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sultamicillin

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Description

sultamicillin: contains ampicillin & sulbactam [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID444022
CHEMBL ID506110
CHEBI ID51770
SCHEMBL ID34392
MeSH IDM0108613

Synonyms (49)

Synonym
vd-1827
cp-49952
sultamicillin (usan/inn)
76497-13-7
D05972
sultamicillin
sultamicilina [spanish]
4-thia-1-azabicyclo(3.2.0)heptane-2-carboxylic acid, 6-((aminophenylacetyl)amino)-3,3-dimethyl-7-oxo-, (((3,3-dimethyl-7-oxo-4-thia-1-azabicyclo(3.2.0)hept-2-yl)carbonyl)oxy)methyl ester, s,s-dioxide, (2s-(2alpha(2r*,5s*),5alpha,6beta(s*)))-
vd 1827
hydroxymethyl (2s,5r,6r)-6-((r)-(2-amino-2-phenylacetamido))-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo(3.2.0)heptane-2-carboxylate, (2s,5r)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo(3.2.0)heptane-2-carboxylate (ester) s,s-dioxide
sultamicillinum [latin]
cp 49952
(2s,5r)-3,3-dimethyl-4,4,7-trioxo-4-thia-1-azabicyclo(3.2.0)heptan-2-carbonyloxymethyl (2s,5r,6r)-6-((r)-2-phenylacetamido)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo(3.2.0)heptan-2-carboxylat
CHEBI:51770 ,
({6beta-[(2r)-2-amino-2-phenylacetamido]-2,2-dimethylpenam-3alpha-carbonyl}oxy)methyl 2,2-dimethylpenam-3alpha-carboxylate 1,1-dioxide
[(2,2-dimethyl-1,1-dioxidopenam-3alpha-carbonyl)oxy]methyl 6beta-[(2r)-2-amino-2-phenylacetamido]-2,2-dimethylpenam-3alpha-carboxylate
sultamicilina
sultamicillinum
CHEMBL506110
cp-49,952
unii-65dt0ml581
sultamicillin [usan:inn:ban]
65dt0ml581 ,
AKOS015963376
hydroxymethyl (2s,5r,6r)-6-[(r)-(2-amino-2-phenylacetamido)]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate, (2s,5r)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate (ester) s,s-dioxide
sultamicillin [usan]
sultamicillin [who-dd]
sultamicillin [inn]
sultamicillin [mi]
1,1-dioxopenicillanoyloxymethyl 6-(d-.alpha.-amino-.alpha.-phenylacetamido)penicillanate
6'-(2-amino-2-phenylacetamido)penicillanoyloxymethyl penicillanate 1,1-dioxide
sultamicillin [mart.]
sultamicillin [ep monograph]
S5411
4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylicacid, 6-[[(2r)-2-amino-2-phenylacetyl]amino]-3,3-dimethyl-7-oxo-,[[[(2s,5r)-3,3-dimethyl-4,4-dioxido-7-oxo-4-thia-1-azabicyclo[3.2.0]hept-2-yl]carbonyl]oxy]methylester, (2s,5r,6r)-
SCHEMBL34392
[(2s,5r)-3,3-dimethyl-4,4,7-trioxo-4lambda6-thia-1-azabicyclo[3.2.0]heptane-2-carbonyl]oxymethyl (2s,5r,6r)-6-[[(2r)-2-amino-2-phenylacetyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate
DB12127
CS-0082687
HY-N7115
DTXSID501010077
(((2s,5r,6r)-6-((r)-2-amino-2-phenylacetamido)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carbonyl)oxy)methyl (2s,5r)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate 4,4-dioxide
76497-13-7 (free)
AS-14087
CCG-270182
sultamicillin for peak identification
[(2s,5r,6r)-6-[(2r)-2-amino-2-phenylacetamido]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carbonyloxy]methyl (2s,5r)-3,3-dimethyl-4,4,7-trioxo-4lambda6-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate
EN300-19766280
gtpl12290

Research Excerpts

Overview

Sultamicillin is an orally absorbed double ester of sulbactam (penicillanic acid sulphone, a semisynthetic inhibitor of the beta-lactamases of many Gram-positive and Gram-negative species) It is a covalent union of ampicillin and the beta lactamase inhibitor, sulbactsam.

ExcerptReferenceRelevance
"Sultamicillin is an orally absorbed double ester of sulbactam (penicillanic acid sulphone, a semisynthetic inhibitor of the beta-lactamases of many Gram-positive and Gram-negative species) and ampicillin. "( Pharmacokinetics and bioavailability of sultamicillin estimated by high performance liquid chromatography.
Bradbrook, ID; Cox, DA; Lees, LJ; Morrison, PJ; ROgers, HJ; Spector, RG, 1983
)
1.98
"Sultamicillin is a mutual prodrug of ampicillin and sulbactam that is chemically linked by a diester bond. "( Comparative study of sultamicillin and amoxicillin-clavulanate: treatment of acute otitis media.
Blatter, MM; Bluestone, CD; Chan, KH; Fall, PA; Reisinger, KS; Tan, LS, 1993
)
2.05
"Sultamicillin is an oral mutual pro-drug composed of double esters of formaldehyde hydrate in which one of the hydroxyl groups is esterified with ampicillin and the other with sulbactam. "( [Studies on sultamicillin hydrolysis].
Hu, CQ; Jin, SH; Liang, H; Liu, W; Wu, Q; Yang, MZ; Zhang, DC, 1997
)
2.12
"Sultamicillin is a mutual prodrug of ampicillin and sulbactam, a beta-lactamase inhibitor. "( The pharmacokinetics of sultamicillin.
Bruckner, G; Hampel, B; Koeppe, P; Lode, H, 1989
)
2.03
"Sultamicillin is a substance in which sulbactam, a beta-lactamase inhibitor, is covalently linked through an ester group to ampicillin. "( Sultamicillin experiences in the field of internal medicine.
Hara, K; Kobayashi, H, 1989
)
3.16
"Sultamicillin is a covalent union of ampicillin and the beta lactamase inhibitor, sulbactam (CP-45,899). "( Two regimens of sultamicillin in treating uncomplicated gonorrhoea.
Farthing, C; Phillips, I; Smith, S; Thin, RN, 1985
)
2.06
"Sultamicillin is a novel therapeutic approach to beta-lactamase-producing bacteria."( Sultamicillin (ampicillin-sulbactam) in the treatment of acute otitis media in children.
Blatter, MM; Bluestone, CD; Fall, PA; Kaleida, PH; Reisinger, KS; Rohn, DD; Wucher, FP,
)
2.3
"Sultamicillin is a compound agent for oral use in which ampicillin and the beta-lactamase inhibitor sulbactam are linked as a double ester."( Sultamicillin--a new antibiotic in the treatment of persistent lower respiratory tract infections caused by Haemophilus influenzae.
Christiansen, L; Høiby, N; Koch, C; Pedersen, SS; Pressler, T; Szaff, M, 1986
)
2.44
"Sultamicillin (SBTPC) is a mutual prodrug of sulbactam (SBT) and ampicillin (ABPC). "( [Clinical and pharmacokinetic studies on sultamicillin fine granules in pediatrics].
Matsumoto, K; Nakanishi, Y; Nakazawa, S; Narita, A; Niino, K; Sato, H; Suzuki, H, 1988
)
1.98
"Sultamicillin (SBTPC) is a combination drug of sulbactam (SBT) and ampicillin (ABPC) in an ester bonding at 1:1 ratio. "( [Experiences with sultamicillin granules in pediatric patients].
Iguchi, K; Inoue, M; Kamiya, H; Kawaguchi, H; Kojima, M; Nishi, H; Sakurai, M; Shimizu, S; Yoshizumi, T, 1988
)
2.05
"Sultamicillin (SBTPC) is a combined drug of ampicillin (ABPC) and sulbactam (SBT) which is an inhibitor of beta-lactamase, in a clinical form of tosylate with equivalent molecules in ester linkages. "( [Pharmacokinetic and clinical studies of sultamicillin granule in the pediatric field].
Aramaki, M; Fujimoto, T; Kawakami, A; Koga, T; Motohiro, T; Oda, K; Sakata, Y; Takajo, N; Tanaka, K; Yamashita, F, 1988
)
1.98
"Sultamicillin (SBTPC) is a semi-synthesized beta-lactam antibiotic consisted of ampicillin (ABPC) and a beta-lactamase inhibitor, sulbactam (SBT), linked with an ester linkage. "( [Pharmacokinetic and clinical studies of sultamicillin fine granules in children].
Hayashi, K; Imamura, H; Nakayama, N; Tsuji, Y; Yanagi, T; Yanagishima, M; Yanai, M, 1988
)
1.98
"Sultamicillin (SBTPC) is a mutual prodrug in which ampicillin (ABPC) and a potent beta-lactamase inhibitor sulbactam (SBT) are ester-bound in an equimolar ratio. "( [Antimicrobial activities of sultamicillin against clinical isolates from upper respiratory tract infections].
Deguchi, K; Fukayama, S; Kato, M; Koguchi, M; Nakane, Y; Nishimura, Y; Oda, S; Sato, K; Tanaka, S; Yokota, N, 1988
)
2.01

