Cefurabol - instructions for use, dose, side effects, contraindications

Cephalosporin antibiotic II generation for parenteral use. It acts bactericidal (it breaks the synthesis of the bacterial cell wall). Has a wide spectrum of antimicrobial action. Highly active with respect to: gram-positive microorganisms: Staphylococcus" aureus, Staphylococcus epidermidis,, including strains resistant to penicillins, but excluding strains resistant to methicillin, Streptococcus pyogenes and others beta-hemolytic streptococci, Streptococcus pneumoniae, Streptococcus group B (Streptococcus agalactiae), Streptococcus mitis (groups viridans), Bordetella pertussis); Gram-negative microorganisms: Escherichia coli, Klebsiella spp., Proteus mirabilis," Providencia spp., Providencia rettgerri, Haemophilus influenzae, including strains resistant to ampicillin, Haemophilus parainfluenzae, including strains resistant to ampicillin, Moraxella catarrhalis, Neisseria gonorrhoeae,, including strains that produce and do not produce penicillinase, Neisseria meningitidis, Salmonella spp., Bacteroides spp., Borrelia burgdorferi; gram-positive and gram-negative anaerobes: including Clostridium spp. (Besides Clostridium difficile), Peptococcus spp., Peptostreptococcus spp., Fusobacterium spp., Propionibacterium spp.

TO cefuroxime insensitive: Clostridium difficile, Pseudomonas spp., Campylobacter spp., Acinetobacter calcoaceticus, Listeria monocytogenes, sustainable to methicillin strains Staphylococcus aureus, sustainable to methicillin strains Staphylococcus epidermidis, Legionella spp., Enterococcus faecalis, Morganella morganii, Proteus vulgaris, Enterobacter cloacae, Citrobacter spp., most strains Serratia spp., Bacteroides fragilis.

Pharmacokinetics:

After intramuscular (intramuscular) administration of 750 mg, the maximum concentration (Cmax) is reached after 15-60 minutes and is 27 μg / ml. With intravenous (IV) administration of 750 mg and 1500 mg of C max in 15 minutes is 50 and 100 μg / ml, respectively. The therapeutic concentration is maintained at 5.3 and 8 hours, respectively. The half-life period (T1 / 2) for IV and IM injection is 1.3-1.5 hours, in newborns 2-2.5 hours. The connection with plasma proteins is 33-50%. '

In the body it is not metabolized. It is excreted by the kidneys by glomerular filtration and tubular secretion unchanged: 85-90% within 8 hours (most of the drug is excreted within the first 6 hours, while creating high concentrations in the urine); after 24 hours it is completely removed (50% by tubular secretion, 50% by glomerular filtration).Therapeutic concentrations are determined in the pleural fluid, bile, sputum, myocardium, skin and soft tissues. Concentrations of cefuroxime exceeding the minimum inhibitory concentrations for most microorganisms can be achieved in bone tissue, synovial and intraocular fluid. When meningitis penetrates the blood-brain barrier, patients with bacterial meningitis in the cerebrospinal fluid achieve therapeutic concentrations of cefuroxime. Passes through the placenta and penetrates into breast milk.

Indications:

Bacterial infections of various localizations caused by microorganisms sensitive to cefuroxime:

- infectious diseases of the respiratory tract (including bronchitis, pneumonia, lung abscess, pleural empyema);

- infections of LOP - organs (including sinusitis, tonsillitis, pharyngitis, otitis media);

- urinary tract infections (including pyelonephritis, cystitis, asymptomatic bacteriuria, gonorrhea);

- infections of the skin and soft tissues (including erysipelas, pyoderma, impetigo, furunculosis, cellulitis, wound infection, erysipelitis);

- infection of bones and joints (including osteomyelitis, septic arthritis);

- Infectious-inflammatory diseases of the pelvic organs (including salpingitis, endometritis, salpingo-oophoritis);

- septicemia;

- meningitis;

- Lyme disease (borreliosis).

It is indicated for antibiotic prophylaxis of infectious complications during operations at the

chest, abdominal, pelvis, joints (including operations on the lungs, heart, esophagus, vascular surgery with a high risk of infection complications, and orthopedic operations).

Contraindications:Hypersensitivity to cefuroxime, other cephalosporins, penicillins and carbapenems.

Carefully:With caution, the drug is used in newborns and prematurity; in weakened and depleted patients; with chronic renal failure (CRF), diseases of the large intestine (including in history and ulcerative colitis); when used simultaneously with aminoglycosides and loop diuretics.

Pregnancy and lactation:

During pregnancy, appoint in cases where the intended benefit to the mother exceeds the possible risk to the fetus, and should be carried out under the supervision of a specialist.

Cefuroxime penetrates into breast milk in low concentrations.If it is necessary to use the drug during lactation, breastfeeding should be stopped.

Dosing and Administration:

Intramuscularly, intravenously struyno and drip.

