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

Antimicrobial preparation of a broad spectrum of action from the group of fluoroquinolones. It is bactericidal. The drug inhibits the DNA enzyme enzyme of bacteria, as a result of which DNA replication and the synthesis of bacterial cell proteins are disturbed. Ciprofloxacin It acts both on multiplying microorganisms, and on those in the resting phase.

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 midtocida, Plesiomonas shigelloides, Campylobacter jejuni, Neisseria spp.), some intracellular pathogens: Legionella pneumophila, Brucella spp., Listeria monocytogenes, Mycobacterium tuberculosis, Mycobacterium kansasii.

Gram-positive aerobic bacteria are also sensitive to ciprofloxacin: Staphylococcus spp. (Staphylococcus aureus, Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus saprophyticus), Streptococcus spp. (Streptococcus pyogenes, Streptococcus agalactiae). Sensitivity of bacteria Streptococcus pneumoniae, Enterococcus faecalis, Mycobacterium aviume (located intracellularly) to ciprofloxacin is moderate. The majority of staphylococci, resistant to methicillin, are resistant to ciprofloxacin.

The drug is sensitive in vitro and in vivo Bacillus anthracis.

Ciprofloxacin is resistant Corynebacterium spp., Bacteroides fragilis, Pseudomonas cepacia, Pseudomonas maltophilia, Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroids.

The drug is not effective against Treponema pallidum.

Pharmacokinetics:

After intravenous infusion of 200 mg or 400 mg of ciprofloxacin, the maximum concentration (C_max) in blood plasma is achieved in 60 minutes and is 2.1 μg / ml and 4.6 μg / ml, respectively. The volume of distribution is 2-3 l / kg, the connection with plasma proteins is 20-40%.

Well distributed ciprofloxacin in the tissues of the body (excluding tissue rich in fats, for example, nerve tissue); its content 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 and in the 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.

Metabolised in the liver (15-30%) with the formation of low-activity metabolites (diethylciprofloxacin, oxocycloploxacin, sulfociprofloxacin, formyl ciprofloxacin).

The half-life period (T1) with intravenous administration is 5-6 hours. In patients with chronic renal insufficiency (CRF), T1 may extend up to 12 hours.

It is excreted mainly by the kidneys through tubular filtration and tubular secretion in unchanged form (50-70%) and in the form of metabolites (10%), the rest - through the intestine. A small amount is excreted in breast milk. With intravenous administration, the concentration in the urine during the first 2 hours after administration is almost 100 times greater than in the serum,which significantly exceeds the minimum inhibitory concentrations (MICs) for most pathogens of urinary tract infections.

Kidney clearance - 3-5 ml / min / kg; total clearance - 8-10 ml / min / kg.

With CRF (creatinine clearance (CK) above 20 ml / min), the percentage of the drug withdrawn through the kidneys decreases, but no cumulation in the body occurs due to a compensatory increase in the metabolism of the drug and excretion of the intestine.

Indications:

Infectious-inflammatory diseases caused by microorganisms sensitive to ciprofloxacin:

lower respiratory tract (including acute and chronic (at the stage of exacerbation) bronchitis, pneumonia, bronchiectatic disease, infectious complications of cystic fibrosis);
ENT organs (including acute sinusitis);
kidney and urinary tract (including cystitis, pyelonephritis);
organs of the small pelvis (including chronic bacterial prostatitis);
the digestive system (including typhoid fever, campylobacteriosis, shigellosis, infectious diarrhea);
skin and soft tissues (including infected ulcers, wounds, burns, abscesses, phlegmon);
bones and joints (including osteomyelitis, septic arthritis);
septicemia;
Complicated intra-abdominal infections (in combination with metronidazole), including peritonitis.
uncomplicated gonorrhea.

Prevention of infections during surgical interventions.

Prevention and treatment of infections in patients with reduced immunity (with immunosuppressant therapy or in patients with neutropenia).