Effects

Sultamicillin has an excellent tolerability profile, which is associated with a low rate of treatment discontinuation. It is clinically effective in non-comparative trials in patients with infections of the respiratory tract, ears, nose and throat, urinary tract, skin and soft tissues.

ExcerptReferenceRelevance
"Sultamicillin has an excellent tolerability profile, which is associated with a low rate of treatment discontinuation."( Use of ampicillin/sulbactam and sultamicillin in pediatric infections: a re-evaluation.
Dajani, A,
)
1.14
"Sultamicillin has an excellent tolerability profile, which is associated with a low rate of treatment discontinuation."( Use of ampicillin/sulbactam and sultamicillin in pediatric infections: a re-evaluation.
Dajani, A,
)
1.14
"Sultamicillin has been shown to be clinically effective in non-comparative trials in patients with infections of the respiratory tract, ears, nose and throat, urinary tract, skin and soft tissues, as well as in obstetric and gynaecological infections, and in the treatment of gonorrhoea."( Sultamicillin. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use.
Campoli-Richards, DM; Friedel, HA; Goa, KL, 1989
)
2.44

Treatment

ExcerptReferenceRelevance
"All sultamicillin-treated and all but three cefuroxime axetil-treated patients experienced cure or improvement; only one cefuroxime axetil-treated patient discontinued treatment due to treatment failure."( An open multicentre study to compare the efficacy and safety of sultamicillin with that of cefuroxime axetil in acute ear nose and throat infections in adults.
Alvart, R, 1992
)
1

Toxicity

Gastrointestinal adverse events occurred in both treatment groups. One patient receiving cefuroxime axetil discontinued treatment due to nausea. Tolerability of sultamicillin was good.

ExcerptReferenceRelevance
" Tolerability of sultamicillin was good and only three possible or probable treatment-related adverse events were recorded."( An open non-comparative pilot study of the safety and efficacy of oral sultamicillin in the treatment of mild to moderate upper respiratory tract infections in children.
Argüello, A, 1992
)
0.86
" Study drug-related adverse events were experienced by 33."( An open comparative study of the efficacy and safety of sultamicillin versus cefaclor in the treatment of acute otitis media in children.
Biolcati, AH, 1992
)
0.53
" Gastrointestinal adverse events occurred in both treatment groups (eight sultamicillin-treated patients and three cefuroxime axetil-treated patients); one patient receiving cefuroxime axetil discontinued treatment due to nausea."( An open multicentre study to compare the efficacy and safety of sultamicillin with that of cefuroxime axetil in acute ear nose and throat infections in adults.
Alvart, R, 1992
)
0.75
" Adverse reactions to oral therapy were minimal."( Efficacy and safety of sequential treatment with parenteral sulbactam/ampicillin and oral sultamicillin for skeletal infections in children.
Aronoff, SC; Blumer, JL; Jacobs, MR; Kalamchi, A; Makley, JT; Scoles, PV,
)
0.35
" Adverse reactions were infrequent with the exception of injection-site pain, which occurred mainly after intramuscular injection and was reduced in incidence by concurrent administration of lidocaine."( Sulbactam plus ampicillin: interim review of efficacy and safety for therapeutic and prophylactic use.
Greenhalgh, K; Knirsch, AK; Lees, L; Milson, JA,
)
0.13
"Both ampicillin/sulbactam and cefuroxime provide safe and effective parenteral antibiotic therapy in pediatric patients with serious skin and skin structure infections."( Efficacy and safety of ampicillin/sulbactam and cefuroxime in the treatment of serious skin and skin structure infections in pediatric patients. UNASYN Pediatric Study Group.
Azimi, PH; Barson, WJ; Janner, D; Swanson, R, 1999
)
0.3
" Drug-related adverse events for both study drugs were comparable in frequency and type."( An open-label, randomized study comparing efficacy and safety of intravenous piperacillin/tazobactam and ampicillin/sulbactam for infected diabetic foot ulcers.
Boghossian, J; Caputo, W; Dana, A; Gray, S; Harkless, L; Pollak, R; Wu, D, 2005
)
0.33
"Although both study drugs provide safe and effective empiric treatment for moderate-to-severe infected diabetic foot ulcers, piperacillin/tazobactam has the advantage of covering Pseudomonas aeruginosa (bacteriologic success rate of 85."( An open-label, randomized study comparing efficacy and safety of intravenous piperacillin/tazobactam and ampicillin/sulbactam for infected diabetic foot ulcers.
Boghossian, J; Caputo, W; Dana, A; Gray, S; Harkless, L; Pollak, R; Wu, D, 2005
)
0.33
" The adverse events ratio for the two groups was the same (p=0."( Efficacy and safety of Sultamicillin (Ampicillin/Sulbactan) and Amoxicillin/Clavulanic acid in the treatment of upper respiratory tract infections in adults--an open-label, multicentric, randomized trial.
Ferreira, JB; Kós, AO; Mocellin, M; Pignatari, SS; Piltcher, OB; Pinheiro, SD; Rapoport, PB; Sakano, E,
)
0.44
"Ampicillin/Sulbactan is as safe and efficient as Amoxicillin/Clavulanate in the empiric treatment of upper respiratory infections in adults."( Efficacy and safety of Sultamicillin (Ampicillin/Sulbactan) and Amoxicillin/Clavulanic acid in the treatment of upper respiratory tract infections in adults--an open-label, multicentric, randomized trial.
Ferreira, JB; Kós, AO; Mocellin, M; Pignatari, SS; Piltcher, OB; Pinheiro, SD; Rapoport, PB; Sakano, E,
)
0.44
" Adverse events were 39."( Efficacy and safety of high-dose ampicillin/sulbactam vs. colistin as monotherapy for the treatment of multidrug resistant Acinetobacter baumannii ventilator-associated pneumonia.
Betrosian, AP; Douzinas, EE; Frantzeskaki, F; Xanthaki, A, 2008
)
0.35
" All treatment-related adverse events were mild or moderate in severity."( Efficacy and safety of intravenous sulbactam/ampicillin 3 g 4 times daily in Japanese adults with moderate to severe community-acquired pneumonia: a multicenter, open-label, uncontrolled study.
Itamura, R; Kadota, J; Kohno, S; Mikamo, H; Niki, Y; Tateda, K, 2015
)
0.42

