Page last updated: 2024-11-04

acebutolol

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

Description

Acebutolol: A cardioselective beta-1 adrenergic antagonist with little effect on the bronchial receptors. The drug has stabilizing and quinidine-like effects on cardiac rhythm, as well as weak inherent sympathomimetic action. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

acebutolol : An ether that is the 2-acetyl-4-(butanoylamino)phenyl ether of the primary hydroxy group of 3-(propan-2-ylamino)propane-1,2-diol. [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]

alpha-D-glucosyl-(1->4)-alpha-D-mannose : An alpha-D-glucosyl-(1->4)-D-mannopyranose in which the anomeric hydroxy group has alpha configuration. [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 CID1978
CHEMBL ID642
CHEBI ID2379
SCHEMBL ID3772
MeSH IDM0000100
PubMed CID10991489
CHEBI ID47937
MeSH IDM0000100

Synonyms (158)

Synonym
BRD-A29260609-003-05-4
butanamide, n-[3-acetyl-4-[2-hydroxy-3-[(1-methylethyl)amino]propoxy]phenyl]-, (.+/-.)-
DIVK1C_000612
KBIO1_000612
3'-(acetyl-4'-(2-hydroxy-3-(isopropylamino)propoxy)butyranilide
1-(2-acetyl-4-n-butyramidophenoxy)-2-hydroxy-3-isopropylaminopropane
acebutololum [inn-latin]
acebutololo
(+-)-3'-acetyl-4'-(2-hydroxy-3-(isopropylamino)propoxy)butyranilide
butanamide, n-(3-acetyl-4-(2-hydroxy-3-((1-methylethyl)amino)propoxy)phenyl)-, (+-)-
acebrutololum [inn-latin]
3'-acetyl-4'-(2-hydroxy-3-isopropylaminopropoxy)butyranilid
einecs 253-539-0
brn 2162244
ccris 9214
(+-)-n-(3-acetyl-4-(2-hydroxy-3-((1-methylethyl)amino)propoxy)phenyl)butanamide
acebutolol [usan:inn:ban]
acetobutolol [inn-spanish]
dl-acebutolol
rp 21823
monitan
SPECTRUM_000491
(+-)-acebutolol
3'-acetyl-4'-(2-hydroxy-3-(isopropylamino)propoxy)butyranilide
sectral
CHEBI:2379 ,
acebutololum
acetobutolol
n-[3-acetyl-4-[2-hydroxy-3-[(1-methylethyl)amino]propoxy]phenyl]butanamide
n-(3-acetyl-4-[2-hydroxy-3-(isopropylamino)propoxy]phenyl)butanamide
5'-butyramido-2'-(2-hydroxy-3-isopropylaminopropoxy)acetophenone
n-{3-acetyl-4-[2-hydroxy-3-(propan-2-ylamino)propoxy]phenyl}butanamide
neptal
PRESTWICK2_000069
SPECTRUM5_001399
BSPBIO_001986
PRESTWICK3_000069
IDI1_000612
bdbm25755
AB00053574
37517-30-9
C06803
acebutolol
(+/-)-acebutolol
DB01193
acebutolol (usan/inn)
D02338
BSPBIO_000257
BPBIO1_000283
KBIO2_000971
KBIO2_003539
KBIO3_001486
KBIO2_006107
KBIOGR_001283
KBIOSS_000971
SPECTRUM2_001340
PRESTWICK0_000069
SPECTRUM3_000573
SPBIO_001499
PRESTWICK1_000069
NINDS_000612
SPBIO_002178
SPECTRUM4_000802
c07ab04
CHEMBL642
L000998
n-[3-acetyl-4-[2-hydroxy-3-(propan-2-ylamino)propoxy]phenyl]butanamide
NCGC00018215-02
AKOS015963037
67p356d8gh ,
butanamide, n-(3-acetyl-4-(2-hydroxy-3-((1-methylethyl)amino)propoxy)phenyl)-,monohydrochloride,(+-)-
unii-67p356d8gh
acebrutololum
EPITOPE ID:146105
gtpl7107
n-(3-acetyl-4-{2-hydroxy-3-[(propan-2-yl)amino]propoxy}phenyl)butanimidic acid
acebutolol [vandf]
acebutolol [mi]
acebutolol [mart.]
butanamide, n-(3-acetyl-4-(2-hydroxy-3-((1-methylethyl)amino)propoxy)phenyl)-, (+/-)-
acebutolol [usan]
acebutolol [inn]
(+/-)-3'-acetyl-4'-(2-hydroxy-3-(isopropylamino)propoxy)butyranilide
acebutolol [who-dd]
1189500-68-2
SCHEMBL3772
DTXSID2048539 ,
wesfalin (salt/mix)
(.+/-.)-n-(3-acetyl-4-(2-hydroxy-3-((1-methylethyl)amino)propoxy)phenyl)butanamide
sectral (salt/mix)
(.+/-.)-3'-acetyl-4'-[2-hydroxy-3-(1-methylethylamino)propoxy]butyranilide
il 17803a (salt/mix)
(.+/-.)-acebutolol
GOEMGAFJFRBGGG-UHFFFAOYSA-N
butanamide, n-[3-acetyl-4-[2-hydroxy-3-[(1-methylethyl)amino]propoxy]phenyl]-
n-(3-acetyl-4-[2-hydroxy-3-(isopropylamino)propoxy]phenyl)butanamide #
(.+/-.)-3'-acetyl-4'-[2-hydroxy-3-(isopropylamino)propoxy]butyranilide
n-(3-acetyl-4-{2-hydroxy-3-[(propan-2-yl)amino]propoxy}phenyl)butanamide
DS-3129
n-(3-acetyl-4-(2-hydroxy-3-(isopropylamino)propoxy)phenyl)butyramide
AB00053574_14
AB00053574_13
SBI-0051584.P003
28197-63-9
FT-0660954
Q418857
BRD-A29260609-003-15-3
n-(3-acetyl-4-(2-hydroxy-3-(isopropylamino)-propoxy)phenyl)butyramide
A935714
discontinued. see: a123800
EN300-7398930
HY-17497
CS-0009240
mfcd00599435
n-(3-acetyl-4-(2-hydroxy-3-(isopropylamino)propoxy)phenyl)butanamide
acebutololum (inn-latin)
n-(3-acetyl-4-(2-hydroxy-3-(propan-2-ylamino)propoxy)phenyl)butanamide
acetobutolol (inn-spanish)
n-(3-acetyl-4-(2-hydroxy-3-((1-methylethyl)amino)propoxy)phenyl)butanamide
dtxcid8028006
acebrutololum (inn-latin)
acebutolol (mart.)
AT39841
d-maltose
d-(+)-maltose ,
4-o-alpha-d-glucopyranosyl-d-glucose
cextromaltose
maltobiose
4-(alpha-d-glucosido)-d-glucose
4-(alpha-d-glucopyranosido)-alpha-glucopyranose
madoros (tn)
sunmalt
maltose hh
finetose f
finetose
maltodiose
sunmalt s
maltose hhh
advantose 100
malt sugar
MALTOSE ,
alpha-d-glucopyranosyl-(1->4)-alpha-d-mannopyranose
alpha-d-glucosyl-(1->4)-alpha-d-mannose
4-o-alpha-d-glucopyranosyl-alpha-d-mannopyranose
CHEBI:47937
4-o-a-d-glucopyranosyl-d-glucose
4-o-alpha-delta-glucopyranosyl-delta-glucose
4-(alpha-delta-glucopyranosido)-alpha-glucopyranose
alpha-delta-glucopyranosyl-(1->4)-delta-glucopyranose
4-(alpha-delta-glucosido)-delta-glucose
madoros
4-o-alpha-delta-glucopyranosyl-delta-glucopyranose
1-alpha-delta-glucopyranosyl-4-alpha-delta-glucopyranose
alpha-delta-glucopyranosyl-(1->4)-delta-glucose
delta-(+)-maltose
delta-maltose
alpha-delta-glcp-(1->4)-delta-glcp
Q27120863

Research Excerpts

Overview

Acebutolol (AC) is a chiral beta-adrenergic receptor-blocking agent. The drug is indicated in hypertension, angina pectoris, and arrhythmia. Ace butolol was found to be an effective hypotensive agent with relatively few side effects.

ExcerptReferenceRelevance
"Acebutolol is a β1-selective adrenergic receptor antagonist with moderate membrane-stabilizing activity and intrinsic sympathomimetic activity; accordingly, the drug is indicated in hypertension, angina pectoris, and arrhythmia. "( A case of fatal acebutolol poisoning: an illustration of the potential of molecular networking.
Allard, PM; Allard, S; Baert, A; Bouvet, R; Gicquel, T; Le Daré, B; Morel, I, 2020
)
2.35
"Acebutolol (AC) is a chiral beta-adrenergic receptor-blocking agent, which has been shown to be clinically effective in hypertension. "( 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
)
2
"Acebutolol is a new investigational beta-antagonist which has intrinsic sympathomimetic and cardioselective properties. "( Comparative effects of oral acebutolol and propranolol at rest and during exercise in ischemic heart disease: double-blind placebo crossover study utilizing radionuclide ventriculography.
Hecht, HS; Hopkins, J; Kaul, S; Seidman, R; Singh, BN, 1984
)
2
"Acebutolol appears to be an effective and well-tolerated antiarrhythmic agent in the treatment of VEB and higher grades of ventricular ectopy."( Reduction of ventricular ectopic beats with oral acebutolol: a double-blind, randomized crossover study.
Dhurandhar, R; Dietrich, P; Hungate, EJ; Laddu, A; Lee, G; Lui, HK; Mason, DT, 1983
)
1.24
"Acebutolol was found to be an effective hypotensive agent with relatively few side effects."( Acebutolol in mild to moderate hypertension: a double-blind crossover study.
Hua, AS; Kalowski, S; Kincaid-Smith, P; Whitworth, JA, 1980
)
2.43
"Acebutolol is a relatively "cardioselective" beta-adrenergic blocking agent with an antihypertensive action. "( The antihypertensive action of acebutolol.
Koh, TH; Low, LP, 1981
)
1.99
"Acebutolol (AC) is a chiral beta-adrenergic blocking drug, possessing intrinsic sympathomimetic activity (ISA), and is useful clinically as the racemate in treating hypertension. "( Pharmacokinetics of acebutolol enantiomers after intravenous administration of racemate in a rat model: a dosing range comparison.
Foster, RT; Mostafavi, SA, 1997
)
2.06
"Acebutolol (AC) is a chiral beta-blocker which is extensively metabolized to an active, chiral metabolite, diacetolol (DC). "( Pharmacokinetics and multiple peaking of acebutolol enantiomers in rats.
Jamali, F; Piquette-Miller, M, 1997
)
2.01
"Acebutolol (AC), is a chiral, beta-adrenergic blocking agent which possesses partial agonist activity and is metabolized to an equipotent chiral metabolite, diacetolol (DC). "( Pharmacokinetics of single oral and multiple intravenous and oral administration of acebutolol enantiomers in a rat model.
Foster, RT; Mostafavi, SA, 1998
)
1.97
"Acebutolol is a unique beta blocker that possesses cardioselectivity, partial agonist activity, and membrane stabilizing activity. "( Acebutolol-induced ventricular tachycardia reversed with sodium bicarbonate.
Donovan, KD; Dreyer, JF; Gerace, RV, 1999
)
3.19
"Acebutolol appears to be a useful anti-hypertensive in the management of hypertension."( Clinical trial of acebutolol (Sectral) in hypertension.
Charoenlarp, K; Jaroonvesama, N, 1978
)
1.31
"Acebutolol is a cardioselective beta-adrenoceptor blocking agent which has marked anti-arrhythmic against arrhythmia induced by methylchloroform and adrenalin in the cat, and also arrhythmia induced by ouabain in dogs and rabbits."( [Pharmacology of acebutolol in animals].
Basil, B, 1975
)
1.32
"Acebutolol (AC) is a chiral beta-blocker which is available as a racemate."( Effect of adjuvant arthritis on the disposition of acebutolol enantiomers in rats.
Jamali, F; Piquette-Miller, M, 1992
)
1.26
"Acebutolol (AC) is a chiral beta-blocker that is metabolized to an equipotent chiral metabolite, diacetolol (DC). "( Effect of aging on the pharmacokinetics of acebutolol enantiomers.
Foster, RT; Jamali, F; Kappagoda, CT; Piquette-Miller, M, 1992
)
1.99
"Acebutolol is a beta blocking agent that induces in C57Bl/6 mice a polyclonal activation of lymphocytes (PAL). "( The beta-blocker acebutolol down modulates the spontaneous polyclonal activation of lymphocytes in NZB X NZW lupus mice.
Alary, C; Appolinaire-Pilipenko, S; f1noist, H; Fournié, GJ; In, S; Lulé, J; Oksman, F; Rollet, C, 1991
)
2.06
"Acebutolol is a relatively new beta-adrenoceptor blocking antagonist, possessing both beta 1-adrenoceptor selectivity and partial agonist activity (PAA). "( Acute and long-term effects of acebutolol on systemic and renal hemodynamics, body fluid volumes, catecholamines, active renin, aldosterone, and lymphocyte beta-adrenoceptor density.
Boomsma, F; Derkx, FH; Fischberg, DJ; Man in 't Veld, AJ; Molinoff, PB; Schalekamp, MA; van den Meiracker, AH; van Eck, HJ, 1988
)
2
"Acebutolol is an efficacious antihypertensive agent when used on a once-daily basis."( Once-daily administration of acebutolol in treatment of hypertension.
Drayer, JI; Weber, MA, 1985
)
1.28
"Acebutolol was shown to be a safe, effective and reliable antihypertensive drug, at least comparable to and probably slightly better than, propranolol in the treatment of hypertension in Black Nigerians."( A double-blind comparison of acebutolol (Sectral) and propranolol (Inderal) in the treatment of hypertension in black Nigerian patients.
Abengowe, CU, 1985
)
1.28
"Acebutolol is a new hydrophilic, cardioselective beta-adrenergic-blocking agent that possesses partial agonist and membrane-stabilizing activities. "( Acebutolol: a review of its pharmacology, pharmacokinetics, clinical uses, and adverse effects.
Singh, BN; Thoden, WR; Wahl, J,
)
3.02
"Acebutolol is a cardioselective beta-adrenoceptor blocking drug possessing both partial agonist (intrinsic sympathomimetic) and membrane stabilising activity. "( Acebutolol. A review of its pharmacological properties and therapeutic efficacy in hypertension, angina pectoris and arrhythmia.
Singh, BN; Thoden, WR; Ward, A, 1985
)
3.15
"Acebutolol is a safe and efficacious drug for the prevention of arrhythmias following coronary surgery."( Prevention by acebutolol of rhythm disorders following coronary bypass surgery.
Collignon, P; Kulbertus, H; Larbuisson, R; Limet, R; Materne, P, 1985
)
1.35

Effects

Acebutolol has a major non-renal route of elimination, but the acetyl metabolite (also a beta-adrenoreceptor blocking drug) is primarily excreted by the kidney and may accumulate in renal failure. It has a significantly smaller effect on resting heart rate than propranolol, metoprolol and atenolol.

Acebutolol has a major non-renal route of elimination, but the acetyl metabolite (also a beta-adrenoreceptor blocking drug) is primarily excreted by the kidney and may accumulate in renal failure. The drug has both antihypertensive and antiarrhythmic effects.

ExcerptReferenceRelevance
"Acebutolol has a major non-renal route of elimination, but the acetyl metabolite (also a beta-adrenoreceptor blocking drug) is primarily excreted by the kidney and may accumulate in renal failure."( Plasma and urine concentrations of acebutolol and its acetyl metabolite in patients with renal functional impairment.
Bailey, RR; Begg, E; Ebert, R; Ferry, DG; Munn, S, 1980
)
1.26
"Acebutolol has a lower lipid solubility."( Comparison of effect on psychomotor performance of single doses of propranolol and acebutolol.
Broadhurst, AD, 1980
)
1.21
"Acebutolol has a significantly smaller effect on resting heart rate than propranolol, metoprolol and atenolol, although direct comparisons with drugs with intrinsic sympathomimetic activity have yet to be undertaken."( Acebutolol. A review of its pharmacological properties and therapeutic efficacy in hypertension, angina pectoris and arrhythmia.
Singh, BN; Thoden, WR; Ward, A, 1985
)
2.43
"Acebutolol (ACE) has been widely used for the treatment of cardiovascular disorders, and its photochemical fate in natural waters is a matter of concern due to its ubiquitous occurrence and its toxicity to aquatic organisms. "( Photodegradation of acebutolol in natural waters: Important roles of carbonate radical and hydroxyl radical.
Guo, Y; Guo, Z; Niu, J; Wang, J; Ye, Z; Yoshimura, C; Zhang, L, 2022
)
2.49
"Acebutolol has a major non-renal route of elimination, but the acetyl metabolite (also a beta-adrenoreceptor blocking drug) is primarily excreted by the kidney and may accumulate in renal failure."( Plasma and urine concentrations of acebutolol and its acetyl metabolite in patients with renal functional impairment.
Bailey, RR; Begg, E; Ebert, R; Ferry, DG; Munn, S, 1980
)
1.26
"Acebutolol has a lower lipid solubility."( Comparison of effect on psychomotor performance of single doses of propranolol and acebutolol.
Broadhurst, AD, 1980
)
1.21
"Acebutolol has both antihypertensive and antiarrhythmic effects."( Pharmacologic properties of acebutolol: relationship of hydrophilicity to central nervous system penetration.
Abernethy, DR; Arendt, RM; Greenblatt, DJ, 1985
)
1.28
"Acebutolol has low lipid solubility and low protein binding; the former property reduces the risk of central side effects, and the latter means that displacement interactions with other drugs are unlikely."( Acebutolol: ten years of experience.
De Bono, G; Kaye, CM; Roland, E; Summers, AJ, 1985
)
2.43
"Acebutolol has minimal metabolic effects and does not elevate levels of blood lipids during long-term therapy; high-density-lipoprotein cholesterol increased with acebutolol in a small number of patients."( Acebutolol: a review of its pharmacology, pharmacokinetics, clinical uses, and adverse effects.
Singh, BN; Thoden, WR; Wahl, J,
)
2.3
"Acebutolol has a significantly smaller effect on resting heart rate than propranolol, metoprolol and atenolol, although direct comparisons with drugs with intrinsic sympathomimetic activity have yet to be undertaken."( Acebutolol. A review of its pharmacological properties and therapeutic efficacy in hypertension, angina pectoris and arrhythmia.
Singh, BN; Thoden, WR; Ward, A, 1985
)
2.43

Actions

Acebutolol seemed to cause stroke earlier with the more rapid BP elevation. It tended to lower the resistance insignificantly in the calf but to increase resistance in the first toe.

