Ciprofloxacin optic drops 0.3%, 5ml

Treatment of corneal ulcers and infections of the anterior segment of the eyeball and its appendages caused by bacteria sensitive to ciprofloxacin in adults, newborns (from 0 to 27 days), infants and babies (from 28 to 23 months), children (from 2 to 11 years) and adolescents (12 to 18 years old).

Ciprofloxacin is used topically. Do not inject the drug subconjunctivally or into the anterior chamber of the eye. In case of corneal ulcers, the drug must be instilled, observing the following intervals between instillations (including at night): on the first day - 2 drops every 15 minutes for the first 6 hours, then 2 drops every 30 minutes for the rest of the day.

On the second day of therapy - 2 drops every hour.

From the third to the 14th day of therapy - 2 drops every 4 hours.

If it is necessary to continue therapy for more than 14 days, the selection of the dosage regimen should be carried out by the attending physician.

In case of diseases of the anterior segment of the eyeball, the drug must be instilled according to the following scheme: 1 or 2 drops per

affected eye (s) 4 times a day.

In severe infections, the dosing regimen for the first 2 days may include instillation of the drug 1 or 2 drops every 2 hours in

period of wakefulness. The duration of drug therapy according to the stated indications should not exceed 21 days.

Use in the pediatric population

The dosage regimen for therapy in children over the age of 1 year corresponds to that in adults. The efficacy and safety of the use of ciprofloxacin in children aged 0 to 12 years has been confirmed in clinical studies involving 230 children. There was no development of serious adverse events in this group of patients.

Application for renal and hepatic insufficiency

There is no information on the use of ciprofloxacin in patients with concomitant liver and kidney diseases.

When using the drug to reduce the risk of developing systemic adverse reactions, it is recommended to lightly press with a finger on the area of ??the inner corner of the eye in the projection of the lacrimal sac within 1-2 minutes after instillation of the drug.

Composition for 1 ml.

Active ingredient: ciprofloxacin hydrochloride - 3.49 mg in terms of ciprofloxacin - 3.0 mg

Excipients: disodium edetate dihydrate (Trilon B) - 0.4 mg sodium chloride - 9.0 mg benzalkonium chloride - 0.2 mg sodium hydroxide solution 1 M - up to pH 3.5-5.5 purified water - up to 1, 0 ml

Hypersensitivity to the active substance and any of the excipients. Hypersensitivity to quinolones.

Pharmacological properties

Pharmacodynamics

A broad-spectrum antimicrobial agent, a fluoroquinolone derivative, inhibits bacterial DNA gyrase (topoisomerases II and IV, which are responsible for the supercoiling of chromosomal DNA around nuclear RNA, which is necessary for reading genetic information); disrupts DNA synthesis, growth and division of bacteria; causes pronounced morphological changes (including cell walls and membranes) and rapid death of the bacterial cell.

Acts bactericidal on gram-negative organisms during dormancy and division (since it affects not only DNA gyrase, but also causes lysis of the cell wall), on gram-positive microorganisms - only during the period of division.

Low toxicity for cells of a macroorganism is explained by the absence of DNA gyrase in them. While taking ciprofloxacin, there is no parallel development of resistance to other antibiotics that do not belong to the group of gyrase inhibitors, which makes it highly effective against bacteria that are resistant, for example, to aminoglycosides, penicillins, cephalosporins, tetracyclines and many other antibiotics.

Gram-negative aerobic bacteria are sensitive to ciprofloxacin:

