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PubMed1979

In vitro studies with cefazedone.

The minimum inhibitory concentrations of the new cephalosporin derivative (6R,7R)-7-(2-[3,5-dichloro-4-oxo-1(4H)-pyridyl]-acetamido)-3-([(5-methyl-1,3,4-thiadiazol-2-yl)-thio]methyl)-8-oxo-5-thia-1-azabicyclo[4,2,3]oct-2-ene-2-carboxylic acid (cefazedone, Refosporen) were tested in vitro against 358 bacterial strains. The antibacterial activity of cefazedone corresponds largely to that of cephalothin. Cefazedone is also active at a concentration of 16 micrograms/ml against 100% of enterococci, which can be classified as moderately effective, compared to cephalothin, which is completely ineffective. The MIC values from the dilution broth technique are in good correlation with the results determined by agar diffusion tests.

Bacteria↗
PubMed1982

[Minimal inhibitory and bactericidal concentrations of cefoperazone, cefotaxime, cefuroxime and cefalotin against 90 bacterial strains].

In this work, the sensitivity in vitro of cefoxitin, cefuroxime, cefotaxime, cefoperazone and cephalothin have been examined. Test of sensitivity in vitro have been performed as by Kirby-Bauer method as by measurement of MIC and MBC. Then the regression lines have been determined. Cefotaxime and cefoperazone provided nearly complete coverage of all Enterobacteriaceae; 80% were inhibited at less than or equal to 2 mcg./ml. This value is far below therapeutically attainable serum concentrations. Cefotaxime has MIC lower than cefoperazone. It has a significant spectrum of activity against Pseudomonas aeruginosa, nonenterococcal Streptococcus sp, non Enterobacteriaceae Gram-negative bacilli. Only enterococci and Acinetobacter species were relatively resistant to cefoperazone and cefotaxime. The cephalothin and the cefoxitin included excellent antimicrobial coverage of the staphylococci and the anaerobic bacteria respectively.

Acinetobacter↗
PubMed1981

Prospective clinical trial of antibiotics for pulmonary resections.

One hundred and seventy-one patients undergoing pulmonary resection were included in a prospective randomized clinical study evaluating the efficacy of prophylactic antibiotics. Eight-three patients randomly chosen received no parenteral antibiotics and 88 received a short course of cephalothin intravenously. Topical antibiotics were used in the pleural cavity and would of all patients. There were no statistically significant differences between the two groups in terms of days of postoperative fever, number of postoperative septic complications and length of postoperative stay. However, when postoperative infectious complications developed in the antibiotic group, they were often secondary to gram-negative organisms resistant to cephalothin.

Administration, Topical↗
PubMed1981

[Study of the minimum inhibiting concentration of a new cephalosporin (HR 756): comparative data with other beta-lactamic antibiotics].

HR 756 is a new beta-lactamase resistant cephalosporin. The activity of HR 756 was compared in vitro to that of cefamandole, cefoxitine, cefuroxime and cephalothin. A concentration of 1 microgram/ml inhibited practically all isolates of E. coli, Salmonella, Shigella, Proteus indole + and indole --, Klebsiella, etc. A lower activity in vitro has been found regarding to Enterobacter, Serratia, Citrobacter and Pasteurella. The cefotaxime has some anti-Pseudomonas activity at concentrations of 7.5-15 micrograms/ml. For most Gram-negative organisms, HR 756 was most active. The cephalothin and the cefoxitine have resulted more active regard to Staph. aureus and Bacteroides fragilis, respectively.

Bacteria↗
PubMed1981

[In vitro susceptibility of Listeria monocytogenes with special reference to newer beta lactam antibiotics (author's transl)].

