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

Ciprofloxacin is a synthetic antimicrobial agent of a broad spectrum of action of a group of fluoroquinolones. The main mechanism of action is the suppression of the bacterial DNA-gyrase enzyme, as a result of which the replication of deoxyribonucleic acid and the synthesis of bacterial cell proteins are violated. The drug has a bactericidal effect on gram-negative microorganisms during rest and division and on Gram-positive microorganisms during the fission period.

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). The majority of staphylococci resistant to methicillin, are resistant to ciprofloxacin.

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

The sensitivity of bacteria Streptococcus pneumoniae, Enterococcus faecalis is moderate. To a drug resistant Corynebacterium spp., Bacteroides fragilis, Pseudomonas cepacia, Pseudomonas maltophilia, Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroides. The effect of the drug against Treponema pallidum has not been adequately studied.

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 or 4.6 μg / ml.

The volume of distribution in the equilibrium state is 2.0-3.0 l / kg. Binding to plasma proteins is low. There is a high concentration of ciprofloxacin in bile, lungs, kidneys, liver, gall bladder, uterus, seminal fluid, prostate tissue, tonsils, endometrium, fallopian tubes and ovaries.The concentration of the drug in these tissues is higher than in the serum. Ciprofloxacin also penetrates well into bones, eye fluid, bronchial secretion, saliva, skin, muscles, pleura, peritoneum, lymph; through the blood-brain barrier penetrates in a small amount.

After intravenous administration, the concentration in the urine during the first two hours of intake is almost 100 times greater than in the serum,

In patients with unchanged kidney function, the elimination half-life is usually 3-5 hours. If the kidney function is impaired, the elimination half-life increases.

The main way to remove ciprofloxacin from the body is the kidney. The kidneys deduce 50-70%. 15 to 30 % is excreted through the intestine.

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:

respiratory tract;
ear, nose and throat;
kidney and urinary tract;
genital organs (gonorrhea, prostatitis, adnexitis), gynecological and postpartum infections;
The digestive system (including the mouth, teeth, jaws),gallbladder and bile ducts;
skin, mucous membranes and soft tissues;
musculoskeletal system;
prevention and treatment of pulmonary form of anthrax (infection with Bacillus anthracis).

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:

increased sensitivity to ciprofloxacin or other drugs from the group of fluoroquinolones;
pregnancy;
lactation period (breastfeeding);
children and adolescents under 18;
simultaneous reception with tizanidine (risk of pronounced decrease in blood pressure, drowsiness)

Carefully:

Severe atherosclerosis of cerebral vessels, cerebral circulation disorder, mental illness, epilepsy, epileptic syndrome, 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 treatment and prevention of pulmonary anthrax (after suspected or proven infection with Bacillus anthracis) (in children 5-17 years of age).

Dosing and Administration:

The drug is 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. For intravenous administration, a single dose of 200 mg (with severe infections of 400 mg), the frequency of administration is 2 times a day.

If desired on / in the treatment of most severe, life-threatening or recurrent infections caused by Pseudomonas spp., Staphylococci, or Streptococcus pneumoniae, the dose may be increased up to 0.4 g with a multiplicity of administration up to 3 times a day.

In acute uncomplicated gonorrhea administered intravenously once 100 mg.

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

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

Pulmonary form of anthrax: adults - 400 mg 2 times / day; children - 10 mg / kg of weight, iv twice a day. Do not exceed the maximum single dose of 400 mg IV (the 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.

With the clearance of creatinine from 31 to 60 ml / min / 1.73 m² or its concentration in blood plasma from 1.4 to 1.9 mg / 100 ml, the maximum dose of ciprofloxacin for intravenous administration should be 800 mg per day.

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

Side effects:

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

From the side of the central 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.

Co side of 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.

Co hematopoiesis side: eosinophilia, leukopenia, neutropenia, change in the number of platelets, hemolytic anemia

Co cardiovascular system: tachycardia, heart rhythm disturbances, arterial hypotension, "tides" of blood to the skin of the face.

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

Co side of laboratory indicators: increased urea concentration, creatinine, increased activity of hepatic transaminases, alkaline phosphatase, lactate dehydrogenase, bilirubin, hypoprothrombinemia.

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

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

Other: superinfection (candidiasis, pseudomembranous colitis), rarely - 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:

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; fromisoxazole 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.

Joint appointment. 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. Due to the decrease in the activity of microsomal oxidation in hepatocytes, it increases the concentration and lengthens the half-life of theophylline and other xanthines, for example, caffeine (an increased risk of toxic action associated with theophylline), oral hypoglycemic drugs, indirect anticoagulants, and decreases the prothrombin index.

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

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

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 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 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.

The infusion solution 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, 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 of solution in a bottle of low density polyethylene. Each vial is packed in a plastic bag or in a polypropylene bag and placed in a cardboard box along with instructions for use.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° 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 N012968 / 01

Date of registration:18.07.2008

The owner of the registration certificate:Ahlkon Parenteralis (India) LimitedAhlkon Parenteralis (India) Limited India

Manufacturer: & nbsp

AHLCON PARENTERALS, Limited India

Information update date: & nbsp19.10.2015

Illustrated instructions

Instructions

Ciprofloxacin (Ciprofloxacin)