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PubMed1974

Cefoxitin and cephalothin: antimicrobial activity, human pharmacokinetics, and toxicology.

Cefoxitin, a semisynthetic cephamycin, has been compared with the widely used parenteral cephalosporin, cephalothin, in terms of antibacterial activity, human pharmacokinetics, and toxicity. For both compounds, minimal inhibitory concentrations were within the therapeutic range against the 156 gram-positive cocci tested (except group D streptococci), but cephalothin was 8 to 20 times more active. Regarding the 313 gram-negative organisms tested, both antibiotics were of approximately equal activity against cephalothin-susceptible strains, but cefoxitin was outstandingly superior against Providencia spp. and indole-producing Proteus spp., and markedly better against Serratia marcescens and Bacteroides fragilis. Against these organisms, cefoxitin but not cephalothin would be expected to be therapeutically valuable. Antibiotic activity levels in the serum and urine of 18 human volunteers after parenteral administration were higher and more prolonged in the case of cefoxitin, which had an average terminal serum half-life of about 45 min and a urinary recovery of about 90%. Cefoxitin was entirely nontoxic and, given intramuscularly, slightly less painful then cephalothin. These preliminary results suggest that cephamycins may prove to be a significant chemotherapeutic advance.

Adult↗
PubMed1976

Protective effect of cephalothin against gentamincin-induced nephrotoxicity in rats.

The possibility that the nephrotoxicity of gentamicin may be potentiated by the concomitant administration of cephalothin was examined in a rat model. Cephalothin given once daily in dosages up to 800 mg/kg per day for 10 days produced no renal damage. Gentamicin, at 6 to 50 mg/kg per day, caused pathological changes which were dosage related and affected primarily the proximal tubular cells. Administration of the two drugs simultaneously resulted in a significant protective effect of cephalothin against gentamicin-related nephrotoxicity (P < 0.01). When the daily injections of the two agents were separated by an interval of 6 h, the protective effect was lost, and the resultant damage was the same as that due to gentamicin alone. The protective effect of cephalothin was reproduced by the administration of equiosmolar amounts of sulfate (sodium sulfate), suggesting that the phenomenon might be related to the presence of nonresorbable anion in the urine. These studies indicate that, in the rat, cephalothin does not potentiate, but, in fact, may prevent the nephrotoxic effects of gentamicin.

Animals↗
PubMed1973

Cefoxitin, a new semi-synthetic cephamycin: an in-vitro and in-vivo comparison with cephalothin.

The activity of cefoxitin was compared with that of cephalothin against 229 bacterial strains. Cefoxitin was more active against most Gram-negative strains, notably against indole-producing Proteus spp., which are usually resistant to the cephalosporins. Cefoxitin was not susceptible to any significant extent to degradation by beta-lactamases produced by Gram-negative organisms. Against Gram-positive organisms, however, cefoxitin was considerably less active than cephalothin, but minimum inhibitory concentrations for Staphylococcus aureus were well within therapeutically attainable blood levels.Pharmacokinetic studies in 18 volunteers showed a higher and longer sustained antibiotic activity in serum and urine after injections of cefoxitin than after equal doses of cephalothin. Urinary recovery of cefoxitin activity was also much higher than that of cephalothin. No evidence of toxicity due to cefoxitin was found. Cefoxitin was slightly less painful after intramuscular injection than cephalothin.

Adolescent↗
PubMed1975

Reversible nephrotoxicity associated with cephalothin therapy.

A 53-year-old man with scalp cellulitis developed acute renal failure after sodium cephalothin therapy. The patient probably had preexisting renal disease. Discontinuance of cephalothin was followed by improvement of the renal function. Specimens from a renal biopsy performed during the recovery phase showed nonspecific changes in the renal tubular epithelium, similar to those seen in animals treated with large doses of cephalothin. Previously reported cases of cephalothin nephrotoxicity, along with this case, caution the clinician to proceed with care in the treatment of azotemic patients with cephalothin.

Acute Kidney Injury↗
PubMed1978

Double-blind comparison of cefazolin and cephalothin in open-heart surgery.

