Page last updated: 2024-11-12

rifamycins

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

Cross-References

ID SourceID
PubMed CID12314962
SCHEMBL ID22389514
MeSH IDM0019113

Synonyms (3)

Synonym
rifamycins ,
SCHEMBL22389514
[(9e,19e,21e)-2,15,17-trihydroxy-11-methoxy-3,7,12,14,16,18,22-heptamethyl-6,23,27,29-tetraoxo-8,30-dioxa-24-azatetracyclo[23.3.1.14,7.05,28]triaconta-1(28),2,4,9,19,21,25-heptaen-13-yl] acetate

Research Excerpts

Overview

Rifamycins are a class of antibiotics that were first discovered in 1957. They are known for their use in treating tuberculosis (TB) Rifampicin is the most commonly prescribed.

ExcerptReferenceRelevance
"Rifamycins are a class of antibiotics that were first discovered in 1957 and are known for their use in treating tuberculosis (TB). "( Rifamycin antibiotics and the mechanisms of their failure.
Adams, RA; Brynildsen, MP; Lemma, AS; Leon, G; Miller, NM; Reyes, SP; Sivaloganathan, DM; Thantrong, CH; Thokkadam, AM; Wan, X, 2021
)
2.06
"Rifamycins are a class of antibiotic compounds of which rifampicin is the most commonly prescribed. "( Characterization of three rifamycins via electrospray mass spectrometry and HPLC-thermospray mass spectrometry.
Bloom, J; Churchwell, MI; Getek, TA; Hansen, EB; Holder, CL; Korfmacher, WA; McManus, KT, 1993
)
2.03

Effects

ExcerptReferenceRelevance
"Rifamycins have been clinically utilized against mycobacterial infections for more than 50 years; however, their biosynthesis has not been fully elucidated. "( A Flavin-Dependent Monooxygenase Mediates Divergent Oxidation of Rifamycin.
Han, L; He, QL; Luo, GC; Peng, SY; Tang, GL; Zhang, K; Zhou, Q, 2021
)
2.06

Actions

Rifamycins inhibit RNA polymerase of most bacterial genera. RifamyCins bind to and inhibit DNA polymerase.

ExcerptReferenceRelevance
"Rifamycins inhibit RNA polymerase of most bacterial genera. "( Rifamycins, Alone and in Combination.
Rothstein, DM, 2016
)
3.32
"Rifamycins bind to and inhibit DNA polymerase."( Use of a macrocyclic antibiotic, rifamycin B, and indirect detection for the resolution of racemic amino alcohols by CE.
Armstrong, DW; Reid, GL; Rundlett, K, 1994
)
1.01

Toxicity

ExcerptReferenceRelevance
" The oral LD50 value for this species was greater than 2000 mg/kg."( Acute, subacute, chronic toxicity and mutagenicity studies of rifaximin (L/105) in rats.
Bertoli, D; Borelli, G, 1986
)
0.27
" Rifaximin was well tolerated; the few treatment-related adverse events showed no consistent pattern or dose relationship."( Evaluation of the efficacy and safety of rifaximin in the treatment of hepatic encephalopathy: a double-blind, randomized, dose-finding multi-centre study.
James, OF; Morgan, MY; Warnes, TW; Williams, R, 2000
)
0.31
" Because therapy is directed largely at relieving symptoms and minimising inconvenience, the chosen antibacterial should ideally be both efficacious and pose a low risk of adverse effects."( Safety and tolerability of the antibacterial rifaximin in the treatment of travellers' diarrhoea.
Ericsson, CD, 2006
)
0.33
" Rifaximin 1,100 mg once daily was well tolerated with no observed differences in adverse events, whether solicited or unsolicited among the two treatment groups."( A randomized, double-blind, placebo-controlled study evaluating the efficacy and safety of rifaximin for the prevention of travelers' diarrhea in US military personnel deployed to Incirlik Air Base, Incirlik, Turkey.
Armstrong, AW; Mostafa, M; Nakhla, I; Riddle, MS; Shaheen, H; Tribble, DR; Ulukan, S; Weiner, M,
)
0.13
" Adverse effects were similar among patients receiving rifaximin or placebo in all studies."( The efficacy and safety of rifaximin for the irritable bowel syndrome: a systematic review and meta-analysis.
Chey, WD; Kim, HM; Maneerattannaporn, M; Menees, SB, 2012
)
0.38
" The profile and rate of adverse events with long-term rifaximin treatment were similar to those of the original RCT."( Rifaximin is safe and well tolerated for long-term maintenance of remission from overt hepatic encephalopathy.
Bass, NM; Bortey, E; Forbes, WP; Frederick, RT; Mullen, KD; Poordad, FF; Sanyal, AJ; Sheikh, MY, 2014
)
0.4
"Long-term treatment (≥24 mo) with rifaximin (550 mg, twice daily) appears to provide a continued reduction in the rate of HE-related and all-cause hospitalization, without an increased rate of adverse events."( Rifaximin is safe and well tolerated for long-term maintenance of remission from overt hepatic encephalopathy.
Bass, NM; Bortey, E; Forbes, WP; Frederick, RT; Mullen, KD; Poordad, FF; Sanyal, AJ; Sheikh, MY, 2014
)
0.4
"To assess and determine the frequency of rifaximin and placebo adverse events (AEs) in phase 2b and phase 3 non-C IBS trials."( Safety and tolerability of rifaximin for the treatment of irritable bowel syndrome without constipation: a pooled analysis of randomised, double-blind, placebo-controlled trials.
Bortey, E; Chang, L; Chey, WD; Forbes, WP; Lembo, A; Paterson, C; Pimentel, M; Schoenfeld, P; Yu, J, 2014
)
0.4
" The overall treatment-emergent adverse event (TEAE) and treatment-related TEAE rates were lower in the rifalazil group (68% and 55%) than in the azithromycin group (71% and 62%), respectively."( Randomized, double-blind, multicenter safety and efficacy study of rifalazil compared with azithromycin for treatment of uncomplicated genital Chlamydia trachomatis infection in women.
Batteiger, BE; Geisler, WM; Hurwitz, SJ; Koltun, WD; Mathew, J; Mayes, A; Morgan, F; Pascual, ML; Sayada, C; Schinazi, RF; Tao, S, 2014
)
0.4
"To compare interventions in terms of patients' adverse events and major clinical outcomes."( Systematic review with network meta-analysis: the comparative effectiveness and safety of interventions in patients with overt hepatic encephalopathy.
Braddock, M; Chen, YP; Huang, GQ; Huang, S; Lin, YQ; Shi, KQ; Wang, LR; Zheng, MH; Zhu, GQ, 2015
)
0.42
" Neomycin appeared to be associated with more adverse events in comparison with non-absorbable disaccharides (OR 10."( Systematic review with network meta-analysis: the comparative effectiveness and safety of interventions in patients with overt hepatic encephalopathy.
Braddock, M; Chen, YP; Huang, GQ; Huang, S; Lin, YQ; Shi, KQ; Wang, LR; Zheng, MH; Zhu, GQ, 2015
)
0.42
" Rifaximin shows the greatest reduction in blood ammonia concentration, and treatment with neomycin demonstrates a higher probability in causing adverse effects among the five compared interventions."( Systematic review with network meta-analysis: the comparative effectiveness and safety of interventions in patients with overt hepatic encephalopathy.
Braddock, M; Chen, YP; Huang, GQ; Huang, S; Lin, YQ; Shi, KQ; Wang, LR; Zheng, MH; Zhu, GQ, 2015
)
0.42
" There was no difference among the studied groups regarding the incidence and severity of adverse events reported."( Efficacy and safety of alternating norfloxacin and rifaximin as primary prophylaxis for spontaneous bacterial peritonitis in cirrhotic ascites: a prospective randomized open-label comparative multicenter study.
Abdelaziz, A; Abdelrashed, M; Assem, M; El-Azab, G; Elemam, S; Elsabaawy, M; Hamed, W; Khodeer, S, 2016
)
0.43
" These properties make rifaximin a safe antibiotic for gut microbiota modulation in patients with IBS."( Rifaximin for the treatment of irritable bowel syndrome - a drug safety evaluation.
Cammarota, G; Gasbarrini, A; Lopetuso, L; Pecere, S; Ponziani, FR; Scaldaferri, F, 2016
)
0.43
" Adverse event rates were low and similar between groups."( Repeat Treatment With Rifaximin Is Safe and Effective in Patients With Diarrhea-Predominant Irritable Bowel Syndrome.
Bortey, E; Cash, B; Forbes, WP; Lembo, A; Paterson, C; Pimentel, M; Rao, SS; Schoenfeld, P; Weinstock, LB, 2016
)
0.43
"Rifaximin treatment seems to be effective and safe for the treatment of SIBO."( Systematic review with meta-analysis: rifaximin is effective and safe for the treatment of small intestine bacterial overgrowth.
Gatta, L; Scarpignato, C, 2017
)
0.46
" About 76% of the patients experienced adverse events (35% diarrhea, 14% nausea and 24% metallic taste), none of which was serious."( Efficacy and safety of rifaximin associated with standard triple therapy (omeprazole, clarithromycin and amoxicillin) for H. pylori eradication: A phase IV pilot clinical trial.
Donday, MG; Gisbert, JP; McNicholl, AG; Ramas, M, 2017
)
0.46
" We included the following outcomes: recurrence of hepatic encephalopathy, adverse events, mortality rate, and time to the first episode of hepatic encephalopathy from the time of randomization (days)."( Efficacy and Safety of Rifaximin in the Prevention of Recurrent Episodes of Hepatic Encephalopathy: A Systematic Review and Meta-analysis.
Abdelsattar, AT; El Mancy, IM; Elmoursi, A; Khalil, F; Mostafa, S; Ramadan, IG; Shabana, H; Zedan, HA, 2023
)
0.91
"The meta-analysis showed that in patients allocated to the rifaximin group, the incidence rate of hepatic encephalopathy was significantly lower when compared with those in the control group with no difference in both groups regarding adverse events and mortality rates."( Efficacy and Safety of Rifaximin in the Prevention of Recurrent Episodes of Hepatic Encephalopathy: A Systematic Review and Meta-analysis.
Abdelsattar, AT; El Mancy, IM; Elmoursi, A; Khalil, F; Mostafa, S; Ramadan, IG; Shabana, H; Zedan, HA, 2023
)
0.91

