Zimar^® (Drops) Instructions for Use

Marketing Authorization Holder

Allergan, Inc. (USA)

Manufactured By

Allergan Sales, LLC (USA)

ATC Code

S01AE06 (Gatifloxacin)

Active Substance

Gatifloxacin (Rec.INN registered by WHO)

Dosage Form

Zimar®

Eye drops 0.3%: 5 ml dropper bottle

Dosage Form, Packaging, and Composition

5 ml – dropper bottles (1) – cardboard packs.

Clinical-Pharmacological Group

Antibacterial drug of the fluoroquinolone group for topical use in ophthalmology

Pharmacotherapeutic Group

Antimicrobial agent – fluoroquinolone

Pharmacological Action

Gatifloxacin is an 8-methoxy fluoroquinolone with a 3-methylpiperazinyl substitution at the C7 position.

The antibacterial action of gatifloxacin is due to the inhibition of DNA gyrase and topoisomerase IV. DNA gyrase is an enzyme involved in the replication, transcription, and repair of bacterial DNA. Topoisomerase IV is an enzyme that plays a key role in the separation of chromosomal DNA during bacterial cell division.

The mechanism of action of fluoroquinolones, including Gatifloxacin, differs from the mechanism of action of antibacterial drugs of the aminoglycoside, macrolide, and tetracycline groups; therefore, Gatifloxacin may be active against pathogenic bacteria that are resistant to the antibiotics listed above, and they, in turn, may be active against pathogenic bacteria resistant to gatifloxacin. Cross-resistance between gatifloxacin and the antibiotics listed above has not been established.

In vitro studies have demonstrated that resistance to gatifloxacin develops as a result of multi-step mutations and occurs at a frequency of 1×10⁷-1×10¹⁰.

Gatifloxacin is active against most of the bacterial strains listed below, both in vitro and in clinical use.

Aerobic Gram-positive bacteria: Corynebacterium propinquum, Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus mitis, Streptococcus pneumoniae.

Aerobic Gram-negative bacteria: Haemophilus influenzae.

Pharmacokinetics

After instillation of 0.3% gatifloxacin eye drops, the plasma concentrations of gatifloxacin remain below the analytical detection threshold (5 ng/ml).

Indications

• Treatment of bacterial conjunctivitis caused by pathogens susceptible to the drug.

ICD codes

Dosage Regimen

Administer topically into the conjunctival sac. Use only during waking hours.

On Days 1 and 2, instill one drop into the affected eye(s)every 2 hours, up to a maximum of 8 times per day.

From Day 3 through Day 7, reduce the frequency. Instill one drop into the affected eye(s) up to 4 times daily.

Complete the full course of therapy, even if symptoms improve. Do not use for more than 7 days without re-evaluation.

Avoid contaminating the dropper tip. Do not let it contact the eye, fingers, or any other surface.

If you use other topical ophthalmic products, administer them at least 5 minutes apart. Apply ointments after drops.

Do not wear contact lenses during treatment for bacterial conjunctivitis.

After instillation, apply gentle pressure to the lacrimal sac (at the inner corner of the eye) for 1-2 minutes. This reduces systemic absorption.

Discard the bottle 28 days after first opening. Do not use the solution if it becomes discolored or cloudy.

Adverse Reactions

When using the drug, the following adverse reactions may develop with the indicated frequency of occurrence – very common (>10%), common (>1%, <10%), uncommon (>0.1%, <1%); rare (>0.01%, <0.1%), very rare (<0.01%).

Eye disorders

Common: conjunctival irritation, increased lacrimation, keratitis, papillary conjunctivitis, chemosis, conjunctival hemorrhage, dryness of the eye mucosa (dry eye syndrome), eye discharge, eye irritation, eye pain, eyelid edema, eye redness, decreased visual acuity.

Nervous system disorders

Common: headache

Metabolism and nutrition disorders

Common: taste perversion

During the post-marketing period, reports of the following adverse reactions for Zimar^® have been received (frequency unknown).

Eye disorders: blepharitis, eye and conjunctival hyperemia, blurred vision, eye pruritus, eye edema (including corneal and conjunctival edema), eye irritation, eye pain. Gastrointestinal disorders: nausea.

Immune system disorders: hypersensitivity, anaphylactic reactions and angioedema (including laryngeal, oral and facial edema).

Respiratory, thoracic and mediastinal disorders: dyspnea.

Skin and subcutaneous tissue disorders: pruritus (including generalized pruritus), rash, urticaria.

Contraindications

• Hypersensitivity to gatifloxacin, other quinolones, or any other component of the drug;
• Children under 1 year of age.

With caution

• In patients receiving systemic quinolone drugs, including Gatifloxacin. Serious, and in some cases fatal, hypersensitivity reactions (anaphylactic reactions) have been observed in this category of patients, in some cases after the first dose of the drug. Some reactions were accompanied by cardiovascular failure, loss of consciousness, angioedema (including edema of the larynx, pharynx, or face), airway obstruction, dyspnea, itching, and urticaria;
• Pregnancy and breastfeeding period;
• In patients with a history of allergic reactions to other topical preparations containing Gatifloxacin. There are extremely rare reports of Stevens-Johnson syndrome development after topical application of gatifloxacin. At the first signs of allergic reactions, the drug should be discontinued immediately.

Use in Pregnancy and Lactation

Due to the lack of adequate and strictly controlled studies in pregnant women, Zimar^® should be used with caution during pregnancy, and only if the expected benefit to the mother outweighs the potential risk to the fetus. It has been confirmed that with topical application of gatifloxacin in the form of eye drops, its systemic plasma concentration is low, so no effect on breastfed infants is anticipated.

Nevertheless, when prescribing Zimar^® during lactation, breastfeeding should be discontinued for the duration of treatment because the excretion of the drug into breast milk with topical application has not been studied.

Pediatric Use

Contraindicated in children under 1 year of age.

Special Precautions

Prolonged use (more than 28 days) of Zimar^®, as well as other antibacterial drugs, may lead to the growth of microorganisms non-susceptible to it, as well as fungi. If superinfection occurs, the drug should be discontinued and alternative therapy instituted.

It is not recommended to wear contact lenses during treatment with Zimar^®. Zimar^® is not intended for injection, including subconjunctival injections, and should not be injected into the anterior chamber of the eye. Avoid contact of the dropper bottle tip with the eye mucosa, hand skin, and any surfaces.

The shelf life of the drug after first opening the dropper bottle is 28 days.

Effect on ability to drive vehicles and operate machinery

Instillation of the drug may cause temporary blurred vision, therefore it is necessary to refrain from driving vehicles and engaging in activities requiring increased concentration and speed of psychomotor reactions until vision is restored.

Overdose

There is a theoretical possibility of Zimar^® overdose when instilled into the eyes. In this case, excess drug can be removed from the eye/eyes by rinsing with warm running water.

Drug Interactions

Studies on the interaction of Zimar^® have not been conducted. Due to the low plasma concentration of gatifloxacin (< 5 ng/ml) after topical application, systemic drug interactions are unlikely.

Storage Conditions

At a temperature not exceeding 25°C (77°F). Keep out of reach of children.

Shelf Life

Shelf life – 2 years.

Dispensing Status

By prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.