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cefotiam

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Description

Cefotiam is a broad-spectrum cephalosporin antibiotic with activity against a wide range of gram-positive and gram-negative bacteria. It is effective against both aerobic and anaerobic organisms. It is synthesized through a multi-step process starting with 7-aminocephalosporanic acid. Cefotiam is often used to treat a variety of infections, including pneumonia, urinary tract infections, and skin infections. It works by interfering with the synthesis of bacterial cell walls, preventing bacteria from growing and multiplying. Cefotiam is often studied due to its effectiveness against multi-drug resistant organisms. It is a valuable therapeutic option for patients who are allergic to penicillin.'

Cefotiam: One of the CEPHALOSPORINS that has a broad spectrum of activity against both gram-positive and gram-negative microorganisms. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

cefotiam : A cephalosporin with ({1-[2-(dimethylamino)ethyl]-1H-tetrazol-5-yl}sulfanyl)methyl and (2-amino-1,3-thiazol-4-yl)acetamido substituents at positions 3 and 7, respectively, of the cephem skeleton. A third generation beta-lactam cephalosporin antibiotic, it is active against a broad spectrum of both Gram positive and Gram negative bacteria. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID43708
CHEMBL ID1296
CHEBI ID355510
SCHEMBL ID149538
SCHEMBL ID11224134
MeSH IDM0023572

Synonyms (58)

Synonym
BRD-K02275692-003-03-4
(6r,7r)-7-{[(2-amino-1,3-thiazol-4-yl)acetyl]amino}-3-[({1-[2-(dimethylamino)ethyl]-1h-tetrazol-5-yl}thio)methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
61622-34-2
cefotiam
PRESTWICK2_000482
BSPBIO_000343
PRESTWICK3_000482
NCGC00179594-01
cefotiam (inn)
D07648
aspil (tn)
BPBIO1_000379
AB00514684
(6r,7r)-7-[2-(2-amino-thiazol-4-yl)-acetylamino]-3-[1-(2-dimethylamino-ethyl)-1h-tetrazol-5-ylsulfanylmethyl]-8-oxo-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylic acid
DB00229
CTM ,
5-thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid, 7-(((2-amino-4-thiazolyl)acetyl)amino)-3-(((1-(2-(dimethylamino)ethyl)-1h-tetrazol-5-yl)thio)methyl)-8-oxo-, (6r-trans)-
cefotiamum [inn-latin]
cefotiam [inn:ban]
cgp 14221e
SPBIO_002264
PRESTWICK1_000482
PRESTWICK0_000482
j01dc07
CHEMBL1296
aspil
(6r,7r)-7-[[2-(2-amino-1,3-thiazol-4-yl)acetyl]amino]-3-[[1-(2-dimethylaminoethyl)tetrazol-5-yl]sulfanylmethyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
(6r,7r)-7-{[(2-amino-1,3-thiazol-4-yl)acetyl]amino}-3-[({1-[2-(dimethylamino)ethyl]-1h-tetrazol-5-yl}sulfanyl)methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
7beta-(2-amino-1,3-thiazol-4-yl)acetamido-3-[({1-[2-(dimethylamino)ethyl]-1h-tetrazol-5-yl}sulfanyl)methyl]-3,4-didehydrocepham-4-carboxylic acid
chebi:355510 ,
cefotiamum
unii-91w6z2n718
91w6z2n718 ,
SCHEMBL149538
cefotiam [who-dd]
cefotiam [inn]
cefotiam [jan]
cefotiam [mi]
J-700162
SCHEMBL11224134
7beta-(2-imino-4-thiazolin-4-yl)acetamido-3-{1-[2-(n,n-dimethylamino)ethyl]-1h-tetrazol-5-yl}thiomethyl-3-cephem-4-carboxylic acid
QYQDKDWGWDOFFU-IUODEOHRSA-N
7beta-[ 2-(2-aminothiazol-4-yl) acetamido]-3-[1-(2-dimethylaminoethyl)-1h-tetrazol-5-yl]thiomethyl-3-cephem-4-carboxylic acid
DTXSID6022763
(6r,7r)-7-[2-(2-amino-1,3-thiazol-4-yl)acetamido]-3-[({1-[2-(dimethylamino)ethyl]-1h-1,2,3,4-tetrazol-5-yl}sulfanyl)methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
C21544
SR-01000841230-2
bdbm50485561
(6r,7r)-7-(2-(2-aminothiazol-4-yl)acetamido)-3-((1-(2-(dimethylamino)ethyl)-1h-tetrazol-5-ylthio)methyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
Q3009984
cefotiam,(s)
5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid,7-[[(2-amino-4-thiazolyl)acetyl]amino]-3-[[[1-[2-(dimethylamino)ethyl]-1h-tetrazol-5-yl]thio]methyl]-8-oxo-,(6r,7r)-
gtpl12254
(6r,7r)-7-[[2-(2-amino-1,3-thiazol-4-yl)acetyl]amino]-3-[[1-[2-(dimethylamino)ethyl]tetrazol-5-yl]sulfanylmethyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid,7-[[(2-amino-4-thiazolyl)acetyl]amino]-3-[[[1-[2-(dimethylamino)ethyl]-1h-tetrazol-5-yl]thio]methyl]-8-oxo-, (6r,7r)-
EN300-19766378
CS-0009630
HY-B0734

Research Excerpts

Overview

Cefotiam (CTM) is a new cephalosporin with a broad spectrum of activity against both Gram-positive and Gram-negative microorganisms. Cefotliam hexetil is a prodrug of cefotium available for oral administration.

