Pharmacological properties ofAntimicrobial broad-spectrum fluoroquinolone derivative, inhibits bacterial DNA-gyrase (topoisomerase II and IV, responsible for the process of super-coiling and uncoiling of chromosomal DNA, which is necessary for reading the genetic information-ray), disrupts DNA synthesis, growth and division of bacteria; causes a marked morphological changes (including cell walls and membranes) and a quick destruction of the bacteria, Alno cells. Acts on gram-negative organisms bakteristaticheski during dormancy and bacterial ritsidno in the period of division (because not only affects DNA gyrase, but also causes lysis of the cell wall-tion) for Gram-positive microorganisms - only during division. Low toxicity to microorganism cells is explained by the absence of bacterial DNA gyrase type. In patients receiving ciprofloxacin is extremely slow sequential development of resistance to other aktibiotikam not belonging to the group of gyrase inhibitors, which makes it highly effective against the bacteria that are resistant, such as the aminoglycosides, penicillins, cephalosporins, tetracyclines, and many other antibiotics. For ciprofloxacin susceptible gram-negative aerobic bacteria: enterobak-Terry (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.), etc. gram-negative bacteria (Haemophilus spp., Pseudomonas aeruginosa, Moraxella catarrhalis, Aeromonas spp., Pasteurella multocida, Plesiomonas shigelloides, Campylobacter jejuni, Neisseria spp.), some intracellular -exact agents - Legionella pneumophila, Brucella spp., Chlamydia trachomatis, Listeria monocytogenes, Mycobacterium tuberculosis, Mycobacterium kansasii, Corynebacterium diphtheriae; aerobic bacteria Gram-positive: Staphylococcus spp. (Staphylococcus aureus, Staphylo-coccus haemolyticus, Staphylococcus hominis, Staphylococcus saprophyticus), Streptococcus spp. (Streptococcus pyogenes, Streptococcus agalactiae). The majority of staphylococci resistant to methicillin resistant and to tsiproflok-satsinu. Sensitivity of Streptococcus pneumoniae, Enterococcus faecalis, Mycobacterium avium (located intracellularly) - moderate (for their suppression requires high concentration). Resistant to the drug: Bacteroides fragilis, Pseudomonas cepacia, Pseudomonas maltophilia, Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroides. Not effective against Treponema pallidum. Resistance develops very slowly, because on the one hand, after the action of the Wii ciprofloxacin is virtually no persistent organisms, and the other - not obligate bacterial cell enzymes, inactivating it. PharmacokineticsQuickly and adequately absorbed from the gastrointestinal tract (predominantly in the 12 duodenal and jejunum). Eating slows the absorption but does not alter the Cmax and bioavailability. Bioavailability - 50-85%, volume of distribution - 2-3.5 L / kg, the relationship to plasma proteins - 20-40%. Tmax after oral administration - 60-90 min, Cmax is linearly dependent on the size of the dose and at doses of 250, 500, 750 and 1000 mg, respectively, 1.2, 2.4, 4.3 and 5.4 ug / ml. At 12 h after ingestion of 250, 500 and 750 mg of the drug concentration in plasma decreased to 0.1, 0.2 and 0.4 ug / ml, respectively. Well distributed in body tissues (excluding fabric, rich in fat, for example brain tissue). Concentration in the tissues in 2.12 times higher than in plasma. Therapeutic concentrations are achieved in the saliva, tonsils, liver, gallbladder, bile, intestine, abdominal and pelvic organs, uterus, seminal fluid, prostate tissue, endomet-theory, fallopian tubes and ovaries, kidneys and urinary organs, the lung tissue, bronze hialnom-secret, bone, muscle, synovial fluid and articular cartilage, peri-tonealnoy liquid skin. In the cerebrospinal fluid enters the small numbers, where its concentration in the absence of inflammation of the meninges is 6-10% of the taco-ing in the blood serum and in inflammatory diseases of the central nervous system - 14-37%. Ciprofloxacin penetrates well as in ocular fluid, bronchial secretion, pleura, peritoneum, lymph, through the placenta. The concentration of ciprofloxacin in neutrophils Cro-integer 2-7 times higher than in serum. Activity is somewhat reduced at pH less than 6. Metabolized in the liver (15-30%) with the formation of inactive metabolites (di-etiltsiprofloksatsin, sulfotsiprofloksatsin, oksotsiprofloksatsin, formiltsiprofloksatsin). T1 / 2 - about 4 hours, with chronic renal failure - up to 12 hours excreted