Adults appoint 750 mg of Z times a day; for infections of severe course, the dose is increased to 1500 mg and administered 3-4 times a day (if necessary, the interval between administrations can be reduced to 6 hours). The average daily dose is 3-6 g.

With bacterial meningitis - in / in; 3 g every 8 hours.

When pneumonia - in / m or / in, 1,500 mg 2-3 times a day for 48-72 h, then go to the inside, 500 mg 2 times a day for 7-10 days.

When exacerbation of chronic bronchitis is prescribed in / m or IV, 750 mg 2-3 times a day in for 48-72 hours, then go to the inside, 500 mg twice a day for 5-10 days.

With gonorrhea - in / m, 1500 mg, once (or as 2 injections of 750 mg with the introduction into different areas, for example, in both gluteal muscles).

Children appoint 30-100 mg / kg / day, the daily dose is divided by 3-4 in / in or in / m of administration. For the treatment of most infections, the optimal dose is 60 mg / kg / day.

Newborns and children under 3 months appoint 30 mg / kg / day, the daily dose is divided into 2-3 injections.

In bacterial meningitis - for children of younger and older age, 150-250 mg / kg / day, the daily dose is divided into 3-4 injections; newborns - 100 mg / kg / day.

Perioperative antibiotic prophylaxis: with operations on the abdominal cavity, pelvic organs and orthopedic operations - IV, 1500 mg together with premedication or introductory anesthesia, but not earlier than an hour before the operation; then additionally in / in or / m 750 mg at 8 and 16 h after the operation. At operations on heart, lungs, an esophagus and vessels - in / in, 1500 mg together with premedication or introductory anesthesia, but not earlier, than one hour prior to the beginning of operation; then IV or IV, 750 mg 3 times daily for the next 24-48 hours. When the joint is completely replaced (in addition to the IV), 1500 mg of the antibiotic powder is mixed dry with each polymer packet methyl methacrylate cement prior to the addition of the liquid monomer. In chronic renal failure (CRF) requires correction mode: the creatinine clearance (CC) of 10-20 ml / min administered in / in or / m to 750 mg 2 times a day, with CC than 10 ml / min - 750 mg once a day. Patients on continuous hemodialysis using an arteriovenous shunt or high-speed haemofiltration in intensive care units are prescribed 750 mg twice daily; for patients on low-velocity haemofiltration, doses recommended for renal impairment are prescribed.

Preparation of solution for injection:

Solution for IM injections:

In a bottle containing 750 mg of dry powder Cefuabral®, add 3 ml of solvent (sterile water for injection, 0.5-1% lidocaine hydrochloride solution). Gently shake until a slurry forms. Enter deeply intramuscularly in areas of the body with a pronounced muscular layer (upper-outer quadrant of the buttock or lateral surface of the thigh).

Solution for intravenous administration:

Dissolve:

- 750 mg of Cefuabral® in 5-6 or more ml of water for injection,

- 1500 mg of Cefuabral® in 15 or more ml of water for injection.

These solutions can be injected directly into the vein or through a special injection site or port for intravenous infusion systems if the patient receives parenterally-compatible fluids with Cefurabol®.

For short-term intravenous infusions (up to 30 minutes), 1500 mg of the drug is dissolved in 50 ml of water for injection or another compatible fluid for infusion.

When mixing a solution of Cefuabral® (1500 mg in 15 ml of water for injection) and metronidazole (50 mg / 100 ml), both components remain active.

Cefuabral® solutions prepared with water for injection can be stored for 24 hours at room temperature. Cefuabral® is compatible with the most commonly used liquid for intravenous administration.The drug is stable up to 24 hours at room temperature when mixed with the following solutions: 0.9% sodium chloride solution, 5% dextrose solution, 10% dextrose solution, Ringer's solution, Hartman's solution. It is allowed to use a yellow solution during storage. The stability of the drug Cefurabol® in a 0.9% solution of sodium chloride and in a 5% solution of dextrose is not impaired in the presence of hydrocortazone sodium phosphate. Cefuabral® is compatible with heparin (10 U / ml and 50 U / ml) in a 0.9% solution of sodium chloride; potassium chloride (10 mEq / L and 40 mEq / L) in a 0.9% solution of sodium chloride. Cefuabral® should not be mixed in the same syringe with antibiotics from the aminoglycoside group. A solution of sodium hydrogencarbonate 2.74% has a pH that significantly affects the color of the solution of the drug Cefurabol ®, so it is not recommended to use it for breeding. However, if a sodium bicarbonate solution is administered to the patient, then, if necessary, can be injected directly into the tube of the infusion system.

Side effects:

Allergic reactions: chills, rash, itching, urticaria, multiforme exudative erythema (including Stevens-Johnson syndrome), bronchospasm, malignant exudative erythema, toxic epidermal necrolysis, vasculitis, anaphylactic shock.

