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phenylpropanolamine

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Description

fawcettimine: from Lyopodium; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Phenylpropanolamine: A sympathomimetic that acts mainly by causing release of NOREPINEPHRINE but also has direct agonist activity at some adrenergic receptors. It is most commonly used as a nasal vasoconstrictor and an appetite depressant. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

phenylpropanolamine : An amphetamine in which the parent 1-phenylpropan-2-amine skeleton is substituted at position 1 with an hydroxy group. A decongestant and appetite suppressant, it is commonly used in prescription and over-the-counter cough and cold preparations. [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]

(-)-norephedrine : An amphetamine that is propylbenzene substituted by a hydroxy group at position 1 and by an amino group at position 2 (the 1R,2S-stereoisomer). It is a plant alkaloid. [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]

Ornade: combination of chlorpheniramine, phenylpropanolamine and isopropamide iodide [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID442475
CHEBI ID4989
SCHEMBL ID14554631
MeSH IDM0016572
PubMed CID10297
CHEMBL ID136560
CHEBI ID80680
SCHEMBL ID152038
MeSH IDM0016572
PubMed CID4786
CHEMBL ID61006
SCHEMBL ID98589
MeSH IDM0016572

Synonyms (204)

Synonym
C09864 ,
fawcettimine
15228-74-7
AC1L9CWK ,
AKOS015966653 ,
CHEBI:4989
SCHEMBL14554631
surecn14554631
DTXSID40331840
Q27106610
(1s,2s,4r,6s,9s)-2-hydroxy-4-methyl-13-azatetracyclo[7.7.0.01,6.02,13]hexadecan-8-one
benzenemethanol, .alpha.-[(1s)-1-aminoethyl]-, (.alpha.r)-
AB01275538-01
benzenemethanol, .alpha.-(1-aminoethyl)-, [r-(r*,s*)]-
PDSP1_001349
erythro-(1r,2s)-norephedrine
dl-alpha-(1-aminoethyl)benzyl alcohol
phenylpropanolamine [inn:ban]
dl-phenylpropanolamine
nsc 17704
benzyl alcohol, alpha-(1-aminoethyl)-
erythro-2-amino-1-phenyl-1-propanol
benzenemethanol, alpha-(1-aminoethyl)-, (r*,s*)-(+-)-
(r*,s*)-(1)-alpha-(1-aminoethyl)benzyl alcohol
benzenemethanol, alpha-((1r)-1-aminoethyl)-, (alphas)-rel-
super odrinex
einecs 207-755-7
benzyl alcohol, alpha-(1-aminoethyl)-, (-)-
l-phenylpropanolamine
ppa [nasal decongestant]
(-)-norephedrin
phenylpropanolaminum [inn-latin]
nsc 9920
einecs 211-850-9
(r,s)-(-)-norephedrine
1-propanol, 2-amino-1-phenyl-, (-)-
benzenemethanol, alpha-(1-aminoethyl)-, (r-(r*,s*))-
phenylpropanolamine (van)
phenylpropanolamina [inn-spanish]
(1r,2s)-2-amino-1-phenyl-1-propanol
(r-(r*,s*))-alpha-(1-aminoethyl)benzyl alcohol
einecs 238-900-2
fenilpropanolamina [italian]
dl-alpha-hydroxy-beta-aminopropylbenzene
benzenemethanol, alpha-(1-aminoethyl)-, (r*,s*)-
(+-)-norephedrin
hsdb 6485
brn 3196918
(1r,2s)-(-)-norephedrine
(1r,2s)-norephedrine
benzenemethanol, alpha-((1s)-1-aminoethyl)-, (alphar)-
SPECTRUM_001103
PDSP2_001333
norephedrine, (-)-
(-)-norephedrine
rhindecon
wln: zy1&yqr -l
benzyl alcohol,.alpha.-(1-aminoethyl)-
usaf cs-6
nsc17704
1-propanol, 2-amino-1-phenyl-
l-norephedrine
propadrine
492-41-1
nsc-9920
dl-1-phenyl-2-aminopropanol-1
mydriatin
mucron
dl-2-amino-1-hydroxy-1-phenylpropane
nsc-17704
SPECTRUM5_001156
l-(-)-ephedrine
C07911
14838-15-4
(+-)-norephedrine
(r*,s*)-(+-)-alpha-(1-aminoethyl)benzenemethanol
phenylpropanolamine
(+-)-phenylpropanolamine
inchi=1/c9h13no/c1-7(10)9(11)8-5-3-2-4-6-8/h2-7,9,11h,10h2,1h3/t7-,9-/m0/s
DB00397
(1r,2s)-(-)-norephedrine, 99%
KBIO2_004151
KBIOSS_001583
KBIO3_001778
KBIO2_001583
KBIOGR_001385
KBIO2_006719
SPECTRUM4_000983
SPBIO_000051
SPECTRUM3_000889
SPECTRUM2_000016
(1r,2s)-2-amino-1-phenylpropan-1-ol
HMS2090P12
chebi:80680 ,
CHEMBL136560 ,
(1r,2s)-phenylpropanolamine
phenylpropanolamine (inn)
D08368
fansia (tn)
phenylfenesin
fansia
rinexin
unii-33ru150wun
33ru150wun ,
phenylpropanolaminum
4-13-00-01875 (beilstein handbook reference)
phenylpropanolamina
(1r,2s)-(-)-phenylpropanolamine
N0608
(1r,2s)-(-)-2-amino-1-phenyl-1-propanol
unii-57b9yg5y1e
fenilpropanolamina
57b9yg5y1e ,
(+/-)-norephedrine
(-)-phenylpropanolamine
AKOS015891206
1-norephedrine
(1r, 2s)-(-)-norephedrine
(1r, 2s)-(-)- norephedrine
1-(-)-ephedrine
(1r,2s)- norephedrine
phenylpropanolamine, l-
phenylpropanolamine, (-)-
(1s,2r)-2-hydroxy-2-phenyl-1-methyl-1-aminoethane
(-)-erythro-2-amino-2-methyl-1-phenylethanol
phenylpropanolamine [who-dd]
phenylpropanolamine [mi]
benzenemethanol, .alpha.-(1-aminoethyl)-, (r*,s*)-, (+/-)-
phenylpropanolamine [inn]
phenylpropanolamine [hsdb]
selegiline hydrochloride impurity c [ep impurity]
phenylpropanolamine [vandf]
phenylpropanolamine [mart.]
CCG-214826
SCHEMBL152038
beta-hydroxyamphetamine
W-106029
1s,2r-phenylpropanolamine hydrochloride
benzenemethanol, .alpha.-((1s)-1-aminoethyl)-, (.alpha.r)-
DTXSID4023466 ,
sr-05000001534
SR-05000001534-2
SR-05000001534-1
Q26840801
DTXSID10889348
dl-1-phenyl-2-aminopropanol-1(chemid)
ppa(chemid)
r01ba01
benzenemethanol, alpha-(1-aminoethyl)-, (r*,s*)-, (+/-)
dtxcid10820534
phenylpropanolamine1534
benzyl alcohol, alpha-(1-aminoethyl)-(chemid)
phenylpropanolaminum (inn-latin)
ppa (nasal decongestant)
(r*,s*)-(1)-alpha-(1-aminoethyl)benzyl alcohol(chemid)
phenylpropanolamin
phenylpropanolamina (inn-spanish)
phenylpropanolamine (mart.)
dl-2-amino-1-hydroxy-1-phenylpropane(chemid)
benzenemethanol, .alpha.-(1-aminoethyl)-
nsc-120735
48115-38-4
nsc120735
(1s,2r)-(+)-norephedrine
KBIO1_000795
DIVK1C_000795
ornade
tavist-d
2-amino-1-phenyl-1-propanol
norephedrine, (.+/-.)-
benzenemethanol, .alpha.-(1-aminoethyl)-, (r*,s*)-(.+/-.)-
IDI1_000795
NINDS_000795
L001077
2-amino-1-phenylpropan-1-ol
(1r, 2s)-2-amino-1-phenyl-propan-1-ol
pseudonorephedrine, (-) [cathine, (-)]
(+)2-amino-1-phenyl-propan-1-ol
2-amino-1-phenyl-propan-1-ol
pseudonorephedrine, (+) [cathine, (+)]
(1r, 2r)-2-amino-1-phenyl-propan-1-ol
norephedrine, (-)
norephedrine, (+)
(1s, 2s)-2-amino-1-phenyl-propan-1-ol
bdbm50022722
(1s, 2r)-2-amino-1-phenyl-propan-1-ol
CHEMBL61006
AKOS015891154
benzenemethanol, .alpha.-[(1r)-1-aminoethyl]-, (.alpha.r)-
benzenemethanol, .alpha.-[(1r)-1-aminoethyl]-, (.alpha.r)-rel-
SCHEMBL98589
(1 s,2r)-(+)-norephedrine
1-phenyl-2-aminopropanol
(1s, 2r)-(+)-norephedrine
alpha-(1-aminoethyl)benzyl alcohol
(1s, 2r )-(+)-norephedrine
benzenemethanol, alpha-(1-aminoethyl)-
683h0r9659 ,
beta-hydroxy-alpha-methylphenethylamine
2-amino-2-methyl-1-phenylethanol
2-amino-1-hydroxy-1-phenylpropane
unii-683h0r9659
DTXSID70859305
2-amino-1-phenylpropane-1-ol

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"A comparison was made among phenylpropanolamine, aspirin, acetaminophen and ibuprofen in terms of their relative safety, as measured by adverse reaction reports published since 1980, the five semiannual reports published by the Drug Abuse Warning Network during 1984-1986 and annual reports from Poison Control Centers from 1983-1986."( A comparison of the relative safety of phenylpropanolamine, acetaminophen, ibuprofen and aspirin as measured by three compendia.
Winick, C, 1989
)
0.28
" While generally safe at recommended doses, PPA can be hazardous to susceptible individuals and we urge physicians to be alert to the potential for PPA related psychiatric reactions."( Psychiatric side effects attributed to phenylpropanolamine.
Lake, CR; Masson, EB; Quirk, RS, 1988
)
0.27
" A search of the English literature from 1966 to 1984 revealed 12 prospective clinical studies out of 37 articles that specifically addressed the potential adverse pressor effect of SMDs."( Are oral decongestants safe in hypertension? An evaluation of the evidence and a framework for assessing clinical trials.
Deck, CC; Radack, K, 1986
)
0.27
"" Toxic effects may result from overdose, drug interactions, or diseases that increase sensitivity to sympathomimetic agents."( Toxicity of over-the-counter stimulants.
Pentel, P, 1984
)
0.27
" Generally, toxic reactions involve excessive CNS stimulation (e."( Managing acute toxicity from nonprescription stimulants.
Conner, CS; Rumack, BH; Sawyer, DR,
)
0.13
"7% for the two adverse events, respectively) than in the T/Ps group (10."( Safety and efficacy of terfenadine/pseudoephedrine versus clemastine/phenylpropanolamine in the treatment of seasonal allergic rhinitis.
Falliers, CJ; Grant, JA; Huster, WJ; McNutt, B; Podleski, WK; Segal, AT; Woehler, TR, 1993
)
0.29
" Tolterodine was safe and generally well tolerated."( Efficacy and safety of two doses of tolterodine versus placebo in patients with detrusor overactivity and symptoms of frequency, urge incontinence, and urgency: urodynamic evaluation. The International Study Group.
Höfner, K; Holmdahl, TH; Jonas, U; Madersbacher, H, 1997
)
0.3
" Safety and tolerability were assessed from adverse events and laboratory measures."( Clinical efficacy and safety of tolterodine in the treatment of overactive bladder: a pooled analysis.
Appell, RA, 1997
)
0.3
" Tolterodine at doses of 1 mg and 2 mg were tolerated significantly better than oxybutynin when adverse events, dry mouth (both frequency and intensity), dose reductions, and patient withdrawals were considered."( Clinical efficacy and safety of tolterodine in the treatment of overactive bladder: a pooled analysis.
Appell, RA, 1997
)
0.3
" Patients receiving tolterodine should not experience these limitations and instead will get safe and long-term effective treatment for their condition."( Clinical efficacy and safety of tolterodine in the treatment of overactive bladder: a pooled analysis.
Appell, RA, 1997
)
0.3
" The incidence of adverse events (mainly mild or moderate antimuscarinic effects) was comparable with placebo at tolterodine dosages of < or = 2 mg."( Efficacy and safety of tolterodine in patients with detrusor instability: a dose-ranging study.
Abrams, P; Cardozo, L; Fall, M; Nelson, E; Rentzhog, L; Stanton, SL, 1998
)
0.3
"We evaluated the efficacy, patient acceptability and side effect profile of tolterodine, a new antimuscarinic agent for treating bladder overactivity."( Clinical efficacy and safety of tolterodine compared to placebo in detrusor overactivity.
Clarke, B; Davis, BE; Dwyer, P; Millard, R; Moore, K; Susset, J; Tuttle, J, 1999
)
0.3
" There was no clinical or electrocardiographic evidence of significant cardiac adverse events."( Clinical efficacy and safety of tolterodine compared to placebo in detrusor overactivity.
Clarke, B; Davis, BE; Dwyer, P; Millard, R; Moore, K; Susset, J; Tuttle, J, 1999
)
0.3
" The incidence of adverse events (mainly mild or moderate antimuscarinic effects) was comparable between placebo and tolterodine dosages of 2 mg twice daily."( Tolterodine in the treatment of overactive bladder: analysis of the pooled phase II efficacy and safety data.
Hallén, B; Larsson, G; Nilvebrant, L, 1999
)
0.3
" Tolterodine was significantly better tolerated than oxybutynin when adverse events (particularly frequency and intensity of dry mouth), dose reduction and patient withdrawals were considered."( Clinical efficacy and safety of tolterodine compared to oxybutynin and placebo in patients with overactive bladder.
Appell, RA; Drutz, HP; Gleason, D; Klimberg, I; Radomski, S, 1999
)
0.3
"Safety and tolerability were evaluated through spontaneously reported adverse events, electrocardiogram, and blood pressure measurements."( Tolterodine: a safe and effective treatment for older patients with overactive bladder.
Malone-Lee, JG; Maugourd, MF; Walsh, JB, 2001
)
0.31
" Neither dosage of tolterodine was associated with serious drug-related adverse events during the study."( Tolterodine: a safe and effective treatment for older patients with overactive bladder.
Malone-Lee, JG; Maugourd, MF; Walsh, JB, 2001
)
0.31
"Tolterodine (taken for 4 weeks) is safe and shows efficacy, particularly at a dosage of 2 mg bid, in the treatment of older patients with urinary symptoms attributable to overactive bladder."( Tolterodine: a safe and effective treatment for older patients with overactive bladder.
Malone-Lee, JG; Maugourd, MF; Walsh, JB, 2001
)
0.31
" However such drugs are associated with a high incidence of anticholinergic adverse effects."( Safety profile of tolterodine as used in general practice in England: results of prescription-event monitoring.
Layton, D; Pearce, GL; Shakir, SA, 2001
)
0.31
"The most common adverse events reported were dry mouth, headache, malaise, constipation, dyspepsia, nausea and vomiting and pain in abdomen."( Safety profile of tolterodine as used in general practice in England: results of prescription-event monitoring.
Layton, D; Pearce, GL; Shakir, SA, 2001
)
0.31
" Dry mouth (of any severity) was the most common adverse event in both the tolterodine ER and placebo treatment arms, irrespective of age (<65: ER 22."( Efficacy, safety, and tolerability of extended-release once-daily tolterodine treatment for overactive bladder in older versus younger patients.
Mattiasson, A; Stanton, SL; Zinner, NR, 2002
)
0.31
" Tolterodine ER was safe and well tolerated."( Long-term safety, tolerability and efficacy of extended-release tolterodine in the treatment of overactive bladder.
Jonas, U; Kreder, K; Mayne, C, 2002
)
0.31
"To determine whether women with urinary incontinence (UI) can identify their allocation in a randomized controlled trial (RCT) of tolterodine (TOL), and whether correct identification is associated with outcomes and adverse effects (AEs)."( "Unblinding" in randomized controlled drug trials for urinary incontinence: Implications for assessing outcomes when adverse effects are evident.
DuBeau, CE; Khullar, V; Versi, E, 2005
)
0.33
" Tolterodine ER was well tolerated and the most common adverse event was dry mouth (33."( Long-term safety, tolerability and efficacy of extended-release tolterodine in the treatment of overactive bladder in Japanese patients.
Homma, Y; Takei, M, 2005
)
0.33
" This is a safe and reliable technique for managing the pancreatic remnant in patients undergoing extended PD for advanced pancreaticobiliary malignancy."( Safe management of the pancreatic remnant with prolamine duct occlusion after extended pancreaticoduodenectomy.
Kosuge, T; Sakamoto, Y; Sano, T; Shimada, K,
)
0.13
" There were no significant between-group differences in the incidence of adverse events."( Safety and tolerability of tolterodine for the treatment of overactive bladder in men with bladder outlet obstruction.
Abrams, P; De Koning Gans, HJ; Kaplan, S; Millard, R, 2006
)
0.33
" The incidence of adverse events (AEs) was similar in the three treatment groups (extended-release oxybutynin, 70%; extended-release tolterodine, 64%; and immediate-release tolterodine, 79%)."( Safety and tolerability of extended-release oxybutynin once daily in urinary incontinence: combined results from two phase 4 controlled clinical trials.
Armstrong, RB; Dmochowski, RR; Macdiarmid, S; Sand, PK, 2007
)
0.34
"The primary objectives of the treatment for the lower urinary tract symptoms (LUTS) associated with benign prostatic hyperplasia (BPH) are to produce rapid, sustained, and safe improvements in the symptoms that affect the quality of life in the majority of men over 50."( Efficacy and safety of combined therapy with terazosin and tolteradine for patients with lower urinary tract symptoms associated with benign prostatic hyperplasia: a prospective study.
Li, HZ; Wang, W; Xiao, H; Yang, Y; Zhang, X; Zhang, Y; Zhao, XF, 2007
)
0.34
" The incidence of adverse effects in the combination group was higher than that in the terazosin group."( Efficacy and safety of combined therapy with terazosin and tolteradine for patients with lower urinary tract symptoms associated with benign prostatic hyperplasia: a prospective study.
Li, HZ; Wang, W; Xiao, H; Yang, Y; Zhang, X; Zhang, Y; Zhao, XF, 2007
)
0.34
" This study, although short term and limited numbers of patients, provides evidence that the combined therapy with terazosin plus tolterodine is a good approach for meeting the objectives of rapid, sustained, and safe improvements in the LUTS associated with BPH."( Efficacy and safety of combined therapy with terazosin and tolteradine for patients with lower urinary tract symptoms associated with benign prostatic hyperplasia: a prospective study.
Li, HZ; Wang, W; Xiao, H; Yang, Y; Zhang, X; Zhang, Y; Zhao, XF, 2007
)
0.34
" Tamsulosin OCAS was well tolerated and the proportion of women discontinuing because of adverse events was low (4."( A randomized double-blind placebo-controlled multicentre study to explore the efficacy and safety of tamsulosin and tolterodine in women with overactive bladder syndrome.
Bolodeoku, J; Cardozo, L; Robinson, D; Terpstra, G, 2007
)
0.34
" Evaluation was by subjective assessment, visual analog scale, urodynamic assessment and adverse drug reaction monitoring."( Comparative efficacy and safety of extended-release and instant-release tolterodine in children with neural tube defects having cystometric abnormalities.
Kaur, B; Mahanta, K; Medhi, B; Narasimhan, KL, 2008
)
0.35
" No adverse effects of hyperpyrexia, flushing or intolerance to outdoor temperatures, or dryness of mouth were observed in either group."( Comparative efficacy and safety of extended-release and instant-release tolterodine in children with neural tube defects having cystometric abnormalities.
Kaur, B; Mahanta, K; Medhi, B; Narasimhan, KL, 2008
)
0.35
" Seven treatment-related adverse events were reported."( Long-term efficacy and safety of tolterodine in children with neurogenic detrusor overactivity.
Borgstein, NG; Ellsworth, PI; Nijman, RJ; Reddy, PP, 2008
)
0.35
")), adverse events, and retention."( Efficacy and safety of tolterodine extended release and dutasteride in male overactive bladder patients with prostates >30 grams.
Chung, DE; Kaplan, SA; Staskin, DR; Te, AE, 2010
)
0.36
" Treatments were generally well tolerated; discontinuation rates due to adverse events were 4%, 2%, 5%, 0%, and 1% with standard- and low-dose pregabalin/tolterodine ER, pregabalin, tolterodine ER, and placebo, respectively."( Investigation of the clinical efficacy and safety of pregabalin alone or combined with tolterodine in female subjects with idiopathic overactive bladder.
Cossons, NH; Darekar, A; Marencak, J; Mills, IW, 2011
)
0.37
" The incidence of adverse events in the tolterodine-treated group (28%) was significantly lower than that in the oxybutnin-treated group (57%) (P<0."( [Comparisons of efficacy and safety of tolterodine and oxybutynin in children with idiopathic overactive bladder].
Chen, CJ; Deng, YJ; Ge, Z; Guo, YF; Lu, RG; Ma, G; Wang, LX; Zhu, HB, 2011
)
0.37
" Adverse events and changes of urodynamic values and clinical data were compared between the solifenacin and tolterodine groups."( Comparisons of urodynamic effects, therapeutic efficacy and safety of solifenacin versus tolterodine for female overactive bladder syndrome.
Chang, TC; Chen, CH; Hsiao, SM; Lin, HH; Wu, WY; Yu, HJ, 2011
)
0.37
"Both solifenacin and tolterodine had similar urodynamic effects, therapeutic efficacy and adverse events in treating women with overactive bladder syndrome; however, tolterodine had a greater effect in increasing heart rate than solifenacin."( Comparisons of urodynamic effects, therapeutic efficacy and safety of solifenacin versus tolterodine for female overactive bladder syndrome.
Chang, TC; Chen, CH; Hsiao, SM; Lin, HH; Wu, WY; Yu, HJ, 2011
)
0.37
" The AMs used to treat OAB differ in their pharmacological profiles, which may affect their potential for causing adverse effects (AEs)."( Pharmacokinetics and toxicity of antimuscarinic drugs for overactive bladder treatment in females.
Alessandri, F; Candiani, M; Ferrero, S; Leone Roberti Maggiore, U; Origoni, M; Remorgida, V; Salvatore, S; Venturini, PL, 2012
)
0.38
"The malting barleys were less immunogenic, with reduced levels of toxic gluten, and were possibly less harmful to CD patients."( Significant differences in coeliac immunotoxicity of barley varieties.
Barro, F; Cebolla, A; Comino, I; de Lorenzo, L; Gil-Humanes, J; López-Casado, MÁ; Lorite, P; Moreno, Mde L; Pistón, F; Real, A; Sousa, C; Torres, MI, 2012
)
0.38
"The incidence rates of overall adverse event, dry mouth, constipation and blurred vision of the experimental group (solifenacin 5 mg once per day) was 26."( [Safety of solifenacin and tolterodine in the treatment of overactive bladder: a meta-analysis].
Jiang, XZ; Xu, C; Xu, ZS; Zhang, NZ; Zhao, HF, 2012
)
0.38
"Dry mouth is the most common adverse event of solifenacin (5 mg once per day) and tolterodine (2 mg twice per day)."( [Safety of solifenacin and tolterodine in the treatment of overactive bladder: a meta-analysis].
Jiang, XZ; Xu, C; Xu, ZS; Zhang, NZ; Zhao, HF, 2012
)
0.38
" The safety analysis included adverse event (AE) reporting, laboratory assessments, ECG, postvoid residual volume and vital signs (blood pressure, pulse rate)."( Mirabegron for the treatment of overactive bladder: a prespecified pooled efficacy analysis and pooled safety analysis of three randomised, double-blind, placebo-controlled, phase III studies.
Angulo, JC; Blauwet, MB; Cambronero, J; Dorrepaal, C; Herschorn, S; Khullar, V; Martin, NE; Nitti, VW; Siddiqui, E; van Kerrebroeck, P, 2013
)
0.39
" The incidence of adverse events was 54."( Phase II study on the efficacy and safety of the EP1 receptor antagonist ONO-8539 for nonneurogenic overactive bladder syndrome.
Abrams, P; Andersson, KE; Chapple, CR; Deacon, S; Kuwayama, T; Masuda, T; Radziszewski, P; Small, M, 2014
)
0.4
" Both solifenacin and tolterodine ER have similar therapeutic efficacies and adverse events."( [Comparisons of therapeutic efficacy and safety of solifenacin versus tolterodine in patients with overactive bladder: a meta-analysis of outcomes].
Li, J; Li, P; Liu, B; Wang, Y; Wu, Y, 2014
)
0.4
"3 mg cathine), but no suspected unexpected serious adverse reactions were noted."( Efficacy and Safety of Cathine (Nor-Pseudoephedrine) in the Treatment of Obesity: A Randomized Dose-Finding Study.
Blüher, M; Chen-Stute, A; Hastreiter, L; Hauner, H; Scholze, J; Werdier, D, 2017
)
0.46

