Page last updated: 2024-12-04

cimetidine

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Description

Cimetidine is a histamine H2 receptor antagonist, commonly used to treat peptic ulcers, gastritis, and gastroesophageal reflux disease (GERD). Its synthesis involves a multi-step process starting with a substituted imidazole derivative. Cimetidine blocks the action of histamine at H2 receptors in the stomach, reducing gastric acid secretion. This action is crucial for the treatment of conditions related to excess stomach acid. Cimetidine is often studied due to its unique pharmacological properties, its therapeutic potential for treating acid-related disorders, and its role in advancing the understanding of histamine receptor antagonism. It has been found to exhibit anti-androgenic effects, which have raised concerns about potential side effects.'

Cimetidine: A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

cimetidine : A member of the class of guanidines that consists of guanidine carrying a methyl substituent at position 1, a cyano group at position 2 and a 2-{[(5-methyl-1H-imidazol-4-yl)methyl]sulfanyl}ethyl group at position 3. It is a H2-receptor antagonist that inhibits the production of acid in stomach. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID2756
CHEMBL ID30
CHEBI ID3699
SCHEMBL ID11282982
SCHEMBL ID1093
SCHEMBL ID1094
MeSH IDM0004479

Synonyms (345)

Synonym
MLS002153265
MLS001148596
MLS002154178
HMS3267A03
AB00052157-03
BRD-K18618618-001-01-6
BRD-K34157611-001-04-6
3-cyano-2-methyl-1-[2-[(5-methyl-1h-imidazol-4-yl)methylsulfanyl]ethyl]guanidine
gtpl1231
guanidine, n-cyano-n'-methyl-n''-[2-[[5-methyl-1h-imidazol-4-yl)methyl]thio]ethyl]-
KBIO1_000166
DIVK1C_000166
NCI60_002936
smr000038895
MLS000069791 ,
LOPAC0_000293
2-cyano-1-methyl-3-(2-{[(5-methyl-1h-imidazol-4-yl)methyl]thio}ethyl)guanidine
cemitidine
; n''''''''''''''''-cyano-n-methyl-n''''''''-(2-(((5-methyl-1h-imidazol-4-yl)methyl)thio)-ethyl)guanidine
n-methyl-n-[2-(5-methyl-1h-4-imidazolylmethylsulfanyl)ethyl]imino(-n-cyano)methanediaminem
n''''''''''''''''-cyano-n-methyl-n''''''''-(2-{[(5-methyl-1h-imidazol-4-yl)methyl]-lambda~4~-sulfanyl}ethyl)guanidine
tagamet hb
n-cyano-n''''''''-methyl-n''''''''''''''''-(2-(((5-methyl-1h-imidazol-4-yl) methyl)thio)ethyl)guanidine(cimetidine)
bdbm22889
2-methylamino-2-[2-(5-methyl-1h-4-imidazolylmethylsulfanyl)ethylamino]-(z)-1-imino cyanide(cimetidine)
n-methyl-n''''''''-[2-(5-methyl-1h-imidazol-4-ylmethylsulfanyl)-ethyl]-n''''''''''''''''-cyano-guanidine(cimetidine)
(cimetidine) n-methyl-n''''''''-[2-(5-methyl-1h-imidazol-4-ylmethylsulfanyl)-ethyl]-guanidine,cyanide
n-methyl-n''''''''-cyano-n''''''''''''''''-[2-(5-methyl-1h-imidazol-4-ylmethylsulfanyl)-ethyl]-guanidine
n''''''''''''''''-cyano-n-methyl-n''''''''-(2-{[(5-methyl-1h-imidazol-4-yl)methyl]thio}ethyl)guanidine (cimetidine)
n-methyl-n''''''''-[2-(5-methyl-1h-imidazol-4-ylmethylsulfanyl)-ethyl]-n''''''''''''''''-cyano-guanidine
n''''''''''''''''-cyano-n-methyl-n''''''''-(2-{[(5-methyl-1h-imidazol-4-yl)methyl]thio}ethyl)guanidine(cimetidine)
n''''''''''''''''''''''''''''''''-cyano-n-methyl-n''''''''''''''''-(2-{[(5-methyl-1h-imidazol-4-yl)methyl]thio}ethyl)guanidine
1-cyano-2-methyl-3-(2-{[(5-methyl-1h-imidazol-4-yl)methyl]sulfanyl}ethyl)guanidine
n-methyl-n-[2-(5-methyl-1h-4-imidazolylmethylsulfanyl)ethyl]-1-cyanoiminomethanediamine
(cimetidine)n-methyl-n-[2-(5-methyl-1h-4-imidazolylmethylsulfanyl)ethyl]cyanomethyliminomethanediamine
n''''''''''''''''-cyano-n-methyl-n''''''''-({[(5-methyl-1h-imidazol-4-yl)methyl]thio}methyl)guanidine(cimetidine)
n''''''''''''''''-cyano-n-methyl-n''''''''-(2-{[(5-methyl-1h-imidazol-4-yl)methyl]thio}ethyl)guanidine
2-chloro-5-(1-hydroxy-3-oxo-2,3-dihydro-1h-isoindol-1-yl)-benzenesulfonamide(cimetidine)
2-methyl-8-phenethyl-imidazo[1,2-a]pyridine-3-carboxylic acid methyl ester(cimetidine)
eureceptor
n-tert-butyl-n''''''''-[4-(1h-imidazol-4-yl)-phenyl]-formamidine(cimetidine)
(cimetidine) n-methyl-n-[2-(5-methyl-1h-4-imidazolylmethylsulfanyl)ethyl]cyanoiminomethanediamine
chembl30 ,
1-cyano-2-methyl-3-(2-((5-methyl-1h-imidazol-4-yl)methylthio)ethyl)guanidine
n-methyl-n-[2-(5-methyl-1h-4-imidazolylmethylsulfanyl)ethyl]cyanoiminomethanediamine (cimetidine)
n-cyanomethyl-n''''''''-methyl-n''''''''''''''''-[2-(5-methyl-1h-imidazol-4-ylmethylsulfanyl)-ethyl]-guanidine ( cimetidine)
2-methylamino-2-[2-(4-methyl-1h-5-imidazolylmethylsulfanyl)ethylamino]-(e)-1-imino cyanide
n-methyl-n''''''''-[2-(5-methyl-1h-imidazol-4-ylmethylsulfanyl)-ethyl]-cyanoguanidine(cimetidine)
gastrobitan
edalene
ulcimet
cimetidinum [inn-latin]
ulcestop
gastromet
valmagen
hsdb 3917
ulcomet
n-cyano-n'-methyl-n''-(2-(((5-methyl-1h-imidazol-4-yl)methyl)thio)ethyl)guanidine
acinil
metracin
tratul
ulhys
peptol
cimetidina [inn-spanish]
ulcedine
skf 92334
guanidine, n-cyano-n'-methyl-n''-(2-(((5-methyl-1h-imidazol-4-yl)methyl)thio) ethyl)-
guanidine, n''-cyano-n-methyl-n'-(2-(((5-methyl-1h-imidazol-4-yl)methyl)thio)ethyl)-
fpf 1002
dyspamet
evicer
tametin
skf-92334
ccris 3247
guanidine, n-cyano-n'-methyl-n''-(2-(((5-methyl-1h-imidazol-4-yl)methyl)thio)ethyl)-
ulcedin
cimetum
ulcofalk
drg-0150
cimal
einecs 257-232-2
acibilin
n''-cyano-n-methyl-n'-[2-[(5-methyl-1h-imidazol-4-yl)methylthio]ethyl]guanidine
guanidine, n-cyano-n'-methyl-n''-[2-[[(5-methyl-1h-imidazol-4-yl)methyl]thio]ethyl]-
nsc-335308
nsc335308
guanidine, n''-cyano-n-methyl-n'-[2-[[(5-methyl-1h-imidazol-4-yl)methyl]thio]ethyl]-
tagamet
1-cyano-2-methyl-3-[2-[[(5-methylimidazol-4-yl)methyl]thio]ethyl]guanidine
brumetidina
ulcomedina
EU-0100293
SPECTRUM_000495
2-cyano-1-methyl-3-(2-{[(5-methyl-1h-imidazol-4-yl)methyl]sulfanyl}ethyl)guanidine
2-cyano-1-methyl-3-(2-(((5-methylimidazol-4-yl)methyl)thio)ethyl)guanidine
1-cyano-2-methyl-3-(2-(((5-methyl-4-imidazolyl)methyl)thio)ethyl)guanidine
PRESTWICK_65
cimetag
cimetidinum
n-cyano-n'-methyl-n''-(2-([(5-methyl-1h-imidazol-4-yl)methyl]sulfanyl)ethyl)guanidine
tagamet hb 200
n''-cyano-n-methyl-n'-(2-{[(5-methyl-1h-imidazol-4-yl)methyl]thio}ethyl)guanidine
cimetidina
CHEBI:3699 ,
lopac-c-4522
NCGC00015240-01
tocris-0902
NCGC00024859-01
SPECTRUM5_001541
IDI1_000166
BSPBIO_000091
BPBIO1_000101
BSPBIO_002978
PRESTWICK3_000026
NCGC00091439-01
UPCMLD-DP029:001
C06952
51481-61-9
cimetidine
2-cyano-1-methyl-3-[2-[(5-methyl-1h-imidazol-4-yl)methylsulfanyl]ethyl]guanidine
n-cyano-n'-methyl-[2-[[[5-methyl-1h-imidazol-4-yl]methyl]thio]ethyl]guanidine
DB00501
UPCMLD-DP029
D00295
cimetidine (jp17/usp/inn)
tagamet (tn)
NCGC00091439-03
NCGC00024859-03
NCGC00024859-05
NCGC00091439-02
KBIO3_002198
KBIOSS_000975
KBIO2_000975
KBIO2_003543
KBIOGR_001323
KBIO2_006111
SPECTRUM3_001389
SPECTRUM2_000782
SPBIO_000884
NINDS_000166
SPECTRUM4_000812
SPECTRUM1500684
NCGC00024859-02
NCGC00024859-04
NCGC00091439-04
L013434
NCGC00015240-03
HMS2092I14
C 4522 ,
HMS2089O03
skf-92334; tagamet
2-cyano-1-methyl-3-[2-(5-methyl-1h-imidazol-4-yl-methylthio)ethyl]guanidine
NCGC00185989-01
L000186
L003827
n-cyano-n'-methyl-n''-(2-(((5-methyl-1h-imidazol-4-yl)methyl)thio)ethyl) guanidine
stomedine
aciloc
HMS500I08
HMS1921C14
1-cyano-2-methyl-3-[2-[(5-methyl-1h-imidazol-4-yl)methylsulfanyl]ethyl]guanidine
NCGC00015240-06
AKOS005460997
NCGC00091439-05
NCGC00188961-01
HMS3259M15
HMS2095E13
HMS3260L08
tox21_201160
NCGC00258712-01
SCHEMBL11282982
STK528249
A828616
1-cyano-2-methyl-3-[2-[(5-methyl-1h-imidazol-4-yl)methylthio]ethyl]guanidine
nsc757428
pharmakon1600-01500684
nsc-757428
dtxcid40329
dtxsid4020329 ,
tox21_110106
CCG-204388
AKOS015951369
HMS2232F16
AKOS016003398
CCG-40160
NCGC00015240-04
NCGC00015240-07
NCGC00015240-02
NCGC00015240-05
brumetadina
bdbm50403559
nsc 335308
unii-80061l1wgd
topcare heartburn relief
cimetidine [usan:usp:inn:ban:jan]
nsc 757428
equaline acid reducer
80061l1wgd ,
FT-0602955
LP00293
AB03708
cimetidine [mart.]
cimetidinum [who-ip latin]
cimetidine [who-dd]
cimetidine [who-ip]
cimetidine [jan]
cimetidine [vandf]
2-cyano-1-methyl-3-(2-(((5-methylimidazol-4-yl)methyl)thio)ethyl)-guanidine
cimetidine [hsdb]
cimetidine [orange book]
cimetidine [usan]
cimetidine [usp-rs]
cimetidine [ep monograph]
cimetidine [mi]
cimetidine [inn]
cimetidine [usp monograph]
cimetidine [iarc]
S1845
AKOS015900557
n-cyano-n'-methyl-n''-[2-[[(4-methyl-1h-imidazol-5-yl)methyl]thio]ethyl]guanidine
AKOS016340377
HMS3369L10
CCG-220026
CCG-221597
HY-14289
NC00501
SCHEMBL1093
SCHEMBL1094
tox21_110106_1
NCGC00091439-07
KS-5087
n-cyano-n'-methyl-n-[2-((4-methyl-5-imidazolyl)methylthio)ethyl]guanidine
n-cyano-n'-methyl-n-[2-((5-methyl-4-imidazolyl)methylthio)-ethyl]guanidine
n-cyano-n'-methyl-n--[2-((4-methyl-5-imidazolyl)methylthio)ethyl]guanidine
n-methyl-n'-{2-[(5-methylimidazol-4-yl)-methylthio]-ethyl}-n-cyanoguanidine
n-cyano-n'-methyl-n-[2-((4-methyl-5-imidazolyl)-methylthio)ethyl]guanidine
n-cyano-n-methyl-n'-[2-(5-methylimidazol-4-ylmethylthio)ethyl]-guanidine
n-cyano-n'-methyl-n-[2-((4-methyl-5-imidazolyl) methylthio)ethyl]guanidine
n-cyano-n'-methyl-n-[2-((4-methyl-5-imidazolyl)- methylthio)ethyl]guanidine
n-cyano-n'-methyl-n- [2-((5-methyl-4-imidazolyl)methylthio)ethyl]guanidine
n-cyano-n'-methyl-n-[2-((5-methyl-4-imidazolyl)methylthio)ethyl]-guanidine
4-(((2-(((cyanoamino)(methylamino)methylene)amino)ethyl)thio)methyl)-5-methyl-1h-imidazole
n-cyano-n'-methyl-n-[2-(5-methyl-4-imidazolylmethylthio)ethyl]guanidine
n-cyano-n-methyl-n'-[2-(5-methylimidazol-4-ylmethylthio)ethyl]guanidine
n-cyano-n'-methyl-n-[2-((5-methyl-4-imidazolyl)methylthio)ethyl]guanidine
n-cyano-n'-methyl-n-[2-((4-methyl-5-imidazolyl)methylthio)ethyl) guanidine
n-cyano-n'-methyl-n-[2-((4-methyl-5-imidazolyl)methyl-thio)ethyl]guanidine
n-cyano-n'-methyl-n-[2-{(5-methyl-1h-imidazol-4-yl)methylthio}ethyl]guanidine
tox21_500293
NCGC00260978-01
943920-67-0
1-cyan-2-methyl-3-(2-{[(5-methylimidazol-4-yl)methyl]thio}ethyl)guanidin
metidine
2984-61-4
cimetidine a
n-cyano-n'-methyl-n''-(2-([(5-methyl-1h-imidazol-4-yl)methyl]sulfanyl)ethyl)guanidine #
Q-200856
Q-200855
n-cyano-n'-methyl-n''-[2-[(5-methyl-1h-imidazol-4-yl)methyl]thio]ethyl]guanidine
AB00052157_05
OPERA_ID_314
AB00052157_04
mfcd00133296
bdbm50103595
us9138393, cimetidine
us9144538, cimetidine
bdbm181119
(z)-1-cyano-2-methyl-3-(2-{[(5-methyl-1h-imidazol-4-yl)methyl]sulfanyl}ethyl)guanidine
AKOS026749950
cimetidine, european pharmacopoeia (ep) reference standard
EX-A1088
AC-8100
SR-05000001750-1
sr-05000001750
(e)-2-cyano-1-methyl-3-(2-(((5-methyl-1h-imidazol-4-yl)methyl)thio)ethyl)guanidine
cimetidine, united states pharmacopeia (usp) reference standard
HMS3651E21
n-cyano-n'-methyl-n''-[2-[[(5-methylimidazol-4-yl]methyl]thio]ethyl)guanidine
sr-05000001434
SR-05000001434-2
SR-05000001434-1
F16651
cimetidine for system suitability, european pharmacopoeia (ep) reference standard
cimetidine for peak identification, european pharmacopoeia (ep) reference standard
cimetidine, pharmaceutical secondary standard; certified reference material
cimetidine 1.0 mg/ml in methanol
guanidine, n-cyano-n'-methyl-n''-[2-[[(5-methyl-1h-imidazol-4-yl)methyl]thio]ethyl]-, (z)-
76181-71-0
SR-01000075260-1
SR-01000075260-3
sr-01000075260
SBI-0050281.P004
n''-cyano-n-methyl-n'-(2-((5-methyl-1h-imidazol-4-yl)-methylthio)ethyl)guanidine
HMS3712E13
guanidine,n-cyano-n'-methyl-n''-[2-[[(5-methyl-1h-imidazol-4-yl)methyl]thio]ethyl]-,(z)-
(z)-3-cyano-1-methyl-2-(2-{[(5-methyl-1h-imidazol-4-yl)methyl]sulfanyl}ethyl)guanidine
SW196380-2
AKOS032949548
Q409492
cimetidine (tagamet)
HMS3678I17
cimetidine,(s)
270574-63-5
HMS3414I17
BRD-K34157611-001-07-9
SDCCGSBI-0050281.P005
HMS3884I12
NCGC00091439-10
HMS3750I05
51481-61-9 (free)
cimetidine 100 microg/ml in acetonitrile
(z)-n''-cyano-n-methyl-n'-(2-{[(5-methyl-1h-imidazol-4-yl)methyl]sulfanyl}ethyl)guanidine
cimetidine for system suitability
cimetidine for peak identification
4h-dithieno[3,2-b :2',3'-d ]pyrrole, 4-(1-octylnonyl)-
n''-cyano-n-methyl-n'-(2-{[(5-methyl-1h-imidazol-4-yl)methyl]sulfanyl}ethyl)guanidine
EN300-73705
EN300-27121293
(e)-n''-cyano-n-methyl-n'-(2-{[(5-methyl-1h-imidazol-4-yl)methyl]sulfanyl}ethyl)guanidine
EN300-27121291
Z1162463430
SY057952
cimetidineacid reducer
cimetidine (usp monograph)
sunmark heartburn reliefacid reducer
cimetidina (inn-spanish)
cimetidine (usp-rs)
n-cyano-n'-methyl-n''-(2-(((5-methyl-1h-imidazol-4-yl)methyl)sulfanyl)ethyl)guanidine
cimetidine (iarc)
n''-cyano-n-methyl-n'-(2-(((5-methyl-1h-imidazol-4-yl)methyl)thio)ethyl)guanidine
2-cyano-1-methyl-3-(2-(((5-methyl-1h-imidazol-4-yl)methyl)sulfanyl)ethyl)guanidine
tratue
a02ba01
good sense heartburn relief
good neighbor pharmacy heartburn relief
sunmark heartburn relief
cimetidinum (inn-latin)
2-cyano-1-methyl-3-(2-((5-methyl-1h-imidazol-4-yl)methylsulfanyl)ethyl)guanidine
cimetidine (mart.)
n-cyano-n'-methyl-n''-(2(((5-methyl-1h-imidazol-4-yl)methyl)thio)ethyl)
cimetidin
cimetidine (ep monograph)
cimetidine (usan:usp:inn:ban:jan)
equate cimetidine
AKOS040824773

Research Excerpts

Overview

Cimetidine (CIM) is an over-the-counter histamine-2 (H2) antagonist that is primarily used to lower acid secretions in the stomach. Cimetidine is a much more potent inhibitor for hMATE1/2-K when metformin is the substrate.

ExcerptReferenceRelevance
"Cimetidine is a potent organic cation transporter 2/multidrug and toxin extrusion protein inhibitor."( A Comprehensive Whole-Body Physiologically Based Pharmacokinetic Drug-Drug-Gene Interaction Model of Metformin and Cimetidine in Healthy Adults and Renally Impaired Individuals.
Ebner, T; Hanke, N; Ishiguro, N; Lehr, T; Müller, F; Nock, V; Selzer, D; Stopfer, P; Türk, D; Wiebe, S, 2020
)
1.49
"Cimetidine is a histamine H2-receptor antagonist used for treatment of gastrointestinal disorders. "( Ecotoxicological assessment of cimetidine and determination of its potential for endocrine disruption using three test organisms: Daphnia magna, Moina macrocopa, and Danio rerio.
Ahn, B; Choi, K; Ji, K; Jung, D; Kho, Y; Kim, P; Lee, S, 2015
)
2.15
"Cimetidine is a histamine H2 receptor blocker which inhibits acid release from stomach and is used for gasterointestinal diseases."( Binding of Cimetidine to Balb/C Mouse Liver Catalase; Kinetics and Conformational Studies.
Jahangirvand, M; Minai-Tehrani, A; Minai-Tehrani, D; Razmi, N; Yazdi, F, 2016
)
1.55
"Cimetidine (CIM) is an over-the-counter histamine-2 (H2) antagonist that is primarily used to lower acid secretions in the stomach."( Cimetidine as a novel adjunctive treatment for early stage Lyme disease.
Shemenski, J, 2019
)
2.68
"Cimetidine is a much more potent inhibitor for hMATE1/2-K when metformin is the substrate but acts as an equally potent inhibitor of hOCT2 and hMATE1/2-K when atenolol is the substrate."( Impact of Substrate-Dependent Inhibition on Renal Organic Cation Transporters hOCT2 and hMATE1/2-K-Mediated Drug Transport and Intracellular Accumulation.
Duan, H; Wang, J; Yin, J, 2016
)
1.16
"Cimetidine is a histamine H"( The topological phase diagram of cimetidine: A case of overall monotropy.
Céolin, R; Rietveld, IB, 2017
)
2.18
"Cimetidine is an H(2)-antagonist with cytochrome P450 (P450) inhibitory activity. "( Effects of cytochrome p450 inhibition by cimetidine on the warm hepatic ischemia-reperfusion injury in rats.
Mehvar, R; Shaik, IH, 2010
)
2.07
"Cimetidine is an H2 receptor antagonist and a potent inhibitor of Na+/H+ antiporter, which is found in the plasma membranes of various cell types, including mesothelial cells."( Effect of cimetidine on the electrophysiologic profile of isolated visceral sheep peritoneum.
Arampatzis, S; Giannopoulou, M; Gourgoulianis, K; Hatzoglou, C; Karioti, A; Kourti, P; Liakopoulos, V; Molyvdas, PA; Musso, C; Stefanidis, I; Zarogiannis, S, 2009
)
1.48
"Cimetidine (CIM) is a histamine H2 receptor inverse agonist used primarily as an anti-stomach acids drug, but recent studies showed that it may also modulate immune responses. "( Cimetidine augments Th1/Th2 dual polarized immune responses to recombinant HBV antigens.
Ding, Z; Kang, Y; Li, R; Su, B; Wang, B; Wang, J; Zhang, W, 2011
)
3.25
"Cimetidine is a H(2)-receptor antagonist used for treatment of gastric ulcers that seems to prevent bone resorption."( Increased apoptosis in osteoclasts and decreased RANKL immunoexpression in periodontium of cimetidine-treated rats.
Cerri, PS; de Oliveira, PA; de Souza Faloni, AP; Longhini, R; Sasso-Cerri, E, 2013
)
1.33
"Cimetidine appears to be a more potent inhibitor of aldehyde oxidase than of CYP3A forms and hence in vivo is likely to have a more marked effect on ZAL metabolism to M2 than on DZAL formation."( Inhibition of zaleplon metabolism by cimetidine in the human liver: in vitro studies with subcellular fractions and precision-cut liver slices.
Ball, SE; Kao, J; Lake, BG; Price, RJ; Renwick, AB; Scatina, JA; Tredger, JM; Walters, DG, 2002
)
1.31
"Cimetidine is a powerful H2 receptor antagonist that eliminates histamine's effects on chemotaxis, phagocytosis, and superoxide anion production by phagocytes. "( Topical H2 antagonist prevents periodontitis in a rabbit model.
Andry, C; Ebrahimi, N; Hasturk, H; Holick, M; Jones, VL; Kantarci, A; Van Dyke, TE, 2006
)
1.78
"Cimetidine is a widely used antiulcer medication that is also a potent inhibitor of the mixed-function oxidase enzymes in the liver. "( Cimetidine drug interactions.
Greene, WL; Levinson, MJ; Self, TH, 1983
)
3.15
"Cimetidine is a histamine type 2 receptor antagonist and indomethacin is an inhibitor of prostaglandin synthesis."( Effects of cimetidine and indomethacin on the growth of dimethylhydrazine-induced or transplanted intestinal cancers in the rat.
Caignard, A; Martin, F; Martin, M; Reisser, D; Thomas, B, 1984
)
1.38
"Cimetidine is a well known inhibitor of the heme-containing enzyme cytochrome P-450. "( Effect of cimetidine on delta-aminolevulinic acid synthase and microsomal heme oxygenase in rat liver.
Bourque, AL; Freedman, ML; Halbrecht, JL; Lew, G; Marcus, DL; Nadel, H, 1984
)
2.11
"Cimetidine is a well known H2 antagonist which is known to inhibit microsomal enzyme drug metabolism."( Influence of cimetidine on the disposition of ibuprofen in the rat.
Christensen, JM; Parrott, KA, 1984
)
1.36
"Cimetidine is a rare cause of drug-induced fever. "( Cimetidine-induced fever.
Landolfo, K; Low, DE; Rogers, AG, 1984
)
3.15
"Cimetidine is a commonly prescribed histamine antagonist useful in the treatment of peptic ulcer disease. "( Cimetidine and the immune response. I. In vivo augmentation of nonspecific and specific immune response.
Burroughs, BJ; Ershler, WB; Hacker, MP; Moore, AL; Myers, CF, 1983
)
3.15
"Cimetidine is a histamine H2-antagonist. "( No evidence of carcinogenicity of N-nitrosocimetidine in rats.
Eisenbrand, G; Habs, H; Habs, M; Schmähl, D, 1982
)
1.97
"Cimetidine appears to be an excellent agent to use as a preventative measure against aspiration during the induction of anaesthesia."( A comparative evaluation of cimetidine and sodium citrate to decrease gastric acidity: effectiveness at the time of induction of anaesthesia.
Foulkes, E; Jenkins, LC, 1981
)
1.28
"Cimetidine is a highly effective and safe drug which, compared with the other treatments currently available, can be considered as the best solution of this problem."( [Cimetidine: solution to a problem?].
Cambielli, M, 1981
)
1.89
"Cimetidine was shown to be a potent inhibitor of gastric ADH."( Hepatic glutathione determination after ethanol administration in rat: evidence of the first-pass metabolism of ethanol.
Battiston, L; Lunazzi, G; Marchi, P; Mazzoran, L; Micheli, L; Moretti, M; Pozzato, G; Tulissi, P, 1995
)
1.01
"Cimetidine is an H2-receptor antagonist which is mainly used to treat gastrointestinal diseases. "( The effect of cimetidine on verruca plana juvenilis: clinical trials in six patients.
Choi, YS; Hann, SK; Park, YK, 1993
)
2.09
"Cimetidine is an inhibitor of hepatic cytochrome P450 (CYP) in vivo and in vitro in both rats and humans. "( Effect of cimetidine on hepatic cytochrome P450: evidence for formation of a metabolite-intermediate complex.
Bellward, GD; Levine, M, 1995
)
2.14
"Cimetidine is an H2 blocker and has been shown to inhibit tumour cell growth."( Effect of histamine and the H2 antagonist cimetidine on the growth and migration of human neoplastic glia.
Finn, PE; Pilkington, GJ; Purnell, P, 1996
)
1.28
"Cimetidine is a commonly used H2-receptor antagonist that has been recommended for the prevention of acid aspiration syndrome and has been shown to potentiate vecuronium-induced neuromuscular block. "( [The effects of cimetidine on the pharmacodynamics of rocuronium].
de Almeida, MC; Kleemann, PP; Latorre, F; Stanek, A; Weiler, N, 1996
)
2.08
"Cimetidine (CIM) is an H2-receptor antagonist with a long history of clinical use in peptic ulcer disease. "( A randomized, placebo-controlled study of oral cimetidine as an immunopotentiator of parenteral immunization with a group B meningococcal vaccine.
Drabick, JJ; Foster, JS; Moran, EE; Tang, DB; Trofa, AF; Zollinger, WD, 1997
)
2
"Cimetidine is a H2-histamine antagonist that has been shown to inhibit several P450-isoforms."( The actions of the H2-blocker cimetidine on the toxicity and biotransformation of the phosphorothioate insecticide parathion.
Agyeman, AA; Sultatos, LG, 1998
)
1.31
"Cimetidine is an H2-receptor antagonist used in the management of peptic ulcer disease and other hypersecretory gastrointestinal disorders. "( A phase II study of high-dose cimetidine and the combination 5-fluorouracil, interferon alpha-2A, and leucovorin in advanced renal cell adenocarcinoma.
Burch, PA; Creagan, ET; Dalton, RJ; Hatfield, AK; Maples, WJ; Pfeifle, DM; Poon, MA; Schaefer, PL; Suman, VJ; Veeder, MH, 1998
)
2.03
"Cimetidine (CIM) is an H2-receptor antagonist that has been used in racehorses in an attempt to reduce the occurrence of stress-related gastric ulceration. "( Cimetidine inhibits nitric oxide associated nitrate production in a soft-tissue inflammation model in the horse.
Dees, AA; Hunter, RP; Keowen, ML; Koch, CE; McClure, JR; Short, CR; VanSteenhouse, JL, 1999
)
3.19
"Cimetidine is a histamine receptor antagonist that has been used mainly to treat peptic ulcer disease."( Oral cimetidine for the management of genital and perigenital warts in children.
Franco, I, 2000
)
1.54
"Cimetidine (Tagamet) is a potent histaminic H2-receptor antagonist, extensively prescribed for ulcers and now available without prescription. "( Cimetidine (Tagamet) is a reproductive toxicant in male rats affecting peritubular cells.
Debeljuk, L; França, LR; Leal, MC; Russell, LD; Sasso-Cerri, E; Vasconcelos, A, 2000
)
3.19
"Cimetidine is a useful medical treatment for bladder pain but the presence or absence of gastrin or histamine-like immunoreactivity does not explain its therapeutic benefit."( Cimetidine in painful bladder syndrome: a histopathological study.
Blackford, HN; Dasgupta, P; Dennis, P; Sharma, SD; Womack, C, 2001
)
3.2
"Cimetidine appears to be a useful candidate for the future development of post-irradiation radioprotectors."( Protective effects of cimetidine on radiation-induced micronuclei and apoptosis in human peripheral blood lymphocytes.
Futatsuya, R; Kojima, Y; Kondo, T; Shoji, M; Zhao, QL, 2002
)
1.35
"Cimetidine is a safe and reliable means to control bleeding from hemorrhagic gastritis."( The treatment of hemorrhagic gastritis with cimetidine.
Delaney, JP; Dunn, DH; Fischer, RC; Howard, RJ; Onstad, GR; Silvis, SE, 1978
)
1.24
"Cimetidine is a specific competitive histamine H2-receptor antagonist which effectively inhibits gastric acid secretion and is advocated for the treatment of chronic peptic ulceration, haemorrhage from erosive gastritis, and the control of gastric hypersecretion and peptic ulceration in the Zollinger-Ellison syndrome. "( Cimetidine: a review of its pharmacological properties and therapeutic efficacy in peptic ulcer disease.
Avery, GS; Brogden, RN; Heel, RC; Speight, TM, 1978
)
3.14
"Cimetidine is an H2-receptor antagonist that is capable of marked suppression of gastric acid and pepsin secretion. "( Cimetidine. H2-receptor blockade in gastrointestinal disease.
Schlippert, W, 1978
)
3.14
"Cimetidine is a histamine H2-receptor antagonist. "( [A case of acute interstitial nephritis and nonoliguria acute renal failure induced by cimetidine].
Koarada, S; Nagano, Y; Sakemi, T; Syouno, Y; Watanabe, T, 1992
)
1.95
"Cimetidine is a free radical scavenger in thermal skin injury and cobra venom-induced lung injury, and was therefore investigated as a scavenger of ethanol-induced free radicals."( Cimetidine as a scavenger of ethanol-induced free radicals.
Jayatilleke, E; Shaw, S,
)
2.3
"Cimetidine is an active H2-receptor antagonist which, combined with other drugs, has antitumor effect. "( [Antiproliferative activity of cimetidine and a copper-cimetidine complex on rat fibroblasts cultured in vitro].
Barni, S; Pippia, P; Sciola, L,
)
1.86
"Cimetidine was found to be a noncompetitive inhibitor of gastric alcohol dehydrogenase at concentrations as low as 1 mM in vitro."( Human gastric alcohol dehydrogenase: in vitro characteristics and effect of cimetidine.
Egerer, G; Oertl, U; Seitz, HK; Simanowski, UA; Waldherr, R, 1992
)
1.23
"Cimetidine is considered to be a general inhibitor of cytochrome P-450 enzymes, but there is indirect evidence that certain cytochrome P-450 enzymes are not inhibited by cimetidine. "( Selective inhibition of rat hepatic microsomal cytochrome P-450. I. Effect of the in vivo administration of cimetidine.
Bandiera, SM; Bellward, GD; Chang, T; Levine, M, 1992
)
1.94
"Cimetidine has proved to be a useful tool for investigating the hematological role of T-lymphocyte subsets in normal and pathological conditions."( Effect of cimetidine on burst-promoting activity of normal T lymphocytes.
Bessone, G; Casti, P; Moccia, F; Morra, L; Ponassi, GA, 1992
)
1.41
"Cimetidine is a commonly prescribed histamine 2-receptor antagonist used in the treatment of gastric acid-related disorders. "( Effect of cimetidine on oral digoxin absorption.
Krissman, PH; Mouser, B; Murphy, JE; Nykamp, D, 1990
)
2.12
"Cimetidine is a H-2-receptor histamine antagonist, cannitracin is an antifungal antibiotic derived from Strp-griseus and tolazoline is an alpha-adrenergic blocker similar to phentolamine."( Effects of cimetidine, progesterone, cannitracin and tolazoline on the weight and DNA content of the testosterone-induced hyperplastic prostate of the rat.
Chen, DY; Chen, W; Kang, JS; Zhou, XM, 1988
)
1.39
"Cimetidine is a potent inhibitor of antipyrine metabolism with a concentration of about 1.25 mg/liter causing a 50% decrease in the total plasma clearance of antipyrine."( Plasma concentration-response relationship for cimetidine inhibition of drug metabolism in the rat.
Aarons, L; Adedoyin, A; Houston, JB,
)
1.11
"Cimetidine seemed to be a suitable drug for treating chronic gastric ulcer, since its healing rate proved to be better than that of placebo, the gain in weight also was favourable and there were no side-effects."( Cimetidine and placebo-cimetidine in the treatment of patients with chronic gastric ulcer (a multiclinical randomized double-blind comparative study).
Deák, G; Mózsik, G; Patty, I; Tárnok, F, 1988
)
2.44
"Cimetidine is an uncompetitive inhibitor of ALP (Ki = 3.2.10(-3) M at pH 10.5), and a good inhibitor of DAO (I50 = 3.8.10(-4) M)."( Comparative inhibition of human alkaline phosphatase and diamine oxidase by bromo-levamisole, cimetidine and various derivatives.
Lalegerie, P; Lehuede, J; Metaye, T; Mettey, Y; Vierfond, JM, 1988
)
1.22
"Cimetidine functions as an H2-receptor antagonist and gastric acid secretion in the rat is inhibited temporarily."( A simple method for the oral transfer of Moniliformis moniliformis (Acanthocephala) between rats.
Crompton, DW; Stoddart, RC, 1988
)
1
"Cimetidine is a histamine H2-receptor antagonist that is used in the treatment of patients with gastric and duodenal ulcers and other hypersecretory conditions. "( Effect of cimetidine on tissue distribution of some trace elements and minerals in the rat.
Bogden, JD; Chung, HR; Naveh, Y; Weis, P, 1987
)
2.12
"Cimetidine is an H2 antagonist which inhibits cytochrome P-450 and reduces hepatic blood flow. "( The effects of cimetidine upon the plasma pharmacokinetics of doxorubicin in rabbits.
Brenner, DE; Collins, JC; Hande, KR, 1986
)
2.07
"Cimetidine is an organic cation and commonly prescribed drug that is eliminated primarily by proximal renal tubular secretion. "( Cimetidine transport in rabbit renal cortical brush-border membrane vesicles.
Kunnemann, ME; McKinney, TD, 1987
)
3.16
"Cimetidine is an H2 receptor-blocking drug frequently given to ICU patients for the prevention of stress ulcers. "( Cimetidine inhibits the hypoxia-induced increase in cerebral blood flow in dogs.
Amend, P; Clozel, JP; Hartemann, D; Saunier, C, 1985
)
3.15

Effects

Cimetidine has been reported as suppressing the excess parathyroid hormone secretion and hypercalcaemia seen in hyperparathyroidism. It has been effective in the treatment of peptic ulcer disease because of its ability to elevate gastric pH.

ExcerptReferenceRelevance
"Cimetidine has a structure that would suggest strong binding to iron ions."( Ferrous sulfate reduces cimetidine absorption.
Anderson, WD; Campbell, NR; Granberg, K; Hasinoff, BB; Meddings, JB; Robertson, S, 1993
)
1.31
"Cimetidine (CIM) has several relevant solid state forms, including four polymorphs (A, B, C and D), an amorphous form (AM) and a monohydrate (M1)."( A dynamic thermal ATR-FTIR/chemometric approach to the analysis of polymorphic interconversions. Cimetidine as a model drug.
Calvo, NL; Kaufman, TS; Maggio, RM, 2014
)
1.34
"Cimetidine has been shown to inhibit heme biosynthesis and results in symptomatic improvement in patients with acute intermittent porphyria (AIP) and porphyria cutanea tarda (PCT)."( Novel Treatment Using Cimetidine for Erythropoietic Protoporphyria in Children.
Sheu, SL; Teng, JM; Tu, JH, 2016
)
1.47
"Cimetidine has been shown to improve the performance of Scr-based GFR formulae."( Evaluating cimetidine for GFR estimation in liver transplant recipients.
Alam, A; Cantarovich, M; Davidson, A; Deschênes, M; Edwardes, MD; Tangri, N, 2010
)
1.47
"Cimetidine has been shown to have anti-metastatic activity and improves the survival of patients with colorectal cancer. "( Cimetidine inhibits the adhesion of gastric cancer cells expressing high levels of sialyl Lewis x in human vascular endothelial cells by blocking E-selectin expression.
Jiang, CG; Li, F; Li, JB; Li, YS; Liu, FR, 2011
)
3.25
"Cimetidine has been shown to play an important role in the treatment of cancer and the regulation of the immune system. "( Perioperative cimetidine administration improves systematic immune response and tumor infiltrating lymphocytes in patients with colorectal cancer.
Cao, F; Gan, M; Li, B; Wang, D; Zhu, Q,
)
1.93
"Cimetidine has been studied as an additive in cancer chemotherapy. "( Influence of cimetidine and its metabolites on Cisplatin--investigation of adduct formation by means of electrochemistry/liquid chromatography/electrospray mass spectrometry.
Brauckmann, C; Faber, H; Karst, U; Lanvers-Kaminsky, C; Sperling, M, 2013
)
2.2
"Cimetidine has been shown to improve various types of human neoplasms and more recently it has been shown to be effective in treating recalcitrant or multiple viral warts in some reports. "( Cimetidine treatment for viral warts enhances IL-2 and IFN-gamma expression but not IL-18 expression in lesional skin.
Iida, K; Kawana, S; Mitsuishi, T,
)
3.02
"Cimetidine has also been shown to have protective properties in humans and in some models of experimental injury."( Comparison of prostaglandin and cimetidine in protection of isolated gastric glands against indomethacin injury.
Brzozowski, T; Gergely, H; Hollander, D; Krause, WJ; Sekhon, S; Tarnawski, A, 2005
)
1.33
"Cimetidine has been shown to stimulate prolactin secretion after a intravenous administration. "( Comparative effect of cimetidine and ranitidine on prolactin secretion.
Nelis, GF; Van de Meene, JG, 1980
)
2.02
"Cimetidine has been shown to inhibit the liver microsomal metabolism of the benzodiazepines diazepam and chlordiazepoxide, resulting in an increase in half-life and decrease in the clearance of these two drugs. "( Diazepam-cimetidine drug interaction: a clinically significant effect.
Ruffalo, RL; Segal, JL; Thompson, JF, 1981
)
2.12
"Cimetidine has been shown not to alter the pharmacokinetics of lorazepam or oxazepam when administered concurrently with either of these benzodiazepines."( Cimetidine-benzodiazepine drug interaction.
Ruffalo, RL; Segal, J; Thompson, JF, 1981
)
2.43
"Cimetidine has been reported to decrease plasma clearance of drugs in humans and animals. "( Drug metabolism by rat and human hepatic microsomes in response to interaction with H2-receptor antagonists.
Crankshaw, DL; Holtzman, JL; Knodell, RG; Stanley, LN; Steele, NM, 1982
)
1.71
"Cimetidine has been demonstrated to impair microsomal oxidative drug metabolism in a dose-dependent manner in an animal model. "( Inhibition of microsomal drug metabolism by histamine H2-receptor antagonists studied in vivo and in vitro in rodents.
Avant, GR; Mitchell, MC; Patwardhan, RV; Schenker, S; Speeg, KV, 1982
)
1.71
"Cimetidine has been shown to impair elimination of a number of drugs metabolized by the hepatic mixed-function oxidase enzymes. "( Effects of cimetidine and ranitidine on hepatic drug metabolism.
Breen, KJ; Bury, R; Desmond, PV; Mashford, ML; Morphett, B; Shaw, RG; Westwood, B, 1982
)
2.1
"Cimetidine has been reported to decrease the biotransformation of drugs metabolized by the MFOE system. "( Cimetidine as an inhibitor of drug metabolism: therapeutic implications and review of the literature.
Bauman, JH; Kimelblatt, BJ, 1982
)
3.15
"Cimetidine also has been reported to decrease hepatic blood flow."( Review of cimetidine drug interactions.
Darvey, DL; Sorkin, EM, 1983
)
1.39
"Cimetidine has been shown to inhibit the hepatic oxidation of a number of drugs and to protect rats from acetaminophen-induced hepatic necrosis."( Selective inhibition of acetaminophen oxidation and toxicity by cimetidine and other histamine H2-receptor antagonists in vivo and in vitro in the rat and in man.
Mitchell, MC; Schenker, S; Speeg, KV, 1984
)
1.23
"Cimetidine has been shown to reduce the metabolic clearance of the benzodiazepines that are biotransformed by oxidative mechanisms."( Noninteraction of temazepam and cimetidine.
Abernethy, DR; Divoll, M; Greenblatt, DJ; Harmatz, JS; Locniskar, A; Shader, RI, 1984
)
1.27
"Cimetidine has hyperprolactinaemic properties and interferes with the peripheral activity of the sexual hormone (DHT) and probably with the pituitary LH secretion."( Endocrine effects of the H2-receptor antagonists cimetidine and ranitidine.
Barbara, L; Corinaldesi, R; Pasquali, R; Raiti, C; Stanghellini, V; Zurita, J, 1983
)
1.24
"Cimetidine has been reported to inhibit the hepatic metabolism of numerous drugs. "( Effect of cimetidine on quinidine clearance.
Fox, T; Garnett, WR; Kline, BJ; Kolb, KW; Small, RE; Vetrovec, GW, 1984
)
2.11
"Cimetidine has been shown to reduce liver blood flow, as measured by indocyanine green clearance, in normal subjects. "( Cimetidine does not reduce liver blood flow in cirrhosis.
Henderson, JM; Ibrahim, SZ; Millikan, WJ; Santi, M; Warren, WD,
)
3.02
"Cimetidine has been shown to lower circulating PTH levels effectively by causing an intraglandular rearrangement of PTH peptides in human parathyroid tissue in instances of primary hyperparathyroidism. "( The preoperative use of cimetidine as a means of preventing symptomatic hypocalcemia following a parathyroid operation.
Ackroyd, FW; Garcia, M; Minervini, D; Seiden, EF; Sherwood, JK; Willis, IH, 1983
)
2.02
"Cimetidine therapy has proved to be effective in healing most duodenal ulcers and in reducing the frequency of reulceration. "( Cimetidine. I. Developments, pharmacology, and efficacy.
Freston, JW, 1982
)
3.15
"Cimetidine has now been on the market for over three years and appears to be safe and effective. "( Cimetidine: clinical uses and possible side effects.
Babb, RR, 1980
)
3.15
"Cimetidine has been administered during 7 days to 28 patients with different degrees of renal failure. "( The effects of cimetidine (Tagamet) on renal function in patients with renal failure.
Bodemar, G; Kågedal, B; Larsson, R; Walan, A, 1980
)
2.06
"Cimetidine has substantially reduced elective peptic ulcer surgery."( Cimetidine and perforated peptic ulcer.
McArdle, CS; McKay, AJ, 1982
)
2.43
"1 Cimetidine has been reported to reduce serum calcium and parathyroid hormone (PTH) levels in primary hyperparathyroidism, but some studies have reported negative findings. "( The effects of cimetidine on serum calcium and parathyroid hormone levels in primary hyperparathyroidism.
Fisken, RA; Heath, DA; Wilkinson, R, 1982
)
1.34
"Cimetidine has recently proved useful in the prophylaxis of certain allergic and other histamine-mediated reactions. "( Cimetidine (Tagamet) combined with steroids and H1 antihistamines for the prevention of serious radiographic contrast material reactions.
Bloom, FL; Myers, GE, 1981
)
3.15
"Cimetidine has been shown to inhibit oxidative metabolism of several drugs while sparing the glucuronidation pathways of drug metabolism. "( Lack of tolerance and rapid recovery of cimetidine-inhibited chlordiazepoxide (Librium) elimination.
Johnson, RF; Patwardhan, RV; Schenker, S; Sinclair, AP; Speeg, KV, 1981
)
1.97
"Cimetidine may have been responsible for the observed complications due to its effect on serum parathyroid hormone level."( Effect of cimetidine on serum calcium levels in an elderly patient.
Edwards, H; King, TC; Zinberg, J, 1981
)
1.39
"Cimetidine has been reported as suppressing the excess parathyroid hormone secretion and hypercalcaemia seen in hyperparathyroidism. "( Failure of cimetidine to suppress immunoreactive parathyroid hormone and hypercalcaemia in primary hyperparathyroidism.
Benton, KG; Mallett, RB; Sainsbury, R, 1981
)
2.1
"Cimetidine has several actions in vivo that may result in drug-drug interactions."( Drug interactions with cimetidine.
Schwinghammer, TL, 1981
)
1.29
"Cimetidine has been effective in the treatment of peptic ulcer disease because of its ability to elevate gastric pH."( Cimetidine for the prophylaxis of potential gastric acid aspiration pneumonitis in trauma patients.
Markovchick, VJ; Moore, EE; Strain, JD; Van Duzer-Moore, S, 1981
)
2.43
"Cimetidine has demonstrated a survival benefit in a randomized trial as adjuvant therapy for gastric cancer. "( A randomized trial of cimetidine with 5-fluorouracil and folinic acid in metastatic colorectal cancer.
Adams, WJ; Clingan, PR; Legge, J; Links, M; Morris, DL; O'Baugh, J; Phadke, K; Ross, WB, 1995
)
2.05
"Cimetidine has been shown to inhibit normal and carcinoma cell growth but the mechanism of the antiproliferative action is incompletely understood. "( Inhibition of ornithine decarboxylase activity but not expression of the gene by cimetidine in intestinal mucosal cells.
Johnson, LR; McCormack, SA; Viar, MJ; Wang, JY, 1995
)
1.96
"Cimetidine has been used as a relatively selective inhibitor of renal organic cation secretion, analogous to the use of probenecid to inhibit organic anion secretion. "( Enhanced transepithelial flux of cimetidine by Madin-Darby canine kidney cells overexpressing human P-glycoprotein.
Dutt, A; Nelson, JA; Pan, BF, 1994
)
2.01
"Cimetidine has been reported to cause antiandrogenic effects in male pups of female rats receiving cimetidine during gestation. "( Development of secondary sex characteristics in male rats after fetal and perinatal cimetidine exposure.
Hoie, EB; Leuschen, MP; Nelson, RM; Swigart, SA, 1994
)
1.96
"Cimetidine has a structure that would suggest strong binding to iron ions."( Ferrous sulfate reduces cimetidine absorption.
Anderson, WD; Campbell, NR; Granberg, K; Hasinoff, BB; Meddings, JB; Robertson, S, 1993
)
1.31
"Cimetidine has been used to inhibit the secretion of creatinine in non-dialysed patients."( Time course of inulin and creatinine clearance in the interval between two haemodialysis treatments.
Arisz, L; Koomen, GC; Krediet, RT; van Acker, BA; van Olden, RW, 1995
)
1.01
"Cimetidine has been demonstrated to block histamine mediated activation of suppressor T cells in man and in animal models, resulting in an anti-tumor immune response."( [Successful treatment of metastatic renal cell carcinoma with cimetidine--report of two cases].
Kurita, T; Matsuda, H; Nagano, T; Park, YC, 1996
)
1.26
"Cimetidine has been hypothesized to exert a cancer preventive effect on the prostate due to its ability to inhibit the binding of dihydrotestosterone to androgen receptors."( Cimetidine use and risk of prostate and breast cancer.
Cushing-Haugen, KL; Rossing, MA; Scholes, D; Voigt, LF, 2000
)
2.47
"Cimetidine has been shown to induce gonadal and sexual dysfunction in men. "( Effects of the prenatal administration of cimetidine on testicular descent and genital differentiation in rats.
Kai, H; Suita, S; Takeshi, S, 2002
)
2.02
"Cimetidine 200 mg has little inhibitory effect beyond 10 hr."( Decrease of intragastric acidity in healthy subjects dosed with ranitidine 75 mg, cimetidine 200 mg, or placebo.
Hamilton, MI; Pounder, RE; Sercombe, J, 2002
)
1.26
"Cimetidine has been shown to have beneficial effects in colorectal cancer patients. "( Cimetidine increases survival of colorectal cancer patients with high levels of sialyl Lewis-X and sialyl Lewis-A epitope expression on tumour cells.
Imaeda, Y; Kobayashi, K; Matsumoto, S; Okamoto, T; Suzuki, H; Umemoto, S, 2002
)
3.2
"Cimetidine has caused dysfunction in the male reproductive system. "( In situ demonstration of both TUNEL-labeled germ cell and Sertoli cell in the cimetidine-treated rats.
Miraglia, SM; Sasso-Cerri, E, 2002
)
1.99
"Cimetidine has been shown to have low acute toxicity."( Characterization and development of cimetidine as a histamine H2-receptor antagonist.
Brimblecombe, RW; Duncan, WA; Durant, GJ; Emmett, JC; Ganellin, CR; Leslie, GB; Parsons, ME, 1978
)
1.25
"Cimetidine has no effect on nocturnal serum gastrin concentration, but, when stimulated by food, serum gastrin concentration is higher after cimetidine than after placebo."( Effect of H2-receptor antagonists on gastric acid secretion and serum gastrin concentration: a review.
Richardson, CT, 1978
)
0.98
"Cimetidine has been used only in complications, in which it has appeared very useful."( [The child's gastroduodenal ulcer (author's transl)].
Braive, JP; Hélias, JP; Salet, J,
)
0.85
"Cimetidine has been associated with gynecomastia as a side effect. "( Cimetidine is an antiandrogen in the rat.
Banks, JL; Loriaux, DL; Winters, SJ, 1979
)
3.15
"Cimetidine has no measurable affinity for rat uterine estradiol receptors, but competes for tritiated dihydrotestosterone-binding sites in mouse kidney preparations with a displacement curve parallel to that for unlabeled dihydrotestosterone."( Cimetidine, a histamine H2 receptor antagonist, occupies androgen receptors.
Funder, JW; Mercer, JE, 1979
)
2.42
"Cimetidine has proved to be of value in conservative treatment of stress induced ulcer haemorrhage and is used increasingly prophylactically."( [Cimetidine for treatment of stress-induced ulcer haemorrhage (author's transl)].
Schiessel, R; Schulz, F, 1979
)
1.89
"1. Cimetidine has no antidopaminergic activity or this hypothetic action is very slight; 2. "( Serum prolactin response to acute and chronic cimetidine administration in man.
Angelini, G; Bovo, P; Cavallini, G; Cominacini, L; Galvanini, G; Lo Cascio, V; Scuro, LA; Vaona, B, 1979
)
1.14
"Cimetidine has been shown to increase the burst-promoting activity (BPA) of uremic T lymphocytes and to partially improve the BPA of normal T lymphocytes preincubated with uremic serum."( Effect of cimetidine on peripheral blood lymphocytes from chronic uremic patients: improvement of burst-promoting activity.
Casti, P; Gurreri, G; Mela, S; Moccia, F; Morra, L; Ponassi, GA, 1992
)
1.41
"Cimetidine has been shown to increase the BPA of normal T lymphocytes, both when added to the culture and when T lymphocytes were preincubated for 1 h with it."( Effect of cimetidine on burst-promoting activity of normal T lymphocytes.
Bessone, G; Casti, P; Moccia, F; Morra, L; Ponassi, GA, 1992
)
1.41
"Cimetidine has been demonstrated to impair microsomal oxidative drug metabolizing and other enzyme systems in mouse liver. "( Interaction of H2-receptor antagonists, cimetidine and ranitidine with microsomal drug metabolizing and other systems in liver.
Gill, M; Sanyal, SN; Sareen, ML, 1991
)
1.99
"Cimetidine has been determined in the presence of its acid-induced degradation products using a second derivative (D2-) spectrophotometric method (method I) or a colorimetric method (method II). "( Spectrophotometric determination of cimetidine in the presence of its acid-induced degradation products.
Bedair, MM; Elsayed, MA; Fahmy, OT; Korany, MA, 1991
)
2
"Cimetidine-induced fever has generally been thought to be due to a direct effect on the thermoregulatory centre in the hypothalamus, on the basis of experimental studies of the injection of cimetidine to the cerebral ventricles."( IgE-mediated drug fever due to histamine H2-receptor blockers.
Hiraide, A; Ohshima, S; Yoshioka, T,
)
0.85
"Cimetidine has also been used successfully to restore immune functions in patients with malignant disorders, hypogammaglobulinemia and AIDS-related complexes."( Cimetidine as an immune response modifier.
Bernell, P; Hansson, M; Hast, R, 1989
)
2.44
"Cimetidine has been defined as a cytoprotective agent and numerous studies have reported that it is able to influence prostaglandin production as well as mechanisms which protect the surface epithelium of the gastric mucosa. "( Influence of cimetidine in low doses (less than ED50) on prostanoid production by human gastric mucosa in vitro.
Andreone, P; Baraldini, M; Bortoluzzi, F; Cursaro, C; Della Monica, A; Gasbarrini, G; Micaletti, E; Miglio, F; Saggioro, A, 1989
)
2.09
"Cimetidine has been shown to inhibit the renal secretion of tetraethyl-ammonium bromide (TEAB) but not p-aminohippuric acid (PAH), suggesting that cimetidine is secreted by an organic cation transport system [Weiner and Roth: J."( Kinetic studies on the competition between famotidine and cimetidine in rats. Evidence of multiple renal secretory systems for organic cations.
Duggan, DE; Lin, JH; Los, LE; Ulm, EH,
)
1.1
"Cimetidine has been found to be physically compatible and chemically stable in crystalline amino acid/dextrose solutions and in crystalline amino acid/dextrose/lipid admixtures."( Cimetidine and parenteral nutrition in the ICU patient.
Baptista, RJ, 1986
)
2.44
"Cimetidine has been shown to up-regulate proliferative and cytotoxic immune responses, which are mediated in part by an increase in interleukin-2 (IL-2) production. "( Cimetidine reduces cyclosporine inhibition of interleukin-2 production.
Gifford, RR; Tilberg, AF, 1988
)
3.16
"Cimetidine has been found to reduce the plasma concentrations of ketoconazole, indomethacin and chlorpromazine by reducing their absorption."( Pharmacokinetic interactions of cimetidine 1987.
Muirhead, M; Somogyi, A, 1987
)
1.28
"Cimetidine has been used in the treatment of human cancer in combination with interferon or coumarin and as a single agent."( Immunologic effects of cimetidine: potential uses.
Mavligit, GM, 1987
)
1.3
"Cimetidine has been reported to interact with liver microsomal enzymes, specifically, the cytochrome P-450 and P-448. "( Effect of cimetidine on in vivo formation of adducts between metabolites of benzo(a)pyrene and DNA.
Boroujerdi, M; Choong, MY, 1988
)
2.12
"Cimetidine has weak antiandrogenic activity in rats, but does not affect fertility in male rats at daily doses up to 950 mg/kg. "( Cimetidine does not demasculinize male rat offspring exposed in utero.
Bond, BC; Bott, JH; Walker, TF, 1987
)
3.16
"Cimetidine presumably has the ability to block androgen action."( Treatment of female androgenetic alopecia with cimetidine.
Aram, H, 1987
)
1.25
"Cimetidine has been shown to inhibit the elimination of carbamazepine after a single oral dose. "( Cimetidine and carbamazepine: a complex drug interaction.
Clark, J; Dalton, MJ; Messenheimer, JA; Powell, JR,
)
3.02
"Cimetidine has been shown to inhibit the oxidative metabolism of a variety of low- and high-extraction drugs. "( Cimetidine and ranitidine increase midazolam bioavailability.
Collier, PS; Dundee, JW; Fee, JP; Howard, PJ, 1987
)
3.16
"Cimetidine has been shown to have low acute toxicity in dogs and rodents. "( Toxicology of cimetidine.
Brimblecombe, RW; Leslie, GB; Walker, TF, 1985
)
2.07
"Cimetidine has been shown to protect against acetaminophen-mediated hepatotoxicity in both rats and mice. "( Ranitidine-acetaminophen interaction: effects on acetaminophen-induced hepatotoxicity in Fischer 344 rats.
Dent, JG; Leonard, TB; Morgan, DG,
)
1.57
"Cimetidine has been reported to decrease the apparent oral clearance of triazolam, resulting in increased triazolam plasma concentrations with the potential for exaggerated triazolam pharmacologic effects."( Central nervous system toxicity associated with concurrent use of triazolam and cimetidine.
Britton, ML; Waller, ES, 1985
)
1.22

Actions

Cimetidine produced an increase in G-17/G-34 in placebo-treated normal subjects and patients with gastric or duodenal ulcers. Cimetidine blunted this increase in all the regions of the brain except the pons and bulb.

ExcerptReferenceRelevance
"Cimetidine might inhibit δ-aminolevulinic acid synthase influencing the heme biosynthesis."( Cimetidine for erythropoietic protoporphyria.
Heerfordt, IM; Lerche, CM; Wulf, HC, 2022
)
2.89
"Cimetidine can enhance the humoral and cellular immune response induced by ROP2 protein."( [Study on immune response in BALB/c mice induced by ROP2 protein of Toxoplasma gondii with cimetidine].
Chen, XZ; Chen, Y; Liu, LL; Shen, JL; Sun, X; Yang, W; Yang, XD, 2013
)
2.05
"Cimetidine is known to cause drug-drug interactions (DDIs) with organic cations in the kidney, and a previous clinical study showed that coadministration of cimetidine or probenecid with fexofenadine (FEX) decreased its renal clearance. "( The inhibition of human multidrug and toxin extrusion 1 is involved in the drug-drug interaction caused by cimetidine.
Horita, S; Inoue, K; Kondo, T; Kusuhara, H; Maeda, K; Matsushima, S; Nakayama, H; Ohta, KY; Sugiyama, Y; Yuasa, H, 2009
)
2.01
"Cimetidine is able to inhibit OCT2-mediated uptake of cisplatin in the kidney, and subsequently ameliorate nephrotoxicity likely with minimal effect on uptake in tumor cells."( Influence of Oct1/Oct2-deficiency on cisplatin-induced changes in urinary N-acetyl-beta-D-glucosaminidase.
Filipski, KK; Franke, RM; Hu, C; Kosloske, AM; Lancaster, CS; Mathijssen, RH; Sparreboom, A; Zolk, O, 2010
)
1.8
"Cimetidine is known to suppress the growth of several tumors, including gastrointestinal cancer, in humans and animals. "( Roxatidine- and cimetidine-induced angiogenesis inhibition suppresses growth of colon cancer implants in syngeneic mice.
Izumi, K; Okabe, S; Tomita, K, 2003
)
2.11
"Cimetidine is known to enhance the survival of gastro-intestinal cancer patients, though the mechanisms involved are incompletely understood. "( The effect of H2 antagonists on proliferation and apoptosis in human colorectal cancer cell lines.
Kumar, P; Mulcahy, H; Patchett, S; Rajendra, S, 2004
)
1.77
"Thus cimetidine probably can produce a sinus bradycardia by blocking the H2-receptor site in the heart."( Electrophysiologic properties of cimetidine in man.
Gould, L; Reddy, CV; Singh, BK; Zen, B, 1981
)
1
"Cimetidine did not enhance release when present a) when basophils were "activated" but did not release histamine ("first stage"), or b) when basophils were no longer susceptible to histamine inhibition ("second stage")."( H2 antihistamines augment antigen-induced histamine release from human basophils in vitro.
Kagey-Sobotka, A; Lichtenstein, LM; Plaut, M; Tung, R, 1982
)
0.99
"Cimetidine failed to increase PRL in rats of 1 and 4 days of age."( Serotoninergic involvement in the cimetidine-induced prolactin release.
Becú, D; Libertun, C, 1983
)
1.27
"Cimetidine prevented an increase in 5-HT in the antrum and protected against ulceration."( The relationship of cimetidine to 5-hydroxytryptamine tissue levels in stress ulceration in the rat.
Max, MH; Pridjian, AK, 1983
)
1.31
"Cimetidine did not cause any change in serum gastrin concentration during and after sham feeding."( Gastric acid and serum gastrin response to sham feeding, and the effect of cimetidine on the response to sham feeding in duodenal ulcer patients.
Földvári, P; Kisfalvi, I; Szücs, K, 1983
)
1.22
"Cimetidine is shown to inhibit in vivo and in vitro the metabolism by both 3-methylcholanthrene-induced P1-450 and control forms of P-450; these data suggest that cimetidine may be acting at the level of P-450 reduction by NADPH-P-450 oxidoreductase."( Effects of cimetidine on theophylline, acetaminophen, and zoxazolamine toxicity in the intact mouse.
Bigelow, SW; Lazarte, RA; Levitt, RC; Nebert, DW, 1984
)
1.38
"Cimetidine is a rare cause of drug-induced fever. "( Cimetidine-induced fever.
Landolfo, K; Low, DE; Rogers, AG, 1984
)
3.15
"Cimetidine can cause significant changes in phenytoin serum levels which may be manifested clinically."( Effect of cimetidine on phenytoin serum levels.
Breland, BD; Jordan, JE; Mishra, SK; Salem, RB, 1983
)
1.39
"Cimetidine may cause mental confusion and should be used with caution and in reduced dosage in the presence of hepatic or renal disease, or both, and in elderly patients."( Cimetidine: clinical uses and possible side effects.
Babb, RR, 1980
)
2.43
"Cimetidine can cause impairment of metabolism of the benzodiazepines by inhibiting the hepatic microsomal enzyme system and its possible role in causing the prolonged somnolence is discussed."( Cimetidine and prolonged post-operative somnolence.
Lam, AM; Parkin, JA, 1981
)
2.43
"Cimetidine's increase of gastric pH has not been shown to result in clinically important drug-drug interactions."( Drug interactions with cimetidine.
Schwinghammer, TL, 1981
)
1.29
"Cimetidine was shown to inhibit gastric ADH with a Ki of 0.167 +/- 0.009 mmol l-1; accordingly, the pretreatment with this drug (20 mg kg-1 b.w."( Hepatic glutathione after ethanol administration in rat: effects of cimetidine and omeprazole.
Battiston, L; Marchi, P; Mazzoran, L; Moretti, M; Pozzato, G; Pussini, E; Tulissi, P, 1995
)
1.25
"Cimetidine did not inhibit the Emax in the elderly as much as it did in the young subjects."( H1- and H2-histamine receptor-mediated vasodilation varies with aging in humans.
Bedarida, G; Blaschke, TF; Bushell, E; Hoffman, BB, 1995
)
1.01
"Cimetidine did not inhibit granulocyte elastase release from activated neutrophils."( Rebamipide attenuates indomethacin-induced gastric mucosal lesion formation by inhibiting activation of leukocytes in rats.
Harada, N; Johno, M; Murakami, K; Okabe, H; Okajima, K; Takatsuki, K; Uchiba, M, 1997
)
1.02
"Cimetidine produced an increase not proportional to the dose in the systemic availability only of 4-MAA, whereas the kinetics of the other metabolites changed proportionally to the increasing dose of metamizol."( Effect of cimetidine on the pharmacokinetics of the metabolites of metamizol.
Bacracheva, N; Drenska, A; Gorantcheva, J; Schinzel, S; Scholl, T; Stoinov, A; Tchakarski, I; Tentcheva, J; Tyutyulkova, N; Vlahov, V, 1997
)
1.42
"Cimetidine did not enhance the antiproliferative effect of any of the anticancer drugs investigated."( Cimetidine enhances the antiproliferative effect of 5-fluorouracil on colon carcinoma SW620.
Kamo, N; Komatsubara, M; Miyauchi, S; Nagata, T,
)
2.3
"Cimetidine is thought to inhibit suppressor T-lymphocyte function and preliminary evidence from a randomized trial indicated that it might prolong survival for patients with operable and inoperable gastric cancer. "( Prospective, double-blind, placebo-controlled randomized trial of cimetidine in gastric cancer. British Stomach Cancer Group.
Burton, A; Dunn, JA; Fielding, JW; Hallissey, MT; Kerr, DJ; Langman, MJ; Whiting, JL, 1999
)
1.98
"Cimetidine promotes the healing of duodenal ulcer, but prolonged use (perhaps in low dosage) seems to be necessary in many cases to prevent relapse. "( Histamine H2-receptor antagonist in treatment of peptic ulcer.
Wyllie, JH, 1978
)
1.7
"Cimetidine significantly promotes healing of duodenal and gastric ulcers; this effect is especially significant in countries with low spontaneous ulcer healing."( [Cimetidine--a new principle in treating peptic lesions (author's transl)].
Arendt, R, 1979
)
1.89
"3. Cimetidine in this dose promotes healing of acute gastric erosions in the rat induced by restraint."( Effect of cimetidine on the healing of restraint-induced gastric erosions in the rat.
Clarke, AC; Lee, SP; Tasman-Jones, C,
)
1.05
"4. Cimetidine alone did not produce neuromuscular paralysis."( Influence of cimetidine on gallamine-induced neuromuscular paralysis in rats.
Mishra, Y; Ramzan, I, 1992
)
1.17
"Cimetidine might inhibit both oxidative pathways to 4OHPPL and NLA, whereas diltiazem might not inhibit the pathway to NLA."( The influence of diltiazem versus cimetidine on propranolol metabolism.
Ebihara, A; Fujimura, A; Ohashi, K; Tateishi, T, 1992
)
1.28
"Cimetidine caused an increase in the concentrations of each stereoisomer, but the difference was significant (p less than 0.05) for only the (S,R)-, (S,S)-, and (R,S)-isomers."( Labetalol pharmacokinetics and pharmacodynamics: evidence of stereoselective disposition.
Bottorff, MB; Drda, KD; Herring, VL; Lalonde, RL; O'Rear, TL; Wainer, IW, 1990
)
1
"Cimetidine inhibited the increase in gastric acid secretion, but papaverine inhibited the increases in both acid secretion and motility."( Roles of gastric acid secretion and motility in gastric mucosal lesion formation induced by water-immersion stress in rats.
Kitagawa, H; Kohei, H; Nishiwaki, H; Takeda, F, 1989
)
1
"Cimetidine may increase propranolol's blood concentrations and potentiate beta blocking effects through inhibition of hepatic microsomal enzymes and possibly through reduction of hepatic blood flow."( Effect of cimetidine and ranitidine on cardiovascular drugs.
Baciewicz, AM; Baciewicz, FA, 1989
)
1.4
"5. Cimetidine appears to produce its effect by stereoselectively inhibiting the elimination of R(+)-nicoumalone."( Cimetidine-nicoumalone interaction in man: stereochemical considerations.
Bottomley, J; Gill, TS; Gupta, SK; Hopkins, KJ; Rowland, M, 1989
)
2.23
"Cimetidine did not cause any significant changes in the pharmacokinetics of bisoprolol."( Interaction of bisoprolol with cimetidine and rifampicin.
Kirch, W; Klingmann, I; Ohnhaus, EE; Pabst, J; Rose, I, 1986
)
1.28
"Cimetidine suppress GH increase induced by baclofen."( [Growth hormone after baclofen in normal and acromegalic subjects].
Campanella, N; Carletti, P; Marchesi, GF; Morosini, PP; Nardi, B; Sarzani, R, 1985
)
0.99
"Cimetidine does not inhibit conjugation mechanisms including glucuronidation, sulphation and acetylation, or deacetylation or ethanol dehydrogenation."( Pharmacokinetic interactions of cimetidine 1987.
Muirhead, M; Somogyi, A, 1987
)
1.28
"Cimetidine failed to increase AGCs in duodenal ulcer patients after 6 weeks of treatment."( Antral gastrin concentrations in duodenal ulcer patients after cimetidine and highly selective vagotomy.
Alp, MH; Butler, RN; Gehling, N; Lawson, MJ; Rofe, SB, 1986
)
1.23
"Cimetidine did not increase the gastrin response to apomorphine in vagotomized dogs."( A long lasting gastrin response to apomorphine revealed by inhibitors of gastric acid secretion.
Brodin, K; Elwin, CE; Goiny, M; Uvnäs-Moberg, K, 1987
)
0.99
"Cimetidine did not enhance cyclosporine nephrotoxicity."( Effect of phenobarbital and cimetidine on experimental cyclosporine nephrotoxicity: preliminary observations.
Benner, KE; Bennett, WM; Houghton, DC; Sasaki, AW; Schwass, DE, 1986
)
1.29
"Cimetidine blunted this increase in all the regions of the brain except the pons and bulb."( Cimetidine inhibits the hypoxia-induced increase in cerebral blood flow in dogs.
Amend, P; Clozel, JP; Hartemann, D; Saunier, C, 1985
)
2.43
"Cimetidine produced an increase in G-17/G-34 in placebo-treated normal subjects and placebo-treated patients with gastric or duodenal ulcers, but the ratio G-17/G-34 was greater in patients with gastric ulcers than in normal subjects."( Postprandial changes in serum concentrations of gastrin-17, gastrin-34, and total gastrin in patients with duodenal or gastric ulcers and in normal subjects.
Brunet, K; Cherry, R; Chitnuyanondh, L; Kirdeikis, P; Mahachai, V; Pinchbeck, B; Sherbaniuk, R; Simpson, I; Walker, K; Zuk, L, 1985
)
0.99

Treatment

Cimetidine pretreatment significantly reversed the loss of BMCs, intestinal lining destruction, and fibrosis seen in the untreated irradiated rats. Cimetidine treatment did not improve anthelmintic efficacy of PLS in a poor drug responder mouse strain.