ExcerptReferenceRelevance
"Cefotiam (CTM) is a new cephem antibiotic which has potent activities against Gram-positive and Gram-negative bacteria. "( [Study on penetration of cefotiam into the cerebrospinal fluid].
Fujiwara, M; Kitsugi, T; Kodama, Y; Sakata, K, 1984
)
2.01
"Cefotiam is a new semisynthetic cephalosporin antibiotic. "( [A clinical study of cefotiam in pediatric field (author's transl)].
Aoyama, R; Asuka, N; Izumi, Y; Kuronuma, T; Nagata, K, 1981
)
2.02
"Cefotiam (CTM) is a new synthetic cephem antibiotic developed in Japan. "( [Fundamental and clinical studies of cefotiam in the field of oral surgery].
Minami, Y; Morihana, T; Nagata, K; Nakao, K; Namba, R; Shimada, K; Taguchi, M; Tsushima, T; Tsutou, H; Ueda, K; Yamamoto, T, 1982
)
1.98
"Cefotiam hexetil is a prodrug of cefotiam. "( Cefotiam concentrations in the sinus fluid of patients with chronic sinusitis after administration of cefotiam hexetil.
Brion, N; Chatelin, A; Cherrier, P; Le Gros, V; Petitjean, O; Tod, M, 1993
)
3.17
"Cefotiam hexetil is a pro-drug of cefotiam available for oral administration. "( Skin tissue fluid levels of cefotiam in healthy man following oral cefotiam hexetil.
Grobecker, H; Kees, F; Korting, HC; Lukacs, A; Schäfer-Korting, M, 1990
)
2.02
"Cefotiam (CTM) is a new cephalosporin with a broad spectrum of activity against both Gram-positive and Gram-negative microorganisms. "( [Augmentation by serrapeptase of tissue permeation by cefotiam].
Anno, H; Arai, T; Hirata, M; Katayama, T; Komatsu, H; Koyama, A; Mori, J; Murakami, K; Tokuda, H; Waku, M, 1986
)
1.96

Toxicity

ExcerptReferenceRelevance
"2%) patients in the former and latter groups respectively reporting adverse events."( A double-blind randomized trial comparing the efficacy and safety of a 5-day course of cefotiam hexetil with that of a 10-day course of penicillin V in adult patients with pharyngitis caused by group A beta-haemolytic streptococci.
Bingen, E; Carbon, C; Chatelin, A; Guetat, F; Orvain, J; Rio, Y; Zuck, P, 1995
)
0.51
" Cephalosporins of the second generation in combination with metronidazole can, therefore, be considered effective and safe drugs in the prevention of postsurgical infections."( [Efficacy and safety of two cephalosporins in the perioperative prophylaxis in patients undergoing abdominal or vaginal hysterectomies or gynaecological laparotomies: a prospective randomized study].
Bier, UW; Eickhoff, C; Hillger, H; Kienle, E; Preuss, MJ; Regidor, PA; Schindler, AE, 2000
)
0.31
" Furthermore, the toxic effects of the two impurities of cefotiam hydrochloride were predicted and it is thought that they could be more toxic than cefotiam."( Isolation, identification and in silico toxicity predictions of two isomers from cefotiam hydrochloride.
Han, Y; Hu, CQ; Tian, Y; Wang, YN; Zhang, X, 2018
)
0.95

Pharmacokinetics

No changes in elimination half-life relative to a normal population occurred with cefuroxime, cefotiam, and ampicillin. Simultaneous administration by the intravenous route does not alter the pharmacokinetic parameters of either compound.

