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Pharmacological properties

the bactericidal effect of the hepataceph drug is due to a slowdown in the synthesis of the bacterial cell wall.

Hepacef is active in vitro with a relatively large number of clinically significant microorganisms. At the same time, it is resistant to many beta-lactamases.

The following microorganisms are sensitive to cefoperazone.

Gram-positive microorganisms: Staphylococcus aureus (strains producing and not producing penicillinase), Staphylococcus epidermidis, Streptococcus pneumoniae (formerly Diplococcus pneumoniae), Streptococcus pyogenes (β-hemolytic streptococcus group A), Streptococcus bactococcus streptococcus Streptococcus streptococcus streptococcus Streptococcus β, hemococcus streptococcus group, Streptococcus streptococcus group Streptococcus faecalis (enterococcus), β-hemolytic streptococcus.

Gram-negative organisms: Escherichia coli, genus Klebsiella, genus Enterobacter, genus Citrobacter, Haemophilus influenzae, Proteus mirabilis, Proteus vulgaris, Morganella morganii (formerly Proteus morganii), Providencia rettgeri (formerly Proteus rettgeri), genus Providenciensa ), the genus Salmonella and Shigella, Pseudomonas aeruginosa and some other Pseudomonas, Acinetobacter calcoaceticus, Neisseria gonorrhoeae (strains producing and not producing β-lactamases), Neisseria meningitidis, Bordetella pertussis, Yersinia enterocolitica.

Anaerobic microorganisms: gram-positive and gram-negative cocci (including the genus Peptococcus, Peptostreptoccus and Velionella); gram-positive bacilli (including the genus Clostridium, Eubacterium and Lactobacillus); gram-negative bacilli (including the genus Fusobacterium, many strains of Bacteroides fragilis and other representatives of the genus Bacteroides).

Pharmacokinetics High levels in the blood, bile and urine are achieved after a single injection of the drug. In the table. 1 shows the concentration of the drug in the blood plasma of healthy adults. These data were obtained after a 15-minute iv injection of 1 g, or 2 g, or 3 g or 4 g of the drug, or a single i / m administration of 1 or 2 g of the drug. Probenecid does not affect the level of cefoperazone in the blood.

Table 1. Concentrations of cefoperazone in blood plasma
Average plasma concentrations, mcg / ml
Dose, route of administration 0* 30 minutes 1 hour 2 h 4 h 8 h 12 h
1g iv 153 114 73 38 16 4 0,5
2 g iv 252 153 114 70 32 8 2
3 g iv 340 210 142 89 41 9 2
4 g iv 506 325 251 161 71 19 6
1 g / m 32** 52 65 57 33 7 1
2 g / m 40** 69 93 97 58 14 4

* Time elapsed after administration of the drug (countdown immediately after the end of the infusion).

** Results obtained 15 minutes after drug administration.

T½ Hepatsef from plasma is about 2 hours, regardless of the method of administration.

Hepatsef reaches therapeutic levels in all body fluids and tissues that have been investigated. Among them there are ascitic and cerebrospinal (with meningitis) fluids, urine, bile and the wall of the gallbladder, sputum and lungs, palatine tonsils and mucous membranes of the sinuses, atria, kidneys, ureter, prostate gland, testes, uterus and fallopian tubes, bones, blood umbilical cord and amniotic fluid.

Hepaceph is excreted in the bile and urine. The concentration of the drug in bile reaches very high levels (usually 1-3 hours after injection) and exceeds similar plasma concentrations by 100 times.

Such concentrations in bile were recorded: from 66 μg / ml after 30 minutes to 6000 μg / ml 3 hours after iv administration of 2 g of the drug to patients without blockage of the bile ducts.

12 hours after administration in different doses and in different ways, an increase in the concentration of cefoperazone in the urine of patients with normal renal function reaches an average of 20-30%. The concentration of the drug in the urine of more than 2200 μg / ml was obtained 15 minutes after iv administration of 2 g of the drug Hepacef. After i / m administration of 2 g of drug Cmax in urine was about 1000 mcg / ml.

Repeated administration of the drug Hepacef does not lead to cumulation of the drug in healthy volunteers.

In patients with impaired liver function T½ drug from blood plasma increases, but excretion in urine also increases. In patients with renal and hepatic insufficiency, Hepacef can accumulate in plasma.

In patients with renal failure Cmax in blood plasma, AUC, as well as T½ from blood plasma are the same as in healthy volunteers.

Indications

Treatment of infections caused by microorganisms sensitive to cefoperazone: upper and lower respiratory tract infections; upper and lower urinary tract; peritonitis, cholecystitis, cholangitis and other intra-abdominal infections; septicemia; meningitis; infections of the skin and soft tissues; infections of bones and joints; pelvic inflammatory diseases, endometritis, gonorrhea and other genital tract infections.

Prevention Hepatsef can be prescribed for the prevention of postoperative complications in abdominal, gynecological, cardiovascular and orthopedic operations.

Application

The drug is intended for IV or IM use.

Before starting therapy with the drug, it is necessary to exclude the patients hypersensitivity to the antibiotic and lidocaine by conducting a skin test.

Adults Typically, the dose is 2–4 g / day, which should be administered every 12 hours in equal distributed doses. In especially severe infections, the dose can be increased to 8 g / day, which is administered every 12 hours in equal distributed doses. With the introduction of the drug Hepacef in a daily dose of 12-16 g, divided into 3 equal doses (with an interval of 8 hours), no complications were revealed. Treatment with the drug can be started before the results of a study of the sensitivity of microorganisms.

The recommended dose for uncomplicated gonococcal urethritis is 500 mg once a / m.

V / m introduction is deep

Tags: Cefoperazone