

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 ciprofloxacin, there is no parallel development of resistance to other antibiotics that do not belong to the group of inhibitors of gyrase, which makes it highly effective against bacteria that are resistant, for example, to aminoglycosides, penicillins, cephalosporins, tetracyclines and many other antibiotics. By ciprofloxacin 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 dipththeria; 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 ciprofloxacin. 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. Ineffective against Treponema pallidum. Resistance develops extremely slowly, because, on the one hand, after the action of ciprofloxacin, there are practically no persistent microorganisms left, and on the other, bacterial cells do not have enzymes that inactivate it. Mechanisms of development of resistance The development of resistance to fluoroquinolones, in particular to ciprofloxacin, is mediated by changes in the genes encoding at least one of the following 4 mechanisms: 1. changes in the structure of target enzymes (DNA gyrase and topoisomerase IV) - enzymes involved in the synthesis Cell DNA; 2. violation of the permeability of the cell wall; 3. active removal of the drug from the cell (increased activity of efflux pumps); 4. plasmid-mediated changes in the work of aminoglycoside 6-N-acetyltransferase.
In ophthalmology: treatment of corneal ulcers and infections of the anterior segment of the eyeball and its appendages caused by bacteria sensitive to ciprofloxacin in adults, newborns (from 0 to 27 days), infants and babies (from 28 days to 23 months), children (from 2 up to 11 years old) and teenagers (from 12 to 18 years old). In otolaryngology: otitis externa, treatment of postoperative infectious complications.
1 ml of the preparation contains: active substance: 0009 Ciprofloxacin 3.0 mg (as ciprofloxacin hydrochloride monohydrate) –3.49 mg excipients: 0009 Mannitol– 44.0 mg Sodium acetate trihydrate – 0.68 mg Disodium edetate dihydrate (Trilon B) - 0.50 mg Benzalkonium chloride - 0.10 mg Glacial acetic acid - to a pH of 3.5-5.5 Water for injection - to 1.0 ml
Ciprofloxacin is marketed under different brands and generic names, and comes in different dosage forms:
Brand name | Manufacturer | Country | Dosage form |
---|---|---|---|
Ciprofloxacin-SOLOpharm | Grotex Ltd | Russia | eye drops |
Ciprolet® | Dr. Reddy`s | India | eye drops |
Ciprofloxacin | PFK Obnovlenie | Russia | eye drops |
Ciprofloxacin pills | Lance farm | Russia | pills |
Ciprofloxacin | Synthesis AKOMP | Russia | vials |
Ciprofloxacin pills | Ozon | Russia | pills |
Oftocipro® | Tatkhimpharmpreparaty | Russia | ointment |
Ciprofloxacin Drops | Synthesis AKOMP | Russia | eye drops |
Cypromed | Sentiss Pharma | India | eye drops |
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The dose of Ciprofloxacin depends on the severity of the disease, the type of infection, the condition of the body, the age, weight and kidney function of the patient. Usually recommended doses: Ciprofloxacin in the dosage form of pills 250 mg and 500 mg for oral administration:
When urinary tract infections take the drug Ciprofloxacin 0.125-0.5 g 2 times a day, in more severe cases, up to 0.75 g 2 times a day. The course of treatment is usually 5 to 15 days.
Diseases of the lower respiratory tract of moderate severity - 250 mg, and in more severe cases, 500 mg, 2 times a day;
For the treatment of gonorrhea, a single dose of Ciprofloxacin at a dose of 250-500 mg is recommended;
Gynecological diseases, enteritis and colitis with severe and high temperature, prostatitis, osteomyelitis - 500 mg 2 times a day (for the treatment of banal diarrhea, you can use a dose of 250 mg 2 times a day).
The drug should be taken on an empty stomach, drinking plenty of liquids. Patients with severe impaired renal function should be given a half dose of the drug. The duration of treatment depends on the severity of the disease, but treatment should always continue for at least another two days after the disappearance of the symptoms of the disease. Usually the duration of treatment is 7-10 days.
On the part of the digestive system: nausea, diarrhea, vomiting, abdominal pain, flatulence, anorexia, cholestatic jaundice (especially in patients with past liver diseases), hepatitis, hepatonecrosis.
CNS and peripheral nervous system: dizziness, headache, fatigue, anxiety, tremor, insomnia, “nightmarish” dreams, peripheral paralgesia (anomaly of pain), sweating, increased intracranial pressure, anxiety, confusion, depression, hallucinations , manifestations of psychotic reactions (sometimes progressing to states in which the patient may harm himself), migraine, syncope, cerebral artery thrombosis.
