Ciprolake - instructions for use, dose, side effects, contraindications

A broad-spectrum antimicrobial agent, a quinolone derivative, suppresses bacterial DNA gyrase (topoisomerases II and IV, responsible for the process of supercoiling the chromosomal DNA around the nuclear RNA, which is necessary for reading the genetic information), disrupts DNA synthesis, growth and division of bacteria; causes significant morphological changes (including the cell wall and membranes) and the rapid death of the bacterial cell.

It acts bactericidal on gram-negative organisms during rest and division (because it affects not only the DNA-gyrase, but also causes lysis of the cell wall), gram-positive microorganisms - only during the fission period.

Low toxicity for macroorganism cells is explained by the absence of DNA-gyrase in them. Against the background of taking ciprofloxacin, there is no parallel development of resistance to other drugs.antibiotics not belonging to the group of inhibitors of gyrase, 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 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 pathogens - Legionella pneumophila, Brucella spp., Listeria monocytogenes, Mycobacterium tuberculosis, Mycobacterium kansasii; Gram-positive aerobic bacteria: Staphylococcus spp. (Staphylococcus aureus, Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus saprophyticus), Streptococcus spp. (Streptococcus pyogenes, Streptococcus agalactiae).

The majority of staphylococci, resistant to methicillin, are resistant to ciprofloxacin. Sensitivity of Streptococcus pneumoniae, Enterococcus faecalis, Mycobacterium avium (located intracellularly) - moderate (high concentrations are required to repress). Bacillus anthracis is also sensitive to ciprofloxacin.

For drug resistant: Bacteroides fragilis, Pseudomonas cepacia, Pseudomonas maltophilia, Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroides. It is effective against Treponema pallidum.

Resistance develops very slowly, because on the one hand, after the action of ciprofloxacin are left with persistent microorganisms, and on the other - the bacterial cells do not have the enzymes that inactivate it.

Pharmacokinetics:

When intravenously administered 200 mg or 400 mg of ciprofloxacin 60 minutes after the start of infusion, the concentration of the active substance in the serum is 2.1 μg / ml and 4.6 μg / ml, respectively.

The volume of distribution in the equilibrium state is 2-3 l / kg. There is a high concentration of ciprofloxacin in the bile, several times higher than its concentration in the plasma.

Well distributed in body tissues (excluding tissue, rich in fats, for example, nervous tissue). Concentration in tissues is 2-12 times higher than in plasma. Therapeutic concentrations are achieved in saliva, tonsils, liver, gall bladder, bile, intestine, abdominal and pelvic organs, uterus, seminal fluid, prostate tissue, endometrium, fallopian tubes and ovaries, kidneys and urinary organs, pulmonary tissue, bronchial secretion , bone tissue, muscles, synovial fluid and articular cartilage, peritoneal fluid, skin. The cerebrospinal fluid penetrates in a small amount, where its concentration in uninflated cerebral membranes is 6-10% of that in the serum, and when inflamed - 14-37%. Ciprofloxacin also well penetrates into the eye fluid, pleura, peritoneum, lymph, through the placenta. The concentration of ciprofloxacin in blood neutrophils is 2-7 times higher than in serum.

After intravenous administration, the concentration in the urine during the first two hours of intake is almost 100 times greater than in the serum, which significantly exceeds the minimum inhibitory concentrations for most pathogens of urinary tract infections.

In patients with unchanged renal function, the half-life period is usually 5-6 hours, with chronic renal failure (CRF) up to 12 hours. It is mainly excreted by the kidneys by tubular filtration and tubular secretion in unchanged form (50-70%) and in the form of metabolites (10%), the rest - through the gastrointestinal tract (GIT). A small amount is excreted in breast milk. With CRF (creatinine clearance (CC) above 20 ml / min), the percentage of the drug withdrawn through the kidneys decreases, but cumulation in the body does not occur due to a compensatory increase in the metabolism of the drug and excretion through the gastrointestinal tract.

Indications:

Infectious-inflammatory diseases caused by sensitive microorganisms:

respiratory tract (acute and chronic (at the stage of exacerbation) bronchitis, pneumonia, bronchiectatic disease, infectious complications in cystic fibrosis);
infection of the ENT organs (acute sinusitis);
infection of the kidneys and urinary tract (cystitis, pyelonephritis);
Complicated intra-abdominal infections (in combination with metronidazole), incl. peritonitis;
chronic bacterial prostatitis;
uncomplicated gonorrhea;
typhoid fever, campylobacteriosis, shigellosis, diarrhea of "travelers";
infections of the skin and soft tissues (infected ulcers, wounds, burns, abscesses, phlegmon);
bones and joints (osteomyelitis, septic arthritis);
septicemia; infection on the background of immunodeficiency (arising in the treatment of immunosuppressive drugs or in patients with neutropenia);
prevention of infections during surgical interventions;
prevention and treatment of pulmonary form of anthrax.

Children.

Therapy of complications caused by Pseudomonas aeruginosa in children with cystic fibrosis of the lungs from 5 to 17 years;
prevention and treatment of pulmonary form of anthrax (infection with Bacillus anthracis).

