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At least 19 recordsLinked to original sources
PubMed1990

Skin tissue fluid levels of cefotiam in healthy man following oral cefotiam hexetil.

Cefotiam hexetil is a pro-drug of cefotiam available for oral administration. To evaluate cefotiam concentrations at the active site in skin and soft-tissue infections, drug levels in skin suction blister fluid (SBF), cantharides blister fluid (CBF) and serum were determined. Six healthy subjects received oral cefotiam 400 mg as cefotiam hexetil. On an other day 200 mg was injected intravenously. Following the oral dose, the bioavailability of cefotiam was 45.5%, and the maximum concentration in serum of 2.6 mg.l-1 was obtained at 2.1 h. Peak concentrations in both types of blister fluid (0.9 mg.l-1) were significantly lower than after the iv dose (SBF 1.4 mg.l-1, CBF 1.5 mg.l-1), and the peak levels occurred later (3.3 versus 1.5 h in CBF). Despite the delay, the extent of penetration was about 100% following either mode of administration (SBF, iv dose 112%, oral dose 117%). The cefotiam level in skin blister fluids declined significantly more slowly than the serum level. Following the oral dose, the mean terminal half life was serum 0.8 h, SBF 2.6 h and CBF 4.6 h. Cefotiam concentrations in the blister fluids were close to the MIC90 of Staphylococcus aureus, S. epidermis and H. influenzae and exceeded the MIC90 of Streptococci, E. coli and Proteus mirabilis. Thus, the oral administration of cefotiam 400 mg t.i.d. should be curative in the majority of bacterial infections of the skin and soft-tissues.

Administration, Oral↗
PubMed1993

Cefotiam concentrations in the sinus fluid of patients with chronic sinusitis after administration of cefotiam hexetil.

Cefotiam hexetil is a prodrug of cefotiam. The concentrations of cefotiam in plasma and sinus secretions were determined in 18 patients (10 males, 8 females, aged 39.3 +/- 13.0 years) with chronic sinusitis. All patients received two 200 mg oral doses of cefotiam hexetil 12 h apart and were divided into four groups according to the time which elapsed between the last dose and collection of secretion samples. The last dose was given 2 h (group I), 3 h (group II), 4 h (group III) or 6 h (group IV) before sinus puncture. Cefotiam concentrations were measured by high-pressure liquid chromatography and microbiological assay, results being very similar with both methods. Mean concentrations of cefotiam with the standard deviation in sinus exudates were 1.04 +/- 0.60 mg/l at 2 h (n = 6), 1.04 +/- 0.33 mg/l at 3 h (n = 4), 0.75 +/- 0.74 mg/l at 4 h (n = 4) and < 0.10 mg/l at 6 h (n = 4). Mean sinus fluid concentrations were higher than mean plasma concentrations in all groups. These results suggest that cefotiam concentrations higher than the MICs for common pathogens are found in sinus secretions up to 4 h after oral administration of cefotiam hexetil.

Adult↗
PubMed1991

The blood binding of cefotiam and cyclohexanol, metabolites of the prodrug cefotiam hexetil, in-vitro.

The binding of cefotiam and cyclohexanol to human serum, isolated proteins and erythrocytes has been studied in-vitro by equilibrium dialysis. The two molecules are 50% bound to serum proteins and the free fraction for both compounds remained constant within the therapeutic concentration range. Human serum albumin (HSA) was exclusively responsible for the cefotiam binding (48%) with a saturable process characterized by one binding site (n = 1.00 +/- 0.14) with a very weak affinity (Ka = 1457 +/- 352 M-1). Like other cephalosporins, cefotiam showed no binding to alpha 1-acid glycoprotein, lipoproteins or gamma-globulins. Cyclohexanol is mainly bound to HSA with a weak affinity (Ka approximately 1,800 M-1) but lipoproteins and alpha 1-acid glycoprotein bind about 30% of bound cyclohexanol in serum. Interactions with free fatty acids (FFA) or bilirubin were studied at physiopathological concentrations. HSA-bound cefotiam was displaced by FFA (1260 microM) and bilirubin (330 microM), whereas the cyclohexanol binding was inhibited only by FFA. The cefotiam binding site seems to be close to the warfarin site (site I) whereas cyclohexanol probably shares the diazepam site (site II) on HSA. There is no mutual inhibition of binding between cefotiam and cyclohexanol at therapeutic levels. The binding of both compounds to erythrocytes is low and restricted when measured in the presence of plasma.

