Page last updated: 2024-12-06

floxacillin

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Description

Floxacillin is a synthetic penicillin antibiotic that is effective against a wide range of gram-positive bacteria, including Staphylococcus aureus. It acts by inhibiting the synthesis of peptidoglycan, a key component of bacterial cell walls. Floxacillin is typically used to treat infections of the skin, respiratory tract, and urinary tract. It is also used to prevent infections in patients undergoing surgery. Floxacillin is well-absorbed from the gastrointestinal tract and has a relatively long half-life. It is available in both oral and intravenous formulations. Research into floxacillin focuses on understanding its mechanism of action, developing new formulations, and investigating its potential for use in treating various infections.'

Floxacillin: Antibiotic analog of CLOXACILLIN. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

flucloxacillin : A penicillin compound having a 6beta-[3-(2-chloro-6-fluorophenyl)-5-methyl-1,2-oxazole-4-carboxamido] side-chain. [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]

obliquine: obliquine is the (3S,4aS,11S,10bS)-isomer; isolated from Cyrtanthus obliquus; structure in first source; do not confuse with obliquin [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID21319
CHEMBL ID222645
CHEBI ID5098
SCHEMBL ID3823
MeSH IDM0008575
PubMed CID443685
CHEMBL ID4167757
CHEBI ID31929
MeSH IDM0008575

Synonyms (69)

Synonym
NCI60_002254
(2s,5r,6r)-6-({[3-(2-chloro-6-fluorophenyl)-5-methylisoxazol-4-yl]carbonyl}amino)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
nsc-277175
mfipc
D04196
flucloxacillin (inn)
floxacillin (usan)
flucloxacillin
5250-39-5
floxacillin
3-(2-chloro-6-fluorophenyl)-5-methyl-4-isoxazolylpenicillin
DB00301
(2s,5r,6r)-6-({[3-(2-chloro-6-fluorophenyl)-5-methyl-1,2-oxazol-4-yl]carbonyl}amino)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
6-(3-(2-chloro-6-fluorophenyl)-5-methyl-4-isoxazolecarboxamido)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo(3.2.0)heptane-2-carboxylic acid
flucloxacilline [inn-french]
4-thia-1-azabicyclo(3.2.0)heptane-2-carboxylic acid, 6-(((3-(2-chloro-6-fluorophenyl)-5-methyl-4-isoxazolyl)carbonyl)amino)-3,3-dimethyl-7-oxo-, (2s(2alpha,5alpha,6beta))
einecs 226-051-0
brl 2039
flucloxacillinum [inn-latin]
floxacillin [usan]
flucloxacilina [inn-spanish]
flucloxacilline
flucloxacilina
CHEBI:5098 ,
flucloxacillin-sodium
6beta-[3-(2-chloro-6-fluorophenyl)-5-methyl-1,2-oxazole-4-carboxamido]-2,2-dimethylpenam-3alpha-carboxylic acid
flucloxacillinum
brl-2039
flucloxacillin sodium anhydrous
CHEMBL222645
floxacillin sodium anhydrous
(2s,5r,6r)-6-[[3-(2-chloro-6-fluorophenyl)-5-methyl-1,2-oxazole-4-carbonyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
(2s,5r,6r)-6-[3-(2-chloro-6-fluorophenyl)-5-methyl-1,2-oxazole-4-amido]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
flucloxacillin [inn]
unii-43b2m34g2v
43b2m34g2v ,
bdbm50370590
EPITOPE ID:117416
floxacillin [mi]
flucloxacillin [who-dd]
flucloxacillin [mart.]
4-thia-1-azabicyclo(3.2.0)heptane-2-carboxylic acid, 6-(((3-(2-chloro-6-fluorophenyl)-5-methyl-4-isoxazolyl)carbonyl)amino)-3,3-dimethyl-7-oxo-, (2s(2.alpha.,5.alpha.,6.beta.))
6-[3-(2-chloro-6-fluorophenyl)-5-methyl-4-isoxazolecarboxamido]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
SCHEMBL3823
flucloxacillin, antibiotic for culture media use only
W-105817
DTXSID8023056
UIOFUWFRIANQPC-JKIFEVAISA-N
4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid,6-[[[3-(2-chloro-6-fluorophenyl)-5-methyl-4-isoxazolyl]carbonyl]amino]-3,3-dimethyl-7-oxo-,(2s,5r,6r)-
NCGC00485420-01
(2s,5r,6r)-6-(3-(2-chloro-6-fluorophenyl)-5-methylisoxazole-4-carboxamido)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
flucloxacillin,(s)
Q1994556
BRD-K27871792-001-01-8
gtpl10910
brl2039
EN300-19766067
CS-0017591
HY-A0246
inchi=1/c26h28n2o5/c1-27-23-12-19(31-2)7-9-26(23)20-13-22-21(32-15-33-22)11-17(20)14-28(24(26)25(27)30)10-8-16-3-5-18(29)6-4-16/h3-7,9,11,13,19,23-24,29h,8,10,12,14-15h2,1-2h3/t19-,23+,24-,26+/m1/s
3s,4as,11s,10bs-3,4,4a,13,11,5,6-heptahydro-5[2-(4-hydroxyphenyl)ethyl]-3-methoxy-13-methyl-[1,3-dioxolo[4,5-g]indolo[3,3a-c]]-isoquinolin-12-one
rel-(3r,4ar,6ar,13br)-7-[2-(4-hydroxyphenyl)ethyl]-3-methoxy-5-methyl-3,4,4a,5,7,8-hexahydro[1,3]dioxolo[4,5-g]indolo[3,3a-c]isoquinolin-6(6ah)-one
obliquine
C12183 ,
CHEBI:31929
(1s,13s,16s,18s)-12-[2-(4-hydroxyphenyl)ethyl]-18-methoxy-15-methyl-5,7-dioxa-12,15-diazapentacyclo[11.7.0.01,16.02,10.04,8]icosa-2,4(8),9,19-tetraen-14-one
Q27114728
bdbm50278119
CHEMBL4167757 ,

Research Excerpts

Overview

Floxacilline is a beta-lactam antibiotic of the penicillin class.

ExcerptReferenceRelevance
"Floxacilline is a beta-lactam antibiotic of the penicillin class. "( [Gangrene of the hand due to accidental intra-arterial injection of floxacilline: about a case].
Aghoutane, EM; Fezzazi, RE; Salama, T, 2016
)
2.11

Toxicity

ExcerptReferenceRelevance
" Remaining BEC preparations exhibited no toxic response."( Indirect cytotoxicity of flucloxacillin toward human biliary epithelium via metabolite formation in hepatocytes.
Balladur, P; Beaune, PH; Becquemont, L; Dansette, PM; Delelo, R; Housset, C; Lakehal, F; Lasnier, E; Poupon, R, 2001
)
0.31
" Considering the high prevalence of soft-tissue infections in HIV patients, we conducted a retrospective study to investigate whether flucloxacillin use was associated with adverse events in HIV patients known to be HLA-B*5701 positive."( The safety of flucloxacillin in HIV-infected patients with positive HLA-B*5701 genotype.
Cooke, G; Mackie, N; Naous, N; Vera, JH; Winston, A, 2013
)
0.39
"To determine the existence of concentration-toxicity relationships for common β-lactam antibiotic adverse effects and define thresholds above which toxicity is more likely."( Too much of a good thing: a retrospective study of β-lactam concentration-toxicity relationships.
Buscher, H; Gentili, S; Imani, S; Marriott, D; Sandaradura, I, 2017
)
0.46
" Adverse events investigated included neurotoxicity, nephrotoxicity, hepatotoxicity and opportunistic Clostridium difficile infection."( Too much of a good thing: a retrospective study of β-lactam concentration-toxicity relationships.
Buscher, H; Gentili, S; Imani, S; Marriott, D; Sandaradura, I, 2017
)
0.46
"Our data reveal an association between toxic concentrations for a number of β-lactam agents and neurotoxic/nephrotoxic effects."( Too much of a good thing: a retrospective study of β-lactam concentration-toxicity relationships.
Buscher, H; Gentili, S; Imani, S; Marriott, D; Sandaradura, I, 2017
)
0.46
" The primary outcome was treatment failure, which was defined as no clinical improvement or occurrence of an adverse event, resulting in a change in empiric antibiotics within 48 h of the first dose."( Efficacy and safety of intravenous ceftriaxone at home versus intravenous flucloxacillin in hospital for children with cellulitis (CHOICE): a single-centre, open-label, randomised, controlled, non-inferiority trial.
Babl, FE; Bryant, PA; Daley, AJ; Hopper, SM; Ibrahim, LF; Orsini, F, 2019
)
0.51
" Fewer children treated at home than in hospital had an adverse event (two [2%] vs ten [11%]; p=0·048)."( Efficacy and safety of intravenous ceftriaxone at home versus intravenous flucloxacillin in hospital for children with cellulitis (CHOICE): a single-centre, open-label, randomised, controlled, non-inferiority trial.
Babl, FE; Bryant, PA; Daley, AJ; Hopper, SM; Ibrahim, LF; Orsini, F, 2019
)
0.51
" We aimed to determine the incidence of flucloxacillin-induced hepatotoxicity in children receiving IV therapy as well as identify risk factors for this adverse drug reaction."( Incidence and predisposing factors for flucloxacillin-related hepatotoxicity in children.
Coombs, S; Gwee, A; Pittet, LF; Tang, K, 2023
)
0.91
" Severe hepatotoxicity (Common Terminology Criteria for Adverse Events grade 3 or above) occurred in 9/66 (14%) for bilirubin, 13/66 (20%) for ALT and 10/66 (15%) for GGT."( Incidence and predisposing factors for flucloxacillin-related hepatotoxicity in children.
Coombs, S; Gwee, A; Pittet, LF; Tang, K, 2023
)
0.91

