Tsefepim Dzhodas

General characteristics. Structure:

Active ingredient: 1 g of a tsefepim of a hydrochloride (in terms of tsefepy).

Excipients: L-arginine.

Pharmacological properties:

Pharmacodynamics. Antibacterial agent from group of cephalosporins IV of generation. Works bakteritsidno, breaking synthesis of a cell wall of microorganisms. Possesses a broad spectrum of activity concerning gram-positive and gram-negative bacteria, strains, resistant to aminoglycosides and/or tsefalosporinovy antibiotics of the III generation. Высокоустойчив to beta lactamelements.

It is active concerning gram-positive aerobes: Staphylococcus aureus and Staphylococcus epidermidis (only metitsillinochuvstvitelny strains), Staphylococcus hominis, Staphylococcus saprophyticus, other strains of Staphylococcus spp.; Streptococcus pyogenes (group A); Streptococcus agalactiae (group B); Streptococcus pneumoniae; other beta and hemolitic Streptococcus spp. (C,G groups, F), Streptococcus bovis (group D), Streptococcus viridans.

It is active concerning gram-negative aerobes: Pseudomonas spp. (including Pseudomonas aeruginosa, Pseudomonas putida and Pseudomonas stutzeri); Escherichia coli, Klebsiella spp. (including Klebsiella pneumoniae, Klebsiella oxytoca, Klebsiella oxaenae); Enterobacter spp. (including Enterobacter cloacae, Enterobacter aerogenes, Enterobacter agglomerans and Enterobacter sakazakii); Proteus spp. (including Proteus mirabilis and Proteus vulgaris); Acinetobacter calcoaceticus (Acinetobacter anitratum, Acinetobacter calcoaceticus subsp. Iwoff); Aeromonas hydrophila; Capnocytophaga spp.; Citrobacter spp. (including Citrobacter diversus, Citrobacter freundii); Campylobacter jejuni, Gardnerella vaginalis, Haemophilus ducreyi, Haemophilus influenzae (including the strains producing beta lactamazu; Haemophilus parainfluenzae, Hafnia alvei, Legionella spp.; Morganella morganii; Moraxella catarrhalis (including the strains producing beta lactamelements); Neisseria gonorrhoeae (including the strains producing beta lactamelements); Neisseria meningitidis, Providencia spp. (including Providencia rettgeri, Providencia stuartii); Salmonella spp.; Serratia spp. (including Serratia marcescens, Serratia liquifaciens); Shigella spp.; Yersinia enterocolitica; anaerobe bacterias: Prevotella spp. (including Prevotella melaninogenicus); Clostridium perfringens; Fusobacterium spp.; Mobiluncus spp.; Peptostreptococcus spp.; Veillonella spp.

Concedes to a ceftazidime on activity concerning Pseudomonas strains. It is inactive concerning Xanthomonas maltophilia; Bacteroides fragilis and Clostridium difficile, metitsillinoustoychivy stafilokokk, resistant to penicillin pneumococci.

Pharmacokinetics. Bioavailability of 100%. Time of achievement of the maximum concentration after intravenous (in/in) and intramuscular introduction (in oil) of introduction in a dose of 500 mg - by the end of infusion and 1-2 h respectively. The maximum concentration at introduction in oil in doses of 500 mg, 1 g and 2 g - 14, 30 and 57 mkg/ml respectively; at in introduction in doses of 250 mg and 500 mg, 1 g and 2 g - 18, 39, 82 and 164 mkg/ml respectively; time of achievement of average therapeutic concentration in plasma - 12 h; average therapeutic concentration at introduction in oil - 0.2 mkg/ml, at in/in - 0.7 mkg/ml.

High concentration are defined in urine, bile, peritoneal liquid, blister exudate, a mucous secret of bronchial tubes, a phlegm, a prostate, an appendix and a gall bladder. Gets into breast milk. Distribution volume - 0.25 l/kg, at children from 2 months to 16 years - 0.33 l/kg. Communication with proteins of plasma - 20%.

It is metabolized in a liver and kidneys for 15%. An elimination half-life (T1/2) - 2 h, the general clearance - 120 ml/min., renal clearance - 110 ml/min. It is removed by kidneys (by glomerular filtering in not changed look - 85%). T1/2 at a hemodialysis is 13 h, at continuous peritoneal dialysis - 19 h.

Indications to use:

Drug is used at the infectious and inflammatory diseases caused by sensitive microorganisms: infections of a respiratory organs (including pneumonia, bronchitis, abscess of lungs, a pleura empyema), digestive tract (including a cholangitis, cholecystitis, an empyema of a gall bladder), urinogenital ways (including pyelonephritis, a pyelitis, an urethritis, cystitis, gonorrhea), bones and joints, skin and soft tissues, peritonitis, sepsis, meningitis, contaminated wounds and burns, a febrile neutropenia, infections against the background of an immunodeficiency. Prevention of a postoperative infection.

