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PubMed2003

Suitability of cefotiam and cefuroxime axetil for the perioperative short-term prophylaxis in tonsillectomy patients.

The efficacy of the perioperative short-term prophylaxis with cefotiam (CAS 66309-69-1) and cefuroxime axetil (CAS 64544-07-6) was analysed by the assessment of the pharmacological kinetics in the serum and the tonsil tissue in 50 patients with recurrent tonsillitis. Twenty-four patients received 1 g cefotiam by the intravenous route 30 min to 4 h before the tonsillectomy, and 26 patients received 250 mg cefuroxime axetil orally 1 to 6 h before the tonsillectomy. Bactericidal serum levels were reached for cefotiam up to 4 h after intravenous application and for cefuroxime axetil up to 3 h after oral application. In the tissue of the tonsil there were proved levels which were definitely above the MIC 90 (MIC = minimum inhibitory concentration) known for the clinically relevant germs for cefotiam after 30 min up to 2 h, for cefuroxime axetil after only 2 h. Considering the distribution areas, the capacity of the protein binding and the microbiological measuring methods, one can expect an efficient antibiotic coverage after an intravenous one-shot bolus injection of 1 g cefotiam from 30 min to 4 h and after oral application of 250 mg cefuroxime axetil on an empty stomach from 1 to 6 h. Because of the short duration of a tonsillectomy and the serum and tonsil tissue kinetics cefotiam and cefuroxime axetil are suitable for the perioperative antibiotic prophylaxis of high-risk patients.

Adolescent↗
PubMed1984

The activity of cefotiam on beta-lactamase-producing bacteria in an in-vitro model.

The activity of cefotiam was tested in an in-vitro model simulating human serum pharmacokinetics. Bacterial strains used for inoculation either produced a penicillinase or a cephalosporinase. The rate of hydrolysis and the MICs of cefotiam were determined in comparison with those of ampicillin and cephalothin. The influence of these beta-lactamases on the killing kinetics and the degradation of cefotiam in the in-vitro model were then measured. Although all beta-lactamases hydrolyzed cefotiam, only the chromosomal cephalosporinases, especially those from Enterobacter and Klebsiella, reduced the elimination of the bacteria by degradation of the drug. A rough correlation between the hydrolytic activity and MIC could be demonstrated for cefotiam but not for ampicillin, while a correlation between killing ability and MIC only existed for strains with cefotiam MICs higher than 16 mg/l.

Ampicillin↗
PubMed1980

Therapeutic effects of cefotiam and cefazolin on experimental pneumonia caused by Klebsiella pneumoniae DT-S in mice.

The efficacies of several dosage schedules, productive of plasma levels of cefotiam and cefazolin of short and long duration and starting at three levels of cefotiam and cefazolin of short and long duration and starting at three different times (3, 18, and 30h) after infection, were examined in experimental pneumonia caused by Klebsiella pneumoniae DT-S in mice. With each of the multiday regimens there was a large segment of the day when plasma levels fell below assayable concentrations. In all cases, cefotiam proved about eight times as active as cefazolin, indicating that the potent in vitro antibacterial activity of cefotiam was well reflected in the therapeutic effect in this model infection. As judged by the total dose administered, the regimen of cefotiam producing a low but sustained plasma level gave better therapeutic effects than that exhibiting a high but transient plasma level. The cefotiam levels in the plasma of mice that received the regimen effective when initiated at 18 h after infection were less than the expected levels in humans after intravenous infusion of the usual clinical dose.

Animals↗
PubMed1986

Biliary elimination of cefotiam, an experimental and clinical study.

