Fortum, 500 mg

Fortum is a III generation cephalosporin antibiotic. It has a bactericidal effect by disrupting the synthesis of the cell wall of microorganisms. It has a wide range of antimicrobial action (including strains of pathogens resistant to gentamicin and other aminoglycoside antibiotics). It is resistant to the action of most β-lactamases.

In in vitro studies, ceftazidime has been shown to be active against:

– Gram-negative bacteria: Pseudomonas aeruginosa, Pseudomonas spp. (including Pseudomonas pseudomallei), Klebsiella spp. (including Klebsiella pneumoniae), Proteus mirabilis, Proteus vulgaris, Morganella morganii, Proteus rettgeri, Providencia spp, Escherichia coli, Enterobacter spp., Citrobacter spp., Serratia spp., Salmonella spp., Shigella spp., Yersinia enterocolitica, Pasteurella multocida, Acinetobacter spp, Neisseria gonorrhoeae, Neisseria meningitidis, Haemophilus influenzae (including ampicillin-resistant strains), Haemophilus parainfluenzae (including ampicillin-resistant strains);

– Gram-positive bacteria: Staphylococcus aureus (strains sensitive to methicillin), Staphylococcus epidermidis (strains sensitive to methicillin), Micrococcus spp., Streptococcus pyogenes (β-haemolytic Streptococcus group A), Streptococcus group B (Streptococcus agalactiae), Streptococcus pneumoniae, Streptococcus mitis, Streptococcus spp. (excluding Streptococcus faecalis);
– anaerobes: Peptococcus spp, Peptostreptococcus spp., Propionibacterium spp., Clostridium perfringers, Fusobacterium spp., Bacteroides spp. (many strains of Bacteroides fragilis are resistant).

Ceftazidime is not active against methicillin-resistant staphylococci, Streptococcus faecalis and many other Enterococcus spp., Listeria monocytogenes, Campylobacter spp., Clostridium difficile.

Pharmacokinetics:

Absorption
After the drug is administered in doses of 500 mg and 1 g in the m/m, Cmax in blood plasma is reached quickly and is 18 mg/L and 37 mg/L, respectively. In 5 min after intravenous bolus administration of the drug in doses of 500 mg, 1 g or 2 g, plasma concentrations of ceftazidime are 46 mg/l, 87 mg/l and 170 mg/l, respectively.

Distribution
After intravenous or intravenous administration, therapeutic concentrations of the active substance in plasma persist for 8-12 hours. Binding to plasma proteins is 10%.

Concentrations of ceftazidime exceeding MPC for most common pathogens can be achieved in bone tissue, heart tissue, bile, sputum, synovial fluid, intraocular fluid, pleural and peritoneal fluid. Ceftazidime easily penetrates through the placental barrier and is excreted with breast milk. In the absence of inflammatory process in meningeal membranes ceftazidime poorly penetrates through the BBB, concentration of the drug in cerebrospinal fluid (CSF) is low. In meningitis in the CSF therapeutic concentrations of ceftazidime of 4-20 mg/l and higher are achieved.

Metabolism
Ceftazidime is not metabolized in the body.

Excretion
T1/2 is about 2 h. Ceftazidime is excreted unchanged in the urine by glomerular filtration. About 80-90% of the dose is excreted with the urine within 24 hours. Less than 1% of the drug is excreted with bile.

Pharmacokinetics in special clinical cases

The excretion rate of ceftazidime is decreased in renal dysfunction.
In hemodialysis the T1/2 is 3-5 h.
In neonates the T1/2 is 3-4 times greater than in adults.

Indications

Prevention of infectious complications during prostate surgery (transurethral resection).

Active ingredient

Composition

Active ingredient:

Cephthasidime (in pentahydrate form) 500 mg.

Auxiliary substances:

Sodium carbonate (anhydrous),

Carbon dioxide.

How to take, the dosage

Iv or IM deep into the upper outer quadrant of the greater gluteal muscle or the lateral thigh.

The ceftazidime solution can be injected directly into a vein or into a tube of an infusion system.

The dose of the drug is determined individually depending on the severity of the disease, localization, type of the causative agent and its sensitivity to the drug as well as the patient’s age and renal function.

The maximum daily dose is 6 g.

Interaction

The simultaneous administration of ceftazidime in high doses and nephrotoxic drugs may have adverse effects on renal function.

“Loop” diuretics, aminoglycosides, vancomycin , clindamycin decrease clearance of ceftazidime, resulting in an increased risk of nephrotoxic effects.

The bacteriostatic antibiotics (including chloramphenicol ) reduce the effect of beta-lactam antibiotics.

Special Instructions

In case of allergic reaction to ceftazidime the drug should be withdrawn immediately, in severe cases adrenaline, hydrocortisone, antihistamines and other emergency measures may be required. When concomitant administration of cephalosporins in high dose with nephrotoxic drugs such as aminoglycosides and diuretics (furosemide), renal function should be monitored.

Because ceftazidime is excreted through the kidneys, in patients with renal impairment its dose should be reduced according to the degree of renal impairment. Prolonged use of broad-spectrum antibiotics, including ceftazidime, may lead to increased growth of insensitive microorganisms (e.g. Candida, Enterococci), and discontinuation of treatment or appropriate therapy may be required.

The patient’s condition must be constantly evaluated during treatment. Some initially sensitive strains of Enterobacter and Serratia may develop resistance when treated with ceftazidime; therefore, periodic antibiotic sensitivity testing should be performed when treating infections caused by these microorganisms.

Ceftazidime has no effect on the results of glucose determination in urine by enzymatic methods, but may have a weak effect on the results of methods based on copper reduction (Benedict, Fehling, Clinitest). Ceftazidime does not affect the quantitative determination of creatinine by the alkaline-picrine method (Jaffe method).

Contraindications

Hypersensitivity to the ingredients of the drug.

Side effects

Local reactions: phlebitis or thrombophlebitis when Fortum is injected intravenously; pain, burning, thickening at the injection site when injected intravenously.

Hypersensitivity reactions: patchy-papular rash, urticaria, fever, pruritus, angioedema, bronchospasm, decreased BP, exudative erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome).

Gastrointestinal disorders: diarrhea, nausea, vomiting, abdominal pain; oropharyngeal candidiasis, colitis. As with other cephalosporins, colitis may be caused by Clostridium difficile and appear as pseudomembranous colitis.

Urogenital system disorders: candidiasis vaginitis, impaired renal function.

Hepatobiliary system and pancreatic disorders: very rare – jaundice.

CNS disorders: headache, dizziness, paresthesias, taste disorders. In patients with renal failure more often than in other patients neurological disorders are noted, including tremor, myoclonia, convulsions, encephalopathy, coma.

Laboratory parameters: eosinophilia, false positive direct Coombs reaction, thrombocytosis, increased activity of liver enzymes – ALT, AST, LDH, gamma-glutamyl transpeptidase and ALP. Sometimes there is a transient increase in blood levels of urea, urea nitrogen and/or creatinine.

Hematopoietic organs: leukopenia, neutropenia, agranulocytosis, thrombocytopenia, lymphocytosis, hemolytic anemia.

Overdose

Symptoms: neurological disorders (including encephalopathy, seizures, Coma ).

Treatment: symptomatic and supportive therapy. Serum ceftazidime concentration may be decreased with hemodialysis or peritoneal dialysis.

Pregnancy use

With caution.

Similarities