Pharmacokinetics

ExcerptReferenceRelevance
" No significant modification of the plasma pharmacokinetic profiles of isoniazid and acetylisoniazid was found."( A study of the effects of rifabutin on isoniazid pharmacokinetics and metabolism in healthy volunteers.
Breda, M; Carpentieri, M; Efthymiopoulos, C; Pianezzola, E; Rimoldi, R; Sassella, D; Strolin Benedetti, M, 1992
)
0.28
" The pharmacokinetic parameters of dexamethasone in rabbits were calculated by methods of residuals."( [Effects of rifamdin on pharmacokinetics of dexamethasone].
Jiang, LM, 1990
)
0.28
" Compared with a control group, the alteration of the half-life both of NA and R-SV was less marked in GS1 than in GS2."( Impaired plasma clearance of nicotinic acid and rifamycin-SV in Gilbert's syndrome: evidence of a functional heterogeneity.
Bronzino, P; Coltorti, M; Gentile, S; Marmo, R; Persico, M, 1985
)
0.27
" MAC organisms were inoculated into tubes containing the medium with or without the addition of test drugs at either 1/10 Cmax, Cmax or C0-8h (average concentrations during the first 8 h) in the blood."( [Anti-Mycobacterium avium complex activities of KRM-1648, clarithromycin and levofloxacin in 7HSF medium at peak or average blood concentrations after their oral administration of clinical dosages].
Akaki, T; Sato, K; Tomioka, H, 1997
)
0.3
"An open randomized cross-over study was conducted in 8 healthy male volunteers to study the pharmacokinetic pattern and the safety of a 300-mg single oral dose of a new 3-azinomethyl-rifamycin (USAN rifametane, SPA-S-565) compared with 300 mg of conventional rifampicin."( Phase I pharmacokinetic study of a new 3-azinomethyl-rifamycin (rifametane) as compared to rifampicin.
Ajay, S; Bruzzese, T; Cooverji, ND; Gogtay, N; Gokhale, P; Kshirsagar, NA; Potkar, C,
)
0.13
" The two antibiotics showed similar peak of serum concentrations, but rifametane showed a longer half-life and higher AUC values."( Pharmacokinetics and tissue distribution of rifametane, a new 3-azinomethyl-rifamycin derivative, in several animal species.
Ajay, S; Bonabello, A; Bruzzese, T; Cooverj, ND; Mozzi, G; Rimaroli, C, 2000
)
0.31
"We performed a pharmacokinetic substudy of patients in a trial of treatment with twice-weekly rifabutin and isoniazid."( Association between acquired rifamycin resistance and the pharmacokinetics of rifabutin and isoniazid among patients with HIV and tuberculosis.
Benator, D; Burman, W; Hodge, T; Jones, B; Khan, A; Peloquin, CA; Silva-Trigo, C; Vernon, A; Weiner, M; Zhao, Z, 2005
)
0.33
"A total of 102 (60%) of 169 patients in the treatment trial participated in the pharmacokinetic substudy, including 7 of 8 patients in whom tuberculosis treatment failure or relapse occurred in association with acquired rifamycin-resistant mycobacteria (hereafter, "ARR failure or relapse")."( Association between acquired rifamycin resistance and the pharmacokinetics of rifabutin and isoniazid among patients with HIV and tuberculosis.
Benator, D; Burman, W; Hodge, T; Jones, B; Khan, A; Peloquin, CA; Silva-Trigo, C; Vernon, A; Weiner, M; Zhao, Z, 2005
)
0.33
" Plasma concentration-time profiles and pharmacokinetic parameters were characterized for EE and 2 major metabolites of norgestimate, norgestrel (NG) and 17-deacetyl norgestimate (17-DNGM)."( Absence of effect of oral rifaximin on the pharmacokinetics of ethinyl estradiol/norgestimate in healthy females.
Bettenhausen, DK; Connolly, M; Forbes, WP; Pentikis, H; Trapnell, CB, 2007
)
0.34
" No differences in pharmacokinetic parameters were observed for EE, NG, or 17-DNGM when a single dose of the OC was administered alone or with rifaximin."( Absence of effect of oral rifaximin on the pharmacokinetics of ethinyl estradiol/norgestimate in healthy females.
Bettenhausen, DK; Connolly, M; Forbes, WP; Pentikis, H; Trapnell, CB, 2007
)
0.34
" Another striking finding was the large reduction of the pharmacokinetic intersubject variability after rifalazil administration with food."( Effect of food on the pharmacokinetics of rifalazil, a novel antibacterial, in healthy male volunteers.
Cabana, B; Chen, YX; Kivel, N; Michaelis, A, 2007
)
0.34
" The geometric mean ratios for the difference between EE alone and following rifalazil for EE Cmax, AUC(0-24) and Cmin were 105."( Lack of effect of rifalazil on ethinyl estradiol pharmacokinetics in healthy postmenopausal women.
Cabana, B; Chen, YX; Gilman, S; Kivel, N; Michaelis, A; Pieniaszek, H, 2007
)
0.34
" Serial plasma samples were collected for pharmacokinetic analyses."( The effect of multiple-dose, oral rifaximin on the pharmacokinetics of intravenous and oral midazolam in healthy volunteers.
Bettenhausen, DK; Connolly, M; Forbes, WP; Pentikis, HS; Trapnell, CB, 2007
)
0.34
"The pharmacokinetic parameters of single-dose intravenous or oral midazolam were determined alone and after coadministration of rifaximin for 3 and 7 days."( The effect of multiple-dose, oral rifaximin on the pharmacokinetics of intravenous and oral midazolam in healthy volunteers.
Bettenhausen, DK; Connolly, M; Forbes, WP; Pentikis, HS; Trapnell, CB, 2007
)
0.34
" Further, pharmacokinetic, pharmacodynamic and in vivo studies are warranted to determine its ultimate place in antibacterial therapy."( In vitro pharmacodynamics of novel rifamycin ABI-0043 against Staphylococcus aureus.
Forrest, A; Kelchlin, PA; Smith, PF; Tsuji, BT; Yang, JC, 2008
)
0.35
"This review will introduce pharmacokinetic parameters for key anti-TB drugs, as well as the indications and limitations of measuring these parameters in clinical practice."( Understanding pharmacokinetics to improve tuberculosis treatment outcome.
Heysell, SK; Reynolds, J, 2014
)
0.4
"Individual pharmacokinetic variability is commonplace, underappreciated and difficult to predict without therapeutic drug monitoring (TDM)."( Understanding pharmacokinetics to improve tuberculosis treatment outcome.
Heysell, SK; Reynolds, J, 2014
)
0.4
" To help inform such an optimization, a physiologically based pharmacokinetic (PBPK) model was developed to predict time course, tissue-specific concentrations of RPT and its active metabolite, 25-desacetyl rifapentine (dRPT), in humans after specified administration schedules for RPT."( Physiologically Based Pharmacokinetic Model of Rifapentine and 25-Desacetyl Rifapentine Disposition in Humans.
Eppers, GJ; Reisfeld, B; Zurlinden, TJ, 2016
)
0.43
" These unique pharmacokinetic properties limit its systemic effects and can correct gut microflora imbalances."( Pharmacokinetic drug evaluation of rifaximin for treatment of diarrhea-predominant irritable bowel syndrome.
Bruzzese, E; Guarino, A; Pesce, M; Sarnelli, G, 2018
)
0.48

Compound-Compound Interactions

ExcerptReferenceRelevance
" However, pronounced antibacterial effects were seen when ethambutol was tested in combination with ciprofloxacin, rifampicin or rifabutin, which corresponded to significantly decreased resistance to these drugs in combination."( Susceptibility of Mycobacterium kansasii to ethambutol and its combination with rifamycins, ciprofloxacin and isoniazid.
Hjelm, U; Hoffner, SE; Kaustová, J; Kubín, M, 1992
)
0.51
"The inhibitory and bactericidal, synergistic, and antagonistic activities of rifabutin combined with ciprofloxacin, ethambutol, clofazimine, cefazolin, and amikacin in dual and triple combinations against various human and animal isolates of Mycobacterium paratuberculosis were determined."( Antimicrobial activity of rifabutin in combination with two and three other antimicrobial agents against strains of Mycobacterium paratuberculosis.
Chiodini, RJ, 1991
)
0.28
"The in vivo activity of amikacin, used alone or in combination with rifabutin or clofazimine or both, was assessed in the treatment of early and established Mycobacterium avium complex infections in beige mice."( In vivo activity of amikacin alone or in combination with clofazimine or rifabutin or both against acute experimental Mycobacterium avium complex infections in beige mice.
Gangadharam, PR; Iseman, MD; Kesavalu, L; Perumal, VK; Podapati, NR, 1988
)
0.27
"The bactericidal interactions in vitro of two antibiotics active at the cell wall (teicoplanin and vancomycin) or two inhibitors of DNA gyrase (coumermycin and ciprofloxacin) combined with two inhibitors of protein synthesis (rifampicin and LM 427) were assessed against five Staphylococcus aureus strains."( Comparative in-vitro activities of teicoplanin, vancomycin, coumermycin and ciprofloxacin, alone and in combination with rifampicin or LM 427, against Staphylococcus aureus.
Joly, P; Van der Auwera, P, 1987
)
0.27
" If chemotherapy is initiated 3 wk after challenge (established infections), the activity of this double drug combination is less effective."( Activity of rifabutin alone or in combination with clofazimine or ethambutol or both against acute and chronic experimental Mycobacterium intracellulare infections.
Farhi, DC; Gangadharam, PR; Iseman, MD; Jairam, BT; Nguyen, AK; Perumal, VK; Rao, PN, 1987
)
0.27
" capsulatum, when used in combination with amphotericin B or alone, was the same as that reported for the inhibition of the reverse transcriptase of ribonucleic acid tumor viruses."( Effects of rifamycin derivatives, alone and in combination with amphotericin B, against Histoplasma capsulatum.
Cheung, SS; Kobayashi, GS; Medoff, G; Schlessinger, D, 1974
)
0.25
" We investigated the activity of three doses of the semisynthetic benzoxazinorifamycin KRM 1648, alone or in combination with ethambutol or clarithromycin, in beige mice challenged with the MAC strain 101."( Activity of KRM 1648 alone or in combination with ethambutol or clarithromycin against Mycobacterium avium in beige mouse model of disseminated infection.
Bermudez, LE; Inderlied, CB; Kolonoski, P; Young, LS, 1994
)
0.29
"In this study, the in vitro and in vivo anti-Mycobacterium leprae activity of the newly developed benzoxazinorifamycin, KRM-1648, in combination with clofazimine (CFZ) or dapsone (DDS) was evaluated."( Therapeutic efficacy of benzoxazinorifamycin, KRM-1648, in combination with other antimicrobials against Mycobacterium leprae infection induced in nude mice.
Dekio, S; Saito, H; Sato, K; Tomioka, H, 1994
)
0.29
"A study was performed on the therapeutic efficacy of KRM-1648 combined with LC9018 in beige mice infected with Mycobacterium intracellulare."( [Therapeutic efficacy of a benzoxazinorifamycin, KRM-1648, combined with a immunopotentiator, LC9018, in Mycobacterium intracellulare infection induced in beige mice].
Hidaka, T; Saito, H; Sato, K; Tomioka, H, 1993
)
0.29
" malmoense isolates to a number of antibacterial drugs as well as their possible synergistic interactions when each of them was combined with ethambutol."( Susceptibility of Mycobacterium malmoense to antibacterial drugs and drug combinations.
Hjelm, U; Hoffner, SE; Källenius, G, 1993
)
0.29
" When combined with one of the three rifamycin analogs, synergism was obtained with KRM-1648 and rifabutin but not with rifampin."( In vitro activity of levofloxacin, singly and in combination with rifamycin analogs, against Mycobacterium leprae.
Dhople, AM; Ibanez, MA, 1995
)
0.29
"The activity of KRM-1648, alone and in combination with isoniazid, was compared with those of isoniazid, rifampin, and the combination of rifampin plus isoniazid in a murine model of tuberculosis."( Activity of KRM-1648 in combination with isoniazid against Mycobacterium tuberculosis in a murine model.
Cynamon, MH; Klemens, SP, 1996
)
0.29
"The in vivo activities of KRM-1648 alone or in combination with both ethambutol (EB) and kanamycin (KM) or clarithromycin (CAM) were tested against Mycobacterium intracellulare infections in beige mice."( Activity of KRM-1648 alone or in combination with both ethambutol and kanamycin or clarithromycin against Mycobacterium intracellulare infections in beige mice.
Amitani, R; Kuze, F; Murayama, T; Suzuki, K; Tanaka, E; Yamamoto, T, 1996
)
0.29
"In the present study, we evaluated the in vivo anti-Mycobacterium leprae activities of KRM-1648 (KRM) given at long intervals in combination with ofloxacin (OFLX), clofazimine (CFZ), and dapsone (DDS)."( Studies on therapeutic activity of benzoxazinorifamycin KRM-1648 in combination with other antimicrobial agents and biological response modifiers interferon-gamma and granulocyte-macrophage colony-stimulating factor against M. leprae infection in athymic
Maw, WW; Saito, H; Sato, K; Tomioka, H, 1997
)
0.3
"The activity of KRM 1648 (KRM), a new benzoxazinorifamycin, and rifabutin (RBT), alone or in combination with clarithromycin (CLA), was evaluated against Mycobacterium avium complex (MAC) that multiplied in human alveolar macrophages (AM)."( Activity of KRM 1648 or rifabutin alone or in combination with clarithromycin against Mycobacterium avium complex in human alveolar macrophages.
Amitani, R; Hashimoto, T; Kuze, F; Matsumoto, H; Suzuki, K; Tanaka, E; Tsuyuguchi, K; Yamamoto, T, 1997
)
0.3
"According to this human alveolar macrophage model of MAC infection, KRM and RBT in combination with CLA was found to be a promising candidate against human pulmonary MAC infection, and deserves clinical evaluation."( Activity of KRM 1648 or rifabutin alone or in combination with clarithromycin against Mycobacterium avium complex in human alveolar macrophages.
Amitani, R; Hashimoto, T; Kuze, F; Matsumoto, H; Suzuki, K; Tanaka, E; Tsuyuguchi, K; Yamamoto, T, 1997
)
0.3
"The effects of half-sized secretory leukocyte protease inhibitor or diclofenac sodium administered alone or in combination with the benzoxazinorifamycin KRM-1648 on the therapeutic efficacy of KRM-1648 against Mycobacterium avium complex (MAC) in mice were studied."( Therapeutic effects of benzoxazinorifamycin KRM-1648 administered alone or in combination with a half-sized secretory leukocyte protease inhibitor or the nonsteroidal anti-inflammatory drug diclofenac sodium against Mycobacterium avium complex infection i
Kawahara, S; Kawauchi, H; Sano, C; Sato, K; Shimizu, T; Tomioka, H, 1999
)
0.3
"Rifalazil (formerly known as KRM-1648) in combination with isoniazid has been found to be more active than rifampin/isoniazid."( Durable cure for tuberculosis: rifalazil in combination with isoniazid in a murine model of Mycobacterium tuberculosis infection.
Cynamon, MH; DeStefano, MS; Shoen, CM, 2000
)
0.31
"The antimicrobial effect of a benzoxazinorifamycin, KRM-1648, either alone or in combination with ofloxacin, was evaluated in vitro against two type strains and six clinical isolates of Mycobacterium ulcerans."( In vitro activity of KRM-1648, either singly or in combination with ofloxacin, against Mycobacterium ulcerans.
Dhople, AM, 2001
)
0.31
" Similar to ofloxacin and levofloxacin, sitafloxacin also exhibited synergistic activity when combined with either rifabutin or KRM-1648, but not with rifampin."( In-vitro activity of sitafloxacin (DU-6859a), either singly or in combination with rifampin analogs, against Mycobacterium leprae.
Dhople, AM; Namba, K, 2003
)
0.32
" To address the high-frequency resistance seen with rifamycins, we assessed the ability of rifalazil, alone and in combination with vancomycin, to both kill cells and to suppress the appearance of resistant mutants in log and stationary phase Staphylococcus aureus cultures, using high cell densities in an in vitro kill curve model."( In vitro time-kill activities of rifalazil, alone and in combination with vancomycin, against logarithmic and stationary cultures of Staphylococcus aureus.
Farquhar, R; Murphy, CK; Osburne, MS; Rothstein, DM, 2006
)
0.58
" To explore strategies to overcome resistance development, we studied the effects of rifalazil in combination with several different antibiotics in an in vitro time-kill model, against both log phase and stationary phase Staphylococcus aureus cells."( Enhanced activity of rifalazil in combination with levofloxacin, linezolid, or mupirocin against Staphylococcus aureus in vitro.
Murphy, CK; Osburne, MS; Rothstein, DM, 2006
)
0.33
"To support drug development, the drug-drug interaction potential (DDI) of an investigational drug (AZX) was assessed against the probe estradiol 17β-glucuronide as well as against simvastatin acid, atorvastatin, pravastatin, pitavastatin, fluvastatin, rosuvastatin and estrone 3-sulfate."( Prediction of the in vivo OATP1B1-mediated drug-drug interaction potential of an investigational drug against a range of statins.
Butters, CJ; Elsby, R; Sharma, P; Smith, V; Surry, D, 2012
)
0.38
" However, concomitant treatment of both conditions is complex, mainly due to significant drug-drug interactions between TB and HIV drugs."( Treatment optimization in patients co-infected with HIV and Mycobacterium tuberculosis infections: focus on drug-drug interactions with rifamycins.
Carvalho, AC; Matteelli, A; Regazzi, M; Villani, P, 2014
)
0.61
" Rifamycin antibiotics are a key component of TB therapy and a common source of drug-drug interactions (DDIs) due to induction of drug metabolizing enzymes (DMEs)."( Hepatocytic transcriptional signatures predict comparative drug interaction potential of rifamycin antibiotics.
Dyavar, SR; Fletcher, CV; Mykris, TM; Podany, AT; Scarsi, KK; Winchester, LC, 2020
)
0.56
" Drug-drug interactions (DDI) caused by rifampicin (RIF) are a major issue."( Model-Based Comparative Analysis of Rifampicin and Rifabutin Drug-Drug Interaction Profile.
Bleyzac, N; Bourguignon, L; France, M; Garreau, R; Goutelle, S; Tod, M; Tuloup, V, 2021
)
0.62
" The 29 studies identified examined warfarin (n = 17), direct oral anticoagulants (DOACs) (n = 8), and antiplatelet agents (n = 4) combined with rifampin (n = 28) or rifabutin (n = 1)."( Systematic review of drug-drug interactions between rifamycins and anticoagulant and antiplatelet agents and considerations for management.
Canonica, T; Keh, C; Louie, J; MacDougall, C; P Phan, BA, 2022
)
0.97