Five isolated rabbit livers were in vitro perfused over a 3-hour period. After addition of 10 mg of cefotiam to the circulating blood, a biliary peak concentration of 76.2 +/- 14.2 micrograms/ml (mean +/- SEM) was reached between the 90th and 120th min; 3.1 +/- 0.4% of the dose given was excreted in the bile during the 3-hour period. In 10 recently cholecystectomized patients provided with a T-tube drain, 1 g of cefotiam was given intravenously. A biliary peak concentration of 340 +/- 81 micrograms/ml was observed 2 h later. 1.8 +/- 0.7% of the administered dose was recovered in the bile during the 12-hour period. In 5 clinically normal subjects given intravenously 1 g of cefotiam, 0.5 +/- 0.2% of the administered dose was found in the duodenal fluid aspirated over a 4-hour period. Cefotiam concentrations measured in choledochal and gallbladder bile collected simultaneously during operation 1 h after intravenous administration of 1 g of the drug to 10 patients were 502 +/- 102 micrograms/ml and 143 +/- 39 micrograms/ml, respectively; they exceeded significantly the concentration determined in the serum sampled at the same time (17.9 +/- 2.6 micrograms/ml). The biliary parameters of cefotiam were compared with those of 14 other beta-lactam antibiotics previously studied by the same procedure. The results of the present study are consistent with a possible beneficial effect of cefotiam in the treatment of biliary tract infections.

Animals↗
PubMed1982

[Concentration of cefotiam in the cerebrospinal fluid].

Cefotiam of 1 to 2 g was intravenously given during 15 to 60 minutes in 10 cases, and blood levels and cerebrospinal fluid (CSF) levels were studied. Following the drip infusion of cefotiam, maximum blood levels of 25.2 to 305 micrograms per ml was an average of 101.2 micrograms per ml were achieved at 15 to 60 minutes in 9 cases. Half life of cefotiam in serum was from 20 to 50 minutes, and mean time was 39.4 minutes. In contrast, maximum CSF levels of cefotiam were ranged 1.4 to 17.2 micrograms per ml and mean value was 5.7 micrograms per ml in 8 cases. The ratios of CSF levels to blood levels were calculated from 1.7 to 6.6% with an average of 4.6%. The CSF levels of cefotiam showed long delay and long decay. The period between the drip infusion and peak levels of cefotiam in CSF showed 60 to 420 minutes and mean time was 194 minutes. Half life varied between 45 and 270 minutes with an average of 178 minutes. No side effects were found in all cases.

Adult↗
PubMed1981

Nephrotoxicity of cefotiam (CGP 14221/E) in rats and rabbits.

Cefotiam (CGP 14221/E; SCE 963), a semisynthetic cephalosporin, was administered as a single dose by i.v. injection to rats l(up to 1.8 g/kg body-weight) and rabbits (up to 1.7 g/kg body-weight). Cephaloridine served as positive control (1.0 and 0.75 g/kg in rats; 0.3 and 0.28 g/kg in rabbits). The animals were sacrificed 24 h after injection and the kidneys preserved for routine histology and enzyme histochemistry (alkaline phosphatase, aminopeptidase, succinate dehydrogenase, esterase). Serum samples (Na+, K+, Cl-, urea, creatinine, LDH, alkaline phosphatase) and 24-h urine (Na+, K+, Cl-, urea, creatinine, protein, LDH, aminopeptidase) were analysed before and 24 h after injection. Minimal, irregularly scattered, degenerative changes in the proximal tubules which were not dose-dependent in degree were observed in rat kidneys following cefotiam injection. A slight dose-dependent degeneration in up to 50% of proximal tubular cells with loss of brush-border membrane enzyme activity was observed in rabbit kidneys. In both animal species the ability to concentrate urine was retained and urea and creatinine serum levels hardly affected. Following cefotiam injection a dose-dependent 4-fold excretion of urinary protein but not of LDH was observed in rabbits only. By contrast, cephaloridine caused extensive degeneration and necrosis in up to 90% of proximal tubular cells in both rats and rabbits, which was accompanied with formation of enzymically active hyaline casts, loss of urine-concentrating capacity of the kidney, elevated serum levels of urea and creatinine and an increased urinary excretion of LDH (60-fold in rats, 20-fold in rabbits) and protein (3-fold in rats, 10-fold in rabbits). Histochemistry and electron microscopy of rabbit kidneys suggested a loss of microvilli from proximal tubule cells by endocytosis and thus degeneration following injection of large doses of cefotiam, whereas cell disruption and necrosis prevailed after cephaloridine. The action of cefotiam on the proximal tubule cells is, therefore, not only quantitatively but possibly also qualitatively different from that of cephaloridine. Semiquantitative evaluation of tubular injuries in alkaline phosphatase-stained kidney sections and measurements of LDH and protein content in 24-h urine samples were advantageous in determining the quantity and the quality of nephrotoxic effects.

