Maxicef

Maxicef is a systemic antimicrobial drug.

Indications Maxicefa

Indicated for the elimination of bacterial infections caused by sensitive microbes:

• infections in the respiratory tract (such as bronchitis with pneumonia, pyothorax and abscessing pneumonia);
• gastrointestinal infections (such as cholecystitis with cholangitis and empyema in the gallbladder area);
• infections of the urogenital ducts (including pyelitis with pyelonephritis, as well as cystitis with urethritis and gonorrhea);
• infections in the area of the skin, joints with bones, and also inside soft tissues;
• in sepsis with peritonitis and meningitis;
• for the treatment of infected burns with wounds;
• neutropenic fever;
• infectious processes that develop as a result of immunodeficiency.

It is also used to prevent the development of postoperative infectious processes.

Release form

It is produced in the form of powder for the preparation of injection solution. Contained in glass bottles with a volume of 10 ml. Inside the pack - 1 bottle with powder.

Pharmacodynamics

Maxicef is an antibacterial drug from the 4th generation cephalosporin category. It has bactericidal properties and destroys the processes of binding the cell walls of pathogenic microbes. The drug has a wide range of action against gram-negative and gram-positive microorganisms, as well as strains resistant to aminoglycosides or cephalosporins (2nd and 3rd generations). It has high resistance to β-lactamases.

Active against gram-positive aerobes: Staphylococcus epidermidis (methicillin-sensitive strains only) and Staphylococcus aureus, Staphylococcus saprophyticus and Staphylococcus hominis, as well as other strains of the staphylococcal group. Active against Streptococcus pyogenes (category A), Streptococcus agalactiae (category B) and Streptococcus pneumoniae together with other β-hemolytic streptococci (categories C, G, and F), as well as Streptococcus bovis (category D) and Streptococcus viridans.

In relation to gram-negative aerobes, it acts on the following microbes: pseudomonads (including Pseudomonas aeruginosa, Pseudomonas putida and Pseudomonas stutzeri), Escherichia coli, Klebsiella (including Klebsiella pneumoniae, Klebsiella oxytoca and Klebsiella oxaenae), Enterobacter (including Enterobacter cloacae, Enterobacter aerogenes, as well as Enterobacter sakazakii and Enterobacter agglomerans), Proteus (including Proteus mirabilis and Proteus vulgaris), and also Acinetobacter calcoaceticus (here Acinetobacter calcoaceticus subsp. Iwoff with Acinetobacter anitratum are noted) and Aeromonas hydrophila. In addition, it acts on Capnocytophaga spp., Citrobacter (including Citrobacter diversus and Cyclobacter freundii), Campylobacter jejuni with Gardnerella vaginalis and Ducrey's bacillus with Haemophilus influenzae (including strains that produce β-lactamase). It is also effective against Haemophilus parainfluenzae, Legionella, Hafnia alve, Morgan's bacillus and Moraxella catarrhalis (including strains that produce β-lactamase). Efficiency also develops against gonococci (including strains that produce β-lactamase), meningococci, Providencia spp. (here, Providence Stuart and Providence Roettger are noted), Salmonella, Serratia (this includes Serratia marcescens and Serratia liquifaciens), as well as Shigella and Yersinia enterocolitica.

Effective against the following anaerobes: Prevotella (here noted Prevotella melaninogenicus), Clostridium perfringens, Fusobacterium spp., as well as Mobiluncus, Peptostreptococcus and Veillonella.

The drug is inferior to ceftazidime in its activity against pseudomonad strains.

It is not active against Stenotrophomonas maltophilia, Bacteroides fragilis and Clostridium difficile, as well as methicillin-resistant staphylococci and penicillin-resistant pneumococci.