Pharmacokinetics

ExcerptReferenceRelevance
"We investigated the pharmacokinetic properties of sulbactam/ampicillin (S/A), after intravenous (0."( Pharmacokinetics of sulbactam/ampicillin in humans after intravenous and intramuscular injection.
Ferrante, L; Prenna, M; Ripa, S, 1990
)
0.28
" The pharmacokinetic parameters of the two components are similar, both being eliminated primarily by renal excretion."( The pharmacokinetics of sultamicillin.
Bruckner, G; Hampel, B; Koeppe, P; Lode, H, 1989
)
0.58
" Although the kinetics of sulbactam in postpartem women and in surgical patients were similar to the kinetics in young men, the half-life of sulbactam (like that of ampicillin) was altered in the elderly, during labor, in neonates, and in patients with renal impairment."( Pharmacokinetics of sulbactam/ampicillin in humans: a review.
Foulds, G,
)
0.13
" The two drugs showed a similar pharmacokinetic profile in humans."( Pharmacokinetics of sulbactam and ampicillin intravenously applied in combination to healthy volunteers and patients. Determination of the ratio of the two drugs in serum and in various tissues.
Engel, K; Lenders, H; Potempa, J; Schilling, A; Schwiersch, U; von Castell, E; Wildfeuer, A, 1988
)
0.27
" A study has been performed to evaluate pharmacokinetic properties and clinical usefulness of SBTPC fine granules in the treatment of pediatric infections."( [Clinical and pharmacokinetic studies on sultamicillin fine granules in pediatrics].
Matsumoto, K; Nakanishi, Y; Nakazawa, S; Narita, A; Niino, K; Sato, H; Suzuki, H, 1988
)
0.54
" Pharmacokinetic studies were done in 2 subjects (a male and a female) following single oral administrations of 5 mg/kg and 10 mg/kg SBTPC fine granules after meal."( [A study on pharmacokinetics, antimicrobial activity and clinical efficacy of sultamicillin in children].
Higashino, H; Hirabayashi, Y; Kitamura, N; Kobayashi, Y; Okazaki, H, 1988
)
0.5
" Pharmacokinetic and clinical studies using SBTPC 10% fine granules were performed in pediatric patients with a variety of infections."( [Pharmacokinetic and clinical studies of sultamicillin fine granules in children].
Hayashi, K; Imamura, H; Nakayama, N; Tsuji, Y; Yanagi, T; Yanagishima, M; Yanai, M, 1988
)
0.54
"To compare the pharmacokinetic and pharmacodynamic activity of three drug regimens: cefotaxime plus metronidazole, cefoxitin, and ampicillin-sulbactam against two organisms frequently isolated in intraabdominal infection, Escherichia coli and Bacteroides fragilis."( Comparison of the pharmacodynamic activity of cefotaxime plus metronidazole with cefoxitin and ampicillin plus sulbactam.
Nightingale, CH; Quintiliani, R; Sullivan, MC; Sweeney, KR,
)
0.13
"To evaluate the pharmacodynamic antibacterial activity of ticarcillin-clavulanic acid (T-C) and ampicillin-sulbactam (A-S) combinations against reference bacterial strains in patients with end-stage renal disease maintained on long-term hemodialysis."( Comparison of ampicillin-sulbactam and ticarcillin-clavulanic acid in patients with chronic renal failure: effects of differential pharmacokinetics on serum bactericidal activity.
Butler, SC; Hardin, TC; Jorgensen, JH; Ross, S; Wakeford, JH,
)
0.13
"An in vitro pharmacokinetic model (IVPM) and a mouse model of lethal bacteremia were used to compare the pharmacodynamics of ampicillin-sulbactam when the two components were dosed simultaneously and in sequence against TEM-1-producing Escherichia coli."( Efficacy of ampicillin-sulbactam is not dependent upon maintenance of a critical ratio between components: sulbactam pharmacokinetics in pharmacodynamic interactions.
Alexov, M; Lister, PD; Sanders, CC, 1996
)
0.29
" Studies in animals, in vitro models, and pharmacokinetic considerations indicate that a change in the MIC breakpoint for ampicillin/sulbactam should be considered."( Microbiologic and pharmacodynamic principals applied to the antimicrobial susceptibility testing of ampicillin/sulbactam: analysis of the correlations between in vitro test results and clinical response.
Dudley, MN; Jones, RN, 1997
)
0.3
" Both drugs had a similar pharmacokinetic behavior after intramuscular administration in sheep."( Pharmacokinetics of an ampicillin-sulbactam combination after intravenous and intramuscular administration to sheep.
Cárceles, CM; Escudero, E; Espuny, A; Vicente, S, 1999
)
0.3
" No changes in elimination half-life relative to a normal population occurred with cefuroxime, cefotiam, and ampicillin."( Pharmacokinetics of antibiotic prophylaxis in major orthopedic surgery and blood-saving techniques.
Dehne, MG; Hempelmann, G; Mühling, J; Nopens, H; Sablotzki, A, 2001
)
0.31
" The plasma concentration-time curves were analysed by compartmental pharmacokinetic and noncompartmental methods."( Pharmacokinetics of an ampicillin/sulbactam (2:1) combination in rabbits.
Cárceles, CM; Escudero, E; Serrano, JM; Vicente, MS, 2002
)
0.31
"Twelve critically ill patients with anuric AKI being treated with ED were enrolled in a prospective, open-label, observational pharmacokinetic study."( Pharmacokinetics of ampicillin/sulbactam in critically ill patients with acute kidney injury undergoing extended dialysis.
Broll, M; Burhenne, H; Burkhardt, O; Clajus, C; Hafer, C; Kaever, V; Kielstein, JT; Knitsch, W; Lorenzen, JM, 2012
)
0.38
" Plasma concentrations of ampicillin were simulated with the pharmacokinetic parameters obtained."( Pharmacokinetics of ampicillin-sulbactam and the renal function-based optimization of dosing regimens for prophylaxis in patients undergoing cardiovascular surgery.
Iguro, Y; Ikawa, K; Imoto, Y; Ishida, S; Matsumoto, K; Morikawa, N; Okano, Y; Shimodozono, Y; Takeda, Y; Watanabe, E; Yamada, K; Yamamoto, H; Yokoyama, Y, 2012
)
0.38
" baumannii using an in vitro pharmacodynamic model."( In vitro pharmacodynamics of human-simulated exposures of ampicillin/sulbactam, doripenem and tigecycline alone and in combination against multidrug-resistant Acinetobacter baumannii.
Hagihara, M; Housman, ST; Kuti, JL; Nicolau, DP, 2013
)
0.39
" Drug exposure was expressed as the ratio of the area under the concentration-time curve for the free, unbound fraction of the drug to the MIC (fAUC/MIC) (VAN) or the time in a 24-h period that the drug concentration for the free, unbound fraction exceeded the MIC under steady-state pharmacokinetic conditions (fT(>MIC)) (SAM and TZP) and linked to the change in log10 CFU/thigh."( An optimized mouse thigh infection model for enterococci and its impact on antimicrobial pharmacodynamics.
Agudelo, M; Gonzalez, JM; Rodriguez, CA; Vesga, O; Zuluaga, AF, 2015
)
0.42
" Pharmacokinetic parameters were estimated and used to predict the free plasma concentrations of ampicillin."( Pharmacokinetics of Prophylactic Ampicillin-Sulbactam and Dosing Optimization in Patients Undergoing Cardiovascular Surgery with Cardiopulmonary Bypass.
Ikawa, K; Imoto, Y; Matsumoto, K; Morikawa, N; Takeda, Y; Watanabe, E; Yamamoto, H; Yokoyama, Y, 2015
)
0.42
" Pharmacokinetic parameters were estimated and used to predict the free plasma concentrations of ampicillin and sulbactam."( The pharmacokinetics of ampicillin-sulbactam in anuric patients: dosing optimization for prophylaxis during cardiovascular surgery.
Ikawa, K; Imoto, Y; Matsumoto, K; Morikawa, N; Takeda, Y; Watanabe, E; Yamamoto, H; Yokoyama, Y, 2016
)
0.43
"We aimed to develop population pharmacokinetic (PK) models of ampicillin and sulbactam using pooled data analysis and to optimize dosing regimens of ampicillin-sulbactam (combination ratio of 2:1) in pediatric patients."( Pharmacodynamic Evaluation of Ampicillin-sulbactam in Pediatric Patients Using Plasma and Urine Data.
Ikawa, K; Ishihara, N; Morikawa, N; Naora, K; Onita, T; Tamaki, H; Yano, T, 2022
)
0.72
" Based on these models, we estimated the probability of attaining a pharmacodynamic (PD) target [50% of time that free drug concentrations above the minimum inhibitory concentration, 50% fT > minimum inhibitory concentration (MIC)] against MIC90 [MIC that blocked the growth of 90% of the strains] of common bacteria in community-acquired pneumonia."( Pharmacodynamic Evaluation of Ampicillin-sulbactam in Pediatric Patients Using Plasma and Urine Data.
Ikawa, K; Ishihara, N; Morikawa, N; Naora, K; Onita, T; Tamaki, H; Yano, T, 2022
)
0.72
"The pharmacokinetic variability of ampicillin-sulbactam in adults has not been extensively described, particularly in patients with a reduced renal function (i."( Population Pharmacokinetics and Dosing Simulations of Ampicillin and Sulbactam in Hospitalised Adult Patients.
Abdul-Aziz, MH; Cotta, MO; Lukas, DL; Parker, S; Roberts, JA; Setiawan, E; Sosilya, H; Wallis, SC; Widjanarko, D, 2023
)
0.91

