Ципрофлоксабол®
Producer: LLC ABOLMED Russia
Code of automatic telephone exchange: J01MA02
Release form: Liquid dosage forms. Solution for infusions.
General characteristics. Structure:
Active ingredient: 2 mg of ciprofloxacin on 1 ml of solution.
Excipients: sodium chloride of 0,9%.
Antimicrobic drug of group of ftorkhinolon 2 generations with a broad spectrum of activity against bacteria, including resistant to aminoglycosides, penicillin, cephalosporins, tetracyclines and many other antibiotics
Pharmacological properties:
Pharmacodynamics. The antimicrobic broad-spectrum agent derivative of a ftorkhinolon, suppresses bacterial DNK-girazu (the topoisomerases II and IV responsible for process of superspiralling of chromosomal DNA around nuclear RNA that is necessary for reading of genetic information), breaks DNA synthesis, growth and division of bacteria; causes the expressed morphological changes (including a cell wall and membranes) and bystry death of a bacterial cell.
Affects bakteritsidno gram-negative organisms during a dormant period and divisions (since influences not only on DNK-girazu, but also causes a lysis of a cell wall), on gram-positive microorganisms - only during division. The hypotoxicity for cells of a macroorganism is explained by absence in them DNK-girazy. Against the background of reception of ciprofloxacin there is no parallel development of resistance to other aktibiotika which are not belonging to group of inhibitors of a giraza that does it highly effective in relation to bacteria which are steady, for example, against aminoglycosides, penicillin, cephalosporins, tetracyclines and many other antibiotics.
Gram-negative aerobic bacteria are sensitive to ciprofloxacin: enterobakteriya (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 activators - Legionella pneumophila, Brucella spp., Chlamydia trachomatis, Listeria monocytogenes, Mycobacterium tuberculosis, Mycobacterium kansasii, Corynebacterium diphtheriae; gram-positive aerobic bacteria: Staphylococcus spp. (Staphylococcus aureus, Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus saprophyticus), Streptococcus spp. (Streptococcus pyogenes, Streptococcus agalactiae).
The majority of the stafilokokk steady against Methicillinum, rezistentna and to ciprofloxacin.
Sensitivity of Streptococcus pneumoniae, Enterococcus faecalis, Mycobacterium avium (located intracellularly) - moderated (for their suppression high concentration are required). To rezistentna drug: Bacteroides fragilis, Pseudomonas cepacia, Pseudomonas maltophilia, Ureaplasma urealyticum, Clostridium difficile, No-cardia asteroides.
He is effective concerning Treponema pallidum.
Resistance develops extremely slowly as, on the one hand, after effect of ciprofloxacin there is practically no persistent microorganism left, and with other - bacterial cells have no enzymes inactivating it.
Pharmacokinetics. At oral administration it is quickly and rather fully soaked up from a GIT (preferential in 12-perstny and a jejunum).
Meal slows down absorption, but does not change Cmax and bioavailability. Bioavailability - 50-85%, distribution volume - 2-3.5 l/kg, communication with proteins of plasma - 20-40%. TCmax at oral administration - 60-90 min., Cmax linearly depends on the size of the accepted dose and makes at doses 250, 500, 750 both 1000 mg respectively 1.2, 2.4, 4.3 and 5.4 mkg/ml. In 12 h after intake of 250, 500 and 750 mg concentration of drug in plasma decreases to 0.1, 0.2 and 0.4 mkg/ml respectively. Later in/in infusions of 200 mg or 400 mg of TCmax - 60 min., Cmax - 2.1 mkg/ml and 4.6 mkg/ml respectively. Distribution volume - 2-3 l/kg.
It is well distributed in body tissues (excepting the fabric rich with fats, for example, nervous tissue). Concentration in fabrics is 2-12 times higher, than in plasma. Therapeutic concentration are reached in saliva, almonds, a liver, a gall bladder, bile, intestines, abdominal organs and a small pelvis, a uterus, semen, prostate tissue, an endometria, fallopian pipes and ovaries, kidneys and urinary bodies, pulmonary fabric, a bronchial secret, a bone tissue, muscles, synovial fluid and joint cartilages, peritoneal liquid, skin.
Gets into SMZh in a small amount where its concentration in the absence of an inflammation of a meninx makes 6-10% of that in blood serum, and at inflamed - 14-37%.
Ciprofloxacin well gets also into eye liquid, a bronchial secret, a pleura, a peritoneum, a lymph, through a placenta. Concentration of ciprofloxacin in neutrophils of blood is 2-7 times higher, than in blood serum. Activity decreases at values рН less than 6 a little.
It is metabolized in a liver (15-30%) with formation of low-active metabolites (diethylciprofloxacin, sulfociprofloxacin, oxociprofloxacin, formylciprofloxacin). T1/2 is about 4 h at a peroral way introduction and 5-6 h - at in/in, at HPN - to 12 h.