Prevention and treatment of pulmonary form of anthrax (infection with Bacillus anthracis).

Pediatric Use

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

Contraindications:

pregnancy;
lactation period (breastfeeding);
children and adolescents (up to 18 years before the completion of the formation of the skeleton, in addition to the treatment of complications caused by Pseudomonas aeruginosa in children with cystic fibrosis of the lungs aged 5 to 17 years, and prevention and treatment of the pulmonary form of anthrax);
increased sensitivity to ciprofloxacin or other drugs from the group of fluoroquinolones;
pseudomembranous colitis;
simultaneous reception with tizanidine (risk of pronounced reduction in blood pressure, drowsiness).

Carefully:

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

Dosing and Administration:

Assigned intravenously (drip) for 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

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) - 100 mg once; Complicated - 200 mg 2 times a day.

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

With infectious diarrhea - 200 mg 2 times a day, the course of treatment - 5-7 days.

In other infections (depending on the severity) - a single dose is 200-400 mg, the frequency of administration - 2 times a day.

For particularly serious life-threatening infections (streptococcal pneumonia, infectious complications of cystic fibrosis, infections of bones and joints, septicemia, peritonitis), especially caused Pseudomonas spp., Staphylococcus spp. and Streptococcus spp., dose increase to 400 mg 3 times a day.

For the prevention of postoperative infections - for 30-60 minutes before the operation, intravenously, 200-400 mg; When the duration of the operation is more than 4 hours, re-enter in the same dose.

With pulmonary form of anthrax (treatment and prevention) 400 mg 2 times a day are administered (maximum single dose is 400 mg, maximum daily dose is 800 mg). Treatment should begin immediately after suspected or confirmed infection. The total duration of treatment with ciprofloxacin in pulmonary form of anthrax is 60 days.

In case of impaired renal function

With a creatinine clearance of 31 to 60 mL / min or a serum creatinine concentration of 1.4 to 1.9 mg / 100 mL, the maximum dose of ciprofloxacin for intravenous administration should be 800 mg per day.

With a creatinine clearance of 30 ml / min and less or a serum creatinine concentration of 2.0 mg / 100 ml or more, the maximum dose of ciprofloxacin for intravenous administration should be 400 mg per day.

With hemodialysis ciprofloxacin injected after a hemodialysis session.

With peritoneal dialysis, a solution of ciprofloxacin is added to the dialysate (intraperitoneally) at a dose of 50 mg per liter of dialysate every 6 hours.

When a violation of liver function

Patients with a violation of the function of the liver dose adjustment is not carried out.

For elderly patients

Elderly patients are prescribed lower doses, depending on the severity of the infection and the CC score.

In Pediatrics

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

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

Duration of treatment

In acute uncomplicated gonorrhea and cystitis - 1 day.

With infections of the kidneys, urinary tract and abdominal cavity - up to 7 days.

In patients with reduced immunity (except for cases of osteomyelitis) - throughout the neutropenic phase. With osteomyelitis treatment can last no more than 2 months.

For all other infections - 7-14 days. With streptococcal infections due to the danger of late complications, treatment should last at least 10 days.

Treatment should be carried out at least 3 days after the normalization of body temperature or the disappearance of clinical symptoms.

After intravenous administration, the treatment can be continued orally.

Compatibility with other solutions

The infusion solution of ciprofloxacin is compatible with 0.9% solution of sodium chloride, 5% or 10% glucose solution (dextrose), a mixture of 5% glucose solution (dextrose) and 0.225% sodium chloride solution, a mixture of 5% glucose solution (dextrose) and 0, 45% sodium chloride solution, 10% fructose solution, Ringer's solution, Ringer's lactate 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 nervous system: dizziness, headache, fatigue, anxiety, tremor, insomnia, nightmarish dreams, peripheral paralysis (anomaly of perception of pain), increased sweating, increased intracranial pressure, confusion, depression, hallucinations, and 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, "tides" of blood to the skin of the face.

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

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.