Compound-Compound Interactions

ExcerptReferenceRelevance
"This in vitro study evaluated the activities of vancomycin, LY333328, and teicoplanin alone and in combination with gentamicin, rifampin, and RP59500 against Staphylococcus aureus isolates with intermediate susceptibilities to vancomycin."( Evaluation of bactericidal activities of LY333328, vancomycin, teicoplanin, ampicillin-sulbactam, trovafloxacin, and RP59500 alone or in combination with rifampin or gentamicin against different strains of vancomycin-intermediate Staphylococcus aureus by
Aeschlimann, JR; Hershberger, E; Moldovan, T; Rybak, MJ, 1999
)
0.3
"We report a case of postsurgical meningitis caused by multiresistant Acinetobacter baumannii successfully treated with high doses of ampicillin/sulbactam combined with rifampicin and fosfomycin."( Postsurgical meningitis due to multiresistant Acinetobacter baumannii successfully treated with high doses of ampicillin/sulbactam combined with rifampicin and fosfomycin.
Clec'h, C; Cohen, Y; Jauréguy, F; Mellon, G; Picard, B, 2012
)
0.38
"Evaluate the in vivo efficacy and resistance prevention of cefiderocol in combination with ceftazidime/avibactam, ampicillin/sulbactam and meropenem using human-simulated regimens (HSR) in the murine infection model."( In vivo efficacy & resistance prevention of cefiderocol in combination with ceftazidime/avibactam, ampicillin/sulbactam or meropenem using human-simulated regimens versus Acinetobacter baumannii.
Echols, R; Gill, CM; Longshaw, C; Nicolau, DP; Santini, D; Takemura, M; Yamano, Y, 2023
)
0.91

Bioavailability

Oral bioavailability of ampicillin when bound to sulbactam (sultamicillin) was assessed. Ampicillin alone and that of amoxycillin with a ligand of clavulanic acid were also assessed.

ExcerptReferenceRelevance
"Oral bioavailability of ampicillin when bound to sulbactam (sultamicillin) compared with ampicillin alone and that of amoxycillin with a ligand of clavulanic acid versus amoxycillin alone were assessed in 16 healthy subjects using an open label, multiple crossover study."( Oral bioavailability of ampicillin and amoxycillin alone and bound in fixed proportions to sulbactam and clavulanic acid.
Costermans, J; Desager, JP; Harvengt, C; Van Nieuwenhuyze, Y,
)
0.37
" First-pass hydrolysis of this prodrug liberates equimolar proportions of sulbactam in plasma, saliva and urine is described and was used to determine the absolute bioavailability of sulbactam and ampicillin from sultamicillin in six normal male volunteers who each received a single 750 mg oral dose of sultamicillin or an iv dose of the equivalent amounts of ampicillin (441 mg) and sulbactam (294 mg)."( Pharmacokinetics and bioavailability of sultamicillin estimated by high performance liquid chromatography.
Bradbrook, ID; Cox, DA; Lees, LJ; Morrison, PJ; ROgers, HJ; Spector, RG, 1983
)
0.72
"5 times greater total bioavailability for ampicillin and sulbactam than when each was used individually."( Pharmacokinetics of sultamicillin in mice, rats, and dogs.
English, AR; Girard, D; Haskell, SL, 1984
)
0.59
" The bioavailability after intramuscular injection was high and similar in both drugs (72."( Pharmacokinetics of an ampicillin-sulbactam combination after intravenous and intramuscular administration to sheep.
Cárceles, CM; Escudero, E; Espuny, A; Vicente, S, 1999
)
0.3
" The bioavailability after intramuscular injection was high and similar in both drugs (73."( Pharmacokinetics of an ampicillin/sulbactam (2:1) combination in rabbits.
Cárceles, CM; Escudero, E; Serrano, JM; Vicente, MS, 2002
)
0.31
" The aim of the present studies, performed in two different groups of volunteers, was to compare the bioavailability of 750 mg sultamicillin tablets (Duobaktam 750 mg tablets, study 1) and sultamicillin 250 mg/5mL suspensions (Duobaktam 250 mg/5mL, study 2)."( Effect of the formulation on the bioequivalence of sultamicillin: tablets and suspension.
Alpan, RS; Erenmemisoglu, A; Koytchev, R; Kunter, U; Ozalp, Y, 2004
)
0.78
" The present study was performed to investigate the relative bioavailability and to assess the bioequivalence of two different sultamicillin suspensions (Devasid 250 mg/5 ml as test preparation and 375 mg/7."( Bioequivalence study of sultamicillin suspensions.
Arnold, P; Erenmemişoğlu, A; Hincal, AA; Kanzik, I; Martin, W; Sailer, R; Tamur, U, 2007
)
0.85

Dosage Studied

Further studies in larger groups of patients are needed to clarify the therapeutic efficacy and safety of sultamicillin. Two dosage schedules were investigated, both resulting in the same to gonorrhoea.

