Page last updated: 2024-12-06

mezlocillin

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Mezlocillin is a broad-spectrum, semisynthetic penicillin antibiotic. It is synthesized by attaching a 2-thienylmethyl group to the 6-amino position of the penicillin nucleus. Mezlocillin exhibits a broad spectrum of activity against Gram-negative bacteria, including Pseudomonas aeruginosa. Its importance lies in its effectiveness against multi-drug resistant strains of bacteria. Mezlocillin is studied for its potential to treat various infections, including urinary tract infections, pneumonia, and septicemia. It is also being investigated for its use in combination therapy with other antibiotics.'

Mezlocillin: Semisynthetic ampicillin-derived acylureido penicillin. It has been proposed for infections with certain anaerobes and may be useful in inner ear, bile, and CNS infections. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

mezlocillin : A penicillin in which the substituent at position 6 of the penam ring is a (2R)-2-[3-(methanesulfonyl)-2-oxoimidazolidine-1-carboxamido]-2-phenylacetamido group. [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]

Kassinin: Dodecapeptide tachykinin found in the central nervous system of the amphibian Kassina senegalensis. It is similar in structure and action to other tachykinins, but is especially effective in contracting smooth muscle tissue and stimulating the micturition reflex. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID656511
CHEMBL ID1731
CHEBI ID6919
SCHEMBL ID34075
MeSH IDM0013722
PubMed CID230280
CHEBI ID28626
SCHEMBL ID37668
SCHEMBL ID2953261
MeSH IDM0013722
PubMed CID45749
SCHEMBL ID20639320
MeSH IDM0013722

Synonyms (99)

Synonym
(2s,5r,6r)-3,3-dimethyl-6-{[(2r)-2-({[3-(methylsulfonyl)-2-oxoimidazolidin-1-yl]carbonyl}amino)-2-phenylacetyl]amino}-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
mezlocillin (usan/inn)
D05021
C07221
mezlin
51481-65-3
mezlocillin
DB00948
6beta-{(2r)-2-[3-(methanesulfonyl)-2-oxoimidazolidine-1-carboxamido]-2-phenylacetamido}penicillanic acid
mezlocilline
(2s,5r,6r)-3,3-dimethyl-6-((r)-2-(3-(methylsulfonyl)-2-oxo-1-imidazolidinecarboxamido)-2-phenylacetamido)-7-oxo-4-thia-1-azabicyclo(3.2.0)heptane-2-carboxylic acid
multocillin
mezlocillinum [inn-latin]
einecs 257-233-8
4-thia-1-azabicyclo(3.2.0)heptane-2-carboxylic acid, 3,3-dimethyl-6-(((((3-(methylsulfonyl)-2-oxo-1-imidazolidinyl)carbonyl)amino)phenylacetyl)amino)-7-oxo-, (2s-(2alpha,5alpha,6beta(s*)))
mezlocilina [inn-spanish]
mezlocilline [inn-french]
NCGC00167470-01
CHEBI:6919 ,
6beta-{(2r)-2-[3-(methanesulfonyl)-2-oxoimidazolidine-1-carboxamido]-2-phenylacetamido}-2,2-dimethylpenam-3alpha-carboxylic acid
mezlocilina
mezlocillinum
bay-f-1353
CHEMBL1731
(2s,5r,6r)-3,3-dimethyl-6-[[(2r)-2-[(3-methylsulfonyl-2-oxoimidazolidine-1-carbonyl)amino]-2-phenylacetyl]amino]-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
cas-51481-65-3
dtxsid1023316 ,
dtxcid603316
tox21_112474
(2s,5r,6r)-3,3-dimethyl-6-[[(2r)-2-[(3-methylsulfonyl-2-oxidanylidene-imidazolidin-1-yl)carbonylamino]-2-phenyl-ethanoyl]amino]-7-oxidanylidene-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
A828617
(2s,5r,6r)-3,3-dimethyl-6-[[(2r)-2-[[(3-methylsulfonyl-2-oxo-1-imidazolidinyl)-oxomethyl]amino]-1-oxo-2-phenylethyl]amino]-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
AKOS016010407
unii-oh2o403d1g
oh2o403d1g ,
mezlocillin [usan:inn:ban]
EPITOPE ID:120371
SCHEMBL34075
mezlocillin [inn]
mezlocillin [usan]
mezlocillin [who-dd]
mezlocillin [mart.]
(2s,5r,6r)-3,3-dimethyl-6-[(r)-2-[3-(methylsulfonyl)-2-oxo-1-imidazolidinecarboxamido]-2-phenylacetamido]-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
mezlocillin [mi]
4-thia-1-azabicyclo(3.2.0)heptane-2-carboxylic acid, 3,3-dimethyl-6-(((((3-(methylsulfonyl)-2-oxo-1-imidazolidinyl)carbonyl)amino)phenylacetyl)amino)-7-oxo-, (2s-(2.alpha.,5.alpha.,6.beta.(s*)))
mezlocillin [vandf]
(2s,5r,6r)-6-[(2r)-2-{[(3-methanesulfonyl-2-oxoimidazolidin-1-yl)carbonyl]amino}-2-phenylacetamido]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
YPBATNHYBCGSSN-VWPFQQQWSA-N
NCGC00167470-03
(2s,5r,6r)-3,3-dimethyl-6-((r)-2-(3-(methylsulfonyl)-2-oxoimidazolidine-1-carboxamido)-2-phenylacetamido)-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
Q3307752
(methylsulfonyl)-2-oxoimidazolidine-1-
(2s,5r,6r)-3,3-dimethyl-6-((r)-2-(3-
carboxamido)-2-phenylacetamido)-7-oxo-
mezlocillin,(s)
AS-11668
gtpl12272
NCGC00167470-05
(2s,5r,6r)-6-[(2r)-2-[(3-methanesulfonyl-2-oxoimidazolidine-1-carbonyl)amino]-2-phenylacetamido]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
EN300-19734688
CS-0013695
4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid, 3,3-dimethyl-6-[[(2r)-2-[[[3-(methylsulfonyl)-2-oxo-1-imidazolidinyl]carbonyl]amino]-2-phenylacetyl]amino]-7-oxo-, (2s,5r,6r)-
HY-B1466A
1h-indol-3-amine
CHEBI:28626
nsc24933
7250-19-3
nsc-24933
1h-indol-3-ylamine
C01819 ,
indolamine
AKOS000302998
STK802146
FT-0678721
AM20041082
SCHEMBL37668
3-aminoindole
SCHEMBL2953261
W-203633
1h-indole-3-amine
1h-indol-3-amine, aldrichcpr
DTXSID40282207
mfcd03848224
CS-0270266
Q27103796
SB74221
1h-indol-3-ylamine hcl
EN300-342283
nsc 24933
gtpl2088
kassinin
bdbm81943
cas_45749
nsc_45749
cid45749; kassinin; l-alpha-aspartyl-l-valyl-l-prolyl-l-lysyl-l-seryl-l-alpha-aspartyl-l-glutaminyl-l-phenylalanyl-l-valyl-glycyl-l-leucyl-l-methioninamide
DTXSID50895029
Q6374755
SCHEMBL20639320
alpha-aspartylvalylprolyllysylseryl-alpha-aspartylglutaminylphenylalanylvalylglycylleucylmethioninamide

