Factive® (Factive)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceGemifloxacinGemifloxacin
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  • Factive®
    pills inwards 
    VEROPHARM SA     Russia
    • Dosage form: & nbspFilm-coated tablets.
    Composition:

    Name

    One 160 mg tablet

    One 320 mg tablet

    Active substance

    hemifloxacin mesylate (in the form of sesquihydrate) in terms of hemifloxacin base anhydrous



    160 mg



    320 mg

    Excipients

    microcrystalline cellulose



    21.95 mg



    43.9 mg

    povidone (polyvinylpyrrolidone)

    7.35 mg

    14.7 mg

    polyplasdone X-El-10 (crospovidone)

    11.7 mg

    23.4 mg

    magnesium stearate

    3.9 mg

    7.8 mg

    Shell

    opadrai II [hypromellose (hydroxypropylmethylcellulose), lactose monohydrate, macrogol (polyethylene glycol 4000), titanium dioxide]

    6, 5 mg

    13.0 mg
    Description:Tablets covered with a film coat of white or almost white color, oblong, biconcave without risks (dosage of 160 mg) and with a risk on both sides (dosage of 320 mg).
    Pharmacotherapeutic group:antimicrobial agent, fluoroquinolone.
    ATX: & nbsp

    J.01.M.A.15   Gemifloxacin

    Pharmacodynamics:

    Gemifloxacin is an antimicrobial agent from the group of fluoroquinolones, it has a wide spectrum of bactericidal action on gram-positive, gram-negative, atypical and anaerobic microorganisms. Gemifloxacin violates the processes of replication,repair and transcription of bacterial DNA by inhibiting the enzymes of DNA-gyrase (topoisomerase II) and topoisomerase IV, necessary for bacterial growth. Gemifloxacin has a high degree of kinship with bacterial topoisomerases II (DNA-gyrase) and IV.

    Strains Streptococcus pneumonia, with mutations in the genes encoding these enzymes, are resistant to most fluoroquinolones. However, in therapeutically significant concentrations hemifloxacin It is able to inhibit altered enzymes. Thus, some strains of Streptococcus pneumonia resistant to fluoroquinolones may be susceptible to hemifloxacin. The mechanism of action of fluoroquinolones, including hemifloxacin, differs from that of beta-lactam antibiotics, macrolides, aminoglycosides and tetracyclines. There was no cross-resistance between hemifloxacin and these groups of antibiotics.
    The main mechanism of development of resistance to fluoroquinolones are mutations in the DNA-gyrase and DNA-topoisomerase IV genes, the incidence of which is 10-7 -10-10 and less.

    Gemifloxacin is active against most strains of microorganisms, both in vitro and in vivo:

    Aerobic Gram-positive microorganisms:

    Streptococcus pneumoniae (including penicillin-resistant, macrolide most resistant to ofloxacin / levofloxacin and MDRSP *), Streptococcus pyogenes (including resistant to macrolides), Streptococcus viridans, Streptococcus agalacticae, Streptococcus milleri, Streptococcus anginosius, Streptococcus constellatus, Streptococcus mitis, and other types of streptokokkov.Staphylococcus aureus (methicillin sensitive), Staphylococcus epidermidis, Staphylococcus saprophyticus, Staphylococcus haemolyticus, and other types of staphylococci. Enterococcus faecalis, Enterococcus faecium and other types of enterococci.

    * MDRSP - group strains Streptococcus pneumoniae, including subspecies previously known as PRSP (Streptococcus pneumoniae penicillin-resistant) and uniting strains resistant to two or more of the following antibiotics: penicillins, cephalosporins, 2nd generation, macrolides, tetracyclines, and trimethoprim / sulfamethoxazole .

    Aerobic Gram-negative microorganisms:

    Haemophilus influenzae (including the presence of beta-lactamase), Haemophilus parainluenzae and other species of Haemophilus.

    Moraxella catarrhalis (with negative and positive beta-lactamase) and other types of Moraxella.Klebsiella pneumoniae, Klebsiella oxutoca and other Klebsiella.Escherichia coli; Neisseria gonorrhoeae; Acinetobacter lwoffi, Acinetobacter anitartus, Acinetobacter calcoaceticus, Acinetobacter haemoliticus and other types of Acinetobacter; Citrobakter freundii, Citrobakter koserin other types of Citrobakter; Salmonella, Shigella; Enterobacter aerogenes, Enterobacter cloacae and other Enterobacter species; Serratia marcescens and other species of Serratia; Proteus mirabilis, Proteus vulgaris and other species of Proteus; Providencia; Morganella morganii and other species of Morganella; Yersinia; Pseudomonas aeruginosa and other species of Pseudomonas; Bordetella pertrussis and other species of Bordetella.

    Atypical:

    Coxiella bumetti and other types of Coxiella, Micoplasma pneumoniae and other Micoplasma, Legionella pneumophilia and other types of Legionella, Chlamidia pneumoniae and other Chlamidia.

