Tsepim
Tsepim: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. Drug interactions
- 13. Analogs
- 14. Terms and conditions of storage
- 15. Terms of dispensing from pharmacies
- 16. Reviews
- 17. Price in pharmacies
Latin name: Cepim
ATX code: J01DE01
Active ingredient: Cefepime (Cefepime)
Manufacturer: JSC SINTEZ (Russia)
Description and photo update: 02.04.
Tsepim - antibacterial drug, cephalosporin; effective in infectious and inflammatory pathologies caused by microorganisms sensitive to cefepime.
Release form and composition
The dosage form of Tsepim is a powder for the preparation of a solution for intravenous (i / v) and intramuscular (i / m) administration: hygroscopic, white or white with a yellowish tint.
The medicinal product in various dosages is placed in cardboard boxes in the following configurations:
- 1 cell contour package, which contains 1 bottle containing 0.5 or 1 g of powder complete with a solvent (water for injection or sodium chloride solution 0.9%) - 1 or 2 ampoules of 5 ml each (with an ampoule knife or scarifier if necessary for ampoules of this type);
- 1 cell contour package, which contains 5 vials containing 0.5 or 1 g of powder each with a solvent (water for injection or sodium chloride solution 0.9%) - 5 or 10 ampoules of 5 ml (with an ampoule knife or scarifier, if necessary for ampoules of this type);
- 1 cell contour package, which contains 5 bottles containing 0.5 or 1 g of powder;
- 2 cell contour packages, each of which contains 5 bottles containing 0.5 or 1 g of powder;
- 1, 5 or 10 vials of 10 or 20 ml each containing 0.5 or 1 g of powder.
Each pack also contains instructions for the use of Tsepim.
Composition for 1 bottle / ampoule of powder:
- active substance: cefepime hydrochloride monohydrate (in terms of cefepime) - 0.5 or 1 g;
- auxiliary component: arginine.
Pharmacological properties
Pharmacodynamics
Cefepime is one of the antibacterial drugs from the group of IV generation cephalosporins. It is characterized by bactericidal activity, manifested in the violation of the synthesis of the cell wall of microorganisms. The substance has a wide spectrum of action against gram-positive and gram-negative bacteria and strains resistant to antibiotics (aminoglycosides and / or cephalosporins of the third generation). It exhibits high resistance to hydrolysis of most β-lactamases and quickly penetrates into gram-negative bacterial cells, inside which there are molecular targets - penicillin-binding proteins.
According to in vitro and in vivo studies, the drug is active against the following microorganisms:
- gram-positive aerobes: streptococcus viridans, pyogenic streptococcus (group A), pneumococcus, Staphylococcus aureus (methicillin-sensitive strains only);
- gram-negative aerobes: Pseudomonas aeruginosa, Proteus mirabilis, Friedlander's bacillus, Escherichia coli, Enterobacter.
In vitro, cefepime is active against the following microorganisms:
- gram-positive aerobes: streptococcus agalactia (group B), saprophytic staphylococcus, epidermal staphylococcus (only strains sensitive to methicillin);
- gram-negative aerobes: serration marcescens, Stewart's providence, Rettger's providence, Proteus vulgaris, Morgan's bacterium, moraxella catarralis (including strains producing β-lactamases), Klebsiella oxytoca, hafnias, Haemophilus influenzae (including strains producing β-lactamase) Citrobacter Freundi, Citrobacter Diversus, Acinetobacters.
Most strains of enterococci, including fecal enterococcus, methicillin-resistant staphylococci, stenotrofomonas maltophilia and clostridium difficile, are not sensitive to Tsepim.
Pharmacokinetics
The bioavailability of cefepime is 100%. Following parenteral administration of 500 mg chainsWe T Cmax (time to reach maximum concentration) in the blood plasma at / in a corresponding duration infusion, by injection / m - h is 1-2 C. Max (maximum concentration) of the substance with / in a at a dose of 500/1000/2000 mg, respectively, reaches 0.014 / 0.03 / 0.057 mg per 1 ml, with an intramuscular injection at a dose of 250/500/1000/2000 mg - 0.018 / 0.039 / 0.082 / 0.164 mg per ml. Time to reach the average therapeutic concentration in blood plasma - 12 hours; with intramuscular administration, this indicator is 0.0002 mg per 1 ml, with intravenous administration - 0.0007 mg per 1 ml.
