Maxitsef

Maxycef is a systemic antimicrobial drug.

Indications of the maksitsaeff

It is indicated for the elimination of infections of bacterial origin provoked by sensitive microbes:

• infections in the respiratory tract (such as bronchitis with pneumonia, pyotorax and abscessed pneumonia);
• infections in the digestive tract (such as cholecystitis with cholangitis and empyema in the gallbladder area);
• infections of urogenital ducts (among them pyelitis with pyelonephritis, as well as cystitis with urethritis and gonorrhea);
• infection in the skin, joints with bones, as well as inside soft tissue;
• with sepsis with peritonitis and meningitis;
• for the treatment of infected burns with wounds;
• neutropenic fever;
• infectious processes that developed as a result of immunodeficiency.

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

Release form

Produced in the form of powder for the manufacture of injection solution. Contained in bottles of glass volume of 10 ml. Inside the pack - 1 bottle of powder.

Pharmacodynamics

Maxi cef is an antibacterial medicine from the category of cephalosporins of the 4th generation. 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, as well as Gram-positive microorganisms, and at the same time resistant to aminoglycosides or cephalosporins (2nd and 3rd generations) strains. He has high resistance against β-lactamases.

Actively influences gram-positive aerobes: epidermal staphylococcus (only susceptible to methicillin strains) and Staphylococcus aureus, Staphylococcus saprophytic and Staphylococcus hominis, as well as other strains from the group of staphylococci. Streptococcus pyogenes (category A), streptococcus agalactia (category B) and pneumococcus along with other β-hemolytic streptococci (categories C, G, and F), as well as Streptococcus bovis (category D) and Streptococcus viridans.

With respect to Gram-negative aerobes, it acts on such microbes: pseudomonas (among them the pseudomonas, Pseudomonas stutzeri pseudomonas and pseudomonas stutzeri), Escherichia coli, Klebsiella (including Klebsiella pneumonia, Klebsiella oxaenae, Klebsiella oxaenae), Enterobacter (among them Enterobacter cloaci, enterobacter aerogenes, as well as Enterobacter sakazakii and Enterobacter agglomerans), proteus (this includes prothus mirabilis and vulgar proteus), and in addition Acinetobacter calcoaceticus (here Acinetobacter calcoaceticus subsp. Iwoff with Acinetobacter anitratum are noted) and hydrophilic aeromonas. In addition, it affects Capnocytophaga spp., Tsitrobacter (here Citrobacter diversus and cyclobacter freundi are included), Campylobacter vaginitis with Gardnerella vaginalis and Ducrea stick with hemophilic rod (this includes strains that produce β-lactamases). It is also effective against Haemophilus parainfluenzae, legionella, Hafnia alve, morgan and moracelli cataralis bacteria (among them strains that produce β-lactamase). Efficacy develops with respect to gonococci (including strains producing β-lactamase), meningococci, Providencia spp. (here Stewart's providential and Providence of Rettger are noted), salmonella, serratia (this includes serratsia marces and serratia liquifaciens), and Shigella and Yersinia enterocolitis.

Effective against such anaerobes: prevotella (Prevotella melaninogenicus is noted here), clostridium perfringence, Fusobacterium spp., As well as mobilunculus, peptostreptococcus and vellonelles.

The drug is inferior to ceftazidime in activity relative to pseudomonas strains.

It has no activity against stentrofomonas maltophilia, bacteroidoid fragilis and clostridium difffile, as well as methicillin-resistant staphylococci and penicillin-resistant pneumococci.

Pharmacokinetics

The level of bioavailability is 100%. After the administration of drugs (in / m or / in) at a dosage of 0.5 g after 1-2 hours peak concentration is observed. After the / m administration of the solution, the peak value (at a dose of 0.5, 1, and also 2 g) is 14, 30, and 57 μg / ml, respectively. After injection of the IV solution (doses of 0.25, 0.5, 1, as well as 2 g), the same index is equal to 18, 39, 82, and 164 μg / ml, respectively. The drug effective value within the plasma reaches 12 hours. The average level of drug concentration after the IM injection is 0.2 μg / ml, and with the / in injection - 0.7 μg / ml.

High rates of drugs are observed in bile with urine, excreted by bronchial mucus, 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 the plasma protein reaches 20%.

Metabolism is carried out inside the kidneys with the liver and is 15%. The half-life is 2 hours, and the level of total clearance is 110 ml / minute.

Excretion occurs through the kidneys (85% of the substance is removed unchanged, by filtering the glomeruli), and also through breast milk. In the procedure of hemodialysis, the half-life is 13 hours, and in the case of continuous peritoneal dialysis it is equal to 19 hours.

Dosing and administration

You can begin treatment before the pathogenic microbial pathogen is detected. The method of administration and the size of the dose are determined taking into account the severity of the infectious process, the sensitivity of the microbe, and in addition the functional state of the kidneys of man. The route of intravenous administration is usually prescribed for people with severe forms of infection, or for life-threatening infectious processes (especially at the risk of a shock condition).