Pharmacokinetics

ExcerptReferenceRelevance
"1 A pharmacokinetic study on flucloxacillin and cloxacillin was performed to investigate the factors contributing to the higher serum concentrations reported for the former after oral administration."( Pharmacokinetics of flucloxacillin and cloxacillin in healthy subjects and patients on chronic intermittent haemodialysis.
Mattie, H; Nauta, EH, 1975
)
0.25
" The terminal half-life averaged 4 h 38 min and was significantly correlated with gestational age."( Pharmacokinetics of free and total flucloxacillin in newborn infants.
Broberger, U; Ehrnebo, M; Herngren, L, 1987
)
0.27
" The pharmacokinetic parameters of both substances basically do not depend on the presence of the other."( Pharmacokinetics of amoxicillin and flucloxacillin following the simultaneous intravenous administration of 4 g and 1 g, respectively.
Adam, D; Heilmann, HD; Koeppe, P,
)
0.13
" The pharmacokinetic (PK)-pharmacodynamic (PD) breakpoint of flucloxacillin has not been determined by the use of population PK."( Population pharmacokinetics at two dose levels and pharmacodynamic profiling of flucloxacillin.
Bulitta, JB; Drusano, GL; Holzgrabe, U; Kinzig-Schippers, M; Kirkpatrick, CM; Landersdorfer, CB; Sörgel, F, 2007
)
0.34
" 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
"To describe the total and unbound plasma concentration-time profiles for highly protein-bound flucloxacillin (95%-97% protein binding) in critically ill patients with hypoalbuminaemia and without severe renal dysfunction, and to use population pharmacokinetic modelling and Monte Carlo simulations to assess the probability of target attainment against an MIC distribution."( Flucloxacillin dosing in critically ill patients with hypoalbuminaemia: special emphasis on unbound pharmacokinetics.
Lipman, J; Rello, J; Roberts, JA; Ulldemolins, M; Wallis, SC, 2010
)
0.36
" Population pharmacokinetic modelling of unbound plasma data and Monte Carlo simulations were then undertaken with NONMEM."( Flucloxacillin dosing in critically ill patients with hypoalbuminaemia: special emphasis on unbound pharmacokinetics.
Lipman, J; Rello, J; Roberts, JA; Ulldemolins, M; Wallis, SC, 2010
)
0.36
" Monte Carlo simulations suggest that continuous infusion of 8 g/24 h flucloxacillin would enable 100% successful attainment of the pharmacodynamic target, 50% fT( > MIC)."( Flucloxacillin dosing in critically ill patients with hypoalbuminaemia: special emphasis on unbound pharmacokinetics.
Lipman, J; Rello, J; Roberts, JA; Ulldemolins, M; Wallis, SC, 2010
)
0.36
"The pharmacokinetic parameters including AUC and T1/2 were significantly different among the PXR genotype groups."( PXR polymorphisms and their impact on pharmacokinetics/pharmacodynamics of repaglinide in healthy Chinese volunteers.
Du, QQ; He, L; Jiang, XH; Wang, L; Wang, ZJ, 2013
)
0.39
" Modern pediatric pharmacokinetic study protocols frequently favor opportunistic, "scavenged" sampling."( Development of a Novel Multipenicillin Assay and Assessment of the Impact of Analyte Degradation: Lessons for Scavenged Sampling in Antimicrobial Pharmacokinetic Study Design.
Barker, CIS; Johnston, A; Kipper, K; Sharland, M; Standing, JF, 2018
)
0.48
"To measure the effect of probenecid, fasting and fed, on flucloxacillin pharmacokinetic and pharmacodynamic endpoints."( Probenecid and food effects on flucloxacillin pharmacokinetics and pharmacodynamics in healthy volunteers.
Begg, EJ; Begg, R; Chambers, ST; Everts, RJ; Gardiner, SJ; Turnidge, J; Zhang, M, 2020
)
0.56
" Flucloxacillin pharmacokinetic and pharmacodynamic endpoints were compared."( Probenecid and food effects on flucloxacillin pharmacokinetics and pharmacodynamics in healthy volunteers.
Begg, EJ; Begg, R; Chambers, ST; Everts, RJ; Gardiner, SJ; Turnidge, J; Zhang, M, 2020
)
0.56
" As an example of this pharmacodynamic improvement, the probability of target attainment of free concentrations above the minimum inhibitory concentration for Staphylococcus aureus (0."( Probenecid and food effects on flucloxacillin pharmacokinetics and pharmacodynamics in healthy volunteers.
Begg, EJ; Begg, R; Chambers, ST; Everts, RJ; Gardiner, SJ; Turnidge, J; Zhang, M, 2020
)
0.56
"Probenecid increased flucloxacillin exposure, with predicted pharmacodynamic effects greater than pharmacokinetic effects because of the altered shape of the concentration-time curve."( Probenecid and food effects on flucloxacillin pharmacokinetics and pharmacodynamics in healthy volunteers.
Begg, EJ; Begg, R; Chambers, ST; Everts, RJ; Gardiner, SJ; Turnidge, J; Zhang, M, 2020
)
0.56
" In critically ill patients, altered pharmacokinetic (PK) behaviour is common and known to influence the achievement of PK/pharmacodynamic targets."( Optimization of flucloxacillin dosing regimens in critically ill patients using population pharmacokinetic modelling of total and unbound concentrations.
Brüggemann, RJM; Jager, NGL; Lipman, J; Roberts, JA; Ulldemolins, M; van Hest, RM; Wong, G; Xie, J, 2020
)
0.56
" We developed a population pharmacokinetic model of free flucloxacillin concentrations within Monolix, and used Monte Carlo simulation to explore optimal dosing regimens to attain PK/PD targets proposed in the literature (free drug time above minimum inhibitory concentration)."( Population pharmacokinetics of free flucloxacillin in patients treated with oral flucloxacillin plus probenecid.
Chambers, ST; Drennan, PG; Everts, RJ; Gardiner, SJ; Green, JK; Kirkpatrick, CMJ; Metcalf, SCL; Zhang, M, 2021
)
0.62
" To identify flucloxacillin dosing regimens that result in theoretically therapeutic concentrations, we developed a population pharmacokinetic (PK) model for the porcine data, and combined it with a human flucloxacillin population PK model for simulations."( Population Pharmacokinetics of Flucloxacillin In Bone and Soft Tissue- Standard Dosing is Not Sufficient to Achieve Therapeutic Concentrations.
Bendtsen, M; Bue, M; Friberg, LE; Hanberg, P; Öbrink-Hansen, K; Pham, AD; Slater, J; Stilling, M; Thorsted, A, 2022
)
0.72

Compound-Compound Interactions

ExcerptReferenceRelevance
"111 febrile episodes in 98 neutropenic children were randomly treated with either ceftazidime (CAZ) 150 mg/kg/day or with piperacillin (PIP) 200 mg/kg/day, both combined with flucloxacillin (FLUC) 50 mg/kg/day."( A randomised comparison of ceftazidime and piperacillin, both in combination with flucloxacillin for treatment of febrile episodes in neutropenic children. Finnish Three-Centre Study.
Herva, E; Hovi, L; Lanning, M; Mäkipernaa, A; Perkkiö, M; Rajantie, J; Renkonen, OV; Ruuskanen, O; Salmi, T; Williams, K, 1990
)
0.28
" The in vitro results corroborated this drug-drug interaction and correlated to the clinical findings."( Dicloxacillin-warfarin drug-drug interaction-A register-based study and in vitro investigations in 3D spheroid primary human hepatocytes.
Dalgård Dunvald, AC; Ernst, MT; Hammer, HS; Järvinen, E; Pottegård, A; Pötz, O; Stage, TB, 2023
)
0.91