    Anaerobic:

    Peprtostreptococcus, Clostridium non-perfringes, Clostridium perfringes and other species of Clostridium, Fusobacterium, Porphyromonas, Prevotella.

    Pharmacokinetics:

    The pharmacokinetics of hemifloxacin is linear in the dose range of 40-640 mg. The preparation practically does not cumulate (less than 30% at a dose of 640 mg for 7 days). With a course of 320 mg gemifloxacin once a day, the equilibrium concentration is reached on the third day.

    Gemifloxacin is rapidly absorbed from the gastrointestinal tract. Time to reach the maximum concentration in the plasma (TCmax) is 0.5-2 hours after taking one tablet. After repeated administration of 320 mg of the drug, its maximum concentration in the blood plasma is 1.61 ± 0.51 pg / ml (0.70-2.62 pg / ml), and the area under the concentration-time curve is 9.93 ± 3.07 μg * ml / h (4.71-20.1 μg * ml / h). Absolute bioavailability for hemifloxacin is approximately 71%.

    The intake of food practically does not change the pharmacokinetics of hemifloxacin, so the drug can be taken regardless of food.

    At repeated admission, 55-73% of the drug binds to plasma proteins, the fraction of bound fraction does not depend on age.

    The concentration of hemifloxacin in bronchoalveolar lavage is higher than that in plasma. Gemifloxacin penetrates well into lung tissue.

    In a small amount hemifloxacin is metabolized in the liver. After 4 hours after taking the unchanged hemifloxacin prevails among the metabolites of the drug (65%) in blood plasma.

    Gemifloxacin is not metabolized by the cytochrome P450 system and does not inhibit the metabolic activity of the enzymes of the cytochrome P450 system.

    In healthy subjects, 61 ± 9.5% of the dose of hemifloxacin is excreted through the intestine, and 36 ± 9.3% by the kidneys in the form of unchanged drug and metabolic products.

    The half-life period from plasma and urine is approximately 8 hours and 15 hours, respectively.

    With hemodialysis, 20-30% of the dose of hemifloxacin from plasma is excreted. The pharmacokinetics of the drug in children has not been studied.

    Age does not affect the pharmacokinetics of hemifloxacin.

    With hepatic insufficiency, a slight increase in the maximum concentration of hemifloxacin in blood plasma, which does not require dose adjustment, is possible.

    With renal failure, there is a slight increase in the time for elimination of hemifloxacin from the plasma, without changing the maximum concentration.

    Correction of the dose in patients with creatinine clearance> 40 ml / min is not required.In patients with creatinine clearance <40 ml / min, it is recommended to change the dose of the drug (see "Method of administration and dose").

