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Logo ZYMAR® eye drops (ophthalmic solution)

SCHEDULING STATUS
Schedule 4

PROPRIETARY NAME
(and dosage form)

ZYMAR® eye drops (ophthalmic solution)

COMPOSITION
Each mL contains 3 mg
gatifloxacin (0,3% m/v)
Preservative: benzalkonium chloride 0,005% m/v

PHARMACOLOGICAL CLASSIFICATION
A 15.1. Ophthalmic preparations with antibiotics and/or sulphonamides

PHARMACOLOGICAL ACTION
Microbiology
Gatifloxacin is an 8-methoxyfluoroquinolone with a 3-methylpiperazinyl substituent at C7. The antibacterial action of gatifloxacin results from inhibition of DNA gyrase and topoisomerase IV. DNA gyrase is an essential enzyme that is involved in the replication, transcription and repair of bacterial DNA. Topoisomerase IV is an enzyme known to play a key role in the partitioning of chromosomal DNA during bacterial cell division.
Resistance to gatifloxacin in vitro develops via multiple-step mutations. The most common reported species showing resistance are methicillin resistantStaphylococcus aureus (0-54%),Pseudomonas aeruginosa (0-13%), Enterobacteriaceae (0-3,4%) and coagulase negativeStaphylococci sp. (0-8%).
Gatifloxacin has been shown to be active against most strains of the following organisms both in vitro and clinically, in conjunctival infections as described in the indications section. In vitro activity does not necessarily imply in vivo activity.
Aerobes, Gram-Positive
Corynebacterium propinquum*, Staphylococcus aureus (variable sensitivity), Staphylococcus epidermidis, Streptococcus mitis*, Streptococcus pneumoniae.
Aerobes, Gram-Negative
Haemophilus influenzae
* Efficacy for this organism was studied in fewer than 10 infections.

Clinical studies
In a randomised double-blind, multicentre clinical trial, where patients were dosed for 5 days, gatifloxacin solution was superior to its vehicle on day 5-7 in patients with conjunctivitis and positive conjunctival cultures. Clinical outcomes for the trial demonstrated clinical cure of 77% (40/52) for the gatifloxacin treated group versus 58% (28/48) for the placebo treated group.
Microbiological outcomes for the same clinical trial demonstrated a statistically superior eradication rate for causative pathogens of 92% (48/52) for gatifloxacin vs. 72% (34/48) for placebo. Please note that microbiological eradication does not always correlate with clinical outcome in anti-infective trials.

Pharmacokinetics
Gatifloxacin ophthalmic solution 0,3% or 0,5% was administered to one eye of 6 healthy male subjects each in an escalated dosing regimen starting with a single 2 drop dose, then 2 drops 4 times daily for 7 days and finally 2 drops 8 times daily for 3 days.
At all time points, serum gatifloxacin levels were below the lower limit of quantification (5 ng/mL) in all subjects.

INDICATIONS
ZYMAR® solution is indicated for the treatment of bacterial conjunctivitis caused by susceptible strains of the following organisms:
Aerobic Gram-Positive bacteria
Corynebacterium propinquum*, Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus mitis*, Streptococcus pneumoniae.
Aerobic Gram-Negative bacteria
Haemophilus influenzae

* Efficacy for this organism was studied in fewer than 10 infections.

CONTRA-INDICATIONS
ZYMAR® solution is contra-indicated in patients with a history of hypersensitivity to gatifloxacin, to other quinolones, or to any of the components in this medication.