Pharmacokinetics

The mechanism involved in the serious adverse effects associated with phenylpropanolamine has not yet been clarified. The aim of this study was to characterize the possibility of pharmacokinetic interactions between PPA and most often comb.

ExcerptReferenceRelevance
" The bioavailability and in vitro pharmacokinetic characteristics of this novel PPA preparation were compared with those of a reference sustained-release 75 mg Q16 PPA tablet (Acutrim), in a pilot, 3 subject, unblinded, cross-over, single dose study."( In-vivo pharmacokinetic characteristics of a transdermal phenylpropanolamine (PPA) preparation.
Devane, J; Foynes, M; Martin, M; Mulligan, S, 1991
)
0.28
"The pharmacokinetic and pharmacodynamic interaction between caffeine and phenylpropanolamine has been investigated in six normal subjects in a double-blind, placebo-controlled, Latin-square design study."( A pharmacodynamic interaction between caffeine and phenylpropanolamine.
Branch, RA; Brown, NJ; Ryder, D, 1991
)
0.28
" A pharmacokinetic basis for the variability in response to racemic phenylpropanolamine was not observed."( Individual variability in the blood pressure response to intravenous phenylpropanolamine: a pharmacokinetic and pharmacodynamic investigation.
O'Connell, MB; Pentel, PR; Zimmerman, CL, 1989
)
0.28
" It is possible that each enantiomer can reflect significant enantioselective differences with regard to both pharmacokinetic and pharmacodynamic effects."( Pharmacokinetics of oral decongestants.
Dowse, R; Kanfer, I; Vuma, V,
)
0.13
" Extravascular distribution of drug was suggested by the high volume of distribution (799 +/- 315 L) and low Cmax (0."( The pharmacokinetics and bioavailability of clemastine and phenylpropanolamine in single-component and combination formulations.
Chang, CT; Gelbert, MB; O'Connor, R; Petryk, L; Schran, HF, 1996
)
0.29
" Significant differences were observed in the pharmacokinetic parameters of each enantiomer when the enantiomers were administered singly and as a racemate."( [Pharmacokinetics of (-)-, (+)- and (+/-)-norephedrine. Plasma concentrations, serum protein binding and urinary excretions].
Kamakura, H; Satake, M, 1998
)
0.3
"To determine whether cytochrome P450 2D6 (CYP2D6) is involved in the metabolism of tolterodine by investigating potential differences in pharmacokinetics and pharmacodynamic (heart rate, accommodation, and salivation) of tolterodine and its 5-hydroxymethyl metabolite between poor metabolizers and extensive metabolizers of debrisoquin (INN, debrisoquine)."( Influence of CYP2D6 polymorphism on the pharmacokinetics and pharmacodynamic of tolterodine.
Alván, G; Bertilsson, L; Brynne, N; Dalén, P; Gabrielsson, J, 1998
)
0.3
" The pharmacokinetics of tolterodine and 5-hydroxymethyl metabolite were determined, and the pharmacodynamic were measured."( Influence of CYP2D6 polymorphism on the pharmacokinetics and pharmacodynamic of tolterodine.
Alván, G; Bertilsson, L; Brynne, N; Dalén, P; Gabrielsson, J, 1998
)
0.3
" Pharmacokinetic parameters were calculated using model independent method."( Pharmacokinetics of a single dose of phenylpropanolamine following oral administration at two different times of the day.
Rambhau, D; Rao, BR; Rao, VV; Srinivasu, P, 1998
)
0.3
" The various pharmacokinetic parameters of phenylpropanolamine were calculated using model independent methods."( Time dependent pharmacokinetic interaction between phenylpropanolamine and chlorpheniramine maleate in human subjects.
Rambhau, D; Rao, BR; Rao, VV; Srinivasu, P, 1999
)
0.3
" The elimination of tolterodine from serum was rapid, with a half-life of less than 2 h in all species."( Pharmacokinetics of tolterodine, a muscarinic receptor antagonist, in mouse, rat and dog. Interspecies relationship comparing with human pharmacokinetics.
Kankaanranta, S; Påhlman, I; Palmér, L, 2001
)
0.31
"The new ER formulation of tolterodine shows no pharmacokinetic interaction with food."( Food does not influence the pharmacokinetics of a new extended release formulation of tolterodine for once daily treatment of patients with overactive bladder.
Olsson, B; Szamosi, J, 2001
)
0.31
"The new once daily ER formulation of tolterodine 4mg shows pharmacokinetic equivalence (AUC24) to the existing IR tablet given at a dose of 2mg twice daily."( Multiple dose pharmacokinetics of a new once daily extended release tolterodine formulation versus immediate release tolterodine.
Olsson, B; Szamosi, J, 2001
)
0.31
" The authors present data evaluating the pharmacokinetic and pharmacodynamic responses to coadministration of oral linezolid with sympathomimetics (pseudoephedrine and phenylpropanolamine) and a serotonin reuptake inhibitor (dextromethorphan)."( Linezolid: pharmacokinetic and pharmacodynamic evaluation of coadministration with pseudoephedrine HCl, phenylpropanolamine HCl, and dextromethorpan HBr.
Antal, EJ; Batts, DH; Hendershot, PE; Hopkins, NK; Welshman, IR, 2001
)
0.31
" Pharmacokinetic assessments were performed on day 14 based on plasma levels of ethinyl estradiol and levonorgestrel up to 24 hours after dosing and serum tolterodine levels at 1 to 3 hours after dosing."( The effect of tolterodine on the pharmacokinetics and pharmacodynamics of a combination oral contraceptive containing ethinyl estradiol and levonorgestrel.
Landgren, BM; Olsson, B, 2001
)
0.31
" There was no evidence of a pharmacokinetic interaction between tolterodine and the steroid hormones in the oral contraceptive used, nor did the oral contraceptive show any relevant pharmacokinetic interaction with tolterodine."( The effect of tolterodine on the pharmacokinetics and pharmacodynamics of a combination oral contraceptive containing ethinyl estradiol and levonorgestrel.
Landgren, BM; Olsson, B, 2001
)
0.31
" These findings indicate that co-administration of tolterodine and warfarin is safe and well tolerated, with no clinically significant pharmacodynamic or kinetic interaction in healthy volunteers."( Effect of tolterodine on the anticoagulant actions and pharmacokinetics of single-dose warfarin in healthy volunteers.
Hallén, B; Narang, P; Rahimy, M, 2002
)
0.31
" The data were evaluated using computerized pharmacokinetic compartmental analysis."( Pharmacokinetics of cathinone, cathine and norephedrine after the chewing of khat leaves.
Harder, S; Kauert, GF; Niess, C; Schramm, M; Toennes, SW, 2003
)
0.32
"As the mechanism involved in the serious adverse effects associated with phenylpropanolamine (PPA) has not yet been clarified, and as PPA in usual cases is not being ingested without other drugs combination, the aim of this study was to characterize the possibility of pharmacokinetic interactions between PPA and most often combined drugs existing in the same dosage."( Pharmacokinetic interactions between phenylpropanolamine, caffeine and chlorpheniramine in rats.
Kaddoumi, A; Nakashima, K; Nakashima, MN; Wada, M, 2004
)
0.32
"The combination of ephedrine and caffeine has been used in herbal products for weight loss and athletic performance-enhancement, but the pharmacokinetic profiles of these compounds have not been well characterized."( Mechanistic pharmacokinetic modelling of ephedrine, norephedrine and caffeine in healthy subjects.
Benowitz, NL; Csajka, C; Haller, CA; Verotta, D, 2005
)
0.33
"The pharmacokinetic model was developed based on the simultaneous modelling using plasma samples gathered from two clinical trials."( Mechanistic pharmacokinetic modelling of ephedrine, norephedrine and caffeine in healthy subjects.
Benowitz, NL; Csajka, C; Haller, CA; Verotta, D, 2005
)
0.33
" The peak concentration ratios for oxybutynin and metabolite also conformed to this range; those for tolterodine did not."( Effect of the proton pump inhibitor omeprazole on the pharmacokinetics of extended-release formulations of oxybutynin and tolterodine.
Chen, A; Dmochowski, R; Gidwani, S; Gupta, S; MacDiarmid, S; Sathyan, G, 2005
)
0.33
" Pharmacokinetic parameters obtained following selegiline transdermal system and pseudoephedrine or phenylpropanolamine were unremarkable."( Evaluation of the potential for pharmacodynamic and pharmacokinetic drug interactions between selegiline transdermal system and two sympathomimetic agents (pseudoephedrine and phenylpropanolamine) in healthy volunteers.
Azzaro, AJ; Blob, LF; Campbell, BJ; Kemper, EM; VanDenBerg, CM; Ziemniak, J, 2007
)
0.34
" Results revealed that as the increase of urinary pH, the mean elimination half-life (t(1/2)), the mean residence time (MRT) and the area under the plasma concentration-time curve (AUC) of PPA, PSE, and FEN were greatly raised, while the total plasma clearance (CL/F) decreased considerably."( Influences of urinary pH on the pharmacokinetics of three amphetamine-type stimulants using a new high-performance liquid chromatographic method.
Feng, F; Wang, L; Wang, XQ; Zhu, L, 2009
)
0.35
" The objective of this study was to establish the pharmacokinetic profile of fesoterodine and to highlight ist potential pharmacokinetic advantages over tolterodine."( The pharmacokinetic profile of fesoterodine: similarities and differences to tolterodine.
Malhotra, B; Simon, HU, 2009
)
0.35
" Blood and urine samples for the analysis of 5-HMT were collected before and multiple times after drug administration for pharmacokinetic analysis."( The pharmacokinetic profile of fesoterodine: similarities and differences to tolterodine.
Malhotra, B; Simon, HU, 2009
)
0.35
"The mean peak plasma concentration (Cmax) of 5-HMT and the mean area under the time versus concentration curve (AUC) increased proportionally with the fesoterodine dose."( The pharmacokinetic profile of fesoterodine: similarities and differences to tolterodine.
Malhotra, B; Simon, HU, 2009
)
0.35
"This head-to-head study confirmed the findings of reduced pharmacokinetic variability of fesoterodine and further delineates that tolterodine, and not 5-HMT, was the principal source of variability after administration of tolterodine extended release."( Comparison of pharmacokinetic variability of fesoterodine vs. tolterodine extended release in cytochrome P450 2D6 extensive and poor metabolizers.
Crownover, P; Darsey, E; Fang, J; Glue, P; Malhotra, B, 2011
)
0.37
" Saliva and plasma samples were collected for 3-5 half-life values of sitagliptin, cinacalcet, metformin, montelukast, tolterodine, hydrochlorothiazide (HCT), lornoxicam, azithromycin, diacerhein, rosuvastatin, cloxacillin, losartan and tamsulosin after oral dosing."( Saliva versus plasma pharmacokinetics: theory and application of a salivary excretion classification system.
Arafat, T; Idkaidek, N, 2012
)
0.38
" To confirm this effect in a clinical setting, we carried out a full pharmacokinetic study of a single oral dose of CYP2D6 substrate tolterodine in 30 healthy Korean individuals (HNF4α wild type: n = 24; HNF4α G60D heterozygotes: n = 6) who were pregenotyped for CYP2D6."( Effect of HNF4α genetic polymorphism G60D on the pharmacokinetics of CYP2D6 substrate tolterodine in healthy Korean individuals.
Ghim, JL; Jiang, F; Kim, DH; Kim, EY; Kim, HS; Lee, SS; Oh, MK; Shin, JG; Shon, JH; Yeo, CW, 2013
)
0.39
" Compared with single-herb extracts, alkaloids in plasma (except methylephedrine, benzoylmesaconine and benzoylhypaconine) showed slower elimination (the mean residence time or half-life was longer), although the maximum plasma concentration and area under the plasma concentration curve values decreased."( Simultaneous quantification and pharmacokinetics of alkaloids in Herba Ephedrae-Radix Aconiti Lateralis extracts.
Huo, H; Li, H; Luo, J; Song, S; Tang, Q; Xing, X,
)
0.13

Compound-Compound Interactions

Study examined potential for drug-drug interactions during treatment with selegiline transdermal system and pseudoephedrine or phenylpropanolamine.

