SILAFOX [Ciprofloxacin] 500 mg Film-coated tablets

SILAFOX

instructions for medical use of the medicinal product

Tradename

Silafox, Силафокс

International non-proprietary name

Ciprofloxacin, Ципрофлоксацин

Composition

Silafox 250 mg

Each film-coated tablet contains:

active ingredient: ciprofloxacin USP (as ciprofloxacin hydrochloride)   250 mg;

excipients: corn starch, hydroxypropyl cellulose , magnesium stearate, hypromellose, polyvinylpyrrolidone, titanium oxide.

Silafox 500 mg

Each film-coated tablet contains:

active ingredient: ciprofloxacin USP (as ciprofloxacin hydrochloride)   500 mg;

excipients: corn starch, hydroxypropyl cellulose , magnesium stearate, hypromellose, polyvinylpyrrolidone, titanium oxide.

Dosage form

Tablets.

Pharmacotherapeutic group

The antimicrobial agent is a fluoroquinolone .

Pharmacological properties

Silafox is a broad-spectrum antimicrobial agent, a fluoroquinolone derivative. The active substance is ciprofloxacin.

Pharmacodynamics

Ciprofloxacin inhibits bacterial DNA gyrase, disrupts DNA synthesis, growth and division of bacteria, causes pronounced morphological changes and rapid death of the bacterial cell. It acts bactericidal on gram-negative organisms during the period of rest and division (because it affects not only DNA gyrase, but also causes lysis of the cell wall), on gram-positive microorganisms - only during the period of division. Low toxicity to macroorganism cells 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 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

(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 pathogens (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).

Majority staphylococci , resistant to methicillin resistant _ and to ciprofloxacin . The sensitivity of Streptococcus pneumoniae, Enterococcus faecalis, Mycobacterium avium (located intracellularly) is moderate (high concentrations are required to suppress them).

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, because 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

After oral administration, ciprofloxacin is rapidly absorbed mainly from the small intestine. Cmax in plasma is reached after 1-2 hours. Bioavailability is about 70-80%. The values of Cmax in blood plasma and AUC increase in proportion to the dose.

After intravenous administration, Cmax of ciprofloxacin is reached at the end of the infusion. With intravenous administration, the pharmacokinetics of ciprofloxacin is linear in the dose range up to 400 mg. With the on / in the introduction 2-3 times / day, no accumulation of ciprofloxacin and its metabolites was noted.

The binding of ciprofloxacin to plasma proteins is 20-30%, the active substance is present in the blood plasma mainly in a non-ionized form. Ciprofloxacin is freely distributed in tissues and body fluids. Vd in the body is 2-3 l / kg. The concentration of ciprofloxacin in tissues significantly exceeds the concentration in blood serum. Metabolized in the liver. Four metabolites of ciprofloxacin can be detected in the blood at low concentrations: diethylciprofloxacin (Ml), sulfocyprofloxacin (M2), oxocyprofloxacin (M3), formylciprofloxacin (M4), three of which (Ml-M3) exhibit antibacterial activity in vitro, comparable to the antibacterial activity of nalidix acids. The in vitro antibacterial activity of the M4 metabolite, which is present in a smaller amount, is more consistent with that of norfloxacin. Ciprofloxacin is excreted from the body mainly by the kidneys by glomerular filtration and tubular secretion, a small amount - through the gastrointestinal tract. Renal clearance is 0.18-0.3 l/h/kg, total clearance is 0.48-0.60 l/h/kg. Approximately 1% of the administered dose is excreted in the bile. In bile, ciprofloxacin is present in high concentrations. In patients with unchanged renal function, T1 / 2 is usually 3-5 hours. In case of impaired renal function, T1 / 2 increases.

Indications for use

Uncomplicated and complicated infections caused by microorganisms sensitive to ciprofloxacin.

adults

• Respiratory tract infections - pneumonia caused by Klebsiella spp., Enterobacter spp., Proteus spp., Escherichia coli, Pseudomonas aeruginosa, Haemophilus spp., Moraxella catarrhalis, Legionella spp., Staphylococcus spp.;

• infections of the middle ear and paranasal sinuses, especially if these infections are caused by Staphylococcus spp. and gram-negative microorganisms, including Pseudomonas aeruginosa;

• kidney infections and/or complicated urinary tract infections;

• genital infections, including adnexitis, gonorrhea, prostatitis;

• infections of the abdominal cavity (bacterial infections of the gastrointestinal tract, biliary tract, peritonitis);

• skin and soft tissue infections;

• infections of bones and joints;

• sepsis;

• infections or prevention of infections in immunocompromised patients (with neutropenia);

• prevention and treatment of pulmonary anthrax.