On the part of the senses: impaired taste and smell, visual impairment (diplopia, change in color perception), tinnitus, hearing loss.
Since the cardiovascular system: tachycardia, cardiac arrhythmias, lower blood pressure, rush of blood to the skin of the face.
On the part of the hematopoietic system: leukopenia, granulocytopenia, anemia, thrombocytopenia, leukocytosis, thrombocytosis, hemolytic anemia.
From the laboratory parameters: hypoprothrombinemia, increased activity of hepatic transaminases and alkaline phosphatase, hypercreatininemia, hyperbilirubinemia, hyperglycemia.
On the part of the urinary system: hematuria, crystalluria (especially with alkaline urine and low diuresis), glomerulonephritis, dysuria, polyuria, urinary retention, albuminuria, urethral bleeding, hematuria, reduced nitrogen-releasing kidney function, interstitial nephritis.
On the part of the musculoskeletal system: arthralgia, arthritis, tendovaginitis, tendon ruptures, myalgia.
Allergic reactions: itching, hives, blisters, accompanied by bleeding, papules forming scabs, drug fever, petechial hemorrhages (petechiae), swelling of the face or throat, shortness of breath, eosinophilia, increased sensitivity, vasculitis, nodular erythema, exudative erythema multiforme syndrome Stevens-Johnson, toxic epidermal necrolysis (Lyell's syndrome).
Others: arthralgia, arthritis, tendovaginitis, tendon ruptures, general weakness, myalgia, superinfection (candidiasis, pseudomembranous colitis), pain and burning at the injection site, phlebitis.
WITHcaution the drug should be prescribed for severe cerebral atherosclerosis, cerebral circulation disorders, mental illness, convulsive syndrome, epilepsy, severe renal and / or hepatic insufficiency, and elderly patients.
Due to a decrease in the activity of microsomal oxidation processes in hepatocytes, ciprofloxacin increases the concentration and lengthens the half-life of theophylline and other xanthines (eg, caffeine), oral hypoglycemic drugs, indirect anticoagulants, and contributes to a decrease in the prothrombin index.
With simultaneous use with NSAIDs (with the exception of acetylsalicylic acid) increases the risk of seizures.
Metoclopramide accelerates the absorption of ciprofloxacin, which reduces the time to reach the maximum concentration of the latter.
Co-administration of uricosuric drugs leads to a slower elimination (up to 50%) and an increase in the plasma concentration of ciprofloxacin.
When combined with other antimicrobial agents (beta-lactam antibiotics, aminoglycosides, clindamycin, metronidazole), synergism is usually observed. Therefore, Ciprofloxacin can be successfully used in combination with azlocillin and ceftazidime for 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.
Ciprofloxacin enhances the nephrotoxic effect of cyclosporine, an increase in serum creatinine is also noted, so these patients need to be monitored 2 times a week.
When taken simultaneously, Ciprofloxacin enhances the effect of indirect anticoagulants.
Ciprofloxacin is contraindicated for use during pregnancy and lactation (breastfeeding).
If severe and prolonged diarrhea occurs during or after treatment with Ciprofloxacin, diagnosis of pseudomembranous colitis should be excluded, which requires immediate discontinuation of the drug and appropriate treatment.
During the period of treatment with Ciprofloxacin, it is necessary to provide a sufficient amount of fluid while observing normal diuresis.
During treatment with Ciprofloxacin, avoid contact with direct sunlight.
Patients with epilepsy, bouts of convulsions in history, vascular diseases and organic brain damage due to the threat of adverse reactions from the CNS Ciprofloxacin should be appointed only for health reasons.
If severe and prolonged diarrhea occurs during or after treatment with Ciprofloxacin, diagnosis of pseudomembranous colitis should be excluded, which requires immediate discontinuation of the drug and appropriate treatment.
In the event of pain in the tendons or the appearance of the first signs of tendovaginitis, treatment should be discontinued due to the fact that isolated cases of inflammation and even tendon rupture during treatment with fluoroquinolones are described.
Influence on ability to drive motor transport and control mechanisms
Patients taking Ciprofloxacin, should be careful when driving a car and doing other potentially hazardous activities that require increased attention and quickness of psychomotor reactions (especially while drinking alcohol).
Treatment: the specific antidote is unknown. It is necessary to carefully monitor the condition of the patient, make a gastric lavage, carry out the usual 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.