Composition, structure and packing
Powder for solution for in / and / m the introduction of white or white with a yellowish tint.
1 vial. - Tsefoksitin (in the form of sodium salt) 500 mg - - 1 g
Solvent: water w / and (5 ml).
Clinico-pharmacological group
II generation cephalosporin
Pharmacological action
Cephalosporin antibiotic II generation of group cephamycin for parenteral administration. Bactericidal action due to blocking of bacterial transpeptidase, which leads to a breach of the final stages of synthesis of cell walls of microorganisms. It has a wide spectrum of antimicrobial action both against aerobic and anaerobic bacteria. Molecular structure tsefoksitina determines its high resistance to bacterial β-lactamases.
It is active against Gram-positive aerobes: Staphylococcus aureus, Staphylococcus epidermidis (including producing strains and neprodutsiruyuschie penicillinase), beta-hemolytic group A streptococci (Streptococcus pyogenes), beta-hemolytic streptococcus group B (Streptococcus agalactiae), Streptococcus pneumoniae; gram aerobes: Escherichia coli, Haemophilus influenzae, Eikenella corrodens (strains that do not produce β-lactamase), Klebsiella pneumoniae, Neisseria gonorrhoeae (including strains producing and neprodutsiruyuschie penicillinase), Morganella morganii, Proteus mirabilis, Proteus vulgaris, Providencia spp. (Including Providencia rettgeri), Salmonella spp., Shigella spp.; Anaerobes: Actinomyces spp., Clostridium spp. (Except for Clostridium difficile), Peptococcus niger, Peptostreptococcus spp., Microaerophilic streptococci, Bacteroides spp. (Including Bacteroides distasonis, Bacteroides fragilis, Bacteroides ovatus, Bacteroides thetaiotaomicron), Prevotella bivia.
Tsefoksitin not active against metitsillinoustoychivyh Staphylococcus spp., Enterococcus spp., Listeria monocytogenes, Enterobacter cloacae, Pseudomonas aeruginosa, Stenotrophomonas maltophilia, Mycobacterium spp., Rickettsia spp., Chlamydia spp., Mycoplasma spp., Ureaplasma spp.
Pharmacokinetics
Distribution
After 5 min after the bolus in / tsefoksitina administration at a dose of 1 g and 2 g Cmax of 110 mg / l and 244 mg / l, respectively. After 4 h after i / in a dose of 1 g of serum concentrations of less than 1 mg / liter.
After a / m administration tsefoksitina a dose of 1 g Cmax is achieved within 20 min and 30 mg / liter.
Well into the various fluids and tissues of the body: in the pleural, ascitic and synovial fluid bactericidal concentrations are determined in the bile. Vd - 0.16 L / kg. Binding to plasma proteins - 70-80%. Provided with breast milk in low concentrations.
Withdrawal
Write mainly in the kidneys in unchanged form (85% by glomerular filtration, 6% - due to tubular secretion), while in the urine are high concentrations of the drug. In the form of inactive metabolites derived only 0.2-5% of the administered dose. T1 / 2 with a / in the introduction of 41-59 min.
Pharmacokinetics in special clinical situations
T1 / 2 for i / v administration in elderly patients is 51-90 minutes.
Indications for use of the drug
Infections caused by susceptible microorganisms:
Infection of lower respiratory tract (including pneumonia, empyema, lung abscess);
abdominal infections (including peritonitis, abscess of the abdominal cavity);
infectious and inflammatory diseases of the pelvic organs (including endometritis, pelvioperitonit, salpingoophoritis);
urinary tract infections (pyelitis, pyelonephritis);
infections of skin and soft tissues;
infections of bones and joints;
uncomplicated gonorrhea;
septicemia.
Prevention of postoperative infectious complications.
Dosage regimen
Depending on the dose and the severity of infection, Anaerotsef ® can be entered in / in (jet or drip) or / m.
Adult sredneterapevticheskaya dose of 1-2 g every 6-8 hours
For uncomplicated urinary tract infection drug prescribed in / m and 1 g 2
In uncomplicated gonorrhea, including caused by penicillinase-producing strains of Neisseria gonorrhoeae, a drug injected once a / m in a dose of 2 g; simultaneously or 1 h later appointed interior 1 g probenecid.