ExcerptReferenceRelevance
"Acebutolol seemed to cause stroke earlier with the more rapid BP elevation."( Effects of beta-adrenergic blocking drugs in hypertensive rats.
Shiono, K; Sokabe, H; Sukamoto, T; Watanabe, TX, 1980
)
0.98
"Acebutolol has a lower lipid solubility."( Comparison of effect on psychomotor performance of single doses of propranolol and acebutolol.
Broadhurst, AD, 1980
)
1.21
"Acebutolol tended to lower the resistance insignificantly in the calf but to increase resistance in the first toe."( Comparative effects of acebutolol and labetalol on peripheral hemodynamics in healthy volunteers.
Duchene-Marullaz, P; Kantelip, JP; Wurm, M, 1988
)
1.31

Treatment

Acebutolol treatment for 15 days (50mg/kg/day) inhibited the polyclonal activation of lymphocytes induced by LPS in C57BL/6 and C57BI/6 nu/nu mice, but increased the humoral response to sheep red blood cells. The treatment was effective inducing an improvement of subjective symptoms.

ExcerptReferenceRelevance
"Acebutolol treatment induced reduction in diastolic pressure, heart rate, and PRA pooled from both phases of the study."( Addition of acebutolol to diuretics in hypertension.
Dziedzic, SW; Elijovich, F; Gorkin, JU; Krakoff, LR, 1981
)
1.36
"Both acebutolol treatments reduced the response; the reduction after twice daily treatment (mean 25 beats/min) was significantly greater than after once daily treatment (mean 19 beats/min)."( Comparison of once and twice daily administration of acebutolol in hypertension.
Littler, WA; Stallard, TJ; Watson, RD, 1980
)
0.97
"With ACEBUTOLOL treatment, during the test described and during dynamic stress on ergometric bicycle, HR and SBP are always less elevated."( [Changes in heart rate and blood pressure in a series of normotensive subjects before and after beta-blocker treatment (double-blind) during physical, dynamic, static and psychosensorial stress].
Cau, G; Daver, C; de Gaudemaris, R; Debru, JL; Mallion, JM; Morin, B; Villemain, P, 1982
)
0.72
"Acebutolol treatment decreased the frequency of angina (diary cards) (placebo, 9.0 +/- 2.4 episodes per week; acebutolol, 6.4 +/- 2.2 episodes per week; P less than 0.05) and decreased the consumption of nitroglycerin (placebo, 9.0 +/- 4.4 tablets per week; acebutolol, 7.4 +/- 4.0 tablets per week; P less than 0.05)."( Favorable effects of acebutolol on exercise performance and angina in men with coronary artery disease.
Gold, F; Steele, P, 1982
)
1.3
"Acebutolol treatment for 15 days (50mg/kg/day) inhibited the polyclonal activation of lymphocytes induced by LPS in C57BL/6 and in C57BI/6 nu/nu mice, but increased the humoral response to sheep red blood cells in C57Bl/6 mice."( Evidence for a dual effect of acebutolol, a beta blocker, on the mouse humoral immune response.
Benoist, H; Fournie, GJ; In, S; Le Lann, AD, 1995
)
1.3
"The treatment with acebutolol was effective inducing an improvement of subjective symptoms (reduction of stenocardiac crises, intensity and duration of angor, trinitrin pearls consumption) and an increase of effort tolerance."( [Effects of the administration of acebutolol in patients with chronic angina of effort].
Baroni, F; Donegani, E; Forni, B; Uslenghi, E; Zardini, P, 1981
)
0.86
"Treatment with acebutolol produced statistically significant reductions in blood pressure and heart rate as compared to the placebo regimen."( Controlled trial of acebutolol in hypertension.
Andersson, O; Berglund, G; Hansson, L; Holm, M, 1977
)
0.92
"Pretreatment with acebutolol, 15 min before starting reperfusion, markedly reduced the arrhythmias."( Cardiovascular effects of acebutolol following coronary artery occlusion and reperfusion in anaesthetized dog.
Chernecki, W; Das, PK; Dhalla, NS; Sharma, GP, 1978
)
0.88
"Pretreatment with acebutolol or propranolol at high concentrations had an inhibitory effect on the contractile response to 5-hydroxytryptamine (5-HT) in most vascular smooth muscles such as rabbit aorta and basilar, mesenteric, renal, femoral arteries and cat coronary artery. "( The inhibitory actions of acebutolol and propranolol on the contractile response to 5-hydroxytryptamine in various isolated vascular smooth muscles.
Satake, N; Shibata, S; Ueda, S, 1985
)
0.9

Toxicity

Acebutolol is as effective as other beta-blocking agents, and in a large, double-blind, parallel study against propranolol was found to cause less reduction in heart rate.

