Throughout his life, a person often encounters the negative effects of microbes on the body. Bacterial pathogens can settle on the skin, in the gastrointestinal tract, in the genitourinary organs and even on the conjunctiva of the eye. In such a situation, only a strong antibacterial agent will help cope with the infection. Most often, treatment begins with medications based on ciprofloxacin, so doctors often prescribe the antibiotic Tsiprolet to patients. Next we will talk about the beneficial properties of this medication.
Release form
Tsiprolet is produced by many pharmaceutical companies, as it is one of the most popular antibacterial agents. It is produced in the following dosage forms:
- infusion solution - in polyethylene bottles of 100 ml, where the content of ciprofloxacin does not exceed 2 mg per ml;
- tablets - each containing 250 mg or 500 mg of the main active ingredient, they are packaged in blisters of 10 pieces;
- eye drops - sold in bottles with a dropper of 5-10 ml, which contain 3 mg of ciprofloxacin per 1 ml of solution.
According to the instructions for use of Tsiprolet 500, these tablets contain the maximum dose of the active substance. They are used to treat severe bacterial lesions in advanced infections.
Tsiprolet 500 mg No. 10 tablet p.o.
Instructions for medical use of the drug Ciprolet® Trade name Ciprolet® International nonproprietary name Ciprofloxacin Dosage form Film-coated tablets, 250 mg, 500 mg Composition One tablet contains the active substance - ciprofloxacin 250 mg or 500 mg, excipients: corn starch, microcrystalline cellulose , croscarmellose sodium, colloidal silicon dioxide, purified talc, magnesium stearate, shell composition: hypromellose, sorbic acid, titanium dioxide, purified talc, macrogol (6000), polysorbate 80, dimethicone. Description White film-coated tablets, round, biconvex and smooth on both sides, height (4.10 ± 0.20) mm and diameter (11.30 ± 0.20) mm (for a dosage of 250 mg) or height (5.50 ± 0.20) mm and diameter (12.60 ± 0.20) mm (for a dosage of 500 mg). Pharmacotherapeutic group Antibacterial drugs for systemic use. Antimicrobial drugs are quinolone derivatives. Fluoroquinolones. Ciprofloxacin. ATC code J01MA02 Pharmacological properties Pharmacokinetics Rapidly absorbed from the gastrointestinal tract. Bioavailability after oral administration is 70%. Food intake has little effect on the absorption of ciprofloxacin. The plasma concentration profile of ciprofloxacin after oral administration is similar to that for intravenous administration, so the oral and intravenous routes of administration can be considered interchangeable. Communication with plasma proteins is 20 - 40%. The average half-life of ciprofloxacin is 6 to 8 hours after a single or multiple dose. Ciprofloxacin penetrates well into organs and tissues: lungs, bronchial mucosa and sputum; organs of the genitourinary system, including the prostate gland; bone tissue, cerebrospinal fluid, polymorphonuclear leukocytes, alveolar macrophages. Excreted primarily in urine and bile. Pharmacodynamics Tsiprolet® is a broad-spectrum antibiotic from the group of fluoroquinolones. Suppresses bacterial DNA gyrase (topoimerases II and IV, responsible for the process of supercoiling of chromosomal DNA around nuclear RNA, which is necessary for reading genetic information), disrupts DNA synthesis, growth and division of bacteria; causes pronounced morphological changes (including cell wall and membranes) and rapid death of the bacterial cell. It acts bacteriostatically on gram-negative microorganisms during the dormant period and bactericidally during the division period (since it affects not only DNA gyrase, but also causes lysis of the cell wall), on gram-positive microorganisms it is bactericidal only during the division period. Low toxicity for the cells of the macroorganism is explained by the absence of DNA gyrase in them. Tsiprolet® is active against most strains of microorganisms in vitro and in vivo: - aerobic gram-positive microorganisms: Corynebacterium diphtheriae, Enterococcus faecalis, Listeria monocytogenes, Staphylococcus spp., including Staphylococcus aureus, epidermidis, Streptococcus pyogenes, agalactiae, pneumoniae, Streptococcus (group C, G), Viridans group streptococci; — aerobic gram-negative microorganisms: Acinetobacter spp., including Acinetobacter anitratus, baumannii, calcoaceticus, Actinobacillus actinomycetemcomitans, Bordetella pertussis, Citrobacter freundii, diversus, Enterobacter spp., including Enterobacter aerogenes, agglomerans, cloacae, sakazakii, Escherichia coli, Gardnerella vaginalis, Ha emophilus ducreyi , influenzae, Haemophilus parainfluenzae, Helicobacter pylori, Klebsiella spp., including Klebsiella oxytoca, pneumoniae, Moraxella catarrhalis, Morganella morganii, Neisseria gonorrhoeae, Neisseria meningitides, including Pasteurella canis, dagmatis, multocida, Proteus mirabilis, vulgaris, Providencia spp., including Pseudom onas aeruginoza, fluorescens, Salmonella spp., Serratia spp., including Serratia marcescens; — anaerobic microorganisms: Bifidobacterium spp., Clostridium perfringens, Fusobacterium spp., Peptostreptococcus, Propionibacterium spp., Veillonella spp.; — intracellular microorganisms: Streptococcus pneumoniae, Enterococcus faecalis, Chlamydia pneumoniae, psittaci, trachomatis, Legionella spp., including Legionella pneumophila, Mycobacterium spp., including Mycobacterium leprae, tuberculosis, Mycoplasma pneumoniae; Rickettsia spp., Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroids, Bacteroides fragilis, Pseudomonas cepatica, Pseudomonas maltophilia, Treponema pallidum are resistant to the drug Ciprolet® Indications for use Uncomplicated and complicated infections caused by microorganisms sensitive to ciprofloxacin: Adults - infections ENT organs ( otitis media, sinusitis, frontal sinusitis, mastoiditis, tonsillitis) - lower respiratory tract infections caused by gram-negative bacteria caused by Klebsiella spp., Enterobacter spp., Proteus spp., Esherichia coli, Pseudomonas spp., Haemophilus spp., Branhamella spp., Legionella spp. ., Staphylococcus spp. (exacerbation of chronic obstructive pulmonary disease, bronchopulmonary infection in cystic fibrosis or bronchiectasis, pneumonia) - urinary tract infections (caused by gonococcus urethritis and cervicitis) - sexually transmitted infections that were caused by Neisseria gonorrhoeae (gonorrhea, chancroid, urogenital chlamydia) - epidymitis-orchitis, including cases caused by Neisseria gonorrhoeae. - inflammation of the pelvic organs in women (pelvic inflammatory disease), including cases caused by Neisseria gonorrhoeae - infections of the abdominal cavity (bacterial infections of the gastrointestinal tract or biliary tract, peritonitis) - infections of the skin, soft tissues - septicemia, bacteremia, infections or prevention of infections in patients immunocompromised patients (eg, patients taking immunosuppressants or those with neuropenia) - prevention and treatment of pulmonary anthrax (Bacillus anthracis infection) - bone and joint infections Children and adolescents - in the treatment of complications caused by Pseudomonas aeruginosa in children over 6 years with cystic fibrosis - complex urinary tract infections and pyeloniphritis - prevention and treatment of pulmonary anthrax (infection with Bacillus anthracis) Method