Animals↗
PubMedDate not supplied

Nephrotoxicity of cefotiam in rats.

Eight-week-old Wistar female rats were treated intramuscularly with 300, 1,000 and 3,000 mg/kg/day of cefotiam for five days. The nephrotoxicity of cefotiam was determined on the basis of the number of tubular epithelial cells excreted, the malate dehydrogenase activity in the urine and the histological examination of the kidneys. Cephalothin (3,000 mg/kg/day) was used as a reference compound. There were slight increases in the number of tubular epithelial cells excreted and in the malate dehydrogenase activity in the urine of some animals receiving 3,000 mg/kg/day of cefotiam or cephalothin. All of these changes disappeared within a few days after the dosing period. The histological examination of the kidneys at the end of both the dosing (5 days) and the recovery (7 days) periods revealed no pathological changes indicating nephrotoxicity. It was concluded that the nephrotoxicity of cefotiam was comparable to that of cephalothin; the urinary changes in animals receiving the highest dose were considered to be an early sign of nephrotoxicity. The maximum non-toxic dose of cefotiam was 1,000 mg/kg/day under the present experimental conditions.

Animals↗
PubMed1985

Pharmacokinetics of cefotiam in humans.

After intravenous bolus injections of 0.5, 1, and 2 g of cefotiam to three healthy volunteers, the mean (+/- standard deviation) total plasma clearances measured for each dose were, respectively, 26.8 +/- 2.7, 22.8 +/- 0.8, and 17.8 +/- 0.9 liters/h; the terminal elimination half-lives were 54.0 +/- 0.1, 68 +/- 15, and 98 +/- 36 min; and the renal clearances were 16.0 +/- 2.9, 13.3 +/- 1.4, and 11.3 +/- 2.6 liters/h. The 24-h urinary recovery was independent of the dose and averaged 53% of the dose. After intramuscular administration of 1 g of cefotiam to three healthy volunteers, a mean (+/- standard deviation) peak concentration of 16.6 +/- 5.1 micrograms/ml was reached at 0.75 to 1 h post dosing. The concurrent intramuscular administration of lidocaine and cefotiam did not modify the kinetics of cefotiam. During a constant-rate infusion, the steady-state plasma clearance decreased slightly when the infusion rate was increased. There was no trend towards accumulation of cefotiam in plasma during chronic treatment with 1 g intravenously every 12 h for 10 days.

Adult↗
PubMed1987

Comparative efficacy of cefotiam, cefmenoxime, and ceftriaxone in experimental endocarditis and correlation with pharmacokinetics and in vitro efficacy.

To determine the influence of in vitro activity, pharmacokinetic properties, and therapeutic regimen on the antibacterial effect in vivo, we compared three cephalosporins, cefotiam, cefmenoxime, and ceftriaxone, in a rabbit model of experimental Escherichia coli endocarditis after 4 days of treatment. The MBCs of cefotiam, cefmenoxime, and ceftriaxone for the E. coli strain were 0.5, 0.125, and 0.06 microgram/ml, respectively. Killing curves at 10 times the MBC were similar for the three cephalosporins. In serum, the elimination half-life of ceftriaxone was twice as much as the elimination half-life of cefotiam or cefmenoxime (2.8 +/- 0.45 versus 1.4 +/- 0.25 or 1.3 +/- 0.4 h, respectively). Ceftriaxone was much more effective than cefotiam. The bacterial titer in the vegetations (log10 CFU per gram of vegetation) was 7.56 +/- 1 with cefotiam and 2.41 +/- 2.6 with ceftriaxone, as their concentrations were 18 and 466 times higher, respectively, than their MBCs. Although ceftriaxone and cefmenoxime exhibited a similar rate of killing and percentage of protein binding, ceftriaxone was more effective than cefmenoxime at the same regimen of 15 mg/kg twice a day (3.08 +/- 1.1 versus 4.82 +/- 3.2 log10 CFU/g of vegetation). When antibiotic was given as a single daily injection of 30 mg/kg, the antibacterial effect persisted for ceftriaxone, but not for cefmenoxime. The longer elimination half-life and the higher local concentration/MBC ratio of ceftriaxone explained these results. The bacterial titer measured 24 h after the fourth injection of 30 mg of ceftriaxone per kg confirmed that this regimen prevented regrowth of bacteria. These results suggest that the local antibiotic level/MBC ratio roughly correlated with the antibacterial effect and could represent an adequate basis to explain the differences observed between the drugs in vivo. They also demonstrate that, provided that the dose is sufficient, a long-acting broad-spectrum cephalosporin may be effective in severe gram-negative infections, even when given at relatively long dosing intervals, in contrast with a rapidly cleared drug with the same intrinsic activity.