ExcerptReferenceRelevance
" Acebutolol is as effective as other beta-blocking agents, and in a large, double-blind, parallel study against propranolol was found to cause less reduction in heart rate, and fewer neurologic side effects and patient withdrawals due to adverse effects."( Acebutolol: a review of its pharmacology, pharmacokinetics, clinical uses, and adverse effects.
Singh, BN; Thoden, WR; Wahl, J,
)
2.48
" Since beta-blockers cross the placenta, it is essential to consider possible adverse effects on the embryo."( Toxicity of beta-blockers in a rat whole embryo culture: concentration-response relationships and tissue concentrations.
Klug, S; Merker, HJ; Neubert, D; Schwabe, R; Thiel, R, 1994
)
0.29
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
" In summary, this study demonstrated that metabolic activation may be a causal factor of adverse reactions of acebutolol."( A proposed mechanism for the adverse effects of acebutolol: CES2 and CYP2C19-mediated metabolism and antinuclear antibody production.
Fukami, T; Muta, K; Nakajima, M, 2015
)
0.88
"We studied the enhancing and toxic effects of five different absorption enhancers on the transport of FITC-dextran with an average molecular weight of 4000 (FD-4) across Caco-2 cell monolayers, and their enhancing effects were also compared with those in rat intestine."( Effectiveness and toxicity screening of various absorption enhancers using Caco-2 cell monolayers.
Fujita, T; Hattori, K; Lundborg, E; Murakami, M; Muranishi, S; Quan, YS; Yamamoto, A, 1998
)
0.3
" Changes in such fingerprint profiles can be used to characterize the effects of toxic insult in in vivo systems."( Metabonomic assessment of toxicity of 4-fluoroaniline, 3,5-difluoroaniline and 2-fluoro-4-methylaniline to the earthworm Eisenia veneta (Rosa): identification of new endogenous biomarkers.
Bailey, NJ; Bundy, JG; Gavaghan, CL; Hankard, PK; Lenz, EM; Lindon, JC; Nicholson, JK; Osborn, D; Sanders, I; Speir, P; Spurgeon, D; Svendsen, C; Tang, H; Trauger, SA; Weeks, JM, 2002
)
0.31
"Parenteral iron carboxymaltose is a safe and effective treatment option for postpartum anemia, with advantages of a shorter treatment period, better compliance, rapid normalization of iron storages, and lower incidence of gastrointestinal side effects."( Comparative efficacy and safety of intravenous ferric carboxymaltose in the treatment of postpartum iron deficiency anemia.
Bejenariu, C; Breymann, C; Gliga, F; Strizhova, N, 2008
)
0.35
" Adverse events after administration of the drug were assessed by using a questionnaire."( Safety and tolerability of ferric carboxymaltose (FCM) for treatment of iron deficiency in patients with chronic kidney disease and in kidney transplant recipients.
Cohen, CD; Fehr, T; Grimmelt, AC; Serra, AL; Wuethrich, RP, 2009
)
0.35
"Mild and transient adverse events (metallic taste, headache, dizziness) occurred in six patients."( Safety and tolerability of ferric carboxymaltose (FCM) for treatment of iron deficiency in patients with chronic kidney disease and in kidney transplant recipients.
Cohen, CD; Fehr, T; Grimmelt, AC; Serra, AL; Wuethrich, RP, 2009
)
0.35
" The primary endpoint was the incidence of treatment-emergent adverse events during each 7-day study period."( Safety and tolerability of intravenous ferric carboxymaltose in patients with iron deficiency anemia.
Bailie, GR; Mason, NA; Valaoras, TG, 2010
)
0.36
" Safety assessments included incidence of adverse events (AEs)."( The safety and efficacy of intravenous ferric carboxymaltose in anaemic patients undergoing haemodialysis: a multi-centre, open-label, clinical study.
Covic, A; Mircescu, G, 2010
)
0.36
" Safety assessments included incidence of adverse events (AEs), clinical laboratory parameters and vital signs."( Pharmacokinetics, safety and tolerability of intravenous ferric carboxymaltose: a dose-escalation study in volunteers with mild iron-deficiency anaemia.
Banké-Bochita, J; Geisser, P, 2010
)
0.36
" Safety assessments: the incidence of adverse events (AEs) and changes in vital signs, physical examinations, and clinical laboratory parameters."( Pharmacodynamics and safety of ferric carboxymaltose: a multiple-dose study in patients with iron-deficiency anaemia secondary to a gastrointestinal disorder.
Geisser, P; Rumyantsev, V, 2010
)
0.36
" Iron repletion has been associated with adverse outcomes in infections."( Clinical use of intravenous iron: administration, efficacy, and safety.
Auerbach, M; Ballard, H, 2010
)
0.36
"Dendrimers have been proved to interact with amyloids, although most of dendrimers assayed in amyloidogenic systems are toxic to cells."( Dense shell glycodendrimers as potential nontoxic anti-amyloidogenic agents in Alzheimer's disease. Amyloid-dendrimer aggregates morphology and cell toxicity.
Appelhans, D; Benseny-Cases, N; Cladera, J; Gella, A; Klementieva, O; Voit, B, 2011
)
0.37
" There were no significant adverse events."( Clinical efficacy and safety of IV ferric carboxymaltose (FCM) treatment of RLS: a multi-centred, placebo-controlled preliminary clinical trial.
Adler, CH; Allen, RP; Bregman, DB; Butcher, A; Du, W; Earley, CJ, 2011
)
0.37
"IV FCM provided a safe and effective treatment for RLS that lasted for at least 24 weeks for some patients."( Clinical efficacy and safety of IV ferric carboxymaltose (FCM) treatment of RLS: a multi-centred, placebo-controlled preliminary clinical trial.
Adler, CH; Allen, RP; Bregman, DB; Butcher, A; Du, W; Earley, CJ, 2011
)
0.37
" Treatment with ferric carboxymaltose is efficious, safe and well tolerated in iron-deficient IBD patients."( Iron status and analysis of efficacy and safety of ferric carboxymaltose treatment in patients with inflammatory bowel disease.
Beigel, F; Brand, S; Breiteneicher, S; Göke, B; Laubender, RP; Löhr, B; Ochsenkühn, T; Schnitzler, F; Seiderer, J; Tillack, C; Weidinger, M, 2012
)
0.38
" Safety and tolerability of both groups were compared on the basis of reported systemic and local adverse events."( Safety and efficacy of high-dose intravenous iron carboxymaltose vs. iron sucrose for treatment of postpartum anemia.
Christoph, P; Pfenniger, A; Schuller, C; Surbek, D, 2012
)
0.38
"Rapid administration of high ICM doses was as well tolerated as IS with overall adverse events of 5% (ICM) vs."( Safety and efficacy of high-dose intravenous iron carboxymaltose vs. iron sucrose for treatment of postpartum anemia.
Christoph, P; Pfenniger, A; Schuller, C; Surbek, D, 2012
)
0.38
"IV ICM is as safe as IS in the management of postpartum (IDA) iron deficiency anemia despite five times of higher dosage."( Safety and efficacy of high-dose intravenous iron carboxymaltose vs. iron sucrose for treatment of postpartum anemia.
Christoph, P; Pfenniger, A; Schuller, C; Surbek, D, 2012
)
0.38
" Demographic data, efficacy measures [hemoglobin, ferritin, and transferrin saturation (TSAT)], and adverse events were compared between FCM and other agents utilized as comparators in the trials."( Comparative review of the safety and efficacy of ferric carboxymaltose versus standard medical care for the treatment of iron deficiency anemia in bariatric and gastric surgery patients.
Barish, C; Bregman, D; He, A; Malone, M, 2013
)
0.39
" The incidence of adverse events in the FCM patients (n = 123) versus patients receiving any IV iron (n = 126) was 61 and 56."( Comparative review of the safety and efficacy of ferric carboxymaltose versus standard medical care for the treatment of iron deficiency anemia in bariatric and gastric surgery patients.
Barish, C; Bregman, D; He, A; Malone, M, 2013
)
0.39
"These data in post-bariatric surgery IDA patients suggest that FCM is a safe and effective alternative to existing iron products permitting higher and thus less frequent individual doses."( Comparative review of the safety and efficacy of ferric carboxymaltose versus standard medical care for the treatment of iron deficiency anemia in bariatric and gastric surgery patients.
Barish, C; Bregman, D; He, A; Malone, M, 2013
)
0.39
" However, parenteral iron supplementation is usually safe and without major side effects."( [Safety aspects of parenteral iron supplementation therapies in patients with chronic kidney disease].
Münch, HG; Potthoff, SA, 2013
)
0.39
"Two 750-mg FCM infusions are safe and superior to oral iron in increasing Hb levels in IDA patients with inadequate oral iron response."( A multicenter, randomized, active-controlled study to investigate the efficacy and safety of intravenous ferric carboxymaltose in patients with iron deficiency anemia.
Acs, P; Akright, B; Barish, C; Bhaskar, BS; Bregman, DB; Butcher, A; Goodnough, LT; Harrington, RA; Koch, TA; Morris, D; Onken, JE; Smith-Nguyen, GN, 2014
)
0.4
" Number and severity of adverse events did not differ between FG and FCM, no severe adverse events occurred."( TIDILAP: Treatment of iron deficiency in lipoprotein apheresis patients --A prospective observational multi-center cohort study comparing efficacy, safety and tolerability of ferric gluconate with ferric carboxymaltose.
Arneth, B; Bornstein, SR; Heigl, F; Hettich, R; Illigens, BM; Julius, U; Prophet, H; Ramlow, W; Schatz, U; Siegels, D; Siegert, G; Siepmann, T, 2015
)
0.42
" Safety assessment was performed by recording adverse events (AEs) during and immediately after infusion, 30 minutes afterwards, and via follow-up at 7 days and 8 weeks."( Safety of ferric carboxymaltose immediately after infliximab administration, in a single session, in inflammatory bowel disease patients with iron deficiency: a pilot study.
Borrás-Blasco, J; Boscá, M; Cortés, E; Cortes, X; Molés, JR, 2015
)
0.42
"Single-session administration of FCM after IFX was safe and effective in IBD patients and can offer a good cost-benefit ratio and improve treatment adherence."( Safety of ferric carboxymaltose immediately after infliximab administration, in a single session, in inflammatory bowel disease patients with iron deficiency: a pilot study.
Borrás-Blasco, J; Boscá, M; Cortés, E; Cortes, X; Molés, JR, 2015
)
0.42
" LC50 values were calculated and the most toxic Ag NPs tested were selected for a second step where sublethal concentrations of each Ag form were tested using a wide array of mechanistic tests in both cell types."( Mechanisms of Toxicity of Ag Nanoparticles in Comparison to Bulk and Ionic Ag on Mussel Hemocytes and Gill Cells.
Arostegui, I; Cajaraville, MP; Gilliland, D; Katsumiti, A, 2015
)
0.42
" Three serious adverse events were reported, but they were considered unrelated to treatment."( Open-label study of the efficacy and safety of intravenous ferric carboxymaltose in pregnant women with restless legs syndrome.
Bassetti, C; Baumann, C; Gyr, T; Hübner, A; Krafft, A; Manconi, M; Schneider, J; Werth, E, 2015
)
0.42
" This novel eleven step desensitization protocol was well tolerated without any adverse reactions and allowed the patients to receive iron supplementation when limited therapeutic options existed."( A Safe and Novel Desensitization Protocol with Ferric Carboxymaltose to Treat Iron Deficiency Anemia.
Fajt, ML; Montandon, SV; Petrov, AA, 2016
)
0.43
"All currently available intravenous iron preparations appear to be safe and effective, but ferric carboxymaltose seems to provide a better and quicker correction of haemoglobin and serum ferritin levels in iron-deficient patients."( Efficacy and Safety of Ferric Carboxymaltose and Other Formulations in Iron-Deficient Patients: A Systematic Review and Network Meta-analysis of Randomised Controlled Trials.
Marmifero, M; Meregaglia, M; Rognoni, C; Tarricone, R; Venturini, S, 2016
)
0.43
" They are often considered as safe alternatives to currently used surfactants in cosmetic industries."( Measurement of cytotoxicity and irritancy potential of sugar-based surfactants on skin-related 3D models.
Chagnault, V; Egles, C; Grand, E; Lu, B; Miao, Y; Pezron, I; Postel, D; Vayssade, M; Vigneron, P; Wadouachi, A, 2017
)
0.46
" The objective of this study was to evaluate the safety and tolerability of DFN-02 (10 mg) in the acute treatment of episodic migraine with and without aura over a 6-month period based on the incidence of treatment-emergent adverse events and the evaluation of results of clinical laboratory tests, vital signs, physical examination, and electrocardiograms."( A multicenter, open-label, long-term safety and tolerability study of DFN-02, an intranasal spray of sumatriptan 10 mg plus permeation enhancer DDM, for the acute treatment of episodic migraine.
Allenby, K; Brand-Schieber, E; Cady, RK; Munjal, S; Rapoport, AM; Spierings, ELH, 2017
)
0.46
" Adverse events were those expected for triptans, as well as for nasally administered compounds."( A multicenter, open-label, long-term safety and tolerability study of DFN-02, an intranasal spray of sumatriptan 10 mg plus permeation enhancer DDM, for the acute treatment of episodic migraine.
Allenby, K; Brand-Schieber, E; Cady, RK; Munjal, S; Rapoport, AM; Spierings, ELH, 2017
)
0.46
" A post hoc analysis of adverse event rates per 100 patient-years was performed to assess the safety of FCM versus oral iron over an extended period."( Safety of intravenous ferric carboxymaltose versus oral iron in patients with nondialysis-dependent CKD: an analysis of the 1-year FIND-CKD trial.
Bock, AH; Carrera, F; Cronin, M; Eckardt, KU; Gaillard, CA; Larroque, S; Macdougall, IC; Meier, Y; Roger, SD; Van Wyck, DB, 2017
)
0.46
" The incidence of one or more adverse events was 91."( Safety of intravenous ferric carboxymaltose versus oral iron in patients with nondialysis-dependent CKD: an analysis of the 1-year FIND-CKD trial.
Bock, AH; Carrera, F; Cronin, M; Eckardt, KU; Gaillard, CA; Larroque, S; Macdougall, IC; Meier, Y; Roger, SD; Van Wyck, DB, 2017
)
0.46
"These results further support the conclusion that correction of iron deficiency anemia with IV FCM is safe in patients with nondialysis-dependent CKD."( Safety of intravenous ferric carboxymaltose versus oral iron in patients with nondialysis-dependent CKD: an analysis of the 1-year FIND-CKD trial.
Bock, AH; Carrera, F; Cronin, M; Eckardt, KU; Gaillard, CA; Larroque, S; Macdougall, IC; Meier, Y; Roger, SD; Van Wyck, DB, 2017
)
0.46
" The median prevalence of adverse drug reactions for IPM (2."( Safety and efficacy of intravenous iron polymaltose, iron sucrose and ferric carboxymaltose in pregnancy: A systematic review.
Grivell, RM; Grzeskowiak, LE; Mol, BW; Qassim, A, 2018
)
0.48
" Intravenous iron compounds were in the past associated with serious adverse reactions and historically were considered a last resort in children."( Safety and efficacy of parenteral iron in children with inflammatory bowel disease.
Epstein, J; Fell, JME; Goto, E; Korologou-Linden, R; Papadopoulos, M; Patel, D; Soondrum, K, 2018
)
0.48
" Safety, tolerability and adverse events were established by case note review."( Safety and efficacy of parenteral iron in children with inflammatory bowel disease.
Epstein, J; Fell, JME; Goto, E; Korologou-Linden, R; Papadopoulos, M; Patel, D; Soondrum, K, 2018
)
0.48
" No serious adverse effects were reported."( Effectiveness and safety of ferric carboxymaltose compared to iron sucrose in women with iron deficiency anemia: phase IV clinical trials.
Ara, R; Bader, GN; Naqash, A, 2018
)
0.48
"Parenteral therapy is effective in IDA, but FCM elevates hemoglobin level and restored iron stores faster than IS with minimum adverse drug reactions."( Effectiveness and safety of ferric carboxymaltose compared to iron sucrose in women with iron deficiency anemia: phase IV clinical trials.
Ara, R; Bader, GN; Naqash, A, 2018
)
0.48
" Ferric Carboxy Maltose is an effective and a safe option which can be administered intravenously in single total correction dose without any serious adverse effects."( Safety and Efficacy of Intravenous Ferric Carboxy Maltose in Iron Deficiency Anaemia During Post-partum Period.
Aggarwal, R; Choudhary, S; Gandhi, K; Mishra, V; Roy, P; Sokabaj, S, 2018
)
0.48
" No serious adverse events were observed after Ferric Carboxy Maltose."( Safety and Efficacy of Intravenous Ferric Carboxy Maltose in Iron Deficiency Anaemia During Post-partum Period.
Aggarwal, R; Choudhary, S; Gandhi, K; Mishra, V; Roy, P; Sokabaj, S, 2018
)
0.48
"Intravenous Ferric Carboxy Maltose was an effective and a safe treatment option for iron deficiency anaemia and has an advantage of single administration of high doses without serious adverse effects."( Safety and Efficacy of Intravenous Ferric Carboxy Maltose in Iron Deficiency Anaemia During Post-partum Period.
Aggarwal, R; Choudhary, S; Gandhi, K; Mishra, V; Roy, P; Sokabaj, S, 2018
)
0.48
" Fourteen of 24 subjects experienced adverse events, but these were neither serious nor led to drug interruption."( Pharmacokinetics, pharmacodynamics, safety, and tolerability of intravenous ferric carboxymaltose: a dose-escalation study in Japanese volunteers with iron-deficiency anemia.
Ikuta, K; Kawabata, Y; Shimura, A; Terauchi, M; Yoshii, K, 2018
)
0.48
" Adverse events [AEs], clinical signs/symptoms, and disease activity indices were also analysed."( Safety and Efficacy of Ferric Carboxymaltose in the Treatment of Iron Deficiency Anaemia in Patients with Inflammatory Bowel Disease, in Routine Daily Practice.
Aksan, A; Dignass, A; Klemm, W; Nip, K; Stein, J; Weber-Mangal, S, 2018
)
0.48
"3% of patients responded, and no adverse drug reactions or drug-attributed serious adverse events [SAEs] or deaths occurred."( Safety and Efficacy of Ferric Carboxymaltose in the Treatment of Iron Deficiency Anaemia in Patients with Inflammatory Bowel Disease, in Routine Daily Practice.
Aksan, A; Dignass, A; Klemm, W; Nip, K; Stein, J; Weber-Mangal, S, 2018
)
0.48
"Ferinject®-therapy was proven to be effective and safe in a large cohort of patients with IBD-associated anaemia in routine practice."( Safety and Efficacy of Ferric Carboxymaltose in the Treatment of Iron Deficiency Anaemia in Patients with Inflammatory Bowel Disease, in Routine Daily Practice.
Aksan, A; Dignass, A; Klemm, W; Nip, K; Stein, J; Weber-Mangal, S, 2018
)
0.48
" Incidence of adverse events was < 60% in both groups, and no significant difference was observed between the treatment groups."( Comparison of efficacy and safety between intravenous ferric carboxymaltose and saccharated ferric oxide in Japanese patients with iron-deficiency anemia due to hypermenorrhea: a multi-center, randomized, open-label noninferiority study.
Hanashi, H; Hirai, K; Ikuta, K; Matsuyama, Y; Momoeda, M; Ota, Y; Shimura, A; Terauchi, M, 2019
)
0.51
" In the full analysis set (n = 39), the incidence of adverse events and adverse drug reactions was 71."( Safety and efficacy of intravenous ferric carboxymaltose in Japanese patients with iron-deficiency anemia caused by digestive diseases: an open-label, single-arm study.
Ikuta, K; Ito, H; Masaki, S; Suzuki, Y; Takahashi, K; Terauchi, M, 2019
)
0.51
" Basic demographics, infusion indication, starting hemoglobin and ferritin, vital signs and medical details of patients who had an adverse reaction were recorded."( Safety profile of iron polymaltose infusions.
Lee, AYS; Leung, SHP, 2019
)
0.51
"Iron polymaltose has a low rate of adverse drug reactions; yet, serious side-effects such as hypotension may occur."( Safety profile of iron polymaltose infusions.
Lee, AYS; Leung, SHP, 2019
)
0.51
" In cases receiving FCM the appearance of adverse events was analysed."( Iron deficiency and safety of ferric carboxymaltose in patients with acute heart failure. AHF-ID study.
Álvarez-Pérez, JM; Berrocal-Gil, P; Borraz-Ordás, C; Comabella, R; Comín-Colet, J; Fernández-Cañadas, JM; Ferre, C; Herrero-Puente, P; Jacob, J; Llopis-García, G; Llorens, P; López-Díez, P; Martín-Sánchez, FJ; Martínez-Gimeno, JL; Mercado, A; Miró, Ò; Pérez-Durá, MJ; Richard-Espiga, F; Roset, A; Valero-Domènech, A, 2020
)
0.56
"1%) presenting adverse events, the most frequent being digestive alterations."( Iron deficiency and safety of ferric carboxymaltose in patients with acute heart failure. AHF-ID study.
Álvarez-Pérez, JM; Berrocal-Gil, P; Borraz-Ordás, C; Comabella, R; Comín-Colet, J; Fernández-Cañadas, JM; Ferre, C; Herrero-Puente, P; Jacob, J; Llopis-García, G; Llorens, P; López-Díez, P; Martín-Sánchez, FJ; Martínez-Gimeno, JL; Mercado, A; Miró, Ò; Pérez-Durá, MJ; Richard-Espiga, F; Roset, A; Valero-Domènech, A, 2020
)
0.56
"In chronic very severe sideropenic anemias, third-generation IVI is effective and safe for quick correction and avoidance of red blood cell transfusion."( Efficacy and safety of high-dose intravenous iron as the first-choice therapy in outpatients with severe iron deficiency anemia.
Beverina, I; Brando, B; Garcia-Erce, JA; Jericó, C; Melli, C; Quintana-Diaz, M; Recasens, V; Rondinelli, MB; Salvadori, U, 2020
)
0.56
"The aim of the study was to assess the efficacy, safety and side-effect profile of ferric carboxymaltose (FCM) for correcting IDA in children and adolescents in paediatric gastroenterology, hepatology, and nutrition."( Ferric Carboxymaltose Across All Ages in Paediatric Gastroenterology Shows Efficacy Without Increased Safety Concerns.
Barclay, A; Curtis, L; Duncan, H; Fraser, S; Hansen, R; McGuckin, C; Nair, M; Russell, RK; Sasankan, N; Shannon, C, 2021
)
0.62
" There were two mild to moderate infusion-related adverse events; and five serious adverse events (three in the intravenous iron group, two in the oral iron group), unrelated to the study medication."( Efficacy and safety of intravenous ferric carboxymaltose compared with oral iron for the treatment of iron deficiency anaemia in women after childbirth in Tanzania: a parallel-group, open-label, randomised controlled phase 3 trial.
Abdulla, S; Asilia, P; Daubenberger, C; Glass, TR; Issa, A; Kuemmerle, A; Lweno, O; Meyer-Monard, S; Mswata, S; Mwebi, KD; Schmidlin, S; Simon, B; Tanner, M; Vanobberghen, F, 2021
)
0.62
"Intravenous iron substitution with ferric carboxymaltose was safe and yielded a better haemoglobin response than oral iron."( Efficacy and safety of intravenous ferric carboxymaltose compared with oral iron for the treatment of iron deficiency anaemia in women after childbirth in Tanzania: a parallel-group, open-label, randomised controlled phase 3 trial.
Abdulla, S; Asilia, P; Daubenberger, C; Glass, TR; Issa, A; Kuemmerle, A; Lweno, O; Meyer-Monard, S; Mswata, S; Mwebi, KD; Schmidlin, S; Simon, B; Tanner, M; Vanobberghen, F, 2021
)
0.62
"To define the risk of serious adverse events following administration of an undiluted, rapid, high-dose ferric carboxymaltose injection."( Safety of rapid injection of undiluted ferric carboxymaltose to patients with iron-deficiency anaemia: a Phase II single-arm study.
Bennett, A; Chunilal, S; Coughlin, E; Dev, A; Gilbertson, M; Indran, T; Opat, S; Pasricha, SR; van Dam, M, 2021
)
0.62
"In a single-arm, Phase II study in 121 patients with iron-deficiency anaemia, we administered up to 1000 mg of ferric carboxymaltose as a rapid undiluted bolus injection, and recorded adverse events and collected blood samples over the first hour, and again at 2 and 4 weeks post-treatment."( Safety of rapid injection of undiluted ferric carboxymaltose to patients with iron-deficiency anaemia: a Phase II single-arm study.
Bennett, A; Chunilal, S; Coughlin, E; Dev, A; Gilbertson, M; Indran, T; Opat, S; Pasricha, SR; van Dam, M, 2021
)
0.62
"No patient experienced a serious adverse event."( Safety of rapid injection of undiluted ferric carboxymaltose to patients with iron-deficiency anaemia: a Phase II single-arm study.
Bennett, A; Chunilal, S; Coughlin, E; Dev, A; Gilbertson, M; Indran, T; Opat, S; Pasricha, SR; van Dam, M, 2021
)
0.62
" The secondary outcome was to compare the safety of FCM and IS, assessed by the incidence of adverse events during iron replacement."( Comparative efficacy and safety of intravenous ferric carboxymaltose and iron sucrose for iron deficiency anemia in obstetric and gynecologic patients: A systematic review and meta-analysis.
Choi, YJ; Go, DY; Jang, YK; Ko, EJ; Lee, SW; Shin, HW; You, HS, 2021
)
0.62
"FCM group showed better efficacy in increasing Hb and ferritin levels and a favorable safety profile with fewer adverse events compared with IS group for IDA treatment among obstetric and gynecologic patients."( Comparative efficacy and safety of intravenous ferric carboxymaltose and iron sucrose for iron deficiency anemia in obstetric and gynecologic patients: A systematic review and meta-analysis.
Choi, YJ; Go, DY; Jang, YK; Ko, EJ; Lee, SW; Shin, HW; You, HS, 2021
)
0.62
" Adverse events and other safety parameters were noted."( Clinical effects and safety of ferric carboxymaltose in pregnancy: An Indian real-life experience.
Gupte, SA; Jangam, SM; Mudholkar, AS; Shah, AS; Venkataraman, G, 2021
)
0.62
" No adverse fetal or neonatal outcomes were observed."( Clinical effects and safety of ferric carboxymaltose in pregnancy: An Indian real-life experience.
Gupte, SA; Jangam, SM; Mudholkar, AS; Shah, AS; Venkataraman, G, 2021
)
0.62
" Adverse effects were assessed."( Clinical efficacy and safety of intravenous ferric carboxymaltose treatment of pediatric restless legs syndrome and periodic limb movement disorder.
Allen, RP; Chen, ML; DelRosso, LM; Ferri, R; Kapoor, V; Mogavero, MP; Picchietti, DL, 2021
)
0.62
"3%) experienced one or two adverse events; all were mild."( Clinical efficacy and safety of intravenous ferric carboxymaltose treatment of pediatric restless legs syndrome and periodic limb movement disorder.
Allen, RP; Chen, ML; DelRosso, LM; Ferri, R; Kapoor, V; Mogavero, MP; Picchietti, DL, 2021
)
0.62
"Erythropoiesis-stimulating agents (ESA) are effective for chemotherapy-induced anemia (CIA) but associated with serious adverse events."( Efficacy and safety of ferric carboxymaltose infusion in reducing anemia in patients receiving chemotherapy for nonmyeloid malignancies: A randomized, placebo-controlled study (IRON-CLAD).
Blackman, N; Boccia, R; Gilreath, JA; Henry, DH; Krupa, A; Makharadze, T, 2021
)
0.62
"Parenteral iron is generally considered safe in adults, and severe adverse events are extremely rare."( Safety of Ferric Carboxymaltose in Children: Report of a Case Series from Greece and Review of the Literature.
Alexiadou, S; Fotoulaki, M; Makis, A; Mantadakis, E; Ntoumpara, M; Panagopoulou, P; Papazoglou, A; Tragiannidis, A, 2022
)
0.72
" No adverse events were reported."( Effectiveness and safety of an on-demand ferric carboxymaltose infusion strategy in patients with inflammatory bowel disease: a real world experience.
Casà, A; Crispino, F; Grova, M; Macaluso, FS; Maida, M; Mannino, M; Orlando, A; Renna, S; Rizzuto, G, 2022
)
0.72
" It is, therefore, a potentially serious adverse effect whose prevalence is unknown and which requires high clinical suspicion to be detected."( Hypophosphatemic osteomalacia, a side effect of iron carboxymaltose administration.
Bernal, L; Gutiérrez Casbas, A; Madero Velázquez, L; Muñoz Pérez, R; Orts, B; Rodríguez, A; Sempere, L, 2022
)
0.72
" The primary outcome was the incidence of adverse reactions within 24 hours of the FDI infusion."( Real-world experience of intravenous ferric derisomaltose evaluated through safety and efficacy reporting in the UK.
Bhandari, S; Kennedy, NA; Nadaraja, S; Sinclair, RCF; Wakatsuki, M, 2022
)
0.72

Pharmacokinetics

Acebutolol Cmax did not significantly differ between the two formulations. The plasma half-life and elimination rate constant for ace butolol showed a four-fold variation but these did not correlate with the degree of renal impairment.