of administration and dosage Tsiprolet® tablets are prescribed to adults orally, before meals or in between meals, without chewing, with a sufficient amount of liquids. When taken on an empty stomach, the active substance is absorbed faster. Ciprofloxacin tablets should not be taken with dairy products (eg milk, yogurt) or fruit juices with added minerals. Doses are determined by the nature and severity of the infection, as well as the sensitivity of the suspected pathogen, the patient's kidney function, and in children and adolescents, the patient's body weight is taken into account. The dose is determined based on the indication, type and severity of infection, sensitivity to ciprofloxacin, treatment depends on the severity of the disease, as well as clinical and bacteriological processes. Treatment of infections caused by certain bacteria (eg, Pseudomonas aeruginosa, Acinetobacter or Stafilococ) requires higher doses of ciprofloxacin and may be combined with one or more other appropriate antibacterial drugs. In the treatment of some infections (for example, pelvic inflammatory disease in women, intra-abdominal infection, infection in neutropenic patients, bone and joint infections), combining one or more compatible antibacterial drugs is possible, depending on the pathogenic microorganisms that cause them. The drug is recommended to be prescribed in the following doses: Adults Indications Daily dose mg Duration of entire treatment (including the possibility of initial parenteral treatment with ciprofloxacin) Lower respiratory tract infections From 2 x 500 mg to 2 x 750 mg. From 7 to 14 days Upper respiratory tract infections Exacerbation of chronic sinusitis From 2 x 500 mg to 2 x 750 mg From 7 to 14 days Chronic suppurative otitis media From 2 x 500 mg to 2 x 750 mg From 7 to 14 days Malignant external otitis 2 x 750 mg From 28 days to 3 months Urinary tract infections Uncomplicated cystitis From 2 x 500 mg to 2 x 750 mg 3 days for women during menopause - once 500 mg Complicated cystitis, uncomplicated pyelonephritis 2 x 500 mg 7 days Complicated pyelonephritis From 2 x 500 mg to 2 x 750 mg Not less 10 days in some cases (for example, with abscesses) - up to 21 days Prostatitis From 2 x 500 mg to 2 x 750 mg 2-4 weeks (acute), 4-6 weeks (chronic) Infections of the genital organs Fungal urethritis and cervicitis 500 mg once a single dose 500 mg Orchiepididymitis and pelvic inflammatory disease From 2 x 500 mg to 2 x 750 mg for at least 14 days Gastrointestinal infections and intra-abdominal infections Diarrhea caused by bacterial infection, including Shigella spp, except Shigella dysenteriae type I and empirical treatment of severe traveler's diarrhea 2 x 500 mg 1 day of diarrhea, caused by shigella dysenteriae type I 2 x 500mg 5 days of diarrhea, caused by Vibrio Cholera 2 x 500 mg 3 days of abdominal typhoid 2 x 500mg 7 days intraabdominal infections caused by gram -negative microorganisms from 2 x 500 mg to 2 x 750mg from 5 to 5 to 5 to 5 to 5 to 5 to 5 to 5 to 5 to 5 to 5 to 5 14 days Skin and soft tissue infections 2 x 500mg to 2 x 750mg 7 to 14 days Joint and bone infections 2 x 500mg to 2 x 750mg max. 3 months Prevention and treatment of infections in patients with neutropenia: recommended in combination with other drugs From 2x500 mg to 2x750 mg therapy continues until the end of the period of neutropenia Prevention of invasive infections caused by Neisseria meningitides 1x500 mg once Post-exposure prophylaxis and treatment of anthrax: treatment should begin as soon as possible after suspected or confirmed infection From 2x500 mg 60 days from the date of confirmation of infection The maximum single dose is 750 mg. Maximum daily dose - 1500 mg Children and adolescents Indications Daily dose mg Duration of entire treatment (including the possibility of initial parenteral treatment with ciprofloxacin) Cystic fibrosis 20 mg/kg body weight 2 times up to 750 mg per day. From 10 to 14 days Complicated cystitis, uncomplicated pyelonephritis From 10 mg/kg body weight 2 times to 20 mg/kg 2 times and a maximum of 750 mg per day. 10 to 14 days Post-exposure prophylaxis and definitive treatment of pulmonary anthrax in individuals who can be treated orally if clinically necessary. The use of the drug should be started as soon as possible after suspected or confirmed contact. 10 mg/kg body weight 2 times a day up to 15 mg/kg body weight with a maximum dose of 750 mg per day. 60 days from the date of confirmed contact with Bacillus anthracis Other severe infections 20 mg/kg body weight 2 times a day with a maximum dose of 750 mg per day. According to the type of infection, the maximum daily dose for children over 6 years of age and adolescents is 750 mg. Elderly Patients Elderly patients should receive a dose selected according to the severity of the infection and creatinine clearance. Renal and liver failure Recommended initial and maintenance doses for patients with impaired renal function Creatinine clearance, ml/min/1.73 m2 Plasma creatinine, µmol/l Oral dose >60 <124 See usual dosage 30-60 124-168 250 –500 mg every 12 hours <30 >169 250–500 mg every 24 hours Patients on hemodialysis >169 250–500 mg every 24 hours (post-dialysis) Patients on peritoneal dialysis >169 250–500 mg every 24 hours In patients with hepatic deficiency there is no need to change the dosage of ciprofloxacin. Studies regarding dosing of the drug for children with impaired renal and/or hepatic function have not been conducted. If the severity of the patient's illness or other reasons (for example, if the patient is receiving enteral nutrition) do not allow the use of ciprofloxacin film-coated tablets, it is recommended to switch to therapy with an IV dosage form of ciprofloxacin. After IV administration, you can continue treatment with the tablet form of the drug. Side effects - increased fatigue, sweating, fever - headache, dizziness, migraine, anxiety, tremor, drowsiness, nightmare dreams, confusion, depression, hallucinations, psychotic reactions - visual and hearing impairment, smell, tactile sensitivity, taste disturbance sensations, including their loss (recovery occurs within a few weeks after stopping treatment) - prolongation of the QT interval, tachycardia, drop in blood pressure, fainting - loss of appetite, nausea, feeling of fullness in the stomach, mild abdominal pain, flatulence, diarrhea - itching, urticaria, erythema multimorpha, allergic pneumonitis, Steven-Johnson syndrome, Lyell's syndrome or toxic epidermal necrolysis, Quincke's edema, photosensitivity - joint and muscle pain, muscle weakness, tendon lesions (including tenosynovitis), muscle lesions (rhabdomyolysis) - cholestasis, liver failure , increased activity of liver enzymes, increased levels of bilirubin, creatinine in the blood serum - neutropenia, agranulocytosis, thrombocytopenia, eosinophilia, leukopenia, hemolytic anemia Contraindications - hypersensitivity to ciprofloxacin, other drugs of the fluoroquinolone group or to any of the excipients of the drug - epilepsy - tendon damage after history of antibiotic treatment - deficiency of glucose-6-phosphate dehydrogenase - pseudomembranous colitis - simultaneous use of ciprofloxacin and tizanidine - pregnancy and lactation - childhood and adolescence up to 6 years of age Drug interactions With the simultaneous use of ciprofloxacin with didanosine, the