ExcerptRelevanceReference
" The daily dosage of Unasyn was 3-12 g/die administered in three to four divided doses, and was determined by the severity of infection, the antibiotic susceptibility of the causative organism(s) and the condition of the patient."( [Sulbactam-ampicillin in surgery. Our experience].
Casiraghi, S; Caspani, P; Germiniani, R; Pace, M; Trabucchi, E, 1992
)
0.28
" All antibiotics were given by intravenous bolus injection in a number of dosing regimens."( Use of ampicillin-sulbactam for treatment of experimental meningitis caused by a beta-lactamase-producing strain of Escherichia coli K-1.
Fournier, MA; Guerra-Romero, L; Kennedy, SL; Täuber, MG; Tureen, JH, 1991
)
0.28
"A total of 124 patients with lower respiratory tract (44) or urinary tract infections (80) were enrolled in an open, multicenter study to evaluate the efficacy and tolerability of sulbactam/ampicillin, administered at the dosage of 3 g/die by intramuscular route."( Clinical results of a multicenter study with sulbactam/ampicillin for the treatment of patients with lower respiratory and urinary tract infections.
Chiodo, F; De Simone, C; Delia, S; Gargiulo, M; Paoloni, M; Pastore, G; Scalise, G; Sorice, F; Tonietti, G; Zanussi, C, 1991
)
0.28
" The dosage was considered appropriate in 88% of the patients."( Use of ampicillin-sulbactam before and after formulary inclusion.
Koch, KE; Taylor, MR, 1991
)
0.28
" The treatment was continued for at least 7 days for 24 patients at the dosage of 3 g sulbactam/ampicillin twice daily, for a further 24 patients at the dosage of 6 g piperacillin twice daily and for two patients at the dosage of 8 g piperacillin twice daily."( Sulbactam/ampicillin combination in the treatment of acute and chronic lower respiratory infections.
Bisetti, A; Grassi, L; Putti, P; Scacciacillani, E, 1991
)
0.28
" No adverse side-effects were reported and dosage adjustment was not required in the elderly."( Clinical efficacy of sulbactam/ampicillin in the treatment of moderately severe bacterial infections.
Boey, ML; Feng, PH; Fong, KY; Howe, HS, 1989
)
0.28
" Several factors support such usage: 1) the superiority of sultamicillin compared with the ampicillin commercial dosage form as a delivery system for ampicillin; 2) the possible occurrence at the infection site of beta-lactamase-producing organisms, not themselves pathogens, which nevertheless impair the activity of the beta-lactam antibiotic against sensitive pathogens; 3) the complementary binding of penicillin-binding proteins by ampicillin and sulbactam in ampicillin-sensitive organisms; 4) the lack of resistance development following repeated exposure of strains sensitive to sulbactam/ampicillin suggested by in vitro studies; and 5) the inability of sulbactam to induce beta-lactamase production."( Worldwide clinical experience with sultamicillin.
Gilbert, GS; Knirsch, AK; Noguchi, Y; Pitts, NE, 1989
)
0.8
" The most common dosage regimen was 375 mg three times daily."( Sultamicillin in the treatment of urinary tract infections.
Kawada, Y, 1989
)
1.72
" Further studies in larger groups of patients are needed to clarify the therapeutic efficacy and safety of sultamicillin in comparison with other antibacterial regimens, and to determine the optimum single dosage for the treatment of gonorrhoea."( Sultamicillin. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use.
Campoli-Richards, DM; Friedel, HA; Goa, KL, 1989
)
1.93
" Sulbactam/ampicillin was given by intravenous bolus in a dosage range of 75-450 mg/kg/day in four divided doses for variable periods of time depending on the type and severity of the infection."( Intravenous sulbactam/ampicillin in the treatment of pediatric infections.
Chen, CM; Chu, ML; Hsu, CY; Huang, LM; Lee, CY; Lee, MJ; Lin, TY,
)
0.13
" The aims were to determine an appropriate dosage regimen and to study the pharmacokinetics."( Pharmacokinetic study of sulbactam and ampicillin administered concomitantly by intraarterial or intravenous infusion in the newborn.
Cockburn, F; McAllister, TA; Sutton, AM; Turner, TL,
)
0.13
" Sulbactam/ampicillin was administered im or iv at a dosage of 3-9 g/day depending on the site and severity of the infection."( Clinical efficacy and safety of sulbactam/ampicillin in patients suffering from chronic liver disease.
Barba, D; Esposito, S; Galante, D; Ruffilli, MP, 1987
)
0.27
" SBTPC fine granules were administered orally to 1 patient with bronchitis, 9 patients with bronchopneumonia, 7 patients with tonsillitis, 4 patients with scarlet fever, 1 patient each with pharyngitis, otitis media, purulent parotitis, and urinary tract infection and 6 patients with skin and soft tissue infections at daily dosage levels of 26."( [Clinical evaluation of sultamicillin fine granules in pediatric patients].
Ito, S; Mayumi, M; Mikawa, H, 1988
)
0.58
" The patients included 9 boys and 10 girls from 11 months to 13 years old and they were given orally a dosage of 15."( [Clinical study of sultamicillin fine granules].
Kawakami, K; Okada, K; Takeda, E, 1988
)
0.6
" The dosage was 10-30 mg/kg daily."( [Efficacy of sultamicillin fine granules in pyoderma, particularly in impetigo contagiosa].
Inoue, Y; Kawashima, T; Tokuda, Y, 1988
)
0.64
" Two dosage schedules were investigated, both resulting in the same total daily dosage (1500 mg sultamicillin)."( Sultamicillin (CP-49, 952): evaluation of two dosage schedules in urinary infection.
Ball, AP; Fox, C; Ghosh, D, 1984
)
1.93
" One patient in each dosage group discontinued the medication because of severe diarrhoea."( Clinical, bacteriological and pharmacokinetic results from an open trial of sultamicillin in patients with acute exacerbations of chronic bronchitis.
Davies, BI; Maesen, FP; van Noord, JA, 1984
)
0.5
"Increasing the dosing interval for T-C in patients with end-stage renal disease may lead to periods of insufficient clavulanic acid to protect ticarcillin from beta-lactamase degradation."( Comparison of ampicillin-sulbactam and ticarcillin-clavulanic acid in patients with chronic renal failure: effects of differential pharmacokinetics on serum bactericidal activity.
Butler, SC; Hardin, TC; Jorgensen, JH; Ross, S; Wakeford, JH,
)
0.13
"An in vitro pharmacokinetic model (IVPM) and a mouse model of lethal bacteremia were used to compare the pharmacodynamics of ampicillin-sulbactam when the two components were dosed simultaneously and in sequence against TEM-1-producing Escherichia coli."( Efficacy of ampicillin-sulbactam is not dependent upon maintenance of a critical ratio between components: sulbactam pharmacokinetics in pharmacodynamic interactions.
Alexov, M; Lister, PD; Sanders, CC, 1996
)
0.29
" Serum bactericidal titers were determined and used to calculate the duration of measurable bactericidal activity over the dosing interval of each of the regimens against two clinical isolates of Bacillus fragilis, Escherichia coli, Enterococcus faecalis, and Pseudomonas aeruginosa."( Comparison of the bactericidal activities of piperacillin-tazobactam, ticarcillin-clavulanate, and ampicillin-sulbactam against clinical isolates of Bacteroides fragilis, Enterococcus faecalis, Escherichia coli, and Pseudomonas aeruginosa.
Klepser, ME; Marangos, MN; Nicolau, DP; Nightingale, CH; Quintiliani, R; Zhu, Z, 1997
)
0.3
" The data on the PAE of Unasyn may be of clinical relevance in determining dosage regimens of the drug."( Postantibiotic effect of ampicillin/sulbactam against mycobacteria.
Harris, EB; Prabhakaran, K; Randhawa, B, 1999
)
0.3
" Ampicillin 2 g-sulbactam 1 g every 3 hours was administered based on history of therapeutic failure of traditional dosing in our thermal injury population."( Nontraditional dosing of ampicillin-sulbactam for multidrug-resistant Acinetobacter baumannii meningitis.
