Maxi cef - instructions for use, doses, side effects, contraindications

Cephalosporin antibiotic IV generation for parenteral use. Has a wide spectrum of action against Gram-positive and Gram-negative bacteria, including those resistant to aminoglycosides and / or cephalosporins of the third generation, as well as to other antibiotics, strains. It acts bactericidal, disrupting the final stages of bacterial cell wall synthesis (inactivates the enzyme transpeptidase).Rapidly penetrates through the outer membrane of gram-negative bacteria; has a high affinity for penicillin-binding proteins, or bacterial transpeptidases. Highly resistant to hydrolysis by most beta-lactamases,

Maksiecef® is active in vivo and in vitro in relation to gram-positive aerobes: Staphylococcus aureus (only methicillin-sensitive strains), Streptococcus pneumoniae, Streptococcus pyogenes (Group A), Streptococcus spp. groups viridans; Gram-negative aerobes: Enterobacter spp., Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Pseudomonas aeruginosa. In vitro is active (but the clinical significance is unknown) for Gram-positive aerobes: Staphylococcus epidermidis (only methicillin-sensitive strains), Staphylococcus saprophytics, Streptococcus agalactiae (group B); Gram-negative aerobes: Acinetobacter Iwoffii, Citrobacter diversus, Citrobacter freundii, Enterobacter agglomerans, Haemophilus influenzae (including strains producing beta-lactamase), Hafriia alvei, Klebsiella oxytoca, Moraxella catarrhalis (including strains producing beta-lactamases), Morganella morganii, Proteus vulgaris, Providencia rettgeri, Providencia stuartii, Serratia marcescens. Most strains Enterococcus spp., in t.ch. Enterococcus faecalis, methicillin-resistant Staphylococcus spp., Stenotrophomonas (formerly known as Xanthomonas maltophilia and Pseudomonas maltophilia), Clostridium difficile are not sensitive to cefepime.

Secondary resistance of microorganisms to Maxycete® develops slowly.

Pharmacokinetics:

After intravenous infusion of cefepime in a dose of 0.5 g, 1 g maximum concentrations (C_max) are 39 mg / l and 82 mg / l, respectively. One hour after the infusion, 0.5 g and 1 g of plasma concentration are reduced almost 2 times and are 22 mg / L, 45 mg / L, respectively. After 8 hours, the plasma contains 1.4 mg / L, 2.4 mg / L cefepime, and after 12 hours 0.2 mg / L and 0.6 mg / L, respectively.

Bioavailability with intramuscular (IM) administration is 100%. C_max after a / m injection at doses of 0.5 g and 1 g in the interval between the first and second hours after the administration are 14 mg / l and 30 mg / l, respectively. 12 hours after the injection of cefepime in doses of 0.5 g and 1 g of plasma concentration are reduced to 0.7 mg / l and 1.4 mg / l, respectively.

The volume of distribution is 0.25 l / kg, in children from 2 months to 16 years - 0.33 l / kg. The degree of binding to plasma proteins is, on average, 20% and does not depend on the concentration of cefepime in the blood.

After IV and IV injections, high concentrations are determined in urine, bile, peritoneal fluid, interstitial tissue and fluid, skin, subcutaneous tissue, bronchial mucosal secretions, lungs, sputum, prostate gland, appendix and gallbladder wall. In small concentrations cefepime penetrates into breast milk. Half-life (T_1/2) is about 2 hours. In patients with renal failure due to delayed excretion of cefepime T_1/2increases, which requires correction of doses and modes of administration.

Approximately 15% of the administered dose is metabolized in the liver. 85% of the administered dose is excreted unchanged through the kidneys; the rest is metabolites.

Indications:

Bacterial infections caused by microorganisms sensitive to cefepime:

- infections of the lower respiratory tract, incl. moderate and severe pneumonia, bronchitis;

- intra-abdominal infections (in combination with metronidazole), including peritonitis, abdominal abscess, bile duct infections, infectious complications of pancreatitis;

- infectious and inflammatory diseases of the pelvic organs in women;

- uncomplicated and complicated urinary tract infections, incl. pyelonephritis, pyelitis;

- infections of the skin and soft tissues;

- febrile neutropenia (empirical therapy);

- sepsis.

Contraindications:

- Hypersensitivity to cefepime, arginine, other cephalosporins, penicillins, other beta-lactam antibiotics;

- children age up to 2 months.

Carefully:Patients with impaired renal function (see Dosage and Administration); with indications for colon diseases, especially ulcerative colitis.

Pregnancy and lactation:

During pregnancy and lactation prescribed for "vital" indications. If you need to use the drug during lactation, you should decide whether to stop breastfeeding.