Bioavailability

ExcerptReferenceRelevance
"The relative bioavailability of the capsule dose form (150 mg) and the effect of high-fat food were assessed in a randomized, three-way crossover trial of rifabutin in 12 healthy male volunteers."( Rifabutin absorption in humans: relative bioavailability and food effect.
Bianchine, JR; Lewis, RC; Narang, PK, 1992
)
0.28
"25 mg/kg RPE, suggesting that FCE would be a better drug than RPE if its bioavailability could be improved, and that the levels following 16 mg/kg RPE were similar to those found in man after 8 mg/kg RPE taken with a fat-rich meal, suggesting good prospects for effective once-fortnightly human treatment."( Activity of two long-acting rifamycins, rifapentine and FCE 22807, in experimental murine tuberculosis.
Dhillon, J; Dickinson, JM; Guy, JA; Mitchison, DA; Ng, TK, 1992
)
0.58
" Serial plasma samples taken under controlled conditions suggested that a decreased rate of absorption was responsible for low one-hour concentrations in one of the subjects."( Ciprofloxacin in patients with mycobacterial infections: experience in 15 patients.
Kahana, LM; Spino, M, 1991
)
0.28
" Application of this method to a bioavailability assessment is presented."( A sensitive method for quantitation of rifabutin and its desacetyl metabolite in human biological fluids by high-performance liquid chromatography (HPLC).
Hatfield, NZ; Lewis, RC; Narang, PK, 1991
)
0.28
" The ig absolute bioavailability ranged from 69-84%."( [Disposition of 3-(N-piperidinomethylarino)methyl-rifamycin SV (FCE 22250) in rats].
Li, D; Liu, L; Sun, SL; Wang, ZY, 1991
)
0.28
" Oral bioavailability was 12 to 20%."( Pharmacokinetics of rifabutin.
Bhatia, G; Blaschke, TF; Harkonen, S; Hsieh, M; Merigan, TC; Pauloin, D; Skinner, MH; Torseth, J, 1989
)
0.28
" These compounds are zwitterionic in nature and are poorly absorbed through the gastroenteric tract but maintain the ability to cross the bacterial cell wall."( 4-Deoxypyrido[1',2':1,2]imidazo[5,4-c]rifamycin SV derivatives. A new series of semisynthetic rifamycins with high antibacterial activity and low gastroenteric absorption.
Brufani, M; Cellai, L; Marchi, E; Mascellani, G; Montecchi, L; Venturini, AP, 1985
)
0.49
" The bioavailability of the active, orally administered rifampicin decreased from 93% after the first single oral dose to 68% after 3 weeks of oral and intravenous rifampicin therapy."( Pharmacokinetics of oral and intravenous rifampicin during chronic administration.
Eichelbaum, M; Jensen, JC; Loos, U; Mikus, G; Musch, E; Schwabe, HK, 1985
)
0.27
" While compounds 1-5 had poor antibacterial activity in vitro, compounds 6-11 were found to be highly active in vitro but poorly absorbed in vivo."( The synthesis of 4-deoxypyrido[1',2'-1,2]imidazo[5,4-c]rifamycin SV derivatives.
Brufani, M; Cellai, L; Marchi, E; Segre, A, 1984
)
0.27
" It is well absorbed at the level of duodenum, achieving a repeated entero-hepatic circuit that provides a prolonged efficient concentration of Reprimun in blood serum."( Reprimun--an antibiotic with large spectrum and immunomodulatory properties.
Păunescu, E,
)
0.13
" High concentrations of rifaximin were often used to reflect topically achieved levels since this compound is poorly absorbed by oral route."( Antimicrobial activity and spectrum of rifaximin, a new topical rifamycin derivative.
Eliopoulos, GM; Gerlach, EH; Hoban, DJ; Hoover, WW; Jones, RN; Pfaller, MA, 1993
)
0.29
" A poorly absorbed drug if effective in treating bacterial diarrhea has pharmacologic and safety advantages over the existing drugs."( Rifaximin: a nonabsorbed antimicrobial in the therapy of travelers' diarrhea.
de la Cabada, FJ; DuPont, HL; DuPont, MW; Ericsson, CD; Jiang, ZD; Mathewson, JJ; Mosavi, A; Palazzini, E,
)
0.13
"Rifampicin (RIF) hydrolyzes in acidic medium to form insoluble and poorly absorbed 3-Formyl rifamycin SV (3-FRSV)."( Stability of rifampicin in dissolution medium in presence of isoniazid.
Kotecha, JS; Rathod, IS; Savale, SS; Shah, PB; Shah, SA; Shishoo, CJ, 1999
)
0.3
" The data indicate that these inhibitors can be used to determine the in vivo relevance of Oatp1 and Oatp2 for the overall bioavailability and disposition of drugs and other Oatp1/2 substrates."( Rifamycin SV and rifampicin exhibit differential inhibition of the hepatic rat organic anion transporting polypeptides, Oatp1 and Oatp2.
Cattori, V; Fattinger, K; Hagenbuch, B; Meier, PJ; Stieger, B, 2000
)
0.31
"Rifaximin is a poorly absorbed rifamycin derivative under investigation for treatment of infectious diarrhea."( Rifaximin versus ciprofloxacin for the treatment of traveler's diarrhea: a randomized, double-blind clinical trial.
Adachi, JA; Ashley, D; DuPont, HL; DuPont, MW; Ericsson, CD; Jiang, ZD; Martinez-Sandoval, F; Mathewson, JJ; Palazzini, E; Riopel, LM, 2001
)
0.31
" The study provides information on the value of the poorly absorbed drug rifaximin in therapy of travelers' diarrhea."( Enteroaggregative Escherichia coli diarrhea in travelers: response to rifaximin therapy.
DuPont, HL; Ericsson, CD; Infante, RM; Jiang, ZD; Ke, S; Riopel, L; Sack, DA; Steffen, R, 2004
)
0.32
"Rifaximin is a poorly absorbed rifamycin antimicrobial drug with in vitro activity against Gram-positive, Gram-negative and anaerobic bacteria."( Rifaximin--a novel antimicrobial for enteric infections.
DuPont, HL; Huang, DB, 2005
)
0.33
"Rifaximin is a rifamycin analogue with a broad spectrum of activity similar to that of rifampin; however, because it is poorly absorbed in the gastrointestinal tract, the focus of its development has been on intestinal infections and diseases."( Rifaximin: a nonabsorbed oral antibiotic.
Baker, DE, 2005
)
0.33
" Being virtually nonabsorbed, its bioavailability within the GI tract is rather high with intraluminal and fecal drug concentrations that largely exceed the minimal inhibitory concentration values observed in vitro against a wide range of pathogenic organisms."( Rifaximin, a poorly absorbed antibiotic: pharmacology and clinical potential.
Pelosini, I; Scarpignato, C, 2005
)
0.33
"Rifaximin is a poorly absorbed semisynthetic rifamycin derivative with a broad spectrum of antibacterial activity including Gram-positive and Gram-negative bacteria, both aerobes and anaerobes."( Rifaximin, a peculiar rifamycin derivative: established and potential clinical use outside the gastrointestinal tract.
Pelosini, I; Scarpignato, C, 2005
)
0.33
" When therapy with poorly absorbed rifaximin was shown to be as effective as therapy with systemically absorbed drugs in shortening the duration of traveler's diarrhea, without the development of resistant coliform flora, the use of rifaximin for the prevention of traveler's diarrhea was studied."( Antibacterial chemoprophylaxis in the prevention of traveler's diarrhea: evaluation of poorly absorbed oral rifaximin.
de la Cabada, FJ; DuPont, HL; DuPont, MW; Ericsson, CD; Jiang, ZD; Ke, S; Martinez-Sandoval, F; Okhuysen, PC, 2005
)
0.33
" Recent evidence suggests a potential role for bacterial overgrowth in some patients with IBS; the study discussed herein provides further support for this concept by describing an amelioration of bloating and flatulence following a short course of the poorly absorbed antibiotic, rifaximin."( Germs, gas and the gut; the evolving role of the enteric flora in IBS.
Quigley, EM, 2006
)
0.33
" Being virtually non-absorbed, its bioavailability within the GI tract is rather high with intraluminal and fecal drug concentrations that largely exceed the minimum inhibitory concentration values observed in vitro against a wide range of pathogenic organisms."( Experimental and clinical pharmacology of rifaximin, a gastrointestinal selective antibiotic.
Pelosini, I; Scarpignato, C, 2006
)
0.33
" With the advent of poorly absorbed (<0."( Current and future developments in travelers' diarrhea therapy.
DuPont, HL; Koo, HL, 2006
)
0.33
" Long term administration of the poorly absorbed antibiotic Rifaximin is safe and well tolerated by the patients, confirming the usefulness of this therapeutic strategy in the overall management of diverticular disease."( Efficacy of long term cyclic administration of the poorly absorbed antibiotic Rifaximin in symptomatic, uncomplicated colonic diverticular disease.
Brandimarte, G; Colecchia, A; Festi, D; Mazzella, G; Pasqui, F; Pistoia, F; Roda, E; Vestito, A, 2007
)
0.34
" In addition, the 90% CI for the bioavailability contrasts (OC alone vs OC with rifaximin) for the maximum plasma concentration, area under the plasma concentration-time curve from zero to the last measurable plasma concentration or to infinity for EE, NG, and 17-DNGM all ranged from 86-118%."( Absence of effect of oral rifaximin on the pharmacokinetics of ethinyl estradiol/norgestimate in healthy females.
Bettenhausen, DK; Connolly, M; Forbes, WP; Pentikis, H; Trapnell, CB, 2007
)
0.34
"Rifaximin, a poorly absorbed rifamycin derivative, exhibited time-dependent bactericidal activity and at concentrations as low as 1/32 of the minimum inhibitory concentration (MIC) caused morphological alterations in both susceptible and resistant bacterial strains."( Effects of rifaximin on bacterial virulence mechanisms at supra- and sub-inhibitory concentrations.
Debbia, EA; Maioli, E; Marchese, A; Roveta, S, 2008
)
0.35
"Rifaximin, a poorly absorbed rifamycin derivative, is a promising alternative for the treatment of Clostridium difficile infections."( Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
Galang, MA; Gerding, DN; Hecht, DW; Johnson, S; O'Connor, JR; Sambol, SP; Vedantam, G, 2008
)
0.35
" bioavailability in preclinical species and humans."( Involvement of intestinal uptake transporters in the absorption of azithromycin and clarithromycin in the rat.
Davis, CB; Dawson, PA; Garver, E; Han, C; Hugger, ED; Rao, A; Shearn, SP, 2008
)
0.35