by the kidneys of the ground by tubular filtration and tubular secretion as unchanged - 40-50% and in the form of metabolites - 15% and the rest - through the gastrointestinal -intestinal tract. Not-a lot of output in breast milk. Renal clearance - 3.5 ml / min / kg, total clearance - 8-10 ml / min / kg. In chronic renal insufficiency (creatinine clearance above 20 mL / min) of the output from the kidneys cent of the drug is reduced, but no accumulation in the body is due to a compensatory increase in drug metabolism and excretion in feces. Patients with severe renal impairment (creatinine clearance below 20 ml/min/1, 73 sq m) should be administered half the daily dose. Indications for use
Dosage and administrationInside, the 250 mg 2-3 times a day, with severe infections - 500-750 mg 2-3 times a day. With infections of the urinary tract - 250-500 mg 2 times a day treatment - 7-10 days. For uncomplicated gonorrhea - 250-500 g once, with a combination of gonococcal in-fektsii with chlamydia and mycoplasma - 750 mg every 12 hours for 7-10 days. When chancroid - 500 mg 2 times a day for several days. When carriers of meningococcus-tion in the nasopharynx - a single dose of 500 or 750 mg. In chronic carriers of Salmonella - 250 mg 4 times a course of treatment - up to 4 weeks. If necessary, dosage may be increased to 500 mg 3 times a day. In pneumonia, osteomyelitis - 750 mg 2 times a day. The duration of treatment of osteomyelitis can be up to 2 months. With infections of the gastrointestinal tract caused by Staphylococcus aureus - 750 mg every 12 hours for 7-28 days. Treatment should continue for at least 3 days in the following normalization of body temperature or the disappearance of clinical symptoms. When the glomerular filtration rate (creatinine clearance 31-60 ml/min/1, 73 m or serum concentration of creatinine from 1.4 to 1.9 mg/100 ml), the maximum daily dose - 1000 mg. When the velocity of glomerular filtration rate below 30 ml/min/1, 73 m or serum creatinine greater than 2 mg/100 ml the maximum daily dose - 500 mg. If the patient is hemodialysis or peritoneal dialysis - 250-500 mg / day, but the drug should be taken after dialysis. In severe infections (eg cystic fibrosis in recurrent, in-fektsiyah abdominal cavity, bones and joints) caused by Pseudomonas or staphylococci, acute pneumonia caused by Streptococcus pneumoniae, and chlamydial infections, urinary tract infection dosage must be increased to 750 mg every 12 hours . The tablets should be swallowed whole without chewing, with a small amount of liquid. To achieve the best bioavailability is preferable to use it on an empty stomach, 2 hours after meals. You should avoid taking antacids at the same time. Are advised to consume enough fluids. Features of the applicationIn order to avoid unacceptable excess of crystalluria the recommended dose of Su-accurate, you also need adequate fluid intake and maintenance of the reaction of acid urine. During the treatment should refrain from activities in potentially hazardous activities that require attention and speed of mental and motor responses. Patients with epilepsy, seizures seizures in history, vascular disease and organic brain disease, due to the threat of adverse reactions in the central nervous system, ciprofloxacin should be used only in situations where the expected benefit exceeds the potential risk of prmeneniya. If you experience during or after treatment of severe and prolonged diarrhea should exclude the diagnosis of pseudomembranous colitis, which calls for immediate withdrawal of St-rata and the assignment of appropriate treatment. When the pain in the tendons or the first signs of tenosynovitis treatment It should be to stop (described isolated cases of inflammation and even tendon rupture during treatment with fluoroquinolones). During treatment you should avoid contact with direct sunlight. PrecautionsSevere atherosclerosis of the brain, the cerebral krovoobra-tion, mental illness, epilepsy, epileptic syndrome, severe renal and / or hepatic failure, advanced age. Side effectPart of the digestive system: nausea, diarrhea, vomiting, abdominal pain, weather-ism, loss of appetite, cholestatic jaundice (especially in patients with previous liver disease), hepatitis, gepatonekroz. The nervous system: dizziness, headache, tired-dependence, anxiety, tremor, and very rare: insomnia, "nightmare" dreams, periph-skaya paralgeziya (anomaly perception of feelings of pain), increased sweating, increased