In severe infections in / route of administration is preferable. Assign to 2 g every 4 hours or 3 g every 6 hours daily dose should not be more than 1912
Tsefoksitin excreted primarily by the kidneys, so patients with renal failure require adjustment in dosage regimen depending on the values of creatinine clearance.
Creatinine clearance Dose interval between doses
30-50 ml / min 1-2 g 8-12 h
10-29 ml / min 1-2 g 12-24 h
5-9 ml / min 0.5-1 g 12-24 h
<5 ml / min 0.5-1 g 24-48 h
Patients who are on hemodialysis is recommended after each hemodialysis introduce additional 1-2 g Anaerotsefa.
Children older than 1 month Anaerotsef injected at the rate of 30-40 mg / kg every 6-8 hours (maximum daily dose should not exceed 12 g). In mild and moderate infections possibly / m injection of the drug, in severe infections are preferable in / injection or in / infusion of the drug. Children up to 3 months Anaerotsef ® introduced only in /.
Babies first week of life in preterm infants weighing over 1500 g is introduced into / in a single dose of 30-40 mg / kg every 12 h; infants 1-4 weeks of life - in / on 30-40 mg / kg every 8 h .
Adults for the prevention of postoperative infectious complications introduced into / in a dose of 2 g for 30 min before the operation; on the testimony of the first day postoperative period - 2 g every 6 hours
In carrying out Cesarean operation Anaerotsef enter in / at a dose of 2 g immediately after clamping the umbilical cord.
Babies and children under 12 years Anaerotsef introduced into / in 30 minutes before the start of the operation at a dose of 30-40 mg / kg. According to testimony, the first postoperative days in addition introduce the drug in doses of 30-40 mg / kg every 6-8 hours (neonates - 8-12 h).
Terms of preparing and implementing solutions
Do not use solutions containing preservatives (eg benzyl alcohol in bacteriostatic water for injection) for preparation of solutions Anaerotsefa used in neonates.
For iv administration we recommend jet dissolving 1 g Anaerotsefa in 10 ml water for injection. The resulting solution should be injected into / in slowly for 3-5 minutes, possibly through the introduction of site for injection systems for in / infusion transfusion of compatible solutions.
When using a long / v infusion of 1 g Anaerotsefa dissolved in 3-5 ml of sterile water for injection, and after complete dissolution of the resulting solution added to 200-400 ml of a compatible infusion medium: 0.9% sodium chloride, 5% dextrose (glucose) aqueous solution containing 5% dextrose (glucose) and 0.9% sodium chloride. Enter in / drip, use the system for to / in infusions.
To prepare the solution for i / m administration, 1 g Anaerotsefa dissolved in 2-3 ml of one of the following solvents: water for injection, 0.5% lidocaine hydrochloride, 1% lidocaine hydrochloride. Enter deeply into the / m in area with a distinct muscular layer (upper-outer quadrant of the buttocks), previously holding an aspiration test, to avoid the introduction of a blood vessel.
Side effect
From the urinary system: increasing serum creatinine, interstitial nephritis, renal failure.
On the part of the digestive system: nausea, vomiting, dry mouth, decreased appetite, diarrhea, pseudomembranous enterocolitis, increase in liver transaminases.
The part of the hemopoietic system: leukopenia, granulocytopenia, neutropenia, anemia, thrombocytopenia, bone marrow suppression, hemolytic anemia.
Since the cardiovascular system: arterial hypotension.
Allergic reactions: rash, exfoliative dermatitis, toxic epidermal necrolysis (Lyell's syndrome), eosinophilia, fever, shortness of breath; rare - anaphylactic reaction, angioedema.
Local reactions: thrombophlebitis after i / v injection; pain, induration in the ground / m injections.
Other: aggravation flow myastenia gravis, patients with azotemia possible false-positive Coombs' reaction.
Contraindications to the use of the drug
Hypersensitivity to tsefoksitinu and other cephalosporin antibiotics.
Precautions should be prescribed to patients with allergic reactions to penicillin in history as possible cross allergy between penicillins and cephalosporins, with guidance on the history of ulcerative colitis in renal insufficiency.
Pregnancy and lactation
Application Anaerotsefa pregnant possible in cases where the intended benefits to the mother outweighs the potential risk to the fetus, and must be supervised by a specialist.
During treatment tsefoksitinom breastfeeding should be discontinued.
Application for violations of renal function
Tsefoksitin excreted primarily by the kidneys, so patients with renal insufficiency requires the introduction of correction mode, depending on the values of creatinine clearance.