In high concentrations, the drug is determined in the gallbladder, bile, appendix, prostate gland, sputum, mucous secretions of the bronchi, exudate of blisters, peritoneal fluid and urine.
The volume of distribution in adults is 0.25 l per 1 kg, in children aged 2 months to 16 years - 0.33 l per 1 kg. The drug binds to plasma proteins at a level of 20%.
The metabolism is carried out in the kidneys and liver by 15%. The half-life of cefepime from blood plasma is 2 hours, the total clearance is 120 ml per minute, and the renal clearance is 110 ml per minute. Excretion is carried out unchanged by the kidneys through glomerular filtration (85%) and in breast milk. The half-life with hemodialysis is 13 hours, with continuous peritoneal dialysis - 19 hours.
Indications for use
Powder for the preparation of a solution for intravenous and intramuscular administration. Tsepim is prescribed for the treatment of infectious and inflammatory diseases caused by microorganisms sensitive to cefepime:
- moderate and severe pneumonia caused by enterobacter, Pseudomonas aeruginosa, Klebsiella pneumonia, pneumococcus, including cases associated with concomitant bacteremia;
- febrile neutropenia (empiric treatment);
- complicated and uncomplicated urinary tract infections, including pyelonephritis, caused by Escherichia coli, Klebsiella pneumoniae or Proteus mirabilis;
- uncomplicated infections of the skin and soft tissues caused by Streptococcus pyogenic or Staphylococcus aureus (only strains sensitive to methicillin);
- complicated intra-abdominal infections caused by bacteroids Fragilis, Enterobacter, Pseudomonas aeruginosa, Klebsiella pneumoniae, Escherichia coli (combined therapy with metronidazole);
- prevention of infections during abdominal surgery.
Contraindications
Absolute:
- children's age: intravenous route of administration - up to 2 months; i / m route of administration - up to 12 years;
- lactation period;
- established hypersensitivity to the components of the drug, as well as to antibacterial agents from the group of cephalosporins, penicillins and other β-lactam antibiotics.
Relative (taking Tsepim requires special care and careful medical supervision):
- chronic renal failure;
- pathology of the gastrointestinal tract, including a history of antibiotic-associated colitis, regional enteritis, ulcerative colitis, pseudomembranous colitis;
- pregnancy.
Tsepim, instructions for use: method and dosage
The solution prepared from Tsepim powder is intended for intravenous and intramuscular administration.
To obtain a single dose of the drug for intravenous administration, 0.5 or 1 g of powder is dissolved in 5 or 10 ml of sterile water for injection, 0.9% sodium chloride solution or 5% dextrose solution. The drug is injected in a jet for 3-5 minutes. For intravenous infusion use, the resulting solution is mixed with other solutions intended for intravenous infusions - 5% dextrose solution, Ringer's solution with lactate, 5 or 10% dextrose solution, or 0.9% sodium chloride solution. The maximum concentration is 0.04 g per 1 ml. Tsepim is administered by drip for half an hour (at least).
To obtain a solution for intramuscular administration, the powder is dissolved in a 0.5 or 1% solution of lidocaine hydrochloride, bacteriostatic water for injection with benzyl alcohol or paraben, 0.9% sodium chloride solution or sterile water for injection (0.5 g of powder - in 1.3 ml of solvent, 1 g in 2.4 ml).
The route of administration and dose of Tsepim is set individually, depending on the sensitivity of the pathogen, the severity of the infection and the condition of the patient's kidneys.