ExcerptReferenceRelevance
"The "cimetidine + ibuprofen"-treated mice displayed greater T-bet expression than the un-treated mice (P<0.006)."( Cimetidine and Ibuprofen Modulate T Cell Responses in a Mouse Model of Breast Cancer.
Hassan, ZM; Jafarzadeh, A; Nemati, M; Oladpour, O; Rezayati, MT; Taghipour, F; Taghipour, Z, 2022
)
2.62
"Cimetidine pretreatment significantly reversed the loss of BMCs, intestinal lining destruction, and fibrosis seen in the untreated irradiated rats and significantly decreased the underlying oxidative stress, inflammation, and Bax/Bcl2 ratio."( Cimetidine a promising radio-protective agent through modulating Bax/Bcl2 ratio: An in vivo study in male rats.
Abdel-Malek, R; Estaphan, S; Mohamed, EA; Rashed, L, 2020
)
2.72
"Cimetidine treatment did not improve anthelmintic efficacy of PLS in a poor drug responder mouse strain."( Host genetic influences on the anthelmintic efficacy of papaya-derived cysteine proteinases in mice.
Behnke, JM; Buttle, DJ; Duce, IR; Lowe, A; Luoga, W; Mansur, F; Stepek, G, 2015
)
1.14
"Cimetidine treatment significantly decreased creatinine, BUN, K, Na, SBP and creatine kinase and increased GFR and urine volume compared to group II."( A study on the effect of cimetidine and L-carnitine on myoglobinuric acute kidney injury in male rats.
Eissa, H; Elattar, S; Estaphan, S; Farouk, M; Rashed, L, 2015
)
1.44
"Cimetidine treatment in a xenograft model using ACHN renal cell carcinoma cells did not differ from vehicle control treatment, similar to the original study (Supplemental Figure 1; Sirota et al., 2011)."( Replication Study: Discovery and preclinical validation of drug indications using compendia of public gene expression data.
Aird, F; Kandela, I, 2017
)
1.18
"Cimetidine treatment completely or partially reversed all the IR-mediated changes, while ranitidine was ineffective."( Effects of cytochrome p450 inhibition by cimetidine on the warm hepatic ischemia-reperfusion injury in rats.
Mehvar, R; Shaik, IH, 2010
)
1.35
"Cimetidine-treated RBCs were optimally prepared at room temperature and needed to be tested on the day of preparation."( Immune hemolytic anemia due to cimetidine: the first example of a cimetidine antibody.
Arndt, PA; Asuncion, DJ; Brasfield, FM; Garratty, G; Vemuri, SL, 2010
)
1.37
"Cimetidine treatment decreased mucus/mucin content after 3 or 6 days of treatment. "( H2 blockers decrease gut mucus production and lead to barrier dysfunction in vitro.
Diebel, LN; Hall-Zimmerman, L; Liberati, DM, 2011
)
1.81
"In cimetidine-treated mucosa, most of the parietal cells were morphologically in the resting state, showing numerous tubulovesicles in their cytoplasm."( The cryofixation of isolated rat gastric mucosa provides new insights into the functional transformation of gastric parietal cells: an in vitro experimental model study.
Aoyama, F; Ide, S; Sawaguchi, A; Suganuma, T, 2005
)
0.84
"Cimetidine treatment decreased the number of proliferating cell nuclear antigen-positive hepatocytes and tended to enhance natural killer (NK) cell activity in splenic lymphocytes."( Anti-tumor effects of cimetidine on hepatocellular carcinomas in diethylnitrosamine-treated rats.
Adachi, K; Amano, Y; Furuta, K; Ishihara, S; Ishine, J; Kinoshita, Y; Miyake, T; Okamoto, E; Sato, S, 2008
)
1.38
"Cimetidine pretreatment failed to influence the histamine level required to elicit symptoms, hydroxyzine pretreatment significantly raised the level required to increase heart rat by 30%, and the combination of antihistamines significantly raised the threshold for histamine to elicit all the response."( Effects of infused histamine: correlation of plasma histamine levels and symptoms.
Kaliner, M; Ottesen, EA; Shelhamer, JH, 1982
)
0.99
"Cimetidine pretreatment also significantly reduced the rate of hepatic glutathione depletion."( Selective inhibition of acetaminophen oxidation and toxicity by cimetidine and other histamine H2-receptor antagonists in vivo and in vitro in the rat and in man.
Mitchell, MC; Schenker, S; Speeg, KV, 1984
)
1.23
"Cimetidine treatment was associated with a 47 per cent increase in the area under the propranolol concentration-time curve and a 17 per cent increase in elimination half-life of propranolol."( The influence of H2-receptor antagonists on steady-state concentrations of propranolol and 4-hydroxypropranolol.
Donn, KH; Eshelman, FN; Powell, JR; Rogers, JF,
)
0.85
"Cimetidine treatment caused no changes in serum calcium, phosphorus, or iPTH or in urinary cAMP (expressed as nanomoles per g creatinine)."( Cimetidine treatment of azotemic secondary hyperparathyroidism.
Heath, H; Johnson, WJ; Robinson, MF, 1982
)
2.43
"Cimetidine treatment, on the other hand, increased the ATPase activity associated with the light microsomes, and produced the heavy microsomal membranes showing only a marginal degree of the ionophore independent H+ accumulation, even though they were very similar to the carbachol-stimulated heavy membranes in the specific activity of K+-stimulated ATPase."( Effect of carbachol or histamine stimulation on rat gastric membranes enriched in (H+-K+)-ATPase.
Blakeman, DP; Fieldhouse, JM; Im, WB; Rabon, EC, 1984
)
0.99
"5 cimetidine-treated patients developed cholestasis, and 5 additional central nervous system problems."( [Ranitidine and cimetidine in the prevention of stress: ulcer hemorrhage a prospective comparative multicenter study].
Barth, HO; Berg, P; Brunner, G; Dammann, HG; Franken, FH; Friedl, W; Greiner, L; Groitl, J; Möckel, W; Müller, P, 1984
)
1.17
"Cimetidine pretreatment had no significant effect on pupil size either before or after morphine administration or on morphine pharmacokinetics."( Relationship of morphine-induced miosis to plasma concentration in normal subjects.
Fedder, IL; Ferguson, RK; Mojaverian, P; Rocci, ML; Rotmensch, HH; Swanson, BN; Vlasses, PH, 1984
)
0.99
"Cimetidine treatment also prolonged survival of mice that did succumb to metastatic disease by about 12 days."( Antimetastatic effect of cimetidine on mice bearing a C3H mouse mammary adenocarcinoma: survival and lymphocyte function studies.
Anthoons, J; Bates, T; Nias, AH; Penhaligon, M; Pilkington, D; Wolstencroft, RA,
)
1.16
"The cimetidine treated patients had more abdominal infectious complications postoperatively but this difference only reached statistical significance when patients who were operated upon for bleeding were excluded."( Does preoperative treatment with cimetidine increase the risk of postoperative infection?
Lundell, L; Persson, G, 1983
)
1.03
"Cimetidine pretreatment blocked the increase in plasma secretin concentration and pancreatic secretion in response to a meat meal and ethanol administration."( Effect of alcohol on plasma secretin concentration and pancreatic secretion in dogs.
Chey, WY; Lee, KY; Nishiwaki, H, 1984
)
0.99
"Cimetidine treatment also inhibited acidification of gastric fluid."( Influence of cimetidine on the disposition of ibuprofen in the rat.
Christensen, JM; Parrott, KA, 1984
)
1.36
"Cimetidine pretreatment with single doses of 62.5 mg/kg or 250 mg/kg had no effect on the bone marrow suppression of azathioprine at 100 mg/kg."( Hematopoietic toxicity by cimetidine. Reexamination using the antimetabolite azathioprine.
Foster, RS; Gamelli, RL; Whisnant, JK, 1983
)
1.29
"The cimetidine treated dogs demonstrated a return to normal levels within ten days following intestinal resection, p less than 0.05."( Effect of cimetidine on intestinal adaptation following massive resection of the small intestine.
Banner, BF; Haklin, MF; Roseman, DL; Saxon, AE; Tomas-de la Vega, JE, 1983
)
1.15
"Cimetidine treatment tended to increase tumor growth in normal hosts but this was statistically significant in only 1 of 3 experiments."( The effect of histamine, antihistamines, and a mast cell stabilizer on the growth of cloudman melanoma cells in DBA/2 mice.
Askenase, PW; Nordlund, JJ, 1983
)
0.99
"The cimetidine-treated group received 300 mg cimetidine orally the evening before the operation and 300 mg intramuscularly between 1 and 3 h preoperatively."( Comparison of cimetidine (Tagamet) with antacid for safety and effectiveness in reducing gastric acidity before elective cesarean section.
Coombs, DW; Gibbs, CP; Glassenberg, R; Hodgkinson, R; Joyce, TH; Ostheimer, GW, 1983
)
1.11
"Cimetidine treatment, besides healing the ulcers, also improved the endoscopic duodenitis and the symptomatic state more than placebo treatment."( The relationship between active peptic ulcer, endoscopic duodenitis and symptomatic state after treatment with cimetidine.
Danielsson, A; Ek, B; Nyhlin, H; Steen, L, 1980
)
1.19
"Cimetidine pretreatment (300 mg intravenously) inhibited histamine-induced insulin secretion by 98% or more at each point during the infusion (p < 0.05), but did not inhibit an effect of histamine to elevate plasma FFA levels."( Cimetidine blockade of histamine-induced insulin secretion.
Grund, VR; Hunninghake, DB; Martino, R, 1980
)
2.43
"The cimetidine treated group healed 17% with 58% pain relief, and the placebo treated group had no ulcers healed at 2 weeks with 60% complete pain relief."( Cimetidine vs placebo: complete gastric ulcer pain relief. Six week controlled double blind study without any antacid therapy.
Collen, MJ; Hánan, MR; Maher, JA; Rent, M; Stubrin, SE, 1980
)
2.18
"Cimetidine-treated subjects with duodenal ulcer had healing rates of 71 and 86% at 6 and 12 weeks."( Ulcer healing and relapse rates after initial treatment with cimetidine or sucralfate.
Girdwood, AH; Lucke, W; Marks, IN; Wright, JP, 1981
)
1.23
"The cimetidine-treated patients had alkaline gastric fluid with pronounced bacterial growth (4.7 +/- 0.6 x 10(4) micro-organisms/ml), whereas 18/20 untreated patients has a sterile gastric fluid."( [Influence of cimetidine on bacterial growth in gastric fluid (author's transl)].
Ducel, G; Forster, A; Intante, F; Morel, D; Niethamer, T; Pitteloud, JJ; Suter, P, 1982
)
1.11
"Cimetidine pretreatment (300 mg intravenously) inhibited histamine-elevated heart rate by 75 per cent (P less than 0.05) and histamine-decreased blood pressure by 54 per cent (P less than 0.05)."( Inhibition of histamine-stimulated increases in heart rate in man with the H2-histamine receptor antagonist cimetidine.
Grund, VR; Hunninghake, DB,
)
1.07
"In cimetidine-treated animals, there was increased retention of 99mTc-pertechnetate by the gastric wall as compared with the untreated animals."( The effect of cimetidine on blood clearance, gastric uptake, and secretion of 99mTc-pertechnetate in dogs.
Piccone, JM; Sagar, VV, 1981
)
1.14
"Cimetidine treatment could be among the factors postponing surgery of about 30,000 PU cases hospitalized in 1978, the first year of its availability."( The complex wane of peptic ulcer. I. Recent national trends in deaths and hospital care in the United States.
Wylie, CM, 1981
)
0.98
"4. Cimetidine treatment of mice prior to ingestion of OVA shows decreased tolerance, while oral administration of pepsin-treated OVA to cimetidine-treated mice leads to a complete immune unresponsiveness; this suggests an important role for gastric digestion in orally induced immune tolerance."( The influence of antigen digestion on orally induced immunity and tolerance.
Jain, SL; Michael, JG, 1995
)
0.81
"Cimetidine treatment slightly increased theophylline volume of distribution by approximately 10%, and that change also was statistically significant (P = .032)."( Controlled study of the putative interaction between famotidine and theophylline in patients with chronic obstructive pulmonary disease.
Bachmann, K; Jauregui, L; King, JD; Miller, K; Reese, JH; Schwartz, J; Scott, M; Stepanavage, M; Sullivan, TJ; Yeh, KC, 1995
)
1.01
"Cimetidine treatment prevented or reverted the increases in the three enzyme activities and in bilirubin content and the fall in proteins."( Cimetidine prevents and partially reverses CCl4-induced liver cirrhosis.
Castillo, C; Mera, E; Mourelle, M; Muriel, P,
)
2.3
"Cimetidine treatment caused irregularities in the reproductive cyclicity of mice."( Effects of cimetidine, H2 receptor antagonist, on follicular and luteal development in the mice.
Jaiswal, K; Krishna, A, 1994
)
1.4
"Cimetidine treated rats had essentially the same running pattern as controls."( Effects of preadaptation to restricted feeding and cimetidine treatment on gastric mucosal injury and wheel running during exposure to activity-stress.
Garrick, T; Morrow, NS, 1993
)
1.26
"Cimetidine pre-treatment slightly, but not significantly, increased the time for half the meal and the Gaviscon to empty from the stomach."( An investigation into the effect of cimetidine pre-treatment on raft formation of an anti-reflux agent.
Robertson, C; Washington, N; Williams, DL; Wilson, CG, 1993
)
1.28
"Cimetidine treatment resulted in a modest increase in preoperative parathyroid hormone level but did not affect any other parameter, including serum calcium level or renal tubular reabsorption of phosphate. "( Failure of cimetidine to reduce postoperative hypocalcemia in patients with primary hyperparathyroidism undergoing neck exploratory operation.
Clark, JR; Georgitis, WJ; Merenich, JA, 1993
)
2.12
"Cimetidine treatment before neck exploratory operation for PHP does not diminish the frequency or severity of postoperative hypocalcemia."( Failure of cimetidine to reduce postoperative hypocalcemia in patients with primary hyperparathyroidism undergoing neck exploratory operation.
Clark, JR; Georgitis, WJ; Merenich, JA, 1993
)
2.12
"Oral cimetidine for the treatment of verruca continues to be a topic of discussion and controversy. "( Cimetidine and a delayed hypersensitivity reaction.
Donohoe, S; Eberly, M; Evans, RD; Yoho, R, 2000
)
2.26
"The cimetidine-treated group showed 4% mucosal damage at the peak potential difference fall after aspirin, significantly less (P less than 0.02) than in the untreated subjects."( Protective effect of cimetidine on aspirin-induced gastric mucosal damage.
Baskin, WN; Ivey, KJ; Krause, WJ; MacKercher, PA, 1977
)
1.06
"The cimetidine-treated patients consumed significantly less antacids than placebo-treated patients and these patients' overall assessments of their wellbeing were significantly better."( Cimetidine in the treatment of active duodenal and prepyloric ulcers.
Bodemar, G; Walan, A, 1976
)
2.18
"Cimetidine pretreatment protected the histamine sensitivity of gastric mucosa from the irreversible blocking action of dibenamine."( Inhibitory effect of cimetidine, an antagonist of histamine H2-receptor, on gastric acid secretion in isolated frog stomach and in anesthetized young chicken.
Goto, Y; Watanabe, K, 1978
)
1.3
"Ten cimetidine-treated patients completed 12 months' treatment without suffering a recurrence of symptoms, whereas 5 of 9 placebo-treated patients suffered a symptomatic relapse after 7 to 18 weeks (P less than 0.025)."( Prophylactic effect of cimetidine in gastric ulcer patients.
Jensen, KB; Madsen, JR; Møllmann, KM; Rahbek, I; Rune, SJ; Wulff, HR, 1979
)
1.05
"The cimetidine-treated patients consumed significantly less antacids than the placebo-treated patients, and the over all assessment of their well-being was significantly better (90.9% patient satisfaction with treatment in the cimetidine group compared to 18.2% in the placebo group)."( Cimetidine in the treatment of reflux oesophagitis.
Brown, P, 1979
)
2.18
"Cimetidine treatment reduced the median healing time to approximately 12 days."( Effect of cimetidine on the healing of restraint-induced gastric erosions in the rat.
Clarke, AC; Lee, SP; Tasman-Jones, C,
)
1.26
"Cimetidine treatment (1200 mg/day) applied to 5 patients for 4 weeks did not produce any clinical or laboratory improvement."( Common variable immunodeficiency: a clinical and laboratory evaluation of 15 cases.
Hilario, MO; Leser, PG; Naspitz, CK; Soares, FJ; Solé, D,
)
0.85
"In cimetidine-pretreated animals, the cerebral blood flow was significantly elevated and the plasma and brain 5-hydroxytryptamine (serotonin) levels were slightly but significantly reduced as compared with the untreated stressed group."( Histamine modulates heat stress-induced changes in blood-brain barrier permeability, cerebral blood flow, brain oedema and serotonin levels: an experimental study in conscious young rats.
Cervos-Navarro, J; Dey, PK; Nyberg, F; Sharma, HS, 1992
)
0.8
"Cimetidine treatment resulted in a significant reduction in diltiazem oral clearance from chronic control with no effect on its systemic clearance."( The effects of chronic oral diltiazem and cimetidine dosing on the pharmacokinetics and negative dromotropic action of intravenous and oral diltiazem in the dog.
Bai, SA; Lankford, S; Maskasame, C, 1992
)
1.27
"Cimetidine treatment inhibited APND, PROD and EMND activities to a greater extent in microsomes from uninduced rats than in those from PB- or DEX-induced rats, suggesting that the induced cytochrome P-450 enzymes were less affected by cimetidine than were those in uninduced rats."( Selective inhibition of rat hepatic microsomal cytochrome P-450. I. Effect of the in vivo administration of cimetidine.
Bandiera, SM; Bellward, GD; Chang, T; Levine, M, 1992
)
1.22
"Cimetidine pretreatment (50 mg s.c."( The role of the vagus nerve in the protective action of acid inhibitors on ethanol-induced gastric mucosal damage in rats.
Chen, BW; Cho, CH; Hui, WM; Lam, SK; Ogle, CW,
)
0.85
"Cimetidine treatment had no effect on milk lipid, solid, or protein content, but at 180 mg/kg/day, caused a significant increase in milk lactose."( Excretion of high concentrations of cimetidine and ranitidine into rat milk and their effects on milk composition and mammary gland nucleic acid content.
Dostal, LA; Schwetz, BA; Weaver, RP, 1990
)
1.28
"Cimetidine treatment and the suppression of the acid-producing function of the stomach augmented enteric dysbacteriosis and H."( [The intestinal microflora and acid-forming function of the stomach in peptic ulcer patients with Helicobacter pylori bacteriosis].
Aruin, LI; Dugasheva, LG; Il'chenko, AA; Korshunova, VM; Radakova, ED; Zhukhovitskiĭ, VG, 1991
)
1
"The cimetidine treatment increased mean pH and reduced the number of spikes but did not affect emptying rates."( Sucralfate versus cimetidine in reflux oesophagitis. The effect on oesophageal pH and motility.
Elsborg, L; Jørgensen, F, 1991
)
1.1
"Cimetidine-treated group consisted of 15, famotidine-treated group of 18, ranitidine-treated group of 19, and antacid-treated group of 5 patients."( Comparative efficacy of cimetidine, famotidine, ranitidine, and mylanta in postoperative stress ulcers. Gastric pH control and ulcer prevention in patients undergoing coronary artery bypass graft surgery.
Castellano, J; Lamothe, PH; Lemole, GM; McNicholas, KW; Rao, E; Serra, AJ; Woronick, CL, 1991
)
1.31
"1. Cimetidine pretreatment of male Sprague-Dawley rats caused a significant increase in the specific content of total hepatic cytochrome P-450, supporting the hypothesis that this H2-receptor antagonist has monooxygenase induction effects. "( Cimetidine: an inhibitor and an inducer of rat liver microsomal cytochrome P-450.
Reilly, PE; Winzor, DJ; Wright, AW, 1991
)
2.35
"(v) Cimetidine pretreatment (30 min) followed by EtOH did not significantly reduce plasma volume, stomach weight, or the gross hemorrhagic lesions compared to EtOH alone, but (vi) misoprostol pretreatment followed by EtOH significantly protected against hemorrhagic lesions and elevated tissue plasma volumes."( Effects of misoprostol, cimetidine, and ethanol on rat gastric plasma volume and morphology.
Hund, P; Lacy, ER; Tietge, J, 1990
)
1.07
"Cimetidine pretreatment resulted in prolongation of cyclophosphamide's half-life from 24.3 +/- 7.3 to 33.5 +/- 9.5 min (mean +/- SD; P = 0.036) but did not significantly alter the AUC0-8 h for the latter drug."( The effect of cimetidine on cyclophosphamide metabolism in rabbits.
Anthony, LB; Hande, KR; Long, QC; Struck, RF, 1990
)
1.36
"More cimetidine-treated patients (35 of 82, 43%) than placebo-treated patients (26 of 79, 33%) had healed ulcers after 4 weeks of therapy."( Acute treatment of benign gastric ulcer with once-daily bedtime dosing of cimetidine compared with placebo.
Frank, WO; Karlstadt, R; Mounce, W; O'Connell, S; Palmer, R; Rockhold, F; Young, MD, 1989
)
0.96
"Cimetidine treatment shortened the median interval until the first decrease in pain, the median interval until the complete resolution of pain and promoted faster complete healing of skin lesions than symptomatic treatment."( Cimetidine as an immunomodulator in the treatment of herpes zoster.
Harel, D; Lahat, N; Laor, A; Miller, A, 1989
)
2.44
"Cimetidine treatment was associated with an initial moderate increase in locomotor activity which was increased significantly as a function of time."( Behavioral and metabolic aspects of cimetidine-ethanol interaction.
Messiha, FS,
)
1.13
"With Cimetidine pretreatment the risk of aspiration and pneumonitis may be prevented."( Usefulness of acid and gastric juice secretion decreasing action of cimetidine in anaesthesia for the prevention of aspiration.
Takács, G, 1989
)
0.97
"4. Cimetidine treatment had no effect (P greater than 0.05) on the time-averaged percent unbound in plasma of R(-)-ibuprofen (C 0.419 +/- 0.051% vs T 0.435 +/- 0.060%) and S(+)-ibuprofen (C 0.643 +/- 0.093% vs T 0.633 +/- 0.053%)."( Lack of effect of cimetidine on the pharmacokinetics of R(-)- and S(+)-ibuprofen.
Evans, AM; Nation, RL; Sansom, LN, 1989
)
1.12
"Cimetidine pretreatment inhibited theobromine 3-demethylation and AMMU formation resulting in a 27% decrease in ClTB in the combined smoker/nonsmoker group."( Influence of cimetidine, sulfinpyrazone, and cigarette smoking on theobromine metabolism in man.
Attwood, J; Birkett, DJ; Miners, JO; Wing, LM,
)
1.22
"The cimetidine-treated group demonstrated a statistically significant decrease in clearance of bupivacaine."( Effects of H-2 antagonists on the elimination of bupivacaine.
Dundas, CR; Noble, DW; Smith, KJ, 1987
)
0.75
"Cimetidine pretreatment decreased PX plasma clearance by 30%."( Paraxanthine metabolism in humans: determination of metabolic partial clearances and effects of allopurinol and cimetidine.
Birkett, DJ; Kjellen, G; Lelo, A; Miners, JO, 1989
)
1.21
"Cimetidine treatment of animals in which suppressor cells were induced resulted in an inability of these mice to transfer cellular suppression as measured by development of a normal immunologic response in the recipient mice."( Inhibition of suppressor cell function by cimetidine in a murine model.
Cleveland, RP; Jin, ZW; Kaufman, DB; Kumar, A; Murray, DL, 1986
)
1.26
"Cimetidine treatment of mice who had also received suppressor cells eliminated the manifestation of suppressor cell activity as measured by the development of normal immunologic response following contact sensitization with DNFB."( "Immunoregulatory effects of cimetidine: inhibition of suppressor cell effector function in vivo".
Cleveland, RP; Kumar, A, 1988
)
1.29
"Cimetidine pretreatment had no effect on either baseline FEV1 or on baseline histamine PC20 (p = 0.461)."( A new role for histamine H2-receptors in asthmatic airways.
Jackson, PJ; Manning, PJ; O'Byrne, PM, 1988
)
1
"Cimetidine pretreatment failed to modify the prolactin rise in this case."( Central histaminergic effect on basal and opioid-induced prolactin secretion.
Antunes-Rodrigues, J; Castro-e-Silva, E, 1988
)
1
"Cimetidine pretreatment reduced the bioavailability of oral melphalan by approximately 30% (P less than 0.05)."( Interaction of cimetidine with oral melphalan. A pharmacokinetic study.
Bateman, DN; Proctor, SJ; Robinson, A; Sviland, L, 1987
)
1.35
"Cimetidine treatment of DU patients did not change the PGE2 action, while the degree of stimulation by histamine was reduced."( Morphologically different biopsy specimens of the human gastric mucosa. II. Adenylate cyclase activity in response to prostaglandin E2 and histamine.
Leyhe, T; Pfaff, G; Rettenmaier, G; Ruoff, HJ; Schmid, E, 1986
)
0.99
"Cimetidine treatment was successful for seven years but dose reduction was followed by intractable hemorrhage which did not respond to H2-receptor antagonists."( Long term management of hemorrhagic esophagitis with cimetidine and omeprazole.
Bonnin, M; Hetzel, DJ, 1986
)
1.24
"The cimetidine treatment induced a partial abrogation of the immunosuppressive effect of Cytoxan as manifested by a significant decline in the volume of the XGVHR from 115.23 +/- 15.72 mm3 (positive control) to 67.3 +/- 11.41 mm3 (P less than 0.01)."( Abrogation of the local xenogeneic graft versus host reaction by preinjection of cimetidine to the immunosuppressed host rats: an experimental model for testing preclinical immunorestorative activity in vivo.
Chu, DT; Mavligit, GM; Wong, WL, 1987
)
0.98
"Cimetidine treatment resulted in a significant increase in plasma testosterone levels which was not found in the ranitidine group."( A comparative study of the effects of ranitidine and cimetidine on carbohydrate tolerance, growth hormone secretion and the hypothalamic-pituitary-gonadal axis in man.
Amphlett, G; Barnes, GD; Hoad, J; Lowry, C; Riley, AJ; Saunders, J; Scobie, IN; Sonksen, PH; Wheeler, MJ, 1986
)
1.24
"Cimetidine treatment enhanced both metronidazole (at 1, 2 and 3 hrs) and tinidazole (only at 1 hr) concentrations in plasma, but this shift was not reflected in the 24-hr urine recoveries of the intact nitroimidazoles."( Effect of enzyme induction and inhibition on the fate of metronidazole and tinidazole in the rat.
Haataja, H; Männistö, PT; Saijonmaa, O, 1987
)
0.99
"Cimetidine treatment significantly promoted the healing of duodenal ulcers and gastric ulcers with extensive acid secreting areas when compared with placebo, but not of the gastric ulcers without extensive acid secreting areas."( Effects of cimetidine on the healing and recurrence of duodenal ulcers and gastric ulcers.
Iishi, H; Okuda, S; Tatsuta, M, 1986
)
1.38
"Cimetidine-treated cultures closed faster and had greater cell proliferation than controls."( Wound healing properties of cimetidine in vitro.
Hanson, VA; Mohamed, S; Nadijcka, MD, 1986
)
1.29
"The cimetidine-treated spleen cells acquired the capacity to lyse the KK cells on day 14."( Effects of cimetidine on tumor growth and immune function in nude mice bearing human ovarian carcinoma.
Kato, K; Kikuchi, Y; Kizawa, I; Oomori, K, 1985
)
1.14
"Cimetidine treatment resulted in significantly more rapid healing than placebo; after 2 and 6 weeks of therapy, 10.0% and 44.8% of patients receiving placebo were healed, as compared to 22.6% and 65.1% receiving cimetidine."( Healing of benign gastric ulcer: comparison of cimetidine and placebo in the United States.
Achord, JL; Akdamar, K; Belsito, AA; Dyck, WP; Englert, E; Graham, DY; Kornfield, RN; Long, WB; Strickland, RG; Vlahcevic, ZR, 1985
)
1.25
"Cimetidine treatment results in redistribution of HDL subfractions in favour of HDL2."( The effect of cimetidine and ranitidine on serum high density lipoprotein subfractions.
Champion, MC; Ooi, TC; Peden, NR; Simo, EI, 1985
)
1.35
"Cimetidine maintenance treatment has no effect on sexual activity, the quality of seminal fluid or the pituitary secretion of gonadotropins or prolactin."( Long-term treatment with cimetidine does not essentially affect the hypothalamic-pituitary-gonadal axis in man.
Barattini, G; Bianchi Porro, G; Petrillo, M; Ragni, G; Ruspa, M, 1985
)
1.29
"Cimetidine treatment was associated with increases of 26 and 18% in carbamazepine area under the concentration-time curve (AUC) and elimination half-life, respectively."( The influence of cimetidine on single-dose carbamazepine pharmacokinetics.
Dalton, MJ; Messenheimer, JA; Powell, JR,
)
1.19
"Cimetidine pretreatment elevated phenylbutazone plasma concentrations during the first 8 h after phenylbutazone administration."( Effects of oral cimetidine on plasma concentrations of phenylbutazone in horses.
Blythe, LL; Christensen, JM; Craig, AM, 1985
)
1.34
"A treatment with cimetidine appears to be an excellent therapeutic option in children with Erythropoietic protoporphyria."( Erythropoietic protoporphyria: case reports for clinical and therapeutic hints.
Berti, I; Burlo, F; De Martino, E; Marchini, S; Pastore, S; Severini, GM; Tommasini, A; Tumminelli, C; Zanon, D, 2023
)
1.24
"Treatment with Cimetidine increased the frequency of CD8+ T cells in the patient's peripheral blood."( Cimetidine effects on the immunosuppression induced by burn injury.
Barough, MS; Hassan, ZM; Kokhaei, P, 2014
)
2.18
"Treatment with cimetidine shifted the concentration-response curve of histamine to the right in the presence of diphenhydramine."( Histamine-induced modulation of vascular tone in the isolated chicken basilar artery: a possible involvement of endothelium.
Miyamoto, A; Obi, T; Okuno, T; Shiraishi, M; Yabuki, A, 2008
)
0.69
"Treatment with cimetidine or ranitidine markedly inhibited suppressor T cell activity in a dose-related manner and enhanced the contact sensitivity response to DNFB."( Inhibition of T suppressor cell expression by histamine type 2 (H2) receptor antagonists.
Alessi, S; Badger, AM; Griswold, DE; Hanna, N; Poste, G, 1984
)
0.61
"Treatment with cimetidine (1 mg kg-1) or dimaprit (1 mg kg-1) did not influence the response capacity to antigen challenge in IgG1- type animals."( Changes in bronchial anaphylactic reactivity induced in guinea-pigs by long-term treatment with histamine H2-agents.
Andersson, P; Bergstrand, H, 1984
)
0.61
"Treatment with cimetidine, but not ranitidine, was associated with a significant increase in the proportion of peripheral blood lymphocytes responding to this optimal mitogenic stimulation."( Mitogen stimulation of peripheral blood lymphocytes of duodenal ulcer patients during treatment with cimetidine or ranitidine.
Beck, JS; Boyd, EJ; Brown, RA; Gibbs, JH; Peden, NR; Potts, RC; Robertson, AJ; Wormsley, KG, 1982
)
0.82
"Treatment with cimetidine in patients with asymptomatic chronic DU disease, reduced gastric acidity to the same level as after highly selective vagotomy (HSV), but increased plasma noradrenaline concentrations insignificantly."( Is there a relationship between gastric acid secretion and plasma catecholamines in duodenal ulcer disease?
Farnebo, LO; Graffner, H; Hamberger, B; Järhult, J, 1983
)
0.61
"Treatment with cimetidine was associated with an increase in pH of gastric aspirate during treatment and increased numbers of bacteria were isolated from the gastric aspirate during treatment, while the pH and bacterial flora of gastric aspirate did not change during tripotassium dicitrato bismuthate treatment."( Effects of tripotassium dicitrato bismuthate (TDB) tablets or cimetidine in the treatment of duodenal ulcer.
Axon, AT; Hamilton, I; O'Connor, HJ; Worsley, BW, 1983
)
0.85
"Treatment with cimetidine did not lead to an increased incidence of rejection of the allograft."( Effect of cimetidine on upper gastrointestinal bleeding after renal transplantation: a prospective study.
Christensen, U; Dahlager Jørgensen, JI; Kjersem, H; Løkkegaard, H; Stadil, F; Thorup Andersen, J; Walter, S, 1984
)
1.01
"Pretreatment with cimetidine for 4 weeks (1000 mg daily) led to increased peak plasma concentrations of 5FU and also area under the plasma concentration-time curve (AUC)."( The influence of cimetidine on the pharmacokinetics of 5-fluorouracil.
Clark, PI; Dilloway, MR; Harvey, VJ; Johnston, A; Lant, AF; Slevin, ML, 1984
)
0.93
"Pretreatment with cimetidine was found to increase both the rate and extent of absorption of ibuprofen."( Influence of cimetidine on the disposition of ibuprofen in the rat.
Christensen, JM; Parrott, KA, 1984
)
0.96
"Treatment with cimetidine resulted in healing of the ulcer, without recurrence and marked amelioration of the cutaneous symptoms of mastocytosis."( Long-term treatment of systemic mastocytosis with histamine H2 receptor antagonists.
Blumenthal, M; Gilbert, HS; Johnson, GJ; Roitman, B; Silvis, SE, 1980
)
0.6
"Pretreatment with cimetidine (H2 receptor antagonism) was necessary to avoid unpleasant side effects of histamine."( Histamine provocation of clinical coronary artery spasm: implications concerning pathogenesis of variant angina pectoris.
Baim, DS; Bristow, MR; Ginsburg, R; Harrison, DC; Kantrowitz, N, 1981
)
0.59
"Treatment with cimetidine potentiated these pharmacodynamic changes, but failed to achieve significant differences from quinidine alone."( Effect of cimetidine on the pharmacokinetics and pharmacodynamics of quinidine.
Golden, L; Hardy, BG; Lalka, D; Schentag, JJ; Zador, IT, 1983
)
1.01
"Treatment with cimetidine 400 mg at bedtime or twice daily for up to 12 months very significantly reduced recurrence of symptomatic ulceration."( Cimetidine treatment for the prevention of recurrence of duodenal ulcer: an international collaborative study.
Beresford, J; Burland, WL; Hawkins, BW, 1980
)
2.04
"Treatment with cimetidine of patients with renal failure may invalidate measurements of serum creatinine and creatinine clearance as standard routine tests for glomerular filtration rate."( The effects of cimetidine (Tagamet) on renal function in patients with renal failure.
Bodemar, G; Kågedal, B; Larsson, R; Walan, A, 1980
)
0.95
"Treatment with cimetidine for 6 weeks resulted in a significant improvement in symptoms and in the endoscopic appearance of the duodenitis when compared to treatment with placebo."( Cimetidine in the management of symptomatic patients with duodenitis: a double-blind controlled trial.
Mackinnon, M; Whitehead, R; Willing, RL, 1982
)
2.05
"Treatment with cimetidine (1000 mg daily in four divided doses) was given for 3--30 weeks to 10 patients with primary hyperparathyroidism (HPT). "( Treatment with cimetidine in patients with primary hyperparathyroidism.
Akerström, G; Johansson, H; Ljunghall, S; Rudberg, C; Selking, O; Wide, L, 1982
)
0.97
"When treated with cimetidine asthmatic patients displayed significantly more bronchospasm at T than with placebo (p less than 0.035)."( Histamine blocking agents in healthy and asthmatic subjects.
Brown, S; Gerstenhaber, B; Lach, E; Schachter, EN, 1982
)
0.59
"Treatment with cimetidine failed in three patients (25%) who were submitted to selective vagotomy and their ulcers healed."( [Cimetidine in the treatment of postoperative peptic ulcer].
de Mello, JB; Ladeia, JC; Navarro, AM; Peixoto, LD; Rajab, I; Tolói Júnior, N,
)
1.38
"Treatment with cimetidine has produced satisfactory control of his symptoms for 16 months, and is an acceptable alternative to total gastrectomy in childhood."( Zollinger-Ellison syndrome in a child: medical treatment with cimetidine.
Atwell, JD; Drake, DP; Maciver, AG, 1980
)
0.84
"Pre-treatment with Cimetidine did not change the basal levels of hepatic GSH, but after oral ethanol load, the decrease of the hepatic GSH content was significantly (p < 0.005) more pronounced than in controls."( Hepatic glutathione determination after ethanol administration in rat: evidence of the first-pass metabolism of ethanol.
Battiston, L; Lunazzi, G; Marchi, P; Mazzoran, L; Micheli, L; Moretti, M; Pozzato, G; Tulissi, P, 1995
)
0.61
"Rats treated with cimetidine had less mucosal injury but had no increased survival when compared to rats injected with the vehicle."( Effects of preadaptation to restricted feeding and cimetidine treatment on gastric mucosal injury and wheel running during exposure to activity-stress.
Garrick, T; Morrow, NS, 1993
)
0.86
"Pretreatment with cimetidine blocked HCl and pepsinogen responses to carbachol but did not affect responses to forskolin."( Nonparallel secretion of pepsinogen and acid by gastric oxyntopeptic cells of the toad (Bufo marinus).
Abad, MJ; Acosta, A; Michelangeli, F; Ruiz, MC, 1993
)
0.61
"Treatment with cimetidine attenuated the sustained relaxation, whereas chlorpheniramine or indomethacin depressed the phasic relaxation."( Histamine actions in dog retinal central arteries as compared to those in middle cerebral and temporal arteries.
Kani, K; Kitamura, Y; Okamura, T; Toda, N, 1995
)
0.63
"Pretreatment with cimetidine (20 micrograms/rat, ICV) prevented the dimaprit-induced changes in SS binding in the frontoparietal cortex, whereas cimetidine alone (20 micrograms/rat, ICV) had no observable effect on this parameter."( Effect of dimaprit and cimetidine on the somatostatinergic system in the rat frontoparietal cortex.
Arilla, E; Puebla, L, 1996
)
0.93
"Treatment with cimetidine locally may be of some value to relieve the clinical symptoms of allergic rhinitis."( The effect of the H2 antagonist cimetidine on the numbers of CD4+ and CD8+ cells in the nasal mucosa of patients with allergic rhinitis.
Fan, DS; Liu, T; Yang, PC; Zhang, TY, 1997
)
0.92
"Treatment of cimetidine did not affect cellular uptake of cisplatin."( Role of cytochrome P-450 as a source of catalytic iron in cisplatin-induced nephrotoxicity.
Baliga, M; Baliga, R; Shah, SV; Ueda, N; Zhang, Z, 1998
)
0.65
"Pretreatment with cimetidine showed a marked protection against this decline in polyamine contents at both the doses tested (37.5 mg kg-1 and 75 mg kg-1) and increased the contents of spermidine and spermine above the control values."( Effect of ulceration on rat gastric tissue polyamine contents in response to different procedures; inhibition of these effects by cimetidine.
Al-shabanah, OA; Raza, M, 1999
)
0.83
"Pretreatment with cimetidine caused a significant reduction in gastric mucosal injury in stressed animals receiving gastric mucosal barrier breakers."( Cimetidine protects against stress-induced gastric injury augmented by mucosal barrier breakers.
Levine, BA; Pruitt, BA; Sirinek, KR, 1979
)
2.03
"Oral treatment with cimetidine, 450 mg/dog/day in three divided doses for 14 days, produced a remarkable acceleration of healing of duodenal ulcers but exerted little influence on gastric ulcers."( Effects of cimetidine on healing of chronic gastric and duodenal ulcers in dogs.
Murata, T; Okabe, S; Takeuchi, K; Urushidani, T, 1978
)
0.96
"2. Treatment with cimetidine in doses of 100 mg/kg 8-hourly during a 24 h period of restraint prevented the development of acute gastric ulceration in the rat."( Prevention of acute gastric ulceration in the rat by cimetidine, a histamine H2-receptor antagonist.
Lee, SP; Tasman-Jones, C,
)
0.7
"Pretreatment with cimetidine (a histamine H2 receptor antagonist) significantly thwarted the increases in the brain water content and the blood-brain barrier permeability."( Histamine modulates heat stress-induced changes in blood-brain barrier permeability, cerebral blood flow, brain oedema and serotonin levels: an experimental study in conscious young rats.
Cervos-Navarro, J; Dey, PK; Nyberg, F; Sharma, HS, 1992
)
0.61
"Treatment with cimetidine reduced circadian and nocturnal (but not diurnal) intragastric acidity significantly, as compared to both placebo and antacid treatment."( Comparison of low-dose antacids, cimetidine, and placebo on 24-hour intragastric acidity in healthy volunteers.
Berstad, A; Osnes, M; Weberg, R, 1992
)
0.9
"Treatment with cimetidine (H2 receptor antagonist) resulted in diarrhea, however, the addition of cyproheptadine (H1 receptor antagonist) was beneficial in amelioration of the cutaneous symptoms of mastocytosis."( Systemic mastocytosis treated with histamine H1 and H2 receptor antagonists.
Falk, ES; Gasior-Chrzan, B, 1992
)
0.62
"Treatment with cimetidine (CAS 51481-61-9) at a dose of 50 mg/kg (twice a day for 3 days) did not affect either the development or the healing of the compound 48/80-induced gastric lesions."( Effect of cimetidine on the mucosal hydroxyproline content of rat gastric lesions induced by compound 48/80.
Arisawa, T; Goto, H; Hase, S; Kuroiwa, M; Ohara, A; Segawa, K; Sugiyama, S; Suzuki, T; Tsuchida, T; Tsukamoto, Y, 1991
)
1.02
"Pretreatment with cimetidine 15, 25 and 50 mg/kg/day i.p."( Effects of cimetidine on drug metabolism in rat pups.
Ikediobi, CO; Kwanashie, HO; Osuide, G; Wambebe, C,
)
0.84
"Treatment with cimetidine, 800 mg u.i.d., for 6-12 weeks was efficacious in the majority of patients with reflux esophagitis grade I-III."( Efficacy of different doses of cimetidine in the treatment of reflux esophagitis. A review of three large, double-blind, controlled trials.
Nicolai, JJ; Reman, FC; Tytgat, GN, 1990
)
0.9
"Treatment with cimetidine caused the remission of cutaneous manifestations and the extracutaneous abnormalities, such as nailfold capillary disturbances and the presence of antithyroid antibodies, improved."( Treatment with cimetidine of atypical fasciitis panniculitis syndrome.
Abrahamson, JE; Boss, JH; Misselevitch, I; Naschitz, JE; Rosner, I; Yeshurun, D, 1990
)
0.97
"Treatment with cimetidine during the induction but not the elicitation of allergic contact hypersensitivity (ACH) produced a significant enhancement of the response throughout the first 48 h."( Cimetidine-induced augmentation of allergic contact hypersensitivity reactions in mice.
Belsito, DV; Kerdel, FA; Potozkin, J; Soter, NA, 1990
)
2.06
"Treatment with cimetidine plus diphenhydramine prevented the endotoxin-induced blood pressure fall, increase in heart rate, and hypoglycemia; increased the 24-hr survival rate from 10 to 60%; and inhibited the small intestinal pathology found in control rats."( The effects of H1 and H2 histamine receptor antagonists on the development of endotoxemia in the conscious, unrestrained rat.
Brackett, DJ; Schaefer, CF; Wilson, MF, 1985
)
0.61
"Treatment with cimetidine of the patient with excessive suppressor activity led to an improvement in his clinical state, reduction in suppressor activity, temporary effect on his proliferative response capacity to mitogens, and an increase in the antigen-specific helper activity."( Common variable immunodeficiency: a family study and therapeutic trial with cimetidine.
Brautbar, C; Dayan, M; Epstein, N; Michalevitch, R; Moses, E; Peller, S; Segal, R; Zecler, E, 1989
)
0.85
"Treatment with cimetidine (50 mg/kg, i.p.) did not prevent compound 48/80-induced gastric lesions."( Fluctuation of the mucosal hydroxyproline content in compound 48/80-induced gastric lesions in rats.
Arisawa, T; Goto, H; Hase, S; Kawabe, Y; Kuroiwa, M; Nakazawa, S; Osada, T; Segawa, K; Tsuchida, T; Tsukamoto, Y, 1989
)
0.62
"Pretreatment with cimetidine did not influence the magnitude of increase in GST concentration."( Preoperative cimetidine does not prevent subclinical halothane hepatotoxicity in man.
Beckett, GJ; Drummond, GB; Howie, AF; Ray, DC, 1989
)
0.97
"Treatment with cimetidine at high doses, either before or after inhalation injury, did not protect the animals from formation of pulmonary edema."( Effect of high-dose cimetidine on pulmonary extravascular water after acute smoke inhalation injury.
Matsubara, G; Santibanez, AS; Stewart, RJ; Yamaguchi, KT,
)
0.79
"Pretreatment with cimetidine (300 mg iv) depressed the drinking response to histamine to 30 +/- 10 ml and to pentagastrin to 58 +/- 24 ml."( Water drinking induced by gastric secretagogues in pigs.
Houpt, TR; Troy, DW; Weixler, LC, 1986
)
0.59
"Treatment with cimetidine or ranitidine (another H2-receptor antagonist) for 5 days induced a marked decrease in basal plasma TSH concentrations (P less than 0.01), with no changes in pituitary concentrations of TSH."( Effects of histamine H1- and H2-receptor antagonists on thyrotrophin secretion in the rat.
Ulloa, ER; Zaninovich, AA, 1986
)
0.61
"Treatment C, cimetidine 300 mg orally four times daily for 4 days and Treatment D, ranitidine 150 mg orally twice daily for 4 days were administered in a randomized, crossover fashion."( The paradoxical effect of cimetidine and ranitidine on glibenclamide pharmacokinetics and pharmacodynamics.
Antal, EJ; Juhl, RP; Kubacka, RT, 1987
)
0.93
"Treatment with cimetidine potentiated contraction in the strips with intact and damaged endothelium to a similar extent and attenuated relaxation."( Mechanism of histamine actions in human coronary arteries.
Toda, N, 1987
)
0.61
"When treatment with cimetidine was initiated after completion of chemotherapy, the depressed IL-2 production was restored to the level of control patients with benign ovarian tumor."( Effects of cimetidine on interleukin-2 production by peripheral blood lymphocytes in advanced ovarian carcinoma.
Iwano, I; Kato, K; Kikuchi, Y; Kita, T; Kizawa, I; Miyauchi, M; Oomori, K, 1988
)
0.98
"Treatment with cimetidine reduced the hepatic cytosolic androgen receptor content compared with ranitidine treatment."( Effect of an antiandrogenic H2 receptor antagonist on hepatic regeneration in rats.
Chapchap, P; Eagon, PK; Kahn, D; Makowka, L; Podesta, L; Starzl, TE; Svanas, GW; Van Thiel, DH, 1988
)
0.61
"Treatment with cimetidine four days after immunization or one day before assay led to a slight decline in PFC level."( Enhancement of anti-sheep erythrocyte plaque-forming cell levels by cimetidine in vivo.
Cleveland, RP; Kumar, A, 1987
)
0.85
"Treatment with cimetidine also causes an increase in the plasma testosterone level without modifying the plasma values of LH and prolactin."( Antiprostatic effect of cimetidine in rats.
Cavallaro, R; Caviezel, F; Cocchi, D; Colombo, R; Faravelli, R; Galmozzi, G; Pinelli, P; Trivulzio, S, 1987
)
0.92
"Pretreatment with Cimetidine did not increase the enzyme concentrations further."( Exocrine pancreatic substitution: facts and controversies.
Worning, H, 1986
)
0.59
"Treatment with cimetidine did not affect the clinical condition of the dogs, but was associated with a slightly less rapid weight gain."( Safety evaluation of cimetidine: report at the termination of a seven-year study in dogs.
Crean, GP; Leslie, GB; Roe, FJ; Walker, TF; Whitehead, SM, 1987
)
0.93
"Pretreatment with cimetidine resulted in a significant, dose-dependent decrease in the CD50 of lidocaine, whereas ranitidine pretreatment did not significantly alter the lidocaine CD50."( Effects of cimetidine and ranitidine on local anesthetic central nervous system toxicity in mice.
Kim, KC; Tasch, MD, 1986
)
0.98
"Pretreatment with cimetidine (histamine H2-receptor antagonist, 40 mg/kg i.p.) had no effect on these plasma variables."( Increase of plasma renin activity after subcutaneous application of compound 48/80 in the rat.
Aoki, T; Ho, S; Izumi, H; Michelakis, AM, 1985
)
0.59
"Treatment with cimetidine resulted in healing of ulcer craters in 68.5 per cent but resolution of the duodenitis was observed in only 28.1 per cent.(ABSTRACT TRUNCATED AT 250 WORDS)"( Duodenitis: a clinical, endoscopic and histopathologic study.
Sircus, W, 1985
)
0.61

Toxicity

Danish Committee on Adverse Drug Reactions received 494 reports concerning a total of 612 suspected adverse reactions to peptic ulcer drugs. In terms of safety, a greater number of patients receiving cimetidine reported adverse clinical experiences than those receiving famotidine.

ExcerptReferenceRelevance
"Our review of published material, manufacturer's files, and submissions to the United States Food and Drug Administration indicates that cimetidine is safe for short term use (up to 8 weeks)."( Safety of cimetidine.
Kruss, DM; Littman, A, 1978
)
0.86
" Most of the early excess in mortality was attributable to cimetidine being given in the late stages of many diseases, often to counter adverse gastric effects of other drugs."( Postmarketing surveillance of the safety of cimetidine: 10 year mortality report.
Colin-Jones, DG; Langman, MJ; Lawson, DH; Logan, RF; Paterson, KR; Vessey, MP, 1992
)
0.79
" The pattern of adverse events reported during long-term treatment was similar to the adverse-event profile in short-term treatment with omeprazole (n = 2,818), ranitidine (n = 1,572) and cimetidine (n = 891)."( Safety experience from long-term treatment with omeprazole.
Joelson, IB; Joelson, S; Lundborg, P; Walan, A; Wallander, MA, 1992
)
0.47
"During the period from the first marketing of cimetidine in 1977 and until 31 March 1990, the Danish Committee on Adverse Drug Reactions received 494 reports concerning a total of 612 suspected adverse reactions to peptic ulcer drugs (ATC group A02B)."( [Adverse effects of ulcer drugs before and after release of cimetidine, ranitidine and sucralfate for over-the-counter sale].
Andersen, M; Schou, JS, 1991
)
0.78
"Reports of adverse drug reactions due to histamine H2-receptor antagonists (H2RAs) are rare considering their wide usage."( Overview of the safety profile of the H2-receptor antagonists.
Hansten, PD, 1990
)
0.28
" The authors report increased serum clozapine levels and adverse side effects during clozapine and cimetidine treatment but not during clozapine and ranitidine treatment in a patient with chronic paranoid schizophrenia."( A case report of cimetidine-induced clozapine toxicity.
Cooper, T; Lieberman, JA; Masiar, S; Picou, D; Szymanski, S, 1991
)
0.84
" Therefore, pretreatment with cimetidine, a potent P450 cytochrome system inhibitor, might be expected to prevent the toxic conversion."( Failure of cimetidine to affect phalloidin toxicity.
Michelson, EA; Schneider, SM; Vanscoy, G, 1991
)
0.96
" As part of the study, cimetidine (800 mg daily) was administered during RT to relieve and prevent adverse reactions of the gastrointestinal tract caused by RT."( Radiation therapy of the para-aortic lymph nodes in carcinoma of the uterine cervix: the concurrent use of cimetidine to reduce acute and subacute side effects from radiation.
Chatani, M; Hishikawa, Y; Ikeda, H; Inoue, T; Kamikonya, N; Matayoshi, Y; Nishiyama, K; Tanaka, S; Teshima, T,
)
0.66
" Both p-HPPH and m-HPPH were much less developmentally toxic than DPH."( Use of Frog Embryo Teratogenesis Assay-Xenopus and an exogenous metabolic activation system to evaluate the developmental toxicity of diphenylhydantoin.
Bantle, JA; Fort, DJ, 1990
)
0.28
" In terms of safety, a greater number of patients receiving cimetidine reported adverse clinical experiences than those receiving famotidine and a greater number of cimetidine patients had to be withdrawn from the study when compared with famotidine patients."( Safety and acid-suppressant properties of histamine2-receptor antagonists for the prevention of stress-related mucosal damage in critical care patients.
Carter, CA; Schentag, JJ; Welage, LS, 1989
)
0.52
" The incidence of serious adverse events reported in comparative short-term studies with H2-receptor antagonists and placebo were similar."( The clinical safety of omeprazole.
Sölvell, L, 1989
)
0.28
" Haematological adverse effects are relatively uncommon and most have been reported in cases of cimetidine administration."( Haematological adverse effects of histamine H2-receptor antagonists.
Aymard, B; Aymard, JP; Bannwarth, B; Netter, P; Streiff, F; Trechot, P,
)
0.35
" The multiple sources of confounding factors, and their high prevalence, make it impossible to detect adverse events which mimic ordinary disease, particularly when a consistent relationship between adverse event and drug exposure is not observed."( Review: post-marketing surveillance of the safety of cimetidine--the problems of data interpretation.
Jones, DG; Langman, MJ; Lawson, DH; Vessey, MP, 1987
)
0.52
" Safety studies, including haematological and biochemical testing over the whole period, revealed no previously unknown adverse reaction."( Six years of continuous cimetidine treatment in peptic ulcer disease: efficacy and safety. Anglo-Irish Cimetidine Long-Term Study Group.
Bardhan, KD, 1988
)
0.58
" Patients recorded their drug compliance, antacid use, ulcer symptoms, and adverse experiences daily."( Enprostil and cimetidine: comparative efficacy and safety in patients with duodenal ulcer.
Almström, C; Carling, L; Cronstedt, J; Ekström, P; Hägg, S; Hansson, B; Unge, P, 1987
)
0.63
"Gastrointestinal symptoms have been the most frequently reported adverse experiences in the misoprostol (Cytotec) studies of both patients with peptic ulcer disease, and healthy subjects."( Focus on misoprostol: review of worldwide safety data.
Wildeman, RA, 1987
)
0.27
" We conclude that smoking adversely affects duodenal ulcer healing by cimetidine and hastens subsequent relapse, and that sucralfate overcomes the adverse effect of smoking on healing as encountered with cimetidine, and results in a subsequent remission period double that of cimetidine."( Sucralfate overcomes adverse effect of cigarette smoking on duodenal ulcer healing and prolongs subsequent remission.
Branicki, FJ; Choi, TK; Fok, PJ; Hui, WM; Lai, CL; Lam, SK; Lau, WY; Lok, AS; Ng, MM; Poon, GP, 1987
)
0.51
" There were no toxic effects on the gastric mucosa of any dog."( Safety evaluation of cimetidine: report at the termination of a seven-year study in dogs.
Crean, GP; Leslie, GB; Roe, FJ; Walker, TF; Whitehead, SM, 1987
)
0.59
" Even patients in the moderate category experienced no life-threatening toxic manifestations."( Cimetidine toxicity: an assessment of 881 cases.
Krenzelok, EP; Lippold, KP; Litovitz, T; McNally, CF, 1987
)
1.72
" If phenobarbital protects from cyclosporine nephrotoxicity because of its enzyme inducing action, it would follow that the parent drug and not a toxic metabolite mediates renal dysfunction."( Effect of phenobarbital and cimetidine on experimental cyclosporine nephrotoxicity: preliminary observations.
Benner, KE; Bennett, WM; Houghton, DC; Sasaki, AW; Schwass, DE, 1986
)
0.57
" We assessed the effects of these drugs on the acute toxicity of parathion in rats by measuring the rate of survival at 24 h after the administration of the oral LD50 of parathion to four groups of rats: control and pretreated with the aforementioned drugs."( Cimetidine enhances and phenobarbital decreases parathion toxicity.
Amezcua, JL; Girón, E; Martinez-Tabche, L; Mourelle, M, 1986
)
1.71
" According to median lethalities, all three known carcinogens were substantially more toxic than nitrosocimetidine whether administered by the intravenous, intraperitoneal, or oral routes."( Comparison of the acute toxicity of N-nitrosocimetidine with three structurally related carcinogens in the rat.
Hard, GC; Jensen, DE; Magee, PN; Ogiu, T, 1986
)
0.75
" A side effect encountered was sinus tachycardia in 4 of 27 patients treated with pirenzepine."( [Prevention of gastroduodenal stress lesions with secretion inhibitors in accident patients needing intensive care: incidence of lesions and adverse effects; consequences].
Barandun, J; Frutiger, A; Kobler, E; Leutenegger, A; Rüedi, T, 1985
)
0.27
" Since some patients with peptic ulcer disease or gastric hyperacidity on mexiletine may benefit from the addition of cimetidine, it was important to rule out any significant adverse interaction between the two drugs in such patients."( Usefulness and safety of cimetidine in patients receiving mexiletine for ventricular arrhythmia.
Klein, AL; Sami, MH, 1985
)
0.78
" The 12 month report noted that cimetidine was being given, knowingly or unknowingly, in the late stages of many diseases and also to counter the adverse gastric effects of other drugs used in the treatment of serious disorders."( Postmarketing surveillance of the safety of cimetidine: mortality during second, third, and fourth years of follow up.
Colin-Jones, DG; Langman, MJ; Lawson, DH; Vessey, MP, 1985
)
0.81
" The scheme successfully detected and quantified some already known adverse effects of cimetidine and did not detect any new effects."( Post-marketing surveillance of the safety of cimetidine: twelve-month morbidity report.
Colin Jones, DG; Langman, MJ; Lawson, DH; Vessey, MP, 1985
)
0.75
" Ranitidine administration (50 mg per kg) enhanced acetaminophen hepatotoxicity throughout the toxic dose range of acetaminophen (600 to 1,000 mg per kg) and potentiation of acetaminophen hepatotoxicity by ranitidine was dose-dependent."( Ranitidine-acetaminophen interaction: effects on acetaminophen-induced hepatotoxicity in Fischer 344 rats.
Dent, JG; Leonard, TB; Morgan, DG,
)
0.13
" The inhibition cannot be explained either by a direct toxic effect on effector cells or by blocking of Fc receptors."( Effect of histamine receptor blocking on human antibody-dependent cell-mediated cytotoxicity.
Gergely, P; Láng, I; Nékám, K; Petrányi, G; Török, K, 1981
)
0.26
" The inhibition cannot be explained either by a direct toxic effect on natural killer (NK) cells or by blocking of Fc receptors."( Effect of histamine-receptor blocking on human spontaneous lymphocyte-mediated cytotoxicity.
Gergely, P; Láng, I; Petrányi, G, 1981
)
0.26
"Worldwide clinical experience has shown the short-term use of H2-blockers is safe and effective."( H2-blockers: how safe and how effective?
Spiro, HM, 1983
)
0.27
" In this model, liver injury is caused by toxic intermediates formed during metabolism of halothane by a reductive pathway."( Effects of cimetidine and ranitidine on halothane metabolism and hepatotoxicity in an animal model.
Cousins, MJ; Hall, PD; Jenner, MA; Plummer, JL; Wanwimolruk, S,
)
0.52
" So far as can be assessed, however, none of these drug-disease associations represented adverse effects of cimetidine treatment; on the contrary, they resulted from cimetidine being used, knowingly or unknowingly, for treating the symptoms of various diseases or for alleviating adverse effects of other agents such as corticosteroids, non-steroidal anti-inflammatory drugs, and radiotherapy."( Postmarketing surveillance of the safety of cimetidine: 12 month mortality report.
Colin-Jones, DG; Langman, MJ; Lawson, DH; Vessey, MP, 1983
)
0.74
"Cimetidine-related neurotoxicity may be characterized by signs of affective dysfunction, toxic delusional state and/or delirium, confusion and/or amnestic signs, coma, epileptic phenomena and focal neurological signs."( Cimetidine neurotoxicity. EEG and behaviour aspects.
Kamphuisen, HA; Van Sweden, B, 1984
)
3.15
" Except for one volunteer who complained of anxiety, weakness and sweating on the 6th day of cimetidine/metoprolol administration, no adverse effects could be observed during the combination therapy with cimetidine and the beta blockers or in monotherapy with beta blockers."( Accumulation and adverse effects of metoprolol and propranolol after concurrent administration of cimetidine.
Kirch, W; Köhler, H; Mutschler, E; Spahn, H, 1983
)
0.7
" Since toxic effects of cimetidine are likely to occur within 1 to 2 days of starting the medication, close observation during this time period, and prompt recognition of psychotoxicity, can prevent disruptive side effects."( Cimetidine psychotoxicity without significant medical illness: case report.
Giller, EL; Harkness, LL, 1983
)
2.02
" In an animal model used to assess the effect of cimetidine on acetaminophen toxicity, the LD50 of acetaminophen alone in Charles River CD-1 mice was 480 mg/kg (95% confidence interval: 436-528 mg/kg)."( Differential effect of cimetidine on drug oxidation (antipyrine and diazepam) vs. conjugation (acetaminophen and lorazepam): prevention of acetaminophen toxicity by cimetidine.
Abernethy, DR; Ameer, B; Divoll, M; Greenblatt, DJ; Shader, RI, 1983
)
0.83
" No serious adverse effects have been caused by this locally-acting agent."( Pharmacology, clinical efficacy, and adverse effects of sucralfate, a nonsystemic agent for peptic ulcer.
Spiro, HM,
)
0.13
"Cimetidine has now been on the market for over three years and appears to be safe and effective."( Cimetidine: clinical uses and possible side effects.
Babb, RR, 1980
)
3.15
" As with virtually all drugs used in the practice of medicine, cimetidine is not without its adverse effects."( A consideration of the adverse effects of cimetidine.
McGuigan, JE, 1981
)
0.77
" Adverse reactions reported secondary to cimetidine during its investigational period and shortly after marketing were minimal."( Cimetidine: adverse reactions and acute toxicity.
Conner, CS; Sawyer, D; Scalley, R, 1981
)
1.97
" The lack of significant adverse effects has revealed a degree of tolerability that, to write a review of the adverse effects, poses a difficult task."( A comparative overview of the adverse effects of antiulcer drugs.
Piper, DW, 1995
)
0.29
" The incidence and type of adverse events were similar in the two age groups."( Association of age with the efficacy and safety of ranitidine and cimetidine in acute duodenal ulcer disease.
Dixon, JS; Ehsanullah, RS; Mills, JG; Wood, JR, 1993
)
0.52
" The use of such therapies, however, may be impeded by a number of major disadvantages, including reduced patient compliance, the incidence of adverse events and primary or acquired antibiotic resistance."( Compliance, adverse events and antibiotic resistance in Helicobacter pylori treatment.
Malfertheiner, P, 1993
)
0.29
"The extensive use of selective histamine H2 receptor antagonists provides a unique opportunity to describe very rare adverse drug reactions."( Nephrotoxicity and hepatotoxicity of histamine H2 receptor antagonists.
Fisher, AA; Le Couteur, DG, 2001
)
0.31
" Compound III was less toxic than the other DHC derivatives in both cell cultures."( Derivatives of dehydrocrotonin, a diterpene lactone isolated from Croton cajucara: cytotoxicity in rat cultured hepatocytes and in V79 cells.
Durán, N; Haun, M; Melo, PS, 2002
)
0.31
" Milonine was less toxic than warifteine in both cell cultures."( Warifteine and milonine, alkaloids isolated from Cissampelos sympodialis Eichl: cytotoxicity on rat hepatocyte culture and in V79 cells.
Barbosa-Filho, JM; de Fátima Formiga Melo Diniz, M; de Medeiros Cavalcante, HM; de Medeiros, IA; Haun, M; Melo, PS, 2003
)
0.32
" The primary constituent, R-(+)-pulegone, is metabolized via hepatic cytochrome P450 to toxic intermediates."( Mitigation of pennyroyal oil hepatotoxicity in the mouse.
Bond, GR; Goetz, RJ; Lindsell, CJ; Otten, EJ; Sztajnkrycer, MD, 2003
)
0.32
" Diosgenin and its derivatives were more toxic in V79 fibroblasts (IC50 40-300 microM) than in hepatocytes (IC50 280-1000 microM)."( Cytotoxicity of the phytosterol diosgenin and its derivatives in rat cultured hepatocytes and V79 fibroblasts.
De Azevedo, MB; Fabrin-Neto, JB; Haun, M; Melo, PS; Zullo, MA, 2004
)
0.32
" It appears that once daily, short-term use of piroxicam alone and in combination with cimetidine in cats is relatively safe based on the parameters evaluated in this study."( Multiple dose pharmacokinetics and acute safety of piroxicam and cimetidine in the cat.
Chun, R; Corse, M; Garrett, L; Heeb, HL; Hunter, RP; Koch, DE; Moore, L; Pellerin, MA; Radlinsky, M, 2005
)
0.79
" There was no clinically significant adverse event in both groups."( Efficacy and safety of ecabet sodium on functional dyspepsia: a prospective, double-blinded, randomized, multi-center controlled trial.
Choi, SR; Hahm, KB; Kim, JJ; Kim, N; Kim, SK; Lee, DH; Lee, EH; Lee, JH; Lee, ST; Park, JJ; Rhee, JC, 2006
)
0.33
" In the present article, the adverse effects of PPIs are reviewed, with special emphasis on those related to their continued administration and on the special circumstances of patients, as in the case of the elderly, those with liver failure, pregnant and breastfeeding mothers and children."( [Safety of proton pump inhibitors].
Esplugues, JV; Martí-Cabrera, M; Ponce, J, 2006
)
0.33
" Their detection in the environment and their bioactivity have resulted in concern for potential adverse effects on non-target species."( Aquatic toxicity of acetaminophen, carbamazepine, cimetidine, diltiazem and six major sulfonamides, and their potential ecological risks in Korea.
Choi, K; Jung, J; Kim, PG; Kim, Y; Park, J; Park, S, 2007
)
0.59
" Furthermore, the use of antidotes that reduced the toxic insult was also recorded using this technique."( Acute liver acetaminophen toxicity in rabbits and the use of antidotes: a metabonomic approach in serum.
Galanopoulou, P; Giannioti, K; Liapi, C; Mikros, E; Papalois, A; Theocharis, S; Zira, A, 2009
)
0.35
" An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential toxic effects early in the drug development process and aid in avoiding such problems."( Developing structure-activity relationships for the prediction of hepatotoxicity.
Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ, 2010
)
0.36
"The serotonin toxicity (ST) is a potentially life-threatening adverse drug reaction results from therapeutic drug use, intentional self-poisoning, or inadvertent interactions between drugs."( Serotonin toxicity: a short review of the literature and two case reports involving citalopram.
Bruno, G; Canevelli, M; Lenzi, GL; Piacentini, E; Pietracupa, S; Talarico, G; Tosto, G, 2011
)
0.37
"The aim of the present work was to clarify the involvement of free radicals, cytochrome P450 toxic metabolites, and deregulation of calcium homeostasis in the mechanism of diethyldithiocarbamate (DDC) hepatotoxicity."( The protective effects of ascorbic acid, cimetidine, and nifedipine on diethyldithiocarbamate-induced hepatic toxicity in albino rats.
Badawy, MM; Gaafa, KM; Hamza, AA, 2011
)
0.64
"Ototoxicity is a dose-limiting side effect of chemotherapeutic treatment with cisplatin."( Cisplatin ototoxicity in rat cochlear organotypic cultures.
Allman, BL; Ding, D; He, J; Jiang, H; Salvi, RJ; Seigel, GM; Yu, D, 2011
)
0.37

Pharmacokinetics

Ranitidine may be used at doses of up to 300 mg twice daily in the healing of duodenal ulcers. The interaction of nifedipine and cimetidine is of clinical significance because of its pharmacodynamic effect.