ExcerptReferenceRelevance
" In healthy subjects, the serum elimination half-life is about 1 hour."( Clinical pharmacokinetics of cefotiam.
Blickle, JF; Brogard, JM; Jehl, F; Lamalle, AM; Monteil, H; Willemin, B, 1989
)
0.57
"Examining blood level values and urinary concentrations taken from pregnant women during the third trimester and nonpregnant female volunteers, the pharmacokinetic dates of cefotiam (a second generation's cephalosporin) have been evaluated."( [Pharmacokinetic studies of cefotiam in late pregnancy].
Bierwisch, I; Michels, W; Schröder, S; Spencker, FB; Voigt, R,
)
0.62
"05) the area under the curve in tissue-cage fluid of ceftriaxone and cefotiam-treated animals, and the terminal half-life of ceftriaxone in their sera (3."( Enhancement of the therapeutic effect of cephalosporins in experimental endocarditis by altering their pharmacokinetics with diclofenac.
Brion, N; Carbon, C; Joly, V; Pangon, B; Vallois, JM, 1988
)
0.51
"To determine the influence of in vitro activity, pharmacokinetic properties, and therapeutic regimen on the antibacterial effect in vivo, we compared three cephalosporins, cefotiam, cefmenoxime, and ceftriaxone, in a rabbit model of experimental Escherichia coli endocarditis after 4 days of treatment."( Comparative efficacy of cefotiam, cefmenoxime, and ceftriaxone in experimental endocarditis and correlation with pharmacokinetics and in vitro efficacy.
Abel, L; Brion, N; Buré, A; Carbon, C; Contrepois, A; Joly, V; Pangon, B; Vallois, JM, 1987
)
0.77
"The pharmacokinetic analysis was enriched, during the last several years, with the method of statistical moment (MSM)--an alternative for the classical compartment approach, presumed as model-non-dependent."( [Noncompartment (model-independent) pharmacokinetic analysis. 1. The method of statistical moments in evaluating the pharmacokinetic characteristics of cefotiam following its intravenous administration].
Terzinvanov, D, 1986
)
0.47
" In 2 cases of 2 day-old neonates given CTM 20 mg/kg by 30-minute intravenous drip infusion, the mean peak concentration at the termination of the infusion was 25."( [Pharmacokinetic and clinical studies of cefotiam in mature neonates].
Nishimura, T; Tabuki, K; Takashima, T, 1986
)
0.54
" At the same time, pharmacokinetic analysis was done to study the maternal fetal transfer."( [Pharmacokinetic and clinical studies of cefotiam in the perinatal period].
Chan, C; Hanabayashi, T; Hayasaki, M; Iida, M; Ito, K; Noda, K; Osugi, S; Ri, J; Takada, Y; Yamada, Y, 1986
)
0.54
"The pharmacokinetic behaviour of cephalosporin antibiotic, second generation after intravenous administration to patients during the early post-operative period was characterized as well as after cholecystectomy."( [Pharmacokinetics of the cephalosporin antibiotic cefotiam following its intravenous administration to patients after cholecystectomy].
Gerova, Z; Terziivanov, D; Vlakhov, V, 1986
)
0.52
" After intramuscular administration of 1 g of cefotiam to three healthy volunteers, a mean (+/- standard deviation) peak concentration of 16."( Pharmacokinetics of cefotiam in humans.
Guibert, J; Lecaillon, JB; Modai, J; Rouan, MC; Schoeller, JP, 1985
)
0.85
"05) between the half-life for biliary excretion and the volume of the biliary flow support that presumption."( [Characterization of the pathways of cefotiam elimination by clearance approaches in patients following cholecystectomy].
Gerova, Z; Terziivanov, D; Vlakhov, V, 1985
)
0.54
"Simultaneous administration by the intravenous route of 1 g of cefotiam and 1 g of cefsulodin does not alter the pharmacokinetic parameters of either compound."( [Pharmacokinetic behavior of cefsulodin and cefotiam alone or in combination after intravenous injection of 1 gram].
Bryskier, A; Fourtillan, JB; Ingrand, I; Lefebvre, MA, 1984
)
0.77
" The average values of the pharmacokinetic parameters obtained after such administration to the control rabbits, with normal biliary excretion, expressed in accordance with a two-compartment open kinetic model were: alpha = 15."( Influence of experimentally induced cholestasis on the pharmacokinetics of cefotiam.
Alonso, IG; Dominguez-Gil, A; Mariño, EL, 1984
)
0.5
" No significant differences were observed with respect to the terminal half-life (1 h) and the area under the curve versus the dose."( Pharmacokinetics of cefotiam administered intravenously and intramuscularly to healthy adults.
Brisson, AM; Bryskier, A; Fourtillan, JB; Millerioux, L, 1984
)
0.59
" This bacteriological and pharmacokinetic study was therefore performed in order to evaluate the potency of cefmenoxime in the treatment of respiratory infections."( Laboratory evaluation of cefmenoxime: a new cephalosporin. In vitro and in vivo antibacterial activities and pharmacokinetic properties.
Harada, T; Matsumoto, K; Nagatake, T; Rikitomi, N; Uzuka, Y, 1983
)
0.27
" The three beta-lactams were rapidly distributed into the different tissues and their pharmacokinetic profiles were found to be very similar."( Pharmacokinetics of ampicillin, sulbactam and cefotiam in patients undergoing orthopedic surgery.
Dahmen, G; Göbel, C; Gotthardt, H; Gruber, H; Hille, E; Mallwitz, J; Pfaff, G; Wildfeuer, A,
)
0.39
" No changes in elimination half-life relative to a normal population occurred with cefuroxime, cefotiam, and ampicillin."( Pharmacokinetics of antibiotic prophylaxis in major orthopedic surgery and blood-saving techniques.
Dehne, MG; Hempelmann, G; Mühling, J; Nopens, H; Sablotzki, A, 2001
)
0.53
" The drug concentrations in plasma and PF were determined and analyzed using population pharmacokinetic modeling."( Development of breakpoints of cephems for intraabdominal infections based on pharmacokinetics and pharmacodynamics in the peritoneal fluid of patients.
Ikawa, K; Ikeda, K; Morikawa, N; Ohge, H; Sueda, T, 2008
)
0.35