ExcerptReferenceRelevance
" Pharmacokinetic data were obtained in hypertensive male patients (4) after treatment with 14C-radioactively labelled acebutolol hydrochloride."( [Pharmacokinetics of acebutolol].
Collins, RF, 1975
)
0.78
" Using a computer program, various pharmacokinetic parameters were estimated from the date of each subject."( Observations on the pharmacokinetics of acebutolol.
Hamer, J; Kaye, CM; Kumana, CR; Leighton, M; Turner, P, 1976
)
0.52
" After the first dose, acebutolol Cmax did not significantly differ between the two formulations; however, on day 10 acebutolol Cmax was significantly higher after SR formulation."( A comparative pharmacokinetic and pharmacodynamic study of conventional and sustained-release preparations of acebutolol in healthy volunteers.
Fleurot, O; Frydman, A; Jaillon, P; Le Liboux, A; Lecocq, B; Lecocq, V; Montay, G, 1991
)
0.8
" Metoprolol is affected by hydralazine, the AUC and Cmax being significantly increased."( The effect of hydralazine on the pharmacokinetics of three different beta adrenoceptor antagonists: metoprolol, nadolol, and acebutolol.
Dean, S; Jack, DB; Kendall, MJ; Laugher, SJ; Tenneson, ME; Zaman, R,
)
0.34
"Higher AUC and Cmax values were obtained for metoprolol, oxprenolol and propranolol in groups receiving the low-dose oestrogen-ethinyl oestradiol oral contraceptive, but statistical significance was reached only with metoprolol AUC."( Beta-adrenoceptor blocker pharmacokinetics and the oral contraceptive pill.
Jack, DB; Kendall, MJ; Quarterman, CP; Smith, SR; Zaman, R, 1984
)
0.27
" The plasma half-life and elimination rate constant for acebutolol showed a four-fold variation but these did not correlate with the degree of renal impairment."( Acebutolol pharmacokinetics in renal failure.
George, CF; Renwick, AG; Smith, RS; Warren, DJ, 1983
)
1.95
" The main pharmacokinetic parameters of acebutolol did not differ significantly: AUC 4492 +/- 272 micrograms l-1h given alone versus 4118 +/- 354 micrograms l-1h with HCT, half-life (7,69 +/- 0,32 h vs 8,10 +/- 0,72 h) and renal clearance (13,1 +/- 0,5 lh-1 vs 13,8 +/- 0,9 lh-1), respectively."( Pharmacokinetics in man of acebutolol and hydrochlorothiazide as single agents and in combination.
Delhotal, B; Flouvat, B; Gaillot, J; Le Liboux, A; Roux, A, 1983
)
0.83
"This study demonstrates the application of neural networks to predict the pharmacokinetic properties of beta-adrenoreceptor antagonists in humans."( Quantitative structure-pharmacokinetic relationships (QSPR) of beta blockers derived using neural networks.
Gobburu, JV; Shelver, WH, 1995
)
0.29
" Stereoselective analysis showed the apparent distribution volume and the area under plasma concentration-time curves (AUC) of R-(+)-propranolol to be, respectively, one-quarter and twice those of the S-(-)-enantiomer and differences in pharmacokinetic parameters between the two were magnified by turpentine oil pretreatment."( Effects of turpentine oil pretreatment on beta-blocker pharmacokinetic parameters in rats.
Hasegawa, R; Kimura, T; Murai-Kushiya, M; Okada, S, 1993
)
0.29
" No statistical differences are observed in apparent volume of distribution (Vd), terminal elimination half-life (t1/2), total body clearance (Clt), or renal clearance (Clr) with respect to dose administered."( Pharmacokinetics of acebutolol enantiomers after intravenous administration of racemate in a rat model: a dosing range comparison.
Foster, RT; Mostafavi, SA, 1997
)
0.62
" 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
)
0.55
" 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
" 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
" Pharmacokinetic parameters were determined after the third infusion of each product."( Pharmacokinetics and tolerability of a new intravenous immunoglobulin preparation, IGIV-C, 10% (Gamunex, 10%).
Ballow, M; Berger, M; Bonilla, FA; Buckley, RH; Cunningham-Rundles, CH; Fireman, P; Kaliner, M; Lathia, C; Ochs, HD; Skoda-Smith, S; Sweetser, MT; Taki, H, 2003
)
0.32
"The pharmacokinetic profiles observed in these trials indicate that IGIV-C, 10% may replace, and be administered in a manner similar to, IGIV-SD, 10%."( Pharmacokinetics and tolerability of a new intravenous immunoglobulin preparation, IGIV-C, 10% (Gamunex, 10%).
Ballow, M; Berger, M; Bonilla, FA; Buckley, RH; Cunningham-Rundles, CH; Fireman, P; Kaliner, M; Lathia, C; Ochs, HD; Skoda-Smith, S; Sweetser, MT; Taki, H, 2003
)
0.32

Compound-Compound Interactions

The efficacy of the calcium channel blocker nitrendipine alone and in combination with the beta blocking agent acebutolol or hydrochlorothiazide was tested in 34 patients with moderate essential hypertension.

ExcerptReferenceRelevance
"The efficacy of the calcium channel blocker nitrendipine alone and in combination with the beta blocking agent acebutolol or hydrochlorothiazide was tested in 34 patients with moderate essential hypertension."( [Therapy of moderate hypertension with the calcium antagonist nitrendipine in combination with beta receptor blocker or diuretic].
Kolloch, R; Müller, HM; Overlack, A; Stumpe, KO, 1990
)
0.49
" By using programmed electrical stimulation in combination with MAP recordings at different pacing rates in the intact dog heart, it was possible to classify and to a certain extent to elucidate the mode of action of various cardioactive drugs in vivo."( Classification of cardioactive drugs in vivo by using programmed electrical stimulation in combination with monophasic action potential recordings at different pacing rates.
Amlie, JP; Landmark, K; Refsum, H, 1981
)
0.26
"5 mg, 25 mg, and 50 mg hydrochlorothiazide combined with 400 mg acebutolol was assessed."( Lack of effect of beta-blocker on flat dose response to thiazide in hypertension: efficacy of low dose thiazide combined with beta-blocker.
Banks, RA; Bayliss, J; MacGregor, GA; Markandu, ND; Roulston, J, 1983
)
0.5
" In the current work, we demonstrate that Gr64f is required in combination with Gr5a for the behavioral response to trehalose and for production of nerve responses to trehalose."( Gr64f is required in combination with other gustatory receptors for sugar detection in Drosophila.
Jiao, Y; Montell, C; Moon, SJ; Ren, Q; Wang, X, 2008
)
0.35

Bioavailability

The pharmacokinetics and bioavailability of diacetolol, the principal metabolite of acebutolol were studied in 6 healthy subjects. Alteration in ace butolol pharmacokinetic was more pronounced in the acute group.

ExcerptReferenceRelevance
"The pharmacokinetics and bioavailability of diacetolol, the principal metabolite of acebutolol, were studied in 6 healthy subjects."( Pharmacokinetics and bioavailability of diacetolol, the main metabolite of acebutolol.
Andre-Fouet, X; Chau, NP; Flouvat, B; Gregoire, J; Roux, A; Viallet, M; Woehrle, R, 1981
)
0.72
" Recently a new method has been proposed to determine absolute bioavailability in the absence of intravenous dose."( Prediction of absolute bioavailability for drugs using oral and renal clearance following a single oral dose: a critical view.
Mahmood, I, 1997
)
0.3
"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
" Alteration in acebutolol pharmacokinetics was more pronounced in the acute group as evidenced by the significantly higher values the area under the plasma concentration time curve, absorption rate constant and maximum plasma concentration compared with chronic or control group."( Pharmacokinetic changes of acebutolol after oral administration in rabbits with diabetes mellitus induced by alloxan.
Bae, HY; Choi, DH; Choi, JS, 2003
)
0.97
" The proposed method is simple, with low instrumentation requirements, suitable for quality control application, bioavailability and bioequivalency studies."( Spectrofluorimetric determination of drugs containing active methylene group using N1-methyl nicotinamide chloride as a fluorigenic agent.
El Barbary, RA; El Dawya, MA; Mabrouk, MM, 2006
)
0.33
"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
" To show the importance of physicochemical properties, the classic QSAR and CoMFA of neonicotinoids and prediction of bioavailability of pesticides in terms of membrane permeability in comparison with drugs are described."( Importance of physicochemical properties for the design of new pesticides.
Akamatsu, M, 2011
)
0.37
" It was concluded that bioavailability is comparable for therapeutic doses of ferrous sulphate and iron polymaltose in iron-deficient subjects."( Absorption of iron polymaltose and ferrous sulphate in rats and humans. A comparative study.
Gregory, MC; Jacobs, P; Wormald, LA, 1979
)
0.26
" The leucine absorption rate was significantly reduced after the bypass, but the absorption rates of glycylleucine and glucose as well as the hydrolysis rate of maltose were unchanged."( Absorptive and digestive function of the jejunum after jejunoileal bypass for treatment of human obesity.
Adibi, SA; Fogel, MR; Ravitch, MM, 1976
)
0.26
" At a physiological low level of maltitol intake, the results also indicated an insignificant calorie-saving effect in comparison to sucrose, an effect based mainly on the slow absorption rate of the maltitol cleavage product sorbitol."( Gastrointestinal transit and digestibility of maltitol, sucrose and sorbitol in rats: a multicompartmental model and recovery study.
Grossklaus, R; Herold, M; Klingebiel, L; Krüger, D; Lorenz, S, 1992
)
0.28
" The water absorption rate of the SP-ED was more than that of the AA-ED."( [Studies on the absorption of carbohydrate and nitrogen sources in elemental diets].
Oheda, Y, 1989
)
0.28
" Fructose appeared to be poorly absorbed from the intestinal tract and did not appear to be converted to glucose."( Apparent inability of channel catfish to utilize dietary mono- and disaccharides as energy sources.
Poe, WE; Wilson, RP, 1987
)
0.27
" The relationship which exists between the rate of absorption of glucose and the concentration in the luminal fluid of either disaccharide or free glucose is of the Michaelis-Menten type."( Disaccharide absorption by amphibian small intestine in vitro.
Parsons, DS; Prichard, JS, 1968
)
0.25
"Because sorbitol is poorly absorbed in the small intestine, it may be the origin of large amounts of residues reaching the large intestine and may be substrate for microbial activity."( Absorption balances and kinetics of nutrients and bacterial metabolites in conscious pigs after intake of maltose- or maltitol-rich diets.
Giusi-Périer, A; Rérat, A; Vaissade, P, 1993
)
0.29
" The bioavailability of azetirelin after the oral administration of this enteric capsule with LM and CA was 43."( Development of an oral formulation of azetirelin, a new thyrotropin-releasing hormone (TRH) analogue, using n-lauryl-beta-D-maltopyranoside as an absorption enhancer.
Fujita, T; Ito, Y; Matsumoto, K; Murakami, M; Muranishi, S; Sasaki, I; Tozaki, H; Yamamoto, A, 1999
)
0.3
"The purpose of this study was to characterize the effects of alkylglycosides on the bioavailability of calcitonin following nasal and ocular administration."( Enhanced bioavailability of calcitonin formulated with alkylglycosides following nasal and ocular administration in rats.
Ahsan, F; Arnold, J; Meezan, E; Pillion, DJ, 2001
)
0.31
" The extent of calcitonin absorption was determined directly from the plasma calcitonin level-time curve and the bioavailability of calcitonin was determined from the area under the plasma calcium level-time curve."( Enhanced bioavailability of calcitonin formulated with alkylglycosides following nasal and ocular administration in rats.
Ahsan, F; Arnold, J; Meezan, E; Pillion, DJ, 2001
)
0.31
" can be effectively used to enhance the bioavailability of nasally and ocularly administered calcitonin."( Enhanced bioavailability of calcitonin formulated with alkylglycosides following nasal and ocular administration in rats.
Ahsan, F; Arnold, J; Meezan, E; Pillion, DJ, 2001
)
0.31
" The relative bioavailability of insulin formulations containing TDM was higher (0."( Pulmonary absorption of insulin mediated by tetradecyl-beta-maltoside and dimethyl-beta-cyclodextrin.
Ahsan, F; Hussain, A; Yang, T; Zaghloul, AA, 2003
)
0.32
" Absolute and relative bioavailability of enoxaparin were increased by two-fold when the alkyl chain length of maltosides was increased from 8 to 14 carbons."( Chain length-dependent effects of alkylmaltosides on nasal absorption of enoxaparin.
Ahsan, F; Khan, MA; Mustafa, F; Yang, T, 2004
)
0.32
" Fungal strains and cyclodextrins were used in order to degrade fluorene and optimize fluorene bioavailability and degradation in soil slurries."( Enhanced degradation of fluorene in soil slurry by Absidia cylindrospora and maltosyl-cyclodextrin.
Garon, D; Sage, L; Seigle-Murandi, F; Wouessidjewe, D, 2004
)
0.32
"The bioavailability of lipophilic substrates is critical for biotransformations with isolated enzymes as well as with whole cells."( Saccharides as efficacious solubilisers for highly lipophilic compounds in aqueous media.
Bertau, M; Jörg, G, 2004
)
0.32
" The implication of this study's results is that alcohol absorption rate may be an important source of confounding effects in behavioral research in the laboratory, because it may be affected by beverages or other experimental conditions."( Does expectancy affect alcohol absorption?
Cole-Harding, S; Michels, VJ, 2007
)
0.34
" Oral iron is a low cost treatment however its effectiveness is limited by low bioavailability and poor tolerability."( State of the iron: how to diagnose and efficiently treat iron deficiency anemia in inflammatory bowel disease.
Bhandari, S; Muñoz, M; Reinisch, W; Staun, M, 2013
)
0.39
" In the present study, we focused on maltosyl-β-cyclodextrin (malt-β-CD) as a new water-soluble carrier and it was investigated whether drug/malt-β-CD microspheres could improve the bioavailability compared with our previously reported drug/mannitol (MAN) microspheres."( Improved bioavailability of a water-insoluble drug by inhalation of drug-containing maltosyl-β-cyclodextrin microspheres using a four-fluid nozzle spray drier.
Kano, Y; Okada, H; Ozeki, T; Tagami, T; Takahashi, N, 2012
)
0.38
"Appropriate assessment of transepithelial permeability in vitro is needed to estimate and model trans-mucosal bioavailability to achieve oral delivery of protein biopharmaceuticals."( The Caco-2 cell culture model enables sensitive detection of enhanced protein permeability in the presence of N-decyl-β-d-maltopyranoside.
Anderluh, G; Caserman, S; Hribar, G; Komel, R; Marušić, M; Zupančič, T, 2013
)
0.39
" In conclusion, FCM has low bioavailability for liver parenchyma cells, therefore liver iron deposition is unlikely."( Iron sucrose and ferric carboxymaltose: no correlation between physicochemical stability and biological activity.
Cornelius, C; Goldenberg, H; Haider, K; Praschberger, M; Scheiber-Mojdehkar, B; Schitegg, M; Sturm, B, 2015
)
0.42
" While DDM led to a 20-fold increase in FD4 bioavailability when it was applied in TM, no significant permeation enhancement was seen in FaSSIFmod/FeSSIFmod6."( Interaction with Mixed Micelles in the Intestine Attenuates the Permeation Enhancing Potential of Alkyl-Maltosides.
Buckley, ST; Gradauer, K; Higashino, H; Kataoka, M; Nishiumi, A; Pedersen, BL; Unrinin, K; Yamashita, S, 2015
)
0.42
" Oral iron is simple and cheap to administer and does not require hospital visits, but is poorly absorbed in advanced CKD and is associated with unpleasant gastrointestinal side effects."( Iron Treatment Strategies in Nondialysis CKD.
Macdougall, IC, 2016
)
0.43
" Rapid rate of absorption is suggested to be important for optimal efficacy."( A multicenter, open-label, long-term safety and tolerability study of DFN-02, an intranasal spray of sumatriptan 10 mg plus permeation enhancer DDM, for the acute treatment of episodic migraine.
Allenby, K; Brand-Schieber, E; Cady, RK; Munjal, S; Rapoport, AM; Spierings, ELH, 2017
)
0.46
"In this paper, we explore the strategy increasingly used to improve the bioavailability of poorly water-soluble crystalline drugs by formulating their amorphous solid dispersions."( Molecular Dynamics and Physical Stability of Ibuprofen in Binary Mixtures with an Acetylated Derivative of Maltose.
Antosik-Rogóż, A; Chmiel, K; Grzybowska, K; Grzybowski, A; Jachowicz, R; Knapik-Kowalczuk, J; Kowalska-Szojda, K; Lodowski, P; Paluch, M; Szafraniec-Szczęsny, J; Woyna-Orlewicz, K, 2020
)
0.56
"Oral sucrosomial iron (SI) combines enhanced bioavailability and tolerance compared to conventional oral iron along with similar efficacy compared to intravenous iron in several conditions associated with iron deficiency (ID)."( Oral sucrosomial iron improves exercise capacity and quality of life in heart failure with reduced ejection fraction and iron deficiency: a non-randomized, open-label, proof-of-concept study.
Balta, D; Farmakis, D; Karavidas, A; Karavidas, IN; Lazaros, G; Parissis, J; Polyzogopoulou, E; Troganis, E, 2021
)
0.62