WARNINGS AND SPECIAL PRECAUTIONS
NOT SUITABLE FOR INJECTION.
ZYMAR® solution should not be injected subconjunctivally, nor should it be introduced directly in the anterior chamber of the eye.
As the possibility of adverse effects on the corneal permeability, and the danger of disruption of the corneal epithelium with prolonged or repeated usage of benzalkonium chloride preserved ophthalmological preparations, cannot be excluded, regular ophthalmological examination is required. Caution should be exercised in the use of benzalkonium chloride preserved topical medication over an extended period in patients with extensive ocular surface diseases.
In patients receiving systemic quinolones, including gatifloxacin, serious and occasionally fatal hypersensitivity (anaphylactic) reactions, some following the first dose, have been reported. Some reactions were accompanied by cardiovascular collapse, loss of consciousness, angioedema (including laryngeal, pharyngeal or facial oedema), airway obstruction, dyspnoea, urticaria, and itching.
There have been reports of Steven-Johnson Syndrome and anaphylactic reaction reported in associated with topical gatifloxacin use. If a rash or an allergic reaction to gatifloxacin occurs, discontinue the medicine and contact your doctor. Serious acute hypersensitivity reactions may require immediate emergency treatment. Oxygen and airway management should be administered as clinically indicated.
Prolonged use may result in overgrowth of non-susceptible organisms, including fungi. If superinfection occurs discontinue use and institute alternative therapy. Whenever clinical judgement dictates, the patient should be examined with the aid of magnification, such as slit lamp biomicroscopy and, where appropriate, fluorescein staining.
Patients should be advised not to wear contact lenses if they have signs and symptoms of bacterial conjunctivitis. ZYMAR® contains the preservative benzalkonium chloride, which may be absorbed by and cause discolouration of soft contact lenses. Patients wearing soft (hydrophilic) contact lenses should be instructed to remove contact lenses prior to administration of ZYMAR® and wait at least 15 minutes following administration before reinserting soft contact lenses.
Patients should be instructed to avoid allowing the tip of the bottle to contact the eye or surrounding structures, fingers, or any other surface.

Paediatric use
Safety and effectiveness in infants below the age of one year have not been established.

Geriatric use
No overall differences in safety or effectiveness have been observed between elderly and younger patients.

Effects on the ability to drive and use machines
If transient blurred vision occurs at instillation, the patient should wait until the vision clears before driving or using machinery.

INTERACTIONS
Specificmedicine interaction studies have not been conducted with ZYMAR® ophthalmic solution. However, the systemic administration of some quinolones has been shown to elevate plasma concentrations of theophylline, interfere with the metabolism of caffeine, and enhance the effects of the oral anticoagulant warfarin and its derivatives, and has been associated with transient elevations in serum creatinine in patients receiving systemic cyclosporine concomitantly.

PREGNANCY AND LACTATION
Because there are no adequate and well-controlled studies in pregnant women, ZYMAR® solution should not be used during pregnancy.
Nursing mothers: It is not known whether this medicine is excreted in human milk. ZYMAR® should not be used by nursing mothers.

DOSAGE AND DIRECTIONS FOR USE
The recommended dosage regimen for the treatment of bacterial conjunctivitis is:
Days 1 and 2: Instil one drop every two hours in the affected eye(s) while awake, up to 8 times daily.
Days 3 through 7: Instil one drop up to four times daily while awake.

SIDE EFFECTS
For each indication the frequency of adverse reactions arising from clinical experience is given as follows: Very common (>1/10); Common (>1/100, <1/10); Uncommon (>1/1 000, <1/100); Rare (>1/10 000, <1/1 000); Very rare (<1/10 000).
Eye disorders
Very common:
Conjunctivitis
Common: Punctate keratitis, papillary conjunctivitis, increased lacrimation, conjunctival disorder, eyelid oedema, reduced visual acuity, red eye, eye irritation, eye pain, eye discharge, dry eye, conjunctival haemorrhage.
Uncommon: Chemosis
Skin and subcutaneous tissue disorders
Common: Erythema
Uncommon: Contact dermatitis
Gastrointestinal disorders
Common: Taste disturbance
Nervous system disorders
Common: Headache
Post-marketing experience
The following adverse reactions have been identified during post-marketing use of ZYMAR® in clinical practice. Because post-marketing reporting of these reactions is voluntary and from a population of uncertain size, it is not always possible to reliably estimate the frequency of these reactions. The reactions have been chosen for inclusion due to a combination of the frequency of reporting and possible causal connection to ZYMAR®.
Eye disorders
Blepharitis, conjunctival/ocular hyperaemia, blurred vision, eye pruritus, eye swelling (including corneal and conjunctival oedema), eye irritation, eye pain
Gastrointestinal disorders
Nausea
Immune system disorders
Hypersensitivity, anaphylactic reactions and angioedema (including pharyngeal, oral or facial oedema)
Respiratory, thoracic and mediastinal disorders
Dyspnoea
Skin and subcutaneous tissue disorders
Pruritus (including generalised pruritus), rash, urticaria

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT
See SIDE EFFECTS. Treatment is symptomatic and supportive.