ExcerptReferenceRelevance
" The woman described in this article died after taking her usual dose of thioridazine, 100 mg/d, in combination with a single capsule of Contac."( Death attributed to ventricular arrhythmia induced by thioridazine in combination with a single Contac C capsule.
Chouinard, G; Ghadirian, AM; Jones, BD, 1978
)
0.26
" The method involved extraction of plasma or urine at a basic pH with diethyl ether, and chromatographic analysis using column switching combined with ion-pair chromatography."( High-performance liquid chromatographic determination of phenylpropanolamine in human plasma and urine, using column switching combined with ion-pair chromatography.
Motohashi, M; Yamashita, K; Yashiki, T, 1990
)
0.28
" It is often combined with caffeine in diet preparations and "look-alike" pills."( Cerebral hemorrhage associated with phenylpropanolamine in combination with caffeine.
Asdell, SM; Mueller, SM; Muller, J,
)
0.13
" In the current paper, this new extraction technique was combined with liquid chromatography-mass spectrometry (LC-MS) for the first time."( Liquid-phase microextraction based on carrier mediated transport combined with liquid chromatography-mass spectrometry. New concept for the determination of polar drugs in a single drop of human plasma.
Anthonsen, HS; Ho, TS; Pedersen-Bjergaard, S; Rasmussen, KE; Reubsaet, JL, 2005
)
0.33
"To compare the urodynamic and morphologic effects of the administration of estriol alone and in combination with phenylpropanolamine on the lower portion of the urogenital tract in female dogs."( Urodynamic and morphologic changes in the lower portion of the urogenital tract after administration of estriol alone and in combination with phenylpropanolamine in sexually intact and spayed female dogs.
Balligand, MH; Farnir, F; Grand, JG; Hamaide, AJ; Le Couls, G; Snaps, FR; Verstegen, JP, 2006
)
0.33
" Because older individuals typically take multiple medications, clinicians must pay special attention to potential drug-drug interactions that may cause adverse events or alter drug efficacy."( Treatment of overactive bladder: selective use of anticholinergic agents with low drug-drug interaction potential.
Chancellor, MB; de Miguel, F, 2007
)
0.34
" This study examined the potential for drug-drug interactions during treatment with selegiline transdermal system and pseudoephedrine or phenylpropanolamine."( Evaluation of the potential for pharmacodynamic and pharmacokinetic drug interactions between selegiline transdermal system and two sympathomimetic agents (pseudoephedrine and phenylpropanolamine) in healthy volunteers.
Azzaro, AJ; Blob, LF; Campbell, BJ; Kemper, EM; VanDenBerg, CM; Ziemniak, J, 2007
)
0.34
"To compare the efficacy of antimuscarinics alone versus antimuscarinics in combination with local oestrogens for OAB; to verify whether risk factors for lower antimuscarinic efficacy can be overcome by the concomitant use of local oestrogens."( Is there a synergistic effect of topical oestrogens when administered with antimuscarinics in the treatment of symptomatic detrusor overactivity?
Bolis, P; Cardozo, L; Salvatore, S; Serati, M; Uccella, S, 2009
)
0.35
"To assess the efficacy and safety of pregabalin alone or in combination with tolterodine extended release (ER) in subjects with idiopathic OAB."( Investigation of the clinical efficacy and safety of pregabalin alone or combined with tolterodine in female subjects with idiopathic overactive bladder.
Cossons, NH; Darekar, A; Marencak, J; Mills, IW, 2011
)
0.37
"To evaluate the efficacy and safety of Tolterodine Tartrate combined with the alpha-receptor blocker in the treatment of benign prostatic hyperplasia with detrusor overactivity (BPH-DO)."( [Tolterodine tartrate combined with alpha-receptor blocker for benign prostatic hyperplasia with detrusor overactivity].
Gan, W; Jia, HT; Li, YF; Luo, MH; Xie, S; Zhang, SF, 2011
)
0.37
"A total of 113 patients with BPH-DO were randomly assigned to receive Tolterodine Tartrate combined with Cardura (Group A) and Cardura alone (Group B), both for 12 weeks."( [Tolterodine tartrate combined with alpha-receptor blocker for benign prostatic hyperplasia with detrusor overactivity].
Gan, W; Jia, HT; Li, YF; Luo, MH; Xie, S; Zhang, SF, 2011
)
0.37
"To evaluate the therapeutic effect of Parkinson's disease combined with overactive bladder syndrome (GAB) treated with combined therapy of oral administration of Tolterodine with low dose and electroacuponcture."( [Parkinson's disease combined with overactive bladder syndrome treated with acupuncture and medication].
Chen, YL; Feng, WJ; Zhang, XL, 2012
)
0.38
"Sixty cases of Parkinson's disease combined with GAB were randomly divided into a combined acupuncture and medication group (group A) and a medication group (group B), 30 cases in each group."( [Parkinson's disease combined with overactive bladder syndrome treated with acupuncture and medication].
Chen, YL; Feng, WJ; Zhang, XL, 2012
)
0.38
"The therapeutic effect of Parkinson' s disease combined with GAB treated with combined therapy of Tolterodine with low dose and electroacupuncture is superior to that of complete dose of Tolterodine with oral administration, with less adverse reactions."( [Parkinson's disease combined with overactive bladder syndrome treated with acupuncture and medication].
Chen, YL; Feng, WJ; Zhang, XL, 2012
)
0.38

Bioavailability

The bioavailability and pharmacokinetics of phenylpropanolamine hydrochloride (PPA HCl) from a Dexatrim controlled-release (CR) caplet and solution was studied. Data are presented to illustrate the suitability of the method for dosage form bioavailability evaluation.

ExcerptReferenceRelevance
", ionic strength) to: (a) correlate in vitro release rates with bioavailability data, (b) discriminate between alternative formulations during dosage form development, or (c) serve as a selective control procedure for a series of sustanined-release dosage forms."( Continuous dissolution rate determination as a function of the pH of the medium.
Dauvois, M; Michaelis, AF; Turi, P, 1976
)
0.26
" Data are presented to illustrate the suitability of the method for dosage form bioavailability evaluation from plasma phenylpropanolamine levels achieved after acute oral administration of a typical dosage form."( Electron-capture GLC determination of phenylpropanolamine as a pentofluorophenyloxazolidine derivative.
Kostenbauder, HB; Neelakantan, L, 1976
)
0.26
" The bioavailability and in vitro pharmacokinetic characteristics of this novel PPA preparation were compared with those of a reference sustained-release 75 mg Q16 PPA tablet (Acutrim), in a pilot, 3 subject, unblinded, cross-over, single dose study."( In-vivo pharmacokinetic characteristics of a transdermal phenylpropanolamine (PPA) preparation.
Devane, J; Foynes, M; Martin, M; Mulligan, S, 1991
)
0.28
"The bioavailability and pharmacokinetics of phenylpropanolamine hydrochloride (PPA HCl) from a Dexatrim controlled-release (CR) caplet and solution was studied."( Bioavailability and cardiovascular safety of Dexatrim (phenylpropanolamine hydrochloride) from a controlled-release caplet.
Brisson, J; Cohen, P; Dennis, S; Shargel, L; Silverman, HI, 1990
)
0.28
" Oral bioavailability from the low-crystalline PVA-MA tablet formulation was 78."( Polyvinyl alcohol-methyl acrylate copolymers as a sustained-release oral delivery system.
CoffinBeach, D; DiLuccio, RC; Hurwitz, AR; Hussain, MA; Shefter, E; Torosian, G, 1989
)
0.28
" Oral absorption from the immediate-release capsule was rapid and bioavailability was 98."( Phenylpropanolamine pharmacokinetics in dogs after intravenous, oral, and oral controlled-release doses.
Aungst, BJ; Hussain, MA; Lam, G; Shefter, E,
)
0.13
" These mixtures gave varying drug release profiles that showed rank-order correlation with plasma concentration profiles obtained in bioavailability studies with suspension dosage forms."( Sustained-release drug delivery system I: Coated ion-exchange resin system for phenylpropanolamine and other drugs.
Amsel, L; Bryant, W; Hinsvark, O; Raghunathan, Y, 1981
)
0.26
" Both PPA and PDE are readily and completely absorbed, whereas PE, with a bioavailability of only approximately 38%, is subject to gut wall metabolism and is thought to be absorbed erratically."( Pharmacokinetics of oral decongestants.
Dowse, R; Kanfer, I; Vuma, V,
)
0.13
" The method considers the probability that the bioavailability of the test product is close to the bioavailability of the reference product, against the probability that the bioavailability of the reference product is close to itself when administered on different occasions."( Assessment of individual and population bioequivalence using the probability that bioavailabilities are similar.
Schall, R, 1995
)
0.29
"In a traditional assessment of the bioequivalence of two formulations of a drug one compares the average bioavailability from the two formulations."( On population and individual bioequivalence.
Luus, HG; Schall, R, 1993
)
0.29
"Studies were conducted in healthy male volunteers (n = 171; age range, 19-49 years; 22-27 subjects per study) to examine the following: pharmacokinetics and dose proportionality of the antihistamine clemastine; the effect of coadministration of phenylpropanolamine and clemastine on the pharmacokinetics of the two drugs; and the bioavailability of clemastine tablets and combination tablets of clemastine and sustained-release phenyl-propanolamine under fasted and fed conditions after single-dose administration and at steady state."( The pharmacokinetics and bioavailability of clemastine and phenylpropanolamine in single-component and combination formulations.
Chang, CT; Gelbert, MB; O'Connor, R; Petryk, L; Schran, HF, 1996
)
0.29
" The absolute bioavailability was highly variable, ranging from 10 to 70%."( Pharmacokinetics and pharmacodynamics of tolterodine in man: a new drug for the treatment of urinary bladder overactivity.
Brynne, N; Edlund, PO; Gabrielsson, J; Hallén, B; Höglund, P; Palmér, L; Stahl, MM, 1997
)
0.3
"05) decrease in the rate of absorption of phenylpropanolamine following its administration in combination with chlorpheniramine maleate at 2200 hours."( Time dependent pharmacokinetic interaction between phenylpropanolamine and chlorpheniramine maleate in human subjects.
Rambhau, D; Rao, BR; Rao, VV; Srinivasu, P, 1999
)
0.3
" Improvements in drug delivery systems have altered drug bioavailability and pharmacokinetics."( Advancements in pharmacologic management of the overactive bladder.
Appell, RA; Dmochowski, RR, 2000
)
0.31
" Bioavailability varied between 2-20% in rodents and 58-63% in the dog."( Pharmacokinetics of tolterodine, a muscarinic receptor antagonist, in mouse, rat and dog. Interspecies relationship comparing with human pharmacokinetics.
Kankaanranta, S; Påhlman, I; Palmér, L, 2001
)
0.31
"To determine whether food intake influences the pharmacokinetics of a new, once daily, extended release (ER) capsule formulation of tolterodine in healthy volunteers, and to compare its bioavailability with that of the existing immediate release (IR) tablet."( Food does not influence the pharmacokinetics of a new extended release formulation of tolterodine for once daily treatment of patients with overactive bladder.
Olsson, B; Szamosi, J, 2001
)
0.31
"No effect of food on the bioavailability of tolterodine ER capsules was apparent and there was no sign of dose-dumping with meals."( Food does not influence the pharmacokinetics of a new extended release formulation of tolterodine for once daily treatment of patients with overactive bladder.
Olsson, B; Szamosi, J, 2001
)
0.31
" The relative bioavailability of ephedrine differed between the herbal supplement compared with the pharmaceutical formulation."( Mechanistic pharmacokinetic modelling of ephedrine, norephedrine and caffeine in healthy subjects.
Benowitz, NL; Csajka, C; Haller, CA; Verotta, D, 2005
)
0.33
"TCl, a quaternary amine, exhibits high solubility in water but low oral bioavailability (9."( Trospium chloride for the treatment of overactive bladder with urge incontinence.
Machado, C; Singh-Franco, D; Tuteja, S; Zapantis, A, 2005
)
0.33
"This study assessed the effect of the proton pump inhibitor omeprazole on the bioavailability of the extended-release formulations of oxybutynin and tolterodine."( Effect of the proton pump inhibitor omeprazole on the pharmacokinetics of extended-release formulations of oxybutynin and tolterodine.
Chen, A; Dmochowski, R; Gidwani, S; Gupta, S; MacDiarmid, S; Sathyan, G, 2005
)
0.33
" The validated LC-ESI-MS method has been used successfully to study tolterodine tartrate pharmacokinetic, bioavailability and bioequivalence in 20 healthy male volunteers."( High performance liquid chromatography-electrospray ionization mass spectrometric determination of tolterodine tartrate in human plasma.
Tian, Y; Xu, F; Zhang, B; Zhang, Z, 2005
)
0.33
" A prodrug approach was necessary for systemic bioavailability of 5-HMT after oral administration."( The design and development of fesoterodine as a prodrug of 5-hydroxymethyl tolterodine (5-HMT), the active metabolite of tolterodine.
Gandelman, K; Malhotra, B; Michel, MC; Sachse, R; Wood, N, 2009
)
0.35
" The data suggest that fesoterodine delivers 5-HMT consistently, regardless of CYP2D6 status, with up to 40% higher bioavailability compared with tolterodine."( Comparison of pharmacokinetic variability of fesoterodine vs. tolterodine extended release in cytochrome P450 2D6 extensive and poor metabolizers.
Crownover, P; Darsey, E; Fang, J; Glue, P; Malhotra, B, 2011
)
0.37
"49 mg/L, and the absolute bioavailability was 27."( Silicone adhesive, a better matrix for tolterodine patches-a research based on in vitro/in vivo studies.
Chen, Y; Fang, L; Li, C; Liu, C; Liu, J; Mu, L; Sun, L; Wang, Z; Xi, H, 2012
)
0.38
" The absolute bioavailability of tolterodine was 11."( Preparation, characterization and pharmacological evaluation of tolterodine hydrogels for the treatment of overactive bladder.
Li, Y; Liu, X; Shi, Y; Sui, C; Sun, F; Wu, Y; Zhou, Y, 2013
)
0.39
" In the pharmacokinetic studies, sustained-release over 24 h and absolute bioavailability of the hydrogels (24."( Design of transparent film-forming hydrogels of tolterodine and their effects on stratum corneum.
Dai, W; Fu, L; Li, Y; Liu, W; Liu, X; Sun, F; Teng, L; Wu, Y; Zhao, J, 2014
)
0.4

Dosage Studied

Plasma levels and blood pressure responses to two dosage regimens of phenylpropanolamine (PPA)-25-mg, immediate-release tablets three times per day and a 75-mg,. controlled-release capsule once per day--were compared in 14 normal subjects. The quantitative determinations of codeine phosphate, guaifenesin, pheniramine maleate,phenylpro Panolamine hydrochloride, and pyrilamine Maleate in a liquid dosage form are described.