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"This study was done to determine if a single drug, mezlocillin (Mezlo), is as safe and as effective as combined clindamycin (Clind) and gentamicin (Gent) in the treatment of penetrating abdominal wounds."( Safety and efficacy of mezlocillin: a single-drug therapy for penetrating abdominal trauma.
Lou, MA; Mandal, AK; Thadepalli, H, 1988
)
0.27
" There were no severe adverse reactions observed in any of the three treatment regimens."( Comparative efficacy and safety of mezlocillin, cefoxitin, and clindamycin plus gentamicin in postpartum endometritis.
Baker, JL; Faro, S; Goodrich, KH; Phillips, LE; Riddle, GD; Turner, RM, 1987
)
0.27
"In a retrospective study we have compared the toxic side effects related to the use of two antibiotic regimens in the treatment of febrile episodes in neutropenic, leukaemic patients undergoing first remission-induction."( Observations on the toxicity of the combination of gentamicin and mezlocillin in the treatment of patients with acute leukaemia.
Jones, DM; Kane, RJ; Lawston, FG; Rankin, EM; Scarffe, JH, 1984
)
0.27
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32

Pharmacokinetics

The pharmacokinetic parameters of mezlocillin were determined in serum and sputum at the first and the seventh day of treatment with 1 g/im/12 h in patients suffering from bronchopulmonary infections.

