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Chemical Compound Review

Haloapor     (6R,7S)-7-[2-(2-amino-1,3- thiazol-4...

Synonyms: cefotiam, Ceradolan, Ceradon, Cefotiamum, Aspil, ...
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Disease relevance of SCE 963


High impact information on SCE 963


Chemical compound and disease context of SCE 963


Biological context of SCE 963

  • Cefotiam obeyed two-compartment model kinetics in all three groups [14].
  • Acylation of 7-AACA with various beta-ketoacids followed by substitution at the 3'-position led to 7 beta-[2-(2-aminothiazol-4-yl)acetamido]-3-[[1-(2-dimethylaminoethyl)-1H-tetrazol-5-yl]thiomethyl]ceph-3-em-4-carboxylic acid (SCE-963, cefotiam), a potent broad-spectrum cephalosporin [15].
  • 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 [16].
  • 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) [17].
  • 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 [18].

Anatomical context of SCE 963

  • 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 [10].
  • High concentrations of cefotiam are observed in several tissues (kidney, heart, ear, prostate and genital tract) as well as in fluids and secretions (bile, ascitic fluid) [8].
  • The systemic absorption of 2 antibiotics (gentamicin and cefotiam) injected into paralysed muscle is also impaired in patients with spinal cord injury, suggesting that a decrease in therapeutic efficacy attributable to this mode of administration may be anticipated [19].
  • Cefotiam concentrations in bile and in the wall of the gallbladder in patients with biliary disease [20].
  • A high-performance liquid chromatographic method is described for the simultaneous determinations of cefsulodin and cefotiam in serum and bone marrow blood samples [21].

Associations of SCE 963 with other chemical compounds

  • The in vitro activity of cefoperazone (CPZ) and cefotiam (CTM) was compared to other available cephalosporins [22].
  • 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 [16].
  • Chemiluminescence of PMN when stimulated by S. aureus treated with more than 0.156 mg/L cefodizime (1/64 MIC) or 1.25 mg/L cefotiam (MIC) increased significantly compared with the untreated cells [23].
  • 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 [24].
  • The studied cephalosporins (with the exception of cefotiam and cefsulodin) were separated from compounds present in biological fluids on 5-microns LiChrosorb RP-18 using the mobile phase 0.2% of 1.8 M H2SO4 in a mixture of methanol and water with various methanol contents [25].

Gene context of SCE 963

  • The activity of cefotiam on beta-lactamase-producing bacteria in an in-vitro model [26].
  • The renal clearance of cefotiam (CLR = 133 ml/min) was an order of magnitude greater than its biliary clearance (CLB = 11.8 ml/min) [27].
  • Most of the carbapenems potentiated the antibacterial activities of ampicillin and cefotiam against beta-lactamase-producing bacteria [28].
  • Orally active 1-(alkyl substituted cyclohexyloxycarbonyloxy)alkyl ester prodrugs (9b-h) of 7 beta-[2-(2-aminothiazol-4-yl)acetamido]-3- [[[1-(2-dimethylaminoethyl)-1H-tetrazol-5-yl]thio]-methyl]ceph+ ++-3- em-4-carboxylic acid (cefotiam, CTM) have been studied as well as the thia (9i) and aza (9j) analogs [29].
  • The activity of rosoxacin, fosfomycin, cefotiam, and spectinomycin on beta-lactamase producing Neisseria gonorrhoeae [30].

Analytical, diagnostic and therapeutic context of SCE 963

  • Pharmacokinetics of cefotiam in patients with impaired renal function and in those undergoing hemodialysis [14].
  • The cefotiam levels in the plasma of mice that received the regimen effective when initiated at 18 h after infection were less than the expected levels in humans after intravenous infusion of the usual clinical dose [31].
  • 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 [10].
  • The results suggest that the dosage calculation of cefotiam, a hydrophilic antibiotic, should be made on the basis of body surface area in morbidly obese athlete or sumo wrestler patients [9].
  • The concentrations of cefsulodin and cefotiam, concurrently administered by the intravenous route to patients subjected to artificial total joint prosthesis, in serum and bone marrow blood collected at 0.5 and 1 hr postinjection were almost equivalent [21].


