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 multocida, Plesiomonas shigelloides, Campylobacter jejuni, Neisseria spp.); some intracellular pathogens: Legionella pneumophila, Brucella spp., Chlamydia trachomatis, Listeria monocytogenes, Mycobacterium tuberculosis, Mycobacterium kansasii, Mycobacterium avium intracellulare.

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). Both in vitro and in vivo studies of ciprofloxacin are also sensitive to Bacillus anthracis.

The majority of staphylococci, resistant to methicillin, are resistant to ciprofloxacin. The sensitivity of bacteria Streptococcus pneumoniae, Enterococcus faecalis is moderate.

The drug is resistant Corynebacterium spp., Bacteroides fragilis, Pseudomonas cepacia, Pseudomonas maltophilia, Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroides. The effect of the drug on Treponema pallidum insufficiently studied.

Pharmacokinetics:

After intravenous infusion of 200 mg or 400 mg, the time to reach the maximum concentration (TC_max) - 60 min, the maximum concentration (C_max) Were 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%.

It is well distributed in body tissues (excluding tissue, rich in fats,

for example, a nervous tissue). The content in the tissues is 2-12 times higher than in the 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, kidney 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 non-inflamed cerebral membranes is 6-10% of that in the blood serum, and when inflamed - 14-37 %. Ciprofloxacin also well penetrates into the eye fluid, pleura, 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, sulfociprofloxacin, oxocycloploxacin, formyl ciprofloxacin).

With IV introduction, the half-life (T1 / 2) is 5-6 hours, with chronic renal failure - up to 12 hours. It is mainly excreted by the kidneys through tubular filtration and tubular secretion in an unchanged form of 50-70% and in the form of metabolites - 10 %, the rest - through the gastrointestinal tract. A small amount is excreted in breast milk.

After 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 maximum limit concentration for most pathogens of urinary tract infections.

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

Patients with severe renal insufficiency (creatinine clearance below 20 ml / min / 1.73 m² it is necessary to prescribe half the daily dose of the drug).

Indications:

Infectious-inflammatory diseases caused by microorganisms sensitive to ciprofloxacin:

- lower respiratory tract;

- ear, nose and throat;

- kidney and urinary tract;

- genital organs;

- Digestive system (including mouth, teeth, jaws); gallbladder and bile ducts;

- skin, mucous membranes and soft tissues;

- musculoskeletal system;

- prevention and treatment of pulmonary form of anthrax.

Ciprofloxacin is indicated for the treatment of sepsis and peritonitis, as well as for the prevention and treatment of infections in patients with reduced immunity (with immunosuppressant therapy).

Contraindications:

Hypersensitivity to fluoroquinolones, children's age (up to 18 years - 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 from 5 to 17 years, prevention and treatment of pulmonary form of anthrax), pregnancy, lactation, simultaneous reception with tizanidine.

Carefully:

Severe atherosclerosis of cerebral vessels, cerebral circulation disorder, mental illness, convulsive syndrome, epilepsy, marked renal and / or hepatic insufficiency, elderly age.

Pediatric Use

Ciprofloxacin is not recommended for use in children under 18 years of age for the treatment of other infectious diseases other than the treatment of complications caused by Pseudomonas aeruginosa in children with cystic fibrosis and treatment and prevention of pulmonary anthrax (after suspected or proven infection with Bacillus anthracis) (in children aged 5 to 17 years).

Dosing and Administration:

The drug should be administered 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 are usually: for intravenous administration, a single dose of 200 mg (in severe infections - 400 mg), the frequency of administration is 2 times / day.

If necessary, in / in the treatment of especially serious, life-threatening or recurrent infections (peritonitis, sepsis, infections of bones and joints) caused by Pseudomonas spp., Staphylococci or Streptococcus pneumoniae, the dose may be increased to 0.4 g with a multiplicity of administration up to 3 times a day .

The duration of treatment depends on the severity of the disease - 1-2 weeks, if necessary and more (with osteomyelitis can reach up to 2 months).

In acute uncomplicated gonorrhea, cystitis in women (before menopause) - once intravenously, 100 mg.

For the prevention of postoperative infections - for 30 - 60 minutes before the IV / 200-400 mg operation.

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.