Animals↗
PubMed1981

Relevance of in vitro antibacterial activities of cefotiam and cefazolin to their therapeutic effects on experimental pneumonia caused by Klebsiella pneumoniae DT-S in mice.

The MICs of cefotiam and cefazolin against K. pneumoniae DT-S were unaffected by the inoculum size and were 0.1 and 1.56 micrograms/ml, respectively. Bactericidal and bacteriolytic activities of the cephalosporins were more potent in bacterial concentrations of 10(7) colony-forming units (CFU)/ml than in concentrations of 10(8) CFU/ml. Both activities of cefotiam were more markedly influenced by bacterial concentrations than those of cefazolin. Therapeutic activity of cefotiam was about 9 approximately 15 times as potent as that of cefazolin in experimental pneumonia caused by K. pneumoniae DT-S in mice, and this finding was in accordance with the ratio of in vitro antibacterial activities of the two cephalosporins as judged by the MICs or the bactericidal and bacteriolytic activities in bacterial suspension of 10(7) CFU/ml. The range of concentrations of cefotiam which induced cell filamentation in vitro, was wider than that of cefazolin. This difference, however, was not reflected on the therapeutic activities of the two cephalosporins in the model infection. In the pneumonic lungs, definite therapeutic doses of both cephalosporins (80 mg of cefotiam per kg and 640 mg of cefazolin per kg) produced mainly bacteriolysis of the challenge organisms.

Animals↗
PubMed1986

[Treatment of peritonitis due to continuous ambulatory peritoneal dialysis using a single daily intraperitoneal dose of 1g cefotiam].

Peritonitis remains the main complication of CAPD. This study demonstrates that most cases can be successfully treated with cefotiam. In 17 patients under CAPD, 33 cases of bacterial peritonitis were observed, with clinical manifestations in 28. The mean cell count in peritoneal dialysis fluid was 2 820/mm3, with 2 200/mm3 polymorphonuclear leukocytes. Causative pathogens were Staphylococcus in 18 cases, Streptococcus in 4, Stomatococcus mucilaginous in 1, Corynebacterium J.K. in 1, Enterobacter in 3, Acinetobacter in 3 and Pseudomonas in 2. Two cultures were negative. First choice treatment was a daily intraperitoneal injection of 1 g cefotiam. 68.80% of patients recovered within 6 days. Failures were due to a methicillin-resistant Staphylococcus epidermidis in 3 cases, a relapsing Stomatococcus mucilaginous infection in 1, a Streptococcus faecalis in 1, an Acinetobacter in 3 and a Pseudomonas in 2. Mean cefotiam concentrations 24 hours after the intraperitoneal injection were 9.4 +/- 7.0 micrograms/ml (range 1.3-26.4 micrograms/ml) in serum and 3.4 +/- 3.3 micrograms/ml (range 0.4-12.2 micrograms/ml) in dialysate. These concentrations are greater than most of cefotiam's MICs for susceptible bacteria, a finding that confirms the value of treatment with a single daily intraperitoneal injection of cefotiam.

Adolescent↗
PubMed1985

[Diffusion of cefotiam into ascitic fluid].