  1. Synthesis and biological activities of the Z isomers of carbapenem antibiotics. Harada, S., Tsubotani, S., Asai, M., Okonogi, K., Kondo, M. J. Med. Chem. (1983) [Pubmed]
  2. Cefotiam therapy of lower respiratory tract infections. Polis, M.A., Tuazon, C.U. Antimicrob. Agents Chemother. (1985) [Pubmed]
  3. Ceftizoxime (FK 749), a new parenteral cephalosporin: in vitro and in vivo antibacterial activities. Kamimura, T., Matsumoto, Y., Okada, N., Mine, Y., Nishida, M., Goto, S., Kuwahara, S. Antimicrob. Agents Chemother. (1979) [Pubmed]
  4. In vitro and in vivo morphological response of Klebsiella pneumoniae to cefotiam and cefazolin. Nakao, M., Nishi, T., Tsuchiya, K. Antimicrob. Agents Chemother. (1981) [Pubmed]
  5. Autolysis of methicillin-resistant Staphylococcus aureus is involved in synergism between imipenem and cefotiam. Matsuda, K., Nakamura, K., Adachi, Y., Inoue, M., Kawakami, M. Antimicrob. Agents Chemother. (1995) [Pubmed]
  6. Cefuroxime axetil. A review of its antibacterial activity, pharmacokinetic properties and therapeutic efficacy. Perry, C.M., Brogden, R.N. Drugs (1996) [Pubmed]
  7. TOC-39, a novel parenteral broad-spectrum cephalosporin with excellent activity against methicillin-resistant Staphylococcus aureus. Hanaki, H., Akagi, H., Masaru, Y., Otani, T., Hyodo, A., Hiramatsu, K. Antimicrob. Agents Chemother. (1995) [Pubmed]
  8. Clinical pharmacokinetics of cefotiam. Brogard, J.M., Jehl, F., Willemin, B., Lamalle, A.M., Blickle, J.F., Monteil, H. Clinical pharmacokinetics. (1989) [Pubmed]
  9. Cefotiam disposition in markedly obese athlete patients, Japanese sumo wrestlers. Chiba, K., Tsuchiya, M., Kato, J., Ochi, K., Kawa, Z., Ishizaki, T. Antimicrob. Agents Chemother. (1989) [Pubmed]
  10. Comparative activities of cefotiam and cefazolin against urinary tract infections with Proteus mirabilis in mice. Iwahi, T., Tsuchiya, K. Antimicrob. Agents Chemother. (1980) [Pubmed]
  11. SCE-963, a new potent cephalosporin with high affinity for penicillin-binding proteins 1 and 3 of Escherichia coli. Nozaki, Y., Imada, A., Yoneda, M. Antimicrob. Agents Chemother. (1979) [Pubmed]
  12. Antibacterial activity of cefpodoxime proxetil in a pharmacokinetic in-vitro model. Wiedemann, B., Jansen, A. J. Antimicrob. Chemother. (1990) [Pubmed]
  13. Cephalosporins. VII. Synthesis and antibacterial activity of new cephalosporins bearing a 2-imino-3-hydroxythiazoline (2-aminothiazole N-oxide) in the C-7 acylamino side chain. Perrone, E., Alpegiani, M., Giudici, F., Buzzetti, F., Nannini, G., Meinardi, G., Grasso, S., Bianchi, A., de Carneri, I. J. Antibiot. (1984) [Pubmed]
  14. Pharmacokinetics of cefotiam in patients with impaired renal function and in those undergoing hemodialysis. Konishi, K., Ozawa, Y. Antimicrob. Agents Chemother. (1984) [Pubmed]
  15. An approach to broad-spectrum cephalosporins. Morita, K., Nomura, H., Numata, M., Ochiai, M., Yoneda, M. Philos. Trans. R. Soc. Lond., B, Biol. Sci. (1980) [Pubmed]
  16. Synergic activity of imipenem/cilastatin combined with cefotiam against methicillin-resistant Staphylococcus aureus. Oka, S., Goto, M., Kaji, Y., Kimura, S., Matsuda, K., Asahi, Y., Sanada, M., Nakagawa, S., Inoue, M., Shimada, K. J. Antimicrob. Chemother. (1993) [Pubmed]
