Maxipim powder for solution for injection
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Active ingredients
Cefepime
Composition
1 fl. cefepime dihydrochloride monohydrate 1 g. Excipients: L-arginine.
Pharmacological effect
Cephalosporin antibiotic IV generation. It has a broad spectrum of activity against gram-positive and gram-negative bacteria, strains resistant to aminoglycosides or third-generation cephalosporin antibiotics. Cefepime is highly resistant to hydrolysis by most β-lactamases, has a low affinity for β-lactamases encoded by chromosomal genes, and quickly penetrates into gram-negative bacterial cells. Maxipim is active against gram-positive aerobic bacteria: Staphylococcus aureus (including strains producing β-lactamase), Staphylococcus epidermidis (including strains producing β-lactamase), other strains of Staphylococcus spp. (including Staphylococcus hominis, Staphylococcus saprophyticus), Streptococcus pyogenes (streptococci of group A), Streptococcus agalactiae (streptococci of group B), Streptococcus pneumoniae (including strains with medium resistance to penicillin - MPC from 0.1 to 1 to 1, for example, for example, for example, for example, for example, for example), for example, for example, for example, for example, for example, for example, for example, for example, for example, for example, for example, for example, for example, for example, for example, for example, for example, for example, for example, for example, for example, IPC from 0.1 to 10% D), Streptococcus viridans, other beta-hemolytic streptococci (groups C, g, F); Gram-negative aerobic bacteria: Pseudomonas spp. (including Pseudomonas aeruginosa, Pseudomonas putida, Pseudomonas stutzeri), Escherichia coli, Klebsiella spp. (including Klebsiella pneumoniae, Klebsiella oxytoca, Klebsiella ozaenae), Enterobacter spp. (including Enterobacter cloacae, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter sakazakii), Proteus spp. (including Proteus mirabilis, Proteus vulgaris), Acinetobacter calcoaceticus (subtype Acinetobacter anitratus, Acinetobacter lwoffii), Aeromonas hydrophila, Capnocytophaga spp., Citrobacter spp. (including Citrobacter diversus, Citrobacter freundii), Campylobacter jejuni, Gardnerella vaginalis, Haemophilus ducreyi, Haemophilus influenzae (including strains that produce β-lactamases), Haemophilus parainfluenzae, Hafnia alvei, Legionella, and you will be able to make a link to make your counterparts, Haemophilus parainfluenzae, Hamophilus influenzae, Haemophilus influenzae; lactamases), Neisseria gonorrhoeae (including strains producing β-lactamases), Neisseria meningitidis, Providencia spp. (including Providencia rettgeri, Providencia stuartii), Salmonella spp., Serratia spp. (including Serratia marcescens, Serratia liquefaciens), Shigella spp., Yersinia enterocolitica; anaerobic bacteria: Bacteroides spp. (including Bacteroides melaninogenicus, other strains of Bacteroides spp. / in the oral cavity /), Clostridium perfringens, Fusobacterium spp., Mobiluncus spp., Peptostreptococcus spp., Veillonella spp. Some strains of Xanthomonas maltophilia (Pseudomonas maltophilia), Bacteroides fragilis, Clostridium difficile are resistant to the drug. Most strains of enterococcus (including Enterococcus faecalis) and methicillin resistant staphylococci are resistant to most cephalosporin antibiotics, including cefepime.