Ackerman, BH; Cawley, MJ; Lee, S; Suh, C, 2002
)
0.31
"The pharmacokinetics of a 2:1 ampicillin-sulbactam combination in six rabbits, after intravenous and intramuscular injection at a single dosage of 20 mg/kg bodyweight (13."( Pharmacokinetics of an ampicillin/sulbactam (2:1) combination in rabbits.
Cárceles, CM; Escudero, E; Serrano, JM; Vicente, MS, 2002
)
0.31
" Dosage was adjusted according to creatinine clearance."( Efficacy and safety of high-dose ampicillin/sulbactam vs. colistin as monotherapy for the treatment of multidrug resistant Acinetobacter baumannii ventilator-associated pneumonia.
Betrosian, AP; Douzinas, EE; Frantzeskaki, F; Xanthaki, A, 2008
)
0.35
" Despite its frequent use in intensive care units, there are no available dosing recommendations for patients with AKI undergoing renal replacement therapy."( Pharmacokinetics of ampicillin/sulbactam in critically ill patients with acute kidney injury undergoing extended dialysis.
Broll, M; Burhenne, H; Burkhardt, O; Clajus, C; Hafer, C; Kaever, V; Kielstein, JT; Knitsch, W; Lorenzen, JM, 2012
)
0.38
" There was no significant accumulation using a twice-daily dosage of 2 g/1 g ampicillin/sulbactam."( Pharmacokinetics of ampicillin/sulbactam in critically ill patients with acute kidney injury undergoing extended dialysis.
Broll, M; Burhenne, H; Burkhardt, O; Clajus, C; Hafer, C; Kaever, V; Kielstein, JT; Knitsch, W; Lorenzen, JM, 2012
)
0.38
"3 m(2); blood and dialysate flow, 160 ml/min; treatment time, 480 minutes), a twice-daily dosing schedule of at least 2 g/1 g ampicillin/sulbactam, with one dose given after ED, should be used to avoid underdosing."( Pharmacokinetics of ampicillin/sulbactam in critically ill patients with acute kidney injury undergoing extended dialysis.
Broll, M; Burhenne, H; Burkhardt, O; Clajus, C; Hafer, C; Kaever, V; Kielstein, JT; Knitsch, W; Lorenzen, JM, 2012
)
0.38
" This study aimed to use renal function to determine the most appropriate timing for intraoperative repeated dosing of ampicillin-sulbactam, a commonly used prophylactic antibiotic, to maintain adequate concentrations throughout the course of surgery."( Pharmacokinetics of ampicillin-sulbactam and the renal function-based optimization of dosing regimens for prophylaxis in patients undergoing cardiovascular surgery.
Iguro, Y; Ikawa, K; Imoto, Y; Ishida, S; Matsumoto, K; Morikawa, N; Okano, Y; Shimodozono, Y; Takeda, Y; Watanabe, E; Yamada, K; Yamamoto, H; Yokoyama, Y, 2012
)
0.38
" In our patient, intraperitoneal dosing of polymyxin B was determined based on limited published pharmacokinetic and pharmacodynamic data."( Successful treatment of extensively drug-resistant Acinetobacter baumannii peritoneal dialysis peritonitis with intraperitoneal polymyxin B and ampicillin-sulbactam.
Esterly, JS; Fitzpatrick, MA; Postelnick, MJ; Sutton, SH,
)
0.13
" In elderly patients without renal impairment and/or in severe infection with less susceptible pathogens, more frequent dosing of ampicillin 2 g/sulbactam 1 g can be necessary to avoid the risk of underdosing in CAP."( Ampicillin/sulbactam in elderly patients with community-acquired pneumonia.
Drewelow, B; Frimmel, S; Klammt, S; Loebermann, M; Majcher-Peszynska, J; Mundkowski, RG; Reisinger, EC; Welte, T, 2014
)
0.4
" The therapeutic challenges for ensuring achievement of optimal dosing of SAM result partly from bacterial susceptibility but also from the pharmacokinetic (PK) alterations common to β-lactam agents in critical illness."( Ampicillin/sulbactam: its potential use in treating infections in critically ill patients.
Adnan, S; Lipman, J; Paterson, DL; Roberts, JA, 2013
)
0.39
" This study aimed to determine the most appropriate timing for intraoperative repeated dosing of ampicillin-sulbactam, a commonly used antibiotic prophylaxis regimen, to maintain adequate concentrations throughout the course of cardiovascular surgery with cardiopulmonary bypass (CPB)."( Pharmacokinetics of Prophylactic Ampicillin-Sulbactam and Dosing Optimization in Patients Undergoing Cardiovascular Surgery with Cardiopulmonary Bypass.
Ikawa, K; Imoto, Y; Matsumoto, K; Morikawa, N; Takeda, Y; Watanabe, E; Yamamoto, H; Yokoyama, Y, 2015
)
0.42
"This study sought to investigate whether dosing frequency (the number of doses per day) affects the antimicrobial efficacy and safety of ampicillin/sulbactam (ABPC/SBT) in Japanese elderly pneumonia patients treated with ABPC/SBT at 6 g/day."( Effects of dosing frequency on the clinical efficacy of ampicillin/sulbactam in Japanese elderly patients with pneumonia: A single-center retrospective observational study.
Nozawa, K; Sato, H; Sato, VH; Sugiyama, E; Suzuki, H; Suzuki, T; Tajima, M; Takahashi, K; Yoshii, M, 2021
)
0.62
" It is important to optimize the dose and dosing interval of ampicillin-sulbactam because in patients with decreased renal function and low skeletal muscle mass, such as the elderly, excess drug may burden renal function."( Dosing Optimization of Ampicillin-Sulbactam Based on Cystatin C in Elderly Patients with Pneumonia.
Enoki, Y; Ikawa, K; Matsubara, K; Matsumoto, K; Morikawa, N; Ohshige, T; Shigemi, A; Takeda, Y; Terazono, H; Watanabe, E; Yokoyama, Y, 2021
)
0.62
"We aimed to develop population pharmacokinetic (PK) models of ampicillin and sulbactam using pooled data analysis and to optimize dosing regimens of ampicillin-sulbactam (combination ratio of 2:1) in pediatric patients."( Pharmacodynamic Evaluation of Ampicillin-sulbactam in Pediatric Patients Using Plasma and Urine Data.
Ikawa, K; Ishihara, N; Morikawa, N; Naora, K; Onita, T; Tamaki, H; Yano, T, 2022
)
0.72
" (Food and Drug Administration-approved maximum dosage in United States) might be better than 45 mg/kg 3 times daily (within approved dosage in Japan) to cover many pathogens."( Pharmacodynamic Evaluation of Ampicillin-sulbactam in Pediatric Patients Using Plasma and Urine Data.
Ikawa, K; Ishihara, N; Morikawa, N; Naora, K; Onita, T; Tamaki, H; Yano, T, 2022
)
0.72
" Adherence rate with first dosing recommendation was 100%, as compared with 41."( Prophylactic Intraoperative Antibiotic Dosing in Head and Neck Surgery: Opportunities for Improvement and Future Study.
Cohen, O; Cook, A; Dibble, J; Mehra, S; Panth, N; Paolillo, D; Shah, R, 2023
)
0.91
"This study investigated the population pharmacokinetics of ampicillin and sulbactam in patients with a wide range of renal functions and sought to define dosing approaches that have a high likelihood for optimising drug exposure."( Population Pharmacokinetics and Dosing Simulations of Ampicillin and Sulbactam in Hospitalised Adult Patients.
Abdul-Aziz, MH; Cotta, MO; Lukas, DL; Parker, S; Roberts, JA; Setiawan, E; Sosilya, H; Wallis, SC; Widjanarko, D, 2023
)
0.91
" Approved dosing regimens of ampicillin-sulbactam were sufficient against MICs ≤ 8 and ≤ 4 mg/L, respectively."( Population Pharmacokinetics and Dosing Simulations of Ampicillin and Sulbactam in Hospitalised Adult Patients.
Abdul-Aziz, MH; Cotta, MO; Lukas, DL; Parker, S; Roberts, JA; Setiawan, E; Sosilya, H; Wallis, SC; Widjanarko, D, 2023
)
0.91
"The described dosing regimen for ampicillin/sulbactam is safe with respect to the defined MIC breakpoints for ampicillin, and continuous subtherapeutic concentration is unlikely."( Evaluation of continuous ampicillin/sulbactam infusion in critically ill patients.
Baehner, T; Passon, SG; Schmidt, AR; Velten, M; Wittmann, M, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
penicillanic acid ester
[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]

