Composition, structure and packing
Powder for solution for in / and / m the introduction of white to light yellow in color.
1 vial. cefuroxime (in the form of sodium salt) 750 mg - 1.5 PM
Clinico-pharmacological group: Cephalosporins II generation.
Pharmacological action
Cephalosporin antibiotic II generation for parenteral use. Effective bactericidal - violates the synthesis of bacterial cell wall. It has a wide spectrum of antimicrobial action.
Highly active against gram-positive microorganisms - Staphylococcus aureus, Staphylococcus epidermidis (including strains resistant to penicillins and with the exception of strains resistant to methicillin), Streptococcus pyogenes (and other beta-hemolytic streptococci), Streptococcus pneumoniae, Streptococcus group B (Streptococcus agalactiae), Streptococcus mitis (group viridans), Bordetella pertussis, the majority of Clostridium spp.); Gram-negative microorganisms - Escherichia coli, Klebsiella spp., Proteus mirabilis, Providencia spp., Proteus rettgeri, Haemophilus influenzae (including strains resistant to ampicillin), Haemophilus parainfluenzae ( including strains resistant to ampicillin), Moraxella (Branhamella) catarrhalis, Neisseria gonorrhoeae, including strains producing and not producing penicillinase, Neisseria meningitidis, Salmonella spp., Bacteroides spp. (Except Bacteroides fragilis), Fusobacterium spp., Propionibacterium spp., Borrelia burgdorferi; gram-positive and Gram-negative anaerobic bacteria (including Peptococcus spp. And Peptostreptococcus spp.).
By following cefuroxime resistant microorganisms: Clostridium difficile, Pseudomonas spp., Campylobacter spp., Acinetobacter calcoaceticus, Listeria monocytogenes, methicillin-resistant strains of Staphylococcus aureus, methicillin-resistant strains of Staphylococcus epidermidis, Legionella spp., Streptococcus (Enterococcus) faecalis, Morganella morganii, Proteus vulgaris, Enterobacter spp., Citrobacter spp., Serratia spp., Bacteroides fragilis.
Pharmacokinetics
Absorption
After i / m injection of the drug at a dose of 750 mg of cefuroxime Cmax plasma levels achieved after 15-60 min and is 27 ug / ml. After i / v administration in doses of 750 mg and 1.5 g Cmax is achieved within 15 minutes and constitutes respectively 50 and 100 ug / ml. Therapeutic concentration persists for 5.3 and 8 h, respectively.
Distribution
Plasma protein binding is 33-50%. Therapeutic concentrations are determined in the pleural fluid, bile, phlegm, myocardium, skin and soft tissues. Concentrations of cefuroxime in excess of the IPC for the most common microorganisms are achieved in bone tissue, synovial fluid and the intraocular fluid. Penetrates through the placental barrier, excreted in breast milk.
Metabolism
Not metabolized in the liver.
Withdrawal
T1 / 2 after i / m and / in the introduction of 80 minutes, the newborn is increased by 3-5 times. Derived by glomerular filtration and tubular secretion - 85-90% unchanged for 8 h; most of the drug appears in the first 6 h, while in the urine are high concentrations. After 24 h is displayed in full (50% - by tubular secretion, 50% - by glomerular filtration).
Pharmacokinetics in special clinical situations
Babies T1 / 2 longer than 3-5 times. When meningitis penetrates through the BBB.
Statement
Infectious-inflammatory diseases caused by microorganisms sensitive to the drug:
respiratory tract infections (including bronchitis, pneumonia, lung abscess, empyema);
infection ENT organs (including sinusitis, tonsillitis, pharyngitis);
urinary tract infections (including pyelonephritis, cystitis, symptomatic bacteriuria, gonorrhea);
infections of skin and soft tissue (including face);
infections of bones and joints (including osteomyelitis, septic arthritis);
pelvic infections (in obstetrics and gynecology);
septicemia;
meningitis.
Prevention of infectious complications after surgery of the thorax, abdomen, pelvis, joints (including the operations in the lungs, heart, esophagus, in vascular surgery at high risk of infectious complications in orthopedic surgery).
Dosage regimen
V / m and / in an adult drug prescribed 750 mg 3 times / day, with severe infections of the flow dose increased to 1.5 g 3-4 times / day (if necessary, the interval between infusions may be shortened to 6 h).