Creatinine clearance Dose interval between doses
30-50 ml / min 1-2 g 8-12 h
10-29 ml / min 1-2 g 12-24 h
5-9 ml / min 0.5-1 g 12-24 h
<5 ml / min 0.5-1 g 24-48 h
Patients who are on hemodialysis is recommended after each hemodialysis introduce additional 1-2 g Anaerotsefa.
Cautions
Anaerotsef used for monotherapy for the treatment of mixed aerobic-anaerobic infections of various sites, including caused by strains of bacteria that are resistant to penicillins, other cephalosporins, and aminoglycosides Lincosamides.
Patients who had a history of allergic reactions to penicillin, may have heightened sensitivity to cephalosporin antibiotics.
For the treatment of newborns should use a solvent without preservatives.
Use of the drug in high doses in children accompanied by an increase in frequency of eosinophilia and increased activity of AST.
Anaerotsef not recommended for treatment of bacterial meningitis.
Using the method of Jaffe may falsely inflated the concentration of creatinine in serum, therefore, not recommended to collect blood samples for determination of creatinine within 2 h after injection tsefoksitina.
Overdose
Data on drug overdose Anaerotsef not available.
Drug Interactions
With the simultaneous use of aminoglycosides observed synergy of antimicrobial action, mainly in respect of Enterobacteriaceae.
Drugs that block tubular secretion, increase the concentration of drug in the blood and the duration of its action.
The simultaneous use of aminoglycosides and other cephalosporins increases the risk of nephrotoxicity.
At the same time / in the introduction of the solution Anaerotsefa possible with the following infusion solutions: 0.9% sodium chloride solution, 5% dextrose (glucose), 10% dextrose (glucose), an aqueous solution containing 5% dextrose (glucose) and 0.9% sodium chloride , Ringer's solution, 2.5%, 5% and 10% mannitol solution.
Because pharmacological incompatibility, do not mix in same syringe, or single infusion medium solutions Anaerotsefa and aminoglycosides.
To the top
Drug prescription.
Terms and Conditions of storage
List B. The drug should be stored in dry, protected from light, away from children at or above 25 ° C. Shelf life - 2 years.
Powder for solution for in / and / m the introduction of white or white with a yellowish tint.
1 vial. - Tsefoksitin (in the form of sodium salt) 500 mg - - 1 g
Solvent: water w / and (5 ml).
Clinico-pharmacological group
II generation cephalosporin
Pharmacological action
Cephalosporin antibiotic II generation of group cephamycin for parenteral administration. Bactericidal action due to blocking of bacterial transpeptidase, which leads to a breach of the final stages of synthesis of cell walls of microorganisms. It has a wide spectrum of antimicrobial action both against aerobic and anaerobic bacteria. Molecular structure tsefoksitina determines its high resistance to bacterial β-lactamases.
It is active against Gram-positive aerobes: Staphylococcus aureus, Staphylococcus epidermidis (including producing strains and neprodutsiruyuschie penicillinase), beta-hemolytic group A streptococci (Streptococcus pyogenes), beta-hemolytic streptococcus group B (Streptococcus agalactiae), Streptococcus pneumoniae; gram aerobes: Escherichia coli, Haemophilus influenzae, Eikenella corrodens (strains that do not produce β-lactamase), Klebsiella pneumoniae, Neisseria gonorrhoeae (including strains producing and neprodutsiruyuschie penicillinase), Morganella morganii, Proteus mirabilis, Proteus vulgaris, Providencia spp. (Including Providencia rettgeri), Salmonella spp., Shigella spp.; Anaerobes: Actinomyces spp., Clostridium spp. (Except for Clostridium difficile), Peptococcus niger, Peptostreptococcus spp., Microaerophilic streptococci, Bacteroides spp. (Including Bacteroides distasonis, Bacteroides fragilis, Bacteroides ovatus, Bacteroides thetaiotaomicron), Prevotella bivia.
Tsefoksitin not active against metitsillinoustoychivyh Staphylococcus spp., Enterococcus spp., Listeria monocytogenes, Enterobacter cloacae, Pseudomonas aeruginosa, Stenotrophomonas maltophilia, Mycobacterium spp., Rickettsia spp., Chlamydia spp., Mycoplasma spp., Ureaplasma spp.