Allergic reactions: dermal itching, urticaria, blistering accompanied by bleeding, and small nodules forming scabs, drug fever, pinpoint hemorrhages (petechiae), face or laryngeal edema, dyspnea, eosinophilia, vasculitis, nodal erythema, exudative erythema multiforme, Stevens-Johnson syndrome malignant exudative erythema), toxic epidermal necrolysis (Lyell's syndrome), anaphylactic shock.

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

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

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

Other: superinfection (candidiasis, pseudomembranous colitis); rarely - increased photosensitivity, general weakness.

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 small amount (less than 10%) of the drug can be excreted.

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), increases the effect of indirect anticoagulants, and decreases the prothrombin index.

Increases the risk of seizures when combined with non-steroidal anti-inflammatory drugs (excluding acetylsalicylic acid).

Strengthens the nephrotoxic effect of cyclosporine (there is an increase in serum creatinine).

Increases the maximum concentration of tizanidine by 7 times (from 4 to 21 times) and AUC by 10 times (from 6 to 24 times), which increases the risk of pronounced decrease in blood pressure and drowsiness.

When combined with glybenklamidom can enhance the effect of the latter, which is manifested by hypoglycemia.

Co-administration with uricosuric drugs (for example, with probenecid) leads to a slowing down of ciprofloxacin (up to 50%) and an increase in its concentration in the plasma.

When combined with other antimicrobial agents (beta-lactam antibiotics, aminoglycosides, clindamycin, metronidazole), synergy is usually observed (can be successfully used in combination with azlocillin and ceftazidime in infections caused by Pseudomonas spp .; with mezlocillin, azlocillin and other beta-lactam antibiotics - with streptococcal infections; with isoxazolyl-penicillins and vancomycin - with staphylococcal infections; with metronidazole and clindamycin - with anaerobic infections).

Solution for ciprofloxacin infusions is pharmaceutically incompatible with all infusion solutions and preparations that are physico-chemically unstable in acidic medium (solution pH for ciprofloxacin infusions is 3.9 to 4.5). Do not mix the ciprofloxacin infusion solution with solutions that have a pH of more than 7.

Special instructions:

Patients with epilepsy, episodes of seizures in history, vascular diseases and organic brain damage due to the threat of development of adverse reactions from the central nervous system ciprofloxacin should be prescribed only for "vital" indications.

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 the tendons or when the first signs of tendovaginitis appear, treatment should be discontinued.

To avoid the development of crystalluria, exceeding the recommended daily dose is inadmissible. Also, during the treatment with ciprofloxacin, it is necessary to ensure the intake of a sufficient amount of fluid while observing normal diuresis and acid urine reaction.

During treatment with ciprofloxacin, UV irradiation should be avoided (including contact with direct sunlight).

In patients taking both ciclosporin and ciprofloxacin, it is necessary to monitor serum creatinine 2 times a week.

With simultaneous intravenous administration of ciprofloxacin and preparations for general anesthesia from the group of barbituric acid derivatives, continuous monitoring of blood pressure and heart function (heart rate, electrocardiogram) is necessary.

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

The solution for infusions is photosensitive; The vial should be removed from the box only before use.

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 infusion 200 mg / 100 ml.

Packaging:100 ml of the drug is placed in a round or flat polyethylene bottle.The bottle is placed in a polypropylene bag and then in a cardboard box along with the instructions for use.

Storage conditions:

Store in a dark place at a temperature of no higher than 30 ° C.

Do not freeze.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N014871 / 01

Date of registration:09.06.2008

The owner of the registration certificate:Orchid Helsker (a division of Orchid Chemicals and Pharmaceuticals Ltd.)Orchid Helsker (a division of Orchid Chemicals and Pharmaceuticals Ltd.) India

Manufacturer: & nbsp

ORCHID HEALTHCARE India

Information update date: & nbsp19.10.2015

Illustrated instructions

Instructions

Ciprofloxacin (Ciprofloxacin)