Dosage Studied

Acebutolol hydrochloride (400 mg/day) can be given to a neonate if the daily maternal dosage exceeds 400 mg/ day and/or renal function in the mother is impaired. The aims of this investigation were to establish the effective dosage range, to study the effect on supine, standing and exercise blood pressure (BP) and heart rate (HR)

ExcerptRelevanceReference
" Both timolol and acebutolol had a significant hypotensive effect at 24 hours and a low incidence of side effects, suggesting that further increases in dosage might be effective and well tolerated."( Randomised study of six beta-blockers and a thiazide diuretic in essential hypertension.
Wilcox, RG, 1978
)
0.59
" 2 Dose-response and time course experiments revealed that propranolol greatly inhibited microsomal and mitochondrial calcium uptake whereas both acebutolol and practolol showed slight depressant effects."( Comparison of the actions of acebutolol, practolol and propranolol on calcium transport by heart microsomes and mitochondria.
Dhalla, NS; Lee, SL, 1976
)
0.75
" Twenty-three patients received acebutolol at a dosage of 400--800 mg daily as sole treatment and nine patients received concurrent treatment with thiazide diuretics."( Clinical trial of acebutolol (Sectral) in hypertension.
Charoenlarp, K; Jaroonvesama, N, 1978
)
0.88
" Optimum dosage defined in an open assessment varied from 200--600 mg twice daily."( Acebutolol in hypertension--double-blind trial against placebo.
Martin, MA; Phillips, CA; Smith, AJ, 1978
)
1.7
" Dosage can be progressively increased up to 30 mg/day."( [Prazosine: a new vasodilator used for treatment of hypertension (author's transl)].
Bret, M; Fillastre, JP; Godin, M, 1978
)
0.26
"Acebutolol at therapeutic dosage may considerably disturb the determination of urinary 17-oxosteroids by Zimmerman's reaction."( [Acébutolol: conditions of its interference in the estimation of urinary 17-oxosteroids. Method of estimation by Zimmerman's reaction (author's transl)].
Firmin, C; Pouclet, J; Thevenet, M, 1979
)
1.7
"An open multicentre trial was carried out in 13 hypertensive patients, who had responded satisfactorily to and been stabilized on treatment with 400 mg acebutolol daily in divided doses, to assess the effectiveness and tolerance of the same daily dosage given as a single morning dose."( Acebutolol (400 mg) given as a single daily dose to hypertensive patients previously stabilized on 400 mg acebutolol daily in divided doses: an open multicentre study.
Ashton, WL,
)
1.77
" There is a more than proportional increase in area with increasing oral doses, and the area over a dosing interval following multiple oral doses is greater than the total area after a single dose of the same size."( Dose-dependent acebutolol disposition after oral administration.
Harrison, DC; Meffin, PJ; Peters, FA; Winkle, RA, 1978
)
0.61
" The initial dosage was 600 mg a day and was sufficient in the majority of patients."( [Results of the treatment of essential arterial hypertension following prolonged (24 months administration of acebutolol)].
Fillastre, JP; Wolf, LM, 1975
)
0.47
" The mean dosage of acebutolol was 10 mg/kg (maximum 22 mg/kg) and the drug was very well tolerated."( [Acebutolol in the treatment of arterial hypertension. Clinical study].
Chaignon, M; Guédon, J; Lucsko, M, 1975
)
1.49
" The hypotensive activity of acebutolol was confirmed when a dosage of 600 mg/day was used, with en absence of side effects."( [Comparative study of acebutolol and propranolol in the treatment of arterial hypertension].
Tacquet, A, 1975
)
0.86
" Our study suggests: 2 The acetyl metabolite was present in concentrations greater than those of acebutolol at all times during the dosing interval in all seven subjects."( Acebutolol metabolite plasma concentration during chronic oral therapy.
Harrison, DC; Meffin, PJ; Ricks, WB; Winkle, RA, 1977
)
1.92
" Data obtained from 15-min infusions were used to predict plateau blood concentrations with good accuracy during an 8-hr dosage regimen."( Acebutolol disposition after intravenous administration.
Harrison, DC; Meffin, PJ; Peters, FA; Winkle, RA, 1977
)
1.7
" In the oral study, the peak effect was achieved at a dosage of 200 mg per day (100 mg twice daily) of acebutolol."( Effect of acebutolol, a new beta-receptor antagonist on heart rate and rate-pressure product in normal subjects.
Sharma, PL, 1976
)
0.87
"Acebutolol, a new cardioselective beta-blocking agent, has been given for 5 days, at a daily dosage of 600 mg to 8 patients with mild essential hypertension."( [Effects of acebutolol on the renin-aldosterone system in essential arterial hypertension].
Corvol, P; Ménard, J; Plouin, PF, 1975
)
2.08
" More specifically, a comparison of the two drugs during the final 6 hours (3 AM to 9 AM) of the dosing interval showed that the mean decrease in diastolic BP of 10."( Antihypertensive effects of beta-blockers administered once daily: 24-hour measurements.
Cheung, DG; Graettinger, WF; Neutel, JM; Schnaper, H; Weber, MA, 1990
)
0.28
" Mean arterial pressure (MAP) began to fall 2-3 h after dosing in parallel with a decrease in SVR."( Acute and long-term effects of acebutolol on systemic and renal hemodynamics, body fluid volumes, catecholamines, active renin, aldosterone, and lymphocyte beta-adrenoceptor density.
Boomsma, F; Derkx, FH; Fischberg, DJ; Man in 't Veld, AJ; Molinoff, PB; Schalekamp, MA; van den Meiracker, AH; van Eck, HJ, 1988
)
0.56
" The dose-response effects of atenolol and acebutolol, two cardioselective compounds, the latter also possessing a degree of ISA, were therefore compared in a single-blind, dose-response, crossover study in patients within 18 h of suffering an uncomplicated acute myocardial infarction."( Cardioselective beta-blockade with atenolol and acebutolol following acute myocardial infarction: a multiple-dose haemodynamic comparison.
Ahuja, RC; Frais, MA; Nelson, GI; Silke, B; Taylor, SH; Verma, SP,
)
0.65
" Each drug was given for a two-month period, the maximum acebutolol dosage reaching 600 mg tid and the maximum propranolol dosage 80 mg tid."( Comparison of acebutolol and propranolol therapy for ventricular arrhythmias.
Berdoff, R; Platia, EV; Reid, PR; Stone, G, 1985
)
0.88
"A double-blind randomized study was designed to investigate differences in the recovery of finger skin temperature after finger cooling during dosing with placebo or one of four beta-blockers: propranolol, atenolol, pindolol, and acebutolol."( The influence of intrinsic sympathomimetic activity and beta-1 receptor selectivity on the recovery of finger skin temperature after finger cooling in normotensive subjects.
de Boo, T; Lemmens, WA; Lenders, JW; Salemans, J; Thien, T; van't Laar, A, 1986
)
0.45
" PRA activity was significantly and markedly reduced by both bunolol and metoprolol shortly after dosing at a time when HR was significantly reduced but MBP was not."( Antihypertensive effects of 12 beta adrenoceptor antagonists in conscious spontaneously hypertensive rats: relationship to changes in plasma renin activity, heart rate and sympathetic nerve function.
Antonaccio, MJ; DeForrest, JM; High, J; Sybertz, E, 1986
)
0.27
" The decrease in diastolic blood pressure at the end of the second week was significantly correlated with the reciprocal of the plasma celiprolol concentration at steady-state at the end of the dosage interval."( Comparison of the antihypertensive effects of celiprolol and acebutolol.
Belovezhdov, N; Gerova, Z; Terziivanov, D; Vlahov, V, 1988
)
0.52
" There was no evidence of a flat dose-response curve in the daily dose range of 12."( Is low-dose hydrochlorothiazide effective?
Freis, ED; Magee, PF, 1986
)
0.27
"02; 2--A more frequent adjustment of daily dosage with MD (n = 15) than with ACE (n = 10) or LAB (n = 7); 3--The absence of any significant difference for uricemia level, platelet counts, foetal cardiac rythm, and occurrence of pre-eclampsia (MD = 4; ACE = 3; LAB = 4; 4--An equivalent birth-weight (MD = 3110 +/- 628 g; ACE = 3115 +/- 645."( [Randomized, comparative study on the treatment of moderate arterial hypertension during pregnancy: methyldopa, acebutolol, labetalol].
Blazquez, G; Gérard, J; Lardoux, H; Leperlier, E, 1988
)
0.49
" Evaluation of the iatrogenic risk shows that pharmacologically active amounts of acebutolol might be received by a neonate if the daily maternal dosage exceeds 400 mg/day and/or renal function in the mother is impaired."( To nurse when receiving acebutolol: is it dangerous for the neonate?
Bianchetti, G; Boutroy, MJ; Dubruc, C; Morselli, PL; Vert, P, 1986
)
0.8
" Nitrendipine (mean dose 32 mg/day) and acebutolol (414 mg/day) were administered in monotherapy in increasing dosage and mefruside was added in patients not controlled by monotherapy."( Calcium entry blockade or beta-blockade in long-term management of hypertension in blacks.
Amery, A; Ditu, M; Fagard, R; Lepira, B; Lijnen, P; Lissens, W; M'Buyamba-Kabangu, JR; Staessen, J; Tshiani, KA, 1987
)
0.54
" However, the drugs were not equivalent: In addition to its greater potency, nadolol differed from propranolol and metoprolol in the slope of its dose-response curve."( Comparison of four beta-blockers as assessed by 24-hour ECG recording.
Coumel, P; Delhotal-Landes, B; Escoubet, B; Gourmel, B; Leclercq, JF; Maison-Blanche, P; Poirier, JM, 1986
)
0.27
"The hemodynamic dose-response effects of intravenous (25 and 50 mg) and oral (200 and 400 mg) acebutolol were compared in a randomized between-group study in men within 17 hours of an acute uncomplicated myocardial infarction."( Circulatory effects of intravenous and oral acebutolol in acute myocardial infarction.
Baliga, G; Clarke, J; Nelson, G; Silke, B; Taylor, SH; Verma, SP, 1985
)
0.75
" Standardized experiments were performed using a chronically reserpinized canine preparation for the assessment of dose-response curves of changes in hemodynamics, left ventricular contractility, heart rate, AV-conduction time, and myocardial oxygen consumption especially at therapeutic doses."( Sympathomimetic and cardiodepressant effects of acebutolol, oxprenolol, pindolol, and propranolol. A comparative study on changes in hemodynamics, contractility, heart rate, and AV-conduction time at therapeutic doses.
Bender, F; Gülker, H; Heuer, H; Kristek, J, 1981
)
0.52
" When applied to the assay of biological fluids collected during single and chronic oral dosing with acebutolol (Sectral), this procedure failed to reveal any important stereoselectivity in the disposition of either acebutolol or diacetolol in man."( Preliminary study of the disposition in man of acebutolol and its metabolite, diacetolol, using a new stereoselective hplc method.
Gulaid, A; Kaye, CM; Sankey, MG, 1984
)
0.74
" Blood pressures during once-a-day dosing were not different from those during twice-a-day dosing at any time."( Once-daily dosing of acebutolol in hypertension.
Hamet, P; Kreeft, JH; Larochelle, P; Marquez-Julio, A; Ogilvie, RI,
)
0.45
" The equipotent beta-blocking dose of each drug was obtained by comparing isoproterenol dose-response curves."( Effects of equipotent blocking doses of acebutolol, acebutolol's primary metabolite, and propranolol on left ventricular hemodynamics in conscious awake dogs.
Griffin, G; Harrison, DC; Kernoff, R; Magder, S; Rubenson, D,
)
0.4
" There was no correlation between the levels of antinuclear antibodies and the dosage or duration of acebutolol treatment."( [Prevalence of antinuclear antibodies in hypertensive diabetics treated with acebutolol].
Abadie, E; Leblanc, H; Lombrail, P; Marre, M; Passa, P, 1984
)
0.71
" 2 Salbutamol airway dose-response curves were obtained by measuring the airway response as the change in specific airway conductance (sGaw) after increasing doses of inhaled salbutamol."( Bronchial and cardiac beta-adrenoceptor blockade--a comparison of atenolol, acebutolol and labetalol.
Baldwin, CJ; Gribbin, HR; Mackay, AD; Tattersfield, AE, 1981
)
0.49
"The hemodynamic dose-response effects of intravenous acebutolol, a cardioselective beta-adrenoceptor antagonist with intrinsic sympathomimetic activity, were evaluated in 12 male subjects with angiographically confirmed coronary artery disease."( Dose-response effects of cardioselective beta blockade in coronary artery disease.
Hussain, M; Nelson, G; Silke, B; Taylor, SH; Verma, SP, 1984
)
0.52
" The dose-response relationship and duration of action of 3'-acetyl-4'-(2-hydroxy-3-isopropylaminopropyl)-butyranilide (acebutolol, Prent) were determined under double-blind conditions in 9 volunteers using heart rate at rest and during exercise as a test parameter."( [Dose-response relationship and duration of action of acebutolol / investigations on heart rate behaviour and ischemic ST-segment depression].
Kaltenbach, M; Kober, G; Mikludy, R; Veidt, J, 1982
)
0.72
" Further increases in acebutolol dosage to a maximum of 2000 mg daily in 13 patients whose hypertension was not well controlled on lower doses resulted in a mean supine blood pressure of 132/92 mmHg."( Antihypertensive action of acebutolol (Sectral) when used concomitantly with hydrochlorothiazide.
Brossard, JJ; McKenzie, JK; Mitenko, PA, 1982
)
0.88
" 4 Forearm blood flow, at rest, was significantly reduced at 2 h after dosing with propranolol, but not after acebutolol."( The effects of oral acebutolol and propranolol on forearm blood flow in hypertensive patients.
Ireland, MA; Littler, WA, 1981
)
0.8
" The aims of this investigation were to establish the effective dosage range, to study the effect on supine, standing and exercise blood pressure (BP) and heart rate (HR), and to compare the efficacy of once daily (OM) with twice daily (BD) dosing of acebutolol."( The antihypertensive action of acebutolol.
Koh, TH; Low, LP, 1981
)
0.73
" The mean daily dosage of diclofurime was 518 mg, the drug being taken in three divided doses."( [Diclofurime, a new major hypotensive agent. Clinical study in 24 patients (author's transl)].
Barthes, P; Chevallier, B; Cribier, A; Letac, B, 1980
)
0.26
" dosing for four days in male Sprague-Dawley rats (n = 6)."( Pharmacokinetics of single oral and multiple intravenous and oral administration of acebutolol enantiomers in a rat model.
Foster, RT; Mostafavi, SA, 1998
)
0.52
" Clinical inputs include agent efficacy, side effects, and compliance with dosing schedules."( An economic evaluation of the JNC hypertension guidelines using data from a randomized controlled trial. Joint National Committee.
Neil, N; Perfetto, E; Ramsey, SD; Sullivan, SD,
)
0.13
" Forty-six outpatients suffering from mild to moderate essential hypertension [diastolic blood pressure (DBP) ranging between 95 and 120 mm Hg] were randomly given either 10 mg of bisoprolol or 400 mg of acebutolol once a day for 8 weeks; this dosage was doubled after 4 weeks if DBP was still above 90 mm Hg."( Effect of bisoprolol and acebutolol on resting blood pressure and on exercise blood pressure profile in hypertensive patients: a comparative, single-blind study.
Bouvier, JM; Herrero, G; Rabot, D, 1990
)
0.77
" The revised document should indicate the conditions under which various classes of substances constitute human health hazards -- including dosage levels and routes of entry."( Essential hormones as carcinogenic hazards.
Bowers, EJ; Clelland, RC; Hickey, RJ, 1979
)
0.26
" The results of the carcinogenic effects of these natural substances is in question because of administered dosage levels, chemical structure of the substances, the route the hormones entered the biological system, and testing done in animals and in vitro."( Essential hormones as carcinogenic hazards.
Bowers, EJ; Clelland, RC; Hickey, RJ, 1979
)
0.26
" Rate constants of transport between the compartments investigated were determined; they showed characteristics which could be related to the substance and the dosage administered."( Gastrointestinal transit and digestibility of maltitol, sucrose and sorbitol in rats: a multicompartmental model and recovery study.
Grossklaus, R; Herold, M; Klingebiel, L; Krüger, D; Lorenz, S, 1992
)
0.28
" Foals were assigned randomly to treatments consisting of 20% (wt/vol) solutions of either maltose, lactose, or sucrose, dosed at 1 g/kg of BW, or glucose, dosed at ."( Use of oral tolerance tests to investigate disaccharide digestion in neonatal foals.
Beede, DK; Borum, P; Johnson, EL; Lieb, S; Ott, EA; Rice, L; Wilcox, CJ, 1992
)
0.28
