Pharmacodynamics and pharmacokinetics
The mechanism of the antibacterial action of Siflox tablets is the inhibition of DNA gyrase, disruption of DNA function, blocking of the processes of segmental despiralization, as well as the spiralization of chromosomes during bacterial reproduction.
Effective against almost all gram(-) and gram(+) pathogens, including:
- Pseudomonas aeruginosa, Hemophilus influenzae and Escherichia coli;
- Shigella, salmonella;
- meningococci, gonococci;
- many strains of staphylococci, some enterococci;
- campylobacter, legionella, mycoplasma, chlamydia, mycobacteria.
Does not affect:
- anaerobic gram-negative bacteria Bacteroides;
- spirochetes.
Pharmacokinetics
Oral administration of Siflox tablets causes very rapid absorption of ciprofloxacin in the gastrointestinal tract, bioavailability reaches 50-85%. When taken on an empty stomach, 0.5-1.5 hours should pass to achieve the highest antibacterial concentration in serum in healthy patients. They differ depending on the dose taken:
- 250 mg – 0.76 mg/ml;
- 500 mg – 1.6 mg/ml;
- 750 mg – 2.5 mg/ml;
- 1000 mg – 3.4 mg/ml.
Siflox 500 mg No. 10 tablet p.o.
Instructions for use of the drug for specialists Siflox ® Trade name Siflox ® International nonproprietary name Ciprofloxacin Dosage form Film-coated tablets Composition One tablet contains the active substance - ciprofloxacin hydrochloride 500 mg excipients: corn starch, microcrystalline cellulose, crospovidone, magnesium stearate, silicon dioxide colloidal composition of the shell: hydroxypropyl methylcellulose, polyethylene glycol 4000, titanium dioxide Description Film-coated tablets, oval, white or yellowish in color with a dividing line on one side Pharmacotherapeutic group Antibacterial drugs-quinolone derivatives. Fluoroquinolones. ATC code J01MA02 Pharmacological properties Pharmacokinetics Absorption When taken orally, Siflox is rapidly absorbed from the gastrointestinal tract. The bioavailability of the drug is 50-85%. The maximum concentration in serum in healthy people when used before meals is achieved after 0.5-1.5 hours. The maximum serum concentrations after oral administration of 250,500,750 and 1000 mg of the drug are 0.76; 1.6; 2.5 3.4 µg/ml. Orally administered ciprofloxacin is widely distributed in body tissues and fluids and creates high concentrations in bile, lungs, kidneys, liver, gallbladder, uterus, seminal fluid, prostate tissue, tonsils, endometrium, fallopian tubes and ovaries. The concentration of ciprofloxan in these tissues is higher than in serum. In addition, ciprofoxacin penetrates well into bones, ocular fluid, bronchial mucus, saliva, skin, muscles, adipose and cartilage tissues, pleura, peritoneum, ascitic fluid and lymph. The concentration in neutrophils is high, 2-7 times higher than in serum. The volume of distribution in the body is 2-3.5 l/kg. Ciprofloxacin penetrates into the cerebrospinal fluid in small quantities. The concentration in the cerebrospinal fluid is 6-10% of the concentration in the serum. The degree of binding of ciprofloxain to plasma proteins is about 30%. Elimination In patients with normal renal function, the half-life is 3-5 hours, and in patients with impaired renal function it is longer. The drug is mainly excreted from the body by the kidneys (50-70% in urine, and 15-30% in excrement). Patients with severe renal failure (creatinine clearance below 20 ml/min/1.73 m) should take half the daily dose. Pharmacodynamics The main mechanism of action is the inhibition of bacterial DNA gyrase. Antibacterial action Sensitive bacteria (MIC below 1 µg/ml): E.coli, Klebsiella, Enterobacter, Serratia, Proteus(indol+), Proteus(indol-), Citrobacter, Shigella, Salmonella, Pseudomonas aeruginosa, Haemophilus, Staphilococcus, Neisseria gonorrhoeae, Providencia ,Morganella, Yersinia, Vibrio, Aeromonas, Pasteurella, Gardnerella, Campylobacter, Legionella, Corynebacterium. Bacteria of moderate sensitivity: Acinetobacter, Streptococcus (Strept. Pneumoniae, Strept. Faecalis), Fusobacterium, Peptococcus, Clostridium, Actiinomyces, Veillonella, Chlamediae, Mycoplazma, Mycobacterium tuberculosis, Listeria. Bacteria difficult to be affected by the drug: Gram-negative anaerobic bacteria (Bacteroides), spirochetes. Sensitivity tests Certain cations (such as magnesium) contained in the pH of the culture medium used may influence the results obtained. The pH environment is considered optimal in the range of 6-8. If