Pharmacokinetics

The bioavailability level is 100%. After the drug administration (i.m. or i.v.) at a dose of 0.5 g, the peak concentration is observed after 1-2 hours. After the i.m. administration of the solution, the peak value (at a dose of 0.5, 1, and 2 g) is 14, 30, and 57 μg/ml, respectively. After the intravenous injection of the solution (doses of 0.25, 0.5, 1, and 2 g), the same value is 18, 39, 82, and 164 μg/ml, respectively. The medicinally effective value in plasma is reached within 12 hours. The average level of drug concentration after i.m. injection is 0.2 μg/ml, and after i.v. injection - 0.7 μg/ml.

High levels of the drug are observed in bile with urine, mucus secreted by the bronchi, exudate with peritoneal fluid and sputum, as well as inside the prostate, gall bladder and appendix. The distribution volume is 0.25 l/kg, and in children (aged 2 months/16 years) it is 0.33 l/kg. Synthesis of the substance with plasma protein reaches 20%.

Metabolism occurs in the kidneys and liver and accounts for 15%. The half-life is 2 hours, and the total clearance rate is 110 ml/minute.

Excretion occurs through the kidneys (85% of the substance is excreted unchanged, by glomerular filtration), and through breast milk. In the hemodialysis procedure, the half-life is 13 hours, and in the case of continuous peritoneal dialysis, it is 19 hours.

Dosing and administration

The course of treatment can be started even before the pathogenic microbe is identified. The route of administration and the dose are determined taking into account the severity of the infectious process, the sensitivity of the microbe, and also the functional state of the person's kidneys. The intravenous route of administration is usually prescribed to people suffering from severe forms of infections or in life-threatening infectious processes (especially with the risk of shock).

Dosages for children weighing over 40 kg and adults (with normal kidney function):

• for moderate and mild forms of infections in the urinary tract - a single dose (IV or IM) is 0.5-1 g (with an interval of 12 hours);
• other infectious processes (moderate or mild form) – a single dose is 1 g (i.m. or i.v.) at intervals of 12 hours;
• severe forms of infections – the dosage is 2 g (intravenous injection) with an interval of 12 hours;
• for life-threatening infections - a single dose is 2 g (administration intravenously) at intervals of 8 hours.

To prevent infection during surgery, a 2 g solution should be administered intravenously (over half an hour). After the procedure, another 0.5 g of metronidazole should be administered intravenously. This solution should not be administered simultaneously with Maxicef. The infusion system should be thoroughly flushed before using metronidazole.

For long-term (12+ hours) surgical procedures, 12 hours after the first dose is administered, a second dose (in the same amount) is required, followed by an injection of metronidazole.

Children from 2 months of age are allowed to administer the drug in doses not exceeding those recommended for adults. The average level of the pediatric dose (in children weighing less than 40 kg) in the treatment of uncomplicated or complicated processes in the urinary tract (including pyelonephritis) and empirical therapy of febrile neutropenia, as well as in the treatment of pneumonia and uncomplicated infectious processes (in soft tissues with skin) is 50 mg / kg every 12 hours.

People with bacterial meningitis and febrile neutropenia are prescribed a solution of 50 mg/kg every 8 hours.

The therapeutic course lasts on average 7-10 days, but when treating severe forms of infections it may be longer.

People with functional renal disorders (with CC less than 30 ml/minute) require a change in the drug dosing regimen. The initial dose remains similar to the level prescribed to people with healthy renal function. But the size of the maintenance doses is selected taking into account the CC level:

• at a rate of 10-30 ml/minute, the recommended dosages are: 1 g every 12 hours; 1 g every 24 hours; 0.5 g every 24 hours;
• at a level of less than 10 ml/minute – 1 g at intervals of 24 hours; 0.5 g at intervals of 24 hours; 0.25 g at intervals of 24 hours.

During hemodialysis procedures, about 68% of the total amount of cefepime administered is excreted from the body over a period of 3 hours. At the end of each procedure, a repeat injection equal to the initial dose is required. When using peritoneal dialysis, the drug is administered in average recommended doses (0.5, 1 or 2 g; the exact amount depends on the severity of the pathology), and the interval between procedures is 48 hours.

