Ophtocypro eye ointment 0.3%, 3 g

• Infectious and inflammatory diseases of the eyes caused by sensitive microorganisms (acute and subacute conjunctivitis, blepharitis, blepharoconjunctivitis, keratitis, keratoconjunctivitis, bacterial corneal ulcer, chronic dacryocystitis, meibomitis, infectious lesions of the eyes after trauma or injury);

• pre- and postoperative prevention of infectious complications in ophthalmic surgery.

Into the conjunctival sac.

Adults and children over 2 years old. A strip of ointment 1Ц1.5 cm long is placed behind the lower eyelid of the affected eye 3 times a day for 2 days. Then, within 5 days, the drug is used 2 times a day. In the case of the development of a severe infectious process, the ointment is applied every 3-4 hours, as the inflammation decreases, the frequency of the drug is reduced. The course of treatment should not exceed 14 days. To apply the ointment, gently pull the lower eyelid down and, lightly pressing the tube, insert a strip of ointment into the conjunctival sac. Then slowly release the eyelid and press it with a cotton swab or cotton swab for 1-2 minutes. After that, you should close your eyes for 1-2 minutes.

Eye ointment

100 g

active substance: ciprofloxacin hydrochloride (in terms of ciprofloxacin) 0.3 g

excipients: nipagin (methyl parahydroxybenzoate); medical petroleum jelly; lanolin anhydrous

• Hypersensitivity;

• pregnancy;

• lactation period;

• children's age (up to 2 years);

• viral and fungal eye infections.

With caution: in patients with cerebral atherosclerosis, cerebrovascular accident, convulsive syndrome.

pharmachologic effect

A broad-spectrum antimicrobial agent, a fluoroquinolone derivative.

Suppresses bacterial DNA gyrase (topoisomerases II and IV, responsible for the process of 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 the cell wall and membranes) and rapid death of the bacterial cell.

It has a bactericidal effect on gram-negative organisms during dormancy and division (because 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 alwards. , Morganella morganii, Vibrio spp., Yersinia spp.), Other gram-negative bacteria (Haemophilus spp., Pseudomonas aeruginosa, Moraxella catarrhalis, Aeromonas spp., Pasteurella multocida, Plesiomonas shigelloides, Campylobacter, jejunella spp.) 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).

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.

Pharmacokinetics

When applied topically, it is rapidly absorbed. 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 values ??that cannot be quantified (<1.0 ng / ml) to 4.7 ng / ml. The average Cmax of ciprofloxacin in blood plasma obtained in this study is approximately 450 times less than after oral administration of ciprofloxacin at a dose of 250 mg. Plasma protein binding of ciprofloxacin is 20-30%; the active substance is present in blood plasma mainly in a non-ionized form. Ciprofloxacin is freely distributed in tissues and body fluids. Vd in the body is 2-3 l / kg. The concentration of ciprofloxacin in the tissues is significantly higher than the concentration in the blood serum. It is metabolized in the liver.Four metabolites of ciprofloxacin can be found in the blood in small concentrations: diethylcyprofloxacin (Ml), sulfocyprofloxacin (M2), oxocyprofloxacin (M3), formylcyprofloxacin (M4), three of which (Ml-M3) exhibit antibacterial activity in vitro, comparable to antibacterial activity acid. The in vitro antibacterial activity of the M4 metabolite, present in a smaller amount, is more consistent with the activity of norfloxacin. Ciprofloxacin is excreted mainly by the kidneys by glomerular filtration and tubular secretion; a small amount - through the digestive tract. Renal clearance is 0.18-0.3 l / h / kg, total clearance is 0.48-0.60 l / h / kg. Approximately 1% of the administered dose is excreted in the bile. In bile, ciprofloxacin is present in high concentrations.In patients with unchanged renal function, T1 / 2 is usually 3-5 hours. With impaired renal function, T1 / 2 increases.

Side effect

From the immune system: hypersensitivity reactions.

From the nervous system: infrequently - headache; rarely - dizziness.

From the side of the organ of vision: often - precipitates on the cornea, discomfort in the eye, conjunctival injection; infrequently - keratopathy, punctate keratitis, corneal infiltrates, photophobia, decreased visual acuity, eyelid edema, blurred vision, eye pain, dry eye sensation, conjunctival and eyelid edema, lacrimation, discharge from the eyes, crusting at the edges of the eyelids, peeling of the skin eyelid, hyperemia of the eyelids; rarely - toxic phenomena from the organ of vision, keratitis, conjunctivitis, defect in the corneal epithelium, diplopia, decreased sensitivity of the cornea, asthenopia, barley.

From the side of the organ of hearing: rarely - pain in the ear.

From the respiratory system: rarely - increased secretion of the detachable mucous membrane of the paranasal sinuses, rhinitis.

From the digestive system: often - dysgeusia; infrequently - nausea; rarely - abdominal pain, diarrhea.

On the part of the skin and subcutaneous tissues: rarely - dermatitis.

From the musculoskeletal system: the frequency is unknown - disorders of the ligamentous apparatus.

Application during pregnancy and lactation

There are no data on the safety of topical use of ciprofloxacin during pregnancy, so its use is justified only in cases where the intended benefit to the mother outweighs the possible risk to the fetus.

When taken orally, ciprofloxacin is excreted in human breast milk. It is not known whether ciprofloxacin is excreted in breast milk when applied topically, but the risk to a breastfed baby cannot be excluded in this case. If necessary, use during lactation requires caution.

Application in children

The drug is approved for use in children and adolescents under the age of 18

Use in elderly patients

The drug is approved for use in elderly patients.

special instructions

The use 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.

Influence on the ability to drive vehicles and 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.

Drug interactions

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.