absorption of ciprofloxacin is reduced due to the formation of complexes of ciprofloxacin with aluminum and magnesium salts contained in didanosine. When used simultaneously with warfarin, the risk of bleeding increases. Concomitant use of ciprofloxacin and theophylline may lead to increased plasma theophylline concentrations due to competitive inhibition at the citrochrome P450 binding sites, resulting in an increase in the elimination half-life of theophylline and an increased risk of theophylline-related toxicity. Simultaneous use of antacids, as well as drugs containing aluminum, zinc, iron or magnesium ions, can cause a decrease in the absorption of ciprofloxacin, therefore the interval between the administration of these drugs should be at least 4 hours. Special instructions Treatment can only be prescribed by doctors experienced in the treatment of cystic fibrosis . Ciprofloxacin may be used to treat severe infection in children and adolescents when needed. In elderly patients, the drug should be used with caution. During treatment, excessive solar and artificial ultraviolet irradiation should be avoided to avoid photosensitivity. If pseudomembranous colitis is suspected, ciprofloxacin should be discontinued immediately and appropriate treatment should be initiated. When using the drug, tendon inflammation and rupture may occur. Such reactions were observed primarily in older patients who were concomitantly using corticosteroids. At the first sign of pain or inflammation, the drug should be discontinued immediately. It should be borne in mind that in patients with a history of brain damage (stroke, severe trauma), seizures may develop; with glucose-6-phosphate dehydrogenase deficiency, there is a risk of hemolysis. In this regard, treatment of such patients with ciprofloxacin should be carried out with great caution. Caution must be exercised when prescribing ciprofloxacin to patients with diabetes mellitus. The use of ciprofloxacin should be discontinued at the first sign of a skin rash or any other allergic reaction. Use in patients with impaired liver and kidney function The drug should be used with caution in patients with impaired renal function, since in such patients the half-life of ciprofloxacin increases. Patients with impaired liver function do not require dose adjustment. The pharmacokinetics of ciprofloxacin in patients with liver cirrhosis did not change. Changes in the pharmacokinetics of the drug in patients with acute hepatitis have not been studied. Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms Ciprofloxacin can cause dizziness and increased reaction to light, the ability to concentrate when driving machines and the speed of psychomotor reactions decreases. Overdose Symptoms: confusion, dizziness, disturbances of consciousness, seizures; gastrointestinal disorders, lesions of the mucous membranes; prolongation of the QT interval. Treatment: symptomatic, there is no specific antidote. Tsiprolet® is not excreted by hemodialysis and peritoneal dialysis. Release form and packaging 10 tablets in a blister pack made of polyvinyl chloride film and printed varnished aluminum foil. 1 blister pack along with instructions for use in the state and Russian languages is placed in a box of cardboard. Storage conditions: In a dry place, protected from light, at a temperature not exceeding 25 °C. Keep out of the reach of children! Shelf life: 3 years Do not use after the expiration date indicated on the package. Conditions for dispensing from pharmacies By prescription, INDIA ADDRESS OF THE ORGANIZATION THAT ACCEPTS CLAIMS FROM CONSUMERS ON PRODUCT QUALITY IN THE TERRITORY OF THE REPUBLIC OF KAZAKHSTAN REPRESENTATIVE OFFICE IN THE REPUBLIC OF KAZAKHSTAN: 050057 ALMATY, ST. DZHANDOSOVA, 21 POST BOX 7, TEL: 8(727)3941688, FAX: 8(727)3941294
Mechanism of action of the drug
Tsiprolet belongs to the group of fluoroquinolones and is an antibacterial drug with a wide range of effects. Its main active ingredient is ciprofloxacin. This chemical compound has the ability to penetrate the DNA structure of the cells that cause the infection, thereby disrupting the vital functions of bacteria, their ability to subsequently reproduce and develop. The result of this influence is the death of harmful microorganisms.
Tsiprolet tablets have a complex effect, effectively destroying microbes that are both at the reproduction stage and in the resting phase. The spectrum of negative effects of this medicine extends to almost all types of gram-positive and gram-negative bacteria, most of the anaerobic pathogens. The instructions for use of Tsiprolet state that its main active component actively eliminates bacterial microflora that are resistant to other antibiotics, for example, the nitrofuran or sulfonamide series. Resistance of microbes to this medicine appears only after a long period of time.
Indications
Ciprofan tablets - what do they help with? This antibiotic is used for the treatment of complicated or uncomplicated bacterial infections that are caused by strains of microorganisms sensitive to ciprofloxacin. The remedy is indicated for the following diseases:
- urinary tract infections;
- bacterial lesions of the gastrointestinal tract;
- sepsis;
- pathologies of ENT organs, especially in case of infection with staphylococcal microflora and gram-negative bacteria, including the Pseudomonas type;
- peritonitis;
- infectious lesions of the respiratory system (for example, pneumonia), if they are caused by Enterobacter, Staphylococcus, Klebsiella, Haemophilus influenzae, Legionella or microbes of the Branhamella, Pseudomonas species;
- inflammatory infectious diseases of the genital organs in men and women (prostatitis, adnexitis);
- infections of the musculoskeletal system and skin;
- some sexually transmitted diseases (gonorrhea);
- bacterial lesions of the eyelid and conjunctiva of the eyes;
- therapy and prevention of infections in patients with low immunity (for example, with neutropenia or after treatment with immunosuppressive drugs).
Tsiprolet (500mg)
INSTRUCTIONS for the use of the medicinal product for medical use CIPROLET®
Registration number: P N016161/01
Trade name of the drug: Tsiprolet®
International nonproprietary name of the drug: ciprofloxacin.
Dosage form: film-coated tablets
Composition Each 250 mg film-coated tablet contains: Active ingredient: ciprofloxacin hydrochloride monohydrate 291.106 mg, equivalent to ciprofloxacin 250 mg. Excipients: corn starch 50.323 mg, microcrystalline cellulose 7.486 mg, croscarmellose sodium 10.000 mg, corn starch 7.561 mg, colloidal silicon dioxide 5.000 mg, talc 5.000 mg, magnesium stearate 3.514 mg. Shell: hypromellose (6 cps) 4.800 mg, sorbic acid 0.080 mg, titanium dioxide 2.000 mg, talc 1.600 mg, macrogol-6000 1.360 mg, polysorbate-80 0.080 mg, dimethicone 0.080 mg. Each 500 mg film-coated tablet contains: Active ingredient: ciprofloxacin hydrochloride monohydrate 582.211 mg, equivalent to ciprofloxacin 500 mg. Excipients: corn starch 27.789 mg, microcrystalline cellulose 5.000 mg, croscarmellose sodium 20.000 mg, corn starch 9.500 mg, colloidal silicon dioxide 5.000 mg, talc 6.000 mg, magnesium stearate 4.500 mg. Shell: hypromellose (6 cps) 5.000 mg, sorbic acid 0.072 mg, titanium dioxide 1.784 mg, talc 1.784 mg, macrogol-6000 1.216 mg, polysorbate-80 0.072 mg, dimethicone 0.072 mg.
