Basijen - instructions for use, doses, side effects, contraindications

One bottle (100 ml) contains: active substance: ciprofloxacin 200 mg; Excipients: sodium chloride 900 mg, disodium edetate 20 mg, citric acid monohydrate 12 mg, lactic acid 70 mg, sodium hydroxide 30 mg, water for injection is.

Description:

Transparent with a yellowish shade solution.

Pharmacotherapeutic group:Antimicrobial agent, fluoroquinolone

ATX: & nbsp

J.01.M.A.02 Ciprofloxacin

Pharmacodynamics:

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 bacteriocally on gram-negative organisms in the period of rest and division (since it affects not only DNA-gyrase, but also causes lysis of the cell wall), Gram-positive microorganisms are effective only during the fission period.

Low toxicity for macroorganism cells is explained by the absence of DNA-gyrase in them. Against the background of ciprofloxacin, there is no parallel development of resistance to other antibiotics that do not belong to the group of DNA-gyrase inhibitors, which makes it highly effective against bacteria that are resistant, for example, to aminoglycosides, penicillins, cephalosporins, tetracyclines.

Ciprofloxacin is sensitive 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., 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).

It is active against Bacillus anthracis.

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).

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:

After an intravenous infusion of 200 mg, the time to reach the maximum concentration (TC_max) - 60 min, the maximum concentration (C_max) - 2.1 μg / ml, the connection with plasma proteins - 20-40%. It is well distributed in the tissues of the body. 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 (endometrium, fallopian tubes and ovaries, uterus), seminal fluid, prostate tissue, kidney and urinary organs, lung tissue, bronchial secretion, bone tissue, muscles, synovial fluid and articular cartilage, peritoneal fluid, skin. In spinal fluid penetrates in a small amount, where its concentration in the absence of inflammation-meninges is 6-10% of that in blood plasma, and when inflamed - 14-37%. Ciprofloxacin well penetrates also into the eye fluid, pleura, peritoneum, lymph, through the placenta. The concentration of ciprofloxacin in blood neutrophils is 2-7 times higher than in blood plasma.

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

The half-life (T1 / 2) is 5-6 hours, with chronic renal failure (CRF) up to 12 hours. It is excreted mainly 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. 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 blood plasma, which significantly exceeds the minimum inhibitory concentration (MIC) 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 (CC) above 20 ml / min), the percentage of the drug released through the kidneys decreases, but no cumulation occurs in the body due to a compensatory increase in the metabolism of the drug and excretion through the gastrointestinal tract.

Indications:

Bacterial infections caused by microorganisms sensitive to ciprofloxacin:

diseases of the lower respiratory tract (exacerbation of chronic bronchitis, pneumonia, bronchiectasis, infectious complications of 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;
infectious diarrhea (including campylobacteriosis, shigellosis, diarrhea "travelers");
infections of the skin and soft tissues (infected ulcers, wounds, burns, abscesses,
phlegmon);
bones and joints (osteomyelitis, septic arthritis);
septicemia;
infection against the background of immunodeficiency (arising in the treatment of immunosuppressive drugs or in patients with neutropenia);
prevention and treatment of pulmonary form of anthrax.

Prevention of infections during surgical interventions.

Children:

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 (infection with Bacillus anthracis).

Contraindications:

Hypersensitivity to ciprofloxacin, any other component of the drug or other drugs from the fluoroquinolones group, simultaneous reception with tizanidine (the risk of pronounced reduction in blood pressure, drowsiness), children and adolescents under 18 years (except for the treatment of complications caused by Pseudomonas aeruginosa in children with cystic fibrosis of the lungs 5 to 17 years, prevention and treatment of pulmonary form of anthrax), pregnancy, lactation.

Carefully:

Severe atherosclerosis of cerebral vessels, cerebral circulation disorder, mental illness, epilepsy, renal and / or hepatic insufficiency, elderly age, tendon lesion with previously treated quinolones.

Dosing and Administration:

Solution for infusion is administered intravenously drip. The duration of intravenous infusion of 200 mg (100 ml infusion solution) should be at least 30 minutes.

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

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.

For the prevention of infections during surgical interventions - 200-400 mg for 0.5-1 h before surgery; When the duration of the operation is more than 4 hours, re-enter in the same dose.

In other infections (depending on the severity of the flow) - 200-400 mg 2 times a day. 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.

Application in patients with chronic renal failure:

At a glomerular filtration rate (CK 31-60 ml / min / 1.73 m2 or plasma 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 plasma 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.

With peritoneal dialysis, the infusion solution is added to dialysate (intraperitoneally) at a dose of 50 mg per liter of dialysate 4 times a day (every 6 hours).

Average course 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 whole period of the neutropenic phase - in patients with weakened protective forces of the body, but no 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 should be carried out at least 3 days after the normalization of body temperature or the disappearance of clinical symptoms.

After intravenous administration, you can continue treatment orally.

Side effects:

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

From the nervous system: dizziness, headache, fatigue, anxiety, tremor, insomnia, nightmarish dreams, peripheral paralysis (anomaly of perception of pain), 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 hematopoiesis: leukopenia, granulocytopenia, anemia, thrombocytopenia, leukocytosis, thrombocytosis, hemolytic anemia.

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

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

Allergic reactions: 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, erythema nodosum, multiforme exudative erythema Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome).

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

Local reactions: phlebitis, tenderness at the injection site.

Other: asthenia, superinfection (candidiasis, pseudomembranous colitis), increased sweating, "hot flashes" of blood to the face, increased photosensitivity.

Overdose:

Treatment: the specific antidote is unknown. It is necessary to carefully monitor the patient's condition, to carry out other emergency measures, to ensure sufficient supply of fluid. 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 lengthens the half-life of theophylline and other xanthines (eg, caffeine), oral hypoglycemic drugs, indirect anticoagulants (increased action), and decreases the prothrombin index.

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 and other beta-lactam antibiotics - with streptococcal infections; with isoxazolylpenicillins and vancomycin - with staphylococcal infections; with metronidazole and clindamycin - with anaerobic infections.

Increases the nephrotoxic effect of cyclosporine, there is an increase in the serum creatinine concentration, in such patients monitoring of this indicator is required 2 times a week.

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

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 C_max 7 times (from 4 to 21 times) and the area under the concentration-time curve (AUC) is 10 times (6 to 24 times) of tizanidine, which increases the risk of pronounced reduction in blood pressure and drowsiness.

The infusion solution is pharmaceutically incompatible with all infusion solutions and drugs that are physico-chemically unstable under acidic conditions (the pH of the infusion solution of ciprofloxacin is 3.5-4.6).Do not mix the intravenous solution with solutions that have a pH of more than 7.

Special instructions:

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

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

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.

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

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

During the treatment should avoid contact with direct sunlight, artificial UV-irradiation.

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

Patients receiving ciprofloxacin, you should refrain from driving a car and taking other potentially dangerous activities that require increased attention and speed of psychomotor reactions.

Form release / dosage:

Solution for infusions 2 mg / ml.

Packaging:For 100 ml of solution in a vial of polyethylene, closed with a lid. Each vial is wrapped with a polypropylene BOPP film. 1 bottle with instructions for use in a cardboard pack.

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 expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-000035

Date of registration:12.11.2010

The owner of the registration certificate:Clarice Otsuka Private LimitedClarice Otsuka Private Limited India

Manufacturer: & nbsp

Clarice Otsuka Private Limited India

Representation: & nbspClarice Otsuka Private Limited Clarice Otsuka Private Limited India

Information update date: & nbsp20.10.2015

Illustrated instructions

Instructions

Basijen (Basidjen)