the pH is below 6, then the resulting MIC values are 4-16 times higher. When using the Curby-Bauer disk diffusion method, 5 microgram ciprofloxacin disks are used. Bacteria with an inhibition zone of 15 mm or less are considered resistant, while those with an inhibition zone of 21 mm or more are considered sensitive. Indications for use - gonorrhea and non-gonococcal urethritis - pneumonia, bronchitis, etc. - infections of the skin and soft tissues (postoperative wound infection, infections due to diabetes mellitus, infected bedsores, etc.) - osteomyelitis, septic arthritis, etc. - adnexitis and prostatitis - biliary tract infections - infections in obstetrics and gynecology - gastrointestinal tract infections - infections of the middle ear and paranasal sinuses - eye infections - peritonitis - sepsis - prevention and treatment of infections in patients with reduced immunity, incl. during treatment with immunosuppressants and with neutropenia. Method of administration and dose Set individually depending on the location and severity of the infection, as well as the sensitivity of the pathogen. - for simple urinary tract infections - 2 times a day, 250 mg - for severe urinary tract infections - 2 times a day, 500 mg - for severe respiratory tract infections, osteomyelitis: 2 times a day, 750 mg - for other severe infections: 2 times per day 500 mg - for acute gonorrhea - 250 mg once. The course of treatment with the drug is prescribed individually by the attending physician. If creatinine clearance in cases of renal failure is below 20 mg/min, then half the dose should be used. Treatment usually continues for 72 hours after clinical and bacteriological recovery. Side effects - nausea, vomiting, diarrhea, lack of appetite - dizziness, headache, insomnia, anxiety - rash, itching, swelling of the tongue - eosinophilia, leukocytosis Very rare - parxysmal tachycardia, migraine - thrombocytopenia, changes in prothrombin levels - joint pain and sensitivity to light - increased liver transaminases and alkaline phosphatase Contraindications - hypersensitivity to the drug, as well as children before the end of the growth period - children under 15 years of age - pregnancy and lactation Drug interactions Antacids containing magnesium and aluminum slow down the absorption process of the drug. Ciprofloxacin should be taken two hours before or two hours after taking antacids. With the simultaneous use of ciprofloxacin and theophylline, the concentration in the blood of the latter may increase. In such cases, it is necessary to adjust the dose of theophylline. Special instructions In patients with a history of seizures, ciprofloxacin should be taken after appropriate anticonvulsant therapy. During treatment with the drug, patients should receive sufficient fluids. When taken on an empty stomach, the absorption process accelerates. Features of the effect of the drug on the ability to drive a vehicle or operate potentially dangerous mechanisms Ciprofloxacin can cause a decrease in attention and reactions, therefore patients taking ciprofloxacin should limit activities associated with the need for rapid concentration and high reactivity. Alcohol can increase the impact of unfavorable factors. Overdose Symptoms: increased side effects Treatment: symptomatic Release form and packaging 10 tablets each in a blister pack made of polyvinyl chloride film and varnished aluminum foil. The contour cell packaging along with instructions for use in the state and Russian languages is enclosed in a cardboard box. Storage conditions Store in a dry place, protected from light, at a temperature from +18°C to +25°C. Keep out of the reach of children! Shelf life: 4 years The drug cannot be used after the expiration date indicated on the package. Conditions for dispensing from pharmacies By prescription Manufacturer Ejzacibashi Saglik Yugunleri San.ve Ticaret A.Sh. Kucukkaristiran 39780 Luleburgaz Kirklareli-Turkey Eczacibasi Saglik Urunleri San.ve Tic.AS Kucukkaristiran 39780 Luleburgaz- Kirklareli-Tyrkey
Side effects
- dyspeptic disorders, including nausea, vomiting, diarrhea , lack of appetite;
- headache;
- insomnia;
- dizziness;
- anxiety;
- skin rashes and itching ;
- swelling of the tongue and/or pharynx;
- leukopenia;
- eosinophilia;
- leukocytosis.
Rare adverse reactions:
- paroxysmal tachycardia ;
- arthralgia;
- crystalluria;
- increased levels of transaminases and alkaline phosphatases in the blood.
