Orally active semisynthetic cephalosporin antibiotic with broad-spectrum activity.
A semisynthetic cephalosporin antibiotic with antimicrobial activity similar to that of CEPHALORIDINE or CEPHALOTHIN, but somewhat less potent. It is effective against both gram-positive and gram-negative organisms.
A group of broad-spectrum antibiotics first isolated from the Mediterranean fungus ACREMONIUM. They contain the beta-lactam moiety thia-azabicyclo-octenecarboxylic acid also called 7-aminocephalosporanic acid.
A semisynthetic cephalosporin analog with broad-spectrum antibiotic action due to inhibition of bacterial cell wall synthesis. It attains high serum levels and is excreted quickly via the urine.
One of the three domains of life (the others being Eukarya and ARCHAEA), also called Eubacteria. They are unicellular prokaryotic microorganisms which generally possess rigid cell walls, multiply by cell division, and exhibit three principal forms: round or coccal, rodlike or bacillary, and spiral or spirochetal. Bacteria can be classified by their response to OXYGEN: aerobic, anaerobic, or facultatively anaerobic; by the mode by which they obtain their energy: chemotrophy (via chemical reaction) or PHOTOTROPHY (via light reaction); for chemotrophs by their source of chemical energy: CHEMOLITHOTROPHY (from inorganic compounds) or chemoorganotrophy (from organic compounds); and by their source for CARBON; NITROGEN; etc.; HETEROTROPHY (from organic sources) or AUTOTROPHY (from CARBON DIOXIDE). They can also be classified by whether or not they stain (based on the structure of their CELL WALLS) with CRYSTAL VIOLET dye: gram-negative or gram-positive.
The giving of drugs, chemicals, or other substances by mouth.

Cefatrizine activity compared with that of other cephalosporins. (1/4)

Cefatrizine, a new orally administered cephalosporin, was tested against 400 clinical isolates. Cefatrizine had excellent activity against gram-positive cocci, inhibiting all except enterococci at minimal inhibitory concentrations below 1 mug/ml. Cefatrizine inhibited the majority of Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, and Salmonella at concentrations below 12.5 mug/ml. Although cefatrizine was not hydrolyzed by many beta-lactamases, it did not inhibit a number of strains of Enterobacter, Serratia, or indole-positive Proteus. Cefatrizine was more active than cephalothin or cephalexin against E. coli, Klebsiella, Enterobacter, Citrobacter, Salmonella, and Shigella. Its overall activity was less than that of cefoxitin against strains resistant to cephalothin, but its activity against cephalothin-susceptible strains was equivalent to that of cefamandole.  (+info)

Human intravenous pharmacokinetics and absolute oral bioavailability of cefatrizine. (2/4)

Cefatrizine was administered intravenously and orally at dose levels of 250, 500, and 1,000 mg to normal male volunteers in a crossover study. Intravenous pharmacokinetics were dose linear over this range; mean peak plasma concentrations at the end of 30-min infusions were, respectively, 18, 37, and 75 micrograms/ml, total body clearance was 218 ml/min per 1.73 m2, renal clearance was 176 ml/min per 1.73 m2, and mean retention time in the body was 1.11 h. Cumulative urinary excretion of intact cefatrizine was 80% of the dose, and half-lives ranged from 1 to 1.4 h. Steady-state volume of distribution was 0.22 liters/kg. On oral administration, the absolute bioavailabilities of cefatrizine were 75% at 250 and 500 mg and 50% at 1,000 mg. The mean peak plasma concentrations and peak times were, respectively, 4.9, 8.6, and 10.2 micrograms/ml at 1.4, 1.6, and 2.0 h, mean residence times were 2.4, 2.6, and 3.1 h, and mean absorption times were 1.3, 1.6, and 1.9 h. Oral renal clearance and half-life values corresponded well to the intravenous values. Cumulative urinary excretion of intact cefatrizine (as percentage of dose) was 60 at 250 mg, 56 at 500 mg, and 42 at 1,000 mg. It is hypothesized that the lack of oral dose linearity between the 500- and 1,000-mg doses is due to a component of cefatrizine absorption by a saturable transport process. Relative absorption at the high dose would be sufficiently slow that an absorption "window" would be passed before maximum bioavailability could be attained. It is not expected that the observed bioavailability decrease at doses exceeding 500 mg will have any therapeutic significance, since clinical studies are establishing efficacy for a recommended unit dosage regimen of 500 mg.  (+info)