ExcerptRelevanceReference
", ionic strength) to: (a) correlate in vitro release rates with bioavailability data, (b) discriminate between alternative formulations during dosage form development, or (c) serve as a selective control procedure for a series of sustanined-release dosage forms."( Continuous dissolution rate determination as a function of the pH of the medium.
Dauvois, M; Michaelis, AF; Turi, P, 1976
)
0.26
" This drug is preferred over ephedrine primarily because of its sustained release, allowing dosage twice a day, and because of its relative freedom from side effects."( Urethral pressure profiles before and after Ornade administration in patients with stress urinary incontinence.
Montague, DK; Stewart, BH, 1979
)
0.26
" Each child received a standard dosage of the study medicine according to a double-blind, crossover design."( A decongestant-antihistamine mixture in the prevention of otitis media in children with colds.
Hendley, JO; Randall, JE, 1979
)
0.26
"The quantitative determinations of codeine phosphate, guaifenesin, pheniramine maleate, phenylpropanolamine hydrochloride, and pyrilamine maleate in a liquid dosage form are described."( Quantitative determinations of codeine phosphate, guaifenesin, pheniramine maleate, phenylpropanolamine hydrochloride, and pyrilamine maleate in an expectorant by high-pressure liquid chromatography.
Ghanekar, AG; Gupta, VD, 1977
)
0.26
" Data are presented to illustrate the suitability of the method for dosage form bioavailability evaluation from plasma phenylpropanolamine levels achieved after acute oral administration of a typical dosage form."( Electron-capture GLC determination of phenylpropanolamine as a pentofluorophenyloxazolidine derivative.
Kostenbauder, HB; Neelakantan, L, 1976
)
0.26
" A simulation of the plasma levels during repeated administration indicated that dosing with the retard suspension at 12-h intervals should yield the same steady-state plasma levels as a 5 times daily administration of a divided dose of the aqueous solution, for both drugs."( Relative bioavailability of carbinoxamine and phenylpropanolamine from a retard suspension after single dose administration in healthy subjects.
Allemon, AM; Deroubaix, X; Laufen, H; Lebacq, E; Stockis, A, 1992
)
0.28
" However, in rats trained on caffeine, PPA had no effect on the dose-response relationship for caffeine; similarly, in rats trained on PPA, caffeine had no effect on the dose-response relationship for PPA (no synergism or antagonism)."( Drug discrimination studies in rats with caffeine and phenylpropanolamine administered separately and as mixtures.
Mariathasan, EA; Stolerman, IP, 1992
)
0.28
" Few data exist on the effect of long-term PPA dosing on blood pressure in normotensive or hypertensive patients."( The effect of multiple doses of phenylpropanolamine on the blood pressure of patients whose hypertension was controlled with beta blockers.
Gross, CR; O'Connell, MB, 1991
)
0.28
" In order to develop a convenient dosage of PPA, a transdermal preparation containing 250 mg PPA has been developed."( In-vivo pharmacokinetic characteristics of a transdermal phenylpropanolamine (PPA) preparation.
Devane, J; Foynes, M; Martin, M; Mulligan, S, 1991
)
0.28
" Dose-response curves for the effects of PPA and amphetamine (administered IP, 15 min presession) were then determined (ED50 = 35."( Evaluation of the pharmacological similarities between phenylpropanolamine and amphetamine: effects on schedule-controlled behavior.
Jarvis, MF; Wagner, GC, 1990
)
0.28
" Twenty-two percent of diet aid users and 7 percent of cold medicine users reported that they deliberately used more than the dosage recommended to improve efficacy."( Phenylpropanolamine and caffeine use among diet center clients.
Lake, CR; Quirk, R; Rosenberg, D, 1990
)
0.28
" Blood pressures (supine and sitting) and heart rates measured at the time of blood sampling after the administration of the PPA HCl dosage forms demonstrated no clinically significant relationship between cardiovascular response and PPA HCl plasma concentration."( Bioavailability and cardiovascular safety of Dexatrim (phenylpropanolamine hydrochloride) from a controlled-release caplet.
Brisson, J; Cohen, P; Dennis, S; Shargel, L; Silverman, HI, 1990
)
0.28
" The pharmacokinetics of PPA were found to be linear in the dosage range 25 to 100 mg."( Steady state pharmacokinetics and dose-proportionality of phenylpropanolamine in healthy subjects.
Dowse, R; Kanfer, I; Scherzinger, SS, 1990
)
0.28
" Thus, different dose-response curves were generated depending upon whether cathine or vehicle was administered the day before testing."( Discriminative stimulus properties of (+)cathine, an alkaloid of the khat plant.
Pehek, EA; Schechter, MD, 1990
)
0.28
" Dosage forms studied were PPA 75 mg sustained release, PPA 25 mg, and placebo."( Subjective profile of phenylpropanolamine: absence of stimulant or euphorigenic effects at recommended dose levels.
Blackburn, GL; Funderburk, FR; Morgan, JP; Noble, R, 1989
)
0.28
" Serum samples were taken at set time intervals and assayed for phenylpropanolamine content, thus allowing blood drug levels to be correlated with the position of the dosage form in the GI tract."( Correlation of phenylpropanolamine bioavailability with gastrointestinal transit by scintigraphic monitoring of 111In-labeled hydroxypropylmethylcellulose matrices.
Davis, SS; Feely, LC, 1989
)
0.28
" Reserpinization shifted the (-)-norephedrine dose-response curve slightly to the right, indicating that only a minor portion of its activity is due to the release of stored endogenous catecholamines."( Adrenergic receptor subtype activation by (+)-, (-)- and (+/-)-norephedrine in the pithed rat.
Maher, TJ; Moya-Huff, FA, 1987
)
0.27
" They are unrelated to duration or dosage of treatment."( [Benign cerebral angiopathies and phenylpropanolamine].
Haguenau, M; Laplane, D; Le Coz, P; Pépin, B; Rougemont, D; Sanson, M; Woimant, F, 1988
)
0.27
" Dosage forms studied were PPA 75 mg sustained-release (SR), PPA SR 75 mg with caffeine 200 mg, caffeine 200 mg, and placebo."( A controlled clinical trial of the cardiovascular and psychological effects of phenylpropanolamine and caffeine.
Noble, R, 1988
)
0.27
" The tendency of PPA to produce tachyphylaxis was evaluated by rhinomanometrie measurements of nasal airway resistance after repeated dose-response provocations."( Influence of topical phenylpropanolamine on tachyphylaxis and mucociliary clearance in the human nose.
Bende, M; Holmberg, K, 1988
)
0.27
"We believe that consumers often assume that double the recommended dosage of an OTC drug is safe and more effective."( A double dose of phenylpropanolamine causes transient hypertension.
Chernow, B; Clymer, R; Lake, CR; Quirk, RM; Zaloga, G, 1988
)
0.27
" Prior reserpinization did not significantly shift the cumulative dose-response curves for l-NOR and PPA."( Cardiovascular differences between phenylpropanolamine and its related norephedrine isomers in the rat.
Kiritsy, PJ; Maher, TJ; Moya-Huff, FA, 1987
)
0.27
" dosing regimen and placebo."( Phenylpropanolamine: effects on subjective and cardiovascular variables at recommended over-the-counter dose levels.
Bigelow, G; Funderburk, FR; Griffiths, RR; Liebson, I, 1987
)
0.27
" One such case is reported in which a self administered high dosage of such a medication can be linked with a potentially life threatening anaesthetic complication."( Contac 400: a possible cause of aspiration under anaesthesia.
Wilkinson, DJ, 1987
)
0.27
" We monitored the effects of acute and chronic PPA dosing using 24-hour ambulatory blood pressure recording as a sensitive method of monitoring blood pressure variability."( The effect of phenylpropanolamine on ambulatory blood pressure.
Barlascini, CO; Goodman, RP; Lambert, CM; McKenney, JM; Wright, JT, 1986
)
0.27
" Plasma concentration data following one 25-mg dose of phenylpropanolamine hydrochloride in four healthy volunteers illustrates the suitability of this analytical method for monitoring plasma levels after oral administration of a typical dosage form."( Electron-capture capillary gas chromatographic determination of phenylpropanolamine in human plasma following derivatization with trifluoroacetic anhydride.
Bayne, WF; Crisologo, N; Dye, D, 1984
)
0.27
"A high-performance liquid chromatographic (HPLC) method has been developed for the quantitation of acetaminophen, chlorpheniramine maleate, dextromethorphan hydrobromide, and phenylpropanolamine hydrochloride in combination in pharmaceutical dosage forms using a single column and three different mobile phases."( Quantitation of acetaminophen, chlorpheniramine maleate, dextromethorphan hydrobromide, and phenylpropanolamine hydrochloride in combination using high-performance liquid chromatography.
Das Gupta, V; Heble, AR, 1984
)
0.27
"An impurity present in all commercial guaifenesin-containing dosage forms examined was isolated and identified as 2-(2-methoxyphenoxy) 1,3-propanediol (VI)."( Determination of the structure of a synthetic impurity in guaifenesin: modification of a high-performance liquid chromatographic method for phenylephrine hydrochloride, phenylpropanolamine hydrochloride, guaifenesin, and sodium benzoate in dosage forms.
Lubey, GS; Newby, DG; Schieffer, GW; Smith, WO, 1984
)
0.27
"Plasma levels and blood pressure responses to two dosage regimens of phenylpropanolamine (PPA)-25-mg, immediate-release tablets three times per day and a 75-mg, controlled-release capsule once per day--were compared in 14 normal subjects."( Comparison of effects of two dosage regimens of phenylpropanolamine on blood pressure and plasma levels in normal subjects under steady-state conditions.
Dolan, MM; Doyne, N; Saltzman, MB, 1983
)
0.27
" The sustained-release action of the dosage form was consistent in all subjects, with a flat plasma concentration-time profile between 2 and 8 h after dose intake."( Steady-state kinetics of sustained-release phenylpropanolamine.
Grahnén, A; Lindström, B; Lönnerholm, G, 1984
)
0.27
" These mixtures gave varying drug release profiles that showed rank-order correlation with plasma concentration profiles obtained in bioavailability studies with suspension dosage forms."( Sustained-release drug delivery system I: Coated ion-exchange resin system for phenylpropanolamine and other drugs.
Amsel, L; Bryant, W; Hinsvark, O; Raghunathan, Y, 1981
)
0.26
" Application of the proposed NMR spectroscopic method to commercial dosage forms, including ephedrine sulfate injections and pseudoephedrine hydrochloride tablets, yielded assay results ranging from 97."( Determination of ephedrine, pseudoephedrine, and norephedrine in mixtures (bulk and dosage forms) by proton nuclear magnetic resonance spectroscopy.
Hanna, GM,
)
0.13
" Two dosage forms were administered orally to beagle dogs."( Evaluation of the correlation between in vivo and in vitro release. Effect of the force of contraction and food on drug release.
Ando, H; Aoki, S; Ida, K; Ishii, M; Ozawa, H; Watanabe, S, 1994
)
0.29
" Second, dose-response relationships for phenylpropanolamine and acetaminophen were such that increased toxicity was observed only when the interaction was sufficient to lower hepatic glutathione concentrations below a level regarded as critical in preventing acetaminophen-induced hepatotoxicity."( Phenylpropanolamine potentiation of acetaminophen-induced hepatotoxicity: evidence for a glutathione-dependent mechanism.
Harbison, RD; James, RC; Roberts, SM, 1993
)
0.29
"5 mg/kg twice a day (phenylpropanolamine) as an initial dosage and to reduce this step by step to the lowest dosage that keeps the dog continent."( [Urinary incontinence in castrated female dogs. 2. Therapy].
Blendinger, C; Blendinger, K; Bostedt, H, 1995
)
0.29
" Tolterodine, in the dosage used, was both objectively and subjectively shown to exert a marked inhibitory effect on micturition in healthy subjects, and the data suggest a more pronounced effect on bladder function than on salivation."( Urodynamic and other effects of tolterodine: a novel antimuscarinic drug for the treatment of detrusor overactivity.
Andersson, KE; Ekström, B; Mattiasson, A; Sparf, B; Stahl, MM, 1995
)
0.29
" Before dosing and at intervals up to 7 hours after dosing, serum pseudoephedrine or phenylpropanolamine concentrations were measured, and pulse and blood pressure were recorded."( Pharmacokinetics of the orally administered decongestants pseudoephedrine and phenylpropanolamine in children.
Gu, X; Simons, FE; Simons, KJ; Watson, WT, 1996
)
0.29
" An optimal efficacy/side-effect profile is obtained with tolterodine, at a dosage of 1 or 2 mg twice daily, which seems to have less propensity to cause dry mouth than the currently available antimuscarinic drugs."( Tolterodine--a new bladder selective muscarinic receptor antagonist: preclinical pharmacological and clinical data.
Hallén, B; Larsson, G; Nilvebrant, L, 1997
)
0.3
"To investigate the efficacy and safety of tolterodine, a new antimuscarinic agent, and define the optimum dosage in patients with symptoms of detrusor instability (urgency, increased frequency of micturition and/or urge incontinence)."( Efficacy and safety of tolterodine in patients with detrusor instability: a dose-ranging study.
Abrams, P; Cardozo, L; Fall, M; Nelson, E; Rentzhog, L; Stanton, SL, 1998
)
0.3
" at a dosage of 2 mg twice daily, the frequency of micturition, episodes of incontinence and pad use were reduced by 20%, 46% and 29%, respectively, while the volume at first contraction increased by 89 mL."( Efficacy and safety of tolterodine in patients with detrusor instability: a dose-ranging study.
Abrams, P; Cardozo, L; Fall, M; Nelson, E; Rentzhog, L; Stanton, SL, 1998
)
0.3
" The optimum dosage appears to be 1-2 mg twice daily."( Efficacy and safety of tolterodine in patients with detrusor instability: a dose-ranging study.
Abrams, P; Cardozo, L; Fall, M; Nelson, E; Rentzhog, L; Stanton, SL, 1998
)
0.3
" Only minor differences in pharmacodynamic effects after tolterodine dosage were observed between the groups."( Influence of CYP2D6 polymorphism on the pharmacokinetics and pharmacodynamic of tolterodine.
Alván, G; Bertilsson, L; Brynne, N; Dalén, P; Gabrielsson, J, 1998
)
0.3
" In order to assess the optimum dosage for use in future clinical studies, a double-blind, randomized, placebo-controlled, parallel-group, multicenter study was performed in 90 patients with detrusor hyperreflexia and symptoms of urinary urgency, frequency, and/or urge incontinence."( Dose-ranging study of tolterodine in patients with detrusor hyperreflexia.
Amarenco, G; Lock, MT; Madersbacher, HG; Messelink, EJ; Soler, JM; Thüroff, JW; Van Kerrebroeck, PE, 1998
)
0.3
" The present work suggests that Rhinopront is an effective nasal decongestant in adults and children with acute congestive rhinitis and supports the adequacy of the proposed twice-daily dosing rate."( Exploratory study of the decongestive effect of Rhinopront syrup in adults and in children with acute rhinitis.
Calderon, P; Deroubaix, X; Gline, JP; Joue, P; Lebacq, E; Schwegler, F; Stockis, A; Van Schoor, O, 1994
)
0.29
" Despite short terminal disposition half-lives of 2-3 and 3-4 hours for tolterodine and its active 5-hydroxy metabolite, respectively, twice/day dosing is effective due to the drug's prolonged pharmacodynamic effects."( Tolterodine, a new antimuscarinic drug for treatment of bladder overactivity.
Guay, DR, 1999
)
0.3
" A dosage of 4 mg twice daily was, however, associated with an increase in residual urinary volume."( Tolterodine in the treatment of overactive bladder: analysis of the pooled phase II efficacy and safety data.
Hallén, B; Larsson, G; Nilvebrant, L, 1999
)
0.3
" The optimal dosage is 1 to 2 mg twice daily, irrespective of metabolic phenotype."( Tolterodine in the treatment of overactive bladder: analysis of the pooled phase II efficacy and safety data.
Hallén, B; Larsson, G; Nilvebrant, L, 1999
)
0.3
" Drug dosage in the 20 patients who tolerated tolterodine was 1 mg bid in 3 and 2 mg bid in 17 (85%)."( Tolterodine for overactive bladder: time to onset of action, preferred dosage, and 9-month follow-up.
Atan, A; Chancellor, MB; Erickson, JR; Kim, DY; Konety, BR; Yokoyama, T, 1999
)
0.3
" The adverse effect profiles of tolterodine and oxybutynin are similar; however, comparative clinical trials have shown significantly fewer patients taking tolterodine require dosage reductions or discontinue therapy due to antimuscarinic adverse effects such as dry mouth."( Tolterodine use for symptoms of overactive bladder.
Morgenstern, NE; Ruscin, JM, 1999
)
0.3
" The warfarin dosage had remained constant for many weeks in both patients prior to and during the tolterodine trials."( Tolterodine-warfarin drug interaction.
Colucci, VJ; Rivey, MP, 1999
)
0.3
" In the first 3 h after administration of PPA, there was a dose-response increase in the systolic and diastolic blood pressures, which then returned to baseline."( Effects of sustained-release oral phenylpropanolamine on the nasal mucosa of healthy subjects.
Graf, P; Hallén, H; Palm, J; Toll, K, 1999
)
0.3
" Similarly, the potential improvements in tolerability associated with different dosage formulations of oxybutynin, and the clinical utility of S-oxybutynin, are yet to be conclusively demonstrated."( Muscarinic receptor antagonists in the treatment of overactive bladder.
Chapple, CR, 2000
)
0.31
" Experimental studies in pregnant rabbits using Primatene in both low and high dosage resulted in limb reduction defects and other malformations in a significant number of the offspring compared with controls."( Association of sympathomimetic drugs with malformations.
Drut, RM; Gilbert-Barness, E, 2000
)
0.31
" The distribution pattern after repeat oral dosing was similar to that after a single dose, although the decline in tissue concentrations was slower."( Tissue distribution of tolterodine, a muscarinic receptor antagonist, and transfer into fetus and milk in mice.
d'Argy, R; Nilvebrant, L; Påhlman, I, 2001
)
0.31
" The intestinal absorption of tolterodine after oral dosing was almost complete in all three species, with peak serum concentrations observed within 1 hour post-dose."( Pharmacokinetics of tolterodine, a muscarinic receptor antagonist, in mouse, rat and dog. Interspecies relationship comparing with human pharmacokinetics.
Kankaanranta, S; Påhlman, I; Palmér, L, 2001
)
0.31
"There were no safety concerns in terms of the change in residual urinary volume for any of the three dosage groups; values were comparable with baseline after 2 weeks of treatment for all three dosages."( The overactive bladder in children: a potential future indication for tolterodine.
Hellström, AL; Hjälmås, K; Läckgren, G; Mogren, K; Stenberg, A, 2001
)
0.31
" Topical phenylpropanolamine (1%) and d-pseudoephedrine (1%) 45 minutes after dosing increased blood pressure +44 and +17 mmHg, respectively, over control animals."( Comparative oral and topical decongestant effects of phenylpropanolamine and d-pseudoephedrine.
Egan, RW; Erickson, CH; Hey, JA; McLeod, RL; Mingo, GG; Pedersen, OF,
)
0.13
" Dosage reduction occurred in 13% of patients."( Treatment of overactive bladder: long-term tolerability and efficacy of tolterodine.
Abrams, P; Appell, RA; Drutz, HP; Millard, R; Van Kerrebroeck, PE; Wein, A, 2001
)
0.31
" Simultaneous determination of these three drugs: anorexic, central nervous stimulant and tranquilizer, respectively, in pharmaceutical dosage forms has not been reported."( Analysis of multicomponent formulations containing phenylpropanolamine hydrochloride, caffeine and diazepam by using LC.
Ferreyra, C; Ortiz, C, 2001
)
0.31
" Neither dosage of tolterodine was associated with serious drug-related adverse events during the study."( Tolterodine: a safe and effective treatment for older patients with overactive bladder.
Malone-Lee, JG; Maugourd, MF; Walsh, JB, 2001
)
0.31
"Tolterodine (taken for 4 weeks) is safe and shows efficacy, particularly at a dosage of 2 mg bid, in the treatment of older patients with urinary symptoms attributable to overactive bladder."( Tolterodine: a safe and effective treatment for older patients with overactive bladder.
Malone-Lee, JG; Maugourd, MF; Walsh, JB, 2001
)
0.31
" Dosage reduction to 1 mg twice daily was required in 23% of patients."( Twelve-month treatment of overactive bladder: efficacy and tolerability of tolterodine.
Abrams, P; Jacquetin, B; Jonas, U; Malone-Lee, J; Tammela, T; Wein, A; Wyndaele, JJ, 2001
)
0.31
" We explore the toxicities of OTC cough and cold medications, discuss mechanisms of dosing errors, and suggest why physicians should be more vigilant in specifically inquiring about OTCs when evaluating an ill child."( Toxicity of over-the-counter cough and cold medications.
Gunn, VL; Liebelt, EL; Serwint, JR; Taha, SH, 2001
)
0.31
" Pharmacokinetic assessments were performed on day 14 based on plasma levels of ethinyl estradiol and levonorgestrel up to 24 hours after dosing and serum tolterodine levels at 1 to 3 hours after dosing."( The effect of tolterodine on the pharmacokinetics and pharmacodynamics of a combination oral contraceptive containing ethinyl estradiol and levonorgestrel.