It is removed generally by kidneys by canalicular filtering and canalicular secretion in not changed look (at intake - 40-50%, at in/in introductions - 50-70%) and in the form of metabolites (at intake - 15%, at in introduction - 10%), other part - through a GIT. A small amount is removed with breast milk. Later in/in introductions concentration in urine during the first 2 h after introduction almost in 100 times more, than in blood serum that considerably surpasses MPK for the majority of causative agents of infections of urinary tract. Renal clearance - 3-5 ml/min.; the general clearance - 8-10 ml/min.
At HPN (KK is higher than 20 ml/min.) the percent of the drug removed through kidneys decreases, but cumulation in an organism does not happen owing to compensatory increase in metabolism of drug and removal with fecal masses. Patients with a heavy renal failure (KK is lower than 20 ml/min. / 1.73 of sq.m) need to appoint 1/2 daily doses.
Indications to use:
The bacterial infections caused by sensitive microorganisms: respiratory diseases - acute and chronic (in an aggravation stage) bronchitis, pneumonia, a bronchoectatic disease, a mucoviscidosis; infections of ENT organs - average otitis, antritis, a frontal sinusitis, sinusitis, a mastoiditis, tonsillitis, pharyngitis; infections of kidneys and urinary tract - cystitis, pyelonephritis; infections of bodies of a small pelvis and generative organs - prostatitis, an adnexitis, a salpingitis, an oophoritis, an endometritis, tubular abscess, a pelviperitonitis, gonorrhea, a venereal ulcer, clamidiosis; infections of an abdominal cavity - bacterial infections of a GIT, bilious ways, peritonitis, intraperitoneal abscesses, salmonellosis, a typhoid, a campilobacteriosis, иерсиниоз, a shigellosis, cholera; infections of skin and soft tissues - the infected ulcers, wounds, burns, abscesses, phlegmon; bones and joints - osteomyelitis, septic arthritis; sepsis; infections against the background of the immunodeficiency (arising at treatment in immunodepressive HP or at patients with a neutropenia); prevention of infections at surgical interventions.
Route of administration and doses:
Infusion solution of the drug Tsiprofloksabol® is entered in/in kapelno; duration of infusion makes 30 min. at a dose of 200 mg and 60 min. - at a dose of 400 mg. Usual therapeutic dosages for adult patients with normal function of kidneys make 200-400 mg 2 times a day. At heavy and life-threatening infections of an infection enter 400 mg 3 times a day.
At patients with a chronic renal failure and the clearance of creatinine (CC) of 31-60 ml/min. / 1.73 sq.m of a body surface or serumal concentration of creatinine from 1.4 to 1.9 mg / 100 ml the maximum daily dose of the drug Ципрофлоксабол® 800 of mg. At KK it is lower than 30 ml/min. / 1.73 of sq.m or serumal concentration of creatinine higher than 2 mg / 100 ml the maximum daily dose - 400 mg. At the patients who are on a hemodialysis, ciprofloxacin is entered after the hemodialysis session.
Important notes: Infusion solutions of the drug Tsiprofloksabol® can be mixed from 0.9% chloride sodium solution, Ringer's solution and Ringer-laktata, 5% solution of a dextrose, 10% solution of a dextrose, 10% fructose solution, and also the aqueous solution containing 5% of a dextrose and 0.225 or 0.45% of sodium of chloride. As infusion solution of the drug Tsiprofloksabol® is sensitive to light influence, the bottle should be taken from packaging just before use.
Features of use:
At simultaneous in administration of ciprofloxacin and HP constant control of ChSS, the ABP, an ECG is necessary for the general anesthesia from group of derivatives of barbituric acid.
In order to avoid development of a crystalluria exceeding of the recommended daily dose is inadmissible, also sufficient consumption of liquid and maintenance of acid reaction of urine is necessary.
During treatment it is necessary to abstain from occupations potentially dangerous types of activity requiring special attention and speed of mental and motor reactions.
The patient with epilepsy, attacks of spasms in the anamnesis, vascular diseases and organic lesions of a brain, in connection with threat of development of side reactions from TsNS, it is necessary to appoint ciprofloxacin only according to "vital" indications.
At emergence in time or after treatment of heavy and long diarrhea it is necessary to exclude the diagnosis of pseudomembranous colitis which demands immediate drug withdrawal and purpose of the corresponding treatment.
At emergence of pains in sinews or at emergence of the first symptoms of a tendovaginitis treatment should be stopped (separate cases of an inflammation and even a rupture of sinews are described during treatment of a ftorkhinolonama).
During treatment it is necessary to avoid contact with direct sunshine
Ciprofloxacin gets through a placental barrier, is emitted with breast milk.
In pilot studies it is established that it causes an arthropathy.
Side effects:
From the alimentary system: nausea, diarrhea, vomiting, an abdominal pain, a meteorism, a loss of appetite, cholestatic jaundice (especially at patients with the postponed liver diseases), hepatitis, ge-patonekroz.