Compound-Compound Interactions

The synergic activity of imipenem/cilastatin combined with cefotiam was studied in a mouse bacteraemia model.

ExcerptReferenceRelevance
"By using checkerboard titrations the effect of cefotiam combined with different beta-lactam antibiotics on fifty strains of Enterobacteriaceae moderately susceptible (minimal inhibiting concentration greater than or equal to 8 mg/l) or resistant (minimal inhibiting concentration greater than or equal to 64 mg/l) to cefotiam was evaluated."( Activity of cefotiam in combination with beta-lactam antibiotics on enterobacterial hospital strains.
Couvreur, ML; de Schepper, N; Hubrechts, JM; Kupperberg, E; Leger, J; Nulens, E; Nyssen, HJ; Vanhoof, R, 1990
)
0.91
" Fifty-one patients were administered CTM in combination with aminoglycoside or (and) penicillin."( [Clinical investigation of cefotiam in combination with aminoglycoside or (and) penicillin against complicated infections with hematopoietic disorders].
Kageyama, S; Kamio, N; Kataoka, Y; Katayama, N; Koh, T; Minami, N; Ono, T; Ota, C; Tanaka, I; Uno, N, 1984
)
0.56
"The synergic activity of imipenem/cilastatin combined with cefotiam was studied in a mouse bacteraemia model."( Synergic activity of imipenem/cilastatin combined with cefotiam against methicillin-resistant Staphylococcus aureus.
Asahi, Y; Goto, M; Inoue, M; Kaji, Y; Kimura, S; Matsuda, K; Nakagawa, S; Oka, S; Sanada, M; Shimada, K, 1993
)
0.78

Bioavailability

Cefotiam is an orally active acyloxymethyl esters of 7-[2-(2-aminothiazol-4-yl)acetamido]

ExcerptReferenceRelevance
" Following the oral dose, the bioavailability of cefotiam was 45."( Skin tissue fluid levels of cefotiam in healthy man following oral cefotiam hexetil.
Grobecker, H; Kees, F; Korting, HC; Lukacs, A; Schäfer-Korting, M, 1990
)
0.83
"In a separate study on the orally active acyloxymethyl esters (1) of 7-[2-(2-aminothiazol-4-yl)acetamido]-3-[[[1-(2-dimethylaminoethyl) - 1H-tetrazol-5-yl]thio]methyl]ceph-3-em-4-carboxylic acid (cefotiam, CTM), we have shown, by quantitative structure-oral bioavailability (BA) relation analysis, that the R2 group in the acyl group R2CO must have both an adequate lipophilicity (Hansch's lipophilic parameter, pi) and steric hindrance (Taft's Es value)."( Preparation of 1-acyloxyethyl esters of 7-[2-(2-aminothiazol-4-yl)acetamido]-3-[[[1-(2-dimethylaminoe thy l)-1H-tetrazol-5-yl]thio]-methyl]ceph-3-em-4-carboxylic acid (cefotiam) and their oral absorption in mice.
Hamaguchi, N; Yashiki, T; Yoshimura, Y, 1986
)
0.65
" The syntheses and oral bioavailability (BA) in mice are described."( Orally active 1-(cyclohexyloxycarbonyloxy)alkyl ester prodrugs of cefotiam.
Hamaguchi, N; Hirai, S; Miyake, A; Nishimura, T; Numata, M; Takanohashi, K; Yamaoka, M; Yashiki, T; Yoshimura, Y, 1987
)
0.51

Dosage Studied

The standard dosing regimen for cefotiam resulted in extremely low plasma concentrations in children. Such low concentrations may lead to antimicrobial drug resistance. The highest SBA-titers against Haemophilus influenzae were achieved at a dosage of 2 g.

