Cipro is a drug, an antibacterial drug from the group of fluoroquinolones II generation.
Buy Cipro Online is one of the most effective fluoroquinolones, it has found wide application in clinical practice, which is reflected, in particular, in a large number of names under which it is produced in different countries.
In 1983, Bayer published the results of in vitro use of cipro. Tablets for oral administration were approved in 1987. Patent Bayer expired in 2004, after which sales of cipro began to bring an average of about 200 million euros per year.
The broad-spectrum antimicrobial agent, a fluoroquinolone derivative, suppresses bacterial DNA gyrase (topoisomerases II and IV, which are responsible for the supercoiling of chromosomal DNA around nuclear RNA, which is necessary for reading genetic information), violates DNA synthesis, growth and division of bacteria; causes pronounced morphological changes (including the cell wall and membranes) and the rapid death of the bacterial cell. It acts bactericidal on Gram-negative organisms in the period of rest and division (as it affects not only the DNA gyrase, but also causes lysis of the cell wall), on gram-positive microorganisms – only in the period of division. Low toxicity to the cells of the microorganism is explained by the absence of DNA gyrase in them. While taking cipro, there is no parallel development of resistance to other antibiotics that do not belong to the group of gyrase inhibitors, which makes it highly effective against bacteria that are resistant, for example to aminoglycosides, penicillins, cephalosporins, tetracyclines, and many other antibiotics. By cipro sensitive Gram negative aerobic bacteria: Enterobacteriaceae (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, Ibrands, Ibrahns spp., Pasteurella multocida, Pastelureas, Psudomonas aeruginosa, Moraxella catarrhalis 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). Most methicillin-resistant staphylococci are resistant to cipro. The sensitivity of Streptococcus pneumoniae, Enterococcus faecalis, Mycobacterium avium (located intracellularly) is moderate (high concentrations are required to suppress them). The drug resistant: Bacteroides fragilis, Pseudomonas cepacia, Pseudomonas maltophilia, Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroides. Not effective against Treponema pallidum. Resistance develops extremely slowly, because, on the one hand, after the action of cipro, there are practically no persistent microorganisms left, and on the other, bacterial cells do not have enzymes that inactivate it.
When taken orally, it is rapidly and completely absorbed from the gastrointestinal tract (mainly in the duodenal and jejunum). Meal slows down absorption, but does not change Cmax and bioavailability. Bioavailability – 50-85%, the volume of distribution – 2-3.5 l / kg, the connection with plasma proteins – 20-40%. TCmax when taken orally – 60-90 minutes, Cmax linearly depends on the size of the dose taken and amounts to 1.2, 2.4, 4.3 and 5.4 μg / ml at doses of 250, 500, 750 and 1000 mg, respectively. 12 hours after ingestion of 250, 500 and 750 mg, the concentration of the drug in plasma decreases to 0.1, 0.2 and 0.4 μg / ml, respectively. After intravenous infusion of 200 mg or 400 mg of TCmax – 60 min, Cmax – 2.1 and 4.6 μg / ml, respectively. Distribution volume – 2-3 l / kg. It is well distributed in the tissues of the body (excluding tissue rich in fats, such as nerve tissue). The concentration in the tissues is 2-12 times higher than in plasma. Therapeutic concentrations are reached in saliva, tonsils, liver, gallbladder, bile, intestines, abdominal and pelvic organs, uterus, seminal fluid, prostate tissue, endometrium, fallopian tubes and ovaries, kidneys and urinary organs, lung tissue, bronchial secretions, bone tissue, muscles, synovial fluid and articular cartilage, peritoneal fluid, skin. In the cerebrospinal fluid penetrates in a small amount, where its concentration in the absence of inflammation of the meninges is 6-10% of that in serum, and in inflamed – 14-37%. Cipro also penetrates well into the eye fluid, bronchial secretion, pleura, peritoneum, lymph, through the placenta. The concentration of cipro in blood neutrophils is 2-7 times higher than in serum. The activity decreases slightly with pH values less than 6. Metabolized in the liver (15-30%) with the formation of low-level metabolites (diethylcyrofloxacin, sulfocyrofloxacin, oxocrofloxacin, formylcyrofloxacin). T1 / 2 – about 4 hours with oral route and 5-6 hours – with intravenous, with chronic renal failure – up to 12 hours. Mainly excreted by the kidneys by tubular filtration and tubular secretion unchanged (when taken orally – 40-50 %, with intravenous administration – 50-70%) and in the form of metabolites (when administered orally – 15%, with intravenous administration – 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 serum, which is significantly superior to BMD for most urinary tract pathogens. Renal clearance – 3-5 ml / min / kg; total clearance – 8-10 ml / min / kg. In chronic renal failure (QC above 20 ml / min), the percentage of the drug excreted through the kidneys decreases, but cumulation in the body does not occur due to a compensatory increase in drug metabolism and excretion with feces.