intracranial pressure, confusion, depression, hallucinations and other manifestations of psychotic reactions (sometimes progressing to states in which the Paci-cient to cause self-harm), migraine, syncope, cerebral arterial thrombosis ry. From the senses: a very rare: a breach of taste and smell, breach of view of the (double vision, color vision changes), tinnitus, hearing loss. Cardio-vascular system: tachycardia is very rare: disorders ser-dechnogo rhythm, blood pressure reduction. With the hematopoietic system: eosinophilia, leukopenia, granulocytopenia, anemia, thrombocytopenia is very rare: leukocytosis, thrombocytosis, haemolytic anemia. From the laboratory parameters: gipoprotrombinemii, increased activity of "liver" enzymes and alkaline phosphatase, hypercreatininemia, hyperbilirubinemia, hyperglycemia. Urinary System: hematuria, crystalluria (particularly in alkaline urine and low diuresis), glomerulonephritis, dysuria, polyuria, urinary retention, al-buminuriya, urethral bleeding, hematuria, decreased azotvydelitelnoy functions in check, interstitial nephritis. Allergic reactions: itching, hives, blisters, accompanied by a bleeding-ing, and the appearance of small nodules that form scabs, drug fever, petechial hemorrhages in the skin (petechiae), swelling of the face or throat, shortness of breath, eosinophils, nofiliya, high photosensitivity, vasculitis , nodular erythema multiforme erythema ex-sudativnaya (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome). Other: arthralgia, arthritis, tendonitis, tendon ruptures (in rare cases), asthenia, myalgia, superinfection (candidiasis, pseudomembranous colitis), "tides" of blood to the face, a violation of the formation of articular cartilage (hondropatiya), teratogenic (to prove in experiments on animals). Contraindications Hypersensitivity, childhood and adolescence (18 years - to complete the process of formation of the skeleton), pregnancy, lactation, deficiency of glucose-6-phosphate dehydrogenase, pseudomembranous colitis. InteractionsDue to decreased activity of microsomal oxidation processes in hepatocytes increases the concentration and prolongs the T1 / 2 of theophylline (xanthine, and others, such as caffeine), ne-roralnyh hypoglycemic drugs, indirect anticoagulants, promotes the reduction of prothrombin exists an index. In combination with other antimicrobial drugs (beta-lactam antibiotics, aminoglycosides, clindamycin, metronidazole) is usually observed synergism, can be used successfully in combination with azlocillin and ceftazidime for infections caused by Pseudomonas spp.; With mezlotsillinom, azlocillin and other beta- lactam antibiotics, ticks - in streptococcal infections, with vancomycin and izoksazolpenitsillinami - with staphylococcal infections, metronidazole and clindamycin - In anaerobic infections-tions. Enhances the nephrotoxic effect of cyclosporine, there is an increase serum creatinine accurately, these patients should be monitored this indicator, 2 times a week. At the same time taking enhances the effect of indirect anticoagulants. Oral administration with Fe-containing drugs, Su-kralfatom and antacid drugs containing Mg2 +, Ca2 + and Al3 +, leads to a decrease in absorption of ciprofloxacin, therefore it should be administered for 1-2 hours before or 4 hours after taking the above of drugs. Nonsteroidal anti-inflammatory drugs (except acetylsalicylic ki-slot) increase the risk of seizures. Didanosine reduces the absorption of ciprofloxacin due to the formation with complexes with didanosine contained in the Al3 + and Mg2 +. Metoclopramide accelerates the absorption, which reduces the time required to reach its Cmax. Joint appointment uricosuric drugs leads to a slowing down NIJ-elimination (50%) and increased plasma concentrations of ciprofloxacin. Joint taking the drug and alcohol significantly reduces the speed of psychomotor reactions. OverdoseSymptoms: The symptoms are not specific. In several cases, this was formed timoe-toxic to the kidney parenchyma. It is recommended to monitor the function is checked. Treatment: No specific antidote is known. We must carefully monitor the patient's condition to gastric lavage and other emergency measures, ensure adequate fluid intake chit. With the help of hemo-or peritoneal dialysis can be deduced-Jet only a small (less than 10%) of the drug. Storage conditionsIn a dry, dark place at a temperature not exceeding 25 � C. Shelf life 2 years. No use after the expiration date. |