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., Morganii , Yersinia spp.), Other gram-negative bacteria (Haemophilus spp., Pseudomonas aeruginosa, Moraxella catarrhalis, Aeromonas spp., Pasteurella multocida, Plesiomonas shigeoides, Campylobacter jejuni, Neisseria spp.); some intracellular pathogens (Legionella pneumophila, Brucella spp., Chlamydia trachomatis, Listeria monocytogenes, Mycobacterium tuberculosis, Mycobacterium kansasii, Corynebacterium diphtheria); gram-positive aerobic bacteria: Staphylococcus spp. (Staphylococcus aureus, Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus saprophyticus),Streptococcus spp. (Streptococcus pyogenes, Streptococcus agalactiae). Most methicillin-resistant staphylococci are also resistant to ciprofloxacin. The sensitivity of Streptococcus pneumoniae, Enterococcus faecalis, Mycobacterium avium (located intracellularly) is moderate (high concentrations are required to suppress them). Resistant to the drug: Bacteroides fragilis, Pseudomonas cepacia, Pseudomonas maltophilia, Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroides. Ineffective against Treponema pallidum. Resistance develops extremely slowly, because, on the one hand, after the action of ciprofloxacin, there are practically no persistent microorganisms, and on the other hand, bacterial cells do not have enzymes that inactivate it.Most methicillin-resistant staphylococci are also resistant to ciprofloxacin. The sensitivity of Streptococcus pneumoniae, Enterococcus faecalis, Mycobacterium avium (located intracellularly) is moderate (high concentrations are required to suppress them). Resistant to the drug: Bacteroides fragilis, Pseudomonas cepacia, Pseudomonas maltophilia, Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroides. Ineffective against Treponema pallidum. Resistance develops extremely slowly, because, on the one hand, after the action of ciprofloxacin, there are practically no persistent microorganisms, and on the other hand, bacterial cells do not have enzymes that inactivate it.Most methicillin-resistant staphylococci are also resistant to ciprofloxacin. The sensitivity of Streptococcus pneumoniae, Enterococcus faecalis, Mycobacterium avium (located intracellularly) is moderate (high concentrations are required to suppress them). Resistant to the drug: Bacteroides fragilis, Pseudomonas cepacia, Pseudomonas maltophilia, Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroides. Ineffective against Treponema pallidum. Resistance develops extremely slowly, since, on the one hand, after the action of ciprofloxacin, there are practically no persistent microorganisms, and on the other hand, bacterial cells do not have enzymes that inactivate it.Mycobacterium avium (located intracellularly) is moderate (high concentrations are required to suppress them). Resistant to the drug: Bacteroides fragilis, Pseudomonas cepacia, Pseudomonas maltophilia, Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroides. Ineffective against Treponema pallidum. Resistance develops extremely slowly, because, on the one hand, after the action of ciprofloxacin, there are practically no persistent microorganisms, and on the other hand, bacterial cells do not have enzymes that inactivate it.Mycobacterium avium (located intracellularly) is moderate (high concentrations are required to suppress them). Resistant to the drug: Bacteroides fragilis, Pseudomonas cepacia, Pseudomonas maltophilia, Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroides. Ineffective against Treponema pallidum. Resistance develops extremely slowly, because, on the one hand, after the action of ciprofloxacin, there are practically no persistent microorganisms, and on the other hand, bacterial cells do not have enzymes that inactivate it.Resistance develops extremely slowly, because, on the one hand, after the action of ciprofloxacin, there are practically no persistent microorganisms, and on the other hand, bacterial cells do not have enzymes that inactivate it.Resistance develops extremely slowly, because, on the one hand, after the action of ciprofloxacin, there are practically no persistent microorganisms, and on the other hand, bacterial cells do not have enzymes that inactivate it.

Mechanisms of development of resistance

The development of resistance to fluoroquinolones, in particular to ciprofloxacin, is mediated by changes in genes encoding at least one of 4 mechanisms:

1. changes in the structure of target enzymes (DNA gyrase and topoisomerase IV) - enzymes involved in the synthesis of cell DNA;

2. violation of the permeability of the cell wall;

3. active elimination of the drug from the cell (increased activity of efflux pumps);

4. Plasmid-mediated changes in the work of aminoglycoside 6-N-acetyltransferase.

Pharmacokinetics

Absorption

When applied topically, it is rapidly absorbed.

Distribution

The concentration of ciprofloxacin in blood plasma after instillation into the conjunctiva of 2 drops of 0.3% solution every 2 hours for 2 days, and then every 4 hours for 5 days ranged from non-quantifiable (& lt; 1.0 ng / ml) to 4.7 ng / ml.

