Ciprofloxacin-AKOS - instructions for use, dose, side effects, contraindications

Active substance: ciprofloxacin hydrochloride (in terms of ciprofloxacin) - 3 mg; Excipients: benzalkonium chloride, disodium edetate (disodium ethylenediaminetetraacetic acid, trilon B), mannitol (mannitol), sodium acetate trihydrate (sodium acetate, 3-water), acetic acid ice, water for injection - up to 1 ml.

Description:Transparent solution slightly yellowish or slightly yellowish-greenish in color.

Pharmacotherapeutic group:Antimicrobial agent, fluoroquinolone.

ATX: & nbsp

J.01.M.A.02 Ciprofloxacin

Pharmacodynamics:

A broad-spectrum antimicrobial agent from the group of fluoroquinolones (a subgroup of monofluoroquinolones) for topical application in ophthalmology. Suppresses bacterial DNA-gyrase (topoisomerases II and IV, responsible for the process of supercoiling the chromosomal DNA around the nuclear RNA, which is necessary for reading the genetic information), violates DNA synthesis, growth and division of bacteria; causes pronounced morphological changes (incl.cell wall and membranes) and rapid death of a bacterial cell.

It acts bactericidal on gram-negative organisms during rest and division (because it affects not only the DNA-gyrase, but also causes lysis of the cell wall), gram-positive microorganisms - only during the fission period. Increases the permeability of the bacterial cell membrane. Low toxicity for macroorganism cells is explained by the absence of DNA-gyrase in them. Against the background of taking ciprofloxacin, there is no parallel development of resistance to other antibiotics that do not belong to the group of inhibitors of gyrase, which makes it highly effective against bacteria that are resistant to aminoglycosides, penicillins, cephalosporins, tetracyclines and many other antibiotics.

Ciprofloxacin is sensitive to: Gram-negative aerobic bacteria: enterobacteria (Escherichia coli, Salmonella spp., Shigella spp., Citrobacter spp., Klebsiella spp., Enterobacter spp., Proteus mirabilis, Proteus vulgaris, Serratia marcescens, Hafnia alvei, Edwardsiella tarda, Providencia spp. , Morganella morganii, Vibrio spp., Yersinia spp.), Other gram-negative bacteria (Haemophilus spp., Pseudomonas aeruginosa, Moraxella catarrhalis, Aeromonas spp., Pasteurella multocida, Plesiomonas shigelloides, Campylobacter jejuni, Neisseria spp.), Some intracellular pathogens - Legionella pneumophila, Brucella spp., Chlamydia trachomatis, Listeria monocytogenes, Mycobacterium tuberculosis, Mycobacterium kansasii, Corynebacterium diphtheriae; Gram-positive aerobic bacteria: Staphylococcus spp. (Staphylococcus aureus, Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus saprophyticus), Streptococcus spp. (Streptococcus pyogenes, Streptococcus agalactiae).

The majority of staphylococci, resistant to methicillin, are resistant to ciprofloxacin. Sensitivity of Streptococcus pneumoniae, Enterococcus faecalis, Mycobacterium avium (located intracellularly) - moderate (high concentrations are required to repress).

The drug is resistant (resistant): Bacteroides fragilis, Pseudomonas cepacia, Pseudomonas maltophilia, Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroides.

Ineffective against Treponema pallidum.

Resistance to ciprofloxacin develops extremely slowly, because, on the one hand, after the action of ciprofloxacin, there is almost no persistent microorganism, and on the other - bacterial cells do not have enzymes that inactivate it.

The drug is low toxicity.

Pharmacokinetics:

With topical application ciprofloxacin well penetrates the tissues of the eye. Penetrates into the cornea and into the anterior chamber of the eye, especially when the epithelial cover of the cornea is disturbed. When the cornea is affected, the concentration of ciprofloxacin in it is effective against most pathogens of corneal infections.

After a single instillation, the concentration of ciprofloxacin in the moisture of the anterior chamber of the eye is reached after 10 minutes and is 100 μg / ml. Maximum Concentration C_max in the moisture of the anterior chamber after 1 h is 190 μg / ml.After 2 hours the concentration of the drug begins to decrease, while its antibacterial action in the tissues of the cornea is kept up to 6 hours, in the moisture of the anterior chamber - up to 4 hours.

After instillation, systemic absorption of the drug is possible. With topical application of eye drops of ciprofloxacin 4 times / day in both eyes for 7 days, the average concentration of ciprofloxacin in blood plasma is less than 2-2.5 ng / ml, the maximum concentration is less than 5 ng / ml.

With the local application of T_1/2from plasma is 4-5 hours. The drug is excreted by the kidneys in unchanged form - up to 50%, and in the form of metabolites - up to 10%; through the intestine - about 15%. Some part of the drug is excreted in breast milk.