ExcerptReferenceRelevance
"The plasma concentration curve after a single oral dose of cimetidine 200 mg was followed in 27 patients with varying degrees of chronic renal failure (creatinine clearance 1--52 ml/min) and in 46 patients with normal serum creatinine."( Oral absorption of cimetidine and its clearance in patients with renal failure.
Bodemar, G; Larsson, R; Norlander, B, 1979
)
0.83
" On average, the Cmax then is approximately 300 ng/ml, which is achieved rapidly within 30 min after drug intake."( Pharmacokinetic profile of nicorandil in humans: an overview.
Frydman, A, 1992
)
0.28
" Due to a short elimination half-life and wide therapeutic index, dosage adjustments are not necessary in patients exhibiting moderate renal dysfunction."( Pharmacokinetics of cefaclor AF: effects of age, antacids and H2-receptor antagonists.
Cerimele, BJ; Coleman, DL; DeSante, KA; Hatcher, BL; Kisicki, J; Satterwhite, JH, 1992
)
0.28
" Pharmacokinetic analyses showed that cimetidine did not affect the rate or extent of temafloxacin absorption, as evidenced by unchanged peak plasma concentration, time to peak plasma concentration, and terminal-phase volume of distribution."( Effect of cimetidine on the pharmacokinetics of temafloxacin.
Granneman, GR; Locke, C; Sörgel, F; Stephan, U, 1992
)
0.96
"The effect of Chinese herbal medicines (Huan Shao Tan and Pu Chung Yi Chi Tang) and western drugs (sodium phenobarbital and cimetidine) on the serum concentration and pharmacokinetic parameters of theophylline and cytochrome P-450 of Sprague-Dawley (SD) rats of three different ages were examined."( Effect of traditional Chinese herbal medicines on the pharmacokinetics of western drugs in Sprague-Dawley rats of different ages (II): Aminophylline-huan shao tan and aminophylline-pu chung yi chi tang.
Chen, SM; Hou, SJ; Lin, SY; Perng, RI; Young, TK, 1992
)
0.49
"A program adapted for use on microcomputers (DCN) has been developed which permits one to perform operations of numerical convolution and deconvolution using polyexponential functions, that are often implemented in pharmacokinetic analysis."( A computer program (DCN) for numerical convolution and deconvolution of pharmacokinetic functions.
Domínguez-Gil, A; Lanao, JM; Sayalero, ML; Vicente, MT, 1992
)
0.28
" The changes in the pharmacokinetic parameters were not accompanied by discernible haemodynamic effects or any change in the tolerability of nimodipine."( Influence of the H2-receptor antagonists cimetidine and ranitidine on the pharmacokinetics of nimodipine in healthy volunteers.
Kuhlmann, J; Mück, W; Rämsch, KD; Seiberling, M; Wingender, W; Woelke, E, 1992
)
0.55
"The influence of usual regimens of the H2 blocking drugs, cimetidine, ranitidine, and nizatidine on the steady-state plasma concentrations and pharmacokinetic characteristics of theophylline was studied in seventeen patients with chronic obstructive pulmonary disease (COPD)."( Comparative investigation of the influence of nizatidine, ranitidine, and cimetidine on the steady-state pharmacokinetics of theophylline in COPD patients.
Bachmann, K; Jauregui, L; Levine, L; Martin, M; Mauro, LS; Sullivan, TJ, 1992
)
0.76
"Theophylline pharmacokinetic parameters after each treatment were determined by model independent pharmacokinetic analysis."( Effect of the addition of ciprofloxacin on theophylline pharmacokinetics in subjects inhibited by cimetidine.
Davis, RL; Kelly, HW; Powell, JR; Quenzer, RW, 1992
)
0.5
"When administered alone, ciprofloxacin and cimetidine caused a significant increase in theophylline elimination half-life and a decrease in clearance."( Effect of the addition of ciprofloxacin on theophylline pharmacokinetics in subjects inhibited by cimetidine.
Davis, RL; Kelly, HW; Powell, JR; Quenzer, RW, 1992
)
0.76
" A pharmacokinetic model incorporating discontinuous absorption was developed to simulate concentration-time profiles with double peaks."( Use of a pharmacokinetic model incorporating discontinuous gastrointestinal absorption to examine the occurrence of double peaks in oral concentration-time profiles.
Brouwer, KL; Pollack, GM; Suttle, AB, 1992
)
0.28
" Mean pirmenol concentration-time curves and pharmacokinetic parameters, including elimination rate constant, were not significantly altered by concomitant administration of cimetidine."( Effect of cimetidine administration on the pharmacokinetics of pirmenol.
Bockbrader, HN; Cetnarowski-Cropp, AB; Chang, T; Goldfarb, AL; Lebsack, ME; Radulovic, LL; Sedman, AJ; Stringer, KA, 1992
)
0.88
" On this day, subjects began taking diazepam (10 mg) orally for one week, with pharmacokinetic studies performed at day 8, when steady state levels of diazepam were reached."( Effect of orally administered misoprostol and cimetidine on the steady state pharmacokinetics of diazepam and nordiazepam in human volunteers.
Andrade, GN; Lima, DR; Santos, RM; Werneck, E,
)
0.39
"6 l h-1 and 89 vs 50 l, respectively), whereas no significant difference in half-life could be demonstrated."( Stereoselective pharmacokinetics of disopyramide and interaction with cimetidine.
Angelo, HR; Bonde, J; Kampmann, JP; Nygaard, E; Pedersen, LE; Ramsing, T, 1991
)
0.52
" Only a minor difference in theophylline half-life between control and continuous cimetidine infusion (7."( Theophylline pharmacokinetics: effect of continuous versus intermittent cimetidine i.v. infusion.
Gaska, JA; Rocci, ML; Tietze, KJ; Vlasses, PH, 1991
)
0.74
" A stochastic modeling approach is presented that is more general than pharmacokinetic models typically employed in stochastic approaches."( Stochastic interpretation of linear pharmacokinetics: a linear system analysis approach.
Veng-Pedersen, P, 1991
)
0.28
"Ranitidine may be used at doses of up to 300 mg twice daily in the healing of duodenal ulcers, and this study investigated the potential for a pharmacokinetic or pharmacodynamic interaction between nifedipine 10 mg three times daily and ranitidine 300 mg twice daily compared with cimetidine 800 mg daily and placebo in a randomised crossover study in 18 healthy male subjects."( The pharmacokinetics and pharmacodynamics of nifedipine at steady state during concomitant administration of cimetidine or high dose ranitidine.
Dixon, JS; Khan, A; Langley, SJ; Mullins, FG; Toon, S, 1991
)
0.67
" Gastric secretion inhibition over the 90 min of IGT correlated with peak concentration exclusively for the subpopulation with peak occurrence at T 150."( [Plasma pharmacokinetics of roxatidine in the healthy man: correlation with gastric antisecretory effect].
Bonfils, S; Chen, WW; Kolsky, H; Lewin, MJ, 1990
)
0.28
" Pharmacokinetic and pharmacodynamic evaluations did not show significant interactions with cimetidine following alpidem 50 mg administration."( Effect of cimetidine on the pharmacodynamics, pharmacokinetics and biotransformation of a single oral dose of alpidem.
Bianchetti, G; Desager, JP; Harvengt, C; Hulhoven, R, 1990
)
0.9
" Co-administration of cimetidine significantly increased Cmax (27%) and AUC (44%) and prolonged the half-life (30%) of cifenline."( The effects of cimetidine and ranitidine on the pharmacokinetics of cifenline.
Aogaichi, K; Defeo, TM; Liguori, J; Massarella, JW; Passe, S, 1991
)
0.95
" This first evidence of labetalol stereoselective disposition is consistent with the findings of previous (R,R)-labetalol pharmacokinetic studies and with previous pharmacodynamic investigations of labetalol and (R,R)-labetalol."( Labetalol pharmacokinetics and pharmacodynamics: evidence of stereoselective disposition.
Bottorff, MB; Drda, KD; Herring, VL; Lalonde, RL; O'Rear, TL; Wainer, IW, 1990
)
0.28
"kg, a half-life of 16."( The effect of liver dysfunction on colchicine pharmacokinetics in the rat.
Bay, MK; Johnson, RF; Leighton, JA; Maldonado, AL; Schenker, S; Speeg, KV, 1990
)
0.28
" The elimination half-life of moricizine is 2 to 6 hours, but its duration of antiarrhythmic action is much longer suggesting active metabolites."( Clinical pharmacokinetics of moricizine.
Barbey, JT; Schwartz, SL; Siddoway, LA; Woosley, RL, 1990
)
0.28
"Amlodipine, a dihydropyridine calcium antagonist, was synthesized in an attempt to develop a compound with a pharmacokinetic profile characteristic of this class, which would also have an increased oral bioavailability and extended clearance time."( The pharmacokinetic profile of amlodipine.
Abernethy, DR, 1989
)
0.28
" After pretreatment with cimetidine, the plasma clearances (CL) of AP and TMO were significantly lower and the elimination half-life (t1/2) of AP was significantly increased."( The effect of roxatidine acetate and cimetidine on hepatic drug clearance assessed by simultaneous administration of three model substrates.
Nakamura, K; Tanaka, E, 1989
)
0.85
"The effects of a new H2-receptor antagonist, roxatidine acetate, have been investigated in both clinical and pharmacodynamic trials in Europe and the United States."( Safety and efficacy of roxatidine acetate. Evidence from pharmacodynamic and clinical trials.
Bender, W; Labs, R; Merki, HS, 1989
)
0.28
"1 L/kg), and terminal half-life (11."( Pharmacokinetics and pharmacodynamics of dilevalol.
Affrime, MB; Bottorff, MB; Given, BD; Kramer, WG; Lalonde, RL; Patrick, JE; Tenero, DM, 1989
)
0.28
" Pharmacokinetic absorption behavior of a sustained-release preparation of theophylline after repetitive oral administration was adequately evaluated using MFA-MULTI."( Pharmacokinetic analysis of single- or multiple-dose plasma drug concentration data with a microcomputer using multi-fraction absorption models.
Murata, K; Noda, K; Samejima, M; Tagawa, K, 1989
)
0.28
"We have studied the mechanisms of the increased dosage requirements of the H2-receptor antagonist cimetidine in paediatric burned patients in a pharmacokinetic and pharmacodynamic study."( Alteration by burn injury of the pharmacokinetics and pharmacodynamics of cimetidine in children.
Greenblatt, DJ; Hagen, J; Hoaglin, DC; Martyn, JA, 1989
)
0.72
" The pharmacokinetic analysis revealed a slower resorption of cimetidine in the patients who had taken the drug in the evening (Tmax = 2 h, resp."( [Chronopharmacokinetics of the preparation biomet400 in patients with duodenal ulcer].
Belovezhdov, N; Kostova, N; Maleev, A; Skrinska, E; Terziivanov, D, 1989
)
0.52
"The influence of cimetidine on piroxicam plasma levels and pharmacokinetic parameters was studied in both rats and healthy volunteers."( Influence of cimetidine on the pharmacokinetics of piroxicam in rat and man.
Foda, AM; Said, SA, 1989
)
0.99
" Concomitant famotidine administration did not alter any of the pharmacokinetic parameters of theophylline (AUC0- infinity; 38."( Cimetidine versus famotidine: the effect on the pharmacokinetics of theophylline in rats.
Ferguson, RK; Mojaverian, P; Rocci, ML; Saccar, CL; Vlasses, PH,
)
1.57
" Moreover, for triazolam, the C max was increased and the plasma elimination half-life was prolonged; oral clearance of the two triazolobenzodiazepines was markedly reduced."( Pharmacokinetic consequences of long term coadministration of cimetidine and triazolobenzodiazepines, alprazolam and triazolam, in healthy subjects.
Desager, JP; Harvengt, C; Hulhoven, R; Pourbaix, S; Smith, RB, 1985
)
0.51
"82 ml/min/kg) and prolonged elimination half-life (29 vs."( Bromazepam pharmacokinetics: influence of age, gender, oral contraceptives, cimetidine, and propranolol.
Burstein, ES; Friedman, H; Greenblatt, DJ; Harmatz, JS; Locniskar, A; Ochs, HR; Shader, RI, 1987
)
0.5
" Both drugs have a similar pharmacokinetic profile."( Pharmacokinetics and pharmacodynamics of oral nizatidine.
Matsumoto, C; McMahon, FG; Offen, WW; Regel, G; Ryan, J; Vargas, R, 1988
)
0.27
" Similarly, the H2 receptor antagonists did not alter the plasma bupivacaine against time curves, half-life or bupivacaine clearance in the three groups studied."( H2 antagonists and bupivacaine clearance.
Brighouse, D; Morgan, B; O'Sullivan, GM; Reynolds, F; Smith, M, 1988
)
0.27
"The reciprocal effects on pharmacokinetic parameters after a single oral dose of the nonsteroidal antiinflammatory drugs (NSAIDs) indomethacin and sulindac and repeated oral doses of the H2-receptor antagonists cimetidine and ranitidine were determined in two groups of nine healthy subjects each (indomethacin and sulindac groups)."( Pharmacokinetic interactions between NSAIDs (indomethacin or sulindac) and H2-receptor antagonists (cimetidine or ranitidine) in human volunteers.
Abel, L; Carbon, C; Delhotal-Landes, B; Flouvat, B; Liote, F; Meyer, P; Vinceneux, P, 1988
)
0.68
" The terminal half-life and renal clearance of tocainide were not altered by either H2-receptor antagonists, compared with placebo."( The effect of histamine-2 receptor antagonists on tocainide pharmacokinetics.
Kapil, RP; Lalonde, RL; Mattern, AL; North, DS, 1988
)
0.27
"The effects of cimetidine (single or repeated administration) on free unchanged captopril plasma levels, pharmacokinetic parameters and plasma converting enzyme inhibitory effects have been investigated in normal healthy volunteers."( Cimetidine does not alter free unchanged captopril pharmacokinetics and biological effects in healthy volunteer.
Bah, M; Cadilhac, M; Giudicelli, JF; Richer, C; Thuillez, C,
)
1.93
" The possibility of a pharmacokinetic interaction between the H2-receptor antagonist cimetidine and the long-acting local anaesthetic agent bupivacaine was studied in seven healthy, non-smoking volunteers."( Lack of effect of cimetidine on the pharmacokinetics of bupivacaine in healthy subjects.
Jantunen, ME; Lindberg, RL; Pihlajamäki, KK, 1988
)
0.83
" A pharmacokinetic and pharmacodynamic study was performed on the third day at each dose."( Influence of repeated administration of cimetidine on the pharmacokinetics and pharmacodynamics of adinazolam in healthy subjects.
Cox, S; Desager, JP; Harvengt, C; Hulhoven, R, 1988
)
0.54
"The number of studies on drug interactions with cimetidine has increased at a rapid rate over the past 5 years, with many of the interactions being solely pharmacokinetic in origin."( Pharmacokinetic interactions of cimetidine 1987.
Muirhead, M; Somogyi, A, 1987
)
0.81
"The potential effect of cimetidine on the pharmacokinetic profiles of quinapril and its active metabolite CI-928 was evaluated in eight healthy volunteers."( Multiple-dose cimetidine administration does not influence the single-dose pharmacokinetics of quinapril and its active metabolite (CI-928).
Cetnarowski, AB; Ferry, JJ; Horvath, AM; Sedman, AJ; Thomas, RW, 1988
)
0.94
" Plasma pharmacokinetic data were first obtained from rabbits given 3 mg/kg doxorubicin."( The influence of ranitidine on the pharmacokinetics and toxicity of doxorubicin in rabbits.
Anthony, LB; Brenner, DE; Collins, JC; Halter, S; Hande, KR; Harris, NL, 1988
)
0.27
" single) and showed no significant effect on total body clearance, serum half-life (T1/2) and AUC of theophylline, while enoxacin by the same pretreatment increased significantly serum theophylline concentrations and resulted in significant effect on all the pharmacokinetic parameters."( Lack of effect of ofloxacin on theophylline pharmacokinetics in rats.
Miyazaki, K; Okazaki, O; Tachizawa, H, 1987
)
0.27
"21 l/h per kg) with a consequent increase in half-life (24."( Dose-dependent pharmacokinetics of cimetidine in the rat.
Aarons, L; Adedoyin, A; Houston, JB, 1987
)
0.55
" After pretreatment with cimetidine, which inhibits the activity of cytochrome P-450, the peak plasma concentration and area under the plasma-time concentration curve for nifedipine were increased by a mean 84%."( Factors affecting the pharmacokinetics of nifedipine.
Challenor, VF; George, CF; Gruchy, B; Le Vie, J; Renwick, AG; Waller, DG, 1987
)
0.58
" The serum cimetidine levels and pharmacokinetic parameters of the patient group did not significantly differ from those of the control group after oral administration."( Pharmacokinetic studies of cimetidine in patients with liver disease.
Arima, T; Nagashima, H; Yamasaki, H, 1987
)
0.96
" Furthermore, variable gastric emptying rates combined with the short plasma elimination half-life and poor gastric absorption of cimetidine can be the cause of the frequently observed plasma level double peaks."( The influence of variable gastric emptying and intestinal transit rates on the plasma level curve of cimetidine; an explanation for the double peak phenomenon.
Amidon, GL; Oberle, RL, 1987
)
0.69
" No significant differences in elimination rate constant, peak concentration, time to peak concentration, volume of distribution, or elimination half-life were noted among treatments."( Effects of cimetidine or ranitidine on the pharmacokinetics of flurbiprofen.
Cox, SR; Rock, WL; Small, RE; Sullivan, KM; Willis, HE, 1986
)
0.66
" Peak plasma quinine concentration and the time of peak concentration were not altered after cimetidine or ranitidine pretreatment."( Effects of cimetidine and ranitidine on the pharmacokinetics of quinine.
Patamasucon, P; Pongmarutai, M; Sunbhanich, M; Wanwimolruk, S, 1986
)
0.88
" The pharmacokinetic parameters at intravenous administration were calculated according to a two-compartment model."( [Cimetidine pharmacokinetics].
Blinkov, IL; Davydov, SM; Karpenko, EV; Katrukha, SP; Kukes, VG,
)
1.04
"005), half-life = 11."( The effects of cimetidine upon the plasma pharmacokinetics of doxorubicin in rabbits.
Brenner, DE; Collins, JC; Hande, KR, 1986
)
0.62
" The possibility of a pharmacokinetic interaction between these drugs was examined in eight patients who received cimetidine and PRZ alone and in combination in a crossover fashion."( Lack of pharmacokinetic interaction between cimetidine and pirenzepine.
Jamali, F; Mahachai, V; Reilly, PA; Thomson, AB, 1985
)
0.74
"Limited pharmacokinetic data have been reported concerning the use of cimetidine in the neonate for the management of gastrointestinal hemorrhage."( The pharmacokinetics of cimetidine and metabolites in a neonate.
Lloyd, CW; Martin, WJ; Taylor, BD, 1985
)
0.81
" The elimination half-life of cimetidine in burned patients was significantly reduced (2."( Increased cimetidine clearance in burn patients.
Abernethy, DR; Greenblatt, DJ; Martyn, JA, 1985
)
0.96
"05) increase in diltiazem levels at most time points, in peak concentration and area under the concentration-time curve."( The effect of ranitidine and cimetidine on single-dose diltiazem pharmacokinetics.
Goodman, RP; McKenney, JM; Winship, LC; Wood, JH; Wright, JT,
)
0.42
"43 l/kg) and mean half-life (2."( Pharmacokinetics of cimetidine in patients with liver disease.
Arancibia, A; Chesta, J; Fajuri, M; González-Martin, G; Novoa, X, 1985
)
0.59
" The data give pharmacodynamic basis for the interaction of histamine-H2-receptor antagonists with bone marrow cells."( Pharmacodynamic basis for the interaction of cimetidine with the bone marrow stem cells (CFUS).
Byron, JW, 1980
)
0.52
"A sensitive and specific high pressure liquid chromatographic procedure for ranitidine estimation is described and pharmacokinetic studies in six healthy volunteers reported."( Pharmacokinetic and gastric secretory studies of ranitidine in man.
Anderson, A; Hanson, RG; Louis, WJ; McNeil, JJ; Mihaly, GW; Smallwood, RA; Yeomans, ND, 1981
)
0.26
" The interaction of nifedipine and cimetidine is thus of clinical significance because of its pharmacodynamic effect."( [Effect of cimetidine and ranitidine on the pharmacokinetics and anti-hypertensive effect of nifedipine].
Heidemann, H; Janisch, HD; Kirch, W; Ohnhaus, EE; Rämsch, K, 1983
)
0.93
" Pharmacodynamic and pharmacokinetic differences exist between the drugs, some of which are of clinical significance."( Comparative pharmacodynamics and pharmacokinetics of cimetidine and ranitidine.
Richards, DA, 1983
)
0.52
" Factors contributing to the transport of solutes through the peritoneal membrane are discussed and the literature concerning the pharmacokinetic aspects of CAPD is reviewed."( Pharmacokinetic aspects during continuous ambulatory peritoneal dialysis: a literature review.
Janknegt, R; Koks, CH, 1984
)
0.27
" Elimination half-life is approximately 2 hours."( Clinical pharmacokinetics of cimetidine.
Gugler, R; Somogyi, A,
)
0.42
" The elimination half-life of 5FU was not altered by cimetidine."( The influence of cimetidine on the pharmacokinetics of 5-fluorouracil.
Clark, PI; Dilloway, MR; Harvey, VJ; Johnston, A; Lant, AF; Slevin, ML, 1984
)
0.86
" Baseline quinidine pharmacokinetic parameters were determined after a single oral 400-mg dose."( Effect of cimetidine on quinidine clearance.
Fox, T; Garnett, WR; Kline, BJ; Kolb, KW; Small, RE; Vetrovec, GW, 1984
)
0.67
"A pharmacokinetic model for calculating the pharmacokinetic parameters for a compound that is recycled in the bile is presented and tested using theoretical as well as experimental data."( Pharmacokinetic analysis of concentration-time data obtained following administration of drugs that are recycled in the bile.
Colburn, WA, 1984
)
0.27
"The pharmacokinetic interaction between clobazam and cimetidine was studied in 9 healthy male volunteers in an open-labelled study."( Pharmacokinetic aspects of the interaction between clobazam and cimetidine.
Grigoleit, HG; Hajdú, P; Hundt, HK; Koeppen, D; Malerczyk, V; Meyer, BH; Müller, FO; Witte, PU, 1983
)
0.75
"04 micrograms/ml), the area under the plasma concentration curve (A."( Pharmacokinetics of cimetidine in patients with unresponsive duodenal ulcer.
Alfieri, G; Benvenuti, C; Foschi, D; Rovati, V, 1983
)
0.59
" Pharmacokinetic analysis was performed on the pseudolinear portion of the elimination curve."( [Pharmacokinetics of alcohol after 3-hour intravenous infusion with and without cimetidine in 10 healthy non-alcoholic subjects].
Albin, H; Amouretti, M; Béraud, C; Betbeder, AM; Bourjac, M; Couzigou, P; Fleury, B; Richard-Molard, B; Vinçon, G, 1984
)
0.49
" doses, elimination half-life of imipramine was increased during cimetidine treatment (22."( Imipramine-cimetidine interaction: impairment of clearance and enhanced absolute bioavailability.
Abernethy, DR; Greenblatt, DJ; Shader, RI, 1984
)
0.9
" Pharmacokinetic parameters displayed wide interpatient variability (coefficients of variation of 30-50%) and significant relationships emerged between some of these parameters and certain patient characteristics."( Pharmacokinetics of cimetidine in critically ill patients.
Cameron, P; Ilett, KF; Nation, RL; Oh, TE; Thompson, W; Tjokrosetio, R, 1984
)
0.59
" No significant change in half-life was found."( Pharmacokinetics of cimetidine in advanced cirrhosis.
Grahnén, A; Jameson, S; Lindström, B; Lööf, L; Tyllström, J, 1984
)
0.59
"03) the elimination of desmethyldiazepam, as shown prolongation of its elimination half-life from 51."( Influence of cimetidine on the pharmacokinetics of desmethyldiazepam and oxazepam.
Klotz, U; Reimann, I, 1980
)
0.63
" In the control state, antipyrine half-life was longer in elderly than in young subjects (16."( Cimetidine impairs clearance of antipyrine and desmethyldiazepam in the elderly.
Abernethy, DR; Divoll, M; Greenblatt, DJ; Shader, RI, 1982
)
1.71
"05), half-life increased 48% (6."( Cimetidine inhibits theophylline clearance in patients with chronic obstructive pulmonary disease: a study using stable isotope methodology during multiple oral dose administration.
Mercer, GD; Musser, B; Thummel, KE; Vestal, RE, 1983
)
1.71
" No differences were observed in cimetidine half-life (2."( [Pharmacokinetics of cimetidine in ascitic cirrhotics].
Albin, H; Béraud, C; Couzigou, P; Fleury, B; Péhourcq, F; Vinçon, G, 1983
)
0.87
"2 g/day for 7 days) on the disposition and pharmacodynamic effects of a single oral dose of quinidine was studied in 6 normal volunteers."( Effect of cimetidine on the pharmacokinetics and pharmacodynamics of quinidine.
Golden, L; Hardy, BG; Lalka, D; Schentag, JJ; Zador, IT, 1983
)
0.67
" Cimetidine inhibited MISO demethylation and increased its half-life and area under the curve."( Effects of cimetidine, antipyrine, and pregnenolone carbonitrile on misonidazole pharmacokinetics.
Donaldson, J; Smith, NC; Workman, P,
)
1.43
" Cimetidine had no effect on nitrazepam absorption kinetics, since peak serum nitrazepam concentration and time of peak concentration were not altered."( Cimetidine impairs nitrazepam clearance.
Abernethy, DR; Greenblatt, DJ; Gugler, R; Locniskar, A; Müntefering, G; Ochs, HR, 1983
)
2.62
"86), the terminal half-life in plasma between 138 and 238 min, the total body clearance (Cltotal) between 178 and 337 ml/min, and the apparent volume of distribution about 1 l/kg."( Pharmacokinetics of cimetidine in patients undergoing hemodialysis.
Bjaeldager, PA; Hvidberg, EF; Jensen, JB; Larsen, NE; Nielsen, LP, 1983
)
0.59
" There was no significant change in the elimination half-life for either drug in the presence of cimetidine."( Effect of cimetidine on the pharmacokinetics of quinidine and lidocaine in the rat.
DiGregorio, GJ; Fruncillo, RJ; Soll, A, 1983
)
0.89
"The pharmacokinetic behavior of cimetidine has not been described in children, and there is no authoritative guideline on cimetidine dosage for children."( Pharmacokinetics of cimetidine in critically ill children.
Baltodano, A; Chin, TW; Edmonds, JF; Fenje, P; MacLeod, SM; Soldin, SJ, 1982
)
0.87
" This corresponded to an average increase in elimination half-life of 73% (range, 50 to 97%)."( Cimetidine decreases theophylline clearance.
Bentley, J; Dorr, R; Jackson, JE; Powell, JR; Wandell, M, 1981
)
1.71
" The pharmacokinetic data observed in these patients do not differ from those of normal subjects and patients."( Oral and intravenous pharmacokinetics of cimetidine in liver cirrhosis.
Benvenuti, C; Lirussi, F; Nassuato, G; Okolicsanyi, L; Orlando, R; Venuti, M, 1982
)
0.53
" Total theophylline clearance (CLtot), apparent volume of distribution (V), and elimination half-life (t 1/2 beta) were calculated."( Impact of cimetidine on the pharmacokinetics of theophylline.
Bachmann, KA; Bond, LW; Mahajan, VK; Schwartz, JI,
)
0.53
" The analysis exemplifies a new approach to pharmacokinetic modeling, which appears to be a valuable alternative to linear compartmental or physiological modeling."( Pharmacokinetic analysis by linear system approach I: cimetidine bioavailability and second peak phenomenon.
Veng Pedersen, P, 1981
)
0.51
" 4 Pharmacokinetic studies showed the mean elimination half-life of cimetidine to be 100 +/- 25 min, the total body cimetidine clearance 652 +/- 223 ml/min, the mean volume of distribution at steady state 65 +/- 181 and the overall bioavailability 78%."( Cimetidine-a clinical and pharmacokinetic study.
Barber, HE; Brunt, PW; Griffiths, R; Hawksworth, GM; Jeffers, TA; Mowat, NA; Petersen, J; Petrie, JC; Webster, J, 1981
)
1.94
" Cimetidine prolonged theophylline half-life compared to that in control periods an average of 36."( Alteration of theophylline clearance and half-life by cimetidine in normal volunteers.
Bernhard, H; Reitberg, DP; Schentag, JJ, 1981
)
1.42
" 3 A significant reduction occurred in the systemic clearance of caffeine and the half-life was prolonged as determined from measurement of caffeine in plasma and saliva."( Decreased systemic clearance of caffeine due to cimetidine.
Broughton, LJ; Rogers, HJ, 1981
)
0.52
" There were no differences in any of the pharmacokinetic parameters between the two ulcer groups, but there was considerable variation which was mainly age-related."( Pharmacokinetics and bioavailability of cimetidine in gastric and duodenal ulcer patients.
Gugler, R; Rohner, HG; Somogyi, A,
)
0.4
"Cimetidine given orally without food after an overnight fast produces a blood concentration curve with a pronounced second peak that does not appear after parenteral administration or when the drug is taken with food."( Pharmacokinetics and bioavailability of cimetidine in humans.
Miller, R; Pedersen, PV, 1980
)
1.97
"A four-way crossover pilot study was conducted to compare the pharmacodynamic response of intermittent famotidine (20 mg every 12 hr) to continuous infusions of cimetidine (1200 mg/24 hr), ranitidine (150 mg/24 hr), and famotidine (40 mg/24 hr) in six normal male volunteers."( Pharmacodynamics of bolus famotidine versus infused cimetidine, ranitidine, and famotidine.
Amsden, GW; D'Andrea, DT; Goss, TF; Harrison, NJ; Schentag, JJ, 1994
)
0.74
" This synergism may be due, at least in part, to a pharmacokinetic effect."( Effect of the H2-antagonist cimetidine on the pharmacokinetics and pharmacodynamics of the H1-antagonists hydroxyzine and cetirizine in patients with chronic urticaria.
Simons, FE; Simons, KJ; Sussman, GL, 1995
)
0.59
" The elimination of alfuzosin being almost entirely metabolic, the potential pharmacokinetic interaction with cimetidine (H2-receptor antagonist) was investigated in 10 healthy young subjects."( The effect of cimetidine on the pharmacokinetics of single oral doses of alfuzosin.
Bianchetti, G; Desager, JP; Harvengt, C; Rosenzweig, P, 1993
)
0.86
" The literature was searched for pharmacokinetic data of intravenously administered theophylline alone and in the presence of cimetidine in humans, dogs and rats."( Interspecies scaling of cimetidine-theophylline pharmacokinetic interaction: interspecies scaling in pharmacokinetic interactions.
Calvo, B; Domínguez-Gil, A; Gascón, AR; Hernández, RM; Pedraz, JL, 1994
)
0.8
"The possibility of a pharmacokinetic interaction between H2-receptor antagonists and alcohol consumed at lunchtime, was investigated in 24 healthy non-alcoholic male subjects, each receiving ranitidine 150 mg four times daily, cimetidine 400 mg four times daily, famotidine 20 mg four times daily and placebo in an open, four-way cross-over study."( Lack of effect of H2-receptor antagonists on the pharmacokinetics of alcohol consumed after food at lunchtime.
Braithwaite, R; Gibson, GJ; Hale, KA; Kendall, MJ; Langman, MJ; Spannuth, F; Walt, RP, 1994
)
0.47
" The variation between different subjects dominated the total variance for all of the pharmacokinetic parameters studied except the rate of disappearance of ethanol from blood (ko)."( Between-subject and within-subject variations in the pharmacokinetics of ethanol.
Jones, AW; Jönsson, KA, 1994
)
0.29
" Cmax was increased significantly when tenoxicam was given with probenecid (2."( Neither cimetidine nor probenecid affect the pharmacokinetics of tenoxicam in normal volunteers.
Day, RO; Geisslinger, G; Paull, P; Williams, KM, 1994
)
0.72
" The hydroxyzine and cetirizine half-life and AUC0-->infinity values were significantly increased and the systemic clearance rates were significantly decreased in the presence of cimetidine."( Effect of the H2-receptor antagonist cimetidine, on the pharmacokinetics and pharmacodynamics of the H1-receptor antagonists hydroxyzine and cetirizine in rabbits.
Chen, X; Simons, FE; Simons, KJ, 1994
)
0.75
" Significant decreases in AUC (16 and 13%) were observed following administration of single- and multiple-dose cimetidine, and a significant decrease in Cmax (14%) was observed following a single dose of ranitidine--all given prior to alcohol ingestion in the morning."( Cimetidine and ranitidine. Lack of effect on the pharmacokinetics of an acute ethanol dose.
Chesher, GB; Dauncey, H; Palmer, RH, 1993
)
1.94
" In clinical settings, the magnitude of the pharmacokinetic difference may warrant dose adjustment to avoid toxic effects of FT when administered with CM."( Effect of cimetidine on the pharmacokinetics of fentiazac in rats.
Kweon, DS; Lee, MH; Shim, CK, 1993
)
0.69
" Pharmacokinetic profiles and morning pre-dose electrocardiograms were obtained whilst the patients were on terfenadine alone and after the addition of cimetidine or rantidine."( Effect of concomitant administration of cimetidine and ranitidine on the pharmacokinetics and electrocardiographic effects of terfenadine.
Cantilena, LR; Conner, DP; Honig, PK; Mullin, JC; Wortham, DC; Zamani, K, 1993
)
0.75
" Time to achieve the maximum plasma concentration, terminal half-life of elimination, and the total area under the plasma concentration-time curve of ritanserin were not altered in comparison with control experiments."( Effect of concomitantly administered cimetidine or ranitidine on the pharmacokinetics of the 5-HT2-receptor antagonist ritanserin.
Benn, HP; Buschmann, M; Jähnchen, E; Seiler, KU; Szathmary, S; Trenk, D, 1993
)
0.56
" The mean elimination half-life of naproxen was 24."( The pharmacokinetics of naproxen, its metabolite O-desmethylnaproxen, and their acyl glucuronides in humans. Effect of cimetidine.
Guelen, PJ; Van Den Biggelaar-Martea, M; Verwey-Van Wissen, CP; Vree, ML; Vree, TB, 1993
)
0.49
" Venous blood sampling for pharmacokinetic assessment was done over a complete dosing interval on day 7 of each phase."( Effects of cimetidine and ranitidine on the pharmacokinetics of a chronotherapeutically formulated once-daily theophylline preparation (Uniphyl).
Babul, N; Buttoo, KM; Fraser, IM; Stewart, JH; Walker, SE,
)
0.52
"The steady-state pharmacokinetic interaction between nefazodone and cimetidine was evaluated in a three-period crossover study consisting of three treatments of 1 week duration with a 1 week washout between treatments."( Lack of interaction between nefazodone and cimetidine: a steady state pharmacokinetic study in humans.
Barbhaiya, RH; Greene, DS; Shukla, UA, 1995
)
0.79
" Blood samples were collected just before each dose of cyclosporine and for up to 36 hours afterward for pharmacokinetic analysis."( Evaluation of the pharmacokinetic interaction between cimetidine or famotidine and cyclosporine in healthy men.
Collier, DS; McGuire, TR; Rossi, SJ; Schaaf, LJ; Shaefer, MS; Stratta, RJ, 1995
)
0.54
" Cyclosporine pharmacokinetic parameters during each of the 3 treatment periods were compared."( Evaluation of the pharmacokinetic interaction between cimetidine or famotidine and cyclosporine in healthy men.
Collier, DS; McGuire, TR; Rossi, SJ; Schaaf, LJ; Shaefer, MS; Stratta, RJ, 1995
)
0.54
" Cimetidine significantly decreased the total body clearance and extended the plasma half-life of theophylline, but did not change its volume of distribution."( Drug interactions between theophylline and H2-antagonists, roxatidine acetate hydrochloride and cimetidine: pharmacokinetic analysis in rats in vivo.
Furuhata, M; Nagai, N; Ogata, H, 1995
)
1.42
" Mean tacrine oral clearance was reduced by 30%; however, mean absorption rate and elimination half-life values were not affected by cimetidine."( Inhibition of tacrine oral clearance by cimetidine.
deVries, TM; Forgue, ST; Reece, PA; Sedman, AJ, 1996
)
0.77
" No statistically significant differences were observed in the pharmacokinetic parameters (Cmax-AUC-T1/2-urinary excretion and metabolic ratio) of sparfloxacin following the 2 treatment."( Cimetidine does not alter sparfloxacin pharmacokinetics.
Alvarez, MP; Azanza, JR; Gries, JM; Honorato, J; Sadaba, B; Singlas, E; Taburet, AM, 1995
)
1.73
" for 6 days) on the pharmacokinetics and pharmacodynamic effects of the angiotensin II receptor antagonist, losartan (100 mg)."( Effects of cimetidine on pharmacokinetics and pharmacodynamics of losartan, an AT1-selective non-peptide angiotensin II receptor antagonist.
Bradstreet, TE; Goldberg, MR; Höglund, P; Lo, MW; Ritter, MA, 1995
)
0.68
"The potential for a pharmacokinetic interaction between butorphanol nasal spray and cimetidine, under steady state conditions, was evaluated in 16 healthy male volunteers."( Lack of pharmacokinetic interaction between butorphanol nasal spray and cimetidine.
Barbhaiya, RH; Shyu, WC, 1996
)
0.75
"The chlorpheniramine and diphenhydramine terminal elimination half-life values and area under the curve values were significantly increased, and the systemic clearance rates were significantly decreased, during concomitant administration of cimetidine."( Effect of cimetidine on the pharmacokinetics and pharmacodynamics of chlorpheniramine and diphenhydramine in rabbits.
Chen, X; Fraser, TG; Simons, FE; Simons, KJ, 1996
)
0.88
"Any enhanced peripheral H1-blockade observed could be attributed, at least in part, to a pharmacokinetic interaction."( Effect of cimetidine on the pharmacokinetics and pharmacodynamics of chlorpheniramine and diphenhydramine in rabbits.
Chen, X; Fraser, TG; Simons, FE; Simons, KJ, 1996
)
0.7
"The aim of this study was to assess the pharmacokinetics and subsequent pharmacodynamic interaction of MPC-1304, a dihydropyridine Ca2+ antagonist, with other drugs in animal experiments."( Interaction of some drugs on the pharmacokinetics or pharmacodynamics of MPC-1304, a dihydropyridine Ca2+ antagonist.
Miyake, H; Miyoshi, K; Nakano, M; Nishizaki, J; Umeno, Y; Yoshida, K,
)
0.13
"This discontinuous oral absorption pharmacokinetic model can be a useful tool in characterizing absorption phases, disposition, and bioavailability of drugs exhibiting two absorption peaks following oral administration."( Applications and simulations of a discontinuous oral absorption pharmacokinetic model.
Boudinot, FD; Witcher, JW, 1996
)
0.29
" Thiamine diphosphate administered intraperitoneally in a dose of 10 mg/kg (one time a day for a week) does not change pharmacokinetic and analgesic effect of naproxene."( [The modification of the pharmacokinetics and analgesic effect of naproxen by cimetidine, phenobarbital and thiamine diphosphate].
Pentiuk, AA; Stanislavchuk, NA; Vovk, OG,
)
0.36
" The pharmacokinetic interaction of albendazole sulfoxide with dexamethasone, associated or not with cimetidine, was investigated in 24 patients with active intraparenchymal brain cysticercosis."( Therapy for neurocysticercosis: pharmacokinetic interaction of albendazole sulfoxide with dexamethasone.
Bonato, PS; Lanchote, VL; Marques, MP; Takayanagui, OM, 1997
)
0.51
" The ideal therapy for GORD will have linear pharmacokinetics, a relatively long plasma half-life (t1/2), a duration of action allowing once daily administration, and a stable effect independent of interactions with food, antacids and other drugs."( Pharmacokinetic optimisation in the treatment of gastro-oesophageal reflux disease.
Berstad, A; Hatlebakk, JG, 1996
)
0.29
" Cimetidine, however, resulted in a 21-23% increase in Cmax of unchanged nebivolol and of each enantiomer plus its hydroxylated metabolites."( A pharmacokinetic and pharmacodynamic interaction study between nebivolol and the H2-receptor antagonists cimetidine and ranitidine.
Ford, GA; Howes, A; Kamali, F; Snoeck, E; Thomas, SH, 1997
)
1.42
" To study its pharmacokinetic characteristics, levels of praziquantel in plasma were determined for eight healthy volunteers after the administration of three oral doses of 25 mg/kg of body weight given at 2-h intervals, alone and with the simultaneous administration of cimetidine."( Pharmacokinetic study of praziquantel administered alone and in combination with cimetidine in a single-day therapeutic regimen.
Castro, N; Corona, T; Jung, H; Medina, R; Sotelo, J, 1997
)
0.7
" The results revealed that cimetidine interacted with 4-MAA by increasing the systemic availability, prolonging the elimination half-life and decreasing the systemic clearance of 4-MAA, whereas the renal clearances of 4-MAA remained unchanged."( Effect of cimetidine on the pharmacokinetics of the metabolites of metamizol.
Bacracheva, N; Drenska, A; Gorantcheva, J; Schinzel, S; Scholl, T; Stoinov, A; Tchakarski, I; Tentcheva, J; Tyutyulkova, N; Vlahov, V, 1997
)
1
" Cefaclor is not metabolized to a significant degree, but it degrades chemically in the body with an approximate half-life of 2 hours."( Pharmacokinetic profile of cefaclor.
Derendorf, H; Schifferer, H; Sourgens, H, 1997
)
0.3
" Pharmacokinetic interactions with other drugs have been described but, in some cases, their mechanism is unknown."( Pharmacokinetic interactions involving clozapine.
Taylor, D, 1997
)
0.3
"Published trials and case reports relevant to the human metabolism of clozapine and to suspected pharmacokinetic interactions were reviewed."( Pharmacokinetic interactions involving clozapine.
Taylor, D, 1997
)
0.3
" time data were analysed by non-linear least squares regression analysis to determine pharmacokinetic parameter estimates."( Pharmacokinetics of intravenous and intragastric cimetidine in horses. I. Effects of intravenous cimetidine on pharmacokinetics of intravenous phenylbutazone.
Ashcraft, SM; Dyke, TM; Gerken, DF; Reed, SM; Sams, RA, 1997
)
0.55
" Steady-state pharmacokinetic parameters (based on an enzyme inhibition assay) and lipid responses were compared."( Cimetidine does not alter atorvastatin pharmacokinetics or LDL-cholesterol reduction.
Gibson, DM; Stern, RH; Whitfield, LR, 1998
)
1.74
" Pharmacokinetic comparisons were made between groups for the day 1 and day 7 profiles."( Concurrent administration of donepezil HCl and cimetidine: assessment of pharmacokinetic changes following single and multiple doses.
Friedhoff, LT; Perdomo, CA; Tiseo, PJ, 1998
)
0.56
"On both day 1 and day 7, a statistically significant difference was observed between the donepezil and the donepezil + cimetidine groups in terms of the Cmax and AUC(0-24) values for donepezil."( Concurrent administration of donepezil HCl and cimetidine: assessment of pharmacokinetic changes following single and multiple doses.
Friedhoff, LT; Perdomo, CA; Tiseo, PJ, 1998
)
0.77
"Co-administration of donepezil HCl (5 mg) and cimetidine (800 mg) did not produce clinically significant changes in the pharmacokinetic profiles of either drug."( Concurrent administration of donepezil HCl and cimetidine: assessment of pharmacokinetic changes following single and multiple doses.
Friedhoff, LT; Perdomo, CA; Tiseo, PJ, 1998
)
0.82
" Small differences were found in mean tmax (0."( Pharmacokinetics of dolasetron with coadministration of cimetidine or rifampin in healthy subjects.
Arumugham, T; Cramer, MB; Dimmitt, DC; Keung, A; Weir, SJ, 1999
)
0.55
"Based on the small changes in the pharmacokinetic parameters of dolasetron and its active metabolites, as well as the favorable safety results, no dosage adjustments for dolasetron mesylate are recommended with concomitant administration of cimetidine or rifampin."( Pharmacokinetics of dolasetron with coadministration of cimetidine or rifampin in healthy subjects.
Arumugham, T; Cramer, MB; Dimmitt, DC; Keung, A; Weir, SJ, 1999
)
0.73
" We report that cimetidine in doses that may cause pharmacokinetic interactions did not affect the concentration-effect relationship of either the stimulating action of theophylline or the depressant activity of ethanol."( The effect of cimetidine on the pharmacodynamics of theophylline-induced seizures and ethanol hypnotic activity.
Gilhar, D; Habib, G; Hoffman, A; Perlstein, I; Pinto, E, 1999
)
1.01
" Pharmacokinetic parameters were determined from plasma and urinary dofetilide concentrations; prolongation of the QTc interval was determined from three-lead electrocardiograms."( Effect of cimetidine and ranitidine on pharmacokinetics and pharmacodynamics of a single dose of dofetilide.
Abel, S; Brearley, CJ; Eve, MD; Nichols, DJ, 2000
)
0.71
" There were no significant differences between the pharmacokinetic parameters of repaglinide when given as monotherapy and when administered concurrently with cimetidine."( Drug interaction studies with repaglinide: repaglinide on digoxin or theophylline pharmacokinetics and cimetidine on repaglinide pharmacokinetics.
Hatorp, V; Thomsen, MS, 2000
)
0.72
"The administration of cimetidine increased the ziprasidone AUC(0,infinity) by 6% but there were no statistically significant differences in Cmax, tmax or lambda(z) between the ziprasidone+cimetidine group and the ziprasidone group."( The pharmacokinetics of ziprasidone in healthy volunteers treated with cimetidine or antacid.
Folger, CJ; Geoffroy, P; Hansen, RA; Wilner, KD, 2000
)
0.85
" It is concluded that, although there was a significant pharmacokinetic drug interaction between ketoconazole or cimetidine and loratadine, this effect was not accompanied by a change in the QTc interval in healthy adult volunteers."( Evaluation of the pharmacokinetics and electrocardiographic pharmacodynamics of loratadine with concomitant administration of ketoconazole or cimetidine.
Affrime, MB; Batra, VK; Cayen, MN; Kosoglou, T; Lim, JM; Salfi, M, 2000
)
0.72
" Assessment of estimated pharmacokinetic variables revealed a significantly faster rate of change in the distribution phase for CyA in combination with cimetidine."( Effect of cimetidine on pharmacokinetics of orally administered cyclosporine in healthy dogs.
Daigle, JC; Foil, CS; Hosgood, G; Hunter, RP, 2001
)
0.91
"The influence of synthetic drugs prescribed for peptic ulcer on the pharmacokinetic fate of glycyrrhizin (GL) from Shaoyao-Gancao-tang (SGT, a traditional Chinese formulation, Shakuyaku-Kanzo-to in Japanese) was investigated in rats."( The influence of commonly prescribed synthetic drugs for peptic ulcer on the pharmacokinetic fate of glycyrrhizin from Shaoyao-Gancao-tang.
Akao, T; He, JX; Nishino, T; Tani, T, 2001
)
0.31
" Further, it was found that oral administration of cimetidine in the quiescent phase resulted in significantly higher bioavailability and in other pharmacokinetic parameters compared to that obtained following administration in the active phase."( Variability in cimetidine absorption and plasma double peaks following oral administration in the fasted state in humans: correlation with antral gastric motility.
Amidon, GL; Barnett, JL; Hayashi, Y; Lesko, LJ; Ramachandran, C; Shah, VP; Takamatsu, N; Welage, LS; Yamamoto, R, 2002
)
0.92
"To examine the effect of concomitant cimetidine or antacid administration on the pharmacokinetic profile of sildenafil citrate in healthy male volunteers in two open-label, randomized studies."( The effects of cimetidine and antacid on the pharmacokinetic profile of sildenafil citrate in healthy male volunteers.
Laboy, L; LeBel, M; Wilner, K, 2002
)
0.94
"Coadministration of cimetidine had no statistically significant effect on the tmax or kel of sildenafil but caused a statistically significant increase in sildenafil AUCt and Cmax of 56% and 54%, respectively (P<0."( The effects of cimetidine and antacid on the pharmacokinetic profile of sildenafil citrate in healthy male volunteers.
Laboy, L; LeBel, M; Wilner, K, 2002
)
0.99
" Antacid coadministration had no effect on the pharmacokinetic profile of sildenafil."( The effects of cimetidine and antacid on the pharmacokinetic profile of sildenafil citrate in healthy male volunteers.
Laboy, L; LeBel, M; Wilner, K, 2002
)
0.67
" Quetiapine plasma concentrations were measured before and after cimetidine coadministration, and quetiapine pharmacokinetic parameters were calculated."( The effect of multiple doses of cimetidine on the steady-state pharmacokinetics of quetiapine in men with selected psychotic disorders.
Keck, PE; Strakowski, SM; Thyrum, PT; Wong, YW; Yeh, C, 2002
)
0.84
" Twelve healthy volunteers (eight males and four females) participated in an open-label, double-phase pharmacokinetic study."( Pharmacokinetics of saquinavir co-administered with cimetidine.
Back, DJ; Boffito, M; Bonora, S; Carriero, P; Di Perri, G; Hoggard, PG; Raiteri, R; Reynolds, HE; Sinicco, A; Trentini, L, 2002
)
0.57
" Furthermore, the effect of cimetidine (CIM) on pharmacokinetic parameters of AC and its metabolite diacetolol (DC) was evaluated."( Influence of cimetidine co-administration on the pharmacokinetics of acebutolol enantiomers and its metabolite diacetolol in a rat model: the effect of gastric pH on double-peak phenomena.
Foster, RT; Mostafavi, SA, 2003
)
0.98
" This was a pharmacokinetic drug-drug interaction study in which the subjects were administered aminophylline as a continuous infusion at low doses (mean 10."( Determination of theophylline clearance after cimetidine infusion in critically ill patients.
Fasihi, M; Hadjibabaie, M; Mojtahedzadeh, M; Rezaee, S; Sadray, S,
)
0.39
" Concomitant ranitidine had no significant effect on voriconazole Cmax or AUCtau."( Histamine H2-receptor antagonists have no clinically significant effect on the steady-state pharmacokinetics of voriconazole.
Kleinermans, D; Nichols, D; Purkins, L; Wood, N, 2003
)
0.32
" A comparison is also presented between several methods based on animal pharmacokinetic data, using the same set of proprietary compounds, and it lends further support for the use of this method, as opposed to methods that require the gathering of pharmacokinetic data in laboratory animals."( Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
Gao, F; Lombardo, F; Obach, RS; Shalaeva, MY, 2004
)
0.32
"The primary route of elimination of granisetron is by oxidative hepatic metabolism, thus its pharmacokinetic profile may be altered by co-administration of other drugs that inhibit or induce hepatic drug metabolizing enzymes."( The effect of repeat dosing with cimetidine on the pharmacokinetics of intravenous granisetron in healthy volunteers.
Youlten, L, 2004
)
0.6
"The purpose of this study was to investigate the pharmacokinetic alteration of diltiazem and its main metabolite, deacetyldiltiazem, after oral administration of diltiazem in rabbits with or without cimetidine co-administration."( The influence of cimetidine on the pharmacokinetics of diltiazem and its main metabolite in rabbits.
Burm, JP; Choi, JS, 2004
)
0.85
" No changes in any plasma pharmacokinetic parameters of fexofenadine were found during cimetidine treatment."( Different effects of three transporting inhibitors, verapamil, cimetidine, and probenecid, on fexofenadine pharmacokinetics.
Sugawara, K; Tateishi, T; Uno, T; Yasui-Furukori, N, 2005
)
0.79
"In view of the good tolerability of escitalopram, the pharmacokinetic changes observed on co-administration with cimetidine or omeprazole are unlikely to be of clinical concern."( The effect of cimetidine or omeprazole on the pharmacokinetics of escitalopram in healthy subjects.
Malling, D; Poulsen, MN; Søgaard, B, 2005
)
0.9
" Pharmacokinetic parameters were determined using noncompartmental analysis."( Multiple dose pharmacokinetics and acute safety of piroxicam and cimetidine in the cat.
Chun, R; Corse, M; Garrett, L; Heeb, HL; Hunter, RP; Koch, DE; Moore, L; Pellerin, MA; Radlinsky, M, 2005
)
0.57
"Four separate studies investigated the pharmacokinetic interaction between single oral doses of aliskiren and lovastatin, atenolol, celecoxib or cimetidine, respectively."( Pharmacokinetic interactions of the oral renin inhibitor aliskiren with lovastatin, atenolol, celecoxib and cimetidine.
Corynen, S; Dieterle, W; Mann, J; Vaidyanathan, S, 2005
)
0.74
" Aliskiren mean Cmax was not affected by either lovastatin or atenolol, although a non-significant 36% increase was observed with celecoxib."( Pharmacokinetic interactions of the oral renin inhibitor aliskiren with lovastatin, atenolol, celecoxib and cimetidine.
Corynen, S; Dieterle, W; Mann, J; Vaidyanathan, S, 2005
)
0.54
"Overall, single doses of aliskiren showed no evidence of clinically important pharmacokinetic interactions with lovastatin, atenolol, celecoxib or cimetidine."( Pharmacokinetic interactions of the oral renin inhibitor aliskiren with lovastatin, atenolol, celecoxib and cimetidine.
Corynen, S; Dieterle, W; Mann, J; Vaidyanathan, S, 2005
)
0.74
" This multiple-dose study investigated the potential for pharmacokinetic interactions between aliskiren and three drugs, each predominantly eliminated by a different clearance/metabolic pathway: allopurinol (glomerular filtration), celecoxib (cytochrome P450 metabolism) and cimetidine (P-glycoprotein and organic anion/cation transporters)."( A study of the pharmacokinetic interactions of the direct renin inhibitor aliskiren with allopurinol, celecoxib and cimetidine in healthy subjects.
Ayalasomayajula, S; Bizot, MN; Dieterich, HA; Dole, WP; Howard, D; Tchaloyan, S; Yeh, CM, 2008
)
0.73
"Three open-label, multiple-dose studies in healthy subjects investigated possible pharmacokinetic interactions between aliskiren 300 mg od and allopurinol 300 mg od (n = 20), celecoxib 200 mg bid (n = 22), or cimetidine 800 mg od (n = 22)."( A study of the pharmacokinetic interactions of the direct renin inhibitor aliskiren with allopurinol, celecoxib and cimetidine in healthy subjects.
Ayalasomayajula, S; Bizot, MN; Dieterich, HA; Dole, WP; Howard, D; Tchaloyan, S; Yeh, CM, 2008
)
0.74
"In this multiple-dose study, aliskiren showed no clinically relevant pharmacokinetic interactions when co-administered with allopurinol, celecoxib or cimetidine in healthy subjects."( A study of the pharmacokinetic interactions of the direct renin inhibitor aliskiren with allopurinol, celecoxib and cimetidine in healthy subjects.
Ayalasomayajula, S; Bizot, MN; Dieterich, HA; Dole, WP; Howard, D; Tchaloyan, S; Yeh, CM, 2008
)
0.75
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
" to rats with or without probenecid (50 mg/kg) or cimetidine (40 mg/kg), and pharmacokinetic parameters were compared."( Role of organic anion transporters in the pharmacokinetics of zonampanel, an alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate receptor antagonist, in rats.
Aoki, T; Hashimoto, T; Kamimura, H; Minematsu, T; Usui, T, 2008
)
0.6
"These findings could help explain possible pharmacokinetic changes of furosemide in various rat disease models (where CYP2C11, 2E1, 3A1 and/or CYP3A2 are altered) and drug-drug interactions between furosemide and other drugs (mainly metabolized via CYP2C11, 2E1, 3A1 and/or 3A2)."( Effects of cytochrome P450 inducers and inhibitors on the pharmacokinetics of intravenous furosemide in rats: involvement of CYP2C11, 2E1, 3A1 and 3A2 in furosemide metabolism.
Choi, YH; Lee, JH; Lee, MG; Lee, U; Yang, KH, 2009
)
0.35
" To predict the expected range of pharmacokinetic plasma concentrations after oral drug administration, a physiologically based pharmacokinetic population model for gastrointestinal transit and absorption was developed and evaluated."( Whole-body physiologically based pharmacokinetic population modelling of oral drug administration: inter-individual variability of cimetidine absorption.
Dressman, JB; Edginton, AN; Jantratid, E; Kleine-Besten, M; Thelen, K; Willmann, S, 2009
)
0.56
"The model facilitates predictions of the inter-individual pharmacokinetic variability after oral drug administration for immediate and extended-release formulations of cimetidine, given reasonable in-vitro dissolution kinetics."( Whole-body physiologically based pharmacokinetic population modelling of oral drug administration: inter-individual variability of cimetidine absorption.
Dressman, JB; Edginton, AN; Jantratid, E; Kleine-Besten, M; Thelen, K; Willmann, S, 2009
)
0.75
" This study investigated (1) the effect of food on alogliptin pharmacokinetics and tolerability and (2) pharmacokinetic interactions between alogliptin and metformin or cimetidine and tolerability of alogliptin when administered with either drug."( Pharmacokinetics of alogliptin when administered with food, metformin, or cimetidine: a two-phase, crossover study in healthy subjects.
Christopher, R; Covington, P; Davenport, M; Fleck, P; Karim, A; Li, X; Mekki, Q; Wann, E, 2010
)
0.79
" Pharmacokinetic parameters were determined after the last dose in each period."( Pharmacokinetics of alogliptin when administered with food, metformin, or cimetidine: a two-phase, crossover study in healthy subjects.
Christopher, R; Covington, P; Davenport, M; Fleck, P; Karim, A; Li, X; Mekki, Q; Wann, E, 2010
)
0.59
"The objective of this study was to assess the pharmacokinetic behavior of floating hydroxypropylmethylcellulose microparticles loaded with cimetidine (FMC) prepared using the non-solvent addition coacervation technique."( Pharmacokinetic study of hydroxypropylmethylcellulose microparticles loaded with cimetidine.
Ahmad, M; Hussain, I; Karim, S; Khan, SA; Kousar, R; Murtaza, G,
)
0.56
" The optimized formulations were subjected to in vivo studies to calculate the various pharmacokinetic parameters for developed optimized microparticulate formulation FMC3."( Pharmacokinetic study of hydroxypropylmethylcellulose microparticles loaded with cimetidine.
Ahmad, M; Hussain, I; Karim, S; Khan, SA; Kousar, R; Murtaza, G,
)
0.36
"The bioavailability parameters were found as: Cmax 1508."( Pharmacokinetic study of hydroxypropylmethylcellulose microparticles loaded with cimetidine.
Ahmad, M; Hussain, I; Karim, S; Khan, SA; Kousar, R; Murtaza, G,
)
0.36
" The primary pharmacokinetics (PK) parameters were plasma peak concentration (Cmax), AUC up to the last measured concentration (AUClast), and renal clearance (CLr) of glycopyrronium."( Effect of cimetidine, a model drug for inhibition of the organic cation transport (OCT2/MATE1) in the kidney, on the pharmacokinetics of glycopyrronium.
Camenisch, G; Drollmann, A; Dumitras, S; Kaiser, G; Pal, P; Sechaud, R; Vaidyanathan, S, 2013
)
0.79
" Cmax was not affected."( Effect of cimetidine, a model drug for inhibition of the organic cation transport (OCT2/MATE1) in the kidney, on the pharmacokinetics of glycopyrronium.
Camenisch, G; Drollmann, A; Dumitras, S; Kaiser, G; Pal, P; Sechaud, R; Vaidyanathan, S, 2013
)
0.79
" The AUC (6 hours ng mL(-1)) and CMAX (6 ng mL(-1)) of methadone significantly increased to 541 hours ng mL(-1) and 47."( Chloramphenicol significantly affects the pharmacokinetics of oral methadone in Greyhound dogs.
KuKanich, B; KuKanich, K, 2015
)
0.42
" The purpose of the present study is to develop a physiologically based pharmacokinetic (PBPK) model for atorvastatin and its two primary metabolites, 2-hydroxy-atorvastatin acid and atorvastatin lactone, using in vitro and in vivo data."( Physiologically based pharmacokinetic modeling of disposition and drug-drug interactions for atorvastatin and its metabolites.
Zhang, T, 2015
)
0.42
" However, expression and/or function of these proteins often fluctuate in pathological conditions, causing individual pharmacokinetic variability."( [Molecular Biological Analysis of Factors Influencing Pharmacokinetics to Achieve Personalized Pharmacotherapy].
Ikemura, K, 2015
)
0.42
" The aim of the current study was to investigate the ability of physiologically-based pharmacokinetic (PBPK) models to simulate the effects of OCT and MATE inhibition by cimetidine on metformin kinetics."( Metformin and cimetidine: Physiologically based pharmacokinetic modelling to investigate transporter mediated drug-drug interactions.
Almond, L; Burt, HJ; Gaohua, L; Harwood, MD; Jamei, M; Neuhoff, S; Rostami-Hodjegan, A; Rowland-Yeo, K; Tucker, GT, 2016
)
0.99
"The aim of this study was (1) to determine how closely physiologically based pharmacokinetic (PBPK) models can predict oral bioavailability using a priori knowledge of drug-specific properties and (2) to examine the influence of the biopharmaceutics classification system class on the simulation success."( Forecasting oral absorption across biopharmaceutics classification system classes with physiologically based pharmacokinetic models.
Aarons, L; Darwich, A; Dressman, J; Hansmann, S; Margolskee, A, 2016
)
0.43
"On account of the disturbance from the distribution phase, the concentration-time curve of drugs cannot fully reflect the characteristics of elimination, and thus, it is difficult for present methods to obtain ideal pharmacokinetic parameters."( A method to determine pharmacokinetic parameters based on andante constant-rate intravenous infusion.
Cao, YX; Yu, RH, 2017
)
0.46
" Pharmacokinetic analysis was based on plasma and urine data concentrations."( The role of organic cation transporter 2 inhibitor cimetidine, experimental diabetes mellitus and metformin on gabapentin pharmacokinetics in rats.
Baviera, AM; Benzi, JRL; de Moraes, NV; Stevens, JH; Yamamoto, PA, 2018
)
0.73
"No differences in pharmacokinetic parameters were observed between vehicle + GAB × cimetidine + GAB and vehicle + GAB × metformin + GAB groups."( The role of organic cation transporter 2 inhibitor cimetidine, experimental diabetes mellitus and metformin on gabapentin pharmacokinetics in rats.
Baviera, AM; Benzi, JRL; de Moraes, NV; Stevens, JH; Yamamoto, PA, 2018
)
0.96
" Despite evidence supporting the inhibition of multidrug and toxin extrusion proteins as the likely DDI mechanism, the previously reported physiologically-based pharmacokinetic (PBPK) model required the substantial lowering of the inhibition constant values of cimetidine for multidrug and toxin extrusion proteins from those obtained in vitro to capture the clinical DDI data between metformin and cimetidine."( Physiologically-Based Pharmacokinetic Modeling Analysis for Quantitative Prediction of Renal Transporter-Mediated Interactions Between Metformin and Cimetidine.
Bister, B; Ishiguro, N; Lee, W; Nishiyama, K; Sugiyama, Y; Toshimoto, K, 2019
)
0.89
"The objective of this study was to provide mechanistic whole-body physiologically based pharmacokinetic models of metformin and cimetidine, built and evaluated to describe the metformin-SLC22A2 808G>T drug-gene interaction, the cimetidine-metformin drug-drug interaction, and the impact of renal impairment on metformin exposure."( A Comprehensive Whole-Body Physiologically Based Pharmacokinetic Drug-Drug-Gene Interaction Model of Metformin and Cimetidine in Healthy Adults and Renally Impaired Individuals.
Ebner, T; Hanke, N; Ishiguro, N; Lehr, T; Müller, F; Nock, V; Selzer, D; Stopfer, P; Türk, D; Wiebe, S, 2020
)
0.97
"The established physiologically based pharmacokinetic models adequately describe the available clinical data, including the investigated drug-gene interaction, drug-drug interaction, and drug-drug-gene interaction studies, as well as the metformin exposure during renal impairment."( A Comprehensive Whole-Body Physiologically Based Pharmacokinetic Drug-Drug-Gene Interaction Model of Metformin and Cimetidine in Healthy Adults and Renally Impaired Individuals.
Ebner, T; Hanke, N; Ishiguro, N; Lehr, T; Müller, F; Nock, V; Selzer, D; Stopfer, P; Türk, D; Wiebe, S, 2020
)
0.77
"Whole-body physiologically based pharmacokinetic models of metformin and cimetidine were built and qualified for the prediction of metformin pharmacokinetics during drug-gene interaction, drug-drug interaction, and different stages of renal disease."( A Comprehensive Whole-Body Physiologically Based Pharmacokinetic Drug-Drug-Gene Interaction Model of Metformin and Cimetidine in Healthy Adults and Renally Impaired Individuals.
Ebner, T; Hanke, N; Ishiguro, N; Lehr, T; Müller, F; Nock, V; Selzer, D; Stopfer, P; Türk, D; Wiebe, S, 2020
)
1
" Aplastic anemia patients were used to establish a population pharmacokinetic model by the nonlinear mixed effect (NONMEM), and concentrations of ciclosporin were simulated by Monte Carlo method."( Effects of cimetidine on ciclosporin population pharmacokinetics and initial dose optimization in aplastic anemia patients.
Chen, X; He, SM; Mao, YZ; Wang, DD; Yang, Y; Yin, D; Zheng, ZQ, 2022
)
1.11
" In this study, we developed a mechanistic lactation physiologically based pharmacokinetic (PBPK) modeling approach incorporating BCRP mediated transport kinetics to simulate the concentration-time profiles of five BCRP drug substrates (acyclovir, bupropion, cimetidine, ciprofloxacin, and nitrofurantoin) in nursing women's plasma and milk."( Physiologically based pharmacokinetic model to predict drug concentrations of breast cancer resistance protein substrates in milk.
Fang, Y; Li, Y; Zhang, T; Zou, P, 2022
)
0.9
" These results were consistent with the cell-level pharmacodynamic (PD) modeling analysis which leveraged the time-course effects of drugs as single agents and drug combinations."( Pharmacodynamic Modeling to Evaluate the Impact of Cimetidine, an OCT2 Inhibitor, on the Anticancer Effects of Cisplatin.
Ait-Oudhia, S; Lesko, LJ; Mody, H; Vaidya, TR, 2022
)
0.97

Compound-Compound Interactions

oxazepam and lorazepom may be the benzodiazepines of choice to use in combination with cimetidine. There is no clinically relevant drug-drug interaction between CHF 5993 and cimetamines.

ExcerptReferenceRelevance
"The present study evaluated the therapeutic effects of rebamipide alone and in combination with cimetidine on experimental gastritis established by the administration of 5 mM sodium taurocholate (TCA) for 6 months in rats."( Therapeutic effects of oral rebamipide and in combination with cimetidine on experimental gastritis in rats.
Fujimura, J; Haruma, K; Kajiyama, G; Kishimoto, S; Kobayashi, H; Machino, H; Sakurai, K; Shimamoto, T; Shimizu, S; Yamasaki, K, 1992
)
0.74
" These involve a decrease in absorption when fluoroquinolones are given in combination with multivalent metal cations and an inhibition in the metabolism of methylxanthines by fluoroquinolones such as ciprofloxacin, enoxacin, and norfloxacin."( Drug interactions with fluoroquinolones.
Stein, GE, 1991
)
0.28
" Ulceration healed up within 2 weeks in 40% of patients treated with cimetidine combined with pirenzepine and in 31."( [Comparison of the results of the treatment with pirenzepine combined with cimetidine and sucralfate of stomach ulcer resistant to cimetidine].
Janke, A; Kozuszyńska, M; Namiot, Z; Stasiewicz, J; Szałaj, W,
)
0.6
" Nine healthy volunteers received three treatments: 1) 10 mg acenocoumarol in combination with cimetidine, 2) 10 mg acenocoumarol in combination with placebo, 3) 10 mg acenocoumarol after one week pretreatment with pentobarbitone."( Detection of drug interactions with single dose acenocoumarol: new screening method?
Cohen, AF; de Boer, A; Edelbroek, PM; Hoogkamer, JF; Kroon, C; Schoemaker, HC; van der Meer, EJ, 1990
)
0.5
" The host strain, biology of the tumour and the drug used in combination with CMTD might be some of the factors responsible for the varied response."( Effects of cimetidine combination with cyclophosphamide in transplanted murine tumors.
Ganu, UK; Gokhale, SV; Khandalekar, DD,
)
0.52
" Drugs that are renally secreted are prone to significant and complex drug-drug interactions, and knowledge of the underlying mechanisms is important."( Drug interactions involving renal transport mechanisms: an overview.
Kosoglou, T; Vlasses, PH, 1989
)
0.28
"The most widely used H2-receptor antagonist, cimetidine, is known to interact with cytochrome P-450 drug-metabolizing enzymes and, therefore, interacts with other drugs which may be administered concurrently."( Comparative effects of H2-receptor antagonists on drug interaction in rats.
Cocchetto, DM; Duggan, DE; Lin, JH; Yeh, KC,
)
0.39
" The potential of famotidine, a new H2-receptor antagonist with a guanylthiazole ring structure, to interact with the cytochrome P450 system has been extensively evaluated."( Famotidine: a notable lack of drug interactions.
Humphries, TJ, 1987
)
0.27
") of stable isotope-labeled theophylline was administered with the oral dose of theophylline."( Aging and drug interactions. I. Effect of cimetidine and smoking on the oxidation of theophylline and cortisol in healthy men.
Cusack, BJ; Dawson, GW; Mercer, GD; Park, BK; Vestal, RE, 1987
)
0.54
"The efficacy of prophylactic therapy with cimetidine or antacids combined with early enteral feeding to prevent gastrointestinal bleeding in patients with severe burns was evaluated."( Prevention of gastrointestinal bleeding in burns: the effects of cimetidine or antacids combined with early enteral feeding.
Hirshowitz, B; Jacobs, R; Kaufman, T; Moscona, R, 1985
)
0.77
" These differences were more pronounced following in vitro exposure of effector cells to interferon alone or in combination with cimetidine."( Immune functions in melanoma patients during treatment with interferon [HuIFN-alpha (Le)] alone or in combination with cimetidine.
Axelsson, B; Boketoft, A; Borgström, S; Flodgren, P; Malmström, P; Sjögren, HO,
)
0.54
"To study the absorption and disposition of clavulanic acid, ten healthy men received one intravenous and one oral dose of 125 mg clavulanic acid in combination with amoxycillin."( Pharmacokinetics of clavulanic acid, given in combination with amoxycillin, in volunteers.
Fellner, H; Hedström, SA; Nilsson-Ehle, I; Nilsson-Ehle, P; Sjövall, J, 1985
)
0.27
" Thus, when clinically indicated, oxazepam and lorazepam may be the benzodiazepines of choice to use in combination with cimetidine to eliminate the clinically significant drug interaction seen with diazepam and chlordiazepoxide."( Diazepam-cimetidine drug interaction: a clinically significant effect.
Ruffalo, RL; Segal, JL; Thompson, JF, 1981
)
0.89
" Thus, effects of these drugs and serum levels, where available, should be more closely followed when used in combination with cimetidine."( Cimetidine drug interactions.
Greene, WL; Levinson, MJ; Self, TH, 1983
)
1.91
"Antacids should not be combined with other anti-ulcer drugs such as carbenoxolone, metoclopramide, domperidone, sulpiride, di-citrato-bis-muthate and alginic acid."( [Antacids in combination with other anti-ulcer agents].
Fritsch, WP, 1983
)
0.27
"Pharmacokinetic drug-drug interactions which involve currently available benzodiazepines may be classified into two major categories: interactions which affect benzodiazepine rate of absorption, and interactions which affect clearance and, therefore, elimination half-life."( Benzodiazepine drug-drug interactions commonly occurring in clinical practice.
Abernethy, DR; Greenblatt, DJ; Ochs, HR; Shader, RI, 1984
)
0.27
"Pharmacokinetic drug-drug interactions which involve currently available benzodiazepines may be classified into 2 major categories: interactions which affect benzodiazepine rate of absorption, and interactions which affect clearance and, therefore, elimination 1/2-life."( Benzodiazepine drug-drug interactions commonly occurring in clinical practice.
Abernethy, DR; Greenblatt, DJ; Ochs, HR; Shader, RI, 1984
)
0.27
" These effects, combined with the common use of cimetidine in clinical practice, make the risk of adverse drug interactions a relatively frequent risk in the clinical setting."( Drug interactions involving cimetidine--mechanisms, documentation, implications.
Greene, W, 1984
)
0.82
"Propranolol is widely used in clinical practice and is frequently administered along with other drugs."( Pharmacokinetic drug interactions with propranolol.
Feely, J; Wood, AJ,
)
0.13
" Brief information on the following reports of drug-drug interactions is given in this article with the intention of giving these reports wider publicity and, possibly, encouraging further observation and research to establish or disprove their validity in a larger and wider range of patients or volunteer subjects."( Early reports on drug interactions.
D'Arcy, PF, 1983
)
0.27
" In some cases, cimetidine (70 mg/kg) was administered in combination with a 2-fold molar excess of sodium nitrite."( Nondetection of O6-methylguanine in rat DNA following in vivo treatment with large doses of cimetidine alone or in combination with sodium nitrite.
Hadjiloucas, E; Kyrtopoulos, SA; Vrotsou, B, 1982
)
0.83
" Cimetidine has several actions in vivo that may result in drug-drug interactions."( Drug interactions with cimetidine.
Schwinghammer, TL, 1981
)
1.48
"Preliminary results of endoscopic electrocoagulation combined with Cimetidine are reported in a prospective series of 60 consecutive patients presenting with active bleeding from gastroduodenal ulcer."( Endoscopic electrocoagulation combined with cimetidine. A pilot study of the applicability in active bleeding from gastroduodenal ulcer.
Amdrup, E; Højsgaard, A; Wara, P, 1980
)
0.76
"In this work, praziquantel (EMBAY 8440, CAS 55268-74-1), an oral antihelminthic drug effective against the three species of schistosomes pathogenic to man, was tested alone and in combination with cimetidine (CAS 51481-61-9), aH2-receptor antagonist having a known potentiative power when combined with other drugs."( Treatment of experimental schistosomiasis mansoni with praziquantel alone and combined with cimetidine.
Bennet, JL; Botros, SS; Ebeid, FA; Metwally, AA, 1994
)
0.7
" The pharmacokinetic literature on racemic drugs contains a vast amount of information on drug-drug interactions derived from the measurement of total drug concentrations in plasma and urine."( Stereoselective and isozyme-selective drug interactions.
Gibaldi, M, 1993
)
0.29
"Many adverse drug-drug interactions are attributable to pharmacokinetic problems and can be understood in terms of alterations of P450-catalyzed reactions."( Role of cytochrome P450 enzymes in drug-drug interactions.
Guengerich, FP, 1997
)
0.3
" The results from in vitro studies are related to the observed clinically significant in vivo drug-drug and drug-chemical interactions."( Drug interactions of H2-receptor antagonists involving cytochrome P450 (CYPs) enzymes: from the laboratory to the clinic.
Rendić, S, 1999
)
0.3
" No direct drug-drug interactions were found in these studies, suggesting that repaglinide may be coprescribed with cimetidine, digoxin, or theophylline at the dosage used for monotherapy."( Drug interaction studies with repaglinide: repaglinide on digoxin or theophylline pharmacokinetics and cimetidine on repaglinide pharmacokinetics.
Hatorp, V; Thomsen, MS, 2000
)
0.73
") or placebo in combination with (commercially available, racemic) mirtazapine (30 mg nocte)."( Concomitant use of mirtazapine and cimetidine: a drug-drug interaction study in healthy male subjects.
Maris, FA; Sitsen, JM; Timmer, CJ, 2000
)
0.58
" Juvenile rockfish were divided into 7 groups, and orally administered praziquantel alone (50, 100 and 200 mg kg(-1) body wt, BW) or in combination with cimetidine at a dose of 200 mg kg(-1) BW for each praziquantel dose."( Treatment of Microcotyle sebastis infestation in cultured rockfish Sebastes schlegeli by oral administration of praziquantel in combination with cimetidine.
Cho, JB; Kim, KH; Kwon, SR; Lee, EH, 2001
)
0.71
" In vivo and in vitro studies were conducted to evaluate the renal drug-drug interaction potential of oseltamivir."( The anti-influenza drug oseltamivir exhibits low potential to induce pharmacokinetic drug interactions via renal secretion-correlation of in vivo and in vitro studies.
Barrett, J; Cihlar, T; Hill, G; Ho, ES; Liu, B; Oo, C; Prior, K; Ward, P; Wiltshire, H, 2002
)
0.31
" After immunization with ovalbumin (OVA), a common dietary constituent, we evaluated the efficacy of pretreatment with histamine-receptor or serotonin-receptor blockers administered alone or in combination with a nitric oxide synthase inhibitor (L-NAME) on OVA-induced anaphylactic shock in Brown Norway rats."( Constitutive nitric oxide synthase inhibition combined with histamine and serotonin receptor blockade improves the initial ovalbumin-induced arterial hypotension but decreases the survival time in brown norway rats anaphylactic shock.
Bellou, A; Gerard, P; Gillois, P; Guéant, JL; Lambert, H; Longrois, D; Mallié, JP; Montémont, C; Sainte-Laudy, J; Vauthier, E, 2003
)
0.32
" In the current paper, this new extraction technique was combined with liquid chromatography-mass spectrometry (LC-MS) for the first time."( Liquid-phase microextraction based on carrier mediated transport combined with liquid chromatography-mass spectrometry. New concept for the determination of polar drugs in a single drop of human plasma.
Anthonsen, HS; Ho, TS; Pedersen-Bjergaard, S; Rasmussen, KE; Reubsaet, JL, 2005
)
0.33
"The renal drug-drug interaction between famotidine (an H(2) receptor antagonist) and probenecid has not been reproduced in rats."( Is the monkey an appropriate animal model to examine drug-drug interactions involving renal clearance? Effect of probenecid on the renal elimination of H2 receptor antagonists.
Chida, M; Fuse, E; Kusuhara, H; Sugiyama, Y; Tahara, H, 2006
)
0.33
" The drug-drug interaction (DDI) potential of these drugs for the hOCT/rOct-mediated hepatic/renal uptake process was also assessed."( Effect of cationic drugs on the transporting activity of human and rat OCT/Oct 1-3 in vitro and implications for drug-drug interactions.
Iwatsubo, T; Kamimura, H; Noguchi, K; Umehara, KI; Usui, T, 2008
)
0.35
"Cimetidine is known to cause drug-drug interactions (DDIs) with organic cations in the kidney, and a previous clinical study showed that coadministration of cimetidine or probenecid with fexofenadine (FEX) decreased its renal clearance."( The inhibition of human multidrug and toxin extrusion 1 is involved in the drug-drug interaction caused by cimetidine.
Horita, S; Inoue, K; Kondo, T; Kusuhara, H; Maeda, K; Matsushima, S; Nakayama, H; Ohta, KY; Sugiyama, Y; Yuasa, H, 2009
)
2.01
" This study investigated (1) the effect of food on alogliptin pharmacokinetics and tolerability and (2) pharmacokinetic interactions between alogliptin and metformin or cimetidine and tolerability of alogliptin when administered with either drug."( Pharmacokinetics of alogliptin when administered with food, metformin, or cimetidine: a two-phase, crossover study in healthy subjects.
Christopher, R; Covington, P; Davenport, M; Fleck, P; Karim, A; Li, X; Mekki, Q; Wann, E, 2010
)
0.79
" To examine the potential for drug-drug interactions at these two transporters, the pharmacokinetics of gabapentin enacarbil were evaluated in healthy adults after administration alone or in combination with either naproxen (an MCT-1 substrate) or cimetidine (an OCT2 substrate)."( Clinical pharmacokinetic drug interaction studies of gabapentin enacarbil, a novel transported prodrug of gabapentin, with naproxen and cimetidine.
Blumenthal, R; Cundy, KC; Ho, J; Lal, R; Luo, W; Sukbuntherng, J; Vicente, V, 2010
)
0.74
" These results suggest that the inhibition of MATEs, but not OCT2, is a likely mechanism underlying the drug-drug interactions with cimetidine in renal elimination."( Competitive inhibition of the luminal efflux by multidrug and toxin extrusions, but not basolateral uptake by organic cation transporter 2, is the likely mechanism underlying the pharmacokinetic drug-drug interactions caused by cimetidine in the kidney.
Inoue, K; Ito, S; Kusuhara, H; Sugiyama, Y; Toyoshima, J; Yokochi, M; Yuasa, H, 2012
)
0.77
"Inhibition of cytochrome P450-mediated drug metabolism by a concomitantly administered second drug is one of the major causes of drug-drug interactions in humans."( Drug-drug interactions and cooperative effects detected in electrochemically driven human cytochrome P450 3A4.
Di Nardo, G; Ferrero, S; Gilardi, G; Sadeghi, SJ, 2012
)
0.38
"The hepatic organic anion transporting polypeptides (OATPs) influence the pharmacokinetics of several drug classes and are involved in many clinical drug-drug interactions."( Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
Artursson, P; Haglund, U; Karlgren, M; Kimoto, E; Lai, Y; Norinder, U; Vildhede, A; Wisniewski, JR, 2012
)
0.38
" The underlying mechanism for TL-118-treatment success was associated with hepatic perfusion attenuation resulting from reduced nitric-oxide (NO) serum levels as elucidated by using hemodynamic response imaging (HRI, a functional MRI combined with hypercapnia and hyperoxia)."( Improved efficacy of a novel anti-angiogenic drug combination (TL-118) against colorectal-cancer liver metastases; MRI monitoring in mice.
Abramovitch, R; Corchia, N; Edrei, Y; Gross, E, 2012
)
0.38
" Drug-drug interactions (DDIs) via inhibition of renal organic anion (OAT) and organic cation (OCT) transporters have been observed in the clinic."( Quantitative prediction of renal transporter-mediated clinical drug-drug interactions.
Corrigan, B; El-Kattan, A; Feng, B; Hurst, S; Lockwood, P; Lu, Y; Rotter, CJ; Varma, MV, 2013
)
0.39
" TL-118, a novel drug combination has been recently developed to inhibit tumor angiogenesis."( TL-118 and gemcitabine drug combination display therapeutic efficacy in a MYCN amplified orthotopic neuroblastoma murine model--evaluation by MRI.
Abramovitch, R; Corchia, N; Dery, E; Fried, I; Gross, E; Komar-Stossel, C; Meir, K, 2014
)
0.4
" Therefore, prediction and evaluation of drug-drug interaction potential is important in the clinic and in the drug development process."( Evaluation of the transporter-mediated herb-drug interaction potential of DA-9801, a standardized dioscorea extract for diabetic neuropathy, in human in vitro and rat in vivo.
Choi, SZ; Jeong, HU; Kang, HE; Kim, EN; Kong, TY; Kwon, SS; Lee, HS; Son, M; Song, IS, 2014
)
0.4
" The model was used to predict the pharmacokinetic profiles and drug-drug interaction (DDI) effect for atorvastatin and its metabolites in different DDI scenarios."( Physiologically based pharmacokinetic modeling of disposition and drug-drug interactions for atorvastatin and its metabolites.
Zhang, T, 2015
)
0.42
" While the final PBPK model has limitations, it demonstrates the benefit of allowing for the complexities of passive permeability combined with active cellular uptake modulated by an electrochemical gradient and active efflux."( Metformin and cimetidine: Physiologically based pharmacokinetic modelling to investigate transporter mediated drug-drug interactions.
Almond, L; Burt, HJ; Gaohua, L; Harwood, MD; Jamei, M; Neuhoff, S; Rostami-Hodjegan, A; Rowland-Yeo, K; Tucker, GT, 2016
)
0.79
"This two-period, open-label, crossover study examined the drug-drug interaction of CHF 5993 and cimetidine."( A Two-Period Open-Label, Single-Dose Crossover Study in Healthy Volunteers to Evaluate the Drug-Drug Interaction Between Cimetidine and Inhaled Extrafine CHF 5993.
Acerbi, D; Ciurlia, G; Mariotti, F; Muraro, A; Spaccapelo, L, 2017
)
0.88
"Overall, this study indicates that there is no clinically relevant drug-drug interaction between CHF 5993 and cimetidine."( A Two-Period Open-Label, Single-Dose Crossover Study in Healthy Volunteers to Evaluate the Drug-Drug Interaction Between Cimetidine and Inhaled Extrafine CHF 5993.
Acerbi, D; Ciurlia, G; Mariotti, F; Muraro, A; Spaccapelo, L, 2017
)
0.87
" In this study, hot melt extrusion of a drug-drug mixture with minimal amount of polymeric excipient was investigated."( Melt Extrusion of High-Dose Co-Amorphous Drug-Drug Combinations : Theme: Formulation and Manufacturing of Solid Dosage Forms Guest Editors: Tony Zhou and Tonglei Li.
Aho, J; Arnfast, L; Baldursdottir, S; Kamruzzaman, M; Löbmann, K; Rades, T; Rantanen, J, 2017
)
0.46
"Using indomethacin-cimetidine as a model drug-drug system, processability of physical mixtures with and without 5% (w/w) of polyethylene oxide (PEO) were studied using Differential Scanning Calorimetry (DSC) and Small Amplitude Oscillatory Shear (SAOS) rheometry."( Melt Extrusion of High-Dose Co-Amorphous Drug-Drug Combinations : Theme: Formulation and Manufacturing of Solid Dosage Forms Guest Editors: Tony Zhou and Tonglei Li.
Aho, J; Arnfast, L; Baldursdottir, S; Kamruzzaman, M; Löbmann, K; Rades, T; Rantanen, J, 2017
)
0.78
" It is recommended by the US Food and Drug Administration as a clinical substrate of organic cation transporter 2/multidrug and toxin extrusion protein for drug-drug interaction studies."( A Comprehensive Whole-Body Physiologically Based Pharmacokinetic Drug-Drug-Gene Interaction Model of Metformin and Cimetidine in Healthy Adults and Renally Impaired Individuals.
Ebner, T; Hanke, N; Ishiguro, N; Lehr, T; Müller, F; Nock, V; Selzer, D; Stopfer, P; Türk, D; Wiebe, S, 2020
)
0.77
"The objective of this study was to provide mechanistic whole-body physiologically based pharmacokinetic models of metformin and cimetidine, built and evaluated to describe the metformin-SLC22A2 808G>T drug-gene interaction, the cimetidine-metformin drug-drug interaction, and the impact of renal impairment on metformin exposure."( A Comprehensive Whole-Body Physiologically Based Pharmacokinetic Drug-Drug-Gene Interaction Model of Metformin and Cimetidine in Healthy Adults and Renally Impaired Individuals.
Ebner, T; Hanke, N; Ishiguro, N; Lehr, T; Müller, F; Nock, V; Selzer, D; Stopfer, P; Türk, D; Wiebe, S, 2020
)
0.97
"The established physiologically based pharmacokinetic models adequately describe the available clinical data, including the investigated drug-gene interaction, drug-drug interaction, and drug-drug-gene interaction studies, as well as the metformin exposure during renal impairment."( A Comprehensive Whole-Body Physiologically Based Pharmacokinetic Drug-Drug-Gene Interaction Model of Metformin and Cimetidine in Healthy Adults and Renally Impaired Individuals.
Ebner, T; Hanke, N; Ishiguro, N; Lehr, T; Müller, F; Nock, V; Selzer, D; Stopfer, P; Türk, D; Wiebe, S, 2020
)
0.77
"Whole-body physiologically based pharmacokinetic models of metformin and cimetidine were built and qualified for the prediction of metformin pharmacokinetics during drug-gene interaction, drug-drug interaction, and different stages of renal disease."( A Comprehensive Whole-Body Physiologically Based Pharmacokinetic Drug-Drug-Gene Interaction Model of Metformin and Cimetidine in Healthy Adults and Renally Impaired Individuals.
Ebner, T; Hanke, N; Ishiguro, N; Lehr, T; Müller, F; Nock, V; Selzer, D; Stopfer, P; Türk, D; Wiebe, S, 2020
)
1
" The objective of the study was to assess the potential drug-drug interaction between imeglimin and cimetidine, a reference inhibitor of these transporters."( Lack of Drug-Drug Interaction Between Cimetidine, a Renal Transporter Inhibitor, and Imeglimin, a Novel Oral Antidiabetic Drug, in Healthy Volunteers.
Bolze, S; Chevalier, C; Dubourg, J; Fouqueray, P; Perrimond-Dauchy, S, 2020
)
1.05
"No clinically significant drug-drug interaction exists between imeglimin and cimetidine, a reference inhibitor of MATE1, MATE2-K, OCT1 and OCT2 transporters."( Lack of Drug-Drug Interaction Between Cimetidine, a Renal Transporter Inhibitor, and Imeglimin, a Novel Oral Antidiabetic Drug, in Healthy Volunteers.
Bolze, S; Chevalier, C; Dubourg, J; Fouqueray, P; Perrimond-Dauchy, S, 2020
)
1.06
" FTIR spectra combined with singular value decomposition (SVD) suggested by absorbance peak shifts of several vibration modes that the polymorphic transformations of the samples affect their molecular interactions."( Effects of Heat Treatment on Indomethacin-Cimetidine Mixture; Investigation of Drug-Drug Interaction Using Singular Value Decomposition in FTIR Spectroscopy.
Goto, S; Kuwashima, W; Otsuka, Y; Shimada, Y; Tanaka, Y; Yamaki, Y, 2021
)
0.89
" Herein, the impacts of metformin alone and in combination with cimetidine/ibuprofen on some Th1- and regulatory T (Treg) cell-related parameters were evaluated using a breast cancer (BC) model."( Modulatory Effects of Metformin Alone and in Combination with Cimetidine and Ibuprofen on T Cell-related Parameters in a Breast Cancer Model.
Hassan, ZM; Jafarzadeh, A; Khorramdelazad, H; Masoumi, J; Nemati, M; Oladpour, O; Rezayati, MT; Taghipour, F; Taghipour, Z, 2021
)
1.1
" Based on nonclinical in vitro characterization of gepotidacin metabolism, two phase I studies were conducted in healthy participants to investigate clinical drug-drug interactions (DDIs)."( Clinical assessment of gepotidacin (GSK2140944) as a victim and perpetrator of drug-drug interactions via CYP3A metabolism and transporters.
Barth, A; Brimhall, DB; Dumont, EF; Nguyen, D; Perry, CR; Shabbir, S; Srinivasan, M; Swift, B; Thomas, S; Zamek-Gliszczynski, MJ, 2023
)
0.91

Bioavailability

Cimetidine's bioavailability and its effect in primary hyperparathyroidism is clearly demonstrated. Means tacrine oral clearance was reduced by 30%; however, mean absorption rate and elimination half-life values were not affected by cimetidine.