In vitro activities of five oral cephalosporins against aerobic pathogenic bacteria. (3/4)

Cefaclor (Lilly 99638) and cefatrizine (BL-S640, SK&F 70771) are orally absorbed, broad-spectrum semisynthetic cephalosporins. They were compared in vitro with cephalexin, cephaloglycin, and cepharadine against a variety of aerobic pathogenic bacteria by an agar dilution procedure. Cefaclor and cefatrizine were found to be similar or superior to cephalexin, cephaloglycin, and cephradine in terms of activity against gram-positive cocci other than enterococci. Only cefatrizine demonstrated any potentially useful activity against some susceptible isolates of enterococci. Cefaclor and cefatrizine also were highly active, equally or more so than the other oral cephalosporins, against several gram-negative species including Escherichia coli, Enterobacter aerogenes, and Klebsiella pneumoniae. None of the cephalosporins were particularly active against Enterobacter cloacae. Both cefaclor and cefatrizine were active against Proteus mirabilis; cefatrizine was uniquely active against indolepositive Proteus species.  (+info)

In-vitro activity of 21 beta-lactam antibiotics against penicillin-susceptible and penicillin-resistant Streptococcus pneumoniae. (4/4)

MICs of 21 beta-lactams were determined by agar dilution against 283 penicillin-susceptible (pen-S), 122 intermediate (pen-I) and 23 fully penicillin-resistant (pen-R) pneumococci. MICs of all beta-lactams increased with increasing MICs of penicillin. Clometocillin was the most active penicillin against pen-I or pen-R pneumococci. All oral cephalosporins except cefuroxime and cefpodoxime were less active than penicillin and none was satisfactory against pen-I or pen-R pneumococci. The parenteral third- and fourth-generation cephalosporins (except ceftazidime) were similar in activity to penicillin against pen-S isolates. Cefpirome showed the lowest mean MICs against pen-I and pen-R strains.  (+info)