Pharmacokinetics
Distribution
After 5 min after the bolus in / tsefoksitina administration at a dose of 1 g and 2 g Cmax of 110 mg / l and 244 mg / l, respectively. After 4 h after i / in a dose of 1 g of serum concentrations of less than 1 mg / liter.
After a / m administration tsefoksitina a dose of 1 g Cmax is achieved within 20 min and 30 mg / liter.
Well into the various fluids and tissues of the body: in the pleural, ascitic and synovial fluid bactericidal concentrations are determined in the bile. Vd - 0.16 L / kg. Binding to plasma proteins - 70-80%. Provided with breast milk in low concentrations.
Withdrawal
Write mainly in the kidneys in unchanged form (85% by glomerular filtration, 6% - due to tubular secretion), while in the urine are high concentrations of the drug. In the form of inactive metabolites derived only 0.2-5% of the administered dose. T1 / 2 with a / in the introduction of 41-59 min.
Pharmacokinetics in special clinical situations
T1 / 2 for i / v administration in elderly patients is 51-90 minutes.
Indications for use of the drug
Infections caused by susceptible microorganisms:
Infection of lower respiratory tract (including pneumonia, empyema, lung abscess);
abdominal infections (including peritonitis, abscess of the abdominal cavity);
infectious and inflammatory diseases of the pelvic organs (including endometritis, pelvioperitonit, salpingoophoritis);
urinary tract infections (pyelitis, pyelonephritis);
infections of skin and soft tissues;
infections of bones and joints;
uncomplicated gonorrhea;
septicemia.
Prevention of postoperative infectious complications.
Dosage regimen
Depending on the dose and the severity of infection, Anaerotsef ® can be entered in / in (jet or drip) or / m.
Adult sredneterapevticheskaya dose of 1-2 g every 6-8 hours
For uncomplicated urinary tract infection drug prescribed in / m and 1 g 2
In uncomplicated gonorrhea, including caused by penicillinase-producing strains of Neisseria gonorrhoeae, a drug injected once a / m in a dose of 2 g; simultaneously or 1 h later appointed interior 1 g probenecid.
In severe infections in / route of administration is preferable. Assign to 2 g every 4 hours or 3 g every 6 hours daily dose should not be more than 1912
Tsefoksitin excreted primarily by the kidneys, so patients with renal failure require adjustment in dosage regimen depending on the values of creatinine clearance.
Creatinine clearance Dose interval between doses
30-50 ml / min 1-2 g 8-12 h
10-29 ml / min 1-2 g 12-24 h
5-9 ml / min 0.5-1 g 12-24 h
<5 ml / min 0.5-1 g 24-48 h
Patients who are on hemodialysis is recommended after each hemodialysis introduce additional 1-2 g Anaerotsefa.
Children older than 1 month Anaerotsef injected at the rate of 30-40 mg / kg every 6-8 hours (maximum daily dose should not exceed 12 g). In mild and moderate infections possibly / m injection of the drug, in severe infections are preferable in / injection or in / infusion of the drug. Children up to 3 months Anaerotsef ® introduced only in /.
Babies first week of life in preterm infants weighing over 1500 g is introduced into / in a single dose of 30-40 mg / kg every 12 h; infants 1-4 weeks of life - in / on 30-40 mg / kg every 8 h .
Adults for the prevention of postoperative infectious complications introduced into / in a dose of 2 g for 30 min before the operation; on the testimony of the first day postoperative period - 2 g every 6 hours
In carrying out Cesarean operation Anaerotsef enter in / at a dose of 2 g immediately after clamping the umbilical cord.
Babies and children under 12 years Anaerotsef introduced into / in 30 minutes before the start of the operation at a dose of 30-40 mg / kg. According to testimony, the first postoperative days in addition introduce the drug in doses of 30-40 mg / kg every 6-8 hours (neonates - 8-12 h).
Terms of preparing and implementing solutions
Do not use solutions containing preservatives (eg benzyl alcohol in bacteriostatic water for injection) for preparation of solutions Anaerotsefa used in neonates.
For iv administration we recommend jet dissolving 1 g Anaerotsefa in 10 ml water for injection. The resulting solution should be injected into / in slowly for 3-5 minutes, possibly through the introduction of site for injection systems for in / infusion transfusion of compatible solutions.