Description White or almost white, round, biconvex tablets with a smooth surface on both sides, film-coated. The appearance of the fracture is a white or almost white mass.
Pharmacotherapeutic group: antimicrobial agent – fluoroquinolone.
ATX code: J01MA02
Pharmacological properties Pharmacodynamics A broad-spectrum antimicrobial agent, a fluoroquinolone derivative, suppresses bacterial DNA gyrase (topoisomerases II and IV, responsible for the process of supercoiling of chromosomal DNA around nuclear RNA, which is necessary for reading genetic information), disrupts DNA synthesis, growth and division of bacteria; causes pronounced morphological changes (including cell wall and membranes) and rapid death of the bacterial cell. It has a bactericidal effect on gram-negative organisms during the period of rest and division (since it affects not only DNA gyrase, but also causes lysis of the cell wall); it acts on gram-positive microorganisms only during the period of division. Low toxicity for the cells of the macroorganism 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 DNA gyrase inhibitors, which makes it highly effective against bacteria that are resistant, for example, to aminoglycosides, penicillins, cephalosporins, tetracyclines and many other antibiotics. Gram-negative aerobic bacteria are sensitive to ciprofloxacin: enterobacteria (Escherichiacoli, Salmonellaspp., Shigellaspp., Citrobacterspp., Klebsiellaspp., Enterobacterspp., Proteusmirabilis, Proteusvulgaris, Serratiamarcescens, Hafniaalvei, Edwardsiellatarda, Providencia spp., Morganellamorganii, Vibriospp. , Yersiniaspp.), others gram-negative bacteria (Haemophilus spp., Pseudomonasaeruginosa, Moraxellacatarrhalis, Aeromonasspp., Pasteurellamultocida, Plesiomonasshigelloides, Campylobacterjejuni, Neisseriaspp.), some intracellular pathogens - Legionellapneumophila, Brucellaspp., Chlamydiatrachomatis, Listeria monocytogenes, Mycobacterium tuberculosis, My cobacteriumkansasii, Corynebacteriumdiphtheriae; gram-positive aerobic bacteria: Staphylococcus spp. (Staphylococcus aureus, Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus saprophyticus), Streptococcus spp. (Streptococcus pyogenes, Streptococcus agalactiae). Most staphylococci resistant to methicillin are also resistant to ciprofloxacin. The sensitivity of Streptococcus pneumoniae, Enterococcus faecalis, Mycobacterium avium (located intracellularly) is moderate (high concentrations are required to suppress them). The following are resistant to the drug: Bacteroides fragilis, Pseudomonas cepacia, Pseudomonas maltophilia, Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroides. Not effective against Treponema pallidum. Resistance develops extremely slowly, since, on the one hand, after the action of ciprofloxacin there are practically no persistent microorganisms left, and, on the other hand, bacterial cells do not have enzymes that inactivate it. Pharmacokinetics When taken orally, it is quickly and fairly completely absorbed from the gastrointestinal tract (GIT), mainly in the duodenum and jejunum. Eating slows down absorption but does not change maximum concentration (Cmax) or bioavailability. Bioavailability – 50-85%, volume of distribution – 2-3.5 l/kg, binding to plasma proteins – 20-40%. The time to reach maximum concentration (TCmax) after oral administration is 60-90 minutes, Cmax linearly depends on the dose taken and is 1.2 at doses of 250, 500, 750 and 1000 mg, respectively; 2.4; 4.3 and 5.4 μg/ml. 12 hours after oral administration 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. Well distributed in body tissues (excluding fat-rich tissue, such as nervous tissue). The concentration in tissues is 2-12 times higher than in plasma. Therapeutic concentrations are achieved in saliva, tonsils, liver, gall bladder, 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. It penetrates into the cerebrospinal fluid in a small amount, where the concentration in the absence of inflammation of the meninges is 6-10% of that in the blood serum, and in the presence of inflammation - 14-37%. Ciprofloxacin also penetrates well into the ocular fluid, bronchial secretions, pleura, peritoneum, lymph, and through the placenta. The concentration of ciprofloxacin in blood neutrophils is 2-7 times higher than in blood serum. Metabolized in the liver (15-30%) with the formation of low-active metabolites (oxo-, diethyl-, sulfo-, formylciprofloxacin). The half-life (T1/2) is about 3-5 hours, in chronic renal failure (CRF) - up to 12 hours. It is excreted mainly by the kidneys by tubular filtration and tubular secretion in unchanged form (40-50%) and in the form of metabolites ( 15%), the rest through the intestines. A small amount is excreted in breast milk. Renal clearance – 3-5 ml/min/kg; total clearance – 8-10 ml/min/kg. With chronic renal failure (creatinine clearance (CC) above 20 ml/min), the percentage of the drug excreted through the kidneys decreases, but accumulation in the body does not occur due to a compensatory increase in the metabolism of the drug and its excretion by the intestines.
Indications for use
Infectious and inflammatory diseases caused by microorganisms sensitive to ciprofloxacin. Adults :
- lower respiratory tract infections: acute and chronic (in the acute stage) bronchitis, pneumonia, bronchiectasis, infectious complications of cystic fibrosis;
- ENT infections: acute sinusitis;
- kidney and urinary tract infections: cystitis, pyelonephritis;
- genital infections, including adnexitis, gonorrhea, prostatitis;
- abdominal infections (bacterial infections of the gastrointestinal tract, biliary tract);
- infections of the skin and soft tissues: infected ulcers, wounds, burns, abscesses, phlegmon;
- infections of bones and joints: osteomyelitis, septic arthritis;
- sepsis and peritonitis;
- infections due to immunodeficiency that occurs during treatment with immunosuppressive drugs or in patients with neutropenia;
- prevention and treatment of pulmonary anthrax.
Children and teenagers (from 5 to 17 years):
- treatment of complications caused by Pseudomonas aeruginosa in children with cystic fibrosis;
- prevention and treatment of pulmonary anthrax (infection with Bacillus anthracis).
Contraindications for use
Hypersensitivity to ciprofloxacin and other drugs of the quinolone group and excipients, children's age (up to 18 years - until the completion of the skeletal formation process, 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 of the pulmonary form anthrax), simultaneous use with tizanidine (risk of a pronounced decrease in blood pressure, drowsiness), pregnancy, lactation (breastfeeding).
With caution Severe atherosclerosis of cerebral vessels, cerebrovascular accident, mental illness, epilepsy, severe renal and/or liver failure, old age, increased risk of prolongation of the QT interval or development of ari (for example, congenital long QT syndrome), heart disease (cardiac failure, myocardial infarction, bradycardia), electrolyte imbalance (for example, with hypokalemia, hypomagnesemia), simultaneous use of drugs that prolong the QT interval (including class IA and III antiarrhythmics, tricyclic antidepressants, macrolides, antipsychotics), simultaneous use with isoenzyme inhibitors CYP450 1A2 (including theophylline, methylxanthine, caffeine, duloxetine, clozapine, ropinirole, olanzapine), patients with a history of tendon damage during previous treatment with quinolones, myasthenia gravis, glucose-6-phosphate dehydrogenase deficiency.