"Rifaximin is a poorly absorbed semisynthetic antibiotic derivative of rifampin licensed for use in the treatment of traveler's diarrhea."( Pretreatment of epithelial cells with rifaximin alters bacterial attachment and internalization profiles.
Brown, EL; Dupont, HL; Jiang, ZD; Xu, Y; Xue, Q, 2010
)
0.36
" Since it is virtually unabsorbed after oral administration, its bioavailability within the GI tract is high, with intraluminal and fecal drug concentrations largely exceeding the minimum inhibitory concentration values observed in vitro against a broad spectrum of bacteria, including Gram-positive and Gram-negative bacteria, both aerobes and anaerobes."( Rifaximin in the management of colonic diverticular disease.
Latella, G; Scarpignato, C, 2009
)
0.35
" The purpose of the present study was to evaluate the antimicrobial effect and bioavailability of rifaximin in aqueous solution in the presence and absence of physiologic concentrations of bile acids."( Bile acids improve the antimicrobial effect of rifaximin.
Ajami, N; Darkoh, C; Dial, EJ; DuPont, HL; Jiang, ZD; Lichtenberger, LM, 2010
)
0.36
"Rifaximin is a poorly absorbed non-systemic antimicrobial agent used in various gastrointestinal disorders."( Rifaximin intake leads to emergence of rifampin-resistant staphylococci.
Hoenigl, M; Krause, R; Leitner, E; Rohn, A; Salzer, HJ; Valentin, T; Zollner-Schwetz, I, 2011
)
0.37
"Rifamycin SV is a broad-spectrum, poorly absorbed antimicrobial agent that, when coupled with MMX technology, is being targeted for the oral treatment of traveler's diarrhea (TD) and Clostridium difficile-associated disease (CDAD)."( In vitro activity and single-step mutational analysis of rifamycin SV tested against enteropathogens associated with traveler's diarrhea and Clostridium difficile.
Biedenbach, DJ; Bozzella, R; Celasco, G; Farrell, DJ; Jones, RN; Moro, L; Putnam, SD, 2011
)
0.37
"Rifaximin is a rifampicin derivative, poorly absorbed by the gastro-intestinal tract."( Rifaximin disc diffusion test for in vitro susceptibility testing of Clostridium difficile.
Allerberger, F; Blaschitz, M; Fiedler, A; Huhulescu, S; Indra, A; Pecavar, V; Sagel, U; Wewalka, G, 2011
)
0.37
" Several randomised trials verified efficacy of a poorly absorbed antibiotic, such as rifaximin-α (rifaximin), in soothing symptoms and preventing diverticulitis."( Meta-analysis: long-term therapy with rifaximin in the management of uncomplicated diverticular disease.
Bianchi, M; Ciaco, A; De Pascalis, B; Dezi, A; Festa, V; Koch, M; Luchetti, R; Mangone, M; Moretti, A; Papi, C; Tornatore, V, 2011
)
0.37
" In this patient population it is plausible that rifaximin bioavailability increases enough to induce CYP3A4, leading to clinically significant reductions in the bioavailability of CYP3A4 substrates, including R-warfarin."( Probable interaction between warfarin and rifaximin in a patient treated for small intestine bacterial overgrowth.
Hartig, C; Hoffman, JT; Lang, M; Sonbol, E, 2011
)
0.37
" Here, we discuss the results of two identically designed, double-blind, placebo-controlled trials (TARGET 1 and TARGET 2) of a poorly absorbed antibiotic, rifaximin, in patients with IBS."( The role of rifaximin therapy in patients with irritable bowel syndrome without constipation.
Rao, SS; Schey, R, 2011
)
0.37
" Rifaximin is a poorly absorbed oral antimicrobial agent increasingly used in the treatment of inflammatory bowel diseases that has been demonstrated to act as a gut-specific ligand for the human nuclear receptor pregnane-X receptor (PXR)."( Inhibition of NF-κB by a PXR-dependent pathway mediates counter-regulatory activities of rifaximin on innate immunity in intestinal epithelial cells.
Baldelli, F; Barbanti, M; Claudio, D; Distrutti, E; Fiorucci, S; Mencarelli, A; Palladino, G; Renga, B; Ricci, P, 2011
)
0.37
" The latter might be one of the reasons for the auto-induction of RFB metabolism and the consequent lower bioavailability of the drug on repeated administration."( In vitro reaction phenotyping studies on rifamycins to explain the auto-induction of rifabutin metabolism.
Prasad, B; Singh, S, 2012
)
0.64
" Rifampicin is also an inducer of the adenosine triphosphate (ATP) binding cassette transporter P-glycoprotein, which may also lead to decreased bioavailability of concomitantly administered antiretrovirals."( Treatment optimization in patients co-infected with HIV and Mycobacterium tuberculosis infections: focus on drug-drug interactions with rifamycins.
Carvalho, AC; Matteelli, A; Regazzi, M; Villani, P, 2014
)
0.61
" The branded rifaximin formulation contains the polymorph rifaximin-α, whose systemic bioavailability is very limited."( Is generic rifaximin still a poorly absorbed antibiotic? A comparison of branded and generic formulations in healthy volunteers.
Blandizzi, C; Marzo, A; Scarpignato, C; Viscomi, GC, 2014
)
0.4
" Aim of this study was to test the efficacy of liquid levodopa with higher bioavailability in patients with SIBO."( Liquid melevodopa versus standard levodopa in patients with Parkinson disease and small intestinal bacterial overgrowth.
Bentivoglio, AR; Bove, F; Fasano, A; Fortuna, S; Gabrielli, M; Gasbarrini, A; Marconi, S; Ragazzoni, E; Tortora, A; Zocco, MA,
)
0.13
" The current marketed rifaximin formulation contains polymorph alpha, the systemic bioavailability of which is very limited."( Impact of crystal polymorphism on the systemic bioavailability of rifaximin, an antibiotic acting locally in the gastrointestinal tract, in healthy volunteers.
Blandizzi, C; Scarpignato, C; Viscomi, GC, 2015
)
0.42
"25) range, indicating higher systemic bioavailability of the amorphous rifaximin."( Impact of crystal polymorphism on the systemic bioavailability of rifaximin, an antibiotic acting locally in the gastrointestinal tract, in healthy volunteers.
Blandizzi, C; Scarpignato, C; Viscomi, GC, 2015
)
0.42
" In this regard, care must be taken when using - as a medicinal product - a formulation containing even small amounts of amorphous form, which may alter the peculiar pharmacologic properties of this poorly absorbed antibiotic."( Impact of crystal polymorphism on the systemic bioavailability of rifaximin, an antibiotic acting locally in the gastrointestinal tract, in healthy volunteers.
Blandizzi, C; Scarpignato, C; Viscomi, GC, 2015
)
0.42
" To study the influence of the microbiota on the bioavailability of naringenin, a group of animals received the antibiotic rifaximin (50 mg/kg per d) for 5 d, and naringenin permeability was determined in the colon."( High gastrointestinal permeability and local metabolism of naringenin: influence of antibiotic treatment on absorption and metabolism.
Escribano-Ferrer, E; Lamuela-Raventos, RM; Martínez-Huélamo, M; Orrego-Lagarón, N; Vallverdú-Queralt, A, 2015
)
0.42
"Rifaximin is a poorly absorbed rifamycin drug with unique pharmacokinetic properties: bile solubility making it highly active against pathogenic and non-pathogenic bacterial flora in the bile-rich small bowel and low water solubility making it active only against highly susceptible bacteria, primarily anaerobes, in the aqueous colon."( Rifaximin: An Antibiotic with Important Biologic Effects.
DuPont, HL, 2015
)
0.42
" Rifaximin is a poorly absorbed oral antibiotic proposed to act on the gut microenvironment, used in the treatment of travelers' diarrhea and hepatic encephalopathy."( Rifaximin for the treatment of diarrhea-predominant irritable bowel syndrome.
Ford, AC; Kane, JS, 2016
)
0.43
" Because gut bacterial translocation is their main pathogenic mechanism, prevention of infections is mostly based on the use of orally administered poorly absorbed antibiotics such as norfloxacin (selective intestinal decontamination)."( Novel prevention strategies for bacterial infections in cirrhosis.
Garcia-Tsao, G; Yan, K, 2016
)
0.43
" Rifaximin, a poorly absorbed antibiotic that targets gut flora, significantly improved symptoms of HE."( Development of an experimental rat model of hyperammonemic encephalopathy and evaluation of the effects of rifaximin.
Fukui, N; Isobe, M; Okada, M; Saito, T; Suzuki, H; Tamaoki, S, 2016
)
0.43
" It is poorly absorbed and thus has a highly favorable safety profile."( Use of rifaximin in gastrointestinal and liver diseases.
Abou Mrad, R; Sharara, AI; Shayto, RH, 2016
)
0.43
" The poorly absorbed antibiotic rifaximin seem to be different from the other antibiotics, because it exerts non-traditional effects additional to the bactericidal/bacteriostatic activity on the gut microbiota."( Eubiotic properties of rifaximin: Disruption of the traditional concepts in gut microbiota modulation.
D'Aversa, F; Gasbarrini, A; Pompili, M; Ponziani, FR; Zocco, MA, 2017
)
0.46
"Rifaximin, a poorly absorbed antibiotics, has gut-specific therapeutic effects."( Emergence of rifampin-resistant staphylococci after rifaximin administration in cirrhotic patients.
Chang, JY; Joo, YH; Jung, HK; Jung, SA; Kim, SE; Kim, TH; Lee, J; Lee, KE; Lee, KH; Moon, CM; Ryu, MS; Shim, KN; Woo, SY, 2017
)
0.46
" Thus, a study was designed to compare this poorly absorbed antibiotic with the systemic agent ciprofloxacin."( Rifamycin SV-MMX® for treatment of travellers' diarrhea: equally effective as ciprofloxacin and not associated with the acquisition of multi-drug resistant bacteria.
Araujo, P; DuPont, HL; Gracias Garcia, ML; Greinwald, R; Jiang, ZD; Nacak, T; Steffen, R; Stiess, M, 2018
)
0.48
"The novel multi-matrix formulation of the broad-spectrum, poorly absorbed antibiotic Rifamycin SV was found non-inferior to the systemic antibiotic ciprofloxacin in the oral treatment of non-dysenteric TD with the advantage of a lower risk of ESBL-E."( Rifamycin SV-MMX® for treatment of travellers' diarrhea: equally effective as ciprofloxacin and not associated with the acquisition of multi-drug resistant bacteria.
Araujo, P; DuPont, HL; Gracias Garcia, ML; Greinwald, R; Jiang, ZD; Nacak, T; Steffen, R; Stiess, M, 2018
)
0.48