The average maximum plasma concentration of ciprofloxacin obtained in this study is approximately 450 times less than after oral administration of ciprofloxacin at a dose of 250 mg.

Ciprofloxacin is widely distributed in body tissues, approximately the volume of distribution is from 1.7 to 5 l / kg. The connection with blood plasma proteins is 20-40%.

Metabolism

There is no information on the pathways of metabolism of ciprofloxacin.

Withdrawal

The plasma half-life is 3-5 hours. Ciprofloxacin and four of its metabolites are excreted in urine and feces. About 2/3 of the total level of ciprofloxacin in plasma is eliminated through the kidneys, while 1/3 of the total level of ciprofloxacin is excreted through the intestine and in the bile. In patients with impaired renal function, there is a slight increase in the half-life of ciprofloxacin due to extrarenal elimination pathways. Likewise, with violations of the liver, the half-life is slightly lengthened.

There is no information on the study of the pharmacokinetic properties of ciprofloxacin when used in children.

Application during pregnancy and during breastfeeding

Fertility

When conducting studies of oral dosage forms of ciprofloxacin in animals, no negative effects on fertility were found. Studies assessing the effect of ciprofloxacin in the form of instillations on human fertility have not been conducted.

Pregnancy

There are no data on the use of ciprofloxacin in the dosage form of eye drops in pregnant women. In animal studies, no results have been obtained indicating a negative effect of ciprofloxacin on reproductive function. The systemic levels of ciprofloxacin are expected to be low when administered in an eye drop dosage form.

Given the lack of data on the safety of use during pregnancy, it is recommended to prescribe ciprofloxacin during pregnancy only in cases where the intended benefit from the use of the drug by the mother outweighs the possible risk to the fetus.

Breastfeeding period

With oral administration of ciprofloxacin by women during breastfeeding, it is excreted into breast milk. It is not known whether ciprofloxacin is excreted in breast milk when it is used as an instillation, but the risk to a breastfed baby cannot be excluded in this case. Caution should be exercised when using the drug in women during breastfeeding.

Application for renal and hepatic insufficiency

There is no information on the use of ciprofloxacin in patients with concomitant liver and kidney diseases.

When using the drug to reduce the risk of developing systemic adverse reactions, it is recommended to lightly press with a finger on the area of ??the inner corner of the eye in the projection of the lacrimal sac within 1-2 minutes after instillation of the drug.

Overdose

In the event of an overdose with local application in the form of instillations, it is necessary to rinse the conjunctival cavity with warm water. It is not expected that toxic effects will develop in case of local overdose, or if the contents of the vial are accidentally swallowed.

Interaction with other medicinal products

Special studies of interaction with the use of ophthalmic dosage forms of ciprofloxacin have not been conducted. Taking into account the low systemic concentration of ciprofloxacin in plasma after instillation into the conjunctival cavity, the interaction between drugs used together with ciprofloxacin is unlikely. In the case of joint use with other local ophthalmic drugs, the interval between their use should be at least 5 minutes, while eye ointments should be applied last.

Ciprofloxacin-Optic solution is incompatible with solutions of drugs with pH 3-4, which are physically or chemically unstable.

special instructions

The solution in the form of eye drops is not intended for intraocular injection. When using other ophthalmic drugs, the interval between their administration should be at least 5 minutes. The drug should be discontinued if any signs of hypersensitivity appear. The patient should be informed that if, after using the drops, conjunctival hyperemia continues or increases for a long time, then you should stop using the drug and consult a doctor. During the period of drug treatment, wearing soft contact lenses is not recommended. When using hard contact lenses, remove them before instillation and put them back on 15-20 minutes after instillation of the drug.

Influence on the ability to drive vehicles, mechanisms

After using eye drops, a decrease in the clarity of visual perception is possible, therefore, immediately after instillation, it is not recommended to drive a car and engage in activities that require increased attention and speed of psychomotor reactions.