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

Has bactericidal action due to inhibition of bacterial cell wall synthesis. Violates the synthesis of the biopolymer peptidoglikana - the main component of the cell wall of bacteria. It inhibits the peptidoglycan transpeptidase, inhibits the activity of the endogenous inhibitor, which leads to activation of murein hydrolase, which cleaves peptidoglycan.Effective against fissile bacteria, in the walls of which the synthesis of peptidoglycan occurs.

It is active against gram-positive microorganisms: Staphylococcus aureus (strains producing and not producing penicillinase), Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes (β-hemolytic streptococci of group A), Streptococcus agalactiae (β-hemolytic streptococcus group B) and other strains of β-hemolytic streptococci, many strains Streptococcus faecalis; against gram-negative microorganisms: Escherichia coli, Klebsiella spp., Enterobacter spp., Citrobacter spp., Haemophilus influenzae (strains producing and not producing β-lactamase), Proteus mirabilis, Proteus vulgaris, Morganella morganii, Providencia spp. (including P. rettgeri), Serratia spp. (including S. marcescens), Salmonella spp., Shigella spp., Pseudomonas aeruginosa and some other strains Pseudomonas, some strains Acinetobacter calcoaceticus, Neisseria gonorrhoeae, (strains producing and not producing β-lactamase), Neisseria meningitidis, Bordetella pertussis, Yersinia enterocolitica.

Effective also for anaerobic microorganisms, including Peptococcus spp., Peptostreptococcus spp., Veillonella spp., Clostridium spp., Lactobacillus spp., Fusobacterium spp., Bacteroides fragilis and other representatives of the genus Bacteroides.

Resistant to the action of β-lactamases.

Pharmacokinetics:

After intramuscular injection, the maximum concentration in the blood plasma is reached after 2 hours, after intravenous administration - after 1 hour. The connection with plasma proteins is 82-93%.

Penetrates into all organs and tissues,is contained in the therapeutic concentration in the peritoneal and ascitic fluid, cerebrospinal fluid (with meningitis), in the urine, bile and gallbladder wall, in sputum and lungs, palatine tonsils and sinus mucosa, kidneys, ureters, prostate, testicles, uterus and fallopian tubes, bones, cord blood and amniotic fluid.

Not exposed to metabolism. Do not cumulate. Penetrates through the placental barrier, is found in breast milk.

The elimination half-life is 2 hours. Elimination by the kidneys.

Indications:

It is used for treatment infectious diseases caused by susceptible to cefoperazone pathogens: respiratory infections, urinary tract infections, peritonitis, cholecystitis, cholangitis, endometritis, gonorrhea, meningitis, septicemia, infections of bones, joints, skin and soft tissues.

Used to prevent infectious complications in the postoperative period.

ICD-10

I.A30-A49.A40 Streptococcal septicemia

I.A30-A49.A41 Other septicemia

X.J00-J06.J00 Acute nasopharyngitis (runny nose)

X.J30-J39.J31.1 Chronic nasopharyngitis

X.J30-J39.J31 Chronic rhinitis, nasopharyngitis and pharyngitis

X.J00-J06.J01 Acute Sinusitis

X.J30-J39.J32 Chronic Sinusitis

X.J30-J39.J31.2 Chronic pharyngitis

X.J00-J06.J02 Acute pharyngitis

X.J30-J39.J35.0 Chronic tonsillitis

X.J00-J06.J03 Acute tonsillitis

X.J00-J06.J04 Acute laryngitis and tracheitis

X.J10-J18.J15 Bacterial pneumonia, not elsewhere classified

X.J20-J22.J20 Acute bronchitis

X.J40-J47.J42 Chronic bronchitis, unspecified

XI.K65-K67.K65.0 Acute peritonitis

XI.K80-K87.K81.1 Chronic cholecystitis

XI.K80-K87.K81.0 Acute cholecystitis

XI.K80-K87.K83.0 Cholangitis

XII.L00-L08.L01 Impetigo

XII.L00-L08.L02 Abscess of skin, boil and carbuncle

XII.L00-L08.L03 Phlegmon

XII.L00-L08.L08.0 Pyoderma

XIII.M00-M03.M00 Pyogenic arthritis

XIII.M86-M90.M86 Osteomyelitis

XIV.N10-N16.N11 Chronic tubulointerstitial nephritis

XIV.N10-N16.N10 Acute tubulointerstitial nephritis

XIV.N30-N39.N30 Cystitis

XIV.N30-N39.N34 Urethritis and urethral syndrome

XIV.N40-N51.N41 Inflammatory diseases of the prostate

XIV.N70-N77.N70 Salpingitis and oophoritis

XIV.N70-N77.N71.0 Acute inflammatory disease of the uterus

XIV.N70-N77.N72 Inflammatory disease of the cervix

XIV.N70-N77.N73.0 Acute parametritis and pelvic cellulite

XXI.Z20-Z29.Z29.2 Another type of preventive chemotherapy

Contraindications:

Individual intolerance of β-lactam antibiotics: penicillins and cephalosporins, neonatal period.

Carefully:

Imbalance of electrolytes or fluids, severe liver damage, colitis in history.

Pregnancy and lactation:

Recommendations for FDA - Category B.It is used with caution during pregnancy and lactation in cases where the intended benefit exceeds the risk to the fetus and newborn.

Dosing and Administration:

Use in children

Intramuscularly and intravenously, 50-200 mg / kg for 2 injections every 12 hours. If necessary, the dose rises to 300 mg / kg of body weight.

Adults

Intravenously slow, intramuscularly deep 2-4 mg every 12 hours. In severe cases, the dose increases to 8 g for two doses. It is permissible to increase the dose to 12-16 g for 3-4 injections.

In uncomplicated gonococcal urethritis, a single-dose intramuscular injection of 0.5 g of cefoperazone is recommended.

The highest daily dose: 16 g.

The highest single dose: 4 g.

Side effects:

Central and peripheral nervous system: rarely - convulsions.

Hemopoietic system: thrombocytopenia, eosinophilia, leukopenia, an increase in prothrombin index and coagulation time.

Digestive system: nausea, vomiting, diarrhea, increased activity of hepatic enzymes, hepatic or cholestatic jaundice, intestinal dysbacteriosis.

Dermatological reactions: local reactions - compaction at the injection site, candidiasis dermatitis,vulvovaginitis.

urinary system: rarely - the development of hypokalemia.

Allergic reactions.

Overdose:

Nausea, vomiting, diarrhea, neuromuscular excitability, convulsive attacks.

Treatment is symptomatic, hemodialysis.

Interaction:

Simultaneous application with probenecid slows the renal excretion of cefoperazone.

"Loop diuretics" block the tubular secretion of cefoperazone.

Special instructions:

Cefoperazone is not recommended for the treatment of meningitis.

Simultaneous use with ethanol can cause a disulfiram-like reaction.

Instructions

Cefoperazone (Cefoperazonum)