Ninety-nine patients undergoing cardiac surgery were randomly assigned to treatment with cefazolin and cephalothin to compare the effectiveness of these cephalosporins in the prevention of postoperative infections. The incidence of infections was low with both antibiotics (cefazolin 2.1 percent, cephalothin 4.6 percent). Intraoperative serum cefazolin levels were more evenly distributed, whereas a wide dispersion of cephalothin levels was observed. There was no measurable antibiotic detected in cardiac tissue samples in the majority of the cases. Adverse reactions (skin rashes) occurred only in three patients, all receiving cephalothin. It is concluded that cefazolin is as safe and effective as cephalothin in the prevention of postoperative infection in patients undergoing open-heart surgery.

Adult↗
PubMed1986

Distribution of cephalothin and ceftriaxone into experimental interstitial tissue fluid in rabbits.

A study was carried out on the access and residence of cephalothin and ceftriaxone in interstitial tissue fluid (ITF) produced experimentally by subcutaneous implantation of spiral steel cages after administration of 30 mg/kg of the two antibiotics to rabbits. The levels reached by the drug in serum and ITF were determined by a microbiological plate diffusion method. The elimination half-lives of cephalothin and ceftriaxone showed mean values of 0.23 and 1.77 h, respectively. Both these values were lower than those found for the disappearance half-lives from ITF. Cephalothin reached a maximum concentration in ITF of 4.37 micrograms/ml at 0.52 h, while ceftriaxone showed a maximum concentration of 24.94 micrograms/ml at 2.09 h. The area under the curve of tissue concentrations of ceftriaxone was approximately 20-fold greater than that of cephalothin at the same dose and using same administration route. The index of the penetration capacity expressed as the quotient of the respective AUC's in ITF and in the systemic circulation gave a value for ceftriaxone which was approximately double that obtained for cephalothin.

Animals↗
PubMed1985

[Decrease of sisomicin nephrotoxicity as affected by cephalothin: pharmacokinetic evaluation].

The effect of cephalothin on the nephrotoxicity and pharmacokinetics of sisomicin was studied on Wistar rats. Sisomicin was injected intramuscularly in doses of 12.5 and 25 mg/kg alone or in combination with cephalothin in a dose of 360 mg/kg once a day for 16 days. It was shown that the combined use of sisomicin and cephalothin resulted in less pronounced functional and morphological changes in the kidneys as compared to the use of sisomicin alone. The decrease in the nephrotoxic effect was accompanied by a decrease in the sisomicin concentration in the blood serum and the site of the nephrotoxic effect (the kidney cortical layer) and the period of the aminoglycoside half-life in the kidney cortical layer under the action of cephalothin. The analysis of the relation between the nephrotoxic effect and the concentration of sisomicin in the kidney cortical layer and blood serum demonstrates that the nephrotoxicity of the sisomicin combination with cephalothin is mainly due to a decrease in the aminoglycoside concentration in the zone of the nephrotoxic effect.

Animals↗
PubMed1979

The effect of hypotensive anesthesia on cephalothin concentrations in bone and muscle of patients undergoing total hip replacement.

Serial blood, muscle, and bone concentrations of cephalothin following intravenous infusion were determined in forty-eight patients during total hip replacement. Thirty patients received hypotensive anesthesia and the remaining eighteen received anesthesia without induced hypotension. The concentrations of cephalothin were determined during the first (early) and second (late) hours of the operation. Late serum levels were lower in the patients who had induced hypotension. In all patients at least one bone specimen contained measurable amounts of cephalothin. When pentolinium (Ansolysen) was used to induce hypotension, the late serum and early bone cephalothin concentrations were lower, while use of trimethaphan (Arfonad) did not appear to result in lower cephalothin concentrations in serum, muscle, or bone compared with patients with normotensive anesthesia.

Arthroplasty↗
PubMed1979

Comparative study of prophylactic antibiotics in cardiac surgery. Clindamycin versus cephalothin.