Landgren, BM; Olsson, B, 2001
)
0.31
" The convenience of once-daily dosing of antimuscarinic agents would be expected to improve patient compliance and further relieve the symptoms of OAB."( Once-daily, extended-release formulations of antimuscarinic agents in the treatment of overactive bladder: a review.
Rovner, ES; Wein, AJ, 2002
)
0.31
" Therefore, these results suggest that the normal dosage of tolterodine (2 mg twice daily) may have less effect on visual accommodation than the equivalent dosage of oxybutynin (5 mg three times daily) in patients with an overactive bladder."( Tolterodine: selectivity for the urinary bladder over the eye (as measured by visual accommodation) in healthy volunteers.
Chapple, CR; Nilvebrant, L, 2002
)
0.31
" The dose was titrated until effective (onset of complete diurnal urinary continence), maximal recommended dosage was achieved or bothersome anticholinergic side effects developed."( Therapeutic efficacy of extended release oxybutynin chloride, and immediate release and long acting tolterodine tartrate in children with diurnal urinary incontinence.
Crocker, J; Reinberg, Y; Vandersteen, D; Wolpert, J, 2003
)
0.32
"The aim of the study was to assess the effect of maximal therapeutic dosing of sympathomimetic amines found in over-the-counter (OTC) decongestant preparations on endurance running."( Physiological, subjective and performance effects of pseudoephedrine and phenylpropanolamine during endurance running exercise.
Chester, N; Mottram, DR; Reilly, T, 2003
)
0.32
"A newly designed flow-through type dissolution test method (FT method) was applied to predict in vivo drug release behaviors in dogs of controlled-release multiple unit dosage forms."( Prediction of in vivo drug release behavior of controlled-release multiple-unit dosage forms in dogs using a flow-through type dissolution test method.
Ikegami, K; Kobayashi, M; Osawa, T; Tagawa, K, 2003
)
0.32
" Sympathomimetic dosage and type, time interval until stroke onset, and neuroimaging findings are described."( Stroke associated with sympathomimetics contained in over-the-counter cough and cold drugs.
Arauz, A; Barinagarrementeria, F; Cantu, C; López, M; Murillo-Bonilla, LM, 2003
)
0.32
" Peak plasma concentrations of oxybutynin and the major active metabolite, N-desethyloxybutynin, are reached 24 - 48 hours after a single application and therapeutic concentrations are maintained throughout the dosage interval."( Transdermal oxybutynin: for overactive bladder.
Bang, LM; Easthope, SE; Perry, CM, 2003
)
0.32
" New antimuscarinic anticholinergic medications have improved the treatment of OAB, offering patients efficacy equal to that of immediate-release oxybutynin with fewer side effects and an improved dosing schedule."( Overactive bladder: improving the efficacy of anticholinergics by dose escalation.
MacDiarmid, SA, 2003
)
0.32
"To study the elimination of ephedrines with reference to the International Olympic Committee (IOC) doping control cut-off levels, following multiple dosing of over-the-counter decongestant preparations."( Elimination of ephedrines in urine following multiple dosing: the consequences for athletes, in relation to doping control.
Chester, N; Mottram, DR; Powell, M; Reilly, T, 2004
)
0.32
"To evaluate the dose-response relationship and safety/tolerability of solifenacin succinate (YM905) in the treatment of overactive bladder (OAB), and to compare its efficacy and safety/tolerability with tolterodine 2 mg twice daily."( Solifenacin appears effective and well tolerated in patients with symptomatic idiopathic detrusor overactivity in a placebo- and tolterodine-controlled phase 2 dose-finding study.
Araño, P; Bosch, JL; Chapple, CR; De Ridder, D; Kramer, AE; Ridder, AM, 2004
)
0.32
"To assess in a phase 3a trial the efficacy of solifenacin succinate, a once-daily oral antimuscarinic agent in development at 5-mg and 10-mg dosage strengths, for the treatment of overactive bladder (OAB) (Yamanouchi Pharmaceutical Co."( Randomized, double-blind placebo- and tolterodine-controlled trial of the once-daily antimuscarinic agent solifenacin in patients with symptomatic overactive bladder.
Al-Shukri, S; Chapple, CR; Everaert, K; Huang, M; Meffan, P; Rechberger, T; Ridder, A, 2004
)
0.32
" The efficacy of oxybutynin chloride has been sufficiently proved; however its dosage and side effects, although scarce in children, usually cause treatment discontinuation."( [Treatment of bladder instability (non-neurogenic hyperactive bladder) in children, with tolterodine].
Caffaratti Sfulcini, J; de la Peña, E; Garat Barredo, JM, 2004
)
0.32
" These findings suggest that there should not be a need for routine adjustment of tolterodine dosage in the presence of duloxetine."( Effect of duloxetine on tolterodine pharmacokinetics in healthy volunteers.
Chan, C; Gonzales, CR; Hua, TC; Knadler, MP; Pan, A; Poo, YK; Skinner, MH; Wise, SD, 2004
)
0.32
" Clinically relevant drug interactions are limited to cytochrome P450 3A4 inhibitors, such as ketoconazole, and co-administration with such agents warrants a tolterodine dosage decrease."( Benefit-risk assessment of tolterodine in the treatment of overactive bladder in adults.
Burrows, L; Garely, AD, 2004
)
0.32
" Tolterodine at the recommended dosage of 2 mg twice daily improves incontinence and bladder volumes compared with placebo, and without significant dry mouth."( Efficacy and safety of tolterodine in people with neurogenic detrusor overactivity.
Bard, RJ; Casey, AR; Ethans, KD; Nance, PW; Schryvers, OI, 2004
)
0.32
" While trospium chloride dosage adjustments based on age or sex appear unwarranted, such adjustments may be needed in patients with severe renal impairment."( Trospium chloride in the management of overactive bladder.
Rovner, ES, 2004
)
0.32
" This finding may be explained by a high placebo response and under dosage of tolterodine among children with greater body weight."( Tolterodine treatment for children with symptoms of urinary urge incontinence suggestive of detrusor overactivity: results from 2 randomized, placebo controlled trials.
Borgstein, NG; Djurhuus, JC; Ellsworth, P; Nijman, RJ, 2005
)
0.33
" Exploratory analyses also showed that children weighing 35 kg or less with detrusor overactivity characterized by incontinence and/or frequent voiding benefited most from tolterodine treatment, suggesting that a weight adjusted dosing regimen may be required for optimal response among older and heavier children."( Tolterodine treatment for children with symptoms of urinary urge incontinence suggestive of detrusor overactivity: results from 2 randomized, placebo controlled trials.
Borgstein, NG; Djurhuus, JC; Ellsworth, P; Nijman, RJ, 2005
)
0.33
" In conclusion, the present method could be potentially applied to prepare controlled release drug delivery beads or pellet dosage forms."( Reparation of controlled release spheronized beads by simple extrusion and modified spheronization process.
Hwang, SJ; Jun, SW; Kim, MS; Lee, S; Park, JS, 2005
)
0.33
"Solifenacin, with a flexible dosing regimen, showed greater efficacy to tolterodine in decreasing urgency episodes, incontinence, urge incontinence and pad usage and increasing the volume voided per micturition."( A comparison of the efficacy and tolerability of solifenacin succinate and extended release tolterodine at treating overactive bladder syndrome: results of the STAR trial.
Bolodeoku, J; Chapple, CR; Drogendijk, T; Martinez-Garcia, R; Selvaggi, L; Toozs-Hobson, P; Warnack, W; Wright, DM, 2005
)
0.33
"Solifenacin, with a flexible dosing regimen, was found to be superior to tolterodine ER with respect to the majority of the efficacy variables."( A comparison of the efficacy and tolerability of solifenacin succinate and extended release tolterodine at treating overactive bladder syndrome: results of the STAR trial.
Bolodeoku, J; Chapple, CR; Drogendijk, T; Martinez-Garcia, R; Selvaggi, L; Toozs-Hobson, P; Warnack, W; Wright, DM, 2005
)
0.33
" We urodynamically evaluated the dose and concentration effects of tolterodine to establish safe and effective dosing regimens."( Use of tolterodine in children with neurogenic detrusor overactivity: relationship between dose and urodynamic response.
Borgstein, NG; Ellsworth, PI; Nijman, RJ; Reddy, PP, 2005
)
0.33
" PK was assessed after 8 weeks, urodynamic assessments were conducted after each 4-week dosing period and 3-day micturition diaries were completed."( Use of tolterodine in children with neurogenic detrusor overactivity: relationship between dose and urodynamic response.
Borgstein, NG; Ellsworth, PI; Nijman, RJ; Reddy, PP, 2005
)
0.33
" In study 3 (11 patients) there were no obvious dose-response relationships."( Use of tolterodine in children with neurogenic detrusor overactivity: relationship between dose and urodynamic response.
Borgstein, NG; Ellsworth, PI; Nijman, RJ; Reddy, PP, 2005
)
0.33
"These results support the safety of age and body weight adjusted dosing regimens for further clinical evaluation of tolterodine in children with neurogenic detrusor overactivity."( Use of tolterodine in children with neurogenic detrusor overactivity: relationship between dose and urodynamic response.
Borgstein, NG; Ellsworth, PI; Nijman, RJ; Reddy, PP, 2005
)
0.33
" The antagonistic effect of oral tolterodine on the dose-response curves to pilocarpine was significantly weaker than that of oxybutynin."( Characterization of muscarinic receptor binding and inhibition of salivation after oral administration of tolterodine in mice.
Maruyama, S; Oki, T; Takagi, Y; Yamada, S; Yamamura, HI, 2006
)
0.33
"To evaluate the efficacy and tolerability of nighttime tolterodine dosing on urgency-related micturitions in patients with overactive bladder (OAB) and nocturia."( Nighttime dosing with tolterodine reduces overactive bladder-related nocturnal micturitions in patients with overactive bladder and nocturia.
Guan, Z; Rackley, R; Rovner, ES; Wang, JT; Weiss, JP, 2006
)
0.33
" Adverse events associated with nighttime dosing of TER versus placebo were few."( Nighttime dosing with tolterodine reduces overactive bladder-related nocturnal micturitions in patients with overactive bladder and nocturia.
Guan, Z; Rackley, R; Rovner, ES; Wang, JT; Weiss, JP, 2006
)
0.33
" Nighttime dosing with TER was associated with few adverse events and adverse event-related withdrawals."( Nighttime dosing with tolterodine reduces overactive bladder-related nocturnal micturitions in patients with overactive bladder and nocturia.
Guan, Z; Rackley, R; Rovner, ES; Wang, JT; Weiss, JP, 2006
)
0.33
" On her next anticoagulation clinic visit, the patient's INR had increased, although the dosage of warfarin had been reduced when the tolterodine had been prescribed."( Probable interaction between tolterodine and warfarin.
Taylor, JR, 2006
)
0.33
"The dosage of the antimuscarinic drugs: Tolterodine ER or Trospium was increased to a higher-than-recommended dosage in patients where the manufacturer's recommended dosage had failed."( Neurogenic bladder treatment by doubling the recommended antimuscarinic dosage.
Aguilar, Y; Horstmann, M; Schaefer, T; Sievert, KD; Stenzl, A, 2006
)
0.33
" If neurogenic detrusor overactivity continued and the medication was well tolerated, the dosage was doubled to either 8 mg of Tolterodine ER [2 x 4 mg (n = 11)] or 90 mg of Trospium [3 x 30 mg (n = 10)]."( Neurogenic bladder treatment by doubling the recommended antimuscarinic dosage.
Aguilar, Y; Horstmann, M; Schaefer, T; Sievert, KD; Stenzl, A, 2006
)
0.33
"The increased dosage of Tolterodine or Trospium is an effective treatment in patients with neurogenic bladder."( Neurogenic bladder treatment by doubling the recommended antimuscarinic dosage.
Aguilar, Y; Horstmann, M; Schaefer, T; Sievert, KD; Stenzl, A, 2006
)
0.33
"To evaluate the efficacy and safety of nighttime dosing with tolterodine extended release (TER) in men with overactive bladder (OAB) and nocturia."( Tolterodine extended release improves overactive bladder symptoms in men with overactive bladder and nocturia.
Dmochowski, R; Guan, Z; Kaplan, SA; Roehrborn, CG; Rovner, ES; Wang, JT, 2006
)
0.33
"Nighttime TER dosing reduced urgency-related micturitions and was well tolerated in men with OAB and nocturia."( Tolterodine extended release improves overactive bladder symptoms in men with overactive bladder and nocturia.
Dmochowski, R; Guan, Z; Kaplan, SA; Roehrborn, CG; Rovner, ES; Wang, JT, 2006
)
0.33
" Thus, the proposed method is simple and suitable for the simultaneous analysis of active ingredients in tablet dosage forms."( Method development and validation for the simultaneous determination of cetirizine dihydrochloride, paracetamol, and phenylpropanolamine hydrochloride in tablets by capillary zone electrophoresis.
Azhagvuel, S; Sekar, R, 2007
)
0.34
" In women, linear trends were also found in recency, duration, and dosage of PPA exposure."( Phenylpropanolamine contained in cold remedies and risk of hemorrhagic stroke.
Bae, HJ; Cho, KH; Chung, DK; Han, MK; Hong, KS; Jeong, SW; Kim, JS; Lee, BC; Lee, SH; Lee, SM; Lee, YS; Park, BJ; Park, JM; Yoo, KM; Yoon, BW; Yu, KH, 2007
)
0.34
" It is a rare complication of therapy for overactive bladder and resolved when dosage was reduced to 1 mg, although overactive bladder symptoms were still controlled."( Cognitive dysfunction with tolterodine use.
Bolis, P; Cardozo, L; Salvatore, S; Serati, M; Uccella, S, 2007
)
0.34
"To evaluate the efficacy of tamsulosin oral-controlled absorption system (OCAS) vs placebo in overactive bladder (OAB), to evaluate the safety and tolerability of once-daily dosing with tamsulosin OCAS, and to compare the efficacy and safety with tolterodine extended-release (ER)."( A randomized double-blind placebo-controlled multicentre study to explore the efficacy and safety of tamsulosin and tolterodine in women with overactive bladder syndrome.
Bolodeoku, J; Cardozo, L; Robinson, D; Terpstra, G, 2007
)
0.34
" This article summarizes the efficacy, contraindications, precautions, dosing and common side effects of these agents."( Pharmacologic management of overactive bladder.
Hilas, O; Lam, S, 2007
)
0.34
"14]) but did not resolve urinary incontinence, with no significant dose-response association."( Systematic review: randomized, controlled trials of nonsurgical treatments for urinary incontinence in women.
Kane, RL; Shamliyan, TA; Wilt, TJ; Wyman, J, 2008
)
0.35
" Ethylcellulose (EC) layered granulation by a fluidized bed granulator might be convenient for the preparation of controlled release dosage forms as compared with a tumbling granulator, because the layered granules prepared by the fluidized bed granulator can granulate and dry at the same time."( Analysis of the release process of phenylpropanolamine hydrochloride from ethylcellulose matrix granules V. Release properties of ethylcellulose layered matrix granules.
Fujii, R; Fukui, A; Sunada, H; Yonezawa, Y, 2008
)
0.35
"A 1-year Markov model was constructed using data from a 12-week, randomised, double-blind study that compared flexible dosing with solifenacin (5 mg and 10 mg) with tolterodine (IR 2 mg bd/ER 4 mg) in adults with OAB."( A cost-utility analysis of once daily solifenacin compared to tolterodine in the treatment of overactive bladder syndrome.
Bolodeoku, J; Khullar, V; Mundy, A; Odeyemi, I; Speakman, M, 2008
)
0.35
"Flexible dosing with solifenacin is likely to be cost-effective versus tolterodine in the treatment of OAB."( A cost-utility analysis of once daily solifenacin compared to tolterodine in the treatment of overactive bladder syndrome.
Bolodeoku, J; Khullar, V; Mundy, A; Odeyemi, I; Speakman, M, 2008
)
0.35
"Only patients with primary nocturnal enuresis refractory to the maximal dosage of desmopressin were enrolled."( Combination therapy with desmopressin and an anticholinergic medication for nonresponders to desmopressin for monosymptomatic nocturnal enuresis: a randomized, double-blind, placebo-controlled trial.
Austin, PF; Campigotto, MJ; Coplen, DE; Ferguson, G; Royer, ME; Yan, Y, 2008
)
0.35
" Therefore, in contrast to tolterodine, no reduction of fesoterodine dosage is required under conditions of reduced elimination."( The pharmacokinetic profile of fesoterodine: similarities and differences to tolterodine.
Malhotra, B; Simon, HU, 2009
)
0.35
"The purpose of the present analysis was to analyze and compare the cost-effectiveness of solifenacin flexible dosing (5-10 mg) with tolterodine 4 mg sustained release (SR) or placebo (assumed to be comparable to no treatment) for patients with overactive bladder (OAB) symptoms."( Cost-effectiveness analysis of solifenacin flexible dosing in patients with overactive bladder symptoms in four Nordic countries.
Axelsen, S; Kulseng-Hansen, S; Mattiasson, A; Milsom, I; Nilsson, CG; Wickstrøm, J, 2009
)
0.35
"Solifenacin flexible dosing was more effective with respect to reducing OAB symptoms compared to both placebo and tolterodine 4 mg."( Cost-effectiveness analysis of solifenacin flexible dosing in patients with overactive bladder symptoms in four Nordic countries.
Axelsen, S; Kulseng-Hansen, S; Mattiasson, A; Milsom, I; Nilsson, CG; Wickstrøm, J, 2009
)
0.35
"Solifenacin flexible dosing was a cost-effective treatment alternative compared to tolterodine 4 mg SR."( Cost-effectiveness analysis of solifenacin flexible dosing in patients with overactive bladder symptoms in four Nordic countries.
Axelsen, S; Kulseng-Hansen, S; Mattiasson, A; Milsom, I; Nilsson, CG; Wickstrøm, J, 2009
)
0.35
" Drug pharmacokinetics was studied after transdermal application to human volunteers compared to the commercial oral dosage form using a newly developed LC-MS/MS assay."( Utility of nanosized microemulsion for transdermal delivery of tolterodine tartrate: ex-vivo permeation and in-vivo pharmacokinetic studies.
Elshafeey, AH; Fathallah, MM; Kamel, AO, 2009
)
0.35
" At least partially due to the avoidance of variations in pharmacokinetic exposures observed with tolterodine, it was possible to develop fesoterodine with the flexibility of two efficacious and well-tolerated dosage regimens of 4 and 8 mg daily."( The design and development of fesoterodine as a prodrug of 5-hydroxymethyl tolterodine (5-HMT), the active metabolite of tolterodine.
Gandelman, K; Malhotra, B; Michel, MC; Sachse, R; Wood, N, 2009
)
0.35
"Although there is a rich body of research available regarding the effect of acute and chronic khat dosing in animal models, research on the behavioral and cognitive effects of khat in human subjects is not extensive and several of the available studies have been done only in the context of observational and single-case studies."( Khat use and neurobehavioral functions: suggestions for future studies.
Al'Absi, M; Hoffman, R, 2010
)
0.36
"In this large group of older patients, flexibly dosed solifenacin was associated with reductions in diary-documented OAB symptoms (VERSUS)."( Efficacy and tolerability of solifenacin in patients aged ≥ 65 years with overactive bladder: post-hoc analysis of 2 open-label studies.
Capo', JP; Forero-Schwanhaeuser, S; He, W; Lucente, V, 2011
)
0.37
" The role of the compounding pharmacist was vital to achieve appropriate dosing of a drug no longer commercially available."( Medical therapy for acquired urinary incontinence in dogs.
Griffin, K; Hill, K; Jordan, D; Mays, AA; Ray, J,
)
0.13
" Therefore, the developed sustained-release tablet formulation of TOL could be an alternative dosage form to the SR capsule for treatment of OAB."( Preparation and evaluation of once-daily sustained-release coated tablets of tolterodine-L-tartrate.
Chang, SW; Kim, JO; Kim, YI; Pradhan, R, 2014
)
0.4
" Each patient's demographic and clinical characteristics, the need for ventilatory support, the use and dosage of medications, the number of nursing staff per bed, the time elapsed from admission to the intensive care unit until the effective start of enteral feeding, and the causes for nonadministration were recorded."( Nurse to bed ratio and nutrition support in critically ill patients.
Azevedo, LC; Bafi, AT; Castro, I; Freitas, FG; Honda, CK; Machado, FR; Mazza, BF; Nascente, AP; Stanich, P, 2013
)
0.39
" Conclusion Achievement of daily calorie goals was inadequate, and the main factors associated with this failure were the use and dosage of midazolam and the number of nurses available."( Nurse to bed ratio and nutrition support in critically ill patients.
Azevedo, LC; Bafi, AT; Castro, I; Freitas, FG; Honda, CK; Machado, FR; Mazza, BF; Nascente, AP; Stanich, P, 2013
)
0.39
" Shortly after the 5-month recheck evaluation, PPA administration was resumed, albeit at a lower dosage than that before surgery, for control of urinary incontinence."( Myocardial hypertrophy associated with long-term phenylpropanolamine use in a dog.
Hanson, KR; Ware, WA, 2018
)
0.48
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
plant metaboliteAny eukaryotic metabolite produced during a metabolic reaction in plants, the kingdom that include flowering plants, conifers and other gymnosperms.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (3)