Average daily dose - 3-6 PM
Children prescribed a dose of 30-100 mg / kg / day in 3-4 reception. For most infections the optimal dose is 60 mg / kg / day. Newborns and children up to 3 months drug is administered in a dose of 30 mg / kg / day in 2-3 reception.
When gonorrhea - a / m at a dose of 1.5 g once (or in the form of 2 injections of 750 mg with an introduction to the different areas, for example, in both gluteal muscles).
With bacterial meningitis - in / in 3 g every 8 h for children younger and older - 150-250 mg / kg / day in 3-4 admission, newborn - 100 mg / kg / day.
In operations on the abdomen, pelvic and orthopedic surgery - in / 1.5 g at induction of anesthesia, then in addition - i / m 750 mg after 8 and 16 h after surgery.
In operations on the heart, lungs, esophagus and blood vessels - in / 1.5 g at induction of anesthesia, then - / m, 750 mg 3 times / day over the next 24-48 h. In total joint replacement - 1.5 g of powder mixed in dry with each package of polymer methyl methacrylate cement before adding the liquid monomer.
When you have pneumonia - a / m or i / v for 1.5 g 2-3 times / day for 48-72 hours, then move on ingestion (use dosage forms for oral administration), 500 mg 2 times / day for 7 - 10 days.
With exacerbation of chronic bronchitis designate the / m or / in the 750 mg 2-3 times / day for 48-72 hours, then move on ingestion (use dosage forms for oral administration), 500 mg 2 times / day for 5-10 days.
In chronic renal failure must be corrected dosing regimen.
When QA 10-20 ml / min appointed in / or / m 750 mg 2 times / day, with spacecraft less than 10 ml / min - 750 mg 1 time / day.
Patients who are on continuous hemodialysis with arterio-venous shunt or hemofiltration a high speed to the ICU, prescribe 750 mg 2 times / d for patients on hemofiltration low speed, prescribe the dose recommended for renal events.
Side effect
Allergic reactions: fever, rash, itching, rash, rarely - erythema multiforme, bronchospasm, Stevens-Johnson syndrome, anaphylactic shock.
On the part of the digestive system: diarrhea, nausea, vomiting or constipation, bloating, cramping and abdominal pain, ulceration of the oral mucosa, oral candidiasis, glossitis, pseudomembranous enterocolitis, abnormal liver function (increased liver enzymes in plasma - AST, ALT , alkaline phosphatase, LDH, bilirubin), cholestasis.
On the part of the urinary system: renal dysfunction (decrease in RR, elevated levels of creatinine and urea nitrogen remaining in the blood), dysuria.
On the part of the reproductive system: an itch in the crotch, vaginitis.
On the part of the hemopoietic system: reduction of hemoglobin and hematocrit, anemia (aplastic or hemolytic), eosinophilia, neutropenia, leukopenia, agranulocytosis, thrombocytopenia, gipoprotrombinemii, lengthening prothrombin time.
Local reactions: irritation, infiltration, and pain at the injection site, phlebitis.
Contraindications
Hypersensitivity to cefuroxime and other cephalosporins, to penicillin and carbapenems.
Precautions should be prescribed the drug newborns, premature babies, with chronic renal failure, bleeding and gastrointestinal diseases (including a history, including UC), weak and debilitated patients.
Pregnancy and lactation
Precautions should be prescribed the drug during pregnancy and lactation.
Application for violations of renal function
In chronic renal failure must be corrected dosing regimen.
When QA 10-20 ml / min appointed in / or / m 750 mg 2 times / day, with spacecraft less than 10 ml / min - 750 mg 1 time / day.
Patients who are on continuous hemodialysis with arterio-venous shunt or hemofiltration a high speed to the ICU, prescribe 750 mg 2 times / d for patients on hemofiltration low speed, prescribe the dose recommended for renal events.
Cautions
Patients with a history of instructions on allergic reactions to penicillin may be the presence of hypersensitivity to cephalosporin antibiotics. In the course of treatment is necessary to monitor kidney function, especially in patients receiving the drug in high doses.
Treatment should continue for 48-72 hours after symptoms disappear in case of infections caused by Streptococcus pyogenes, it is recommended to continue treatment for at least 10 days. During treatment, the possible false-positive direct Coombs' reaction and false-positive reaction for urine glucose.