When using a long / v infusion of 1 g Anaerotsefa dissolved in 3-5 ml of sterile water for injection, and after complete dissolution of the resulting solution added to 200-400 ml of a compatible infusion medium: 0.9% sodium chloride, 5% dextrose (glucose) aqueous solution containing 5% dextrose (glucose) and 0.9% sodium chloride. Enter in / drip, use the system for to / in infusions.
To prepare the solution for i / m administration, 1 g Anaerotsefa dissolved in 2-3 ml of one of the following solvents: water for injection, 0.5% lidocaine hydrochloride, 1% lidocaine hydrochloride. Enter deeply into the / m in area with a distinct muscular layer (upper-outer quadrant of the buttocks), previously holding an aspiration test, to avoid the introduction of a blood vessel.
Side effect
From the urinary system: increasing serum creatinine, interstitial nephritis, renal failure.
On the part of the digestive system: nausea, vomiting, dry mouth, decreased appetite, diarrhea, pseudomembranous enterocolitis, increase in liver transaminases.
The part of the hemopoietic system: leukopenia, granulocytopenia, neutropenia, anemia, thrombocytopenia, bone marrow suppression, hemolytic anemia.
Since the cardiovascular system: arterial hypotension.
Allergic reactions: rash, exfoliative dermatitis, toxic epidermal necrolysis (Lyell's syndrome), eosinophilia, fever, shortness of breath; rare - anaphylactic reaction, angioedema.
Local reactions: thrombophlebitis after i / v injection; pain, induration in the ground / m injections.
Other: aggravation flow myastenia gravis, patients with azotemia possible false-positive Coombs' reaction.
Contraindications to the use of the drug
Hypersensitivity to tsefoksitinu and other cephalosporin antibiotics.
Precautions should be prescribed to patients with allergic reactions to penicillin in history as possible cross allergy between penicillins and cephalosporins, with guidance on the history of ulcerative colitis in renal insufficiency.
Pregnancy and lactation
Application Anaerotsefa pregnant possible in cases where the intended benefits to the mother outweighs the potential risk to the fetus, and must be supervised by a specialist.
During treatment tsefoksitinom breastfeeding should be discontinued.
Application for violations of renal function
Tsefoksitin excreted primarily by the kidneys, so patients with renal insufficiency requires the introduction of correction mode, depending on the values of creatinine clearance.
Creatinine clearance Dose interval between doses
30-50 ml / min 1-2 g 8-12 h
10-29 ml / min 1-2 g 12-24 h
5-9 ml / min 0.5-1 g 12-24 h
<5 ml / min 0.5-1 g 24-48 h
Patients who are on hemodialysis is recommended after each hemodialysis introduce additional 1-2 g Anaerotsefa.
Cautions
Anaerotsef used for monotherapy for the treatment of mixed aerobic-anaerobic infections of various sites, including caused by strains of bacteria that are resistant to penicillins, other cephalosporins, and aminoglycosides Lincosamides.
Patients who had a history of allergic reactions to penicillin, may have heightened sensitivity to cephalosporin antibiotics.
For the treatment of newborns should use a solvent without preservatives.
Use of the drug in high doses in children accompanied by an increase in frequency of eosinophilia and increased activity of AST.
Anaerotsef not recommended for treatment of bacterial meningitis.
Using the method of Jaffe may falsely inflated the concentration of creatinine in serum, therefore, not recommended to collect blood samples for determination of creatinine within 2 h after injection tsefoksitina.
Overdose
Data on drug overdose Anaerotsef not available.
Drug Interactions
With the simultaneous use of aminoglycosides observed synergy of antimicrobial action, mainly in respect of Enterobacteriaceae.
Drugs that block tubular secretion, increase the concentration of drug in the blood and the duration of its action.
The simultaneous use of aminoglycosides and other cephalosporins increases the risk of nephrotoxicity.
At the same time / in the introduction of the solution Anaerotsefa possible with the following infusion solutions: 0.9% sodium chloride solution, 5% dextrose (glucose), 10% dextrose (glucose), an aqueous solution containing 5% dextrose (glucose) and 0.9% sodium chloride , Ringer's solution, 2.5%, 5% and 10% mannitol solution.
Because pharmacological incompatibility, do not mix in same syringe, or single infusion medium solutions Anaerotsefa and aminoglycosides.
To the top
Drug prescription.
Terms and Conditions of storage
List B. The drug should be stored in dry, protected from light, away from children at or above 25 ° C. Shelf life - 2 years.
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