Dosage Studied

ExcerptRelevanceReference
" Basing their comment on the published literature, they analyze the properties, pharmacology, toxicity, and side-effects of each medication, and define their dosage and modes of administration."( [Principles underlying the use of antituberculosis medication in children (author's transl)].
Besson-Leaud, M; Ollivier, A,
)
0.13
" A dose-response experiment was performed with clarithromycin at 50, 100, 200, or 300 mg/kg of body weight administered daily by gavage to mice infected with approximately 10(7) viable MAC."( Activity of clarithromycin against Mycobacterium avium complex infection in beige mice.
Cynamon, MH; DeStefano, MS; Klemens, SP, 1992
)
0.28
" Oral administration of rifampin at three times the intra-articular dosage was devoid of any therapeutic activity."( Clinical improvement in ankylosing spondylitis with rifamycin SV infiltrations of peripheral joints.
Caruso, I; Cazzola, M; Santandrea, S, 1992
)
0.28
" The weekly dosage of Rifamycin SV was 500 mg; the average duration of treatment was 6 weeks."( The treatment of idiopathic and secondary hydrarthrosis of the knee by intra-articular Rifamycin SV.
Calciolari, CA; Cimino, V; Sarzi Puttini, P; Setti, G; Zanini, A,
)
0.13
" A drug is likely to be particularly effective in widely spaced intermittent dosage if it has a long half-life and high bactericidal activity."( In vitro activities against mycobacteria of two long-acting rifamycins, FCE22807 and CGP40/469A (SPA-S-565).
Dickinson, JM; Mitchison, DA, 1990
)
0.52
" Six or more patients were studied at each of four different oral dosage levels: 300, 600, 900, and 1,200 mg/day."( Pharmacokinetics of rifabutin.
Bhatia, G; Blaschke, TF; Harkonen, S; Hsieh, M; Merigan, TC; Pauloin, D; Skinner, MH; Torseth, J, 1989
)
0.28
" In the same subjects, rifabutin in the proposed therapeutic dosage (300 mg daily) for 7 days also enhanced the metabolic elimination of antipyrine, with preferential stimulation of the demethylation pathway, and increased the excretion of 6-beta-hydroxycortisol, but the magnitude of the effects was significantly less than after rifampicin."( Comparative effects of rifabutin and rifampicin on hepatic microsomal enzyme activity in normal subjects.
Frigo, GM; Grimaldi, R; Mönig, H; Ohnhaus, EE; Perucca, E; Sardi, A, 1988
)
0.27
" Therapeutic activities of R-76-1 versus RMP and DL 473 versus RMP were compared, respectively, in the experimental infection of mice with Mycobacterium lepraemurium by different treatment schedules (immediate and delayed) and dosage regimens."( Antimycobacterial activities of two newer ansamycins, R-76-1 and DL 473.
Chen, JK; Hou, YH; Ji, BH; Lu, XZ; Ni, GX; Tang, QK; Wang, SY; Zhou, DH, 1986
)
0.27
" Rifaximin proved to be active on both aerobic and anaerobic bacteria and is thus effective, even at the dosage used, in the treatment of HE."( A non-absorbable rifamycin for treatment of hepatic encephalopathy.
Celle, G; De Leo, C; Eftimiadi, C; Rovida, S; Schito, GC; Sukkar, GS; Testa, R, 1985
)
0.27
" Also in dogs, after oral administration of L/105 in a single dose (25 mg/kg) and a multiple dosage (10 mg/kg/day, for 8 days), no traces of the compound were detected in the serum."( Pharmacokinetics of L/105, a new rifamycin, in rats and dogs, after oral administration.
Venturini, AP, 1983
)
0.27
" PMNs from the two sources were characterized by different responsiveness to this pharmacological agent: blood cells activated chemotaxis in a dose-response way during rifamycin therapy, whereas synovial polymorphs did not modify their locomotor behaviour."( Chemotactic behaviour of peripheral and synovial neutrophils during rifamycin SV therapy in rheumatoid arthritis.
Dovigo, L; Marangoni, C; Spisani, S; Traniello, S, 1984
)
0.27
" The patients were treated for 15 consecutive days with rifaximin, an antibiotic which is not absorbed by the intestinal wall, at a dosage of 1200 mg/day in association with sufficient lactulose to induce 2 or 3 evacuations per day."( Rifaximin in the treatment of chronic hepatic encephalopathy.
Ferrieri, A; Massimetti, A; Puxeddu, A; Quartini, M, 1995
)
0.29
" bovis Ravenel infection, three rifamycin derivatives gave "distinctive dose-response curves" in the correlation of dose sizes with the mean survival times or "log10CFU/lungs reductions"."( [Therapeutic efficacy of benzoxazinorifamycin KRM-1648 against experimental murine tuberculosis: (1). A study on the efficacy of short course treatment with the intratracheal and intravenous infection model].
Doi, N, 1998
)
0.3
" Thus, lower concentration of RIF may be available for absorption leading to poor bioavailability of RIF from combination dosage forms (RIF+INH) as compared to formulations containing only RIF."( Stability of rifampicin in dissolution medium in presence of isoniazid.
Kotecha, JS; Rathod, IS; Savale, SS; Shah, PB; Shah, SA; Shishoo, CJ, 1999
)
0.3
" If the allergen is to be identified, the testing dosage should be less than 10 per cent of the original dosage, along with prepared procedures for emergen tresale."( [Report on side effects of antituberculous agents].
, 1998
)
0.3
" The addition of GE23077 to plasmolyzed cells resulted in an immediate and specific inhibition of intracellular RNA biosynthesis, in a dose-response manner, strongly suggesting that cell penetration is the main obstacle for effective antimicrobial activity of the antibiotic."( Mode of action of the microbial metabolite GE23077, a novel potent and selective inhibitor of bacterial RNA polymerase.
Corti, E; Miele, A; Monti, F; Sarubbi, E; Selva, E, 2004
)
0.32
"To review the pharmacology, pharmacokinetics, clinical efficacy, adverse effects, drug interactions and precautions, and dosing recommendations of rifaximin, a new nonabsorbed antimicrobial agent for travelers' diarrhea."( Rifaximin: a new treatment for travelers' diarrhea.
Pakyz, AL, 2005
)
0.33
" Mesalazine is as effective as rifaximin (higher dosage schedule) for diminishing some symptoms, but it appears to be better than rifaximin for improving the global score in those patients."( Efficacy of mesalazine in the treatment of symptomatic diverticular disease.
Aragona, G; Cavallaro, LG; Cavestro, GM; Comparato, G; Di Mario, F; Fanigliulo, L; Franzé, A; Gnocchi, A; Iori, V; Leandro, G; Maino, M; Mazzocchi, G; Moussa, AM, 2005
)
0.33
"We examined the possibility of reducing relapse by increasing dosing schedules."( Dosing schedules of 6-month regimens and relapse for pulmonary tuberculosis.
Chan, SL; Chang, KC; Leung, CC; Tam, CM; Yew, WW, 2006
)
0.33
"We conducted a systematic review of published clinical trials involving adult cohorts with pulmonary tuberculosis treated using 6-mo rifamycin-containing regimens, which were grouped under seven categories ordered by dosing schedules."( Dosing schedules of 6-month regimens and relapse for pulmonary tuberculosis.
Chan, SL; Chang, KC; Leung, CC; Tam, CM; Yew, WW, 2006
)
0.33
" aureus septicemia model following administration by either oral or parenteral dosing routes."( Synthesis and antibacterial evaluation of a novel series of rifabutin-like spirorifamycins.
Chapo, K; Combrink, KD; Ding, CZ; Kim, IH; Ma, Z; Morris, TW; Pulse, M; Renick, P; Simecka, JW; Yan, D, 2007
)
0.57
"Administration of a 3 day dosing regimen of oral rifaximin was well tolerated and did not alter the pharmacokinetics of a commonly used combination OC containing EE and norgestimate."( Absence of effect of oral rifaximin on the pharmacokinetics of ethinyl estradiol/norgestimate in healthy females.
Bettenhausen, DK; Connolly, M; Forbes, WP; Pentikis, H; Trapnell, CB, 2007
)
0.34
"Consenting adults with acute diarrhea (> or =3 unformed stools in 24 hours with > or =1 symptom of enteric infection) were randomized to receive rifaximin 200 mg 3 times daily for 3 days; loperamide 4 mg initially followed by 2 mg after each unformed stool; or a combination of both drugs using the same dosing regimen."( Treatment of travelers' diarrhea: randomized trial comparing rifaximin, rifaximin plus loperamide, and loperamide alone.
Adachi, JA; Belkind-Gerson, J; De La Cabada, FJ; Dupont, HL; Dupont, MW; Ericsson, CD; Huang, DB; Jaini, S; Jiang, ZD; Ke, S; Martinez Sandoval, F; Okhuysen, PC; Taylor, DN, 2007
)
0.34
" The ability to measure rifampicin drug concentrations in both plasma and in cells may be useful in evaluating the suitability of dosage regimens for populations and individuals."( A rapid and sensitive HPLC-MS method for the detection of plasma and cellular rifampicin.
Ardrey, A; Ashleigh, S; Back, DJ; Chaponda, M; Davies, G; Hartkoorn, RC; Khoo, S; Tjia, JF; Waitt, CJ; Ward, SA, 2007
)
0.34
" Directly observed therapy short course (DOTS) effectiveness requires that each drug's effects persist equally throughout the dosing interval."( Acquired rifamycin resistance: pharmacology and biology.
Fourie, PB; Wallis, RS; Weyer, K, 2008
)
0.35
" Other possible improvements may come from inhaled delivery or split dosing (linezolid) of anti-TB drugs for which toxicity (ethionamide) or lack of absorption (aminoglycosides and polypeptides) precludes delivery of maximally effective, oral doses, once daily."( Tuberculosis pharmacotherapy: strategies to optimize patient care.
McGee, B; Mitnick, CD; Peloquin, CA, 2009
)
0.35
" To perform the immediate effect analysis (GPi or zero time), of each mixture either at room or refrigerator temperature, the preparation procedure was similar, although GPR, iodoform, Rifocort and camphorated paramonochlorophenol were stored in the refrigerator and then taken out, dosed and manipulated, and had their immediate effect tested after a 1-week period at storage of 4 degrees C average temperature."( Antimicrobial action of a filling paste used in pulp therapy in primary teeth under different storage conditions.
Ferreira, FV; Friedrich, RS; Guedes-Pinto, AC; Praetzel, JR; Weiss, RN, 2008
)
0.35
" Further studies are needed to evaluate efficacy and optimal dosing of rifaximin in this population."( Use and safety of rifaximin in children with inflammatory bowel disease.
Gulati, R; Hupertz, V; Mohr, F; Muniyappa, P, 2009
)
0.35
" The results demonstrated that simultaneous administration of α-AMA and each of tested antidotes (BPCN, CEFT, RIFSV) effectively protected human hepatocytes; however, in the group dosed with BPCN, the highest hepatocyte viability was observed."( Comparative antidotal efficacy of benzylpenicillin, ceftazidime and rifamycin in cultured human hepatocytes intoxicated with α-amanitin.
Dziędgiel, P; Gomułkiewicz, A; Magdalan, J; Ostrowska, A; Piotrowska, A; Szeląg, A, 2009
)
0.35
" The study provides data showing that bile acids solubilize rifaximin on a dose-response basis, increasing the drug's bioavailability and antimicrobial effect."( Bile acids improve the antimicrobial effect of rifaximin.
Ajami, N; Darkoh, C; Dial, EJ; DuPont, HL; Jiang, ZD; Lichtenberger, LM, 2010
)
0.36
" Animals received methylcellulose, neomycin (179 mg/kg/d) or variably dosed rifaximin (150-2000 mg/kg/d) one hour after irradiation and daily throughout the study period."( Rifaximin diminishes neutropenia following potentially lethal whole-body radiation.
Brawner, WR; Faircloth, J; Jahraus, CD; Powell, C; Ramos, M; Rynders, P; Schemera, B, 2010
)
0.36
"2 and remained suppressed throughout the duration of her rifaximin regimen despite incremental warfarin dosage increases (highest dose, 15 mg/day for 2 days, followed by 11."( Probable interaction between warfarin and rifaximin in a patient treated for small intestine bacterial overgrowth.
Hartig, C; Hoffman, JT; Lang, M; Sonbol, E, 2011
)
0.37
"At the end of the 12-week treatment period, 62% of patients who received the 800-mg dosage of rifaximin-EIR (61 of 98) were in remission, compared with 43% of patients who received placebo (43 of 101) (P = ."( Rifaximin-extended intestinal release induces remission in patients with moderately active Crohn's disease.
Danese, S; Gionchetti, P; Grimaldi, M; Lochs, H; Prantera, C; Scribano, ML, 2012
)
0.38
" The optimal dosage still needs to be better defined."( Rifaximin in the treatment of inflammatory bowel disease.
Guslandi, M, 2011
)
0.37
" High dosage rifampicin may be better able than RPT to cause high peaks."( Pharmacokinetic/pharmacodynamic parameters and the choice of high-dosage rifamycins.
Mitchison, DA, 2012
)
0.61
" Rifaximin at a dosage of 25 mg for 5 days modulated the vaginal proteome, counteracting the alterations associated with the BV condition."( Proteome profiles of vaginal fluids from women affected by bacterial vaginosis and healthy controls: outcomes of rifaximin treatment.
Brigidi, P; Calanni, F; Cruciani, F; Donders, G; Turroni, S; Vitali, B; Wasinger, V, 2013
)
0.39
" Limitations of evidence for probiotics include small populations analyzed and lack of clarity in optimal dosing regimen; antimicrobial evidence would benefit from better understanding of the effects of repeated treatment in patients with IBS."( Emerging role of probiotics and antimicrobials in the management of irritable bowel syndrome.
Cash, BD, 2014
)
0.4
" Based on these results, it is anticipated that the PBPK model developed in this study will be useful in evaluating dosing regimens for RPT and for characterizing tissue-level doses that could be predictors of problems related to efficacy or safety."( Physiologically Based Pharmacokinetic Model of Rifapentine and 25-Desacetyl Rifapentine Disposition in Humans.
Eppers, GJ; Reisfeld, B; Zurlinden, TJ, 2016
)
0.43
" The study purpose was to determine efficacy of traditional rifaximin dosing (400 mg three times daily) compared with newer dosing (550 mg twice daily) via readmission rates for the prevention of recurrent HE."( Retrospective cross-sectional pilot study of rifaximin dosing for the prevention of recurrent hepatic encephalopathy.
Likar, E; Lyon, KC; Martello, JL; Regier, M, 2017
)
0.46
" We need new strategies to rapidly assess the use of rifamycins, new anti-tuberculosis drugs and antiretroviral drugs together as information on safety and dosing of individual drugs becomes available."( Antiretroviral treatment in HIV-infected children who require a rifamycin-containing regimen for tuberculosis.
Cotton, MF; Decloedt, EH; Frigati, L; Garcia-Prats, AJ; Hesseling, A; Lallemant, M; Rabie, H; Schaaf, HS, 2017
)
0.7
" Future studies should study the most effective dosing regimen for rifaximin chemoprophylaxis, as well as profile local antimicrobial resistance/susceptibility data in less developed regions to further guide rifaximin use."( A meta-analysis of the use of rifaximin to prevent travellers' diarrhoea.
Chan, HW; Ho, CYX; Ng, QX; Shin, D; Venkatanarayanan, N, 2017
)
0.46
" Further research is needed to focus on specific mitigation strategies beyond opioid agent selection, such as dosing adjustment recommendations."( Clinical outcomes of concomitant rifamycin and opioid therapy: A systematic review.
Covvey, JR; Kinney, EM; Nemecek, BD; Vijapurapu, S, 2021
)
0.62
" These analyses evaluate dosing for prevention of cirrhosis complication-related hospitalizations/mortality and overt hepatic encephalopathy (OHE) treatment."( Dosing of Rifaximin Soluble Solid Dispersion Tablets in Adults With Cirrhosis: 2 Randomized, Placebo-controlled Trials.
Bajaj, JS; Hassanein, TI; Heimanson, Z; Israel, RJ; Pyrsopoulos, NT; Rahimi, RS; Rockey, DC; Sanyal, AJ, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (2,133)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990764 (35.82)18.7374
1990's288 (13.50)18.2507
2000's389 (18.24)29.6817
2010's598 (28.04)24.3611
2020's94 (4.41)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 64.48