After reconstitution store at room temperature for 7 h in the refrigerator - for 48 hours is allowed to use yellowed during storage solution. In the period of treatment should avoid alcohol. Patients receiving cefuroxime, when determining the level of glucose in the blood recommend the use of tests with glucose oxidase or hexokinase.
The treatment of meningitis in children may be hearing loss. In the transition from parenteral to receive inside should take into account the gravity of infection, the sensitivity of microorganisms and the general condition of the patient. If within 72 h after administration of cefuroxime into the clinical improvement is noted, it is necessary to continue parenteral administration.
Overdose
Symptoms: central nervous system excitation, convulsions.
Treatment: the appointment of anticonvulsants, providing ventilation and function of the cardiovascular system, control and maintenance of vital body functions, hemodialysis and peritoneal dialysis.
Drug Interactions
In case of simultaneous appointment inside the "loop" diuretics has slowed tubular secretion, reduction in renal clearance, increasing plasma concentrations and an increase in T1 / 2 of cefuroxime.
With the simultaneous use of aminoglycosides and diuretics and increased risk of nephrotoxic effects.
Drugs that reduce gastric acidity, reduce the absorption of cefuroxime and its bioavailability.
Pharmaceutical interactions
Pharmaceutical compatible with metronidazole, azlotsillinom, xylitol, with an aqueous solution containing 1% lidocaine, 0.9% sodium chloride solution, 5% dextrose, 0.18% sodium chloride solution and 4% dextrose, 5% dextrose and 0.9% solution sodium chloride, 5% dextrose and 0.45% sodium chloride solution, 5% dextrose and 0.225% sodium chloride solution, 10% dextrose, 10% invert sugar in water for injection, Ringer's solution, a solution of sodium lactate, Hartmann's solution, 0.9 % solution of sodium chloride, 5% dextrose and hydrocortisone, heparin (10 U / ml and 50 U / ml) in 0.9% sodium chloride, potassium chloride (10 mEq / L and 40 mEq / L) in 0.9% solution of sodium chloride.
Pharmaceutical incompatible with aminoglycosides, a solution of sodium bicarbonate, 2.74%.
Terms and Conditions of storage
List B. The drug should be stored in a dry, protected from light and away from children at or above 25 ° C. Shelf life - 2 years.
Powder for solution for in / and / m the introduction of white to light yellow in color.
1 vial. cefuroxime (in the form of sodium salt) 750 mg - 1.5 PM
Clinico-pharmacological group: Cephalosporins II generation.
Pharmacological action
Cephalosporin antibiotic II generation for parenteral use. Effective bactericidal - violates the synthesis of bacterial cell wall. It has a wide spectrum of antimicrobial action.
Highly active against gram-positive microorganisms - Staphylococcus aureus, Staphylococcus epidermidis (including strains resistant to penicillins and with the exception of strains resistant to methicillin), Streptococcus pyogenes (and other beta-hemolytic streptococci), Streptococcus pneumoniae, Streptococcus group B (Streptococcus agalactiae), Streptococcus mitis (group viridans), Bordetella pertussis, the majority of Clostridium spp.); Gram-negative microorganisms - Escherichia coli, Klebsiella spp., Proteus mirabilis, Providencia spp., Proteus rettgeri, Haemophilus influenzae (including strains resistant to ampicillin), Haemophilus parainfluenzae ( including strains resistant to ampicillin), Moraxella (Branhamella) catarrhalis, Neisseria gonorrhoeae, including strains producing and not producing penicillinase, Neisseria meningitidis, Salmonella spp., Bacteroides spp. (Except Bacteroides fragilis), Fusobacterium spp., Propionibacterium spp., Borrelia burgdorferi; gram-positive and Gram-negative anaerobic bacteria (including Peptococcus spp. And Peptostreptococcus spp.).
By following cefuroxime resistant microorganisms: Clostridium difficile, Pseudomonas spp., Campylobacter spp., Acinetobacter calcoaceticus, Listeria monocytogenes, methicillin-resistant strains of Staphylococcus aureus, methicillin-resistant strains of Staphylococcus epidermidis, Legionella spp., Streptococcus (Enterococcus) faecalis, Morganella morganii, Proteus vulgaris, Enterobacter spp., Citrobacter spp., Serratia spp., Bacteroides fragilis.