Bioavailability

ExcerptReferenceRelevance
"Magnapen is a combination of two well-proven semi-snythetic penicillins which together offer the theoretical advantages of a broad spectrum of activity, good bioavailability and a low incidence of side-effects."( Magnapen treatment of infections in the elderly.
Middleton, RS; Sinha, HK, 1979
)
0.26
" This assay has been employed in a study of the relative bioavailability of two commercial flucloxacillin sodium capsules in ten healthy volunteers."( Optimization of high-performance liquid chromatographic analysis for isoxazolyl penicillins using factorial design.
Hung, CT; Lam, FC; Lim, JK; Zoest, AR, 1988
)
0.27
"The bioavailability of commercial liquid preparations of di- and flucloxacillin was compared in infants and children."( Plasma concentration following oral administration of di- and flucloxacillin in infants and children.
Bergdahl, S; Eriksson, M; Finkel, Y, 1987
)
0.27
" Bioavailability after oral administration, when corrected for changes in terminal half-life, was 47."( Pharmacokinetics of free and total flucloxacillin in newborn infants.
Broberger, U; Ehrnebo, M; Herngren, L, 1987
)
0.27
"The bioavailability of flucloxacillin (Heracillin) following oral administration was determined in infants and children."( Oral absorption of flucloxacillin in infants and young children.
Bergdahl, S; Eriksson, M; Finkel, Y; Lännergren, K, 1986
)
0.27
"The bioavailability of cloxacillin and flucloxacillin were compared after the oral administration, in capsule form, of 500 mg cloxacillin or 250 mg flucloxacillin to healthy volunteers."( Comparative bioavailability and half-lives of cloxacillin and flucloxacillin.
Paton, DM, 1986
)
0.27
"The comparative bioavailability of two formulations of 250 mg flucloxacillin sodium capsules in eight fasted healthy volunteers was examined."( Bioavailability and half-life of two preparations of flucloxacillin.
Avery, RJ; Mander, P; Paton, DM, 1982
)
0.26
"The pharmacokinetics and oral bioavailability of flucloxacillin were studied in five female and two male patients (age 68-87 yr) who had been hospitalized for orthopedic surgeries."( Pharmacokinetics and bioavailability of flucloxacillin in elderly hospitalized patients.
Charles, B; Gath, J; Sampson, J; Smithurst, B, 1995
)
0.29
"Two new bioavailability parameters were recently suggested [Koeleman et al."( The application of new bioavailability parameters in the bioequivalence testing of antimicrobial agents.
Ellis, SM; Koeleman, HA; Steyn, HS; Wessels, JC, 1993
)
0.29
"The utilization of the membrane transport protein PEPT1 as a drug delivery system is a promising strategy to enhance the oral bioavailability of drugs."( Three-dimensional quantitative structure-activity relationship analyses of beta-lactam antibiotics and tripeptides as substrates of the mammalian H+/peptide cotransporter PEPT1.
Biegel, A; Brandsch, M; Gebauer, S; Hartrodt, B; Neubert, K; Thondorf, I, 2005
)
0.33
" Human oral bioavailability is an important pharmacokinetic property, which is directly related to the amount of drug available in the systemic circulation to exert pharmacological and therapeutic effects."( Hologram QSAR model for the prediction of human oral bioavailability.
Andricopulo, AD; Moda, TL; Montanari, CA, 2007
)
0.34
"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
" Prospective studies evaluating bioavailability of antimicrobial agents after oral administration in SBS patients are lacking."( Oral antimicrobial agents in patients with short bowel syndrome: worth a try!
Brüggemann, RJM; Gompelman, M; Jager, NGL; Korzilius, JW; Rovers, CP; Wanten, GJA; Wezendonk, GTJ, 2023
)
0.91
"To determine the bioavailability of orally administered antimicrobial agents commonly used for treatment in SBS patients to guide clinical decision making when faced with infections."( Oral antimicrobial agents in patients with short bowel syndrome: worth a try!
Brüggemann, RJM; Gompelman, M; Jager, NGL; Korzilius, JW; Rovers, CP; Wanten, GJA; Wezendonk, GTJ, 2023
)
0.91
" Primary outcome was the oral bioavailability of these antimicrobial agents."( Oral antimicrobial agents in patients with short bowel syndrome: worth a try!
Brüggemann, RJM; Gompelman, M; Jager, NGL; Korzilius, JW; Rovers, CP; Wanten, GJA; Wezendonk, GTJ, 2023
)
0.91
" The median observed (IQR) bioavailability of ciprofloxacin, clindamycin, flucloxacillin and fluconazole were 36% (24-50), 93% (56-106), 50% (32-76) and 98% (61-107), respectively."( Oral antimicrobial agents in patients with short bowel syndrome: worth a try!
Brüggemann, RJM; Gompelman, M; Jager, NGL; Korzilius, JW; Rovers, CP; Wanten, GJA; Wezendonk, GTJ, 2023
)
0.91
"The bioavailability of selected antimicrobial agents in certain patients with SBS appeared to be better than expected, providing a feasible treatment option."( Oral antimicrobial agents in patients with short bowel syndrome: worth a try!
Brüggemann, RJM; Gompelman, M; Jager, NGL; Korzilius, JW; Rovers, CP; Wanten, GJA; Wezendonk, GTJ, 2023
)
0.91
" Oral population PK models for flucloxacillin and amoxicillin enabled estimation of first-order absorption rate constants (1."( The Neonatal and Paediatric Pharmacokinetics of Antimicrobials study (NAPPA): investigating amoxicillin, benzylpenicillin, flucloxacillin and piperacillin pharmacokinetics from birth to adolescence.
Barker, CIS; Johnston, A; Kim, M; Kipper, K; Lonsdale, DO; Sharland, M; Standing, JF; Thompson, G; Turner, MA; Wright, K, 2023
)
0.91