ClassDescription
azaspiro compoundAn azaspiro compound is a spiro compound in which at least one of the cyclic components is a nitrogen heterocyle.
amphetaminesAmines that constitute a class of central nervous system stimulants based on the structure of the parent amphetamine 1-phenylpropan-2-amine.
phenethylamine alkaloid
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (9)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Alpha-1B adrenergic receptorMesocricetus auratus (golden hamster)Ki9.60000.00002.01679.6000AID37181
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Ki8.40000.00000.929610.0000AID35599
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Ki8.40000.00000.970810.0000AID35599
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Ki8.40000.00000.937510.0000AID35599
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki8.40000.00000.575110.0000AID35599
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki9.80000.00000.965010.0000AID36152
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.27540.00010.807410.0000AID36078
Alpha-1B adrenergic receptorMesocricetus auratus (golden hamster)Ki9.54990.00002.01679.6000AID37188
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Ki0.26300.00000.929610.0000AID36377
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki8.51140.00000.575110.0000AID35742
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki9.77240.00000.965010.0000AID37046
[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)
Alpha-1A adrenergic receptorHomo sapiens (human)EC50 (µMol)230.00000.00010.50987.1000AID36421
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (74)

Processvia Protein(s)Taxonomy
methylationPhenylethanolamine N-methyltransferaseBos taurus (cattle)
epinephrine biosynthetic processPhenylethanolamine N-methyltransferaseBos taurus (cattle)
MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of heart rate involved in baroreceptor response to increased systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine vasoconstriction involved in regulation of systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of heart rate by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
apoptotic processAlpha-1A adrenergic receptorHomo sapiens (human)
smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
activation of phospholipase C activityAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1A adrenergic receptorHomo sapiens (human)
adult heart developmentAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of cell population proliferationAlpha-1A adrenergic receptorHomo sapiens (human)
response to xenobiotic stimulusAlpha-1A adrenergic receptorHomo sapiens (human)
response to hormoneAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of autophagyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle hypertrophyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of action potentialAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
calcium ion transport into cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
cell growth involved in cardiac muscle cell developmentAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of protein kinase C signalingAlpha-1A adrenergic receptorHomo sapiens (human)
pilomotor reflexAlpha-1A adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cytokine productionAlpha-2A adrenergic receptorHomo sapiens (human)
DNA replicationAlpha-2A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
Ras protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
Rho protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2A adrenergic receptorHomo sapiens (human)
actin cytoskeleton organizationAlpha-2A adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell migrationAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
cellular response to hormone stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2A adrenergic receptorHomo sapiens (human)
vasodilationAlpha-2A adrenergic receptorHomo sapiens (human)
glucose homeostasisAlpha-2A adrenergic receptorHomo sapiens (human)
fear responseAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of potassium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAP kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion-dependent exocytosisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2A adrenergic receptorHomo sapiens (human)
intestinal absorptionAlpha-2A adrenergic receptorHomo sapiens (human)
thermoceptionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of lipid catabolic processAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of membrane protein ectodomain proteolysisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretion involved in cellular response to glucose stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of uterine smooth muscle contractionAlpha-2A adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
phospholipase C-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of wound healingAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transmembrane transporter activityAlpha-2A adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (14)

Processvia Protein(s)Taxonomy
phenylethanolamine N-methyltransferase activityPhenylethanolamine N-methyltransferaseBos taurus (cattle)
alpha1-adrenergic receptor activityAlpha-1A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1A adrenergic receptorHomo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein kinase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-1B adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-2C adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
thioesterase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
heterotrimeric G-protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
norepinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2A adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (17)

Processvia Protein(s)Taxonomy
nucleusAlpha-1A adrenergic receptorHomo sapiens (human)
nucleoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
caveolaAlpha-1A adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
basolateral plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
neuronal cell bodyAlpha-2A adrenergic receptorHomo sapiens (human)
axon terminusAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic active zone membraneAlpha-2A adrenergic receptorHomo sapiens (human)
dopaminergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
postsynaptic density membraneAlpha-2A adrenergic receptorHomo sapiens (human)
glutamatergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
GABA-ergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
receptor complexAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (52)

Assay IDTitleYearJournalArticle
AID37497Effective concentration in vitro against rat spleen Alpha-1B adrenergic receptor indicates EC50 < 15% at a concentration of 10 uM2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
AID36152Binding affinity towards rat submaxillary gland Alpha-1 adrenergic receptor; value ranges from (6.2 - 15)2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
AID235160Selectivity ratio as the ratio of Ki value towards Alpha1D receptor to that of Alpha1A receptor.2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
AID35599Binding affinity towards rat cloned Alpha-1D adrenergic receptor; value ranges from (5.5 -13)2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
AID41727Dose corresponding to a 20 mmHg increase in mean arterial pressure (MAP) was determined in vivo in isoflurane anesthetized female beagles2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
AID231931Ratio expressed as 100x Vmax/Km1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
Stereochemical aspects of phenylethanolamine analogues as substrates of phenylethanolamine N-methyltransferase.
AID36421Effective concentration in vitro against rabbit urethra Alpha-1 adrenergic receptor2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
AID233244Functional selectivity ratio as the ratio of EC50 value towards Alpha1D receptor to that of Alpha1A receptor.2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
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.
AID37181Binding affinity towards hamster cloned Alpha-1B adrenergic receptor mean;value ranges from( 6.4 -14)2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
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.
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.
AID22819Vmax of compound was determined1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
Stereochemical aspects of phenylethanolamine analogues as substrates of phenylethanolamine N-methyltransferase.
AID41728Dose corresponding to a 5 mmHg increase in Intraurethral pressure (IUP) was determined in vivo in isoflurane anesthetized female beagles2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
AID6406Affinity against 5-hydroxytryptamine receptors in rat fundus model1980Journal of medicinal chemistry, Mar, Volume: 23, Issue:3
Serotonin receptor affinities of psychoactive phenalkylamine analogues.
AID165763In vitro percent efficacy of compound was tested in rabbit urethra2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
AID156058In vitro binding affinity of compound towards bovine adrenal phenylethanolamine N-methyl-transferase (PNMT)1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
Stereochemical aspects of phenylethanolamine analogues as substrates of phenylethanolamine N-methyltransferase.
AID195189In vitro percent efficacy of compound was tested in rat aorta2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID196271In vitro percent efficacy of compound was tested rat spleen2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
AID233243Functional selectivity ratio as the ratio of EC50 value towards Alpha1B receptor to that of Alpha1A receptor.2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
AID234458Uroselectivity as the ratio of MAPED20 to that of IUP ED5.2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
AID235159Selectivity ratio as the ratio of Ki value towards Alpha1B receptor to that of Alpha1A receptor.2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID35586Effective concentration in vitro against rat aorta Alpha-1D adrenergic receptor;* indicates EC50 < 15% at a concentration of 10 uM2002Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
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.
AID59114Uroselectivity was determined by measuring effective dose required for 20 mmHg increase of mean arterial pressure (MAP) in vivo in dog2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID36097Functional agonism of the compounds to constrict tissue containing the alpha-2A adrenoceptor in rat prostatic vas deferens2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID229761Ratio of IUP ED delta5 to that of MAP ED delta202004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID234277Selectivity is ratio of efficacy of alpha-1B to that of alpha1A adrenoceptor2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID234278Selectivity is ratio of efficacy of Alpha-1D to that of alpha-1A adrenoceptor2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID1144272Potentiation of (-)-norepinephrine-induced tissue contraction in albino Sprague-Dawley rat reserpine-treated adrenergically innervated vas deferens at 3 x 10'-6 M after 15 mins by isotonic myograph analysis1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Stereochemical studies of adrenergic drugs. Diastereomeric 2-amino-1-phenylcyclobutanols.
AID37188In vitro binding affinity towards alpha-1B adrenergic receptor of hamster clone in radioligand binding assay2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID1144270Intrinsic activity of (-)-norepinephrine-induced tissue contraction in albino Sprague-Dawley rat reserpine-treated adrenergically innervated vas deferens at 1 x 10'-5 to 3 x 10'-5 M after 15 mins by isotonic myograph analysis1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Stereochemical studies of adrenergic drugs. Diastereomeric 2-amino-1-phenylcyclobutanols.
AID35742In vitro binding affinity towards alpha-1D adrenergic receptor of rat clone in radioligand binding assay2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID36766Functional agonism of the compounds to constrict tissue containing the alpha-1A adrenergic receptor in rabbit urethra2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID234280Relative affinities for alpha2B and alpha1A receptors2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID37499Efficacy relative to phenylephrine (PE) constriction of rat spleen containing alpha-1B adrenergic receptor2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID1144271Intrinsic activity of (-)-norepinephrine-induced tissue contraction in albino Sprague-Dawley rat reserpine-treated adrenergically innervated vas deferens at 3 x 10'-6 M after 15 mins by isotonic myograph analysis1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Stereochemical studies of adrenergic drugs. Diastereomeric 2-amino-1-phenylcyclobutanols.
AID35589Efficacy relative to phenylephrine (PE) constrict tissue containing the alpha-1D adrenergic receptor in rat aorta2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID234282Selectivity is ratio of pKi (binding affinity) of alpha-1B receptor to that of alpha-1A receptor.2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID36092Efficacy relative to phenylephrine (PE) to constrict tissue containing the alpha-2A adrenergic receptor in rat prostatic vas deferens2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID37046In vitro binding affinity towards alpha-1A adrenergic receptor of rat submaxillary gland in radioligand binding assay2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID36377In vitro binding affinity towards alpha-2B adrenergic receptor of rat neonatal lung in radioligand binding assay2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID36764Efficacy relative to phenylephrine (PE) to constrict tissue containing the alpha-1A adrenergic receptor in rabbit urethra2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID234283Selectivity is ratio of pKi (binding affinity) of Alpha-1D to that of alpha1A2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID35617Functional agonism of the compounds to constrict tissue containing the alpha-1D adrenergic receptor in rat aorta2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID234279Selectivity is ratio of efficacy of alpha-2A to that of alpha1A adrenoceptor2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID234281Relative affinities for alpha-2a and alpha-1A receptors2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID36078In vitro binding affinity towards alpha-2A adrenergic receptor of human clone in radioligand binding assay2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID35157Functional agonism of the compounds to constrict tissue containing the alpha-1B adrenergic receptor in rat spleen2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
AID59116Uroselectivity was determined by measuring effective dose required for 5 mmHg increase of intraurethral pressure (IUP) in vivo in dog2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,781)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990608 (34.14)18.7374
1990's255 (14.32)18.2507
2000's619 (34.76)29.6817
2010's281 (15.78)24.3611
2020's18 (1.01)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 73.25

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 Index73.25 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.21 (4.65)
Search Engine Demand Index141.46 (26.88)
Search Engine Supply Index2.35 (0.95)