ExcerptReferenceRelevance
" Pharmacokinetic parameters were calculated by noncompartmental methods."( Alteration in the pharmacokinetic disposition of ciprofloxacin by simultaneous administration of azlocillin.
Barriere, SL; Catlin, DH; Frost, RW; Noe, A; Orlando, PL, 1990
)
0.28
"The pharmacokinetic disposition of cefotaxime, desacetyl cefotaxime, and mezlocillin after the administration of each drug singly and in combination was examined in eight healthy volunteers and in five anuric patients with end-stage renal disease (ESRD)."( Influence of coadministration on the pharmacokinetics of mezlocillin and cefotaxime in healthy volunteers and in patients with renal failure.
Barriere, SL; Flaherty, JF; Gambertoglio, JG; Rodondi, LC; Schoenfeld, P, 1989
)
0.28
" Apparent total, renal, and nonrenal clearances and the volume of distribution at steady-state all decreased by 45 to 50% with the higher dose, and the elimination half-life was longer (8 +/- 2 versus 15 +/- 3 min)."( Dose-dependent pharmacokinetics of mezlocillin in rats.
Jungbluth, GL; Jusko, WJ, 1989
)
0.28
" The relevant pharmacokinetic parameters of the single substances were essentially unchanged when administered in combination."( Studies on the synergism of sulbactam and beta-lactam antibiotics under in vitro conditions and in healthy volunteers after intravenous administration. Antibacterial activity in vitro, compatibility and pharmacokinetics of the drugs in combination.
Eibel, G; Pfaff, G; Räder, K; Schmalreck, A; Wildfeuer, A, 1989
)
0.28
" On the basis of pharmacokinetic investigations, administration of the antibiotic 30 min preoperatively fulfills this requirement."( [Bacteriological, clinical, and pharmacokinetic studies of perioperative antibiotic prophylaxis in head and neck surgery].
Anagnostou, M; Bleier, R; Borneff, M; Geyer, G; Hartmetz, G; Roser, F, 1987
)
0.27
" Renal function was estimated by creatinine clearance (CLCR) and pharmacokinetic parameters of mezlocillin was were determined from serum concentrations and urinary excretion rates."( Developmental pharmacokinetics of mezlocillin in 4 newborn infants.
Janicke, DM; Jungbluth, GL; Jusko, WJ; Rubio, TT; Wirth, FH, 1988
)
0.27
" Both drug regimens demonstrated similar pharmacokinetic characteristics, which suggests that the reported dose-dependent elimination of mezlocillin is not an important factor in the clinical use of mezlocillin at the dosages currently used."( Pharmacokinetics of two multiple-dose mezlocillin regimens.
Apicella, MA; Cafarell, RF; Janicke, DM; Jusko, WJ; Parker, SW, 1988
)
0.27
" Serum half-life and clearance were, respectively, 82."( Pharmacokinetics of the acyclureidopenicillins piperacillin and mezlocillin in the postpartum patient.
Cotton, DB; Dorman, K; Faro, S; Feldman, S; Martens, MG; Riddle, GD, 1987
)
0.27
" Previous studies have examined the pharmacokinetic but not the pharmacodynamic aspects of this effect."( Effect of dose on pharmacokinetics and serum bactericidal activity of mezlocillin.
Barriere, SL; Flaherty, JF; Gambertoglio, JG; Mordenti, J, 1987
)
0.27
"01) and Cmax (216."( Pharmacokinetic properties of mezlocillin in ambulatory elderly subjects.
Bradbury, K; Hirschman, SZ; McMurdo, L; Mendelson, MH; Meyers, BR; Srulevitch-Chin, E, 1987
)
0.27
" Since both drugs were tested with the same dosis in the same subjects, their pharmacokinetic parameters could be compared: mezlocillin, being more lipophilic than azlocillin, showed a higher volume of distribution and therefore lower serum concentrations."( [The effect of infusion rate on pharmacokinetic parameters of azlocillin and mezlocillin].
Adam, D; Frank, U; Haen, E; Remien, J; Richter, E, 1985
)
0.27
" The same applied to the serum half-life (t 1/2), whereas the total body clearance was reduced."( Dose-dependent pharmacokinetics of azlocillin compared to mezlocillin.
Bergan, T; Steingrimsson, O; Thorsteinsson, SB, 1982
)
0.26
" The pharmacokinetic parameters of mezlocillin were calculated automatically using a two-compartment model."( [Pharmacokinetics and dosage of mezlocillin administered by intravenous infusion].
Dvorácek, K; Janků, I; Krebs, V; Modr, Z, 1982
)
0.26
" The half-life of mezlocillin in cerebrospinal fluid (CSF) was approximately twice that in serum of experimentally infected animals, and the penetration of drug into CSF was 5 to 15% after a single dose and 5 to 20% after continuous-infusion experiments."( Pharmacokinetics and bacteriological efficacy of mezlocillin in experimental Escherichia coli and Listeria monocytogenes meningitis.
McCracken, GH; Odio, C; Thomas, ML, 1984
)
0.27
" The decline in serum antibiotic levels was biphasic in all groups, and serum data were interpreted in terms of the pharmacokinetic two-compartment model."( Mezlocillin pharmacokinetics after single intravenous doses to patients with varying degrees of renal function.
Brodey, MV; Bundtzen, RW; Craig, WA; Frimodt-Möller, N; Madsen, PO; Maigaard, S; Toothaker, RD; Welling, PG, 1980
)
0.26
" The half-life of mezlocillin increased with decreasing renal function from an average of 53 min in subjects with normal function to 165 min in oligoanuric patients."( Effects of impaired renal function, hemodialysis, and peritoneal dialysis on the pharmacokinetics of mezlocillin.
Förster, D; Kampf, D; Schurig, R; Weihermüller, K, 1980
)
0.26
" Serum pharmacokinetic data on the individual patients are computer derived using a modified open two-compartment model."( [Pharmacokinetic studies on the penetration of azlocillin and mezlocillin into bone and tissue fluid (author's transl)].
Schassan, HH; Seidel, H; Wittmann, DH, 1981
)
0.26
" The ultimate half-life t 1/2 of mezlocillin (46."( [Pharmacokinetics of mezlocillin. Comparison with ampicillin and influence of probenecid (author's transl)].
de Schepper, PJ; Tjandramaga, TB; Verbesselt, R; Verbist, L, 1982
)
0.26
" The pharmacokinetic parameters of mezlocillin were determined in serum and sputum at the first and the seventh day of treatment with 1 g/im/12 h in patients suffering from bronchopulmonary infections."( Kinetics of penetration and clearance of mezlocillin in the bronchopulmonary tract.
Braga, PC; Faravelli, M; Fraschini, F; Marchi, E; Scaglione, F; Scarpazza, G, 1984
)
0.27
"The pharmacokinetic properties of mezlocillin were evaluated in newborn infants."( Pharmacokinetic properties of mezlocillin in newborn infants.
McCraken, GH; Odio, C; Thomas, ML; Threlkeld, N, 1984
)
0.27
" The serum half-life of mezlocillin was prolonged (1."( The biliary excretion and pharmacokinetics of mezlocillin in jaundiced patients with external bile drainage.
Brumfitt, W; Dooley, JS; Gooding, A; Hamilton-Miller, JM; Sherlock, S, 1983
)
0.27
" Mezlocillin (75 mg/kg IV or IM) was substituted for ampicillin, serum was assayed microbiologically, and noncompartmental pharmacokinetic parameters were calculated."( Developmental pharmacokinetics of mezlocillin in newborn infants.
Janicke, DM; Jusko, WJ; Karotkin, EH; Rubio, TT; Wirth, FH, 1984
)
0.27
"Since mezlocillin 5 g every 8 hours is currently proving to be effective at many institutions, and since piperacillin 4 g demonstrates superior pharmacokinetic and pharmacodynamic activity, we believe that piperacillin 4 g every 8 hours could be used instead, with resulting cost savings."( Comparison of the pharmacokinetic and pharmacodynamic activity of piperacillin and mezlocillin.
Nightingale, CH; Quintiliani, R; Sullivan, MC; Sweeney, K,
)
0.13
" However, pharmacokinetic data on oral perioperative prophylaxis in patients with preoperative surgical and anesthesiological preparation are not available."( Pharmacokinetic basis for oral perioperative prophylaxis with ofloxacin in general surgery.
Beger, HG; Ebeling, P; Isenmann, R; Schwarz, M; Thomsen, J; Weikert, E, 2001
)
0.31
" Antibiotic concentrations were measured perioperatively and pharmacokinetic data calculated."( Pharmacokinetic basis for oral perioperative prophylaxis with ofloxacin in general surgery.
Beger, HG; Ebeling, P; Isenmann, R; Schwarz, M; Thomsen, J; Weikert, E, 2001
)
0.31
" Pharmacokinetic data were not influenced by preoperative surgical or anesthesiological preparation."( Pharmacokinetic basis for oral perioperative prophylaxis with ofloxacin in general surgery.
Beger, HG; Ebeling, P; Isenmann, R; Schwarz, M; Thomsen, J; Weikert, E, 2001
)
0.31
" Pharmacokinetic data confirm that oral ofloxacin may be used effectively as single-dose perioperative antibiotic prophylaxis."( Pharmacokinetic basis for oral perioperative prophylaxis with ofloxacin in general surgery.
Beger, HG; Ebeling, P; Isenmann, R; Schwarz, M; Thomsen, J; Weikert, E, 2001
)
0.31
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
" However, due to the absence of population pharmacokinetic studies in neonates and young infants, dosing regimens differ considerably in clinical practice."( Population pharmacokinetics and dosing optimization of mezlocillin in neonates and young infants.
Guo, ZX; Jiang, L; Lin, X; Tang, BH; Van Den Anker, J; Wang, ZR; Wu, YE; Yang, JJ; Yao, BF; Zhang, YX; Zhang, ZL; Zhao, W; Zhou, J, 2022
)
0.72
"A prospective, open-label pharmacokinetic study of mezlocillin was carried out in newborns."( Population pharmacokinetics and dosing optimization of mezlocillin in neonates and young infants.
Guo, ZX; Jiang, L; Lin, X; Tang, BH; Van Den Anker, J; Wang, ZR; Wu, YE; Yang, JJ; Yao, BF; Zhang, YX; Zhang, ZL; Zhao, W; Zhou, J, 2022
)
0.72
"A population pharmacokinetic model of mezlocillin in neonates and young infants was established."( Population pharmacokinetics and dosing optimization of mezlocillin in neonates and young infants.
Guo, ZX; Jiang, L; Lin, X; Tang, BH; Van Den Anker, J; Wang, ZR; Wu, YE; Yang, JJ; Yao, BF; Zhang, YX; Zhang, ZL; Zhao, W; Zhou, J, 2022
)
0.72