A randomized, prospective study of the relative effectiveness of clindamycin versus cephalothin was performed in 263 adult patients having cardiac surgery from September, 1977, to August, 1978. There were no statistically significant differences in frequency of postoperative infections in these two antibiotic groups. Wound infection developed in 6.5 percent of the cephalothin group and 3.2 percent of the clindamycin group. Urinary tract infection developed in 5.6 percent of the clindamycin group and 2.1 percent of the cephalothin group. Four bacteremic episodes occurred in the clindamycin-treated patients, and one episode of bacteremia occurred in a cephalothin-treated patient. No cases of endocarditis occurred during the study. Clindamycin deserved consideration as an alternative prophylactic agent to cephalothin for cardiac surgery.

Bacterial Infections↗
PubMed2000

Enzymatic synthesis of cephalothin by penicillin G acylase*

Enzymatic synthesis of cephalothin from 7-aminocephalosporanic acid (7-ACA) and amide derivatives of 2-thienylacetic acid (2-TA) using penicillin G acylase (pen G acylase) was studied. Two amide derivatives of 2-TA namely 2-thienylacetamide (2-TAA) and 2-thienylacetohydroxamic acid (2-TAH) were used in this study. The main reason for choosing amide but not the methyl ester derivative of 2-TA for the enzymatic synthesis was to increase their solubilities in water. The solubility of 2-TA methyl ester (2-TAM), 2-TAA, and 2-TAH in aqueous solution is 8 +/- 0.05 mM, 87 +/- 0.75 mM and 120 +/- 1.65 mM, respectively. Enzymatic conversion of 2-TAH to cephalothin yielded side products but they were not found in the conversion of 2-TAA to cephalothin. The side products were derived from reactions between hydroxyamine and 7-ACA. The effects of pH, temperature, initial substrate concentrations and reaction time on the conversion of 2-TAA and 7-ACA to cephalothin were examined. The optimum reaction condition was determined at pH 6.5 and 10 approximately 15 degrees C. The best conversion yield of 72% was obtained when the initial concentration of 2-TAA and 7-ACA was at 0.4 M and 0.1 M, respectively. Furthermore, a one-step method was developed to purify cephalothin from the enzymatic reaction mixture with the purity of 91% and the recovery yield of 96%.

Journal Article↗
PubMed1964

MORPHOLOGICAL CHANGES IN GRAM-NEGATIVE BACILLI EXPOSED TO CEPHALOTHIN.

Chang, Te-Wen (Tufts University School of Medicine, Boston, Mass.), and Louis Weinstein. Morphological changes in gram-negative bacilli exposed to cephalothin. J. Bacteriol. 88:1790-1797. 1964.-Exposure of gram-negative bacteria to cephalothin (7-[thiophene-2-acetamido]-cephalosporanic acid) revealed the formation of long filaments and large bodies, which were capable of reverting to normal cells when removed from contact with the drug. The degree of morphological change was found to be related to the concentration of antibiotic in which the organisms were suspended. The large bodies were altered by contact with solutions of varying osmolarity. Different species showed variation in the ability to develop large bodies. A relationship between antibiotic sensitivity and the capacity to resist morphological alteration was observed. Though most sensitive gram-negative bacilli were strikingly changed by exposure to cephalothin, naturally resistant ones were unaffected. Organisms made drug-resistant in vitro underwent changes in cellular form which were qualitatively the same but less intense than those which developed in parent strains originally sensitive to cephalothin.

Anti-Bacterial Agents↗
PubMedDate not supplied

Pharmacokinetic study of cefazaflur compared to cephalothin and cefazolin.

A single 1-Gm dose of cefazaflur, a new semisynthetic cephalosporin derivative, was compared in a crossover study to the same dose of cephalothin and cefazolin by intramuscular injection in seven healthy volunteers. Serum concentrations were measured at several time intervals during 6 hours following each administration. The mean peak serum levels obtained after 30 minutes were 25.2, 17.2, and 62.3 mug/ml, respectively, for cefazaflur, cephalothin, and cefazolin. In each of the seven subjects, serum concentrations were higher at each sampling time with cefazolin than with the other two cephalosporins. The percentage of total administered dose recovered in urine in a microbiologically active form for the 0-24-hour collection was, respectively, 92.7, 59.2, and 94.9 per cent with cefazaflur, cephalothin, and cefazolin, the largest part being excreted during the first 6 hours. Neither drug appeared to have any pronounced effect on various laboratory tests. Local reactions at the site of intramuscular injection were minor with cefazaflur and cefazolin, but were more pronounced with cephalothin.