Method of administration and dosage Tablets should be taken orally, regardless of meals, without chewing, with a small amount of liquid. If the drug is used on an empty stomach, the active substance is absorbed faster. In this case, the tablets should not be taken with dairy products or drinks fortified with calcium (for example, milk, yogurt, juices with a high calcium content). Calcium contained in regular food does not affect the absorption of ciprofloxacin. Recommended dosage regimen: Adults - respiratory tract infections (depending on the severity of the infection and the patient's condition): from 500 mg 2 times a day to 750 mg 2 times a day; - infections of the genitourinary system: acute, uncomplicated: from 250 mg 2 times a day to 500 mg 2 times a day; cystitis in women (before menopause): 500 mg 1 time per day; complicated: from 500 mg 2 times a day to 750 mg 2 times a day; genital infections (except gonorrhea): from 500 mg 2 times a day to 750 mg 2 times a day; gonorrhea: 500 mg once a day once; - diarrhea: 500 mg 2 times a day; - other infections (see section “Indications for use”): 500 mg 2 times a day; especially severe, life-threatening (especially in the presence of Pseudomonaspp., Staphylococcusspp., Streptococcusspp.), incl. streptococcal pneumonia, infections of bones and joints, septicemia, peritonitis: 750 mg 2 times a day. Dosage regimen in elderly patients (after 65 years): Elderly patients should be prescribed lower doses of ciprofloxacin depending on the severity of the disease and creatinine clearance. Dosage regimen for patients with renal failure: - with creatinine clearance from 30 to 60 ml/min/1.73 m2 or its concentration in blood plasma from 1.4 to 1.9 mg/100 ml, the maximum daily dose of ciprofloxacin is 1000 mg; - with creatinine clearance below 30 ml/min/1.73 m2 or plasma concentrations of 2 mg/100 ml or more, the maximum daily dose of ciprofloxacin is 500 mg; - patients with renal failure on hemodialysis: with creatinine clearance from 30 to 60 ml/min/1.73 m2 or its concentration in blood plasma from 1.4 to 1.9 mg/100 ml, the maximum daily dose of ciprofloxacin is 1000 mg; with a creatinine clearance of 30 ml/min/1.73 m2 or less or its concentration in the blood plasma of 2 mg/100 ml or more, the maximum daily dose of ciprofloxacin is 500 mg. On hemodialysis days, ciprofloxacin is taken after the procedure. Outpatients with renal failure on continuous peritoneal dialysis: maximum daily dose of ciprofloxacin is 500 mg. Patients with hepatic impairment: no dose adjustment is required. The duration of treatment depends on the severity of the disease, clinical and bacteriological control. It is important to continue treatment systematically for at least 3 days after the disappearance of fever or other clinical symptoms. Average duration of treatment: 1 day - for acute uncomplicated gonorrhea and cystitis; up to 7 days - for kidney infections, urinary tract infections, intra-abdominal infections; the entire period of neutropenia in immunocompromised patients; no more than 2 months - for osteomyelitis; from 7 to 14 days - for other infections. For infections caused by Streptococcus spp., due to the risk of late complications, treatment should continue for at least 10 days; for infections caused by Chlamydiasp., treatment should also be continued for at least 10 days. For the prevention and treatment of pulmonary anthrax - 500 mg 2 times a day for 60 days. The drug should be started immediately after suspected or confirmed infection. Children and adolescents In the absence of other prescriptions, the following dosage regimen should be followed: For the treatment of complications caused by Pseudomonas aeruginosa in children from 5 to 17 years old with cystic fibrosis - 20 mg/kg 2 times a day (maximum dose 1500 mg). Duration of treatment is 10-14 days. For pulmonary anthrax (prevention and treatment) – 15 mg/kg 2 times a day. The maximum single dose is 500 mg, daily dose is 1000 mg. The total duration of taking ciprofloxacin is 60 days. Children with renal impairment There is no information available on dosage adjustment patterns for children with renal impairment.
Side effect
Depending on the frequency of occurrence, the following groups of side effects are distinguished: frequent (>1% and <10%), infrequent (>0.1 and <1%), rare (>0.01 and <0.1%), very rare (<0.01%).
From the central and peripheral nervous system: infrequently - dizziness, headache, increased fatigue; rarely – insomnia, tremor; very rarely - anxiety, “nightmare” dreams, peripheral paralgesia (anomaly in the perception of pain), increased sweating, increased intracranial pressure, including benign intracranial hypertension, confusion, depression (which can lead to self-harmful behavior such as suicidal behavior/ thoughts, as well as attempted or successful suicide), hallucinations, as well as other manifestations of psychotic reactions (which can lead to self-injurious behavior such as suicidal acts/thoughts, as well as attempted or successful suicide), migraines, fainting states, cerebral thrombosis arteries, agitation, disorientation, paresthesia and dysesthesia, hypoesthesia, convulsions, vertigo, impaired coordination of movements, gait disturbance, hyperesthesia, peripheral neuropathy and polyneuropathy, epileptic attacks.
From the senses: infrequently - taste disturbances; rarely – visual disturbances, tinnitus, hearing loss; very rarely - impaired sense of smell, impaired color perception, impaired hearing.
From the cardiovascular system: in very rare cases - tachycardia, other heart rhythm disturbances, decreased blood pressure, prolongation of the QT interval, ventricular arrhythmias (including pirouette type).
From the digestive system: infrequently - nausea, vomiting, diarrhea, abdominal pain, flatulence, decreased appetite and amount of food taken; rarely – cholestatic jaundice (especially in patients with previous liver diseases), pancreatitis; very rarely - hepatitis, hepatonecrosis.
From the hematopoietic system: uncommon – eosinophilia, leukopenia, granulocytopenia, thrombocytopenia, anemia; very rarely - leukocytosis, thrombocytosis, hemolytic anemia, neutropenia, agranulocytosis, pancytopenia, suppression of bone marrow hematopoiesis, serum sickness.
From the urinary system: rarely - hematuria, crystalluria (primarily with alkaline urine and low diuresis), dysuria, polyuria, urinary retention, albuminuria; very rarely - glomerulonephritis, urethral bleeding, decreased nitrogen excretory function of the kidneys, interstitial nephritis, renal failure.
From the respiratory system: rarely - respiratory distress (including bronchospasm). Allergic reactions: infrequently - skin 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); rarely - swelling of the face or larynx, shortness of breath, eosinophilia, increased photosensitivity; very rarely - vasculitis, erythema nodosum, exudative erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), anaphylactic reactions, anaphylactic shock. From laboratory parameters: infrequently - increased activity of liver transaminases and alkaline phosphatase, hyperbilirubinemia; rarely - changes in prothrombin levels (including hypoprothrombinemia), hyperglycemia or hypoglycemia, increased amylase activity; frequency unknown - hypercreatininemia. Other: infrequently - “flushes” of blood to the face; rarely - arthralgia, arthritis, tenosynovitis; very rarely - tendon ruptures (mainly Achilles), asthenia, myalgia, increased muscle tone, muscle weakness, exacerbation of myasthenia gravis symptoms, superinfections (candidiasis, pseudomembranous colitis); frequency unknown - acute generalized pustular exanthema, increase in international normalized ratio (in patients receiving vitamin K antagonists).