Minimal inhibitory (MIC) and minimal lethal concentrations (MLC) of ampicillin, mezlocillin, piperacillin, cephalothin, cefamandole cefoxitin, cefuroxime, cefotaxime, gentamicin, and doxycycline against 44 strain of Listeria monocytogenes from clinical specimens were determined by broth dilution tests. With regard to the MIC90 and MLC90 values (concentrations which inhibited or killed 90 percent of the strains) ampicillin showed the greatest anti-listeric activity with 0,48 and 20,8 microgram/ml. The corresponding results for mezlocillin were 8,0 and 54,4 microgram/ml, for piperacillin 5,2 and 128 microgram/ml, resp. Among the cephalosporins, cephalothin showed the best activity (MIC90, 5,8 microgram/ml, MLC90, 76,8 microgram/ml). The MIC90 values of cefamandole and cefoxitin were 7,8 and 89,6 microgram/ml, resp. and the MLC90 was more than 128 microgram/ml while there was no clinically relevant activity of cefuroxime and cefotaxime (MIC90 more than 128 microgram/ml). The MIC90 and MLC90 results of gentamicin were 12 and 15,2 microgram/ml, resp, and those of doxycycline 8 and 25,6 microgram/ml, resp. There were only slight differences between gentamicin MIC and MLC values. Henceforward the drug of choice for the treatment of generalized listeric infections should be ampicillin eventually in combination with gentamicin.

Ampicillin↗
PubMed1983

Antibiotic prophylaxis for coronary bypass grafting. Comparison of a five-day and a two-day course.

A trial was conducted to compare the effectiveness of a 2 day and a 5 day course of antibiotic prophylaxis after coronary bypass grafting. One hundred sixty patients were randomized to one of the two courses. The 2 day course comprised 48 hours of intramuscular kanamycin and intravenous cephalothin. The 5 day course comprised 48 hours of intramuscular kanamycin and intravenous cephalothin followed by 3 days of oral cephalexin. After the 2 day course, there were two wound infections and two respiratory tract infections in 79 patients (5.1%), and after the 5 day course, one wound infection and two respiratory tract infections in 81 patients (3.7%). Subsequently, in 171 patients undergoing coronary bypass grafting and given the 2 day course, the infection rate was 3.5%. There was no significant difference in infection rates among the three groups (p greater than 0.05). We conclude that no more than 2 days of antibiotic prophylaxis are necessary for patients undergoing coronary bypass grafting.

Adult↗
PubMed1984

In vitro susceptibility of Streptococcus bovis to six antibiotics.

A recent report of two isolates of Streptococcus bovis resistant to killing by low levels of penicillin G prompted this study of the in vitro susceptibility of 100 clinical isolates of S bovis to six antibiotics. Using a microdilution method, we found the minimum bactericidal concentrations for 99% of the isolates to be as follows: penicillin G, 0.5 microgram/ml; methicillin, 16 micrograms/ml; ampicillin, 0.5 microgram/ml; cephalothin, 2 micrograms/ml; clindamycin, 2 micrograms/ml; and vancomycin, 2 micrograms/ml. The high-level resistance of S bovis to penicillin G previously described was not seen. This study suggests that penicillin G can still prove effective in treating most infections caused by S bovis, including infective endocarditis, and that cephalothin and vancomycin are useful alternative agents.

Ampicillin↗
PubMed1978

Evaluation of three antibiotic programs in newborn infants.

Emergence of gram-negative bacteria resistnant to a number of antibiotics in intensive care nurseries for neonates emphasizes the need for alternatives in antibiotic combinations. One commonly used combination, gentamicin-ampicillin, and two newer combinations, tobramycin-cephalothin and amikacinampicillin, were evaluated prospectively in 60 newborns in such a nursery. Subjects were randomly assigned to one of the above therapy groups. Dosages in mg/kg.d were 100 for ampicillin and cephalothin, 6 for gentamicin and tobramycin and 15 for amikacin. Aminoglycoside serum concentrations, clinical tolerance and toxicity were monitored. Aminoglycoside concentrations after intravenous administration of the drugs were within the expected range (gentamicin and tobramycin 4 to 6 microgram/mL and amikacin 15 to 20 microgram/mL). There was no hematologic, renal or hepatic toxicity attributable to antibiotic therapy and the combinations were tolerated equally; no bilirubin displacement was detected in vitro or in vivo.

Amikacin↗
PubMed1978

Intramuscular injection-site complications.