Bacterial infections caused by susceptible microorganisms: respiratory diseases – acute and chronic (in the acute stage) bronchitis, pneumonia, bronchiectasis, cystic fibrosis; infections of upper respiratory tract – otitis media, antritis, sinusitis, sinusitis, mastoiditis, tonsillitis, pharyngitis; infections of the kidneys and urinary tract – cystitis, pyelonephritis; infections of the pelvic organs and genital organs – prostatitis, adnexitis, salpingitis, oophoritis, endometritis, tubular abscess, pelvioperitonitis, gonorrhea, soft chancre, chlamydia; infections of the abdominal cavity – bacterial infections of the gastrointestinal tract, biliary tract, peritonitis, intraperitoneal abscesses, salmonellosis, typhoid fever, campylobacteriosis, yersiniosis, shigellosis, cholera; infections of the skin and soft tissues – infected ulcers, wounds, burns, abscesses, cellulitis; bones and joints – osteomyelitis, septic arthritis; sepsis; infections on the background of immunodeficiency (arising from the treatment of immunosuppressive drugs or in patients with neutropenia); infection prevention during surgical interventions; prevention and treatment of pulmonary anthrax. 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 anthrax (infection with Bacillus anthracis).
Dosage regimen is individual. Inside – 250-750 mg 1-2 times / day. The duration of treatment is from 7-10 days to 4 weeks.
For the on / in the introduction of a single dose – 200-400 mg, the frequency of administration – 2 times / day. ; the duration of treatment is 1-2 weeks, if necessary, and more. You can enter in / in the jet, but more preferably drip introduction within 30 minutes.
When applied topically, 1-2 drops are instilled into the lower conjunctival sac of the affected eye every 1-4 hours. After improving the condition, the intervals between instillations can be increased.
The maximum daily intake for adults when administered orally is 1.5 g.
Hypersensitivity, simultaneous use with tizanidine (risk of marked reduction of blood pressure, drowsiness), children age (up to 18 years – until the skeleton formation process is completed, except for the treatment of complications caused by Pseudomonas aeruginosa in children with cystic fibrosis of the lungs from 5 to 17 years; prevention and treatment pulmonary anthrax), pregnancy, lactation.
Severe cerebral vascular atherosclerosis, impaired cerebral circulation, mental illness, epilepsy, epileptic syndrome, severe renal and / or liver failure, old age.
With simultaneous intravenous administration of cipro and drugs for general anesthesia from the group of barbituric acid derivatives, constant monitoring of heart rate, blood pressure, electrocardiogram is necessary. In order to avoid the development of crystalluria, it is unacceptable to exceed the recommended daily dose, it is also necessary to have sufficient fluid intake and to keep the urine acidic. During treatment, you should refrain from engaging in potentially hazardous activities that require increased attention and speed of mental and motor responses. Patients with epilepsy, bouts of convulsions in history, vascular diseases and organic brain damage, due to the threat of adverse reactions from the central nervous system, cipro should be prescribed only for “vital” indications. If severe and prolonged diarrhea occurs during or after treatment, the diagnosis of pseudomembranous colitis should be excluded, which requires immediate discontinuation of the drug and appropriate treatment. If there is pain in the tendons or the first signs of tendovaginitis, treatment should be stopped (isolated cases of inflammation and even tendon rupture during the treatment with fluoroquinolones are described). During the period of treatment should avoid contact with direct sunlight.