ExcerptReferenceRelevance
" The age-related increase in bioavailability of oral cimetidine, as measured by AUC, was probably due to decreased total clearance of the drug, which resulted from the opposed changes (by themselves not significant) of distribution volume towards a decrease and of half-life towards an increase with age."( Blood level of cimetidine in relation to age.
Borgogelli, E; Lodola, E; Redolfi, A, 1979
)
0.86
"The bioavailability of parenteral cimetidine was tested in 12 volunteers in a balanced three-way crossover study."( Bioavailability of cimetidine in man.
Dubb, JW; Intoccia, AP; Randolph, WC; Stote, RM; Walkenstein, SS; Westlake, WJ, 1978
)
0.87
" 2 No significant changes in bioavailability were seen during treatment measured as the area under the blood concentration curve (AUC)."( The absorption of cimetidine before and during maintenance treatment with cimetidine and the influence of a meal on the absorption of cimetidine--studies in patients with peptic ulcer disease.
Bodemar, G; Fransson, L; Norlander, B; Walan, A, 1979
)
0.59
" Thus, it easily enters the systemic blood flow, resulting in almost complete bioavailability (75-100%)."( Pharmacokinetic profile of nicorandil in humans: an overview.
Frydman, A, 1992
)
0.28
"The pharmacokinetics and bioavailability of cefaclor advanced formulation (cefaclor AF) were investigated in two studies, one comparing healthy elderly and younger volunteers and the other assessing the effects of an antacid and H2-receptor antagonist on cefaclor AF bioavailability."( Pharmacokinetics of cefaclor AF: effects of age, antacids and H2-receptor antagonists.
Cerimele, BJ; Coleman, DL; DeSante, KA; Hatcher, BL; Kisicki, J; Satterwhite, JH, 1992
)
0.28
" We found that salicylic acid absorption from this solution was delayed but complete whereas the absorption of atenolol, cimetidine, frusemide and hydrochlorothiazide was four- to five-fold lower than expected from oral bioavailability studies."( Absorption of polar drugs following caecal instillation in healthy volunteers.
Kim, M; Riley, SA; Rowland, M; Sutcliffe, F; Turnberg, LA, 1992
)
0.49
" and cimetidine 1000 mg/d for 7 days led to a significant increase of the relative bioavailability of nimodipine."( Influence of the H2-receptor antagonists cimetidine and ranitidine on the pharmacokinetics of nimodipine in healthy volunteers.
Kuhlmann, J; Mück, W; Rämsch, KD; Seiberling, M; Wingender, W; Woelke, E, 1992
)
1.06
" The effect of gastric emptying and GI transit rate constants (Kl and K1, respectively), number of hypothetical gut compartments, and absorption rate constant at each site (Ka1, Ka2) on the time of occurrence of each peak (Tp1, Tp2), the theoretical fraction of the dose absorbed at each site (phi 1, phi 2), and the contribution of the second site to systemic drug exposure (expressed as phi 2rel) were examined."( Use of a pharmacokinetic model incorporating discontinuous gastrointestinal absorption to examine the occurrence of double peaks in oral concentration-time profiles.
Brouwer, KL; Pollack, GM; Suttle, AB, 1992
)
0.28
" In this study, the absorption and bioavailability of oral doses of each of three H2RAs, which are possible factors in these effects, were studied in healthy volunteers."( Does H2 receptor antagonist-resistant ulcer exist?--A review based on bioavailability in man.
Kawai, K, 1992
)
0.28
"The comparative bioavailability of cimetidine in cimetidine-alginate combinations has been investigated in twelve healthy volunteers in an open crossover study."( The comparative bioavailability of cimetidine-alginate treatments.
Britton, AM; Draper, PR; Nichols, JD, 1991
)
0.84
"To determine whether the H2-receptor antagonist, ranitidine, which is a potent inhibitor of gastric alcohol dehydrogenase activity in vitro, increases the bioavailability of orally administered ethanol (0."( Effects of ranitidine on blood alcohol levels after ethanol ingestion. Comparison with other H2-receptor antagonists.
Baraona, E; DiPadova, C; Frezza, M; Gentry, RT; Lieber, CS; Roine, R, 1992
)
0.28
"Peak blood alcohol concentrations, areas under the blood alcohol curve, first-pass metabolism, and bioavailability of orally consumed ethanol."( Effects of ranitidine on blood alcohol levels after ethanol ingestion. Comparison with other H2-receptor antagonists.
Baraona, E; DiPadova, C; Frezza, M; Gentry, RT; Lieber, CS; Roine, R, 1992
)
0.28
" First-pass metabolism of ethanol was decreased from 70 +/- 10 to 31 +/- 9 mg/kg of body weight, with a corresponding increase in ethanol bioavailability of 79."( Effects of ranitidine on blood alcohol levels after ethanol ingestion. Comparison with other H2-receptor antagonists.
Baraona, E; DiPadova, C; Frezza, M; Gentry, RT; Lieber, CS; Roine, R, 1992
)
0.28
"The effect of food intake on the bioavailability of sulpiride from a commercial film-coated tablet (100 mg/T) treated with polyvinylacetal diethylaminoacetate (AEA), which remains undissolved at pH above 4 approximately 5, were investigated in four healthy male subjects in the normal state or in a drug-induced achlorhydric state."( Effects of food intake on the bioavailability of sulpiride from AEA film-coated tablet having a pH-dependent dissolution characteristic in normal or drug-induced achlorhydric subjects.
Hamaguchi, T; Kobayashi, M; Mizuno, N; Shinkuma, D; Yamanaka, Y, 1991
)
0.28
" Residence probability functions and drug delivery probability functions provided by the approach appear useful for extending kinetic bioavailability concepts into a purely stochastic realm."( Stochastic interpretation of linear pharmacokinetics: a linear system analysis approach.
Veng-Pedersen, P, 1991
)
0.28
" In vivo, therapeutic doses of cimetidine (but not of famotidine) increased blood ethanol levels when ethanol was given orally, but not when it was given intravenously, indicating a significant contribution of the gastric ADH to the bioavailability and thereby the potential toxicity of ethanol."( Human gastric alcohol dehydrogenase: its inhibition by H2-receptor antagonists, and its effect on the bioavailability of ethanol.
Baraona, E; Caballeria, J; Greenstein, R; Hernández-Muñoz, R; Lieber, CS; Uppal, R, 1990
)
0.57
" The absolute oral bioavailability of moclobemide increased significantly after cimetidine administration (54% versus 68%), as did the maximum plasma concentration after a single oral dose (575 versus 787 ng/ml)."( Cimetidine alters the disposition kinetics of the monoamine oxidase-A inhibitor moclobemide.
Dellenbach, M; Eggers, H; Hoevels, B; Mayersohn, M; Pfefen, JP; Schoerlin, MP, 1991
)
1.95
" The bioavailability of cimetidine (200 mg) after oral administration to awake dogs was increased significantly by using tablets containing alginate."( [Biological availability of different oral cimetidine preparations in the dog].
Plass, H; Turnheim, K; Viernstein, H, 1990
)
0.85
"Moricizine is well absorbed after oral administration and undergoes extensive first-pass metabolism."( Clinical pharmacokinetics of moricizine.
Barbey, JT; Schwartz, SL; Siddoway, LA; Woosley, RL, 1990
)
0.28
" Cimetidine significantly increased the procainamide area under the serum concentration-time curve by 43%, decreased renal clearance by 36%, and decreased the ratio of systemic clearance of procainamide to bioavailability by 28%."( Interaction of steady-state procainamide with H2-receptor antagonists cimetidine and ranitidine.
Gallastegui, J; Jung, D; Paloucek, FP; Rodvold, KA, 1987
)
1.42
" The proposed method is rapid, accurate and precise, and it should be useful for clinical, bioavailability and pharmacokinetic studies of cimetidine."( An improved high performance liquid chromatographic method for determination of cimetidine and its major metabolite in plasma.
Cervantes-Campos, C; Delgadillo-Valencia, MP; Girard-Cuesy, ME; León-Urrea, F; Montoya-Cabrera, MA,
)
0.56
"In order to find ways to increase the usually very low bioavailability of praziquantel, the effect of cytochrome P-450 inhibitors on the metabolism of praziquantel was investigated in rats."( Inhibitory effects of cimetidine ketoconazole and miconazole on the metabolism of praziquantel.
Diekmann, HW; Overbosch, D; Schneidereit, M, 1989
)
0.59
"Amlodipine, a dihydropyridine calcium antagonist, was synthesized in an attempt to develop a compound with a pharmacokinetic profile characteristic of this class, which would also have an increased oral bioavailability and extended clearance time."( The pharmacokinetic profile of amlodipine.
Abernethy, DR, 1989
)
0.28
"The bioavailability of sulpiride taken in film-coated tablet form with sodium bicarbonate or cimetidine or with natural orange juice or diluted hydrochloric acid was studied."( The bioavailability of sulpiride taken as a film-coated tablet with sodium bicarbonate, cimetidine, natural orange juice or hydrochloric acid.
Hamaguchi, T; Kobayashi, M; Mizuno, N; Shinkuma, D; Yamanaka, Y, 1989
)
0.72
" The bioavailability of cimetidine was not significantly affected by metoclopramide and it was marginally reduced by the antacid."( Effects on cimetidine bioavailability of metoclopramide and antacids given two hours apart.
Barzaghi, N; Crema, F; Mescoli, G; Perucca, E, 1989
)
0.97
" The limitation of the MAT parameter is due to the fact that this parameter is scale independent in that it only considers the shape and not the magnitude of the drug level or absorption rate curve."( Center of gravity of drug level curves: a model-independent parameter useful in bioavailability studies.
Tillman, LG; Veng-Pedersen, P, 1989
)
0.28
" The area under the concentration curve after oral administration (AUCpo) was increased by 62% and the plasma oral clearance (Clpo) was decreased by 39% by cimetidine treatment, whereas the bioavailability (F) was not changed."( The inhibitory effects of cimetidine on elimination and distribution of propranolol in rats.
Asahina, M; Kawamata, Y; Kojo, M; Nishigaki, R; Shibasaki, S; Umemura, K, 1989
)
0.77
" This study indicates: (1) Simultaneous administration of aluminum hydroxide gel does not alter the bioavailability of cimetidine."( [Effect of antacids on the bioavailability and therapeutic efficacy of cimetidine].
Bai, G; Jia, BQ, 1989
)
0.72
" Cimetidine, when administered concurrently with metoprolol, could possibly cause an increase in plasma metoprolol concentrations or bioavailability through inhibition of hepatic P-450 metabolizing enzymes."( Effect of cimetidine and ranitidine on cardiovascular drugs.
Baciewicz, AM; Baciewicz, FA, 1989
)
1.59
" There were no changes in the rate of absorption and the renal clearance of rimantadine when it was administered with cimetidine."( Effect of cimetidine on the disposition of rimantadine in healthy subjects.
Brown, SY; Choma, N; Holazo, AA; Lee, LF; Wills, RJ, 1989
)
0.89
" Comparison of parenteral to enteral potencies suggests that ORF 17578 was well absorbed from the gastrointestinal tract of both species with a bioavailability profile similar to that of ranitidine."( Pharmacology of ORF 17578, a new histamine H2-receptor antagonist: comparison with cimetidine and ranitidine.
Katz, LB; Scott, CK; Shriver, DA, 1986
)
0.5
"), total pepsin output, and is well absorbed from the gastrointestinal tract."( Pharmacological profile of etintidine, a new histamine H2-receptor antagonist.
Katz, LB; Scott, CK; Shriver, DA, 1986
)
0.27
" These data indicate that cimetidine, but not ranitidine, causes a decrease in the bioavailability of tocainide and that neither agent alters the apparent elimination rate of tocainide."( The effect of histamine-2 receptor antagonists on tocainide pharmacokinetics.
Kapil, RP; Lalonde, RL; Mattern, AL; North, DS, 1988
)
0.58
" There was no difference in the area under the plasma concentration-time curve, rate of absorption or half-life of elimination of ibuprofen between the three treatments."( Do nizatidine and cimetidine interact with ibuprofen?
Forsyth, DR; Jayasinghe, KS; Roberts, CJ, 1988
)
0.61
" These results indicate that gastric alcohol dehydrogenase activity governs, in part, the systemic bioavailability of ethanol."( Effects of cimetidine on gastric alcohol dehydrogenase activity and blood ethanol levels.
Baraona, E; Caballeria, J; Lieber, CS; Rodamilans, M, 1989
)
0.67
" Although not affecting the pharmacodynamics of metoprolol, cimetidine did produce an increase in the bioavailability of metoprolol through inhibition of enzymes responsible for the first-pass elimination of the beta-blocker."( The racemic metoprolol H2-antagonist interaction.
Batra, H; Bowes, RJ; Davidson, EM; Garstang, FM; Rowland, M; Toon, S, 1988
)
0.52
" In Study II, the effect of food on the bioavailability of the two EB preparations was studied after a single dose of 500 mg (2 x 250 mg enterocoated tablets) and after multiple dosing (2 x 250 mg tid)."( Absorption of erythromycin acistrate and erythromycin base in the fasting and non-fasting state.
Männistö, PT; Pohto, P; Solkinen, A; Tuominen, RK; Vuorela, A, 1988
)
0.27
" The intimate relationship of the bioavailability of cimetidine and its effect in primary hyperparathyroidism is clearly demonstrated."( Hyperparathyroid crisis reviewed: a role for parenteral cimetidine?
Ackroyd, FW; Garcia, M; Glick, H; Goldstone, RJ; Minervini, D; Sherwood, JK, 1986
)
0.77
" This would suggest that cimetidine either increases the bioavailability of clobazam or reduces that of NDMC."( The effect of cimetidine on the single dose pharmacokinetics of oral clobazam and N-desmethylclobazam.
Edwards, D; Feely, MP; Haigh, JR; Peaker, S; Pullar, T, 1987
)
0.94
" The ileac pH value (measured by a pH meter with a micro pH combination electrode) was slightly higher than that in other intestinal sites, and the absorption rate constant (ka) following the administration of cimetidine into the ligated ileac loop was larger than that in the ligated duodenal and jejunal loops."( Study of the absorption site of cimetidine.
Funaki, T; Furuta, S; Kaneniwa, N; Watari, N, 1986
)
0.74
" The observed interaction can be explained by an increase in bioavailability or, more probably, by a decrease in biotransformation of flecainide in the presence of cimetidine."( Altered pharmacokinetics of oral flecainide by cimetidine.
de Schepper, PJ; Tjandra-Maga, TB; van Hecken, A; van Melle, P; Verbesselt, R, 1986
)
0.72
" The results indicate that sucralfate did not reduce the bioavailability of cimetidine."( Effect of sucralfate on the bioavailability of cimetidine.
Albin, H; Amouretti, M; Couzigou, P; Lalague, MC; Vincon, G, 1986
)
0.76
"2 1/kg/h, bioavailability 36%."( [Cimetidine pharmacokinetics].
Blinkov, IL; Davydov, SM; Karpenko, EV; Katrukha, SP; Kukes, VG,
)
1.04
"Metoclopramide was found to increase the absorption rate constant (ka) of cimetidine by the duodenum and jejunum in both ligated and unligated rats."( Effect of metoclopramide on the absorption of cimetidine in rats.
Funaki, T; Furuta, S; Kaneniwa, N, 1986
)
0.76
" 1980] have shown that the bioavailability of Augmentin is not affected by food."( Augmentin bioavailability following cimetidine, aluminum hydroxide and milk.
Clarke, HL; Horton, R; Jackson, D; Lau, D; Staniforth, DH, 1985
)
0.54
" Relative bioavailability during concurrent cimetidine treatment was 123% of that during the control trial."( Doxepin-cimetidine interaction: increased doxepin bioavailability during cimetidine treatment.
Abernethy, DR; Todd, EL, 1986
)
0.97
" 506 +/- 82 ng/ml X hr) and absolute bioavailability (35% +/- 7% vs."( Lack of interaction between verapamil and cimetidine.
Abernethy, DR; Schwartz, JB; Todd, EL, 1985
)
0.53
" The altered cimetidine effectiveness was not associated with reduced oral bioavailability and serum calcium was unchanged."( Development of cimetidine resistance in the Zollinger-Ellison syndrome.
Andersen, BN; Larsen, NE; Rune, SJ; Worning, H, 1985
)
0.99
" The bioavailability of the oral dose averaged 60."( Pharmacokinetics of clavulanic acid, given in combination with amoxycillin, in volunteers.
Fellner, H; Hedström, SA; Nilsson-Ehle, I; Nilsson-Ehle, P; Sjövall, J, 1985
)
0.27
" Cimetidine bioavailability parameters were identical in both groups, but Non-Responders had a higher peak concentration and a shorter time of peak concentration."( Factors predicting the therapeutic outcome of duodenal ulcer treatment with H2-receptor antagonists.
Gugler, R; Jensen, JC; Reimnitz, P; Rohner, HG; Somogyi, A, 1985
)
1.18
"The bioavailability of oral and intravenous cimetidine and ranitidine was studied in patients with compensated liver cirrhosis."( The pharmacokinetics of H2 receptor blocking agents in compensated liver cirrhosis.
Iemmolo, RM; Lirussi, F; Nassuato, G; Okolicsányi, L; Orlando, R; Strazzabosco, M; Venuti, M, 1984
)
0.53
" Bioavailability was unaffected by food and AUC increased linearly with dose to 100 mg."( Pharmacokinetic and gastric secretory studies of ranitidine in man.
Anderson, A; Hanson, RG; Louis, WJ; McNeil, JJ; Mihaly, GW; Smallwood, RA; Yeomans, ND, 1981
)
0.26
" Additionally, cimetidine decreases liver blood flow and increases the bioavailability of drugs with high hepatic extraction ratios."( Cimetidine as an inhibitor of drug metabolism: therapeutic implications and review of the literature.
Bauman, JH; Kimelblatt, BJ, 1982
)
2.06
" 2 Cimetidine caused no significant changes in the bioavailability of any of the two beta-adrenoceptor blockers and the rate of elimination of metoprolol was unaffected by the histamine H2-receptor blocker."( The effect of pretreatment with cimetidine on the bioavailability and disposition of atenolol and metoprolol.
Houtzagers, JJ; Regårdh, CG; Streurman, O, 1982
)
1.17
" These mechanisms include: (1) impaired hepatic drug metabolism due to inhibition of hepatic microsomal enzymes, (2) reduced hepatic blood flow, resulting in decreased clearance of drugs that are highly extracted by the liver, (3) increased potential for myelosuppression when administered concurrently with other drugs capable of causing myelosuppression, and (4) altered bioavailability of acid-labile drugs."( Review of cimetidine drug interactions.
Darvey, DL; Sorkin, EM, 1983
)
0.67
" Before pirenzepine will be given in combination with antacids, bioavailability of the drug should be proved during antacid treatment."( [Antacids in combination with other anti-ulcer agents].
Fritsch, WP, 1983
)
0.27
" Bioavailability and/or biotransformation are the factors most likely to account for the differences observed between species, and between in vivo and in vitro studies for this long-acting antisecretory agent."( In vivo and in vitro effects of CM 57755, a new gastric antisecretory agent acting on histamine H2 receptors.
Aureggi, G; Bianchetti, A; Carminati, P; Lavezzo, A; Manzoni, L; Nisato, D, 1984
)
0.27
" Temazepam bioavailability after oral administration is unchanged after either H2 receptor antagonist, or after the emulsion antacid."( The influence of H2 receptor antagonists on the plasma concentrations of midazolam and temazepam.
Collier, PS; Dundee, JW; Elliott, P; Elwood, RJ, 1984
)
0.27
" Systemic bioavailability is approximately 70% with cimetidine and 50% with ranitidine."( Comparative pharmacodynamics and pharmacokinetics of cimetidine and ranitidine.
Richards, DA, 1983
)
0.77
" The absolute bioavailability in healthy subjects is about 60%."( Clinical pharmacokinetics of cimetidine.
Gugler, R; Somogyi, A,
)
0.42
"05), and systemic bioavailability was reduced from 30."( The effects of enzyme induction and enzyme inhibition on labetalol pharmacokinetics.
Daneshmend, TK; Roberts, CJ, 1984
)
0.27
" Assessment of methylprednisolone disposition following oral and intravenous doses revealed no effect of cimetidine on the bioavailability (74 to 81 percent absorption) or plasma clearance (22 to 24 liters per hour) of the steroid."( Cimetidine-methylprednisolone-theophylline metabolic interaction.
Ebling, WF; Gardner, MJ; Green, AW; Jusko, WJ, 1984
)
1.92
" No influence can be expected from cimetidine on the bioavailability of these metal ions, the opposite being also true."( An assessment of the physiological significance of cimetidine interactions with copper and zinc in biofluids as based on the computer-simulated distribution of the involved complexes at therapeutic levels of the drug.
Akrivos, F; Berthon, G; Blais, MJ; Hoffelt, J, 1984
)
0.8
"In view of contradictory reports on the bioavailability of cimetidine in the presence of concomitantly administered antacids we studied the areas under the plasma concentration time curves (AUC) of cimetidine, the maximal concentrations (cmax) and the time, at which cmax was reached (tmax) in eight patients (five patients with duodenal ulcer, three patients with gastric ulcer) with and without the administration of an aluminum hydroxide magnesium hydroxide containing antacid (Maaloxan)."( Absence of in vivo and in vitro interactions of an aluminum hydroxide, magnesium hydroxide containing antacid with cimetidine in patients with peptic ulcer.
Allgayer, H; Paumgartner, G; Röllinghoff, W, 1983
)
0.72
" The failure of cimetidine to control gastric hypersecretion in these patients was attributed to both a diminished oral bioavailability and a decreased pharmacologic response to the drug."( Failure of cimetidine in Zollinger-Ellison syndrome.
Adamonis, AJ; Dreyer, M; Madura, M; Olinger, EJ; Schentag, JJ; Ziemniak, JA, 1983
)
1
" It was assumed that pretreatment with cimetidine, because of its inhibition of metabolic pathways of both demethylation and hydroxylation as well as its ability to reduce hepatic extraction of these drugs, would increase bioavailability and decrease clearance of both drugs."( Cimetidine interaction with imipramine and nortriptyline.
Henauer, SA; Hollister, LE, 1984
)
1.98
" After cimetidine, lidocaine apparent oral clearance (Clo) reduced 42% +/- 7%; oral bioavailability increased 35% +/- 10%; and systemic clearance (Cls) and volume of distribution at steady-state (Vdss) decreased 21% +/- 6% and 20% +/- 7%."( Lidocaine disposition--sex differences and effects of cimetidine.
Birkett, DJ; Foenander, T; Lillywhite, K; Miners, JO; Wanwimolruk, S; Wing, LM, 1984
)
0.97
" The results indicate that aluminium phosphate does not reduce the bioavailability of cimetidine and prednisolone."( Effect of aluminium phosphate on the bioavailability of cimetidine and prednisolone.
Albin, H; Bedjaoui, A; Begaud, B; Demotes-Mainard, F; Vincon, G, 1984
)
0.74
" imipramine doses indicated absolute bioavailability was 40."( Imipramine-cimetidine interaction: impairment of clearance and enhanced absolute bioavailability.
Abernethy, DR; Greenblatt, DJ; Shader, RI, 1984
)
0.66
" In contrast, measurement of urinary excretion showed higher bioavailability in the patients (66 +/- 23 vs 51 +/- 8%)."( Pharmacokinetics of cimetidine in advanced cirrhosis.
Grahnén, A; Jameson, S; Lindström, B; Lööf, L; Tyllström, J, 1984
)
0.59
"A two-way crossover bioavailability study of two commercial cimetidine formulations was performed on 24 healthy male volunteers."( Comparative bioavailability study of two tablet formulations of cimetidine.
Berardi, RR; Cohen, IA; Hyneck, ML; Lockwood, GF; Sakmar, E; Shukla, UA; Wagner, JG; Wells, JJ,
)
0.61
" The area under the plasma level curve as a measure for bioavailability was significantly increased in the two gastrectomy groups (17% and 23%, resp."( [Bioavailability of cimetidine after partial gastrectomy (author's transl)].
Gugler, R; Kliems, G; Somogyi, A; Wolf, H, 1980
)
0.58
" To study the bioavailability of cimetidine, it was necessary to develop a rapid and reliable high-performance liquid chromatography procedure for quantitating the drug in body fluids."( Bioanalysis of cimetidine by high-performance liquid chromatography.
Bartlett, JM; Segelman, AB, 1983
)
0.9
"The bioavailability and pharmacokinetics of cimetidine were studied following single oral and intravenous doses in subjects with severely impaired renal function (SIRF) and normal renal function (NRF)."( Comparison of bioavailability and pharmacokinetics of cimetidine in subjects with normal and impaired renal function.
Bockbrader, HN; Dancik, J; Guay, DR; Matzke, GR,
)
0.64
" Measurement of the plasma concentration of unchanged omeprazole revealed an intraduodenal bioavailability of approximately 70% whereas the oral bioavailability was only approximately 15%."( Inhibition of gastric acid secretion by omeprazole in the dog and rat.
Carlsson, E; Junggren, U; Larsson, H; Olbe, L; Sjöstrand, SE; Skånberg, I; Sundell, G, 1983
)
0.27
"1 The pharmacokinetics and bioavailability of cimetidine were studied after 200 mg oral and intravenous doses in 14 patients with liver cirrhosis, and results were compared to a control group of 12 ulcer patients."( Altered disposition and availability of cimetidine in liver cirrhotic patients.
Gugler, R; Müller-Liebenau, B; Somogyi, A, 1982
)
0.79
" The bioavailability of cimetidine calculated by deconvolution agrees with previous findings."( Pharmacokinetic analysis by linear system approach I: cimetidine bioavailability and second peak phenomenon.
Veng Pedersen, P, 1981
)
0.82
" The bioavailability of cimetidine measured as the ratio between the areas under the plasma concentration-time curves (AUC) after oral and intravenous administration was 76%."( Pharmacokinetics of cimetidine after single doses and during continuous treatment.
Bodemar, G; Norlander, B; Walan, A,
)
0.76
" It is shown for linear systems that if the absorption response and the response from an intravenous infusion or bolus administration are both well approximated by a polyexponential function, then the rate of absorption can be expressed as a sum of exponentials."( An algorithm and computer program for deconvolution in linear pharmacokinetics.
Veng-Pedersen, P, 1980
)
0.26
" 4 Pharmacokinetic studies showed the mean elimination half-life of cimetidine to be 100 +/- 25 min, the total body cimetidine clearance 652 +/- 223 ml/min, the mean volume of distribution at steady state 65 +/- 181 and the overall bioavailability 78%."( Cimetidine-a clinical and pharmacokinetic study.
Barber, HE; Brunt, PW; Griffiths, R; Hawksworth, GM; Jeffers, TA; Mowat, NA; Petersen, J; Petrie, JC; Webster, J, 1981
)
1.94
"01) reduced the bioavailability (area under the plasma level-time curve) of cimetidine, on average by one third."( Impaired cimetidine absorption due to antacids and metoclopramide.
Brand, M; Gugler, R; Somogyi, A, 1981
)
0.91
" 4 The oral bioavailability of caffeine was found to be complete in the one subject studied."( Decreased systemic clearance of caffeine due to cimetidine.
Broughton, LJ; Rogers, HJ, 1981
)
0.52
" 6 The bioavailability of tetracycline from tablets and suspension was found to be similar (31."( Effect of cimetidine on the absorption of orally administered tetracycline.
Bradbrook, ID; Fisher, P; House, F; Inns, P; Morrison, PJ; Rogers, HJ, 1980
)
0.66
"The pharmacokinetics and bioavailability of cimetidine after 200 mg given intravenously and orally was studied in 6 gastric and 6 duodenal ulcer patients aged between 28 and 64 years."( Pharmacokinetics and bioavailability of cimetidine in gastric and duodenal ulcer patients.
Gugler, R; Rohner, HG; Somogyi, A,
)
0.66
" The special problems associated with the evaluation of bioavailability in the presence of reabsorption are discussed."( Pharmacokinetics and bioavailability of cimetidine in humans.
Miller, R; Pedersen, PV, 1980
)
0.53
" Antibiotic bioavailability was measured by area under the plasma level-time curve, peak plasma level and urinary elimination."( Effect of cimetidine on absorption of oral tetracycline in mice.
Garty, M; Hurwitz, A, 1980
)
0.66
" Antibiotic bioavailability as measured by area under the serum level-time curve, peak serum level, and urinary elimination was not affected by cimetidine or sodium bicarbonate."( Effect of cimetidine and antacids on gastrointestinal absorption of tetracycline.
Garty, M; Hurwitz, A, 1980
)
0.86
" The bioavailability of cimetidine was unchanged (84 +/- 4% and 97 +/- 7%)."( Cimetidine clearance and bioavailability in hepatic cirrhosis.
Andreasen, PB; Døssing, M; Larsen, NE; Poulsen, HE; Sonne, J, 1981
)
2.01
" In the present work, absorption of cimetidine after a single dose in the fasted state was studied as a function of gastric pH in male beagle dogs to determine whether gastric pH plays a role in the double peak phenomenon and/or can account for the decrease in bioavailability when antacids are coadministered."( Gastric pH influences the appearance of double peaks in the plasma concentration-time profiles of cimetidine after oral administration in dogs.
Amidon, GL; Dressman, JB; Mummaneni, V, 1995
)
0.78
"Etoposide demonstrates incomplete and variable bioavailability after oral dosing, which may be due to its concentration and pH-dependent stability in artificial gastric and intestinal fluids."( Pharmacological attempts to improve the bioavailability of oral etoposide.
Clark, PI; Craft, H; Heap, L; Joel, SP; Robbins, S; Slevin, ML; Webster, L, 1995
)
0.29
"A biopharmaceutics drug classification scheme for correlating in vitro drug product dissolution and in vivo bioavailability is proposed based on recognizing that drug dissolution and gastrointestinal permeability are the fundamental parameters controlling rate and extent of drug absorption."( A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability.
Amidon, GL; Crison, JR; Lennernäs, H; Shah, VP, 1995
)
0.29
"The effects of cimetidine, bicarbonate and glucose on the bioavailability of the two brands of praziquantel (CAS 55268-74-1) available in Egypt were studied in normal healthy volunteers."( Effect of cimetidine, bicarbonate and glucose on the bioavailability of different formulations of praziquantel.
Bennett, JL; Botros, S; Ebeid, F; Metwally, A, 1995
)
1.05
" Second, the effect of magnesium/aluminium hydroxide on the relative bioavailability of nizatidine, famotidine, cimetidine and ranitidine was evaluated in healthy volunteers."( Drug interactions of H2-receptor antagonists.
Bachmann, KA; Jauregui, L; Levine, L; Miller, K; Reese, J; Sullivan, TJ, 1994
)
0.5
"The influence of concomitant antacid administration on the relative bioavailability of the H2-receptor antagonists cimetidine, famotidine, nizatidine and ranitidine, was investigated in a panel of 21 healthy, adult male volunteers in an eight-way crossover trial."( Short report: a comparative study of the interaction between antacid and H2-receptor antagonists.
Bachmann, KA; Jauregui, L; Levine, L; Miller, K; Reese, JH; Sullivan, TJ, 1994
)
0.5
" Comparison of the parenteral and enteral potencies indicated that FRG-8813 has a lower bioavailability than famotidine and cimetidine in rats and dogs."( Gastric antisecretory effect of FRG-8813, a new histamine H2 receptor antagonist, in rats and dogs.
Chida, Y; Inaba, N; Ohnishi, H; Onodera, S; Shibata, M; Yamaura, T, 1993
)
0.49
" Since the rate of absorption is also strongly influenced by the rapidity of gastric emptying, we have compared the relative importance of gastric acidity and gastric emptying in overall F absorption."( Influence of gastric acidity on fluoride absorption in rats.
Messer, HH; Ophaug, RH, 1993
)
0.29
" These effects are of minor clinical importance and seem most likely be due to a decrease of the rate of absorption of ritanserin during concurrent administration of cimetidine/ranitidine."( Effect of concomitantly administered cimetidine or ranitidine on the pharmacokinetics of the 5-HT2-receptor antagonist ritanserin.
Benn, HP; Buschmann, M; Jähnchen, E; Seiler, KU; Szathmary, S; Trenk, D, 1993
)
0.75
" Mean tacrine oral clearance was reduced by 30%; however, mean absorption rate and elimination half-life values were not affected by cimetidine."( Inhibition of tacrine oral clearance by cimetidine.
deVries, TM; Forgue, ST; Reece, PA; Sedman, AJ, 1996
)
0.77
"The aim of the study was to investigate whether mannitol at amounts relevant to pharmaceutical formulations would alter the oral bioavailability of cimetidine, a drug primarily absorbed from the small bowel."( The effect of mannitol on the oral bioavailability of cimetidine.
Adkin, DA; Davis, SS; Huckle, PD; Sparrow, RA; Wilding, IR, 1995
)
0.74
" This open, randomized, crossover study was conducted to examine the effects of aspirin, the antacid Maalox (Rhone-Poulenc Rorer, Cologne, Germany), and cimetidine on the pharmacokinetics and bioavailability of a single oral dose of meloxicam 30 mg in healthy male volunteers."( Interaction of meloxicam with cimetidine, Maalox, or aspirin.
Busch, U; Heinzel, G; Narjes, H; Nehmiz, G, 1996
)
0.78
" The model was also used to simulate bioavailability and plasma concentrations versus time profiles for various parameter values."( Applications and simulations of a discontinuous oral absorption pharmacokinetic model.
Boudinot, FD; Witcher, JW, 1996
)
0.29
" Simulations demonstrate the effects of various absorption parameters and gastroin-testinal tract transit parameters on bioavailability and plasma concentration profiles."( Applications and simulations of a discontinuous oral absorption pharmacokinetic model.
Boudinot, FD; Witcher, JW, 1996
)
0.29
"This discontinuous oral absorption pharmacokinetic model can be a useful tool in characterizing absorption phases, disposition, and bioavailability of drugs exhibiting two absorption peaks following oral administration."( Applications and simulations of a discontinuous oral absorption pharmacokinetic model.
Boudinot, FD; Witcher, JW, 1996
)
0.29
" The pharmacokinetic parameters maximum plasma concentration, time to maximum plasma concentration, absorption half-life, and absorption rate constant did not differ between groups, suggesting that the formation of albendazole sulfoxide was not altered by the administration of dexamethasone, combined or not with cimetidine."( Therapy for neurocysticercosis: pharmacokinetic interaction of albendazole sulfoxide with dexamethasone.
Bonato, PS; Lanchote, VL; Marques, MP; Takayanagui, OM, 1997
)
0.47
" The median (range) extent of intragastric bioavailability was 14."( Pharmacokinetics of intravenous and intragastric cimetidine in horses. I. Effects of intravenous cimetidine on pharmacokinetics of intravenous phenylbutazone.
Ashcraft, SM; Dyke, TM; Gerken, DF; Reed, SM; Sams, RA, 1997
)
0.55
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents."( QSAR model for drug human oral bioavailability.
Topliss, JG; Yoshida, F, 2000
)
0.31
"The low bioavailability of albendazole affects the therapeutic response in patients with echinococcosis."( Effect of dose increase or cimetidine co-administration on albendazole bioavailability.
Butter, JJ; Kager, PA; Koopmans, RP; Nagy, J; Schipper, HG; Van Boxtel, CJ,
)
0.43
"The role of gastrointestinal motility and pH in determining cimetidine bioavailability as well as double peaks in plasma profiles following oral administration, in the quiescent or active phase of antral motility, to humans in the fasted state was examined."( Variability in cimetidine absorption and plasma double peaks following oral administration in the fasted state in humans: correlation with antral gastric motility.
Amidon, GL; Barnett, JL; Hayashi, Y; Lesko, LJ; Ramachandran, C; Shah, VP; Takamatsu, N; Welage, LS; Yamamoto, R, 2002
)
0.91
" One limitation to its use is the necessity of co-injecting cimetidine to increase its bioavailability and hence its sensitivity for PET detection."( Use of 5-[(76)Br]bromo-2'-fluoro-2'-deoxyuridine as a ligand for tumour proliferation: validation in an animal tumour model.
Bergström, M; Borbath, I; Grégoire, V; Långström, B; Laryea, D; Pauwels, S, 2002
)
0.56
" Apparent volume of distribution normalized by the bioavailability (Vd/F) of diltiazem increased significantly in rabbits pretreated with cimetidine increased."( The influence of cimetidine on the pharmacokinetics of diltiazem and its main metabolite in rabbits.
Burm, JP; Choi, JS, 2004
)
0.87
"This study suggests that verapamil increases fexofenadine exposure probably because of an increase in bioavailability through P-glycoprotein inhibition and that probenecid slightly increases the area under the plasma concentration-time curve of fexofenadine as a result of a pronounced reduction in renal clearance."( Different effects of three transporting inhibitors, verapamil, cimetidine, and probenecid, on fexofenadine pharmacokinetics.
Sugawara, K; Tateishi, T; Uno, T; Yasui-Furukori, N, 2005
)
0.57
"Cytochrome P450 3A4 (CYP3A4) and P-glycoprotein (PGP) are important determinants of the oral bioavailability and clearance of tacrolimus."( Impact of gastric acid suppressants on cytochrome P450 3A4 and P-glycoprotein: consequences for FK506 assimilation.
Lemahieu, WP; Maes, BD; Vanrenterghem, Y; Verbeke, K, 2005
)
0.33
"5% w/v pectin gels formed in situ in rabbit stomach was sustained over a period of 12 hours giving a theophylline bioavailability some seven fold higher than when administered from a commercial syrup."( Oral sustained delivery of theophylline and cimetidine from in situ gelling pectin formulations in rabbits.
Attwood, D; Itoh, K; Kubo, W; Miyazaki, S, 2005
)
0.59
" The area under the plasma concentration-time curve from 0 to 12 hours (AUC(12)) and AUC from time zero to infinity (AUC(infinity)), peak plasma concentration (C(max)), absolute bioavailability (F) and mean residence time (MRT) were evaluated and statistically compared among formulations."( Feasibility of biowaiver extension to biopharmaceutics classification system class III drug products: cimetidine.
Amidon, GL; Dressman, JB; Jantratid, E; Prakongpan, S, 2006
)
0.55
" Human oral bioavailability is an important pharmacokinetic property, which is directly related to the amount of drug available in the systemic circulation to exert pharmacological and therapeutic effects."( Hologram QSAR model for the prediction of human oral bioavailability.
Andricopulo, AD; Moda, TL; Montanari, CA, 2007
)
0.34
"Naproxen, a non-steroidal anti-inflammatory drug (NSAID), is a biopharmaceutics classification system (BCS) class II drug whose bioavailability is rate-limited by its dissolution."( Enhanced dissolution rate and synchronized release of drugs in binary systems through formulation: Amorphous naproxen-cimetidine mixtures prepared by mechanical activation.
Aaltonen, J; Allesø, M; Chieng, N; Rades, T; Rantanen, J; Rehder, S, 2009
)
0.56
" A mean absolute bioavailability of 75% was calculated following a single oral administration of 5 mg cimetidine/kg body weight."( Pharmacokinetics of cimetidine in dogs after oral administration of cimetidine tablets.
Burgaud, S; Horspool, LJ; Le Traon, G, 2009
)
0.89
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
0.36
" The compound was well absorbed and exhibited approximately linear pharmacokinetics in the oral dose range of 100 to 1000 mg in human."( Preclinical and clinical evidence for the collaborative transport and renal secretion of an oxazolidinone antibiotic by organic anion transporter 3 (OAT3/SLC22A8) and multidrug and toxin extrusion protein 1 (MATE1/SLC47A1).
Adams, WJ; Balogh, LM; Brayman, TG; Cox, SR; Kumar, V; Lai, Y; Sampson, KE; Stevens, JC, 2010
)
0.36
"The Biopharmaceutical Classification System (BCS) guidance issued by the FDA allows waivers for in vivo bioavailability and bioequivalence studies for immediate-release (IR) solid oral dosage forms only for BCS class I drugs."( The biowaiver extension for BCS class III drugs: the effect of dissolution rate on the bioequivalence of BCS class III immediate-release drugs predicted by computer simulation.
Amidon, GL; Tsume, Y, 2010
)
0.36
" Protective effect of ginger extract (GE) against ulcer is well documented, but therapeutic use is compromised due to poor bioavailability and physicochemical properties."( Development and evaluation of a gastro-retentive delivery system for improved antiulcer activity of ginger extract (Zingiber officinale).
Kumar Singh, P; Pal Kaur, I, 2011
)
0.37
"The bioavailability parameters were found as: Cmax 1508."( Pharmacokinetic study of hydroxypropylmethylcellulose microparticles loaded with cimetidine.
Ahmad, M; Hussain, I; Karim, S; Khan, SA; Kousar, R; Murtaza, G,
)
0.36
"For prolonged drug release in the stomach, developed floating microparticles of cimetidine (FMC3) may be used, thereby improving the bioavailability and patient compliance."( Pharmacokinetic study of hydroxypropylmethylcellulose microparticles loaded with cimetidine.
Ahmad, M; Hussain, I; Karim, S; Khan, SA; Kousar, R; Murtaza, G,
)
0.58
" The absorption rate coefficients of all the assayed compounds did not show statistically significant differences between male and female rats consequently all the individual values were combined to compare between reabsorption methods."( Validation of phenol red versus gravimetric method for water reabsorption correction and study of gender differences in Doluisio's absorption technique.
Bermejo, M; Gonzalez-Alvarez, I; Gonzalez-Alvarez, M; Tuğcu-Demiröz, F, 2014
)
0.4
"A reliable prediction of the oral bioavailability in humans is crucial and of high interest for pharmaceutical and food industry."( A new approach to predict human intestinal absorption using porcine intestinal tissue and biorelevant matrices.
Grossouw, D; Krul, CA; van de Steeg, E; Verwei, M; Westerhout, J; Wortelboer, HM; Zeijdner, EE, 2014
)
0.4
" The first finding is that the oral bioavailability of cyclosporine A (CsA), which is an immunosuppressant, was decreased by increased first-pass metabolism due to elevated CYP3A and P-glycoprotein (P-gp) specifically in the upper small intestine after liver I/R."( [Molecular Biological Analysis of Factors Influencing Pharmacokinetics to Achieve Personalized Pharmacotherapy].
Ikemura, K, 2015
)
0.42
", ip) indicate that the liver is the primary site of biotransformation of the compound, suggesting that both 22a and its metabolite(s) are active, compensating probably low bioavailability of the parent molecule."( Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
Bednarski, M; Gunia-Krzyżak, A; Marona, H; Nitek, W; Pękala, E; Powroźnik, B; Słoczyńska, K; Walczak, M; Waszkielewicz, AM; Żesławska, E, 2016
)
0.43
"The aim of this study was (1) to determine how closely physiologically based pharmacokinetic (PBPK) models can predict oral bioavailability using a priori knowledge of drug-specific properties and (2) to examine the influence of the biopharmaceutics classification system class on the simulation success."( Forecasting oral absorption across biopharmaceutics classification system classes with physiologically based pharmacokinetic models.
Aarons, L; Darwich, A; Dressman, J; Hansmann, S; Margolskee, A, 2016
)
0.43
" The apparent permeability coefficients of PBDEs indicated that tri- to hepta-BDEs were poorly absorbed compounds."( The transepithelial transport mechanism of polybrominated diphenyl ethers in human intestine determined using a Caco-2 cell monolayer.
An, J; Lei, B; Wang, M; Yang, D; Yu, Y; Zhang, K; Zhang, X; Zhong, Y, 2017
)
0.46
" The purpose of this study was to determine if administration of oral tramadol with suspected metabolism inhibitors (ketoconazole, cimetidine) would lead to improved bioavailability of tramadol and M1."( The effects of ketoconazole and cimetidine on the pharmacokinetics of oral tramadol in greyhound dogs.
Black, J; KuKanich, B; KuKanich, K, 2017
)
0.94
"Docetaxel (DTX) was effective in the treatment of neoplasm but could only be administered intravenously with the poor oral bioavailability owing to its undesirable solubility, remarkably metabolic conversion, and other factors."( Preparation of Deoxycholate-Modified Docetaxel-Cimetidine Complex Chitosan Nanoparticles to Improve Oral Bioavailability.
Fang, T; Shen, Q; Sun, L; Xu, Y; Yang, Y, 2019
)
0.77
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

Cimetidine was used at a dosage of one gram per day and treatment continued over a period of 4 weeks. This DRF at the low dosage of cimetidine used in this study compared with known radioprotectors is very promising.