Bioassays (30)

Assay IDTitleYearJournalArticle
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]
AID352617Antimicrobial activity against methicillin-resistant Staphylococcus aureus isolates by tube dilution method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis and in vitro antimicrobial activity of some novel substituted benzimidazole derivatives having potent activity against MRSA.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID392753Antibacterial activity against Escherichia coli 25922 after 18 to 24 hrs by tube dilution method2009Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
Synthesis and antimicrobial evaluation of some new substituted purine derivatives.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID363845Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 after 18 hrs by macro broth dilution assay2008European journal of medicinal chemistry, Jul, Volume: 43, Issue:7
Synthesis, potent anti-staphylococcal activity and QSARs of some novel 2-anilinobenzazoles.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID363844Antibacterial activity against Staphylococcus aureus ATCC 25923 after 18 hrs by macro broth dilution assay2008European journal of medicinal chemistry, Jul, Volume: 43, Issue:7
Synthesis, potent anti-staphylococcal activity and QSARs of some novel 2-anilinobenzazoles.
AID392752Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate after 18 to 24 hrs by tube dilution method2009Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
Synthesis and antimicrobial evaluation of some new substituted purine derivatives.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID352616Antimicrobial activity against methicillin-resistant Staphylococcus aureus ATCC 431300 by tube dilution method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis and in vitro antimicrobial activity of some novel substituted benzimidazole derivatives having potent activity against MRSA.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID352615Antimicrobial activity against Staphylococcus aureus ATCC 25923 by tube dilution method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis and in vitro antimicrobial activity of some novel substituted benzimidazole derivatives having potent activity against MRSA.
AID352619Antimicrobial activity against Bacillus subtilis ATCC 6633 by tube dilution method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis and in vitro antimicrobial activity of some novel substituted benzimidazole derivatives having potent activity against MRSA.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID392751Antibacterial activity against methicillin-resistant Staphylococcus aureus 431300 after 18 to 24 hrs by tube dilution method2009Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
Synthesis and antimicrobial evaluation of some new substituted purine derivatives.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID392750Antibacterial activity against Staphylococcus aureus ATCC 25923 after 18 to 24 hrs by tube dilution method2009Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
Synthesis and antimicrobial evaluation of some new substituted purine derivatives.
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]
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]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID392754Antibacterial activity against Bacillus subtilis 6633 after 18 to 24 hrs by tube dilution method2009Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
Synthesis and antimicrobial evaluation of some new substituted purine derivatives.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' 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
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' 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]
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (500)

TimeframeStudies, This Drug (%)All Drugs %
pre-199059 (11.80)18.7374
1990's156 (31.20)18.2507
2000's112 (22.40)29.6817
2010's123 (24.60)24.3611
2020's50 (10.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 75.10

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 Index75.10 (24.57)
Research Supply Index6.55 (2.92)
Research Growth Index4.83 (4.65)
Search Engine Demand Index132.29 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (75.10)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials120 (20.76%)5.53%
Reviews43 (7.44%)6.00%
Case Studies111 (19.20%)4.05%
Observational6 (1.04%)0.25%
Other298 (51.56%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (17)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Multicenter, Randomized, Open-Label Comparison of the Safety And Efficacy of Tigecycline With That of Ampicillin-Sulbactam or Amoxicillin-Clavulanate to Treat Complicated Skin And Skin Structure Infections [NCT00368537]Phase 4550 participants (Actual)Interventional2006-09-30Completed
Antibiotic Prophylaxis for Early Ventilator-associated Pneumonia in Neurological Patients: A Randomized Trial [NCT01118403]Phase 40 participants (Actual)Interventional2011-03-31Withdrawn(stopped due to He could not be started due to lack of funds)
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)
A Randomized Controlled Trial Assessing Noninferiority of Three Antimicrobial Regimens for the Treatment of Grade III Open Fractures [NCT03560232]Phase 417 participants (Actual)Interventional2018-07-09Terminated(stopped due to Unable to recruit patients in a timely fashion and unable to recruit sufficient patients)
Ampicillin / Sulbactam Versus Cefuroxime as Antimicrobial Prophylaxis for Cesarean Section: a Randomized Study [NCT01138852]Phase 4176 participants (Actual)Interventional2004-07-31Completed
Is an Antibiotic Prescription Required After Laparoscopic Cholecystectomy for Acute Calculous Cholecystitis? [NCT04290104]Phase 42 participants (Anticipated)Interventional2020-10-15Not yet recruiting
Comparing Oral Versus Parenteral Antimicrobial Therapy (COPAT) Trial [NCT05977868]Phase 4135 participants (Anticipated)Interventional2023-08-04Enrolling by invitation
Cefiderocol and Ampicillin-sulbactam vs. Colistin or Colistin-meropenem for Carbapenem Resistant Acinetobacter Baumannii Bacteremia or Hospital-acquired Pneumonia: Controlled Clinical Study With Historical Controls (CASCADE) [NCT05922124]Phase 4734 participants (Anticipated)Interventional2024-01-31Not yet recruiting
A Comparative Study of Ampicillin/Sulbactam Versus Moxifloxacin in the Treatment of Complicated Intra-abdominal Infections [NCT00952796]Phase 4100 participants (Anticipated)Interventional2009-01-31Completed
A Prospective, Double-blind, Multi Center, Randomized Clinical Study to Compare the Efficacy and Safety of Ertapenem 3 Days Versus Ampicillin-Sulbactam 3 Days in the Treatment of Localized Community Acquired Intra-abdominal Infection (IAI). (T.E.A. Study [NCT00630513]Phase 4142 participants (Actual)Interventional2008-01-31Completed
Ciprofloxacin, Ampicillin-sulbactam and Placebo Prophylaxis in Laparoscopic Cholecystectomy. A Randomized Controlled Study [NCT01888822]Phase 4138 participants (Actual)Interventional2013-06-30Terminated
Multiple-dose Pharmacokinetics of Ampicillin / Sulbactam and Amoxicillin / Clavulanic Acid During Haemodialysis in Longterm Haemodialysis Patients [NCT02007603]Phase 316 participants (Actual)Interventional2013-08-31Completed
Phase IV Study of Determining the Efficacy of Ampicillin/Sulbactam Combination as Antibiotic Prophylaxis During Breast Cancer Surgery in Patients With a Body Mass Index (BMI) Over 25. [NCT00356148]Phase 4372 participants (Actual)Interventional2003-10-31Completed
The Impact of Cefepime and Unictam on Preventing Post-Cesarean Surgical Site Infections [NCT06048692]Phase 3213 participants (Actual)Interventional2023-01-01Active, not recruiting
A Multicenter, Open Label Trial Evaluating Intravenous Azithromycin Plus Intravenous Ampicillin/Sulbactam Followed by Oral Azithromycin Plus Intravenous Ampicillin/Sulbactam for the Treatment of Hospitalized Subjects With Community-Acquired Pneumonia (CAP [NCT00137007]Phase 4151 participants (Actual)Interventional2003-11-30Completed
Randomized Double Blind Placebo-controlled Study to Demonstrate That Antibiotics Are Not Needed in Moderate Acute Exacerbations of COPD - The ABACOPD Study [NCT01892488]Phase 4295 participants (Actual)Interventional2013-06-07Completed
The Evaluation of Postoperative Antibiotics in Non-Infected Mandible Fractures [NCT04198129]Phase 1174 participants (Anticipated)Interventional2020-10-01Recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00356148 (2) [back to overview]Number of Patients With Body Mass Index (BMI) Over 25 Who Developed Surgical Site Infection (SSI) in Groups Who Received Antibiotic Prophylaxis (Prophylaxis Group) and no Prophylaxis (No Prophylaxis Group).
NCT00356148 (2) [back to overview]Overall SSI-related Prophylaxis and Treatment Cost in Patients With BMI Over 25 Who Received Prophylaxis (Prophylaxis Group) and Not (No Prophylaxis Group).
NCT00368537 (5) [back to overview]Number of Clinically Evaluable (CE) Patients With Clinical Response of Cure at the Test-of-cure (TOC) Visit
NCT00368537 (5) [back to overview]Number of Microbiologically Evaluable Patients With Clinical Response of Cure at the Test-of-cure (TOC) Visit
NCT00368537 (5) [back to overview]Inpatient Healthcare Resource Utilization on or Before Test-of-Cure - Number of Patients
NCT00368537 (5) [back to overview]Minimum Inhibitory Concentration (MIC) 50 and 90 by Baseline Isolate
NCT00368537 (5) [back to overview]Number of Microbiologically Evaluable Patients by Microbiologic Response at Test-of-Cure (TOC) Visit