Dosing and Administration:

- Intravenous (intravenously), intramuscularly (in / m).

Adults and children with a body weight of more than 40 kg with normal renal function.

Intravenously (IV) in the form of infusion duration of at least 30 minutes or intramuscularly (IM).

For mild to moderate infections of the urinary tract - 0.5-1 g IV or IM every 12 hours; for mild and moderate infections of other sites

- g IV or IM every 12 h; in severe infections - 2 g IV every 12 hours; with very serious and life-threatening infections - 2 g IV every 8 hours. The average duration of the course of MTC treatment is 7-10 days.

Children from 2 months with a body weight of up to 40 kg. The usual recommended dose for

complicated or uncomplicated urinary tract infections, infections skin and soft tissues, pneumonia is 50 mg / kg 2 times a day; with severe infections and febrile neutropenia - 50 mg / kg 3 times a day. The maximum single dose should not exceed 2 g.

The average duration of Maxitsef® therapy is 7-10 days.In the treatment of febrile neutropenia, the administration of Maxicef® is continued for 7 days or until neutropenia is resolved.

Patients with impaired renal function. With renal failure, dose adjustment is required depending on the creatinine clearance. The initial dose of Maxi cef® should be the same as for patients with normal renal function. Recommended maintenance doses are presented in the table.

Clearance creatinine, ml / min	Recommended maintenance doses
>50	(Usual dose (depending on the severity of the infection), correction is not required).
>50	2 g every 8 hours	2 g every 12 h	1 g every 12 h	0.5 g every 12 h
30-50	2 g every 12 h	2 g every 24 h	1 g every 24 h	0.5 g every 24 hours
11-29	2 g every 24 h	1 g every 24 h	0.5 g every 24 hours	0.5 g every 24 hours
<10	1 g every 24 h	0.5 g every 24 hours	0.25 g every 24 h	0.25 g every 24 h
Patients on hemodialysis *	0.5 g every 24 hours	0.5 g every 24 hours	0.5 g every 24 hours	0.5 g every 24 hours

* - For patients on hemodialysis: in the first day - loading

dose of 1 g, then 0.5 g every 24 hours for all infections other than febrile neutropenia, at which the maintenance dose is 1 g every 24 hours. On dialysis days, Maxiceft® should be administered at the end of the dialysis procedure. If possible, the drug should be administered every day at the same time.

Data on the use of the drug in children with concomitant chronic renal insufficiency (CRF) are not available, however, given the similar pharmacokinetics in children and adults, the dosage regimen (dose reduction or increase in the interval between administrations) in children with chronic renal insufficiency resembles the adult dosing regimen .

Intramuscular injection

For intravenous administration, the sterile Maxycef® powder is dissolved in sterile water for injection, 0.9% sodium chloride solution, 0.5% or 1% lidocaine solution. The following minimum amounts of solvent are added directly to the bottle with a dry antibiotic powder:

Vial containing 0.5 g Maxicerate® 1.3 ml solvent

A vial containing 1.0 g of Maxicef®® with 2.4 ml of solvent

The resulting solution, an approximate concentration of cefepime in which 280 mg / ml, is administered intramuscularly to areas of the body with a pronounced muscular layer (upper to outer quadrant of the buttock or lateral surface of the thigh). It is recommended that an aspiration test be carried out to avoid undesirable introduction of the solution into the blood vessel.

Intravenous administration

For intravenous administration, Maxicef® is dissolved in sterile water for injection, 0.9% solution of sodium chloride or 5% solution of dextrose. The following minimum amounts of solvent are added directly to the bottle with a dry antibiotic powder:

Vial containing 0.5 g Maxicerate® 5 ml solvent

Bottle containing 1.0 g of Maxicef® 10 ml of solvent

The resulting solution, an approximate concentration of cefepime in which 100 mg / ml, is administered ip slowly, for 3-5 min; it is possible to administer through a special node or port for injection of a system for intravenous infusions if the patient receives fluids parenterally.

For intravenous drip injection, 0.5 g of Maxicef® is dissolved in 5 ml, 1 g in 10 ml of sterile water for injection, 0.9% solution of sodium chloride or 5% solution of dextrose. The resulting solution is added to a vial containing 50-100 ml of a compatible infusion medium. Enter through the system for IV infusions for at least 30 minutes. Maksichefa® solutions are compatible with 0.9% sodium chloride solution, 5% dextrose solution; solution for infusions containing 0.45% sodium chloride and 5% dextrose; solution for infusions containing 0.9% sodium chloride and 5% dextrose; 5% dextrose solution in Ringer's solution with lactate.

