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A method was developed to determine cefazolin in serum or urine. The drug is extracted from serum or urine with ethyl acetate, separated by TLC, and determined by fluorescence quenching densitometry. The method was developed to study the pharmacokinetics of the compound in humans.
The solid-state 13C-NMR spectra of the polymorphs of benoxaprofen, nabilone, and cefazolin are reported using the cross-polarization/magic-angle spinning (CP/MAS) technique. In general, the spectra of the different crystal forms are different. In favorable cases the spectra of the drug in a pharmaceutical granulation can be discerned. These results provide a preliminary indication that solid-state NMR spectroscopy is a useful technique for the investigation of drug polymorphs and drugs in their dosage forms.
By simultaneously performing broth dilution, agar dilution, and agar diffusion tests with Bacteroidaceae and Peptococcaceae, the influence of methodology upon the outcome of susceptibility testing to cefazolin, cefamandole and cefoxitin was studied. With beta-lactamase positive and negative Bacteroidaceae, the results of the broth dilution and agar dilution tests were in good agreement for cefoxitin. However, when tested with cefaxolin and cefamandole, beta-lactamase positive Bacteroides strains had mostly high broth dilution MICs and relatively low agar dilution MICs. The statistical analysis of the relationship between zone size and broth dilution or agar dilution MICs frequently showed lack of stochastic linearity or relatively low correlation coefficients.
The activity of cefazolin (CEZ) and cephradine (CED) was studied in experimentally infected neutropenic mice. Neutropenia was induced by 600 rad whole-body irradiation; an infection was induced by the injection of 5 X 10(6) Escherichia coli into the thigh on Day 5 after irradiation. Antibiotics were administered 1 h later, and antibacterial activity was estimated from bacteria counts made in the homogenized individual thighs 3 h after infection. The effect of a low dose of each of the cephalosporins on the infection was significantly lower in the absence of granulocytes than in animals with intact host defence; at higher dosages the effect of both antibiotics on the infection was the same in neutropenic and unirradiated mice. In the neutropenic mice, CEZ was 2.95 times more active than CED against E. coli in vivo, this difference in activity being similar to that found earlier in normal mice.
Two strains each of sensitive, penicillinase-producing, methicillin-resistant and "tolerant" Staphylococcus aureus were used to infect mice intramuscularly. The mice were then treated with three doses each of fosfomycin, vancomycin, rifampicin, fusidic acid, penicillin G, flucloxacillin or cefazolin intravenously. Infections due to sensitive strains were effectively treated with all antibiotics investigated except fusidic acid. Fosfomycin, vancomycin, rifampicin and flucloxacillin showed the best activity against penicillinase-producing strains. Fosfomycin and vancomycin were equally effective against infections due to methicillin-resistant S. aureus. Infections caused by "tolerant" strains again responded best to fosfomycin, vancomycin and rifampicin.
A 43-year-old patient with preexisting mitral valve prolapse and Cardiobacterium hominis endocarditis with partial destruction of the posterior mitral valve leaflet is described. Successful treatment was achieved with partial resection of the posterior mitral valve leaflet and antibiotic therapy. Because of a hypersensitivity reaction, initial therapy with penicillin G and gentamicin was stopped and substituted with cefazolin. No relapse of endocarditis was observed after 12 months of follow-up. Using micro broth dilution technique the isolated strain was shown to be most susceptible to penicillin G, cephalothin, and ciprofloxacin, with minimal inhibitory concentrations of 0.00025, 0.004, and 0.002 mg/l, respectively; and with minimal bactericidal concentrations (99.9% killing) of 0.25, 0.12, and 0.008 mg/l, respectively. We conclude that cephalosporins of the first generation or ciprofloxacin may be good alternatives to penicillin G in the treatment of C. hominis infection in patients known to be hypersensitive to penicillin.
Three initial treatment schedules of peritonitis during continuous ambulatory peritoneal dialysis are analysed. In 20 patients 56 episodes of peritonitis were treated by co-trimoxazole, 29 episodes in 20 patients by cefazolin, and 29 infections in 22 patients by vancomycin. The efficiency of the treatment modes was comparable. Vancomycin was found to be appropriate in particular because of the resistance characteristics of bacterial isolates.
A prospective, double-blind, randomized study was undertaken to compare perioperative parenteral metronidazole and erythromycin, One neomycin, and cefazolinhundred fifty-five patients were randomized into two groups by the pharmacy department. The resulting difference between the overall septic complication rate in patients receiving erythromycin, neomycin, and cefazolin (10.9 percent) and the rate in patients receiving metronidazole alone (31.9 percent) was significant. This indicates that an antibiotic to cover aerobic bacteria should be added to the regimen when metronidazole is used.