ExcerptRelevanceReference
" When the H2-receptor antagonists burimamide, metiamide and cimetidine were labelled with 35S, 14C or 3H and dosed to rats, whole body autoradiography showed that the stomach was predominantly labelled in the glandular mucosa from 5 to 120 min after administration."( Localization of histamine and histamine H2-receptor antagonists in the gastric mucosa.
Cross, SA, 1977
)
0.5
"For the definition of histamine receptors the following prerequisites must be fulfilled: (1) Course of dose-response curves according to the mass-action law; (2) parallel displacement of these curves to the right in the presence of antagonists; (3) inhibition only by specific histamine antagonists; (4) slope of a Schild-plot not significantly different from unity."( [Histamine and its role in peptic gastric diseases: the discovery of histamine-H2-receptor antagonists].
Barth, H; Lorenz, W, 1978
)
0.26
" Dose-response curves to impromidine were displaced to the right in the presence of cimetidine."( Cardiovascular studies with impromidine (SK&F 92676), a new very potent and specific histamine H2-receptor agonist.
Gristwood, RW; Harvey, CA; Owen, DA, 1979
)
0.48
" Each amine was given in 45-min incremental step doses to constitute full dose-response curves."( Evidence for a histamine H2 receptor that inhibits pepsin secretion in the dog.
Hirschowitz, BI; Hutchison, GA, 1977
)
0.26
" When cimetidine is to be used for recurrent ulceration probably the dosage and duration of treatment should be increased."( Cimetidine for recurrent ulcer after vagotomy or gastrectomy: a randomised controlled trial.
Kennedy, T; Spencer, A, 1978
)
2.18
" Cimetidine was safe in the dosage and duration used, no symptomatic, haematological, or biochemical abnormalities occurring during the trial."( Controlled trial of maintenance cimetidine treatment in healed duodenal ulcer: short and long-term effects.
Batchelor, AJ; Dronfield, MW; Langman, MJ; Larkworthy, W, 1979
)
1.45
" Group III (n = 4) dogs were not operated upon and received all drugs in full dosage in order to test any direct toxic effect on normal kidneys."( Cimetidine for kidney transplantation: experimental observations.
Toledo-Pereyra, LH; Zammit, M, 1979
)
1.7
" According to American studies, antacid therapy in the above-mentioned dosage may achieve a similar healing rate in duodenal ulcer patients in acute attack."( [Cimetidine versus antacids].
Halter, F, 1979
)
1.17
" Intragastric administration of PB, CM or TP produced dose-dependent inhibition of gastric ulceration with parallel dose-response curves."( Synergistic actions of propantheline bromide with cimetidine and thiopropazate hydrochloride in the prevention of stress ulcer formation in rats.
Bianchi, RG; Calhoun, DW; Dajani, EZ, 1979
)
0.51
" Cimetidine was used at a dosage of one gram per day and treatment continued over a period of 4 weeks."( A double-blind study of cimetidine in patients with duodenal or gastric ulcer in Greece.
Kalogerakou-Ioannidi, E; Manousos, ON; Nicolaou, A; Scandalis, N; Zografos, A, 1978
)
1.48
" Due to a short elimination half-life and wide therapeutic index, dosage adjustments are not necessary in patients exhibiting moderate renal dysfunction."( Pharmacokinetics of cefaclor AF: effects of age, antacids and H2-receptor antagonists.
Cerimele, BJ; Coleman, DL; DeSante, KA; Hatcher, BL; Kisicki, J; Satterwhite, JH, 1992
)
0.28
" From this series, compound 17c (SK&F 96067) was shown to be a potent inhibitor of histamine-stimulated gastric acid secretion after oral dosing in the Heidenhain pouch dog and was selected for further development and evaluation in man."( Reversible inhibitors of the gastric (H+/K+)-ATPase. 3. 3-substituted-4-(phenylamino)quinolines.
Brown, TH; Ife, RJ; Keeling, DJ; Leach, CA; Meeson, ML; Parsons, ME; Reavill, DR; Theobald, CJ; Wiggall, KJ, 1992
)
0.28
" The results were opposite to other studies, probably because the dose and dosing intervals were different."( Effect of traditional Chinese herbal medicines on the pharmacokinetics of western drugs in Sprague-Dawley rats of different ages (II): Aminophylline-huan shao tan and aminophylline-pu chung yi chi tang.
Chen, SM; Hou, SJ; Lin, SY; Perng, RI; Young, TK, 1992
)
0.28
"5% of the 27 patients were treated with a maintenance dosage of H2 blockers and 29."( Peptic ulcer in cirrhotic patients: a short- and long-term study with antisecretory drugs.
Battaglia, G; Burra, P; Di Mario, F; Dotto, P; Germanà, B; Gottardello, L; Grassi, SA; Leandro, G; Salvagnini, M; Vianello, F,
)
0.13
"6 and 10 mg/kg), resulting in a parallel, rightward shift in the MOR dose-response curve."( Modulation of morphine antinociception by antagonism of H2 receptors in the periaqueductal gray.
Hough, LB; Nalwalk, JW, 1992
)
0.28
" There was no significant difference of integrated 6-h plasma ethanol concentration, peak ethanol concentration, or time to reach peak ethanol concentration after dosing with either ranitidine, cimetidine or famotidine or placebo."( Ranitidine, cimetidine, famotidine have no effect on post-prandial absorption of ethanol 0.8 g/kg taken after an evening meal.
Fraser, AG; Hudson, M; Pounder, RE; Rosalki, SB; Sawyerr, AM; Smith, M, 1992
)
0.85
" Chronic oral dosing significantly lowered both the systemic and oral clearance of diltiazem, with no changes in either the volume of distribution or blood binding of diltiazem."( The effects of chronic oral diltiazem and cimetidine dosing on the pharmacokinetics and negative dromotropic action of intravenous and oral diltiazem in the dog.
Bai, SA; Lankford, S; Maskasame, C, 1992
)
0.55
" dosing of this selective compound is necessary for achieving adequate results."( Famotidine in gastroesophageal reflux disease (GERD).
Wesdorp, IC, 1992
)
0.28
" Patients were dosed to steady-state with an oral, sustained-release formulation of theophylline given in therapeutic doses twice daily for 2 weeks."( Comparative investigation of the influence of nizatidine, ranitidine, and cimetidine on the steady-state pharmacokinetics of theophylline in COPD patients.
Bachmann, K; Jauregui, L; Levine, L; Martin, M; Mauro, LS; Sullivan, TJ, 1992
)
0.51
"In a 48-week study of 319 duodenal ulcer patients, symptomatic self-care with an histamine H2-receptor antagonist (flexible self-chosen dosing with cimetidine 0, 400 or 800 mg/day) was compared with maintenance treatment (cimetidine 400 mg nocte)."( The long-term management of duodenal ulceration using an H2-antagonist: symptomatic self-care compared with maintenance treatment.
Festen, H; Korman, M; Pounder, RE, 1992
)
0.48
" However, many authors report that an H2RA resistant ulcer can be cured by increasing the dosage of H2RA, or using another H2RA."( Does H2 receptor antagonist-resistant ulcer exist?--A review based on bioavailability in man.
Kawai, K, 1992
)
0.28
" While very safe, clinicians need to know correct dosing guidelines, drug interactions, and side effect profiles."( The clinical use of histamine-2 receptor antagonists.
Michocki, RJ; Richardson, JP, 1992
)
0.28
" A statistically significant rise in nocturnal acidity was observed after all regimens, except after dosing with famotidine."( Rebound intragastric hyperacidity after abrupt withdrawal of histamine H2 receptor blockade.
Nwokolo, CU; Pounder, RE; Sawyerr, AM; Smith, JT, 1991
)
0.28
" At each dosage level, semilogarithmic plots of concentration vs."( Elimination of the antiviral drug 5-ethyl-2'-deoxyuridine by the isolated perfused rat liver.
Joly, JM; Williams, WM,
)
0.13
" Histamine increased in a dose-dependent manner cellular cAMP content in L cells permanently transfected with this gene, and preincubation of the cells with the H2-selective antagonist cimetidine shifted the dose-response curve to the right."( Molecular cloning of a gene encoding the histamine H2 receptor.
Campbell, V; DelValle, J; Gantz, I; Logsdon, C; Schäffer, M; Uhler, M; Yamada, T, 1991
)
0.47
" Six dogs were given cimetidine at dosage of 10 mg/kg orally every 8 hours, and 6 dogs were given omeprazole orally at dosage of 2 mumol/kg (0."( Comparison of effects of cimetidine and omeprazole on mechanically created gastric ulceration and on aspirin-induced gastritis in dogs.
Bright, RM; DeNovo, RC; Jenkins, CC; Patton, CS; Rohrbach, BW, 1991
)
0.9
"A new chewable tablet containing cimetidine 200 mg and alginic acid 500 mg, at a dosage of one tablet four times daily, was compared in a 12 week randomised study with the standard dosage of cimetidine (400 mg four times daily) in the management of oesophageal reflux disease."( Combination of cimetidine and alginic acid: an improvement in the treatment of oesophageal reflux disease. Cooperative Oesophageal Group.
, 1991
)
0.92
" In a separate group of ten patients whose previous reactions to RCM were life threatening (shock), pretreatment was accompanied by a provocative dosing regimen."( Comparison of three pretreatment protocols to prevent anaphylactoid reactions to radiocontrast media.
Lieberman, PL; Marshall, GD, 1991
)
0.28
" Each group had a control study and a repeat study after 7 days dosing with either placebo or an H2-receptor antagonist (300 mg ranitidine nocte, 800 mg cimetidine nocte, or 40 mg famotidine nocte)."( The effect of ranitidine, cimetidine or famotidine on low-dose post-prandial alcohol absorption.
Fraser, AG; Hudson, M; Pounder, RE; Prewett, EJ; Rosalki, SB; Sawyerr, AM, 1991
)
0.78
" Cimetidine was also tested in these subjects at half the dosage administered to the first group of subjects."( Inhibition of gastric acid secretion reduces zinc absorption in man.
D'Inca, R; D'Odorico, A; Martin, A; Montino, MC; Naccarato, R; Rossetto, L; Sturniolo, GC, 1991
)
1.19
" At repeat endoscopy after four weeks of therapy, complete ulcer healing was achieved in 78% of patients on twice daily dosage and 79% of patients on single daily dosage."( Controlled trial of twice a day versus once a day cimetidine therapy for duodenal ulcer.
Aggarwal, R; Goenka, MK; Gupta, BB; Kochhar, R; Mehta, SK, 1990
)
0.53
" The aims of the present study were, first, to determine whether low-dose cimetidine treatment was as effective as standard doses in acute duodenal ulcer treatment of patients in Singapore, and second, to compare a single nocturnal dosage regimen with a twice daily regimen."( Low-dose cimetidine in the acute treatment of duodenal ulcer. Comparison of a single nocturnal dose regimen with a twice daily regimen.
Guan, R; Kang, JY; Labrooy, SJ; Math, MV; Tay, HH; Wee, A; Yap, I,
)
0.78
" Thioperamide did not alter the dose-response curve to exogenous histamine (0."( Histamine H3 receptors modulate antigen-induced bronchoconstriction in guinea pigs.
Barnes, PJ; Ichinose, M, 1990
)
0.28
"The efficacy and safety of two dosage regimens of cimetidine were compared in a single-blind study of 50 adults with endoscopically proven duodenal ulcers."( A comparative clinical trial of duodenal ulcer healing with two regimens of cimetidine: 800 mg once nightly and 400 mg twice daily.
Arvanitakis, C; Giannoulis, E; Nikopoulos, A; Theoharidis, A; Tourkantonis, A,
)
0.61
"The effects of steady state dosing with omeprazole and cimetidine on plasma diazepam levels have been studied in 12 healthy males."( Effect of omeprazole and cimetidine on plasma diazepam levels.
Andersson, T; Andrén, K; Cederberg, C; Edvardsson, G; Heggelund, A; Lundborg, P, 1990
)
0.83
"This study was done to determine if the pharmacokinetics and gastric pH response of intravenous cimetidine are superior to oral dosing in seriously ill patients."( Pharmacokinetics and pharmacodynamics of oral and intravenous cimetidine in seriously ill patients.
Cutler, RE; Forland, SC; Sandborn, WJ; Strong, RM, 1990
)
0.74
" Two separate dose-response tests were also conducted with DPH and HPPH with a MAS modulated by various mixed functional oxidase inhibitors [carbon monoxide (CO) (broad spectrum cytochrome P450), cimetidine (mainly cytochrome P450), and ellipticine (cytochrome P448)] and an epoxide hydrolase inhibitor (cyclohexene oxide)."( Use of Frog Embryo Teratogenesis Assay-Xenopus and an exogenous metabolic activation system to evaluate the developmental toxicity of diphenylhydantoin.
Bantle, JA; Fort, DJ, 1990
)
0.47
" Blood samples for the determination of ciprofloxacin concentrations were taken at 0, 1, 2, 4, 6, and 12 hr after dosing on the first and seventh day of drug administration."( Metabolic interactions of ciprofloxacin.
Csiba, A; Graber, H; Ludwig, E; Székely, E,
)
0.13
"Bioavailability of Different Oral Dosage Forms of Cimetidine in Dogs."( [Biological availability of different oral cimetidine preparations in the dog].
Plass, H; Turnheim, K; Viernstein, H, 1990
)
0.79
" The steady-state serum concentrations of digoxin and digitoxin can be affected if the changes in absorption are of sufficient magnitude, and adjustments in digoxin or digitoxin dosage may be required."( Current status of cardiac glycoside drug interactions.
Hooymans, PM; Merkus, FW,
)
0.13
" A cutaneous vasodilator response was also observed in substance P treated and contralateral ears, but a bell-shaped dose-response relationship was apparent."( Histamine involvement in the local and systemic microvascular effects produced by intradermal substance P.
Ledgard, SE; Owen, DA; Pipkin, MA; Woodward, DF, 1985
)
0.27
" The dose-response curve for carbachol was biphasic."( Stimulation of acid formation by histamine, carbachol and pentagastrin in isolated pig parietal cells.
Ljungström, M; Mårdh, S; Norberg, L; Vega, FV, 1986
)
0.27
" Dose-response curves to TG showed nonparallel increases in both parameters."( Stimulation of oxyntic and histaminergic cells in gastric mucosa by gastrin C-terminal tetrapeptide.
Michelangeli, F; Ruiz, MC, 1986
)
0.27
" This study demonstrates the efficacy and safety of enprostil in the treatment of active duodenal ulcer at the dosage of 35 micrograms twice daily."( [Efficacy and tolerability of enprostil in the treatment of duodenal ulcer. Comparison with cimetidine].
Andrieu, J; Evreux, M; Frexinos, J; Guerre, J; Joubert, M; Michel, H; Vicari, F, 1989
)
0.5
" BWA1433U induced a parallel shift of the adenosine dose-response curve to the right; however, it had no significant inhibitory effect on the decrease in lobar arterial pressure in response to ATP."( Adenosine does not mediate the pulmonary vasodilator response of adenosine 5'-triphosphate in the feline pulmonary vascular bed.
Hyman, AL; Kadowitz, PJ; Lippton, H; Neely, CF; Neiman, M, 1989
)
0.28
" Intravenous dosing of TA-2711 (10-100 mg/kg) never produced such effects on ethanol-induced lesions and pepsin activity as observed by oral administration."( Effects of 12-sulfodehydroabietic acid monosodium salt (TA-2711), a new anti-ulcer agent, on gastric secretion and experimental ulcers in rats.
Magaribuchi, T; Onoda, Y; Tamaki, H, 1989
)
0.28
" The dose-response (D-R) curves for histamine (H) in the HT group shifted leftward and upward as compared with the sham-operated (S) group."( Effect of histamine on isolated working guinea pig heart with left ventricular hypertrophy produced by pressure overload.
Guo, ZG; Luo, WS, 1989
)
0.28
" With chronic oral dosing of amlodipine once daily for 14 days, support was provided for the linearity of amlodipine's pharmacokinetics and absence of such with chronic oral dosing with verapamil, diltiazem, and nifedipine."( The pharmacokinetic profile of amlodipine.
Abernethy, DR, 1989
)
0.28
" Both slopes of the dose-response regression line are parallel in effect."( Effect of the radioprotector WR-2721 on operant behavior in the rat.
Lee, JD; Lee, SF; Lin, CH; Liu, WF; Ma, C; Shih, JH,
)
0.13
" The two high bioavailability subjects took one tablet (100 mg) with 100 ml of water (1) alone, (2) together with 1 g of sodium bicarbonate or (3) during concurrent dosing with cimetidine, 200 mg three times a day."( The bioavailability of sulpiride taken as a film-coated tablet with sodium bicarbonate, cimetidine, natural orange juice or hydrochloric acid.
Hamaguchi, T; Kobayashi, M; Mizuno, N; Shinkuma, D; Yamanaka, Y, 1989
)
0.69
" No changes in DNA synthesis, percentage of labelled nuclei and transaminase were detected when the agents were added to the hepatocytes in culture at concentrations within the effective pharmacological dosage and 30 times higher."( Effect of cimetidine, ranitidine, famotidine and omeprazole on hepatocyte proliferation in vitro.
Amoruso, A; Barone, M; Di Leo, A; Francavilla, A; Ingrosso, M; Makowka, L; Panella, C; Polimeno, L; Starzl, TE, 1989
)
0.68
" A chronic dosing study was conducted in eight healthy subjects who received, in random order, amiloride (5 mg daily), cimetidine (400 mg twice daily), both drugs together, and a control phase in which no drug was present."( Renal tubular secretion of amiloride and its inhibition by cimetidine in humans and in an animal model.
Bochner, F; Hovens, CM; Muirhead, MR; Somogyi, AA,
)
0.58
" At a dosage one fifth of Cimetidine (0."( Anti-acid secretion activity of drugs cimetidine, ranitidine, tiotidine D 15,144 in dogs fixed with gastric fistulae.
Jais, AM; Ridzwan, BH; Waton, NG, 1989
)
0.85
" Cimetidine dosing intervals were based upon the degree of renal and hepatic dysfunction due to pharmacokinetic considerations."( Safety and acid-suppressant properties of histamine2-receptor antagonists for the prevention of stress-related mucosal damage in critical care patients.
Carter, CA; Schentag, JJ; Welage, LS, 1989
)
1.19
" It was found that non-toxic dosage of cimetidine had no significant effect on CFU-s of the normal mouse, but it inhibited CFU-GM growth with a dosage-dependent relationship and the recovery of CFU-s formation from sublethal gamma-ray irradiation."( [Effects of histamine H2-receptor antagonists on hemopoietic reconstruction in bone marrow].
Du, XX; Xu, YH; Zhou, YJ, 1989
)
0.55
" Few if any of these studies have attempted to address the rationale for the dosage and/or dosage regimens being studied."( Determining the optimal dosage regimen for H2-receptor antagonist therapy--a dose validation approach.
Braverman, A; Dickson, BD; Frank, WO; Mounce, W; Peace, KP; Young, MD, 1989
)
0.28
" Eventual discontinuation of cimetidine therapy led to a return of schizophrenic symptoms, which responded to an increase in chlorpromazine dosage to previous levels."( Adverse interaction between cimetidine and chlorpromazine in two cases of chronic schizophrenia.
Byrne, A; O'Shea, B, 1989
)
0.86
" The secretion of pepsin and of mucus was markedly inhibited at every dosage of the compound."( [Potentiation of the gastro-protective effect of sulglicotide in the presence of cimetidine in the rat].
Morini, G, 1989
)
0.5
" With increasing doses of histamine, a dose-response relationship was seen in the activity of RAR."( Action of histamine on the rapidly adapting airway receptors in the dog.
Kappagoda, CT; Ravi, K; Teo, KK, 1989
)
0.28
"The dose-response and plasma concentration-response relationships of cyclosporine after both inducing and inhibiting its metabolism were studied in a mouse heart transplant model."( In vivo evaluation of the effects of altered cyclosporine metabolism on its immunosuppressive potency.
Babany, G; Babany, I; Kates, RE; Morris, RE; Shepherd, S, 1989
)
0.28
" At 12 weeks, the risk of overlooking a difference in favor of one of the two dosage regimens was less than 20 percent."( Two daily doses of sucralfate or cimetidine in the healing of gastric ulcer. A comparative randomized study.
Beck, H; Hjortrup, A; Hoffmann, J; Schroeder, M; Svendsen, LB, 1989
)
0.56
" Immediately after operation (or the decision not to operate) 181 patients were subdivided at random to treatment with a placebo or cimetidine in a dosage of 400 mg twice daily for two years or until death."( [Cimetidine treatment of stomach cancer].
Bülow, S; Damm, P; Fischerman, K; Hesselfeldt, P; Hjortrup, A; Knigge, UP; Pedersen, IK; Pedersen, VM; Siemssen, OJ; Tønnesen, H, 1989
)
1.39
" This endotoxin dosage resulted in 50% mortality in rats."( Disposition kinetics of cimetidine and ranitidine in endotoxin pretreated rats.
al-Khamis, KI; Kaka, JS; Tanira, MO, 1989
)
0.58
"In a pilot study, 26 rheumatoid arthritic patients taking continuous, stable dosage regimens of nonsteroidal anti-inflammatory drugs and with developed gastric and duodenal lesions were administered sucralfate 1 g four times per day (14 patients) or cimetidine 400 mg twice daily (12 patients) in a single-blind regimen for six weeks."( Effect of sucralfate and cimetidine on rheumatoid patients with active gastroduodenal lesions who are taking nonsteroidal anti-inflammatory drugs. A pilot study.
Cox, N; Fine, D; Hillier, K; Jewell, R; Shepherd, HA, 1989
)
0.76
"We have studied the mechanisms of the increased dosage requirements of the H2-receptor antagonist cimetidine in paediatric burned patients in a pharmacokinetic and pharmacodynamic study."( Alteration by burn injury of the pharmacokinetics and pharmacodynamics of cimetidine in children.
Greenblatt, DJ; Hagen, J; Hoaglin, DC; Martyn, JA, 1989
)
0.72
"The effects of roxatidine acetate hydrochloride and cimetidine during multiple dosing on the pharmacokinetics of theophylline was studied in nine healthy volunteers, five smokers and four non-smokers, in comparison with placebo treatment."( Effects of roxatidine acetate hydrochloride and cimetidine on the pharmacokinetics of theophylline in healthy subjects.
Aoi, R; Ishioka, T; Ogata, H; Takeuchi, H; Yoshimura, N, 1989
)
0.78
" An increase in malondialdehyde level was observed after ethanol exposure, whereas suppression of lipid peroxidation occurred after dosing with indomethacin."( Lipid peroxidation in normal and ulcerated gastric mucosa of rats treated with pentacaine and cimetidine.
Nosál, R; Nosálová, V; Petríková, M, 1989
)
0.5
" The effect of SK&F 104353 was also examined in combination with a pyrilamine-cimetidine dosing regimen sufficient to remove the histaminergic component of cutaneous immediate hypersensitivity."( Interactive effects of peptidoleukotrienes and histamine on microvascular permeability and their involvement in experimental cutaneous and conjunctival immediate hypersensitivity.
Gary, RK; Gleason, JG; Nieves, AL; Wasserman, MA; Williams, LS; Woodward, DF, 1989
)
0.51
" Rates of adverse reactions also did not differ by dosage or trial duration."( Cimetidine and adverse reactions: a meta-analysis of randomized clinical trials of short-term therapy.
Colditz, GA; Delea, TE; Huse, DM; Oster, G; Richter, JM, 1989
)
1.72
" Flurbiprofen showed a linear dose-response relationship with respect to gastric injury and serum drug levels."( The effects of flurbiprofen, aspirin, cimetidine, and antacids on the gastric and duodenal mucosa of normal volunteers. An endoscopic and photographic study.
Friedman, H; Lanza, FL; Royer, GL; Schwartz, JH; Seckman, CE; Stubbs, CM, 1989
)
0.55
" The dose-response curve for histamine in each culture was progressively displaced to the right with increasing concentrations of the histamine H2 receptor antagonist cimetidine."( Demonstration of histamine H2 receptors on human melanoma cells.
Evanson, JM; Hart, IR; Taylor, DJ; Whitehead, RJ; Woolley, DE, 1988
)
0.47
" According to the two dosing schedules adopted to evaluate the duration of action, mifentidine, compared to cimetidine and ranitidine, required considerably lower oral dosages to display its protective effect."( Cimetidine, ranitidine and mifentidine in specific gastric and duodenal ulcer models.
Cereda, E; Del Soldato, P; Donetti, A; Ghiorzi, A, 1985
)
1.92
" beta-Adrenoceptor antagonists produced a bell-shaped dose-response curve on histamine contractions in cat isolated lung parenchyma strip."( The response of cat airways to histamine in vivo and in vitro.
Blaber, LC; Fryer, AD, 1985
)
0.27
" Pentagastrin-stimulated acid secretion remained decreased (50% of control) 12 hr after oral dosing with 20 mg famotidine."( Famotidine, a new H2-receptor antagonist. Effect on parietal, nonparietal, and pepsin secretion in man.
Chremos, AN; Gamal, MA; Graham, DY; Smith, JL, 1985
)
0.27
" Omeprazole, in contrast, did not alter gastric emptying at a similar antisecretory dosage level."( Effects of H2-receptor antagonists upon physiological acid secretory states in animals.
Cook, PG; Mangel, AW; Pendleton, RG; Shepherd-Rose, A, 1985
)
0.27
" For all substances a dose-response curve concerning the change of vessel diameters was obtained."( The microvasculature of the small-intestinal mucosa of the rat: quantification of hemodynamic effects of topically applied cimetidine, ranitidine, somatostatin, and vasopressin.
Anliker, M; Frick, P; Knoblauch, M; Métry, JM; Neff, M, 1985
)
0.48
" It is suggested that the combined treatment cimetidine-alprazolam requires a reduced daily dosage (one third) of alprazolam or increased dosage intervals (b."( Pharmacokinetic consequences of long term coadministration of cimetidine and triazolobenzodiazepines, alprazolam and triazolam, in healthy subjects.
Desager, JP; Harvengt, C; Hulhoven, R; Pourbaix, S; Smith, RB, 1985
)
0.77
" In the second set of experiments, equiactive doses (that is the respective ED50s calculated from the previously established dose-response curves) of all the compounds were infused during dimaprit-induced acid hypersecretion, in order to evaluate their duration of action."( Effect of the new H2-receptor antagonist mifentidine on gastric acid secretion in the cat: comparison with cimetidine and ranitidine.
Bertaccini, G; Scarpignato, C; Tangwa, M; Tramacere, R, 1985
)
0.48
"Theobromine metabolism and clearance were investigated at steady-state under chronic oral dosing conditions in eight healthy volunteers, four of whom were cigarette smokers."( Influence of cimetidine, sulfinpyrazone, and cigarette smoking on theobromine metabolism in man.
Attwood, J; Birkett, DJ; Miners, JO; Wing, LM,
)
0.5
" the respective ED50s calculated from the previously established dose-response curves) of all the three antagonists was completely different."( The effect of the new H2-receptor antagonist mifentidine on gastric secretion, gastric emptying and experimental gastric and duodenal ulcers in the rat: comparison with cimetidine and ranitidine.
Del Soldato, P; Scarpignato, C; Tangwa, M; Tramacere, R, 1986
)
0.47
" The maximum pepsin output obtained from a set of complete dose-response curves of dimaprit was not statistically different from basal values."( Comparison of the effects of structurally different H2-antagonists on acid and pepsin activity stimulated by dimaprit in conscious cats.
Barocelli, E; Chiavarini, M; Impicciatore, M; Molina, E; Morini, G; Plazzi, PV, 1985
)
0.27
" The ganglion blocking activity of cimetidine was much weaker than that of hexamethonium; the ED50 ratio (cimetidine:hexamethonium) calculated from the cumulative log dose-response curves for the two drugs was 64."( Ganglion blocking activity of cimetidine in the anaesthetized cat.
Cheah, LS; Gwee, MC; Lee, HS,
)
0.7
" A dose-response relationship for cimetidine and ranitidine was developed, confirming the greater potency of cimetidine."( Effect of H2-receptor antagonists on steady-state extraction of indocyanine green and lidocaine by the perfused rat liver.
Heath, CA; Johnson, RF; Roberts, RK; Schenker, S; Speeg, KV, 1986
)
0.55
" The dose-response curve for stimulation by histamine of adenylate cyclase was shifted to the right in a dose-dependent manner by increasing concentrations of several H2-antagonists."( A study of the H2-receptor for histamine stimulating adenylate cyclase in homogenates of guinea-pig lung parenchyma.
Foreman, JC; Norris, DB; Rising, TJ; Webber, SE, 1986
)
0.27
" The other five patients, who were free of complication, initially received a standard regimen of omeprazole 60 mg orally once a day; dosage was subsequently adjusted until the basal acid output, measured 1 hr before the next dose of the drug, was less than 10 mmol/hr."( Effectiveness of omeprazole in seven patients with Zollinger-Ellison syndrome resistant to histamine H2-receptor antagonists.
Bader, JP; Cortot, A; Delchier, JC; Goldfain, D; Isal, JP; Mignon, M; Soule, JC; Travers, B, 1986
)
0.27
" ORF 17910 retains 43 and 37% of its antisecretory potency 16 hr after dosing in dogs and rats, respectively, suggesting a long duration of action, whereas ranitidine is either inactive (rats) or loses 97% of its potency (dogs) at this time."( Pharmacological comparison of ORF 17910, a potent, long-acting histamine H2-receptor antagonist, to cimetidine and ranitidine.
Katz, LB; Scott, CK; Shriver, DA, 1986
)
0.49
" Also, no difference in efficacy of either drug was observed and changes in dosing of digoxin were not required."( Drug interaction studies and encainide use in renal and hepatic impairment.
Gallo, DG; Quart, BD; Sami, MH; Wood, AJ, 1986
)
0.27
" Gastric acid hypersecretion was controlled in seven patients with less frequent dosing with famotidine than with cimetidine or ranitidine."( Famotidine in the therapy of gastric hypersecretory states.
Gardner, JD; Howard, JM; Jensen, RT; Maton, PN; Slaff, JI; Vinayek, R; Wank, SA, 1986
)
0.48
" At UC Davis, we compared constant infusion with intermittent dosing (300 mg of cimetidine every six hours) in patients admitted to the intensive care unit with upper gastrointestinal bleeding."( A dosage alternative for H2-receptor antagonists--constant infusion.
Siepler, JK, 1986
)
0.5
" When steady state was reached (nine days), cimetidine was begun concomitantly in a dosage of 300 mg QID or 800 mg HS for ten days."( Safety: cimetidine and concomitant theophylline or warfarin--drug interactions and their implications.
Frank, WO, 1986
)
0.97
" Intravenous infusion of CM 57755 induced a parallel shift to the right of the dimaprit dose-response curve."( Inhibition of dimaprit- and pentagastrin-induced gastric acid secretion in cats by the new histamine H2 antagonist, CM 57755.
Bianchetti, A; Lavezzo, A; Manara, L; Manzoni, L, 1986
)
0.27
" However, when the preparations were precontracted with histamine (10(-5)M), dose-response curves for relaxation were shifted to the right, and low-concentrations of all three histamine H2-antagonists augmented histamine-induced tone."( Direct effects of H2-receptor antagonists on airway smooth muscle and on responses mediated by H1- and H2-receptors.
Hashimoto, Y; Iwatsuki, N; Koga, Y, 1987
)
0.27
" The dosage was increased to 975 mg every 6 hours, and he has had no further hypotensive episodes on this regime for 2 years."( Systemic mastocytosis: management of an unusual case with histamine (H1 and H2) antagonists and cyclooxygenase inhibition.
Crawhall, JC; Wilkinson, RD, 1987
)
0.27
" The current trend in therapy is toward less frequent dosing patterns with more attention toward controlling nocturnal acid secretion."( H2-receptor antagonists: development and application.
Feldman, S,
)
0.13
" These results suggest that within the normal therapeutic dosage ranges for both drugs, it is unlikely that a clinically significant interaction between them will occur."( Lack of interaction between cimetidine and buspirone.
Faulkner, HC; Gammans, RE; Goodson, PJ; Pfeffer, M; Rehm, KD; Westrick, ML, 1987
)
0.57
" Cimetidine produced a parallel displacement of the histamine dose-response curve, suggesting competitive inhibition between this classical H2 receptor antagonist and histamine in the two experimental groups."( Up- and down-regulation of membrane receptors as possible mechanisms related to the antiulcer actions of milk in rat gastric mucosa.
Chastre, E; Emami, S; Gespach, C; Launay, JM; Rosselin, G, 1987
)
1.18
" Dose-response curves to dimaprit in stimulating gastric secretion were displaced to the right in a dose-related fashion by both drugs."( Kinetic analysis of the interaction of mifentidine with gastric H2-receptors in the conscious dog.
Giachetti, A; Pagani, F; Zecca, M, 1987
)
0.27
" Practical means of avoiding this risk consists in limiting such drug combinations, reducing benzodiazepine dosage and, if a combined treatment is necessary, using by preference either benzodiazepines degraded by conjugation instead of oxidation, or macrolides, or anti-H2 compounds with reduced inhibitory effect on microsomes."( [Psychotic disorders linked to the inhibition of benzodiazepine catabolism].
Begaud, B; Hugues, FC; Jouglard, J; Le Jeunne, C; Moulin, M,
)
0.13
" Therefore, the same dosage schedule as in uraemia may be applied in patients with dialysis."( Pharmacokinetics of histamine (H2)-receptor antagonists, including roxatidine, in chronic renal failure.
Brockmeier, D; Lameire, N; Rosenkranz, B, 1988
)
0.27
" In contrast, the steady-state midazolam concentration after ranitidine dosing (61."( Effect of single doses of cimetidine and ranitidine on the steady-state plasma levels of midazolam.
Arvela, P; Klotz, U; Rosenkranz, B, 1985
)
0.57
" Animals were then treated with the four agents in carefully defined dosage regimens, and survival was again determined on the tenth postburn day."( Postburn immunosuppression in an animal model. IV. Improved resistance to septic challenge with immunomodulating drugs.
Bartle, EJ; Bender, EM; Carter, WH; Hansbrough, JF; Mansour, MA; Zapata-Sirvent, RL, 1986
)
0.27
" In an apparently all-or-none manner, both caused a sinistral shift in dose-response curves for the phasic component of the contractile response to histamine at H1 receptors on the ileum."( Metronidazole and 5-aminosalicylic acid enhance the contractile activity of histaminergic agonists on the guinea-pig isolated ileum.
Barker, LA; Winbery, SL, 1986
)
0.27
" Cyproterone acetate allows differentiated treatment according to the various grades of hirsutism by modification of dosage and application."( [The concept of the causal therapy of hirsutism].
Schmidt, JB, 1986
)
0.27
" The selective histamine H1-receptor antagonist chlorpheniramine shifted the dose-response curves of histamine and 2-PEA for inducing vasoconstriction to the right."( Characteristics of histamine receptors in the isolated and perfused canine coronary arteries.
Chiba, S; Nakane, T, 1987
)
0.27
" In contrast to cimetidine, basal and pentagastrin-stimulated gastric acid secretion measured 12 h after dosing was significantly inhibited during treatment with famotidine."( A comparison of the effects of treatment with either famotidine 40 mg or cimetidine 800 mg nocte on gastric acid secretion and serum gastrin.
Crean, GP; Fullarton, GM; Laferla, G; McColl, KE, 1988
)
0.85
" The dose-response curve for histamine in each culture was progressively displaced to the right with increasing concentrations of cimetidine, an H2-receptor antagonist."( Histamine H2 receptors on chondrocytes derived from human, canine and bovine articular cartilage.
Brown, DM; Taylor, DJ; Woolley, DE; Yoffe, JR, 1985
)
0.47
" Dose-response curves were constructed and characterized in terms of the EC50, slope and maximal response attainable relative to histamine."( Histamine-induced inositol phospholipid breakdown in the longitudinal smooth muscle of guinea-pig ileum.
Donaldson, J; Hill, SJ, 1985
)
0.27
" Cimetidine affected neither captopril pharmacokinetic parameters nor its biological effects, suggesting that no change in captopril dosing is necessary when cimetidine is co-administered."( Cimetidine does not alter free unchanged captopril pharmacokinetics and biological effects in healthy volunteer.
Bah, M; Cadilhac, M; Giudicelli, JF; Richer, C; Thuillez, C,
)
2.48
" With Pancrease, the number of daily dosage units is decreased even when fat intake is increased."( Efficacy of pancreatic enzyme supplementation in children with cystic fibrosis: comparison of two preparations by random crossover study and a retrospective study of the same patients at two different ages.
Ansaldi-Balocco, N; Santini, B; Sarchi, C, 1988
)
0.27
" These dosage regimens were derived from single-dose pharmacokinetic studies of the drug."( Dosage regimen of cimetidine reviewed. Possible drug accumulation after multiple oral doses.
Prandota, J; Smith, IJ; Wilson, JT, 1988
)
0.61
" However, no such intoxication has been reported with CBS used at its recommended dosage in the acute treatment of peptic ulcer disease, and no other serious adverse effects have been associated with CBS."( Colloidal bismuth subcitrate. A review of its pharmacodynamic and pharmacokinetic properties, and its therapeutic use in peptic ulcer disease.
Benfield, P; Monk, JP; Wagstaff, AJ, 1988
)
0.27
" Ulcer-healing trials using four times daily dosing appear to parallel the antisecretory dose-response curve up to a dose of 200 micrograms qid."( Overview of misoprostol clinical experience.
Herting, RL; Nissen, CH, 1986
)
0.27
" As a result of these studies we recommend a cimetidine maintenance dosage of 400 mg twice a day for all patients whose ulcers are slow to heal on 1 g cimetidine a day and in patients with prepyloric ulcer disease regardless of rate of healing."( Results of short- and long-term cimetidine treatment in patients with juxtapyloric ulcers, with special reference to gastric acid and pepsin secretion.
Berstad, A; Bodemar, G; Ström, M; Walan, A, 1986
)
0.81
" Compared with the control treatment, cimetidine increased the glibenclamide AUC (973 vs 710 ng ml-1 h), but during ranitidine dosing glibenclamide AUC (726 ng ml-1 h) was not significantly different from the control."( The paradoxical effect of cimetidine and ranitidine on glibenclamide pharmacokinetics and pharmacodynamics.
Antal, EJ; Juhl, RP; Kubacka, RT, 1987
)
0.84
" Two thirds were treated continuously with 400 mg at bedtime supplemented by temporary increases in dosage if they had symptomatic relapses (group 1), and the remaining third were given intermittent "healing" doses for four to eight weeks if a symptomatic recurrence was judged to have occurred (group 2)."( Long term management of duodenal ulcer in general practice: how best to use cimetidine?
Rowley-Jones, D; Wade, AG, 1988
)
0.5
" Pentoxifylline and metabolite plasma concentrations over one dosing interval were measured on day 7 of each phase."( Alteration of pentoxifylline pharmacokinetics by cimetidine.
Hageman, JH; Mauro, LS; Mauro, VF, 1988
)
0.53
" Once-daily dosing with 300 mg ranitidine had no significant effect on theophylline pharmacokinetics."( The effects of once-daily dosing with ranitidine and cimetidine on theophylline pharmacokinetics.
McEwen, J; McMurdo, ME; Moreland, TA,
)
0.38
" An initial dose-response study in 48 subjects showed that 200- and 400-mg doses of cimetidine conferred a sufficient reduction in gastric mucosal injury to warrant further study."( Reduction of endoscopically assessed acute aspirin-induced gastric mucosal injury with cimetidine.
Chapman, RC; Kimmey, MB; Saunders, DR; Silverstein, FE, 1987
)
0.72
" We conclude that cimetidine dosage adjustments are apparently not necessary for patients with acutely restricted nutrient intake, although other weakly acidic and basic drugs may require dosage changes."( The effect of dietary protein-calorie restriction on the renal elimination of cimetidine.
Gersema, LM; Kitt, TM; Park, GD; Spector, R, 1987
)
0.83
" In Study II, the effect of food on the bioavailability of the two EB preparations was studied after a single dose of 500 mg (2 x 250 mg enterocoated tablets) and after multiple dosing (2 x 250 mg tid)."( Absorption of erythromycin acistrate and erythromycin base in the fasting and non-fasting state.
Männistö, PT; Pohto, P; Solkinen, A; Tuominen, RK; Vuorela, A, 1988
)
0.27
" Propranolol and cimetidine serum samples were measured over the 24-hour dosing interval after the last propranolol dose."( The effect of cimetidine dose timing on oral propranolol kinetics in adults.
Asgharnejad, M; Danis, M; Donn, KH; Powell, JR, 1988
)
0.98
" Isometric tension studies of control vein and vein bypass grafts treated with histamine resulted in sigmoid dose-response curves."( Mast cell infiltration: a possible mechanism for vein graft vasospasm.
Cross, KS; el-Sanadiki, MN; Hagen, PO; McCann, RL; Mikat, EM; Murray, JJ, 1988
)
0.27
" Clemastine significantly shifted the histamine dose-response curves to the right in both groups of lung strips."( Pharmacological analysis of reactivity changes in airways due to acute inflammation in cats.
Bánovcin, P; Korpás, J; Visnovský, P, 1987
)
0.27
"Cumulative dose-response curves for histamine induced responses in mesometrial (ME) and antimesometrial (AME) regions of uterine horns isolated from rats at 7th, 16th and 22nd days of pregnancy, were constructed."( Is there a prostaglandin involvement in the positive inotropic action of histamine in isolated pregnant rat uterus, apparently mediated via H1-receptors activation?
Dveksler, G; Franchi, AM; Gimeno, AL; Gimeno, MF; Viggiano, M, 1987
)
0.27
" Patients received either cimetidine or ranitidine via continuous infusion, with dosage adjustments for patients with renal insufficiency."( The comparative efficacy of cimetidine and ranitidine in controlling gastric pH in critically ill patients.
Bayliff, CD; Reid, SR, 1986
)
0.87
" According to these findings, dosage adjustments of Ci on the basis of Clcrea measurements appear to be valid for renal transplant recipients."( Cimetidine kinetics in renal transplant recipients.
Bozkurt, F; Hoppe-Seyler, G; Keller, E; Schollmeyer, P, 1986
)
1.71
" Dosage during maintenance therapy was kept as low as possible to keep patients free of symptoms."( Results of long-term treatment with cimetidine.
Worning, H, 1986
)
0.55
"In a sequential observational study efficacy and safety of two dosage regimens of cimetidine for the treatment of reflux-oesophagitis (RE) were examined."( [Therapy and prevention of reflux esophagitis. Results of a multicenter study with cimetidine. I: Epidemiology and results of acute therapy].
Döpfer, H; Heilmann, K; Neiss, A; Ottenjann, R; Siewert, JR, 1986
)
0.72
" It was clear that cimetidine 800 mg is the most appropriate dosage in the acute therapy of duodenal ulcer, combining optimal healing with maximum pain relief."( Dose validation and study design criteria in current cimetidine studies.
Braverman, AJ, 1986
)
0.85
" Dosing schedules are inexact and there remains a need to develop predictive models for its administration."( Approaches to the problem of individual doxorubicin dosing schedules.
Brenner, DE, 1987
)
0.27
" Thus, at the dosage used in our trial, ranitidine is more efficient for healing DU at 4 weeks than cimetidine but not for pain relief."( [Comparative effectiveness of ranitidine (150 mg X 2) and cimetidine (400 mg x 2) in the treatment of acute duodenal ulcer. A French multicenter controlled clinical trial].
Cortot, A; Henry-Amar, M; Pappo, M; Paris, JC, 1987
)
0.73
" Cimetidine produced a significant increase in the AUC of both single and steady state dosing of nifedipine."( Ranitidine and cimetidine; drug interactions with single dose and steady-state nifedipine administration.
Beerahee, A; Jack, DB; Kendall, MJ; Lobo, J; Smith, SR; Wilkins, MR, 1987
)
1.54
" In five elderly subjects aged 56-68 years, a week of dosing with cimetidine caused a rise in t1/2 (7."( Cimetidine inhibition of theophylline elimination: the influence of adult age and the time course.
Adebayo, GI; Coker, HA,
)
1.81
" This was not achieved with dosing at 1800 h although the duration of inhibition of gastric acidity was longer."( Large single daily dose of histamine H2 receptor antagonist for duodenal ulcer. How much and when? A clinical pharmacological study.
Burland, WL; Deakin, M; Glenny, HP; Mills, JG; Ramage, JK; Williams, JG, 1987
)
0.27
" The cimetidine dose-response curves and the calculated ED50 values were similar in the different experimental situations."( Effects of cimetidine, atropine and pirenzepine on basal and stimulated gastric acid secretion in the rat.
Ekelund, M; Håkanson, R; Vallgren, S, 1987
)
1.18
" However, the patients' compliance is just as important; the dosage must be individualized."( Enzyme substitution in pancreatic disease.
Andrén-Sandberg, A, 1987
)
0.27
"The histamine H2-receptor on the human parietal cell has been characterized by using dose-response curves and the negative logarithm of the molar concentration of an antagonist (pA2) analyses of cimetidine antagonism of betazole, histamine, and impromidine stimulation in isolated human and rabbit gastric glands."( Histamine H2-receptor of human and rabbit parietal cells.
Elander, B; Fellenius, E; Haglund, U; Leth, R; Olbe, L, 1987
)
0.46
" It was concluded that a reduction of cimetidine dosage is not necessary in patients with liver disease as far as their renal function is not disturbed, since the metabolism of cimetidine was not affected by the liver dysfunction itself."( Pharmacokinetic studies of cimetidine in patients with liver disease.
Arima, T; Nagashima, H; Yamasaki, H, 1987
)
0.84
" and the circulating blood levels of intact and denitrosated compound 5 min after dosing quantified."( Evidence for cytosolic glutathione transferase-mediated denitrosation of nitrosocimetidine and 1-methyl-2-nitro-1-nitrosoguanidine.
Jensen, DE; Stelman, GJ, 1987
)
0.5
" Two of the more potent compounds tested that were selected for more detailed dose-response evaluation were 4-amino-1-ethyl-1,2-dihydro-2-oxonaphthyridine-3-carboxylic acid ethyl ester (35) and 1-ethyl-1,2-dihydro-7-methyl-4-(4-methyl-1-piperazinyl)-2- oxo-1,8-naphthyridine-3-carboxylic acid ethyl ester (77)."( 2-Oxo-1,8-naphthyridine-3-carboxylic acid derivatives with potent gastric antisecretory properties.
Bauer, RF; Bell, SC; Santilli, AA; Scotese, AC, 1987
)
0.27
" Vital to the occurrence of double peaks are (i) dosing time relative to phasic activity, (ii) variability in flow out of the stomach, and (iii) a small emptying rate constant Qs/Vs, for a period of time within the first hour after administration."( The influence of variable gastric emptying and intestinal transit rates on the plasma level curve of cimetidine; an explanation for the double peak phenomenon.
Amidon, GL; Oberle, RL, 1987
)
0.49
" Blood and urine samples were collected frequently for 24 hours after dosing with triamterene alone (100 mg/day) for 4 days and concomitant cimetidine (400 mg twice daily) for an additional 4 days."( Effect of cimetidine on renal and hepatic drug elimination: studies with triamterene.
Bochner, F; Muirhead, MR; Rolan, PE; Somogyi, AA, 1986
)
0.88
" The expected antisecretory effect of a particular dosage regimen in patients with duodenal ulcer can be predicted mathematically from data derived from studies in normal volunteers."( Comparison of the effects of gastric antisecretory agents in healthy volunteers and patients with duodenal ulcer.
Burget, DW; Howden, CW; Hunt, RH; Jones, DB, 1986
)
0.27
" There were 3 further study days repeated after 1 and 2 weeks of cimetidine dosing and 1 week after stopping cimetidine."( Pharmacokinetics of cimetidine after subchronic administration.
Chin, TW; MacLeod, SM; Mahon, WA; Soldin, SJ; Spino, M, 1986
)
0.83
" Cimetidine shifted the dose-response curve for histamine to the right, but chlorpheniramine did not alter the response."( Mechanisms of histamine-induced relaxation in isolated monkey and dog coronary arteries.
Toda, N, 1986
)
1.18
" The results of clinical trials conducted in the United States and Europe demonstrated that 800 mg of cimetidine at bedtime is the optimal dosage regimen, providing rapid pain relief and ulcer healing in approximately 80% of the patients."( Goals of therapy: aggressive or moderate acid suppression?
Sabesin, SM, 1986
)
0.49
" Acetaminophen, cimetidine, or ranitidine were begun 24 hours prior to oxaprozin dosage and continued for the 10-day duration of each trial."( Interaction of oxaprozin with acetaminophen, cimetidine, and ranitidine.
Greenblatt, DJ; Harmatz, JS; Matlis, R; Scavone, JM, 1986
)
0.88
" Therefore, increases in total lidocaine concentrations after cimetidine administration were considerably less than those previously reported and empiric dosage reductions of lidocaine in patients receiving cimetidine may not be appropriate."( The effect of oral cimetidine on total and unbound serum lidocaine concentrations in patients with suspected myocardial infarction.
Bauman, JL; Berk, SI; Douglas, JB; Gal, P; McCue, JD; Powell, JR, 1987
)
0.84
" In contrast, tiotidine produced both a dextral shift of the log dose-response curve, as well as a previously unreported suppression in the maximal response produced by histamine."( Antagonistic activity of tiotidine and ranitidine on guinea-pig and rabbit atria.
Hughes, MJ; Kilpatrick, C; Light, KE; Serbus, DC, 1986
)
0.27
" Serum samples were serially drawn during each dosing interval for determination of cimetidine and PRZ concentrations by HPLC and RIA, respectively."( Lack of pharmacokinetic interaction between cimetidine and pirenzepine.
Jamali, F; Mahachai, V; Reilly, PA; Thomson, AB, 1985
)
0.75
" The drugs were administered by intravenous infusion, and up to three dosage increments fo each of the drugs were titrated against the pH of the aspirated gastric juice."( Randomized, prospective trial of cimetidine and ranitidine for control of intragastric pH in the critically ill.
Boutagy, JS; More, DG; Munro, IA; Raper, RF; Shenfield, GM; Watson, CJ, 1985
)
0.55
" Ethmozine dosing was repeated 15 days later after cimetidine, 300 mg four times a day for 7 days."( Cimetidine inhibition of ethmozine metabolism.
Biollaz, J; Shaheen, O; Wood, AJ, 1985
)
1.96
" After 4 weeks, healing rates of 72% and 76%, respectively, were observed for the two dosage regimens."( A comparative trial of 400 mg cimetidine twice daily and 1000 mg daily in the short-term treatment of duodenal ulceration.
Kalantzis, N; Kanaghinis, T; Papadopoulos, C; Rekoumis, G, 1985
)
0.56
" Standard therapeutic dosage regimens were used in each group."( Sucralfate and cimetidine as single agents and in combination for treatment of active duodenal ulcers. A double-blind, placebo-controlled trial.
Schneidman, D; Van Deventer, GM; Walsh, JH, 1985
)
0.62
" Coexisting disease states, such as renal or hepatic dysfunction, may require individualized dosing of these agents."( Individualization of calcium entry-blocker dosage for systemic hypertension.
Piepho, RW, 1985
)
0.27
"In a Canadian multicenter trial, a new dosing regimen of cimetidine (Tagamet)-600 mg given twice a day-was compared with the standard regimen of 300 mg four times a day in 118 evaluable patients with endoscopically proved esophagitis."( Cimetidine therapy for gastroesophageal reflux disease.
Archambault, AP; Cleator, IG; Farley, A; Hershfield, NB; Navert, H; Prokipchuk, EJ; Thomson, AB, 1985
)
1.96
"The effects of two dosage levels of a synthetic prostaglandin E1 analogue, misoprostol, and cimetidine on short-term duodenal ulcer healing were compared in a double-blind, endoscopically controlled 4-week study."( Misoprostol, a synthetic prostaglandin E1 analogue, in the treatment of duodenal ulcers. A double-blind, cimetidine-controlled trial.
Mannion, G; Naiker, N; O'Keefe, SJ; Spitaels, JM, 1985
)
0.7
" 1988 patients with endoscopically-proven peptic ulceration initially underwent an acute treatment over 6-12 weeks (open study) with 1000 mg cimetidine-the dosage could be increased to 1600 mg daily if necessary."( Long term cimetidine therapy for the prevention of recurring peptic ulcer: a multicenter study.
Rohner, HG, 1985
)
0.87
" Histamine dose-response characteristics in the presence of mepyramine and clemastine suggest the H1 antagonism to be competitive in nature."( H1-histaminergic activation stimulates inositol-1-phosphate accumulation in chromaffin cells.
Bommer, M; Costa, T; Herz, A; Noble, EP; Sincini, E, 1986
)
0.27
" Dosage and schedules for antacid prophylaxis in pediatric burn patients require further study."( Cimetidine and/or antacid for the control of gastric acidity in pediatric burn patients.
Martyn, JA, 1985
)
1.71
" After these dose-response curve determinations, chronic daily treatment with haloperidol (0."( Effects of drugs on schedule-controlled behavior in rats during chronic haloperidol administration.
McMillan, DE; Rastogi, SK, 1985
)
0.27
" Thirty-five failed to respond to cimetidine in a dose of 1 g/day, whilst 22 relapsed on reduction of dosage to 400 mg daily or on cessation of therapy."( Proximal gastric vagotomy in patients resistant to cimetidine.
Temple, JG; Weaver, RM, 1985
)
0.8
" This same dosage in obese individuals with normal serum creatinine values should result in the same average steady-state serum concentrations."( Cimetidine clearance in the obese.
Bauer, LA; Dellinger, EP; Edwards, WA; Ferreri, L; Jack, R; Raisys, V; Simonowitz, D; Wareing-Tran, C, 1985
)
1.71
"A double-blind controlled trial was conducted in which the efficacy of cimetidine in a dosage of 20 mg/kg/24 h in preventing upper gastrointestinal hemorrhage was tested in 34 critically ill patients on assisted ventilation."( Prevention of stress-induced upper gastrointestinal bleeding by cimetidine in patients on assisted ventilation.
van Blankenstein, M; van den Berg, B, 1985
)
0.74
" The minor alterations in prednisolone kinetics during concomitant cimetidine dosing are not likely to induce clinically significant alterations in steroid effect."( Effects of cimetidine and ranitidine on the conversion of prednisone to prednisolone.
Eshelman, FN; Ferguson, RK; Rocci, ML; Sirgo, MA; Vlasses, PH, 1985
)
0.9
" Since cimetidine did not affect acetaminophen pharmacokinetics to any significant extent, clinical combination of both medications at therapeutic dosage presumably would not produce adverse interactions."( Cimetidine--acetaminophen interaction in humans.
Chen, MM; Lee, CS, 1985
)
2.17
" A cimetidine dosage regimen of approximately 30 mg/kg per day in three to four divided doses would be an appropriate dose in children."( Cimetidine pharmacokinetics and dosage requirements in children.
Becker, M; Gugler, R; Somogyi, A, 1985
)
2.33
" Twenty patients had dosage decreases during the first cycle, and 14 of the 16 patients remaining on study after the first cycle required dosage reductions."( Phase II study of recombinant leukocyte A interferon (IFN-rA) plus cimetidine in disseminated malignant melanoma.
Ahmann, DL; Creagan, ET; Frytak, S; Green, SJ; Itri, LM; Long, HJ, 1985
)
0.51
" Previous cimetidine dosing recommendations have been empiric because of a lack of knowledge about cimetidine disposition kinetics in children."( Pharmacokinetics and pharmacodynamics of cimetidine and metabolites in critically ill children.
Hauser, AR; Lloyd, CW; Martin, WJ; Taylor, BD, 1985
)
0.94
"Before and after an education program to improve appropriate prescribing of cimetidine in an 810-bed teaching hospital, all new prescriptions written during a 4-week period were investigated, and information was obtained as to the indications for use, the dosage and concurrent drug therapy."( Medical education reduces inappropriate use of cimetidine in a teaching hospital.
Champion, MC; Gardiner, DC; Kozakowski, K; Sweet, D; Wielgosz, A, 1985
)
0.76
"Nine healthy normal subjects received verapamil, 10 mg iv, before (control) and during cimetidine dosing (300 mg every 6 hours), and verapamil, 120 mg po, twice in the same manner."( Lack of interaction between verapamil and cimetidine.
Abernethy, DR; Schwartz, JB; Todd, EL, 1985
)
0.76
" Modification of cimetidine dosage is therefore presumably not necessary in patients with compensated liver disease."( Pharmacokinetics of cimetidine in patients with liver disease.
Arancibia, A; Chesta, J; Fajuri, M; González-Martin, G; Novoa, X, 1985
)
0.93
" In 5 cases gastric pH monitoring was repeated after continuation of the ranitidine treatment; healing of ulcer was observed in 4 cases, always associated with a nocturnal pH score lower than 10 (in 2 cases after increasing the dosage of ranitidine)."( [Does nocturnal monitoring of gastric pH permit the prediction of therapeutic response in severe duodenal ulcer treated with ranitidine?].
Colin, R; Denis, P; Galmiche, JP; Guillard, JF; Lehur, PA; N'Djitoyap, C; Tranvouez, JL,
)
0.13
" With ranitidine under the dosage mentioned above, a prophylactic sufficient control, yet not a complete control of intragastric pH-value was accomplished."( [Control of the intragastric pH value in infection and peritonitis by ranitidine versus cimetidine. A double-blind study].
Hölscher, AH; Ketterl, R; Siewert, JR; Weiser, HF, 1984
)
0.49
" The more convenient dosage schedule of ranitidine may be important for patient compliance with initial therapy of peptic ulcer disease, and the greater duration of ranitidine antisecretory effects may enhance effectiveness of long-term maintenance therapy by providing more complete inhibition of nocturnal acid secretion."( Review of peptic ulcer maintenance trials.
Robinson, M, 1984
)
0.27
" Most of the commercially available and investigational compounds have similar efficacy; therefore the optimal drug may be the one associated with the fewest adverse effects and the most convenient dosing regimen."( Problems associated with medical treatment of peptic ulcer disease.
Zimmerman, TW, 1984
)
0.27
" Dose-response curves were performed to aerosol histamine in 11 dogs both before and 1 hr after H2 receptor blockade with cimetidine (1 mg/kg as a rapid intravenous infusion)."( In vivo effect of cimetidine on canine pulmonary responsiveness to aerosol histamine.
Braasch, PS; Drazen, JM; Ingram, RH; Loring, SH; Snapper, JR, 1980
)
0.8
" Mepyramine alone displaced the histamine dose-response curve to the right."( Antagonism of vasodepressor and gastric secretory responses to histamine by the H2-receptor antagonists, ranitidine and cimetidine, in the anaesthetized dog.
Daly, MJ; Humphray, JM; Stables, R, 1981
)
0.47
"The H2-receptor antagonists ranitidine and cimetidine were tested against gastric secretory dose-response curves to histamine, pentagastrin and bethanechol in the Heidenhain-pouch dog."( The effect of ranitidine on gastric acid secretory response curves to histamine, pentagastrin or bethanechol in the dog with a Heidenhain pouch.
Bunce, KT; Daly, MJ; Humphray, JM; Stables, R, 1981
)
0.53
"Gastric mucosal lesions were produced in rats by dosing orally with aspirin, 300 mg/kg."( H2-receptor antagonists protect against aspirin-induced gastric lesions in the rat.
Bunce, KT; Daly, MJ; Humphray, JM; Stables, R, 1981
)
0.26
" Furthermore, chronic dosing with cimetidine does not result in tolerance to the inhibitory effect."( Inhibition of microsomal drug metabolism by histamine H2-receptor antagonists studied in vivo and in vitro in rodents.
Avant, GR; Mitchell, MC; Patwardhan, RV; Schenker, S; Speeg, KV, 1982
)
0.54
" Twice-daily dosage improved compliance."( Clinical and endocrine aspects of treatment with ranitidine.
Boyd, EJ; Browning, MC; Peden, NR; Saunders, JH; Wormsley, KG, 1981
)
0.26
"Patients with Zollinger-Ellison syndrome whose gastric acid secretion or symptoms were not controlled by cimetidine in conventional dosage were selected for studies of responsiveness of their acid secretion to increasing doses of cimetidine, used either alone or in combination with a long-acting anticholinergic agent, isopropamide iodide."( Effect of isopropamide on response to oral cimetidine in patients with Zollinger--Ellison syndrome.
Hyman, PE; McCarthy, DM, 1982
)
0.74
" Twenty-four hour monitoring of intragastric pH showed that oxmetidine 400 mg twice daily reduced mean hourly 24 hour intragastric pH by 59%, suggesting that a twice daily dosage regimen should be evaluated in the treatment of duodenal ulceration."( Oxmetidine: clinical pharmacological studies with a new H2-receptor antagonist.
Brunet, PL; Burland, WL; Griffiths, R; Hunt, RH; Mills, JG; Milton-Thompson, GJ; Vincent, D, 1982
)
0.26
" Pretreatment of parenchymal strips with cimetidine or YM-11170, H2-receptor antagonists, resulted in a parallel shift of the dimaprit dose-response curve to the right."( Effects of histamine H2-receptor agonists and antagonists on isolated guinea-pig airway muscles.
Tomioka, K; Yamada, T, 1982
)
0.53
" When appropriate, reducing the dosage of these agents or switching to an alternative drug will minimize the incidence of side effects."( Cimetidine as an inhibitor of drug metabolism: therapeutic implications and review of the literature.
Bauman, JH; Kimelblatt, BJ, 1982
)
1.71
" The present work investigates in vitro the inhibitory dose-response curves to histamine, 4-methyl-histamine and 2-pyridylethylamine in depolarized (KCl 37 mM) uterus from estrogenous sensitized rats."( [Inhibitory action of histamine on the isolated rat uterus].
Esplugues, J; Marti-Bonmati, E; Morales-Olivas, FJ; Morcillo, E; Rubio, E,
)
0.13
"The new histamine-H2-receptor agonist, impromidine, was assessed for its effect on gastric acid secretion using a dose-response format."( Dose-response curve analysis of gastric secretory responses in the dog and man to impromidine: a new histamine-H2-receptor agonist.
Flannery, MC; Johnston, BJ; McIsaac, RL, 1983
)
0.27
" In the recommended dosage of 150 mg twice daily, ranitidine is as effective as cimetidine in healing duodenal and gastric ulcers and has the advantages of less frequent dosing and fewer side effects."( Pharmacology and clinical efficacy of ranitidine, a new H2-receptor antagonist.
Helman, CA; Tim, LO,
)
0.36
" Using quantitative cytochemistry of CA activity in guinea-pig oxyntic cells, we compared the dose-response relationships (1."( Evidence for histamine H1 and H2 receptors in guinea-pig oxyntic cells.
Heldsinger, AA; Skoglund, ML; Vinik, AI, 1983
)
0.27
" administration of pure ND in two dogs, has shown that ND declines biexponentially with a t1/2 beta similar to the one estimated after CZP dosing in control animals."( Cimetidine interaction with dipotassium clorazepate disposition in the anesthetized dog.
Colin, P; Lelorier, J; Sirois, G, 1984
)
1.71
" For comparison, the DNA methylation produced by the carcinogen N-methyl-N-nitro-N-nitrosoguanidine (MNNG) dosed orally was measured."( DNA-methylation by nitrosocimetidine and N-methyl-N-nitro-N-nitrosoguanidine in the intact rat.
Gombar, CT; Magee, PN, 1982
)
0.56
" Both substance P and histamine produced sigmoid dose-response curves for the following parameters: 1 min and 5 min planimetrically measured areas of erythema, and mean diameter of weal."( Vascular responses of human skin to injection of substance P and mechanism of action.
Coutts, AA; Eady, RA; Greaves, MW; Jorizzo, JL, 1983
)
0.27
" The clinical implications from this study necessitate dosage adjustments of procainamide in patients being concomitantly treated with cimetidine."( Cimetidine-procainamide pharmacokinetic interaction in man: evidence of competition for tubular secretion of basic drugs.
Heinzow, B; McLean, A; Somogyi, A, 1983
)
1.91
"Sprague-Dawley male albino rats showed in a dose-response study a maximal drinking response to a 5 U/kg dose of SC insulin in a 2-hr test."( Histaminergic mechanism for drinking elicited by insulin in the rat.
Hecht, ES; Kraly, FS; Miller, LA, 1983
)
0.27
" The dose-response curves to ACh showed nonparallel increases in H+ secretion and histamine release."( Evidence for a direct action of acetylcholine on the gastric oxyntic cell of the amphibian.
Michelangeli, F; Ruiz, MC, 1984
)
0.27
" All parameters were examined for agonist and antagonist potency using dose-response curves, ED50 and pA2 values."( Histamine responsiveness of isolated gastric glands.
Berglindh, T; Chew, CS; Hersey, SJ; Sachs, G, 1980
)
0.26
"To investigate the mechanism of intracellular transmission of three representative stimuli for gastric acid secretion, the dose-response relations of cyclic nucleotides accompanied by acid secretion stimulated by histamine, pentagastrin and bethanechol were comparatively studied using an in vitro preparation of guinea pig gastric mucosa surviving with a constant potential difference and acid secretion sensitive to amytal."( Cyclic nucleotide response to acid-secreting stimuli in guinea pig gastric mucosa in vitro.
Matsumoto, H; Miyoshi, A; Ohe, K; Shirakawa, T, 1981
)
0.26
" The dose-response curve of the adenylate cyclase activity was not shifted to the left."( Adenylate cyclase activity in gastric mucosal biopsies and cAMP in gastric juice before and after cimetidine treatment in healthy subjects.
Aadland, E; Berstad, A; Ruoff, HJ; Torjesen, P, 1981
)
0.48
" A dose-response relationship between ranitidine and PRL was established, and a dose of 65 mg ranitidine was found to be the minimal effective PRL-releasing dose."( Comparison between dose-responses of prolactin, thyroid stimulating hormone and growth hormone to two different histamine H-2 receptor antagonists in normal men.
Christiansen, PM; Dejgarrd, A; Knigge, U; Thuesen, B; Wollesen, F, 1981
)
0.26
"The dose-response curve of histamine-induced cyclic AMP elevation in monolayer cultures of primary foetal-bovine articular chondrocytes was displaced to the right by cimetidine."( Histamine H2 receptors on foetal-bovine articular chondrocytes.
Taylor, DJ; Woolley, DE; Yoffe, JR, 1983
)
0.46
"The pharmacology, pharmacokinetics, clinical efficacy, adverse reactions, drug interactions, and dosage of ranitidine are reviewed; specific comparisons are made of this new H2-receptor antagonist with the older agent, cimetidine."( Ranitidine: a new H2-receptor antagonist.
Berner, BD; Conner, CS; Sawyer, DR; Siepler, JK,
)
0.32
" Nocturnal acid output was controlled significantly better with ranitidine at night, twice daily dosage of ranitidine, and cimetidine at night, than by the twice daily dosage of cimetidine."( Single nocturnal dose of an H2 receptor antagonist for the treatment of duodenal ulcer.
Buck, M; Gledhill, T; Howard, OM; Hunt, RH; Paul, A, 1983
)
0.47
" A significant difference was not found between the two cimetidine dosages, indicating dose independence of the interaction over the dosage range studied."( Inhibition of theophylline clearance by cimetidine but not ranitidine.
Cross, RE; Eshelman, FN; Powell, JR; Rogers, JF; Wargin, WA, 1984
)
0.78
" Lipid content is increased by ranitidine in livers of rats dosed with ethanol."( Effects of cimetidine and ranitidine on the "lipoperoxide" and lipid content of liver of rats treated with CCl4, colchicine, ethanol, ethionine and emetine.
Agostini, C; Di Segni, M, 1984
)
0.66
" Cimetidine dosage in clinical practice should therefore be calculated on the basis of IBW, which better reflects lean body mass, instead of total body weight, which reflects adipose tissue weight in addition to lean body mass."( Cimetidine disposition in obesity.
Abernethy, DR; Greenblatt, DJ; Gugler, R; Matlis, R, 1984
)
2.62
"4% of the dosage given before versus 28."( Long-term cimetidine in children with cystic fibrosis: a randomized double-blind study.
Kläy, MP; Kraemer, R; Lentze, MJ; Mordasini, RC; Riesen, WF; Rossi, E; Ruedeberg, A; Schöni, M, 1984
)
0.67
" We studied the clinical importance of this effect in 10 patients, who were receiving long-term treatment with diazepam for anxiety, tension, or difficulty in sleeping, in an eight-week double-blind controlled study during which the diazepam dosage remained constant."( Clinical importance of the interaction of diazepam and cimetidine.
Abernethy, DR; Greenblatt, DJ; Harmatz, JS; Morse, DS; Shader, RI, 1984
)
0.51
" Both dosage regimens were equally effective in reducing ulcer pain and consumption of antacids."( Comparison of cimetidine 800 mg once daily and 400 mg twice daily in acute duodenal ulceration.
Capurso, L; Dal Monte, PR; Mazzeo, F; Menardo, G; Morettini, A; Saggioro, A; Tafner, G, 1984
)
0.63
"A reversal phase partition chromatographic system analysis cimetidine and zolimidine in pharmaceutical dosage forms is proposed."( [Analysis of active principles in pharmaceutical dosage forms by high pressure liquid chromatography - cimetidine and zolimidine].
Cozzolino, S; La Rotonda, MI; Schettino, O, 1980
)
0.72
" This suggests that no change in ibuprofen dosing is necessary when cimetidine is co-administered."( Cimetidine does not alter ibuprofen kinetics after a single dose.
Bliss, M; Conrad, KA; Mayersohn, M, 1984
)
1.95
" Simultaneous application of Hi and 10 micrograms of diphenhydramine, pyrilamine or promethazine, apparently causing no analgesic effect from a single administration, caused a parallel shift of the dose-response curve of Hi to the right."( Analgesic effect of histamine induced by intracerebral injection into mice.
Chung, YH; Kamei, C; Miyake, H; Tasaka, K, 1984
)
0.27
" The shapes of the dose-response curves for inhibition of the organic cation and organic anion transport are different, and the inhibition is competitive in each case."( Mechanisms for the renal secretion of cisplatin.
Herbert, BH; Nelson, JA; Santos, G, 1984
)
0.27
" Following controlled alcohol doses to eight healthy volunteers without cimetidine and after three days cimetidine in the two dosage regimens, blood alcohol concentrations were determined and the degree of intoxication was recorded subjectively on a 100 mm scale."( [The effect of cimetidine on the metabolism and effects of alcohol].
Fenzl, E; Hein, B; Johnson, KI, 1984
)
0.85
") given 30 min prior to SU-88 dosing blocked this protective effect, whereas it was not affected when indomethacin was given 30 min after the SU-88 dosing."( Cytoprotective effect of SU-88, an anti-ulcer agent, in the rat.
Kyogoku, K; Mori, Y; Nakazima, M; Shinozaki, A; Suwa, T, 1984
)
0.27
"Both the pharmacokinetics and the pharmacodynamics of cimetidine were investigated in three patients with Zollinger-Ellison syndrome, who were unresponsive to conventional dosing regimens."( Failure of cimetidine in Zollinger-Ellison syndrome.
Adamonis, AJ; Dreyer, M; Madura, M; Olinger, EJ; Schentag, JJ; Ziemniak, JA, 1983
)
0.9
"The disposition of cimetidine after oral and intravenous administration during multiple dosing was studied in 11 patients with Laennec's cirrhosis."( Cimetidine disposition in patients with Laennec's cirrhosis during multiple dosing therapy.
Cello, JP; Oie, S, 1983
)
2.04
" It is concluded that cimetidine clearance is decreased in patients with severe liver disease, mostly due to an impairment of the tubular secretion of unchanged drug, and that a reduction of cimetidine dosage is warranted in these patients, even in the presence of a normal creatinine clearance."( Cimetidine kinetics and dynamics in patients with severe liver disease.
Arsène, D; Fortunet-Fouin, H; Villeneuve, JP,
)
1.89
" In seven nonanesthetized sheep, maternal dosage produced mean steady-state plasma concentrations of 776 +/- 217 ng/ml in the mother and 32 +/- 15 ng/ml in the fetus."( Placental transfer and renal elimination of cimetidine in maternal and fetal sheep.
Ching, MS; Hardy, KJ; Jones, DB; Mihaly, GW; Morgan, DJ; Smallwood, RA; Webster, LK, 1983
)
0.53
"25-20 mg/kg) in a dose-response study."( A probe for a histaminergic component of drinking in the rat.
Kraly, FS, 1983
)
0.27
" These results suggest that similar to clonidine, a high dosage of tizanidine influences gastric acid secretion and gastric ulcers, although the activity is lower than that of clonidine."( [Influence of a muscle relaxant, tizanidine, on gastric acid secretion and gastric ulcer in rats].
Kanaoka, R; Maeda-Hagiwara, M; Watanabe, H; Watanabe, K, 1983
)
0.27
" During multiple dosing of cimetidine, significant accumulation of cimetidine metabolites may be expected."( The pharmacokinetics and metabolism of cimetidine in neonates.
Aranda, JV; Schentag, JJ; Wynn, RJ; Zarowitz, BJ; Ziemniak, JA, 1984
)
0.83
" Prescribers should be aware of this potential interaction and reduce theophylline dosage where appropriate."( Cimetidine-theophylline interaction in patients with chronic obstructive airways disease.
Grice, J; McGuffie, C; Roberts, RK, 1984
)
1.71
"5 micrograms/ml were maintained for the entire dosing interval in seven of 10 subjects."( Effect of antacids on predicted steady-state cimetidine concentrations.
Doering, PL; Guild, RT; Lopez, LM; Normann, SA; Russell, WL, 1984
)
0.53
"To examine for a relationship between in vivo nonspecific bronchial reactivity to histamine and in vitro smooth muscle response to histamine, we performed inhalation dose-response curves prior to lung surgery in 12 patients and compared this with their bronchial smooth muscle response in vitro."( A comparison of in vivo and in vitro human airway reactivity to histamine.
Armour, CL; Chan, N; Hogg, JC; Lazar, NM; Paré, PD; Schellenberg, RR; Taylor, SM, 1984
)
0.27
" In aortic ring segments, precontracted by norepinephrine, three types of dose-response curves were found: relaxation (rat), contraction (guinea-pig, cat, mouse) and relaxation followed by contraction at higher doses (rabbit)."( Effect of histamine on aorta preparations of different species.
Leusen, I; Van de Voorde, J, 1984
)
0.27
" This relationship might prove to be a useful method of individualizing cimetidine dosage in critically ill patients."( Pharmacokinetics of cimetidine in critically ill patients.
Cameron, P; Ilett, KF; Nation, RL; Oh, TE; Thompson, W; Tjokrosetio, R, 1984
)
0.82
" Extensive placebo-controlled trials have not been reported for antacid treatment of gastric ulcer, but regular antacid dosing was as effective as cimetidine in one trial."( Antacid therapy for duodenal and gastric ulcer: the experience in the United States.
Ippoliti, AF, 1982
)
0.46
" Dosage guidelines and formulation procedures are described in the paper, as are other possible therapeutic alternatives (dialysis, acetazolamide, cimetidine)."( Treating severe metabolic alkalosis.
Martin, WJ; Matzke, GR,
)
0.33
"1 To study the effect of cimetidine on gonadal function in man, eleven male subjects with chronic duodenal ulcer were given cimetidine orally at a dosage of 1000 mg per day 3 months and 400 mg nocte for the subsequent 3 months."( Effect of cimetidine on gonadal function in man.
Lai, CL; Lam, KC; Wang, C; Yeung, KK, 1982
)
0.97
" Interactions at the absorption level can be avoided by administering the antacid one hour after intake of the other drugs (one hour after meals) which is also the optimum dosing schedule to ensure good antacid effect."( [Metabolic effects of antacids and interactions with other drugs].
Gugler, R; Musch, E, 1983
)
0.27
" Although there was wide variation in dosage of cimetidine and duration of therapy, no significant difference was noted in the dosage regimen of responders and non-responders to cimetidine."( Cimetidine in primary duodenal ulcer in children.
Attenburrow, AA; Goel, KM; Thomson, RB, 1983
)
1.96
"Cimetidine disposition was determined in six patients undergoing continuous ambulatory peritoneal dialysis to ascertain the need for modification of conventional dosing regimens."( Cimetidine disposition in patients undergoing continuous ambulatory peritoneal dialysis.
Jones, W; Kazama, RM; Kogan, FJ; Mayersohn, M; Michael, UF; Perrier, D; Sampliner, RE,
)
3.02
"In order to establish improved guidelines for dosage adjustments of cimetidine before and during hemodialysis, the kinetics of this drug was investigated in 7 uremic patients undergoing regular hemodialysis."( Pharmacokinetics of cimetidine in patients undergoing hemodialysis.
Bjaeldager, PA; Hvidberg, EF; Jensen, JB; Larsen, NE; Nielsen, LP, 1983
)
0.82
" Because of the 40% decrease in total clearance, dosage in cirrhotic patients with a history of PSE should be reduced to minimize the risk of CNS side effects associated with cimetidine."( Hepatic encephalopathy and altered cimetidine kinetics.
Bernhard, H; Schentag, JJ; Ziemniak, JA, 1983
)
0.74
" Consequently, a computer program was developed for cimetidine dosage regimen prediction which can be used for "normal" subjects, young and geriatric patients without and with renal impairment."( Prediction of cimetidine disposition in the aged.
Ritschel, WA, 1983
)
0.88
"The pharmacokinetic behavior of cimetidine has not been described in children, and there is no authoritative guideline on cimetidine dosage for children."( Pharmacokinetics of cimetidine in critically ill children.
Baltodano, A; Chin, TW; Edmonds, JF; Fenje, P; MacLeod, SM; Soldin, SJ, 1982
)
0.87
" In each course, dosing was initiated at half the recommended dosage of 600 mg daily, and mental status deteriorated shortly after dosing began."( Dose and serum concentration relationships in cimetidine-associated mental confusion.
Berg, MJ; Calleri, G; Cerra, FB; Kimelblatt, BJ; McMillen, MA; Schentag, JJ, 1980
)
0.52
" Cimetidine may cause mental confusion and should be used with caution and in reduced dosage in the presence of hepatic or renal disease, or both, and in elderly patients."( Cimetidine: clinical uses and possible side effects.
Babb, RR, 1980
)
2.61
"Over a 15-month period, 75 critically ill patients at risk of acute gastrointestinal bleeding were randomized into two groups: one group (38 patients) received the H2-blocker cimetidine intravenously at an initial dosage of 300 mg every six hours, and the other group (37 patients) received antacid (Mylanta II) through a nasogastric tube at an intial dosage of 30 ml every hour."( Antacid versus cimetidine in preventing acute gastrointestinal bleeding. A randomized trial in 75 critically ill patients.
Bushnell, LS; Long, PC; Priebe, HJ; Silen, W; Skillman, JJ, 1980
)
0.81
" Results suggest that acid secretion blockage with limited dosage has no advantage in micromucosal visualization."( Double-blind evaluation of cimetidine as an adjunct to the routine double contrast upper-gastrointestinal examination.
Carrier, JW; Kutzen, B; Radcliffe, RV, 1980
)
0.56
"6 gm/day of cimetidine for the next three weeks, while the other patients remained on the initial dosage schedule for three more weeks."( Long-term treatment of gastric ulcer with cimetidine.
Da Silva, EP; Zaterka, S, 1981
)
0.91
" The results suggest that ulcer recurrence is not commoner after treatment with standard dose of cimetidine than after a low dosage of cimetidine or trimipramine."( Relapse of duodenal ulcer after treatment with trimipramine/antacids or cimetidine/antacids.
Aadland, E; Berstad, A; Bjerke, K; Carlsen, E, 1981
)
0.71
"A multicenter double-blind study was made to compare whether 1,000 mg dosage of cimetidine, the dose commonly employed in the United Kingdom, was as effective as the 1,200 mg."( Double-blind multicenter comparison of 1,200 mg. and 1,000 mg. cimetidine in hospitalized and ambulatory duodenal ulcer patients.
Cohen, NN; Davis, WD; Font, RG; Graham, DY; Mann, JA; Sabesin, SM; Schwartz, JT, 1981
)
0.73
" After ulcer healing, drug dosage was reduced (cimetidine to 400 mg at night and Caved-S to two tablets twice daily)."( Comparison between cimetidine and Caved-S in the treatment of gastric ulceration, and subsequent maintenance therapy.
Darnborough, A; McAdam, WA; Morgan, AG; Pacsoo, C, 1982
)
0.85
"0 g cimetidine/day in divided doses before dosing with 40 mg furosemide produced no significant effects on furosemide plasma levels or in its effects on urinary water and electrolyte excretion."( Effect of cimetidine on the absorption and efficacy of orally administered furosemide.
Bradbrook, ID; House, FR; Morrison, P; Rogers, HJ, 1982
)
1.22
" The plasma concentrations of the sulphoxide metabolite increased successively with time after dosing and no elimination phase was observed still 9 h after dose."( The pharmacokinetics of cimetidine and its sulphoxide metabolite in patients with normal and impaired renal function.
Bertler, A; Bodemar, G; Erlanson, P; Fransson, L; Larsson, R; Norlander, B; Walan, A, 1982
)
0.57
" It is concluded that cimetidine on this dosage schedule is not effective in the prevention of gastric erosions in a cervical cord section rat model, whereas the ulceroprotective effects of 16,16-dmPGE2 and antacids are significant."( Effects of antacids, cimetidine, and 16,16-dimethyl prostaglandin E2 on acute gastric erosions in a spinal rat.
Gillich, A; Sigman, HH, 1982
)
0.9
" It appears that both dosage and underlying disease state are important factors determining the nature and severity of cimetidine-associated mental status changes."( Mental status, the intensive care unit, and cimetidine.
Cerra, FB; Fitzgerald, GC; Karwande, SV; Leising, M; McMillen, M; Schentag, JJ, 1982
)
0.73
" Twice a day dosage is likely to improve patient compliance, costs less, and may reduce dose-related side effects."( Twice-a-day dosage of cimetidine in the short-term treatment of peptic ulcer.
Eaves, R; Korman, MG, 1982
)
0.58
"Using a recently developed computer program based on a correlation between methods to predict the elimination half-life and apparent volume of distribution of cimetidine and actual data from patients, ideal dosage regimens were generated for patients with renal impairment and for geriatric patients, together with the corresponding maximum and minimum steady state concentrations."( Cimetidine dosage regimen for patients with renal failure and for geriatric patients.
Ritschel, WA, 1982
)
1.9
" Dosing began in March 1976."( Safety evaluation of cimetidine: 54 month interim report on long-term study in dogs.
Crean, GP; Leslie, GB; Roe, FJ; Walker, TF; Whitehead, SM, 1981
)
0.58
" No dosage adjustment need be made when patients receiving cimetidine undergo any form of dialysis; hemoperfusion may be of some benefit in removing drug from the central as well as tissue compartments in an acute overdose situation."( Removal of cimetidine by peritoneal dialysis, hemodialysis, and charcoal hemoperfusion.
Moore, MC; Pizzella, KM; Schentag, JJ; Schultz, RW; Walshe, J, 1980
)
0.89
" The dosage was not adjusted in over 50% of the patients in whom impairment of renal function was serious enough to warrant consideration of a dosage reduction."( Use of cimetidine in hospital patients.
Behun, M; Hall, KW; Irvine-Meek, J; Otten, N, 1981
)
0.72
" Bronchial response was monitored with serial measurements of specific airways conductance (sGaw) and a dose-response curve was constructed for each challenge."( The role of histamine receptors in asthma.
Eiser, NM; Guz, A; Mills, J; Snashall, PD, 1981
)
0.26
" The authors suggest that the dosage of surface antacids should be expressed in anti-acid mEq, knowing that 50 mEq produce as therapeutic effect lasting approximately 30 minutes."( [Radiotelemetric study of the effects of antacids and cimetidine on intragastric pH (author's transl)].
Caulin, C; Isal, JP; Lamotte, M, 1981
)
0.51
" Similar effects were observed with chronic dosing of cimetidine."( Cimetidine: a specific inhibitor of hepatic aryl hydrocarbon hydroxylase (AHH) in the rat.
Drew, R; Grygiel, JJ; Rowell, J, 1981
)
1.95
" In order to determine whether a high dosage therapy with a calcium-containing antacid accelerates the healing of the ulcer or retards it through the "Acid-rebound" effect of the calcium, we examined in a clinical study 10 patients with an endoscopically proven duodenal ulcer."( [Calcium-containing antacids in the therapy of duodenal ulcers].
Kunert, H; Weingart, J, 1981
)
0.26
" The recovery of the content of mucus glycoprotein in drug dosed rats occurred within 3 h after aspirin dosing and was nearly 90% of control at 5 h in all cases."( Efficacy of anti-ulcer drugs on the recovery of gastric mucosal glycoproteins with aspirin-induced gastric damage in rat.
Azuumi, Y; Hotta, K; Ishihara, K; Ohara, S; Okabe, H, 1981
)
0.26
" Some adjustment in theophylline dosage may be needed in treated patients who are also given cimetidine, and these patients who are also given cimetidine, and these patients should be studied closely with theophylline serum concentration measurements and careful clinical assessments."( Alteration of theophylline clearance and half-life by cimetidine in normal volunteers.
Bernhard, H; Reitberg, DP; Schentag, JJ, 1981
)
0.73
" The presence of specific H1 histamine receptors was further supported by shifts in the dose-response curve to histamine by four different concentrations of diphenhydramine."( Mechanisms of histamine stimulated secretion in rabbit ileal mucosa.
Higgs, NB; Linaker, BD; McKay, JS; Turnberg, LA, 1981
)
0.26
" 4 Administration of 400 mg cimetidine 8 hourly and at night for 6 days and dosing with 500 mg tetracycline as tablets or suspension on the fifth day produced no alteration in tetracycline kinetics."( Effect of cimetidine on the absorption of orally administered tetracycline.
Bradbrook, ID; Fisher, P; House, F; Inns, P; Morrison, PJ; Rogers, HJ, 1980
)
0.96
" The study indicates that the correlation between plasma cimetidine levels and gastric acid secretion is poor, but that the cimetidine dosage used suppressed acid output during the entire dosing interval."( Relationship between cimetidine plasma levels and gastric acidity in acutely ill patients.
Bombeck, CT; Cohen, IA; Nation, R; Nyhus, LM; Siepler, JK, 1980
)
0.83
" Cimetidine caused parallel displacement of the dose-response curve to histamine, but failed to alter the response to carbachol or gastrin."( Secretagogue stimulation of [14C]aminopyrine accumulation by isolated canine parietal cells.
Soll, AH, 1980
)
1.17
" If confirmed with the solid dosage form in man, the present study suggests that unlike magnesium aluminum hydroxide gel, cimetidine may be used as an effective means of reducing gastric acid in patients who take tetracycline."( Effect of cimetidine on absorption of oral tetracycline in mice.
Garty, M; Hurwitz, A, 1980
)
0.87
" Dose-response curves were constructed and analysed in the presence of H1- and H2-antagonists."( The effect of histamine and histamine antagonists on gastric acid secretion and mucosal blood flow in man.
Knight, SE; McIsaac, RL; Rennie, CD, 1980
)
0.26
" Cumulative dose-response contraction curves were constructed."( A dual action of histamine on isolated human pulmonary arteries.
Boe, J; Boe, MA; Simonsson, BG, 1980
)
0.26
" The observed milk/serum ratio for the three dosing regimens were not significantly different from one another."( Active transport of cimetidine into human milk.
Desai, N; Kuhn, RJ; McNamara, PJ; Oo, CY, 1995
)
0.61
"Full dose-response curves to histamine were constructed in 16 healthy volunteers (mean age, 47 +/- 20 years; age range, 21 to 80 years) by infusing histamine (2 to 136 ng/min) into dorsal hand veins preconstricted with the alpha-adrenergic selective agonist phenylephrine."( H1- and H2-histamine receptor-mediated vasodilation varies with aging in humans.
Bedarida, G; Blaschke, TF; Bushell, E; Hoffman, BB, 1995
)
0.29
" Dose-response curves to histamine were repeated after infusion of the H2-selective antagonist cimetidine at a dose sufficient to completely block the H2-mediated response (49 micrograms/min)."( H1- and H2-histamine receptor-mediated vasodilation varies with aging in humans.
Bedarida, G; Blaschke, TF; Bushell, E; Hoffman, BB, 1995
)
0.51
" Some compounds also proved to be effective inhibitors of stimulated acid secretion in both the rat and dog when dosed intravenously."( Reversible inhibitors of the gastric (H+/K+)-ATPase. 5. Substituted 2,4-diaminoquinazolines and thienopyrimidines.
Blurton, P; Brown, TH; Ife, RJ; Keeling, DJ; Leach, CA; Meeson, ML; Parsons, ME; Theobald, CJ, 1995
)
0.29
" The drug dosage can be reduced, freeing the patient of the adverse reaction, but leaving behind a background activity adequate to produce a therapeutically beneficial effect."( A comparative overview of the adverse effects of antiulcer drugs.
Piper, DW, 1995
)
0.29
" Dosage requirements vary according to age and clinical condition, and children require a relatively higher drug dosage (mg/kg) than adults."( Do H2 receptor antagonists have a therapeutic role in childhood?
Kelly, DA, 1994
)
0.29
" Moreover, the inhibitory effect of YM-14471 was more prolonged than those of famotidine and cimetidine by either route, and it was as long as that of omeprazole dosed orally."( Antisecretory effects of a novel and long-lasting histamine H2-receptor antagonist, YM-14471, in rats and dogs.
Fujihara, A; Kamato, T; Miyata, K; Nishida, A; Takeda, M; Yuki, H, 1993
)
0.51
" We conclude that gastric mucosal concentrations of histamine H2-receptor blockers achieved after oral dosing are probably too low to cause significant inhibition of gastric ADH in vivo."( Inhibition of gastric alcohol dehydrogenase activity by histamine H2-receptor antagonists has no influence on the pharmacokinetics of ethanol after a moderate dose.
Bergmann, JF; Blanc, LE; Delchier, JC; Dhumeaux, D; Dutreuil, C; Mallat, A; Roudot-Thoraval, F; Simonneau, G; Trout, H, 1994
)
0.29
"Male Sprague-Dawley rats had their bile ducts cannulated and were dosed with [3H]taxol (2 mg/kg, 68-77 microCi/mg) as a continuous intravenous infusion for 6 hr so that the plasma concentrations, tissue distribution, metabolism, and biliary secretion of taxol could be studied."( Effect of cimetidine, probenecid, and ketoconazole on the distribution, biliary secretion, and metabolism of [3H]taxol in the Sprague-Dawley rat.
Collins, JM; Egorin, MJ; Erkmen, K; Jamis-Dow, CA; Klecker, RW; Parker, RJ; Stevens, R,
)
0.53
" The inclusion of oral and intravenous dosage data of alcohol is mandatory to positively identify first-pass metabolism in any individuals."( H2-antagonists and alcohol. Do they interact?
Gugler, R, 1994
)
0.29
" Schedule dependency and dose-response evaluations involving Taxol were studied in the SC M109 model."( Taxol-based combination chemotherapy and other in vivo preclinical antitumor studies.
Rose, WC, 1993
)
0.29
" A program designed to reduce dosages to maintenance therapy after eight weeks at treatment dosage was developed by the Pharmacy and Therapeutics Committee with staff physician input."( Antiulcer prescribing program in a state correctional system.
Cason, DM; Helling, DK; Keith, MR, 1994
)
0.29
"The follow-up DUE showed the mean daily dosage for prescribed histamine2-receptor antagonists decreased (cimetidine from 694 to 454 mg, ranitidine from 280 to 183 mg) and the mean duration of therapy decreased from 14 to 10 months."( Antiulcer prescribing program in a state correctional system.
Cason, DM; Helling, DK; Keith, MR, 1994
)
0.5
" Moreover, if omeprazole is administered at a pharmacologically effective dosage for a short period of time, it may not have serious effects on the ultrastructure of human parietal cells."( The effects of omeprazole on the ultrastructure of gastric parietal cells.
Fujii, T; Kato, S; Naganuma, H; Nakagawa, H; Nakano, K, 1994
)
0.29
" In the PAG/DR, the HA dose-response curve had an inverted U-shape, showing that HA can induce both antinociceptive (0."( Histamine-induced modulation of nociceptive responses.
Hough, LB; Mischler, SA; Nalwalk, JW; Thoburn, KK, 1994
)
0.29
" The subjects consumed 50 g alcohol after a standard lunch on the eighth day of dosing with study medication."( Lack of effect of H2-receptor antagonists on the pharmacokinetics of alcohol consumed after food at lunchtime.
Braithwaite, R; Gibson, GJ; Hale, KA; Kendall, MJ; Langman, MJ; Spannuth, F; Walt, RP, 1994
)
0.29
" We conclude that twice-daily cimetidine at a dosage of 20 mg/kg/day is as effective for the symptomatic improvement and healing of peptic ulcer as the conventional three- or four-times-daily regimens."( Efficacy of twice-daily cimetidine in pediatric peptic ulcer.
Kato, S; Nakagawa, H; Ohtake, M; Ozawa, A; Shibuya, H, 1994
)
0.88
"A titrimetric method, with N,N-dibromodimethylhydantoin as reagent, has been developed for the determination of cimetidine in pure form and in dosage forms."( Determination of cimetidine in pure form and in dosage forms using N,N-dibromodimethylhydantoin.
Karpagaselvi, L; Kumar, KG, 1994
)
0.84
" Twelve healthy subjects received a single 20 mg dose of ebastine on day 2 of a multiple oral dosing regimen of either cimetidine (400 mg three times daily and 800 mg in the evening on the day preceding ebastine administration and 400 mg four times daily on the 2 following days) or placebo in a randomised cross-over design."( Cimetidine does not influence the metabolism of the H1-receptor antagonist ebastine to its active metabolite carebastine.
Breimer, DD; Bruno, R; Cohen, AF; Reinhoudt, JF; Schoemaker, HC; Van Rooij, J, 1993
)
1.94
" This DRF at the low dosage of cimetidine used in this study compared with known radioprotectors is very promising and it might be useful as a potent radioprotector."( Radioprotective effects of cimetidine in mouse bone marrow cells exposed to gamma-rays as assayed by the micronucleus test.
Gharbali, A; Mozdarani, H, 1993
)
0.87
"This multicenter, double-blind, randomized, placebo-controlled trial investigated QID and BID regimens of cimetidine (total daily dosage of 1600 mg) in adult patients with moderate or severe gastroesophageal reflux disease."( Cimetidine QID and BID in rapid heartburn relief and healing of lesions in gastroesophageal reflux disease.
Hedrich, DA; Karlstadt, RG; Miller, DM; Palmer, RH,
)
1.79
" A strong dose-response relation was present among cimetidine users."( Risk of gynaecomastia associated with cimetidine, omeprazole, and other antiulcer drugs.
García Rodríguez, LA; Jick, H, 1994
)
0.81
" In healthy volunteers full dose-response curves were constructed by infusing histamine, before and after administration of an H1 or H2 antagonist or both antagonists, into dorsal hand veins preconstricted with the alpha-adrenergic agonist phenylephrine."( Histamine-induced venodilation in human beings involves both H1 and H2 receptor subtypes.
Bedarida, G; Blaschke, TF; Dachman, WD; Hoffman, BB, 1994
)
0.29
"5 g/kg) of ethanol under four challenge conditions: (a) a single dose of placebo prior to alcohol ingestion in the morning, (b) a single dose of H2-antagonist prior to alcohol ingestion in the morning, (c) 14-day chronic dosing with H2-antagonist prior to alcohol ingestion in the evening, and (d) 28-day chronic dosing with H2-antagonist prior to alcohol ingestion in the morning."( Cimetidine and ranitidine. Lack of effect on the pharmacokinetics of an acute ethanol dose.
Chesher, GB; Dauncey, H; Palmer, RH, 1993
)
1.73
" In addition to the patient's age and the prescriber's medical specialty, specific DUE criteria included the reason given in the medical record for use; dosage regimen and adjustments made on the basis of the patient's renal function; other GI drugs taken concurrently; pharmacist intervention; simultaneous use of oral medications; occurrence of adverse events; H2-antagonist use with specified drug products known to affect serum drug concentrations of one or both medications; and use of gastric pH monitoring."( Use of i.v. cimetidine, ranitidine, and famotidine in 40 hospitals.
Ben-Joseph, R; Oh, T; Russell, WL; Segal, R, 1993
)
0.66
"5 mg/h, was compared with sucralfate, administered via nasogastric tube, at a dosage of 1 g every 6 hours suspended in 20 mL of sterile water."( Nosocomial pneumonia during stress ulcer prophylaxis with cimetidine and sucralfate.
Celoria, G; Dawson, J; Navab, F; Ryan, P; Teres, D, 1993
)
0.53
" They were obtained by the chi-square (chi 2) goodness-of-fit test, recently applied for the evaluation of dose-response curves."( Modern approach to the evaluation of combined effects of single-dose trials and clinical time-course studies, exemplified by combinations of pirenzepine and H2-receptor antagonists.
Londong, W; Pöch, G, 1993
)
0.29
" (3) Group C, after healing of DU, 54 patients received a maintenance dosage of cimetidine 400 at night for up to 1 year."( [Study on omeprazole 20 mg twice weekly in prevention of duodenal ulcer relapse].
Bei, L; Chen, SP; Wen, SH, 1993
)
0.51
" The only risk factor for ranitidine was for patients who did not have their dosage corrected for renal function ("overdose"); these patients were twice as likely to experience a PADR compared with patients who received the correct dosage as determined by their renal function."( Risk for adverse events among patients receiving intravenous histamine2-receptor antagonists.
Ben-Joseph, R; Russell, WL; Segal, R, 1993
)
0.29
" A standardized dosage of cyclosporine was given orally, and the duration was calculated for the maximum whole blood level of cyclosporine to be achieved; the dosage/level quotient was calculated."( The influence of gastrointestinal agents on resorption and metabolism of cyclosporine after heart transplantation: experimental and clinical results.
Markewitz, A; Meiser, BM; Muschiol, F; Nollert, G; Pfeiffer, M; Reichart, B; Reichenspurner, H; Uberfuhr, P; Wagner, F,
)
0.13
"4 mg/kg as an intravenous infusion over 5 min (a dosage previously used to test drug interactions with cimetidine and ranitidine) were evaluated in 7 patients with chronic obstructive pulmonary disease (COPD) and peptic ulcer disease before and after 8 days' treatment with famotidine 40mg at night."( Famotidine and theophylline pharmacokinetics. An unexpected cimetidine-like interaction in patients with chronic obstructive pulmonary disease.
Dal Negro, R; Pomari, C; Turco, P, 1993
)
0.74
" In the guinea pig ileum, millimolar concentrations of cimetidine and famotidine shifted the dose-response curve of the contractile response to acetylcholine rightward."( Comparative effects of cimetidine and famotidine on the vagally stimulated acid secretion in the isolated mouse whole stomach.
Kanaoka, S; Watanabe, K; Yamamoto, M; Yano, S, 1993
)
0.84
" For patients refractory to these drugs or for which once-a-day dosing is desirable, omeprazole has an advantage."( Antiulcer therapy.
Papich, MG, 1993
)
0.29
" Venous blood sampling for pharmacokinetic assessment was done over a complete dosing interval on day 7 of each phase."( Effects of cimetidine and ranitidine on the pharmacokinetics of a chronotherapeutically formulated once-daily theophylline preparation (Uniphyl).
Babul, N; Buttoo, KM; Fraser, IM; Stewart, JH; Walker, SE,
)
0.52
" When nefazodone and cimetidine were co-administered for 1 week, no change in steady-state pharmacokinetic parameters for cimetidine, nefazodone or hydroxynefazodone was observed compared with each drug dosed alone."( Lack of interaction between nefazodone and cimetidine: a steady state pharmacokinetic study in humans.
Barbhaiya, RH; Greene, DS; Shukla, UA, 1995
)
0.87
"6 h) dosing periods."( Evaluation of the pharmacokinetic interaction between cimetidine or famotidine and cyclosporine in healthy men.
Collier, DS; McGuire, TR; Rossi, SJ; Schaaf, LJ; Shaefer, MS; Stratta, RJ, 1995
)
0.54
" Based on the observation that neither cimetidine nor ranitidine had a significant effect on serum concentrations of zidovudine or zidovudine glucuronide, a change in the dosage of zidovudine is not warranted."( The effect of cimetidine and ranitidine administration with zidovudine.
Balfour, HH; Fletcher, CV; Henry, WK; Noormohamed, SE; Rhame, FS,
)
0.76
" Clinical considerations may dictate a reduction in tacrine dosage when tacrine is coadministered with cimetidine."( Inhibition of tacrine oral clearance by cimetidine.
deVries, TM; Forgue, ST; Reece, PA; Sedman, AJ, 1996
)
0.78
" SKF92374 showed strong similarities to cimetidine in analgesic efficacy, slope of dose-response curves and chemical structure, suggesting that these compounds share a common analgesic mechanism."( Characterization of the antinociceptive properties of cimetidine and a structural analog.
Barker, LA; Cumming, P; Hough, LB; Li, BY; Nalwalk, JW; Parsons, ME, 1996
)
0.81
" Results showed that both antihistamines, applied topically of dosed orally, reduced sneezing even when significant increases of histamine concentration in nasal secretions were evidenced immediately after NAC."( The activity of recent anti-allergic drugs in the treatment of seasonal allergic rhinitis.
Clement, P; De Waele, M; Smitz, J; Wang, D, 1996
)
0.29
" Statistically significant reductions in the AUC0-24 and maximum plasma concentration values were observed with the mannitol dosage forms compared to the sucrose controls."( The effect of mannitol on the oral bioavailability of cimetidine.
Adkin, DA; Davis, SS; Huckle, PD; Sparrow, RA; Wilding, IR, 1995
)
0.54
" Histamine decreased lymphocyte proliferation while (in order of potency) cimetidine, the hydroxy metabolite of metronidazole, imidazole and metronidazole, increased the mitogenic response to PHA in a dose-response fashion."( Effects of metronidazole and its metabolites on histamine immunosuppression activity.
Elizondo, G; Ostrosky-Wegman, P, 1996
)
0.52
" Hourly dosing with hydrochloric acid reversed the protective effect of ranitidine, cimetidine and loxtidine on macroscopic damage and, histologically, this was associated with the widespread appearance of antral ulcers and a reduction in the proportion of mucosal damage caused by superficial erosions."( The role of acid in the pathogenesis of indomethacin-induced gastric antral ulcers in the rat.
Clayton, NM; Oakley, I; Trevethick, MA; Williams, LV, 1996
)
0.52
" Changes in [Ca2+]i and inositol phosphate production exhibit a similar dose-response relationship for histamine (maximal effect at 10(-4) M), with both phenomena being blocked by the H1 antagonist mepyramine and being insensitive to pertussis toxin treatment."( Histamine activates phospholipase C in human airway epithelial cells via a phorbol ester-sensitive pathway.
Barzanti, F; Gruenert, DC; Hrelia, S; Rugolo, M, 1996
)
0.29
" Butorphanol nasal spray and cimetidine can be co-administered without any adjustment of dosage for either drug."( Lack of pharmacokinetic interaction between butorphanol nasal spray and cimetidine.
Barbhaiya, RH; Shyu, WC, 1996
)
0.82
" Paclitaxel dosage was escalated in 10 mg/m2/wk increments in subsequent patients, to a maximum dosage of 90 mg/m2/wk."( Schedule- and dose-intensified paclitaxel as weekly 1-hour infusion in pretreated solid tumors: results of a phase I/II trial.
Freund, W; Hausamen, TU; Lipke, J; Löffler, TM, 1996
)
0.29
" The optimal dosage and duration of treatment with cimetidine have not been established and are likely to be patient-specific."( Cimetidine in the treatment of acute intermittent porphyria.
Rogers, PD, 1997
)
1.99
"Profiles of 20-h intragastric acidity were measured simultaneously in 24 healthy subjects who were dosed (at 12."( Inhibition of intragastric acidity in healthy subjects dosed with ranitidine 75 mg: a comparative study with cimetidine and placebo.
Constantinides, S; Grimley, CE; Mills, JG; Nwokolo, CU; Snell, CC, 1997
)
0.51
" (i) Daytime (0-10 h post-dose): when dosed with placebo the weighted intragastric acidity was 31."( Inhibition of intragastric acidity in healthy subjects dosed with ranitidine 75 mg: a comparative study with cimetidine and placebo.
Constantinides, S; Grimley, CE; Mills, JG; Nwokolo, CU; Snell, CC, 1997
)
0.51
" Methylprednisolone sodium succinate was given at a dosage of 30 mg/kg of body weight prior to myelography, followed by a second full or half dose 2 to 4 hours later at clinician discretion."( Clinical evaluation of cimetidine, sucralfate, and misoprostol for prevention of gastrointestinal tract bleeding in dogs undergoing spinal surgery.
Bostwick, DR; Hanson, SM; Smith, MO; Twedt, DC, 1997
)
0.61
" Histamine dose-response curves showed that concentrations between 5 nm and 5 microM increased permeability, while concentrations from 50 microM to 5 mM reduced it."( Regulation of cerebral microvascular permeability by histamine in the anaesthetized rat.
Easton, AS; Fraser, PA; Sarker, MH, 1998
)
0.3
" Dose-response relationships to histamine were done in rings of canine pulmonary artery from heartworm and control dogs, in the presence and absence of endothelial cells, the H1 receptor blocker tripelennamine, or the H2 receptor blocker cimetidine."( Dirofilaria immitis: heartworm infection converts histamine-induced constriction to endothelium-dependent relaxation in canine pulmonary artery.
Kaiser, L; Williams, JF, 1998
)
0.48
" Twelve healthy subjects were administered single doses of clarithromycin alone and with oral cimetidine dosed to steady state."( Oral cimetidine prolongs clarithromycin absorption.
Amsden, GW; Cheng, KL; Nafziger, AN; Peloquin, CA, 1998
)
1.03
" Comparisons of mean AUCs for each 15 min period after dosing showed that decrease in acidity was significantly greater after cimetidine 200 mg effervescent than after famotidine 10 mg for the first 60 min."( Low-dose famotidine and effervescent cimetidine in healthy subjects: a placebo-controlled overnight pH study.
Cottrell, J; Grimley, CE; Mann, SG; Nwokolo, CU; Raskin, S; Reilly, TG; Usselmann, B, 1998
)
0.78
"Inhibition of gastric acidity over the 12 h post-dose period was significantly greater and endured longer after famotidine 10 mg than after effervescent cimetidine 200 mg, but for the 60 min period immediately after dosing the effect on intragastric pH was significant following effervescent cimetidine 200 mg but not famotidine 10 mg."( Low-dose famotidine and effervescent cimetidine in healthy subjects: a placebo-controlled overnight pH study.
Cottrell, J; Grimley, CE; Mann, SG; Nwokolo, CU; Raskin, S; Reilly, TG; Usselmann, B, 1998
)
0.77
" The effects of a minimum of 2 weeks of dosing with cimetidine, ranitidine and omeprazole were examined."( Omeprazole, ranitidine, and cimetidine have no effect on peak blood ethanol concentrations, first pass metabolism or area under the time-ethanol curve under 'real-life' drinking conditions.
Brown, AS; James, OF, 1998
)
0.84
" Whole EN activity was not stimulated even by the highest dose (1 x 10(-1) M) of histamine when the nose was pretreated with saline, but was substantially stimulated by histamine in a dose-response fashion (1 x 10(-2) M) after pretreatment with HCI or H2SO4."( Does histamine stimulate trigeminal nasal afferents?
Kuwahara, M; Sekizawa, S; Sugano, S; Tsubone, H, 1998
)
0.3
"These results suggest that, in contrast to cimetidine, the inhibitory effect of omeprazole on AII-stimulated aldosterone production following dosing with furosemide is negligible."( Effect of omeprazole and cimetidine on plasma aldosterone response to angiotensin II.
Fujimura, A; Maeda, A; Sasaki, M, 1998
)
0.87
"In a 1400-bed teaching hospital, an audit (by specially trained personnel) was conducted to monitor inpatient prescribing of omeprazole (1) in preference to H2-antagonists and other drugs according to agreed criteria (Helicobacter pylori eradication, severe reflux esophagitis, rapid ulcer healing deemed urgent because of severe symptoms or complications, high-dose steroid therapy of > or =30 mg/day prednisolone) and (2) appropriateness of intravenous dosing (oral route not feasible or contraindicated)."( Antiulcer drug prescribing in hospital successfully influenced by "immediate concurrent feedback".
Chan, CK; Cheung, E; Ching, TY; Chu, KM; Kong, Y; Kou, M; Kumana, CR; Lam, SK; Seto, WH, 1998
)
0.3
"Prediction of the drug level in the volume of distribution was made using a numerical model taking into account the following facts: the kinetics of drug release out of the dosage form along the gastrointestinal tract, the kinetics of absorption in the blood compartment and the kinetics of elimination."( Assessment of blood level with controlled-release dosage forms: effect of the rate constant of elimination of the drug.
Aïnaoui, A; Vergnaud, JM,
)
0.13
" cimetidine or famotidine for stress ulcer prophylaxis were reviewed during a two-month period in 1997, and information on demographics, dosage and duration of H2RA therapy, admission date, laboratory test values, and adverse drug reactions was collected."( Using multiple pharmacoeconomic methods to conduct a cost-effectiveness analysis of histamine H2-receptor antagonists.
Blayney-Chandramouli, J; McCoy, S; Mutnick, A, 1998
)
1.21
" The results indicate that dimaprit, an H2 agonist, facilitated retention (25 and 50 pg) with a U-shaped dose-response curve typical of drugs acting at postsynaptic receptors."( Effect of histamine H2 and H3 receptor modulation in the septum on post-training memory processing.
Flood, JF; Morley, JE; Uezu, K, 1998
)
0.3
"Based on the small changes in the pharmacokinetic parameters of dolasetron and its active metabolites, as well as the favorable safety results, no dosage adjustments for dolasetron mesylate are recommended with concomitant administration of cimetidine or rifampin."( Pharmacokinetics of dolasetron with coadministration of cimetidine or rifampin in healthy subjects.
Arumugham, T; Cramer, MB; Dimmitt, DC; Keung, A; Weir, SJ, 1999
)
0.73
" The time to onset of action and the degree of gastric acid inhibition of the H2 -RAs famotidine and cimetidine at dosage levels approved for over-the-counter use (10 mg famotidine and 200 mg cimetidine) were compared."( The action of 10 mg famotidine versus 200 mg cimetidine: onset and magnitude of antisecretory action within the first 2 hours after administration.
Decktor, D; Houle, JM; Pierce, CH, 1998
)
0.78
"At Cabrini Medical Center, drug usage evaluation (DUE) and monthly purchasing data analysis were used to determine the indications for which H2 antagonists were being used, the appropriateness of parenteral therapy, the use of extended dosing intervals, and the cost effectiveness of cimetidine (Tagamet)."( Multi-purpose evaluation of H2-antagonist usage.
Gianarkis, D, 1992
)
0.46
" Forty hospitals provided data about purchase prices for each IV H2-RA dosage form purchased (cimetidine, ranitidine, and famotidine), the number of each dosage form used during the 12-month study period, purchase price and extent of usage for supplies, labor costs for preparing and administering IV H2-RAs, and IV H2-RA dosage schedules."( A pharmacoeconomic analysis of IV H2-receptor antagonist use in 40 hospitals.
Ben-Joseph, R; Oh, T; Russell, WL; Segal, R, 1994
)
0.51
" Comparison of the dose-response curves between TPA-induced hydrogen (H+) secretion, as measured by aminopyrine (AP) uptake, and the membrane-associated PKC-alpha suggests that translocation of PKC-alpha is not involved in the H+ secretory process in PC."( Expression and characterization of protein kinase C in isolated rabbit parietal cells.
Kim, SW; Levine, RA; Loo, A; Nandi, J, 1999
)
0.3
" Appropriateness of dosage could not be determined in 42 (16."( A prospective evaluation of cimetidine drug use.
Andritz, MB; Hamilton, RA; Kowalsky, SF; Platek, TE, 1989
)
0.57
" Cetirizine shifted the histamine dose-response at both temperatures: statistically significantly at 14 degrees C only."( Histamine response and local cooling in the human skin: involvement of H1- and H2-receptors.
Grossmann, M; Jamieson, MJ; Kirch, W, 1999
)
0.3
" Oral clearance during the nighttime dosing interval was 13% greater than the daytime oral clearance for nonsmokers and 22% greater for smokers, showing a greater circadian rhythm for smokers."( The effect of low-dose cimetidine (200 mg twice daily) on the pharmacokinetics of theophylline.
Boike, SC; Boyle, DA; Di Cicco, RA; Jorkasky, DK; Miller, AK; Nix, DE; Schentag, JJ; Zariffa, N, 1999
)
0.61
"To determine the effects of the maximum recommended over-the-counter (OTC) cimetidine dosage on phenytoin concentrations in ambulatory seizure patients on long-term phenytoin therapy."( Effect of over-the-counter cimetidine on phenytoin concentrations in patients with seizures.
Driscoll-Bannister, SM; Frazier, LM; Garnett, WR; O'Hara, KA; Pugh, CB; Rafi, JA,
)
0.66
"It is possible that the lack of change in phenytoin concentrations was a result of the low daily dosage of cimetidine used or other factors related to the "real world" setting of the study."( Effect of over-the-counter cimetidine on phenytoin concentrations in patients with seizures.
Driscoll-Bannister, SM; Frazier, LM; Garnett, WR; O'Hara, KA; Pugh, CB; Rafi, JA,
)
0.64
" No direct drug-drug interactions were found in these studies, suggesting that repaglinide may be coprescribed with cimetidine, digoxin, or theophylline at the dosage used for monotherapy."( Drug interaction studies with repaglinide: repaglinide on digoxin or theophylline pharmacokinetics and cimetidine on repaglinide pharmacokinetics.
Hatorp, V; Thomsen, MS, 2000
)
0.73
" Subsequent studies confirmed that multiple daily dosing of histamine-2 receptor antagonists (H2RAs) was mandatory for GERD treatment, with clear dose-response relationships for each agent."( Drugs, bugs, and esophageal pH profiles.
Robinson, M,
)
0.13
" Flow-through electrodes, selective to chlorpromazine, amitriptyline, propantheline, cimetidine, and ranitidine, have been constructed and used for the dissolution studies of 18 dosage forms using the rotating basket apparatus."( Dissolution studies of drug formulations using ion-selective electrodes as sensors in an air-segmented continuous flow analyzer.
Christopoulos, TK; Diamandis, EP; Koupparis, MA; Mitsana-Papazoglou, A, 1987
)
0.5
" If an underlying problem requires long-term immunosuppressive medication, it is wiser to choose cimetidine rather than increasing the steroid dosage to resolve atypical PFAPA."( PFAPA syndrome (Periodic Fever, Aphthous stomatitis, Pharyngitis, Adenitis).
Chen, LC; Huang, JL; Lee, KF; Lee, WI; Lin, SJ; Yang, MH; Yeh, KW, 1999
)
0.52
" A possible explanation for the inhibitory effects of histamine at 10-mM dosage was apparently found in that the effects of the high concentration may be supraphysiological; and furthermore, there is a difference in the mechanism by which histamine exerts its effects mediated by the histamine receptors on the cochlea."( The effects of histamine and its antagonists on the cochlear microphonic and the compound action potential of the guinea pig.
Masuyama, K; Minoda, R; Toriya, T; Yumoto, E, 2001
)
0.31
" This newly developed capillary electrophoresis (CE) method was applied for the determination of analytes extracted from plasma taken from a volunteer dosing a cimetidine, ranitidine, and nizatidine tablet simultaneously."( Head-column field-amplified sample stacking in capillary electrophoresis for the determination of cimetidine, famotidine, nizatidine, and ranitidine-HCl in plasma.
Chen, SH; Ho, YH; Ko, HS; Wu, HL; Wu, SM, 2001
)
0.72
" When dosed with placebo, mean daytime intragastric acidity (0-10 hr after dose) was 37."( Decrease of intragastric acidity in healthy subjects dosed with ranitidine 75 mg, cimetidine 200 mg, or placebo.
Hamilton, MI; Pounder, RE; Sercombe, J, 2002
)
0.54
"Cimetidine co-administration produced an increase in sildenafil plasma levels; however, this increase is not sufficient to warrant dosage adjustment of either drug."( The effects of cimetidine and antacid on the pharmacokinetic profile of sildenafil citrate in healthy male volunteers.
Laboy, L; LeBel, M; Wilner, K, 2002
)
2.11
" pylori eradication (which was possible in 84% of the patients), at the end of the 1-year study period, on an intention to treat basis 62% of the patients could either stop or significantly reduce dosage of their H2RA."( Helicobacter pylori eradication in patients on long-term H2 receptor antagonists. Economic and symptomatic benefits. A large prospective study in primary care.
Giaffer, MH; Verma, S, 2002
)
0.31
" pylori eradication led to significant improvement in symptom scores and reduction in dosage of H2RA being consumed."( Helicobacter pylori eradication in patients on long-term H2 receptor antagonists. Economic and symptomatic benefits. A large prospective study in primary care.
Giaffer, MH; Verma, S, 2002
)
0.31
" Dosage of H2RAs should be lowered accordingly."( [What is important in treating elderly with H2 receptor antagonists].
Kurosawa, S, 2002
)
0.31
" The proposed method was used successfully for stability testing of the pure drugs in the presence of up to 90% of their degradates, in bulk powder and dosage forms."( Determination of cimetidine, famotidine, and ranitidine hydrochloride in the presence of their sulfoxide derivatives in pure and dosage forms by high-performance thin-layer chromatography and scanning densitometry.
Aziz, AM; Farrah, LA; Hegazy, MA; Kelani, KM,
)
0.47
" Weekly paclitaxel at a dose of 67 mg/m2/week was found to have a better safety profile and seemed to be as effective as the equivalently dosed schedule every 3 weeks."( Randomized trial of single agent paclitaxel given weekly versus every three weeks and with peroral versus intravenous steroid premedication to patients with ovarian cancer previously treated with platinum.
Andersson, H; Boman, K; Parö, G; Puistola, U; Ridderheim, M; Rosenberg, P; Sorbe, B, 2002
)
0.31
" When HSR was observed administration of paclitaxel was temporally stopped and before the re-challenge additional intravenous dosage of hydrocortisone (200-500 mg) and diphenhydramine (25 mg) was given."( [Paclitaxel hypersensitivity reactions in patients with advanced ovarian carcinoma].
Emerich, J; Kobierski, J; Majdak, E; Mielcarek, P, 2002
)
0.31
"Urapidil at a dosage of 25 mg intravenously reduced WHVP from 33."( [Effects of urapidil and cimetidine on wedged hepatic venous pressure and systemic hemodynamics in cirrhotic patients with portal hypertension].
Du, R; Feng, H; Leng, X; Li, S; Zhong, C; Zhu, J, 2000
)
0.61
" We showed by theoretical simulations based on the CTC model of dose-response and binding experiments that tiotidine biases the system to a G-protein-coupled form of the receptor that is unable to evoke a response."( Tiotidine, a histamine H2 receptor inverse agonist that binds with high affinity to an inactive G-protein-coupled form of the receptor. Experimental support for the cubic ternary complex model.
Baldi, A; Davio, C; Fernandez, N; Legnazzi, BL; Monczor, F; Riveiro, ME; Shayo, C, 2003
)
0.32
" Subjects (n = 12; 18-60 years) received granisetron (40 microg kg(-1)) infused over 3 min, six days before and on the eighth day of dosing with cimetidine (200 mg, four times a day)."( The effect of repeat dosing with cimetidine on the pharmacokinetics of intravenous granisetron in healthy volunteers.
Youlten, L, 2004
)
0.81
" These observations suggested that the metabolism of diltiazem to deacetyldiltiazem was reduced by cimetidine treatment and that the dosage of diltiazem should be adjusted when the drug is co-administered chronically with cimetidine in a clinical setting."( The influence of cimetidine on the pharmacokinetics of diltiazem and its main metabolite in rabbits.
Burm, JP; Choi, JS, 2004
)
0.88
" The cats were dosed for 10 days followed by at least a 2-week washout period between trials."( Multiple dose pharmacokinetics and acute safety of piroxicam and cimetidine in the cat.
Chun, R; Corse, M; Garrett, L; Heeb, HL; Hunter, RP; Koch, DE; Moore, L; Pellerin, MA; Radlinsky, M, 2005
)
0.57
") dosing in rats, six of eight drugs produced dose- and time-related antinociception on both the tail flick and hot plate tests over a nearly eight-fold range of potencies."( Antinociceptive, brain-penetrating derivatives related to improgan, a non-opioid analgesic.
Hough, LB; Lu, Q; Montero, MJ; Nalwalk, JW; Shan, Z; Svokos, K; Wentland, MP, 2005
)
0.33
" However, we report that E-selectin has risen after the cimetidine dosage was cancelled in the cimetidine administrated group."( [An interesting change of E-selectin in cimetidine administration during anticancer drug use].
Imaeda, Y; Kawase, J; Kobayashi, K; Matsumoto, S; Umemoto, S, 2005
)
0.84
"Literature data relevant to the decision to allow a waiver of in vivo bioequivalence (BE) testing for the approval of immediate release (IR) solid oral dosage forms containing cimetidine are reviewed."( Biowaiver monographs for immediate release solid oral dosage forms: cimetidine.
Amidon, GL; Barends, DM; Dressman, JB; Jantratid, E; Junginger, HE; Midha, KK; Prakongpan, S, 2006
)
0.76
" To avoid postoperative symblepharon, ankyloblepharon, dry eye, and possible corneal neovascularization after extensive lesion excision, oral CIM at a dosage of 200 mg 4 times daily was administered for 4 months before surgery."( Oral cimetidine adjuvant therapy for recalcitrant, diffuse conjunctival papillomatosis.
Chang, SW; Huang, ZL, 2006
)
0.85
" The proposed method was successfully applied to the determination of the investigated drugs in pure and pharmaceutical dosage forms (recovery was 98."( Spectrophotometric determination of H(2)-receptor antagonists via their oxidation with cerium(IV).
Darwish, IA; Hassan, AI; Hussein, SA; Mahmoud, AM, 2008
)
0.35
" Efficacy may have been limited by inadequate dosing in some of the trials."( Use of histamine2-antagonists for the treatment of verruca vulgaris.
Fit, KE; Williams, PC, 2007
)
0.34
" Repeated dosing was administered intraperitoneally every 4 to 6 hours for 48 hours."( Comparative treatment of alpha-amanitin poisoning with N-acetylcysteine, benzylpenicillin, cimetidine, thioctic acid, and silybin in a murine model.
Betten, DP; Clark, RF; Favata, M; Hernandez, M; Richardson, WH; Riffenburgh, RH; Tanen, DA; Tong, TC, 2007
)
0.56
" Because a) the mechanism of action of improgan remains unknown and b) this drug may indirectly activate cannabinoid CB(1) receptors, the effects of the CB(1) antagonist/inverse agonist rimonabant (SR141716A) and 3 congeners with varying CB(1) potencies were studied on improgan antinociception after intracerebroventricular (icv) dosing in rats."( Significance of cannabinoid CB1 receptors in improgan antinociception.
Abood, ME; Gehani, NC; Hough, LB; Martin, BR; Nalwalk, JW; Razdan, RK; Sun, X; Wentland, M, 2007
)
0.34
" It can be concluded that a combination of mannitol, erythritol, Glucidex 9, Kollidon CL, colloidal silicon dioxide and polyoxyethylene 20 sorbitan monooleate allowed the spray drying of highly dosed drug substances (acetaminophen, ibuprofen, cimetidine) in order to obtain 'ready-to-compress' powder mixtures on lab-scale and production-scale equipment."( Coprocessing via spray drying as a formulation platform to improve the compactability of various drugs.
Gonnissen, Y; Peeters, E; Remon, JP; Verhoeven, E; Vervaet, C, 2008
)
0.53
"The regular dosage of cimetidine showed an inhibitory effect on the motility of SO, while famotidine had no obvious effects otherwise."( Choledochoscope manometry about different drugs on the Sphincter of Oddi.
Chen, JZ; Kong, J; Li, ZS; Shi, G; Wang, W; Wu, SD; Zhang, XB, 2008
)
0.66
"Three simple, accurate, and sensitive colorimetric methods for the determination of cimetidine (Cim) in pure form, in dosage forms, and in the presence of its oxidative degradates were developed."( Colorimetric assay of cimetidine in the presence of its oxidative degradates.
Amin, AS; Dessouki, HA; Gouda, EA; Shama, SA,
)
0.67
"The Biopharmaceutical Classification System (BCS) guidance issued by the FDA allows waivers for in vivo bioavailability and bioequivalence studies for immediate-release (IR) solid oral dosage forms only for BCS class I drugs."( The biowaiver extension for BCS class III drugs: the effect of dissolution rate on the bioequivalence of BCS class III immediate-release drugs predicted by computer simulation.
Amidon, GL; Tsume, Y, 2010
)
0.36
" We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts."( FDA-approved drug labeling for the study of drug-induced liver injury.
Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011
)
0.37
" The proposed method can be used for the determination of the three H(2) antagonists in raw materials, dosage forms and biological fluids."( Determination of ranitidine, nizatidine, and cimetidine by a sensitive fluorescent probe.
Chang, YX; Du, LM; Guo, M; Li, CF; Qiu, YQ, 2011
)
0.63
" Successful treatment required aggressive surgical debridement, three times daily voriconazole dosing and cimetidine CYP2C19 inhibition."( Disseminated Scedosporium prolificans infection in an 'extensive metaboliser': navigating the minefield of drug interactions and pharmacogenomics.
Paratz, E; Slavin, MA; Teh, BW; Thursky, KA; Todaro, M; Trubiano, JA; Wolf, M, 2014
)
0.62
" The aim of this study was to assess whether appropriate dosage adjustments were made in hospitalized patients with renal impairment."( Drug dosage adjustment in hospitalized patients with renal impairment at Tikur Anbessa specialized hospital, Addis Ababa, Ethiopia.
Getachew, H; Shibeshi, W; Tadesse, Y, 2015
)
0.42
" Data regarding serum creatinine level, age, sex and prescribed drugs and their dosage was collected from the patients' medical records."( Drug dosage adjustment in hospitalized patients with renal impairment at Tikur Anbessa specialized hospital, Addis Ababa, Ethiopia.
Getachew, H; Shibeshi, W; Tadesse, Y, 2015
)
0.42
"The findings indicate that dosing errors were common among hospitalized patients with renal impairment."( Drug dosage adjustment in hospitalized patients with renal impairment at Tikur Anbessa specialized hospital, Addis Ababa, Ethiopia.
Getachew, H; Shibeshi, W; Tadesse, Y, 2015
)
0.42
" To conclude, tramadol and M1 concentrations were low and variable in dogs after oral dosing of tramadol, even in combination with cimetidine or ketoconazole, but effective concentrations in dogs have not been defined."( The effects of ketoconazole and cimetidine on the pharmacokinetics of oral tramadol in greyhound dogs.
Black, J; KuKanich, B; KuKanich, K, 2017
)
0.94
" These PBPK models are useful to predict the PK profiles of those five drugs in the milk for different dosing regimens."( Physiologically based pharmacokinetic model to predict drug concentrations of breast cancer resistance protein substrates in milk.
Fang, Y; Li, Y; Zhang, T; Zou, P, 2022
)
0.72
" Administration of mirogabalin on a long-term basis is a flexible dosage regimen for patients with PHN."( The Clinical Application and Progress of Mirogabalin on Neuropathic Pain as a Novel Selective Gabapentinoids.
Duan, Y; Li, D; Lu, J; Tang, H, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (5)