Among 26,294 hospitalized medical patients monitored by the Boston Collaborative Drug Surveillance Program, 46% received at least one intramuscular (IM) injection. Drugs for which IM injection was the route of administration in more than 80% of all exposures included penicillin G procaine, mercurial diuretics, cyanocobalamin, streptomycin sulfate, colistimethate sodium, meperidine hydrochloride, cephaloridine, scopolamine hydrobromide, kanamycin sulfate, and iron dextran injection. Local complications of IM injection were reported in a total of only 48 patients (0.4% of all IM recipients). Local complications were most commonly associated with IM injection of cephalothin sodium. Clinically important local complications are uncommonly associated with IM injections in general. However, certain drugs, eg, cephalothin, produce injection-site complications with relatively high frequency; the clinical role of IM injection of such drugs should be reevaluated.

Abscess↗
PubMed1983

The effect of hypotensive anesthesia on cephalosporin concentrations in serum, soft tissue, and bone.

The objective of this study was to determine the efficacy of a hypotensive anesthetic in enhancing tissue perfusion while simultaneously controlling surgical blood loss. One hundred ten patients undergoing 126 total hip arthroplasties were administered either cephalothin or cefamandole on a double-blind basis. Hypotensive anesthesia was administered to 64 patients; 46 received a normotensive anesthetic. Degree of tissue perfusion was measured by the concentration of cephalosporin found in samplings of serum, soft tissue, and bone. These samples, obtained during the course of total joint arthroplasty, indicate that the hypotensive anesthetic sodium nitroprusside did not significantly alter the concentrations of cefamandole or cephalothin from those found in the normotensive group.

Anesthesia↗
PubMed1983

Reactivity and binding of beta-lactam antibiotics in rabbit renal cortex.

In studies designed to evaluate the reactivity of the beta-lactam antibiotics in the rabbit kidney, the binding to cortical macromolecules of isotopically labeled cephaloglycin (highly toxic) was compared in vivo and in vitro with that of cephalothin (minimally toxic) and benzylpenicillin (nontoxic). Three hours after administration of equal doses, the amounts of firmly bound antibiotic in whole cortex and in nuclear, mitochondrial, microsomal and cytosolic fractions of cortex were greatest for cephaloglycin (cortical concentration 7% of that measured at 0.5 hr), intermediate for cephalothin (2%) and least for benzylpenicillin (1%); the amounts of firmly bound antibiotic were unrelated to the earlier, peak cortical concentrations. Binding to cortical microsomes in vitro showed a similar pattern (greatest for cephaloglycin, least for benzylpenicillin); in addition, the binding in vitro of cephaloglycin was decreased by the addition of an NADPH-generating system and was not decreased by piperonyl butoxide. These studies provide evidence that the spontaneous reactivity of the beta-lactam ring may be an important determinant of the nephrotoxicity of the cephalosporins and fail to support the existence of a role of the cytochrome P-450 mixed-function oxidases in this reactivity.

Animals↗
PubMed1982

[Is resistance to antibiotics changing? Development of resistance of Enterobactericeae from specimens 1977-1980].

The results of sensitivity testing from the last 4 years of the enterobacteria isolates have been evaluated for ampicillin, cephalothin, gentamicin, and trimethoprim-sulfamethoxazole. There was a remarkable decrease of cephalothin resistant E. coli, proteus mirabilis, and klebsiella strains. The number of strains resistant to ampicillin was only decreased in the case of proteins mirabilis. The resistance frequency to gentamicin was unchanged. In contrast, an increasing number of resistant strains of E. coli and proteins mirabilis was observed with regard to trimethoprim-sulfamethoxazole.

Ampicillin↗
PubMed1980

Aortocoronary bypass procedures and sternotomy infections: a study of antistaphylococcal prophylaxis.

In a prospective study of cephalothin prophylaxis for patients who underwent aortocoronary bypass an unacceptably high rate (44%) of Staphylococcus aureus sternotomy infections occurred in a placebo-treated group. In two other groups of patients, one group given cephalothin intraoperatively and the other given the antibiotic both intra- and postoperatively, such infections occurred with similar frequency (2.6% and 2.1% respectively). This study demonstrates the need for antistaphylococcal agents during aortocoronary bypass operation. No advantage is derived by extending this therapy beyond the operative period.