This is an open-label, single-centre, non-randomized study to investigate the pharmacokinetics of GSK3191607, administered as a single intravenous (IV) dose in
ABSTRACT. Diminazene remains one of South Africas most commonly used antiprotozoal agents for the management of babesiosis in dogs . Although the drug has been on the market for over 40 years, its intravenous pharmacokinetics are poorly known. To better understand the pharmacokinetics of the drug Berenil®, it was reconstituted in sterile water and administered intravenously to 6 adult German shepherd dogs. All 6 dogs demonstrated the previously described secondary peak in the plasma concentration versus time profile. The plasma pharmacokinetics for diminazene are described by both non-compartmental and compartmental models. From non-compartmental analysis, the area under curve to the last sample point (AUQast), clearance (CL) and volume of distribution (Vz) were 4.65 ± 1.95 ng/ml/h, 0.77 ± 0.18 l/kg/h and2.28 ± 0.60 l/kg respectively. For compartmental modelling, the plasma concentrations were fitted to both a 2-compartmental open model and a recirculatory enterohepatic model. From the ...
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TY - JOUR. T1 - Physicochemical properties of amphoteric β-lactam antibiotics. IV. First- and second-order degradations of cefaclor and cefatrizine in aqueous solution and kinetic interpretation of the intestinal absorption and degradation of the concentrated antibiotics. AU - Nakashima, E.. AU - Tsuji, A.. AU - Nakamura, M.. AU - Yamana, T.. PY - 1985. Y1 - 1985. N2 - A kinetic study on the degradations of cefaclor and cefatrizine was carried out at 35°C as a function of pH and initial drug concentration by the use of high-performance liquid chromatography. At constant pH and temperature, the degradation followed pseudo-first-order kinetics at the initial concentration of 5 mM. The shape of the rate-constant-pH profile of cefaclor resembled those for cefatrizine and other aminocephalosporins. At neutral pH, cefaclor was degraded via intramolecular nucleophilic attack of the α-amino group on the β-lactam moiety. The intramolecular reaction rate was very similar to that in the cases of ...
TY - JOUR. T1 - Characterization of the Oral Absorption of β-Lactam Antibiotics. I. Cephalosporins. T2 - Determination of Intrinsic Membrane Absorption Parameters in the Rat Intestine In Situ. AU - Sinko, Patrick J.. PY - 1988/10. Y1 - 1988/10. N2 - The oral absorption of five cephalosporin antibiotics, cefaclor, cefadroxil, cefatrizine, cephalexin, and cephradine, has been studied using a single-pass intestinal perfusion technique in rats. Intrinsic membrane absorption parameters, unbiased by the presence of an aqueous permeability (diffusion or stagnant layer), have been calculated utilizing a boundary layer mathematical model. The resultant intrinsic membrane absorption parameters are consistent with a significant carrier-mediated, Michaelis-Menten-type kinetic mechanism and a small passive component in the jejunum. Cefaclor colon permeability is low and does not exhibit concentration dependent behavior. The measured carrier parameters (±SD) for the jejunal perfusions are as follows: ...
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... is a broad-spectrum cephalosporin antibiotic. Dunn GL, Hoover JR, Berges DA, Taggart JJ, Davis LD, Dietz EM, et al ... Structure-activity studies related to cefatrizine (SK&F 60771)". The Journal of Antibiotics. 29 (1): 65-80. doi:10.7164/ ...
The molecular formula C18H18N6O5S2 (molar mass: 462.505 g/mol) may refer to: Cefamandole Cefatrizine This set index page lists ...
... cefatrizine (INN) cefazaflur (INN) cefazedone (INN) cefazolin (INN) cefbuperazone (INN) cefcanel daloxate (INN) cefcanel (INN) ...
... may refer to: (-)-2β-Carbomethoxy-3β-(4-fluorophenyl)tropane Cefatrizine, a cephalosporin antibiotic Crystal field theory, ...
... cefatrizine MeSH D02.065.589.099.249.200.180 - cephaloglycin MeSH D02.065.589.099.249.200.185 - cephradine MeSH D02.065.589.099 ...
Cefalexin J01DB02 Cefaloridine J01DB03 Cefalotin J01DB04 Cefazolin J01DB05 Cefadroxil J01DB06 Cefazedone J01DB07 Cefatrizine ...
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Cefatrizine - Preferred Concept UI. M0003717. Scope note. Orally active semisynthetic cephalosporin antibiotic with broad- ...
Cefatrizine (substance). Code System Preferred Concept Name. Cefatrizine (substance). Concept Status. Published. ...
InChI=1S/C25H27N9O8S2/c1-3-32-8-9-33(21(39)20(32)38)24(42)27-15(12-4-6-14(35)7-5-12)18(36)26-16-19(37)34-17(23(40)41)13(10-43-22(16)34)11-44-25-28-29-30-31(25)2/h4-7,15-16,22,35H,3,8-11H2,1-2H3,(H,26,36)(H,27,42)(H,40,41)/t15-,16-,22-/m1/s1 ...
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Cefatrizine .. BL-S 640 .. BL-S640 .. S 640-P .. S-640P .. SK&F-60771 .. SKF-60771 .. BL S 640 .. BL S640 .. BLS 640 .. BLS640 ... D02.886.665.074.200.165.125 Cefatrizine .. D03 Heterocyclic Compounds .. D03.066 Acids, Heterocyclic .. D03.066.160 Cinoxacin . ... D03.633.100.300.249.200.165.125 Cefatrizine .. D03.633.300 Heterocyclic Compounds, 3-Ring .. D03.633.300.160 Cinoxacin .. G07 ... D02.065.589.099.249.200.165.125 Cefatrizine .. D02.241 Carboxylic Acids .. D02.241.081 Acids, Acyclic .. D02.241.081.114 ...
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Brief summary - 1,8-Naphthyridine 1,8-Naphthyridine is an organic compound with the formula C8H6N2. It is the most well-studied of the six isomeric naphthyridines, a subset of diazanaphthalenes with nitrogen in the separate rings. Enoxacin, nalidixic acid, and trovafloxacin are 1,8-naphthyridine derivatives with antibacterial properties related to the fluoroquinolones.
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