From the digestive system: diarrhea or constipation, nausea, vomiting, flatulence, spasms and abdominal pain, ulceration of the oral mucosa, candidiasis of the oral cavity, glossitis, pseudomembranous colitis, impaired hepatic function (increased activity of aspartate aminotransferase, alanine aminotransferase, lactate dehydrogenase, alkaline phosphatase, bilirubin concentration) cholestasis.

From the genitourinary system: impaired renal function (decreased creatinine clearance, increased creatinine and residual urea nitrogen in the blood), interstitial nephritis, dysuria, pruritus, and vaginitis.

From the hematopoiesis: reduction of hemoglobin and hematocrit, anemia (aplastic or hemolytic), eosinophilia, neutropenia, leukopenia, agranulocytosis, thrombocytopenia, hypoprothrombinemia, prolongation of prothrombin time.

Local reactions: irritation, infiltration and pain at the injection site, phlebitis.

From the central nervous system: convulsions.

From the sense organs: hearing loss.

Overdose:

Symptoms: CNS excitation, convulsions.

Treatment: the appointment of antiepileptic drugs, control and maintenance of vital body functions, hemodialysis and peritoneal dialysis.

Interaction:

Simultaneous oral administration of "loop" diuretics slows tubular secretion, reduces renal clearance, increases plasma concentration and increases T1 / 2 cefuroxime.

When used simultaneously with aminoglycosides and diuretics, the risk of nephrotoxic effects increases.

Pharmaceutically compatible with metronidazole, azlocillin, xylitol, with aqueous solutions containing up to 1% lidocaine hydrochloride; 0.9% solution of sodium chloride, 5% and 10% solutions of dextrose, an aqueous solution containing 0.18% sodium chloride and 4% dextrose, an aqueous solution containing 5% dextrose and 0.9% sodium chloride, an aqueous solution containing 5% dextrose; and 0.45% sodium chloride, Ringer's solution, Hartman's solution, sodium lactate solution, heparin (10 U / ml and 50 U / ml) in a 0.9% solution of sodium chloride.

Pharmaceutically incompatible with aminoglycosides, sodium bicarbonate solution.

Special instructions:

Patients who had a history of allergic reactions to penicillins, may have a hypersensitivity to cephalosporin antibiotics. In the process of treatment, control of kidney function is necessary, especially in patients receiving the drug in high doses.Treatment continues for 48-72 hours after the disappearance of symptoms, in the case of infections caused by Streptoccocus pyogenes, treatment course - at least 7-10 days.

During treatment, a false positive Coombs reaction and a false positive urine reaction to glucose are possible.

In patients receiving cefurabol ®, at a certain concentration of glucose in the blood, it is recommended to use tests with glucose oxidase or hexokinase. Against the background of treatment of meningitis in children, hearing loss is possible.

When switching from parenteral administration to ingestion, the severity of the infection, the sensitivity of microorganisms and the general condition of the patient should be taken into account. If 72 hours after taking cefuroxime inside, there is no improvement, it is necessary to continue parenteral administration.

Effect on the ability to drive transp. cf. and fur:Studies on the effect of Cefuabral® on the performance of potentially hazardous activities requiring special attention and rapidity of reactions have not been conducted. Given the potential for side effects from the nervous system and sensory organs, when using Cefuabral®, care must be taken when driving vehicles and when engaging in other potentially hazardous activities,requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Powder for the preparation of solution for intravenous and intramuscular administration of 750 mg and 1500 mg.

Packaging:

750 mg of active substance into glass bottles with a capacity of 10 ml, 1500 mg of active substance into 20 ml glass vials, hermetically sealed with rubber stoppers, crimped with aluminum caps or crimped caps combined (aluminum with safety plastic caps).

1.1 a vial of the preparation and instruction for use is placed in a pack of cardboard.

For a dosage of 750 mg:

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

1.1 a bottle of the drug and 1 ampoule are packed in a cardboard pack. In the pack insert instruction for use.

2. 1 bottle of preparation and 1 ampoule with solvent are packed in a contour mesh box made of polyvinylchloride film and foil of aluminum lacquered or without foil. One contour mesh package and instructions for use are put in a pack of cardboard.

3.5 bottles with the preparation are packed in contour mesh packages from polyvinyl chloride film and foil of aluminum lacquered or without foil.One contour mesh package and instructions for use are put in a pack of cardboard.

4. 5 bottles with the preparation complete with 5 ampoules of the solvent are packed in contoured cell packs made of polyvinylchloride film and foil of aluminum lacquered or without foil. One contour mesh package with the preparation, one contour mesh 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 N000129 / 01

Date of registration:01.02.2012

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

Manufacturer: & nbsp

PREBAND PFC LLC Russia

Information update date: & nbsp26.11.2015

Illustrated instructions

Instructions

Cefuabral® (Cefurabol®)