Aged↗
PubMed1982

The pharmacokinetics of prophylactic antibiotics administered by intraoperative irrigation at the time of cesarean section.

Thirty patients at term undergoing cesarean section received intraoperative irrigation with either cefamandole, cephalothin, or ampicillin to prevent postoperative infection. Serum drug levels were measured at 15, 60 and 120 minutes after completion of irrigation. Serum levels at each sampling interval were highest for cefamandole and lowest for cephalothin. Les than 2% of the total drug dose was excreted in the urine during the first 2 postoperative hours. In most patients, maximum serum antibiotic concentrations exceeded minimal inhibitory concentrations for several recognized pelvic pathogens. It is concluded that the mechanism of action of intraoperative irrigation may in part be due to systemic absorption of antibiotic and not simply to a local effect on the endometrium. Moreover, the degree of systemic absorption may be sufficient to cause allergic drug reactions and to exert selective pressures for the emergence of drug-resistant microorganisms.

Adult↗
PubMed1981

[Intra-arterial antibiotic therapy in the management of chronic post-traumatic osteomyelitis of the extremities (experimental and clinical studies].

Authors examined the changes of antibiotic concentration in the inflammatory focus after administering Gentamycin and Cephalothin intravenously or intraarterially in case of experimentally induced osteomyelitis in the tibia of rabbit. Administering Gentamycin i. v. no therapeutic level could be measured, while Cephalothin showed a therapeutic level of antibiotic concentration just for a short period. When the same doses of these antibiotics were administered in the femoral artery, effective local antibiotic concentration could be detected for 3 hours. Authors' clinical studies also support these experimental results. Performing 43 i. a. treatments in 38 patients with osteomyelitis 39 was rated as effective.

Animals↗
PubMed1980

Antibiotic activity in surgical incisions. The basis of prophylaxis in selected operations.

Perioperative antibiotic administration to produce systemic effects reduces the frequency of operative wound infection in selected procedures. Controlled clinical trials now indicate that cephalothin sodium may not be effective in this role, whereas cephaloridine and cefazolin sodium have been beneficial. Review of estimates of incisional antibiotic concentrations taken during prospective patient studies display patterns compatible with these data. EAch drug reaches acceptable incisional concentrations, which are relatively well maintained for cephaloridine and cefazolin; cephalothin disappears from human incisions so rapidly as to provide little wound protection in operations lasting more than one hour.

Anti-Bacterial Agents↗
PubMed1977

Rational and irrational use of antibiotics in a Canadian teaching hospital.

Parenteral therapy with gentamicin, cloxacillin, ampicillin and cephalothin was surveyed on a surgical, a gynecologic and medical ward of a teaching hospital. During a 3-month period 219 patients (12.9% of the total number admitted to the three wards) received at least one of the four antibiotics parenterally. Ampicillin and gentamicin were used most frequently on the three wards when the indication for therapy was either infection or empirical use. Cephalothin was used most frequently for prophylaxis in the gynecologic and surgical patients; no medical patient received this drug. Overall, therapy was assessed to be irrational in 42.0, 50.0 and 12.0% of the surgical, gynecologic and medical patients, respectively. Prophylaxis was the indication for therapy in 76.9 and 86.8% of the surgical and gynecologic patients, respectively, for whom the therapy was assessed to be irrational.

Ampicillin↗
PubMed1977

Drug-protein interaction: the binding of cephalosporins to albumins.

The binding of some cephalosporin antibiotics, namely cephalothin, cephaloridine and cephalexin, to serum albumins was quantitized using a fluorescence probe technique. The results suggest that these drugs bind to hydrophobic sites on serum albumins. The association constants of the three drugs with bovine serum albumin showed the strongest binding for cephalothin (Ka 1.2 x 10(3) M(1)) and weaker ones for cephaloridine and cephalexin (Ka 0.59 and 0.4 x 10(3) M(-1)). Serum albumin from different species was also investigated, only minor variations in the binding properties being found.

Animals↗