5% and talk to your doctor.

You may become dizzy, sleepy or less alert after taking IOPIDINE 0.5%. Do not drive or operate

machines until these symptoms pass.

Contact lens wearers

IOPIDINE 0.5% contains the preservative benzalkonium chloride, which can stain contact lenses

and cause eye irritation. Remove your contact lenses before applying IOPIDINE 0.5%. Wait at

least 15 minutes before you put your contacts back in.

Tell your healthcare professional

about all the medicines you take, including any drugs,

vitamins, minerals, natural supplements or alternative medicines.

The following may interact with IOPIDINE 0.5%:

Monoamine oxidase inhibitors (MAOIs).

Alcohol.

Antidepressants, including barbiturates and tricyclic antidepressants.

Opiates (class of painkillers).

Sedatives.

Anesthetics.

Beta-blockers (medicines used to treat some heart problems).

Anti-hypertensives (medications used to treat high blood pressure).

Heart

medications,

including

those

used

treat

heart

failure

irregular

heartbeats.

How to take IOPIDINE 0.5%:

Always use IOPIDINE 0.5% exactly as your doctor has told you.

Get the IOPIDINE 0.5% bottle and a mirror (if needed).

IOPIDINE Product Monograph

Page 26 of 29

Wash your hands.

Twist off the cap. If the security snap collar is loose after removing the cap, remove the

snap collar before using IOPIDINE 0.5%.

Hold the bottle, pointing down, between your thumb and fingers.

Tilt your head back. Pull down your eyelid with a clean finger, until there is a ‘pocket’

between the eyelid and your eye. The drop will go in here (picture 1).

Bring the bottle tip close to the eye. Use the mirror if it helps.

Don’t touch your eye or eyelid, surrounding areas or other surfaces with dropper. It could

contaminate the drops.

Gently press on the base of the bottle to release one drop of IOPIDINE 0.5% at a time

(picture 2). Do not squeeze the bottle: it is designed so that a gentle press on the bottom

of the bottle is all that it needs.

If you miss the eye, wipe up and try again.

If you take drops in both eyes, repeat the steps for your other eye.

Close the bottle cap firmly immediately after use.

Wait at least 5 minutes between applying each eye drop solution you are taking, including

IOPIDINE 0.5%.

Usual adult dose:

Apply 1-2 drops in the eye(s) 2 or 3 times a day. Wait at least 5 minutes between applying each

eye drop solution you are taking, including IOPIDINE 0.5%.

Overdose:

If you apply more IOPIDINE 0.5% than you should, rinse your eyes with lukewarm water. Do

not apply any more drops until it is time for your next regular dose.

think

have

accidentally

ingest

IOPIDINE

0.5%,

contact

your

healthcare

professional, hospital emergency department or regional Poison Control Centre immediately,

even if there are no symptoms.

Missed Dose:

If you forget to apply IOPIDINE 0.5%, apply a single drop as soon as you remember. If it is

close to your next regular dose, skip the missed dose. Do not use a double dose to make up for

the missed dose.

What are possible side effects from using IOPIDINE 0.5%?

These are not all the possible side effects you may feel when taking IOPIDINE 0.5%. If you

experience any side effects not listed here, contact your healthcare professional. Please also see

Warnings and Precautions.

Related to the eyes:

Redness.

Itching.

Discomfort.

IOPIDINE

®

Product Monograph

Page 27 of 29

Increased tearing.

Swelling.

A feeling that something is in eye.

Dry eye.

Blurred, abnormal or reduced vision.

Eyelid margin crusting or scales.

Discharge.

Damage to or staining of the cornea.

Eyelid redness, itching, or swelling.

Pain.

Irritation.

Sensitivity to light.

Eyelid spasms or drooping.

Dilation of the pupils.

Related to rest of body:

Dry mouth.

Headache.

Feeling unwell or tired.

Chest pain.

Coordination problems.

Swelling of the hands of feet.

Abnormal heartbeat.

Sleepiness.

Drowsiness.

Depression.

Nervousness.

Difficulty sleeping.

Tingling of the hands or feet.

Constipation.

Nausea.

Muscle pain.

Dry nose.

Itchy nose or throat.

Problems breathing.

Skin rash.

Bad taste in the mouth.

Problems identifying smells.

Feeling irritable.

Runny nose.

Throat irritation.

Allergy (hypersensitivity)

IOPIDINE Product Monograph

Page 28 of 29

Serious side effects and what to do about them

Symptom / effect

Talk to your healthcare professional

Stop taking drug

and get immediate

medical help

Only if severe

In all cases

UNKNOWN

Allergic-like reaction: eye

redness, itching or discomfort;

increased tearing; foreign body

sensation; swelling of the eye or

eyelid

If you have a troublesome symptom or side effect that is not listed here or becomes bad enough

to interfere with your daily activities, talk to your healthcare professional.

Reporting Side Effects

You can help improve the safe use of health products for Canadians by reporting serious and

unexpected side effects to Health Canada. Your report may help to identify new side effects

and change the product safety information.

3 ways to report

Online at

MedEffect;

By calling 1-866-234-2345 (toll-free);

By completing a Consumer Side Effect Reporting Form and sending it by:

Fax to 1-866-678-6789 (toll-free), or

Mail to:

Canada Vigilance Program

Health Canada, Postal Locator 1908C

Ottawa, ON

K1A 0K9

Postage paid labels and the Consumer Side Effect Reporting Form are available

at MedEffect.

NOTE: Contact your health professional if you need information about how to manage your

side effects. The Canada Vigilance Program does not provide medical advice.

Storage:

Store between 2

C and 30

C. Do not freeze. Protect from light.

Keep out of reach and sight of children.

If you want more information about IOPIDINE 0.5%:

Talk to your healthcare professional

Find the full product monograph that is prepared for healthcare professionals and

includes this Patient Medication Information by visiting the Health Canada website; the

manufacturer’s website www.novartis.ca, or by calling 1-800-363-8883.

This leaflet was prepared by Novartis Pharmaceuticals Canada Inc.

Last Revised: February 8, 2018

IOPIDINE

®

Product Monograph

Page 29 of 29

IOPIDINE is a registered trademark

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