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 Index64.48 (24.57)
Research Supply Index7.85 (2.92)
Research Growth Index4.58 (4.65)
Search Engine Demand Index113.64 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (64.48)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials203 (8.63%)5.53%
Reviews344 (14.63%)6.00%
Case Studies87 (3.70%)4.05%
Observational7 (0.30%)0.25%
Other1,710 (72.74%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (19)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Conjunctivitis Incidence in the Newborn Within the First Week of Life: Impact of the Prophylactic Use of Rifamycine(CRY NOT). [NCT03528915]881 participants (Actual)Observational2015-09-09Completed
Efficacy and Safety of CB-01-11 200mg Tablets in Infectious Diarrhoea. A Pilot, Dose Finding, Double-blind, Randomized, Multicentre Study [NCT03447821]Phase 240 participants (Actual)Interventional2008-02-29Completed
A Phase 1b/2a, Single-center, Randomized, Double-blind, Placebo-controlled Study to Evaluate the Safety, Tolerability, Pharmacokinetic Characteristics and Preliminary Efficacy of Multiple Ascending Doses of TNP-2092 Capsules in Liver Cirrhosis Patients Wi [NCT06135675]Phase 1/Phase 236 participants (Actual)Interventional2020-08-27Completed
Evaluation of the Effects of Irrigation of the Extraction Socket With Rifamycine on Postoperative Pain, Edema and Trismus in Impacted Lower Third Molar Surgery [NCT04349579]Phase 435 participants (Actual)Interventional2018-11-15Active, not recruiting
Phase I Clinical Trial to Evaluate the Efficacy of Sulforaphane as an Antagonist to Human PXR-mediated Drug-drug Interactions [NCT00621309]Phase 129 participants (Actual)Interventional2008-03-31Completed
A Phase 2a Study of the Early Bactericidal Activity of Rifampin (RIF) in Combination With Meropenem Plus Amoxicillin/Clavulanate Among Adults With Rifampin-resistant or Rifampin-susceptible Pulmonary Tuberculosis [NCT03174184]Phase 2112 participants (Actual)Interventional2017-08-23Completed
A Phase 3, Multicenter, Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Safety and Efficacy of Rifamycin SV MMX for the Treatment of Traveler's Diarrhea [NCT01142089]Phase 3264 participants (Actual)Interventional2010-05-27Completed
A Double-Blind Randomized Placebo-Controlled Trial of Rifamycin SV MXX in Minimal Hepatic Encephalopathy (RIVET Trial) [NCT04082780]Phase 230 participants (Actual)Interventional2019-09-01Completed
A Randomised, Double-blind, Double-dummy, Multi-centre, Comparative Parallel-group Study to Evaluate the Efficacy of Oral Rifamycin SV-MMX® 400 mg b.i.d. vs. Rifamycin SV-MMX® 600 mg t.i.d. vs. Placebo in the Treatment of Acute Uncomplicated Diverticuliti [NCT01847664]Phase 2204 participants (Actual)Interventional2013-08-31Completed
A Randomized Open Label Trial Evaluating the Efficacy of AEMCOLO (Rifamycin SV MMX) in the Treatment of Small Intestinal Bacterial Overgrowth (SIBO) [NCT04501380]Phase 230 participants (Anticipated)Interventional2020-06-30Enrolling by invitation
A Randomised, Double-blind, Double-dummy, Multi-centre, Comparative Parallel-group Study to Evaluate the Efficacy and Safety of Oral Daily Rifamycin SV-MMX® 400 mg b.i.d. vs. Ciprofloxacin 500 mg b.i.d. in the Treatment of Acute Infectious Diarrhoea in Tr [NCT01208922]Phase 3835 participants (Actual)Interventional2010-11-30Completed
Pharmacokinetics and Safety Study of Rifamycin SV-MMX® 600 mg Tablets After Single and Multiple t.i.d. Doses in Healthy Male and Female Volunteers. Single and Multiple Dose, Open Label, Pharmacokinetics and Safety Study [NCT02969252]Phase 118 participants (Actual)Interventional2015-07-31Completed
Double Blind, Multi-center Study to Evaluate the Safety and Efficacy of 100 mg Twice Daily Rifamycin SV MMX® Added to Standard ORT Versus Placebo Plus ORT, in the Treatment of Traveler's Diarrhea in Children Age 6 to 11 Years [NCT04026984]Phase 2142 participants (Anticipated)Interventional2024-06-30Not yet recruiting
Immune Activation and Drug Absorption in HIV-Infected Patients [NCT01845298]7 participants (Actual)Interventional2014-06-30Completed
A Phase I/II Trial of the Pharmacokinetics, Tolerability, and Safety of Once-Weekly Rifapentine and Isoniazid in HIV-1-infected and HIV-1-uninfected Pregnant and Postpartum Women With Latent Tuberculosis Infection [NCT02651259]Phase 1/Phase 250 participants (Actual)Interventional2017-03-13Completed
A Pragmatic Trial With Optimized Dose of Rifampicin and Moxifloxacin for the Treatment of Drug Susceptible Pulmonary Tuberculosis [NCT05575518]Phase 3414 participants (Anticipated)Interventional2023-08-11Recruiting
The Safety, Completion Rate and Prevention Effect by Rifamycin-containing Regimens for Latent Tuberculosis Infection in Patients With Kidney Transplantation: a Prospective Intervention Pilot Study [NCT05588492]Phase 4500 participants (Anticipated)Interventional2022-01-01Recruiting
A Phase II, Multicentre, Randomised, Double-blind, Placebo Controlled, Proof of Concept Study of Efficacy and Safety of Rifamycin SV-MMX® 600 mg Tablets Administered Three or Two Times Daily to Patients With Diarrhoea-predominant Irritable Bowel Syndrome [NCT03099785]Phase 2279 participants (Actual)Interventional2017-12-18Completed
Double Blind Study to Evaluate the Safety and Efficacy of 400 mg Twice Daily Rifamycin SV MMX® Added to Standard Oral Rehydration Therapy (ORT) Versus Placebo Plus ORT, in the Treatment of Traveler's Diarrhea in Children Age 12 to 17 Years [NCT04027894]Phase 2142 participants (Anticipated)Interventional2024-01-31Not yet recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00621309 (1) [back to overview]Midazolam Clearance (Pharmacokinetic Measure of Cytochrome P450 3A4 Activity)
NCT01142089 (2) [back to overview]Time to Last Unformed Stool (TLUS)
NCT01142089 (2) [back to overview]Clinical Cure
NCT01208922 (2) [back to overview]Number of Patients With Clinical Cure
NCT01208922 (2) [back to overview]Time to Last Unformed Stool (TLUS)
NCT02651259 (24) [back to overview]Cord Blood Concentrations of Rifapentine (RPT) Among Infants
NCT02651259 (24) [back to overview]Plasma Concentrations of Rifapentine (RPT) Among Infants
NCT02651259 (24) [back to overview]Volume of Distribution of INH
NCT02651259 (24) [back to overview]Volume of Distribution Relative to Bioavailability (Vc/F) for Rifapentine (RPT)
NCT02651259 (24) [back to overview]Area Under the Curve From 0 to 24 Hours (AUC0-24) for RPT and Area Under the Curve From 0 to 24 Hours (AUC0-24) for Des-RPT Pregnant Women in 2nd and 3rd Trimester
NCT02651259 (24) [back to overview]Clearance (CL/F) of INH
NCT02651259 (24) [back to overview]Maximum Concentration (Cmax) for RPT Maximum Concentration (Cmax) for Des-RPT Pregnant Women in 2nd and 3rd Trimester
NCT02651259 (24) [back to overview]Absorption (ka) of INH
NCT02651259 (24) [back to overview]Absorption Rate Constant (ka) for Rifapentine (RPT)
NCT02651259 (24) [back to overview]Clearance Relative to Bioavailability (CL/F) for Rifapentine (RPT)
NCT02651259 (24) [back to overview]Clearance Relative to Bioavailability (CL/F) for Rifapentine (RPT) for Intensive and Sparse PK
NCT02651259 (24) [back to overview]Clearance Relative to Bioavailability (CLmet/F) for Desacetyl Rifapentine (Des-RPT)
NCT02651259 (24) [back to overview]Cord Blood Concentrations of Desacetyl Rifapentine (Des-RPT) Among Infants
NCT02651259 (24) [back to overview]Maximum Concentration (Cmin) for RPT and Maximum Concentration (Cmin) for Des-RPT Pregnant Women in 2nd and 3rd Trimester
NCT02651259 (24) [back to overview]Incidence of Related Serious Adverse Events (SAEs) in Pregnant and Postpartum Women Taking Once-weekly RPT + INH
NCT02651259 (24) [back to overview]Number of Infants With Active TB up to 24 Weeks of Life
NCT02651259 (24) [back to overview]Number of Mothers With Active TB up to 24 Weeks Postpartum
NCT02651259 (24) [back to overview]Number of Participants With Discontinuation of Study Drug Due to Intolerance (Tolerability of Study Drug Regimen - i.e., RPT, INH, and Pyridoxine)
NCT02651259 (24) [back to overview]Percentage of Participants With All AEs Leading to Permanent Discontinuation of Study Drug Regimen (i.e., RPT, INH, and Pyridoxine)
NCT02651259 (24) [back to overview]Percentage of Participants With All Grade 3 and 4 AEs
NCT02651259 (24) [back to overview]Percentage of Participants With All Serious AEs
NCT02651259 (24) [back to overview]Percentage of Participants With Grade 2 Adverse Events (AEs) Judged to be Related to Study Drug Regimen
NCT02651259 (24) [back to overview]Percentage of Participants With Related Serious Adverse Events (AEs) in Infants Born to Women Taking Once-weekly RPT + INH
NCT02651259 (24) [back to overview]Plasma Concentrations of Desacetyl Rifapentine (Des-RPT) Among Infants
NCT03174184 (5) [back to overview]AUC for Rifampin
NCT03174184 (5) [back to overview]Distribution of Minimum Inhibitory Concentration (MIC) of Rifampin
NCT03174184 (5) [back to overview]Estimate of the 14-day Early Bactericidal Activity (EBA), Based on Colony Forming Unit Counts, of the Combination of Meropenem and Amoxicillin/Clavulanate, Without Versus With Rifampin
NCT03174184 (5) [back to overview]Estimate the Antimycobacterial Activity Based on Liquid Culture Time-to-positivity
NCT03174184 (5) [back to overview]Frequency of Grade 2 or Higher Adverse Events
NCT03447821 (2) [back to overview]The Number of Unformed Stools Passed Per 24-h Interval
NCT03447821 (2) [back to overview]Time to Last Unformed Stool (TLUS)

