Cefurozine, 750 mg

Pharmacotherapeutic group

Cephalosporin antibiotic

ATX code: J01DC02

Pharmacodynamics:

A second generation cephalosporin antibiotic for parenteral use. It has a bactericidal effect (disrupts the synthesis of the bacterial cell wall).

Highly active against Gram-positive microorganisms (Staphylococcus aureus Staphylococcus epidermidis including strains resistant to penicillins and except for strains resistant to methicillin Streptococcus pyogenes and others). beta-haemolytic Streptococcus pneumoniae Streptococcus group B (Streptococcus agalactiae) Streptococcus mitis (viridans group) Bordetella pertussis most Clostridium spp.) Gram-negative microorganisms (Escherichia coli Klebsiella spp. Proteus mirabilis Providencia spp. Proteus rettgeri Haemophilus influenzae including ampicillin resistant strains Haemophilus parainfluenzae including ampicillin resistant strains Moraxella (Branhamella) catarrhalis Neisseria gonorrhoeae including penicillinase producing and non-producing strains Neisseria meningitidis Salmonella spp. Bacteroides spp. Fusobacterium spp. Propionibacterium spp. Borrelia burgdorferi) Gram-positive and Gram-negative anaerobes (including Peptococcus spp. and Peptostreptococcus spp.).

The following are not sensitive to cefuroxime: Clostridium difficile Pseudomonas spp. Campylobacter spp. Acinetobacter calcoaceticus Listeria monocytogenes methicillin-resistant strains of Staphylococcus aureus methicillin-resistant strains of Staphylococcus epidermidis Legionella spp. Streptococcus (Enterococcus) faecalis Morganella morganii Proteus vulgaris Enterobacter spp. Citrobacter spp. Serratia spp. Bacteroides fragilis.
Pharmacokinetics: Parenteral administration: After intravenous administration of 750 mg the maximum concentration is reached after 15-60 min and is 27 µg/ml. With intravenous administration of 750 mg and 1.5 g, the maximum concentration after 15 min is 50 and 100 µg/ml, respectively. Therapeutical concentration is retained for 5.3 and 8 hours respectively.

Half-life after injection is 80 minutes; it is 3-5 times longer in newborn children.

Plasma protein binding is 33-50%. It is not metabolized in the liver.

It is excreted by kidneys via glomerular filtration and tubule secretion 85-90% unchanged during 8 hours (the most part of the preparation is excreted during first 6 hours, thus creating high concentrations in the urine); in 24 hours it is eliminated completely (50% – by glomerular secretion, 50% – by tubule filtration).

Therapeutic concentrations are registered in pleural fluid bile sputum myocardium skin and soft tissues. Concentrations of cefuroxime exceeding the minimum suppressive concentration for most common microorganisms can be achieved in bone tissue synovial fluid and intraocular fluid. In meningitis penetrates the blood-brain barrier. Passes through the placenta and penetrates into breast milk.

Indications

Treatment of infections caused by susceptible strains of microorganisms in the following diseases:

– Lower respiratory tract infections (pneumonia caused by Streptococcus pneumoniae, Haemophilus influenzae, including ampicillin-resistant strains, Klebsiella species, Staphylococcus aureus, including ampicillin-resistant strains (but not methicillin-resistant), Streptococcus pyogenes and Escherichia coli);

– urinary tract infections caused by Escherichia coli and Klebsiella species;

– soft tissue infections caused by Staphylococcus aureus, including ampicillin-resistant strains (but not methicillin-resistant), Streptococcus pyogenes, Escherichia coli and Klebsiella species;

– meningitis caused by Staphylococcus aureus, including ampicillin-resistant (but not methicillin-resistant) strains, Streptococcus pneumoniae, Haemophilus influenzae and Neisseria meningitidis;

– gonorrhea caused by Neisseria gonorrhoeae, including ampicillin-resistant strains;

– bone and joint infections caused by Staphylococcus aureus (penicillinase-producing and non-producing strains).

Preoperative prophylactic administration of cefuroxime may prevent the growth of susceptible pathogenic bacteria and thus reduce the incidence of certain postoperative infections in patients undergoing surgical procedures (e.g., vaginal hysterectomy) that are classified as contaminated or potentially contaminated; in patients undergoing open heart surgery, in whom surgical site infections are a serious risk. If signs of infection occur after surgery, culture specimens should be obtained to identify the pathogen and appropriate antimicrobial therapy should be administered.

Active ingredient

Composition

How to take, the dosage

Interaction

The concomitant use of aminoglycosides and some cephalosporins causes nephrotoxicity. Although transient increase in serum urea nitrogen and creatinine levels has been observed in clinical trials, there is no evidence that cefuroxime has significant nephrotoxicity when used alone.

The concomitant use of strong diuretics, such as furosemide and etacrynic acid, may increase the risk of renal adverse events with cephalosporins.

Special Instructions

Contraindications

Side effects

The following adverse reactions have been observed during the use of cefuroxime.

Hypersensitivity reactions: rash and eosinophilia. Anaphylaxis, urticaria, pruritus and drug-induced fever have also been observed with cephalosporins. There are rare reports about the development of erythema multiforme, Stevens-Johnson syndrome and toxic epidermal necrolysis (exanthematous necrolysis).

Local reactions: thrombophlebitis, stiffness at the injection site and inflammatory reactions at the injection site; varying degrees of soreness have been reported following an intravenous injection using water as a diluent.

With blood: increased sedimentation rate and decreased Hb levels, eosinophilia, leukopenia and neutropenia; some patients had a positive Coombs direct test.

Urogenital system disorders: increase in serum urea nitrogen and creatinine.

Liver disorders: temporary increase in serum bilirubin, transaminases and alkaline phosphatase.

Others: drowsiness, liquid stools, weakness, sweating, palpitations and candida intertrigo.

Overdose

Symptoms: cefuroxime overdose may cause brain damage leading to seizures.

Treatment: general supportive treatment; specific antidote is unknown. Excess serum cefuroxime levels can be reduced with dialysis.

Pregnancy use

The safety of cefuroxime during pregnancy has not been established. The use of cefuroxime in pregnant women requires that the potential benefit of its use be weighed against the possible risk to the mother and fetus. Animal studies have shown that cefuroxime affects fetal bone calcification and exhibits maternal toxicity in rabbits.

Cefuroxime is excreted with human breast milk at low concentrations (0.5 mg/L). The clinical significance of this is unknown, so caution should be exercised when using cefuroxime in breastfeeding.

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