Moxiflo
In some cases, after the first use of the drug, hypersensitivity and allergic reactions may develop, which should be reported to your doctor immediately. Very rarely, even after the first use of the drug, anaphylactic reactions can progress to life-threatening anaphylactic shock. In these cases, treatment with moxifloxacin should be stopped and the necessary therapeutic measures (including anti-shock) should be started immediately.
QT interval prolongation may occur in some patients when using moxifloxacin. Moxifloxacin should be used with caution in women and elderly patients. Because women have a longer QT interval than men, they may be more sensitive to drugs that prolong the QT interval. Elderly patients are also more susceptible to drugs that affect the QT interval.
Prolongation of the QT interval is associated with an increased risk of ventricular arrhythmias, including polymorphic ventricular tachycardia.
The degree of QT interval prolongation may increase with increasing drug concentrations, so the recommended dose should not be exceeded. However, in patients with pneumonia, no correlation was observed between moxifloxacin plasma concentrations and QT interval prolongation. None of the 9,000 patients treated with moxifloxacin experienced cardiovascular complications or deaths associated with QT prolongation. When using moxifloxacin, the risk of developing ventricular arrhythmias may increase in patients with conditions predisposing to arrhythmias. In this regard, moxifloxacin is contraindicated in:
- changes in electrophysiological parameters of the heart, expressed in prolongation of the QT interval: congenital or acquired documented prolongation of the QT interval, electrolyte disturbances, especially uncorrected hypokalemia, clinically significant bradycardia; clinically significant heart failure with reduced left ventricular ejection fraction; a history of rhythm disturbances accompanied by clinical symptoms;
- use with other drugs that prolong the QT interval (see section “Interaction with other drugs”).
Moxifloxacin should be used with caution:
- in patients with potentially proarrhythmic conditions, such as acute myocardial ischemia and cardiac arrest;
- in patients with liver cirrhosis (since in this category of patients the risk of developing a prolongation of the QT interval cannot be excluded).
Cases of fulminant hepatitis, potentially leading to liver failure (including fatal cases), have been reported with the use of moxifloxacin (see section "Side effects"). The patient should be informed that if symptoms of liver failure occur, it is necessary to consult a doctor before continuing treatment with moxifloxacin.
Cases of bullous skin lesions such as Stevens-Johnson syndrome or toxic epidermal necrolysis have been reported with the use of moxifloxacin (see section "Side effects"). The patient should be informed that if symptoms of skin or mucous membrane lesions occur, they should consult a doctor before continuing treatment with moxifloxacin.
The use of quinolone drugs is associated with a possible risk of developing seizures. Moxifloxacin should be used with caution in patients with central nervous system diseases and central nervous system disorders that predispose to seizures or lower the threshold for seizure activity.
The use of broad-spectrum antibacterial drugs, including moxifloxacin, is associated with a risk of developing pseudomembranous colitis. This diagnosis should be considered in patients who develop severe diarrhea during treatment with moxifloxacin. In this case, appropriate therapy should be prescribed immediately. Drugs that inhibit intestinal motility are contraindicated in the development of severe diarrhea.
Moxifloxacin should be used with caution in patients with myasthenia gravis due to possible exacerbation of the disease.
During therapy with quinolones, including moxifloxacin, tendonitis and tendon rupture may develop, especially in the elderly and patients receiving glucocorticosteroids. Cases have been described that occurred within several months after completion of treatment. At the first symptoms of pain or inflammation at the site of injury, the drug should be stopped and the affected limb should be unloaded.
When using quinolones, photosensitivity reactions are observed. However, during preclinical and clinical studies, as well as with the use of moxifloxacin in practice, no photosensitivity reactions were observed. However, patients receiving moxifloxacin should avoid exposure to direct sunlight and ultraviolet light.
The use of moxifloxacin in the form of oral tablets is not recommended in patients with complicated pelvic inflammatory diseases (for example, associated with tubo-ovarian or pelvic abscesses).
The use of moxifloxacin is not recommended to treat infections caused by methicillin-resistant Staphylococcus aureus (MRSA). In cases of suspected or confirmed infections caused by MRSA, treatment with appropriate antibacterial drugs should be prescribed (see section "Pharmacodynamics").
The ability of moxifloxacin to inhibit the growth of mycobacteria may cause in vitro interaction of moxifloxacin with the test for Mycobacterium spp., leading to false negative results when analyzing samples from patients who are being treated with the drug during this period.