ExcerptRelevanceReference
" Because the serum levels were yet effective and nearly equal 6 hours after intravenous injection we state that it is not necessary to change the dosage and the application interval of cefotiam during pregnancy."( [Pharmacokinetic studies of cefotiam in late pregnancy].
Bierwisch, I; Michels, W; Schröder, S; Spencker, FB; Voigt, R,
)
0.62
" However, appropriate dosage regimens in this group of patients have not been fully known for many antibiotics."( Cefotiam disposition in markedly obese athlete patients, Japanese sumo wrestlers.
Chiba, K; Ishizaki, T; Kato, J; Kawa, Z; Ochi, K; Tsuchiya, M, 1989
)
1.72
"In continuation of our clinical observations on perioperative prophylaxis by application of Halospor and Gentamicin the dosage of Halospor has been reduced to 2 grams once only."( [Once again: the perioperative antibiotic prophylaxis in cesarean section].
Bellée, H; Fiedler, FB; Link, M, 1988
)
0.27
" They also demonstrate that, provided that the dose is sufficient, a long-acting broad-spectrum cephalosporin may be effective in severe gram-negative infections, even when given at relatively long dosing intervals, in contrast with a rapidly cleared drug with the same intrinsic activity."( Comparative efficacy of cefotiam, cefmenoxime, and ceftriaxone in experimental endocarditis and correlation with pharmacokinetics and in vitro efficacy.
Abel, L; Brion, N; Buré, A; Carbon, C; Contrepois, A; Joly, V; Pangon, B; Vallois, JM, 1987
)
0.58
" A crossover analysis of concentrations of CMX in bile of patients given doses of 1 g and 2 g revealed a dose-response relationship."( [Clinical studies on the transference of cephem-type antibiotics into bile and gallbladder tissues with special reference to cefotiam and cefmenoxime].
Aeba, S; Hasegawa, S; Iijima, K; Kusaba, T; Matsumoto, H; Mishima, T; Okano, A; Shiozaki, H; Totsuka, S; Usui, R, 1986
)
0.48
" A dose-response relationship was observed."( [Pharmacokinetic and clinical studies of cefotiam in mature neonates].
Nishimura, T; Tabuki, K; Takashima, T, 1986
)
0.54
" The antibiotic dosage was calculated so that the serum level remained constant for a given period of time."( [Intraocular penetration of systemically administered cephalosporins under steady-state conditions in animal experiments].
Mendel, N; Mester, U; Völker, B, 1985
)
0.27
" The recommended dosage regimens (i."( Clinical evaluation of cefotiam and cefamandole in respiratory tract infections.
Beumer, HM; Kahn, M; Olislagers, WP; van Hamersveld, JD, 1985
)
0.58
" The dosage schedule for cefotiam in patients with normal renal function can be used in the presence of renal failure when the creatinine clearance is equal to or greater than 1 l/h (16."( Pharmacokinetics and dosage adjustment of cefotiam in renal impaired patients.
Bammatter, F; Binswanger, U; Guibert, J; Rouan, MC; Schoeller, JP; Theobald, W, 1984
)
0.84
" Thus, the chosen dosage regimens considered apt for gonorrhea led to high initial as well as long-standing drug levels."( Plasma and skin blister fluid levels of cefotiam and cefmenoxime after single intramuscular application of 1 g in gonorrhea.
Korting, HC, 1984
)
0.54
" These results suggest that the pharmacokinetics of the two drugs are not modified by their simultaneous administration and that the dosing schedule previously proposed for administration of the two cephalosporins alone in the presence of renal insufficiency can be applied without modification when they are given together."( Pharmacokinetics of cefotiam and cefsulodin after simultaneous administration to patients with impaired renal function.
Binswanger, U; Guibert, J; Lecaillon, JB; Rouan, MC; Schoeller, JP, 1984
)
0.59
" Over the above dosing range and routes of administration, cefotiam pharmacokinetics were essentially linear, with plasma clearances varying from 19."( Pharmacokinetics of cefotiam administered intravenously and intramuscularly to healthy adults.
Brisson, AM; Bryskier, A; Fourtillan, JB; Millerioux, L, 1984
)
0.83
" We give recommendations for dosage adjustment in patients with renal insufficiency."( Pharmacokinetics of cefotiam in patients with impaired renal function and in those undergoing hemodialysis.
Konishi, K; Ozawa, Y, 1984
)
0.59
" We conclude that the percent penetration of CTM into CSF increases in the presence of the inflamed meninges and that prophylactic dosage of CTM for postoperative meningitis will be intravenous administration of 2 g of CTM in adults."( [Penetration of cefotiam dihydrochloride into cerebrospinal fluid (author's transl)].
Furuno, M; Kojima, T; Morikawa, A; Okada, M; Shimizu, T; Waga, S, 1982
)
0.61
" Cefotiam was given intramuscularly in monotherapy, at the daily dosage of 1 and 2 g in two injections during 7 to 28 days."( [Clinical evaluation of cefotiam in adults urinary tract infections (author's transl)].