" Subclones of each gene derived from the MAL6 locus were inserted into the multicopy shuttle plasmid YEp13, introduced into MAL1 and mal1 strains and the effects of altered gene dosage of each gene, or a combination of them, on MAL gene expression investigated."( Regulation of MAL gene expression in yeast: gene dosage effects.
Buchferer, B; Goldenthal, MJ; Marmur, J; Vanoni, M, 1987
)
0.27
" Dose-response studies of GS-Mal treatment of intact cells suggested that some functional carriers lack a reactive external sulfhydryl, which can be partially regenerated by pretreatment with excess cysteine."( Reaction of an exofacial sulfhydryl group on the erythrocyte hexose carrier with an impermeant maleimide. Relevance to the mechanism of hexose transport.
May, JM, 1988
)
0.27
" The detailed biochemical analysis of the lipid composition rules out the possible interference of this disaccharide on the lipid metabolism, at least with the dosage and duration of treatment used in the experiment."( Nutritional studies on maltitol. Part 2: Effect on lipid metabolism and fatty acid composition of different rat tissues.
Barzanti, V; Carenini, G; Gentili, P; Maranesi, M, 1984
)
0.27
" ruminantium SS2/R5 failed to establish in sheep which were dosed twice daily with 10 g of sorbitol."( Isolation and attempted introduction of sugar alcohol-utilizing bacteria in the sheep rumen.
Walker, ND; Wallace, RJ, 1993
)
0.29
"05, U test of Mann-Whitney), although the improvement only could be seen at a low dosage during the first hour."( Inhibitory effect and mechanism of acarbose combined with gymnemic acid on maltose absorption in rat intestine.
Hiji, Y; Imoto, T; Luo, H; Wang, LF, 2001
)
0.31
" Dose-response studies revealed that within the family of alkylmaltoside derivatives, (C(8-16)), maximal increases in insulin absorption took place when tetradecylmaltoside (C(14)) was added to the formulation."( Synthetic long-chain alkyl maltosides and alkyl sucrose esters as enhancers of nasal insulin absorption.
Ahsan, F; Arnold, JJ; Balusubramanian, BM; Meezan, E; Pillion, DJ; Piraner, O, 2002
)
0.31
" When CF and LM were orally administered to rats using chitosan capsules, the plasma concentration of CF was much higher than those in other dosage forms including solution and gelatin capsules."( Improvement of absorption enhancing effects of n-dodecyl-beta-D-maltopyranoside by its colon-specific delivery using chitosan capsules.
Artersson, P; Attia, M; Fetih, G; Fujita, T; Habib, F; Itoh, K; Lindberg, S; Okada, N; Yamamoto, A, 2005
)
0.33
" Titration of the IVIg showed a clear dose-response effect."( Therapeutic efficacy of high-dose intravenous immunoglobulin in Mycobacterium tuberculosis infection in mice.
Brennan, J; Coade, S; Colston, MJ; Dagg, B; Grigorieva, E; Jolles, S; Lowrie, DB; Roy, E; Stavropoulos, E; Tascon, RE; Walker, B, 2005
)
0.33
"Adsorption characteristics of medicinal carbon powder (JP 14) for acetaminophen were examined at 37 degrees C using conventional incubation in an attempt to obtain an effective oral dosage form."( Medicinal carbon tablets for treatment of acetaminophen intoxication: adsorption characteristics of medicinal carbon powder and its tablets.
Ito, A; Machida, Y; Onishi, H; Yamamoto, K, 2006
)
0.33
"Medicinal carbon (MC) tablets were prepared to obtain an oral dosage form that can be easily taken."( Evaluation of binders in the preparation of medicinal carbon tablets by wet granule compression.
Ito, A; Machida, Y; Onishi, H; Yamamoto, K, 2006
)
0.33
" Thus, granules and tablet are useful as a compact dosage form of MC; though the reduced adsorption capacity must be taken into account in order to expect efficacy equivalent to that of MC alone."( In vitro and in vivo evaluation of medicinal carbon granules and tablet on the adsorption of acetaminophen.
Ito, A; Machida, Y; Onishi, H; Yamamoto, K, 2007
)
0.34
"Most glucose meter comparisons to date have focused on performance specifications likely to impact subcutaneous dosing of insulin."( Evaluation of the impact of hematocrit and other interference on the accuracy of hospital-based glucose meters.
Bryant, SC; Dubois, JA; Griesmann, L; Karon, BS; Presti, S; Santrach, PJ; Scott, R; Shirey, TL, 2008
)
0.35
"A fast-disintegrating dosage form has been developed as a user-friendly formulation that disintegrates in the mouth immediately."( Formulation design of an oral, fast-disintegrating dosage form containing taste-masked particles of famotidine.
Itai, S; Kajiyama, A; Kawai, H; Mizumoto, T; Tamura, T, 2008
)
0.35
" Therefore, we recommend preparing the tablets with XYL or SOR as a binder using the wet granule compression method to produce a compact dosage form of MC."( Preparation and evaluation of medicinal carbon tablets with different saccharides as binders.
Ito, A; Machida, Y; Yamamoto, K, 2009
)
0.35
"The simpler FCM-based dosing regimen showed better efficacy and compliance, as well as a good safety profile, compared with the Ganzoni-calculated IS dose regimen."( FERGIcor, a randomized controlled trial on ferric carboxymaltose for iron deficiency anemia in inflammatory bowel disease.
Bokemeyer, B; Chopey, IV; Evstatiev, R; Gasche, C; Gutzwiller, FS; Iqbal, T; Khalif, IL; Marteau, P; Riopel, L; Stein, J, 2011
)
0.37
" The ICER of FCM compared with placebo was €4414 per QALY gained for the FAIR-HF dosing regimen."( Health economic assessment of ferric carboxymaltose in patients with iron deficiency and chronic heart failure based on the FAIR-HF trial: an analysis for the UK.
Anker, SD; Blank, PR; Braunhofer, PG; Gutzwiller, FS; Mori, C; Ponikowski, P; Schwenkglenks, M; Szucs, TD, 2012
)
0.38
" Ferric carboxymaltose has a comparable safety profile to iron sucrose but offers the advantage of a much higher iron dosage at a time reducing the need for repeated applications and increasing patients' comfort."( Intravenous iron treatment in pregnancy: comparison of high-dose ferric carboxymaltose vs. iron sucrose.
Christoph, P; De Tejada, BM; Irion, O; Schuller, C; Studer, H; Surbek, D, 2012
)
0.38
"Currently available intravenous (IV) iron agents vary in indication, dosing regimens and safety profiles."( Intravenous ferric carboxymaltose versus standard medical care in the treatment of iron deficiency anemia in patients with chronic kidney disease: a randomized, active-controlled, multi-center study.
Bernardo, MV; Bregman, DB; Butcher, A; Charytan, C; Koch, TA; Morris, D, 2013
)
0.39
" Costs per 200/500/1,000 mg total dosage treatment cycle were CHF 101/210/420 for ferric carboxymaltose and CHF 144/375/721 for iron sucrose."( Budget impact of parenteral iron treatment of iron deficiency: methodological issues raised by using real-life data.
Braunhofer, P; Brock, E; Schneider, H; Troxler, J, 2014
)
0.4
"Rigorous data are sparse concerning the optimal route of administration and dosing strategy for iron therapy with or without concomitant erythropoiesis-stimulating agent (ESA) therapy for the management of iron deficiency anaemia in patients with non-dialysis dependent chronic kidney disease (ND-CKD)."( The FIND-CKD study--a randomized controlled trial of intravenous iron versus oral iron in non-dialysis chronic kidney disease patients: background and rationale.
Bock, A; Carrera, F; Cushway, T; Eckardt, KU; Gaillard, C; Macdougall, IC; Roger, SD; Roubert, B; Van Wyck, D, 2014
)
0.4
"FIND-CKD was a 56-week, open-label, multicentre, prospective, randomized three-arm study (NCT00994318) of 626 patients with ND-CKD and iron deficiency anaemia randomized to (i) intravenous (IV) ferric carboxymaltose (FCM) at an initial dose of 1000 mg iron with subsequent dosing as necessary to target a serum ferritin level of 400-600 µg/L (ii) IV FCM at an initial dose of 200 mg with subsequent dosing as necessary to target serum ferritin 100-200 µg/L or (iii) oral ferrous sulphate 200 mg iron/day."( The FIND-CKD study--a randomized controlled trial of intravenous iron versus oral iron in non-dialysis chronic kidney disease patients: background and rationale.
Bock, A; Carrera, F; Cushway, T; Eckardt, KU; Gaillard, C; Macdougall, IC; Roger, SD; Roubert, B; Van Wyck, D, 2014
)
0.4
" The subjects consumed six different mixtures of dextrose, maltitol and scFOS added in a chocolate dairy dessert at a dosage of 35 g."( Digestive tolerance and postprandial glycaemic and insulinaemic responses after consumption of dairy desserts containing maltitol and fructo-oligosaccharides in adults.
Cazaubiel, M; Chauveau, P; Gendre, D; Hilpipre, C; Maudet, C; Respondek, F; Wagner, A, 2014
)
0.4
" Further ratio and dose-response research should determine if meaningful performance benefits of composites accrue with ingestion <1."( Fructose-Glucose Composite Carbohydrates and Endurance Performance: Critical Review and Future Perspectives.
Bailey, D; Brown, F; Houltham, S; Musa-Veloso, K; Paulionis, L; Rowlands, DS, 2015
)
0.42
" Hb levels remained stable throughout the study, despite a significant reduction of ESA dosage (from 3426 g/week at baseline to 1116 and 1710 g/week, after 4 and 24 weeks, respectively)."( [Clinical experience with ferric carboxymaltose in non-dialysis chronic kidney disease].
Conte, G; De Nicola, L; Garofalo, C; Liberti, ME; Minutolo, R; Pacilio, M; Provenzano, M; Sagliocca, A; Sagliocchi, A; Santangelo, S; Savino, M; Scarpati, L; Sguazzo, A,
)
0.13
" Studies were heterogeneous in the number of patients randomised, iron deficiency-related conditions addressed, trial inclusion criteria, time horizon, treatment dosage and outcomes assessed."( Efficacy and Safety of Ferric Carboxymaltose and Other Formulations in Iron-Deficient Patients: A Systematic Review and Network Meta-analysis of Randomised Controlled Trials.
Marmifero, M; Meregaglia, M; Rognoni, C; Tarricone, R; Venturini, S, 2016
)
0.43
" IV iron can be given as large intermittent doses (loading therapy) or in smaller doses at frequent intervals (maintenance dosing regimen)."( Iron Treatment Strategies in Dialysis-Dependent CKD.
Coyne, DW; Daloul, R; Pandey, R, 2016
)
0.43
" Iron deficiency was modeled using dosing tables and retreatments were modeled based on a pooled retrospective analysis."( Intravenous iron treatments for iron deficiency anemia in inflammatory bowel disease: a budget impact analysis of iron isomaltoside 1000 (Monofer) in the UK.
Muduma, G; Pollock, RF, 2017
)
0.46
" In this study, the extraction condition of β-amylase from brewer's malt and the optimal dosage of β-amylase in maltose syrup production were optimized using response surface methodology and uniform design method."( Process optimization of the extraction condition of β-amylase from brewer's malt and its application in the maltose syrup production.
Li, Q; Li, Y; Liu, C; Niu, C; Zheng, F, 2018
)
0.48
" Moreover, the cytotoxicity results against L929 fibroblast cell line revealed that p(ML) based particle are biocompatible up to 100 μg/mL with 85% cell viability regardless of their nature, and at 200 μg/mL dosage of p(ML), m-p(ML)/TA and m-p(ML)/DETA particles, the cell viabilities were determined as 83."( One step preparation of polymeric maltitol particles, from a sugar molecule, maltitol for biomedical applications.
Sahiner, N, 2018
)
0.48
" Iron deficits were modeled using dosing tables and a joint distribution of bodyweight [mean 75."( An Economic Evaluation of Iron Isomaltoside 1000 Versus Ferric Carboxymaltose in Patients with Inflammatory Bowel Disease and Iron Deficiency Anemia in Denmark.
Muduma, G; Pollock, RF, 2018
)
0.48
" The convenient dosing with lesser number of total doses to complete the treatment will lead to better compliance in community setting."( Comparison of ferric Carboxymaltose and iron sucrose complex for treatment of iron deficiency anemia in pregnancy- randomised controlled trial.
Bhatla, N; Jose, A; Kalaivani, M; Kriplani, A; Mahey, R; Saxena, R; Sharma, JB, 2019
)
0.51
"Ferritin and TSAT were serially determined over four weeks after the administration of ferric carboxymaltose (FCM) in hemodialysis patients on a stable maintenance FCM dosing regimen of 100 mg or 200 mg every four weeks."( Evaluation of iron stores in hemodialysis patients on maintenance ferric Carboxymaltose dosing.
Diebold, M; Kistler, AD, 2019
)
0.51
" Temporal coordination of blood sampling for iron status evaluation with the maintenance IV iron dosing schedule is advisable."( Evaluation of iron stores in hemodialysis patients on maintenance ferric Carboxymaltose dosing.
Diebold, M; Kistler, AD, 2019
)
0.51
" Several IV iron formulations are available with different dosing characteristics affecting infusion speed and maximum dose."( Development of a Resource Impact Model for Clinics Treating Pre-Operative Iron Deficiency Anemia in Ireland.
Loughnane, F; Muduma, G; Pollock, RF, 2020
)
0.56
" The tool modeled clinic throughput based on their different dosing characteristics in a specific IDA population, capturing fixed overheads, variable costs, clinic income from private and publicly-funded patients, and savings associated with IV iron."( Development of a Resource Impact Model for Clinics Treating Pre-Operative Iron Deficiency Anemia in Ireland.
Loughnane, F; Muduma, G; Pollock, RF, 2020
)
0.56
" While FCM is reported to induce hypophosphatemia, the frequency of hypophosphatemia after an equivalent dosage of FDI had not been assessed prospectively."( Hypophosphatemia after high-dose iron repletion with ferric carboxymaltose and ferric derisomaltose-the randomized controlled HOMe aFers study.
Böhm, M; Brandenburg, VM; D'Amelio, R; Emrich, IE; Fliser, D; Heine, GH; Kaddu-Mulindwa, D; Lizzi, F; Seiler-Mussler, S; Siegel, JD; Ukena, C; Wagenpfeil, S, 2020
)
0.56
" Before hospital discharge, participants were randomly assigned (1:1) to receive intravenous ferric carboxymaltose or placebo for up to 24 weeks, dosed according to the extent of iron deficiency."( Ferric carboxymaltose for iron deficiency at discharge after acute heart failure: a multicentre, double-blind, randomised, controlled trial.
Anker, SD; Butler, J; Cohen-Solal, A; Comin-Colet, J; Danchin, N; Dargie, HJ; Doehner, W; Dorobantu, M; Drozdz, J; Fabien, V; Filippatos, G; Friede, T; Göhring, UM; Jankowska, EA; Jensen, KH; Keren, A; Khintibidze, I; Kirwan, BA; Kragten, H; Lewis, BS; Martinez, FA; McDonagh, T; Metra, M; Milicic, D; Motro, M; Nicolau, JC; Ohlsson, M; Parkhomenko, A; Pascual-Figal, DA; Pocock, S; Ponikowski, P; Ruschitzka, F; Sim, D; Skouri, H; van der Meer, P; von Haehling, S, 2020
)
0.56
" The results obtained from the dose-response experiments show that 8 at a concentration of 1000 µM reduced the enzyme activity of Sco GlgE1-V279S by 65%."( Stereoselective synthesis of a 4-⍺-glucoside of valienamine and its X-ray structure in complex with Streptomyces coelicolor GlgE1-V279S.
Jayasinghe, TD; Kapil, S; Ronning, DR; Si, A; Sucheck, SJ; Thanvi, R, 2021
)
0.62
" Erythropoiesis-stimulating agent dosing did not differ between groups."( Comparison of Iron Dosing Strategies in Patients Undergoing Long-Term Hemodialysis: A Randomized Controlled Trial.
Bielesz, B; Gabriel, M; Gleiss, A; Hörl, WH; Lorenz, M; Monteforte, R; Prikoszovich, T; Sunder-Plassmann, G; Wolzt, M, 2021
)
0.62
" Appropriate patient selection and patient-adjusted dosage selection facilitated safe and effective administration of high-dose (≥1000 mg) FDI."( Ferric derisomaltose for the treatment of iron deficiency anemia with postpartum hemorrhage: Results of a single-arm, open-label, phase 3 study in Japan.
Ito, N; Kishimoto, U; Ohtani, Y; Sugimura, M; Tamai, S, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
beta-adrenergic antagonistAn agent that binds to but does not activate beta-adrenergic receptors thereby blocking the actions of endogenous or exogenous beta-adrenergic agonists. beta-Adrenergic antagonists are used for treatment of hypertension, cardiac arrhythmias, angina pectoris, glaucoma, migraine headaches and anxiety.
anti-arrhythmia drugA drug used for the treatment or prevention of cardiac arrhythmias. Anti-arrhythmia drugs may affect the polarisation-repolarisation phase of the action potential, its excitability or refractoriness, or impulse conduction or membrane responsiveness within cardiac fibres.
antihypertensive agentAny drug used in the treatment of acute or chronic vascular hypertension regardless of pharmacological mechanism.
sympathomimetic agentA drug that mimics the effects of stimulating postganglionic adrenergic sympathetic nerves. Included in this class are drugs that directly stimulate adrenergic receptors and drugs that act indirectly by provoking the release of adrenergic transmitters.
[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 (7)