Dosage Studied

ExcerptRelevanceReference
" Once-daily dosing of amikacin produced greater initial killing than thrice daily dosing (P less than ."( Amikacin, ceftazidime, and flucloxacillin against suspended and adherent Pseudomonas aeruginosa and Staphylococcus epidermidis in an in vitro model of infection.
Blaser, J; Vergères, P, 1992
)
0.28
" Dose-response relations and kinetics of killing of intracellular bacteria by antibiotics in the free and encapsulated form were studied under different conditions using J 774 mouse macrophages, because phagocytes from CGD patients are not available in great amounts."( Staphylococci surviving intracellularly in phagocytes from patients suffering from chronic granulomatous disease are killed in vitro by antibiotics encapsulated in liposomes.
Hockertz, S; Lohmann-Matthes, ML; Roesler, J; Vogt, B, 1991
)
0.28
"19F NMR spectroscopy was used to monitor the metabolites of flucloxacillin in the urine of a rat dosed with its sodium salt."( 19F NMR spectroscopy study of the metabolites of flucloxacillin in rat urine.
Everett, JR; Jennings, K; Woodnutt, G, 1985
)
0.27
" Patients were assigned at random to receive 4 to 10 days' treatment with either mupirocin applied 3-times daily or one of the oral antibiotics in the dosage normally used by the general practitioner for skin infections."( A comparison of the new topical antibiotic mupirocin ('Bactroban') with oral antibiotics in the treatment of skin infections in general practice.
Ah Chan, M; Fetherston, J; Hague, IK; Haycock, D; Hunter, P; Kanji, K; Robertson, WD; Villiger, JW, 1986
)
0.27
" After this period revascularization of a bone graft may be assumed to have progressed to such a degree, that thereafter the graft can "defend itself" against invading micro-organisms, if necessary supported by further lower dosage antibiotic treatment."( Wound infection after mandibular reconstruction with autogenous graft.
Egyedi, P, 1986
)
0.27
" The flucloxacillin dosage used was 1 g orally three times daily for three days, and the serum and exudate concentrations were measured repeatedly during a 10 h-period following the first and the seventh dose."( Flucloxacillin in chronic leg ulcers. Penetration of flucloxacillin into chronic leg ulcer exudate and the effect on the bacteria.
Hofmann, B; Sandberg Sørensen, T; Slotsbjerg, T; Stürup, J, 1987
)
0.27
"Per-operative serum and wound fluid concentrations achieved by two flucloxacillin dosage regimens were measured in twelve patients undergoing open heart surgery."( Flucloxacillin concentration in serum and wound exudate during open heart surgery.
Farrington, M; Fenn, A; Phillips, I, 1985
)
0.27
" The dosage schedules used for cloxacillin and flucloxacillin gave satisfactory serum concentrations peroperatively."( Pacemaker infections. A clinical study with special reference to prophylactic use of some isoxazolyl penicillins.
Bluhm, G, 1985
)
0.27
" In the other 27 courses there was an excellent clinical response, judged to be as good as our former high dosage carbenicillin and tobramycin combination though with much greater patient acceptability."( Ceftazidime - a significant advance in the treatment of cystic fibrosis.
Connor, PJ; David, TJ; Phillips, BM, 1983
)
0.27
" For oxytetracycline, flucloxacillin and amoxycillin, the conventional bioavailability parameters indicated partial equivalence whereas using the te and to parameters, more realistic indications of the possible extent of the performance of a drug from dosage forms were obtained than with the conventional bioequivalence parameters."( The application of new bioavailability parameters in the bioequivalence testing of antimicrobial agents.
Ellis, SM; Koeleman, HA; Steyn, HS; Wessels, JC, 1993
)
0.29
" In this study, we have been able to demonstrate the usefulness of a reproducible long-time antimicrobial dosage regime from the internal phase of the implant as compared to surface coated polymers."( Drug delivery concepts for the efficacious prevention of foreign-body infections.
Pulverer, G; Rump, A; Schierholz, JM, 1996
)
0.29
" The method is applicable for the assay of the four drugs under investigation in different dosage forms and the results are in good agreement with those obtained by the official method."( Spectrophotometric determination of ampicillin, dicluxacillin, flucloxacillin and amoxicillin antibiotic drugs: ion-pair formation with molybdenum and thiocyanate.
Mohamed, GG, 2001
)
0.31
"These cases suggest that flucloxacillin should be used with greater caution and guidelines for dosing and clinical monitoring (regular neutrophil counts) need to be reassessed, despite none of these patients experiencing serious sequelae."( Flucloxacillin associated neutropenia in children treated for bone and joint infections.
Kristiansen, JB; Stott, NS; van den Boom, J; Voss, LM,
)
0.13
" The proposed methods were applied successfully to the determination of the examined drug either in pure or pharmaceutical dosage forms with good accuracy and precision."( Spectrophotometric and electrical studies of charge-transfer complexes of sodium flucloxacillin with pi-acceptors.
El-Didamony, AM; Refat, MS, 2006
)
0.33
" The current dosage regimen, 25 or 50 mg/kg every 8 or 12 hours, did not result in effective plasma concentrations for the treatment of Staphylococcus aureus in 17 (31%) of the 55 neonates."( Population pharmacokinetics and dosing of flucloxacillin in preterm and term neonates.
de Rozario, L; Degraeuwe, PL; Pullen, J; Stolk, LM; van Tiel, FH; Zimmermann, LJ, 2006
)
0.33
"A simple, rapid, accurate sensitive spectrophotometry procedure for the determination of amoxycillin (Amox) and flucloxacillin (Fluclox) in bulk samples and in dosage forms are developed."( Utilization of ion exchanger and spectrophotometry for assaying amoxycillin and flucloxacillin in dosage form.
Aly, HM; Amin, AS, 2007
)
0.34
" Because of the high variability of protein binding among infants, it is difficult to devise a flucloxacillin dosage regimen effective for all infants."( Protein binding of flucloxacillin in neonates.
Degraeuwe, PL; Neef, C; Pullen, J; Stolk, LM; van Tiel, FH; Zimmermann, LJ, 2007
)
0.34
" We compared the breakpoints for flucloxacillin between several dosage regimens."( Population pharmacokinetics at two dose levels and pharmacodynamic profiling of flucloxacillin.
Bulitta, JB; Drusano, GL; Holzgrabe, U; Kinzig-Schippers, M; Kirkpatrick, CM; Landersdorfer, CB; Sörgel, F, 2007
)
0.34
" Parallel one-dimensional (1D) 800 MHz 1H and 753 MHz 19F{1H} spectra (n = 21) were obtained on urine samples collected from volunteers (n = 6) at various intervals up to 24 h after oral dosing with 500 mg of flucloxacillin."( Heteronuclear 19F-1H statistical total correlation spectroscopy as a tool in drug metabolism: study of flucloxacillin biotransformation.
Athersuch, TJ; Beckonert, O; Holmes, E; Keun, HC; Lindon, JC; Nicholson, JK; Saric, J; Shockcor, JP; Wang, Y; Wilson, ID, 2008
)
0.35
" 800 MHz (1)H spectra of human urine (n = 21) collected over 10 h following dosing with the antibiotic flucloxacillin and 600 MHz (1)H NMR spectra of rat urine (n = 27) collected over 48 h following exposure to the renal papillary toxin 2-bromoethanamine (BEA)."( Statistical total correlation spectroscopy editing of 1H NMR spectra of biofluids: application to drug metabolite profile identification and enhanced information recovery.
Coen, M; Ebbels, TM; Holmes, E; Lindon, JC; Maher, AD; Nicholson, JK; Sands, CJ, 2009
)
0.35
" Unbound flucloxacillin concentrations after 2 g bolus fell below 1 mg/L 4 h after the end of the infusion, providing evidence that standard dosing would be insufficient for the treatment of methicillin-susceptible Staphylococcus aureus (MSSA) (MIC = 2 mg/L)."( Flucloxacillin dosing in critically ill patients with hypoalbuminaemia: special emphasis on unbound pharmacokinetics.
Lipman, J; Rello, J; Roberts, JA; Ulldemolins, M; Wallis, SC, 2010
)
0.36
" Our data emphasize the importance of using unbound concentrations for determining dosage regimens for highly bound antibiotics."( Flucloxacillin dosing in critically ill patients with hypoalbuminaemia: special emphasis on unbound pharmacokinetics.
Lipman, J; Rello, J; Roberts, JA; Ulldemolins, M; Wallis, SC, 2010
)
0.36
" We designed a simplified OAT (test B) in which iv therapy is continued and oral dosing is performed after a 1-hour fast."( A simplified oral flucloxacillin absorption test for patients requiring long-term treatment.
Burggraaf, J; Dijkmans, AC; Hartigh, Jd; van Dissel, JT, 2012
)
0.38
"The British National Formulary for Children (BNFC) recommends dosing oral penicillins according to age-bands, weight-bands, or weight-based calculations."( Oral penicillin prescribing for children in the UK: a comparison with BNF for Children age-band recommendations.
Barker, C; Ismael, Z; Long, PF; Murray, ML; Saxena, S; Sharland, M; Wong, IC, 2014
)
0.4
" Similar variations in dosing across age-bands were observed for phenoxymethylpenicillin and flucloxacillin."( Oral penicillin prescribing for children in the UK: a comparison with BNF for Children age-band recommendations.
Barker, C; Ismael, Z; Long, PF; Murray, ML; Saxena, S; Sharland, M; Wong, IC, 2014
)
0.4
"There is wide variation in the dosing of penicillins for children in UK primary care, with very few children being prescribed the current national recommended doses."( Oral penicillin prescribing for children in the UK: a comparison with BNF for Children age-band recommendations.
Barker, C; Ismael, Z; Long, PF; Murray, ML; Saxena, S; Sharland, M; Wong, IC, 2014
)
0.4
"1 µg/mL) with standard intermittent bolus dosing of 2 g every 4 hours."( Low flucloxacillin concentrations in a patient with central nervous system infection: the need for plasma and cerebrospinal fluid drug monitoring in the ICU.
Abdul-Aziz, MH; Lipman, J; McDonald, C; McWhinney, B; Roberts, JA; Ungerer, JP, 2014
)
0.4
"There is a need to understand better the reasons for increased prescribing of flucloxacillin in primary care, optimal dosing (and the need to co-prescribe other antibiotics) and the reasons why one in five patients are prescribed a further antibiotic within 4 weeks."( Understanding flucloxacillin prescribing trends and treatment non-response in UK primary care: a Clinical Practice Research Datalink (CPRD) study.
Butler, CC; Francis, NA; Hood, K; Lyons, R, 2016
)
0.43
" Beta-lactam chemical instability in plasma can cause misleading pharmacokinetic modeling results, which could impact upon model-based dosing recommendations and the forthcoming era of beta-lactam therapeutic drug monitoring."( Development of a Novel Multipenicillin Assay and Assessment of the Impact of Analyte Degradation: Lessons for Scavenged Sampling in Antimicrobial Pharmacokinetic Study Design.
Barker, CIS; Johnston, A; Kipper, K; Sharland, M; Standing, JF, 2018
)
0.48
" Dopamine dosing was increased and norepinephrine infusion was added subsequently with immediate stabilisation of DBP."( Teenage boy with high fever and rash: what could we be missing?
Carvalho, L; Costa, FD; Costa, S; Dionísio, T; Oliveira, GN, 2018
)
0.48
"Flucloxacillin dosing may be guided by measurement of its total plasma concentrations."( Total flucloxacillin plasma concentrations poorly reflect unbound concentrations in hospitalized patients with Staphylococcus aureus bacteraemia.
Begg, EJ; Chambers, ST; Chin, PKL; Dalton, SC; Drennan, PG; Gardiner, SJ; Zhang, M, 2018
)
0.48
" For this, OAT IV therapy is continued and oral dosing is performed after a one-hour fast and implemented after a small study."( The simplified oral flucloxacillin absorption test: an accurate method to identify patients with inadequate oral flucloxacillin absorption.
Balmforth, C; Burggraaf, J; Dijkmans, AC; Kamerling, IMC; Kweekel, DM; van Dissel, JT; van Esdonk, MJ, 2019
)
0.51
"To describe population PK and optimized dosing regimens for flucloxacillin in critically ill patients."( Optimization of flucloxacillin dosing regimens in critically ill patients using population pharmacokinetic modelling of total and unbound concentrations.
Brüggemann, RJM; Jager, NGL; Lipman, J; Roberts, JA; Ulldemolins, M; van Hest, RM; Wong, G; Xie, J, 2020
)
0.56
" Finally, frequently prescribed dosing regimens were evaluated using Monte Carlo simulations."( Optimization of flucloxacillin dosing regimens in critically ill patients using population pharmacokinetic modelling of total and unbound concentrations.
Brüggemann, RJM; Jager, NGL; Lipman, J; Roberts, JA; Ulldemolins, M; van Hest, RM; Wong, G; Xie, J, 2020
)
0.56
" The concentrations of the antibiotics showed a wide range because of the fixed dosing regimen in a mixed population with variable kidney function."( Measurement of Free Plasma Concentrations of Beta-Lactam Antibiotics: An Applicability Study in Intensive Care Unit Patients.
Dorn, C; Hitzenbichler, F; Kees, F; Kees, MG; Kratzer, A; Lubnow, M; Salzberger, B; Schießer, S, 2021
)
0.62
" However, currently recommended dosing regimens may expose patients to excessive flucloxacillin concentrations, potentially resulting in drug-related organ damage."( Probability of pharmacological target attainment with flucloxacillin in Staphylococcus aureus bloodstream infection: a prospective cohort study of unbound plasma and individual MICs.
Bassetti, S; Dräger, S; Guertler, N; Hinic, V; Moser, S; Osthoff, M; Rehm, S; Rentsch, KM; Sendi, P, 2021
)
0.62
" The aims of this study were to develop a population PK model of free flucloxacillin when administered orally with probenecid, and to identify optimal dosing regimens for this combination."( Population pharmacokinetics of free flucloxacillin in patients treated with oral flucloxacillin plus probenecid.
Chambers, ST; Drennan, PG; Everts, RJ; Gardiner, SJ; Green, JK; Kirkpatrick, CMJ; Metcalf, SCL; Zhang, M, 2021
)
0.62
" We developed a population pharmacokinetic model of free flucloxacillin concentrations within Monolix, and used Monte Carlo simulation to explore optimal dosing regimens to attain PK/PD targets proposed in the literature (free drug time above minimum inhibitory concentration)."( Population pharmacokinetics of free flucloxacillin in patients treated with oral flucloxacillin plus probenecid.
Chambers, ST; Drennan, PG; Everts, RJ; Gardiner, SJ; Green, JK; Kirkpatrick, CMJ; Metcalf, SCL; Zhang, M, 2021
)
0.62
" Predicted PK/PD target attainment was suboptimal with standard dosing regimens with flucloxacillin alone, but substantially improved in the presence of probenecid."( Population pharmacokinetics of free flucloxacillin in patients treated with oral flucloxacillin plus probenecid.
Chambers, ST; Drennan, PG; Everts, RJ; Gardiner, SJ; Green, JK; Kirkpatrick, CMJ; Metcalf, SCL; Zhang, M, 2021
)
0.62
" Patients with higher FFM and eGFR may require the addition of probenecid and 6-hourly dosing to achieve PK/PD targets."( Population pharmacokinetics of free flucloxacillin in patients treated with oral flucloxacillin plus probenecid.
Chambers, ST; Drennan, PG; Everts, RJ; Gardiner, SJ; Green, JK; Kirkpatrick, CMJ; Metcalf, SCL; Zhang, M, 2021
)
0.62
"To describe the unbound and total flucloxacillin pharmacokinetics in critically ill patients and to define optimal dosing strategies."( High unbound flucloxacillin fraction in critically ill patients.
Brüggemann, RJ; Burger, DM; de Lange, DW; de Maat, MM; Frenzel, T; Gieling, EM; Kolwijck, E; Pickkers, P; Schouten, JA; Ten Oever, J; Ter Heine, R; van Leeuwen, H; Wallenburg, E, 2021
)
0.62
" Monte Carlo simulations were performed to predict the unbound flucloxacillin concentrations for different dosing strategies and different categories of endogenous CLCR."( High unbound flucloxacillin fraction in critically ill patients.
Brüggemann, RJ; Burger, DM; de Lange, DW; de Maat, MM; Frenzel, T; Gieling, EM; Kolwijck, E; Pickkers, P; Schouten, JA; Ten Oever, J; Ter Heine, R; van Leeuwen, H; Wallenburg, E, 2021
)
0.62
" To identify flucloxacillin dosing regimens that result in theoretically therapeutic concentrations, we developed a population pharmacokinetic (PK) model for the porcine data, and combined it with a human flucloxacillin population PK model for simulations."( Population Pharmacokinetics of Flucloxacillin In Bone and Soft Tissue- Standard Dosing is Not Sufficient to Achieve Therapeutic Concentrations.
Bendtsen, M; Bue, M; Friberg, LE; Hanberg, P; Öbrink-Hansen, K; Pham, AD; Slater, J; Stilling, M; Thorsted, A, 2022
)
0.72
"A four-compartment model was developed, and various dosing regimens and modes of administration were simulated."( Population Pharmacokinetics of Flucloxacillin In Bone and Soft Tissue- Standard Dosing is Not Sufficient to Achieve Therapeutic Concentrations.
Bendtsen, M; Bue, M; Friberg, LE; Hanberg, P; Öbrink-Hansen, K; Pham, AD; Slater, J; Stilling, M; Thorsted, A, 2022
)
0.72
" For intermittent IV dosing (4, 8 and 12g/24h), fT>MIC (0."( Population Pharmacokinetics of Flucloxacillin In Bone and Soft Tissue- Standard Dosing is Not Sufficient to Achieve Therapeutic Concentrations.
Bendtsen, M; Bue, M; Friberg, LE; Hanberg, P; Öbrink-Hansen, K; Pham, AD; Slater, J; Stilling, M; Thorsted, A, 2022
)
0.72
" Sufficient target tissue concentrations for treatment of spondylodiscitis may require a dose increase or alternative dosing regimens."( Steady-state concentrations of flucloxacillin in porcine vertebral cancellous bone and intervertebral disc following oral and intravenous administration assessed by microdialysis.
Bendtsen, MAF; Bue, M; Hanberg, P; Hansen, J; Öbrink-Hansen, K; Slater, J; Stilling, M, 2022
)
0.72
" This diagnosis was confirmed by an organic acid dosage in the urine."( [A case of pyroglutamic metabolic acidosis after cotreatment by flucloxacillin and paracetamol].
Desgranges, A; Hu, K; Monney Chaubert, C, 2022
)
0.72
"The proportion of patients with invasive methicillin-susceptible Staphylococcus aureus (MSSA) infection who achieve target concentrations of flucloxacillin or cefazolin with standard dosing regimens is uncertain."( Frequency of pharmacological target attainment with flucloxacillin and cefazolin in invasive methicillin-susceptible Staphylococcus aureus infection: a prospective cohort study in hospitalized patients.
Campbell, PO; Chambers, ST; Chin, PKL; Dalton, SC; Douglas, NM; Metcalf, SCL, 2023
)
0.91
"Standard dosing of flucloxacillin and cefazolin in the treatment of invasive MSSA infections may not achieve target plasma concentrations for a subgroup of patients."( Frequency of pharmacological target attainment with flucloxacillin and cefazolin in invasive methicillin-susceptible Staphylococcus aureus infection: a prospective cohort study in hospitalized patients.
Campbell, PO; Chambers, ST; Chin, PKL; Dalton, SC; Douglas, NM; Metcalf, SCL, 2023
)
0.91
" Monte Carlo dosing simulations were performed to assess target attainment."( Target attainment and population pharmacokinetics of flucloxacillin in critically ill patients: a multicenter study.
Foudraine, NA; Janssen, PKC; le Noble, JLML; Meenks, SD; Neef, K; Punt, N, 2023
)
0.91
"Based on our dosing simulations, standard flucloxacillin daily doses of up to 12 g may substantially enhance the risk of underdosing in critically ill patients."( Target attainment and population pharmacokinetics of flucloxacillin in critically ill patients: a multicenter study.
Foudraine, NA; Janssen, PKC; le Noble, JLML; Meenks, SD; Neef, K; Punt, N, 2023
)
0.91
"Standard once-daily dosing of ceftriaxone may not lead to adequate antibiotic exposure in all cases of Staphylococcus aureus bacteraemia (SAB)."( Comparative effectiveness of β-lactams for empirical treatment of methicillin-susceptible Staphylococcus aureus bacteraemia: a prospective cohort study.
Bonten, MJM; Buis, DTP; Herpers, BL; Jansen, RR; Prins, JM; Rozemeijer, W; Sieswerda, E; Sigaloff, KCE; Soetekouw, R; van der Meer, JTM; van der Vaart, TW; van Twillert, G; van Werkhoven, CH; Veenstra, J, 2023
)
0.91
" Four different dosing regimens were simulated: intermittent infusion in 30 min, prolonged infusion in 4 h, continuous infusion, and continuous infusion with a loading dose."( Optimization of β-Lactam Dosing Regimens in Neonatal Infections: Continuous and Extended Administration versus Intermittent Administration.
de Grauw, AM; Kruizinga, MD; Leegwater, E; Storm, BN; van Veen, M; Wewerinke, L, 2023
)
0.91
"For all antibiotics except cefotaxime, continuous infusion with a loading dose resulted in a higher PTA compared with other dosing regimens."( Optimization of β-Lactam Dosing Regimens in Neonatal Infections: Continuous and Extended Administration versus Intermittent Administration.
de Grauw, AM; Kruizinga, MD; Leegwater, E; Storm, BN; van Veen, M; Wewerinke, L, 2023
)
0.91
" Tacrolimus concentrations should be closely monitored, and dosing adjusted during and after flucloxacillin administration."( It cuts both ways: A single-center retrospective review describing a three-way interaction between flucloxacillin, voriconazole and tacrolimus.
Burrows, FS; Carlos, LM; Marriott, DJE; Stojanova, J, 2023
)
0.91
"Pharmacokinetic (PK) data underlying paediatric penicillin dosing remain limited, especially in critical care."( The Neonatal and Paediatric Pharmacokinetics of Antimicrobials study (NAPPA): investigating amoxicillin, benzylpenicillin, flucloxacillin and piperacillin pharmacokinetics from birth to adolescence.
Barker, CIS; Johnston, A; Kim, M; Kipper, K; Lonsdale, DO; Sharland, M; Standing, JF; Thompson, G; Turner, MA; Wright, K, 2023
)
0.91
" Antibiotic dosing followed standard of care."( The Neonatal and Paediatric Pharmacokinetics of Antimicrobials study (NAPPA): investigating amoxicillin, benzylpenicillin, flucloxacillin and piperacillin pharmacokinetics from birth to adolescence.
Barker, CIS; Johnston, A; Kim, M; Kipper, K; Lonsdale, DO; Sharland, M; Standing, JF; Thompson, G; Turner, MA; Wright, K, 2023
)
0.91
[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.
isoquinolinesA class of organic heteropolycyclic compound consisting of isoquinoline and its substitution derivatives.
[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 (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Bile salt export pumpRattus norvegicus (Norway rat)IC50 (µMol)429.10000.40002.75008.6000AID1209456
Bile salt export pumpHomo sapiens (human)IC50 (µMol)109.30000.11007.190310.0000AID1209455; AID1449628
Solute carrier family 15 member 1Homo sapiens (human)Ki3,200.00000.18003.39339.8000AID238858
AcetylcholinesteraseHomo sapiens (human)IC50 (µMol)200.00000.00000.933210.0000AID1501977
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (42)