This Compound (73.25)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Trials369 (19.83%)5.53%
Trials0 (0.00%)5.53%
Reviews3 (10.34%)6.00%
Reviews155 (8.33%)6.00%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies194 (10.42%)4.05%
Case Studies2 (40.00%)4.05%
Observational0 (0.00%)0.25%
Observational3 (0.16%)0.25%
Observational0 (0.00%)0.25%
Other26 (89.66%)84.16%
Other1,140 (61.26%)84.16%
Other3 (60.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (27)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
An Open Label, Balanced, Randomized, Two-treatment, Two-period, Two-sequence, Single Dose, Crossover, Oral Bioequivalence Study of Guaifenesin and Pseudoephedrine Hydrochloride Extended Release Tablets 1200/120 mg of Dr. Reddy's Laboratories Ltd., India C [NCT03706300]Phase 180 participants (Actual)Interventional2014-12-31Completed
Comparative Efficacy of the Suppository Composed by Guaiacol, Eucalyptol, Menthol and Camphor Versus Guaiacol Suppository Versus Guaifenesin Syrup in Pediatric Patients With Cough Due the Infectious Origin [NCT01119534]Phase 3270 participants (Anticipated)Interventional2011-05-31Not yet recruiting
A Non-pharmacological Cough Control Therapy as an Adjuvant of Pulmonary Rehabilitation in People With Interstitial Lung Diseases and Chronic Cough - A Feasibility Study [NCT04767074]24 participants (Anticipated)Interventional2020-09-01Recruiting
Multicentric, Randomized, Open-label Trial to Evaluate the Superiority of Fixed Dose Combination of Oxomemazine, Guaifenesin and Potassium Iodate to Guaifenesin Monotherapy in Acute Cough Treatment [NCT01257243]Phase 3260 participants (Actual)Interventional2012-10-01Completed
Comparison Between Dexchlorpheniramine and Dexchlorpheniramine/Pseudoephedrine/Guaifenesin in the Relief of Allergic Symptoms in Rhinitic Patients With Viral Upper Respiratory Tract Infections and Productive Cough [NCT01085721]Phase 3170 participants (Anticipated)InterventionalNot yet recruiting
A Methodology Study to Assess Cough Counts in Subjects With Acute Upper Respiratory Tract Infections [NCT01062256]265 participants (Actual)Interventional2010-01-31Completed
An Open-Label, Randomized, Multiple-Dose, 2-Way Crossover Comparative Bioavailability Steady State Study of Codeine Phosphate/Guaifenesin Extended-Release Tablet in Healthy Subjects [NCT02572375]Phase 138 participants (Actual)Interventional2014-10-31Completed
Assessing the Effectiveness of Integrative Treatment That Combines Interior and Exterior Treatment Plans in Pediatric Pneumonia: a Program by PRC National Clinical Research Base of Traditional Chinese Medicine for Major Diseases [NCT02069665]451 participants (Actual)Interventional2011-12-31Completed
An Open-Label, Single-Dose, Crossover Comparative Bioavailability and Pharmacokinetic Study of Codeine Phosphate/Guaifenesin Extended-Release Tablet With Immediate-Release Tablet [NCT02157649]Phase 126 participants (Actual)Interventional2014-06-30Completed
An Open-Label, 2-way Crossover Placebo-Controlled , Radio-Labeled Tracer Study Evaluating the Effect of MUCINEX® 1200 mg on Mucociliary and Cough Clearance From The Human Lung In Healthy, Non-Smoking Adults [NCT00902707]Phase 112 participants (Actual)Interventional2009-05-31Completed
Randomized Clinical Trial to Evaluate Guidelines for Acute Rhinosinusitis (Phase IV Study) [NCT00377403]Phase 4172 participants (Actual)Interventional2006-10-31Completed
A Phase I, Open- Label, Randomized, Multiple-dose, 3-way Crossover Relative Bioavailability Study to Characterize the Pharmacokinetics of the 3 Marketed Products Containing 200 mg Guaifenesin Under Fasted Conditions in Normal Healthy Subjects. [NCT03643575]Phase 130 participants (Actual)Interventional2009-06-30Completed
A Study Designed to Examine the Potential for a Drug-drug Interaction Between Guaifenesin and Hydrocodone Bitartrate in Normal Healthy Volunteers [NCT03642873]Phase 124 participants (Actual)Interventional2007-05-05Completed
A Randomized, Double-Blind, Placebo-Controlled, Parallel-Group, Multicenter Study of the Safety and Efficacy of Mucinex D for Symptomatic Therapy in Patients With Acute Upper Respiratory Tract Who Seek Treatment [NCT01202279]Phase 41,179 participants (Actual)Interventional2009-10-31Completed
Double Blind, Randomized, Placebo Controlled Study of Mucinex® for the Treatment of Symptoms of an Acute Respiratory Tract Infection When Two 600 mg Tablets Are Given Every 12 Hours for 7 Days [NCT01046136]Phase 2378 participants (Actual)Interventional2009-12-31Completed
A Pilot, Multicentric and Observational Study of Safety of Sulfamethoxazole + Trimethoprim + Guaifenesin (Balsamic Bactrim) in Pediatric Patients With Acute Bronchitis [NCT02879981]51 participants (Actual)Observational2016-11-10Completed
A Pilot, Multicentric and Observational Study of Safety of Sulfamethoxazole + Trimethoprim + Guaifenesin (Balsamic Bactrim) in Adult Patients With Acute Bronchitis [NCT02902640]52 participants (Actual)Observational2016-11-15Completed
A Phase I, Open-label, Single-dose, Randomized, 2-way Crossover Bioequivalence Study Comparing Mucinex® SE Extended-Release 600 mg Bi-layer Tablet to a Reference Immediate-Release Guaifenesin 600 mg (Taken as 200 mg q4h) in Normal Healthy Subjects. [NCT03644095]Phase 130 participants (Actual)Interventional2009-01-16Completed
A Randomized, Double-Blind, Parallel-Group, Multicenter, Placebo-Controlled Study of the Safety and Efficacy of Mucinex D as Adjunct Therapy to Antibiotic Treatment of Acute Respiratory Infection [NCT00441246]Phase 4600 participants (Anticipated)Interventional2007-02-28Completed
Management of HIV-Infected Patients at Risk of Recurrent Purulent Sinusitis: Role of Anti-Inflammatory, Antibacterial, and Decongestant Prophylaxis [NCT00000752]Phase 20 participants (Actual)InterventionalWithdrawn
An Open-label, Single-dose, Randomized, Two-way Crossover Study to Evaluate the Pharmacokinetics of Guaifenesin in Adults and Adolescents at Immediate-release Doses of 200 mg and 400 mg. [NCT03633448]Phase 124 participants (Actual)Interventional2011-06-18Completed
[NCT01114581]Phase 238 participants (Actual)Interventional2010-04-30Completed
An Open Label, In-use Study to Assess the Warming Sensation, Acceptability and Local Tolerability of Paracetamol 500 mg + Phenylephrine 10mg + Guaifenesin 200 mg Syrup Given as a 30 ml Single Dose in Subjects Suffering From Symptoms of an Upper Respirator [NCT01576809]Phase 351 participants (Actual)Interventional2012-03-31Completed
A SingleDose Rand, TwoPeriod, Crossover Bioequivalence Study Between a Combination Tablet With Paracetamol, Guaifenesin and Penylephrine HCL (Wrafton Lab Ltd, UK) and Vicks Active SymptoMax Plus, Powder for Oral Solution (Wrafton Lab Ltd, UK) in Healthy A [NCT03213353]Phase 172 participants (Actual)Interventional2017-07-03Completed
The Effect of Oral Guaifenesin on Pediatric Chronic Rhinitis: A Pilot Study [NCT01364467]Phase 230 participants (Actual)Interventional2011-05-31Completed
Randomized, Double-Blind, Double Dummy, Placebo-Controlled Study of the Safety and Efficacy Mucinex (2400 mg/d) and Immediate-Release Guaifenesin (800 mg/d) in the Treatment of Symptoms of Acute Upper Respiratory Tract Infections For 7 Days [NCT01537081]Phase 2/Phase 32,810 participants (Actual)Interventional2011-09-30Completed
A Proof of Principle Study to Explore the Utility of Guaifenesin in Upper Back Pain [NCT01562548]78 participants (Actual)Interventional2012-02-29Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00377403 (1) [back to overview]SNOT-16 Score (Sino-Nasal Outcomes Test) at Day 3
NCT01046136 (3) [back to overview]Number of Patients With Adverse Events
NCT01046136 (3) [back to overview]Mean Change From Baseline in a 6 Point Severity Scale (0 = None, 1 = Very Mild, 2 = Mild or Slight, 3 = Moderate, 4 = Severe or 5 = As Bad as it Can be) for Cough.
NCT01046136 (3) [back to overview]Investigator's End of Study Assessment of Treatment
NCT01062256 (6) [back to overview]Number of Cough Bouts Over 2-hour Postdose Period
NCT01062256 (6) [back to overview]Number of Cough Bouts Over 4-hour Postdose Period
NCT01062256 (6) [back to overview]Change From Baseline in Cough Severity Scale
NCT01062256 (6) [back to overview]Number of Cough Bouts Within Each 15-minute Time Interval Postdose
NCT01062256 (6) [back to overview]Number of Participant With Cough Severity
NCT01062256 (6) [back to overview]Number of Participants With Global Evaluation of Study Medication
NCT01114581 (2) [back to overview]Percent of Inhaled Radioactive Tracer Particles Cleared From Lungs
NCT01114581 (2) [back to overview]Guaifenesin AUC(0-3)
NCT01202279 (2) [back to overview]Antibiotic Sparing
NCT01202279 (2) [back to overview]Change From Baseline in Total Symptom Score of the Wisconsin Upper Respiratory Symptom Survey - 21 (WURSS-21).
NCT01364467 (2) [back to overview]Nasal Volume
NCT01364467 (2) [back to overview]Change in Subjective Nasal Scoring
NCT01537081 (2) [back to overview]Summary Scores on the SUM8 Daily Cough and Phlegm Diary Card On the Morning of Day 5
NCT01537081 (2) [back to overview]Summary Scores on the SUM8 Daily Cough and Phlegm Diary Card On the Morning of Day 4
NCT01562548 (11) [back to overview]Mean Change From Baseline of Both AM and PM NRS Muscle Stiffness Assessment Scores
NCT01562548 (11) [back to overview]Muscle Relaxation Scores
NCT01562548 (11) [back to overview]Upper Back/Neck/Shoulder Pain Disability (Vernon-Mior) Index Scores
NCT01562548 (11) [back to overview]Mean Change From Baseline of Both AM and PM NRS Discomfort Assessment Scores
NCT01562548 (11) [back to overview]Mean Change From Baseline of Both AM and PM NRS Pain Assessment Scores
NCT01562548 (11) [back to overview]Mean Change From Baseline of Both AM and PM NRS Tension Assessment Scores
NCT01562548 (11) [back to overview]Mean Change From Baseline of Both AM and PM Spasm Assessment Scores
NCT01562548 (11) [back to overview]Global Assessment of Headache Frequency (GAHF)
NCT01562548 (11) [back to overview]Global Assessment of Headache Intensity (GAHI)
NCT01562548 (11) [back to overview]Global Assessment of Sleep Disturbance (GASD)
NCT01562548 (11) [back to overview]Global Assessment of Treatment Helpfulness (GATH)
NCT01576809 (3) [back to overview]Warming Sensation Caused by the Excipient IFF Flavor 316 282, in a Syrup Containing Paracetamol 500 mg + Phenylephrine 10mg + Guaifenesin 200 mg Per 30 ml Syrup
NCT01576809 (3) [back to overview]Safety and Tolerability of the Syrup
NCT01576809 (3) [back to overview]Subject Acceptability of the Syrup
NCT03633448 (8) [back to overview]Area Under Plasma Concentration-time Curve From Time 0 to the Last Measurable Concentration (AUC(0-t)) of Guaifenesin
NCT03633448 (8) [back to overview]Area Under Plasma Concentration-time Curve From Time 0 to Infinity (AUC(0-inf)) of Guaifenesin
NCT03633448 (8) [back to overview]Apparent First-order Terminal Elimination Half-life (t½)
NCT03633448 (8) [back to overview]Percent of AUC 0-inf Extrapolated (AUC%Extrapolated)
NCT03633448 (8) [back to overview]Time to Maximum Observed Concentration (Tmax) of Guaifenesin
NCT03633448 (8) [back to overview]Number of Adverse Events (AEs) of Participants
NCT03633448 (8) [back to overview]Apparent First-order Terminal Elimination Rate Constant (Kel)
NCT03633448 (8) [back to overview]Maximum Observed Plasma Concentration (Cmax) of Guaifenesin
NCT03642873 (7) [back to overview]Maximum Observed Plasma Concentration (Cmax) of Guaifenesin
NCT03642873 (7) [back to overview]Time to Maximum Observed Concentration (Tmax) of Guaifenesin
NCT03642873 (7) [back to overview]Number of Adverse Events(AEs) Experienced by Participants
NCT03642873 (7) [back to overview]Area Under Plasma Concentration-time Curve From Time 0 to the Last Measurable Concentration (AUC(0-t)) of Guaifenesin
NCT03642873 (7) [back to overview]Apparent Terminal Elimination Half-life (T1/2) of Guaifenesin
NCT03642873 (7) [back to overview]Apparent Terminal Elimination Rate Constant (Kel) of Guaifenesin
NCT03642873 (7) [back to overview]Area Under Plasma Concentration-time Curve From Time 0 to Infinity (AUC(0-inf)) of Guaifenesin
NCT03643575 (17) [back to overview]Time to Maximum Observed Plasma Concentration (Tmax) of Guaifenesin
NCT03643575 (17) [back to overview]Peak Plasma Concentrations at Steady State (Swing) of Guaifenesin
NCT03643575 (17) [back to overview]Observed Plasma Concentration at the End of Dosing Interval at Steady State (Cmin,ss) of Guaifenesin Following the Third Dose
NCT03643575 (17) [back to overview]Maximum Observed Plasma Concentration (Cmax) of Guaifenesin
NCT03643575 (17) [back to overview]Maximum Measured Plasma Concentration at Steady State (Cmax,ss) of Guaifenesin Following the Third Dose
NCT03643575 (17) [back to overview]Degree of Fluctuation (DF) of Guaifenesin
NCT03643575 (17) [back to overview]Average Plasma Concentration (Cav) of Guaifenesin Following the Third Dose
NCT03643575 (17) [back to overview]Area Under the Plasma Concentration Versus Time Curve From Time 0 to the Time of the Last Measurable Concentration [AUC(0-t)] of Guaifenesin
NCT03643575 (17) [back to overview]Area Under Plasma Concentration Versus Time Curve From Time 8 to 12 Hours [AUC(8-12)] of Guaifenesin
NCT03643575 (17) [back to overview]Area Under Plasma Concentration Versus Time Curve From Time 0 to Infinity [AUC(0-inf)] of Guaifenesin
NCT03643575 (17) [back to overview]Area Under Plasma Concentration Versus Time Curve From 0 to 4 Hours [AUC(0-4)] of Guaifenesin
NCT03643575 (17) [back to overview]Area Under Plasma Concentration Curve Ratio (AUCR) of Guaifenesin
NCT03643575 (17) [back to overview]Apparent First-order Terminal Elimination Half-life (T1/2) of Guaifenesin
NCT03643575 (17) [back to overview]Accumulation Index (AI) of Guaifenesin
NCT03643575 (17) [back to overview]Apparent First-order Terminal Elimination Rate Constant (Kel) of Guaifenesin
NCT03643575 (17) [back to overview]Number of Participants With Adverse Events (AEs)
NCT03643575 (17) [back to overview]Time to Maximum Observed Plasma Concentration at Steady State (Tmax,ss) of Guaifenesin Following the Third Dose
NCT03644095 (8) [back to overview]Apparent Terminal Elimination Rate Constant (Kel) of Guaifenesin
NCT03644095 (8) [back to overview]Area Under Plasma Concentration Curve Ratio (AUCR) of Guaifenesin
NCT03644095 (8) [back to overview]Area Under Plasma Concentration-time Curve From Time 0 to Infinity (AUC(0-inf)) of Guaifenesin
NCT03644095 (8) [back to overview]Area Under Plasma Concentration-time Curve From Time 0 to the Last Measurable Concentration (AUC(0-t)) of Guaifenesin
NCT03644095 (8) [back to overview]Maximum Observed Plasma Concentration (Cmax) of Guaifenesin
NCT03644095 (8) [back to overview]Time to Maximum Observed Concentration (Tmax) of Guaifenesin
NCT03644095 (8) [back to overview]Number of Adverse Events (AE) of Participants
NCT03644095 (8) [back to overview]Apparent Terminal Elimination Half-life (t1/2) of Guaifenesin

SNOT-16 Score (Sino-Nasal Outcomes Test) at Day 3

The Sino-Nasal Outcomes Test (SNOT-16) assesses disease-specific quality of life for acute and chronic rhinosinusitis. This brief instrument assesses 16 sinus-related symptoms and was administered by phone. The respondent reported how much they were bothered by each item considering both its severity and frequency. Response options include no problem (0), mild or slight problem (1), moderate problem (2), severe problem (3). The SNOT-16 score is the mean score from all 16 items and ranges from 0 (minimal impact) to 3 (significant impact). (NCT00377403)
Timeframe: 4 days

InterventionUnits on a scale (Mean)
Intervention Arm1.12
Symptomatic Treatments Only1.14

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Number of Patients With Adverse Events

Total number of patients with adverse events that were possibly or probably related. (NCT01046136)
Timeframe: 7 days

Interventionparticipants (Number)
Mucinex12
Placebo6

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Mean Change From Baseline in a 6 Point Severity Scale (0 = None, 1 = Very Mild, 2 = Mild or Slight, 3 = Moderate, 4 = Severe or 5 = As Bad as it Can be) for Cough.

Mean change from baseline in a 6 point severity scale between treatment groups(0 = None, 1 = Very mild, 2 = Mild or slight, 3 = Moderate, 4 = Severe or 5 = As bad as it can be) for cough. (NCT01046136)
Timeframe: Baseline and Day 4

Interventionunits on a scale (Mean)
Mucinex-1.1
Placebo-0.9

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Investigator's End of Study Assessment of Treatment

Yes the investigator would use this treatment for cold symptoms in the future. (NCT01046136)
Timeframe: 7 days

Interventionparticipants (Number)
Mucinex163
Placebo149

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Number of Cough Bouts Over 2-hour Postdose Period

Cough bouts defined as one or several cough sounds occurring after one inspiration (one explosive bout between inspiration and expiration). Audio recordings made of participants during first 2 hours postdose. Based on audio recordings, a trained cough counter counted and recorded the number of cough bouts. (NCT01062256)
Timeframe: 0 to 2 hours postdose

Interventioncough bouts (Mean)
Placebo83.8
Buckwheat Honey79.8
Guaifenesin75.0

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Number of Cough Bouts Over 4-hour Postdose Period

Cough bouts defined as one or several cough sounds occurring after one inspiration (one explosive bout between inspiration and expiration). Audio recordings made of participants during 4-hour period after dosing. Based on audio recordings, a trained cough counter counted and recorded the number of cough bouts. (NCT01062256)
Timeframe: 0 to 4 hours postdose

InterventionCough bouts (Mean)
Placebo139.6
Buckwheat Honey131.3
Guaifenesin126.4

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Change From Baseline in Cough Severity Scale

Participant's self-assessment of cough severity using a 4-point categorical scale (0 = none; no cough present, 1 = mild; cough present but with minimal awareness, easily tolerated, 2 = moderate; cough definitely present and bothersome, but tolerable, or 3 = severe; cough was hard to tolerate; may have caused interference with daily activities and sleeping). Change from baseline derived by subtracting post baseline cough severity from baseline cough severity. Change from baseline values could have ranged from -1.0 to 3.0 with higher values indicative of greater improvement. (NCT01062256)
Timeframe: 1, 2, 3, and 4 hours postdose

,,
Interventionunits on a scale (Mean)
1 hour postdose2 hours postdose3 hours postdose4 hours postdose
Buckwheat Honey0.50.71.01.1
Guaifenesin0.30.60.81.0
Placebo0.40.60.81.0

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Number of Cough Bouts Within Each 15-minute Time Interval Postdose

Cough bouts defined as one or several cough sounds occurring after one inspiration (one explosive bout between inspiration and expiration). Audio recordings made of participants during 4-hour (240-minute) period after dosing. Based on audio recordings, a trained cough counter counted and recorded the number of cough bouts in 15 minute intervals. (NCT01062256)
Timeframe: every 15 minutes postdose up to 240 minutes postdose

,,
Interventioncough bouts (Mean)
15 minutes30 minutes45 minutes60 minutes75 minutes90 minutes105 minutes120 minutes135 minutes150 minutes165 minutes180 minutes195 minutes210 minutes225 minutes240 minutes
Buckwheat Honey14.510.910.69.68.78.78.68.47.27.17.06.96.35.75.85.9
Guaifenesin14.211.09.58.78.28.07.97.96.66.87.06.95.96.36.06.3
Placebo14.912.411.510.18.19.49.68.36.87.97.76.56.16.87.27.1

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Number of Participant With Cough Severity

Participant's self-assessment of cough severity using 4-point categorical scale (0 = none; no cough present, 1 = mild; cough present but with minimal awareness, easily tolerated, 2 = moderate; cough definitely present and bothersome, but tolerable, or 3 = severe; cough was hard to tolerate; may have caused interference with daily activities and sleeping). Participants were eligible for study if severity of cough at baseline was at least moderate. (NCT01062256)
Timeframe: Baseline

,,
InterventionParticipants (Number)
ModerateSevere
Buckwheat Honey9210
Guaifenesin1016
Placebo513

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Number of Participants With Global Evaluation of Study Medication

"Participant-rated evaluation of study product; Participants responded to the following question:~How would you rate this product as a cough reliever? 0=poor, 1=fair, 2=good, 3=very good, and 4=excellent" (NCT01062256)
Timeframe: 4 hours postdose or early termination

,,
Interventionparticipants (Number)
PoorFairGoodVery GoodExcellent
Buckwheat Honey92833229
Guaifenesin113929235
Placebo51818102

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Percent of Inhaled Radioactive Tracer Particles Cleared From Lungs

Percentage of inhaled radioactive tracer (Ave180Clear) (NCT01114581)
Timeframe: 3 hours following inhalation of radioactive tracer particles

InterventionPercentage of inhaled radioactive tracer (Mean)
Guaifenesin21.4
Placebo23.1

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Guaifenesin AUC(0-3)

(NCT01114581)
Timeframe: 3 hours following dose administration

Interventionng*hr/mL (Geometric Mean)
Guaifenesin4060

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Antibiotic Sparing

Number of patients who received an antibiotic (NCT01202279)
Timeframe: Day 7

InterventionParticipants (Number)
Mucinex D89
Placebo121

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Change From Baseline in Total Symptom Score of the Wisconsin Upper Respiratory Symptom Survey - 21 (WURSS-21).

WURSS-21 is made up of 21 questions with a scoring from 0 = no symptom to 7 = severe symptom. With a minimum score of 0 to a maximum score of 147. (NCT01202279)
Timeframe: Baseline and 7 Days

Interventionunits on a scale (Mean)
Mucinex D-14.2
Placebo-13.4

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Nasal Volume

Acoustic rhinometry is used to measure cross-sectional volume of the nasal cavity allowing the calculation of nasal volume. (NCT01364467)
Timeframe: 15 Minutes

,
InterventionSquare centimeters (Mean)
Right nostrilLeft nostril
Guaifenesin1.131.08
Placebo1.100.83

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Change in Subjective Nasal Scoring

The Sinus and Nasal Quality of Life Survey (SN-5) questionnaire assesses the impact of infection on nasal symptoms, emotion, and activity. The SN-5 is a 5-item scale with each item rated on a scale of worsening symptoms from 1 (none of the time) through 7 (all of the time). Items were averaged to yield a single score ranging from 1 (better outcomes) to 7 (worse outcomes). Scores were used to asses change in disease severity and the impact of interventions on subjective complaints from baseline to follow-up. (NCT01364467)
Timeframe: Baseline to 10 Minutes

Interventionscore on a scale (Mean)
Placebo0.62
Guaifenesin1.53

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Summary Scores on the SUM8 Daily Cough and Phlegm Diary Card On the Morning of Day 5

Participants completed diary cards twice a day that asked questions about their cough and phlegm status. The Daily Cough and Phlegm Diary Card consisted of eleven questions, eight core questions plus three questions that were answered dependent upon the response to core questions. The SUM8 consisted of the sum of the answers to the eight core questions. Each question was answered on a scale of 0-4, with 4 representing the greatest severity of symptoms. The SUM8 thus had a scale range of 0-32 with 0 representing best possible symptoms, and 32 representing greatest severity of symptoms. (NCT01537081)
Timeframe: Day 5

Interventionunits on a scale (Mean)
Mucinex 2400 mg/Day10.92
Immediate-release Guaifenesin 800 mg/Day10.80
Placebo11.05

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Summary Scores on the SUM8 Daily Cough and Phlegm Diary Card On the Morning of Day 4

Participants completed diary cards twice a day that asked questions about their cough and phlegm status. The Daily Cough and Phlegm Diary Card consisted of eleven questions, eight core questions plus three questions that were answered dependent upon the response to core questions. The SUM8 consisted of the sum of the answers to the eight core questions. Each question was answered on a scale of 0-4, with 4 representing the greatest severity of symptoms. The SUM8 thus had a scale range of 0-32 with 0 representing best possible symptoms, and 32 representing greatest severity of symptoms. (NCT01537081)
Timeframe: Day 4

Interventionunits on a scale (Mean)
Mucinex 2400 mg/Day12.96
Immediate-release Guaifenesin 800 mg/Day12.87
Placebo12.71

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Mean Change From Baseline of Both AM and PM NRS Muscle Stiffness Assessment Scores

The score was measured as 'assessment at baseline' minus 'assessment after treatment' over 7 day period (mean of all AM and PM changes from baseline). Measurements were based on an 11 categorical Numerical Rating Scale (NRS) with a range from 0 - no stiffness to 10 - unbearable stiffness. (NCT01562548)
Timeframe: 7 Days