Contraindications:

Hypersensitivity, incl. to fluoroquinolones, deficiency of glucose-6-phosphate dehydrogenase,childhood and adolescence (up to 18 years before the completion of the formation of the skeleton except for the treatment of complications caused by Pseudomonas aeruginosa in children with cystic fibrosis of the lungs from 5 to 17 years, prevention and treatment of pulmonary form of anthrax), pregnancy, lactation, simultaneous reception with tizanidine (risk of pronounced decrease in blood pressure, drowsiness).

Carefully:

Severe atherosclerosis of cerebral vessels, cerebral circulation disorder, mental illness, epileptic syndrome, epilepsy, severe renal and / or hepatic insufficiency, tendon damage with previous treatment with fluoroquinolones, elderly age.

Dosing and Administration:

Ciprofloxacin is administered as an intravenous infusion lasting at least 30 minutes (200 mg) and 60 minutes (400 mg). The dose of ciprofloxacin depends on the severity of the disease, the type of infection, the body's condition, age, weight and kidney function in the patient.

Recommended doses are usually for intravenous administration: a single dose of 200 mg (in severe infections - 400 mg), the frequency of administration is 2 times a day; the duration of treatment depends on the severity of the disease -1-2 weeks, if necessary and more.

In infections of the lower respiratory tract 200-400 mg 2 times a day.

With infections of the urinary tract: acute uncomplicated -100 mg 2 times a day; cystitis in women (before menopause) - once 100 mg; Complicated - 200 mg 2 times a day.

With uncomplicated gonorrhea -100 mg once, with extragenital -100 mg 2 times a day.

Infectious diarrhea - 200 mg 2 times, the course of treatment - 5-7 days.

Especially severe infections (streptococcal pneumonia, infectious complications of cystic fibrosis, infections of bones and joints, septicemia, peritonitis), especially caused by Pseudomonas, Staphylococcus - 400 mg 3 times a day.

Pulmonary form of anthrax (treatment and prophylaxis): 400 mg 2 times a day.

To prevent infections during surgical interventions - 0.2-0.4 g for 0.5-1 h before surgery; When the duration of the operation is more than 4 hours, re-enter in the same dose. Older patients are prescribed lower doses, depending on the severity of the infection and the CC score.

In pediatrics:

in the treatment of complications caused by Pseudomonas aeruginosa in children with cystic fibrosis of the lungs from 5 to 17 years - 10 mg / kg 3 times a day (maximum dose of 1200 mg). Duration of treatment is 10-14 days.

With a pulmonary form of anthrax (prevention and treatment) - 10 mg / kg 2 times a day.The maximum single dose is 400 mg, the daily dose is 800 mg. The total duration of taking ciprofloxacin is 60 days.

CRF: at a glomerular filtration rate (CK 31-60 ml / min / 1.73 square meters or serum creatinine concentration from 1.4 to 1.9 mg / 100 ml), the maximum daily dose is 800 mg. At a glomerular filtration rate (CC below 30 ml / min / 1.73 square meters or serum creatinine concentration above 2 mg / 100 ml) and during hemodialysis the maximum daily dose is 400 mg; in hemodialysis ciprofloxacin injected after a hemodialysis session. Infusion solution of ciprofloxacin is added to the dialysate (intraperitoneally): 50 mg of ciprofloxacin per liter of dialysate is administered 4 times a day every 6 hours.

Average duration of treatment: 1 day - with acute uncomplicated gonorrhea and cystitis; up to 7 days - with infections of the kidneys, urinary tract and abdominal cavity; during the entire period of the neutropenic phase in patients with immunodeficiency, but not more than 2 months. - with osteomyelitis and 7-14 days - with all other infections. With streptococcal infections due to the danger of late complications, treatment should last at least 10 days. Treatment is carried out for at least 3 days after the normalization of body temperature or the disappearance of clinical symptoms.

Infusion solutions ready for use can be combined with 0.9 % solution of sodium chloride, Ringer's solution and Ringer-lactate, 5 and 10% dextrose solution, 10% fructose solution, and also a solution containing 5% dextrose solution with 0.225% or 0.45% sodium chloride solution.

Side effects:

From the digestive system: nausea, diarrhea, vomiting, abdominal pain, flatulence, decreased appetite, cholestatic jaundice (especially in patients with liver disease), hepatitis, hepatonecrosis.

From the urinary system: hematuria, crystalluria (especially in alkaline urine and low diuresis), glomerulonephritis, dysuria, polyuria, urinary retention, albuminuria, urethral bleeding, decreased renal nitrogen function, interstitial nephritis.

From the central nervous system: dizziness, headache, fatigue, anxiety, tremor, insomnia, nightmarish dreams, peripheral paralysis (anomaly of perception of pain), sweating, increased intracranial pressure, confusion, depression, hallucinations,as well as other manifestations of psychotic reactions (occasionally progressing to conditions in which the patient can do harm to himself), migraine, fainting, thrombosis of the cerebral arteries.