From the digestive system
Nausea, diarrhea, vomiting, abdominal pain, flatulence, loss of appetite, cholestatic jaundice (especially in patients with previous liver diseases), hepatitis, hepatonecrosis.
The nervous system
Dizziness, headache, fatigue, anxiety, tremor, insomnia, “nightmarish” dreams, peripheral paralgesia (abnormal perception of pain), increased sweating, increased intracranial pressure, confusion, depression, hallucinations, and other manifestations of psychotic reactions (rarely progressive to conditions in which the patient may harm himself), migraine, fainting, cerebral artery thrombosis.
From the senses
Disorders of taste and smell, blurred vision (diplopia, change in color perception), tinnitus, hearing loss.
Since the cardiovascular system
Tachycardia, heart rhythm disturbances, lowering blood pressure.
From the hemopoietic system
Leukopenia, granulocytopenia, anemia, thrombocytopenia, leukocytosis, thrombocytosis, hemolytic anemia.
From the laboratory indicators
Hypoprothrombinemia, increased activity of “liver” transaminases and alkaline phosphatase, hypercreatininemia, hyperbilirubinemia, hyperglycemia.
On the part of the urinary system
Hematuria, crystalluria (primarily with alkaline urine and low diuresis), glomerulonephritis, dysuria, polyuria, urinary retention, albuminuria, urethral hemorrhage, hematuria, reduced nitrogen-excreting kidney function, interstitial nephritis.
Pruritus, urticaria, blistering, accompanied by bleeding, and the appearance of small nodules that form scabs, drug fever, punctate hemorrhages on the skin (petechiae), swelling of the face or larynx, shortness of breath, eosinophilia, increased photosensitivity, vasculitis, nodal erythema (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome).
Arthralgia, arthritis, tendovaginitis, tendon ruptures, asthenia, myalgia, superinfection (candidiasis, pseudomembranous colitis), blood flushes to the face.
Owing to a decrease in the activity of microsomal oxidation processes in hepatocytes, it increases the concentration and lengthens the T1 / 2 of theophylline (and other xanthines, such as caffeine), oral hypoglycemic drugs, and indirect anticoagulants, helps to reduce the prothrombin index. When combined with other antimicrobial drugs (beta-lactam antibiotics, aminoglycosides, clindamycin, metronidazole), synergism is usually observed; it can be successfully used in combination with azlocillin and ceftazidime in infections caused by Pseudomonas spp .; with mezlocillin, azlocillin and other beta-lactam antibiotics – for streptococcal infections; with isoxazolpenicillins and vancomycin – for staphylococcal infections; with metronidazole and clindamycin – for anaerobic infections. Enhances the nephrotoxic effect of cyclosporine, an increase in serum creatinine, there is a need in these patients to control this indicator 2 times a week. At the same time, it enhances the effect of indirect anticoagulants. Oral administration in conjunction with Fe-containing drugs, sucralfate and antacid drugs containing Mg2 +, Ca2 + and Al3 +, reduces the absorption of cipro, so it should be administered 1-2 hours before or 4 hours after taking the above medicines. NSAIDs (excluding ASA) increase the risk of seizures. Didanosine reduces the absorption of cipro due to the formation of complexes with it containing Al3 + and Mg2 + contained in didanosine. Metoclopramide accelerates absorption, which leads to a decrease in the time to reach its Cmax. Co-administration of uricosuric drugs leads to a slowdown of excretion (up to 50%) and an increase in the plasma concentration of cipro. Increases Cmax 7 times (from 4 to 21 times) and AUC 10 times (from 6 to 24 times) tizanidine, which increases the risk of marked reduction in blood pressure and drowsiness. The infusion solution is pharmaceutically incompatible with all infusion solutions and drugs that are physically and chemically unstable in an acidic environment (the pH of the cipro infusion solution is 3.9-4.5). Do not mix the solution for intravenous administration with solutions having a pH greater than 7.
The specific antidote is unknown. It is necessary to carefully monitor the patient’s condition, to wash the stomach and other emergency measures, to ensure adequate fluid intake. With the help of hemo- or peritoneal dialysis, only an insignificant (less than 10%) amount of the drug can be derived.