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

• with moderate and mild forms of infection 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) - one-time dosage is 1 g (IM or IV) with an interval of 12 hours;
• severe forms of infections - dosage is 2 g (intravenous injection) with an interval of 12 hours;
• for life-threatening infections - a single dose is 2 g (iv administration) at an interval of 8 hours.

As a prophylaxis of the development of infection during surgery, it is necessary to inject an IV solution in the amount of 2 g (for half an hour). At the end of the procedure, another 0.5 g of metronidazole is to be injected intravenously. This solution can not be administered simultaneously with Maxi cef. The infusion system must be thoroughly rinsed before using metronidazole.

With prolonged (12+ hours) surgical procedures 12 hours after the introduction of the 1st dose, it is required to re-administer (in the same size) with the subsequent injection of metronidazole.

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

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

The therapeutic course lasts for 7-10 days on average, but it can be longer in the treatment of severe forms of infections.

People with functional renal disorders (with a QC less than 30 ml / minute) require a change in the dosage regimen. The size of the initial dose remains the same as that prescribed for people with a healthy renal function. But the size of the supporting doses is selected taking into account the level of MC:

• at a rate of 10-30 ml / minute the recommended dosages are - 1 g after every 12 hours; 1 g after every 24 hours; 0.5 g after every 24 hours;
• at a level of less than 10 ml / minute - 1 g with an interval of 24 hours; 0.5 g with an interval of 24 hours; 0.25 g with an interval of 24 hours.

In hemodialysis procedures for a period of 3 hours from the body excreted about 68% of the total number of introduced cefepime. At the end of each procedure, it is required to inject a second injection equal to the initial dose. When using peritoneal dialysis, the drug is administered at the average recommended dosages (0.5, 1 or 2 g, the exact number depends on the level of severity of the pathology), and the interval between the procedures is 48 hours.

Rules for the preparation of medicinal solution. To prepare the solution for intravenous administration, it is necessary to dissolve the powder in sterile water used for injections (10 ml volume), and also in a solution of glucose (5%) or a solution of sodium chloride (0.9%). Intravenous intravenous injection of drugs is carried out for 3-5 minutes. To introduce it through the infusion system, it is required to mix the prepared solution with other solutions for intravenous injections, and then to enter a minimum of half an hour.

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

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

Use of the maksitsaeff during pregnancy

Pregnant women, as well as lactating women, are prescribed with caution.

Contraindications

Contraindication is the expressed intolerance of arginine and cefepime (or other penicillins with cephalosporins, as well as β-lactam antibiotics). In addition, it is forbidden to apply the solution to infants younger than 2 months.

Side effects of the maksitsaeff

As a result of using the medication, these side effects may appear:

• allergic manifestations: rash on the skin (also erythematous in nature), fever, severe itching, positive result of Coombs test, and also anaphylactoid manifestations, development of eosinophilia or Stevens-Johnson syndrome; in rare cases - Lyell's syndrome;
• local reactions: during intravenous injection - development of phlebitis, with intravenous injection - painful sensations, as well as hyperemia at the site of administration;
• organs of the National Assembly: dizziness with headaches, development of seizures or paresthesias, anxiety, insomnia and confusion;
• organs of the urogenital system: development of vaginitis;
• organs of the urination system: functional kidney disorder;
• organs of the digestive system: nausea, constipation, diarrhea and vomiting, as well as dyspepsia, abdominal pain and the development of pseudomembranous form of enterocolitis;
• hematopoietic system: the development of neutro-, thrombocyto-, pancito-, and also leukopenia, and in addition anemia (including hemolytic form) and the appearance of bleeding;
• organs of the respiratory system: the appearance of cough;
• organs of the cardiovascular system: the emergence of peripheral edemas or dyspnea, the development of tachycardia;
• data analysis: a decrease in hematocrit, an increase in the values of urea, PTV, the activity of liver transaminases and alkaline phosphatase, and in addition the development of hyperbilirubinemia, hypercalcemia or hypercreatininaemia;
• other: pain in the back, chest or throat, the development of hyperhidrosis, asthenia, and in addition to oral mucosal candidiasis, as well as superinfection.

[1]

Overdose

Overdose is manifested (mainly in people with kidney failure in chronic form) in the form of encephalopathy, excitation, as well as convulsive seizures.

Treatment requires procedures aimed at eliminating signs of impairment, and conducting hemodialysis.

Interactions with other drugs

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

The tubular secretion of the ceptepime weakens when combined with aminoglycosides by diuretics, as well as polymyxin B. Simultaneously, the data of the drug increase its serum values and prolong the half-life, as well as increase nephrotoxic properties (the probability of nephronecrosis increases).

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

Maksicef strengthens the ototoxic and nephrotoxic properties of furosemide, as well as aminoglycosides.

[2], [3], [4]

Storage conditions

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

[5], [6], [7]

Shelf life

Maxitsef is suitable for use in the period of 2 years from the moment of its release. The finished solution can be stored for 24 hours at room temperature or 7 days if it is kept in the refrigerator.

[8]