Coppens, H; Guibert, J; Yvelin, C, 1982
)
1.48
" All of these changes disappeared within a few days after the dosing period."( Nephrotoxicity of cefotiam in rats.
Chiba, S; Miyajima, H; Nakai, Y; Suhara, I; Takano, K; Yamazaki, M,
)
0.47
"The efficacies of several dosage schedules, productive of plasma levels of cefotiam and cefazolin of short and long duration and starting at three levels of cefotiam and cefazolin of short and long duration and starting at three different times (3, 18, and 30h) after infection, were examined in experimental pneumonia caused by Klebsiella pneumoniae DT-S in mice."( Therapeutic effects of cefotiam and cefazolin on experimental pneumonia caused by Klebsiella pneumoniae DT-S in mice.
Nishi, T; Tsuchiya, K, 1980
)
0.8
" In this study, we tested cefotiam, a member of this group of antibiotics, for its suitability in this indication, and determined the intraperitoneal dosage needed to achieve effective serum levels."( [Transperitoneal resorption of cefotiam in CAPD patients with and without peritonitis].
Koblinger, S; Thomae, U, 1994
)
0.87
" These results indicate that the timing of dosing of each antibiotic influences synergy, and administration of cefotiam 2 h after imipenem is more effective than the other regimens."( Synergic activity of imipenem/cilastatin combined with cefotiam against methicillin-resistant Staphylococcus aureus.
Asahi, Y; Goto, M; Inoue, M; Kaji, Y; Kimura, S; Matsuda, K; Nakagawa, S; Oka, S; Sanada, M; Shimada, K, 1993
)
0.74
"Reductions of frequency of administration and dosage of antibiotic agents used in colorectal surgery may lower costs and the occurrence of adverse side effects."( Low-dose, single-shot perioperative antibiotic prophylaxis in colorectal surgery.
Peiper, C; Schumpelick, V; Seelig, M; Treutner, KH,
)
0.13
" Cefotiam as a low dosage combined with metronidazole was as effective as cefoxitin."( [Efficacy and safety of two cephalosporins in the perioperative prophylaxis in patients undergoing abdominal or vaginal hysterectomies or gynaecological laparotomies: a prospective randomized study].
Bier, UW; Eickhoff, C; Hillger, H; Kienle, E; Preuss, MJ; Regidor, PA; Schindler, AE, 2000
)
1.22
" Changes in circulating retinol with time for chronic dosing showed drug treatment (P<0."( Flupenthixol and cefotiam: effects on vitamin A metabolism in rats.
Fielenbach, T; Rave, G; Schindler, R, 2004
)
0.66
"Intraoperative repeated antimicrobial dosing is therefore recommended to prevent the surgical wound infection for prolonged colorectal surgery."( The significance of the intraoperative repeated dosing of antimicrobials for preventing surgical wound infection in colorectal surgery.
Fukushima, Y; Hiraoka, N; Morimoto, T; Morita, S; Nishisho, I; Nomura, T; Shibata, N, 2005
)
0.33
" These results should help us to understand better the peritoneal pharmacokinetics of cefotiam while also helping us to choose the appropriate dosage for intra-abdominal infections."( Penetration and exposure of cefotiam into the peritoneal fluid of abdominal surgery patients after intravenous administration.
Fukuhara, K; Hayato, S; Ikawa, K; Ikeda, K; Morikawa, N; Ohge, H; Soga, Y; Sueda, T, 2008
)
0.86
" The bacteriostatic and bactericidal breakpoints were determined as the highest MIC values at which the bacteriostatic and bactericidal probabilities in PF were > or =80%, which values varied with drug and dosing regimen."( Development of breakpoints of cephems for intraabdominal infections based on pharmacokinetics and pharmacodynamics in the peritoneal fluid of patients.
Ikawa, K; Ikeda, K; Morikawa, N; Ohge, H; Sueda, T, 2008
)
0.35
" The present study was conducted to evaluate whether the standard cefotiam dosing regimen resulted in a subtherapeutic concentrations in children."( Cefotiam Treatment in Children: Evidence of Subtherapeutic Levels.
Hao, GX; Huang, X; Jiang, YF; Kan, M; Shi, HY; Su, LQ; Wu, L; Wu, YE; Zhao, W; Zheng, Y; Zhou, XW, 2020
)
2.24
"Data were prospectively collected from pediatric patients with suspected or confirmed community-acquired pneumonia who were receiving cefotiam at the standard dosing regimen (40-80 mg/kg, 2 or 3 times daily)."( Cefotiam Treatment in Children: Evidence of Subtherapeutic Levels.
Hao, GX; Huang, X; Jiang, YF; Kan, M; Shi, HY; Su, LQ; Wu, L; Wu, YE; Zhao, W; Zheng, Y; Zhou, XW, 2020
)
2.2
"The standard dosing regimen for cefotiam resulted in extremely low plasma concentrations in children; such low concentrations may lead to antimicrobial drug resistance."( Cefotiam Treatment in Children: Evidence of Subtherapeutic Levels.
Hao, GX; Huang, X; Jiang, YF; Kan, M; Shi, HY; Su, LQ; Wu, L; Wu, YE; Zhao, W; Zheng, Y; Zhou, XW, 2020
)
2.28
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
antibacterial drugA drug used to treat or prevent bacterial infections.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (3)

