Universal reference book for medicines
Product name: FACTIVE

Active substance: gemifloxacin

Type: Antibacterial drug of the group of fluoroquinolones

Manufacturer: VEROPHARM (Russia)
Composition, form of production and packaging
The tablets covered with a film membrane of
white or almost white color, oblong, biconcave, without risks.

1 tab.

hemifloxacin (in the form of mesylate sesquihydrate) 160 mg

Excipients: microcrystalline cellulose - 21.95 mg, povidone (polyvinylpyrrolidone) - 7.35 mg, crospovidone (polyplasdone X-El-10) - 11.7 mg, magnesium stearate - 3.9 mg.

The composition of the shell: opadrai II (hypromellose (hydroxypropylmethylcellulose), lactose monohydrate, macrogol (polyethylene glycol), titanium dioxide) - 6.5 mg.

5 pieces.
- packings of cellular contour (1) - packs cardboard.
7 pcs.
- packings of cellular contour (1) - packs cardboard.
5 pieces.
- polymer cans (1) - packs of cardboard.
7 pcs.
- polymer cans (1) - packs of cardboard.
The tablets covered with a film membrane of white or almost white color, oblong, biconcave, with a risk from both sides.

1 tab.

hemifloxacin (in the form of mesylate sesquihydrate) 320 mg

Excipients: microcrystalline cellulose - 43.9 mg, povidone (polyvinylpyrrolidone) - 14.7 mg, crospovidone (polyplasdone X-El-10) - 23.4 mg, magnesium stearate - 7.8 mg.

Sheath composition: opadrai II (hypromellose (hydroxypropylmethylcellulose), lactose monohydrate, macrogol (polyethylene glycol), titanium dioxide) - 13 mg.

5 pieces.
- packings of cellular contour (1) - packs cardboard.
7 pcs.
- packings of cellular contour (1) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.

The product description was approved by the manufacturer for the 2009 print edition.

PHARMACHOLOGIC EFFECT

Antibacterial drug of the group of fluoroquinolones.
Has a bactericidal effect. It disrupts 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 affinity with bacterial topoisomerases II and IV.
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 .
Strains of Streptococcus pneumonia, with mutations in the genes encoding these enzymes, are resistant to most fluoroquinolones.
However, in therapeutically significant concentrations, hemifloxacin is able to inhibit the altered enzymes. Thus, some strains of Streptococcus pneumonia resistant to fluoroquinolones may be susceptible to hemifloxacin.
The drug is active against a wide range of microorganisms , both in vitro and in vivo: Gram-positive aerobic bacteria : Streptococcus spp., Incl.
Streptococcus pneumoniae (including strains resistant to penicillin and macrolides and most ofloxacin / levofloxacin-resistant strains, including a group of Streptococcus pneumoniae strains, including a subspecies previously known as PRSP (Streptococcus pneumoniae resistant to penicillin), and combining strains resistant to penicillin two or more of the following antibiotics: penicillins, second-generation cephalosporins, macrolides, tetracyclines and trimethoprim / sulfamethoxazole), Streptococcus pyogenes (including macrolide resistant), Streptococcus viridans, Streptococcus agalactiae, Streptococcus milleri, Streptococcus angiosus, Streptococcus con stellatus, Streptococcus mitis; Staphylococcus spp. (including Staphylococcus aureus / susceptible to methicillin /, Staphylococcus epidermidis, Staphylococcus saprophyticus, Staphylococcus haemolyticus), Enterococcus spp. (including Enterococcus faecalis, Enterococcus faecium); Gram-negative aerobic bacteria : Haemophilus spp. (including Haemophilus influenzae, including strains producing α-lactamases, Haemophilus parainluenzae), Moraxella spp. (including Moraxella catarrhalis, producing and non-producing? -lactamase), Klebsiella spp. (including Klebsiella pneumoniae, Klebsiella oxytoca), Escherichia coli, Neisseria gonorrhoeae, Acinetobacter spp. (including Acinetobacter lwoffii, Acinetobacter anitartus, Acinetobacter calcoaceticus, Acinetobacter haemolyticus), Citrobacter spp.(including Citrobaсter freundii, Citrobaсter koseri), Salmonella spp., Shigella spp., Enterobacter spp. (including Enterobacter aerogenes), Serratia spp. (including Serratia marcescens), Proteus spp. (including Proteus mirabilis, Proteus vulgaris), Providencia spp., Morganella spp. (including Morganella morganii), Yersinia spp., Pseudomonas spp. (including Pseudomonas aeruginosa), Bordetella spp. (including Bordetella pertrussis); as well as atypical bacteria : Coxiella spp. (including Coxiella burnetti), Mycoplasma spp. (including Mycoplasma pneumoniae), Legionella spp. (including Legionella pneumophila), Chlamydia spp. (including Chlamydia pneumoniae); anaerobic bacteria : Peptostreptococcus spp., Clostridium spp. (including Clostridium non-perfringes, Clostridium perfringes), Fusobacterium spp., Porphyromonas spp., Prevotella spp.
PHARMACOKINETICS