Overdose Symptoms: nausea, vomiting, confusion, mental agitation. Treatment: specific antidote is unknown. It is necessary to carefully monitor the patient's condition, perform gastric lavage and other emergency measures, and ensure sufficient fluid intake. To prevent the development of crystalluria, it is recommended to monitor renal function, including urine pH and acidity. Using hemo- or peritoneal dialysis, only a small (less than 10%) amount of the drug can be removed.
Interactions with other drugs Drugs known to prolong the QT interval Caution should be exercised when ciprofloxacin, like other fluoroquinolones, is used concomitantly in patients receiving drugs known to prolong the QT interval (e.g., class IA and III antiarrhythmics, tricyclic antidepressants, macrolides, neuroleptics). Formation of chelate compounds Simultaneous intake of tablet forms of ciprofloxacin and cation-containing drugs, mineral supplements containing calcium, magnesium, aluminum, iron; sucralfate, antacids, polymeric phosphate compounds (sevelamer, lanthanum carbonate) and drugs with a large buffer capacity (such as didanosine tablets) containing magnesium, aluminum or calcium reduce the absorption of ciprofloxacin. In such cases, ciprofloxacin should be taken either 1-2 hours before or 4 hours after taking these drugs. This restriction does not apply to drugs belonging to the class of H2-histamine receptor blockers. Ingestion of food and dairy products The concomitant use of ciprofloxacin and dairy products or mineral-fortified drinks (milk, yogurt, calcium-fortified orange juice) should be avoided as the absorption of ciprofloxacin may be reduced. However, calcium contained in other foods does not significantly affect the absorption of ciprofloxacin. Omeprazole With the combined use of ciprofloxacin and omeprazole, a slight decrease in Cmax in plasma and a decrease in the area under the concentration-time pharmacokinetic curve (AUC) may be observed. Theophylline The simultaneous use of ciprofloxacin and drugs containing theophylline may cause an undesirable increase in the concentration of theophylline in the blood plasma and, accordingly, the occurrence of theophylline-induced adverse events; in very rare cases, these adverse events can be life-threatening for the patient. If the simultaneous use of these two drugs is necessary, it is recommended to constantly monitor the concentration of theophylline in the blood plasma and, if necessary, reduce the dose of theophylline. Other xanthine derivatives The simultaneous use of ciprofloxacin and caffeine or pentoxifylline (oxpentifylline) may lead to an increase in the concentration of xanthine derivatives in the blood serum. Non-steroidal anti-inflammatory drugs The combination of very high doses of quinolones and some non-steroidal anti-inflammatory drugs (except acetylsalicylic acid) can provoke seizures. Cyclosporine With simultaneous use of ciprofloxacin and drugs containing cyclosporine, a short-term transient increase in plasma creatinine concentration was observed. In such cases, it is necessary to determine the concentration of creatinine in the blood twice a week. Oral hypoglycemic agents With simultaneous use of ciprofloxacin and oral hypoglycemic agents, mainly sulfonylureas (for example, glibenclamide, glimepiride), the development of hypoglycemia may be due to an increase in the effect of oral hypoglycemic agents. Probenecid Probenecid slows the rate of renal excretion of ciprofloxacin. The simultaneous use of ciprofloxacin and drugs containing probenecid leads to an increase in the concentration of ciprofloxacin in the blood serum. Phenytoin With the simultaneous use of ciprofloxacin and phenytoin, a change (increase or decrease) in the content of phenytoin in the blood plasma was observed. It is recommended to monitor phenytoin therapy in patients taking both drugs, including determination of phenytoin plasma levels. Methotrexate With simultaneous use of methotrexate and ciprofloxacin, the renal tubular transport of methotrexate may slow down, which may be accompanied by an increase in the concentration of methotrexate in the blood plasma. This may increase the likelihood of developing side effects of methotrexate. In this regard, patients receiving concomitant therapy with methotrexate and ciprofloxacin should be closely monitored. Tizanidine As a result of a clinical study involving healthy volunteers with simultaneous use of ciprofloxacin and drugs containing tizanidine, an increase in the concentration of tizanidine in the blood plasma was detected: an increase in Cmax by 7 times (from 4 to 21 times), an increase in AUC by 10 times (from 6 to 24 once). Hypotensive and sedative side effects are associated with increased serum concentrations of tizanidine. Therefore, the simultaneous use of ciprofloxacin and drugs containing tizanidine is contraindicated. Duloxetine During clinical studies, it was shown that the simultaneous use of duloxetine and strong inhibitors of the CYP450 1A2 isoenzyme (such as fluvoxamine) may lead to an increase in the AUC and Cmax of duloxetine. Although there is no clinical data on possible interactions with ciprofloxacin, the likelihood of such an interaction can be anticipated when ciprofloxacin and duloxetine are used concomitantly. Ropinirole The simultaneous use of ropinirole and ciprofloxacin, a moderate inhibitor of the CYP450 1A2 isoenzyme, leads to an increase in the Cmax and AUC of ropinirole by 60 and 84%, respectively. Monitor for adverse effects of ropinirole during coadministration with ciprofloxacin and for a short time after completion of combination therapy. Lidocaine In a study on healthy volunteers, it was found that the simultaneous use of drugs containing lidocaine and ciprofloxacin, a moderate inhibitor of the CYP450 1A2 isoenzyme, leads to a 22% decrease in the clearance of lidocaine when administered intravenously. Despite the good tolerability of lidocaine, when used simultaneously with ciprofloxacin, side effects may increase due to interaction. Clozapine With simultaneous use of clozapine and ciprofloxacin at a dose of 250 mg for 7 days, an increase in serum concentrations of clozapine and N-desmethylclozapine was observed by 29% and 31%, respectively. The patient's condition should be monitored and, if necessary, the dosage regimen of clozapine should be adjusted during its combined use with ciprofloxacin and for a short time after completion of combination therapy. Sildenafil When ciprofloxacin at a dose of 500 mg and sildenafil at a dose of 50 mg was used simultaneously in healthy volunteers, a 2-fold increase in the Cmax and AUC of sildenafil was observed. In this regard, the use of this combination is possible only after assessing the benefit/risk ratio. Vitamin K antagonists The combined use of ciprofloxacin and vitamin K antagonists (for example, warfarin, acenocoumarol, phenprocoumon, fluindone) may lead to an increase in their anticoagulant effect. The magnitude of this effect may vary depending on concomitant infections, age and general condition of the patient, so it is difficult to assess the effect of ciprofloxacin on increasing the international normalized ratio (INR). The INR should be monitored fairly frequently during co-administration of ciprofloxacin and vitamin K antagonists, as well as for a short time after completion of combination therapy.