ClassDescription
cephalosporinA class of beta-lactam antibiotics differing from the penicillins in having a 6-membered, rather than a 5-membered, side ring. Although cephalosporins are among the most commonly used antibiotics in the treatment of routine infections, and their use is increasing over time, they can cause a range of hypersensitivity reactions, from mild, delayed-onset cutaneous reactions to life-threatening anaphylaxis in patients with immunoglobulin E (IgE)-mediated allergy.
semisynthetic derivativeAny organic molecular entity derived from a natural product by partial chemical synthesis.
beta-lactam antibiotic allergenAny beta-lactam antibiotic which causes the onset of an allergic reaction.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Solute carrier family 22 member 6Rattus norvegicus (Norway rat)IC50 (µMol)718.00000.50000.50000.5000AID680340
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (47)

Assay IDTitleYearJournalArticle
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID535643Antimicrobial activity against Group B streptococcus serotype III N3 by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Genetic heterogeneity in pbp genes among clinically isolated group B Streptococci with reduced penicillin susceptibility.
AID559859Antimicrobial activity against Streptococcus agalactiae clinical isolates by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Capsular type and antibiotic resistance in Streptococcus agalactiae isolates from patients, ranging from newborns to the elderly, with invasive infections.
AID535633Antimicrobial activity against Group B streptococcus serotype Ia R7 harboring T77I, F395V and S353F in PBP 2X; V80A and G613R in PBP 2B; and L45P, N163K, N723S and Y470F in PBP 1A by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Genetic heterogeneity in pbp genes among clinically isolated group B Streptococci with reduced penicillin susceptibility.
AID535637Antimicrobial activity against Group B streptococcus serotype Ib R3 harboring Q557E, A400V mutations in PBP 2X and T567I, G539E mutations in PBP 2B by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Genetic heterogeneity in pbp genes among clinically isolated group B Streptococci with reduced penicillin susceptibility.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID543413Antimicrobial activity against Shigella sonnei UIH-1 expressing beta-lactamase CTX-M-64 by disk diffusion method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Novel chimeric beta-lactamase CTX-M-64, a hybrid of CTX-M-15-like and CTX-M-14 beta-lactamases, found in a Shigella sonnei strain resistant to various oxyimino-cephalosporins, including ceftazidime.
AID535635Antimicrobial activity against Group B streptococcus serotype VI R5 harboring F395L, V405A, R433H, H438Y, and G648A mutations in PBP 2X and T567I mutation in PBP 2B by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Genetic heterogeneity in pbp genes among clinically isolated group B Streptococci with reduced penicillin susceptibility.
AID43737Beta-lactamase inhibitory activity against penicillinase of Klebsiella pneumoniae. TN16981983Journal of medicinal chemistry, May, Volume: 26, Issue:5
Synthesis and biological activities of the Z isomers of carbapenem antibiotics.
AID535647Antimicrobial activity against Group B Streptococcus serotype V 2603 V/R harboring E63K mutation in PBP 2A and L41S mutation in PBP 1B by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Genetic heterogeneity in pbp genes among clinically isolated group B Streptococci with reduced penicillin susceptibility.
AID535642Antimicrobial activity against Group B streptococcus serotype VI N4 harboring E63K mutation in PBP 2A and L41S mutation in PBP 1B by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Genetic heterogeneity in pbp genes among clinically isolated group B Streptococci with reduced penicillin susceptibility.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID535632Antimicrobial activity against Group B streptococcus R8 harboring T77I, S353F and A514V in PBP 2X; V80A and G613R in PBP 2B; and L45P, N163K, N723S and G527V in PBP 1A by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Genetic heterogeneity in pbp genes among clinically isolated group B Streptococci with reduced penicillin susceptibility.
AID535644Antimicrobial activity against Group B streptococcus serotype Ib N2 harboring E63K mutation in PBP 2A and L41S mutation in PBP 1B by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Genetic heterogeneity in pbp genes among clinically isolated group B Streptococci with reduced penicillin susceptibility.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID543417Antimicrobial activity against rifampicin-resistant Escherichia coli X1037 transconjugant by disk diffusion method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Novel chimeric beta-lactamase CTX-M-64, a hybrid of CTX-M-15-like and CTX-M-14 beta-lactamases, found in a Shigella sonnei strain resistant to various oxyimino-cephalosporins, including ceftazidime.
AID535640Antimicrobial activity against Group B streptococcus serotype Ib C2 harboring E63K mutation in PBP 2A and L41S mutation in PBP 1B by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Genetic heterogeneity in pbp genes among clinically isolated group B Streptococci with reduced penicillin susceptibility.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID535645Antimicrobial activity against Group B Streptococcus serotype Ia N1 harboring E63K mutation in PBP 2A and L41S mutation in PBP 1B by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Genetic heterogeneity in pbp genes among clinically isolated group B Streptococci with reduced penicillin susceptibility.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID535639Antimicrobial activity against Group B streptococcus serotype VI R1 harboring F395L, V405A, R433H, H438Y, and G648A mutations in PBP 2X and T567I mutation in PBP 2B by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Genetic heterogeneity in pbp genes among clinically isolated group B Streptococci with reduced penicillin susceptibility.