Bilirubin↗
PubMed1992

Automated high-performance liquid chromatographic method for the simultaneous determination of cefotiam and delta 3-cefotiam in human plasma using column switching.

An automated high-performance liquid chromatographic method using column switching was established for the simultaneous determination of cefotiam (I) and delta 3-cefotiam (II) in human plasma after oral administration of cefotiam hexetil dihydrochloride. The method allowed the determination of analytes in plasma by the direct injection of diluted specimen with phosphate buffer. The analytes were enriched onto the C18 short pretreatment column by 0.05 M phosphate buffer (pH 7.7), while proteins and endogenous hydrophilic substances in plasma were washed off to waste. The enriched analytes were then back-flushed onto the analytical C18 column, separated by a mixture of 0.05 M phosphate buffer (pH 7.7)-acetonitrile (88:12, v/v) and detected by the ultraviolet absorbance at 254 nm. Recoveries from spiked plasma were quantitative, and the coefficients of variation were below 4%. The lower detection limits in plasma were 10 ng/ml for both I and II. Concentrations of I and II in plasma determined by the present method were in good agreement with those obtained by the conventional deproteinization method.

Cefotiam↗
PubMed1984

[Studies on the skin test of cefotiam and anti-cefotiam antibody].

Patients having previously not received cefotiam (CTM), a recently introduced cephem antibiotic, were subjected to skin tests with a 300 micrograms/ml solution of CTM in physiological saline before and after CTM therapy to detect sensitization with the drug. Anti-CTM antibody titration was carried out on sera from patients who showed a positive skin test and those who developed signs of hypersensitivity during CTM therapy. The results were as follows: Of 1,927 patients examined by skin test with CTM prior to initiation of CTM therapy, 31 patients (1.61%) showed positive reactions with formation of a wheal and erythema. There were 7 patients (0.36%) who proved negative in the skin test but developed mild symptoms of hypersensitivity in association with the skin test. The 847 patients negative on the CTM skin test were retested after a completion of CTM therapy, of whom 6 (0.71%) were found to have become positive showing formation of a wheal and erythema and 3 others (0.35%) showing a negative skin test developed mild adverse reactions associated with the skin test. Sixty-eight serum samples collected from the patients positive on the CTM skin test and those who developed manifestations of hypersensitivity following CTM therapy were examined for anti-CTM antibody by the Prausnitz-K ustner reaction, passive cutaneous anaphylaxis test and hemagglutination test. All proved negative in these tests. Of various background factors assessed, none was found to have causal relation to the skin reaction in any of the patients showing positive skin reactions to CTM.

Adolescent↗
PubMed1993

[Bacteriological evaluations of combination effects with cefotiam and other antimicrobial agents against methicillin-resistant Staphylococcus aureus. I. Synergistic actions of cefotiam with imipenem and vancomycin].

We assessed the bacteriological efficacies of cefotiam (CTM) plus imipenem (IPM) and CTM plus vancomycin (VCM) therapies against methicillin-resistant Staphylococcus aureus (MRSA) in an in vitro system. The results are summarized as follows. 1. It appeared that the bacteriological efficacies of CTM+IPM therapy against MRSA strains were different against different target MRSA strains. In other words, the FIC indices of CTM+IPM were distributed in a wide range of < or = 0.5- > 2.0. The strains showing MIC levels of < or = 8 micrograms/ml in IPM concentrations showed a strong correlation with FIC index values of < or = 0.5, and the strains showing the MIC level of > or = 128 micrograms/ml in IPM concentration showed a strong correlation with FIC index values of > 2.0. Hence, the strains showing FIC indices < or = 0.5 were considered to be newborn strains with penicillin-binding protein 2' (PBP-2'), those showing FIC indices > 0.5- < or = 2.0 were considered to be strains with increasing production in PBP-2', and those showing FIC indices > 2.0 were considered to be strains with increasing productions in both PBP-2' and PBP-m2. In strains with FIC indices higher than 2.0, the 2 drugs may possibly share the action mechanism and the activity center thus they compete with each other.(ABSTRACT TRUNCATED AT 250 WORDS)