Processvia Protein(s)Taxonomy
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
monoatomic ion transportSolute carrier family 15 member 1Homo sapiens (human)
protein transportSolute carrier family 15 member 1Homo sapiens (human)
peptide transportSolute carrier family 15 member 1Homo sapiens (human)
dipeptide import across plasma membraneSolute carrier family 15 member 1Homo sapiens (human)
tripeptide import across plasma membraneSolute carrier family 15 member 1Homo sapiens (human)
proton transmembrane transportSolute carrier family 15 member 1Homo sapiens (human)
acetylcholine catabolic process in synaptic cleftAcetylcholinesteraseHomo sapiens (human)
regulation of receptor recyclingAcetylcholinesteraseHomo sapiens (human)
osteoblast developmentAcetylcholinesteraseHomo sapiens (human)
acetylcholine catabolic processAcetylcholinesteraseHomo sapiens (human)
cell adhesionAcetylcholinesteraseHomo sapiens (human)
nervous system developmentAcetylcholinesteraseHomo sapiens (human)
synapse assemblyAcetylcholinesteraseHomo sapiens (human)
receptor internalizationAcetylcholinesteraseHomo sapiens (human)
negative regulation of synaptic transmission, cholinergicAcetylcholinesteraseHomo sapiens (human)
amyloid precursor protein metabolic processAcetylcholinesteraseHomo sapiens (human)
positive regulation of protein secretionAcetylcholinesteraseHomo sapiens (human)
retina development in camera-type eyeAcetylcholinesteraseHomo sapiens (human)
acetylcholine receptor signaling pathwayAcetylcholinesteraseHomo sapiens (human)
positive regulation of cold-induced thermogenesisAcetylcholinesteraseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (21)