AID535636Antimicrobial activity against Group B streptococcus serotype VI R4 harboring Q557E mutation in PBP 2X and T567I, Y262N mutations in PBP 2B by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Genetic heterogeneity in pbp genes among clinically isolated group B Streptococci with reduced penicillin susceptibility.
AID543429Antimicrobial activity against Escherichia coli XL-1 Blue harboring plasmid CL1920 by disk diffusion method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Novel chimeric beta-lactamase CTX-M-64, a hybrid of CTX-M-15-like and CTX-M-14 beta-lactamases, found in a Shigella sonnei strain resistant to various oxyimino-cephalosporins, including ceftazidime.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID543421Antimicrobial activity against rifampicin-resistant Escherichia coli X1037 by disk diffusion method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Novel chimeric beta-lactamase CTX-M-64, a hybrid of CTX-M-15-like and CTX-M-14 beta-lactamases, found in a Shigella sonnei strain resistant to various oxyimino-cephalosporins, including ceftazidime.
AID535641Antimicrobial activity against Group B streptococcus serotype V C1 harboring E63K mutation in PBP 2A and L41S mutation in PBP 1B by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Genetic heterogeneity in pbp genes among clinically isolated group B Streptococci with reduced penicillin susceptibility.
AID543425Antimicrobial activity against Escherichia coli XL-1 Blue transconjugant harboring beta-lactamase CTX-M-64 by disk diffusion method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Novel chimeric beta-lactamase CTX-M-64, a hybrid of CTX-M-15-like and CTX-M-14 beta-lactamases, found in a Shigella sonnei strain resistant to various oxyimino-cephalosporins, including ceftazidime.
AID113536In vivo protective effect in mice infected with Proteus vulgaris GN4815 at (dose mg/kg) administered sc1983Journal of medicinal chemistry, May, Volume: 26, Issue:5
Synthesis and biological activities of the Z isomers of carbapenem antibiotics.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID679146TP_TRANSPORTER: uptake in Xenopus laevis oocytes2002Drug metabolism and pharmacokinetics, , Volume: 17, Issue:2
Rat renal organic anion transporter rOAT1 mediates transport of urinary-excreted cephalosporins, but not of biliary-excreted cefoperazone.
AID535634Antimicrobial activity against Group B streptococcus serotype VI R6 harboring F395L, V405A, R433H, H438Y, A374V and G648A mutations in PBP 2X and T567I mutation in PBP 2B by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Genetic heterogeneity in pbp genes among clinically isolated group B Streptococci with reduced penicillin susceptibility.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID535646Antimicrobial activity against Group B Streptococcus serotype III NEM 316 by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Genetic heterogeneity in pbp genes among clinically isolated group B Streptococci with reduced penicillin susceptibility.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID197862Beta-lactamase inhibitory activity against penicillinase of Staphylococcus aureus 18401983Journal of medicinal chemistry, May, Volume: 26, Issue:5
Synthesis and biological activities of the Z isomers of carbapenem antibiotics.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID535638Antimicrobial activity against Group B streptococcus serotype VI R2 harboring F395L, V405A, R433H, H438Y, and G648A mutations in PBP 2X and T567I mutation in PBP 2B by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Genetic heterogeneity in pbp genes among clinically isolated group B Streptococci with reduced penicillin susceptibility.
AID680340TP_TRANSPORTER: inhibition of PAH uptake in Xenopus laevis oocytes2002Drug metabolism and pharmacokinetics, , Volume: 17, Issue:2
Rat renal organic anion transporter rOAT1 mediates transport of urinary-excreted cephalosporins, but not of biliary-excreted cefoperazone.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (409)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990255 (62.35)18.7374
1990's89 (21.76)18.2507
2000's44 (10.76)29.6817
2010's14 (3.42)24.3611
2020's7 (1.71)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 44.11

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index44.11 (24.57)
Research Supply Index6.17 (2.92)
Research Growth Index4.23 (4.65)
Search Engine Demand Index69.74 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (44.11)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials51 (12.00%)5.53%
Reviews8 (1.88%)6.00%
Case Studies52 (12.24%)4.05%
Observational0 (0.00%)0.25%
Other314 (73.88%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (2)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Efficiency and Safety of Prophylactic Use of Antibiotics in Endoscopic Injection of Tissue Adhesive in Gastric Varices: A Randomized Controlled Trial [NCT02693951]120 participants (Anticipated)Interventional2016-02-29Recruiting
Efficacy and Safety of Prophylactic Use of Antibiotics in Endoscopic Injection of Tissue Adhesive in Gastric Varices: A Multicenter Randomized Controlled Trial [NCT03045783]912 participants (Anticipated)Interventional2016-12-31Active, not recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]