Pharmacokinetics
Absorption: Cmax in plasma of cefepime with intravenous administration in doses of 500 mg, 1 g and 2 g is 39.1 ± 3.5 mcg / ml, 81.7 ± 5.1 mcg / ml and 163.9 ± 25.3 mcg / ml, respectively. After i / m administration, cefepime is absorbed completely. At doses of 500 mg, 1 g and 2 g of Cmax, cefepime in plasma is 13.9 ± 3.4 μg / ml, 29.6 ± 4.4 μg / ml, 57.5 ± 9.5 μg / ml, respectively; Tmax is 1.4 ± 0.9 h, 1.6 ± 0.4 h, 1.5 ± 0.4 h, respectively. Distribution Binding to plasma proteins is less than 19% and does not depend on the concentration of cefepime in serum.In healthy people with the on / in the introduction of Maxipima at a dose of 2 g with an interval of 8 hours for 9 days was not observed cumulation of cefepime in the body. Therapeutic concentrations of cefepime are found in urine, bile, peritoneal fluid, the contents of burn blisters, bronchial mucous secretions, prostate tissues, appendix and gall bladder. Metabolism and excretion: Cefepime is metabolized to N-methylpyrrolidine, which quickly turns into N-methylpyrrolidine oxide. The average T1 / 2 of cefepime is about 2 hours. The total clearance is on average 120 ml / min. Cefepime is derived almost entirely due to renal regulation mechanisms, mainly by glomerular filtration (mean renal clearance is 110 ml / min). In the urine, approximately 85% of cefepime administered is found unchanged, less than 1% N-methylpyrrolidine, about 6.8% N-methylpyrrolidine oxide, and about 2.5% cefepime epimer. Pharmacokinetics in special clinical situations: After a single intravenous injection of the drug in a dose of 1 g, patients over 65 years old showed an increase in AUC and a decrease in renal clearance, compared with young patients. Patients with impaired renal function require correction dosing regimen. In patients with renal insufficiency of varying severity of T1 / 2 from the body increases. In severe impaired renal function requiring dialysis sessions, T1 / 2 averages 13 hours during hemodialysis and 19 hours during peritoneal dialysis. Cefepime pharmacokinetics in patients with impaired liver function or cystic fibrosis is not changed. Dose adjustment for these patients is not required. In children aged 2 months to 11 years after a single intravenous or intramuscular injection of the drug at a dose of 50 mg / kg body weight and after the introduction of several doses of the drug every 8 hours (n = 29) or every 12 hours (n = 13), but not less than 48 hours, the total clearance and Vd were 3.3 ± 1.0 ml / min / kg and 0.3 ± 0.1 l / kg. The removal of cefepime unchanged with urine was 60.4 ± 30.4% of the administered dose, and the average renal clearance was 2.0 ± 1.1 ml / min / kg. The age and sex of the patients did not have a significant effect on the total clearance and Vd, taking into account the correction for the body weight of each. With the introduction of the drug at a dose of 50 mg / kg every 12 hours (n = 13), cefepime was not cumulated, while Cmax, AUC and T1 / 2 increased by about 15% at steady state with the introduction of 50 mg / kg every 8 h.The pharmacokinetic parameters of cefepime in children after iv administration at a dose of 50 mg / kg are comparable to the pharmacokinetic parameters of the drug in adults after iv administration at a dose of 2 g. for a median of 0.75 h. After 8 h after i / m administration, the concentration of cefepime in plasma was on average 6 μg / ml. The absolute bioavailability of cefepime after i / m injection averages 82%.
Indications
Treatment of infectious and inflammatory diseases caused by microorganisms sensitive to the drug: - infections of the lower respiratory tract (including pneumonia and bronchitis) - urinary tract infections (both complicated, including pyelonephritis and uncomplicated) - infections of the skin and soft tissues - intra-abdominal infections (including peritonitis and infections of the biliary tract) - gynecological infections - septicemia - neutropenic fever (as an empirical therapy) - bacterial meningitis in children. Prevention of infections during abdominal surgery.
Contraindications
- hypersensitivity to cefepime or L-arginine, as well as to cephalosporin antibiotics, penicillins or other beta-lactam antibiotics.
Use during pregnancy and lactation
Adequate and strictly controlled studies of the safety of using Maxipime during pregnancy have not been conducted; use of the drug is possible only under medical supervision. Cefepime is excreted in breast milk at very low concentrations. The use of the drug during lactation (breastfeeding) is possible in the case when the intended benefit to the mother outweighs the potential risk to the infant. In experimental studies on laboratory animals, no effect on the reproductive function or any fetotoxic effect of cefepime was detected.