Cefotiam↗
PubMed1993

[Bacteriological evaluations of combination effects with cefotiam and other antimicrobial agents against methicillin-resistant Staphylococcus aureus. II. Synergistic actions of cefotiam with arbekacin and minocycline].

We assessed the bacteriological efficacies of cefotiam (CTM) plus arbekacin (ABK) and CTM plus minocycline (MINO) therapies against methicillin-resistant Staphylococcus aureus (MRSA) in an in vitro system. The results are summarized as follows. 1. Both of CTM+ABK and CTM+MINO demonstrated almost perfect antibacterial activities against MRSA strains at ABK and MINO concentrations of MIC levels as clinically expected plasma ABK or MINO levels, and also showed antibacterial activities at ABK or MINO concentrations of sub-MIC levels. But no results suggesting antagonism were obtained. 2. The potent antibacterial effect of CTM+ABK or CTM+MINO against MRSA strains was considered to be the result of damage to the cellular membrane of target strains by ABK or MINO with ABK or MINO concentrations at MIC or sub-MIC levels and by the subsequent antibiotic effect of CTM. 3. A combination of drugs which are different from each other in mechanisms of action and points of action is likely to show a consistent antibacterial effect, but a combination of drugs which are competitive to each other because they share mechanism and point of action possibly cause antagonism.

Aminoglycosides↗
PubMed1979

[Morphological studies on antibacterial activities of cefotiam (author's transl)].

1. Cefotiam was demonstrated to be more potent than cefazolin in its antibacterial activities against clinical isolates of E. coli, Klebsiella, Serratia, Proteus mirabilis, Proteus morganii and Proteus inconstans. MICs of cefotiam with 10(6) cells/ml inoculum size were considerably lower than those with 10(8) cells/ml. 2. Organisms lysed when exposed to cefotiam at concentrations higher than the MICs with 10(8) cells/ml. Morphological changes of organisms into filament occurred even at concentrations lower than the MICs with 10(6) cells/ml. This indicates that cefotiam is incorporated into organisms at remarkably low concentrations and exerts its antibacterial activities. 3. Cefotiam showed a high affinity for penicillin-binding proteins (PBP) 1A, 1Bs and 3. The formation of filament at low concentrations of cefotiam is possibly attributable to the high affinity of cefotiam for PBP 3 in addition to its high permeability through outer cell membrane. 4. As the antibacterial activities of cefotiam are displayed at lower concentrations, it is reasonable to consider that doses of cefotiam on clinical use can be reduced in comparison with those of conventional cephalosporins.

Cefazolin↗
PubMed1987

Prophylactic antibiotics for patients undergoing elective biliary tract surgery: a prospective randomized study of cefotiam and cefoperazone.

Cefotiam, a second generation cephalosporin and cefoperazone, a third generation cephalosporin have a broad spectrum of activity against a majority of organisms commonly found in the bile. Although cefoperazone is excreted into the human bile to a greater extent than is cefotiam, there are no comparative data available that cefoperazone prophylaxis is safer and more effective than cefotiam for patients undergoing biliary tract surgery. A prospective randomized study was performed to compare the safety and efficacy of cefotiam with those of cefoperazone for prophylaxis in patients undergoing elective biliary tract surgery. The incidence of postoperative infection was not significantly different between the cefotiam group (n = 86) and the cefoperazone group (n = 86). The rate of side effects, however, was significantly different. In the cefotiam group, only one patient had diarrhea whereas in the cefoperazone group, eight had diarrhea and one skin eruption. Clostridium difficile cytotoxin was nil in those with diarrhea. Diarrhea in all patients was mild and recovery was rapid. Cefotiam is thus safer and as effective as cefoperazone in preventing postoperative infections following biliary tract surgery. We suggest that cefotiam is the first choice antibiotic for prophylaxis in biliary tract surgery.