IDENTIFICATION
ZYMAR® is a sterile, clear, pale yellow coloured solution.

PRESENTATION
ZYMAR® (gatifloxacin ophthalmic solution) is supplied sterile in a white, low density polyethylene (LDPE) bottle with a controlled dropper tip and a beige, high impact polystyrene (HIPS) cap in the following pack size: 5 mL in an 8 mL bottle.

STORAGE INSTRUCTIONS
Store below 25ºC. Do not freeze. KEEP OUT OF REACH OF CHILDREN.
Do not use more than 30 days after opening. Discard any unused portion.

REGISTRATION NUMBER
A39/15.1/0367

NAME AND BUSINESS ADDRESS OF THE HOLDER OF THE CERTIFICATE OF REGISTRATION
Allergan Pharmaceuticals (Pty) Ltd
30 New Road (entrance off Bavaria Road)
Randjespark Ext. 11, Midrand, 1682
Johannesburg, Gauteng
SOUTH AFRICA

DATE OF PUBLICATION OF THE PACKAGE INSERT
Date of registration: 20 October 2006
Date of most recently revised package insert as approved by Council: 20 October 2006

Updated on this site: October 2017
Source: Pharmaceutical Industry

PATIENT INFORMATION LEAFLET

SCHEDULING STATUS
Schedule 4

PROPRIETARY NAME, STRENGTH AND PHARMACEUTICAL FORM
ZYMAR®gatifloxacin
3,0 mg/mL eye drops (ophthalmic solution)

Read all of this leaflet carefully before you start using ZYMAR®
Keep this leaflet. You may need to read it again.
If you have further questions, please ask your doctor or your pharmacist.
ZYMAR® has been prescribed for you personally and you should not share your medicine with otherpeople. It may harm them, even if their symptoms are the same as yours.

1. WHAT ZYMAR® CONTAINS
The active ingredient is 3 mg/mL gatifloxacin.
The other ingredients are benzalkonium chloride as preservative, edetate disodium, purified water and sodium chloride. May contain hydrochloric acid and/or sodium hydroxide.

2. WHAT ZYMAR® IS USED FOR
ZYMAR®is an antibiotic ophthalmic solution and is used for the treatment of conjunctivitis caused by bacteria.

3. BEFORE YOU USE ZYMAR®
Do not use ZYMAR®
If you are hypersensitive (allergic) to gatifloxacin, other quinolones or to any of the components in this medication.
Do not use in infants under the age of one year.
Take special care with ZYMAR®
NOT SUITABLE FOR INJECTION
As the possibility of adverse effects on the corneal permeability, and the danger of disruption of the corneal epithelium with prolonged or repeated usage of benzalkonium chloride preserved ophthalmological preparations, cannot be excluded, regular ophthalmological examination is required. Caution should be exercised in the use of benzalkonium chloride preserved topical medication over an extended period in patients with extensive ocular surface diseases.

Before using ZYMAR®, tell your doctor:
If you have allergies to any medicines;
If you wear contact lenses.

Pregnancy and breastfeeding
If you are pregnant or breastfeeding your baby, please consult your doctor, pharmacist or other healthcare professional for advice before using ZYMAR®.

If you are pregnant or breastfeeding your baby, you should not use ZYMAR®. It is not known whether ZYMAR® is excreted in human milk.

Driving and using machinery
Your sight may become blurred for a short time after using ZYMAR®. You should not drive or use machines until your sight is clear again.

Important information about some of the ingredients of ZYMAR®
Benzalkonium chloride: Special care should be taken if you have an extensive eye surface disease. Do not use ZYMAR® for a prolonged period of time and have regular eye examinations.

If you wear soft contact lenses, remove your contact lenses before using ZYMAR®, and wait at least 15 minutes after using ZYMAR® before reinserting your contact lenses. The preservative in ZYMAR®, benzalkonium chloride, may be absorbed by and cause discolouration of soft contact lenses.

Using ZYMAR® with other medicines
Always tell your healthcare professional if you are taking any other medicine. (This includes complementary or traditional medicines.)