Recommended dosage regimen of Tsepim:
- moderate and severe pneumonia caused by enterobacter, Pseudomonas aeruginosa, Klebsiella pneumonia, pneumococcus, including cases associated with concomitant bacteremia: IV, 1-2 g every 12 hours for 10 days;
- febrile neutropenia (empiric treatment): IV, 2 g of Tsepim every 8 hours for 7 days or until the condition resolves;
- complicated and uncomplicated urinary tract infections of mild and moderate severity, caused by Escherichia coli, Klebsiella pneumoniae or Proteus mirabilis: IV or only for infections caused by Escherichia coli - IM, 0.5-1 g every 12 hours over a period from 7 to 10 days;
- severe complicated or uncomplicated urinary tract infections, including pyelonephritis, caused by Klebsiella pneumonia or Escherichia coli: IV, 2 g every 12 hours for 10 days;
- moderate and severe infections of the skin and soft tissues caused by Streptococcus pyogenic or Staphylococcus aureus (only strains sensitive to methicillin): IV, 2 g of Tsepim every 12 hours for 10 days;
- complicated intra-abdominal infections (combination therapy with metronidazole), the causative agent of which is the bacteroids Fragilis, Enterobacter, Pseudomonas aeruginosa, Klebsiella pneumoniae or Escherichia coli: 2 g intravenously every 12 hours for a period of 7 to 10 days;
- prevention of infection during surgical operations on the abdominal organs: 1 hour before the operation, 2 g of Tsepim is administered intravenously for half an hour. Additionally, at the end of the drug infusion, 0.5 g of metronidazole is administered intravenously. You can not simultaneously enter a solution of metronidazole with cefepime. It is important to flush the infusion set before introducing the first one. During prolonged (more than 12 hours) surgical interventions 12 hours after the first dose, 2 g of the drug is re-administered intravenously for half an hour, followed by the introduction of 0.5 g of metronidazole.
The dose of Tsepim for children aged 2 months to 16 years and weighing no more than 40 kg for all indications, except for febrile neutropenia, is set on the basis of 0.05 g per 1 kg of body weight every 12 hours IV. With febrile neutropenia - 0.05 g per 1 kg of body weight every 8 hours. The duration of therapy is from 7 to 10 days.
In case of impaired renal function [creatinine clearance (CC) <30 ml in 1 min] the dose of Tsepim is adjusted. The initial dose of the drug should be similar to that for patients with normal renal function. Correction of the dosage regimen depending on the initial value is (CC 30-50 ml / min; 11-29 ml / min; <10 ml / min, respectively):
- 2 g every 8 hours: 2 g every 8 hours; 1 g every 12 hours; 1 g every 24 hours;
- 2 g every 12 hours: 2 g every 12 hours; 1 g every 24 hours; 0.5 g every 24 hours;
- 1 g every 12 hours: 1 g every 12 hours; 0.5 g every 24 hours; 0.25 g every 24 hours;
- 0.5 g every 12 hours: 0.5 g every 12 hours; 0.5 g every 24 hours; 0.25 g every 24 hours
Patients on hemodialysis are administered 1 g of Tsepim on the first day, then 0.5 g every 24 hours for all infections and 1 g for the treatment of febrile neutropenia. On the day of hemodialysis, the drug is applied after the end of the procedure. It is advisable to inject Tsepim at the same time every day.
There are no data regarding the use of Tsepim in children with chronic renal failure. However, taking into account the similarity of pharmacokinetics in children with that in adults, the dosing regimen (dose reduction or increase in the interval between injections) in chronic renal failure, regardless of the age group of patients, will be similar.
Side effects
Possible adverse events Tsepima [> 10% - very common; (> 1% and 0.1% and 0.01% and <0.1%) - rarely; <0.01% - very rare; frequency cannot be established from the available data - with an unspecified frequency]:
- allergic reactions: fever, pruritus, rash (including erythematous rash), exudative erythema multiforme (including Stevens-Johnson syndrome), eosinophilia, anaphylactoid reactions; rarely - Lyell's syndrome (toxic epidermal necrolysis);
- nervous system: insomnia, dizziness, headache, confusion, anxiety, convulsions, paresthesia, encephalopathy (in the absence of correction of the dosage regimen in patients with impaired renal function);
- genitourinary system: vaginitis;
- urinary system: impaired renal function;
- gastrointestinal tract: abdominal pain, nausea, diarrhea, vomiting, dyspepsia, constipation / diarrhea, pseudomembranous colitis;
- hematopoietic organs: bleeding, hemolytic anemia, pancytopenia, neutropenia, leukopenia, thrombocytopenia, anemia;
- respiratory system: chest pain, cough;
- cardiovascular system: peripheral edema, shortness of breath, tachycardia;
- laboratory indicators: positive results of the Coombs' test (without hemolysis), hyperbilirubinemia, increased activity of hepatic transaminases and alkaline phosphatase, hypercalcemia, hypercreatininemia, increased urea, increased prothrombin time, decreased hematocrit;
- local reactions: with intravenous administration - phlebitis; with intramuscular injection - pain and hyperemia at the injection site;
- others: increased sweating, pain in the back, throat, oropharyngeal candidiasis, the development of superinfection, asthenia, thoracalgia.