ClassDescription
ethanolamines
propanolamine
secondary amino compoundA compound formally derived from ammonia by replacing two hydrogen atoms by organyl groups.
etherAn organooxygen compound with formula ROR, where R is not hydrogen.
monocarboxylic acid amideA carboxamide derived from a monocarboxylic acid.
aromatic amideAn amide in which the amide linkage is bonded directly to an aromatic system.
alpha-D-glucosyl-(1->4)-D-mannopyranose
[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 (11)

PathwayProteinsCompounds
Acebutolol Action Pathway478
Starch and Sucrose Metabolism1626
Glycogen Synthetase Deficiency1626
Glycogenosis, Type III. Cori Disease, Debrancher Glycogenosis1626
Glycogenosis, Type IV. Amylopectinosis, Anderson Disease1626
Glycogenosis, Type VI. Hers Disease1626
Mucopolysaccharidosis VII. Sly Syndrome1626
Sucrase-Isomaltase Deficiency1626
AtMetExpress overview0109
Glucose sensing and signaling010
Biochemical pathways: part I0466

Protein Targets (5)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Solute carrier family 22 member 1 Homo sapiens (human)Ki95.80000.55004.26507.4600AID681146
Beta-1 adrenergic receptorHomo sapiens (human)IC50 (µMol)0.73100.00021.46819.0000AID625204
Beta-1 adrenergic receptorHomo sapiens (human)Ki0.42200.00011.33919.9840AID625204
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki10.00000.00010.739610.0000AID4411
[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)
Beta-2 adrenergic receptorHomo sapiens (human)Kd13.36130.00000.62888.9130AID1798580
Beta-1 adrenergic receptorHomo sapiens (human)Kd13.36130.00010.803910.0000AID1798580
Beta-3 adrenergic receptorHomo sapiens (human)Kd13.36130.00010.76318.9130AID1798580
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (71)

Processvia Protein(s)Taxonomy
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)
diet induced thermogenesisBeta-2 adrenergic receptorHomo sapiens (human)
regulation of sodium ion transportBeta-2 adrenergic receptorHomo sapiens (human)
transcription by RNA polymerase IIBeta-2 adrenergic receptorHomo sapiens (human)
receptor-mediated endocytosisBeta-2 adrenergic receptorHomo sapiens (human)
smooth muscle contractionBeta-2 adrenergic receptorHomo sapiens (human)
cell surface receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
activation of transmembrane receptor protein tyrosine kinase activityBeta-2 adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
endosome to lysosome transportBeta-2 adrenergic receptorHomo sapiens (human)
response to coldBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of protein kinase A signalingBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of bone mineralizationBeta-2 adrenergic receptorHomo sapiens (human)
heat generationBeta-2 adrenergic receptorHomo sapiens (human)
negative regulation of multicellular organism growthBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeBeta-2 adrenergic receptorHomo sapiens (human)
bone resorptionBeta-2 adrenergic receptorHomo sapiens (human)
negative regulation of G protein-coupled receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIBeta-2 adrenergic receptorHomo sapiens (human)
negative regulation of smooth muscle contractionBeta-2 adrenergic receptorHomo sapiens (human)
brown fat cell differentiationBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of mini excitatory postsynaptic potentialBeta-2 adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of protein serine/threonine kinase activityBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of cold-induced thermogenesisBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of autophagosome maturationBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of lipophagyBeta-2 adrenergic receptorHomo sapiens (human)
cellular response to amyloid-betaBeta-2 adrenergic receptorHomo sapiens (human)
response to psychosocial stressBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of cAMP-dependent protein kinase activityBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of AMPA receptor activityBeta-2 adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressureBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of heart rate by epinephrine-norepinephrineBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrineBeta-1 adrenergic receptorHomo sapiens (human)
diet induced thermogenesisBeta-1 adrenergic receptorHomo sapiens (human)
response to coldBeta-1 adrenergic receptorHomo sapiens (human)
heat generationBeta-1 adrenergic receptorHomo sapiens (human)
negative regulation of multicellular organism growthBeta-1 adrenergic receptorHomo sapiens (human)
fear responseBeta-1 adrenergic receptorHomo sapiens (human)
regulation of circadian sleep/wake cycle, sleepBeta-1 adrenergic receptorHomo sapiens (human)
brown fat cell differentiationBeta-1 adrenergic receptorHomo sapiens (human)
regulation of postsynaptic membrane potentialBeta-1 adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of cold-induced thermogenesisBeta-1 adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressureBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeBeta-1 adrenergic receptorHomo sapiens (human)
receptor-mediated endocytosisBeta-3 adrenergic receptorHomo sapiens (human)
negative regulation of G protein-coupled receptor signaling pathwayBeta-3 adrenergic receptorHomo sapiens (human)
diet induced thermogenesisBeta-3 adrenergic receptorHomo sapiens (human)
carbohydrate metabolic processBeta-3 adrenergic receptorHomo sapiens (human)
generation of precursor metabolites and energyBeta-3 adrenergic receptorHomo sapiens (human)
energy reserve metabolic processBeta-3 adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerBeta-3 adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayBeta-3 adrenergic receptorHomo sapiens (human)
response to coldBeta-3 adrenergic receptorHomo sapiens (human)
heat generationBeta-3 adrenergic receptorHomo sapiens (human)
negative regulation of multicellular organism growthBeta-3 adrenergic receptorHomo sapiens (human)
eating behaviorBeta-3 adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeBeta-3 adrenergic receptorHomo sapiens (human)
brown fat cell differentiationBeta-3 adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayBeta-3 adrenergic receptorHomo sapiens (human)
positive regulation of cold-induced thermogenesisBeta-3 adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressureBeta-3 adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (35)

Processvia Protein(s)Taxonomy
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)
amyloid-beta bindingBeta-2 adrenergic receptorHomo sapiens (human)
beta2-adrenergic receptor activityBeta-2 adrenergic receptorHomo sapiens (human)
protein bindingBeta-2 adrenergic receptorHomo sapiens (human)
adenylate cyclase bindingBeta-2 adrenergic receptorHomo sapiens (human)
potassium channel regulator activityBeta-2 adrenergic receptorHomo sapiens (human)
identical protein bindingBeta-2 adrenergic receptorHomo sapiens (human)
protein homodimerization activityBeta-2 adrenergic receptorHomo sapiens (human)
protein-containing complex bindingBeta-2 adrenergic receptorHomo sapiens (human)
norepinephrine bindingBeta-2 adrenergic receptorHomo sapiens (human)
beta-adrenergic receptor activityBeta-1 adrenergic receptorHomo sapiens (human)
beta1-adrenergic receptor activityBeta-1 adrenergic receptorHomo sapiens (human)
protein bindingBeta-1 adrenergic receptorHomo sapiens (human)
PDZ domain bindingBeta-1 adrenergic receptorHomo sapiens (human)
alpha-2A adrenergic receptor bindingBeta-1 adrenergic receptorHomo sapiens (human)
protein heterodimerization activityBeta-1 adrenergic receptorHomo sapiens (human)
G protein-coupled neurotransmitter receptor activity involved in regulation of postsynaptic membrane potentialBeta-1 adrenergic receptorHomo sapiens (human)
norepinephrine bindingBeta-3 adrenergic receptorHomo sapiens (human)
beta-adrenergic receptor activityBeta-3 adrenergic receptorHomo sapiens (human)
protein bindingBeta-3 adrenergic receptorHomo sapiens (human)
beta3-adrenergic receptor activityBeta-3 adrenergic receptorHomo sapiens (human)
beta-3 adrenergic receptor bindingBeta-3 adrenergic receptorHomo sapiens (human)
protein homodimerization activityBeta-3 adrenergic receptorHomo sapiens (human)
epinephrine bindingBeta-3 adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (17)

Processvia Protein(s)Taxonomy
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)
nucleusBeta-2 adrenergic receptorHomo sapiens (human)
lysosomeBeta-2 adrenergic receptorHomo sapiens (human)
endosomeBeta-2 adrenergic receptorHomo sapiens (human)
early endosomeBeta-2 adrenergic receptorHomo sapiens (human)
Golgi apparatusBeta-2 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-2 adrenergic receptorHomo sapiens (human)
endosome membraneBeta-2 adrenergic receptorHomo sapiens (human)
membraneBeta-2 adrenergic receptorHomo sapiens (human)
apical plasma membraneBeta-2 adrenergic receptorHomo sapiens (human)
clathrin-coated endocytic vesicle membraneBeta-2 adrenergic receptorHomo sapiens (human)
neuronal dense core vesicleBeta-2 adrenergic receptorHomo sapiens (human)
receptor complexBeta-2 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-2 adrenergic receptorHomo sapiens (human)
early endosomeBeta-1 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-1 adrenergic receptorHomo sapiens (human)
Schaffer collateral - CA1 synapseBeta-1 adrenergic receptorHomo sapiens (human)
neuronal dense core vesicleBeta-1 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-1 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-3 adrenergic receptorHomo sapiens (human)
receptor complexBeta-3 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-3 adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (151)

Assay IDTitleYearJournalArticle
AID679253TP_TRANSPORTER: transepithelial transport (basal to apical) in Caco-2 cells1996The Journal of pharmacy and pharmacology, Oct, Volume: 48, Issue:10
Active secretion of drugs from the small intestinal epithelium in rats by P-glycoprotein functioning as an absorption barrier.
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.
AID1091958Hydrophobicity, log P of the compound in octanol-water by shaking-flask method2011Journal of agricultural and food chemistry, Apr-13, Volume: 59, Issue:7
Importance of physicochemical properties for the design of new pesticides.
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.
AID679101TP_TRANSPORTER: transepithelial transport of Acebutolol at a concentration of 20 uM in MDR1-expressing MDCK cells2003Pharmaceutical research, Aug, Volume: 20, Issue:8
Novel experimental parameters to quantify the modulation of absorptive and secretory transport of compounds by P-glycoprotein in cell culture models of intestinal epithelium.
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.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID40539Selectivity for beta-1 receptor1988Journal of medicinal chemistry, Nov, Volume: 31, Issue:11
Modeling of beta-adrenoceptors based on molecular electrostatic potential studies of agonists and antagonists.
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).
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.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID4411Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
Binding of arylpiperazines, (aryloxy)propanolamines, and tetrahydropyridylindoles to the 5-HT1A receptor: contribution of the molecular lipophilicity potential to three-dimensional quantitative structure-affinity relationship models.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID350218Octanol-water partition coefficient, log PC of the compound2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
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).
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
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.
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.
AID288185Permeability coefficient through artificial membrane in presence of stirred water layer2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
QSAR study on permeability of hydrophobic compounds with artificial membranes.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
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.
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
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.
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.
AID288192Partition coefficient, log P of the compound2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
QSAR study on permeability of hydrophobic compounds with artificial membranes.
AID1091955Dissociation constant, pKa of the compound at pH 7.32011Journal of agricultural and food chemistry, Apr-13, Volume: 59, Issue:7
Importance of physicochemical properties for the design of new pesticides.
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.
AID288184Permeability coefficient through artificial membrane in presence of unstirred water layer by PAMPA2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
QSAR study on permeability of hydrophobic compounds with artificial membranes.
AID237416Distribution coeeficient for the compound at pH7.4 (Log D7.4) 2004Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
Contribution of ionization and lipophilicity to drug binding to albumin: a preliminary step toward biodistribution prediction.
AID19006Calculated membrane partition coefficient (Kmemb)2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
Surface activity profiling of drugs applied to the prediction of blood-brain barrier permeability.
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.
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).
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.
AID515780Intrinsic solubility of the compound in water2010Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
QSAR-based solubility model for drug-like compounds.
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.
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).
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID41891Tested for intrinsic sympathomimetic activity (ISA); antagonist with partial agonistic properties1988Journal of medicinal chemistry, Nov, Volume: 31, Issue:11
Modeling of beta-adrenoceptors based on molecular electrostatic potential studies of agonists and 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.
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]
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.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
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.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID350219Lipophilicity, log K at pH 2 by by hydrophilic interaction chromatography using 95% acetonitrile as mobile phase2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
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.
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.
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.
AID312896Partition coefficient, log P by UPLC method2008Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
High-throughput log P determination by ultraperformance liquid chromatography: a convenient tool for medicinal chemists.
AID1147035In vivo beta-2 adrenergic receptor blocking activity in iv dosed cat assessed as half dose required for desensitizing isoproterenol-induced diastolic hypotensive response after 3.5 mins1976Journal of medicinal chemistry, Mar, Volume: 19, Issue:3
A new series of cardioselective adrenergic beta-receptor blocking compounds. 1-(2-Acyl-4-acylaminophenoxy)-3-isopropylaminopropan-2-ols.
AID312895Partition coefficient, log P of the compound2008Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
High-throughput log P determination by ultraperformance liquid chromatography: a convenient tool for medicinal chemists.
AID781328pKa (acid-base dissociation constant) as determined by Luan ref: Pharm. Res. 20052014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID350220Lipophilicity, log K at pH 2 by by hydrophilic interaction chromatography using 100% water as mobile phase2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
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.
AID679102TP_TRANSPORTER: transepithelial transport of Acebutolol at a concentration of 20 uM in Caco-2 cells2003Pharmaceutical research, Aug, Volume: 20, Issue:8
Novel experimental parameters to quantify the modulation of absorptive and secretory transport of compounds by P-glycoprotein in cell culture models of intestinal epithelium.
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.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
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.
AID237474Percentage of drug bound in bovine plasma albumin2004Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
Contribution of ionization and lipophilicity to drug binding to albumin: a preliminary step toward biodistribution prediction.
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.
AID1091956Apparent hydrophobicity, log D of the compound in Octanol-buffer2011Journal of agricultural and food chemistry, Apr-13, Volume: 59, Issue:7
Importance of physicochemical properties for the design of new pesticides.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
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.
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.
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.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
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.
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.
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).
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).
AID567091Drug absorption in human assessed as human intestinal absorption rate2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Prediction of drug intestinal absorption by new linear and non-linear QSPR.
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.
AID29812Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
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.
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.
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.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
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.
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.
AID781326pKa (acid-base dissociation constant) as determined by Avdeef ref: DOI: 10.1002/047145026X2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID350216Dissociation constant, pKa of the compound2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
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).
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.
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.
AID27167Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
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.
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.
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.
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.
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).
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.
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.
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.
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.
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.
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.
AID28681Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID395328Lipophilicity, log P of the compound2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
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.
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.
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.
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.
AID603954In-vivo blood/plasma to lung partition coefficients of the compound, logP(lung) in rat2008European journal of medicinal chemistry, Mar, Volume: 43, Issue:3
Air to lung partition coefficients for volatile organic compounds and blood to lung partition coefficients for volatile organic compounds and drugs.
AID1750325Protein binding in human plasma assessed as bound fraction by HPLC-MS/MS analysis2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
From Celecoxib to a Novel Class of Phosphodiesterase 5 Inhibitors: Trisubstituted Pyrazolines as Novel Phosphodiesterase 5 Inhibitors with Extremely High Potency and Phosphodiesterase Isozyme Selectivity.
AID1147037Antiarrhythmic activity in iv dosed dog assessed as dose required for reversal of ouabain-induced cardiac arrhythmia1976Journal of medicinal chemistry, Mar, Volume: 19, Issue:3
A new series of cardioselective adrenergic beta-receptor blocking compounds. 1-(2-Acyl-4-acylaminophenoxy)-3-isopropylaminopropan-2-ols.
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).
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).
AID41489Selectivity towards beta-2 adrenergic receptor;Not selective towards beta-2 adrenergic receptor1988Journal of medicinal chemistry, Nov, Volume: 31, Issue:11
Modeling of beta-adrenoceptors based on molecular electrostatic potential studies of agonists and antagonists.
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).
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.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
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.
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.
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
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.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
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.
AID1147034In vivo beta-1 adrenergic receptor blocking activity in iv dosed cat assessed as half dose required for desensitizing isoproterenol-induced tachycardia after 3.5 mins1976Journal of medicinal chemistry, Mar, Volume: 19, Issue:3
A new series of cardioselective adrenergic beta-receptor blocking compounds. 1-(2-Acyl-4-acylaminophenoxy)-3-isopropylaminopropan-2-ols.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID239884pKa value of the compound2004Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
Contribution of ionization and lipophilicity to drug binding to albumin: a preliminary step toward biodistribution prediction.
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]
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.
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.
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.
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.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
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.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
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.
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.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
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).
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).
AID679124TP_TRANSPORTER: uptake in K562 and K562/ADR cell1996The Journal of pharmacy and pharmacology, Oct, Volume: 48, Issue:10
Active secretion of drugs from the small intestinal epithelium in rats by P-glycoprotein functioning as an absorption barrier.
AID395325Lipophilicity, log P by microemulsion electrokinetic chromatography2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID1147036Ratio of in vivo beta-2 adrenergic receptor blocking activity in iv dosed cat assessed as half dose required for desensitizing isoproterenol-induced diastolic hypotensive response to in vivo beta-1 adrenergic receptor blocking activity in iv dosed cat ass1976Journal of medicinal chemistry, Mar, Volume: 19, Issue:3
A new series of cardioselective adrenergic beta-receptor blocking compounds. 1-(2-Acyl-4-acylaminophenoxy)-3-isopropylaminopropan-2-ols.
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).
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]
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).
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.
AID350217Octanol-water partition coefficient, log P of the cationic form of the compound2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
AID1890430Plasma protein binding in human by LC-MS/MS analysis2022European journal of medicinal chemistry, Apr-05, Volume: 233Design, synthesis, and behavioral evaluation of dual-acting compounds as phosphodiesterase type 10A (PDE10A) inhibitors and serotonin ligands targeting neuropsychiatric symptoms in dementia.
AID1091957Apparent permeability of the compound by PAMPA2011Journal of agricultural and food chemistry, Apr-13, Volume: 59, Issue:7
Importance of physicochemical properties for the design of new pesticides.
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.
AID17985803H-CGP 12177 Whole Cell Binding Assay from Article 10.1038/sj.bjp.0706048: \\The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.\\2005British journal of pharmacology, Feb, Volume: 144, Issue:3
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5,606)