Adult↗
PubMed1976

Therapy of infections in neutropenic patients: results with gentamicin in combination with cephalothin or chloramphenicol.

Gentamicin in combination with cephalothin (Gent-Ceph) or with chloramphenicol (Gent-Chloro) was utilized in the treatment of 55 infections occurring in 49 cancer patients. Responses were obtained in 78% of the infections treated with Gent-Ceph and in 64% of those treated with Gent-Chloro. Pneumonia and septicemia were the most common infections in this study. Among the cases of penumonia, 64% responded to Gent-Ceph and 67% to Gent-Chloro. Among the cases of septicemia, 88% responded to Gent-Ceph and 50% to Gent-Chloro. All of the identified organisms producing infection were gram-negative bacilli. Of these, E. coli was the most common. All organisms were resistant to cephalothin in vitro, and only 41% of them were resistant to chloramphenicol. However, resistant organisms responded significantly better to the Gent-Ceph combination (p less than 0.025). Also, response to therapy among patients with severe neutropenia (less than 100 neutrophils/mm3) was better for those patients treated with Gent-Ceph (p = 0.07). The combination of gentamicin with cephalothin or with chloramphenicol did not increase the frequency of side effects expected from gentamicin alone. No significant hematological toxicity was seen among those patients treated with chloramphenicol. Gentamicin in combination with cephalothin or chloramphenicol is an effective and safe antibiotic combination against gram-negative bacilli infections occurring in cancer patients. The efficacy of Gent-Ceph in patients with severe neutropenia is particularly advantageous.

Agranulocytosis↗
PubMed1976

Comparative clinical pharmacology of intravenous cefoxitin and cephalothin.

Intravenous doses of 0.5, 1, and 2 g cephalothin and cefoxitin, a semi-synthetic cephamycin antibiotic highly resistant to bacterial cephalosporinase, were infused over a period of 3 minutes into 18 normal adult males by a randomized, crossover design. Serum and urine data on cefoxitin best fit a two-compartment open model. Serum concentrations following cefoxitin were higher and more prolonged and urine recoveries higher than those following equal doses of cephalothin. The terminal serum half-life of cefoxitin was longer at all dose levels. Renal clearance of cephalothin-like activity exceeded that of cefoxitin, which may possess dose-dependent kinetics. Whereas cephalothin has been reported to metabolize by greater than 35% to the less active desacetyl form, cefoxitin was metabolized by 0.1 to 6% to the descarbamyl form in individual subjects.

Adult↗
PubMed1979

Preoperative prophylactic cephalothin fails to control septic complications of colorectal operations: results of controlled clinical trial. A Veterans Administration cooperative study.

Data obtained from a survey of the membership of the Society for Surgery of the Alimentary Tract and the American Society of Colon and Rectal Surgeons indicated that concomitant administration of oral neomycin-erythromycin base and systemic cephalothin, together with mechanical colon cleansing, was the most popular method of colon preparation. We designed a prospective double blind clinical trial to compare administration of intravenous cephalothin, oral neomycin-erythromycin base, and the combination of both the intravenous and oral antibiotics. Intake of patients to the intravenous cephalothin group was stopped because the data indicated that this method of prophylaxis resulted in significantly higher numbers of septic complications. The incidence of wound infection was 30 per cent and the overall incidence of septic complications was 39 per cent in patients receiving only intravenous cephalothin combined with mechanical colon cleansing. The incidence of wound infection and the overall incidence of septic complications was only 6 per cent in the comparison group, and the differences are highly significant.