The effect of unreacted residual 2-mercapto-5-methyl-1,3,4-thiadiazole (MMTD), the reagent for 3-[5-methyl-1,3,4-thiadiazole-2-yl]-7-aminocephalosporanic acid (M-7-ACA) synthesis, on the enzymatic acylation of M-7-ACA by the methyl ester of 1,2,3,4-tetrazol-1-acetic acid (MeTzAA) to produce cefazolin (CEZ) was studied. In the two-step process of synthesizing CEZ from 7-aminocephalosporanic acid (7-ACA), one of the key parameters controlling the overall CEZ yield was the ratio of MMTD to 7-ACA in M-7-ACA synthesis. The increase of the ratio showed opposing effects by increasing the M-7-ACA yield in the first step, while decreasing CEZ yield in the subsequent enzymatic reaction by the inhibitory effect of the increased content of MMTD as an impurity in the M-7-ACA preparation. It was revealed that the decrease of CEZ yield in the enzymatic reaction was caused by the selective retardation of the rate of CEZ synthesis reaction by a typical competitive inhibition, while not affecting the rate of MeTzAA hydrolysis reaction. The optimum MMTD-to-7-ACA ratio rendering the highest overall CEZ yield over 7-ACA was 1.2:1.
Conventional microbiological assay procedures for cephalosporins in serum do not allow the determination of serum concentrations if more than one cephalosporin is present in a single sample. An HPLC procedure has been developed which permits the simultaneous quantitative determination of cefazolin sodium and cephalothin sodium in serum. Reverse phase chromatography using methanol in 0.2 M ammonium acetate as the mobile phase was employed to separate and quantitate the two cephalosporins in a trichloroacetic acid supernatant solution prepared from serum.
Infection has been one of the most common causes of problems and complications after the operation despite the advance in surgical techniques and the availability of newly developed antibiotics. Local antibiotic delivery beads for treatment of various surgical infections had been studied recently especially in osteomyelitis. This current paper used cefazolin sodium and gentamicin sulfate combined with biodegradable polymers (50:50 poly(DL-lactide):co-glycolide) as antibiotic beads for a long-term drug release. To manufacture an antibiotic bead, polylactide-polyglycolide copolymers were mixed with the antibiotics. The mixture was compressed and sintered at 55 degrees C to form beads of different sizes. The beads were placed in 3 ml of phosphate buffered saline and incubated at 37 degrees C. An elution method combined with a bacterial inhibitory test was employed to characterize the release rate of the antibiotics over a 30-day period. The results suggested that the biodegradable beads released high concentrations of antibiotic (well above the minimum inhibitory concentration) in vitro for the period of time needed to treat bone infection; i.e. 2-4 weeks. This provides advantages as a first line choice of long-term antibiotics for patients with osteomyelitis and various infections such as thoracic, abdominal, and pelvic infections, as well as for the prophylaxis of these infections.
Moxalactam is a newer beta-lactam antibiotic with increased activity and an extended antimicrobial spectrum. Three 1 gm doses were given to women scheduled for elective vaginal hysterectomy. This perioperative regimen was prospectively compared to identical doses of cefazolin, a first-generation cephalosporin of proved efficacy. The overall incidence of major postoperative infection in 193 women was less than 5% and there were no significant interregimen differences. The incidence of major infection was directly related to the type of procedure performed.
Corneal iontophoresis produces high concentrations of drugs in the anterior segment but not in the vitreous humor of the phakic eye, presumably because transport is impeded by the lens-iris barrier. We have used two modifications to produce high levels of commonly used antibiotics in the vitreous humor of the phakic rabbit eye: the device is placed over the pars plana, circumventing the lens-iris barrier; the contact area of the column of fluid is kept small (less than or equal to 1 mm diameter) so as to provide a high current density. Applying 2 mAmp for 10 minutes, we were able to achieve mean vitreal concentrations of cefazolin, ticarcillin, and gentamicin of 94-207 micrograms/ml in the normal rabbit eye. Drug penetration showed a correlation with strength of current (0.1-2 mAmp) and with duration of iontophoresis (1-10 minutes) but not with concentration of the drug solution. Transscleral iontophoresis is a promising noninvasive technique to achieve high vitreal levels of charged solutes.