From the sense organs: violation of taste and smell, visual impairment (diplopia, change in color perception), tinnitus, hearing loss.

From the cardiovascular system: tachycardia, heart rhythm disturbances, lowering blood pressure.

From the hematopoietic system: leukopenia, granulocytopenia, anemia, thrombocytopenia, leukocytosis, thrombocytosis, hemolytic anemia.

From the musculoskeletal system: arthralgia, arthritis, tendovaginitis, tendon ruptures, myalgia.

Laboratory indicators: hypoprothrombinemia, increased activity of "liver" transaminases and alkaline phosphatase, hypercreatininemia, hyperbilirubinemia, hyperglycemia.

Allergic reactions: itching, urticaria, the formation of blisters accompanied by bleeding, and small nodules forming scabs, drug fever, pinpoint hemorrhages on the skin (petechiae), swelling of the face or larynx, dyspnea, eosinophilia, vasculitis, nodal erythema,exudative erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome).

Local reactions: pain and burning at the injection site, phlebitis.

Other: general weakness, superinfection (candidiasis, pseudomembranous colitis), increased photosensitivity, "tides" of blood to the face.

Overdose:

The specific antidote is unknown. It is necessary to carefully monitor the patient's condition, to carry out usual emergency measures, to ensure sufficient fluid intake. With the help of hemo- or peritoneal dialysis, only a minor (less than 10) %) amount of preparation.

Interaction:

Due to the decrease in the activity of microsomal oxidation in hepatocytes, it increases the concentration and prolongs the half-life of theophylline (and other xanthines, for example, caffeine), oral hypoglycemic drugs, indirect anticoagulants, and decreases the prothrombin index.

Simultaneous reception with tizanidine increases the maximum plasma concentration of the latter by 7 times (from 4 to 21 times) and AUC by 10 times (from 6 to 24 times),which increases the risk of a marked decrease in blood pressure and drowsiness.

When combined with other antimicrobial agents (beta-lactam antibiotics, aminoglycosides, vancomycin, clindamycin, metronidazole) the activity of ciprofloxacin increases. It can be successfully applied in combination with azlocillin and ceftazidime in infections caused by Pseudomonas spp .; with mezlocillin, azlocillin and other beta-lactam antibiotics - with streptococcal infections; with isoxazolylpenicillins and vancomycin - with staphylococcal infections; from metronidazole and clindamycin - in anaerobic infections.

Strengthens the effect of warfarin and other indirect anticoagulants, prolonging the time of bleeding.

Increases the nephrotoxic effect of cyclosporine, there is an increase in serum creatinine. Such patients need control of this indicator 2 times a week. Nonsteroidal anti-inflammatory drugs (excluding aminosalicylic acid) increase the risk of seizures.

Joint appointment of uricosuric drugs leads to a delay in excretion (up to 50%) and an increase in the plasma concentration of ciprofloxacin.

The infusion solution is pharmaceutically incompatible with all infusion solutions and drugs that are physically and chemically unstable under acidic conditions (the pH of the infusion solution of ciprofloxacin is 3.9-4.5). Do not mix the IV solution with solutions having a pH of more than 7.

Special instructions:

Ciprofloxacin is not a drug of choice in suspected or established pneumonia caused by Streptococcus pneumoniae.

If a severe and prolonged diarrhea occurs during or after treatment with ciprofloxacin, the diagnosis of pseudomembranous colitis should be excluded, which requires immediate discontinuation of the drug and the appointment of appropriate treatment.

If pain occurs in tendons or when the first signs of tendovaginitis appear, treatment should be discontinued (individual cases of inflammation and even rupture of tendons during treatment with fluoroquinolones are described).

To avoid the development of crystalluria, exceeding the recommended daily dose is inadmissible, adequate fluid intake and maintenance of acid urine reaction are also necessary.

Patients with epilepsy, seizures in the anamnesis, vascular diseases and organic brain lesions,in connection with the threat of development of adverse reactions from the central nervous system ciprofloxacin should be prescribed only for "vital" indications.

With simultaneous intravenous administration of ciprofloxacin and drugs for general anesthesia, the barbituric acid derivative group requires constant monitoring of heart rate, blood pressure, and ECG.

During the treatment period, direct exposure to ultraviolet light should be avoided.

Effect on the ability to drive transp. cf. and fur:

Patients receiving ciprofloxacin, care should be taken when driving a car and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Solution for infusions 2 mg / ml.

Packaging:To 100 ml in a plastic bottle, packed in a transparent polypropylene bag. The bottle together with the instruction for use is placed in a cardboard box.

Storage conditions:

In dry, dark place at a temperature of not more than 25 ⁰ C. Do not freeze.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the time specified on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N014029 / 02

Date of registration:12.01.2010

The owner of the registration certificate:La Car Pharma LimitedLa Car Pharma Limited India

Manufacturer: & nbsp

LA CARE FARMA, Ltd. India

Representation: & nbspJodas Expoim, Open CompanyJodas Expoim, Open Company

Information update date: & nbsp19.10.2015

Illustrated instructions

Instructions

Ciprolakeer (Ciprolacare)