Suction

After ingestion, hemifloxacin is rapidly absorbed from the digestive tract.
After a single dose of 320 mg C max in the blood plasma is achieved within 0.5-2 hours after repeated administration of 320 mg C max in blood plasma is 1.61 ± 0.51 μg / ml (0.70-2.62 / μg / ml), and AUC - 9.93 ± 3.07 μg x h / ml (4.71-20.1 μg x h / ml). The intake of food practically does not change the pharmacokinetics of hemifloxacin, therefore the drug can be taken regardless of the food intake. The pharmacokinetics of hemifloxacin is linear in the dosage range of 40-640 mg. The preparation practically does not cumulate (less than 30% at a dose of 640 mg for 7 days).
Distribution

With a course of 320 mg gemifloxacin 1 time / day C max is achieved on the third day.
At repeated admission, 55-73% of the drug binds to plasma proteins, the fraction of the bound fraction does not depend on age.
Gemifloxacin penetrates well into the lung tissue.
The concentration of hemifloxacin in bronchoalveolar lavage is higher than that in plasma.
Metabolism

In a small amount, hemifloxacin is metabolized in the liver.
After 4 hours after administration, unchanged hemifloxacin is predominant among the metabolites of the drug (65%) in the blood plasma.
Gemifloxacin is not biotransformed with microsomal hepatic enzymes of the cytochrome P 450 system .

Excretion

In healthy subjects, 61.0 ± 9.5% of the dose of hemifloxacin is excreted through the intestines, and 36.0 ± 9.3% in the urine in the form of unchanged drug and metabolic products.

At a hemodialysis from plasma 20-30% of a dose of hemifloxacin is deduced.

Pharmacokinetics in special clinical cases

The pharmacokinetics of the drug in children has not been studied.

In adults, age does not affect the pharmacokinetics of hemifloxacin.

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

With renal insufficiency, there is a slight increase in the time for elimination of hemifloxacin from plasma without changing the C max .

INDICATIONS

Infectious-inflammatory diseases caused by microorganisms sensitive to the preparation:

- exacerbation of chronic bronchitis;

- Community-acquired pneumonia (including caused by multidrug-resistant strains);

acute sinusitis.

DOSING MODE

Assign 320 mg 1 time / day.
With an exacerbation of chronic bronchitis treatment course is 5 days, with community-acquired pneumonia - 7 days, with acute sinusitis- 5 days.
For mild and moderate renal dysfunction (KC more than 40 ml / min), dose adjustment is not required.
For severe renal dysfunction (CC less than 40 ml / min),as well as for patients on continuous hemodialysis and long-term outpatient peritoneal dialysis, the recommended dose is 160 mg 1 time / day.
Older patients , patients with impaired liver function, do not need to change the dosage regimen.

Tablets should be taken orally, without chewing, washed down with a small amount of water, regardless of food intake.

SIDE EFFECT

Allergic reactions: sometimes - itching, hives;
in some cases - Stevens-Johnson syndrome (malignant exudative erythema), toxic epidermal necrolysis (Lyell's syndrome), increased photosensitivity, allergic pneumonitis.
On the part of the digestive system: nausea, diarrhea;
sometimes - vomiting, abdominal pain, flatulence, anorexia; rare - acute liver failure, hepatitis, increased activity of hepatic transaminases, the level of total bilirubin.
From the side of the central nervous system and peripheral nervous system: rarely - tremor, anxiety, anxiety, confusion, hallucinations, paranoid syndrome, depression, drowsiness (when symptoms of CNS damage occur, cease hemifloxacin);
in some cases - sensory or sensorimotor axonal polyneuropathy, manifested by paresthesias, hypoesthesia and other disorders of sensitivity, weakness.
From the senses: rarely - a violation of taste and smell, visual impairment (diplopia, change in color perception), tinnitus, dizziness, hearing loss.

