Vero-tsiprofloksatsin

General characteristics. Structure:

Active agent: Ciprofloxacin a hydrochloride (in terms of Ciprofloxacin) — 250 mg and 500 mg. Excipients: sodium carboxymethylstarch, cellulose microcrystallic, полипласдон Ickx Al (кросповидон), polyvinylpirrolidone or povidone 8000, magnesium stearate, aerosil, oksipropilmetiltsellyuloza, twin-80, titanium dioxide, talc.

Description: tablets of color, white or white with a yellowish shade, film coated color, white or white with a yellowish shade, with a biconvex surface.

Pharmacological properties:

Pharmacodynamics. Antimicrobic drug of a broad spectrum of activity from group of ftorkhinolon. Works bakteritsidno. Drug inhibits DNK-girazu enzyme of bacteria owing to what DNA replication and synthesis of cellular proteins of bacteria are broken. Ciprofloxacin affects both the breeding microorganisms, and on being in a resting phase. 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, Mycobacterium avium-intracellulare. Also gram-positive aerobic bacteria are sensitive to Ciprofloxacin: Staphylococcus spp., (S.aureus, S.haemolyticus, S.hominis, S.saprophyticus), Streptococcus spp. (St.pyogenes, St.agalactiae). The majority of the stafilokokk steady against Methicillinum are steady also against Ciprofloxacin. Sensitivity of bacteria of Streptococcus pneumoniae, Enterococcus faecalis is moderate. To Corynebacterium spp rezistentna drug., Bacteroides fragilis, Pseudomonas cepacia, Pseudomonas maltophilia, Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroides. Effect of drug concerning Treponema pallidum is studied insufficiently.

Pharmacokinetics. At oral administration Ciprofloxacin is quickly soaked up from a GIT. Bioavailability of drug makes 50–85%. The maximum concentration of drug in blood serum of healthy volunteers at oral administration (to food) 250, 500, 750 and 1000 mg of drug is reached in 1 — 1,5 hour and makes 1,2; 2,4; 4,3 and 5,4 mkg/ml respectively. Orally accepted Ciprofloxacin is distributed in fabrics and liquids of an organism. High concentration of drug are observed in bile, lungs, kidneys, a liver, a gall bladder, a uterus, semen, prostate tissue, almonds, an endometria, fallopian pipes and ovaries. Concentration of drug in these fabrics is higher, than in serum. Ciprofloxacin also well gets into bones, eye liquid, a bronchial secret, saliva, skin, muscles, a pleura, a peritoneum, a lymph. The collecting concentration of Ciprofloxacin in neutrophils of blood is 2 — 7 times higher, than in serum. Distribution volume in an organism makes 2 — 3,5 l/kg. Drug gets into cerebrospinal fluid in a small amount where its concentration makes 6 — 10% of that serum. Extent of linkng of Ciprofloxacin with proteins of plasma makes 30%. At patients with not changed function of kidneys the elimination half-life makes usually 3 — 5 hours. At a renal failure the elimination half-life increases. The main way of removal of Ciprofloxacin from an organism — a kidney. With urine 50 — 70% are removed. From 15 to 30% are removed with excrement. Patients with a heavy renal failure (the clearance of creatinine is lower than 20 ml/min. / 1,73 m 2) need to appoint a half of a daily dose of drug.

Indications to use:

The infections and inflammatory diseases caused by microorganisms, sensitive to Tsiprofloksatsin:

- respiratory tracts;
- fish soup, throat and nose;
- kidneys and urinary tract;
- generative organs;
- alimentary system ( including mouth, teeth, jaws);
- gall bladder and biliary tract;
- integuments, mucous membranes and soft tissues;
 - a musculoskeletal system.

Ciprofloxacin is shown for treatment of sepsis and peritonitis, and also for prevention and treatment of infections at patients with reduced immunity (at therapy by immunodepressants).

Route of administration and doses:

The dose of Ciprofloxacin depends on disease severity, type of an infection, a condition of an organism, age, weight and function of kidneys at the patient. The doses recommended usually: Ciprofloxacin in a dosage form of a tablet on 250 mg and 500 mg for oral administration: — uncomplicated diseases of kidneys and urinary tract — on 250 mg, and in the complicated cases on 500 mg 2 times a day; — diseases of lower parts of moderately severe respiratory tracts — on 250 mg, and in more hard cases — on 500 mg, 2 times a day; — for treatment of gonorrhea the single dose of Ciprofloxacin in a dose of 250 — 500 mg is recommended; — gynecologic diseases, enterita and colitis with a heavy current and high temperature, prostatitises, osteomyelites — on 500 mg 2 times a day (for treatment of banal diarrhea it is possible to use in a dose 250 mg 2 times a day). Drug should be accepted on an empty stomach, washing down with enough liquid. Patients with the expressed renal failures should appoint a half dose of drug. Duration of treatment depends on disease severity, but treatment always has to continue at least two more days after disappearance of symptoms of a disease. Usually duration of treatment makes 7–10 days. The table of the recommended drug doses for patients with a chronic renal failure:

Clearance of creatinine of ml/min.	Dose
> 50	usual mode of dosing
30 — 50	250–500 mg of 1 times at 12 o'clock
5 — 29	250–500 mg of 1 times at 18 o'clock
-nye, nakh-sya on haemo - or peritoneal dialysis after dialysis	250–500 mg of 1 times at 24 o'clock

Features of use:

The patient with epilepsy, attacks of spasms in the anamnesis, vascular diseases and organic lesions of a brain in connection with threat of development of side reactions from TsNS it is necessary to appoint Ciprofloxacin only according to vital indications. At emergence in time or after treatment by Ciprofloxacin of heavy and long diarrhea it is necessary to exclude the diagnosis of pseudomembranous colitis which demands immediate drug withdrawal and purpose of the corresponding treatment. When developing pains in sinews or at emergence of the first symptoms of a tendovaginitis treatment should be stopped  because separate cases of an inflammation and even a rupture of sinews are described during treatment of a ftorkhinolonama. During treatment it is necessary to provide with Ciprofloxacin enough liquid at observance of a normal diuresis. During treatment by Ciprofloxacin it is necessary to avoid contact with direct sunshine. Influence on ability to driving of motor transport and to control of mechanisms. The patients accepting Ciprofloxacin should be careful during the driving of the car and occupations other potentially dangerous types of activity requiring special attention and speed of psychomotor reactions (especially at simultaneous alcohol intake).

Side effects:

- From the alimentary system: nausea, diarrhea, vomiting, abdominal pains, a meteorism, anorexia, cholestatic jaundice (especially at patients with the postponed liver diseases), hepatitis, гепатонекроз.
- From a nervous system: dizziness, a headache, increased fatigue, uneasiness, a tremor, sleeplessness, "dreadful" dreams, a peripheral paralgeziya (anomaly of perception of feeling of pain), perspiration, increase in intracranial pressure, uneasiness, confusion of consciousness, a depression, hallucinations, and also other manifestations of psychotic reactions (which are occasionally progressing to states in which the patient can do himself harm), migraine, a faint, thrombosis of cerebral arteries.
- From sense bodys: disturbances of taste and sense of smell, vision disorder (diplopia, change of color perception), sonitus, decrease in hearing.
- From CCC: tachycardia, disturbances of a cordial rhythm, decrease in the ABP, rushes of blood to face skin.
- From the hemopoietic system: leukopenia, granulocytopenia, anemia, thrombocytopenia, leukocytosis, thrombocytosis, hemolitic anemia.
- From laboratory indicators: prothrombinopenia, increase in activity of "hepatic" transaminases and ShchF, giperkreatininemiya, hyperbilirubinemia, hyperglycemia.
- From an urinary system: a hamaturia, a crystalluria (first of all at alkalinuria and a hypouresis), a glomerulonephritis, a dysuria, a polyuria, an ischuria, an albuminuria, urethral bleedings, a hamaturia, decrease in azotvydelitelny function of kidneys, intersticial nephrite.
- Allergic reactions: a skin itch, a small tortoiseshell, blistering, followed by bleedings, and the small small knots forming crusts, medicinal fever, dot hemorrhages (petechias), a face edema or throats, an asthma, an eosinophilia, the raised photosensitivity, a vasculitis, a nodal erythema, an exudative multiformny erythema, Stephens-Johnson's syndrome (a malignant exudative erythema), a toxic epidermal necrolysis (Lyell's disease).
- Other: arthralgia, arthritis, tendovaginitis, ruptures of sinews, general weakness, mialgiya, superinfections (candidiasis, pseudomembranous colitis).

Interaction with other medicines:

At simultaneous use of Ciprofloxacin with didanoziny absorption of Ciprofloxacin decreases owing to formation of complexes of Ciprofloxacin with  the aluminum and magnesian salts which are contained in the didanozena. The concomitant use of Ciprofloxacin and theophylline can lead to increase in concentration of theophylline in a blood plasma, at the expense of competitive inhibition in P450 cytochrome binding sites that leads to increase in an elimination half-life of theophylline and increase of risk of development of the toxic action connected with theophylline. The concomitant use of antacids, and also the drugs containing ions of aluminum, zinc, iron or magnesium can cause decrease in absorption of Ciprofloxacin therefore the interval between purpose of these drugs has to be not less than 4 h. At simultaneous use of Ciprofloxacin and anticoagulants the bleeding time is extended. At simultaneous use of Ciprofloxacin and Cyclosporine nephrotoxic action of the last amplifies.

Contraindications:

- pregnancy;
- breastfeeding period;
- children's and teenage age up to 18 years;
- hypersensitivity to Ciprofloxacin or other drugs from group of ftorkhinolon.

Overdose:

The specific antidote is unknown. It is necessary to control carefully a condition of the patient, to make a gastric lavage, to carry out usual measures of acute management, to provide sufficient intake of liquid. By means of haemo - or peritoneal dialysis the amount of drug can be removed only insignificant (less than 10%).

Storage conditions:

List B. In the dry, protected from light place. At a temperature not above 25 °C. To store in the place, unavailable to children.
Period of validity - 2 years. Not to use after the term specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets, coated, on 250 mg and 500 mg. On 10 tablets in a blister strip packaging; on 1 blister strip packaging together with  the application instruction in a pack. On 10 tablets in bank. Each can together with  the application instruction in a pack.