Route of administration and doses:

Drug is used intravenously (in/in), intramusculary (in oil). To adults and children 12 years - 2 g/days in 2 receptions are more senior; a course of treatment - 7-10 days.
• At infections of urinary tract - 0.5-1 g 2 times a day. • At infections of other localization - on 1 g each 12 h.
• At the heavy course of an infection - 4 g/days in 2 receptions, with an interval of 12 h • At life-threatening infections, a febrile neutropenia - on 2 g in/in each 8 h within 7 days.
• To children (2 months are more senior) at the neoput infections of uric ways, infections of skin and soft tissues, pneumonia appoints in a dose 50 mg/kg each 12 hours. • The patient with neytropenichesky fever and bacterial meningitis –
each 8 hours. The maximum dose should not exceed the recommended dose for adults.
• At the clearance of creatinine (CC) of 30-60 ml/min. depending on weight of an infection - 0.5, 1 g or 2 g 1-2 times a day,
at KK of 11-29 ml/min. - 0.5 g, 1 g of 1 times a day, less than 11 ml/min. - once. • During a hemodialysis repeatedly enter an initial dose at the end of each session. • At peritoneal dialysis - in a usual dose each 48 h.
• For in/in introductions drug is dissolved in 10 ml (1.0 g) of sterile water for injections, by 5% solution of a dextrose or 0.9% chloride sodium solution, enter within 3-5 minutes; for intravenous infusion the prepared solution is combined
with other solutions for intravenous infusions (0.9% solution of sodium of chloride, 5% or 10% dextrose solution, Ringer's solution with a lactate and 5% dextrose solution; the maximum concentration of 40 mg/ml) also enter during
not less than 30 minutes;
• For introduction in oil drug is dissolved in sterile water for injections, by 0.9% chloride sodium solution, bacteriostatic water for injections with paraben or benzyl alcohol, in 0.5% and 1% hydrochloride lidocaine solution (1.0 g – 2.4 ml).

Features of use:

Use at pregnancy and in the period of a lactation. Use of drug at pregnancy is possible only when the estimated advantage for mother exceeds potential risk for a fruit. In need of use of drug in the period of a lactation it is necessary to resolve an issue of the breastfeeding termination.

At development of pseudomembranous colitis with long diarrhea stop administration of drug and appoint Vancomycinum (inside) or metronidazole.

Cross hypersensitivity at patients with allergic reactions to penicillin is possible. At a simultaneous heavy renal and liver failure, it is regularly necessary to define concentration of drug in plasma (carry out dose adjustment depending on clearance of creatinine). At prolonged treatment regular control of peripheral blood, indicators of a functional condition of a liver and kidneys is necessary.

At the mixed aerobic-anaerobic infection before identification of activators the combination with medicines active concerning anaerobe bacterias is reasonable.

To patients who of the remote center of an infection have a meningeal dissimination there are suspicions of meningitis or the diagnosis of meningitis is confirmed, it is necessary to appoint an alternative antibiotic with the clinical performance confirmed for this situation.

Detection of positive test of Koombs, the false positive glucose test in urine is possible.

Discoloration does not influence activity of drug.

Side effects:

Allergic reactions: skin rash (including erythematic rashes), urticaria, an itch, fever, anaphylactoid reactions, positive reaction of Koombs, an eosinophilia, a multiformny exudative erythema (including Stephens-Johnson's syndrome), it is rare - a toxic epidermal necrolysis (Lyell's disease).

From a nervous system: headache, dizziness, sleeplessness, paresthesias, feeling of concern, confusion of consciousness, spasm.

From urinogenital system: vaginitis.

From an urinary system: renal failure.

From digestive tract: diarrhea, nausea, vomiting, locks, abdominal pain, pseudomembranous coloenteritis.

From bodies of a hemopoiesis: anemia, thrombocytopenia, leukopenia, neutropenia, pancytopenia, hemolitic anemia, bleedings.

From respiratory system: cough.

From cardiovascular system: tachycardia, short wind, peripheral hypostases.

Local reactions: at intravenous administration - phlebitis, at intramuscular - a hyperemia and morbidity in an injection site.

Laboratory indicators: decrease in a hematocrit, increase in a prothrombin time, increase in concentration of urea, giperkreatininemiya, hypercalcemia, increase in activity of "hepatic" transaminases and alkaline phosphatase, hyperbilirubinemia.

Others: a pharyngalgia, a thoracalgia, the increased sweating, dorsodynias, an adynamy, development of superinfection, orofaringealny candidiasis.

Interaction with other medicines:

Pharmaceutical drug is incompatible with other antimicrobic medicines and heparin.

Diuretics, aminoglycosides, polymyxin B reduce canalicular secretion of drug and increase its concentration in blood serum, extend T1/2, increase nephrotoxicity (the risk of development of a nefronekroz increases).

Non-steroidal anti-inflammatory drugs, slowing down removal of cephalosporins, increase risk of development of bleeding.

At co-administration with bactericidal antibiotics (aminoglycosides) a synergism, with bacteriostatic (macroleads, chloramphenicol, tetracyclines) - antagonism is shown.

Contraindications:

Hypersensitivity to a tsefepim (including to other cephalosporins, penicillin, another beta лактамным to antibiotics), to arginine, children's age up to 2 months.

With care. Pregnancy, lactation period; children's age (up to 12 years – efficiency and safety are not established); digestive tract diseases (including in the anamnesis): ulcer colitis, regional enteritis or the antibiotiko-associated colitis, a renal failure.

Overdose:

Symptoms (arise at patients with a chronic renal failure more often): spasms, encephalopathy, excitement.

Treatment: hemodialysis.

Storage conditions:

To store in the dry, protected from light place, at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity 3 years. Not to use after expiry date.

Issue conditions:

According to the recipe

Packaging:

Powder for preparation of solution for intravenous and intramuscular administration of 1,0 g. On 1,0 g in the bottle of colourless glass corked by a stopper from the chlorbutyl rubber which is pressed out by an aluminum cap with a safety plastic cap. On 1 bottle together with the application instruction in a cardboard pack. For hospitals: On 10,20,48 and 100 bottles together with the application instruction in a cardboard box.