Adult↗
PubMed1991

The effect of combinations of cefotiam and other antibiotics on methicillin-resistant Staphylococcus aureus in vitro.

The in-vitro activities of cefmetazole, flomoxef, imipenem, vancomycin and enramycin alone and in combination with cefotiam against eighteen clinically isolated methicillin-resistant Staphylococcus aureus was investigated. Cefotiam, cefmetazole, flomoxef and imipenem inhibited the growth of clinical isolates at concentrations ranging from 100 to 1600, 6.25 to 400, 6.25 to 400 and 0.78 to 200 mg/L, respectively. Synergic effects were observed with combinations of cefotiam and cefmetazole, flomoxef or imipenem against more than 70% of the strains. The fractional inhibitory concentration (FIC) index values were less than 0.1. Vancomycin and enramycin alone inhibited the growth of all strains at concentrations ranging from 0.39 to 1.56 mg/L and 0.2 to 0.78 mg/L, respectively. Moreover, vancomycin and enramycin in combination with cefotiam showed synergy against strains in which no synergic effects were observed when cefotiam was combined with other beta-lactam agents. About 50% of the strains tested were inhibited synergically by cefmetazole, flomoxef or imipenem, at clinically relevant concentrations in combination with 0.78 mg/L of cefotiam. The effects of vancomycin or enramycin in combination with cefotiam on the growth of a homogeneous resistant clone, which was derived from one of the clinical isolates, TS-65, was also studied. Regrowth in the presence of vancomycin or enramycin alone was suppressed when cefotiam was added.

Cefotiam↗
PubMed1993

Synergic activity of imipenem/cilastatin combined with cefotiam against methicillin-resistant Staphylococcus aureus.

The synergic activity of imipenem/cilastatin combined with cefotiam was studied in a mouse bacteraemia model. Combinations of imipenem plus cefotiam in ratios from 1:5 to 1:160 were more effective than either imipenem alone or cefotiam alone (P < 0.05). Synergy was observed against both beta-lactamase producing and beta-lactamase non-producing MRSA. Staggered combinations of imipenem with cefotiam (each drug was administered at a different time) were studied in an in-vitro pharmacokinetic system to clarify relationships between killing kinetics and pharmacodynamics of the combinations. In the in-vitro system, cefotiam (1 g over 30 min) administered 2 h after imipenem administration (250 mg over 30 min) reduced viable cell counts to an undetectable level and maintained this for 4 h, while the simultaneous administration of imipenem and cefotiam maintained an undetectable cell count for only 2 h. Furthermore, imipenem administered after cefotiam showed no synergy. These results indicate that the timing of dosing of each antibiotic influences synergy, and administration of cefotiam 2 h after imipenem is more effective than the other regimens.

Animals↗
PubMed1991

Intra-operative antibiotic prophylaxis in neurosurgery. A prospective, randomized, controlled study on cefotiam.

In this prospective, randomized and controlled study the effect of cefotiam for the prevention of wound infections following trepanations was investigated. The main interest was centered on the rate of post-operative bone flap infections requiring operative revision. Administration of cefotiam was randomized for patients undergoing major craniotomies. The antibiotic was administered intravenously in a single dose of 2 g with induction of anaesthesia. Only clean or clean contaminated cases were included. Excluded were contaminated cases, operations with a transnasal-transsphenoidal approach, shunt-operations and patients with any other preoperative infection or antibiotic therapy. Outpatients were excluded due to difficulties in obtaining sufficient clinical information. From originally 918 consecutive patients operated on 711 fulfilled the entry criteria. With regard to age, sex, diagnosis and the site of te trepanation, control patients (n = 355) and cefotiam treated patients (n = 356) were shown to be comparable. In the various subgroups formed for different primary diagnoses, concomitant steroidal therapy and concomitant severe internal medical diseases cefotiam treated patients and controls were comparable as well. A highly significant difference for bone flap infection could be shown with 0.3% in the cefotiam group versus 5.1% in the control group (p less than 0.001). The overall rate of post-operative deep wound infections including meningitis and abscesses was also significantly (p less than 0.005) different with 3.1% in the cefotiam versus 9.0% in the control group. Thus it was concluded that a single dose of cefotiam significantly reduces post-operative deep wound infection.