RoleDescription
H2-receptor antagonistH2-receptor antagonists are the drugs that selectively bind to but do not activate histamine H2 receptors, thereby blocking the actions of endogenous histamine.
P450 inhibitorAn enzyme inhibitor that interferes with the activity of cytochrome P450 involved in catalysis of organic substances.
anti-ulcer drugOne of various classes of drugs with different action mechanisms used to treat or ameliorate peptic ulcer or irritation of the gastrointestinal tract.
analgesicAn agent capable of relieving pain without the loss of consciousness or without producing anaesthesia. In addition, analgesic is a role played by a compound which is exhibited by a capability to cause a reduction of pain symptoms.
adjuvantAny pharmacological or immunological agent that modifies the effect of other agents such as drugs or vaccines while having few if any direct effects when given by itself.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (4)

ClassDescription
guanidinesAny organonitrogen compound containing a carbamimidamido (guanidino) group. Guanidines have the general structure (R(1)R(2)N)(R(3)R(4)N)C=N-R(5) and are related structurally to amidines and ureas.
imidazolesA five-membered organic heterocycle containing two nitrogen atoms at positions 1 and 3, or any of its derivatives; compounds containing an imidazole skeleton.
aliphatic sulfide
nitrileA compound having the structure RC#N; thus a C-substituted derivative of hydrocyanic acid, HC#N. In systematic nomenclature, the suffix nitrile denotes the triply bound #N atom, not the carbon atom attached to it.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Pathways (3)

PathwayProteinsCompounds
Cimetidine Action Pathway1012
Cimetidine Metabolism Pathway11
Drug induction of bile acid pathway025

Protein Targets (78)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency39.81070.003245.467312,589.2998AID1705
interleukin 8Homo sapiens (human)Potency66.82420.047349.480674.9780AID651758
phosphopantetheinyl transferaseBacillus subtilisPotency46.59090.141337.9142100.0000AID1490
AR proteinHomo sapiens (human)Potency27.09290.000221.22318,912.5098AID1259243; AID1259247
thyroid stimulating hormone receptorHomo sapiens (human)Potency1.58490.001318.074339.8107AID926; AID938
progesterone receptorHomo sapiens (human)Potency0.00070.000417.946075.1148AID1346784
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency11.88320.001530.607315,848.9004AID1224849
estrogen nuclear receptor alphaHomo sapiens (human)Potency10.67170.000229.305416,493.5996AID743075
GVesicular stomatitis virusPotency13.80290.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency15.48710.00108.379861.1304AID1645840
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency24.31620.023723.228263.5986AID743223
arylsulfatase AHomo sapiens (human)Potency6.30961.069113.955137.9330AID720538
alpha-galactosidaseHomo sapiens (human)Potency22.38724.466818.391635.4813AID2107
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency12.78280.035520.977089.1251AID504332
cytochrome P450 2C19 precursorHomo sapiens (human)Potency31.62280.00255.840031.6228AID899
gemininHomo sapiens (human)Potency0.09200.004611.374133.4983AID624296
DNA polymerase kappa isoform 1Homo sapiens (human)Potency28.18380.031622.3146100.0000AID588579
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency2.27940.005612.367736.1254AID624032
survival motor neuron protein isoform dHomo sapiens (human)Potency8.96720.125912.234435.4813AID1458
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency20.48390.031610.279239.8107AID884; AID885
M-phase phosphoprotein 8Homo sapiens (human)Potency33.58750.177824.735279.4328AID488949
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency0.08910.00106.000935.4813AID943
lamin isoform A-delta10Homo sapiens (human)Potency5.01190.891312.067628.1838AID1487
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency20.48391.000012.224831.6228AID885
Interferon betaHomo sapiens (human)Potency13.80290.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency13.80290.01238.964839.8107AID1645842
Cellular tumor antigen p53Homo sapiens (human)Potency60.57150.002319.595674.0614AID651631
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency20.48391.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency20.48391.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency20.48391.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency20.48391.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency20.48391.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency20.48391.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency20.48391.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency20.48391.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency20.48391.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency20.48391.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency20.48391.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency20.48391.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency20.48391.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency20.48391.000012.224831.6228AID885
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency13.80290.01238.964839.8107AID1645842
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency20.48391.000012.224831.6228AID885
cytochrome P450 2C9, partialHomo sapiens (human)Potency13.80290.01238.964839.8107AID1645842
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency0.75690.060110.745337.9330AID485368
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Solute carrier family 22 member 1Mus musculus (house mouse)IC50 (µMol)0.59000.28001.32753.9000AID678794
Solute carrier family 22 member 2Homo sapiens (human)IC50 (µMol)23.00000.40003.10009.7000AID692192
Solute carrier family 22 member 2Homo sapiens (human)Ki57.00000.10001.52203.4000AID680368
Solute carrier family 22 member 1 Homo sapiens (human)IC50 (µMol)124.50000.21005.553710.0000AID1442002; AID692194
Solute carrier family 22 member 1 Homo sapiens (human)Ki166.00000.55004.26507.4600AID681146
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Solute carrier family 22 member 6Rattus norvegicus (Norway rat)IC50 (µMol)2,000.00000.50000.50000.5000AID680339
Solute carrier family 22 member 6Rattus norvegicus (Norway rat)Ki1,000.00001.60005.744010.0000AID680342
Solute carrier family 22 member 2Mus musculus (house mouse)IC50 (µMol)8.00002.80004.76678.0000AID678785
cGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)IC50 (µMol)100.00000.00001.18439.6140AID167650
Bile salt export pumpHomo sapiens (human)IC50 (µMol)422.66670.11007.190310.0000AID1443980; AID1449628; AID1473738
ATP-dependent translocase ABCB1Mus musculus (house mouse)IC50 (µMol)50.00000.06404.012610.0000AID150754; AID681128
ATP-dependent translocase ABCB1Homo sapiens (human)IC50 (µMol)50.00000.00022.318510.0000AID150752; AID150755; AID681122
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)507.50000.00011.753610.0000AID428564; AID54923
Cytochrome P450 2D6Homo sapiens (human)Ki77.00000.00011.19868.0000AID589096
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)50.00000.00002.800510.0000AID1210069
Potassium-transporting ATPase alpha chain 1Homo sapiens (human)IC50 (µMol)50.41000.04001.09603.8000AID167650; AID167652
ATP-dependent translocase ABCB1Mus musculus (house mouse)IC50 (µMol)50.00000.20004.713010.0000AID150753; AID681119
Histamine H2 receptorHomo sapiens (human)IC50 (µMol)1.17420.02202.298710.0000AID1285633; AID1336328; AID1433974; AID340249; AID346426; AID625270; AID751879; AID752241
Histamine H2 receptorHomo sapiens (human)Ki1.06200.00062.197310.0000AID1063783; AID1433974; AID346426; AID625270; AID751879
Histamine H2 receptorCavia porcellus (domestic guinea pig)IC50 (µMol)1.02000.00402.15557.2000AID566261
Histamine H2 receptorCavia porcellus (domestic guinea pig)Ki0.30200.00071.02045.1250AID88326
Potassium-transporting ATPase subunit betaHomo sapiens (human)IC50 (µMol)50.41000.04001.09603.8000AID167650; AID167652
Cytochrome P450 2J2Homo sapiens (human)IC50 (µMol)50.00000.01202.53129.4700AID1210069
Aldehyde oxidaseHomo sapiens (human)Ki155.00000.00090.46072.3000AID547838
Solute carrier family 22 member 6Homo sapiens (human)IC50 (µMol)492.00000.27004.53069.9000AID682026
Solute carrier family 22 member 1Rattus norvegicus (Norway rat)IC50 (µMol)329.00000.18003.68578.8000AID679826
Solute carrier family 22 member 1Rattus norvegicus (Norway rat)Ki5.70000.13002.37856.9000AID681574
Multidrug and toxin extrusion protein 2Homo sapiens (human)IC50 (µMol)39.00000.16003.95718.6000AID692196
Solute carrier family 22 member 8Homo sapiens (human)IC50 (µMol)92.40004.93007.39009.9200AID678815
Solute carrier family 22 member 8Homo sapiens (human)Ki53.00000.04004.22979.0000AID679677
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
Multidrug and toxin extrusion protein 1Homo sapiens (human)IC50 (µMol)3.03330.01002.765610.0000AID1848080; AID692195; AID721754
Histamine H4 receptorHomo sapiens (human)Ki10.00000.00060.478710.0000AID1798265
Solute carrier family 22 member 11Homo sapiens (human)IC50 (µMol)2,000.00002.03004.66507.3000AID678973
Solute carrier family 22 member 2Rattus norvegicus (Norway rat)IC50 (µMol)373.00001.00004.446710.0000AID678970
Solute carrier family 22 member 2Rattus norvegicus (Norway rat)Ki103.70000.39002.32959.4000AID679294; AID681590
Solute carrier family 22 member 8Rattus norvegicus (Norway rat)IC50 (µMol)166.00006.03006.03006.0300AID678805
Solute carrier family 22 member 8Rattus norvegicus (Norway rat)Ki46.80003.09005.54009.1000AID679633
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Histamine H1 receptorCavia porcellus (domestic guinea pig)Kd0.95500.00080.12280.9550AID88140
Histamine H2 receptorCavia porcellus (domestic guinea pig)Kd0.41900.01170.15720.9550AID88140; AID88141; AID88142; AID88151
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Solute carrier family 22 member 2Homo sapiens (human)Km60.00000.02891.04072.6000AID771318
Solute carrier family 22 member 8Homo sapiens (human)Km103.20000.34501.32173.1000AID679305; AID681141
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (329)

Processvia Protein(s)Taxonomy
activation of cysteine-type endopeptidase activity involved in apoptotic processSolute carrier family 22 member 2Homo sapiens (human)
positive regulation of gene expressionSolute carrier family 22 member 2Homo sapiens (human)
organic cation transportSolute carrier family 22 member 2Homo sapiens (human)
monoatomic cation transportSolute carrier family 22 member 2Homo sapiens (human)
neurotransmitter transportSolute carrier family 22 member 2Homo sapiens (human)
serotonin transportSolute carrier family 22 member 2Homo sapiens (human)
body fluid secretionSolute carrier family 22 member 2Homo sapiens (human)
organic cation transportSolute carrier family 22 member 2Homo sapiens (human)
quaternary ammonium group transportSolute carrier family 22 member 2Homo sapiens (human)
prostaglandin transportSolute carrier family 22 member 2Homo sapiens (human)
amine transportSolute carrier family 22 member 2Homo sapiens (human)
putrescine transportSolute carrier family 22 member 2Homo sapiens (human)
spermidine transportSolute carrier family 22 member 2Homo sapiens (human)
acetylcholine transportSolute carrier family 22 member 2Homo sapiens (human)
choline transportSolute carrier family 22 member 2Homo sapiens (human)
dopamine transportSolute carrier family 22 member 2Homo sapiens (human)
norepinephrine transportSolute carrier family 22 member 2Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 2Homo sapiens (human)
epinephrine transportSolute carrier family 22 member 2Homo sapiens (human)
histamine transportSolute carrier family 22 member 2Homo sapiens (human)
serotonin uptakeSolute carrier family 22 member 2Homo sapiens (human)
histamine uptakeSolute carrier family 22 member 2Homo sapiens (human)
norepinephrine uptakeSolute carrier family 22 member 2Homo sapiens (human)
thiamine transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
purine-containing compound transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
amino acid import across plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
dopamine uptakeSolute carrier family 22 member 2Homo sapiens (human)
L-arginine import across plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
export across plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
transport across blood-brain barrierSolute carrier family 22 member 2Homo sapiens (human)
L-alpha-amino acid transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
spermidine transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
L-arginine transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
cellular detoxificationSolute carrier family 22 member 2Homo sapiens (human)
xenobiotic transport across blood-brain barrierSolute carrier family 22 member 2Homo sapiens (human)
xenobiotic metabolic processSolute carrier family 22 member 1 Homo sapiens (human)
neurotransmitter transportSolute carrier family 22 member 1 Homo sapiens (human)
serotonin transportSolute carrier family 22 member 1 Homo sapiens (human)
establishment or maintenance of transmembrane electrochemical gradientSolute carrier family 22 member 1 Homo sapiens (human)
organic cation transportSolute carrier family 22 member 1 Homo sapiens (human)
quaternary ammonium group transportSolute carrier family 22 member 1 Homo sapiens (human)
prostaglandin transportSolute carrier family 22 member 1 Homo sapiens (human)
monoamine transportSolute carrier family 22 member 1 Homo sapiens (human)
putrescine transportSolute carrier family 22 member 1 Homo sapiens (human)
spermidine transportSolute carrier family 22 member 1 Homo sapiens (human)
acetylcholine transportSolute carrier family 22 member 1 Homo sapiens (human)
dopamine transportSolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine transportSolute carrier family 22 member 1 Homo sapiens (human)
thiamine transportSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 1 Homo sapiens (human)
epinephrine transportSolute carrier family 22 member 1 Homo sapiens (human)
serotonin uptakeSolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine uptakeSolute carrier family 22 member 1 Homo sapiens (human)
thiamine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
metanephric proximal tubule developmentSolute carrier family 22 member 1 Homo sapiens (human)
purine-containing compound transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
dopamine uptakeSolute carrier family 22 member 1 Homo sapiens (human)
monoatomic cation transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
transport across blood-brain barrierSolute carrier family 22 member 1 Homo sapiens (human)
(R)-carnitine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
acyl carnitine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
spermidine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
cellular detoxificationSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transport across blood-brain barrierSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
positive regulation of cardiac muscle hypertrophycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
regulation of nitric oxide mediated signal transductioncGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
T cell proliferationcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
negative regulation of T cell proliferationcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cGMP catabolic processcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
oocyte developmentcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
negative regulation of cardiac muscle contractioncGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
relaxation of cardiac musclecGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
positive regulation of oocyte developmentcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cAMP-mediated signalingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
G2/M transition of mitotic cell cycleATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic metabolic processATP-dependent translocase ABCB1Homo sapiens (human)
response to xenobiotic stimulusATP-dependent translocase ABCB1Homo sapiens (human)
phospholipid translocationATP-dependent translocase ABCB1Homo sapiens (human)
terpenoid transportATP-dependent translocase ABCB1Homo sapiens (human)
regulation of response to osmotic stressATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
transepithelial transportATP-dependent translocase ABCB1Homo sapiens (human)
stem cell proliferationATP-dependent translocase ABCB1Homo sapiens (human)
ceramide translocationATP-dependent translocase ABCB1Homo sapiens (human)
export across plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
positive regulation of anion channel activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
regulation of chloride transportATP-dependent translocase ABCB1Homo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2D6Homo sapiens (human)
steroid metabolic processCytochrome P450 2D6Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2D6Homo sapiens (human)
estrogen metabolic processCytochrome P450 2D6Homo sapiens (human)
coumarin metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid catabolic processCytochrome P450 2D6Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2D6Homo sapiens (human)
isoquinoline alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2D6Homo sapiens (human)
retinol metabolic processCytochrome P450 2D6Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of bindingCytochrome P450 2D6Homo sapiens (human)
oxidative demethylationCytochrome P450 2D6Homo sapiens (human)
negative regulation of cellular organofluorine metabolic processCytochrome P450 2D6Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
response to xenobiotic stimulusPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
regulation of proton transportPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
establishment or maintenance of transmembrane electrochemical gradientPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
monoatomic ion transmembrane transportPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
pH reductionPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
potassium ion transmembrane transportPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
intracellular sodium ion homeostasisPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
sodium ion export across plasma membranePotassium-transporting ATPase alpha chain 1Homo sapiens (human)
intracellular potassium ion homeostasisPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
potassium ion import across plasma membranePotassium-transporting ATPase alpha chain 1Homo sapiens (human)
proton transmembrane transportPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
gastric acid secretionHistamine H2 receptorHomo sapiens (human)
immune responseHistamine H2 receptorHomo sapiens (human)
positive regulation of vasoconstrictionHistamine H2 receptorHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayHistamine H2 receptorHomo sapiens (human)
chemical synaptic transmissionHistamine H2 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerHistamine H2 receptorHomo sapiens (human)
cell adhesionPotassium-transporting ATPase subunit betaHomo sapiens (human)
response to organonitrogen compoundPotassium-transporting ATPase subunit betaHomo sapiens (human)
response to lipopolysaccharidePotassium-transporting ATPase subunit betaHomo sapiens (human)
pH reductionPotassium-transporting ATPase subunit betaHomo sapiens (human)
potassium ion transmembrane transportPotassium-transporting ATPase subunit betaHomo sapiens (human)
proton transmembrane transportPotassium-transporting ATPase subunit betaHomo sapiens (human)
potassium ion import across plasma membranePotassium-transporting ATPase subunit betaHomo sapiens (human)
intracellular potassium ion homeostasisPotassium-transporting ATPase subunit betaHomo sapiens (human)
sodium ion export across plasma membranePotassium-transporting ATPase subunit betaHomo sapiens (human)
intracellular sodium ion homeostasisPotassium-transporting ATPase subunit betaHomo sapiens (human)
fatty acid metabolic processCytochrome P450 2J2Homo sapiens (human)
icosanoid metabolic processCytochrome P450 2J2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2J2Homo sapiens (human)
regulation of heart contractionCytochrome P450 2J2Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2J2Homo sapiens (human)
linoleic acid metabolic processCytochrome P450 2J2Homo sapiens (human)
organic acid metabolic processCytochrome P450 2J2Homo sapiens (human)
lipid metabolic processAldehyde oxidaseHomo sapiens (human)
xenobiotic metabolic processAldehyde oxidaseHomo sapiens (human)
monoatomic anion transportSolute carrier family 22 member 6Homo sapiens (human)
response to organic cyclic compoundSolute carrier family 22 member 6Homo sapiens (human)
inorganic anion transportSolute carrier family 22 member 6Homo sapiens (human)
organic anion transportSolute carrier family 22 member 6Homo sapiens (human)
prostaglandin transportSolute carrier family 22 member 6Homo sapiens (human)
alpha-ketoglutarate transportSolute carrier family 22 member 6Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 6Homo sapiens (human)
sodium-independent organic anion transportSolute carrier family 22 member 6Homo sapiens (human)
transmembrane transportSolute carrier family 22 member 6Homo sapiens (human)
metanephric proximal tubule developmentSolute carrier family 22 member 6Homo sapiens (human)
renal tubular secretionSolute carrier family 22 member 6Homo sapiens (human)
organic cation transportMultidrug and toxin extrusion protein 2Homo sapiens (human)
transmembrane transportMultidrug and toxin extrusion protein 2Homo sapiens (human)
proton transmembrane transportMultidrug and toxin extrusion protein 2Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneMultidrug and toxin extrusion protein 2Homo sapiens (human)
monoatomic ion transportSolute carrier family 22 member 8Homo sapiens (human)
response to toxic substanceSolute carrier family 22 member 8Homo sapiens (human)
inorganic anion transportSolute carrier family 22 member 8Homo sapiens (human)
prostaglandin transportSolute carrier family 22 member 8Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 8Homo sapiens (human)
transmembrane transportSolute carrier family 22 member 8Homo sapiens (human)
transport across blood-brain barrierSolute carrier family 22 member 8Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
organic cation transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
putrescine transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
xenobiotic transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
thiamine transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
amino acid import across plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-arginine import across plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-alpha-amino acid transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
proton transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-arginine transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
inflammatory responseHistamine H4 receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationHistamine H4 receptorHomo sapiens (human)
biological_processHistamine H4 receptorHomo sapiens (human)
regulation of MAPK cascadeHistamine H4 receptorHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayHistamine H4 receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayHistamine H4 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerHistamine H4 receptorHomo sapiens (human)
chemical synaptic transmissionHistamine H4 receptorHomo sapiens (human)
monoatomic ion transportSolute carrier family 22 member 11Homo sapiens (human)
inorganic anion transportSolute carrier family 22 member 11Homo sapiens (human)
organic anion transportSolute carrier family 22 member 11Homo sapiens (human)
prostaglandin transportSolute carrier family 22 member 11Homo sapiens (human)
urate metabolic processSolute carrier family 22 member 11Homo sapiens (human)
transmembrane transportSolute carrier family 22 member 11Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (156)

Processvia Protein(s)Taxonomy
amine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
acetylcholine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
neurotransmitter transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
monoamine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
organic cation transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
L-amino acid transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
pyrimidine nucleoside transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
choline transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
thiamine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
putrescine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
efflux transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
spermidine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
quaternary ammonium group transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
toxin transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
xenobiotic transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
L-arginine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
acetylcholine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
neurotransmitter transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
dopamine:sodium symporter activitySolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine:sodium symporter activitySolute carrier family 22 member 1 Homo sapiens (human)
protein bindingSolute carrier family 22 member 1 Homo sapiens (human)
monoamine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
secondary active organic cation transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
organic cation transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
pyrimidine nucleoside transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
thiamine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
putrescine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
spermidine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
quaternary ammonium group transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
toxin transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
identical protein bindingSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
(R)-carnitine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
3',5'-cyclic-nucleotide phosphodiesterase activitycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
protein bindingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cGMP bindingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
metal ion bindingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATP bindingATP-dependent translocase ABCB1Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
efflux transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ATP hydrolysis activityATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ubiquitin protein ligase bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylcholine floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylethanolamine flippase activityATP-dependent translocase ABCB1Homo sapiens (human)
ceramide floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
monooxygenase activityCytochrome P450 2D6Homo sapiens (human)
iron ion bindingCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activityCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2D6Homo sapiens (human)
heme bindingCytochrome P450 2D6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C9 Homo sapiens (human)
magnesium ion bindingPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
ATP bindingPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
P-type potassium:proton transporter activityPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
ATP hydrolysis activityPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
potassium ion bindingPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
P-type sodium:potassium-exchanging transporter activityPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-dependent translocase ABCB1Mus musculus (house mouse)
histamine receptor activityHistamine H2 receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityHistamine H2 receptorHomo sapiens (human)
neurotransmitter receptor activityHistamine H2 receptorHomo sapiens (human)
protein bindingPotassium-transporting ATPase subunit betaHomo sapiens (human)
P-type potassium:proton transporter activityPotassium-transporting ATPase subunit betaHomo sapiens (human)
heterocyclic compound bindingPotassium-transporting ATPase subunit betaHomo sapiens (human)
ATPase activator activityPotassium-transporting ATPase subunit betaHomo sapiens (human)
monooxygenase activityCytochrome P450 2J2Homo sapiens (human)
iron ion bindingCytochrome P450 2J2Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
isomerase activityCytochrome P450 2J2Homo sapiens (human)
linoleic acid epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
hydroperoxy icosatetraenoate isomerase activityCytochrome P450 2J2Homo sapiens (human)
arachidonic acid 5,6-epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
heme bindingCytochrome P450 2J2Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2J2Homo sapiens (human)
aldehyde oxidase activityAldehyde oxidaseHomo sapiens (human)
iron ion bindingAldehyde oxidaseHomo sapiens (human)
identical protein bindingAldehyde oxidaseHomo sapiens (human)
protein homodimerization activityAldehyde oxidaseHomo sapiens (human)
molybdopterin cofactor bindingAldehyde oxidaseHomo sapiens (human)
flavin adenine dinucleotide bindingAldehyde oxidaseHomo sapiens (human)
NAD bindingAldehyde oxidaseHomo sapiens (human)
2 iron, 2 sulfur cluster bindingAldehyde oxidaseHomo sapiens (human)
FAD bindingAldehyde oxidaseHomo sapiens (human)
solute:inorganic anion antiporter activitySolute carrier family 22 member 6Homo sapiens (human)
protein bindingSolute carrier family 22 member 6Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 6Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier family 22 member 6Homo sapiens (human)
alpha-ketoglutarate transmembrane transporter activitySolute carrier family 22 member 6Homo sapiens (human)
antiporter activitySolute carrier family 22 member 6Homo sapiens (human)
transmembrane transporter activitySolute carrier family 22 member 6Homo sapiens (human)
chloride ion bindingSolute carrier family 22 member 6Homo sapiens (human)
identical protein bindingSolute carrier family 22 member 6Homo sapiens (human)
xenobiotic transmembrane transporter activitySolute carrier family 22 member 6Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activitySolute carrier family 22 member 6Homo sapiens (human)
organic cation transmembrane transporter activityMultidrug and toxin extrusion protein 2Homo sapiens (human)
antiporter activityMultidrug and toxin extrusion protein 2Homo sapiens (human)
transmembrane transporter activityMultidrug and toxin extrusion protein 2Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug and toxin extrusion protein 2Homo sapiens (human)
polyspecific organic cation:proton antiporter activityMultidrug and toxin extrusion protein 2Homo sapiens (human)
solute:inorganic anion antiporter activitySolute carrier family 22 member 8Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 8Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier family 22 member 8Homo sapiens (human)
xenobiotic transmembrane transporter activitySolute carrier family 22 member 8Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
protein bindingMultidrug and toxin extrusion protein 1Homo sapiens (human)
organic cation transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-amino acid transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
thiamine transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
antiporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
putrescine transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-arginine transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
polyspecific organic cation:proton antiporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
histamine receptor activityHistamine H4 receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityHistamine H4 receptorHomo sapiens (human)
G protein-coupled acetylcholine receptor activityHistamine H4 receptorHomo sapiens (human)
solute:inorganic anion antiporter activitySolute carrier family 22 member 11Homo sapiens (human)
protein bindingSolute carrier family 22 member 11Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 11Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier family 22 member 11Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activitySolute carrier family 22 member 11Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (55)

Processvia Protein(s)Taxonomy
plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
basal plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
membraneSolute carrier family 22 member 2Homo sapiens (human)
basolateral plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
apical plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
extracellular exosomeSolute carrier family 22 member 2Homo sapiens (human)
presynapseSolute carrier family 22 member 2Homo sapiens (human)
plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
basal plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
membraneSolute carrier family 22 member 1 Homo sapiens (human)
basolateral plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
apical plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
lateral plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
presynapseSolute carrier family 22 member 1 Homo sapiens (human)
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
cellular_componentcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cytosolcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
cytoplasmATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
cell surfaceATP-dependent translocase ABCB1Homo sapiens (human)
membraneATP-dependent translocase ABCB1Homo sapiens (human)
apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
extracellular exosomeATP-dependent translocase ABCB1Homo sapiens (human)
external side of apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
mitochondrionCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulumCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2D6Homo sapiens (human)
cytoplasmCytochrome P450 2D6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
extracellular spacePotassium-transporting ATPase alpha chain 1Homo sapiens (human)
plasma membranePotassium-transporting ATPase alpha chain 1Homo sapiens (human)
potassium:proton exchanging ATPase complexPotassium-transporting ATPase alpha chain 1Homo sapiens (human)
apical plasma membranePotassium-transporting ATPase alpha chain 1Homo sapiens (human)
plasma membranePotassium-transporting ATPase alpha chain 1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Mus musculus (house mouse)
plasma membraneHistamine H2 receptorHomo sapiens (human)
synapseHistamine H2 receptorHomo sapiens (human)
plasma membraneHistamine H2 receptorHomo sapiens (human)
dendriteHistamine H2 receptorHomo sapiens (human)
plasma membranePotassium-transporting ATPase subunit betaHomo sapiens (human)
potassium:proton exchanging ATPase complexPotassium-transporting ATPase subunit betaHomo sapiens (human)
apical plasma membranePotassium-transporting ATPase subunit betaHomo sapiens (human)
sodium:potassium-exchanging ATPase complexPotassium-transporting ATPase subunit betaHomo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2J2Homo sapiens (human)
extracellular exosomeCytochrome P450 2J2Homo sapiens (human)
cytoplasmCytochrome P450 2J2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2J2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
cytosolAldehyde oxidaseHomo sapiens (human)
extracellular exosomeAldehyde oxidaseHomo sapiens (human)
plasma membraneSolute carrier family 22 member 6Homo sapiens (human)
caveolaSolute carrier family 22 member 6Homo sapiens (human)
basal plasma membraneSolute carrier family 22 member 6Homo sapiens (human)
basolateral plasma membraneSolute carrier family 22 member 6Homo sapiens (human)
extracellular exosomeSolute carrier family 22 member 6Homo sapiens (human)
protein-containing complexSolute carrier family 22 member 6Homo sapiens (human)
plasma membraneMultidrug and toxin extrusion protein 2Homo sapiens (human)
apical plasma membraneMultidrug and toxin extrusion protein 2Homo sapiens (human)
membraneMultidrug and toxin extrusion protein 2Homo sapiens (human)
plasma membraneSolute carrier family 22 member 8Homo sapiens (human)
basolateral plasma membraneSolute carrier family 22 member 8Homo sapiens (human)
apical plasma membraneSolute carrier family 22 member 8Homo sapiens (human)
extracellular exosomeSolute carrier family 22 member 8Homo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
basolateral plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
apical plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
plasma membraneHistamine H4 receptorHomo sapiens (human)
plasma membraneHistamine H4 receptorHomo sapiens (human)
dendriteHistamine H4 receptorHomo sapiens (human)
synapseHistamine H4 receptorHomo sapiens (human)
plasma membraneSolute carrier family 22 member 11Homo sapiens (human)
external side of plasma membraneSolute carrier family 22 member 11Homo sapiens (human)
basal plasma membraneSolute carrier family 22 member 11Homo sapiens (human)
apical plasma membraneSolute carrier family 22 member 11Homo sapiens (human)
extracellular exosomeSolute carrier family 22 member 11Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (556)

Assay IDTitleYearJournalArticle
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID88027Ratio of potency (3*10e-5M) to that of agonist for histamine H2 receptor, in an assay for guinea pig atria chronotropic response1981Journal of medicinal chemistry, Sep, Volume: 24, Issue:9
Potential histamine H2-receptor blockers. 3- and 2-indole derivatives as immobile analogues of tautomeric forms of cimetidine.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID234825Slope value of the compound1982Journal of medicinal chemistry, Mar, Volume: 25, Issue:3
Inhibitors of gastric acid secretion: 3,4-diamino-1,2,5-thiadiazole 1-oxides and 1,1-dioxides as urea equivalents in a series of histamine H2-receptor antagonists.
AID78024Inhibition of histamine-stimulated chronotropic response in the isolated guinea pig right atrium at 1*10e-6 g/mL1998Bioorganic & medicinal chemistry letters, Jun-02, Volume: 8, Issue:11
Anti-Helicobacter pylori agents. 2. Structure activity relationships in a new series of 2-alkylguanidino-4-furylthiazoles.
AID1221960Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID681164TP_TRANSPORTER: ATP hydrolysis in membrane fraction from High Five (BTI-TN5B1-4) cells2001Pharmaceutical research, Dec, Volume: 18, Issue:12
Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein.
AID496821Antimicrobial activity against Leishmania2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID15267Log of (Cbrain/Cblood) in rats1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Development of a new physicochemical model for brain penetration and its application to the design of centrally acting H2 receptor histamine antagonists.
AID176289Antisecretory activity was evaluated in acute gastric fistula of rat after intravenous administration; ND means no data1987Journal of medicinal chemistry, May, Volume: 30, Issue:5
Antisecretory activity of human, dog, and rat metabolites of fenoctimine.
AID624622Apparent permeability (Papp) from apical to basolateral side determined in MDR1-MDCKII cells2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID178935Effective dose required for the inhibition of total acid secretion in pylorus-ligated rats1988Journal of medicinal chemistry, Sep, Volume: 31, Issue:9
Synthesis of (aryloxy)alkylamines. 1. Novel antisecretory agents with H+K+-ATPase inhibitory activity.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID150759P-gp activity was measured by a direct transport assay, using polarized LLC-mdr1a epithelial cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID680407TP_TRANSPORTER: inhibition of TEA uptake (TEA: 60 uM, Cimetidine: 1000 uM) in Xenopus laevis oocytes1999The Journal of pharmacology and experimental therapeutics, May, Volume: 289, Issue:2
Novel membrane transporter OCTN1 mediates multispecific, bidirectional, and pH-dependent transport of organic cations.
AID141955Percentage inhibition for muscarinic acetylcholine receptor at concentration 10e-6 M.1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Synthesis and antiulcer activity of 5,11-dihydro[1]benzoxepino[3,4-b]pyridines.
AID414579Apparent permeability from apical to basolateral side of human Caco-2 cells2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Novel peptidomimetics containing a vinyl ester moiety as highly potent and selective falcipain-2 inhibitors.
AID60732Maximum percent inhibition of acid output in penta gastrin-stimulated Heidenhain pouch dogs at a dose of 10 mg/kg, given intravenously (iv).1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Bioisosteric prototype design of biaryl imidazolyl and triazolyl competitive histamine H2-receptor antagonists.
AID679824TP_TRANSPORTER: uptake in OCT1-expressing HEK293 cells1999Molecular pharmacology, Jul, Volume: 56, Issue:1
Selective substrates for non-neuronal monoamine transporters.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID589096Mechanism based inhibition of human cytochrome P450 2D6 measured by dextromethorphan O-demethylation2005Current drug metabolism, Oct, Volume: 6, Issue:5
Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.
AID679206TP_TRANSPORTER: inhibition of TEA uptake (TEA: 500 uM, Cimetidine: 5000 uM) in OCT1A expressing Xenopus laevis oocytes1997The Journal of biological chemistry, Jun-27, Volume: 272, Issue:26
Cloning and functional characterization of a rat renal organic cation transporter isoform (rOCT1A).
AID183686Inhibition of histamine stimulated gastric acid secretion in lumen perfused anaesthetized rats after 1 mg/kg intravenous dose1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
Studies on antiulcer drugs. 7. 2-Guanidino-4-pyridylthiazoles as histamine H2-receptor antagonists with potent gastroprotective effects against nonsteroidal antiinflammatory drug-induced injury.
AID87702Antagonism of histamine stimulated rate of beating of guinea pig right atrium mediated by Histamine H2 receptor1987Journal of medicinal chemistry, Jul, Volume: 30, Issue:7
Zwitterionic analogues of cimetidine as H2 receptor antagonists.
AID87861Competitive antagonism of compound at histamine H2 receptor compared to 4-methylhistamine induced chronotropic response in guinea pig atria; + Potency ratio greater than 1.01981Journal of medicinal chemistry, Sep, Volume: 24, Issue:9
Potential histamine H2-receptor blockers. 3- and 2-indole derivatives as immobile analogues of tautomeric forms of cimetidine.
AID88013Evaluated in vitro for histamine H2 receptor antagonist activity by using histamine-stimulated chronotropic response of the guinea pig atrium1984Journal of medicinal chemistry, Mar, Volume: 27, Issue:3
(Imidazolylphenyl)formamidines. A structurally novel class of potent histamine H2 receptor antagonists.
AID177057Compound was evaluated for antiulcer activity in rats due to stress after oral administration1983Journal of medicinal chemistry, Aug, Volume: 26, Issue:8
Pyridazinones. 3. Synthesis, antisecretory, and antiulcer activities of 2-cyanoguanidine derivatives.
AID1221962Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID692186Therapeutic index, ratio of Cmax in human to IC50 for human OCT12011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2.
AID681005TP_TRANSPORTER: inhibition of Glutarate uptake (Glutarate: 5 uM, Cimetidine: 1000 uM) in Xenopus laevis oocytes2002Molecular pharmacology, Jul, Volume: 62, Issue:1
Isolation, characterization and differential gene expression of multispecific organic anion transporter 2 in mice.
AID699541Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID88141Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.41987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Studies on the active molecular species of the H2 receptor antagonists cimetidine and mifentidine.
AID1135363Solubility of the compound in water at 37 degC1977Journal of medicinal chemistry, Jul, Volume: 20, Issue:7
Cyanoguanidine-thiourea equivalence in the development of the histamine H2-receptor antagonist, cimetidine.
AID59669Effective dose for acid output in pentagastrin-stimulated Heidenhain pouch dog1985Journal of medicinal chemistry, Nov, Volume: 28, Issue:11
Pseudosymmetry and bioisosterism in biaryl pyridyl competitive histamine H2-receptor antagonists.
AID496824Antimicrobial activity against Toxoplasma gondii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496818Antimicrobial activity against Trypanosoma brucei brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID679305TP_TRANSPORTER: cell accumulation in hOAT3 expressing HEK cells2006The Journal of pharmacology and experimental therapeutics, Mar, Volume: 316, Issue:3
Is the monkey an appropriate animal model to examine drug-drug interactions involving renal clearance? Effect of probenecid on the renal elimination of H2 receptor antagonists.
AID496827Antimicrobial activity against Leishmania amazonensis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID682026TP_TRANSPORTER: inhibition of PHA uptake (PHA: 5uM) in hOAT1-expressing S2 cells2004Journal of pharmacological sciences, Feb, Volume: 94, Issue:2
Interactions of human- and rat-organic anion transporters with pravastatin and cimetidine.
AID183872In Vivo gastric Mucosal protective activity against gastric mucosal lesions induced by 0.6 N HCl in rats. (200 mg/kg, po)1992Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13
Synthesis and antiulcer activity of N-substituted N'-[3-[3-(piperidinomethyl)phenoxy]propyl]ureas: histamine H2-receptor antagonists with a potent mucosal protective activity.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID624647Inhibition of AZT glucuronidation by human UGT enzymes from liver microsomes2005Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
UDP-glucuronosyltransferases and clinical drug-drug interactions.
AID681706TP_TRANSPORTER: inhibition of TEA uptake (TEA: 20 uM, Cimetidine: 2500 uM) in OCTN2-expressing HRPE cells1999The Journal of pharmacology and experimental therapeutics, Sep, Volume: 290, Issue:3
Functional characteristics and tissue distribution pattern of organic cation transporter 2 (OCTN2), an organic cation/carnitine transporter.
AID62974Percent reduction of histamine stimulated gastric acid secretion in adult mongrel dog after intravenous administration at 5 mg/kg.1981Journal of medicinal chemistry, Aug, Volume: 24, Issue:8
Gastric antisecretory agents. 2. Antisecretory activity of 9-[(aminoalkyl)thio]-9H-xanthenes and 5-[(aminoalkyl)thio]-5H-[1]benzopyrano[2,3-b]pyridines.
AID496826Antimicrobial activity against Entamoeba histolytica2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID183685Inhibition of aspirin induced gastric lesions in rats after peroral dose of 32 mg/kg1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
Studies on antiulcer drugs. 7. 2-Guanidino-4-pyridylthiazoles as histamine H2-receptor antagonists with potent gastroprotective effects against nonsteroidal antiinflammatory drug-induced injury.
AID60177The intravenous dose of cimetidine required to reduce acid output to 50% of control value in histamine stimulated dogs1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
Antiulcer agents. 2. Gastric antisecretory, cytoprotective, and metabolic properties of substituted imidazo[1,2-a]pyridines and analogues.
AID679277TP_TRANSPORTER: transepithelial transport (apical to basal) of Cimetidine at 64.5 nM in MDR1-expressing LLC-PK1 cells2001Pharmaceutical research, Dec, Volume: 18, Issue:12
Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1511118Permeability of the compound measured after compound dilution in PBS/EtOH buffer (70:30) by PAMPA-BBB assay2019European journal of medicinal chemistry, Oct-15, Volume: 180A novel class of multitarget anti-Alzheimer benzohomoadamantane‒chlorotacrine hybrids modulating cholinesterases and glutamate NMDA receptors.
AID588992Inhibitors of transporters of clinical importance in the absorption and disposition of drugs, MATE2-K2010Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
Membrane transporters in drug development.
AID150752Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID26362Ionization constant (pKa)2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID59659Effective dose administarted intravenously required for 50 % inhibition of acid output in dogs value ranges from 1.37-2.461983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Conformational requirements for histamine H2-receptor inhibitors: a structure-activity study of phenylene analogues related to cimetidine and tiotidine.
AID150751Inhibition of P-glycoprotein using ATPase in MDR1 membranes2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID692188Therapeutic index, ratio of Cmax in human to IC50 for human OCT22011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2.
AID59309Acid concentration of histamine stimulated inhibition of gastric secretion when administered perorally in dogs1983Journal of medicinal chemistry, Apr, Volume: 26, Issue:4
Inhibitors of gastric acid secretion: antisecretory 2-pyridylurea derivatives.
AID681169TP_TRANSPORTER: uptake in OCTN2-expressing HEK293 cells1999The Journal of pharmacology and experimental therapeutics, Nov, Volume: 291, Issue:2
Na(+)-dependent carnitine transport by organic cation transporter (OCTN2): its pharmacological and toxicological relevance.
AID28925Highest effective permeability across hexadecane membrane (pH 4-8)2001Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6
High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes.
AID771318Cellular uptake in human HEK293 cells assessed as human OCT2-mediated drug transport after 4 mins by LC-MS/MS analysis2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Identification of novel substrates and structure-activity relationship of cellular uptake mediated by human organic cation transporters 1 and 2.
AID26093pKa of urea component measured as proton lost ( a reference pKa for N,N''- dimethyl -N- cyanoguanidine in water); pKa is >11, upper limit of potentiometric method with glass electrode1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Conformational requirements for histamine H2-receptor inhibitors: a structure-activity study of phenylene analogues related to cimetidine and tiotidine.
AID230085Ratio of number of determinations at pH 7.8 to pH 7.41987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Studies on the active molecular species of the H2 receptor antagonists cimetidine and mifentidine.
AID183996Gastric antisecretory activity at the dose of 100 mg/kg in pylorus lygated rats1983Journal of medicinal chemistry, Mar, Volume: 26, Issue:3
Pyridazinones. 2. Synthesis and antisecretory and antiulcer activities of thiourea and 2-cyanoguanidine derivatives.
AID1319973Permeability of the compound by PAMPA assay2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis and biological evaluation of N-cyanoalkyl-, N-aminoalkyl-, and N-guanidinoalkyl-substituted 4-aminoquinoline derivatives as potent, selective, brain permeable antitrypanosomal agents.
AID682177TP_TRANSPORTER: inhibition of benzylpenicillin uptake by Cimetidine at a concentration of 1000uM in Oat3-expressing oocyte cells2004The Journal of pharmacology and experimental therapeutics, Jun, Volume: 309, Issue:3
Mouse reduced in osteosclerosis transporter functions as an organic anion transporter 3 and is localized at abluminal membrane of blood-brain barrier.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID682230TP_TRANSPORTER: inhibition of Guanidine uptake (Guanidine: 35 uM, Cimetidine: 5000 uM) in OCT3-expressing HeLa cells1998The Journal of biological chemistry, Jun-26, Volume: 273, Issue:26
Cloning and functional characterization of a potential-sensitive, polyspecific organic cation transporter (OCT3) most abundantly expressed in placenta.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID88096Minimum inhibitory concentration required to inhibit macroscopic colonial growth of Helicobacter pylori; ranges from (800-1600)2002Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
Anti-Helicobacter pylori agents. 5. 2-(Substituted guanidino)-4-arylthiazoles and aryloxazole analogues.
AID1133949Antiulcer activity in albino rat pyloric ligation model assessed as elevation of gastric pH at 100 mg/kg, po administered as single dose 1 hr prior ligation (Rvb =1.1 no_unit)1977Journal of medicinal chemistry, Apr, Volume: 20, Issue:4
Experimental antiulcer drugs. 1. Indole-1-alkanamides and pyrrole-1-alkanamides.
AID167652Antisecretory activity evaluated by the inhibition of 14C -AP uptake in isolated rabbit parietal cells stimulated by exogenous histamine1988Journal of medicinal chemistry, Sep, Volume: 31, Issue:9
Synthesis of (aryloxy)alkylamines. 1. Novel antisecretory agents with H+K+-ATPase inhibitory activity.
AID19260Logarithm of partition coefficient of the neutral form of compound given for octanol/water solvent system1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Development of a new physicochemical model for brain penetration and its application to the design of centrally acting H2 receptor histamine antagonists.
AID1209581Fraction unbound in Sprague-Dawley rat brain homogenates at 5 uM by equilibrium dialysis analysis2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID679677TP_TRANSPORTER: inhibition of E1S uptake in OAT3 expressing oocytes2004European journal of pharmacology, Oct-25, Volume: 503, Issue:1-3
Different transport properties between famotidine and cimetidine by human renal organic ion transporters (SLC22A).
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1511119Permeability of the compound at 25 ug/ml by PAMPA-BBB assay2019European journal of medicinal chemistry, Oct-15, Volume: 180A novel class of multitarget anti-Alzheimer benzohomoadamantane‒chlorotacrine hybrids modulating cholinesterases and glutamate NMDA receptors.
AID91481Binding constant against human serum albumin (HSA)2001Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25
Cheminformatic models to predict binding affinities to human serum albumin.
AID679499TP_TRANSPORTER: uptake in OCT2-expressing mIMCD3 cells2000British journal of pharmacology, Sep, Volume: 131, Issue:1
The organic cation transporter OCT2 mediates the uptake of beta-adrenoceptor antagonists across the apical membrane of renal LLC-PK(1) cell monolayers.
AID28399Cellular permeability (Pc) (Caco-2 cell monolayer)2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
Experimental and computational screening models for the prediction of intestinal drug absorption.
AID60178The oral dose of cimetidine required to reduce acid output to 50% of control value in histamine stimulated dogs1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
Antiulcer agents. 2. Gastric antisecretory, cytoprotective, and metabolic properties of substituted imidazo[1,2-a]pyridines and analogues.
AID681037TP_TRANSPORTER: inhibition of Ochratoxin A uptake (OTA: 1 uM, Cimetidine: 200 uM) in OAT3-expressing S2 cells2001Life sciences, Sep-21, Volume: 69, Issue:18
Characterization of ochratoxin A transport by human organic anion transporters.
AID1433974Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation counting2017Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
Pyrimidine-Based Inhibitors of Dynamin I GTPase Activity: Competitive Inhibition at the Pleckstrin Homology Domain.
AID1221982Fraction absorbed in human2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID74332Antisecretory activity (total acid output) at 6 mg/kg dose administered in Gastric pouch dog was determined by dose related inhibition of food stimulated gastric acid secretion1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
2-Oxo-1,8-naphthyridine-3-carboxylic acid derivatives with potent gastric antisecretory properties.
AID1285633Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
AID681337TP_TRANSPORTER: Western blot, HK-2 cells2002Toxicology and applied pharmacology, Sep-01, Volume: 183, Issue:2
Influence of different chemicals on MDR-1 P-glycoprotein expression and activity in the HK-2 proximal tubular cell line.
AID26066pKa (association constant) value at a physiological pH of 7.41983Journal of medicinal chemistry, Jan, Volume: 26, Issue:1
Bioisosteric design of conformationally restricted pyridyltriazole histamine H2-receptor antagonists.
AID1636268Permeability of the compound at pH 7.4 after 18 hrs by PAMPA-BBB assay2016Bioorganic & medicinal chemistry, 10-15, Volume: 24, Issue:20
Design, synthesis and biological evaluation of N-methyl-N-[(1,2,3-triazol-4-yl)alkyl]propargylamines as novel monoamine oxidase B inhibitors.
AID678973TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in hOAT4-expressing S2 cells2004Journal of pharmacological sciences, Feb, Volume: 94, Issue:2
Interactions of human- and rat-organic anion transporters with pravastatin and cimetidine.
AID467613Volume of distribution at steady state in human2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID678716Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID178862Antisecretory activity in a pylorus-ligated rat model1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Antiulcer agents. 4-substituted 2-guanidinothiazoles: reversible, competitive, and selective inhibitors of gastric H+,K(+)-ATPase.
AID1264447Permeability of the compound by PAMPA method2015European journal of medicinal chemistry, Nov-13, Volume: 105Multicomponent reaction-based synthesis and biological evaluation of tricyclic heterofused quinolines with multi-trypanosomatid activity.
AID1223578Ratio of Ki for CYP3A4.16 (unknown origin) to Ki for CYP3A4.1 (unknown origin)2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
Comparison of the inhibitory profiles of itraconazole and cimetidine in cytochrome P450 3A4 genetic variants.
AID346426Displacement of radiolabeled cimetidine from human histamine H2 receptor2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.
AID88140Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.01987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Studies on the active molecular species of the H2 receptor antagonists cimetidine and mifentidine.
AID678841TP_TRANSPORTER: inhibition of PHA uptake (PHA: 1000uM) in mOat3-expressing oocytes2004Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 32, Issue:5
Renal transport of organic compounds mediated by mouse organic anion transporter 3 (mOat3): further substrate specificity of mOat3.
AID681690TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 0.1? uM, cimetidine: 100 uM) in OCT3-expressing HEK293 cells1998Nature neuroscience, Sep, Volume: 1, Issue:5
Molecular identification of the corticosterone-sensitive extraneuronal catecholamine transporter.
AID678718Metabolic stability in human liver microsomes assessed as high signal/noise ratio (S/N of >100) by measuring GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID679235TP_TRANSPORTER: transepithelial transport (basal to apical) in MDR1-expressing MDCK cells2000Pharmaceutical research, Dec, Volume: 17, Issue:12
Influence of passive permeability on apparent P-glycoprotein kinetics.
AID725597inhibition of human PAD4 preincubated at 1 uM for 15 mins before substrate addition measured after 20 mins by spectrophotometry2013Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3
Novel small molecule protein arginine deiminase 4 (PAD4) inhibitors.
AID26266Log distribution coefficient between 1-octanol and aqueous buffer at pH of 9.2.1983Journal of medicinal chemistry, Jan, Volume: 26, Issue:1
Bioisosteric design of conformationally restricted pyridyltriazole histamine H2-receptor antagonists.
AID1135362Octanol-water partition coefficient, log P of the compound at pH 9.21977Journal of medicinal chemistry, Jul, Volume: 20, Issue:7
Cyanoguanidine-thiourea equivalence in the development of the histamine H2-receptor antagonist, cimetidine.
AID624628Drug-stimulated Pgp ATPase activity ratio determined in MDR1-Sf9 cell membranes with test compound at a concentration of 20uM2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID496817Antimicrobial activity against Trypanosoma cruzi2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID223862Antisecretory activity at 8 mg/kg dose administered intraduodenally in the pylorus-ligated rat was determined and value given as total acid output(TAO) as % of control1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
2-Oxo-1,8-naphthyridine-3-carboxylic acid derivatives with potent gastric antisecretory properties.
AID481446Effective permeability across human jejunum2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID1223571Inhibition of CYP3A4.1 (unknown origin)-mediated testosterone 6beta-hydroxylation incubated for 10 mins prior to NADPH addition measured after 20 mins by HPLC-UV analysis2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
Comparison of the inhibitory profiles of itraconazole and cimetidine in cytochrome P450 3A4 genetic variants.
AID59645Cytoprotective activity in rats against the ethyl alcohol stimulated ulcers measured as effective dose; NA means inactive1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
Antiulcer agents. 2. Gastric antisecretory, cytoprotective, and metabolic properties of substituted imidazo[1,2-a]pyridines and analogues.
AID679898TP_TRANSPORTER: inhibition of Vinblastine transepithelial transport (basal to apical)(Vinblastine: 0.004 uM, Cimetidine: 3000 uM) in Caco-2 cells2000Pharmaceutical research, Dec, Volume: 17, Issue:12
Influence of passive permeability on apparent P-glycoprotein kinetics.
AID1209582Unbound volume of distribution in Sprague-Dawley rat brain slices at 100 nM after 5 hrs2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID60393Histamine-stimulated gastric acid secretion in Heidenhain pouch dog at 4uM/Kg, on iv administration of the compound1995Journal of medicinal chemistry, Jul-07, Volume: 38, Issue:14
Reversible inhibitors of the gastric (H+/K+)-ATPase. 5. Substituted 2,4-diaminoquinazolines and thienopyrimidines.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1223572Inhibition of CYP3A4.2 (unknown origin)-mediated testosterone 6beta-hydroxylation incubated for 10 mins prior to NADPH addition measured after 20 mins by HPLC-UV analysis2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
Comparison of the inhibitory profiles of itraconazole and cimetidine in cytochrome P450 3A4 genetic variants.
AID1223579Ratio of Ki for CYP3A4.18 (unknown origin) to Ki for CYP3A4.1 (unknown origin)2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
Comparison of the inhibitory profiles of itraconazole and cimetidine in cytochrome P450 3A4 genetic variants.
AID223859Antisecretory activity at 32 mg/kg dose administered intraduodenally in the pylorus-ligated rat1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
2-Oxo-1,8-naphthyridine-3-carboxylic acid derivatives with potent gastric antisecretory properties.
AID576507Antiplasmodial activity against Plasmodium falciparum 3D7 infected in RBCs by firefly luciferase reporter gene assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Discovery of potent small-molecule inhibitors of multidrug-resistant Plasmodium falciparum using a novel miniaturized high-throughput luciferase-based assay.
AID681155TP_TRANSPORTER: increase in bodipy intracellular accumulation (Bodipy: 0.2 uM) in SK-E2 cells (expressing BSEP)2003Pharmaceutical research, Apr, Volume: 20, Issue:4
Fluorescent substrates of sister-P-glycoprotein (BSEP) evaluated as markers of active transport and inhibition: evidence for contingent unequal binding sites.
AID1909448Permeability of the compound by PAMPA-BBB assay2022European journal of medicinal chemistry, Jun-05, Volume: 236Design, synthesis, and in vitro and in vivo characterization of new memantine analogs for Alzheimer's disease.
AID678815TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in hOAT3-expressing S2 cells2004Journal of pharmacological sciences, Feb, Volume: 94, Issue:2
Interactions of human- and rat-organic anion transporters with pravastatin and cimetidine.
AID88232The lowest drug concentration that inhibited macroscopic colonial growth against Helicobacter pylori; Value ranges from 800-16002000Journal of medicinal chemistry, Aug-24, Volume: 43, Issue:17
Anti-Helicobacter pylori agents. 4. 2-(Substituted guanidino)-4-phenylthiazoles and some structurally rigid derivatives.
AID467611Dissociation constant, pKa of the compound2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID1149787Inhibition of histamine-induced gastric acid secretion in iv dosed rat in perfused stomach preparation measured after 15 mins1977Journal of medicinal chemistry, Oct, Volume: 20, Issue:10
Compounds with gastric antisecretory activity. 1. Phenoxyalkylamines.
AID62976Percent reduction of histamine stimulated gastric acid secretion in adult mongrel dog after peroral administration of compound at 8 mg/kg1981Journal of medicinal chemistry, Aug, Volume: 24, Issue:8
Gastric antisecretory agents. 2. Antisecretory activity of 9-[(aminoalkyl)thio]-9H-xanthenes and 5-[(aminoalkyl)thio]-5H-[1]benzopyrano[2,3-b]pyridines.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID59999Inhibition of histamine stimulated gastric acid secretion was tested in heidenhain pouch dog upon intravenous administration1992Journal of medicinal chemistry, Sep-04, Volume: 35, Issue:18
Reversible inhibitors of the gastric (H+/K+)-ATPase. 3. 3-substituted-4-(phenylamino)quinolines.
AID87965Minimum inhibitory concentration that inhibited macroscopic colony growth of Helicobacter pylori1999Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
Anti-Helicobacter pylori agents. 3. 2-[(Arylalkyl)guanidino]-4-furylthiazoles.
AID1848077Inhibition of Haemophilus influenza HmrM transporter expressed in Escherichia coli KAM32 assessed as inhibition of bacterial resistance to norfloxacin by measuring reduction in bacterial growth at 100 uM incubated for 18 hrs by microbroth dilution method 2022Bioorganic & medicinal chemistry, 11-15, Volume: 74Fluorophenylalkyl-substituted cyanoguanidine derivatives as bacteria-selective MATE transporter inhibitors for the treatment of antibiotic-resistant infections.
AID195507Percent reduction of gastric acid secretion in pylorus ligated rat after intraperitoneal administration at 40 mg/kg.1981Journal of medicinal chemistry, Aug, Volume: 24, Issue:8
Gastric antisecretory agents. 2. Antisecretory activity of 9-[(aminoalkyl)thio]-9H-xanthenes and 5-[(aminoalkyl)thio]-5H-[1]benzopyrano[2,3-b]pyridines.
AID1223577Ratio of Ki for CYP3A4.1 (unknown origin) to Ki for CYP3A4.7 (unknown origin)2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
Comparison of the inhibitory profiles of itraconazole and cimetidine in cytochrome P450 3A4 genetic variants.
AID233937Ratio (po/iv) value of the compound1982Journal of medicinal chemistry, Mar, Volume: 25, Issue:3
Inhibitors of gastric acid secretion: 3,4-diamino-1,2,5-thiadiazole 1-oxides and 1,1-dioxides as urea equivalents in a series of histamine H2-receptor antagonists.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID62846Antisecretory activity was evaluated in adult mongrel dog after po administration at 8 mg/kg of dose, expressed as reduction of gastric output1981Journal of medicinal chemistry, Aug, Volume: 24, Issue:8
Gastric antisecretory agents. 1. Antisecretory and antiulcer activity of 5H-[1]benzopyrano[2,3-b]pyridin-5-ylureas and 5H-[1]benzothiopyrano[2,3-b]pyridin-5-ylureas.
AID1133961Antiulcer activity in albino rat pyloric ligation model assessed as inhibition of total acid output at 100 mg/kg, po administered as single dose 1 hr prior ligation relative to control1977Journal of medicinal chemistry, Apr, Volume: 20, Issue:4
Experimental antiulcer drugs. 1. Indole-1-alkanamides and pyrrole-1-alkanamides.
AID496830Antimicrobial activity against Leishmania major2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID1739432Permeability across apical to basolateral side in human Caco-2 cells assessed as luciferase yellow leakage at 10 uM incubated for 2 hrs LC-MS/MS analysis2020European journal of medicinal chemistry, Aug-15, Volume: 200Substituted benzothiophene and benzofuran derivatives as a novel class of bone morphogenetic Protein-2 upregulators: Synthesis, anti-osteoporosis efficacies in ovariectomized rats and a zebrafish model, and ADME properties.
AID692183Protein binding in human plasma2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2.
AID176290Antisecretory activity was evaluated in acute gastric fistula of rat after peroral administration1987Journal of medicinal chemistry, May, Volume: 30, Issue:5
Antisecretory activity of human, dog, and rat metabolites of fenoctimine.
AID1209593Dissociation constant, pKa of the acidic compound by capillary electrophoresis-mass spectrometry analysis2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods.
AID692191Inhibition of human OCT2 expressed in HEK-293-Flp-In cells at 500 uM incubated for 3 mins by ASP+ substrate uptake assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2.
AID721754Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling.
AID1848080Inhibition of human MATE12022Bioorganic & medicinal chemistry, 11-15, Volume: 74Fluorophenylalkyl-substituted cyanoguanidine derivatives as bacteria-selective MATE transporter inhibitors for the treatment of antibiotic-resistant infections.
AID28233Fraction ionized (pH 7.4)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID455986Permeability across human Caco-2 cells2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Computational modeling of novel inhibitors targeting the Akt pleckstrin homology domain.
AID87709In vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenate1982Journal of medicinal chemistry, Mar, Volume: 25, Issue:3
Inhibitors of gastric acid secretion: 3,4-diamino-1,2,5-thiadiazole 1-oxides and 1,1-dioxides as urea equivalents in a series of histamine H2-receptor antagonists.
AID409956Inhibition of mouse brain MAOB2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID231333Ratio of [(apical to basal)/(basal to apical)] (Caco-2 cell monolayer)2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
Experimental and computational screening models for the prediction of intestinal drug absorption.
AID1221957Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID771316Cellular uptake in human HEK293 cells assessed as human OCT2-mediated drug transport at 2.5 uM after 4 mins by LC-MS/MS analysis2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Identification of novel substrates and structure-activity relationship of cellular uptake mediated by human organic cation transporters 1 and 2.
AID1223574Inhibition of CYP3A4.16 (unknown origin)-mediated testosterone 6beta-hydroxylation incubated for 10 mins prior to NADPH addition measured after 20 mins by HPLC-UV analysis2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
Comparison of the inhibitory profiles of itraconazole and cimetidine in cytochrome P450 3A4 genetic variants.
AID225273Dose required to inhibit ulcer induced by stress in rats1983Journal of medicinal chemistry, Mar, Volume: 26, Issue:3
Pyridazinones. 2. Synthesis and antisecretory and antiulcer activities of thiourea and 2-cyanoguanidine derivatives.
AID21233Partition coefficient of compound in to biological membranes1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Reevaluating equilibrium and kinetic binding parameters for lipophilic drugs based on a structural model for drug interaction with biological membranes.
AID1196050Cytotoxicity against human HepG2 cells at 0.1 to 100 uM after 24 hrs by Hoechst 33342 staining-based fluorescence assay2015European journal of medicinal chemistry, Mar-06, Volume: 92Evaluating the risk of phospholipidosis using a new multidisciplinary pipeline approach.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID87867Histamine H2 receptor antagonist activity (chronotropic response to histamine) in guinea pig right atrium1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
Studies on histamine H2 receptor antagonists. 2. Synthesis and pharmacological activities of N-sulfamoyl and N-sulfonyl amidine derivatives.
AID481444Octanol-water partition coefficient, log P of the compound2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID59308Acid concentration of gastrin tetrapeptide stimulated inhibition of gastric secretion when administered perorally in dogs1983Journal of medicinal chemistry, Apr, Volume: 26, Issue:4
Inhibitors of gastric acid secretion: antisecretory 2-pyridylurea derivatives.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID29337Ionisation constant (pKa)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID682099TP_TRANSPORTER: no change in tissue distribution in Oct1 -/- mouse2001Molecular and cellular biology, Aug, Volume: 21, Issue:16
Reduced hepatic uptake and intestinal excretion of organic cations in mice with a targeted disruption of the organic cation transporter 1 (Oct1 [Slc22a1]) gene.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID60179Volume of gastrin tetrapeptide stimulated inhibition of gastric secretion when administered perorally in dogs1983Journal of medicinal chemistry, Apr, Volume: 26, Issue:4
Inhibitors of gastric acid secretion: antisecretory 2-pyridylurea derivatives.
AID60225Evaluated against tetragastrin stimulated gastric acid secretion in conscious Hiedenhain-pouch dogs at a dose of 22 mg/kg, po1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
Studies on antiulcer drugs. 7. 2-Guanidino-4-pyridylthiazoles as histamine H2-receptor antagonists with potent gastroprotective effects against nonsteroidal antiinflammatory drug-induced injury.
AID88335Histamine H2 receptor antagonism in isolated guinea pig right atrium at concentration of 1*10e-6 g/mL of histamine hydrochloride1999Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
Anti-Helicobacter pylori agents. 3. 2-[(Arylalkyl)guanidino]-4-furylthiazoles.
AID681956TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 0.85 uM, Cimetidine: 5000 uM) in Xenopus laevis oocytes1997Molecular pharmacology, Jun, Volume: 51, Issue:6
Cloning and functional expression of a human liver organic cation transporter.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID88014Dissociation constant of H2 receptor antagonist activity against guinea pig atrium1985Journal of medicinal chemistry, Nov, Volume: 28, Issue:11
Pseudosymmetry and bioisosterism in biaryl pyridyl competitive histamine H2-receptor antagonists.
AID481439Absolute bioavailability in human2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID496825Antimicrobial activity against Leishmania mexicana2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID620399Permeability of the compound by PAMPA2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Hybrids of oxoisoaporphine-tacrine congeners: novel acetylcholinesterase and acetylcholinesterase-induced β-amyloid aggregation inhibitors.
AID1221967Ratio of intestine AUC in po dosed mdr1 knock out mouse to intestine AUC in po dosed wild type mouse2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID178857Antisecretory activity against histamine stimulated gastric acid secretion in Shay rats expressed as ED50 value ranges from (7.4-118)1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Synthesis and antisecretory and antiulcer activities of derivatives and analogues of 2-(2-pyridyl)tetrahydrothiophene-2-carbothioamide.
AID1739431Permeability across apical to basolateral side in human Caco-2 cells assessed as transepithelial electrical resistance at 10 uM incubated for 2 hrs LC-MS/MS analysis2020European journal of medicinal chemistry, Aug-15, Volume: 200Substituted benzothiophene and benzofuran derivatives as a novel class of bone morphogenetic Protein-2 upregulators: Synthesis, anti-osteoporosis efficacies in ovariectomized rats and a zebrafish model, and ADME properties.
AID223216Inhibition of histamine-stimulated chronotropic response in isolated guinea pig right atrium at 1*10e-6 g/mL2002Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
Anti-Helicobacter pylori agents. 5. 2-(Substituted guanidino)-4-arylthiazoles and aryloxazole analogues.
AID181893In vivo gastric antisecretory activity in acute fistula rats (12.5 mg/kg, id)1992Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13
Synthesis and antiulcer activity of N-substituted N'-[3-[3-(piperidinomethyl)phenoxy]propyl]ureas: histamine H2-receptor antagonists with a potent mucosal protective activity.
AID624694Mechanism based inhibition of rat cytochrome P450 CYP2C11 measured by testosterone 2-alpha hydroxylase activity2005Current drug metabolism, Oct, Volume: 6, Issue:5
Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.
AID1183278Permeability of the compound by PAMPA2014European journal of medicinal chemistry, Sep-12, Volume: 84Tetrahydrobenzo[h][1,6]naphthyridine-6-chlorotacrine hybrids as a new family of anti-Alzheimer agents targeting β-amyloid, tau, and cholinesterase pathologies.
AID167650Antisecretory activity evaluated by the inhibition of 14C -AP uptake in isolated rabbit parietal cells stimulated by dibutyryl cyclic adenosine 3', 5' -monophosphate (dcAMP)1988Journal of medicinal chemistry, Sep, Volume: 31, Issue:9
Synthesis of (aryloxy)alkylamines. 1. Novel antisecretory agents with H+K+-ATPase inhibitory activity.
AID680342TP_TRANSPORTER: inhibition of PAH uptake in Oat1-expressing LLC-PK1 cells2002Molecular pharmacology, May, Volume: 61, Issue:5
Expression and functional characterization of rat organic anion transporter 3 (rOat3) in the choroid plexus.
AID1319976Permeability of the compound at 25 ug/ml at 7.4 pH after 18 hrs by PAMPA2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis and biological evaluation of N-cyanoalkyl-, N-aminoalkyl-, and N-guanidinoalkyl-substituted 4-aminoquinoline derivatives as potent, selective, brain permeable antitrypanosomal agents.
AID678813TP_TRANSPORTER: trans-stimulation in Xenopus laevis oocytes2003Cellular physiology and biochemistry : international journal of experimental cellular physiology, biochemistry, and pharmacology, , Volume: 13, Issue:5
Human organic anion transporter 3 (hOAT3) can operate as an exchanger and mediate secretory urate flux.
AID678806TP_TRANSPORTER: inhibition of TEA uptake in Octn1-HRPE cells2000Biochimica et biophysica acta, Jun-01, Volume: 1466, Issue:1-2
Structural and functional characteristics and tissue distribution pattern of rat OCTN1, an organic cation transporter, cloned from placenta.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID29925Volume of distribution in man (IV dose)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID177813Compound was evaluated in vivo for the gastric antisecretory activity in the lumen perfused stomach of the anesthetized rat after iv administration1984Journal of medicinal chemistry, Mar, Volume: 27, Issue:3
(Imidazolylphenyl)formamidines. A structurally novel class of potent histamine H2 receptor antagonists.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID679370TP_TRANSPORTER: uptake in Xenopus laevis oocytes2003American journal of physiology. Renal physiology, Mar, Volume: 284, Issue:3
Transport of cimetidine by flounder and human renal organic anion transporter 1.
AID236268Fraction absorbed in human intestine after oral administration compound was measured2005Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2
Exploring the role of different drug transport routes in permeability screening.
AID78484Dose representing 50% inhibition of positive chronotropic response to histamine in guinea pig atrium (5 x 10e -6M)1984Journal of medicinal chemistry, Jul, Volume: 27, Issue:7
Histamine H2 receptor antagonists. 1. Synthesis of N-cyano and N-carbamoyl amidine derivatives and their biological activities.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID19424Partition coefficient (logD7.4)2001Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15
ElogD(oct): a tool for lipophilicity determination in drug discovery. 2. Basic and neutral compounds.
AID481442Transcellular permeability at pH 6.5 calculated from in vitro P app values in Caco-2 and/or MDCK cells2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID1135358Antagonist at histamine H2 receptor in rat uterus assessed as inhibition of histamine-induced response1977Journal of medicinal chemistry, Jul, Volume: 20, Issue:7
Cyanoguanidine-thiourea equivalence in the development of the histamine H2-receptor antagonist, cimetidine.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID624626Ratio of apparent permeability from basolateral to apical side over apical to basolateral side determined in MDR1-MDCKII cells2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID681120TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in Caco-2 cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID682269TP_TRANSPORTER: inhibition of TEA uptake (TEA: 20 uM, Cimetidine: 5000 uM) in OCTN2-expressing HeLa cells1998Biochemical and biophysical research communications, May-29, Volume: 246, Issue:3
cDNA sequence, transport function, and genomic organization of human OCTN2, a new member of the organic cation transporter family.
AID88018Evaluated for antagonist activity against histamine H2 receptor and represented as KB.1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
Histamine H3 ligands: just pharmacological tools or potential therapeutic agents?
AID1223573Inhibition of CYP3A4.7 (unknown origin)-mediated testosterone 6beta-hydroxylation incubated for 10 mins prior to NADPH addition measured after 20 mins by HPLC-UV analysis2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
Comparison of the inhibitory profiles of itraconazole and cimetidine in cytochrome P450 3A4 genetic variants.
AID318592Elevation in glycogen level in fasting BALB/c mouse at 11.40 mg/kg, ip after 3 hrs2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Pharmacophore modeling, quantitative structure-activity relationship analysis, and in silico screening reveal potent glycogen synthase kinase-3beta inhibitory activities for cimetidine, hydroxychloroquine, and gemifloxacin.
AID183249Inhibition of histamine stimulated gastric acid secretion in lumen perfused stomach of anesthetized rats (1 mg/kg iv)2000Journal of medicinal chemistry, Aug-24, Volume: 43, Issue:17
Anti-Helicobacter pylori agents. 4. 2-(Substituted guanidino)-4-phenylthiazoles and some structurally rigid derivatives.
AID679259TP_TRANSPORTER: transepithelial transport (basal to apical) in Caco-2 cells2000Pharmaceutical research, Dec, Volume: 17, Issue:12
Influence of passive permeability on apparent P-glycoprotein kinetics.
AID28236Unbound fraction (tissues)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID678717Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID481441Aqueous diffusivity at 37C2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID88318Histamine H2 receptor antagonism at a concentration of 1 umolar on the isolated guinea pig right atrium.1992Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12
Iodoaminopotentidine and related compounds: a new class of ligands with high affinity and selectivity for the histamine H2 receptor.
AID59668Reduction in acid response to histamine(160 ug/kg/h i.v.) in anesthetized dogs with acute gastric fistula.1984Journal of medicinal chemistry, Jul, Volume: 27, Issue:7
Histamine H2 receptor antagonists. 1. Synthesis of N-cyano and N-carbamoyl amidine derivatives and their biological activities.
AID204449Inhibitory activity against sigma receptor isolated from guinea pig brain cortex membrane using [3H]DTG as radioligand; Inactive1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
New sigma and 5-HT1A receptor ligands: omega-(tetralin-1-yl)-n-alkylamine derivatives.
AID28924Effective permeability (Pe) across a hexadecane membrane (pH 6.8)2001Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6
High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes.
AID236914Permeability Coefficient in hexadecane membranes model2005Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2
Exploring the role of different drug transport routes in permeability screening.
AID60990Inhibition of acid output in dogs (po)1982Journal of medicinal chemistry, Mar, Volume: 25, Issue:3
Inhibitors of gastric acid secretion: 3,4-diamino-1,2,5-thiadiazole 1-oxides and 1,1-dioxides as urea equivalents in a series of histamine H2-receptor antagonists.
AID188853Percent protection from gastric damage in rats relative to vehicle control following intraperitoneal administration of 20 mg/Kg1995Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
Synthesis and biological evaluation of substituted flavones as gastroprotective agents.
AID751879Binding affinity to human histamine H2 receptor by radioligand displacement assay2013European journal of medicinal chemistry, May, Volume: 63Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.
AID77616Antagonism of the positive chronotropic action of histamine in the isolated guinea pig atrium1982Journal of medicinal chemistry, Mar, Volume: 25, Issue:3
1,2,5-thiadiazole 1-oxide and 1,1-dioxide derivatives. A new class of potent histamine H2-receptor antagonists.
AID692195Inhibition of human MATE1 expressed in HEK-293-Flp-In cells incubated for 3 mins by ASP+ substrate uptake assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2.
AID1336328Displacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting method2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH
AID150757P-gp activity was measured by a direct transport assay, using polarized LLC-MDR1 epithelial cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID29844Fraction absorbed after oral administration in humans2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
Experimental and computational screening models for the prediction of intestinal drug absorption.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID88326Inhibition of [125I]APT binding to H2 receptors in guinea pig cerebral membranes.1992Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12
Iodoaminopotentidine and related compounds: a new class of ligands with high affinity and selectivity for the histamine H2 receptor.
AID692184Therapeutic index, ratio of Cmax in human to IC50 for human MATE2-K2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2.
AID88329Inhibition of the positive chronotropic response (H2-antagonism) of guinea pig right atrium relative to cimetidine.1992Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12
Iodoaminopotentidine and related compounds: a new class of ligands with high affinity and selectivity for the histamine H2 receptor.
AID185122The antiulcer activity against stress-induced ulcer in rats by 30 mg/kg peroral administration.1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Synthesis and antiulcer activity of 5,11-dihydro[1]benzoxepino[3,4-b]pyridines.
AID182170Compound was measured for percentage inhibition of aspirin-induced ulcers at 10 mg/kg after po administration1981Journal of medicinal chemistry, Aug, Volume: 24, Issue:8
Gastric antisecretory agents. 1. Antisecretory and antiulcer activity of 5H-[1]benzopyrano[2,3-b]pyridin-5-ylureas and 5H-[1]benzothiopyrano[2,3-b]pyridin-5-ylureas.
AID752241Binding affinity to human histamine H2 receptor by radioligand displacement assay2013Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.
AID28912Partition coefficient (logD) (octanol/borax buffer)1986Journal of medicinal chemistry, Jan, Volume: 29, Issue:1
Dipole moment in relation to H2 receptor histamine antagonist activity for cimetidine analogues.
AID25362Compound was evaluated for the ionization constant (pKa) by using potentiometric titration (ionization of end group)1984Journal of medicinal chemistry, Mar, Volume: 27, Issue:3
(Imidazolylphenyl)formamidines. A structurally novel class of potent histamine H2 receptor antagonists.
AID223861Antisecretory activity at 64 mg/kg dose administered intraduodenally in the pylorus-ligated rat was determined and value given as total acid output(TAO) as % of control1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
2-Oxo-1,8-naphthyridine-3-carboxylic acid derivatives with potent gastric antisecretory properties.
AID678785TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 1 uM) in Xenopus laevis oocytes2002Biochemical and biophysical research communications, Aug-23, Volume: 296, Issue:3
Functional characterization of mouse cation transporter mOCT2 compared with mOCT1.
AID678970TP_TRANSPORTER: inhibition of TEA uptake (TEA: 100 uM) in Xenopus laevis oocytes1999Biochimica et biophysica acta, Mar-04, Volume: 1417, Issue:2
Molecular mechanisms of organic cation transport in OCT2-expressing Xenopus oocytes.
AID15430Log (Cbrain/Cblood) in rats1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Development of a new physicochemical model for brain penetration and its application to the design of centrally acting H2 receptor histamine antagonists.
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1858750Antisecretory activity in Sprague-Dawley rat assessed as inhibition of gastric acid accumulation at 20 mg/kg,ID2021European journal of medicinal chemistry, Jan-15, Volume: 210Research progress in biological activities of isochroman derivatives.
AID678722Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID135327BBB penetration classification2000Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11
Predicting blood-brain barrier permeation from three-dimensional molecular structure.
AID1221964Transporter substrate index ratio of permeability from basolateral to apical side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID428564Inhibition of CYP3A42009European journal of medicinal chemistry, Jul, Volume: 44, Issue:7
Comparative chemometric modeling of cytochrome 3A4 inhibitory activity of structurally diverse compounds using stepwise MLR, FA-MLR, PLS, GFA, G/PLS and ANN techniques.
AID236913Permeability Coefficient in Caco-2 cell culture model2005Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2
Exploring the role of different drug transport routes in permeability screening.
AID680484TP_TRANSPORTER: inhibition of Levofloxacin transepithelial transport (basal to apical) (Levofloxacin: 100 uM, Cimetidine: 2500 uM) in MDR1-expressing LLC-PK1 cells1997The Journal of pharmacology and experimental therapeutics, Aug, Volume: 282, Issue:2
Transport of quinolone antibacterial drugs by human P-glycoprotein expressed in a kidney epithelial cell line, LLC-PK1.
AID150754Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID1221965Transporter substrate index of efflux ratio in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID176286Antisecretory activity was evaluated in acute gastric fistula of rat after administration; ND means no data1987Journal of medicinal chemistry, May, Volume: 30, Issue:5
Antisecretory activity of human, dog, and rat metabolites of fenoctimine.
AID1210069Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID340249Inhibition of histamine H2 receptor2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.
AID681139TP_TRANSPORTER: increase in dihydrofluorescein intracellular accumulation (dihydrofluorescein: 1 uM) in SK-E2 cells (expressing BSEP)2003Pharmaceutical research, Apr, Volume: 20, Issue:4
Fluorescent substrates of sister-P-glycoprotein (BSEP) evaluated as markers of active transport and inhibition: evidence for contingent unequal binding sites.
AID80446inhibition of the histamine stimulated chronic response in the isolated guinea pig right atrium at 1x 10 e-6 g/mL1997Journal of medicinal chemistry, Aug-01, Volume: 40, Issue:16
Anti-Helicobacter pylori agents. 1. 2-(Alkylguanidino)-4-furylthiazoles and related compounds.
AID178013Effective dose for 50 percent inhibition of gastric antisecretory activity in the 4 hr pylorus-ligated rat1983Journal of medicinal chemistry, Aug, Volume: 26, Issue:8
Pyridazinones. 3. Synthesis, antisecretory, and antiulcer activities of 2-cyanoguanidine derivatives.
AID1063783Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)2014Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2
The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1134561Antisecretory activity in 5-hrs pyloric ligated rat assessed as pH of gastric contents at 100 mg/kg, po administered 2 hrs prior to pyloric ligation measured after 1 hr (Rvb = 1.1 no-unit)1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Experimental antiulcer drugs. 2. 2-Substituted 2,4,5,6-tetrahydro-1,3,4,6,6-pentamethylcyclopenta[c]pyrrole-4-carboxamides.
AID1221963Transporter substrate index ratio of permeability from apical to basolateral side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID678805TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in rOAT3-expressing S2 cells2004Journal of pharmacological sciences, Feb, Volume: 94, Issue:2
Interactions of human- and rat-organic anion transporters with pravastatin and cimetidine.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1848075Antimicrobial activity against Escherichia coli KAM32 harboring pBR322hrmM assessed as inhibition of bacterial growth at 100 uM incubated for 18 hrs by microbroth dilution method2022Bioorganic & medicinal chemistry, 11-15, Volume: 74Fluorophenylalkyl-substituted cyanoguanidine derivatives as bacteria-selective MATE transporter inhibitors for the treatment of antibiotic-resistant infections.
AID1161578Permeability of the compound by PAMPA-BBB assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Shogaol-huprine hybrids: dual antioxidant and anticholinesterase agents with β-amyloid and tau anti-aggregating properties.
AID29813Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID185619inhibition of histamine stimulated gastric secretion in lumen perfused stomach of anesthetized rats at 1 mg/kg intravenously1997Journal of medicinal chemistry, Aug-01, Volume: 40, Issue:16
Anti-Helicobacter pylori agents. 1. 2-(Alkylguanidino)-4-furylthiazoles and related compounds.
AID678967TP_TRANSPORTER: uptake in Xenopus laevis oocytes1999The Journal of biological chemistry, May-07, Volume: 274, Issue:19
Molecular cloning and characterization of a new multispecific organic anion transporter from rat brain.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID178277Anticholinergic activity against carbachol-induced gastric emptying (GE) in rat when administered perorally1983Journal of medicinal chemistry, Apr, Volume: 26, Issue:4
4-(Diphenylmethyl)-1-[(imino)methyl]piperidines as gastric antisecretory agents.
AID62845Antisecretory activity was evaluated in adult mongrel dog after iv administration at 5 mg/kg of dose, expressed as reduction of gastric output1981Journal of medicinal chemistry, Aug, Volume: 24, Issue:8
Gastric antisecretory agents. 1. Antisecretory and antiulcer activity of 5H-[1]benzopyrano[2,3-b]pyridin-5-ylureas and 5H-[1]benzothiopyrano[2,3-b]pyridin-5-ylureas.
AID60989Reduction in gastric acid secretion under histamine[160 ug/(kg h)] stimulation in anesthetized dogs after intravenous administration1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
Studies on histamine H2 receptor antagonists. 2. Synthesis and pharmacological activities of N-sulfamoyl and N-sulfonyl amidine derivatives.
AID588985Inhibitors of transporters of clinical importance in the absorption and disposition of drugs, OCT22010Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
Membrane transporters in drug development.
AID12234881-Octanol-water distribution coefficient, log D of the compound at pH 7.42012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Predicting phenolic acid absorption in Caco-2 cells: a theoretical permeability model and mechanistic study.
AID589249Mechanism based inhibition of human cytochrome P450 2C19 measured by S-mephenytoin hydroxylation2005Current drug metabolism, Oct, Volume: 6, Issue:5
Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID59365Acid antisecretory activity against pentagastrin-stimulated Heidenhain pouch dogs after intravenous administration1983Journal of medicinal chemistry, Jan, Volume: 26, Issue:1
Bioisosteric design of conformationally restricted pyridyltriazole histamine H2-receptor antagonists.
AID1848076Inhibition of Haemophilus influenza HmrM transporter expressed in Escherichia coli KAM32 assessed as inhibition of bacterial resistance to norfloxacin by measuring norfloxacin MIC at 100 uM incubated for 18 hrs by microbroth dilution method (Rvb = 64 ng/m2022Bioorganic & medicinal chemistry, 11-15, Volume: 74Fluorophenylalkyl-substituted cyanoguanidine derivatives as bacteria-selective MATE transporter inhibitors for the treatment of antibiotic-resistant infections.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID150755Inhibition of P-glycoprotein using calcein-AM assay transfected in porcine PBCEC2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID547838Inhibition of human aldehyde oxidase2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Aldehyde oxidase: an enzyme of emerging importance in drug discovery.
AID26070pKa of heterocyclic component measured as proton gained1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Conformational requirements for histamine H2-receptor inhibitors: a structure-activity study of phenylene analogues related to cimetidine and tiotidine.
AID524796Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID592681Apparent permeability across human Caco2 cell membrane after 2 hrs by LC-MS/MS analysis2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
QSAR-based permeability model for drug-like compounds.
AID692192Inhibition of human OCT2 expressed in HEK-293-Flp-In cells incubated for 3 mins by ASP+ substrate uptake assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2.
AID681122TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID205269Inhibition of binding of Batrachotoxinin [3H]BTX-B to high-affinity sites on voltage-dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 100 uM1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID1071344Permeability of the compound by BBB-PAMPA2014European journal of medicinal chemistry, Feb-12, Volume: 731,2,3,4-Tetrahydrobenzo[h][1,6]naphthyridines as a new family of potent peripheral-to-midgorge-site inhibitors of acetylcholinesterase: synthesis, pharmacological evaluation and mechanistic studies.
AID648667Permeability of the compound in porcine brain lipid assessed as ratio of compound in acceptor plate to amount of compound in donor plate at 5 mg/ml after 10 hrs by PAMPA assay2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
Novel oxoisoaporphine-based inhibitors of acetyl- and butyrylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID8002Observed volume of distribution2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID678793TP_TRANSPORTER: uptake in OCT2A-expressing HEK293 cells2002Journal of the American Society of Nephrology : JASN, Jul, Volume: 13, Issue:7
cDNA cloning, functional characterization, and tissue distribution of an alternatively spliced variant of organic cation transporter hOCT2 predominantly expressed in the human kidney.
AID1442001Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Discovery of Competitive and Noncompetitive Ligands of the Organic Cation Transporter 1 (OCT1; SLC22A1).
AID26267Log distribution coefficient between 1-octanol and aqueous buffer at specified pH of 9.2.1983Journal of medicinal chemistry, Jan, Volume: 26, Issue:1
Bioisosteric design of conformationally restricted pyridyltriazole histamine H2-receptor antagonists.
AID681385TP_TRANSPORTER: RT-PCR in HK-2 cell2002Toxicology and applied pharmacology, Sep-01, Volume: 183, Issue:2
Influence of different chemicals on MDR-1 P-glycoprotein expression and activity in the HK-2 proximal tubular cell line.
AID236916Percentage of mass balance in hexadecane membranes model2005Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2
Exploring the role of different drug transport routes in permeability screening.
AID1133955Antiulcer activity in albino rat pyloric ligation model assessed as inhibition of gastric volume at 100 mg/kg, po administered as single dose 1 hr prior ligation relative to control1977Journal of medicinal chemistry, Apr, Volume: 20, Issue:4
Experimental antiulcer drugs. 1. Indole-1-alkanamides and pyrrole-1-alkanamides.
AID182438Percent inhibition of gastric antisecretory activity in the 4 hr pylorus-ligated rat to that of control at a dose of 100 mg/kg1983Journal of medicinal chemistry, Aug, Volume: 26, Issue:8
Pyridazinones. 3. Synthesis, antisecretory, and antiulcer activities of 2-cyanoguanidine derivatives.
AID88142Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.81987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Studies on the active molecular species of the H2 receptor antagonists cimetidine and mifentidine.
AID78011Anticholinergic activity in Guinea pig ileum with respect to acetylcholine was determined; ND means no data1987Journal of medicinal chemistry, May, Volume: 30, Issue:5
Antisecretory activity of human, dog, and rat metabolites of fenoctimine.
AID680362TP_TRANSPORTER: uptake in OCT1-expressing HeLa cells1998The Journal of pharmacology and experimental therapeutics, Jul, Volume: 286, Issue:1
Functional characterization of an organic cation transporter (hOCT1) in a transiently transfected human cell line (HeLa).
AID1209583Unbound drug partitioning coefficient, Kp of the compound assessed as ratio of unbound concentration in Sprague-Dawley rat brain to unbound concentration in plasma2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods.
AID1196045Cytotoxicity against human HepG2 cells assessed as disruption of membrane integrity up to 100 uM after 24 hrs by LDH release assay2015European journal of medicinal chemistry, Mar-06, Volume: 92Evaluating the risk of phospholipidosis using a new multidisciplinary pipeline approach.
AID29423HPLC capacity factor (k')2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID87703Histamine H2 receptor blocking activity was determined in the isolated guinea pig right atrium against histamine stimulated tachycardia1986Journal of medicinal chemistry, Jan, Volume: 29, Issue:1
Dipole moment in relation to H2 receptor histamine antagonist activity for cimetidine analogues.
AID27167Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID141953Percentage inhibition for muscarinic acetylcholine receptor at concentration 10 e-5M.1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Synthesis and antiulcer activity of 5,11-dihydro[1]benzoxepino[3,4-b]pyridines.
AID681141TP_TRANSPORTER: uptake in Xenopus laevis oocytes2001Molecular pharmacology, May, Volume: 59, Issue:5
Identification and characterization of human organic anion transporter 3 expressing predominantly in the kidney.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1149788Inhibition of histamine-induced gastric acid secretion in po dosed rat in ligated stomach preparation administered 1 hr prior to the ligation of the pylorus1977Journal of medicinal chemistry, Oct, Volume: 20, Issue:10
Compounds with gastric antisecretory activity. 1. Phenoxyalkylamines.
AID361986Lipophilicity, log D of compound at pH 7.4 by shake flask method2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Determination of log D via automated microfluidic liquid-liquid extraction.
AID692193Inhibition of human OCT2 A270S mutant expressed in HEK-293-Flp-In cells incubated for 3 mins by ASP+ substrate uptake assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2.
AID28235Unbound fraction (plasma)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID89556Evaluated for antagonist activity against histamine H3 receptor and represented as KB.1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
Histamine H3 ligands: just pharmacological tools or potential therapeutic agents?
AID404304Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control2008Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).
AID88011Antagonistic activity against histamine H2 receptor from guinea pig atrium, activity is expressed as KB (dissociation constant) at 10e-9 M1983Journal of medicinal chemistry, Jan, Volume: 26, Issue:1
Bioisosteric design of conformationally restricted pyridyltriazole histamine H2-receptor antagonists.
AID771315Cellular uptake in human HEK293 cells assessed as human OCT1-mediated drug transport at 2.5 uM after 4 mins by LC-MS/MS analysis relative to passive uptake2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Identification of novel substrates and structure-activity relationship of cellular uptake mediated by human organic cation transporters 1 and 2.
AID195484Antisecretory activity was evaluated in pylorus ligated rat after iv administration at 40 mg/kg of dose, expressed as reduction of gastric output1981Journal of medicinal chemistry, Aug, Volume: 24, Issue:8
Gastric antisecretory agents. 1. Antisecretory and antiulcer activity of 5H-[1]benzopyrano[2,3-b]pyridin-5-ylureas and 5H-[1]benzothiopyrano[2,3-b]pyridin-5-ylureas.
AID194626Inhibition of histamine stimulated gastric acid secretion in lumen perfused stomach of anesthetized rats at 1 mg/kg i.v. dose1999Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
Anti-Helicobacter pylori agents. 3. 2-[(Arylalkyl)guanidino]-4-furylthiazoles.
AID680339TP_TRANSPORTER: inhibition of PHA uptake (PHA: 5uM) in rOAT1-expressing S2 cells2004Journal of pharmacological sciences, Feb, Volume: 94, Issue:2
Interactions of human- and rat-organic anion transporters with pravastatin and cimetidine.
AID87882H2 receptor antagonistic activity against histamine stimulated chronotropic response in isolated guinea pig right atrium at 1x10E-6 g/mL.1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
Studies on antiulcer drugs. 7. 2-Guanidino-4-pyridylthiazoles as histamine H2-receptor antagonists with potent gastroprotective effects against nonsteroidal antiinflammatory drug-induced injury.
AID496828Antimicrobial activity against Leishmania donovani2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1221956Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID699540Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID467612Fraction unbound in human plasma2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID19468Partition coefficient (logP)2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID59672Effective dose on oral administration was evaluated for the inhibition of acid output in penta gastrin stimulated Heidenhain pouch dogs1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Bioisosteric prototype design of biaryl imidazolyl and triazolyl competitive histamine H2-receptor antagonists.
AID681711TP_TRANSPORTER: inhibition of Carnitine uptake (Carnitine: 0.025 uM, Cimetidine: 2000 uM) in OCTN2-expressing HRPE cells1999The Journal of pharmacology and experimental therapeutics, Sep, Volume: 290, Issue:3
Functional characteristics and tissue distribution pattern of organic cation transporter 2 (OCTN2), an organic cation/carnitine transporter.
AID60180Volume of histamine stimulated inhibition of gastric secretion when administered perorally in dogs1983Journal of medicinal chemistry, Apr, Volume: 26, Issue:4
Inhibitors of gastric acid secretion: antisecretory 2-pyridylurea derivatives.
AID1223575Inhibition of CYP3A4.18 (unknown origin)-mediated testosterone 6beta-hydroxylation incubated for 10 mins prior to NADPH addition measured after 20 mins by HPLC-UV analysis2011Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
Comparison of the inhibitory profiles of itraconazole and cimetidine in cytochrome P450 3A4 genetic variants.
AID59859Inhibition of gastric acid secretion in dogs stimulated by gastrin tetrapeptide when administered perorally1983Journal of medicinal chemistry, Nov, Volume: 26, Issue:11
A deuterium isotope effect on the inhibition of gastric secretion by N,N-dimethyl-N'-[2-(diisopropylamino)ethyl]-N'-(4,6-dimethyl-2-pyridyl)urea. Synthesis of metabolites.
AID28392Apparent permeability coefficient (Papp) (Caco-2 cell monolayer)2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
Experimental and computational screening models for the prediction of intestinal drug absorption.
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID28234% absorbed in human GI-tract2001Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6
High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes.
AID88019Histamine H2 receptor antagonistic activity was evaluated in guinea pig atrium.1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Bioisosteric prototype design of biaryl imidazolyl and triazolyl competitive histamine H2-receptor antagonists.
AID88010Antagonistic activity against histamine H2 receptor from guinea pig atrium1983Journal of medicinal chemistry, Jan, Volume: 26, Issue:1
Bioisosteric design of conformationally restricted pyridyltriazole histamine H2-receptor antagonists.
AID679826TP_TRANSPORTER: inhibition of TEA uptake (TEA: 100 uM) in Xenopus laevis oocytes1999Biochimica et biophysica acta, Mar-04, Volume: 1417, Issue:2
Molecular mechanisms of organic cation transport in OCT2-expressing Xenopus oocytes.
AID692185Cmax in human2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2.
AID54923Inhibition of human cytochrome P450 3A42003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID1221958Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID76425Inhibition of histamine stimulated chronotropic response in isolated guinea pig right atrium (1*10e-6 g/mL)2000Journal of medicinal chemistry, Aug-24, Volume: 43, Issue:17
Anti-Helicobacter pylori agents. 4. 2-(Substituted guanidino)-4-phenylthiazoles and some structurally rigid derivatives.
AID679358TP_TRANSPORTER: uptake in Xenopus laevis oocytes1999The Journal of biological chemistry, May-07, Volume: 274, Issue:19
Molecular cloning and characterization of a new multispecific organic anion transporter from rat brain.
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID59372Inhibition of acid output in pentagastrin-stimulated Heidenhain pouch dog at a dose 1(mg/kg) administered intravenously1985Journal of medicinal chemistry, Nov, Volume: 28, Issue:11
Pseudosymmetry and bioisosterism in biaryl pyridyl competitive histamine H2-receptor antagonists.
AID692196Inhibition of human MATE2-K expressed in HEK-293-Flp-In cells incubated for 3 mins by ASP+ substrate uptake assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2.
AID87707Evaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atrium1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Conformational requirements for histamine H2-receptor inhibitors: a structure-activity study of phenylene analogues related to cimetidine and tiotidine.
AID1264455Permeability of the compound by high throughput PAMPA method2015European journal of medicinal chemistry, Nov-13, Volume: 105Multicomponent reaction-based synthesis and biological evaluation of tricyclic heterofused quinolines with multi-trypanosomatid activity.
AID681419TP_TRANSPORTER: inhibition of Homovanillic acid uptake (HVA: 0.2 uM, Cimetidine: 1000 uM) in Xenopus laevis oocytes2003Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism, Apr, Volume: 23, Issue:4
Rat organic anion transporter 3 (rOAT3) is responsible for brain-to-blood efflux of homovanillic acid at the abluminal membrane of brain capillary endothelial cells.
AID1135360Ionization constant, pKa of the imidazole ring of the compound1977Journal of medicinal chemistry, Jul, Volume: 20, Issue:7
Cyanoguanidine-thiourea equivalence in the development of the histamine H2-receptor antagonist, cimetidine.
AID589084Mechanism based inhibition of human cytochrome P450 2C9 measured by S-warfarin and Tolbutamide as specific substrates2005Current drug metabolism, Oct, Volume: 6, Issue:5
Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.
AID681590TP_TRANSPORTER: inhibition of TEA uptake (basolateral to cell) in OCT2-expressing MDCK cells1998The Journal of pharmacology and experimental therapeutics, Nov, Volume: 287, Issue:2
Functional characteristics and membrane localization of rat multispecific organic cation transporters, OCT1 and OCT2, mediating tubular secretion of cationic drugs.
AID678794TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 1 uM) in Xenopus laevis oocytes2002Biochemical and biophysical research communications, Aug-23, Volume: 296, Issue:3
Functional characterization of mouse cation transporter mOCT2 compared with mOCT1.
AID681996TP_TRANSPORTER: inhibition of TEA uptake (TEA: 5 uM, Cimetidine: 1000 uM) in OCT2A-expressing HEK293 cells2002Journal of the American Society of Nephrology : JASN, Jul, Volume: 13, Issue:7
cDNA cloning, functional characterization, and tissue distribution of an alternatively spliced variant of organic cation transporter hOCT2 predominantly expressed in the human kidney.
AID231715Ratio between gastric emptying (GE) and acute gastric fistula (AGF)1983Journal of medicinal chemistry, Apr, Volume: 26, Issue:4
4-(Diphenylmethyl)-1-[(imino)methyl]piperidines as gastric antisecretory agents.
AID361985Lipophilicity, log D of compound at pH 7.4 by microfluidic liquid-liquid extraction method2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Determination of log D via automated microfluidic liquid-liquid extraction.
AID681146TP_TRANSPORTER: inhibition of TEA uptake in OCT1-expressing HeLa cells1998The Journal of pharmacology and experimental therapeutics, Jul, Volume: 286, Issue:1
Functional characterization of an organic cation transporter (hOCT1) in a transiently transfected human cell line (HeLa).
AID87697In vitro Histamine H2 receptor antagonist activity in the histamine-stimulated guinea pig right atrium1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Development of a new physicochemical model for brain penetration and its application to the design of centrally acting H2 receptor histamine antagonists.
AID25363Compound was evaluated for the ionization constant (pKa) by using potentiometric titration (ionization of imidazole group)1984Journal of medicinal chemistry, Mar, Volume: 27, Issue:3
(Imidazolylphenyl)formamidines. A structurally novel class of potent histamine H2 receptor antagonists.
AID681997TP_TRANSPORTER: inhibition of TEA uptake (TEA: 5 uM, Cimetidine: 1000 uM) in OCT2-expressing HEK293 cells2002Journal of the American Society of Nephrology : JASN, Jul, Volume: 13, Issue:7
cDNA cloning, functional characterization, and tissue distribution of an alternatively spliced variant of organic cation transporter hOCT2 predominantly expressed in the human kidney.
AID236912Permeability Coefficient in 2/4/A1 cell model2005Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2
Exploring the role of different drug transport routes in permeability screening.
AID185121Inhibition of stress-induced ulcer formation in rats by 10 mg/kg p.o. administration.1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Synthesis and antiulcer activity of 5,11-dihydro[1]benzoxepino[3,4-b]pyridines.
AID496832Antimicrobial activity against Trypanosoma brucei rhodesiense2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID176449Percent inhibition of gastric antisecretory activity in the pylorus-ligated rat at a dose of 100 mg/kg administered intraduodenally1982Journal of medicinal chemistry, Aug, Volume: 25, Issue:8
Pyridazinones. 1. Synthesis and antisecretory and antiulcer activities of thio amide derivatives.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1442002Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of YM155 after 1 min2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Discovery of Competitive and Noncompetitive Ligands of the Organic Cation Transporter 1 (OCT1; SLC22A1).
AID588208Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset2010Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5
Predicting phospholipidosis using machine learning.
AID60214Compound was evaluated for the inhibition of gastrin-stimulated gastric acid secretion in conscious heidenhain pouch dogs when administered 1 mg/kg perorally1998Bioorganic & medicinal chemistry letters, Jun-02, Volume: 8, Issue:11
Anti-Helicobacter pylori agents. 2. Structure activity relationships in a new series of 2-alkylguanidino-4-furylthiazoles.
AID88156Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium2003Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
Synthesis and pharmacological activity of fluorescent histamine H2 receptor antagonists related to potentidine.
AID60392Histamine-stimulated gastric acid secretion in Heidenhain pouch dog at 1uM/Kg, on iv administration of the compound1995Journal of medicinal chemistry, Jul-07, Volume: 38, Issue:14
Reversible inhibitors of the gastric (H+/K+)-ATPase. 5. Substituted 2,4-diaminoquinazolines and thienopyrimidines.
AID178846Antisecretory activity against acute gastric fistula (AGF) in rat when administered perorally; value ranges from 5.7-10.81983Journal of medicinal chemistry, Apr, Volume: 26, Issue:4
4-(Diphenylmethyl)-1-[(imino)methyl]piperidines as gastric antisecretory agents.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID588991Inhibitors of transporters of clinical importance in the absorption and disposition of drugs, MATE12010Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
Membrane transporters in drug development.
AID1713986Effective permeability of the compound in PBS/ethanol buffer (9:1) at 25 ug/ml after 10 hrs by UV plate reader based PAMPA-BBB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Multitarget-directed oxoisoaporphine derivatives: Anti-acetylcholinesterase, anti-β-amyloid aggregation and enhanced autophagy activity against Alzheimer's disease.
AID225128Antiulcer activity in male Wistar rats for 50% inhibition of stress induced gastric lesions after peroral administration.1982Journal of medicinal chemistry, Aug, Volume: 25, Issue:8
Pyridazinones. 1. Synthesis and antisecretory and antiulcer activities of thio amide derivatives.
AID680368TP_TRANSPORTER: inhibition of TEA uptake in OCT2 expressing oocytes2004European journal of pharmacology, Oct-25, Volume: 503, Issue:1-3
Different transport properties between famotidine and cimetidine by human renal organic ion transporters (SLC22A).
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID496819Antimicrobial activity against Plasmodium falciparum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID476929Human intestinal absorption in po dosed human2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
Neural computational prediction of oral drug absorption based on CODES 2D descriptors.
AID692187Therapeutic index, ratio of Cmax in human to IC50 for human MATE12011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2.
AID1221961Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1739430Apparent permeability across apical to basolateral side in human Caco-2 cells at 10 uM incubated for 2 hrs LC-MS/MS analysis2020European journal of medicinal chemistry, Aug-15, Volume: 200Substituted benzothiophene and benzofuran derivatives as a novel class of bone morphogenetic Protein-2 upregulators: Synthesis, anti-osteoporosis efficacies in ovariectomized rats and a zebrafish model, and ADME properties.
AID680330TP_TRANSPORTER: uptake in OCT3-expressing HEK293 cells1999Molecular pharmacology, Jul, Volume: 56, Issue:1
Selective substrates for non-neuronal monoamine transporters.
AID87945Evaluated for antimicrobial activity against Helicobacter pylori1997Journal of medicinal chemistry, Aug-01, Volume: 40, Issue:16
Anti-Helicobacter pylori agents. 1. 2-(Alkylguanidino)-4-furylthiazoles and related compounds.
AID177911Inhibition of gastric acid secretion in the pylorus-ligated rat (after 2h)1982Journal of medicinal chemistry, Mar, Volume: 25, Issue:3
1,2,5-thiadiazole 1-oxide and 1,1-dioxide derivatives. A new class of potent histamine H2-receptor antagonists.
AID223858Antisecretory activity at 16 mg/kg dose administered intraduodenally in the pylorus-ligated rat was determined and value given as total acid output(TAO) as % of control1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
2-Oxo-1,8-naphthyridine-3-carboxylic acid derivatives with potent gastric antisecretory properties.
AID681128TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID625277FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of less concern for DILI2011Drug discovery today, Aug, Volume: 16, Issue:15-16
FDA-approved drug labeling for the study of drug-induced liver injury.
AID699539Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID60987Inhibition of acid output in dogs (iv)1982Journal of medicinal chemistry, Mar, Volume: 25, Issue:3
Inhibitors of gastric acid secretion: 3,4-diamino-1,2,5-thiadiazole 1-oxides and 1,1-dioxides as urea equivalents in a series of histamine H2-receptor antagonists.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID150753Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID59358The intraperitoneal dose of cimetidine that produced a 50% inhibition of the 4-h acid output in the pylorus-ligated rat1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
Antiulcer agents. 2. Gastric antisecretory, cytoprotective, and metabolic properties of substituted imidazo[1,2-a]pyridines and analogues.
AID228172Inhibition of histamine-stimulated gastric acid secretion in lumen-perfused stomach of anesthetized rats after 1 mg/kg iv administration2002Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
Anti-Helicobacter pylori agents. 5. 2-(Substituted guanidino)-4-arylthiazoles and aryloxazole analogues.
AID26825Acid dissociation constant was determined for the compound; ND means no data.1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Studies on the active molecular species of the H2 receptor antagonists cimetidine and mifentidine.
AID692189Therapeutic index, ratio of Cmax in human to IC50 for human OCT2 A270S mutant2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2.
AID1196043Cytotoxicity against human HepG2 cells assessed as reduction in cell viability at 0.1 to 100 uM after 24 hrs by Neutral red uptake assay2015European journal of medicinal chemistry, Mar-06, Volume: 92Evaluating the risk of phospholipidosis using a new multidisciplinary pipeline approach.
AID150758P-gp activity was measured by a direct transport assay, using polarized LLC-PK1 epithelial cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID176750Dose required to inhibit gastric secretory activity in pylorus lygated rats1983Journal of medicinal chemistry, Mar, Volume: 26, Issue:3
Pyridazinones. 2. Synthesis and antisecretory and antiulcer activities of thiourea and 2-cyanoguanidine derivatives.
AID680960TP_TRANSPORTER: inhibition of TEA uptake (TEA: 20 uM, Cimetidine: 5000 uM) in OCT3-expressing HRPE cells2000American journal of physiology. Renal physiology, Sep, Volume: 279, Issue:3
Structure, function, and regional distribution of the organic cation transporter OCT3 in the kidney.
AID680502TP_TRANSPORTER: inhibition of Doxorubicin transepithelial transport (basal to apical)(Doxorubicin: 3 uM, Cimetidine: 50 uM) in MDR1-expressing LLC-PK1 cells2000European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, Sep, Volume: 11, Issue:3
Specificity of doxorubicin versus rhodamine-123 in assessing P-glycoprotein functionality in the LLC-PK1, LLC-PK1:MDR1 and Caco-2 cell lines.
AID409954Inhibition of mouse brain MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID1443980Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch2010Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
AID230084Ratio of number of determinations at pH 7.4 to pH 7.01987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Studies on the active molecular species of the H2 receptor antagonists cimetidine and mifentidine.
AID60000Inhibition of histamine stimulated gastric acid secretion was tested in heidenhain pouch dog upon oral administration1992Journal of medicinal chemistry, Sep-04, Volume: 35, Issue:18
Reversible inhibitors of the gastric (H+/K+)-ATPase. 3. 3-substituted-4-(phenylamino)quinolines.
AID24179logBB, log(C brain/C blood)1996Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24
Computation of brain-blood partitioning of organic solutes via free energy calculations.
AID678713Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID624629Inhibition of Pgp expressed in MDR1-MDCKII cells measured by calcein-AM assay2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID26616Acid dissociation constant was determined for the compound1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Studies on the active molecular species of the H2 receptor antagonists cimetidine and mifentidine.
AID678712Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID681679TP_TRANSPORTER: inhibition of Carnitine uptake (Carnitine: 0.010? uM, Cimetidine: 500 uM) in OCTN2-expressing HEK293 cells1999The Journal of pharmacology and experimental therapeutics, Nov, Volume: 291, Issue:2
Na(+)-dependent carnitine transport by organic cation transporter (OCTN2): its pharmacological and toxicological relevance.
AID386623Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
AID681574TP_TRANSPORTER: inhibition of TEA uptake (basolateral to cell) in OCT1-expressing MDCK cells1998The Journal of pharmacology and experimental therapeutics, Nov, Volume: 287, Issue:2
Functional characteristics and membrane localization of rat multispecific organic cation transporters, OCT1 and OCT2, mediating tubular secretion of cationic drugs.
AID771317Cellular uptake in human HEK293 cells assessed as human OCT1-mediated drug transport at 2.5 uM after 4 mins by LC-MS/MS analysis2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Identification of novel substrates and structure-activity relationship of cellular uptake mediated by human organic cation transporters 1 and 2.
AID59661Effective dose administarted perorally required for 50 % inhibition of acid output in dogs1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Conformational requirements for histamine H2-receptor inhibitors: a structure-activity study of phenylene analogues related to cimetidine and tiotidine.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID205268Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 10 uM1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID1196049Cytotoxicity against human HepG2 cells assessed as NBD-PC phospholipid accumulation at 0.1 to 100 uM after 24 hrs by Hoechst 33342 normalization-based fluorescence assay2015European journal of medicinal chemistry, Mar-06, Volume: 92Evaluating the risk of phospholipidosis using a new multidisciplinary pipeline approach.
AID588209Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset2010Chemical research in toxicology, Jul-19, Volume: 23, Issue:7
Developing structure-activity relationships for the prediction of hepatotoxicity.
AID771800Gastroprotective activity in Wistar rat assessed as inhibition of HCl/ethanol-induced gastric ulcer at 100 mg/kg, ip administered 30 mins prior to HCl/ethanol challenge measured after 1 hr relative to vehicle-treated control
AID678715Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID497005Antimicrobial activity against Pneumocystis carinii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID624623Apparent permeability (Papp) from basolateral to apical side determined in MDR1-MDCKII cells2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID184316Inhibition of histamine-stimulated gastric acid secretion in lumen-perfused stomach of the anaesthetized rats when administered 1 mg/kg intravenously1998Bioorganic & medicinal chemistry letters, Jun-02, Volume: 8, Issue:11
Anti-Helicobacter pylori agents. 2. Structure activity relationships in a new series of 2-alkylguanidino-4-furylthiazoles.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID59311Acid output of histamine stimulated inhibition of gastric secretion when administered perorally in dogs1983Journal of medicinal chemistry, Apr, Volume: 26, Issue:4
Inhibitors of gastric acid secretion: antisecretory 2-pyridylurea derivatives.
AID28681Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID496829Antimicrobial activity against Leishmania infantum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID679294TP_TRANSPORTER: inhibition of TEA uptake (apical to cell) in OCT2-expressing NIH3T3 cells1999Toxicological sciences : an official journal of the Society of Toxicology, Feb, Volume: 47, Issue:2
A transfected cell model for the renal toxin transporter, rOCT2.
AID1135357Antagonist at histamine H2 receptor in guinea pig atrium assessed as inhibition of histamine-induced response1977Journal of medicinal chemistry, Jul, Volume: 20, Issue:7
Cyanoguanidine-thiourea equivalence in the development of the histamine H2-receptor antagonist, cimetidine.
AID414580Apparent permeability from basolateral to apical side of human Caco-2 cells2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Novel peptidomimetics containing a vinyl ester moiety as highly potent and selective falcipain-2 inhibitors.
AID1129361Unbound fraction in HEK293 cell homogenate at 0.1 uM by equilibrium dialysis based UPLC-MS/MS analysis2014Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7
A high-throughput cell-based method to predict the unbound drug fraction in the brain.
AID678714Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID681168TP_TRANSPORTER: uptake in Oat3-expressing oocyte cells2004The Journal of pharmacology and experimental therapeutics, Jun, Volume: 309, Issue:3
Mouse reduced in osteosclerosis transporter functions as an organic anion transporter 3 and is localized at abluminal membrane of blood-brain barrier.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID410341Inhibition of water-immersion stress-induced ulcer formation in rat at 30 mg/kg2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Possible involvement of radical intermediates in the inhibition of cysteine proteases by allenyl esters and amides.
AID178922Effective dose required for gastric antisecretory activity in the pylorus-ligated rat after intraduodenal administration.1982Journal of medicinal chemistry, Aug, Volume: 25, Issue:8
Pyridazinones. 1. Synthesis and antisecretory and antiulcer activities of thio amide derivatives.
AID87705In vitro inhibition of Histamine H2 receptor by measuring its ability to block dimaprit-stimulated chronotropic response of guinea pig atrium strips1982Journal of medicinal chemistry, Mar, Volume: 25, Issue:3
Inhibitors of gastric acid secretion: 3,4-diamino-1,2,5-thiadiazole 1-oxides and 1,1-dioxides as urea equivalents in a series of histamine H2-receptor antagonists.
AID679633TP_TRANSPORTER: inhibition of PCG uptake in OAT3-expressing LLC-PK1 cells2002Molecular pharmacology, May, Volume: 61, Issue:5
Expression and functional characterization of rat organic anion transporter 3 (rOat3) in the choroid plexus.
AID566261Inhibition of guinea pig histamine H2 receptor2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: de
AID692190Partial inhibition of human OCT2 expressed in HEK-293-Flp-In cells at 20 uM incubated for 3 mins by ASP+ substrate uptake assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2.
AID1173449Effective permeability of the compound by PAMPA assay2014Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
Synthesis and antiprotozoal activity of oligomethylene- and p-phenylene-bis(methylene)-linked bis(+)-huprines.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID725596inhibition of human PAD4 preincubated at 10 uM for 15 mins before substrate addition measured after 20 mins by spectrophotometry2013Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3
Novel small molecule protein arginine deiminase 4 (PAD4) inhibitors.
AID679537TP_TRANSPORTER: inhibition of Ochratoxin A uptake (OTA: 1 uM, Cimetidine: 200 uM) in OAT1-expressing S2 cells2001Life sciences, Sep-21, Volume: 69, Issue:18
Characterization of ochratoxin A transport by human organic anion transporters.
AID771314Cellular uptake in human HEK293 cells assessed as human OCT2-mediated drug transport at 2.5 uM after 4 mins by LC-MS/MS analysis relative to passive uptake2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Identification of novel substrates and structure-activity relationship of cellular uptake mediated by human organic cation transporters 1 and 2.
AID21234Partition coefficient of compound in to octanol/buffer1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Reevaluating equilibrium and kinetic binding parameters for lipophilic drugs based on a structural model for drug interaction with biological membranes.
AID496820Antimicrobial activity against Trypanosoma brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID311524Oral bioavailability in human2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Hologram QSAR model for the prediction of human oral bioavailability.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID681119TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID150756Inhibition of P-gp was determined using rhodamine-assay in human CaCo-2 cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID188520Antiulcer activity against restraint-induced gastric erosions in rats, following 100 mg/kg p.o. administration.1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Synthesis and antisecretory and antiulcer activities of derivatives and analogues of 2-(2-pyridyl)tetrahydrothiophene-2-carbothioamide.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID88151In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.1992Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13
Synthesis and antiulcer activity of N-substituted N'-[3-[3-(piperidinomethyl)phenoxy]propyl]ureas: histamine H2-receptor antagonists with a potent mucosal protective activity.
AID7783Unbound fraction (plasma)2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID692194Inhibition of human OCT1 expressed in HEK-293-Flp-In cells incubated for 3 mins by ASP+ substrate uptake assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2.
AID496831Antimicrobial activity against Cryptosporidium parvum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID28679Partition coefficient (logD6.8)2001Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6
High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes.
AID496823Antimicrobial activity against Trichomonas vaginalis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1223490Apparent permeability across human differentiated Caco2 cells2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Predicting phenolic acid absorption in Caco-2 cells: a theoretical permeability model and mechanistic study.
AID1713987Effective permeability of the compound at 25 ug/ml after 18 hrs by UV plate reader based PAMPA-BBB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Multitarget-directed oxoisoaporphine derivatives: Anti-acetylcholinesterase, anti-β-amyloid aggregation and enhanced autophagy activity against Alzheimer's disease.
AID588210Human drug-induced liver injury (DILI) modelling dataset from Ekins et al2010Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12
A predictive ligand-based Bayesian model for human drug-induced liver injury.
AID481440Dissociation constant, pKa of the compound2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID59310Acid output of gastrin tetrapeptide stimulated inhibition of gastric secretion when administered perorally in dogs1983Journal of medicinal chemistry, Apr, Volume: 26, Issue:4
Inhibitors of gastric acid secretion: antisecretory 2-pyridylurea derivatives.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID223860Antisecretory activity at 4 mg/kg dose administered intraduodenally in the pylorus-ligated rat was determined and value given as total acid output(TAO) as % of control1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
2-Oxo-1,8-naphthyridine-3-carboxylic acid derivatives with potent gastric antisecretory properties.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1798265H4R Radioligand Binding Assay from Article 10.1124/jpet.105.087965: \\Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.\\2005The Journal of pharmacology and experimental therapeutics, Sep, Volume: 314, Issue:3
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.
AID1345181Human Plasma membrane monoamine transporter (SLC29 family)2016Clinical pharmacology and therapeutics, Nov, Volume: 100, Issue:5
The plasma membrane monoamine transporter (PMAT): Structure, function, and role in organic cation disposition.
AID1346095Human H2 receptor (Histamine receptors)2013European journal of medicinal chemistry, May, Volume: 63Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.
AID1345181Human Plasma membrane monoamine transporter (SLC29 family)2005Molecular pharmacology, Nov, Volume: 68, Issue:5
Interaction of organic cations with a newly identified plasma membrane monoamine transporter.
AID1346133Rat H2 receptor (Histamine receptors)1997British journal of pharmacology, Nov, Volume: 122, Issue:5
Heterologous expression of rat epitope-tagged histamine H2 receptors in insect Sf9 cells.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8,840)

