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. Ciprofloxacin is sensitive to gram-negative aerobic bacteria: 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. (S. aureus, S. haemolyticus, S. hominis, S.saprophyticus), Streptococcus spp. (St. pyogenes, St.agalactiae). The majority of staphylococci, resistant to methicillin, are resistant to ciprofloxacin.

Sensitivity of bacteria Streptococcus pneumoniae, Enterococcus faecalis is moderate.

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

Pharmacokinetics:

After IV infusion, 200 mg or 400 mg TCmah - 60 min, Stach - 2.1 mcg / ml and 4.6 mkg/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, 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, kidneys and urinary organs, pulmonary tissue, bronchial secretion, bone tissue, muscles, synovial fluid and articular cartilage, peritoneal fluid, skin. In CSF penetrates in a small amount, where its concentration in uninflated cerebral membranes is 6-10% of that in the blood serum, and when inflamed - 14-37%. Ciprofloxacin also well penetrates into the eye fluid, bronchial secretion, pleura, peritoneum, lymph, through the placenta. The concentration of ciprofloxacin in blood neutrophils is 2-7 times higher than in serum.

The activity decreases slightly at acidic pH values.

Metabolised in the liver (15-30%) with the formation of low-activity metabolites (diethylciprofloxacin, sulfociprofloxacin, oxociprofloxacin,

formylcycloxacin).

With iv injection of T1 / 2 - 5-6 hours, with CRI - up to 12 hours. It is mainly excreted by the kidneys by tubular filtration and tubular secretion in unchanged form (with IV introduction - 50-70%) and in the form of metabolites (with iv introduction - 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 injection is almost 100 times greater than in the serum, which is significantly superior to the MIC for most pathogens of urinary tract infections.

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

With CRF (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 with the feces.Patients with severe renal failure (CC below 20 ml / min / 1.73 m 2) should be prescribed half the daily dose.

Indications:

Infectious-inflammatory diseases caused by microorganisms sensitive to Ciprofloxacin:

- respiratory tract;

- ear, nose and throat;

- kidneys and urinary tract;

- genital organs (gonorrhea, prostatitis); gynecological (adnexitis) and postpartum infections;

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

- skin, mucous membranes and soft tissues;

- musculoskeletal system.

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, deficiency of glucose-6-phosphate dehydrogenase, pseudomembranous colitis, children's age (up to 18 years - the completion of the formation of the skeleton), pregnancy, lactation.

Carefully:

pronounced atherosclerosis of cerebral vessels, cerebral circulation disorder, mental illness, convulsive syndrome, epilepsy,severe renal and / or hepatic impairment, advanced age.

Pregnancy and lactation:contraindicated

Dosing and Administration:

Assigned intravenously.

The dose of ciprofloxacin depends on the severity of the disease, the type of infection, the condition of the body, the age, weight and function of the kidneys 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; the duration of treatment depends on the severity of the disease - 1-2 weeks, if necessary and more. It can be injected intravenously, but more preferably a drip for 30 minutes (200 mg) and 60 minutes (400 mg).

In acute gonorrhea - once intravenously, 100 mg.

For the prevention of postoperative infections - 30 - 60 minutes before the operation in / in the 200-

400 mg.

Side effects:

On the part of the digestive system: 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, anxiety, confusion, depression, hallucinations, as well as other manifestations of psychotic reactions (occasionally progressing to conditions in which the patient can harm himself) , migraine, fainting, thrombosis of the cerebral arteries.

From the senses: a violation of taste and smell, visual impairment (diplopia, change in color perception), noise in the ears, hearing loss.

On the part of the CCC: tachycardia, heart rhythm disturbances, lower blood pressure, flushes of blood to the skin of the face.

From the hematopoietic system: leukopenia, granulocytopenia, anemia,

thrombocytopenia, leukocytosis, thrombocytosis, hemolytic anemia.

From laboratory indicators: hypoprothrombinemia, increased activity of "hepatic" transaminases and alkaline phosphatase, hypercreatininemia, hyperbilirubinemia, hyperglycemia.

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

Allergic reactions: skin itching, hives, blistering,

blood flow and small nodules forming scabs, drug fever, pinpoint hemorrhages (petechiae), edema of the face or larynx, dyspnea, eosinophilia, increased photosensitivity, vasculitis, nodal erythema, exudative erythema multiforme, Stevens-Johnson syndrome (malignant exudative erythema), toxic epidermal necrolysis (Lyell's syndrome).

Other: arthralgia, arthritis, tendovaginitis, tendon ruptures, general weakness, myalgia, superinfections (candidiasis, pseudomembranous colitis), pain and burning at the injection site, phlebitis.

Overdose:

The specific antidote is unknown. It is necessary to carefully monitor the patient's condition, make gastric lavage, carry out usual emergency measures, 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 a decrease in the activity of microsomal oxidation in hepatocytes, it increases the concentration and lengthens T1 / 2 theophylline (et al.xanthines, for example, caffeine), oral hypoglycemic drugs, indirect anticoagulants, helps to reduce the prothrombin index. NSAIDs (excluding ASA) increase the risk of seizures.

Metoclopramide accelerates absorption, which leads to a decrease in the time to reach it

Stach.

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

When combined with other antimicrobial agents (beta-lactams, 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.

Increases the nephrotoxic effect of cyclosporine, there is an increase in serum creatinine, so these patients need to monitor this indicator 2 times a week.

With simultaneous reception increases the effect of indirect anticoagulants.

The infusion solution is pharmaceutically incompatible with all infusion solutions and preparations that are physico-chemically unstable in an acidic medium (pH of the infusion
ciprofloxacin solution - 3.9-4.5). Do not mix the IV solution with solutions having a pH of more than 7.

Special instructions:

If a severe and prolonged diarrhea occurs during or after treatment with ciprofloxacin, the diagnosis of pseudomembranous colitis should be ruled out, 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.

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

During treatment with ciprofloxacin, avoid direct exposure to sunlight.

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 the drug in polyethylene bottles. The bottle with instructions for use is placed in a pack of cardboard or in a bag of polyethylene film.

Storage conditions:

List B. In the dark place at a temperature of no higher than 25 ° C, protect from freezing. Keep out of the reach of children.

Shelf life:

2 years. Do not use after the time specified on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N003873 / 01

Date of registration:15.12.2009

The owner of the registration certificate:MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC Russia

Manufacturer: & nbsp

MOSHIMFARM PREPARATES them. NA Semashko OJSC Russia

Information update date: & nbsp15.12.2009

Illustrated instructions

Instructions

Ciprofloxacin (Ciprofloxacin)