Compound-Compound Interactions

YTR 830, a new beta-lactamase inhibitor, combined with four extended-spectrum penicillins against ticarcillin-resistant clinical isolates of Gram-negative enteric bacilli.

ExcerptReferenceRelevance
"The in vitro antimicrobial activity of ticarcillin (TICAR), mezlocillin (MEZLO), piperacillin (PIPER), cefoperazone (CPZ), cefotaxime (CTX) and ceftazidime (CAZ), alone and in combination with 8 micrograms/ml of sulbactam (SULB), was studied by agar dilution against TICAR resistant strains isolated in 8 hospitals over a period of 3 months in 1989 (747 enterobacteria, 110 Ps."( [In vitro activity of beta-lactam antibiotics in combination with sulbactam against enterobacteriaceae, Pseudomonas aeruginosa and Acinetobacter. Results of a multicenter study].
Acar, JF; Denis, F; Drugeon, H; Fleurette, J; Kazmierczak, A; Siebor, E; Sirot, J; Soussy, CJ; Thabaut, A, 1991
)
0.28
"An open multicenter study on inpatients of 12 german hospitals was performed to investigate efficacy and safety of sulbactam in combination with mezlocillin, piperacillin or cefotaxim in severe bacterial infections."( [Sulbactam in combination with mezlocillin, piperacillin or cefotaxime. Clinical and bacteriological results in the treatment of severe bacterial infections].
Heizmann, WR; Manncke, K; Sonntag, HG; Springsklee, M, 1991
)
0.28
" In comparison with the antibiotic alone, the most marked reductions in the number of resistant strains on combination with sulbactam were as follows (the percentage of reduction is shown in brackets): for SUL + AMP and Acine-tobacter spp."( In vitro activity against clinically important gram-positive and gram-negative bacteria of sulbactam, alone and in combination with ampicillin, cefotaxime, mezlocillin, and piperacillin.
Schmalreck, AF; Wildfeuer, A, 1990
)
0.28
" MICs and MBCs of netilmicin alone and combined with azlocillin, mezlocillin and imipenem were studied."( In vitro activity of netilmicin alone and in combination with azlocillin, mezlocillin and imipenem against 149 coagulase-negative staphylococci.
Allocati, N; Cellini, L; D'Antonio, D; D'Eletto, MR; Di Girolamo, A; Piccolomini, R; Ravagnan, G, 1989
)
0.28
" Thus the physicochemical and pharmacological properties of sulbactam apparently permit flexible dosage in combination with different penicillins or cephalosporins and sulbactam can be administered as non-fixed combination in the clinical treatment of bacterial infections."( Studies on the synergism of sulbactam and beta-lactam antibiotics under in vitro conditions and in healthy volunteers after intravenous administration. Antibacterial activity in vitro, compatibility and pharmacokinetics of the drugs in combination.
Eibel, G; Pfaff, G; Räder, K; Schmalreck, A; Wildfeuer, A, 1989
)
0.28
"The in-vitro synergistic activity of YTR 830, a new beta-lactamase inhibitor, combined with four extended-spectrum penicillins (ticarcillin, piperacillin, mezlocillin and apalcillin) against ticarcillin-resistant clinical isolates of Gram-negative enteric bacilli was compared with that of clavulanate and sulbactam."( Comparative activities of the beta-lactamase inhibitors YTR 830, clavulanate and sulbactam combined with extended-spectrum penicillins against ticarcillin-resistant Enterobacteriaceae and pseudomonads.
Aronoff, SC; Jacobs, MR; Johenning, S; Yamabe, S, 1986
)
0.27
"Over a two year period 174 evaluable episodes of fever in neutropenic patients were treated in a randomized study comparing four beta-lactam antibiotics, each given in combination with netilmicin."( A randomized trial of empirical antibiotic therapy with one of four beta-lactam antibiotics in combination with netilmicin in febrile neutropenic patients.
Blacklock, H; Corringham, R; Devereux, S; Guimaraes, M; Hann, I; Hoffbrand, AV; Prentice, HG; Sage, R; Stirling, L; Trikka, E, 1988
)
0.27
"A total of 103 isolates of Pseudomonas aeruginosa were studied to compare the in vitro effectiveness of three beta-lactam antibiotics (piperacillin, ticarcillin, and mezlocillin) when used alone and in combination with four aminoglycosides (tobramycin, gentamicin, amikacin, and netilmicin)."( In vitro activity of piperacillin, ticarcillin, and mezlocillin alone and in combination with aminoglycosides against Pseudomonas aeruginosa.
Cloud, GA; Cobbs, CG; Lyon, MD; Saag, MS; Smith, KR, 1986
)
0.27
"The antibacterial activity of ciprofloxacin, either alone or in combination with azlocillin, imipenem, mezlocillin or tobramycin, was tested against enterococcus and pseudomonas species."( [Ciprofloxacin in combination with other antimicrobial substances].
Mellinghoff, D; Shah, PM; Stille, W, 1988
)
0.27
"Fifty-three clinical isolates of Klebsiella and fifty-one clinical isolates of Pseudomonas aeruginosa, twenty-six of which were carbenicillin-(CARB) resistant, were tested for susceptibility to mezlocillin (MEZ), azlocillin (AZL), and piperacillin (PIP), both alone and in combination with tobramycin (TOB) using the microtiter broth diluent method and an inoculum density of 10(6) CFU/ml."( Synergism of azlocillin, mezlocillin, piperacillin in combination with tobramycin against Klebsiella and Pseudomonas.
Andriole, VT; Downs, JT; Ryan, JL,
)
0.13
" Evaluation of therapeutic efficacy of ureidopenicillins combined with sisomicin was performed on 90 rabbits, infected intravenously with heavy inocula."( In vitro and in vivo action of mezlocillin and azlocillin combined with sisomicin.
Dzierzanowska, D; Jeljaszewicz, J, 1983
)
0.27
"The in vitro and in vivo activities of mezlocillin and ampicillin, alone and in combination with gentamicin, against Streptococcus faecalis were compared."( Comparative efficacies of mezlocillin and ampicillin alone or in combination with gentamicin in the treatment of Streptococcus faecalis endocarditis in rabbits.
Fass, RJ; Wright, CA, 1984
)
0.27
"Serum bactericidal activity (SBA) was studied in vitro after intravenous administration of cefoperazone alone or in combination with mezlocillin or amikacin to human volunteers."( Comparative study of the serum bactericidal activity of cefoperazone alone and in combination with amikacin or mezlocillin against gram-negative bacilli and Staphylococcus aureus.
Klastersky, J; Lagast, H; Standiford, H; Viollier, A,
)
0.13
"The MIC and MBC activity of mezlocillin alone and in combination with two concentrations of ceftizoxime, moxalactam, and amikacin and a single concentration of cefoxitin was studied in a broth microdilution partial checkerboard against 472 strains of aerobic gram-negative and gram-positive bacteria."( In vitro activities of ureidopenicillins alone and in combination with amikacin and three cephalosporin antibiotics.
Gerding, DN; Moody, JA; Peterson, LR, 1984
)
0.27
"The efficacies of mezlocillin and ticarcillin, each alone and in combination with gentamicin, in the therapy of experimental left-sided Enterobacter aerogenes endocarditis in rabbits were compared."( Mezlocillin and ticarcillin alone and combined with gentamicin in the treatment of experimental Enterobacter aerogenes endocarditis.
Kobasa, WD; Levison, ME, 1984
)
0.27