From a nervous system: dizziness, a headache, increased fatigue, uneasiness, a tremor, sleeplessness, "dreadful" dreams, a peripheral paralgeziya (anomaly of perception of feeling of pain), the increased sweating, increase in intracranial pressure, confusion of consciousness, a depression, hallucinations, and also other manifestations of the psychotic reactions (which are occasionally progressing to states in which the patient can do himself harm), migraine, unconscious states, thrombosis of cerebral arteries.
From sense bodys: disturbances of taste and sense of smell, vision disorder (diplopia, change of color perception), sonitus, decrease in hearing.
From CCC: tachycardia, disturbances of a cordial rhythm, decrease in the ABP.
From the hemopoietic system: leukopenia, granulocytopenia, anemia, thrombocytopenia, leukocytosis, thrombocytosis, hemolitic anemia. From laboratory indicators: prothrombinopenia, increase in activity of "hepatic" transaminases and ShchF, giperkreatininemiya, hyperbilirubinemia, hyperglycemia.
From an urinary system: a hamaturia, a crystalluria (first of all at alkalinuria and a hypouresis), a glomerulonephritis, a dysuria, a polyuria, an ischuria, an albuminuria, urethral bleedings, a hamaturia, decrease in azotvydelitelny function of kidneys, intersticial nephrite.
Allergic reactions: a skin itch, a small tortoiseshell, blistering, followed by bleedings, and emergence of the small small knots forming crusts, medicinal fever, dot hemorrhages on skin (petechia), a face edema or throats, an asthma, an eosinophilia, the raised photosensitivity, a vasculitis, a nodal erythema, a multiformny exudative erythema (including Stephens-Johnson's syndrome), a toxic epidermal necrolysis (Lyell's disease).
Others: an arthralgia, arthritis, a tendovaginitis, ruptures of sinews, an adynamy, a mialgiya, superinfections (candidiasis, pseudomembranous colitis), "inflows" of blood to the person.
Interaction with other medicines:
Owing to decrease of the activity of processes of a microsomal oxidation in hepatocytes increases concentration and extends theophylline T1/2 (etc. xanthines, for example, caffeine), peroral hypoglycemic HP, indirect anticoagulants, promotes decrease in a prothrombin ratio.
At a combination to other antimicrobic HP (beta лактамные antibiotics, aminoglycosides, clindamycin, metronidazole) a synergism is usually observed; it can successfully be applied in a combination with azlotsilliny and a ceftazidime at the infections caused by Pseudomonas spp.; with mezlotsilliny, azlotsilliny, etc. beta лактамными antibiotics - at streptococcal infections; with izoksazolpenitsillina and Vancomycinum - at staphylococcal infections; with metronidazole and clindamycin - at mephitic gangrenes.
Strengthens nephrotoxic effect of cyclosporine, increase in serumal creatinine is noted, at such patients control of this indicator 2 times a week is necessary.
At a concomitant use strengthens effect of indirect anticoagulants.
Oral administration together with Fe in the containing HP, sukralfaty and the antiacid HP containing Mg2+ of Ca2 + and Al3+, leads to decrease in absorption of ciprofloxacin therefore it is necessary to appoint it for 1-2 h to or in 4 h after reception of the above-stated HP.
NPVP (excepting ASK) increase risk of development of spasms.
Didanozin reduces absorption of ciprofloxacin owing to formation of complexes with it with Al3 which are contained in the didanozena + and Mg2+.
Metoclopramidum accelerates absorption that leads to reduction of time of achievement of its Cmax.
Joint purpose of uricosuric HP leads to removal delay (up to 50%) and increase in plasma concentration of ciprofloxacin.
Infusion solution pharmaceutical is incompatible with all infusion solutions and HP which physical and chemically are unstable at acid medium (рН infusion solution of ciprofloxacin - 3.9-4.5).
It is impossible to mix solution for intravenous administration with the solutions having рН more than 7.
Contraindications:
Hypersensitivity, concomitant use with tizanidiny (risk of the expressed decrease in the ABP, drowsiness), children's age (up to 18 years - before completion of process of formation of a skeleton, except therapy of the complications caused by Pseudomonas aeruginosa in children with a mucoviscidosis of easy from 5 to 17 years; prevention and treatment of a pulmonary form of a malignant anthrax), pregnancy, period laktatsii.s care. The expressed atherosclerosis of vessels of a brain, disturbance of cerebral circulation, mental diseases, epilepsy, the expressed renal and/or liver failure, advanced age.
Overdose:
Treatment: the specific antidote is unknown. It is necessary to control carefully a condition of the patient, to carry out a gastric lavage, etc. measures of acute management, to provide sufficient intake of liquid.
By means of haemo - or peritoneal dialysis the amount of drug can be removed only insignificant (less than 10%).
Storage conditions:
List B. In the place protected from light at a temperature not вышк 25 градусок Celsius. To protect from children!
Issue conditions:
According to the recipe
Packaging:
Solution for infusions on 100 ml in glass bottles. On 1 bottle (bottle) in cardboard packaging.