Processvia Protein(s)Taxonomy
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
proton-dependent oligopeptide secondary active transmembrane transporter activitySolute carrier family 15 member 1Homo sapiens (human)
peptide:proton symporter activitySolute carrier family 15 member 1Homo sapiens (human)
tripeptide transmembrane transporter activitySolute carrier family 15 member 1Homo sapiens (human)
dipeptide transmembrane transporter activitySolute carrier family 15 member 1Homo sapiens (human)
amyloid-beta bindingAcetylcholinesteraseHomo sapiens (human)
acetylcholinesterase activityAcetylcholinesteraseHomo sapiens (human)
cholinesterase activityAcetylcholinesteraseHomo sapiens (human)
protein bindingAcetylcholinesteraseHomo sapiens (human)
collagen bindingAcetylcholinesteraseHomo sapiens (human)
hydrolase activityAcetylcholinesteraseHomo sapiens (human)
serine hydrolase activityAcetylcholinesteraseHomo sapiens (human)
acetylcholine bindingAcetylcholinesteraseHomo sapiens (human)
protein homodimerization activityAcetylcholinesteraseHomo sapiens (human)
laminin bindingAcetylcholinesteraseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (23)

Processvia Protein(s)Taxonomy
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
plasma membraneSolute carrier family 15 member 1Homo sapiens (human)
brush borderSolute carrier family 15 member 1Homo sapiens (human)
membraneSolute carrier family 15 member 1Homo sapiens (human)
apical plasma membraneSolute carrier family 15 member 1Homo sapiens (human)
plasma membraneSolute carrier family 15 member 1Homo sapiens (human)
apical plasma membraneSolute carrier family 15 member 1Homo sapiens (human)
extracellular regionAcetylcholinesteraseHomo sapiens (human)
basement membraneAcetylcholinesteraseHomo sapiens (human)
extracellular spaceAcetylcholinesteraseHomo sapiens (human)
nucleusAcetylcholinesteraseHomo sapiens (human)
Golgi apparatusAcetylcholinesteraseHomo sapiens (human)
plasma membraneAcetylcholinesteraseHomo sapiens (human)
cell surfaceAcetylcholinesteraseHomo sapiens (human)
membraneAcetylcholinesteraseHomo sapiens (human)
neuromuscular junctionAcetylcholinesteraseHomo sapiens (human)
synaptic cleftAcetylcholinesteraseHomo sapiens (human)
synapseAcetylcholinesteraseHomo sapiens (human)
perinuclear region of cytoplasmAcetylcholinesteraseHomo sapiens (human)
side of membraneAcetylcholinesteraseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (83)