In patients treated with quinolones, including moxifloxacin, cases of sensory or sensorimotor polyneuropathy leading to paresthesia, hypoesthesia, dysesthesia or weakness have been described. Patients treated with moxifloxacin should be warned to seek immediate medical attention before continuing treatment if symptoms of neuropathy, including pain, burning, tingling, numbness or weakness, occur (see section "Side Effects").
Psychiatric reactions may occur even after the first use of fluoroquinolones, including moxifloxacin. In very rare cases, depression or psychotic reactions progress to the occurrence of suicidal thoughts and behavior with a tendency to self-harm, including suicide attempts (see section "Side effects"). In case of development of any side effects from the central nervous system, including mental disorders, you should immediately discontinue Moxiflo and begin appropriate therapy. In these cases, it is recommended to switch to therapy with an antibiotic other than a fluoroquinolone, if possible. Caution should be exercised when using moxifloxacin in patients with psychosis and/or a history of psychiatric illness.
Due to the widespread and increasing incidence of infections caused by fluoroquinolone-resistant Neisseria gonorrhoeae, moxifloxacin monotherapy should not be used in the treatment of patients with pelvic inflammatory disease. unless the presence of fluoroquinolone-resistant Neisseria gonorrhoeae is excluded. If the presence of fluoroquinolone-resistant Neisseria gonorrhoeae cannot be excluded, consideration should be given to supplementing empiric moxifloxacin therapy with an appropriate antibacterial drug that is active against Neisseria gonorrhoeae (eg, a cephalosporin).
Dysglycemia
As with other fluoroquinolones, changes in blood glucose concentrations, including hypo- and hyperglycemia, including the development of hypoglycemic coma, were observed when using moxifloxacin. During therapy with moxifloxacin, dysglycemia occurred more often in elderly patients and patients with diabetes mellitus receiving concomitant therapy with oral hypoglycemic drugs (for example, sulfonylureas) or insulin. It is necessary to inform patients about the symptoms of hypoglycemia (confusion, dizziness, ravenous appetite, headache, nervousness, palpitations or increased pulse rate, pale skin, perspiration, trembling, weakness). If the patient develops hypoglycemia, treatment with moxifloxacin should be discontinued immediately and appropriate therapy should be initiated. In these cases, it is recommended to switch to therapy with an antibiotic other than a fluoroquinolone, if possible. When treating elderly patients with moxifloxacin and patients with diabetes mellitus, careful monitoring of blood glucose concentrations is recommended.
Siflox, instructions for use (Method and dosage)
Siflox tablets should be taken orally.
Uncomplicated urinary tract infections:
- daily dose: 500 mg, divided into 2 doses per day.
Severe urinary tract infections:
- daily dose: 1000 mg, divided into 2 doses per day.
Severe respiratory tract infections or osteomyelitis:
- daily dose: 1500 mg, divided into 2 doses per day.
Other infections:
- daily dose: 100 mg, divided into 2 doses per day.
Acute gonorrhea:
- a single dose of 250 mg.
Duration of treatment
- for gonorrhea - 1 day;
- for infections of the kidneys and ureters: 7-10 days;
- streptococcal infections - 10 days or more.
Patients with creatinine clearance less than 20 mg per minute are prescribed half the dose and treatment is continued for another 3 days after complete clinical recovery and positive microbiological tests.
Prevention of crystalluria requires ensuring sufficient fluid intake.
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** The Drug Directory is intended for informational purposes only. For more complete information, please refer to the manufacturer's instructions. Do not self-medicate; Before starting to use the drug Siflox, you should consult a doctor. EUROLAB is not responsible for the consequences caused by the use of information posted on the portal. Any information on the site does not replace medical advice and cannot serve as a guarantee of the positive effect of the drug.
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Analogs
Level 4 ATC code matches:
Hyleflox
Leflobakt
Lefoccin
Gatifloxacin
Ofloxacin
Faktiv
Tigeron
Lebel
Zanotsin
Lomefloxacin
Eleflox
Lomflox
Pefloxacin
Tsiprobay
Sparflo
Tariwid
Zoflox
Abaktal
Moxifloxacin
Levofloxacin
The list of substitutes includes:
- Ciprofloxacin
- Tsiprolet
- Procipro
- Tsifran
- Oftocipro
- Tsiprinol