Overdose
The main symptoms (often noted against the background of chronic renal failure): neuromuscular agitation, encephalopathy, convulsions.
Therapy: supportive care, hemodialysis.
special instructions
Against the background of the use of Tsepim, pseudomembranous colitis may develop. It is important to take this diagnosis into account if diarrhea occurs during therapy. In cases of mild forms of colitis, special treatment is not carried out, it is enough to cancel the drug; in moderate or severe forms, special therapy may be required.
Patients with allergic reactions to penicillins are likely to develop cross-hypersensitivity.
With a combination of severe hepatic and renal failure, it is important to regularly determine the content of cefepime in the blood plasma and adjust the dosage depending on the CC.
Against the background of prolonged use of Tsepim, it is necessary to systematically monitor the indicators of the functional state of the kidneys and liver, the picture of peripheral blood.
In cases of mixed aerobic-anaerobic infection, prior to identification of pathogens, it is advisable to use them in combination with drugs that are active against anaerobic microorganisms. If meningitis is suspected, the diagnosis of meningitis or meningeal dissemination from a remote focus of infection is confirmed, an alternative antibacterial agent is prescribed that has proven clinical efficacy for this situation.
It should be borne in mind that during the period of use of Tsepim, a false-positive result of the Coombs' test and the test for determining glucose in urine is possible.
Application during pregnancy and lactation
The use of Tsepim during pregnancy is allowed only in cases where the predicted therapeutic effect for the mother is higher than the possible risks for the fetus.
If it is necessary to use the drug during lactation, breastfeeding is stopped.
Pediatric use
Tsepim for intravenous injection is not prescribed to patients under the age of 2 months, since the safety and efficacy profile of its use in children of this age has not been established. The intramuscular route of administration of Tsepim is contraindicated for children under 12 years of age.
With impaired renal function
Chronic renal failure is a relative contraindication to the use of Tsepim, the dosage regimen should be adjusted depending on the QC.
Drug interactions
Tsepim is pharmaceutically incompatible with heparin and other antimicrobial drugs.
Recommended combinations to take into account:
- polymyxin B, aminoglycosides, diuretics: lower the tubular secretion of the drug, increase the concentration in the blood serum, lengthen the half-life, increase nephrotoxicity (the likelihood of nephronecrosis increases);
- aminoglycosides: cefepime potentiates their ototoxicity;
- non-steroidal anti-inflammatory drugs: by slowing the elimination of cephalosporins, increase the risk of bleeding;
- bactericidal antibiotics (aminoglycosides): synergize with cefepime;
- bacteriostatic antibiotics (tetracyclines, chloramphenicol, macrolides): show antagonism to the drug.
Tsepim is incompatible with metronidazole solution. Before the introduction of the latter (for the prevention of infections during surgical interventions), the infusion system is washed from the cefepime solution. To avoid potential drug interactions with other drugs, cefepime solution, like most other β-lactam antibiotics, is not administered in combination with netilmicin, tobramycin, gentamycin and vancomycin solutions. In cases where such combinations are prescribed, each antibiotic is administered separately.
Analogs
Analogs of Tsepim are: Cefepim, Movizar, Cefepim-Jodas, Maxicef, Kefsepim, Cefepim-Vial, Maxipim, Cefomax, Cefepim-Alkem, Efipim.
Terms and conditions of storage
Store at temperatures up to 30 ° C. Keep out of the reach of children.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Tsepima
There are few reviews of Tsepima, indicating its effectiveness.
Price for Tsepim in pharmacies
The approximate price for Tsepim (in the package 1 bottle with 1 g of powder for the preparation of a solution for i / v and i / m administration) is 143.3 rubles.
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