Bioavailability

ExcerptReferenceRelevance
" A dual intravenous/intramuscular nonlinear regression model yielded an apparent intramuscular bioavailability of 84%."( Developmental pharmacokinetics of mezlocillin in newborn infants.
Janicke, DM; Jusko, WJ; Karotkin, EH; Rubio, TT; Wirth, FH, 1984
)
0.27
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

Two dosing regimens of cefoperazone plus mezlocillin were compared in a prospective, randomized trial for therapy of febrile cancer patients. Urine levels of mez Locillin were uniformly greater than the minimum inhibitory concentration for susceptible organisms for 12 h after dosing in all patients who produced urine. This relationship suggests it may be prudent to adjust the dosage and the dosage interval of meZlocillin in patients with hepatobiliary dysfunction.

ExcerptRelevanceReference
" Dosage regimens are proposed for various situations in impaired renal function."( Elimination kinetics of mezlocillin in normal and impaired renal function including the effects of dialysis.
Bounia, A; Daikos, GK; Doundoulaki, P; Kosmidis, J; Stathakis, C; Zerefos, N, 1979
)
0.26
" We report an innovative approach of high dosage intrahepatic arterial antibiotic infusion for the therapy of hepatic abscesses, which are resistant to conventional treatments."( Hepatic intraarterial antibiotic therapy for resistant hepatic abscesses.
Ben-Yosef, R; Biran, S; Durst, AL; Finkelstein, R; Krausz, MM; Lebensart, P; Peretz, TY,
)
0.13
" The pharmacokinetics of mezlocillin appeared to be independent of dose over the dosage range studied."( Investigation of mezlocillin disposition with a porcine model.
Boudinot, FD; Cheung, RP; Davis, JB; DiPiro, JT; Sisley, JF,
)
0.13
" Thus the physicochemical and pharmacological properties of sulbactam apparently permit flexible dosage in combination with different penicillins or cephalosporins and sulbactam can be administered as non-fixed combination in the clinical treatment of bacterial infections."( Studies on the synergism of sulbactam and beta-lactam antibiotics under in vitro conditions and in healthy volunteers after intravenous administration. Antibacterial activity in vitro, compatibility and pharmacokinetics of the drugs in combination.
Eibel, G; Pfaff, G; Räder, K; Schmalreck, A; Wildfeuer, A, 1989
)
0.28
" Thus, we compared various aminoglycoside dosing schedules in neutropenic (n = 153) and nonneutropenic (n = 192) guinea pigs with Pseudomonas aeruginosa pneumonia."( Single, large, daily dosing versus intermittent dosing of tobramycin for treating experimental pseudomonas pneumonia.
Carpenter, T; Chambers, HF; Hackbarth, CJ; Kapusnik, JE; Sande, MA, 1988
)
0.27
" Patients received an initial dosing regimen of 4 g every 6 h or 5 g every 8 h, which was switched to the alternative regimen after 5 days of treatment."( Pharmacokinetics of two multiple-dose mezlocillin regimens.
Apicella, MA; Cafarell, RF; Janicke, DM; Jusko, WJ; Parker, SW, 1988
)
0.27
" Pharmacists on the nursing units were responsible for enforcing the program stipulations regarding modified dosage regimens and for reporting adverse reactions and unexpected therapeutic failures."( Multidisciplinary cost-containment program promoting less frequent administration of injectable mezlocillin.
Briceland, LL; Cooper, BW; Nightingale, CH; Quintiliani, R, 1988
)
0.27
"Two dosing regimens of cefoperazone plus mezlocillin were compared in a prospective, randomized trial for therapy of febrile cancer patients."( Cefoperazone plus mezlocillin for empiric therapy of febrile cancer patients.
Bodey, GP; Fainstein, V; Jones, P; Riccardi, S; Rolston, K, 1988
)
0.27
" The synergistic effect of ciprofloxacin represents an important advantage in allowing the reduction of the dosage of associated drugs such as aminoglycosides or beta-lactams that can potentially be responsible for damage or side-effects."( In vitro synergy of ciprofloxacin and three other antibiotics against Bacteroides fragilis.
Esposito, S; Gupta, A; Thadepalli, H, 1987
)
0.27
" It is concluded that the intravenous chemoprophylaxis should be preferred because of the lowest dosage and therefore the fewest side-effects."( [Antimicrobial chemoprevention in colorectal interventions: a single parenteral dose at the start of surgery is adequate].
Berker-von-Schlichting, C; Hancke, E; Jensen, JC; Marklein, G; Stute, H; Voigt, U, 1986
)
0.27
" In the absence of clear guidelines from human studies which relate serum concentrations to clinical response, the available data indicate that the more frequent dosage schedule is appropriate for severe infections."( Comparative pharmacokinetics of two multiple-dose mezlocillin regimens in normal volunteers.
Colaizzi, PA; Coniglio, AA; Karnes, HT; Polk, RE; Poynor, WJ; Vishniavsky, N, 1986
)
0.27
" This relationship suggests it may be prudent to adjust the dosage and the dosage interval of mezlocillin in patients with hepatobiliary dysfunction."( Pharmacokinetics of mezlocillin in patients with hepatobiliary dysfunction.
Hirschman, SZ; Jacobson, J; Meyers, BR; Sacks, HS; Srulevitch, ES; Wormser, GP; Worner, TM, 1986
)
0.27
" A total daily dosage of 300 mg/kg or 9 gm/m2 given in four to six divided dosages should produce peak concentrations of approximately 150 micrograms/ml, and concentrations greater than 16 micrograms/ml for at least 2 hours after each administration."( Clinical pharmacology of extended-spectrum penicillins in infants and children.
Koup, JR; Wilson, CB, 1985
)
0.27