Assay IDTitleYearJournalArticle
AID409956Inhibition of mouse brain MAOB2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' 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
AID369812Plasma concentration in human at 500 mg, iv infused for 5 mins2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Population pharmacokinetics at two dose levels and pharmacodynamic profiling of flucloxacillin.
AID369817Nonrenal clearance in human at 1000 mg, iv infused for 5 mins2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Population pharmacokinetics at two dose levels and pharmacodynamic profiling of flucloxacillin.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID369807Total body clearance in human at 500 mg, iv infused for 5 mins2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Population pharmacokinetics at two dose levels and pharmacodynamic profiling of flucloxacillin.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID369808Renal clearance in human at 500 mg, iv infused for 5 mins2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Population pharmacokinetics at two dose levels and pharmacodynamic profiling of flucloxacillin.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1209457Unbound Cmax in human plasma2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.
AID369813Terminal half life in human at 500 mg, iv infused for 5 mins2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Population pharmacokinetics at two dose levels and pharmacodynamic profiling of flucloxacillin.
AID369835Bacteriostatic activity against methicillin-susceptible Staphylococcus aureus infected human at MIC of 0.75 mg/l at 1.5 g, iv administered every 6 hrs as 0.5 hrs infusion2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Population pharmacokinetics at two dose levels and pharmacodynamic profiling of flucloxacillin.
AID369816Renal clearance in human at 1000 mg, iv infused for 5 mins2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Population pharmacokinetics at two dose levels and pharmacodynamic profiling of flucloxacillin.
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.
AID369811Volume of distribution at steady state in human at 500 mg, iv infused for 5 mins2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Population pharmacokinetics at two dose levels and pharmacodynamic profiling of flucloxacillin.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID369819Volume of distribution at steady state in human at 1000 mg, iv infused for 5 mins2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Population pharmacokinetics at two dose levels and pharmacodynamic profiling of flucloxacillin.
AID369831Bactericidal activity against methicillin-susceptible Staphylococcus aureus infected human at MIC of 0.25 mg/l at 1.5 g, iv administered every 6 hrs as 0.5 hrs infusion2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Population pharmacokinetics at two dose levels and pharmacodynamic profiling of flucloxacillin.
AID369832Bactericidal activity against methicillin-susceptible Staphylococcus aureus infected human at MIC of 1 mg/l at 2 g, iv administered every 4 hrs as 0.5 hrs infusion2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Population pharmacokinetics at two dose levels and pharmacodynamic profiling of flucloxacillin.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
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]
AID404304Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control2008Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).
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]
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID369821Terminal half life in human at 1000 mg, iv infused for 5 mins2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Population pharmacokinetics at two dose levels and pharmacodynamic profiling of flucloxacillin.
AID369826Total clearance in human at 1 g, iv infused for 5 mins2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Population pharmacokinetics at two dose levels and pharmacodynamic profiling of flucloxacillin.
AID369829Bactericidal activity against methicillin-susceptible Staphylococcus aureus infected human at MIC of 0.75 mg/l at 2 g, iv administered every 8 hrs as 4 hrs infusion2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Population pharmacokinetics at two dose levels and pharmacodynamic profiling of flucloxacillin.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID369824Renal clearance in human at a loading dose of 1 g and maintenance dose of 1.2 g/h for 3 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Population pharmacokinetics at two dose levels and pharmacodynamic profiling of flucloxacillin.
AID311524Oral bioavailability in human2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Hologram QSAR model for the prediction of human oral bioavailability.
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]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID369810Metabolic stability in human assessed as urinary excretion of unchanged drug level at 500 mg, iv infused for 5 mins2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Population pharmacokinetics at two dose levels and pharmacodynamic profiling of flucloxacillin.
AID278860Antiproliferative effect against HeLa cells after 48 hrs2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Influence on mitochondria and cytotoxicity of different antibiotics administered in high concentrations on primary human osteoblasts and cell lines.
AID278861Inhibition of metabolic activity in HeLa cells assessed as MTT reduction after 48 hrs2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Influence on mitochondria and cytotoxicity of different antibiotics administered in high concentrations on primary human osteoblasts and cell lines.
AID369815Total body clearance in human at 1000 mg, iv infused for 5 mins2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Population pharmacokinetics at two dose levels and pharmacodynamic profiling of flucloxacillin.
AID369827Protein binding in human plasma2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Population pharmacokinetics at two dose levels and pharmacodynamic profiling of flucloxacillin.
AID409954Inhibition of mouse brain MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID278859Inhibition of metabolic activity in MG63 cells assessed as MTT reduction after 48 hrs2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Influence on mitochondria and cytotoxicity of different antibiotics administered in high concentrations on primary human osteoblasts and cell lines.
AID369825Nonrenal clearance in human at a loading dose of 1 g and maintenance dose of 1.2 g/h for 3 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Population pharmacokinetics at two dose levels and pharmacodynamic profiling of flucloxacillin.
AID1209455Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.
AID278856Antiproliferative effect against primary human osteoblasts assessed as BrdU incorporation into DNA after 48 hrs2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Influence on mitochondria and cytotoxicity of different antibiotics administered in high concentrations on primary human osteoblasts and cell lines.
AID369820Plasma concentration in human at 1000 mg, iv infused for 5 mins2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Population pharmacokinetics at two dose levels and pharmacodynamic profiling of flucloxacillin.
AID369823Total clearance in human at a loading dose of 1 g and maintenance dose of 1.2 g/h for 3 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Population pharmacokinetics at two dose levels and pharmacodynamic profiling of flucloxacillin.
AID369830Bactericidal activity against methicillin-susceptible Staphylococcus aureus infected human at MIC of 0.75 mg/l at 6 g, iv administered as continuous infusion for 4 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Population pharmacokinetics at two dose levels and pharmacodynamic profiling of flucloxacillin.
AID238858Binding affinity against membrane transport protein PEPT1 in human Caco-2 cells2005Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
Three-dimensional quantitative structure-activity relationship analyses of beta-lactam antibiotics and tripeptides as substrates of the mammalian H+/peptide cotransporter PEPT1.
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.
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.
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.
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]
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
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.
AID369833Bacteriostatic activity against methicillin-susceptible Staphylococcus aureus infected human at MIC of 1.5 mg/l at 2 g, iv administered every 8 hrs as 4 hrs infusions2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Population pharmacokinetics at two dose levels and pharmacodynamic profiling of flucloxacillin.
AID369822Mean residence time in human at 1000 mg, iv infused for 5 mins2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Population pharmacokinetics at two dose levels and pharmacodynamic profiling of flucloxacillin.
AID369836Bacteriostatic activity against methicillin-susceptible Staphylococcus aureus infected human at MIC of 2 mg/l at 2 g, iv administered every 4 hrs as 0.5 hrs infusion2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Population pharmacokinetics at two dose levels and pharmacodynamic profiling of flucloxacillin.
AID369814Mean residence time in human at 500 mg, iv infused for 5 mins2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Population pharmacokinetics at two dose levels and pharmacodynamic profiling of flucloxacillin.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID369818Metabolic stability in human assessed as urinary excretion of unchanged drug level at 1000 mg, iv infused for 5 mins2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Population pharmacokinetics at two dose levels and pharmacodynamic profiling of flucloxacillin.
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.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
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]
AID369809Nonrenal clearance in human at 500 mg, iv infused for 5 mins2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Population pharmacokinetics at two dose levels and pharmacodynamic profiling of flucloxacillin.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
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.
AID278857Inhibition of metabolic activity in primary human osteoblasts assessed as MTT reduction after 48 hrs2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Influence on mitochondria and cytotoxicity of different antibiotics administered in high concentrations on primary human osteoblasts and cell lines.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID369834Bacteriostatic activity against methicillin-susceptible Staphylococcus aureus infected human at MIC of 0.75 mg/l at 6 g, iv administered as continuous infusion for 4 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Population pharmacokinetics at two dose levels and pharmacodynamic profiling of flucloxacillin.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID278858Antiproliferative effect against MG63 cells assessed as BrdU incorporation into DNA after 48 hrs after 48 hrs2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Influence on mitochondria and cytotoxicity of different antibiotics administered in high concentrations on primary human osteoblasts and cell lines.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1209456Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.
AID369828Antibacterial activity against methicillin-susceptible Staphylococcus aureus2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Population pharmacokinetics at two dose levels and pharmacodynamic profiling of flucloxacillin.
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.
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.
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.
AID1501977Inhibition of AChE (unknown origin)2017Journal of natural products, 09-22, Volume: 80, Issue:9
Acetylcholinesterase Inhibitory Alkaloids from the Whole Plants of Zephyranthes carinata.
AID1634701Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production at 200 uM after 24 hrs by Griess assay2016Journal of natural products, Apr-22, Volume: 79, Issue:4
Galanthamine, Plicamine, and Secoplicamine Alkaloids from Zephyranthes candida and Their Anti-acetylcholinesterase and Anti-inflammatory Activities.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (792)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990188 (23.74)18.7374
1990's139 (17.55)18.2507
2000's157 (19.82)29.6817
2010's233 (29.42)24.3611
2020's75 (9.47)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 97.28

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 very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index97.28 (24.57)
Research Supply Index6.84 (2.92)
Research Growth Index4.66 (4.65)
Search Engine Demand Index176.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (97.28)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials94 (11.15%)5.53%
Trials0 (0.00%)5.53%
Reviews49 (5.81%)6.00%
Reviews1 (20.00%)6.00%
Case Studies325 (38.55%)4.05%
Case Studies0 (0.00%)4.05%
Observational11 (1.30%)0.25%
Observational0 (0.00%)0.25%
Other364 (43.18%)84.16%
Other4 (80.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (18)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
DetectAB - Detecting Antibiotics - A Pilot Project [NCT03678142]17 participants (Actual)Observational2018-10-01Completed
Duration of Antibiotic Therapy for Cellulitis (DANCE): a Randomized Controlled Trial Comparing 6 to 12 Days of Antibiotic Therapy for Patients Hospitalized With Cellulitis [NCT02032654]Phase 4151 participants (Actual)Interventional2014-08-26Terminated(stopped due to Budget exceeded)
CHOICE Trial: Cellulitis at Home Or Inpatient in Children From ED [NCT02334124]190 participants (Actual)Interventional2015-01-31Completed
The Safety and Efficacy of the Enhanced Recovery After Surgery(ERAS) Applied on Cardiac Surgery With Cardiopulmonary Bypass: a Single Center, Randomized, Controlled Clinical Study [NCT02479581]Phase 2226 participants (Actual)Interventional2015-07-31Completed
A Phase 2 Randomized Study Investigating the Safety, Efficacy and Pharmacokinetics of Daptomycin 6 mg/kg and 8 mg/kg Versus Comparator in the Treatment of Subjects Undergoing Surgical Standard of Care for Osteomyelitis Associated With an Infected Prosthet [NCT00428844]Phase 275 participants (Actual)Interventional2007-06-26Completed
An Open Label, Multi-center, Randomized, Comparative Phase IIIb Study to Compare Efficacy and Safety of Intravenous (i.v.) Daptomycin With That of Semi-Synthetic Penicillins (SSPs) or Vancomycin in the Treatment of Elderly Patients (Aged ≥ 65 Years) With [NCT01184872]Phase 3120 participants (Actual)Interventional2010-03-31Completed
A RCT in Sweden of Acupuncture and Care Interventions for the Relief of Inflammatory Symptoms of the Breast During Lactation [NCT00405158]210 participants Interventional2002-01-31Completed
Oral Flucloxacillin Alone Versus Flucloxacillin and Phenoxymethylpenicillin for the Emergency Department Outpatient Treatment of Cellulitis: a Non-inferiority Randomised Controlled Trial. [NCT02922686]Phase 4414 participants (Anticipated)Interventional2016-12-31Not yet recruiting
A Double Blind Randomised Control Trial to Measure the Effect of the Addition of Clindamycin to Flucloxacillin for the Treatment of Limb Cellulitis [NCT01876628]Phase 4410 participants (Actual)Interventional2013-10-31Completed
Study on the Effect of Flucloxacillin on the Serum Level of P-cresol in Peritoneal Dialysis Patients [NCT00433342]Phase 19 participants (Actual)Interventional2006-03-31Terminated
Pharmacokinetics of Flucloxacillin Given by Continuous or Intermittent Infusion as Therapy to Patients With an Infection in the Intensive Care Unit (ICU) [NCT02993575]30 participants (Actual)Observational2017-06-01Completed
Pilot Randomised Controlled Trial of Penicillin Versus Flucloxacillin for Definitive Treatment of Invasive Penicillin Susceptible Staphylococcus Aureus [NCT03632642]Phase 40 participants (Actual)Interventional2019-07-01Withdrawn(stopped due to Study never commenced)
Early Oral Switch Therapy in Low-risk Staphylococcus Aureus Bloodstream Infection [NCT01792804]Phase 3215 participants (Actual)Interventional2013-12-31Completed
A Blinded, Non-inferiority Phase III Trial of 5 Versus 7 Days of Oral Flucloxacillin in Primary Care Patients With Lower Limb Cellulitis [NCT05584007]Phase 3356 participants (Anticipated)Interventional2023-06-01Not yet recruiting
CAMERA 2 - Combination Antibiotic Therapy for Methicillin Resistant Staphylococcus Aureus Infection - An Investigator-initiated, Multi-centre, Parallel Group, Open Labelled Randomised Controlled Trial [NCT02365493]Phase 3358 participants (Actual)Interventional2015-08-26Terminated(stopped due to Recommendation of the Data Safety Monitoring Committee)
A Mono-center, Open, Randomized, Three-way, Twelve-sequence, Cross-over Study to Determine the Extent of Absorption (Absolute Bioavailability), Rate of Absorption and to Further Characterize Distribution and Elimination Characteristics of a Commercial 250 [NCT00358371]Phase 124 participants (Actual)Interventional2005-01-06Completed
Flucloxacillin as an Inducer of CYP-enzymes [NCT04840641]Phase 114 participants (Actual)Interventional2021-03-25Completed
BonE and Joint Infections - Simplifying Treatment in Children Trial [NCT04538053]Phase 4285 participants (Anticipated)Interventional2021-06-01Recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00428844 (6) [back to overview]Any Creatine Phosphokinase (CPK) Elevation > 500 Units Per Liter (U/L)
NCT00428844 (6) [back to overview]Pharmacokinetic Parameter: Area Under the Concentration-time Curve During a Dosing Interval at Steady State (AUCss)
NCT00428844 (6) [back to overview]Pharmacokinetic Parameter: Maximum Plasma Concentration (Cmax)
NCT00428844 (6) [back to overview]Microbiological Response
NCT00428844 (6) [back to overview]Overall Clinical Outcome
NCT00428844 (6) [back to overview]Safety - Notable Laboratory Abnormalities
NCT01184872 (5) [back to overview]Duration of Treatment (Intravenous)
NCT01184872 (5) [back to overview]Duration of Treatment (Intravenous and Oral)
NCT01184872 (5) [back to overview]Number of Participants With Microbiological Response at Test-of-Cure (TOC) Visit
NCT01184872 (5) [back to overview]Number of Patients With Adverse Events, Serious Adverse Events and Death
NCT01184872 (5) [back to overview]Number of Patients With Clinical Success at the Test-Of-Cure (TOC) Visit