Antibacterial activity of four crystalline modifications (ground, solvated and two desolvated) of cefazolin sodium (CZS) have been studied. Their antibacterial properties have been determined by means of minimal inhibitory concentrations (MIC(50) and MIC(90)) and of disk diffusion inhibition zone values. The above-mentioned crystalline modifications (Mod.) of CZS-I, II, III and IV, respectively, have been shown to have differences in their antibacterial properties in comparison with the trade CZS as well as between themselves. Mod. I has higher or the same activity as CZS. The obtained results we have explained with the formation of different intermolecular H-bonds in the modifications could be due to the rotation about C(alpha)- C' and C-N bonds in the amide groups in their molecules.
A rapid, specific and very sensitive liquid chromatographic assay using standard ultraviolet detection has been developed to measure cefazolin (CFZ) or ceftriaxone (CFX) in small samples (200 microl) of plasma using either drug as the internal standard for measurement of the other. A rapid extraction was performed using C18 bonded Sep Pak cartridges with high extraction efficiency for both drugs. The chromatographic system employed the use of a Nova-Pak C18 4-microm cartridge with a radial compression system preceded by a Guard-Pak with a C18 insert. The mobile phase consisted of an aqueous solution containing 10 mM of dibasic potassium phosphate and 10 mM cetyltrimethylammonium bromide (pH 6.5) with acetonitrile (73:27 v/v). The drug and internal standard (CFZ/CFX) were detected using a UV detector set at a wavelength of 274 nm. Assay results were linearly related to the concentration (r > 0.997) for the wide range which was examined (0.005-120 microg/ml) for either drug. We report the precision, accuracy, recovery, linearity, sensitivity and specificity of this assay. The intra-run and inter-run CV was less than 9.02%. This method is currently being used for clinical therapeutic monitoring and pharmacokinetic studies of CFZ and CFX in patients undergoing cesarean section.
One thousand thirty-seven cefazolin-resistant, gram-negative clinical isolates including members of the family Enterobacteriaceae, pseudomonads, and other nonfermenters were tested against a variety of newer antimicrobial agents by microdilution. Most of the Enterobacteriaceae were resistant to the second-generation cephalosporins, but highly susceptible to the third-generation agents and the broad-spectrum penicillins, 90% of the strains being inhibited at attainable serum concentrations. Cefoperazone and the penicillins had good activity against the Pseudomonas species, but the aminoglycosides remained the most active agents against all the gram-negative bacilli tested except Pseudomonas maltophilia.
In a prospective randomized two center trial, short-term prophylaxis with cefuroxime (CFX) in 189 patients was compared with cefazolin (CFZ) in 196 patients submitted to elective cardiac surgery. A total of 3 g was administered over 24 h in both groups. One major adverse reaction with CFX was noted. Patients were prospectively screened by infectious disease nurses for surgical wound and secondary infections. Sternal wound infections occurred in eight patients treated with CFX and all were minor. One patient from this group eventually died of infectious causes. In the CFZ-treated patients two major and six minor wound infections occurred requiring extensive debridement in two. Secondary infections occurred less frequently in the CFX group (13.2 per 100) than in the CFZ group (16.8 per 100) with two infection-related deaths in the CFX and one in the CFZ group. The most commonly identified organisms were Staphylococcus aureus and a variety of gram-negative organisms. No major differences were observed between the CFX and CFZ groups. Short-term administration of 3 g CFZ or CFX in this study could not demonstrate the advantage of one of the antibiotics used over the other in terms of clinical outcome, incidence or site of infection or organisms identified. The 24 h administration of 3 g CFZ or CFX provided suboptimal prophylaxis for wound infection or secondary infections in patients undergoing elective open heart surgery.
The hygroscopicity behavior of the pentahydrate, monohydrate, amorphous, and dehydrated forms of solid cefazolin sodium (CEZ) was studied under different relative humidity (RH) conditions. Between 42 and 86% RH, the pentahydrate (alpha form), the monohydrate, and their dehydrated forms absorbed atmospheric moisture equivalent to their hydrate numbers. The pentahydrate demonstrated a hysteresis effect at 15 and 31% RH. On the other hand, the water content of the amorphous form increased linearly with increases in RH. The noncrystalline state was maintained below 56% RH. For the dehydrated alpha form there was a distinct birefringence when viewed under polarizing light, the X-ray diffraction pattern was weak and diffuse, and the infrared (IR) spectra were discernibly different from that of the amorphous form. The freeze-dried CEZ showed hygroscopic behavior almost similar to that of the dehydrated alpha form. Two-component mixtures of various CEZ forms showed a linear relationship between the water content and the mixing ratio when stored at 31, 42, and 56% RH. From the hygroscopicity data, the crystallinity of freeze-dried CEZ could be estimated as the percentage of the dehydrated alpha form.