Project Description

Ciprofloxacin, solution 0,3 % eye drops

Solutio Сiprofloxacini 0,3 % (guttae ophthalmicae)

international nonproprietary name

Ciprofloxacin – Ciprofloxacin

Ref

BP-0027

Pharmacotherapeutic group

Synthetic antibacterial agents. Fluoroquinolones.

Composition of the preparation

Active substance– ciprofloxacin hydrochloride in recalculation on ciprofloxacin – 3,0 g.

Additives– Mannitol, benzalconium chloride, sodium acetic,salt of disodium ethylenediamine -N, N, N ‘, N ‘ – tetraacetic acid dihydrous, acetic acid, water for injections – to 1 l.

Pharmacological action

Pharmacodynamics

The antimicrobial preparation, derivative of fluoroquinolone. Acts as bactericid. Inhibits bacterial DNA-gyrase. Inhibits DNA synthesis, growth and division of bacteria, causes the expressed morphological changes of cell wall, membranes and rapid destruction of bacterial cell. Acts on gram-negative microorganisms in rest and division periods (due to influence on DNA-gyrase and ability to cause cell walllysis). Influences on gram-positive microorganisms only during division.

Low hypotoxicity for macroorganism cells is explained by absence DNA-gyrase in them. On a background of ciprofloxacin intake there is no parallel development of resistance to other antibiotics which are not belonging to group of gyrase inhibitors (including to aminoglycosides, penicillins, cephalosporins, tetracyclines).

Ciprofloxacin is active in relation to gram-negative aerobic bacteria – 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., Haemophilus spp., Pseudomonas aeruginosa, Moraxella catarrhalis, Aeromonas spp., Pasteurella multocida, Plesiomonas shigelloides, Campylobacter jejuni, Neisseria spp.; gram-positive aerobic bacteria – Staphylococcus spp. (Staphylococcus aureus, Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus saprophyticus), Streptococcus pyogenes, Streptococcus agalactiae. The preparation is also active in relation to some intracellular pathogens – Legionella pneumophila, Brucella spp., Chlamydia trachomatis, Listeria monocytogenes, Mycobacterium tuberculosis, Mycobacterium kansasii, Corynebacterium diphtheriae. Streptococcus pneumoniae, Enterococcus faecalis, Mycoplasma hominis, Gardnerella spp., Mycobacterium avium-intracellulare are moderately sensitive to the preparation (for their suppression high concentration are required). Bacteroides fragilis, Pseudomonas cepacia, Pseudomonas maltophilia, Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroides are steady in relation to the preparation. The preparation is inactive in relation to Trеponema pallidum. The majority of staphilococcuses, steady against Methicillin, are resistant  to ciprofloxacin too. The resistance is developed slowly.

Pharmakokinetics

At use of eye drops in recommended doses the maximal concentration of the preparation in blood plasma is less than 5 ng/ml, and average concentration is less than 2,5 ng/ml.

Now it is not established, whether ciprofloxacin passes into breast milk at instillation in eye, however it is known, that at single preparation per oral intake in a dose of 500 mg it is found in breast milk.

Indications 

Infectious-inflammatory eyes diseases (acute and subacute conjunctivitis, blepharitis, blepharoconjunctivitis, keratitis, keratoconjunctivitis, bacterial corneaulcer, chronic dacryocystitis, meibomitis); infectious lesions of eyes after traumas or foreign bodies penetration; pre- and postoperative prophylaxis of infectious complications in ophthalmosurgery.

special indication

The preparation can be applied only locally; it cannot be introduced subconjunctivally or directly in the front chamber of eye.

It is not recommended to use soft contact lenses during treatment by the preparation. At use of rigid contact lenses it is necessary to take off them before instillation and again put them in 15 – 20 minutes after the preparation instillation.

It is necessary to close a vial after each use. It is not necessary to touch an eye with the end of a pipette.

Influence on ability to control machines and potentially dangerous mechanisms:it is not recommended to drive a car or to work with the complex equipment directly after preparationinstillation in patientswhose sharpness of vision is temporarily lost after application of ciprofloxacin in the form of eye drops.

special warning

Not established

Dosage and method of administration

At mild and moderate infection instill per 1 – 2 drops of the preparation in conjunctival bag of the affected eye (or both eyes) every 4 h, at serious infection – per 2 drops each hour. After condition improvement a dose and frequency of instillation is decreased.

At bacterial corneal ulcer instill per 1 drop of the preparation each 15 minutes during 6 h, then per 1 drop each 30 minutes at wakefulness in the 1st  day; in 2nd day per 1 drop each hour of wakefulness; from 3rd  to 14th  day per 1 drop every 4 h at wakefulness. If after 14 days of therapy the epithelization has not occurred, the treatment can be continued.

overdosage

There is no data on the preparation overdosage.

safety measures

The preparation should be administrated with care to patients with atherosclerosis of brain vessels, cerebral circulationabnormalities, convulsion syndrome.

The patient should be informed that if after application of drops conjunctival hyperemia continues for a long time or increases, it is necessary to withdrawn the preparation and to consult with a  doctor.

Side effects

Application of the preparation can be accompanied by local by-effects (allergic reactions, itch, burning, mild painfulness and hyperemia of conjunctiva, nausea; seldom – eyelid edema, photophobia, foreign body sensation in eyes, unpleasant taste in a mouth right after instillation, decrease of visual acuity, appearance of white crystalline precipitate in patients with corneal ulcer, keratitis, keratopathy, occurrence of maculae or cornea infiltration).

Contraindications

Hypersensitivity to ciprofloxacin or to other preparations of fluoroquinolones group, deficiency of glucose 6-phosphate dehydrogenase, age under 18 years, pregnancy, lactation (for the period of treatment breast feeding should be stopped).

Interactions with other medicinal preparations

Activity increases at combination with beta-lactam antibiotics, aminoglycosides, vancomycin, clindamycin, metronidazol.

The form of release

0,3 % sterile solution of ciprofloxacin (eye drops) in 5 ml vials.