4. HOW TO USE ZYMAR®
Do not share medicines prescribed for you with any other person.
Always use ZYMAR®exactly as your doctor has instructed you. You should check with your doctor or pharmacist if you are unsure.
The usual dose is:
Days 1 and 2: Instil one drop every two hours in the affected eye(s) while awake, up to 8 times daily.
Days 3 through 7: Instil one drop up to four times daily while awake.
If you have the impression the effect of ZYMAR®is too strong or too weak, tell your doctor or pharmacist.

Things to be careful of:
ZYMAR®solution should not be injected into the eye or any other part of the body.
Avoid contaminating the applicator tip with material from the eye, fingers or other source.
Do not wear contact lenses if you have signs and symptoms of bacterial conjunctivitis, and while using ZYMAR®.

If you use more ZYMAR® than you should
In the event of overdosage, consult your doctor or pharmacist. If neither is available,contact the nearest hospital or poison control centre.

The eye(s) should be flushed with water. If you have questions or concerns, or are not sure about something, please consult your doctor or pharmacist.

If you forget to use ZYMAR®
Use the eye drops as soon as you remember, and then go back to using them as you would normally.
If it is almost time for your next dose, ignore the dose you missed and put the drops in when you are meant to.
Do not take a double dose to make up for the dose that you missed.
If you have missed several doses, consult your doctor.
If you have trouble remembering when to use your medicine, ask your pharmacist for some hints.

5. POSSIBLE SIDE EFFECTS
ZYMAR®can have side effects.
If you experience inflamed or itchy skin, swelling or redness of the skin, or hives (urticaria) stop using ZYMAR® and contact your doctor or hospital immediately. You may be experiencing an allergic reaction to ZYMAR® which may be serious. You may need urgent medical attention.
Not all side effects reported for ZYMAR® are included in this leaflet. Should your general health worsen or if you experience any untoward effects while using ZYMAR®, please consult your doctor, pharmacist or other health care professional for advice.
You may experience the following effects:
Frequent side effects:
inflammation, bleeding or other disorders of the see-through layer covering the surface of the eye (conjunctiva)
inflammation of the surface of the eye (cornea)
red and painful eyes
watery eyes
eyelid swelling
decreased vision
eye irritation
eye discharge
dry eye
skin redness
headache
taste disturbances

Less frequent side effects:
swelling of the see-through layer which covers the surface of the eye
red and itchy skin

Side effects of unkown frequency:
inflamed eyelids
eye redness
blurred vision
itchy eyes
eye swelling
nausea
allergic reactions
severe allergic reactions (anaphylactic reactions)
swelling of the skin including the throat, mouth and face
difficulty breathing
itchy skin
rash
hives
If you notice any side effects not mentioned in this leaflet, please inform your doctor or pharmacist.

6. STORING AND DISPOSING OF ZYMAR®
Store below 25°C. STORE ALL MEDICINES OUT OF REACH OF CHILDREN. Do not use more than 30 days after opening. Discard any unused portion. Store in the original eye drop bottle. To avoid contamination of the solution, keep container tightly closed and do not touch dropper tip to any surface. Contents are sterile if seal is intact. Do not put the eye drops in the freezer. Return all unused medicines to your pharmacist. Do not dispose of unused medicines in drains or sewerage systems (e.g. toilets).

7. PRESENTATION OF ZYMAR®
ZYMAR®is supplied sterile in a white, plastic bottle with a controlled dropper tip and a beige cap in a 5 mL pack size.

8. IDENTIFICATION OF ZYMAR®
ZYMAR®is a sterile, clear, pale yellow coloured solution.

9. REGISTRATION NUMBER
A39/15.1/0367

10. NAME AND ADDRESS OF REGISTRATION HOLDER
Allergan Pharmaceuticals (Pty) Ltd
30 New Road (entrance off Bavaria Road)
Randjespark Ext. 11, Midrand, 1682
Johannesburg, Gauteng
SOUTH AFRICA
Telephone number: 011 545 6600

11. DATE OF PUBLICATION
Date of registration: 20 October 2007
Date of the most recently revised Patient Information Leaflet as approved by Council: 20 October 2007

Updated on this site: October 2017
Source: Pharmaceutical Industry

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