    Indications:Infectious diseases caused by susceptible to hemifloxacin microorganisms:
    Community-acquired pneumonia, incl. caused by multidrug resistant strains.
    exacerbation of chronic bronchitis,
    acute sinusitis.
    Contraindications:- Hypersensitivity to hemifloxacin and other fluoroquinolones.
    - Pregnancy and lactation.
    - Children under 18 years.
    - Loss of tendons, transferred earlier due to the use of fluoroquinolones.
    Carefully:- epilepsy and predisposition to convulsive reactions
    - Elongation of QT-interval on ECG, incl. inborn.
    - deficiency of glucose-6-phosphate dehydrogenase (risk of hemolytic anemia)
    - patients receiving steroids, especially the elderly, due to the increased risk of tendon damage;
    - simultaneous reception with drugs that extend the QT-interval: antiarrhythmic drugs IA class (quinidine, procainamide) and III class (amiodarone, sotalol);
    - Patients with severe impairment of renal function;
    - patients with disturbances of water-electrolyte balance (hypokalemia, hypomagnesemia).
    Pregnancy and lactation:Factors should not be used in pregnant women, since safety in pregnant women is not established. If it is necessary to use during lactation, breastfeeding should be stopped
    Dosing and Administration:Inside. Apply regardless of food intake, without chewing, with a little water.
    The recommended daily dose is 320 mg once a day.
    Community-acquired pneumonia - 320 mg once a day - 7 days. If necessary, treatment can be extended up to 14 days.
    Exacerbation of chronic bronchitis - 320 mg once a day - 5 days.
    Acute sinusitis - 320 mg once a day - 5 days.
    Dose adjustment is not required for patients with mild to moderate renal impairment (creatinine clearance> 40 mL / min). If the severity of renal failure is severe (creatinine clearance less than 40 ml / min), as well as for patients on hemodialysis or permanent ambulatory peritoneal dialysis, the recommended dose is -160 mg once a day.
    In patients with hepatic insufficiency, dose adjustment is not required.
    In elderly patients, dose adjustment is not required.
    Side effects:Allergic reactions: sometimes itching, hives; reactions
    hypersensitivity: in some cases - Stevens-Johnson syndrome (malignant exudative erythema), toxic epidermal necrolysis (Lyell's syndrome); very rarely increased photosensitivity, allergic pneumonitis.
    From the digestive system: nausea, diarrhea; sometimes vomiting, abdominal pain, flatulence, anorexia; very rarely acute liver failure, hepatitis.
    From the nervous system: very rarely tremor, anxiety, anxiety, confusion, hallucinations, paranoid syndrome, depression, drowsiness. When symptoms of CNS lesions occur, the hemifloxacin is stopped. In some cases: sensory or sensorimotor axonal polyneuropathy, manifested by paresthesia, hyposthenia and other disorders of sensitivity, weakness.
    From the sense organs: very rarely a violation of taste and smell, visual impairment (diplopia, change in color perception), tinnitus, dizziness, hearing loss.
    From the hematopoietic system: leukopenia; rarely thrombocytopenia; very rarely pancytopenia, thrombocytopenic purpura,agranulocytosis and / or other hematologic disorders; in some cases - anemia, including hemolytic and aplastic.
    From the urinary system: rarely crystalluria; in some cases - interstitial nephritis, acute renal failure.
    From the laboratory indicators: rarely increase the sodium content, decrease the potassium concentration, increase the total bilirubin, decrease the calcium concentration, increase the number of platelets, reduce the number of neutrophils in the blood, change the hematocrit, increase the activity of "liver" transaminases, increase the concentration of creatine phosphokinase.
    From the musculoskeletal system: very rarely arthralgia, arthritis, tendovaginitis, myalgia, tendon ruptures of the shoulder, arm, Achilles tendon and other tendons.
    Other: vasculitis, superinfections (candidiasis, pseudomembranous colitis).
    Overdose:Treatment is symptomatic. The specific antidote is unknown. In cases of acute overdose, it is recommended to induce vomiting or rinse the stomach. You need abundant drinking and dynamic supervision. With hemodialysis, 20-30% of the dose of hemifloxacin from the blood plasma is excreted.
    Interaction:Antacids: the bioavailability of hemifloxacin decreases with the appointment of antacids containing aluminum, magnesium, or ferrous sulphate. Antacids should be taken at least 3 hours before or no earlier than 2 hours after taking hemifloxacin.
    Sucralfate decreases the bioavailability of hemifloxacin. Sucralfate should be taken no earlier than 2 hours after taking hemifloxacin.
    Oral contraceptives: estrogen-progesterone contraceptives slightly reduce the bioavailability of hemifloxacin. The course of treatment with hemifloxacin does not affect the pharmacokinetics of ethinyl estradiol / levonorgestrel contraceptives.
    The intake of hemifloxacin by healthy volunteers who simultaneously received probenecid increased the AUC (Area Under Curve - the area under the concentration-time curve) by an average of 45% and reduced the mean renal clearance of hemifloxacin by approximately 50%. Effects in the population at this level were not associated with an increase in the incidence of adverse events.
    Factive had no significant effect on the anticoagulant effect of heparin in healthy individuals who received stable therapy with heparin.When quinolones were used, including Factin, episodes of an increase in INR (international normalized ratio), PV (prothrombin time), or the development of clinical episodes of bleeding were noted with warfarin or its derivatives.
    Special instructions:Precautions for use
    During the treatment with hemifloxacin, it is necessary to provide a sufficient amount of fluid to maintain a normal diuresis.
    When taking the drug (as with other fluoroquinolones), photosensitization reactions may occur, therefore, it is recommended to avoid contact with direct sunlight. Treatment should be discontinued if symptoms of photosensitivity are observed (for example, skin changes resemble sunburn).
    At the first signs of tendonitis (pain and swelling in the tendon area), the drug should be discontinued, exercise should be avoided and the doctor consulted. The risk of tendon damage may increase in patients receiving glucocorticosteroids, especially the elderly, with the appearance of pain in the tendon area during exercise,inflammation or rupture of the tendon, the ceasing of the hemyfloxacin (tendon ruptures can be observed both during the treatment with any fluoroquinolone and after it).
    Pseudomembranous colitis should be suspected in patients with diarrhea that developed after the onset of treatment with hemifloxacin. The most frequent causative agent of colitis is Clostridium difficile. In most cases, cessation of reception of hemifloxacin is sufficient for the disappearance of symptoms of colitis (in rare cases it may be necessary to prescribe antibacterial drugs that are active against C. difficile).
    Effect on the ability to drive transp. cf. and fur:Care must be taken when driving a car and engaging in other potentially hazardous activities that require a high concentration of attention and speed of psychomotor reactions, especially when using ethanol at the same time.
    Form release / dosage:Tablets, film-coated 160 mg and 320 mg.
    Packaging:For 5 or 7 tablets in a contour mesh package. For 5 or 7 tablets in a jar of polymer materials.
    1 jar or 1 contour pack of 5 or 7 tablets together with the instructions for use are placed in a pack of cardboard.
    Storage conditions:In a dry, protected from light place at a temperature of no higher than 25 ° C. Keep out of the reach of children.
    Shelf life:3 years. Do not use after the expiry date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LS-001010
    Date of registration:20.10.2011
    The owner of the registration certificate:VEROPHARM SA VEROPHARM SA Russia
    Manufacturer: & nbsp
    Information update date: & nbsp2015-12-10
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