Pulmonary form of anthrax: adults - 400 mg 2 times / day; children - 10 mg / kg body weight, I / 2 times a day (it should not exceed the maximum single dose of 400 mg / in (maximum daily dose - 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.

Impaired renal function:

With the clearance of creatinine from 31 to 60 ml / min / 1.73 m² or a plasma concentration of from 1.4 to 1.9 mg / 100 ml at a maximum dose of ciprofloxacin / introduction should be 800 mg per day.

When the creatinine clearance is 30 ml / min / 1.73 m² or less, or a blood plasma concentration from 2.0 mg / 100 ml or more at the maximum dose of ciprofloxacin / introduction should be 400 mg per day.

The infusion solution can be combined with 0.9% sodium chloride solution, Ringer's solution, 5% and 10% dextrose solution, 10% fructose solution, and also a solution containing 5% dextrose solution with 0.225 % or 0.45% solution of sodium chloride.

Side effects:

From the gastrointestinal tract: nausea, diarrhea, vomiting, abdominal pain, flatulence, anorexia, 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), 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, violation of the heart rate, lowering blood pressure, "tides" of blood to the skin of the face

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

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 musculoskeletal system: arthralgia, edema in the joint, arthritis, tendovaginitis, tendon ruptures, myalgia.

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

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

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

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

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:

Simultaneous reception of ciprofloxacin and theophylline may lead to an increase in the concentration of theophylline in the blood plasma, due to competitive inhibition in the binding sites of cytochrome P₄₅₀, which leads to an increase in the half-life of theophylline and an increased risk of toxic action associated with theophylline.

Increases the concentration and lengthens T1 / 2 oral hypoglycemic drugs, indirect anticoagulants, helps reduce the prothrombin index.

With simultaneous use of ciprofloxacin and anticoagulants, bleeding time is prolonged.

With the simultaneous use of ciprofloxacin and cyclosporine, the nephrotoxic effect of the latter is enhanced.

When combined with other antimicrobial drugs (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, etc. beta-lactam antibiotics - with streptococcal infections; with isoxazole penicillins and vancomycin - with staphylococcal infections; with metronidazole and clindamycin - with anaerobic infections.

Non-steroidal anti-inflammatory drugs (excluding acetylsalicylic acid) increase the risk of seizures.

Metoclopramide accelerates absorption, which leads to a decrease in the time to reach its C_max.

The joint administration of uricosuric medicines leads to a delay in excretion (up to 50%) and an increase in the plasma concentration of ciprofloxacin.

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

With simultaneous use with warfarin, the risk of bleeding increases.

Pharmaceutical interaction: a solution of ciprofloxacin is incompatible with solutions or drugs with pH 3-4 that are physically or chemically unstable. The infusion solution of ciprofloxacin is not compatible with solutions having 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 life 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 tendons or when the first signs of tendovaginitis appear, treatment should be discontinued due to the fact that individual cases of inflammation and even rupture of tendons during treatment with fluoroquinolones are described.

During the treatment with ciprofloxacin it is necessary to provide a sufficient amount of fluid while observing a normal diuresis.

During treatment with ciprofloxacin, contact with direct sunlight should be avoided.

It is not recommended to use ciprofloxacin in children for the treatment of other diseases, except for the treatment of complications caused by Pseudomonas aeruginosa in children with cystic fibrosis of the lung and treatment and prevention of pulmonary anthrax form (after the alleged or proven infection of Bacillus anthracis).

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

Patients receiving ciprofloxacin, caution should be exercised when driving a car and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions (especially with simultaneous use of alcohol).

Form release / dosage:

Solution for infusions 2 mg / ml.

Packaging:

100 ml in plastic bottles made of low density polyethylene. Each bottle is sealed in a plastic bag and packed in a cardboard box with instructions for use.

Storage conditions:

At a temperature of no higher than 25 ° C, in a place protected from light. Do not freeze.

Keep out of the reach of children.

Shelf life:3 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N012386 / 02

Date of registration:18.03.2008

The owner of the registration certificate:M.Biotek LimitedM.Biotek Limited United Kingdom

Manufacturer: & nbsp

MARCK BIOSCIENCES, Ltd. India

Representation: & nbspSharan Pharma, LLCSharan Pharma, LLC

Information update date: & nbsp20.10.2015

Illustrated instructions

Instructions

Ciprofloxacin (Ciprofloxacin)