TimeframeStudies, This Drug (%)All Drugs %
pre-19905840 (66.06)18.7374
1990's1809 (20.46)18.2507
2000's735 (8.31)29.6817
2010's370 (4.19)24.3611
2020's86 (0.97)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 98.90

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 Index98.90 (24.57)
Research Supply Index9.32 (2.92)
Research Growth Index4.15 (4.65)
Search Engine Demand Index189.53 (26.88)
Search Engine Supply Index2.02 (0.95)

This Compound (98.90)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1,687 (17.81%)5.53%
Reviews542 (5.72%)6.00%
Case Studies904 (9.54%)4.05%
Observational1 (0.01%)0.25%
Other6,339 (66.92%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (63)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Persona® Ti-Nidium® Personalized Total Knee System A Post-Market Clinical Follow-up Study to Provide Safety, Performance and Clinical Benefits Data Using the Persona Ti-Nidium Total Knee System and Instrumentation [NCT04817969]240 participants (Anticipated)Interventional2021-06-01Recruiting
Comparison of in Vivo Kinematics of Different Implants in ACL-sacrificing vs. Medially Stabilized Arthroplasty (Implant Design Study) [NCT02965690]26 participants (Actual)Interventional2016-11-30Active, not recruiting
Airway Intervention Registry (AIR) Extension: Recurrent Respiratory Papillomatosis [NCT03465280]400 participants (Anticipated)Observational [Patient Registry]2018-04-01Recruiting
Metal-metal Articulations vs Standard 28 mm Cementless Total Hip Arthroplasty in Younger Patients. Randomized Studies [NCT01113762]Phase 271 participants (Actual)Interventional2007-02-28Active, not recruiting
An Open-label, One-sequence Study to Assess the Effect of Repeated Oral Doses of Cimetidine on the Single Dose Pharmacokinetics, Safety and Tolerability of Imeglimin in Healthy Caucasian Subjects [NCT03618316]Phase 116 participants (Actual)Interventional2018-06-19Completed
A Pharmacokinetic, Multi-cohort Study in Healthy Adult Subjects to Assess Gepotidacin as Victim and as Perpetrator of Drug-Drug Interactions Via CYP450, Renal and Intestinal Transporters, and to Assess Gepotidacin Pharmacokinetics in Japanese Healthy Adul [NCT04493931]Phase 164 participants (Actual)Interventional2020-08-14Completed
Postpartum Activity and Expression of BCRP and OCT1 Drug Transporters in the Mammary Gland [NCT06056583]Phase 450 participants (Anticipated)Interventional2024-01-15Recruiting
The Effect of Concomitant Cimetidine p.o. 400 mg t.i.d. and p.o. Ranitidine 300 mg Once Daily on Single Dose Pharmacokinetics of Tiotropium (14.4 µg) Given Intravenously Over 15 Minutes in Healthy Male and Female Subjects of 50-65 Years (Randomized, Open [NCT02172417]Phase 118 participants (Actual)Interventional2000-07-31Completed
The Effect of Implant Coating With Hydroxyapatite Deposited Electrochemically (BoneMaster) on Migration and Clinical Outcome in Hip Arthroplasty With the Exceed Cup [NCT02311179]56 participants (Actual)Interventional2013-01-31Active, not recruiting
Oxford Partial Knee Replacement: A Randomized Clinical Trial of Three Implant Types. [NCT00679120]75 participants (Anticipated)Interventional2009-05-31Active, not recruiting
The Efficacy of Cimetidin for Acute - Extrinsic Atopic Dermatitis Treated With Standard Therapy, a Study of Immunoglobulin E, Interleukin-4, Interleukin-12, and Interferon-Ɣ Serum Levels [NCT04018131]Phase 326 participants (Anticipated)Interventional2018-03-26Recruiting
Effect of Repeated Oral Doses of BI 1060469, BI 1021958 and Active Controls, Cimetidine and Naproxen, on Measured GFR Via Renal Clearance of Iohexol in Healthy Male Subjects (a Phase I Study; Single-blind, Randomized, Placebo-controlled Within BI Groups a [NCT02202512]Phase 153 participants (Actual)Interventional2014-09-30Completed
An Open-label Phase I Study to Evaluate the Drug-drug Interaction of HSK16149 Capsule With Probenecid Tablets or Cimetidine Tablets in Healthy Subjects [NCT05881811]Phase 147 participants (Actual)Interventional2023-03-20Completed
Open-label, Randomized, Single Dose, 2-sequence, 2-period Cross-over Study to Investigate the Effect of Inhibition of the Organic Cation Transport in the Kidneys by Cimetidine on the Pharmacokinetics of the CHF5993 in Healthy Volunteers [NCT02287272]Phase 125 participants (Actual)Interventional2014-05-31Completed
A Multicenter Prospective Cohort Study on Persona Total Knee System [NCT03495232]700 participants (Anticipated)Observational2016-11-01Recruiting
A Multicenter Prospective Randomized Control Study on Persona Total Knee System vs NexGen Total Knee System in Total Knee Arthroplasty [NCT03073941]314 participants (Actual)Interventional2016-12-31Active, not recruiting
A Single-center, Open-label Study to Investigate the Effect of Cimetidine on the Pharmacokinetics of Lucerastat in Healthy Male Subjects [NCT03380455]Phase 114 participants (Actual)Interventional2018-01-09Completed
Post-market Clinical Follow-up Study to Provide Safety, Performance and Clinical Benefits Data of the Biomet Cannulated Bone Screw System (Implants and Instrumentation) - A Retrospective/Prospective Study [NCT04002518]300 participants (Anticipated)Observational2019-08-07Enrolling by invitation
ExploR™ Modular Radial Head Data Collection [NCT00521846]50 participants (Anticipated)Observational2007-08-31Active, not recruiting
A Phase II Study: Paclitaxel and Pelvic Radiation for Stage I-IIIA Papillary Serous Carcinoma of the Endometrium [NCT00515073]Phase 230 participants (Actual)Interventional2001-04-30Completed
Evaluation of Excipient Effects on Biopharmaceuticals Classification System (BCS) Class 3 Drug Cimetidine [NCT01256879]Phase 425 participants (Actual)Interventional2011-03-31Completed
Randomized Comparison Between the Fitmore and the CLS Stem in Patients Operated in One-stage Due to Bilateral Symptomatous Hip Disease [NCT03112785]44 participants (Actual)Interventional2011-03-17Active, not recruiting
Success Rate of Immediately Loaded Implants With Platform Switched Design Placed in the Anterior Part of the Mandible and Restored With Fixed Prostheses: a Randomized, Split-mouth, Masked, Prospective, Open, Comparison, Monocenter Trial [NCT00780273]Phase 419 participants (Actual)Interventional2008-09-30Completed
"Effect of Orally Administered Two Successive Doses of PPIs and/ or H2RAs Without or With a Prokinetic Drug, on the Intragastric pH and Volume and Bile Refluxate in Adults Patients Undergoing Elective Surgery." [NCT02703896]Phase 41,920 participants (Actual)Interventional2012-01-31Completed
A Migration and Bone Density Study Comparing Refobacin Bone Cement R vs. Refobacin Plus Bone Cement in the OptiPac Bone Cement Mixing System. A Prospective Randomized Study on Primary Total Knee Arthroplasty [NCT00678236]54 participants (Actual)Interventional2008-06-30Completed
Whole Blood Metal Ion Concentrations in Metal-on-metal Total Hip Arthroplasty and Hip Resurfacing - A Randomized Controlled Trial With 5-years Follow up Including 75 Patients [NCT04585022]75 participants (Actual)Interventional2006-11-01Terminated(stopped due to High early failure rates and adverse reactions in similar devices)
Patient Reported Outcome After Stemmed Versus Stemless Total Shoulder Arthroplasty for Glenohumeral Osteoarthritis: a Patient Blinded Randomized Clinical Trial [NCT03877315]78 participants (Anticipated)Interventional2019-08-01Active, not recruiting
Survivibility of the Total Temporomandibular Joint Replacement System [NCT00762944]93 participants (Actual)Observational2005-09-21Completed
Effect of Oral Cimetidine in the Protoporphyrias [NCT05020184]Phase 220 participants (Anticipated)Interventional2022-06-14Recruiting
Proton Pump Inhibitors and the Risk of Hospitalization for Community-acquired Pneumonia: Replicated Cohort Studies With Meta-analysis [NCT02555852]4,238,504 participants (Actual)Observational2011-09-30Completed
Healing Response if Peri-implant Tissues to Different Abutment Materials - Double-blinded Randomized Clinical Trial [NCT01961635]60 participants (Actual)Interventional2016-01-31Completed
Marginal Bone Behavior of Dental Implants to Different Rehabilitation Protocols [NCT01971268]50 participants (Anticipated)Observational2014-01-31Not yet recruiting
A Phase 1, Open-Label, Randomized, Cross-Over Study To Estimate The Effects Of Steady-State Cimetidine On The Pharmacokinetics Of A Single Dose Of PD 0332334 In Healthy Subjects [NCT00800280]Phase 112 participants (Actual)Interventional2009-01-31Terminated(stopped due to Please see Detailed Description for termination reason.)
Effectiveness of Using Closed-suction Drainage in Treating Proximal Femur Fracture With Cephalomedullary Nail [NCT04229212]60 participants (Actual)Interventional2018-12-11Completed
Pharmacokinetic Drug-Drug Interaction Study to Identify Biomarkers of Kidney Transporters [NCT05365451]Early Phase 132 participants (Actual)Interventional2022-04-11Completed
Evaluation of Biopharmaceutics Classification System Class 3 Drugs for Possible Biowaivers [NCT01010698]Phase 148 participants (Actual)Interventional2009-06-30Completed
Performance of Cimetidine-corrected MDRD Equation in Renal Transplant Patients [NCT00475059]59 participants (Actual)Interventional2007-03-31Completed
Postoperative Function Following Partial and Total Knee Replacement [NCT00492219]324 participants (Anticipated)Interventional2006-10-31Terminated(stopped due to No longer have access to equipment used for functional data collection)
A Comparison of Two Total Hip Replacements: Hip Resurfacing System Versus Mallory-Head/Exeter [NCT00116948]Phase 450 participants (Anticipated)Interventional2005-01-31Completed
An Open-Label Study to Assess the Effect of Cimetidine on the Pharmacokinetics of Dexpramipexole (BIIB050) in Healthy Volunteers [NCT01536249]Phase 114 participants (Actual)Interventional2012-03-31Completed
Safety & Efficacy of Omeprazole Sodium Bicarbonate for the Prevention of Upper GI Bleeding in the Critically Ill [NCT00045799]Phase 3354 participants (Actual)Interventional2002-05-31Completed
Direct Anterior Versus Posterior Total Hip Arthroplasty Surgical Approaches [NCT01807494]60 participants (Anticipated)Interventional2012-11-30Active, not recruiting
Patient-specific Positioning Guides (PSPG) Technique Versus Conventional Technique in Total Knee Arthroplasty - a Prospective Randomized Study. [NCT01696552]109 participants (Anticipated)Interventional2011-09-30Active, not recruiting
Safely Stopping Pre-Medications in Patients Receiving Paclitaxel: A Randomized Trial [NCT04862585]Phase 2/Phase 3100 participants (Anticipated)Interventional2021-10-07Recruiting
ALPHA INTERFERON, TUMOR INFILTRATING LYMPHOCYTES, AND INTERLEUKIN-2 IN THE TREATMENT OF CANCER [NCT00002733]Phase 230 participants (Anticipated)Interventional1996-01-31Completed
A Multi-center, Randomised, Double-blind, Parallel-group Phase III Study to Assess High Dose Esomeprazole Na i.v. Treatment (Bolus Infusion of 80 mg Followed by a Continuous Infusion of 8 mg Per Hour Administered for 72 Hours) for Prevention of Rebleeding [NCT01757275]Phase 3239 participants (Actual)Interventional2013-02-28Completed
A Study to Evaluate the Effect of Cimetidine on CD4 Lymphocyte Counts in HIV Infection [NCT00002092]0 participants InterventionalCompleted
The Effect of Potent Inhibitors of Drug Transporters (Verapamil, Rifampin, Cimetidine, Probenecid) on Pharmacokinetics of a Transporter Probe Drug Cocktail Consisting of Digoxin, Furosemide, Metformin and Rosuvastatin (an Open-label, Randomised, Crossover [NCT03307252]Phase 145 participants (Actual)Interventional2017-10-25Completed
Effect of Histamine 2 Receptor Antagonist (H2RA) and Proton Pump Inhibitor (PPI) on the Positivity Rates and Clinical Outcomes of Coronavirus Disease-19 (COVID-19). [NCT04834752]400,000 participants (Anticipated)Observational2021-05-01Not yet recruiting
In Vivo Determination of Knee Kinematics for Subjects Having a Zimmer-Biomet Persona PCR or PS TKA [NCT04103515]50 participants (Actual)Observational2019-01-03Completed
Peri-implant Health of Dental Implants in the Posterior Region; an Evaluation After 10 Years [NCT05650099]126 participants (Actual)Observational [Patient Registry]2022-10-06Completed
The Effect of Immediate Implant Placement and Provisionalization in The Esthetic Zone: A Randomized Clinical Trial [NCT02021331]5 participants (Actual)Interventional2012-12-31Terminated(stopped due to Low enrollment so sponsor stopped funding the study (did not renew))
Clinical and Histological Evaluation of Demineralized Bone Allograft and Lyophilized Equine Bone Allograft for Sinus Lift: Double Blind, Parallel, Randomized Clinical Trial. [NCT02865590]16 participants (Actual)Interventional2011-06-30Completed
Gait Analysis of a Lateral-Pivot Design Total Knee Replacement [NCT04275362]102 participants (Anticipated)Observational2017-02-02Recruiting
Effect of Intravenous Esomeprazole Versus Cimetidine in Prevention of Stress Ulcer Prophylaxis in Chinese Seriously Ill Patients - a Randomized, Double-blind, Parallel-group Study [NCT02157376]Phase 3343 participants (Actual)Interventional2014-07-31Completed
The Incidence of Anterior Knee Pain Between Unisex Knee Prosthesis and Gender Specific Knee Prosthesis Following Minimally Invasive Surgery Total Knee Arthroplasty: A Randomized Controlled Trial [NCT05045651]80 participants (Actual)Interventional2014-08-01Completed
Comprehensive Reverse Shoulder Clinical Outcomes Study [NCT03404778]175 participants (Anticipated)Observational2010-03-07Enrolling by invitation
Comparison of Unconstrained and Semi-constrained Artificial Disc Implants Used in Cervical Disc Arthroplasty [NCT05701059]20 participants (Anticipated)Observational2023-02-01Not yet recruiting
Randomized Control Trial Comparing Zimmer Biomet Persona Medial Congruent Versus Posterior Stabilized Total Knee Arthroplasty for Treatment of Knee Arthritis Using the ROSA Knee System [NCT05391828]200 participants (Anticipated)Interventional2023-09-27Recruiting
PPK: A Functional and Clinical Comparison of a Partial and Total Knee Replacement [NCT04913987]50 participants (Anticipated)Interventional2021-04-26Enrolling by invitation
Cemented Versus Uncemented Arthroplasty in Elderly Patients With Displaced Femoral Neck Fractures: a Randomized Controlled Trial [NCT01798472]Phase 2/Phase 3140 participants (Anticipated)Interventional2009-11-30Recruiting
Comprehensive Shoulder System Database Retrieval [NCT03409718]160 participants (Actual)Observational [Patient Registry]2011-02-24Active, not recruiting
A Clinical Registry to Collect Patient Outcome Data for the BIOMET® EBI Bone Healing System, BIOMET® OrthoPak® Non-invasive Bone Growth Stimulator System, and the BIOMET® SpinalPak® Non-Invasive Spine Fusion Stimulator System [NCT01750840]8 participants (Actual)Observational [Patient Registry]2012-10-31Terminated(stopped due to Slow enrollment and poor patient follow-up following enrollment)
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00515073 (1) [back to overview]Overall Survival at 2 Years and 5 Years
NCT00780273 (3) [back to overview]Effectiveness - Treatment Difference in Mean Change in Crestal Bone Level
NCT00780273 (3) [back to overview]Effectiveness - Treatment Difference in Mean Change in Crestal Bone Level
NCT00780273 (3) [back to overview]Effectiveness - Treatment Difference in Mean Change in Crestal Bone Level
NCT01256879 (1) [back to overview]AUC
NCT01750840 (1) [back to overview]Radiographic Assessment of Healing
NCT01757275 (9) [back to overview]Rate of Clinically Significant Rebleeding During 7 Days
NCT01757275 (9) [back to overview]Number of Blood Units Transfused Within 30 Days
NCT01757275 (9) [back to overview]Number of Blood Units Transfused Within 72 Hours
NCT01757275 (9) [back to overview]Number of Patients With Endoscopic Re-treatment Within 30 Days
NCT01757275 (9) [back to overview]Number of Patients With Endoscopic Re-treatment Within 72 Hours
NCT01757275 (9) [back to overview]Number of Patients With Surgery Due to Rebleeding Within 30 Days
NCT01757275 (9) [back to overview]Number of Patients With Surgery Due to Rebleeding Within 72 Hours
NCT01757275 (9) [back to overview]Rate of Clinically Significant Rebleeding During 30 Days
NCT01757275 (9) [back to overview]Rate of Clinically Significant Rebleeding Within 72 Hours
NCT02021331 (1) [back to overview]Implant Survival
NCT02157376 (2) [back to overview]Proportion of Patients With Any Overt Upper-GI Bleeding (Significant and Non-significant) During the Treatment Evaluation Phase
NCT02157376 (2) [back to overview]The Percent of Patients With Clinically Significant Upper-GI Bleeding During the Treatment Evaluation Phase
NCT02865590 (1) [back to overview]Histomorphometric Evaluation of New Bone Formation.
NCT03307252 (12) [back to overview]Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) (T1 vs. R1)
NCT03307252 (12) [back to overview]Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz) (Cimetidine + R1 (T3) vs. R1)
NCT03307252 (12) [back to overview]Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz) (Probenecid + R1 (T4) vs. R1)
NCT03307252 (12) [back to overview]Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz) (Rifampin + R1 (T2) vs. R1)
NCT03307252 (12) [back to overview]Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz) (Verapamil + R1 (T1) vs. R1)
NCT03307252 (12) [back to overview]Maximum Measured Concentration of the Analytes: Digoxin, Furosemide, Metformin, and Rosuvastatin (Cmax) (T1 vs. R1)
NCT03307252 (12) [back to overview]Maximum Measured Concentration of the Analytes: Digoxin, Furosemide, Metformin, and Rosuvastatin (Cmax) (T2 vs. R1)
NCT03307252 (12) [back to overview]Maximum Measured Concentration of the Analytes: Digoxin, Furosemide, Metformin, and Rosuvastatin (Cmax) (T3 vs. R1)
NCT03307252 (12) [back to overview]Maximum Measured Concentration of the Analytes: Digoxin, Furosemide, Metformin, and Rosuvastatin (Cmax) (T4 vs. R1)
NCT03307252 (12) [back to overview]Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) (T2 vs. R1)
NCT03307252 (12) [back to overview]Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) (T4 vs. R1)
NCT03307252 (12) [back to overview]Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) (T3 vs. R1)
NCT04103515 (4) [back to overview]Lateral Condyle Kinematic Translations - Step up
NCT04103515 (4) [back to overview]Lateral Condyle Kinematics Translations - Deep Knee Bend
NCT04103515 (4) [back to overview]Medial Condyle Kinematics Translations - Deep Knee Bend
NCT04103515 (4) [back to overview]Medial Condyle Kinematics Translations - Step Up
NCT04493931 (139) [back to overview]Cohort 3: AUC(0-infinity) of Digoxin in Plasma
NCT04493931 (139) [back to overview]Cohort 3: AUC(0-infinity) of Midazolam in Plasma
NCT04493931 (139) [back to overview]Cohort 3: AUC(0-t) of Digoxin in Plasma
NCT04493931 (139) [back to overview]Cohort 3: AUC(0-t) of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)
NCT04493931 (139) [back to overview]Cohort 3: AUC(0-t) of Midazolam in Plasma
NCT04493931 (139) [back to overview]Cohort 3: AUC(0-tau) of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)
NCT04493931 (139) [back to overview]Cohort 3: AUC(0-tau) of Gepotidacin in Plasma First Dose of 3000 mg (First Dose)
NCT04493931 (139) [back to overview]Cohort 3: AUC(0-tau) of Gepotidacin in Urine Following Two 3000 mg Doses (First Dose + Second Dose)
NCT04493931 (139) [back to overview]Cohort 3: CL/F of Digoxin in Plasma
NCT04493931 (139) [back to overview]Cohort 3: CL/F of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)
NCT04493931 (139) [back to overview]Cohort 3: CL/F of Midazolam in Plasma
NCT04493931 (139) [back to overview]Cohort 3: CLr of Gepotidacin Following Two 3000 mg Doses (First Dose + Second Dose)
NCT04493931 (139) [back to overview]Cohort 3: Cmax of Digoxin in Plasma
NCT04493931 (139) [back to overview]Cohort 3: Cmax of Gepotidacin in Plasma After the First Dose of 3000 mg (First Dose)
NCT04493931 (139) [back to overview]Cohort 3: Cmax of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)
NCT04493931 (139) [back to overview]Cohort 3: Cmax of Midazolam in Plasma
NCT04493931 (139) [back to overview]Cohort 3: Cmin of Midazolam in Plasma
NCT04493931 (139) [back to overview]Cohort 3: Minimum Observed Concentration (Cmin) of Digoxin in Plasma
NCT04493931 (139) [back to overview]Cohort 3: Percentage of the Given Dose of Drug Excreted in Urine (fe%) Following Two 3000 mg Doses of Gepotidacin (First Dose + Second Dose )
NCT04493931 (139) [back to overview]Cohort 3: RoAUC of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)
NCT04493931 (139) [back to overview]Cohort 3: RoCmax of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)
NCT04493931 (139) [back to overview]Cohort 3: T1/2 of Digoxin in Plasma
NCT04493931 (139) [back to overview]Cohort 3: T1/2 of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose+ Second Dose)
NCT04493931 (139) [back to overview]Cohort 3: T1/2 of Midazolam in Plasma
NCT04493931 (139) [back to overview]Cohort 3: Tlag of Digoxin in Plasma
NCT04493931 (139) [back to overview]Cohort 3: Tlag of Gepotidacin in Plasma After the First Dose of 3000 mg (First Dose)
NCT04493931 (139) [back to overview]Cohort 3: Tlag of Midazolam in Plasma
NCT04493931 (139) [back to overview]Cohort 3: Tmax of Digoxin in Plasma
NCT04493931 (139) [back to overview]Cohort 3: Tmax of Gepotidacin in Plasma After the First Dose of 3000 mg (First Dose)
NCT04493931 (139) [back to overview]Cohort 3: Tmax of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)
NCT04493931 (139) [back to overview]Cohort 3: Tmax of Midazolam in Plasma
NCT04493931 (139) [back to overview]Cohort 3: Vz/F of Digoxin in Plasma
NCT04493931 (139) [back to overview]Cohort 3: Vz/F of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)
NCT04493931 (139) [back to overview]Cohort 3: Vz/F of Midazolam in Plasma
NCT04493931 (139) [back to overview]Cohort 4: Accumulation Ratio Based on AUC(0-tau) (RoAUC) of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)-Fed State
NCT04493931 (139) [back to overview]Cohort 4: Accumulation Ratio Based on Cmax (RoCmax) of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)-Fed State
NCT04493931 (139) [back to overview]Cohort 4: Ae Total of Gepotidacin Following Single Dose of 1500 mg Under Fed Condition in Urine
NCT04493931 (139) [back to overview]Cohort 4: Ae Total of Gepotidacin in Urine Following Two 3000 mg Doses-Fed State
NCT04493931 (139) [back to overview]Cohort 4: Area Under the Concentration-time Curve From Time 0 (Pre-dose) to the Concentration at 24 Hours Post-dose (AUC[0-24]) of Gepotidacin Following Single Dose of 1500 mg in Plasma
NCT04493931 (139) [back to overview]Cohort 4: Area Under the Concentration-time Curve From Time 0 (Pre-dose) to the Concentration at 48 Hours Post-dose (AUC[0-48]) of Gepotidacin Following Single Dose of 1500 mg in Plasma
NCT04493931 (139) [back to overview]Cohort 4: AUC From Time 0 (Predose) to Time Tau (AUC[0-tau]) of Gepotidacin in Plasma After the First Dose of 3000 Mg-Fed State
NCT04493931 (139) [back to overview]Cohort 4: AUC(0-24) of Gepotidacin Following Single Dose of 1500 mg Under Fed Condition in Urine
NCT04493931 (139) [back to overview]Cohort 4: AUC(0-24) of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)-Fed State
NCT04493931 (139) [back to overview]Cohort 4: AUC(0-24) of Gepotidacin in Urine Following Two 3000 mg Doses-Fed State
NCT04493931 (139) [back to overview]Cohort 4: AUC(0-48) of Gepotidacin Following Single Dose of 1500 mg Under Fed Condition in Urine
NCT04493931 (139) [back to overview]Cohort 4: AUC(0-48) of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)-Fed State
NCT04493931 (139) [back to overview]Cohort 4: AUC(0-48) of Gepotidacin in Urine Following Two 3000 mg Doses-Fed State
NCT04493931 (139) [back to overview]Cohort 4: AUC(0-infinity) of Gepotidacin Following Single Dose of 1500 mg in Plasma
NCT04493931 (139) [back to overview]Cohort 4: AUC(0-infinity) of Gepotidacin Following Single Dose of 1500 mg in Plasma - Food Effect in Japanese Participants
NCT04493931 (139) [back to overview]Cohort 4: AUC(0-t) of Gepotidacin Following Single Dose of 1500 mg in Plasma
NCT04493931 (139) [back to overview]Cohort 4: AUC(0-t) of Gepotidacin Following Single Dose of 1500 mg in Plasma - Food Effect in Japanese Participants
NCT04493931 (139) [back to overview]Cohort 4: AUC(0-t) of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)-Fed State
NCT04493931 (139) [back to overview]Cohort 4: AUC(0-tau) of Gepotidacin Following Single Dose of 1500 mg Under Fed Condition in Urine
NCT04493931 (139) [back to overview]Cohort 4: AUC(0-tau) of Gepotidacin in Plasma After the Second Dose of 3000 mg (Evening Dose)-Fed State
NCT04493931 (139) [back to overview]Cohort 2: CL/F of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 4: CL/F of Gepotidacin Following Single Dose of 1500 mg in Plasma
NCT04493931 (139) [back to overview]Cohort 4: CL/F of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)-Fed State
NCT04493931 (139) [back to overview]Cohort 4: CLr of Gepotidacin Following Single Dose of 1500 mg Under Fed Condition
NCT04493931 (139) [back to overview]Cohort 4: CLr of Gepotidacin Following Two 3000 mg Dose-Fed State
NCT04493931 (139) [back to overview]Cohort 4: Cmax of Gepotidacin Following Single Dose of 1500 mg in Plasma
NCT04493931 (139) [back to overview]Cohort 4: Cmax of Gepotidacin Following Single Dose of 1500 mg in Plasma - Food Effect in Japanese Participants
NCT04493931 (139) [back to overview]Cohort 4: Cmax of Gepotidacin in Plasma After the First Dose of 3000 mg -Fed State
NCT04493931 (139) [back to overview]Cohort 4: Cmax of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)-Fed State
NCT04493931 (139) [back to overview]Cohort 4: Percentage of the Given Dose of Drug Excreted in Urine (fe%) for Gepotidacin 1500 mg Under Fed Condition
NCT04493931 (139) [back to overview]Cohort 4: Percentage of the Given Dose of Drug Excreted in Urine (fe%) of Gepotidacin Following Two 3000 mg Doses-Fed State
NCT04493931 (139) [back to overview]Cohort 4: T1/2 of Gepotidacin Following Single Dose of 1500 mg in Plasma
NCT04493931 (139) [back to overview]Cohort 4: T1/2 of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose )-Fed State
NCT04493931 (139) [back to overview]Cohort 4: Tlag of Gepotidacin Following Single Dose of 1500 mg in Plasma - Food Effect in Japanese Participants
NCT04493931 (139) [back to overview]Cohort 4: Tlag of Gepotidacin in Plasma After the First Dose of 3000 mg (First Dose)-Fed State
NCT04493931 (139) [back to overview]Cohort 4: Tmax of Gepotidacin Following Single Dose of 1500 mg in Plasma
NCT04493931 (139) [back to overview]Cohort 4: Tmax of Gepotidacin Following Single Dose of 1500 mg in Plasma - Food Effect in Japanese Participants
NCT04493931 (139) [back to overview]Cohort 4: Tmax of Gepotidacin in Plasma After the First Dose of 3000 mg -Fed State
NCT04493931 (139) [back to overview]Cohort 4: Tmax of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)-Fed State
NCT04493931 (139) [back to overview]Cohort 4: Vz/F of Gepotidacin Following Single Dose of 1500 mg in Plasma
NCT04493931 (139) [back to overview]Cohort 4: Vz/F of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)-Fed State
NCT04493931 (139) [back to overview]Cohort 1: Amount of Drug Excreted in Urine in a Time Interval (Ae[t1-t2]) of Gepotidacin
NCT04493931 (139) [back to overview]Cohort 1: Number of Participants With Any Increase in Maximum Post-Baseline ECG Parameter QTc Interval
NCT04493931 (139) [back to overview]Cohort 1: Number of Participants With SAE and Non-SAE
NCT04493931 (139) [back to overview]Cohort 1: Number of Participants With Worst Case Clinical Chemistry Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT04493931 (139) [back to overview]Cohort 1: Number of Participants With Worst Case Hematology Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT04493931 (139) [back to overview]Cohort 1: Number of Participants With Worst Case Urinalysis Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT04493931 (139) [back to overview]Cohort 1: Number of Participants With Worst Case Vital Sign Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT04493931 (139) [back to overview]Cohort 2: Ae(t1-t2) of Gepotidacin
NCT04493931 (139) [back to overview]Cohort 2: Number of Participants With Any Increase in Maximum Post-Baseline ECG Parameter QTc Interval
NCT04493931 (139) [back to overview]Cohort 2: Number of Participants With SAE and Non-SAE
NCT04493931 (139) [back to overview]Cohort 2: Number of Participants With Worst Case Clinical Chemistry Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT04493931 (139) [back to overview]Cohort 2: Number of Participants With Worst Case Hematology Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT04493931 (139) [back to overview]Cohort 2: Number of Participants With Worst Case Urinalysis Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT04493931 (139) [back to overview]Cohort 2: Number of Participants With Worst Case Vital Sign Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT04493931 (139) [back to overview]Cohort 3: Amount of Drug Excreted in Urine in a Time Interval (Ae[t1-t2]) of Gepotidacin Following Two 3000 mg Doses (First Dose + Second Dose)
NCT04493931 (139) [back to overview]Cohort 3: Number of Participants With Any Increase in Maximum Post-Baseline ECG Parameter QTc Interval
NCT04493931 (139) [back to overview]Cohort 3: Number of Participants With SAE and Non-SAE
NCT04493931 (139) [back to overview]Cohort 3: Number of Participants With Worst Case Clinical Chemistry Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT04493931 (139) [back to overview]Cohort 3: Number of Participants With Worst Case Hematology Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT04493931 (139) [back to overview]Cohort 3: Number of Participants With Worst Case Urinalysis Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT04493931 (139) [back to overview]Cohort 3: Number of Participants With Worst Case Vital Sign Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT04493931 (139) [back to overview]Cohort 4: Ae(t1-t2) of Gepotidacin Following Single Dose of 1500 mg Under Fed Condition in Urine
NCT04493931 (139) [back to overview]Cohort 4: Ae(t1-t2) of Gepotidacin in Urine Following Two 3000 mg Doses-Fed State
NCT04493931 (139) [back to overview]Cohort 1: Apparent Oral Clearance (CL/F) of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 4: Number of Participants With Serious Adverse Events (SAE) and Non-serious Adverse Events (Non-SAE)
NCT04493931 (139) [back to overview]Cohort 4: Number of Participants With Worst Case Clinical Chemistry Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT04493931 (139) [back to overview]Cohort 4: Number of Participants With Worst Case Hematology Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT04493931 (139) [back to overview]Cohort 4: Number of Participants With Worst Case Urinalysis Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT04493931 (139) [back to overview]Cohort 4: Number of Participants With Worst Case Vital Sign Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT04493931 (139) [back to overview]Cohort 1: Apparent Volume of Distribution (Vz/F) of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 1: Area Under the Concentration-time Curve From Time 0 (Pre-dose) to the Time of the Last Quantifiable Concentration (AUC [0-t]) of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 1: AUC (0-24) of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 1: AUC From Time 0 (Pre-dose) Extrapolated to Infinite Time (AUC[0-infinity]) of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 1: AUC(0-24) of Gepotidacin in Urine
NCT04493931 (139) [back to overview]Cohort 1: AUC(0-48) of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 1: AUC(0-48) of Gepotidacin in Urine
NCT04493931 (139) [back to overview]Cohort 1: Maximum Observed Concentration (Cmax) of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 1: Percentage of the Given Dose of Drug Excreted in Urine (fe%) of Gepotidacin
NCT04493931 (139) [back to overview]Cohort 1: Renal Clearance (CLr) of Gepotidacin
NCT04493931 (139) [back to overview]Cohort 1: Terminal Phase Half-life (t1/2) of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 1: Time to Reach Maximum Observed Concentration (Tmax) of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 4: AUC(0-tau) of Gepotidacin in Urine Following Two 3000 mg Doses-Fed State
NCT04493931 (139) [back to overview]Cohort 1: Tlag of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 1: Total Unchanged Drug (Ae Total) of Gepotidacin in Urine
NCT04493931 (139) [back to overview]Cohort 2: Ae Total of Gepotidacin in Urine
NCT04493931 (139) [back to overview]Cohort 2: AUC(0-24) of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 2: AUC(0-24) of Gepotidacin in Urine
NCT04493931 (139) [back to overview]Cohort 2: AUC(0-48) of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 2: AUC(0-48) of Gepotidacin in Urine
NCT04493931 (139) [back to overview]Cohort 2: AUC(0-infinity) of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 2: AUC(0-t) of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 2: CLr of Gepotidacin
NCT04493931 (139) [back to overview]Cohort 2: Cmax of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 2: Lag Time Before Observation of Drug Concentrations (Tlag) of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 2: Percentage of the Given Dose of Drug Excreted in Urine (fe%) of Gepotidacin
NCT04493931 (139) [back to overview]Cohort 2: T1/2 of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 2: Tmax of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 2: Vz/F of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 3: Ae Total of Gepotidacin in Urine Following Two 3000 mg Doses (First Dose + Second Dose )
NCT04493931 (139) [back to overview]Cohort 3: AUC (0-48) of Gepotidacin in Urine Following Two 3000 mg Doses (First Dose + Second Dose)
NCT04493931 (139) [back to overview]Cohort 3: AUC(0-24) of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)
NCT04493931 (139) [back to overview]Cohort 3: AUC(0-24) of Gepotidacin in Urine Following Two 3000 mg Doses (First Dose + Second Dose)
NCT04493931 (139) [back to overview]Cohort 3: AUC(0-48) of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)
NCT04493931 (139) [back to overview]Cohort 4: Number of Participants With Any Increase in Maximum Post-Baseline Electrocardiogram (ECG) Parameter Corrected QT (QTc) Interval
NCT04585022 (4) [back to overview]Metal Ion Concentrations in Blood
NCT04585022 (4) [back to overview]SF-36
NCT04585022 (4) [back to overview]Harris Hip Score
NCT04585022 (4) [back to overview]Number of Patients Undergoing Revision

Overall Survival at 2 Years and 5 Years

The percentage of participants who are still alive for A designated period of time (2 years and 5 years) after starting treatment. Continual Assessments every 3 months for 1 year, then every 4 months for 2 years, then every 6 months for 2 years, then once a year. (NCT00515073)
Timeframe: Assessment at 2 years and 5 years

Interventionpercentage of participants (Number)
2 Years5 Years
Paclitaxel (Taxol) + Pelvic Radiation9385

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Effectiveness - Treatment Difference in Mean Change in Crestal Bone Level

Incidence of greater than 2 mm crestal bone (mesial or distal) loss. Reported in the percentage of analyzed implants. (NCT00780273)
Timeframe: 12 months after surgery

InterventionPercentage of implants (Number)
Ankylos Dental Implants.20
3i Prevail Dental Implants.56

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Effectiveness - Treatment Difference in Mean Change in Crestal Bone Level

Incidence of greater than 2 mm crestal bone (mesial or distal) loss. Reported in the percentage of analyzed implants. (NCT00780273)
Timeframe: 24 months after surgery

InterventionPercentage of implants (Number)
Ankylos Dental Implants.11
3i Prevail Dental Implants.70

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Effectiveness - Treatment Difference in Mean Change in Crestal Bone Level

Incidence of greater than 2 mm crestal bone (mesial or distal) loss. Reported in the percentage of analyzed implants. (NCT00780273)
Timeframe: 6 months after surgery

InterventionPercentage of implants (Number)
Ankylos Dental Implants.13
3i Prevail Dental Implants.55

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AUC

pharmacokinetic exposure (ng*hr/ml) (NCT01256879)
Timeframe: 0-10 hours

Interventionng*hr/ml (Mean)
Experimental: CimTest-A3896
Experimental: CimTest-B3661
Active Comparator: Sorbitol-free Cimetidine Solution3495
Experimental: Commercial Cimetidine Solution3512

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Radiographic Assessment of Healing

Bone healing was assessed on x-rays and/or CT scan. (NCT01750840)
Timeframe: The time frame for healing determination was not pre-specified. Patients were evaluated at regular doctors' visits for up to 12 months. The physician determined the time point at which healing occurred for each patient at their regular visits.

Interventionpercentage of healed fractures (Number)
Stimulation Group100

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Rate of Clinically Significant Rebleeding During 7 Days

"Diagnostic criteria for clinically significant rebleeding based on either A, B or C:~A) Endoscopy - initiated by clinical signs of bleeding defined as one of B1 or B2 or B3 and endoscopic verification, ie one of A1 or A2.~A1: Blood in stomach (this criteria cannot be used during the first 6 hours after primary endoscopic haemostasis). A2: A verified active bleeding from a peptic ulcer (Forrest Ia, Ib).~B) A true clinically based definition, at least two of B1 and/or B2 and/or B3. B1: Vomiting of fresh blood or fresh blood in a gastric tube or haematochezia or melaena after a normal stool. B2: Decrease in Hb >20g/L (or Hct >6%) during 24 hours or an increase in Hb <10g/L (or Hct <3%) despite ≥2 units of blood has been transfused during 24hours. B3: Unstable circulation systolic blood pressure ≤ 90 mmHg or pulse ≥110/min (after have had a stable circulation).~C) Haematemesis. Vomiting significant amounts (>200 ml) of fresh blood as estimated by the investigator." (NCT01757275)
Timeframe: 7 days

,
Interventionparticipants (Number)
No rebleedingRebleeding
Cimetidine1016
Esomeprazole1053

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Number of Blood Units Transfused Within 30 Days

(NCT01757275)
Timeframe: within 30 days

Interventionblood units (Number)
Esomeprazole18
Cimetidine21

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Number of Blood Units Transfused Within 72 Hours

(NCT01757275)
Timeframe: within 72 hours

Interventionblood units (Number)
Esomeprazole14
Cimetidine21

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Number of Patients With Endoscopic Re-treatment Within 30 Days

(NCT01757275)
Timeframe: 30 days

,
Interventionparticipants (Number)
No re-treatmentRe-treatment
Cimetidine1061
Esomeprazole1062

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Number of Patients With Endoscopic Re-treatment Within 72 Hours

(NCT01757275)
Timeframe: 72 hours

,
Interventionparticipants (Number)
No re-treatmentRe-treatment
Cimetidine1061
Esomeprazole1080

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Number of Patients With Surgery Due to Rebleeding Within 30 Days

(NCT01757275)
Timeframe: within 30 days

,
Interventionparticipants (Number)
No surgerySurgery
Cimetidine1061
Esomeprazole1080

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Number of Patients With Surgery Due to Rebleeding Within 72 Hours

(NCT01757275)
Timeframe: within 72 hours

,
Interventionparticipants (Number)
No surgerySurgery
Cimetidine1070
Esomeprazole1080

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Rate of Clinically Significant Rebleeding During 30 Days

"Diagnostic criteria for clinically significant rebleeding based on either A, B or C:~A) Endoscopy - initiated by clinical signs of bleeding defined as one of B1 or B2 or B3 and endoscopic verification, ie one of A1 or A2.~A1: Blood in stomach (this criteria cannot be used during the first 6 hours after primary endoscopic haemostasis). A2: A verified active bleeding from a peptic ulcer (Forrest Ia, Ib).~B) A true clinically based definition, at least two of B1 and/or B2 and/or B3. B1: Vomiting of fresh blood or fresh blood in a gastric tube or haematochezia or melaena after a normal stool. B2: Decrease in Hb >20g/L (or Hct >6%) during 24 hours or an increase in Hb <10g/L (or Hct <3%) despite ≥2 units of blood has been transfused during 24hours. B3: Unstable circulation systolic blood pressure ≤ 90 mmHg or pulse ≥110/min (after have had a stable circulation).~C) Haematemesis. Vomiting significant amounts (>200 ml) of fresh blood as estimated by the investigator." (NCT01757275)
Timeframe: 30 days

,
Interventionparticipants (Number)
No rebleedingRebleeding
Cimetidine1016
Esomeprazole1053

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Rate of Clinically Significant Rebleeding Within 72 Hours

"Diagnostic criteria for clinically significant rebleeding based on either A, B or C:~A) Endoscopy - initiated by clinical signs of bleeding defined as one of B1 or B2 or B3 and endoscopic verification, ie one of A1 or A2.~A1: Blood in stomach (this criteria cannot be used during the first 6 hours after primary endoscopic haemostasis). A2: A verified active bleeding from a peptic ulcer (Forrest Ia, Ib).~B) A true clinically based definition, at least two of B1 and/or B2 and/or B3. B1: Vomiting of fresh blood or fresh blood in a gastric tube or haematochezia or melaena after a normal stool. B2: Decrease in Hb >20g/L (or Hct >6%) during 24 hours or an increase in Hb <10g/L (or Hct <3%) despite ≥2 units of blood has been transfused during 24hours. B3: Unstable circulation systolic blood pressure ≤ 90 mmHg or pulse ≥110/min (after have had a stable circulation).~C) Haematemesis. Vomiting significant amounts (>200 ml) of fresh blood as estimated by the investigator." (NCT01757275)
Timeframe: 72 hours

,
Interventionparticipants (Number)
No rebleedingRebleeding
Cimetidine1016
Esomeprazole1071

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Implant Survival

Checking to make sure the implant is stable. (NCT02021331)
Timeframe: 2wk, 4wk, 6wk, 3mo, 6mo, 12mo

,
InterventionParticipants (Count of Participants)
2wk4wk6wk3mo6mo12mo
Immediate Implant Placement With Immediate Provisionalization321111
Immediate Implant Placement Without Provisionalization222222

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Proportion of Patients With Any Overt Upper-GI Bleeding (Significant and Non-significant) During the Treatment Evaluation Phase

"Criteria for a significant upper GI bleeding as described in primary outcome measure or,~Criteria for a non-significant upper GI bleeding as:~Bright red blood per NG or OG tube that clear after NG or OG tube adjustment and 5 to 10 minutes of lavage with room temperature normal saline or,~Persistent gastroccult- positive coffee ground material~During IMP treatment Day 1-2:~Persistent gastroccult - positive coffee ground material for at less than eight consecutive hours or that clear with at least 100 ml of lavage with room temperature normal saline.~During IMP treatment Day 3-14:~Persistent gastroccult - positive coffee ground material in less than three consecutive gastric aspirates within 2 to 4 hours (at least 60±20 minutes apart), or that clear with at least 100 ml of lavage with room temperature normal saline or,~Any clinical signs of hematemesis or melena or haematochezia judged (by the Investigator) to be from an upper GI source." (NCT02157376)
Timeframe: 1-14 days

Interventionproportion of participants (Number)
Esomeprazole0.109
Cimetidine0.105

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The Percent of Patients With Clinically Significant Upper-GI Bleeding During the Treatment Evaluation Phase

"Criteria for a clinically significant upper GI bleeding as:~Bright red blood per NG or OG tube that did not clear after NG or OG tube adjustment and 5 to 10 minutes of at least 100 ml lavage with room temperature normal saline-or,~Persistent gastroccult- positive coffee ground material~During IMP treatment Day 1-2:~Persistent gastroccult- positive coffee ground material for at least eight consecutive hours that did not clear with at least 100 ml of lavage with room temperature normal saline.~During IMP treatment Day 3-14:~Persistent gastroccult- positive coffee ground material in at least three consecutive gastric aspirates within 2 to 4 hours (at least 60 ±20 minutes apart), that did not clear with at least 100 ml of lavage with room temperature normal saline." (NCT02157376)
Timeframe: 1-14 days

Intervention% of participants (Number)
Esomeprazole2.7
Cimetidine4.6

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Histomorphometric Evaluation of New Bone Formation.