Rules for preparing a medicinal solution. To prepare a solution for intravenous administration, it is necessary to dissolve the powder in sterile water used for injections (volume - 10 ml), and also in a glucose solution (5%) or a sodium chloride solution (0.9%). Jet intravenous injection of the drug is carried out for 3-5 minutes. To administer it through an infusion system, the prepared solution must be mixed with other solutions for intravenous injections, and then administered for at least half an hour.

Maxicef solution with a concentration of 1-40 mg/ml is compatible with the following solutions (administered parenterally): sodium chloride injection solution (0.9%), glucose injection solution (5% or 10%), sodium lactate injection solution M/6. In addition, with a mixture of sodium chloride injection solutions (0.9%) and glucose (5%), as well as with a mixture of Ringer's lactate and glucose injection solutions (5%).

To prepare a solution for intramuscular injections, the powder should be dissolved in sterile water (volume 2.5 ml), and also in an injection solution of glucose (5%) or sodium chloride (0.9%). A bacteriostatic injection liquid with phenylcarbinol or paraben, mixed with a solution of lidocaine hydrochloride (0.5% or 1%), is also used.

Use Maxicefa during pregnancy

The drug is prescribed to pregnant and lactating women with caution.

Contraindications

Contraindications include severe intolerance to arginine and cefepime (or other penicillins with cephalosporins, as well as β-lactam antibiotics). In addition, the solution is prohibited for use in infants under 2 months of age.

Side effects Maxicefa

As a result of using the medicine, the following side effects may occur:

• allergic manifestations: skin rash (also of an erythematous nature), fever, severe itching, a positive Coombs test result, as well as anaphylactoid manifestations, the development of eosinophilia or Stevens-Johnson syndrome; in rare cases, Lyell's syndrome;
• local reactions: during intravenous injection – development of phlebitis, during intramuscular injection – pain, as well as hyperemia at the injection site;
• nervous system organs: dizziness with headaches, development of convulsions or paresthesia, feeling of anxiety, insomnia and confusion;
• urogenital system organs: development of vaginitis;
• urinary system organs: functional disorder of the kidneys;
• digestive system organs: nausea, constipation, diarrhea and vomiting, as well as dyspeptic symptoms, abdominal pain and the development of pseudomembranous enterocolitis;
• hematopoietic system: development of neutro-, thrombocyto-, pancyto-, and also leukopenia, as well as anemia (including its hemolytic form) and the appearance of bleeding;
• respiratory system: appearance of cough;
• cardiovascular system: occurrence of peripheral edema or dyspnea, development of tachycardia;
• test results: decreased hematocrit, increased urea, PT, liver transaminase and alkaline phosphatase activity, and also the development of hyperbilirubinemia, hypercalcemia or hypercreatininemia;
• other: pain in the back, chest or throat, development of hyperhidrosis, asthenia, and in addition to this, candidiasis of the oral mucosa, as well as superinfection.

Overdose

Overdose manifests itself (mainly in people with chronic renal failure) in the form of encephalopathy, agitation, and seizures.

Treatment requires procedures aimed at eliminating the signs of the disorder and hemodialysis.

Interactions with other drugs

The solution has pharmaceutical incompatibility with other antimicrobial drugs, as well as heparin.

Tubular excretion of cepefim is weakened when combined with aminoglycosides, diuretics, and polymyxin B. At the same time, these drugs increase its serum values and prolong the half-life, and also increase nephrotoxic properties (the likelihood of nephronecrosis increases).

Combination with NSAIDs increases the likelihood of bleeding and also inhibits the process of excretion of cephalosporins.

Maxicef enhances the ototoxic and nephrotoxic properties of furosemide, as well as aminoglycosides.

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Storage conditions

The powder should be stored in a dark place, protected from moisture, and inaccessible to children. Temperature data - within 15-25 ° C. The prepared solution is stored either at room temperature or in the refrigerator (at a temperature of 2-8 ° C).

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Shelf life

Maxicef is suitable for use within 2 years from the date of its release. The prepared solution can be stored for 24 hours at room temperature or 7 days if kept in the refrigerator.