Indications:

Infectious-inflammatory diseases of the eyes caused by microorganisms sensitive to the preparation:

acute and subacute conjunctivitis;
blepharitis, blepharoconjunctivitis;
keratitis, keratoconjunctivitis;
anterior uveitis;
bacterial corneal ulcer;
dacryocystitis;
meibomite (barley);
trachoma;
infectious lesions of the eyes after injuries or foreign bodies.

Preventive maintenance and treatment of infectious complications at traumas of an eye and its appendages (incl.after removal of the foreign body from the cornea, conjunctiva, after exposure to chemical or physical agents) and in operations on the eyeball (pre- and postoperative infection prevention in ophthalmic surgery).

Contraindications:

Hypersensitivity to ciprofloxacin or other fluoroquinolone group drugs, children under 1 year of age, pregnancy, lactation (breastfeeding).

Pregnancy and lactation:

Contraindicated.

Dosing and Administration:

Locally, 1-2 drops in the conjunctival sac of the affected eye. The frequency of instillations depends on the severity of the inflammatory process.

With mild and moderately severe infection, 1-2 drops are injected into the conjunctival sac of the affected eye (or both eyes) every 4 hours, with severe infection - 2 drops every hour. After the condition is improved, the dose and frequency of instillations are reduced.

With acute bacterial conjunctivitis, simple, scaly and ulcerative blepharitis - 4-8 times / day, depending on the severity of the inflammatory process, the course of treatment - from 5 to 14 days. In keratitis - 1 drop at least 6 times / day.

If there is a positive effect, the duration of therapy depends on the severity of the corneal lesion and is usually 2-4 weeks.

When a corneal lesion is caused by Pseudomonas aeruginosa, - 1 drop at least 8-12 times / day.The duration of therapy depends on the course of the disease and is usually about 2-3 weeks.

With anterior uveitis, the drug is prescribed 1 drop 8-12 times a day. With acute dacryocystitis and canaliculitis - 1 drop 6-12 times / day, with chronic - 4-8 times / day.

With a bacterial ulcer of the cornea: on the first day - every 15 minutes for 6 hours, then 1 drop every 30 minutes during waking hours; the second day - 1 drop every hour during waking hours; from 3 to 14 days - 1 drop every 4 hours during waking hours. If after 14 days of therapy epithelization has not occurred, then the treatment can be continued.

For the prevention of secondary infection in case of trauma to the eye and its appendages - 1 drop 4-8 times / day for 1-2 weeks. For the prevention of inflammatory diseases after surgery with perforation of the eyeball - 1 drop 4-6 times / day during the entire postoperative period (usually from 5 days to 1 month).

Side effects:

Allergic reactions, itching, burning, mild tenderness and congestion hyperemia, nausea, rarely - eyelid edema, photophobia, lacrimation, sensation of foreign body in the eyes, unpleasant aftertaste in the mouth, drop in visual acuity,appearance of white crystalline precipitate in patients with corneal ulcer, keratitis, keratopathy, appearance of spots or infiltration of the cornea, development of superinfection.

Overdose:Data on drug overdose are absent.

Interaction:

Pharmaceutical interaction: the ciprofloxacin solution is incompatible with drug solutions having pH values of 3-4 that are physically or chemically unstable.

When combined with other antimicrobial agents, synergic interaction is usually observed (beta-lactam antibiotics, aminoglycosides, clindamycin, metronidazole).

Special instructions:

Solution in the form of eye drops is not intended for intraocular injection!

The drug can not be administered subconjunctivally or directly into the anterior chamber of the eye!

When using other ophthalmic drugs, the interval between their administration should be at least 5 minutes.

If after the application of drops for a long time continues or increases conjunctival hyperemia, then stop using the drug and see a doctor.

During the treatment with the drug, it is not recommended to wear soft contact lenses.When using hard lenses, remove them before instillation and re-put them 15-20 minutes after the instillation of the drug.

Effect on the ability to drive transp. cf. and fur:

Patients who temporarily lose visual clarity after application are not advised to drive or work with complicated equipment, machines or any other complex equipment that requires clear vision immediately after instillation of the drug.

Form release / dosage:

Eye drops 0,3%.

Packaging:

5 ml in bottles for eye drops with a nozzle-dispenser and a cap screwed from plastic.

5 ml in bottles - droppers polymer with a cap screwed and a stopper - a dropper.

Each vial with instructions for use is placed in a pack of cardboard.

Storage conditions:

Store in a dark place at a temperature of 15 to 25 ° C. Freezing is not allowed. Keep out of the reach of children.

Shelf life:

2 years. After opening the vial, the shelf life of the drug is 1 month.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N001587 / 02

Date of registration:05.11.2008

The owner of the registration certificate:SYNTHESIS, OJSC SYNTHESIS, OJSC Russia

Manufacturer: & nbsp

SYNTHESIS, OJSC Russia

Information update date: & nbsp19.10.2015

Illustrated instructions

Instructions

Ciprofloxacin-AKOS (Ciprofloxacin-AKOS)