Special instructions Severe infections, staphylococcal infections and infections caused by gram-positive and anaerobic bacteria When treating severe infections, staphylococcal infections and infections caused by anaerobic bacteria, ciprofloxacin should be used in combination with appropriate antibacterial agents. Infections due to Streptococcus pneumoniae Ciprofloxacin is not recommended for the treatment of infections caused by Streptococcus pneumoniae due to limited effectiveness against the pathogen. Genital tract infections For genital infections suspected of being caused by fluoroquinolone-resistant strains of Neisseria gonorrhoeae, local information on resistance to ciprofloxacin should be considered and susceptibility confirmed by laboratory tests. Cardiac disorders Ciprofloxacin has the effect of prolonging the QT interval. Given that women have a longer average QT interval compared to men, they are more sensitive to drugs that cause QT prolongation. Elderly patients also have increased sensitivity to the effects of such drugs. Use ciprofloxacin with caution in combination with drugs that prolong the QT interval (e.g., class IA and III antiarrhythmics, tricyclic antidepressants, macrolides, antipsychotics) or in patients with an increased risk of QT prolongation or development of QT syndrome (e.g., congenital long interval syndrome). QT), heart disease (heart failure, myocardial infarction, bradycardia), uncorrected electrolyte imbalance (for example, hypokalemia, hypomagnesemia). Use in children Ciprofloxacin, like other drugs of this class, causes arthropathy of large joints in animals. When analyzing the current data on the safety of ciprofloxacin in children under 18 years of age, most of whom have cystic fibrosis, no connection has been established between cartilage or joint damage with the drug. It is not recommended to use ciprofloxacin in children for the treatment of diseases other than the treatment of complications of cystic fibrosis of the lungs (in children from 5 to 17 years old) associated with Pseudomonas aeruginosa and for the treatment and prevention of pulmonary anthrax. Hypersensitivity In rare cases, after the first use, anaphylactic reactions up to anaphylactic shock may occur. In these cases, the use of ciprofloxacin should be stopped immediately and appropriate treatment should be instituted. Gastrointestinal tract 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 the appointment of appropriate treatment. Hepatobiliary system Cases of liver necrosis and life-threatening liver failure have been reported with the use of ciprofloxacin. If you have symptoms of liver disease such as anorexia, jaundice, dark urine, itching, a painful abdomen, the use of ciprofloxacin should be discontinued. Patients taking ciprofloxacin who have had liver disease may experience a temporary increase in the activity of liver transaminases and alkaline phosphatase or cholestatic jaundice. Musculoskeletal system In patients with myasthenia gravis, ciprofloxacin should be used with caution, as an exacerbation of symptoms is possible. At the first signs of tendinitis (painful swelling, inflammation in the joint area), treatment with ciprofloxacin should be stopped and physical activity should be avoided. When using ciprofloxacin, cases of tendinitis and tendon rupture (mainly Achilles tendon), sometimes bilateral, may occur within the first 48 hours after the start of therapy; inflammation and tendon rupture can occur even several months after stopping treatment with ciprofloxacin. Elderly patients and patients with tendon diseases who are simultaneously treated with glucocorticosteroids have an increased risk of tendinopathy. Ciprofloxacin should be used with caution in patients with a history of tendon diseases associated with quinolones. Nervous system Ciprofloxacin, like other fluoroquinolones, can provoke seizures and lower the seizure threshold. In patients with epilepsy and a history of central nervous system diseases (lowered seizure threshold, history of seizures, cerebrovascular accidents, organic brain lesions or stroke) due to the risk of developing adverse reactions from the central nervous system, ciprofloxacin should be used only after assessing the benefit/risk ratio . Cases of status epilepticus have been reported with the use of ciprofloxacin. If seizures occur, use of the drug should be discontinued. Psychiatric reactions may occur even after the first use of fluoroquinolones, including ciprofloxacin. In rare cases, depression or psychotic reactions may progress to suicidal thoughts and self-harmful behavior, such as attempted or completed suicide; if the patient develops one of these reactions, the drug should be stopped and the doctor informed. Cases of sensory or sensorimotor neuropathy have been reported in patients taking fluoroquinolones. If symptoms such as pain, burning, tingling, numbness, or weakness occur, the patient should inform the doctor before continuing to use ciprofloxacin. Skin During the treatment period, contact with direct sunlight and UV irradiation in a solarium should be avoided. Cytochrome P450 Ciprofloxacin is a moderate inhibitor of CYP450 1A2 isoenzymes. Caution should be exercised during the simultaneous use of ciprofloxacin and drugs metabolized by these enzymes (including tizanidine, theophylline, methylxanthine, caffeine, duloxetine, ropinirole, clozapine, olanzapine), since an increase in the concentration of these drugs in the blood serum due to inhibition of their metabolism by ciprofloxacin, may cause specific adverse reactions. Prevention of crystalluria To avoid the development of crystalluria, exceeding the recommended daily dose is unacceptable; sufficient fluid intake and maintaining an acidic urine reaction are also necessary. Diagnosis of infection caused by Mycobacterium spp. In vitro, ciprofloxacin may interfere with the bacteriological study of Mycobacterium tuberculosis, inhibiting its growth, which can lead to false negative results when diagnosing this pathogen in patients taking ciprofloxacin.
Impact on the ability to drive vehicles and machinery
During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Release form Film-coated tablets, 250 mg and 500 mg. 10 tablets in a PVC/aluminum blister. 1 or 2 blisters along with instructions for use in a cardboard pack.
Storage conditions : Protected from light at a temperature not exceeding 25 °C. Keep out of the reach of children!
Shelf life 3 years. Do not use after the expiration date stated on the packaging.
Conditions for dispensing from pharmacies By prescription.
Manufacturer Dr. Reddy's Laboratories Ltd., India Dr. Reddy's Laboratories Ltd., India
Address of the place of production 1. Survey No. 42, 45 & 46, Bachupally Village, Qutbullapur Mandal, Ranga Reddy District, Telangana State, India. 2. Khol, Nalagarh Road, Baddi, Dist. Solan, Himachal Pradesh, India.
Information about complaints and adverse drug reactions should be sent to the following address: Representative office: 115035, Moscow, Ovchinnikovskaya embankment, 20, building 1 tel. fax
Dosage and methods of application
The antibiotic Tsiprolet is prescribed by a doctor after examining the patient. The dose of the drug is selected based on the type of infection, the severity of the disease and the patient’s condition. The dosage regimen is also influenced by the functional ability of the urinary organs and the person’s body weight (when used in adolescence and childhood).
For the most severe cases of infection and when it is impossible to take the medication in tablet form, Tsiprolet is prescribed in the form of infusion solutions. Then the intravenous infusions of the drug are gradually stopped, and the patient switches to internal administration of the medication. The tablets do not need to be chewed; they simply need to be swallowed whole and washed down with a small amount of water. Take Tsiprolet, regardless of food intake, 500-750 mg twice a day.
The duration of therapy depends on the severity of the pathology and can vary from 3 to 21 days. Usually the doctor prescribes the use of this antibiotic for a period of 7 to 14 days.
Ciprolet®
Drugs that cause prolongation of the OT interval
Caution should be exercised when ciprofloxacin, like other fluoroquinolones, is used concomitantly in patients receiving drugs known to prolong the QT interval (for example, class IA and III antiarrhythmic drugs, tricyclic antidepressants, macrolides, antipsychotics).