" The antibiotic dosage given to mice was calculated on a body weight basis from the doses recommended for humans."( Effects of cefotaxime, clindamycin, mezlocillin, and piperacillin on mouse sarcoma L-1 tumor.
Jeljaszewicz, J; Ko, HL; Pulverer, G; Roszkowski, K; Roszkowski, W, 1984
)
0.27
" These zone standards are still tentative since the dosage schedule has not yet been defined and sufficient clinical experience has not yet been gathered to support the validity of these MIC breakpoints."( Cefsulodin: antibacterial activity and tentative interpretive zone standards for the disk susceptibility test.
Barry, AL; Jones, RN; Thornsberry, C, 1981
)
0.26
" This relation was used to calculate the loading doses, the maintenance doses and the dosage intervals adjusted to the degree of renal impairment, allowing assessment of useful dosage recommendations."( Pharmacokinetics of mezlocillin in patients with kidney impairment: special reference to hemodialysis and dosage adjustments in relation to renal function.
Brogard, JM; Comte, F; Lavillaureix, J; Spach, MO, 1982
)
0.26
" On the basis of our studies, half the dosage does not appear to be sufficient."( [Mezlocillin concentrations in the serum of children with impaired renal function].
Diekmann, L; Niemann, A; Ritzerfeld, W, 1982
)
0.26
" Urine levels of mezlocillin were uniformly greater than the minimum inhibitory concentration for susceptible organisms for 12 h after dosing in all patients who produced urine."( Mezlocillin pharmacokinetics after single intravenous doses to patients with varying degrees of renal function.
Brodey, MV; Bundtzen, RW; Craig, WA; Frimodt-Möller, N; Madsen, PO; Maigaard, S; Toothaker, RD; Welling, PG, 1980
)
0.26
" Both dosage regimens provided similar efficacy."( Potential of mezlocillin as empiric single-agent therapy in febrile granulocytopenic cancer patients.
Fortner, CL; Moody, MR; Newman, KA; Schimpff, SC; Wade, JC; Wiernik, PH; Young, VM, 1980
)
0.26
" The fosfomycin breakpoint for the low dosage of 2-3 times 3 g per infusion daily was defined with 16 micro g/ml and for the high dosage of 2-3 times 5 g fosfomycin per infusion with 64 micro g/ml."( [Fosfomycin, a new antibiotic: in vitro activity compared with mezlocillin, cefuroxime and gentamicin].
Lindenschmidt, EG; Schassan, HH, 1980
)
0.26
" While the patients are on haemodialysis, dosage may be as in patients with normal renal function."( Pharmacokinetics of mezlocillin during haemodialysis.
Asmundsson, P; Bergan, T; Steingrimsson, O; Thorsteinsson, SB, 1981
)
0.26
" Drug loss by hemodialysis is small and should have little effect on therapeutic dosage needs."( Mezlocillin disposition in chronic hemodialysis patients.
Janicke, DM; Jusko, WJ; Mangione, A; Schultz, RW, 1981
)
0.26
" This should enable dosage adjustment according to renal function, as assessed by laboratory criteria."( [Pharmacokinetics of intravenous mezlocillin in patients with normal and impaired renal function (author's transl)].
Cano, JP; Charpin, J; Gevaudan, MJ; Murisasco, A; Rigault, JP; Saingra, S, 1982
)
0.26
" The loading doses providing steady state serum concentrations were determined for various dosage intervals (2, 3, 4, 6 and 8 hours)."( [Pharmacokinetics of intramuscular mezlocillin in patients with normal and impaired renal function (author's transl)].
Brogard, JM; Comte, F; Dorner, M; Kopferschmitt, J, 1982
)
0.26
" The daily dosage ranged from 100 to 250 mg/kg (6 to 15 g) divided into three 8-hourly intravenous bolus injections or infusions, or 2 to 3 g doses administered intramuscularly."( [Clinical experience of mezlocillin in France (author's transl)].
Konopka, CA; Perin, G, 1982
)
0.26
" We found that repetitive large daily doses that are equivalent to 30 g/day in patients with normal renal function can be administered to patients with impaired renal function as a reduced dose every 4 h instead of prolonging the dosing interval, as suggested by Mangione et al."( Effect of saturable clearance during high-dose mezlocillin therapy.
Auger, F; Caplan, ES; Drusano, GL; Fiore, D; Forrest, A, 1984
)
0.27
" We propose a dosage schedule of 75 mg of mezlocillin per kg administered every 12 h to preterm (gestational age less than 38 weeks) infants less than or equal to 7 days old, every 8 h to preterm infants greater than 7 days old or term infants less than or equal to 7 days old, and every 6 h to term infants greater than 7 days old."( Pharmacokinetic properties of mezlocillin in newborn infants.
McCraken, GH; Odio, C; Thomas, ML; Threlkeld, N, 1984
)
0.27
" For dicloxacillin, however, the same dosage adjustment is required irrespective of whether administration is single or combined."( Effects of mezlocillin on the pharmacokinetics of oxacillin and dicloxacillin.
Kampf, D, 1983
)
0.27
" Elimination-constant halflife, distribution volume and area under the curve were determined to propose dosage recommendations."( [Experiences using acylureido-penicillins (azlocillin, mezlocillin) in pediatrics].
Patsch, R; Sitka, U; Thiemann, HH; Weingärtner, L,
)
0.13
" Blood samples were obtained over one dosage interval at steady state."( Mezlocillin pharmacokinetics in pediatric oncology patients.
Culbert, S; Frankel, LS; Kramer, WG; Pickering, LK, 1984
)
0.27
" Although mezlocillin disposition is affected by age and therapeutic factors, weight alone may adequately predict dosing requirements."( Developmental pharmacokinetics of mezlocillin in newborn infants.
Janicke, DM; Jusko, WJ; Karotkin, EH; Rubio, TT; Wirth, FH, 1984