  17. The blood binding of cefotiam and cyclohexanol, metabolites of the prodrug cefotiam hexetil, in-vitro. Querol-Ferrer, V., Zini, R., Tillement, J.P. J. Pharm. Pharmacol. (1991) [Pubmed]
  18. Skin tissue fluid levels of cefotiam in healthy man following oral cefotiam hexetil. Korting, H.C., Schäfer-Korting, M., Kees, F., Lukacs, A., Grobecker, H. Eur. J. Clin. Pharmacol. (1990) [Pubmed]
  19. Clinical pharmacokinetics in patients with spinal cord injuries. Segal, J.L., Brunnemann, S.R. Clinical pharmacokinetics. (1989) [Pubmed]
  20. Cefotiam concentrations in bile and in the wall of the gallbladder in patients with biliary disease. Satake, K., Cho, K., Taniura, M., Oka, I., Koo, I. J. Antimicrob. Chemother. (1982) [Pubmed]
  21. Simultaneous determinations of cefsulodin and cefotiam in serum and bone marrow blood by high-performance liquid chromatography. Yamamura, K., Nakao, M., Yamada, J., Yotsuyanagi, T. Journal of pharmaceutical sciences. (1983) [Pubmed]
  22. Cefoperazone and cefotiam--two new cephalosporins: an in-vitro comparison. Wise, R., Andrews, J.M., Bedford, K.A. J. Antimicrob. Chemother. (1981) [Pubmed]
  23. Electrophoretic mobility of cefodizime-treated Staphylococcus aureus and chemiluminescence of human polymorphonuclear leucocytes. Muratsugu, M., Tomonaga, M., Miyake, Y., Terayama, K., Ishida, N. J. Antimicrob. Chemother. (1991) [Pubmed]
  24. Automated high-performance liquid chromatographic method for the simultaneous determination of cefotiam and delta 3-cefotiam in human plasma using column switching. Yamashita, K., Motohashi, M., Yashiki, T. J. Chromatogr. (1992) [Pubmed]
  25. Systematic approach to the determination of cephalosporins in biological fluids by reversed-phase liquid chromatography. Rouan, M.C., Abadie, F., Leclerc, A., Juge, F. J. Chromatogr. (1983) [Pubmed]
  26. The activity of cefotiam on beta-lactamase-producing bacteria in an in-vitro model. Wiedemann, B., Seeberg, A.H. J. Antimicrob. Chemother. (1984) [Pubmed]
  27. Pharmacokinetics and quantitative characterization of cefotiam excretion after intravenous administration to patients after cholecystectomy. Terziivanov, D., Gerova, Z., Vlahov, V., Merdzhanov, A., Damjanov, D. Eur. J. Clin. Pharmacol. (1986) [Pubmed]
  28. Beta-lactamase inhibitory activities and synergistic effects of 5,6-cis-carbapenem antibiotics. Okonogi, K., Harada, S., Shinagawa, S., Imada, A., Kuno, M. J. Antibiot. (1982) [Pubmed]
  29. Orally active 1-(cyclohexyloxycarbonyloxy)alkyl ester prodrugs of cefotiam. Nishimura, T., Yoshimura, Y., Miyake, A., Yamaoka, M., Takanohashi, K., Hamaguchi, N., Hirai, S., Yashiki, T., Numata, M. J. Antibiot. (1987) [Pubmed]
  30. The activity of rosoxacin, fosfomycin, cefotiam, and spectinomycin on beta-lactamase producing Neisseria gonorrhoeae. Dickgiesser, N., Kuntz, P. The British journal of venereal diseases. (1984) [Pubmed]
  31. Therapeutic effects of cefotiam and cefazolin on experimental pneumonia caused by Klebsiella pneumoniae DT-S in mice. Nishi, T., Tsuchiya, K. Antimicrob. Agents Chemother. (1980) [Pubmed]
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