Ciprofloxacin

General characteristics. Structure:

Active ingredient: 200 mg of ciprofloxacin in 1 bottle.

Excipients: sodium chloride, the EDTA sodium salt, lactic acid, sodium hydroxide, Acidum hydrochloricum, water for injections.

Pharmacological properties:

Pharmacodynamics. Antimicrobic drug of a broad spectrum of activity from group of ftorkhinolon. Works bakteritsidno.

The mechanism of action is connected with inhibition of DNK-girazy 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 asteroids.

Pharmacokinetics. Later in/in administrations of ciprofloxacin of 200 mg and 400 mg of Cmax in a blood plasma in 60 min. makes 2.1 and 4.6 mg/ml, in 12 h - 0.1 and 0.2 mg/ml respectively.

Ciprofloxacin is well distributed in an organism and reaches therapeutic concentration in most bodies and fabrics in 2 h later in/in introductions. Drug is found in saliva, almonds, pulmonary tissue, a liver, bile and a gall bladder, intestines, a uterus, an endometria, fallopian pipes and ovaries, tissues of a prostate gland, semen, kidneys and urinary bodies, a bone tissue, muscles, synovial fluid and joint cartilages, skin. Ciprofloxacin also well gets into eye liquid, a bronchial secret, a pleura, a peritoneum, a lymph, through a placenta. Concentration of ciprofloxacin in cerebrospinal liquid makes 10%, at an inflammation of a meninx to 37% of that in a blood plasma.

Linkng with proteins of a blood plasma is insignificant (20-40%). Vd - 2-3 l/kg. T1/2 makes 5-6 h. About 50-70% of the appointed dose are allocated in not changed look during 24 h by means of glomerular filtering and tubular secretion through kidneys, 1-2% are allocated in the form of a metabolite through bile, and 15% are removed with a stake within 5 days after reception.

Indications to use:

— the pneumonia, bronchial pneumonia, infectious pleurisy, emphysema, abscesses infected bronchiectasias, acute and chronic bronchitis, cystous fibrosis;

— peritonitis, intrabdominalny abscesses, cholangitis, cholecystitis, empyema of a gall bladder;

— acute and chronic pyelonephritis, prostatitis, cystitis, chronic epididymite;

— outside and average otitis, sinusitis, mastoiditis;

— salpingitis, endometritis;

— acute and chronic osteomyelitis, septic arthritis;

— the infected ulcers, wounds, burns;

— sepsis, bacteremia;

— clamidiosis, gonorrhea;

— conjunctivitis, blefarokonjyunktivit, a blepharitis, a keratitis;

— keratoconjunctivitis, bacterial helcoma;

— prevention of postoperative infections.

Route of administration and doses:

For in/in introductions a single dose - 200 mg (at heavy infections - 400 mg), frequency rate of introduction - 2 times/days.

Duration of treatment depends on disease severity, but treatment always has to continue 2 more days after disappearance of symptoms of a disease. Usually duration of treatment makes 7-10 days. Solution of ciprofloxacin of 200 mg in 100 ml for intravenous administration is appointed kapelno within 30-60 min.

At acute gonorrhea - once in/in 100 mg.

For prevention of postoperative infections - 200-400mg in 30-60 min. prior to operation.

Features of use:

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.

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. Considering side effects, it is necessary to be careful during the driving and service of moving mechanisms.

Side effects:

Perhaps: nausea, diarrhea, vomiting, abdominal pains, meteorism, anorexia, cholestatic jaundice, hepatitis, candidiasis, pseudomembranous colitis, dizziness, headache, increased fatigue, tremor, sleeplessness, perspiration, increase in intracranial pressure, confusion of consciousness, depression, hallucinations, migraine, tachycardia, disturbances of a cordial rhythm, lowering of arterial pressure, leukopenia, granulocytopenia, anemia, thrombocytopenia, leukocytosis, thrombocytosis, hemolitic anemia, prothrombinopenia, increase, activities of hepatic transaminases and ShchF, giperkreatininemiya, hyperbilirubinemia, hyperglycemia, hamaturia, crystalluria, glomerulonephritis, dysuria, polyuria, delay, urine, albuminuria, urethral bleedings, hamaturia, decrease, azotvydelitelny function of kidneys, intersticial nephrite, skin itch, small tortoiseshell, fever, eosinophilia, nodal erythema, exudative multiformny erythema, Stephens-Johnson's syndrome, Lyell's disease, disturbances of taste and sense of smell, diplopia, change of color perception, sonitus, decrease in hearing, arthralgia, arthritis, tendovaginitis, mialgiya, pain and burning in an injection site, phlebitis.

Interaction with other medicines:

Owing to decrease of the activity of processes of a microsomal oxidation in hepatocytes, increases concentration and extends theophylline T1/2 (etc. xanthines, for example, caffeine), peroral hypoglycemic drugs, indirect anticoagulants, promotes decrease in a prothrombin ratio.

At a combination to other antimicrobic drugs (beta lactams, aminoglycosides, clindamycin, metronidazole) a synergism is usually observed.

At simultaneous use of antacids, the containing magnesium or aluminum hydroxide, it is possible delay of absorption of a tsiprfloksatsin what leads to reduction of its concentration in serum and urine therefore the interval between their receptions has to make not less than 4 h.

Contraindications:

— hypersensitivity to ciprofloxacin;

— pseudomembranous colitis;

— children's age up to 18 years;

— pregnancy;

— lactation period.

Overdose:

Symptoms: nausea, vomiting, diarrhea, headache, faint, hallucinations, spasms.

Treatment: there is no specific antidote. It is necessary to control carefully a condition of the patient, 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:

To store in dry, protected from light, the place at a temperature not above 25 °C. To store in the place, unavailable to children! A period of validity - 3 years. Not to apply after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

100 ml - bottles plastic (1) - packagings cardboard.