)
0.27
" Single agents with broad-spectrum activity have proven efficacy, but dosage and duration are still controversial."( Injury severity dictates individualized antibiotic therapy in penetrating abdominal trauma.
Betcher, E; Griswold, JA; Muakkassa, FF; Poole, GV, 1993
)
0.29
" Renal dysfunction is significantly more frequent in cirrhotic patients treated with netilmicin but with careful attention to dosage and fluid management the clinical effect is likely to be relatively modest."( A prospective randomized trial of ceftazidime versus netilmicin plus mezlocillin in the empirical therapy of presumed sepsis in cirrhotic patients.
Burroughs, AK; Chin, JK; Greenslade, L; Kibbler, CC; McCormick, PA; McIntyre, N, 1997
)
0.3
"In this study, we investigated the pharmacokinetics of the acylureidopenicillin mezlocillin and the beta-lactamase inhibitor sulbactam during CVVHD and deduced dosage recommendations from the kinetic parameters with the goal of maintaining trough levels of above 10 mg."( Pharmacokinetics of mezlocillin and sulbactam under continuous veno-venous hemodialysis (CVVHD) in intensive care patients with acute renal failure.
Drewelow, B; Ehmcke, H; Hickstein, H; Rohde, B; Werner, U, 1997
)
0.3
"Due to high hepatobiliary clearance of mezlocillin, dosage adjustments in patients with acute renal failure, treated by CVVHD, are needed only with concurrent impaired liver function."( Pharmacokinetics of mezlocillin and sulbactam under continuous veno-venous hemodialysis (CVVHD) in intensive care patients with acute renal failure.
Drewelow, B; Ehmcke, H; Hickstein, H; Rohde, B; Werner, U, 1997
)
0.3
" However, due to the absence of population pharmacokinetic studies in neonates and young infants, dosing regimens differ considerably in clinical practice."( Population pharmacokinetics and dosing optimization of mezlocillin in neonates and young infants.
Guo, ZX; Jiang, L; Lin, X; Tang, BH; Van Den Anker, J; Wang, ZR; Wu, YE; Yang, JJ; Yao, BF; Zhang, YX; Zhang, ZL; Zhao, W; Zhou, J, 2022
)
0.72
" When increasing the dosing frequency to q8h, a dose of 20 mg/kg resulted in 74."( Population pharmacokinetics and dosing optimization of mezlocillin in neonates and young infants.
Guo, ZX; Jiang, L; Lin, X; Tang, BH; Van Den Anker, J; Wang, ZR; Wu, YE; Yang, JJ; Yao, BF; Zhang, YX; Zhang, ZL; Zhao, W; Zhou, J, 2022
)
0.72
" Optimal dosing regimens based on this model were provided for use in neonatal infections."( Population pharmacokinetics and dosing optimization of mezlocillin in neonates and young infants.
Guo, ZX; Jiang, L; Lin, X; Tang, BH; Van Den Anker, J; Wang, ZR; Wu, YE; Yang, JJ; Yao, BF; Zhang, YX; Zhang, ZL; Zhao, W; Zhou, J, 2022
)
0.72
" Current studies focused on the effects of co- and/or postinhibition of VMAT2 on the acute and chronic effects of MDMA and on the dose-response relationship between MDMA-induced elevations in body temperature and subsequent reductions in indolamine concentrations."( Concurrent Inhibition of Vesicular Monoamine Transporter 2 Does Not Protect Against 3,4-Methylenedioxymethamphetamine (Ecstasy) Induced Neurotoxicity.
Cholanians, AB; Lau, SS; Monks, TJ; Phan, AV, 2019
)
0.51
" The tachykinin antagonist (20 microM) produced a shift to the right of the dose-response curves for inositol phosphate accumulation caused by SP and kassinin."( Effect of the tachykinin antagonist, [D-Pro4, D-Trp7,9,10] substance P-(4-11), on tachykinin- and histamine-induced inositol phosphate generation in intestinal smooth muscle.
Bailey, SJ; Holzer, P; Lippe, IT, 1987
)
0.27
" The order of potency, the maximal effect and the slope of the dose-response curve were examined with six tachykinins - substance P (SP), physalaemin, phyllomedusin, uperolein, eledoisin, kassinin - and several substance P fragments - SP-(2-11), SP-(3-11), SP-(4-11) and SP-(6-11)."( Interaction of tachykinins with an adrenergic receptor in the rat urinary bladder.
Mathison, R; Solomos, D, 1985
)
0.27
" Apnoea occurred with K and E throughout the effective dosage range."( Effect of substance P and other tachykinins on arterial pressure in guinea-pigs.
Hancock, JC; Hoover, DB, 1985
)
0.27
" Phenoxybenzamine did not affect the dose-response curves to SP, eledoisin-related peptide (ERP), kassinin, eledoisin or physalaemin, nor did it affect the responses to individual doses of DPDPDT or DT79."( A study of [D-Pro2, D-Phe7, D-Trp9]-substance P and [D-Trp7,9]-substance P as tachykinin partial agonists in the rat colon.
Bailey, SJ; Jordan, CC, 1984
)
0.27
[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
penicillinAny member of the group of substituted penams containing two methyl substituents at position 2, a carboxylate substituent at position 3 and a carboxamido group at position 6.
penicillin allergenAny penicillin which causes the onset of an allergic reaction.
indolamine
[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 (6)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
AR proteinHomo sapiens (human)Potency21.78260.000221.22318,912.5098AID743040; AID743042; AID743054
estrogen nuclear receptor alphaHomo sapiens (human)Potency11.88320.000229.305416,493.5996AID743079
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency21.13170.001723.839378.1014AID743083
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency12.12960.000323.4451159.6830AID743065; AID743067
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.81070.009610.525035.4813AID1479145
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (52)