From the hematopoietic system: sometimes - leukopenia;
rarely - thrombocytopenia; in some cases - pancytopenia, thrombocytopenic purpura, agranulocytosis, anemia (including hemolytic and aplastic).
From the side of the urinary system: rarely - crystalluria;
in some cases - interstitial nephritis, acute renal failure.
From the musculoskeletal system: rarely - arthralgia, arthritis, tendovaginitis, myalgia, ruptures of tendons of the shoulder, arm, Achilles tendon and other tendons.

On the part of laboratory indicators: rarely - increase the sodium content, decrease the potassium level, decrease the level of calcium, change the hematocrit, increase the activity of CK.

Other: rarely - vasculitis, superinfection (candidiasis, pseudomembranous colitis).

CONTRAINDICATIONS

- Pregnancy;

- the period of lactation (breastfeeding);

- children and adolescence under 18;

- prolongation of QT interval on ECG (including congenital);

- affections of tendons, transferred earlier due to the use of fluoroquinolones;

- individual intolerance to hemifloxacin and other fluoroquinolones.

Caution should be given to the drug at an increased risk of arrhythmias (including clinically significant bradycardia and acute myocardial ischemia), glucose-6-phosphate dehydrogenase deficiency (risk of hemolytic reaction), patients, especially the elderly, who receive SCS (due to the increased risk of tendon damage) , with epilepsy and a tendency to convulsions, with simultaneous reception with drugs that extend the QT interval (antiarrhythmic drugs I A class (quinidine, procainamide) and III class (amiodarone, sotalol), with impairment
s water and electrolyte balance (hypokalemia, hypomagnesemia).
PREGNANCY AND LACTATION

The drug is contraindicated for use in pregnancy.
If it is necessary to use the drug during lactation, breastfeeding should be stopped.
APPLICATION FOR FUNCTIONS OF THE LIVER

For mild and moderate renal dysfunction (KC more than 40 ml / min), dose adjustment is not required.
For severe renal dysfunction (CC less than 40 ml / min),as well as for patients on continuous hemodialysis and long-term outpatient peritoneal dialysis, the recommended dose is 160 mg 1 time / day.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

patients with hepatic dysfunction are not required to change the dosage regimen.

APPLICATION FOR CHILDREN

Contraindicated: children and adolescence under 18 years.

APPLICATION IN ELDERLY PATIENTS

With caution should prescribe the drug to patients, especially the elderly, receiving SCS (due to the increased risk of tendon damage),

SPECIAL INSTRUCTIONS

During the treatment with hemifloxacin, it is necessary to ensure the supply of a sufficient amount of fluid while observing 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).

The risk of tendon damage may increase in patients receiving SCS, especially elderly patients.
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.
In patients with diarrhea that developed after the initiation of treatment by Actual, it is possible to presume the development of pseudomembranous colitis.
The most frequent causative agent of colitis is Clostridium difficile. In most cases, discontinuation of the drug is sufficient to eliminate the symptoms of colitis (in rare cases it may be necessary to prescribe antibacterial drugs that are active against Clostridium difficile).
Impact on the ability to drive vehicles and manage mechanisms

Care must be taken when driving a car and engaging in other potentially dangerous activities that require increased attention and speed of psychomotor reactions, especially when using ethanol at the same time.

OVERDOSE

Treatment: gastric lavage, artificial vomiting, abundant drinking, if necessary, conduct symptomatic therapy.
The specific antidote is unknown. In hemodialysis, 20-30% of the dose of hemifloxacin is excreted from the blood plasma.
DRUG INTERACTION

With concomitant administration of Faktive with antacids containing aluminum and magnesium or with ferrous sulfate, the bioavailability of hemifloxacin is reduced.Antacids should be taken at least 3 hours before or no earlier than 2 hours after taking hemifloxacin.

Sucralfate with simultaneous use reduces the bioavailability of hemifloxacin.
Sucralfate should be taken no earlier than 2 hours after taking hemifloxacin.
Estrogen-progestational oral contraceptives slightly reduce the bioavailability of hemifloxacin.

The course of treatment with hemifloxacin does not affect the pharmacokinetics of oral contraceptives containing ethinylestradiol / levonorgestrel.

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

List B. The drug should be stored in a dry, protected from light and out of reach of children at a temperature of no higher than 25 ° C.
Shelf life - 3 years.
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