TimeframeStudies, This Drug (%)All Drugs %
pre-19902406 (42.92)18.7374
1990's830 (14.81)18.2507
2000's926 (16.52)29.6817
2010's1075 (19.18)24.3611
2020's369 (6.58)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 67.31

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 Index67.31 (24.57)
Research Supply Index7.06 (2.92)
Research Growth Index4.26 (4.65)
Search Engine Demand Index118.96 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (67.31)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials266 (29.59%)5.53%
Trials197 (3.97%)5.53%
Reviews37 (4.12%)6.00%
Reviews164 (3.31%)6.00%
Case Studies59 (6.56%)4.05%
Case Studies68 (1.37%)4.05%
Observational0 (0.00%)0.25%
Observational29 (0.58%)0.25%
Other537 (59.73%)84.16%
Other4,504 (90.77%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (6)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
N-of-1 Trials for Deprescribing Beta-blockers in HFpEF [NCT04767061]Phase 49 participants (Actual)Interventional2021-04-01Completed
Association Between Angiotensin Converting Enzyme Inhibitor or Angiotensin Receptor Blocker Use and COVID-19 Severity and Mortality Among US Veterans [NCT04467931]22,213 participants (Actual)Observational2020-01-19Completed
N-of-1 Trials for Deprescribing Beta-blockers in HFpEF [NCT04757584]Phase 49 participants (Actual)Interventional2021-04-01Completed
[NCT00000522]Phase 20 participants Interventional1985-08-31Completed
An Open-label, Single-dose, Two-treatment, Randomized, Cross-over Study to Investigate the Effects of the SLCO2B1 c.1457C>T Polymorphism and Apple Juice on the Pharmacokinetics and Pharmacodynamics of Acebutolol in Healthy Korean and Japanese Volunteers [NCT01514019]Phase 416 participants (Actual)Interventional2012-01-31Completed
Efficacy and Safety of Propranolol Versus Acebutolol on the Proliferative Phase of Infantile Hemangioma [NCT01743885]Phase 355 participants (Actual)Interventional2012-11-30Terminated
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT04767061 (10) [back to overview]Change in Exercise Capacity When on Beta-blocker Versus When Off Beta-blocker, as Measured by Peak Oxygen Consumption (VO2) During Cardiopulmonary Exercise Test (CPET)
NCT04767061 (10) [back to overview]Change in Lower Extremity Function When on Beta-blocker Versus When Off Beta-blocker, as Measured by the Balance Portion of a Modified Version of the Short Physical Performance Battery.
NCT04767061 (10) [back to overview]Change in Lower Extremity Function When on Beta-blocker Versus When Off Beta-blocker, as Measured by the Chair Rise Portion of a Modified Version of the Short Physical Performance Battery.
NCT04767061 (10) [back to overview]Change in Lower Extremity Function When on Beta-blocker Versus When Off Beta-blocker, as Measured by the Gait Speed Portion of a Modified Version of the Short Physical Performance Battery.
NCT04767061 (10) [back to overview]Change in Patient-reported Cognitive Function When on Beta-blocker Versus When Off Beta-blocker, as Measured by Patient-Reported Outcome Measurement Information System-Short Form 6a (PROMIS SF-6a)
NCT04767061 (10) [back to overview]Change in Patient-reported Health Status When on Beta-blocker Versus When Off Beta-blocker, as Measured by Kansas City Cardiomyopathy Questionnaire (KCCQ-12)
NCT04767061 (10) [back to overview]Change in Patient-reported Health When on Beta-blocker Versus When Off Beta-blocker, as Measured by the EuroQol-5D Visual Analogue System (EQ-5D VAS)
NCT04767061 (10) [back to overview]Change in Patient-reported Sexual Function When on Beta-blocker Versus When Off Beta-blocker, as Measured by Patient-Reported Outcome Measurement Information System-Sexual Function (PROMIS-Sexual Function)
NCT04767061 (10) [back to overview]Change in Physical Activity When on Beta-blocker Versus When Off Beta-blocker, as Measured by Step Count on Wearable Activity Monitoring Device
NCT04767061 (10) [back to overview]Change in Patient-reported Quality of Life When on Beta-blocker Versus When Off Beta-blocker, as Measured by Patient-Reported Outcome Measurement Information System-29 (PROMIS-29)

Change in Exercise Capacity When on Beta-blocker Versus When Off Beta-blocker, as Measured by Peak Oxygen Consumption (VO2) During Cardiopulmonary Exercise Test (CPET)

"Cardiopulmonary exercise testing (CPET) measures breath-by-breath oxygen production during symptom-limited exercise on a stationary bike. This permits the calculation of peak oxygen consumption (VO2). Percent predicted peak VO2 for body weight will also be calculated. Due to the nature of N-of-1 trials, the duration of a subject's period varies based on the subject's home dose of beta-blocker prior to enrollment, therefore, each subject's respective time period for the OFF and ON periods could range between 3 - 6 weeks. The outcome measure data is the mean of the data collected during the span of the outcome measure time frame." (NCT04767061)
Timeframe: The maximum amount of time a subject could have been assessed for this outcome measure is 6-weeks. This outcome was measured at the end of the first and second visit.

Interventionml/kg/min (Mean)
ON Beta Blockers10.0
OFF Beta Blockers11.4

[back to top]

Change in Lower Extremity Function When on Beta-blocker Versus When Off Beta-blocker, as Measured by the Balance Portion of a Modified Version of the Short Physical Performance Battery.

"The Short Physical Performance Battery assesses gait speed, core strength when rising from a chair without using the upper extremities, and balance while standing without a cane or walker. The balance test portion of the SPPB assesses the subject's ability to stand unassisted without the use of a cane or walker. Balance test scores range from 0 - 4 with higher scores indicating better ability to stand unassisted. Our research team conducted the balance test according to SPPB standards. Due to the nature of N-of-1 trials, the duration of a subject's period varies based on the subject's home dose of beta-blocker prior to enrollment, therefore, each subject's respective time period for the OFF and ON periods could range between 3 - 6 weeks. The outcome measure data is the mean of the data collected during the span of the outcome measure time frame." (NCT04767061)
Timeframe: The maximum amount of time a subject could have been assessed for this outcome measure is 24-weeks. This outcome was measured at baseline and at each end of period visit.

Interventionscore on a scale (Mean)
ON Beta Blockers3.9
OFF Beta Blockers3.6

[back to top]

Change in Lower Extremity Function When on Beta-blocker Versus When Off Beta-blocker, as Measured by the Chair Rise Portion of a Modified Version of the Short Physical Performance Battery.

"The Short Physical Performance Battery assesses gait speed, core strength when rising from a chair without using the upper extremities, and balance while standing without a cane or walker. The chair rise portion of the SPPB assesses core strength. When comparing the number of seconds it takes to complete 5 chair rises, quicker speeds indicate better core strength. Our research team has chosen on comparing the speed at which subjects were able to complete the test. Due to the nature of N-of-1 trials, the duration of a subject's period varies based on the subject's home dose of beta-blocker prior to enrollment, therefore, each subject's respective time period for the OFF and ON periods could range between 3 - 6 weeks. The outcome measure data is the mean of the data collected during the outcome measure time frame." (NCT04767061)
Timeframe: The maximum amount of time a subject could have been assessed for this outcome measure is 24-weeks. This outcome was measured at baseline and at each end of period visit.

Interventionseconds (Mean)
ON Beta Blockers16
OFF Beta Blockers15.1

[back to top]

Change in Lower Extremity Function When on Beta-blocker Versus When Off Beta-blocker, as Measured by the Gait Speed Portion of a Modified Version of the Short Physical Performance Battery.

"The Short Physical Performance Battery assesses gait speed, core strength when rising from a chair without using the upper extremities, and balance while standing without a cane or walker. The gait speed portion of the SPPB assesses the subject's lower extremity function. When comparing the number of seconds it takes to complete the 4-meter gait speed test, quicker speeds indicate better lower extremity function. Our research team conducted the 4-meter gait speed test according to SPPB standards, but have chosen on comparing the speed at which subjects were able to complete the test. Due to the nature of N-of-1 trials, the duration of a subject's period varies based on the subject's home dose of beta-blocker prior to enrollment, therefore, each subject's respective time period for the OFF and ON periods could range between 3 - 6 weeks. The outcome measure data is the mean of the data collected during the span of the outcome measure time frame." (NCT04767061)
Timeframe: The maximum amount of time a subject could have been assessed for this outcome measure is 24-weeks. This outcome was measured at baseline and at each end of period visit.

Interventionseconds (Mean)
ON Beta Blockers4.3
OFF Beta Blockers4.6

[back to top]

Change in Patient-reported Cognitive Function When on Beta-blocker Versus When Off Beta-blocker, as Measured by Patient-Reported Outcome Measurement Information System-Short Form 6a (PROMIS SF-6a)

"Patient-Reported Outcome Measurement Information System-Short Form 6a (PROMIS SF-6a) is a survey of patient-perceived cognitive deficits. Questions are ranked on a 5-point Likert scale, with higher scores indicating better cognitive function. Scores are mapped so the values follow a normal distribution with a population mean T-score of 50 and an SD of 10. Instead of having a min or max, the raw scores have been transformed into t-scores for comparison to a reference population (the US general population) with a mean of 50 and SD of 10. Scores lower than 50 indicate worse cognitive function compared to the US general population. Due to the nature of N-of-1 trials, the duration of a subject's period varies based on the subject's home dose of beta-blocker prior to enrollment, therefore, each subject's respective time period for the OFF and ON periods could range between 3-6 weeks. The outcome measure data is the mean of the data collected during the span of the measured time points." (NCT04767061)
Timeframe: The maximum amount of time a subject could have been assessed for this measure is 76-weeks (24-week max intervention phase,1-year follow-up phase). This outcome was measured at baseline, weekly, end of period and intervention visits, and during follow-up.

Interventionscore on a scale (Mean)
ON Beta Blockers53.8
OFF Beta Blockers52.4

[back to top]

Change in Patient-reported Health Status When on Beta-blocker Versus When Off Beta-blocker, as Measured by Kansas City Cardiomyopathy Questionnaire (KCCQ-12)

"The Kansas City Cardiomyopathy Questionnaire (KCCQ-12) is a heart failure-specific health status survey. Questions are ranked on 5- to 7-point Likert scales, with higher scores indicating better health status. KCCQ scores are scaled from 0 to 100 and frequently summarized in 25-point ranges, where scores represent health status as follows: 0 to 24: very poor to poor; 25 to 49: poor to fair; 50 to 74: fair to good; and 75 to 100: good to excellent. Due to the nature of N-of-1 trials, the duration of a subject's period varies based on the subject's home dose of beta-blocker prior to enrollment, therefore, each subject's respective time period for the OFF and ON periods could range between 3 - 6 weeks. The outcome measure data is the mean of the data collected during the span of the outcome measure time frame." (NCT04767061)
Timeframe: The max amount of time a subject could have been assessed for this measure is 76-weeks (24-week max intervention phase,1-year follow-up phase). This outcome was measured at baseline, bi-weekly, end of period and intervention visits, and during follow-up.

Interventionscore on a scale (Mean)
ON Beta Blockers58.7
OFF Beta Blockers66.0

[back to top]

Change in Patient-reported Health When on Beta-blocker Versus When Off Beta-blocker, as Measured by the EuroQol-5D Visual Analogue System (EQ-5D VAS)

"The EuroQol-5D Visual Analogue System (EQ-5D VAS) indicates patient-perceived health on a vertical visual analogue scale. The scale ranges from 0, indicating poorest health, to 100, indicating the best health. Due to the nature of N-of-1 trials, the duration of a subject's period varies based on the subject's home dose of beta-blocker prior to enrollment, therefore, each subject's respective time period for the OFF and ON periods could range between 3 - 6 weeks. The outcome measure data is the mean of the data collected during the span of the outcome measure time frame." (NCT04767061)
Timeframe: The maximum amount of time a subject could have been assessed for this outcome measure is 24-weeks. This outcome was measured at baseline and at each end of period visit.

Interventionscore on a scale (Mean)
ON Beta Blockers68.9
OFF Beta Blockers67.8

[back to top]

Change in Patient-reported Sexual Function When on Beta-blocker Versus When Off Beta-blocker, as Measured by Patient-Reported Outcome Measurement Information System-Sexual Function (PROMIS-Sexual Function)

"Patient-Reported Outcome Measurement Information System-Sexual Function (PROMIS-Sexual Function) measures self-reported sexual function and satisfaction. Questions are ranked on a 6-point Likert scale, with higher scores indicating poorer sexual function and satisfaction. Due to the nature of N-of-1 trials, the duration of a subject's period varies based on the subject's home dose of beta-blocker prior to enrollment, therefore, each subject's respective time period for the OFF and ON periods could range between 3 - 6 weeks. The outcome measure data is the mean of the data collected during the span of the outcome measure time frame. The score ranges from 0-10 with higher scores meaning worsened sexual function." (NCT04767061)
Timeframe: The maximum amount of time a subject could have been assessed for this measure is 76-weeks (24-week max intervention phase,1-year follow-up phase). This outcome was measured at baseline, end of period and intervention visits, and during follow-up.

Interventionscore on a scale (Mean)
ON Beta Blockers1.8
OFF Beta Blockers2.1

[back to top]

Change in Physical Activity When on Beta-blocker Versus When Off Beta-blocker, as Measured by Step Count on Wearable Activity Monitoring Device

"The wearable activity monitoring device measures daily step count. Due to the nature of N-of-1 trials, the duration of a subject's periods varies based on the subject's home dose of beta-blocker prior to enrollment, therefore, each subject's respective time period for the OFF and ON periods could range between 3 and 6 weeks. We will compare average step counts over 2-week periods, which will be the final 2 weeks of each period when subjects are either on their home (ON Beta Blockers) or minimally tolerated (OFF Beta Blockers) dose. The outcome measure data is the mean collected during the outcome measure time frame." (NCT04767061)
Timeframe: The maximum amount of time a subject could have been assessed for this outcome measure is 8-weeks (last 2 weeks of each period for up to 4 periods).

InterventionCount of Steps (Mean)
ON Beta Blockers2790.5
OFF Beta Blockers3167.3

[back to top]

Change in Patient-reported Quality of Life When on Beta-blocker Versus When Off Beta-blocker, as Measured by Patient-Reported Outcome Measurement Information System-29 (PROMIS-29)

"The PROMIS-29 assesses 7 domains with 4 questions with an additional pain intensity numeric rating scale. The patients' answers to the PROMIS-29 are scored from 1-5 (except for the pain numeric rating scale). The sum of the PROMIS-29 is the raw score transformed into a final T-score metric. Scores are mapped so that the values follow a normal distribution with a population mean T-score of 50 and an SD of 10. Instead of having a min or max, the PROMIS-29 raw scores have been transformed into t-scores for comparison to a reference population (the US general population) with a mean of 50 and SD of 10. Scores lower than 50 indicate worse health compared to the US general population. Due to the nature of N-of-1 trials, the duration of a subject's period varies based on the subject's home dose of beta-blocker before enrollment, therefore, each subject's respective period for the OFF and ON periods could range between 3 - 6 weeks. The values measured over the time points were averaged." (NCT04767061)
Timeframe: The maximum amount of time a subject could have been assessed for this measure is 76-weeks (24-week max intervention phase,1-year follow-up phase). This outcome was measured at baseline, weekly, end of period and intervention visits, and during follow-up.

,
Interventionscore on a scale (Mean)
Physical Health ComponentMental Health Component
OFF Beta Blockers40.047.9
ON Beta Blockers39.846.8

[back to top]