Number of Patients With Body Mass Index (BMI) Over 25 Who Developed Surgical Site Infection (SSI) in Groups Who Received Antibiotic Prophylaxis (Prophylaxis Group) and no Prophylaxis (No Prophylaxis Group).

(NCT00356148)
Timeframe: 1 month

Interventionparticipants (Number)
Prophylaxis Group9
No Prophylaxis Group25

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Number of Clinically Evaluable (CE) Patients With Clinical Response of Cure at the Test-of-cure (TOC) Visit

Investigator assigned clinical response of cure of the cSSSI defined as: resolution of all clinical signs and symptoms of infection (healing of chronic underlying skin ulcer not required) or improvement of signs or symptoms of the infection to such an extent that no further antibacterial therapy was necessary. CE population were those who completed TOC assessment of cure or failure (but not indeterminate) or, in case of premature discontinuation due to lack of efficacy, had completed end of treatment assessment such that assessment of clinical response could be made. (NCT00368537)
Timeframe: up to 6 weeks

Interventionparticipants (Number)
Tigecycline162
Ampicillin-Sulbactam or Amoxicillin-Clavulanate152

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Number of Microbiologically Evaluable Patients With Clinical Response of Cure at the Test-of-cure (TOC) Visit

Investigator assigned clinical response of cure of the cSSSI defined as: resolution of all clinical signs and symptoms of infection (healing of chronic underlying skin ulcer not required) or improvement of signs or symptoms of the infection to such an extent that no further antibacterial therapy was necessary. ME population were subjects who were CE and had baseline culture with at least 1 identified isolate that was susceptible to study drug and comparator. TOC performed 8-50 days after last dose of study drug. (NCT00368537)
Timeframe: up to 6 weeks

Interventionparticipants (Number)
Tigecycline96
Ampicillin-Sulbactam or Amoxicillin-Clavulanate77

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Inpatient Healthcare Resource Utilization on or Before Test-of-Cure - Number of Patients

Healthcare resource utilization assessment included intensive care unit (ICU) and non-ICU inpatient hospitalization. TOC performed 8-50 days after last dose of study drug. (NCT00368537)
Timeframe: up to 6 weeks

,
Interventionparticipants (Number)
Intensive care unitNon-ICU inpatient hospitalization
Ampicillin-Sulbactam or Amoxicillin-Clavulanate9263
Tigecycline6268

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Minimum Inhibitory Concentration (MIC) 50 and 90 by Baseline Isolate

In vitro activity of the study drugs against a range of pathogenic bacteria that cause complicated skin and skin structure infection (cSSSI) were analyzed using MIC. MIC 50 and MIC 90 are the lowest concentrations of a drug that inhibit the growth of 50% and 90% of a microorganism, respectively. TOC performed 8-50 days after last dose of study drug. (NCT00368537)
Timeframe: up to 6 weeks

,
Interventionmcg/mL (Number)
Enterococcus Faecalis MIC50 (n=20,20)Enterococcus Faecalis MIC90 (n=20,20)Escherichia Coli MIC50 (n=29,29)Escherichia Coli MIC90 (n=29,29)Klebsiella Pneumoniae MIC50 (n=13,13)Klebsiella Pneumoniae MIC90 (n=13,13)Staphylococcus Aureus MIC50 (n=176,176)Staphylococcus Aureus MIC90 (n=176,176)Streptococcus Agalactiae MIC50 (n=18,18)Streptococcus Agalactiae MIC90 (n=18,18)Streptococcus Pyogenes MIC50 (n=18,18)Streptococcus Pyogenes MIC90 (n=18,18)
Ampicillin-Sulbactam or Amoxicillin-Clavulanate1.001.008.0032.002.008.002.008.000.120.120.060.06
Tigecycline0.120.250.250.500.502.000.120.250.030.060.030.06

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Number of Microbiologically Evaluable Patients by Microbiologic Response at Test-of-Cure (TOC) Visit

Microbiological response assessed at patient level. Eradication=baseline isolate not present in repeat culture from the original infection site; Presumed Eradication=clinical response of cure precluded the availability of a specimen for culture; Persistence=baseline isolate present in repeat culture from the original infection site; Presumed Persistence=culture data not available for patients with a clinical response of failure; Superinfection=culture from the primary infection site had new pathogen not identified as a baseline isolate and clinical response was failure. (NCT00368537)
Timeframe: up to 6 weeks

,
Interventionparticipants (Number)
Eradication + presumed eradicationPersistence + Presumed persistenceSuperinfection
Ampicillin-Sulbactam or Amoxicillin-Clavulanate76231
Tigecycline95252

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