Dosage and administration
Maxipim treatment can begin even before the identification of the pathogen microorganism. The dose and route of administration is determined depending on the sensitivity of the pathogen, the severity of the infection, as well as the state of the patient’s kidney function. In / in the route of administration is preferable for patients with severe or life-threatening infections. Adults and children weighing more than 40 kg with normal kidney function, the drug is prescribed in the following doses.Severity of the disease Single dose Interval between administrations Mild to moderate urinary tract infections 0.5-1 g intramuscularly or intramuscularly every 12 hours Other infections of mild to moderate severity 1 g intravenous or intramuscularly every 12 hours Severe infections 2 g IV every 12 hours Very heavy and life-threatening infections 2 g IV every 8 hours To prevent possible infections during surgical operations 60 minutes before the start of surgery, the drug is administered at a dose of 2 g IV for 30 minutes. . After the end of the infusion, metronidazole is also prescribed intravenously in a dose of 500 mg. Solutions of metronidazole should not be administered simultaneously with the drug Maxipime. The infusion system should be flushed before administering metronidazole. During long (more than 12 hours) surgeries 12 hours after the first dose, it is recommended to re-administer an equal dose of the drug Maxipime, followed by the introduction of metronidazole. For children from 2 months of age, the maximum dose should not exceed the recommended dose for adults. The average dose for children weighing up to 40 kg in complicated or uncomplicated urinary tract infections (including pyelonephritis), uncomplicated infections of the skin and soft tissues, pneumonia, and empirical treatment of neutropenic fever is 50 mg / kg every 12 hours. For patients with neutropenic fever and bacterial meningitis drug is prescribed at 50 mg / kg every 8 hours. The average duration of therapy is 7-10 days. For severe infections, longer treatment may be required. In patients with impaired renal function (CC less than 30 ml / min), a correction is necessary for the dosage regimen of the drug. The initial dose of Maxipima should be the same as for patients with normal renal function. Maintenance doses of the drug is determined depending on the values of QC. Creatinine clearance (ml / min) Recommended doses of 2 g every 8 h 2 g every 12 h 1 g every 12 h 500 mg every 12 h> 50 recommended dose, correction does not require 50-30 2 g every 12 h 2 g every 24 h 1 g every 24 h 500 mg every 24 h 29-11 2 g every 24 h 1 g every 24 h 500 mg every 24 h 500 mg every 24 h ≤ 10 1 g every 24 h 500 mg every 24 h 250 mg every 24 h 250 mg every 24 hours Approximately 68% of the total amount of cefepime is removed from the body during hemodialysis in 3 hours. At the end of each session, you must enter a repeated dose equal to the initial dose.In patients on continuous ambulatory peritoneal dialysis, Maxipime can be used in the average recommended dose, i.e. 500 mg, 1 g or 2 g, depending on the severity of the infection, with an interval between injections of a single dose of 48 hours. In children with impaired renal function, the same changes in dosing regimen as for adults are recommended in accordance with the table above. Rules for preparation and administration of solutions To prepare a solution for iv administration, powder for injection in a vial is dissolved in 5 ml or 10 ml of sterile water for injection, 5% glucose solution or 0.9% sodium chloride solution, as indicated in the table below. In / in the jet Maxipim injected for 3-5 minutes. For the introduction through the system for IV infusion, the prepared solution is combined with other IV solutions for injections and administered for at least 30 minutes. Solutions of Maxipim in concentrations from 1 to 40 mg / ml are compatible with the following solutions for parenteral administration: 0.9% sodium chloride solution for injection, 5% or 10% glucose solution for injection, M / 6 sodium solution of injection lactate, solution 5% glucose and 0.9% sodium chloride for injection, Ringer's solution with lactate and 5% glucose solution for injection. To prepare a solution for i / m administration, the powder for injection in the vial is dissolved in sterile water for injection, 5% glucose solution for injection or 0.9% solution of sodium chloride for injection, bacteriostatic water for injection with paraben or benzyl alcohol, in 0.5% or 1 % solution of lidocaine hydrochloride, as indicated in the table. Powder for injection The volume of the solution for dilution (ml) The volume of the obtained solution (ml) The concentration of cefepime (mg / ml) B / in the introduction of 500 mg / fl. 5 5.6 100 1 g / fl. 10 11.3 100 V / m administration of 500 mg / fl. 1.3 1.8 280 1 g / fl. 2.4 3.6 280 During storage, the powder in the vial or solution may darken, but this does not affect the activity of the preparation.