Midazolam Clearance (Pharmacokinetic Measure of Cytochrome P450 3A4 Activity)

(NCT00621309)
Timeframe: 7 days

,,
Interventionng*min/ml (Mean)
MDZ AUC Day 1MDZ AUC Day 8
Broccoli Sprout Extract Alone541558
Broccoli Sprout Extract Plus Rifampin552135
Rifampicin Alone604156

[back to top]

Time to Last Unformed Stool (TLUS)

"The primary endpoint is TLUS defined as the interval in hours between the first dose of study drug and the last unformed stool passed just before the start of Clinical Cure. An unformed stool is defined as either a soft or watery stool. TLUS will be calculated for each patient in the following manner:~Step 1: Identify when the patient achieves Clinical Cure.~Step 2: Moving backwards from this time, identify the time of the last unformed stool.~Step 3: The TLUS equals the time from the first dose of study drug to the time of the last unformed stool identified in Step 2." (NCT01142089)
Timeframe: 24 hours

,
InterventionTLUS (hours) (Mean)
25th percentile50th percentile75th percentile
Placebo37.468NA
Rifamycin SV MMX21.4672.2

[back to top]

Clinical Cure

"Clinical Cure is defined as either of the following:~Passage of two or fewer soft stools and no watery stools, no fever (>100.4 ºF or 38 ºC), and no signs or symptoms of enteric infection (other than mild excess gas/flatulence) during a 24 hour interval in the 120-hr data collection period after the first dose of study drug~Passage of no stools or only formed stools and no fever during a 48-hour interval in the 120-hr data collection period after the first dose of study drug, with or without other signs or symptoms of enteric infection" (NCT01142089)
Timeframe: 24 hours

InterventionParticipants (Count of Participants)
Placebo35
Rifamycin SV MMX162

[back to top]

Number of Patients With Clinical Cure

Clinical Cure Rate: 24-hour period with no clinical symptoms except mild flatulence, no fever, no watery stools and no more than 2 soft stools OR 48-hour period with no stools or only formed stools, and no fever, with our without symptoms of enteric infection. (NCT01208922)
Timeframe: 5 days

InterventionParticipants (Count of Participants)
Group A357
Group B352

[back to top]

Time to Last Unformed Stool (TLUS)

Time to Last Unformed Stool (TLUS), defined as the interval in hours between the first dose of study drug and the last unformed stool passed, after which clinical cure was declared. (NCT01208922)
Timeframe: 5 days

Interventionhours (Median)
Group A44.3
Group B40.3

[back to top]

Cord Blood Concentrations of Rifapentine (RPT) Among Infants

Cord blood concentrations were summarized using using R (version 3.5.1). (NCT02651259)
Timeframe: at delivery - (within 3 days of life for infants)

Interventionmcg/mL (Mean)
All Cohorts2.97

[back to top]

Plasma Concentrations of Rifapentine (RPT) Among Infants

Plasma concentrations were summarized using using R (version 3.5.1). (NCT02651259)
Timeframe: at delivery - (within 3 days of life for infants).

Interventionmcg/mL (Mean)
All Cohorts2.47

[back to top]

Volume of Distribution of INH

"PK parameters were determined from plasma concentration-time profiles using a nonlinear mixed effects model (version 7.4; ICON PLC, Dublin, Ireland).~• Estimated a single INH Vc/F for the whole population" (NCT02651259)
Timeframe: Data used in the population PK analysis included the intensive PK visit (pre-dose (t0) and 0.5, 1, 2. 4, 5, 8, 12, 24, 48, 72 hours post-dose) and sparse PK visit (1, 4, 24, 48 hours post-dose).

InterventionL (Mean)
All Cohorts107

[back to top]

Volume of Distribution Relative to Bioavailability (Vc/F) for Rifapentine (RPT)

"PK parameters were determined from plasma concentration-time profiles using a nonlinear mixed effects model (version 7.4; ICON PLC, Dublin, Ireland).~Developed a 1 compartment PK model with transit compartments for oral absorption~Estimated a single RPT Vc/F for for the whole population Note: that the mean stated below is actually the value that is obtained from a population analysis and represents a population estimate with the relative standard error" (NCT02651259)
Timeframe: Data used in the population PK analysis included the intensive PK visit (pre-dose (t0) and 0.5, 1, 2. 4, 5, 8, 12, 24, 48, 72 hours post-dose) and sparse PK visit (1, 4, 24, 48 hours post-dose).

InterventionL (Mean)
All Cohorts30.1

[back to top]

Area Under the Curve From 0 to 24 Hours (AUC0-24) for RPT and Area Under the Curve From 0 to 24 Hours (AUC0-24) for Des-RPT Pregnant Women in 2nd and 3rd Trimester

"PK parameters were determined from plasma concentration-time profiles using a nonlinear mixed effects model (version 7.4; ICON PLC, Dublin, Ireland).~Developed a 1 compartment PK model with transit compartments for oral absorption~Obtained AUC by model-based integration" (NCT02651259)
Timeframe: Data used in the population PK analysis included the intensive PK visit (pre-dose (t0) and 0.5, 1, 2. 4, 5, 8, 12, 24, 48, 72 hours post-dose) and sparse PK visit (1, 4, 24, 48 hours post-dose).

,
Interventionhour*mg/L (Mean)
AUC (0-24) for RPTAUC (0-24) for des-RPT
Cohort 1 (Pregnant Women Enrolled in the Second Trimester)424.7158.7
Cohort 2 (Pregnant Women Enrolled in the Third Trimester)406.8153.7

[back to top]

Clearance (CL/F) of INH

"PK parameters were determined from plasma concentration-time profiles using a nonlinear mixed effects model (version 7.4; ICON PLC, Dublin, Ireland).~Developed a 1 compartment PK model with 2 mixtures to characterize subpopulations based on acetylation status~Estimated a separate INH CL/F based on acetylation status (fast, slow)" (NCT02651259)
Timeframe: Data used in the population PK analysis included the intensive PK visit (pre-dose (t0) and 0.5, 1, 2. 4, 5, 8, 12, 24, 48, 72 hours post-dose) and sparse PK visit (1, 4, 24, 48 hours post-dose).

InterventionL/hr (Mean)
CL/F (slow acetylators)CL/F (fast acetylators)
All Cohorts8.9832.7

[back to top]

Maximum Concentration (Cmax) for RPT Maximum Concentration (Cmax) for Des-RPT Pregnant Women in 2nd and 3rd Trimester

"PK parameters were determined from plasma concentration-time profiles using a nonlinear mixed effects model (version 7.4; ICON PLC, Dublin, Ireland).~Developed a 1 compartment PK model with transit compartments for oral absorption~Obtained Cmax by model-based estimation" (NCT02651259)
Timeframe: Data used in the population PK analysis included the intensive PK visit (pre-dose (t0) and 0.5, 1, 2. 4, 5, 8, 12, 24, 48, 72 hours post-dose) and sparse PK visit (1, 4, 24, 48 hours post-dose).

,
Interventionmg/L (Mean)
Cmax for RPTCmax for des-RPT
Cohort 1 (Pregnant Women Enrolled in the Second Trimester)30.28.76
Cohort 2 (Pregnant Women Enrolled in the Third Trimester)28.68.50

[back to top]

Absorption (ka) of INH

"PK parameters were determined from plasma concentration-time profiles using a nonlinear mixed effects model (version 7.4; ICON PLC, Dublin, Ireland).~• Estimated a single absorption rate constant (ka) for the whole population" (NCT02651259)
Timeframe: Data used in the population PK analysis included the intensive PK visit (pre-dose (t0) and 0.5, 1, 2. 4, 5, 8, 12, 24, 48, 72 hours post-dose) and sparse PK visit (1, 4, 24, 48 hours post-dose).

Interventionhr-1 (Mean)
All Cohorts1.74

[back to top]

Absorption Rate Constant (ka) for Rifapentine (RPT)

"PK parameters were determined from plasma concentration-time profiles using a nonlinear mixed effects model (version 7.4; ICON PLC, Dublin, Ireland).~Developed a 1 compartment PK model with transit compartments for oral absorption~Estimated the transit compartment rate constant (ktr), which is synonymous with the absorption constant (ka), for the whole population Note that the mean stated below is actually the value that is obtained from a population analysis and represents a population estimate" (NCT02651259)
Timeframe: Data used in the population PK analysis included the intensive PK visit (pre-dose (t0) and 0.5, 1, 2. 4, 5, 8, 12, 24, 48, 72 hours post-dose) and sparse PK visit (1, 4, 24, 48 hours post-dose).

Interventionhr-1 (Mean)
All Cohorts1.43

[back to top]

Clearance Relative to Bioavailability (CL/F) for Rifapentine (RPT)

"PK parameters from postpartum women were determined from plasma concentration-time profiles using a nonlinear mixed effects model (version 7.4; ICON PLC, Dublin, Ireland).~Developed a 1 compartment PK model with transit compartments for oral absorption~Calculated an average CL for all post-partum individuals" (NCT02651259)
Timeframe: Data used in the population PK analysis for postpartum women included the intensive PK visit (pre-dose (t0) and 0.5, 1, 2. 4, 5, 8, 12, 24, 48, 72 hours post-dose) and sparse PK visit (1, 4, 24, 48 hours post-dose).