Pharmacokinetics
Absorption
After i / m injection of the drug at a dose of 750 mg of cefuroxime Cmax plasma levels achieved after 15-60 min and is 27 ug / ml. After i / v administration in doses of 750 mg and 1.5 g Cmax is achieved within 15 minutes and constitutes respectively 50 and 100 ug / ml. Therapeutic concentration persists for 5.3 and 8 h, respectively.
Distribution
Plasma protein binding is 33-50%. Therapeutic concentrations are determined in the pleural fluid, bile, phlegm, myocardium, skin and soft tissues. Concentrations of cefuroxime in excess of the IPC for the most common microorganisms are achieved in bone tissue, synovial fluid and the intraocular fluid. Penetrates through the placental barrier, excreted in breast milk.
Metabolism
Not metabolized in the liver.
Withdrawal
T1 / 2 after i / m and / in the introduction of 80 minutes, the newborn is increased by 3-5 times. Derived by glomerular filtration and tubular secretion - 85-90% unchanged for 8 h; most of the drug appears in the first 6 h, while in the urine are high concentrations. After 24 h is displayed in full (50% - by tubular secretion, 50% - by glomerular filtration).
Pharmacokinetics in special clinical situations
Babies T1 / 2 longer than 3-5 times. When meningitis penetrates through the BBB.
Statement
Infectious-inflammatory diseases caused by microorganisms sensitive to the drug:
respiratory tract infections (including bronchitis, pneumonia, lung abscess, empyema);
infection ENT organs (including sinusitis, tonsillitis, pharyngitis);
urinary tract infections (including pyelonephritis, cystitis, symptomatic bacteriuria, gonorrhea);
infections of skin and soft tissue (including face);
infections of bones and joints (including osteomyelitis, septic arthritis);
pelvic infections (in obstetrics and gynecology);
septicemia;
meningitis.
Prevention of infectious complications after surgery of the thorax, abdomen, pelvis, joints (including the operations in the lungs, heart, esophagus, in vascular surgery at high risk of infectious complications in orthopedic surgery).
Dosage regimen
V / m and / in an adult drug prescribed 750 mg 3 times / day, with severe infections of the flow dose increased to 1.5 g 3-4 times / day (if necessary, the interval between infusions may be shortened to 6 h).
Average daily dose - 3-6 PM
Children prescribed a dose of 30-100 mg / kg / day in 3-4 reception. For most infections the optimal dose is 60 mg / kg / day. Newborns and children up to 3 months drug is administered in a dose of 30 mg / kg / day in 2-3 reception.
When gonorrhea - a / m at a dose of 1.5 g once (or in the form of 2 injections of 750 mg with an introduction to the different areas, for example, in both gluteal muscles).
With bacterial meningitis - in / in 3 g every 8 h for children younger and older - 150-250 mg / kg / day in 3-4 admission, newborn - 100 mg / kg / day.
In operations on the abdomen, pelvic and orthopedic surgery - in / 1.5 g at induction of anesthesia, then in addition - i / m 750 mg after 8 and 16 h after surgery.
In operations on the heart, lungs, esophagus and blood vessels - in / 1.5 g at induction of anesthesia, then - / m, 750 mg 3 times / day over the next 24-48 h. In total joint replacement - 1.5 g of powder mixed in dry with each package of polymer methyl methacrylate cement before adding the liquid monomer.
When you have pneumonia - a / m or i / v for 1.5 g 2-3 times / day for 48-72 hours, then move on ingestion (use dosage forms for oral administration), 500 mg 2 times / day for 7 - 10 days.
With exacerbation of chronic bronchitis designate the / m or / in the 750 mg 2-3 times / day for 48-72 hours, then move on ingestion (use dosage forms for oral administration), 500 mg 2 times / day for 5-10 days.
In chronic renal failure must be corrected dosing regimen.
When QA 10-20 ml / min appointed in / or / m 750 mg 2 times / day, with spacecraft less than 10 ml / min - 750 mg 1 time / day.
Patients who are on continuous hemodialysis with arterio-venous shunt or hemofiltration a high speed to the ICU, prescribe 750 mg 2 times / d for patients on hemofiltration low speed, prescribe the dose recommended for renal events.
Side effect
Allergic reactions: fever, rash, itching, rash, rarely - erythema multiforme, bronchospasm, Stevens-Johnson syndrome, anaphylactic shock.