The large apparent volume of distribution of cefotiam (reported by Fourtillan et al. [4]), prompted an investigation of cefotiam diffusion into ascitic fluid. Eight patients with non-infected ascites were each given a single intravenous bolus of 2 gr cefotiam. Samples of blood and ascitic fluid were collected 0.5, 1, 2, 3, 4, 6 and 8 hours after the injection. Plasma and ascitic fluid concentrations of unchanged cefotiam were determined using HPLC. Peak concentration in ascitic fluid averaged 18 micrograms/ml and was reached at two hours. Concentrations were still high (approximately 13 micrograms/ml) at 8 hours, leading to further assays 12 and 24 hours after the injection in three subjects. Cefotiam concentrations achieved in ascitic fluid seem adequate for the treatment of infected ascites, given the antibiotic's MICs for the organisms most commonly involved.

Ascitic Fluid↗
PubMed1985

[Passage of cefotiam into prostatic tissue].

20, 30 and 90 minutes after a single intravenous injection of 2 g of cefotiam prostatic tissue and serum samples were taken from 12 patients who underwent transabdominal prostatectomy for prostatic adenoma. Cefotiam was assayed by HPLC. Mean serum and prostatic concentrations were respectively 157 +/- 39 mg/ml and 42 +/- 23 mg/g at 20 mn, 77 +/- 52 mg/ml and 54 +/- 2 mg/g at 30 mn, 36 +/- 21 mg/ml and 16 +/- 18 mg/g at 90 mn. Elimination half-life of cefotiam was 1 h 39 mn for serum and 1 h 10 mn for prostatic tissue. These findings confirm the satisfactory diffusion of cefotiam within prostatic tissue, although saturation occurs after 30 mn. Treatment of prostatitis by cefotiam can be expected to give excellent results.

Adenoma↗
PubMed1982

[Clinical laboratory approach for determination of effective dose of cefotiam. Observation from disc susceptibility test and MICs].

Reliability of cefotiam disc diffusion susceptibility test was investigated for determining whether the disc results correlate with minimal inhibitory concentration (MIC) or not. The results of Showa disc and Oxoid disc were well correlated. The inhibitory zone size of Showa disc and MIC were also well correlated, indicating reliability of the cefotiam disc test. The disc result, was observed over 84% of clinically isolated S. aureus, S. epidermidis, S. pneumoniae, S. pyogenes, E. coli, K. pneumoniae, P. mirabilis and H. influenzae. Their mean MICs were less than about 1.5 microgram/ml. Such a result should be useful for the determination of drug dose in various clinical conditions in order to obtain the proper drug levels in blood and tissues. The results of antibiotic disc diffusion susceptibility test with various bacteria isolated from clinical materials were compared. Cefotiam revealed a potent antimicrobial activity against Gram-positive cocci, showing a similar potency to that of cephalothin and cefazolin. However, it showed a stronger activity against Gram-negative bacilli than that of cephalothin, cefazolin, cephalexin and cefoxitin, revealing less resistant strains. Cephalosporins developed recently such as cefotaxime, cefoperazone, ceftizoxime, latamoxef etc. show very potent antimicrobial activity against Gram-negative bacilli, but their activity against S. aureus and S. epidermidis is weaker than that of cefotiam, cephalothin, cefazolin etc. Therefore, cefotiam can be considered as one of the drugs of first choice for surgical perioperative prophylaxis and blind therapy.

Bacteria↗
PubMed1994

[Transperitoneal resorption of cefotiam in CAPD patients with and without peritonitis].