InterventionL/hr (Mean)
All Cohorts1.64

[back to top]

Clearance Relative to Bioavailability (CL/F) for Rifapentine (RPT) for Intensive and Sparse PK

"PK parameters were determined from plasma concentration-time profiles using a nonlinear mixed effects model (version 7.4; ICON PLC, Dublin, Ireland).~Developed a 1 compartment PK model with transit compartments for oral absorption~Calculated an average CL for all women in the 2nd trimester (cohort I) and all women in the 3rd trimester (cohort II)" (NCT02651259)
Timeframe: Data used in the population PK analysis included the intensive PK visit (pre-dose (t0) and 0.5, 1, 2. 4, 5, 8, 12, 24, 48, 72 hours post-dose) and sparse PK visit (1, 4, 24, 48 hours post-dose).

InterventionL/hr (Mean)
Cohort 1 (Pregnant Women Enrolled in the Second Trimester)1.4
Cohort 2 (Pregnant Women Enrolled in the Third Trimester)1.50

[back to top]

Clearance Relative to Bioavailability (CLmet/F) for Desacetyl Rifapentine (Des-RPT)

"PK parameters were determined from plasma concentration-time profiles using a nonlinear mixed effects model (version 7.4; ICON PLC, Dublin, Ireland).~Developed a 1 compartment PK model with transit compartments for oral absorption and a separate compartment for metabolite formation~Estimated a single des-RPT CLmet/F for the whole population Note: that the mean stated below is actually the value that is obtained from a population analysis and represents a population estimate with the relative standard error" (NCT02651259)
Timeframe: Data used in the population PK analysis included the intensive PK visit (pre-dose (t0) and 0.5, 1, 2. 4, 5, 8, 12, 24, 48, 72 hours post-dose) and sparse PK visit (1, 4, 24, 48 hours post-dose).

InterventionL/hr (Mean)
All Cohorts2.82

[back to top]

Cord Blood Concentrations of Desacetyl Rifapentine (Des-RPT) Among Infants

Cord blood concentrations were summarized using using R (version 3.5.1). (NCT02651259)
Timeframe: at delivery (within 3 days of life for infants).

Interventionmcg/mL (Mean)
All Cohorts3.24

[back to top]

Maximum Concentration (Cmin) for RPT and Maximum Concentration (Cmin) for Des-RPT Pregnant Women in 2nd and 3rd Trimester

"PK parameters were determined from plasma concentration-time profiles using a nonlinear mixed effects model (version 7.4; ICON PLC, Dublin, Ireland).~Developed a 1 compartment PK model with transit compartments for oral absorption~Obtained Cmin by model-based estimation" (NCT02651259)
Timeframe: Data used in the population PK analysis included the intensive PK visit (pre-dose (t0) and 0.5, 1, 2. 4, 5, 8, 12, 24, 48, 72 hours post-dose) and sparse PK visit (1, 4, 24, 48 hours post-dose).

,
Interventionmg/L (Mean)
Cmin for RPTCmin for des-RPT
Cohort 1 (Pregnant Women Enrolled in the Second Trimester)1.451.06
Cohort 2 (Pregnant Women Enrolled in the Third Trimester)1.581.20

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Number of Infants With Active TB up to 24 Weeks of Life

Based on site-specified confirmatory TB test. If women and infants were diagnosed with active TB during study they would be referred to local care for TB management and treatment. (NCT02651259)
Timeframe: Measured from birth through participants' last study visit at 24 weeks after delivery

InterventionParticipants (Count of Participants)
Cohort 1(Infants Born to Women Enrolled in Second Trimester)0
Cohort 2 (Infants Born to Women Enrolled in Third Trimester)0

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Number of Mothers With Active TB up to 24 Weeks Postpartum

Based on site-specified confirmatory TB test. If women and infants were diagnosed with active TB during study they would be referred to local care for TB management and treatment. (NCT02651259)
Timeframe: Measured from study entry through participants' last study visit at 24 weeks after delivery

InterventionParticipants (Count of Participants)
Cohort 1 (Pregnant Women Enrolled in the Second Trimester)0
Cohort 2 (Pregnant Women Enrolled in the Third Trimester)0

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Number of Participants With Discontinuation of Study Drug Due to Intolerance (Tolerability of Study Drug Regimen - i.e., RPT, INH, and Pyridoxine)

At entry and follow-up, all lab results, sign and symptoms, and diagnoses will be recorded. Also, during follow-up grade 2 events related to pregnancy complications, hepatotoxicity, hemorrhage, or peripheral neuropathy, and all grade 3 or events that result in discontinuation of study drug regimen, and that meet criteria for EAE reporting will be further evaluated and recorded. The DAIDS Table for Grading Adult and Pediatric Adverse Events (V 2.0) and Expedited AE Manual (V 2.0) were used. (NCT02651259)
Timeframe: Measured from study entry through participants' last study visit at 24 weeks after delivery

InterventionParticipants (Count of Participants)
Cohort 1 (Pregnant Women Enrolled in the Second Trimester)0
Cohort 2 (Pregnant Women Enrolled in the Third Trimester)0

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Percentage of Participants With All AEs Leading to Permanent Discontinuation of Study Drug Regimen (i.e., RPT, INH, and Pyridoxine)

At entry and follow-up, all lab results, sign and symptoms, and diagnoses were recorded. Also, during follow-up grade 2 events related to pregnancy complications, hepatotoxicity, hemorrhage, or peripheral neuropathy, and all grade 3 or events that resulted in discontinuation of study drug regimen, and that met criteria for EAE reporting would further be evaluated and recorded. The DAIDS Table for Grading Adult and Pediatric Adverse Events (V 2.0) and Expedited AE Manual (V 2.0) were used. (NCT02651259)
Timeframe: Measured from study entry through participants' last study treatment dispensation (approximately for 12 weeks)

Interventionpercent of participants (Number)
Cohort 1 (Pregnant Women Enrolled in the Second Trimester)0
Cohort 2 (Pregnant Women Enrolled in the Third Trimester)0

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Percentage of Participants With All Grade 3 and 4 AEs

At entry and follow-up, all lab results, sign and symptoms, and diagnoses were recorded. Also, during follow-up grade 2 events related to pregnancy complications, hepatotoxicity, hemorrhage, or peripheral neuropathy, and all grade 3 or events that resulted in discontinuation of study drug regimen, and that met criteria for EAE reporting would further be evaluated and recorded. The DAIDS Table for Grading Adult and Pediatric Adverse Events (V 2.0) and Expedited AE Manual (V 2.0) were used. (NCT02651259)
Timeframe: Measured from study entry through participants' last study visit at 24 weeks after delivery

Interventionpercent of participants (Number)
Cohort 1 (Pregnant Women Enrolled in the Second Trimester)20
Cohort 2 (Pregnant Women Enrolled in the Third Trimester)16

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Percentage of Participants With All Serious AEs

At entry and follow-up, all lab results, sign and symptoms, and diagnoses were recorded. Also, during follow-up grade 2 events related to pregnancy complications, hepatotoxicity, hemorrhage, or peripheral neuropathy, and all grade 3 or events that resulted in discontinuation of study drug regimen, and that met criteria for EAE reporting would further be evaluated and recorded. The DAIDS Table for Grading Adult and Pediatric Adverse Events (V 2.0) and Expedited AE Manual (V 2.0) were used. (NCT02651259)
Timeframe: Measured from study entry through participants' last study visit at 24 weeks after delivery

Interventionpercent of participants (Number)
Cohort 1 (Pregnant Women Enrolled in the Second Trimester)8
Cohort 2 (Pregnant Women Enrolled in the Third Trimester)12

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Plasma Concentrations of Desacetyl Rifapentine (Des-RPT) Among Infants

Plasma blood concentrations were summarized using using R (version 3.5.1). (NCT02651259)
Timeframe: at delivery - (within 3 days of life for infants).

Interventionmcg/mL (Mean)
All Cohorts5.31

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AUC for Rifampin

Rifampin AUC0-last in Arms A and C (NCT03174184)
Timeframe: 14 days

Interventionh*mg/L (Mean)
Rifampin Resistant A105
Rifampin Susceptible C109

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Distribution of Minimum Inhibitory Concentration (MIC) of Rifampin

The distribution of rifampin MIC in the drug-resistant arms (NCT03174184)
Timeframe: 14 days

Interventionmcg/mL (Median)
Rifampin Resistant A1.28
Rifampin Resistant B1.28

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Estimate of the 14-day Early Bactericidal Activity (EBA), Based on Colony Forming Unit Counts, of the Combination of Meropenem and Amoxicillin/Clavulanate, Without Versus With Rifampin

The Early Bactericidal Activity (EBA) over a 14 days period (EBA0-14), as determined by the median rate of change in log10 Colony Forming Units (CFU) per mL sputum. A non-linear mixed effects model of log10 CFU/mL sputum on time was developed using aggregated participant data for each treatment arm. A basic model was developed based on mono- or bi-exponential bacterial killing functions. Afterwards, covariate modelling to identify relationships between demographics, disease severity, secondary pharmacokinetic summary indices (area under the curve from time 0 to last measured concentration (AUC0-last) and maximum observed plasma concentration (Cmax), and model parameters describing log10 CFU/mL sputum over time was performed. Finally, the treatment regimen was tested using different functions supported by the graphical analysis. (NCT03174184)
Timeframe: 14 days

Interventionrate of change in log10 CFU/mL/day (Mean)
Rifampin Resistant A-0.06
Rifampin Resistant B-0.11
Rifampin Susceptible C-0.14
Rifampin Susceptible D-0.12
Rifampin Susceptible E-0.05
Rifampin Susceptible F-0.02

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Estimate the Antimycobacterial Activity Based on Liquid Culture Time-to-positivity

Change in time-to-positivity in Mycobacteria Growth Indicator Tube (MGIT) liquid media over 14 days of treatment (EBA0-14(TTP)) (time to positivity) for the study treatments. The Early Bactericidal Activity (EBA) over a 14 days period (EBA0-14), as determined by the median rate of change in TTP (expressed in log10 hours/day). A non-linear mixed effects model of log10 hours/day on time was developed using aggregated participant data for each treatment arm. A basic model was developed based on mono- or bi-exponential bacterial killing functions. Afterwards, covariate modelling to identify relationships between demographics, disease severity, secondary pharmacokinetic summary indices (area under the curve from time 0 to last measured concentration (AUC0-last) and maximum observed plasma concentration (Cmax), and model parameters describing TTP over time was performed. Finally, the treatment regimen was tested using different functions supported by the graphical analysis. (NCT03174184)
Timeframe: 14 days

Interventionrate of change in log10 hours/day (Mean)
Rifampin Resistant A0.19
Rifampin Resistant B0.31
Rifampin Susceptible C0.53
Rifampin Susceptible D0.20
Rifampin Susceptible E0.09
Rifampin Susceptible F0.09

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Frequency of Grade 2 or Higher Adverse Events

Grade 2 or higher Adverse Events (AE) that constitute any untoward medical occurrence in a study participant and which does not necessarily have a causal relationship with this treatment. An adverse event can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with the use of a medicinal product, whether or not related to the medicinal product. (NCT03174184)
Timeframe: From the time a study participant receives the first dose of study drug through the final study visit, up to 28 days

InterventionEvents (Number)
Rifampin Resistant A28
Rifampin Resistant B15
Rifampin Susceptible C5
Rifampin Susceptible D8
Rifampin Susceptible E3
Rifampin Susceptible F7

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The Number of Unformed Stools Passed Per 24-h Interval

The number of unformed stools passed per 24-h interval, after dosing (NCT03447821)
Timeframe: 192 hours

,,
InterventionUnformed stools (Mean)
0-24 h24-48 h48-72 h72-96 h96-120 h120-144 h144-168 h168-192 h
1200 mg Rifamycin SV Dosage4.732.641.71.80.75111
400 mg Rifamycin SV Dosage5.232.152.091.51.5330
800 mg Rifamycin SV Dosage4.671.51.291.671.50.511

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Time to Last Unformed Stool (TLUS)

The safety and preliminary efficacy data of the three doses of the new rifamycin SV formulation tested based upon the time elapsed from the ingestion of the 1st dose of study medication to the passage of the last unformed stool (TLUS) (NCT03447821)
Timeframe: Up to 7 days

Interventionhours (Mean)
400 mg Rifamycin SV Dosage59.3
800 mg Rifamycin SV Dosage51.4
1200 mg Rifamycin SV Dosage57.4

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