Children

• treatment of cystic fibrosis;

• prevention and treatment of pulmonary anthrax.

The use of ciprofloxacin in children should only be started after a benefit/risk assessment due to possible side effects on the joints and periarticular tissues.

Contraindications

Hypersensitivity to ciprofloxacin or other drugs from the fluoroquinolone group, pregnancy, breastfeeding period.

Children's age: for oral administration - children's age up to 3 years, for intravenous administration - up to 18 years - until the completion of the skeletal formation process for all indications (except for the treatment of complications caused by Pseudomonas aeruginosa in children with cystic fibrosis of the lungs up to 5 years, prevention and treatment of pulmonary anthrax).

Carefully

Epilepsy, decreased seizure threshold (or history of seizures); severe atherosclerosis of cerebral vessels, cerebrovascular accident, organic brain damage or stroke; mental illness (depression, psychosis); severe renal and / or liver failure; tendon damage with previous treatment with quinolones; increased risk of QT interval prolongation or torsades de pointes (eg, congenital long QT interval syndrome, heart disease (heart failure, myocardial infarction, bradycardia), electrolyte imbalance (eg, hypokalemia, hypomagnesemia); concomitant use of drugs that prolong QT interval (including antiarrhythmic class IA and III, tricyclic antidepressants, macrolides, neuroleptics), simultaneous use with CYP1A2 isoenzyme inhibitors (including theophylline, methylxanthine, caffeine, duloxetine, clozapine, ropinirole, olanzapine, agomelatine) ; myasthenia gravis; use in elderly patients, in patients with diabetes mellitus receiving concomitant therapy with oral hypoglycemic drugs (for example, sulfonylurea drugs) or insulin.

Dosage and administration

inside. The drug should be taken on an empty stomach with a sufficient amount of liquid without chewing.

The dose depends on the severity of the disease, type of infection, body condition, age and kidney function of the patient. Recommended doses:

- uncomplicated diseases of the kidneys and urinary tract - 250 mg, and in complicated cases - 500 mg, 2 times a day;

- diseases of the lower respiratory tract of moderate severity - 250 mg, and in more severe cases - 500 mg, 2 times a day;

- gonorrhea - a single dose of 250-500 mg is recommended;

- gynecological diseases, enteritis and colitis with severe course and high fever, prostatitis, osteomyelitis - 500 mg 2 times a day (for the treatment of banal diarrhea can be used at a dose of 250 mg 2 times a day).

- in severe cases - 750 mg 2 times a day (if parenteral therapy is not carried out).

Try to take the drug every day at about the same time.

Patients with severe renal impairment should be given a half dose of the drug. The duration of treatment depends on the severity of the disease, but treatment should always be continued for at least two more days after the symptoms of the disease have disappeared. The average duration of treatment is 7-14 days.

In case of especially severe infectious diseases and the impossibility of taking pills inside, they begin with intravenous administration of the drug.

Special instructions and precautions

Prescribed with caution in: mental illness, epilepsy, lowering the convulsive threshold, apoplexy, severe atherosclerosis of cerebral vessels (risk of circulatory disorders, stroke), in old age, with severe impairment of kidney and liver function (control of plasma concentration is necessary). During the treatment period, solar and UV radiation, intense physical exertion should be avoided, drinking regime, urine pH should be controlled. May reduce the rate of psychomotor reactions, especially against the background of alcohol, which should be considered in patients working with potentially dangerous mechanisms or driving vehicles. If severe diarrhea develops, pseudomembranous colitis (in which ciprofloxacin is contraindicated) must be ruled out. Simultaneous intravenous administration of barbiturates requires monitoring of the function of the cardiovascular system (BP, ECG parameters). Adolescents under 18 years of age are prescribed only in case of resistance of the pathogen to other chemotherapeutic drugs.