On the part of the digestive system: diarrhea, nausea, vomiting or constipation, bloating, cramping and abdominal pain, ulceration of the oral mucosa, oral candidiasis, glossitis, pseudomembranous enterocolitis, abnormal liver function (increased liver enzymes in plasma - AST, ALT , alkaline phosphatase, LDH, bilirubin), cholestasis.
On the part of the urinary system: renal dysfunction (decrease in RR, elevated levels of creatinine and urea nitrogen remaining in the blood), dysuria.
On the part of the reproductive system: an itch in the crotch, vaginitis.
On the part of the hemopoietic system: reduction of hemoglobin and hematocrit, anemia (aplastic or hemolytic), eosinophilia, neutropenia, leukopenia, agranulocytosis, thrombocytopenia, gipoprotrombinemii, lengthening prothrombin time.
Local reactions: irritation, infiltration, and pain at the injection site, phlebitis.
Contraindications
Hypersensitivity to cefuroxime and other cephalosporins, to penicillin and carbapenems.
Precautions should be prescribed the drug newborns, premature babies, with chronic renal failure, bleeding and gastrointestinal diseases (including a history, including UC), weak and debilitated patients.
Pregnancy and lactation
Precautions should be prescribed the drug during pregnancy and lactation.
Application for violations of renal function
In chronic renal failure must be corrected dosing regimen.
When QA 10-20 ml / min appointed in / or / m 750 mg 2 times / day, with spacecraft less than 10 ml / min - 750 mg 1 time / day.
Patients who are on continuous hemodialysis with arterio-venous shunt or hemofiltration a high speed to the ICU, prescribe 750 mg 2 times / d for patients on hemofiltration low speed, prescribe the dose recommended for renal events.
Cautions
Patients with a history of instructions on allergic reactions to penicillin may be the presence of hypersensitivity to cephalosporin antibiotics. In the course of treatment is necessary to monitor kidney function, especially in patients receiving the drug in high doses.
Treatment should continue for 48-72 hours after symptoms disappear in case of infections caused by Streptococcus pyogenes, it is recommended to continue treatment for at least 10 days. During treatment, the possible false-positive direct Coombs' reaction and false-positive reaction for urine glucose.
After reconstitution store at room temperature for 7 h in the refrigerator - for 48 hours is allowed to use yellowed during storage solution. In the period of treatment should avoid alcohol. Patients receiving cefuroxime, when determining the level of glucose in the blood recommend the use of tests with glucose oxidase or hexokinase.
The treatment of meningitis in children may be hearing loss. In the transition from parenteral to receive inside should take into account the gravity of infection, the sensitivity of microorganisms and the general condition of the patient. If within 72 h after administration of cefuroxime into the clinical improvement is noted, it is necessary to continue parenteral administration.
Overdose
Symptoms: central nervous system excitation, convulsions.
Treatment: the appointment of anticonvulsants, providing ventilation and function of the cardiovascular system, control and maintenance of vital body functions, hemodialysis and peritoneal dialysis.
Drug Interactions
In case of simultaneous appointment inside the "loop" diuretics has slowed tubular secretion, reduction in renal clearance, increasing plasma concentrations and an increase in T1 / 2 of cefuroxime.
With the simultaneous use of aminoglycosides and diuretics and increased risk of nephrotoxic effects.
Drugs that reduce gastric acidity, reduce the absorption of cefuroxime and its bioavailability.
Pharmaceutical interactions
Pharmaceutical compatible with metronidazole, azlotsillinom, xylitol, with an aqueous solution containing 1% lidocaine, 0.9% sodium chloride solution, 5% dextrose, 0.18% sodium chloride solution and 4% dextrose, 5% dextrose and 0.9% solution sodium chloride, 5% dextrose and 0.45% sodium chloride solution, 5% dextrose and 0.225% sodium chloride solution, 10% dextrose, 10% invert sugar in water for injection, Ringer's solution, a solution of sodium lactate, Hartmann's solution, 0.9 % solution of sodium chloride, 5% dextrose and hydrocortisone, heparin (10 U / ml and 50 U / ml) in 0.9% sodium chloride, potassium chloride (10 mEq / L and 40 mEq / L) in 0.9% solution of sodium chloride.
Pharmaceutical incompatible with aminoglycosides, a solution of sodium bicarbonate, 2.74%.
Terms and Conditions of storage
List B. The drug should be stored in a dry, protected from light and away from children at or above 25 ° C. Shelf life - 2 years.
No comments:
Post a Comment