Chelation formation
Concomitant use of tablet forms of ciprofloxacin and cation-containing drugs, mineral supplements containing calcium, magnesium, aluminum, iron, sucralfate, antacids, polymeric phosphate compounds (sevelamer, lanthanum carbonate) and drugs with a large buffer capacity (such as didanosine tablets) containing magnesium, aluminum or calcium reduces the absorption of ciprofloxacin. In such cases, ciprofloxacin should be taken either 1-2 hours before or 4 hours after taking these drugs.
This restriction does not apply to drugs belonging to the class of histamine H2 receptor blockers.
Intake of food and dairy products
The simultaneous use of ciprofloxacin and dairy products or drinks fortified with minerals (milk, yogurt, calcium-fortified orange juice) should be avoided as the absorption of ciprofloxacin may be reduced. However, calcium contained in other foods does not significantly affect the absorption of ciprofloxacin.
Omeprazole
With the combined use of ciprofloxacin and omeprazole, a slight decrease in plasma Cmax and a decrease in the area under the concentration-time pharmacokinetic curve (AUC) may be observed.
Theophylline
The simultaneous use of ciprofloxacin and drugs containing theophylline may cause an undesirable increase in the concentration of theophylline in the blood plasma and, accordingly, the occurrence of theophylline-induced adverse events; in very rare cases, these adverse events can be life-threatening for the patient. If the simultaneous use of these two drugs is necessary, it is recommended to constantly monitor the concentration of theophylline in the blood plasma and, if necessary, reduce the dose of theophylline.
Other xanthine derivatives
The simultaneous use of ciprofloxacin and caffeine or pentoxifylline (oxpentifylline) may lead to an increase in the concentration of xanthine derivatives in the blood serum.
Nonsteroidal anti-inflammatory drugs
The combination of very high doses of quinolones and some non-steroidal anti-inflammatory drugs (excluding acetylsalicylic acid) can provoke seizures.
Cyclosporine
With the simultaneous use of ciprofloxacin and drugs containing cyclosporine, it was observed
short-term transient increase in plasma creatinine concentration. In such cases, it is necessary to determine the concentration of creatinine in the blood twice a week.
Oral hypoglycemic agents
With the simultaneous use of ciprofloxacin and oral hypoglycemic agents, mainly sulfonylureas (for example, glibenclamide, glimepiride), the development of hypoglycemia may be due to an increase in the effect of oral hypoglycemic agents.
Probenecid
Probenecid slows down the rate of excretion of ciprofloxacin by the kidneys. The simultaneous use of ciprofloxacin and drugs containing probenecid leads to an increase in the concentration of ciprofloxacin in the blood serum.
Phenytoin
With the simultaneous use of ciprofloxacin and phenytoin, a change (increase or decrease) in the content of phenytoin in the blood plasma was observed. It is recommended to monitor phenytoin therapy in patients taking both drugs, including determination of phenytoin plasma levels.
Methotrexate
With the simultaneous use of methotrexate and ciprofloxacin, the renal tubular transport of methotrexate may slow down, which may be accompanied by an increase in the concentration of methotrexate in the blood plasma. This may increase the likelihood of developing side effects of methotrexate. In this regard, patients receiving concomitant therapy with methotrexate and ciprofloxacin should be closely monitored.
Tizanidine
As a result of a clinical study involving healthy volunteers with the simultaneous use of ciprofloxacin and drugs containing tizanidine, an increase in the concentration of tizanidine in the blood plasma was revealed: an increase in Cmax by 7 times (from 4 to 21 times), an increase in AUC by 10 times (from 6 to 24 times ). Hypotensive and sedative side effects are associated with increased serum concentrations of tizanidine. Therefore, the simultaneous use of ciprofloxacin and drugs containing tizanidine is contraindicated.
Duloxetine
Clinical studies have shown that the simultaneous use of duloxetine and potent inhibitors of the CYP450 1A2 isoenzyme (such as fluvoxamine) may lead to an increase in the AUC and Cmax of duloxetine. Although there is no clinical data on possible interactions with ciprofloxacin, the likelihood of such an interaction can be anticipated when ciprofloxacin and duloxetine are used concomitantly.
Ropinirole
The simultaneous use of ropinirole and ciprofloxacin, a moderate inhibitor of the CYP450 1A2 isoenzyme, leads to an increase in the Cmax and AUC of ropinirole by 60 and 84%, respectively. Monitor for adverse effects of ropinirole during coadministration with ciprofloxacin and for a short time after completion of combination therapy.
Lidocaine
In a study on healthy volunteers, it was found that the simultaneous use of drugs containing lidocaine and ciprofloxacin, a moderate inhibitor of the CYP450 1A2 isoenzyme, leads to a decrease in the clearance of lidocaine by 22% when administered intravenously. Despite the good tolerability of lidocaine, when used simultaneously with ciprofloxacin, side effects may increase due to interaction.
Clozapine
With the simultaneous use of clozapine and ciprofloxacin at a dose of 250 mg for 7 days, an increase in serum concentrations of clozapine and N-desmethylclozapine was observed by 29% and 31%, respectively. The patient's condition should be monitored and, if necessary, the dosage regimen of clozann should be adjusted during its combined use with ciprofloxacin and for a short time after completion of combination therapy.
Sildenafil
With simultaneous use of ciprofloxacin at a dose of 500 mg and sildenafil at a dose of 50 mg in healthy volunteers, a 2-fold increase in Cmax and AUC of sildenafil was observed. In this regard, the use of this combination is possible only after assessing the benefit/risk ratio.
Vitamin K antagonists
The combined use of ciprofloxacin and vitamin K antagonists (for example, warfarin, acenocoumarol, phenprocoumon, fluindone) may lead to an increase in their anticoagulant effect. The magnitude of this effect may vary depending on concomitant infections, age and general condition of the patient, so it is difficult to assess the effect of ciprofloxacin on increasing the international normalized ratio (INR). The INR should be monitored fairly frequently during co-administration of ciprofloxacin and vitamin K antagonists, as well as for a short time after completion of combination therapy.
Adverse reactions and contraindications for use
Tsiprolet very rarely causes allergic reactions. After treatment with this medication, the following side effects most often develop: dyspeptic disorders, nausea and vomiting, skin itching and rash, shortness of breath.
The use of this medicine is contraindicated in the following cases:
- during pregnancy;
- if you are allergic to ciprofloxacin and quinolone drugs;
- in adolescence and childhood;
- during lactation.
Tsiprolet is prescribed with caution to elderly patients. The medication is used only in special cases for people suffering from epilepsy, vascular pathologies, and organic diseases of the brain. Such patients are more likely to experience side effects due to taking the drug, so this antibiotic is indicated for them only in life-threatening situations. In case of allergic reactions and other complaints (for example, joint pain, myalgia), use of the medicine should be discontinued.
Special information
Tsiprolet is not effective against streptococci, so it is not prescribed for the treatment of pathologies caused by bacteria of this group. In case of severe infection by anaerobes and staphylococcal microflora, it is better to take the medication in combination with other antibiotics, which will help enhance the therapeutic effect of ciprofloxacin.
The instructions for Tsiprolet tablets indicate that this drug can have an effect on the patient’s body, changing the ability to concentrate. Therefore, it should not be used by transport drivers and persons servicing complex mechanisms and machines. It is unacceptable to use the medication in combination with alcohol. Tsiprolet is available only with a doctor's prescription.