(NCT02865590)
Timeframe: 6 months

,
Interventionpercentage of millimeters (Mean)
newly formed bonemarrow spacesresidual graft material
Deproteinized Bovine Bone Allograft22.8446.2030.94
Lyophilized Equine Bone Allograft22.2050.7727

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Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) (T1 vs. R1)

AUC0-∞, area under the concentration-time curve of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) in plasma over the time interval from 0 extrapolated to infinity is presented. AUC0-∞ not displayed for Digoxin analyte as precision was considered non-sufficient. gMean presented here is an adjusted gMean and SE presented is a gSE. (NCT03307252)
Timeframe: Samples were taken within 0:20 hh:mm prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole*hour/litre (nmol*h/L) (Geometric Mean)
FurosemideMetforminRosuvastatin
Cocktail (R1)191.291365.8594.14
Verapamil + R1 (T1)176.441147.23116.80

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Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz) (Cimetidine + R1 (T3) vs. R1)

AUC0-tz, area under the concentration-time curve of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) in plasma over the time interval from 0 to the last quantifiable data point is presented. gMean presented here is an adjusted gMean and SE presented is a gSE. (NCT03307252)
Timeframe: Samples were taken within 0:20 hh:mm prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole*hour/litre (nmol*h/L) (Geometric Mean)
DigoxinFurosemideMetforminRosuvastatin
Cimetidine + R1 (T3)19.03196.392006.60139.54
Cocktail (R1)15.15194.051532.41129.90

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Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz) (Probenecid + R1 (T4) vs. R1)

AUC0-tz, area under the concentration-time curve of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) in plasma over the time interval from 0 to the last quantifiable data point is presented. gMean presented here is an adjusted gMean and SE presented is a gSE. (NCT03307252)
Timeframe: Samples were taken within 0:20 hh:mm prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole*hour/litre (nmol*h/L) (Geometric Mean)
DigoxinFurosemideMetforminRosuvastatin
Cocktail (R1)13.52177.961321.20106.69
Probenecid + R1 (T4)14.44483.381331.83238.16

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Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz) (Rifampin + R1 (T2) vs. R1)

AUC0-tz, area under the concentration-time curve of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) in plasma over the time interval from 0 to the last quantifiable data point is presented. gMean presented here is an adjusted gMean and SE presented is a gSE. (NCT03307252)
Timeframe: Samples were taken within 0:20 hh:mm prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole*hour/litre (nmol*h/L) (Geometric Mean)
DigoxinFurosemideMetforminRosuvastatin
Cocktail (R1)13.61176.851357.3487.29
Rifampin + R1 (T2)17.89211.821473.38303.81

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Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz) (Verapamil + R1 (T1) vs. R1)

AUC0-tz, area under the concentration-time curve of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) in plasma over the time interval from 0 to the last quantifiable data point is presented. Geometric mean (gMean) presented here is an adjusted gMean and standard error (SE) presented is a geometric SE (gSE). (NCT03307252)
Timeframe: Samples were taken within 0:20 hour:minutes (hh:mm) prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole*hour/litre (nmol*h/L) (Geometric Mean)
DigoxinFurosemideMetforminRosuvastatin
Cocktail (R1)13.61176.851357.3487.29
Verapamil + R1 (T1)13.71165.801126.2298.98

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Maximum Measured Concentration of the Analytes: Digoxin, Furosemide, Metformin, and Rosuvastatin (Cmax) (T1 vs. R1)

Cmax, maximum measured concentration of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) is presented. gMean presented here is an adjusted gMean and SE presented is a gSE. (NCT03307252)
Timeframe: Samples were taken within 0:20 hh:mm prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole/ litre (nmol/ L) (Geometric Mean)
DigoxinFurosemideMetforminRosuvastatin
Cocktail (R1)1.1788.59223.786.84
Verapamil + R1 (T1)1.4284.32179.457.90

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Maximum Measured Concentration of the Analytes: Digoxin, Furosemide, Metformin, and Rosuvastatin (Cmax) (T2 vs. R1)

Cmax, maximum measured concentration of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) is presented. gMean presented here is an adjusted gMean and SE presented is a gSE. (NCT03307252)
Timeframe: Samples were taken within 0:20 hh:mm prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole/ litre (nmol/ L) (Geometric Mean)
DigoxinFurosemideMetforminRosuvastatin
Cocktail (R1)1.1788.59223.786.84
Rifampin + R1 (T2)2.55119.66251.3277.00

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Maximum Measured Concentration of the Analytes: Digoxin, Furosemide, Metformin, and Rosuvastatin (Cmax) (T3 vs. R1)

Cmax, maximum measured concentration of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) is presented. gMean presented here is an adjusted gMean and SE presented is a gSE. (NCT03307252)
Timeframe: Samples were taken within 0:20 hh:mm prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole/ litre (nmol/ L) (Geometric Mean)
DigoxinFurosemideMetforminRosuvastatin
Cimetidine + R1 (T3)1.6597.69316.8313.21
Cocktail (R1)1.3593.23258.3311.30

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Maximum Measured Concentration of the Analytes: Digoxin, Furosemide, Metformin, and Rosuvastatin (Cmax) (T4 vs. R1)

Cmax, maximum measured concentration of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) is presented. gMean presented here is an adjusted gMean and SE presented is a gSE. (NCT03307252)
Timeframe: Samples were taken within 0:20 hh:mm prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole/ litre (nmol/ L) (Geometric Mean)
DigoxinFurosemideMetforminRosuvastatin
Cocktail (R1)1.3090.00243.4910.11
Probenecid + R1 (T4)1.13110.64246.7843.29

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Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) (T2 vs. R1)

AUC0-∞, area under the concentration-time curve of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) in plasma over the time interval from 0 extrapolated to infinity is presented. AUC0-∞ not displayed for Digoxin analyte as precision was considered non-sufficient. gMean presented here is an adjusted gMean and SE presented is a gSE. (NCT03307252)
Timeframe: Samples were taken within 0:20 hh:mm prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole*hour/litre (nmol*h/L) (Geometric Mean)
FurosemideMetforminRosuvastatin
Cocktail (R1)191.291365.8594.14
Rifampin + R1 (T2)215.631482.76320.72

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Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) (T4 vs. R1)

AUC0-∞, area under the concentration-time curve of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) in plasma over the time interval from 0 extrapolated to infinity is presented. AUC0-∞ not displayed for Digoxin analyte as precision was considered non-sufficient. gMean presented here is an adjusted gMean and SE presented is a gSE. (NCT03307252)
Timeframe: Samples were taken within 0:20 hh:mm prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole*hour/litre (nmol*h/L) (Geometric Mean)
FurosemideMetforminRosuvastatin
Cocktail (R1)188.111330.47113.78
Probenecid + R1 (T4)489.281346.62244.94

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Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) (T3 vs. R1)

AUC0-∞, area under the concentration-time curve of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) in plasma over the time interval from 0 extrapolated to infinity is presented. AUC0-∞ not displayed for Digoxin analyte as precision was considered non-sufficient. gMean presented here is an adjusted gMean and SE presented is a gSE. (NCT03307252)
Timeframe: Samples were taken within 0:20 hh:mm prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole*hour/litre (nmol*h/L) (Geometric Mean)
FurosemideMetforminRosuvastatin
Cimetidine + R1 (T3)202.172023.33148.32
Cocktail (R1)200.611540.21139.21

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Lateral Condyle Kinematic Translations - Step up

Lateral Condyle Kinematics Translations during stepping up activity. Data represents the motion of a specific part of the femur bone (in this case lateral femoral condyle) during the specified activity (in this case a step up). The kinematics (motion) is measured from the beginning of the activity to the end of the activity. Positive represents anterior motion of the femur, and negative represents posterior rollback of the femur. Data is only collected at a single time point and therefore refers to the motion of the femur bone during a specific activity at a single point in time. (NCT04103515)
Timeframe: Baseline

Interventionmm (Mean)
Subjects Implanted With PCR TKA1.15
Subjects Implanted With PS TKA2.28

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Lateral Condyle Kinematics Translations - Deep Knee Bend

Lateral Condyle Kinematics Translations during deep knee bend activity. Data represents the motion of a specific part of the femur bone (in this case lateral femoral condyle) during the specified activity (in this case a deep knee bend). The kinematics (motion) is measured from the beginning of the activity to the end of the activity. Positive represents anterior motion of the femur, and negative represents posterior rollback of the femur. Data is only collected at a single time point and therefore refers to the motion of the femur bone during a specific activity at a single point in time. (NCT04103515)
Timeframe: Baseline

Interventionmm (Mean)
Subjects Implanted With PCR TKA-1.52
Subjects Implanted With PS TKA-6.80

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Medial Condyle Kinematics Translations - Deep Knee Bend

Medial Condyle Kinematics Translations during deep knee bend activity. Medial Condyle Kinematics Translations during stepping up activity. Data represents the motion of a specific part of the femur bone (in this case medial femoral condyle) during the specified activity (in this case a deep knee bend). The kinematics (motion) is measured from the beginning of the activity to the end of the activity. Positive represents anterior motion of the femur, and negative represents posterior rollback of the femur. Data is only collected at a single time point and therefore refers to the motion of the femur bone during a specific activity at a single point in time. (NCT04103515)
Timeframe: Baseline

Interventionmm (Mean)
Subjects Implanted With PCR TKA0.13
Subjects Implanted With PS TKA-4.25

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Medial Condyle Kinematics Translations - Step Up

Medial Condyle Kinematics Translations during stepping up activity. Data represents the motion of a specific part of the femur bone (in this case medial femoral condyle) during the specified activity (in this case a step up). The kinematics (motion) is measured from the beginning of the activity to the end of the activity. Positive represents anterior motion of the femur, and negative represents posterior rollback of the femur. Data is only collected at a single time point and therefore refers to the motion of the femur bone during a specific activity at a single point in time. (NCT04103515)
Timeframe: Baseline

Interventionmm (Mean)
Subjects Implanted With PCR TKA-0.36
Subjects Implanted With PS TKA0.16

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Cohort 3: AUC(0-infinity) of Digoxin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of digoxin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 24 Hours, 36 Hours, 48 Hours, 72 Hours, 96 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours*picograms per milliliter (Geometric Least Squares Mean)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg30743.6
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg34456.5

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Cohort 3: AUC(0-infinity) of Midazolam in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of midazolam was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours*nanograms per milliliter (Geometric Least Squares Mean)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg24.9
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg47.4

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Cohort 3: AUC(0-t) of Digoxin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of digoxin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 24 Hours, 36 Hours, 48 Hours, 72 Hours, 96 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours*picograms per milliliter (Geometric Least Squares Mean)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg25353.1
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg30842.3

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Cohort 3: AUC(0-t) of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 Hours, 14 Hours, 14 Hours 30 Hours, 15, 16,18,20,24,36, 48, 60 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg85.2

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Cohort 3: AUC(0-t) of Midazolam in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of midazolam was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours*nanograms per milliliter (Geometric Least Squares Mean)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg23.3
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg44.8

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Cohort 3: AUC(0-tau) of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 Hours, 14 Hours, 14 Hours 30 Hours, 15, 16,18,20,24,36, 48, 60 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours* micrograms per milliliter (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg41.9

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Cohort 3: AUC(0-tau) of Gepotidacin in Plasma First Dose of 3000 mg (First Dose)

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 Hours, 14 Hours, 14 Hours 30 Hours, 15, 16,18,20,24,36, 48, 60 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg29.8

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Cohort 3: AUC(0-tau) of Gepotidacin in Urine Following Two 3000 mg Doses (First Dose + Second Dose)

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-14 Hours, 14-16 Hours, 16-18 Hours, 18-20 Hours, 20-24 Hours, 24-36 Hours, 36-48 Hours, 48-60 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg4770.8

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Cohort 3: CL/F of Digoxin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of digoxin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 24 Hours, 36 Hours, 48 Hours, 72 Hours, 96 Hours post-dose in each Treatment Periods 1 and 2

InterventionLiters per Hour (Geometric Least Squares Mean)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg16.26
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg14.51

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Cohort 3: CL/F of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 Hours, 14 Hours, 14 Hours 30 Hours, 15, 16,18,20,24,36, 48, 60 Hours post-dose in each Treatment Periods 1 and 2

InterventionLiters per Hour (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg69.99

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Cohort 3: CL/F of Midazolam in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of midazolam was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionLiters per Hour (Geometric Least Squares Mean)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg80.17
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg42.16

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Cohort 3: CLr of Gepotidacin Following Two 3000 mg Doses (First Dose + Second Dose)

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-14 Hours, 14-16 Hours, 16-18 Hours, 18-20 Hours, 20-24 Hours, 24-36 Hours, 36-48 Hours, 48-60 Hours post-dose in each Treatment Periods 1 and 2

InterventionLiters per Hour (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg13.19

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Cohort 3: Cmax of Digoxin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of digoxin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 24 Hours, 36 Hours, 48 Hours, 72 Hours, 96 Hours Post-dose in each Treatment Periods 1 and 2

InterventionPicograms per milliliter (Geometric Least Squares Mean)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg1553.135
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg2381.259

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Cohort 3: Cmax of Gepotidacin in Plasma After the First Dose of 3000 mg (First Dose)

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 Hours, 14 Hours, 14 Hours 30 Hours, 15, 16,18,20,24,36, 48, 60 Hours post-dose in each Treatment Periods 1 and 2

InterventionMicrograms per milliliter (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg7.867

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Cohort 3: Cmax of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 Hours, 14 Hours, 14 Hours 30 Hours, 15, 16,18,20,24,36, 48, 60 Hours post-dose in each Treatment Periods 1 and 2

InterventionMicrograms per milliliter (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg10.051

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Cohort 3: Cmax of Midazolam in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of midazolam was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionNanograms per milliliter (Geometric Least Squares Mean)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg5.238
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg6.507

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Cohort 3: Cmin of Midazolam in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of midazolam was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionNanograms per milliliter (Geometric Least Squares Mean)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg0.192
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg0.222

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Cohort 3: Minimum Observed Concentration (Cmin) of Digoxin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of digoxin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 24 Hours, 36 Hours, 48 Hours, 72 Hours, 96 Hours post-dose in each Treatment Periods 1 and 2

InterventionPicograms per milliliter (Geometric Least Squares Mean)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg44.127
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg77.447

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Cohort 3: Percentage of the Given Dose of Drug Excreted in Urine (fe%) Following Two 3000 mg Doses of Gepotidacin (First Dose + Second Dose )

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. fe% was calculated as: (Ae total divided by Dose) multiplied by 100 %. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-14 Hours, 14-16 Hours, 16-18 Hours, 18-20 Hours, 20-24 Hours, 24-36 Hours, 36-48 Hours, 48-60 Hours post-dose in each Treatment Periods 1 and 2

InterventionPercent dose excreted (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg17.77

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Cohort 3: RoAUC of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Accumulation ratio was calculated as AUC(0-tau) after the second dose, where 0 is the timepoint prior to second dose, divided by AUC(0-tau) after the first dose, where 0 is the predose timepoint prior to the first dose. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 Hours, 14 Hours, 14 Hours 30 Hours, 15, 16,18,20,24,36, 48, 60 Hours post-dose in each Treatment Periods 1 and 2

InterventionRatio (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg1.406

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Cohort 3: RoCmax of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Accumulation ratio was calculated as Cmax after the second dose divided by Cmax after the first dose. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 Hours, 14 Hours, 14 Hours 30 Hours, 15, 16,18,20,24,36, 48, 60 Hours post-dose in each Treatment Periods 1 and 2

InterventionRatio (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg1.278

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Cohort 3: T1/2 of Digoxin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of digoxin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 24 Hours, 36 Hours, 48 Hours, 72 Hours, 96 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours (Geometric Least Squares Mean)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg39.367
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg32.777

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Cohort 3: T1/2 of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose+ Second Dose)

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 Hours, 14 Hours, 14 Hours 30 Hours, 15, 16,18,20,24,36, 48, 60 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg9.501

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Cohort 3: T1/2 of Midazolam in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of midazolam was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours (Geometric Least Squares Mean)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg5.320
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg6.075

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Cohort 3: Tlag of Digoxin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of digoxin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 24 Hours, 36 Hours, 48 Hours, 72 Hours, 96 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours (Median)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg0.000
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg0.000

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Cohort 3: Tlag of Gepotidacin in Plasma After the First Dose of 3000 mg (First Dose)

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 Hours, 14 Hours, 14 Hours 30 Hours, 15, 16,18,20,24,36, 48, 60 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours (Median)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg0.250

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Cohort 3: Tlag of Midazolam in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of midazolam was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours (Median)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg0.000
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg0.000

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Cohort 3: Tmax of Digoxin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of digoxin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 24 Hours, 36 Hours, 48 Hours, 72 Hours, 96 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours (Median)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg2.000
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg1.275

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Cohort 3: Tmax of Gepotidacin in Plasma After the First Dose of 3000 mg (First Dose)

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 Hours, 14 Hours, 14 Hours 30 Hours, 15, 16,18,20,24,36, 48, 60 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours (Median)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg2.500

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Cohort 3: Tmax of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 Hours, 14 Hours, 14 Hours 30 Hours, 15, 16,18,20,24,36, 48, 60 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours (Median)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg2.000

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Cohort 3: Tmax of Midazolam in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of midazolam was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours (Median)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg0.650
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg0.500

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Cohort 3: Vz/F of Digoxin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of digoxin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 24 Hours, 36 Hours, 48 Hours, 72 Hours, 96 Hours post-dose in each Treatment Periods 1 and 2

InterventionLiters (Geometric Least Squares Mean)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg923.75
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg688.49

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Cohort 3: Vz/F of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 Hours, 14 Hours, 14 Hours 30 Hours, 15, 16,18,20,24,36, 48, 60 Hours post-dose in each Treatment Periods 1 and 2

InterventionLiters (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg959.42

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Cohort 3: Vz/F of Midazolam in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of midazolam was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionLiters (Geometric Least Squares Mean)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg615.36
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg371.24

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Cohort 4: Accumulation Ratio Based on AUC(0-tau) (RoAUC) of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)-Fed State

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Accumulation ratio was calculated as AUC(0-tau) after the second dose, where 0 is the timepoint prior to second dose, divided by AUC(0-tau) after the first dose, where 0 is the predose timepoint prior to the first dose. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 minutes, 14 Hours, 14 Hours 30 minutes, 15, 16, 18, 20, 24, 36, 48, 60 Hours post-dose in Treatment Period 3

InterventionRatio (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed1.254

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Cohort 4: Accumulation Ratio Based on Cmax (RoCmax) of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)-Fed State

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Accumulation ratio was calculated as Cmax after the second dose divided by Cmax after the first dose. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 minutes, 14 Hours, 14 Hours 30 minutes, 15, 16, 18, 20, 24, 36, 48, 60 Hours post-dose in Treatment Period 3

InterventionRatio (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed1.103

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Cohort 4: Ae Total of Gepotidacin Following Single Dose of 1500 mg Under Fed Condition in Urine

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Ae total was calculated by adding all the fractions of drug collected over all the allotted time intervals. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours, 24-36 Hours, 36-48 Hours post-dose in each Treatment Periods 1 and 2

InterventionMilligrams (Geometric Mean)
Cohort 4: Gepotidacin 1500 mg Fed293.50

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Cohort 4: Ae Total of Gepotidacin in Urine Following Two 3000 mg Doses-Fed State

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Ae total was calculated by adding all the fractions of drug collected over all the allotted time intervals. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-14 Hours, 14-16 Hours, 16-18 Hours, 18-20 Hours, 20-24 Hours, 24-36 Hours, 36-48 Hours, 48-60 Hours post-dose in Treatment Period 3

InterventionMilligrams (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed1334.42

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Cohort 4: Area Under the Concentration-time Curve From Time 0 (Pre-dose) to the Concentration at 24 Hours Post-dose (AUC[0-24]) of Gepotidacin Following Single Dose of 1500 mg in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 1500 mg Fed20.9
Cohort 4: Gepotidacin 1500 mg Fasted19.0

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Cohort 4: Area Under the Concentration-time Curve From Time 0 (Pre-dose) to the Concentration at 48 Hours Post-dose (AUC[0-48]) of Gepotidacin Following Single Dose of 1500 mg in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 1500 mg Fed21.9
Cohort 4: Gepotidacin 1500 mg Fasted20.0

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Cohort 4: AUC From Time 0 (Predose) to Time Tau (AUC[0-tau]) of Gepotidacin in Plasma After the First Dose of 3000 Mg-Fed State

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 minutes, 14 Hours, 14 Hours 30 minutes, 15, 16, 18, 20, 24, 36, 48, 60 Hours post-dose in Treatment Period 3

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed37.3

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Cohort 4: AUC(0-24) of Gepotidacin Following Single Dose of 1500 mg Under Fed Condition in Urine

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 1500 mg Fed2142.4

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Cohort 4: AUC(0-24) of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)-Fed State

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 minutes, 14 Hours, 14 Hours 30 minutes, 15, 16, 18, 20, 24 Hours post-dose in Treatment Period 3

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed84.6

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Cohort 4: AUC(0-24) of Gepotidacin in Urine Following Two 3000 mg Doses-Fed State

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-14 Hours, 14-16 Hours, 16-18 Hours, 18-20 Hours, 20-24 Hours post-dose in Treatment Period 3

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed14729.5

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Cohort 4: AUC(0-48) of Gepotidacin Following Single Dose of 1500 mg Under Fed Condition in Urine

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours, 24-36 Hours, 36-48 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 1500 mg Fed2293.7

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Cohort 4: AUC(0-48) of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)-Fed State

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 minutes, 14 Hours, 14 Hours 30 minutes, 15, 16, 18, 20, 24, 36, 48 Hours post-dose in Treatment Period 3

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed90.8

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Cohort 4: AUC(0-48) of Gepotidacin in Urine Following Two 3000 mg Doses-Fed State

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-14 Hours, 14-16 Hours, 16-18 Hours, 18-20 Hours, 20-24 Hours, 24-36 Hours, 36-48 Hours post-dose in Treatment Period 3

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed15768.2

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Cohort 4: AUC(0-infinity) of Gepotidacin Following Single Dose of 1500 mg in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 1500 mg Fed22.3
Cohort 4: Gepotidacin 1500 mg Fasted20.4

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Cohort 4: AUC(0-infinity) of Gepotidacin Following Single Dose of 1500 mg in Plasma - Food Effect in Japanese Participants

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*Micrograms per milliliter (Geometric Least Squares Mean)
Cohort 4: Gepotidacin 1500 mg Fed22.3
Cohort 4: Gepotidacin 1500 mg Fasted20.4

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Cohort 4: AUC(0-t) of Gepotidacin Following Single Dose of 1500 mg in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 1500 mg Fed21.9
Cohort 4: Gepotidacin 1500 mg Fasted20.0

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Cohort 4: AUC(0-t) of Gepotidacin Following Single Dose of 1500 mg in Plasma - Food Effect in Japanese Participants

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*Micrograms per milliliter (Geometric Least Squares Mean)
Cohort 4: Gepotidacin 1500 mg Fed21.9
Cohort 4: Gepotidacin 1500 mg Fasted20.0

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Cohort 4: AUC(0-t) of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)-Fed State

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 minutes, 14 Hours, 14 Hours 30 minutes, 15, 16, 18, 20, 24, 36, 48, 60 Hours post-dose in Treatment Period 3

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed91.4

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Cohort 4: AUC(0-tau) of Gepotidacin Following Single Dose of 1500 mg Under Fed Condition in Urine

Urine samples were collected at indicated time points. AUC(0-tau) can be calculated only for multiple doses and not for single dose as tau refers to the dosing interval. Hence, AUC(0-tau) could not be calculated for Gepotidacin 1500 mg single dose as mentioned in Reporting and Analysis Plan. The results for this outcome measure will never be posted. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours, 24-36 Hours, 36-48 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 1500 mg FedNA

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Cohort 4: AUC(0-tau) of Gepotidacin in Plasma After the Second Dose of 3000 mg (Evening Dose)-Fed State

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 minutes, 14 Hours, 14 Hours 30 minutes, 15, 16, 18, 20, 24, 36, 48, 60 Hours post-dose in Treatment Period 3

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed46.7

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Cohort 2: CL/F of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionLiters per Hour (Geometric Mean)
Cohort 2:Period 1: Gepotidacin 1500 mg77.55
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg155.43

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Cohort 4: CL/F of Gepotidacin Following Single Dose of 1500 mg in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionLiters per Hour (Geometric Mean)
Cohort 4: Gepotidacin 1500 mg Fed67.26
Cohort 4: Gepotidacin 1500 mg Fasted73.50

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Cohort 4: CL/F of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)-Fed State

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 minutes, 14 Hours, 14 Hours 30 minutes, 15, 16, 18, 20, 24, 36, 48, 60 Hours post-dose in Treatment Period 3

InterventionLiters per Hour (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed68.83

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Cohort 4: CLr of Gepotidacin Following Single Dose of 1500 mg Under Fed Condition

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours, 24-36 Hours, 36-48 Hours post-dose in each Treatment Periods 1 and 2

InterventionLiters per Hour (Geometric Mean)
Cohort 4: Gepotidacin 1500 mg Fed13.42

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Cohort 4: CLr of Gepotidacin Following Two 3000 mg Dose-Fed State

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-14 Hours, 14-16 Hours, 16-18 Hours, 18-20 Hours, 20-24 Hours, 24-36 Hours, 36-48 Hours, 48-60 Hours post-dose in Treatment Period 3

InterventionLiters per Hour (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed14.61

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Cohort 4: Cmax of Gepotidacin Following Single Dose of 1500 mg in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionMicrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 1500 mg Fed5.436
Cohort 4: Gepotidacin 1500 mg Fasted5.143

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Cohort 4: Cmax of Gepotidacin Following Single Dose of 1500 mg in Plasma - Food Effect in Japanese Participants

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionMicrograms per milliliter (Geometric Least Squares Mean)
Cohort 4: Gepotidacin 1500 mg Fed5.421
Cohort 4: Gepotidacin 1500 mg Fasted5.158

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Cohort 4: Cmax of Gepotidacin in Plasma After the First Dose of 3000 mg -Fed State

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 minutes, 14 Hours, 14 Hours 30 minutes, 15, 16, 18, 20, 24, 36, 48, 60 Hours post-dose in Treatment Period 3

InterventionMicrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed11.204

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Cohort 4: Cmax of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)-Fed State

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 minutes, 14 Hours, 14 Hours 30 minutes, 15, 16, 18, 20, 24, 36, 48, 60 Hours post-dose in Treatment Period 3

InterventionMicrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed12.363

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Cohort 4: Percentage of the Given Dose of Drug Excreted in Urine (fe%) for Gepotidacin 1500 mg Under Fed Condition

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. fe% was calculated as: (Ae total divided by Dose) multiplied by 100%. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours, 24-36 Hours, 36-48 Hours post-dose in each Treatment Periods 1 and 2

InterventionPercent dose excreted (Geometric Mean)
Cohort 4: Gepotidacin 1500 mg Fed19.57

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Cohort 4: Percentage of the Given Dose of Drug Excreted in Urine (fe%) of Gepotidacin Following Two 3000 mg Doses-Fed State

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. fe% was calculated as: (Ae total divided by Dose) multiplied by 100 %. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-14 Hours, 14-16 Hours, 16-18 Hours, 18-20 Hours, 20-24 Hours, 24-36 Hours, 36-48 Hours, 48-60 Hours post-dose in Treatment Period 3

InterventionPercent dose excreted (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed22.24

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Cohort 4: T1/2 of Gepotidacin Following Single Dose of 1500 mg in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours (Geometric Mean)
Cohort 4: Gepotidacin 1500 mg Fed12.848
Cohort 4: Gepotidacin 1500 mg Fasted12.540

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Cohort 4: T1/2 of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose )-Fed State

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 minutes, 14 Hours, 14 Hours 30 minutes, 15, 16, 18, 20, 24, 36, 48, 60 Hours post-dose in Treatment Period 3

InterventionHours (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed12.599

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Cohort 4: Tlag of Gepotidacin Following Single Dose of 1500 mg in Plasma - Food Effect in Japanese Participants

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours (Median)
Cohort 4: Gepotidacin 1500 mg Fed0.000
Cohort 4: Gepotidacin 1500 mg Fasted0.000

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Cohort 4: Tlag of Gepotidacin in Plasma After the First Dose of 3000 mg (First Dose)-Fed State

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 minutes, 14 Hours, 14 Hours 30 minutes, 15, 16, 18, 20, 24, 36, 48, 60 Hours post-dose in Treatment Period 3

InterventionHours (Median)
Cohort 4: Gepotidacin 3000 mg Fed0

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Cohort 4: Tmax of Gepotidacin Following Single Dose of 1500 mg in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours (Median)
Cohort 4: Gepotidacin 1500 mg Fed2.000
Cohort 4: Gepotidacin 1500 mg Fasted1.500

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Cohort 4: Tmax of Gepotidacin Following Single Dose of 1500 mg in Plasma - Food Effect in Japanese Participants

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours (Median)
Cohort 4: Gepotidacin 1500 mg Fed2.000
Cohort 4: Gepotidacin 1500 mg Fasted1.500

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Cohort 4: Tmax of Gepotidacin in Plasma After the First Dose of 3000 mg -Fed State

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 minutes, 14 Hours, 14 Hours 30 minutes, 15, 16, 18, 20, 24, 36, 48, 60 Hours post-dose in Treatment Period 3

InterventionHours (Median)
Cohort 4: Gepotidacin 3000 mg Fed2.000

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Cohort 4: Tmax of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)-Fed State

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 minutes, 14 Hours, 14 Hours 30 minutes, 15, 16, 18, 20, 24, 36, 48, 60 Hours post-dose in Treatment Period 3

InterventionHours (Median)
Cohort 4: Gepotidacin 3000 mg Fed2.000

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Cohort 4: Vz/F of Gepotidacin Following Single Dose of 1500 mg in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionLiters (Geometric Mean)
Cohort 4: Gepotidacin 1500 mg Fed1246.70
Cohort 4: Gepotidacin 1500 mg Fasted1329.83

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Cohort 4: Vz/F of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)-Fed State

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 minutes, 14 Hours, 14 Hours 30 minutes, 15, 16, 18, 20, 24, 36, 48, 60 Hours post-dose in Treatment Period 3

InterventionLiters (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed1251.05

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Cohort 1: Amount of Drug Excreted in Urine in a Time Interval (Ae[t1-t2]) of Gepotidacin

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Ae(t1-t2) measured the amount of drug excreted in urine at defined time intervals. (NCT04493931)
Timeframe: 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours, 24-36 Hours, 36-48 Hours post-dose in each Treatment periods 1 and 2

,
InterventionMilligrams (Geometric Mean)
Ae (0-2), n=14, 13Ae (2-4), n=14, 12Ae (4-6), n=14, 13Ae (6-8); n=14, 13Ae (8-12), n=12, 13Ae (12-24), n=14, 13Ae (24-36), n=14, 13Ae (36-48), n=14, 13
Cohort 1: Gepotidacin 1500 mg28.6689.1850.5234.3829.9025.4410.884.50
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mgNA142.9982.7746.2230.9722.048.764.08

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Cohort 1: Number of Participants With Any Increase in Maximum Post-Baseline ECG Parameter QTc Interval

A 12-lead ECG was recorded with the participant in a semi-supine position after a rest of at least 10 minutes using an ECG machine that automatically calculated the QTc interval. Number of participants with any increase of >450 milliseconds in corrected QT interval using the QTcB Interval and QTcF Interval has been reported. (NCT04493931)
Timeframe: Up to 17 days

,
InterventionParticipants (Count of Participants)
QTcB IntervalQTcF Interval
Cohort 1: Gepotidacin 1500 mg30
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg41

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Cohort 1: Number of Participants With SAE and Non-SAE

An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of a study intervention, whether or not considered related to the study intervention. An SAE is defined as any serious adverse event that, at any dose results in death, is life-threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth defect or any other situations as per Medical or scientific judgment. (NCT04493931)
Timeframe: Up to 17 days

,
InterventionParticipants (Count of Participants)
Any SAEAny non-SAE
Cohort 1: Gepotidacin 1500 mg00
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg00

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Cohort 1: Number of Participants With Worst Case Clinical Chemistry Results Relative to Normal Range Post-Baseline Relative to Baseline

Blood samples were collected at indicated time points for analysis of clinical chemistry parameters including ALT, Albumin, Alk Phos, AST, Bilirubin, Calcium, Carbon Dioxide, Chloride, Creatine Kinase, Creatinine, Direct Bilirubin, Glucose, Magnesium, Potassium, Protein, Sodium, BUN. Participants were counted in the worst case category that their value changes to (low, normal or high), unless there was no change in their category. Participants whose lab value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the 'To Normal or No Change' category. Participants were counted twice if the participant had values that changed 'To Low' and 'To High', so the percentages may not add to 100%. High and low indicated that participants had values flagged as high and low respectively for the particular parameter any time on-treatment. (NCT04493931)
Timeframe: Up to 17 days

,
InterventionParticipants (Count of Participants)
ALT; To LowALT; To Normal or No ChangeALT; To HighAlbumin; To LowAlbumin; To Normal or No ChangeAlbumin; To HighAlk Phos; To LowAlk Phos; To Normal or No ChangeAlk Phos; To HighAST; To LowAST; To Normal or No ChangeAST; To HighBilirubin; To LowBilirubin; To Normal or No ChangeBilirubin; To HighCalcium; To LowCalcium; To Normal or No ChangeCalcium; To HighCarbon Dioxide; To LowCarbon Dioxide; To Normal or No ChangeCarbon Dioxide; To HighChloride; To LowChloride; To Normal or No ChangeChloride; To HighCreatine Kinase; To LowCreatine Kinase; To Normal or No ChangeCreatine Kinase; To HighCreatinine; To LowCreatinine; To Normal or No ChangeCreatinine; To HighDirect Bilirubin; To LowDirect Bilirubin; To Normal or No ChangeDirect Bilirubin; To HighGlucose; To LowGlucose; To Normal or No ChangeGlucose; To HighMagnesium; To LowMagnesium; To Normal or No ChangeMagnesium; To HighPotassium; To LowPotassium; To Normal or No ChangePotassium; To HighProtein; To LowProtein; To Normal or No ChangeProtein; To HighSodium; To LowSodium; To Normal or No ChangeSodium; To HighBUN; To LowBUN; To Normal or No ChangeBUN; To High
Cohort 1: Gepotidacin 1500 mg01400140014001400140014011300140113001400140014001400140014001400140
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg01121120013001211120013001300121013001030130013001300121013001300130

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Cohort 1: Number of Participants With Worst Case Hematology Results Relative to Normal Range Post-Baseline Relative to Baseline

Blood samples were collected at indicated time points for analysis of hematology parameters including Basophils, Eosinophils, MCH, MCV, Erythrocytes, Hematocrit, Hemoglobin, Leukocytes, Lymphocytes, Monocytes, Neutrophils, Platelets. Participants were counted in the worst case category that their value changes to (low, normal or high), unless there was no change in their category. Participants whose lab value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the 'To Normal or No Change' category. Participants were counted twice if the participant had values that changed 'To Low' and 'To High', so the percentages may not add to 100 %. High and low indicated that participants had values flagged as high and low respectively for the particular parameter any time on-treatment. (NCT04493931)
Timeframe: Up to 17 days

,
InterventionParticipants (Count of Participants)
Basophils; To LowBasophils; To Normal or No ChangeBasophils; To HighEosinophils; To LowEosinophils; To Normal or No ChangeEosinophils; To HighMCH; To LowMCH; To Normal or No ChangeMCH; To HighMCV; To LowMCV; To Normal or No ChangeMCV; To HighErythrocytes; To LowErythrocytes; To Normal or No ChangeErythrocytes; To HighHematocrit; To LowHematocrit; To Normal or No ChangeHematocrit; To HighHemoglobin; To LowHemoglobin; To Normal or No ChangeHemoglobin; To HighLeukocytes; To LowLeukocytes; To Normal or No ChangeLeukocytes; To HighLymphocytes; To LowLymphocytes; To Normal or No ChangeLymphocytes; To HighMonocytes; To LowMonocytes; To Normal or No ChangeMonocytes; To HighNeutrophils; To LowNeutrophils; To Normal or No ChangeNeutrophils; To HighPlatelets; To LowPlatelets; To Normal or No ChangePlatelets; To High
Cohort 1: Gepotidacin 1500 mg014001400140013101400131014001310140013101310140
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg011201300130013021101120013001300121013011200130

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Cohort 1: Number of Participants With Worst Case Urinalysis Results Relative to Normal Range Post-Baseline Relative to Baseline

Urine samples were collected at indicated time points for the analysis of urinalysis parameters including pH of urine, presence of glucose, protein, blood, ketones, bilirubin, nitrite, leukocyte esterase in urine by dipstick. Specific gravity of urine was measured by microscopic examination. Participants were counted in the worst case category that their value changes to (low, normal, high, or abnormal), unless there is no change in their category. Participants whose lab value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the 'To Normal or No Change' category. Participants were counted twice if the participant has values that changed 'To Low' and 'To High', so the percentages may not add to 100%. High and low indicated that participants had values flagged as high and low respectively for the particular parameter any time on-treatment. (NCT04493931)
Timeframe: Up to 17 days

,
InterventionParticipants (Count of Participants)
Bilirubin; To Normal or No ChangeBilirubin; To AbnormalGlucose; To Normal or No ChangeGlucose; To AbnormalKetones; To Normal or No ChangeKetones; To AbnormalLeukocyte Esterase; To Normal or No ChangeLeukocyte Esterase; To AbnormalNitrite; To Normal or No ChangeNitrite; To AbnormalOccult Blood; To Normal or No ChangeOccult Blood; To AbnormalProtein; To Normal or No ChangeProtein; To AbnormalpH; To LowpH; To Normal or No ChangepH; To HighSpecific Gravity; To LowSpecific Gravity; To Normal or No ChangeSpecific Gravity; To High
Cohort 1: Gepotidacin 1500 mg14014014012214013114001400131
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg13013013013013011213001300130

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Cohort 1: Number of Participants With Worst Case Vital Sign Results Relative to Normal Range Post-Baseline Relative to Baseline

Vital signs including SBP, DBP and pulse rate were measured in a semi-supine position after 5 minutes rest. Participants were counted in the worst case category that their value changes to (low, normal or high), unless there was no change in their category. Participants whose value category was unchanged (e.g., High to High), or whose value became normal, were recorded in the 'To Normal or No Change' category. Participants were counted twice if the participant had values that changed 'To Low' and 'To High', so the percentages may not add to 100%. High and low indicated that participants had values flagged as high and low respectively for the particular parameter any time on-treatment. (NCT04493931)
Timeframe: Up to 17 days

,
InterventionParticipants (Count of Participants)
DBP; To LowDBP; To Normal or No ChangeDBP; To HighSBP; To LowSBP; To Normal or No ChangeSBP; To HighPulse rate; To LowPulse rate; To Normal or No ChangePulse rate; To High
Cohort 1: Gepotidacin 1500 mg014001400140
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg013001300130

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Cohort 2: Ae(t1-t2) of Gepotidacin

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Ae(t1-t2) measured the amount of drug excreted in urine at defined time intervals. (NCT04493931)
Timeframe: 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours, 24-36 Hours, 36-48 Hours post-dose in each Treatment Periods 1 and 2

,
InterventionMilligrams (Geometric Mean)
Ae (0-2)Ae (2-4)Ae (4-6)Ae (6-8)Ae (8-12)Ae (12-24)Ae (24-36)Ae (36-48)
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mgNA55.8121.6613.829.1911.514.742.75
Cohort 2:Period 1: Gepotidacin 1500 mg12.6779.8467.4833.9227.5921.1711.043.61

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Cohort 2: Number of Participants With Any Increase in Maximum Post-Baseline ECG Parameter QTc Interval

A 12-lead ECG was recorded with the participant in a semi-supine position after a rest of at least 10 minutes using an ECG machine that automatically calculated the QTc interval. Number of participants with any increase of >450 milliseconds in corrected QT interval using the QTcB Interval and QTcF Interval has been reported. (NCT04493931)
Timeframe: Up to 26 days

,
InterventionParticipants (Count of Participants)
QTcB IntervalQTcF Interval
Cohort 2: Period 1: Gepotidacin 1500 mg20
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg21

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Cohort 2: Number of Participants With SAE and Non-SAE

An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of a study intervention, whether or not considered related to the study intervention. An SAE is defined as any serious adverse event that, at any dose results in death, is life-threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth defect or any other situations as per Medical or scientific judgment. (NCT04493931)
Timeframe: Up to 26 days

,,
InterventionParticipants (Count of Participants)
Any SAEAny non-SAE
Cohort 2: Period 1: Gepotidacin 1500 mg03
Cohort 2: Period 2 (Days 1 to 7) Rifampicin 600 mg02
Cohort 2: Period 2 (Days 8 to 9) Gepotidacin 1500 mg + Rifampicin 600 mg02

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Cohort 2: Number of Participants With Worst Case Clinical Chemistry Results Relative to Normal Range Post-Baseline Relative to Baseline

Blood samples were collected at indicated time points for analysis of clinical chemistry parameters including ALT, Albumin, Alk Phos, AST, Bilirubin, Calcium, Carbon Dioxide, Chloride, Creatine Kinase, Creatinine, Direct Bilirubin, Glucose, Magnesium, Potassium, Protein, Sodium, BUN. Participants were counted in the worst case category that their value changes to (low, normal or high), unless there was no change in their category. Participants whose lab value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the 'To Normal or No Change' category. Participants were counted twice if the participant had values that changed 'To Low' and 'To High', so the percentages may not add to 100%. High and low indicated that participants had values flagged as high and low respectively for the particular parameter any time on-treatment. (NCT04493931)
Timeframe: Up to 26 days

,
InterventionParticipants (Count of Participants)
ALT; To LowALT; To Normal or No ChangeALT; To HighAlbumin; To LowAlbumin; To Normal or No ChangeAlbumin; To HighAlk Phos; To LowAlk Phos; To Normal or No ChangeAlk Phos; To HighAST; To LowAST; To Normal or No ChangeAST; To HighBilirubin; To LowBilirubin; To Normal or No ChangeBilirubin; To HighCalcium; To LowCalcium; To Normal or No ChangeCalcium; To HighCarbon Dioxide; To LowCarbon Dioxide; To Normal or No ChangeCarbon Dioxide; To HighChloride; To LowChloride; To Normal or No ChangeChloride; To HighCreatine Kinase; To LowCreatine Kinase; To Normal or No ChangeCreatine Kinase; To HighCreatinine; To LowCreatinine; To Normal or No ChangeCreatinine; To HighDirect Bilirubin; To LowDirect Bilirubin; To Normal or No ChangeDirect Bilirubin; To HighGlucose; To LowGlucose; To Normal or No ChangeGlucose; To HighMagnesium; To LowMagnesium; To Normal or No ChangeMagnesium; To HighPotassium; To LowPotassium; To Normal or No ChangePotassium; To HighProtein; To LowProtein; To Normal or No ChangeProtein; To HighSodium; To LowSodium; To Normal or No ChangeSodium; To HighBUN; To LowBUN; To Normal or No ChangeBUN; To High
Cohort 2: Period 1: Gepotidacin 1500 mg01700170017001700170017001700170017001610170017001700161017001700170
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg01520170017001612150017031400170017001610170016101700152017001700170

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Cohort 2: Number of Participants With Worst Case Hematology Results Relative to Normal Range Post-Baseline Relative to Baseline

Blood samples were collected at indicated time points for analysis of hematology parameters including Basophils, Eosinophils, MCH, MCV, Erythrocytes, Hematocrit, Hemoglobin, Leukocytes, Lymphocytes, Monocytes, Neutrophils, Platelets. Participants were counted in the worst case category that their value changes to (low, normal or high), unless there was no change in their category. Participants whose lab value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the 'To Normal or No Change' category. Participants were counted twice if the participant had values that changed 'To Low' and 'To High', so the percentages may not add to 100%. High and low indicated that participants had values flagged as high and low respectively for the particular parameter any time on-treatment. (NCT04493931)
Timeframe: Up to 26 days

,
InterventionParticipants (Count of Participants)
Basophils; To LowBasophils; To Normal or No ChangeBasophils; To HighEosinophils; To LowEosinophils; To Normal or No ChangeEosinophils; To HighMCH; To LowMCH; To Normal or No ChangeMCH; To HighMCV; To LowMCV; To Normal or No ChangeMCV; To HighErythrocytes; To LowErythrocytes; To Normal or No ChangeErythrocytes; To HighHematocrit; To LowHematocrit; To Normal or No ChangeHematocrit; To HighHemoglobin; To LowHemoglobin; To Normal or No ChangeHemoglobin; To HighLeukocytes; To LowLeukocytes; To Normal or No ChangeLeukocytes; To HighLymphocytes; To LowLymphocytes; To Normal or No ChangeLymphocytes; To HighMonocytes; To LowMonocytes; To Normal or No ChangeMonocytes; To HighNeutrophils; To LowNeutrophils; To Normal or No ChangeNeutrophils; To HighPlatelets; To LowPlatelets; To Normal or No ChangePlatelets; To High
Cohort 2: Period 1: Gepotidacin 1500 mg017001520170017001700143017001700170115101700170
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg016101430170017001700152017011600152314041300161

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Cohort 2: Number of Participants With Worst Case Urinalysis Results Relative to Normal Range Post-Baseline Relative to Baseline

Urine samples were collected at indicated time points for the analysis of urinalysis parameters including pH of urine, presence of glucose, protein, blood, ketones, bilirubin, nitrite, leukocyte esterase in urine by dipstick. Specific gravity of urine was measured by microscopic examination. Participants were counted in the worst case category that their value changes to (low, normal, high, or abnormal), unless there is no change in their category. Participants whose lab value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the 'To Normal or No Change' category. Participants were counted twice if the participant has values that changed 'To Low' and 'To High', so the percentages may not add to 100%. High and low indicated that participants had values flagged as high and low respectively for the particular parameter any time on-treatment. (NCT04493931)
Timeframe: Up to 26 days

,
InterventionParticipants (Count of Participants)
Bilirubin; To Normal or No ChangeBilirubin; To AbnormalGlucose; To Normal or No ChangeGlucose; To AbnormalKetones; To Normal or No ChangeKetones; To AbnormalLeukocyte Esterase; To Normal or No ChangeLeukocyte Esterase; To AbnormalNitrite; To Normal or No ChangeNitrite; To AbnormalOccult Blood; To Normal or No ChangeOccult Blood; To AbnormalProtein; To Normal or No ChangeProtein; To AbnormalpH; To LowpH; To Normal or No ChangepH; To HighSpecific Gravity; To LowSpecific Gravity; To Normal or No ChangeSpecific Gravity; To High
Cohort 2: Period 1: Gepotidacin 1500 mg17017017016117017017001700143
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg16016016014215114216001600151

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Cohort 2: Number of Participants With Worst Case Vital Sign Results Relative to Normal Range Post-Baseline Relative to Baseline

Vital signs including SBP, DBP and pulse rate were measured in a semi-supine position after 5 minutes rest. Participants were counted in the worst case category that their value changes to (low, normal or high), unless there was no change in their category. Participants whose value category was unchanged (e.g., High to High), or whose value became normal, were recorded in the 'To Normal or No Change' category. Participants were counted twice if the participant had values that changed 'To Low' and 'To High', so the percentages may not add to 100%. High and low indicated that participants had values flagged as high and low respectively for the particular parameter any time on-treatment. (NCT04493931)
Timeframe: Up to 26 days

,
InterventionParticipants (Count of Participants)
DBP; To LowDBP; To Normal or No ChangeDBP; To HighSBP; To LowSBP; To Normal or No ChangeSBP; To HighPulse rate; To LowPulse rate; To Normal or No ChangePulse rate; To High
Cohort 2: Period 1: Gepotidacin 1500 mg016101700170
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg014001400140

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Cohort 3: Amount of Drug Excreted in Urine in a Time Interval (Ae[t1-t2]) of Gepotidacin Following Two 3000 mg Doses (First Dose + Second Dose)

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Ae(t1-t2) measured the amount of drug excreted in urine at defined time intervals. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-14 Hours, 14-16 Hours, 16-18 Hours, 18-20 Hours, 20-24 Hours, 24-36 Hours, 36-48 Hours, 48-60 Hours post-dose in each Treatment Periods 1 and 2

InterventionMilligrams (Geometric Mean)
Ae (0-2), n=17Ae (2-4), n=18Ae (4-6), n=16Ae (6-8); n=16Ae (8-12), n=18Ae (12-14), n=17Ae (14-16), n=15Ae (16-18), n=14Ae (18-20), n=15Ae (20-24), n=17Ae (24-36), n=18Ae (36-48); n=18Ae (48-60), n=18
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mgNA117.61103.1170.9867.4264.49142.36146.8993.0574.4470.0120.168.51

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Cohort 3: Number of Participants With Any Increase in Maximum Post-Baseline ECG Parameter QTc Interval

A 12-lead ECG was recorded with the participant in a semi-supine position after a rest of at least 10 minutes using an ECG machine that automatically calculated the QTc interval. Number of participants with any increase of >450 milliseconds in corrected QT interval using the QTcB Interval and QTcF Interval has been reported. (NCT04493931)
Timeframe: Up to 30 days

,
InterventionParticipants (Count of Participants)
QTcB IntervalQTcF Interval
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg20
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg50

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Cohort 3: Number of Participants With SAE and Non-SAE

An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of a study intervention, whether or not considered related to the study intervention. An SAE is defined as any serious adverse event that, at any dose results in death, is life-threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth defect or any other situations as per Medical or scientific judgment. (NCT04493931)
Timeframe: Up to 30 days

,
InterventionParticipants (Count of Participants)
Any SAEAny non-SAE
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg01
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg011

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Cohort 3: Number of Participants With Worst Case Clinical Chemistry Results Relative to Normal Range Post-Baseline Relative to Baseline

Blood samples were collected at indicated time points for analysis of clinical chemistry parameters including ALT, Albumin, Alk Phos, AST, Bilirubin, Calcium, Carbon Dioxide, Chloride, Creatine Kinase, Creatinine, Direct Bilirubin, Glucose, Magnesium, Potassium, Protein, Sodium, BUN. Participants were counted in the worst case category that their value changes to (low, normal or high), unless there was no change in their category. Participants whose lab value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the 'To Normal or No Change' category. Participants were counted twice if the participant had values that changed 'To Low' and 'To High', so the percentages may not add to 100%. High and low indicated that participants had values flagged as high and low respectively for the particular parameter any time on-treatment. (NCT04493931)
Timeframe: Up to 30 days

,
InterventionParticipants (Count of Participants)
ALT; To LowALT; To Normal or No ChangeALT; To HighAlbumin; To LowAlbumin; To Normal or No ChangeAlbumin; To HighAlk Phos; To LowAlk Phos; To Normal or No ChangeAlk Phos; To HighAST; To LowAST; To Normal or No ChangeAST; To HighBilirubin; To LowBilirubin; To Normal or No ChangeBilirubin; To HighCalcium; To LowCalcium; To Normal or No ChangeCalcium; To HighCarbon Dioxide; To LowCarbon Dioxide; To Normal or No ChangeCarbon Dioxide; To HighChloride; To LowChloride; To Normal or No ChangeChloride; To HighCreatine Kinase; To LowCreatine Kinase; To Normal or No ChangeCreatine Kinase; To HighCreatinine; To LowCreatinine; To Normal or No ChangeCreatinine; To HighDirect Bilirubin; To LowDirect Bilirubin; To Normal or No ChangeDirect Bilirubin; To HighGlucose; To LowGlucose; To Normal or No ChangeGlucose; To HighMagnesium; To LowMagnesium; To Normal or No ChangeMagnesium; To HighPotassium; To LowPotassium; To Normal or No ChangePotassium; To HighProtein; To LowProtein; To Normal or No ChangeProtein; To HighSodium; To LowSodium; To Normal or No ChangeSodium; To HighBUN; To LowBUN; To Normal or No ChangeBUN; To High
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg01901180019001810190118001900190018101900190019001900181019001900190
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg01710171018001800180117001800171018001800180018001800180018001801170

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Cohort 3: Number of Participants With Worst Case Hematology Results Relative to Normal Range Post-Baseline Relative to Baseline

Blood samples were collected at indicated time points for analysis of hematology parameters including Basophils, Eosinophils, MCH, MCV, Erythrocytes, Hematocrit, Hemoglobin, Leukocytes, Lymphocytes, Monocytes, Neutrophils, Platelets. Participants were counted in the worst case category that their value changes to (low, normal or high), unless there was no change in their category. Participants whose lab value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the 'To Normal or No Change' category. Participants were counted twice if the participant had values that changed 'To Low' and 'To High', so the percentages may not add to 100%. High and low indicated that participants had values flagged as high and low respectively for the particular parameter any time on-treatment. (NCT04493931)
Timeframe: Up to 30 days

,
InterventionParticipants (Count of Participants)
Basophils; To LowBasophils; To Normal or No ChangeBasophils; To HighEosinophils; To LowEosinophils; To Normal or No ChangeEosinophils; To HighMCH; To LowMCH; To Normal or No ChangeMCH; To HighMCV; To LowMCV; To Normal or No ChangeMCV; To HighErythrocytes; To LowErythrocytes; To Normal or No ChangeErythrocytes; To HighHematocrit; To LowHematocrit; To Normal or No ChangeHematocrit; To HighHemoglobin; To LowHemoglobin; To Normal or No ChangeHemoglobin; To HighLeukocytes; To LowLeukocytes; To Normal or No ChangeLeukocytes; To HighLymphocytes; To LowLymphocytes; To Normal or No ChangeLymphocytes; To HighMonocytes; To LowMonocytes; To Normal or No ChangeMonocytes; To HighNeutrophils; To LowNeutrophils; To Normal or No ChangeNeutrophils; To HighPlatelets; To LowPlatelets; To Normal or No ChangePlatelets; To High
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg019001900190018121701171018101900190018101900190
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg018001620180018011702142115201710171117001710180

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Cohort 3: Number of Participants With Worst Case Urinalysis Results Relative to Normal Range Post-Baseline Relative to Baseline

Urine samples were collected at indicated time points for the analysis of urinalysis parameters including pH of urine, presence of glucose, protein, blood, ketones, bilirubin, nitrite, leukocyte esterase in urine by dipstick. Specific gravity of urine was measured by microscopic examination. Participants were counted in the worst case category that their value changes to (low, normal, high, or abnormal), unless there is no change in their category. Participants whose lab value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the 'To Normal or No Change' category. Participants were counted twice if the participant has values that changed 'To Low' and 'To High', so the percentages may not add to 100%. High and low indicated that participants had values flagged as high and low respectively for the particular parameter any time on-treatment. (NCT04493931)
Timeframe: Up to 30 days

,
InterventionParticipants (Count of Participants)
Bilirubin; To Normal or No ChangeBilirubin; To AbnormalGlucose; To Normal or No ChangeGlucose; To AbnormalKetones; To Normal or No ChangeKetones; To AbnormalLeukocyte Esterase; To Normal or No ChangeLeukocyte Esterase; To AbnormalNitrite; To Normal or No ChangeNitrite; To AbnormalOccult Blood; To Normal or No ChangeOccult Blood; To AbnormalProtein; To Normal or No ChangeProtein; To AbnormalpH; To LowpH; To Normal or No ChangepH; To HighSpecific Gravity; To LowSpecific Gravity; To Normal or No ChanSpecific Gravity; To High
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg19019016313619014516301900163
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg18018017113518013516201800108

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Cohort 3: Number of Participants With Worst Case Vital Sign Results Relative to Normal Range Post-Baseline Relative to Baseline

Vital signs including SBP, DBP and pulse rate were measured in a semi-supine position after 5 minutes rest. Participants were counted in the worst case category that their value changes to (low, normal or high), unless there was no change in their category. Participants whose value category was unchanged (e.g., High to High), or whose value became normal, were recorded in the 'To Normal or No Change' category. Participants were counted twice if the participant had values that changed 'To Low' and 'To High', so the percentages may not add to 100%. High and low indicated that participants had values flagged as high and low respectively for the particular parameter any time on-treatment. (NCT04493931)
Timeframe: Up to 30 days

,
InterventionParticipants (Count of Participants)
DBP; To LowDBP; To Normal or No ChangeDBP; To HighSBP; To LowSBP; To Normal or No ChangeSBP; To HighPulse rate; To LowPulse rate; To Normal or No ChangePulse rate; To High
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg019001900190
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg018001800180

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Cohort 4: Ae(t1-t2) of Gepotidacin Following Single Dose of 1500 mg Under Fed Condition in Urine

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Ae(t1-t2) measured the amount of drug excreted in urine at defined time intervals. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours, 24-36 Hours, 36-48 Hours post-dose in each Treatment Periods 1 and 2

InterventionMilligrams (Geometric Mean)
Ae (0-2)Ae (2-4)Ae (4-6)Ae (6-8)Ae (8-12)Ae (12-24)Ae (24-36)Ae (36-48)
Cohort 4: Gepotidacin 1500 mg FedNA102.2360.0531.6116.5117.165.724.28

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Cohort 4: Ae(t1-t2) of Gepotidacin in Urine Following Two 3000 mg Doses-Fed State

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Ae(t1-t2) measured the amount of drug excreted in urine at defined time intervals. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-14 Hours, 14-16 Hours, 16-18 Hours, 18-20 Hours, 20-24 Hours, 24-36 Hours, 36-48 Hours, 48-60 Hours post-dose in Treatment Period 3

InterventionMilligrams (Geometric Mean)
Ae (0-2); n=11Ae (2-4); n=10Ae (4-6); n=11Ae (6-8); n=11Ae (8-12); n=11Ae (12-14); n=11Ae (14-16); n=11Ae (16-18); n=11Ae (18-20); n=11Ae (20-24); n=11Ae (24-36); n=11Ae (36-48); n=11Ae (48-60); n=10
Cohort 4: Gepotidacin 3000 mg FedNA221.19103.6867.5865.06112.83174.62136.6690.8180.5457.6214.479.67

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Cohort 1: Apparent Oral Clearance (CL/F) of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionLiters per Hour (Geometric Mean)
Cohort 1: Gepotidacin 1500 mg72.72
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg64.14

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Cohort 4: Number of Participants With Serious Adverse Events (SAE) and Non-serious Adverse Events (Non-SAE)

An adverse event (AE) is any untoward medical occurrence in a clinical study participant, temporally associated with the use of a study intervention, whether or not considered related to the study intervention. An SAE is defined as any serious adverse event that, at any dose results in death, is life-threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth defect or any other situations as per Medical or scientific judgment. (NCT04493931)
Timeframe: Up to 22 days

,,,
InterventionParticipants (Count of Participants)
Any SAEAny non-SAE
Cohort 4: Gepotidacin 1500 mg Fasted02
Cohort 4: Gepotidacin 1500 mg Fed01
Cohort 4: Gepotidacin 3000 mg Fed04
Cohort 4: Placebo00

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Cohort 4: Number of Participants With Worst Case Clinical Chemistry Results Relative to Normal Range Post-Baseline Relative to Baseline

Blood samples were collected at indicated time points for analysis of clinical chemistry parameters including Alanine Aminotransferase (ALT), Albumin, Alkaline Phosphatase (Alk Phos), Aspartate Aminotransferase (AST), Bilirubin, Calcium, Carbon Dioxide, Chloride, Creatine Kinase, Creatinine, Direct Bilirubin, Glucose, Magnesium, Potassium, Protein, Sodium, Blood Urea Nitrogen (BUN). Participants were counted in the worst case category that their value changes to (low, normal or high), unless there was no change in their category. Participants whose lab value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the 'To Normal or No Change' category. Participants were counted twice if the participant had values that changed 'To Low' and 'To High', so the percentages may not add to 100%. High and low indicated that participants had values flagged as high and low respectively for the particular parameter any time on-treatment. (NCT04493931)
Timeframe: Up to 22 days

,,,
InterventionParticipants (Count of Participants)
ALT; To LowALT; To Normal or No ChangeALT; To HighAlbumin; To LowAlbumin; To Normal or No ChangeAlbumin; To HighAlk Phos; To LowAlk Phos; To Normal or No ChangeAlk Phos; To HighAST; To LowAST; To Normal or No ChangeAST; To HighBilirubin; To LowBilirubin; To Normal or No ChangeBilirubin; To HighCalcium; To LowCalcium; To Normal or No ChangeCalcium; To HighCarbon Dioxide; To LowCarbon Dioxide; To Normal or No ChangeCarbon Dioxide; To HighChloride; To LowChloride; To Normal or No ChangeChloride; To HighCreatine Kinase; To LowCreatine Kinase; To Normal or No ChangeCreatine Kinase; To HighCreatinine; To LowCreatinine; To Normal or No ChangeCreatinine;To HighDirect Bilirubin; To LowDirect Bilirubin; To Normal or No ChangeDirect Bilirubin; To HighGlucose; To LowGlucose; To Normal or No ChangeGlucose; To HighMagnesium; To LowMagnesium; To Normal or No ChangeMagnesium; To HighPotassium; To LowPotassium; To Normal or No ChangePotassium; To HighProtein; To LowProtein; To Normal or No ChangeProtein; To HighSodium; To LowSodium; To Normal or No ChangeSodium; To HighBUN; To LowBUN; To Normal or No ChangeBUN; To High
Cohort 4: Gepotidacin 1500 mg Fasted01100110011001100110011011000110011001100110011001100110011001100110
Cohort 4: Gepotidacin 1500 mg Fed01100110011001100110011001100110011001100110011001100110011001100110
Cohort 4: Gepotidacin 3000 mg Fed0110011001100110011001100110011019101100110011001100110011001100110
Cohort 4: Placebo030120030030021030030030120030021030030021030030030

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Cohort 4: Number of Participants With Worst Case Hematology Results Relative to Normal Range Post-Baseline Relative to Baseline

Blood samples were collected at indicated time points for analysis of hematology parameters including Basophils, Eosinophils, Erythrocyte Mean Corpuscular Hemoglobin (MCH), Erythrocyte Mean Corpuscular Volume (MCV), Erythrocytes, Hematocrit, Hemoglobin, Leukocytes, Lymphocytes, Monocytes, Neutrophils, Platelets. Participants were counted in the worst case category that their value changes to (low, normal or high), unless there was no change in their category. Participants whose laboratory (lab) value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the 'To Normal or No Change' category. Participants were counted twice if the participant had values that changed 'To Low' and 'To High', so the percentages may not add to 100 (%). High and low indicated that participants had values flagged as high and low respectively for the particular parameter any time on-treatment. (NCT04493931)
Timeframe: Up to 22 days

,,,
InterventionParticipants (Count of Participants)
Basophils; To LowBasophils; To Normal or No ChangeBasophils; To HighEosinophils; To LowEosinophils; To Normal or No ChangeEosinophils; To HighMCH; To LowMCH; To Normal or No ChangeMCH; To HighMCV; To LowMCV; To Normal or No ChangeMCV; To HighErythrocytes; To LowErythrocytes; To Normal or No ChangeErythrocytes; To HighHematocrit; To LowHematocrit; To Normal or No ChangeHematocrit; To HighHemoglobin; To LowHemoglobin; To Normal or No ChangeHemoglobin; To HighLeukocytes; To LowLeukocytes; To Normal or No ChangeLeukocytes; To HighLymphocytes; To LowLymphocytes; To Normal or No ChangeLymphocytes; To HighMonocytes; To LowMonocytes; To Normal or No ChangeMonocytes; To HighNeutrophils; To LowNeutrophils; To Normal or No ChangeNeutrophils; To HighPlatelets; To LowPlatelets; To Normal or No ChangePlatelets; To High
Cohort 4: Gepotidacin 1500 mg Fasted09201010110010101100110011001100110011011000110
Cohort 4: Gepotidacin 1500 mg Fed011001010110010101010101010101100110011001100110
Cohort 4: Gepotidacin 3000 mg Fed01010101011009211000101011011000110011011001100
Cohort 4: Placebo030030030021030030030030030030030030

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Cohort 4: Number of Participants With Worst Case Urinalysis Results Relative to Normal Range Post-Baseline Relative to Baseline

Urine samples were collected at indicated time points for the analysis of urinalysis parameters including potential of hydrogen (pH) of urine, presence of glucose, protein, blood, ketones, bilirubin, nitrite, leukocyte esterase in urine by dipstick. Specific gravity of urine was measured by microscopic examination. Participants were counted in the worst case category that their value changes to (low, normal, high, or abnormal), unless there is no change in their category. Participants whose lab value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the 'To Normal or No Change' category. Participants were counted twice if the participant has values that changed 'To Low' and 'To High', so the percentages may not add to 100%. High and low indicated that participants had values flagged as high and low respectively for the particular parameter any time on-treatment. (NCT04493931)
Timeframe: Up to 22 days

,,,
InterventionParticipants (Count of Participants)
Bilirubin; To Normal or No ChangeBilirubin; To AbnormalGlucose; To Normal or No ChangeGlucose; To AbnormalKetones; To Normal or No ChangeKetones; To AbnormalLeukocyte Esterase; To Normal or No ChangeLeukocyte Esterase; To AbnormalNitrite; To Normal or No ChangeNitrite; To AbnormalOccult Blood; To Normal or No ChangeOccult Blood; To AbnormalProtein; To Normal or No ChangeProtein; To AbnormalpH; To LowpH; To Normal or No ChangepH; To HighSpecific Gravity; To LowSpecific Gravity; To Normal or No ChangeSpecific Gravity; To High
Cohort 4: Gepotidacin 1500 mg Fasted11011011011011010111001100110
Cohort 4: Gepotidacin 1500 mg Fed1101101109211011011001100110
Cohort 4: Gepotidacin 3000 mg Fed1101101109210110111001100110
Cohort 4: Placebo30302121302130030030

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Cohort 4: Number of Participants With Worst Case Vital Sign Results Relative to Normal Range Post-Baseline Relative to Baseline

Vital signs including systolic blood pressure (SBP), diastolic blood pressure (DBP) and pulse rate were measured in a semi-supine position after 5 minutes rest. Participants were counted in the worst case category that their value changes to (low, normal or high), unless there was no change in their category. Participants whose value category was unchanged (e.g., High to High), or whose value became normal, were recorded in the 'To Normal or No Change' category. Participants were counted twice if the participant had values that changed 'To Low' and 'To High', so the percentages may not add to 100%. High and low indicated that participants had values flagged as high and low respectively for the particular parameter any time on-treatment. (NCT04493931)
Timeframe: Up to 22 days

,,,
InterventionParticipants (Count of Participants)
DBP; To LowDBP; To Normal or No ChangeDBP; To HighSBP; To LowSBP; To Normal or No ChangeSBP; To HighPulse rate; To LowPulse rate; To Normal or No ChangePulse rate; To High
Cohort 4: Gepotidacin 1500 mg Fasted011011000110
Cohort 4: Gepotidacin 1500 mg Fed110011000110
Cohort 4: Gepotidacin 3000 mg Fed011001100110
Cohort 4: Placebo030030030

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Cohort 1: Apparent Volume of Distribution (Vz/F) of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionLiters (Geometric Mean)
Cohort 1: Gepotidacin 1500 mg1190.16
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg1143.29

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Cohort 1: Area Under the Concentration-time Curve From Time 0 (Pre-dose) to the Time of the Last Quantifiable Concentration (AUC [0-t]) of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90% CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Least Squares Mean)
Cohort 1: Gepotidacin 1500 mg20.3
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg23.4

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Cohort 1: AUC (0-24) of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 1: Gepotidacin 1500 mg19.3
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg21.9

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Cohort 1: AUC From Time 0 (Pre-dose) Extrapolated to Infinite Time (AUC[0-infinity]) of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90% CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours* micrograms per milliliter (Geometric Least Squares Mean)
Cohort 1: Gepotidacin 1500 mg20.6
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg23.9

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Cohort 1: AUC(0-24) of Gepotidacin in Urine

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90% CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours Post-dose in each Treatment periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Least Squares Mean)
Cohort 1: Gepotidacin 1500 mg3292.1
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg3612.4

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Cohort 1: AUC(0-48) of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 1: Gepotidacin 1500 mg20.3
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg23.0

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Cohort 1: AUC(0-48) of Gepotidacin in Urine

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90% CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours, 24-36 Hours, 36-48 Hours Post-dose in each Treatment periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Least Squares Mean)
Cohort 1: Gepotidacin 1500 mg3578.2
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg3831.1

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Cohort 1: Maximum Observed Concentration (Cmax) of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric least square (LS) mean and 90 percent (%) confidence interval (CI) of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionMicrograms per milliliter (Geometric Least Squares Mean)
Cohort 1: Gepotidacin 1500 mg4.817
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg4.548

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Cohort 1: Percentage of the Given Dose of Drug Excreted in Urine (fe%) of Gepotidacin

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. fe% was calculated as: (Ae total divided by Dose) multiplied by 100 percent (%). (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours, 24-36 Hours, 36-48 Hours Post-dose in each Treatment periods 1 and 2

InterventionPercent dose excreted (Geometric Mean)
Cohort 1: Gepotidacin 1500 mg22.72
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg26.90

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Cohort 1: Renal Clearance (CLr) of Gepotidacin

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90% CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours, 24-36 Hours, 36-48 Hours Post-dose in each Treatment periods 1 and 2

InterventionLiters per Hour (Geometric Least Squares Mean)
Cohort 1: Gepotidacin 1500 mg16.06
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg17.59

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Cohort 1: Terminal Phase Half-life (t1/2) of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90% CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours (Geometric Least Squares Mean)
Cohort 1: Gepotidacin 1500 mg11.344
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg12.415

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Cohort 1: Time to Reach Maximum Observed Concentration (Tmax) of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours (Median)
Cohort 1: Gepotidacin 1500 mg2.500
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg2.500

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Cohort 4: AUC(0-tau) of Gepotidacin in Urine Following Two 3000 mg Doses-Fed State

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-14 Hours, 14-16 Hours, 16-18 Hours, 18-20 Hours, 20-24 Hours, 24-36 Hours, 36-48 Hours, 48-60 Hours post-dose in Treatment Period 3

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed4996.9

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Cohort 1: Tlag of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours (Median)
Cohort 1: Gepotidacin 1500 mg0.000
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg0.000

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Cohort 1: Total Unchanged Drug (Ae Total) of Gepotidacin in Urine

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Ae total was calculated by adding all the fractions of drug collected over all the allotted time intervals. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours, 24-36 Hours, 36-48 Hours Post-dose in each Treatment periods 1 and 2

InterventionMilligrams (Geometric Least Squares Mean)
Cohort 1: Gepotidacin 1500 mg337.92
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg410.10

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Cohort 2: Ae Total of Gepotidacin in Urine

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Ae total was calculated by adding all the fractions of drug collected over all the allotted time intervals. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours, 24-36 Hours, 36-48 Hours post-dose in each Treatment Periods 1 and 2

InterventionMilligrams (Geometric Least Squares Mean)
Cohort 2:Period 1: Gepotidacin 1500 mg312.73
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg156.05

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Cohort 2: AUC(0-24) of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 2:Period 1: Gepotidacin 1500 mg17.9
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg8.9

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Cohort 2: AUC(0-24) of Gepotidacin in Urine

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Least Squares Mean)
Cohort 2:Period 1: Gepotidacin 1500 mg3081.3
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg1352.4

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Cohort 2: AUC(0-48) of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 2:Period 1: Gepotidacin 1500 mg19.0
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg9.5

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Cohort 2: AUC(0-48) of Gepotidacin in Urine

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours, 24-36 Hours, 36-48 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Least Squares Mean)
Cohort 2:Period 1: Gepotidacin 1500 mg3370.1
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg1476.8

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Cohort 2: AUC(0-infinity) of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Least Squares Mean)
Cohort 2:Period 1: Gepotidacin 1500 mg19.3
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg9.3

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Cohort 2: AUC(0-t) of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90% CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Least Squares Mean)
Cohort 2:Period 1: Gepotidacin 1500 mg19.0
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg9.0

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Cohort 2: CLr of Gepotidacin

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours, 24-36 Hours, 36-48 Hours post-dose in each Treatment Periods 1 and 2

InterventionLiters per Hour (Geometric Least Squares Mean)
Cohort 2:Period 1: Gepotidacin 1500 mg16.49
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg17.07

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Cohort 2: Cmax of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90% CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionMicrograms per milliliter (Geometric Least Squares Mean)
Cohort 2:Period 1: Gepotidacin 1500 mg3.735
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg2.728

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Cohort 2: Lag Time Before Observation of Drug Concentrations (Tlag) of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours (Median)
Cohort 2:Period 1: Gepotidacin 1500 mg0.000
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg0.000

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Cohort 2: Percentage of the Given Dose of Drug Excreted in Urine (fe%) of Gepotidacin

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. fe% was calculated as: (Ae total divided by Dose) multiplied by 100 %. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours, 24-36 Hours, 36-48 Hours post-dose in each Treatment Periods 1 and 2

InterventionPercent dose excreted (Geometric Mean)
Cohort 2:Period 1: Gepotidacin 1500 mg20.85
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg10.42

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Cohort 2: T1/2 of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours (Geometric Mean)
Cohort 2:Period 1: Gepotidacin 1500 mg10.882
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg10.972

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Cohort 2: Tmax of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours (Median)
Cohort 2:Period 1: Gepotidacin 1500 mg2.500
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg2.000

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Cohort 2: Vz/F of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionLiters (Geometric Mean)
Cohort 2:Period 1: Gepotidacin 1500 mg1217.45
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg2460.46

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Cohort 3: Ae Total of Gepotidacin in Urine Following Two 3000 mg Doses (First Dose + Second Dose )

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Ae total was calculated by adding all the fractions of drug collected over all the allotted time intervals. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-14 Hours, 14-16 Hours, 16-18 Hours, 18-20 Hours, 20-24 Hours, 24-36 Hours, 36-48 Hours, 48-60 Hours post-dose in each Treatment Periods 1 and 2

InterventionMilligrams (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg1066.21

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Cohort 3: AUC (0-48) of Gepotidacin in Urine Following Two 3000 mg Doses (First Dose + Second Dose)

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-14 Hours, 14-16 Hours, 16-18 Hours, 18-20 Hours, 20-24 Hours, 24-36 Hours, 36-48 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg16682.1

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Cohort 3: AUC(0-24) of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 Hours, 14 Hours, 14 Hours 30 Hours, 15, 16,18,20,24 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg73.2

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Cohort 3: AUC(0-24) of Gepotidacin in Urine Following Two 3000 mg Doses (First Dose + Second Dose)

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-14 Hours, 14-16 Hours, 16-18 Hours, 18-20 Hours, 20-24 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg14333.9

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Cohort 3: AUC(0-48) of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 Hours, 14 Hours, 14 Hours 30 Hours, 15, 16,18,20,24,36, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg81.2

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Cohort 4: Number of Participants With Any Increase in Maximum Post-Baseline Electrocardiogram (ECG) Parameter Corrected QT (QTc) Interval

A 12-lead ECG was recorded with the participant in a semi-supine position after a rest of at least 10 minutes using an ECG machine that automatically calculated the QTc interval. Number of participants with any increase of >450 milliseconds in corrected QT interval using the Bazett formula (QTcB) Interval and corrected QT interval using the Fridericia formula (QTcF) Interval has been reported. (NCT04493931)
Timeframe: Up to 22 days

,,,
InterventionParticipants (Count of Participants)
QTcB IntervalQTcF Interval
Cohort 4: Gepotidacin 1500 mg Fasted30
Cohort 4: Gepotidacin 1500 mg Fed81
Cohort 4: Gepotidacin 3000 mg Fed92
Cohort 4: Placebo11

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Metal Ion Concentrations in Blood

Chromium and cobalt concentrations in whole blood (NCT04585022)
Timeframe: at 5 years follow up

,
Interventionmicrograms/liter (Median)
ChromiumCobalt
Magnum1.361.67
Recap1.210.92

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SF-36

Short Form 36 Health Survey Questionnaire (SF-36) (0-100, higher values meaning better outcome) (NCT04585022)
Timeframe: at 5 years follow up

,
Interventionscore on a scale (Median)
Physical functionPhysical restrictionBodily painGeneral healthVitalitySocial functionEmotional restrictionMental Health
Magnum901009274.577.510010092
Recap901008479.57510010088

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Harris Hip Score

Harris Hip Score (0-100, higher values meaning better outcome) (NCT04585022)
Timeframe: at 5 years follow up

Interventionunits on a scale (Median)
Magnum100
Recap100

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Number of Patients Undergoing Revision

Rate of revision during the follow-up period, calculated as number of revisions (numerator) out of the total number of patients starting the study (denominator) (NCT04585022)
Timeframe: at 5 years follow up

InterventionParticipants (Count of Participants)
Magnum0
Recap6

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