The simultaneous use of the drug and dairy products or drinks enriched with minerals (for example, milk, yogurt, orange juice fortified with calcium) should be avoided, since the absorption of ciprofloxacin may decrease. Calcium, which is part of other foods, does not significantly affect the absorption of ciprofloxacin.

Use during pregnancy and during breastfeeding

Use during pregnancy and during breastfeeding is contraindicated.

Interaction with other drugs

If you are taking any other medicines, be sure to inform your doctor, and if you are self-treating, consult your doctor about the possibility of using the drug.

Simultaneous administration increases the concentration and slows down the excretion of theophylline and other xanthines (for example, caffeine, pentoxifylline, oxpentifylline), phenytoin, clozapine, oral hypoglycemic drugs, indirect anticoagulants, and helps to reduce the prothrombin index. Enhances the effect of tizanidine.

Non-steroidal anti-inflammatory drugs (excluding acetylsalicylic acid) increase the risk of seizures.

Enhances the effect of other antimicrobial drugs (beta-lactam antibiotics, aminoglycosides, clindamycin, metronidazole). 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 - with staphylococcal infections; with metronidazole and clindamycin - for anaerobic infections.

Enhances the nephrotoxic effect of cyclosporine, increases the toxicity of methotrexate.

Oral administration together with iron-containing drugs, sucralfate and antacids containing magnesium, calcium and aluminum ions, didanosine leads to a decrease in the absorption of ciprofloxacin, so it should be taken 1-2 hours before or 4 hours after taking the above funds.

Metoclopramide accelerates the absorption of ciprofloxacin.

The joint appointment of uricosuric drugs leads to a slowdown in excretion (up to 50%) and an increase in the concentration of ciprofloxacin.

Caution should be exercised when ciprofloxacin is co-administered with class I A or class III antiarrhythmic drugs, as ciprofloxacin may prolong the QT interval.

The simultaneous use of ciprofloxacin and ropinirole, preparations containing lidocaine, clozapine, sildenafil leads to an increase in the concentration and bioavailability of the latter, in connection with this, the use of these combinations is possible only after assessing the benefit / risk ratio.  

Side effect

Nausea, vomiting, anorexia, diarrhea, constipation, pseudomembranous colitis, epigastric and abdominal pain, abdominal discomfort, hiccups, ulcers, dryness and soreness of the oral mucosa, flatulence, bleeding in the gastrointestinal tract, pancreatitis, cholestatic jaundice, hepatitis, cell necrosis liver, headache, dizziness, agitation, anxiety, insomnia, nightmares, depression, phobias, fatigue, visual impairment (chromatopsia, diplopia, nystagmus, eye pain), taste, smell, tinnitus, transient hearing loss, mood change, gait disturbance, increased intracranial pressure, paresthesia, sweating, ataxia, tremor, convulsions, toxic psychosis, paranoia, hallucinations, hyperpigmentation, eosinophilia, fever, photosensitivity, leukopenia, leukocytosis, anemia, thrombocytopenia, thrombocytosis, prothrombin level change, transient increased hepatic transaminases, alkaline phosphatase, creatinine, urea, serum triglycerides , glucose, potassium, bilirubin, hypotension, syncope, cardiovascular collapse, arrhythmias, cerebral thrombosis, paroxysmal tachycardia, pulmonary embolism, dyspnea, respiratory distress, bronchospasm, pleural effusion, arthralgia, myalgia, tendovaginitis, urinary frequency, crystalluria, hematuria, cylindruria , polyuria, proteinuria, acidosis, urinary retention, hemorrhagic cystitis, nephritis, vaginitis, gynecomastia, rash, petechiae, blisters, papules, cutaneous vasculitis, Stevens-Johnson syndrome, Lyell's syndrome, erythema multiforme exudative, exfoliative dermatitis, pruritus, lip edema , face, neck, conjunctiva, extremities, angioedema, urticaria, anaphylactic shock, dysbacteriosis, candidiasis.

Overdose

Symptoms: There are no specific symptoms.

Treatment: it is necessary to carry out a gastric lavage, to ensure sufficient fluid intake.

Storage conditions

Store in a cool and dry place, at a temperature not exceeding 30º C.

Keep out of the reach of children!

Best before date

3 years. Do not use after the expiry date stated on the package.

Holiday conditions

Released by prescription.