Aminoglycosides↗
PubMed2006

Randomized controlled trial on prevention of postcesarean infection using penicillin and cephalothin in Brazil.

BACKGROUND: There is a need to assess the effects of different antibiotic administration models on infectious complications among women from low-income populations who undergo cesarean delivery, and the cost benefit. DESIGN: Randomized, blinded controlled clinical trial study of a single preoperative dose of cephalothin, versus a postcesarean scheme for infection prophylaxis, versus no antibiotics. METHODS: The setting was a tertiary Brazilian center with 1,500 deliveries annually. Pregnant women (n = 600) with an indication for emergency or elective cesarean section were randomly allocated consecutively to one of three groups and treated as follows: Group 1 (n = 200), no antibiotics; Group 2 (n = 200), the standard antibiotics scheme followed at this center; Group 3 (n = 200), a single dose of intravenous cephalothin 2 g, intraoperatively. MAIN OUTCOME MEASUREMENTS: Prevalences of wound infection, puerperal and postcesarean infections, and costs of antibiotics used. RESULTS: Antibiotics reduced the incidence of puerperal infection, but did not change the percentages of wound and postcesarean infections and no use of antibiotics increased the puerperal infection risk sixfold. Cephalothin reduced the relative risk of puerperal infection by 89% (95% confidence interval: 7-87%). Penicillin reduced it by 78%, but this was not statistically significant. No deaths occurred. The costs of the two schemes were similar (almost US 1.00 dollars). CONCLUSIONS. Prophylactic cephalothin use was associated with decreased postcesarean puerperal infection and presented a cost benefit.

Anti-Bacterial Agents↗
PubMed1981

Temperature effect on cephalothin sensitivity of methicillin-resistant Staphylococcus aureus.

Nineteen methicillin-resistant Staphylococcus aureus isolates from clinical specimens were tested for cephalothin sensitivity by disk diffusion and tube-dilution methods using incubation temperatures of 35 C and 30 C. Resistant colonies were observed to grow within the zones of antibiotic inhibition for 17 of the 19 isolates at 30 C but not at 35 C incubation. Twenty control strains known to be methicillin-sensitive did not show these resistant colonies at 30 C. Five of the methicillin-resistant isolates were sensitive, one of intermediate sensitivity to cephalothin, and the rest were resistent by tube-dilution testing at 35 C. At 30 C, however, two isolates were of intermediate sensitivity, and the rest were resistant to cephalothin by tube-dilution testing. These observations strongly suggest that the 30 C incubation temperature is more reliable in detecting in-vitro resistance of methicillin-resistant strains of Staphylococcus aureus to cephalothin in agar as well as in liquid media.

Cephalothin↗
PubMed1975

Experimental osteomyelitis. IV. Therapeutic trials with rifampin alone and in combination with gentamicin, sisomicin, and cephalothin.

Levels of rifampin, gentamicin, sisomicin, and cephalothin in normal and osteomyelitic rabbit bones were measured, and the efficacy of these drugs in the treatment of osteomyelitis was evaluated. Single drug regimens, including rifampin for 14 days and gentamicin, sisomicin, and cephalothin each for 28 days, were relatively ineffective (5%-33% sterile bone cultures). Rifampin, administered for 28 days, sterilized the bones of 55% of treated animals. The combination of gentamicin and rifampin, given for either 14 or 28 days, sterilized the bones of 67% of treated animals. The combinations of rifampin plus sisomicin and of rifampin plus cephalothin, given for 28 days, were significantly more effective than these agents alone, sterilizing 90%-95% of bones. The combination of rifampin, sisomicin, and cephalothin, given for only 14 days, sterilized the bones of all treated rabbits. Staphylococci isolated from the bones of therapeutic failures that had received rifampin alone or in combination with other antibiotics were highly resistant to rifampin (minimal inhibitory concentration, greater than 250 mug/ml), whereas the organisms recovered from animals not receiving rifampin remained sensitive. Results of in vitro studies of synergy and/or bactericidal activity of antibiotic combinations correlated with in vivo results in some, but not all, instances.

Animals↗