Overview
Cefoperazone is active in vitro and in the treatment of clinical infections against gram-positive aerobes: Staphylococcus aureus (non-producing and producing penicillinase strains), Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes (beta-hemolytic streptococcus streptococcus group A) B), Enterococcus (Streptococcus faecalis, S.faecium, S.durans), gram-negative aerobes: Escherichia coli, Klebsiella spp. (including Klebsiella pneumoniae), Enterobacter spp., Citrobacter spp., Haemophilus influenzae, Proteus mirabilis, Proteus vulgaris, Morganella morganii, Providencia stuartii, Providencia rettgeri, Serratia marcescens, Pseudomoneronas aeruginosa, Pseudoceromonas aeruginosa, Pseudoceromonasonugeronas aeruginosa, Pseudoceromonas aeruginosa, Active against anaerobic organisms, including: gram-positive cocci (including Peptococcus and Peptostreptococcus), Clostridium spp., Bacteroides fragilis, other Bacteroides spp.).
Cefoperazone also exhibits in vitro activity against Salmonella spp., Shigella spp., Serratia liquefaciens, Neisseria meningitidis, Bordetella pertussis, Yersinia enterocolitica, Clostridium difficile, Fusobacterium spp., Ebacterium spp., Beta-laeridae. Cefoperazone is stable against broad-spectrum plasmid beta-lactamases (TEM − 1,2, SHV − 1), however, it is destroyed by the action of extended-spectrum enzymes (TEM − 3–2, SHV − 2–5).
After a single dose of cefoperazone was administered, high concentrations of the substance were observed in blood serum and bile. One hour after a single 15-minute iv infusion of cefoperazone at a constant rate of 1, 2, 3, or 4 g, the serum concentrations of cefoperazone were 73, 114, 142, and 251 μg / ml. After a single i / m injection at a dose of 1 and 2 g Tmax was 1 h; serum cefoperazone concentrations were Benzone and 93 μg / ml. The maximum concentrations of cefoperazone in bile were observed 1-3 hours after administration and exceeded those in serum by about 100 times. Cefoperazone biliary concentrations ranged from 66 μg / ml after 30 minutes to more than 6000 μg / ml 3 hours after an intravenous bolus injection of 2 g.
After a 15-minute infusion of 2 g, the concentration in the urine was more than 2200 mcg / ml. Twelve hours after a single intravenous or intravenous administration of cefoperazone in the urine, 20–30% of the substance was determined. After a / m injection of 2 g Cmax in urine was almost 1000 mcg / ml. T1/2 cefoperazone from Benzone blood - about 2 hours (does not depend on the route of administration - IM or IV). C parametersmax, AUC and T1/2 from serum in patients with severe renal impairment did not differ from those in normal volunteers. With impaired liver function T1/2 cefoperazone from serum is prolonged (up to 3–7 hours) and urinary excretion increases. With simultaneous renal / hepatic insufficiency, cumulation of cefoperazone in serum is possible. In newborns with low body weight T1/2 cefoperazone from serum - 6-10 hours; in children aged about 1 month - 4-6 hours; in infants and children aged 2 months to 2 years - 2.2 hours. Cefoperazone binds to plasma proteins (82–93%). Despite the high serum content of cefoperazone, it practically does not penetrate into the cerebrospinal fluid, accumulates in antibacterial concentrations in ascites, amniotic and peritoneal fluids, urine, sputum, lungs, palatine tonsils, mucous membrane of the sinuses, myocardium, genitals, bones, etc. Clinical in bile reaches very high values. It is removed mainly with bile (70–80%).
Application
Bacterial infections of the upper and lower respiratory tract; pneumonia, including nosocomial; urinary tract infections (including gonococcal urethritis) and genitals (endometritis), skin and soft tissues, bones and joints, intraabdominal infections (peritonitis, cholecystitis, cholangitis), septicemia, sepsis, meningitis, gonorrhea; prevention of infectious postoperative complications after abdominal, gynecological and orthopedic operations, as well as in cardiovascular surgery.
Pseudomonas aeruginosa infections.
Cefoperazone: Contraindications
Hypersensitivity, including to other cephalosporins; renal and / or liver failure.
Pregnancy and lactation
According to indications, taking necessary precautions.
Cefoperazone: Side Effects
From the cardiovascular system and blood (hematopoiesis, hemostasis): reversible neutropenia, hypocoagulation (due to hypoprothrombinemia), increased PV, anemia, decreased hemoglobin and hematocrit, unusual bleeding or hemorrhage.
From the digestive tract: nausea, vomiting, diarrhea, pseudomembranous colitis.
Other: vitamin K deficiency, probably due to suppression of intestinal flora, impaired renal function, increased activity of hepatic transaminases and alkaline phosphatase, hypercreatininemia; local reactions - pain at the injection site (with i / m administration), phlebitis (with i / v administration).
Interaction
Perhaps the use of cefoperazone in combination therapy with other antibiotics. Increases antimicrobial effect and nephrotoxicity of aminoglycosides; cefoperazone is pharmaceutically incompatible with aminoglycosides (if necessary, concomitant use is prescribed as a sequential medical iv administration using two separate iv catheters, cefoperazone is administered first).
Does not interact with probenecid. Enhances the effect of open. With the simultaneous use of cefoperazone with drugs that reduce platelet aggregation (NSAIDs, salicylates), the risk of bleeding increases. Drugs that reduce tubular secretion slow down the elimination of cefoperazone and increase its level in the blood. With the interaction of cefoperazone with alcohol, a teturam-like reaction is possible.
Cefoperazone: Dosage and Administration
Children: 100-150 mg / kg / day, the dose of cefoperazone is divided into 2-3 injections.
Adults: 2–4 g / day; the dose of cefoperazone related link divided into 2–3 administrations; maximum dose of 12 g / day. When pseudomonas infections are administered 4 times Benzone day.
Precautions
Alcohol intake excluded during treatment with cefoperazone.
In case of vitamin K deficiency (most likely in patients with malnutrition, malabsorption, for example, cystic fibrosis, alcoholism, and prolonged parenteral nutrition), the determination of PV and, if necessary, the administration of vitamin K are necessary. A false positive reaction to glucose in the urine may occur. and positive reaction in the Coombs test.
Cefoperazone is used with caution if there is a history of allergic reactions, especially to penicillin.
