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

Has bactericidal action due to inhibition of bacterial cell wall synthesis. Violates synthesis biopolymer peptidoglycan - the main component of the bacterial cell wall. 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.

Sulbactam

It has no clinically significant effect, but, having a β-lactam structure associated with penicillins, competitively inhibits β-lactamase, preventing the inactivation of cefoperazone and expanding its spectrum of activity. It shows bactericidal activity against Neisseriaceae and Acinetobacter.

Pharmacokinetics:

Cefoperazone

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%.

It penetrates into all organs and tissues, is contained in therapeutic concentration in peritoneal and ascitic fluid, cerebrospinal fluid (with meningitis), in urine, bile and gallbladder wall, in sputum and lungs, palatine tonsils and mucous membrane of sinuses, kidneys, ureters, prostate gland, 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.

Sulbactam

After intravenous administration, the maximum concentration in the blood plasma is reached after 1 hour. The connection with plasma proteins is 25%. It penetrates the placental barrier and enters the breast milk.

Metabolism in the liver.

The elimination half-life is 64 minutes. Elimination by the kidneys.

The drug is removed during hemodialysis.

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.A39 Meningococcal infection

I.A30-A49.A40 Streptococcal septicemia

I.A30-A49.A41 Other septicemia

VI.G00-G09.G00 Bacterial meningitis, not elsewhere classified

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

X.J00-J06.J02 Acute pharyngitis

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

X.J30-J39.J32 Chronic Sinusitis

X.J30-J39.J35.0 Chronic tonsillitis

X.J30-J39.J37 Chronic laryngitis and laryngotracheitis

X.J40-J47.J42 Chronic bronchitis, unspecified

XI.K65-K67.K65.0 Acute peritonitis

XI.K80-K87.K81.0 Acute cholecystitis

XI.K80-K87.K81.1 Chronic 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.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.N72 Inflammatory disease of the cervix

XIV.N70-N77.N71.9 Inflammatory disease of uterus, unspecified

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

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

Contraindications:

Individual intolerance to β-lactam antibiotics: penicillins and cephalosporins.

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, every 6-12 hours for 20-80 mg / kg per day. In severe cases, the administration of 160 mg / kg per day is permissible, the dose should be divided into 2-4 equal parts.

For newborns, the maximum dose is 80 mg / kg per day.

Adults

Intramuscularly in a 2% solution of lidocaine or intravenously, 2 grams every 12 hours. In severe cases, the dose may be doubled, up to 8 g for two doses.

The highest daily dose: 8 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: 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 + Sulbactam (Cefoperazonum + Sulbactamum)