Side effects
On the part of the digestive system: 1.2% - diarrhea; > 0.1-1% - nausea, vomiting, colitis (including pseudomembranous colitis); 0.05-0.1% - abdominal pain, constipation, change in taste. Allergic reactions: 1.8% - rash; > 0.1-1% - itching, urticaria; less than 0.05% - anaphylactic reactions. From the side of the central nervous system and peripheral nervous system:> 0.1-1% - headaches; 0.05-0.1% - dizziness, paresthesia; less than 0.05% are convulsions. Dermatological reactions: 0.05-0.1% - redness of the skin. Most common in children is rash. From the hemopoietic system: ≤2% - anemia.From the side of laboratory research indicators: 3.2% - increased ALT, 2.7% - increased AST; ≤2% - an increase in alkaline phosphatase, an increase in total bilirubin, eosinophilia, an increase in prothrombin time or partial thromboplastin time; less than 0.5% - a temporary increase in blood urea nitrogen and / or serum creatinine, transient thrombocytopenia, transient leukopenia and neutropenia; 18.3% - a positive Coombs test without hemolysis. Local reactions: 5.2% - with the on / in the introduction (2.9% - phlebitis, 0.1% - inflammation); 2.6% - inflammation or pain with a / m injections. Other:> 0.1-1% - fever, vaginitis, erythema; 0.05-0.1% - shortness of breath, chills, genital itching, candidiasis. Maxipim is usually well tolerated. In clinical trials, the incidence of side effects associated with the use of the drug was low. The most frequent side effects were symptoms of the digestive system and allergic reactions. When using other antibiotic cephalosporin: possible rash, Stevens-Johnson syndrome, multiple erythema, toxic necrolysis epidermis, colitis, renal failure, toxic nephropathy, aplastic anemia, hemolytic anemia, bleeding, seizures, abnormal liver function, including cholestasis, and false positive urine glucose test results.
Overdose
Symptoms: with a significant overdose, symptoms of encephalopathy are described. Treatment: in cases of significant excess of the recommended doses, especially in patients with impaired renal function, hemodialysis is indicated.
Interaction with other drugs
In vitro studies have shown synergism of the action of Maxipime with respect to aminoglycosides. With simultaneous use of drugs, the risk of nephrotoxicity and ototoxicity of aminoglycoside antibiotics increases.
special instructions
Relevant tests should be performed to identify the causative microorganism and determine sensitivity to cefepime. If there is a risk of a mixed aerobic / anaerobic (including Bacterioides fragilis) infection, treatment with Maxipime in combination with an anaerobic drug can be started before identification of the pathogen. With the development of a severe allergic reaction during the administration of Maxipime, it may be necessary to urgently introduce intracranial corticosteroids, antihistamines, vasopressor drugs, intravenous infusion of physiological solutions and measures aimed at maintaining respiratory function. If diarrhea occurs during treatment with Maxipime, the possibility of pseudomembranous colitis should be considered.Mild forms of colitis can pass on their own after stopping the drug; moderate to severe cases may require special treatment. When using Maxipima (as well as other antibiotics), superinfection may develop, which requires discontinuation of the drug and appropriate treatment. With the simultaneous administration of Maxipime solution (like most other beta-lactam antibiotics) with solutions of metronidazole, vancomycin, gentamicin, tobramycin sulfate and netilmicin sulfate, a pharmaceutical interaction is possible. When prescribing Maxipima with the listed drugs, each antibiotic should be administered separately. Use in Pediatrics The safety profile of the drug in children and adults is the same. The safety and efficacy of the drug in children under the age of 2 months has not been established. The drug is recommended for use in children from 2 months.