Brain Abscess↗
PubMed1980

Comparative activities of cefotiam and cefazolin against urinary tract infections with Proteus mirabilis in mice.

The therapeutic effect of cefotiam on experimental urinary tract infections with Proteus mirabilis IFO 3849 in mice was compared with that of cefazolin. The minimal inhibitory concentrations of cefotiam and cefazolin against the test organism were 1.56 and 25 micrograms/ml, respectively. Beginning 3 days after infection, various doses of each cephalosporin were given subcutaneously twice a day for 5 days. Doses of 100 mg of cefotiam per kg or more sterilized the urine within 3 days and effected a marked reduction or complete eradication of bacteria in the bladder walls and kidneys of mice sacrificed the day after treatment was terminated. A dose of cefazolin greater than 800 mg/kg was required for equivalent therapeutic results. Clearance of bacteria from urinary tract organs was as rapid or more rapid with 50-mg/kg doses of cefotiam as with 200-mg/kg doses of cefazolin. Much more rapid clearance was attained with 200-mg/kg doses of cefotiam. The concentrations of cefotiam attained in plasma, kidney, and urine were lower than the cefazolin levels achieved at an equivalent dose. The superiority of cefotiam over cefazolin in treatment of experimental urinary tract infections appears to be due to its greater activity against the test organism.

Animals↗
PubMed1995

Autolysis of methicillin-resistant Staphylococcus aureus is involved in synergism between imipenem and cefotiam.

Imipenem-induced autolysis and the activity of imipenem plus cefotiam were studied in 16 strains of methicillin-resistant Staphylococcus aureus (MRSA). The degree of imipenem-induced autolysis and the rate of synergistic action of imipenem plus cefotiam varied among strains and did not correlate with susceptibility to either imipenem or cefotiam. However, the degree of autolysis correlated well with susceptibility to the synergistic action of imipenem plus cefotiam. In methicillin-susceptible S. aureus strains, both imipenem-induced autolysis and the synergistic activity of the combined drugs were less than those observed in MRSA strains. Differences in the degree of autolysis were not due to differences in autolytic enzyme production. The autolysis of imipenem-pretreated MRSA was enhanced further by cefotiam, while treatment of cells in the reverse order did not enhance autolysis. These findings indicate that cell wall impairment in MRSA is caused by exposure to imipenem but not to cefotiam and that this difference in drug actions results in synergism between imipenem and cefotiam. The possible participation of penicillin-binding proteins PBP 2' and PBP4 in the observed effect is discussed.

Bacterial Proteins↗
PubMed1986

Pharmacokinetics and quantitative characterization of cefotiam excretion after intravenous administration to patients after cholecystectomy.

Six patients, aged 52 to 71 years, with T-tube drainage of the common bile duct and a urinary catheter after cholecystectomy, were studied in order to evaluate the urinary and biliary excretion and pharmacokinetics of cefotiam in the early postoperative period. Each patient received cefotiam 1 g i.v. as a bolus injection. Cefotiam in plasma, urine, and bile were determined by HPLC. A 2-compartment open model with elimination from the central compartment satisfactorily fitted the plasma levels of the drug. The renal clearance of cefotiam (CLR = 133 ml/min) was an order of magnitude greater than its biliary clearance (CLB = 11.8 ml/min). Glomerular filtration was the main mechanism for elimination of cefotiam. The values of CLR and CLB in relation to the total plasma clearance (CL = 138. ml/min) demonstrated the negligible role of metabolism in elimination of cefotiam in these patients.

Aged↗