Eyexacin: Medicine to treat conjunctivitis

2021-07-04 05:53 PM

Eyexacin treats conjunctivitis caused by susceptible strains of bacteria: Haemophilus influenzae, Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae.

Ingredient

Per 5mL: Levofloxacin hemihydrate equivalent to levofloxacin 25mg.

Pharmacodynamic

Pharmacotherapeutic group

Antibiotic of the quinolone group (fluoroquinolone subgroup).

ATC code: S01AE05.

Pharmacology and mechanism of activation

Levofloxacin is a synthetic fluoroquinolone antibiotic with bactericidal action. It inhibits the enzymes topoisomerase II (DNA-gyrase) and/or topoisomerase IV, which are essential enzymes in bacterial DNA replication, transcription, and repair. Levofloxacin is a broad-spectrum antibiotic that is active against many strains of Gram-negative and Gram-positive bacteria.

Sensitive bacteria

Gram-negative aerobic bacteria: Enterobacter cloacae, E.coli, H. influenzae, H. parainfluenzae, Klebsiella pneumoniae, Legionella pneumophila, Moraxella catarrhalis, Proteus mirabilis, Pseudomonas aeruginosa.

Other bacteria: Chlamydia pneumoniae, Mycoplasma pneumoniae.

Gram-positive aerobic bacteria: Bacillus anthracis, Staphylococcus epidermidis, methicillin-sensitive Staphylococcus aureus (meti-S), methicillin-susceptible Staphylococcus coagulase, Streptococcus pneumoniae.

Anaerobic bacteria: Fusobacterium, Peptostreptococcus, Propionibacterium.

In vitro susceptible bacteria

Gram-positive aerobic bacteria: Enterococcus faecalis.

Anaerobic bacteria: Bacteroid fragilis, Prevotella.

Bacteria resistant to levofloxacin

Gram-positive aerobic bacteria: Enterococcus faecium, Staphylococcus aureus meti-R, Staphylococcus coagulase negative meti-R.

Cross-resistance: In vitro, there is cross-resistance between levofloxacin and other fluoroquinolones.

Pharmacokinetics

Levofloxacin plasma concentrations were measured in 15 healthy adult volunteers at different time points during 15 days of treatment with levofloxacin 0.5% eye drops: mean levofloxacin plasma concentrations after 1-hour dosing ranged from 0.86 ng/mL on day 1 to 2.05 ng/mL on day 15. The mean peak levofloxacin concentration was 2.25 ng/mL on day 4, after 2 days: use the drug every 2 hours for a total of 8 doses a day. Peak levofloxacin concentrations increased from 0.94 ng/mL on day 1 to 2.15 ng/mL on day 15, which is 1000-fold lower than reported following oral administration of standard doses.

Levofloxacin tear concentrations were measured in 30 healthy adults at different time points after instillation of one drop of levofloxacin 0.5% eye drops: mean levofloxacin tear concentrations ranged from 34.9 -221.1 mcg/mL for 60 minutes after a single dose. Mean ocular concentrations measured were approximately 17.0 mcg/mL after 4 hours of dosing and 6.6 mcg/mL after 6 hours of dosing. The clinical effects of the drug at these concentrations have not been studied.

Indications and uses

Treatment of conjunctivitis caused by susceptible strains of bacteria: Haemophilus influenzae, Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae.

Dosage and Administration

Adults and children over 1-year-old:

Days 1 and 2: Instill 1-2 drops into the infected eye, every 2 hours while awake, up to 8 times/day.

Days 3 to 7: Instill 1-2 drops in the infected eye, every 4 hours while awake, up to 4 times/day.

Note:

Do not use it more than 15 days after opening or past the expiry date. To avoid contamination or spoilage, avoid touching the cap and mouth of the bottle, or let your eyelids touch the mouth of the bottle.

Close the cap tightly after each use, do not share the vial with others.

Overdose

Do not use more than prescribed by the doctor.

In case of an overdose, the eye can be washed with warm water.

Contraindications

Patients with a history of hypersensitivity to levofloxacin, to other quinolones, or to any of the excipients. Seizures, G6PD deficiency, history of fluoroquinolone-induced tendon disease.

Use in pregnant and lactating women

Pregnancy: Do not use levofloxacin in pregnant women.

Lactation: Breastfeeding is not recommended while taking levofloxacin because of the risk of cartilage damage in young children.

Interactive

Specific drug interaction studies have not been performed specifically with levofloxacin eye drops. However, systemic absorption may occur after levofloxacin ophthalmic administration, as with other antibacterial quinolones the potential for drug interactions with theophylline, caffeine, oral anticoagulants, and cyclosporine should be considered.

Adverse Effects (ADRs)

Common: Temporarily reduced vision in one eye or both, fever, headache, dry eyes, eye pain or discomfort, pharyngitis, photophobia.

Uncommon: Allergic reactions, eyelid edema, dry eyes, itchy eyes.

Cautions

Hypersensitivity reactions with various clinical manifestations, even anaphylaxis, have been associated with the use of quinolones, including levofloxacin. The drug should be discontinued at the first signs of hypersensitivity reactions and appropriate management measures instituted.

Prolonged use may lead to the overgrowth of non-susceptible strains, including fungi. If superinfection occurs, discontinue use and institute appropriate therapy.

Patients should be advised not to wear contact lenses if there are signs and symptoms of bacterial conjunctivitis.

Effects of Drugs on Driving and Using Machines: Do not drive or operate machinery or do activities requiring alertness until the effects of levofloxacin are known.

Preservation

Store in a dry place, at a temperature not exceeding 30°C, protected from light.

Presentation and packaging

Eye drops a box of 1 5mL vial.