Assay IDTitleYearJournalArticle
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' 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]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
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
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID523273Antimicrobial activity against Escherichia coli HN1157/pHSG576oxa72010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Kinetic parameters of efflux of penicillins by the multidrug efflux transporter AcrAB-TolC of Escherichia coli.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID523266Activity at Escherichia coli isolate 7181 beta-lactamase OXA-72010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Kinetic parameters of efflux of penicillins by the multidrug efflux transporter AcrAB-TolC of Escherichia coli.
AID523271Lipophilicity, log P of the compound2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Kinetic parameters of efflux of penicillins by the multidrug efflux transporter AcrAB-TolC of Escherichia coli.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID660265Antimicrobial activity against wild type Escherichia coli expressing AcrAB-TolC efflux pump2012European journal of medicinal chemistry, Jun, Volume: 52Computational analysis of structure-based interactions and ligand properties can predict efflux effects on antibiotics.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID567091Drug absorption in human assessed as human intestinal absorption rate2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Prediction of drug intestinal absorption by new linear and non-linear QSPR.
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]
AID523272Antimicrobial activity against Escherichia coli HN1157/pHSG576oxa7 assessed as minimal drug concentration2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Kinetic parameters of efflux of penicillins by the multidrug efflux transporter AcrAB-TolC of Escherichia coli.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID523269Binding affinity to Escherichia coli isolate HN1157 AcrAB-TolC efflux transporter2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Kinetic parameters of efflux of penicillins by the multidrug efflux transporter AcrAB-TolC of Escherichia coli.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
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]
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID523268Activity at Escherichia coli isolate HN1157 AcrAB-TolC efflux transporter2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Kinetic parameters of efflux of penicillins by the multidrug efflux transporter AcrAB-TolC of Escherichia coli.
AID660261Ratio of MIC for wild type Escherichia coli JC7623 to MIC for acrAB-deficient Escherichia coli JZM1202012European journal of medicinal chemistry, Jun, Volume: 52Computational analysis of structure-based interactions and ligand properties can predict efflux effects on antibiotics.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
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]
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]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID523270Permeability across Escherichia coli HN1157/pHSG576oxa7 assessed as permeability coefficient in presence of proton uncoupler carbonyl cyanide meta-chlorophenylhydrazone2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Kinetic parameters of efflux of penicillins by the multidrug efflux transporter AcrAB-TolC of Escherichia coli.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID523274Activity at Escherichia coli isolate 7181 beta-lactamase OXA-7 measured per mg of protein2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Kinetic parameters of efflux of penicillins by the multidrug efflux transporter AcrAB-TolC of Escherichia coli.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346346Human NK1 receptor (Tachykinin receptors)1996The Journal of biological chemistry, Aug-23, Volume: 271, Issue:34
The unpredicted high affinities of a large number of naturally occurring tachykinins for chimeric NK1/NK3 receptors suggest a role for an inhibitory domain in determining receptor specificity.
AID1346386Human NK3 receptor (Tachykinin receptors)1996The Journal of biological chemistry, Aug-23, Volume: 271, Issue:34
The unpredicted high affinities of a large number of naturally occurring tachykinins for chimeric NK1/NK3 receptors suggest a role for an inhibitory domain in determining receptor specificity.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (714)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990560 (78.43)18.7374
1990's94 (13.17)18.2507
2000's25 (3.50)29.6817
2010's17 (2.38)24.3611
2020's18 (2.52)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 41.13

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 Index41.13 (24.57)
Research Supply Index4.45 (2.92)
Research Growth Index4.27 (4.65)
Search Engine Demand Index59.70 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (41.13)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials157 (23.75%)5.53%
Trials0 (0.00%)5.53%
Trials0 (0.00%)5.53%
Reviews16 (2.42%)6.00%
Reviews6 (13.04%)6.00%
Reviews3 (3.53%)6.00%
Case Studies38 (5.75%)4.05%
Case Studies1 (2.17%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other450 (68.08%)84.16%
Other39 (84.78%)84.16%
Other82 (96.47%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (1)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Prospective Randomized Study to Compare Clinical Outcomes in Patients With Osteomyelitis Treated With Intravenous Antibiotics Versus Intravenous Antibiotics With an Early Switch to Oral Antibiotics [NCT02099240]Early Phase 111 participants (Actual)Interventional2014-03-06Terminated(stopped due to Not enough patient enrollment and lack of staffing)
[information is prepared from clinicaltrials.gov, extracted Sep-2024]