Side effects:

Maxi cef® is usually well tolerated.Undesirable drug reactions are rare and transient.

Allergic reactions: urticaria, pruritus, anaphylactoid reactions, fever, erythema multiforme exudative, Stevens-Johnson syndrome, Lyell syndrome.

From the gastrointestinal tract: diarrhea, nausea, vomiting, constipation, abdominal pain, dyspepsia, pseudomembranous colitis.

From the side of the cardiovascular system: pain behind the breastbone, tachycardia, peripheral edema, dyspnea.

From the respiratory system: cough.

From the central nervous system: headache, dizziness, insomnia, paresthesia, anxiety, confusion, convulsions.

From the hematopoiesis: Thrombocytopenia, leukopenia, including neutropenia; anemia, pancytopenia, bleeding.

Local reactions: phlebitis after intravenous administration, hyperemia and tenderness in places with / m injections.

Changes in laboratory indicators: hyperbilirubinemia, increased activity of "hepatic" enzymes - alanine aminotransferase, aspartate aminotransferase, alkaline phosphatase, increased urea concentration, hypercreatininaemia,false positive test of Coombs; increased prothrombin time.

From the organs of the urinary system: toxic nephropathy.

Other: asthenia, excessive sweating, sore throat, back pain, vaginitis, oropharyngeal candidiasis.

Overdose:Symptoms: convulsions, encephalopathy, agitation. Treatment: symptomatic and maintenance therapy, hemodialysis.

Interaction:

"Loop" diuretics, aminoglycosides, polymyxin B reduce the tubular secretion of cefepime, extend T1 / 2 and increase its concentration in serum, increasing the risk of developing nephrotoxicity.

Pharmaceutically incompatible with aminoglycosides (gentamycin, tobramycin, amikacin, netilmicin), vancomycin, metronidazole; Do not mix these antibiotics in one syringe or one infusion medium; with intravenous administration cefepime and other antibiotics are recommended to be administered separately, either by observing a certain sequence with a certain time interval between injections (infusions), or by injecting through separate intravenous catheters; Before the introduction of a solution of metronidazole, the infusion system should be rinsed from the cefepime solution.

Nonsteroidal anti-inflammatory drugs, slowing the excretion of cephalosporins, increase the risk of bleeding.

With simultaneous use with aminoglycosides, a pronounced synergism of antimicrobial effect is observed.

Special instructions:

If diarrhea occurs during treatment with Maxi cef®, caution should be exercised because of the possible development of pseudomembranous colitis. If a diagnosis of antibiotic-associated diarrhea or pseudomembranous colitis is established, Maxieff® administration should be immediately discontinued and appropriate treatment should be prescribed.

Maxi cef® can be used in the form of monotherapy before identifying the microorganism-pathogen. In patients with a possible mixed aerobic-anaerobic infection, treatment with Maksitsefom® in combination with an anaerobic drug can be started.

As with other antibiotics, the use of Maxi cef® can lead to the colonization of insensitive microflora and the development of superinfection.

Possible false positive test Coombs and a false positive test result for glucose in the urine.

With prolonged treatment, regular monitoring of peripheral blood is necessary,indicators of the functional state of the liver and kidneys.

Effect on the ability to drive transp. cf. and fur:When using cefepime, caution should be exercised when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Powder for solution for intravenous and intramuscular injection 0.5 g and 1.0 g.

Packaging:

0.5 g and 1.0 g of active substance into 10 ml glass vials, hermetically sealed with plugs crimped with aluminum caps or crimped caps with combined (aluminum with safety plastic caps).

The solvent - "Water for injection" in glass ampoules of 5 ml.

1 bottle with the drug and instructions for use are placed in a pack of cardboard.

1 bottle with the drug and 1 ampoule with a solvent and instructions for use are placed in a pack of cardboard.

1 bottle with the drug and 1 ampoule with solvent are packaged in a contour mesh package.

One contour mesh package and instructions for use are put in a pack of cardboard.

5 bottles of the drug are packaged in contoured cell packs. One contour mesh package and instructions for use are put in a pack of cardboard.

5 bottles of the drug complete with 5 ampoules of the solvent are packaged in contoured cell packs. One outline package with the preparation, one outline package with a solvent and instruction for use is put in a pack of cardboard.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:2 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N003298 / 01

Date of registration:02.03.2009 / 15.01.2018

Expiration Date:Unlimited

The owner of the registration certificate:PREBAND PFC, LLCPREBAND PFC, LLC Russia

Manufacturer: & nbsp

PREBAND PFC LLC Russia

Information update date: & nbsp28.03.2018

Illustrated instructions

Instructions

Maxitsef® (Maxicef®)