Ciprofloxacin Bufus

General characteristics. Structure:

Active ingredients: 3 mg of ciprofloxacin of a hydrochloride (in terms of ciprofloxacin).

Excipients: dinatrium эдетат (Trilonum of B), Mannitolum (mannitol), sodium acetate, acetic acid, a benzalkoniya chloride, water for injections.

Pharmacological properties:

Pharmacodynamics. The antimicrobic broad-spectrum agent derivative of a ftorkhinolon, suppresses bacterial DNK-girazu (the topoisomerases II and IV responsible for DNA untwisting, for ensuring further process of a transcription), breaks DNA synthesis, growth and division of bacteria.

Affects bakteritsidno gram-negative organisms during a dormant period and divisions, on gram-positive microorganisms – only during division.

Gram-negative aerobic bacteria are sensitive to ciprofloxacin: enterobakteriya (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 activators – 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 the stafilokokk steady against Methicillinum, rezistentna and to ciprofloxacin. Sensitivity of Streptococcus pneumoniae, Enterococcus faecalis, Mycobacterium avium (located intracellularly) – moderated (for their suppression high concentration are required).

To rezistentna drug: Bacteroides fragilis, Pseudomonas cepacia, Pseudomonas maltophilia, Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroides. It is inefficient concerning Treponema pallidum.

Resistance develops extremely slowly as, on the one hand, after effect of ciprofloxacin there is practically no persistent microorganism left, and with another – bacterial cells have no enzymes inactivating it.

Pharmacokinetics. Ciprofloxacin at topical administration well gets into eye tissues. After single instillation its concentration in moisture of an anterior chamber of an eye in 10 minutes makes 0,1 mg/ml. The maximum concentration defined in 1 hour in moisture of an anterior chamber makes 0,19 mg/ml.

After 2 hours concentration begins to decrease, however its antibacterial action in fabrics of a cornea remains till 6 o'clock, in moisture of an anterior chamber till 4 o'clock.

The elimination half-life at topical administration makes 4-5 hours of blood serum. Cmax in plasma – less than 5 ng/ml. Average concentration in plasma – is lower than 2,5 ng/ml.

Drug is removed through kidneys preferential (to 50%) in an invariable look and to 10% in the form of metabolites; about 15% are removed through intestines; at nursing mothers – it is partially removed with breast milk.

After instillation system absorption of drug is possible. At treatment within 7 days, on average, 4 times a day in both eyes, average concentration makes 2 ng/ml.

Indications to use:

Infectious and inflammatory diseases of eyes (acute and subacute conjunctivitis, a blepharitis, blefarokonjyunktivit, a keratitis, a keratoconjunctivitis, a bacterial helcoma, a meibomitis, an acute dacryocystitis, infectious defeats after an eye injury), before - and postoperative prevention of infectious complications in an ophthalmosurgery.

Route of administration and doses:

Locally. Drug is dug in on 1-2 cap in a conjunctival sac. Frequency of instillation depends on weight of inflammatory process.

At acute bacterial conjunctivitis, simple, scaly and ulcer blepharites, meibomites of drug appoint from 4th to 8 times a day depending on disease severity. Course of treatment from 5 to 14 days.

At a keratitis drug is appointed on 1 drop not less than 6 times a day, with positive effect the maximum course of treatment depending on weight of defeat of a cornea makes about 2-4 weeks.

At a bacterial helcoma: on 1 cap each 15 min. during 6 h, then on 1 cap each 30 min. in hours of wakefulness; for the 2nd day – on 1 cap each hour in hours of wakefulness; from 3 to 14 day – on 1 cap each 4 h in hours of wakefulness. If after 14 days of therapy epithelization did not occur, it is possible to continue treatment 1 week.

At acute dacryocystites drug is appointed by 6-12 times a day on 1 drop, the course of treatment should not exceed 14 days.

At eye injuries, including hit of foreign bodys, for prevention of infectious complications drug is appointed within 1-2 weeks on 1 drop of 4-8 times a day.

During the preoperative period: on 1 drop 4 times a day within two days before operation and on 1 drop each 10 min. 5 times just before operation.

For prevention of inflammatory diseases after surgical interventions drug is appointed by 4-6 times a day on 1 drop to all term of the postoperative period, usually from 5 days to 1 month.

Features of use:

Solution in the form of eye drops is not intended for intraocular injections.

When using other ophthalmologic medicines the interval between their introduction has to make not less than 15 min.

Right after use of drug the illegibility of visual perception is possible that it can entail difficulties at control of vehicles and during the work with mechanisms; it is recommended to get to work (driving) in 15 minutes after drug use.

During treatment drug does not recommend carrying contact lenses. After opening of a bottle it is necessary to use drug no more than 14 days.

Side effects:

Allergic reactions, itch and burning in an eye, easy morbidity and a hyperemia of a conjunctiva, nausea, it is rare – the century, a photophobia, dacryagogue, feeling of a foreign body in eyes, unpleasant smack in a mouth right after an instillation, decrease in visual acuity, emergence of white crystal precipitated calcium superphosphate in patients with a helcoma, a keratitis, a keratopathy, infiltration of a cornea, development of superinfection swelled.

Interaction with other medicines:

There are data that system use of some hinolon leads to increase in concentration of theophylline in a blood plasma, strengthens effect of indirect anticoagulants (including warfarin and its derivatives).

At combined use of ciprofloxacin and caffeine decrease in metabolism of caffeine in a liver is observed (delay of its removal and increase in concentration in blood).

It was reported about temporary increase in concentration of creatinine in blood serum at patients to whom appointed cyclosporine together with system use of ciprofloxacin.

Contraindications:

Hypersensitivity to drug components, virus and fungal infections of eyes, pregnancy, the feeding period a breast, children's age till 1 year.

Overdose:

Data on overdose of drug are absent. At accidental administration of drug inside specific symptoms are absent. Developing of nausea, vomiting, diarrhea, headache, faint, feeling of alarm is possible.

Treatment: standard measures of acute management, sufficient intake of liquid in an organism, creation of acid reaction of urine for prevention of a crystalluria.

Storage conditions:

List B. In the place protected from light at a temperature from 15 to 25 °C. Not to allow freezing. To store in the place, unavailable to children. A period of validity - 2 years. Not to apply after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Drops eye 0,3%. On 5 ml, 10 ml in bottles from a tube glass the FO type. On 5 ml, 10 ml in bottles polymeric with a screw mouth and the screwed cover with the condensing element and a nozzle doser or a nozzle doser with the condensing elements or in bottles polymeric, pressurized by droppers with the screwed covers.

On 1 ml, 1,5 ml, 2 ml, 5 ml, 10 ml in a tube dropper with the valve or a screw mouth, from polyethylene of high pressure or from polyethylene of low pressure, or from polyethylene for the medical purposes, or from polyethylene or polypropylene for infusion solutions and eye drops.

The tube dropper with a screw mouth is corked the screwed covers from polymeric materials.

Each bottle or 1, 2, 5, 10 tube droppers with the application instruction place in a pack from a cardboard. The investment in a cover dropper pack is allowed.