Any Creatine Phosphokinase (CPK) Elevation > 500 Units Per Liter (U/L)

Number of subjects with CPK >500 U/L between Day 3 and 7 days following the last dose of study medication (Day 7P) as measured by the central laboratory. (NCT00428844)
Timeframe: From the 3rd day of therapy to 1 week post last dose (approximately week 7)

InterventionParticipants (Number)
Daptomycin 6 mg/kg4
Daptomycin 8 mg/kg5
Comparator2

[back to top]

Pharmacokinetic Parameter: Area Under the Concentration-time Curve During a Dosing Interval at Steady State (AUCss)

The pharmacokinetic (PK) parameters of daptomycin at steady state for the 6 mg/kg and 8 mg/kg dose groups. On treatment day 4, PK samples for daptomycin levels were to be obtained prior to start of daptomycin infusion (0 hr) and at 0.5 hr (end of infusion), 1-1.5 hr, 3-5 hr, 8-12 hr, and 24 hr after the start of daptomycin infusion. (NCT00428844)
Timeframe: Day 4 (steady state)

Interventionµg•hr/mL (Median)
Daptomycin 6 mg/kg499
Daptomycin 8 mg/kg821

[back to top]

Pharmacokinetic Parameter: Maximum Plasma Concentration (Cmax)

The pharmacokinetic (PK) parameters of daptomycin at steady state for the 6 mg/kg and 8 mg/kg dose groups. On treatment day 4, PK samples for daptomycin levels were to be obtained prior to start of daptomycin infusion (0 hr) and at 0.5 hr (end of infusion), 1-1.5 hr, 3-5 hr, 8-12 hr, and 24 hr after the start of daptomycin infusion. (NCT00428844)
Timeframe: Day 4 (steady state)

Interventionµg/mL (Median)
Daptomycin 6 mg/kg59.1
Daptomycin 8 mg/kg92.3

[back to top]

Microbiological Response

Sponsor's assessment of subject-level microbiological response at the test-of-cure visit for the modified Intent-to-Treat (mITT) population. (NCT00428844)
Timeframe: Approximately 6 weeks post last dose (approximately week 12)

,,
InterventionParticipants (Number)
SuccessFailureNon-evaluable
Comparator867
Daptomycin 6 mg/kg1284
Daptomycin 8 mg/kg1238

[back to top]

Overall Clinical Outcome

The sponsor determined overall clinical outcome based on blinded review of clinical, microbiological, and radiological response of the subject including, but not limited to, clinical signs and symptoms of PJI, microbiological assessments, radiographic findings, and surgical procedures performed. Subjects were a success if both clinical and microbiological responses were success. A subject who failed to respond clinically or microbiologically was a failure. If microbiological response was non-evaluable and/or clinical evaluation at TOC was not performed, the subject was non-evaluable. (NCT00428844)
Timeframe: Approximately 6 weeks post last dose (approximately week 12)

,,
InterventionParticipants (Number)
SuccessFailureNonevaluable
Comparator8112
Daptomycin 6 mg/kg13101
Daptomycin 8 mg/kg1382

[back to top]

Safety - Notable Laboratory Abnormalities

Summary of Notable Laboratory Abnormalities - description of the proportion of subjects within each treatment group that had clinical laboratory values outside the reference range. (NCT00428844)
Timeframe: From the 1st day of therapy to maximum of 23 weeks post last dose (up to maximum of week 30)

,,
InterventionParticipants (Number)
Hematocrit (<30%, >60%)Hemoglobin (<9,>19 g/dL)Red Blood Cell (Female <2.5,>6.0; Male <3.0, >6.5)White Blood Cell (<2, >20 x 10^9/L)Platelets (<40, >450 x 10^9/L)Albumin (<3, >6 g/dL)Alkaline Phosphatase (>1350 U/L)Alanine aminotransferase (>235 U/L)Aspartate aminotransferase (>185 U/L)Total bilirubin (>2.2 mg/dL)Blood Urea Nitrogen (>50 mg/dL)Creatinine (Female >2.0; Male>2.8 mg/dL)
Comparator151230104000012
Daptomycin 6 mg/kg121021137001021
Daptomycin 8 mg/kg101040134000000

[back to top]

Duration of Treatment (Intravenous)

Duration of treatment is the interval from first to last intravenous (i.v.) administration. It was preferable that a patient complete the whole antibiotic treatment with the randomized i.v. study drug only. Duration of treatment in patients with bacteremia could be extended up to 28 days. (NCT01184872)
Timeframe: Up to 28 days

InterventionDays (Mean)
Daptomycin7.8
Vancomycin or Semi-Synthetic Penicillins (SSPs)7.3

[back to top]

Duration of Treatment (Intravenous and Oral)

Duration of treatment is the interval from first to last intravenous (i.v.) or to last oral administration if patients switched to an oral antibiotic therapy. It was preferable that a patient complete the whole antibiotic treatment with the randomized i.v. study drug only. Duration of treatment in patients with bacteremia could be extended up to 28 days. (NCT01184872)
Timeframe: Up to 28 days

,
InterventionDays (Mean)
intravenous onlyintravenous + oral
Daptomycin7.88.7
Vancomycin or Semi-Synthetic Penicillins (SSPs)7.39.6

[back to top]

Number of Participants With Microbiological Response at Test-of-Cure (TOC) Visit

Microbiological Success: All infecting Gram-positive pathogens isolated at baseline were eradicated or presumed to be eradicated at the Test-of-Cure (TOC) evaluation and a super infecting pathogen was not isolated either prior to or at the TOC evaluation. Microbiological Failure: Persistence or relapse / re-infection of one or more infecting Gram-positive pathogens or isolation of a super infecting pathogen prior to or at the TOC evaluation. (NCT01184872)
Timeframe: Baseline and 7 to 14 days after end of therapy

,
Interventionparticipants (Number)
SuccessFailure
Daptomycin5411
Vancomycin or Semi-Synthetic Penicillins (SSPs)234

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Number of Patients With Adverse Events, Serious Adverse Events and Death

(NCT01184872)
Timeframe: Continuously from baseline up to 28 days after end of antibiotic treatment.

,
Interventionparticipants (Number)
Adverse EventsSerious Adverse EventsDeath
Daptomycin5070
Vancomycin or Semi-Synthetic Penicillins (SSPs)2640

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Number of Patients With Clinical Success at the Test-Of-Cure (TOC) Visit

Success: Clinically significant signs and symptoms associated with the skin infection present at the pre-treatment infection site resolved (cure), or improved without need of further antibacterial therapy. Failure: Persistence or progression of signs and symptoms or development of new clinical signs and symptoms at the infection site, or concomitant antibacterial therapy with activity against isolated organisms, or treatment duration longer than pre-specified, or switch back to intravenous therapy due to relapse, or requirement of a major surgical procedure as adjunct or follow-up therapy. (NCT01184872)
Timeframe: Baseline and 7 to 14 days after end of therapy

,
Interventionparticipants (Number)
SuccessFailure
Daptomycin658
Vancomycin or Semi-Synthetic Penicillins (SSPs)255

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