BACKGROUND: Cephalosporins of the second generation have been repeatedly recommended for the treatment of peritonitis associated with continuous ambulatory peritoneal dialysis (CAPD), because they are effective against most of the clinically relevant bacteria. In this study, we tested cefotiam, a member of this group of antibiotics, for its suitability in this indication, and determined the intraperitoneal dosage needed to achieve effective serum levels. PATIENTS AND METHODS: IN 10 CAPD-patients with and 10 without peritonitis, cefotiam was added to the dialysis bags (2 l) over a period of seven days. Prior to initiating antibiotic treatment, a sample of dialysis fluid was submitted to bacteriological and cytological examination. During the treatment period, the bags were changed four times a day. In the first three patients 0.5 g cefotiam/bag was administered. Two to four days after initiating treatment, these patients developed nausea and occasional vomiting. Thereupon, all the other patients were given a dose of 0.5 cefotiam/bag only on the first day--a loading dose--followed by 0.25 g/bag for the next six days. Samples of blood and dialysate were obtained after 24, 48, 72, 96, 120, 144 and 168 hours. The cefotiam concentration was determined by the agar diffusion technique. Side effects were checked by clinical observation and measurement of GOT, GOP, alkaline phosphatase, gamma GT, Na, K, and creatinine together with a blood count at the beginning and end of the trial. RESULTS: Among the peritonitis patients, Staphylococcus epidermidis and Staphylococcus pyogenes aureus were each found in four, and Pseudomonas aeruginosa in two patients. In all patients effective serum levels were reached after one day of treatment. In the following period, these levels were maintained. Serum concentrations were higher in patients with than in those without peritonitis (18 to 21 micrograms/ml and 11 to 16 micrograms/ml, respectively). The first three patients had toxic cefotiam levels of about 30 micrograms/ml. All the cases of staphylococcus-induced peritonitis were cured with this therapeutic regimen, while those with Pseudomonas aeruginosa peritonitis required additional treatment with tobramycin. Neither clinical nor chemical side effects were observed. CONCLUSION: Using the regimen described, cefotiam is an effective and safe first-line antibiotic for the treatment of CAPD-related peritonitis.

Adult↗
PubMedDate not supplied

Pharmacokinetics of ampicillin, sulbactam and cefotiam in patients undergoing orthopedic surgery.

As perioperative prophylaxis for major orthopedic operations 81 patients were given the fixed combination of ampicillin (1 g)/sulbactam (0.5 g) or cefotiam (2 g) as short infusions. The three beta-lactams were rapidly distributed into the different tissues and their pharmacokinetic profiles were found to be very similar. It was noteworthy that ampicillin, sulbactam and cefotiam penetrated within minutes, not only into skin, fat and muscles, but also into bone. Thus 0.25 h after starting the infusion the following mean concentrations were measured in bone: 21.8 +/- 10.5 mg/kg ampicillin, 4.9 +/- 2.2 mg/kg sulbactam and 19.4 +/- 10.6 mg/kg cefotiam. For a period of at least 2 h the concentrations measured in serum and in the different tissues affected by the operation (skin, fat, muscle, bone) were above the MICs for pathogens which are involved in postoperative wound infections. On the basis of pharmacokinetic data, ampicillin/sulbactam and cefotiam seem about equally suitable for perioperative prophylaxis in major orthopedic operations.

Adult↗
PubMed1990

Activity of cefotiam in combination with beta-lactam antibiotics on enterobacterial hospital strains.

By using checkerboard titrations the effect of cefotiam combined with different beta-lactam antibiotics on fifty strains of Enterobacteriaceae moderately susceptible (minimal inhibiting concentration greater than or equal to 8 mg/l) or resistant (minimal inhibiting concentration greater than or equal to 64 mg/l) to cefotiam was evaluated. The following compounds were tested: cefamandole, cefazolin, cefmenoxime, cefotaxime, cefotiam, ceftazidime, cefuroxime, mecillinam and piperacillin. The synergistic effect varied markedly. The combination cefotiam-mecillinam showed the highest rate of synergistic activity. Antagonism was found in 1% of the combinations.

Anti-Bacterial Agents↗
PubMed2001

Randomized trial of cefotiam prophylaxis in the prevention of postoperative infectious morbidity after elective cesarean section.

A prospective, randomized study was performed in order to evaluate the effect of cefotiam in the prevention of postoperative infectious morbidity in patients undergoing low-risk elective cesarean section. A total of 146 patients were randomly assigned to receive either intraoperative single-shot prophylaxis with 2 g cefotiam (study group, n =76) or no prophylaxis (control group, n=70). Due to a higher rate of urinary tract infections, the incidence of infectious morbidity after cefotiam prophylaxis was higher in the study group than in the control group (16% vs. 9%, P=0.1). Postoperative infectious morbidity following low-risk elective cesarean section cannot be reduced by intraoperative cefotiam prophylaxis.

Adult↗