InterventionScore on a scale (Mean)
Guaifenesin 600mg1.90
Placebo Matching Guaifenesin 600mg2.09
Guaifenesin 1200mg1.87
Placebo Matching Guaifenesin 1200mg1.77

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Muscle Relaxation Scores

The score was measured as mean of both AM and PM assessment scores at Days 4 and 7. Measurements were based on a 5 categorical scale: 0 - no relaxation, 1- a little relaxation, 2 - fair relaxation, 3 - good relaxation, 4 - complete muscle relaxation. (NCT01562548)
Timeframe: 4 Days, 7 Days

,,,
InterventionScore on a scale (Mean)
Degree of Muscle Relaxation at Day 4Degree of Muscle Relaxation at Day 7
Guaifenesin 1200mg1.852.17
Guaifenesin 600mg1.801.86
Placebo Matching Guaifenesin 1200mg1.351.69
Placebo Matching Guaifenesin 600mg1.902.27

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Upper Back/Neck/Shoulder Pain Disability (Vernon-Mior) Index Scores

Vernon-Mior upper back/neck/shoulder components were assessed before the treatment and at Days 4 and 7. Each component (pain intensity, personal care, lifting, reading, headaches, concentration, work, driving, sleeping, and recreation) was assessed based on a 6-point categorical scale (1 to 6), with 1 being the most positive and 6 being the worst. (NCT01562548)
Timeframe: Before treatment, 4 Days, 7 Days

,,,
InterventionScore on a scale (Mean)
Pain Intensity-before treatmentPain Intensity-Day 4Pain Intensity-Day 7Personal Care-before treatmentPersonal Care-Day 4Personal Care-Day 7Lifting-before treatmentLifting-Day 4Lifting-Day 7Reading-before treatmentReading-Day 4Reading-Day 7Headache-before treatmentHeadache-Day 4Headache-Day 7Concentration-before treatmentConcentration-Day 4Concentration-Day 7Work-before treatmentWork-Day 4Work-Day 7Driving-before treatmentDriving-Day 4Driving-Day 7Sleeping-before treatmentSleeping-Day 4Sleeping-Day 7Recreation-before treatmentRecreation-Day 4Recreation-Day 7
Guaifenesin 1200mg3.252.291.882.001.501.292.922.582.042.291.881.581.792.041.751.881.541.462.501.921.752.211.791.462.962.422.042.882.171.88
Guaifenesin 600mg3.882.722.481.961.721.603.042.802.563.002.402.001.721.761.602.121.751.762.642.201.963.122.562.483.162.762.563.442.442.29
Placebo Matching Guaifenesin 1200mg3.622.831.922.001.751.463.152.422.002.922.381.852.232.232.002.082.001.623.002.462.083.002.382.153.232.921.923.232.542.08
Placebo Matching Guaifenesin 600mg3.672.532.202.071.601.333.132.272.002.672.201.731.871.671.672.201.601.532.802.131.732.672.132.003.472.672.203.272.401.73

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Mean Change From Baseline of Both AM and PM NRS Discomfort Assessment Scores

The score was measured as 'assessment at baseline' minus 'assessment after treatment' over 7 day period (mean of all AM and PM changes from baseline). Measurements were based on an 11 categorical Numerical Rating Scale (NRS) with a range from 0 - no discomfort to 10 - unbearable discomfort. (NCT01562548)
Timeframe: 7 Days

InterventionScore on a scale (Mean)
Guaifenesin 600mg1.95
Placebo Matching Guaifenesin 600mg2.57
Guaifenesin 1200mg2.33
Placebo Matching Guaifenesin 1200mg1.12

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Mean Change From Baseline of Both AM and PM NRS Pain Assessment Scores

The score was measured as 'assessment at baseline' minus 'assessment after treatment' over 7 day period (mean of all AM and PM changes from baseline). Measurements were based on an 11 categorical Numerical Rating Scale (NRS) with a range from 0 - no pain to 10 - unbearable pain. (NCT01562548)
Timeframe: 7 Days

InterventionScore on a scale (Mean)
Guaifenesin 600mg1.65
Placebo Matching Guaifenesin 600mg2.41
Guaifenesin 1200mg2.14
Placebo Matching Guaifenesin 1200mg1.41

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Mean Change From Baseline of Both AM and PM NRS Tension Assessment Scores

The score was measured as 'assessment at baseline' minus 'assessment after treatment' over 7 day period (mean of all AM and PM changes from baseline). Measurements were based on an 11 categorical Numerical Rating Scale (NRS) with a range from 0 - no tension to 10 - unbearable tension. (NCT01562548)
Timeframe: 7 Days

InterventionScore on a scale (Mean)
Guaifenesin 600mg1.74
Placebo Matching Guaifenesin 600mg1.98
Guaifenesin 1200mg1.97
Placebo Matching Guaifenesin 1200mg1.54

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Mean Change From Baseline of Both AM and PM Spasm Assessment Scores

The score was measured as 'assessment at baseline' minus 'assessment after treatment' over 7 day period (mean of all AM and PM changes from baseline). Measurements were based on an 11 categorical Numerical Rating Scale (NRS) with a range from 0 - no spasm to 10 - unbearable spasm. (NCT01562548)
Timeframe: 7 Days

InterventionScore on a Scale (Mean)
Guaifenesin 600mg1.66
Placebo Matching Guaifenesin 600mg1.87
Guaifenesin 1200mg1.91
Placebo Matching Guaifenesin 1200mg1.54

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Global Assessment of Headache Frequency (GAHF)

Categorized after treatment as: 'decreased', 'increased' or 'stayed the same'. (NCT01562548)
Timeframe: 7 Days

,,,
Interventionparticipants (Number)
Headache frequency-decreasedHeadache frequency-increasedHeadache frequency-stayed same
Guaifenesin 1200mg7116
Guaifenesin 600mg9313
Placebo Matching Guaifenesin 1200mg409
Placebo Matching Guaifenesin 600mg906

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Global Assessment of Headache Intensity (GAHI)

Categorized after treatment as: 'decreased', 'increased' or 'stayed the same'. (NCT01562548)
Timeframe: 7 Days

,,,
Interventionparticipants (Number)
Headache Intensity-decreasedHeadache Intensity-increasedHeadache Intensity-stayed same
Guaifenesin 1200mg9114
Guaifenesin 600mg10114
Placebo Matching Guaifenesin 1200mg409
Placebo Matching Guaifenesin 600mg906

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Global Assessment of Sleep Disturbance (GASD)

Categorized after treatment as: 'decreased', 'increased' or 'stayed the same'. (NCT01562548)
Timeframe: 7 Days

,,,
Interventionparticipants (Number)
Global Assessment of Sleep Disturbance-DecreasedGlobal Assessment of Sleep Disturbance-IncreasedGlobal Assessment of Sleep Disturbance-Stayed same
Guaifenesin 1200mg10212
Guaifenesin 600mg8116
Placebo Matching Guaifenesin 1200mg715
Placebo Matching Guaifenesin 600mg807

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Global Assessment of Treatment Helpfulness (GATH)

Measured as an overall qualitative score on a 5 point categorical scale: 0-poor, 1-fair, 2-good, 3-very good and 4-excellent. (NCT01562548)
Timeframe: 4 Days, 7 Days

,,,
InterventionScore on a scale (Mean)
Global Assessment of Treatment Helpfulness- Day 4Global Assessment of Treatment Helpfulness- Day 7
Guaifenesin 1200mg1.631.71
Guaifenesin 600mg1.481.56
Placebo Matching Guaifenesin 1200mg0.851.38
Placebo Matching Guaifenesin 600mg1.531.73

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Warming Sensation Caused by the Excipient IFF Flavor 316 282, in a Syrup Containing Paracetamol 500 mg + Phenylephrine 10mg + Guaifenesin 200 mg Per 30 ml Syrup

Intensity of warming sensation felt by subjects between predose to 1 minute postdose where 0= no warming sensation and 100= strongest possible warming sensation (NCT01576809)
Timeframe: 1 minutes

Interventionmm (Mean)
Upper Respiratory Tract Infection34.6

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Safety and Tolerability of the Syrup

Number of participants with adverse events. (NCT01576809)
Timeframe: 1 hour

Interventionparticipants (Number)
Upper Respiratory Tract Infection6

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Subject Acceptability of the Syrup

"In response to the question How did you like the warming sensation you have experienced for this product?, the number of patients answering Like extremely or Like very much or Like moderately or Like slightly~Possible responses are :~Like extremely Like very much Like moderately Like slightly Neither like nor dislike Dislike slightly Dislike moderately Dislike very much Dislike extremely" (NCT01576809)
Timeframe: 1 hour

Interventionparticipants (Number)
Upper Respiratory Tract Infection36

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Area Under Plasma Concentration-time Curve From Time 0 to the Last Measurable Concentration (AUC(0-t)) of Guaifenesin

Area under the plasma concentration versus time curve from time 0 to the time of the last measurable concentration, as calculated by the linear trapezoidal method. (NCT03633448)
Timeframe: 0 (pre-dose), 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, and 8 hours

Interventionng*hr/mL (Mean)
Treatment A (Adolescents)1990
Treatment A (Adults)1700
Treatment B (Adolescents)4390
Treatment B (Adults)3910

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Area Under Plasma Concentration-time Curve From Time 0 to Infinity (AUC(0-inf)) of Guaifenesin

Area under the plasma concentration versus time curve from time 0 to infinity, calculated as AUC 0-t + C last/kel, where C last is the last measurable concentration and kel is the apparent first-order terminal elimination rate constant. (NCT03633448)
Timeframe: 0 (pre-dose), 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, and 8 hours

Interventionng*hr/mL (Mean)
Treatment A (Adolescents)2090
Treatment A (Adults)1710
Treatment B (Adolescents)4400
Treatment B (Adults)3930

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Apparent First-order Terminal Elimination Half-life (t½)

Apparent first-order terminal elimination half-life, calculated as ln(2)/kel. (NCT03633448)
Timeframe: 0 (pre-dose), 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, and 8 hours

Interventionhr (Mean)
Treatment A (Adolescents)1.05
Treatment A (Adults)1.10
Treatment B (Adolescents)0.963
Treatment B (Adults)0.963

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Percent of AUC 0-inf Extrapolated (AUC%Extrapolated)

Percent of AUC 0-inf extrapolated, calculated as (1 - AUC 0-t / AUC 0-inf) x 100. (NCT03633448)
Timeframe: 0 (pre-dose), 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, and 8 hours

InterventionPercentage (Mean)
Treatment A (Adolescents)0.469
Treatment A (Adults)0.736
Treatment B (Adolescents)0.476
Treatment B (Adults)0.386

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Time to Maximum Observed Concentration (Tmax) of Guaifenesin

Pharmacokinetic Parameter (Tmax) Time of the maximum observed plasma concentration. (NCT03633448)
Timeframe: 0 (pre-dose), 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, and 8 hours

Interventionhr (Mean)
Treatment A (Adolescents)0.458
Treatment A (Adults)0.711
Treatment B (Adolescents)0.524
Treatment B (Adults)0.646

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Number of Adverse Events (AEs) of Participants

"Intensity determination:~Mild=AE does not limit usual activities;subject may experience slight discomfort; Moderate= AE results in some limitation of usual activities; subject may experience significant discomfort; Severe=AE results in an inability to carry out usual activities; subject may experience intolerable discomfort or pain; Unlikely=Slight but remote chance that the AE was caused by study drug but the balance of judgment is that it was most likely not due to the study drug Possible=Reasonable suspicion that the AE was caused by the study drug; Probable=Most likely that the AE was caused by study drug." (NCT03633448)
Timeframe: Upto Day 1

,,,
InterventionEvents (Number)
TEAE by severity: MildTEAE by severity: ModerateTEAE by severity: SevereRelationship to Drug: DefiniteRelationship to Drug: ProbableRelationship to Drug: PossibleRelationship to Drug: UnlikelyRelationship to Drug: None
Treatment A (Adolescents)00000000
Treatment A (Adults)00000000
Treatment B (Adolescents)00000000
Treatment B (Adults)11000002

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Apparent First-order Terminal Elimination Rate Constant (Kel)

Apparent first-order terminal elimination rate constant calculated from a semilog plot of the plasma concentration versus time curve. The parameter was calculated by linear least-squares (LS) regression analysis using the maximum number of points (e.g., three or more non-zero plasma concentrations) in the terminal log-linear phase. (NCT03633448)
Timeframe: 0 (pre-dose), 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, and 8 hours

Intervention1/hr (Mean)
Treatment A (Adolescents)0.678
Treatment A (Adults)0.655
Treatment B (Adolescents)0.731
Treatment B (Adults)0.726

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Maximum Observed Plasma Concentration (Cmax) of Guaifenesin

Pharmacokinetic Parameter (Cmax) Maximum observed plasma concentration. (NCT03633448)
Timeframe: 0 (pre-dose), 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, and 8 hours

Interventionng/mL (Mean)
Treatment A (Adolescents)1360
Treatment A (Adults)887
Treatment B (Adolescents)2690
Treatment B (Adults)1950

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Maximum Observed Plasma Concentration (Cmax) of Guaifenesin

Pharmacokinetic Parameter Cmax (Maximum measured plasma concentration) (NCT03642873)
Timeframe: 0 (pre-dose), 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.5, 6, 7, 8, 8.5, 9, 9.5, 10, 11, 13, 16, 20, 24, and 26 hours Post dose

Interventionng/mL (Mean)
Treatment A (Reference) - Plasma Guaifenesin1770
Treatment C (Test) - Plasma Guaifenesin1810
Treatments B (Reference) - Plasma Hydrocodone Bitartrate11.3
Treatment C (Test) - Plasma Hydrocodone Bitartrate11.3

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Time to Maximum Observed Concentration (Tmax) of Guaifenesin

Pharmacokinetic Parameter (Tmax) Time of the maximum measured plasma concentration. (NCT03642873)
Timeframe: 0 (pre-dose), 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.5, 6, 7, 8, 8.5, 9, 9.5, 10, 11, 13, 16, 20, 24, and 26 hours Post dose

Interventionhr (Mean)
Treatment A (Reference) - Plasma Guaifenesin1.08
Treatment C (Test) - Plasma Guaifenesin1.04
Treatments B (Reference) - Plasma Hydrocodone Bitartrate9.59
Treatment C (Test) - Plasma Hydrocodone Bitartrate9.33

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Number of Adverse Events(AEs) Experienced by Participants

"Intensity was determined by the Investigator. For symptomatic AEs the following definitions were applied.~Mild = AE did not limit usual activities; subject may have experienced slight discomfort.~Moderate = AE resulted in some limitation of usual activities; subject may have experienced significant discomfort.~Severe = AE resulted in an inability to carry out usual activities; subject may have experienced intolerable discomfort/ pain.~Relationship to Investigational Medicinal Products (IMP) Unlikely = Slight, but remote, chance that AE was caused by IMP. Possible = Reasonable suspicion that the AE was caused by IMP. Probable = Most likely that AE was caused by IMP." (NCT03642873)
Timeframe: Upto Day 17

,,
InterventionEvents (Number)
TEAE by severity: MildTEAE by severity: ModerateTEAE by severity: SevereRelationship to IMP - UnlikelyRelationship to IMP - PossibleRelationship to IMP - Probable
Treatment A700430
Treatment B1210085
Treatment C25001816

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Area Under Plasma Concentration-time Curve From Time 0 to the Last Measurable Concentration (AUC(0-t)) of Guaifenesin

Pharmacokinetic Parameter AUC(0-t) The area under the plasma concentration versus time curve from time 0 to time of the last measurable concentration. (NCT03642873)
Timeframe: 0 (pre-dose), 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.5, 6, 7, 8, 8.5, 9, 9.5, 10, 11, 13, 16, 20, 24, and 26 hours Post dose

Interventionng*hr/mL (Mean)
Treatment A (Reference) - Plasma Guaifenesin8286.2
Treatment C (Test) - Plasma Guaifenesin8186.7
Treatments B (Reference) - Plasma Hydrocodone Bitartrate133.36
Treatment C (Test) - Plasma Hydrocodone Bitartrate132.99

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Apparent Terminal Elimination Half-life (T1/2) of Guaifenesin

Apparent first-order terminal elimination half-life was calculated as 0.693/Kel. (NCT03642873)
Timeframe: 0 (pre-dose), 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.5, 6, 7, 8, 8.5, 9, 9.5, 10, 11, 13, 16, 20, 24, and 26 hours Post dose

Interventionhr (Mean)
Treatment A (Reference) - Plasma Guaifenesin4.82
Treatment C (Test) - Plasma Guaifenesin5.34
Treatments B (Reference) - Plasma Hydrocodone Bitartrate4.71
Treatment C (Test) - Plasma Hydrocodone Bitartrate4.60

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Apparent Terminal Elimination Rate Constant (Kel) of Guaifenesin

Apparent first-order terminal elimination rate constant calculated from a semi-log plot of the plasma concentration versus time curve. The parameter was calculated by linear least-squares regression analysis using the maximum number of points in the terminal log-linear phase. (NCT03642873)
Timeframe: 0 (pre-dose), 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.5, 6, 7, 8, 8.5, 9, 9.5, 10, 11, 13, 16, 20, 24, and 26 hours Post dose

Intervention1/hr (Mean)
Treatment A (Reference) - Plasma Guaifenesin0.205
Treatment C (Test) - Plasma Guaifenesin0.207
Treatments B (Reference) - Plasma Hydrocodone Bitartrate0.151
Treatment C (Test) - Plasma Hydrocodone Bitartrate0.155

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Area Under Plasma Concentration-time Curve From Time 0 to Infinity (AUC(0-inf)) of Guaifenesin

The area under the plasma concentration versus time curve from time 0 to infinity, calculated as AUC(0-t) + Ct/ Kel, where Ct is the last measurable concentration. (NCT03642873)
Timeframe: 0 (pre-dose), 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.5, 6, 7, 8, 8.5, 9, 9.5, 10, 11, 13, 16, 20, 24, and 26 hours Post dose

Interventionng*hr/mL (Mean)
Treatment A (Reference) - Plasma Guaifenesin8501.5
Treatment C (Test) - Plasma Guaifenesin8347.8
Treatments B (Reference) - Plasma Hydrocodone Bitartrate140.44
Treatment C (Test) - Plasma Hydrocodone Bitartrate139.70

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Time to Maximum Observed Plasma Concentration (Tmax) of Guaifenesin

Pharmacokinetic Parameter Tmax is the time of the maximum observed plasma concentration. (NCT03643575)
Timeframe: 0 (Pre-dose), 0.5, 0.75, 1, 1.5, 2, 3, 4, 4.5, 4.75, 5, 5.5, 6, 7, 8, 8.5, 8.75, 9, 9.5, 10, 11, 12, 14 and 16 hours

Interventionhr (Mean)
Treatment A2.66
Treatment B2.94
Treatment C3.91

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Peak Plasma Concentrations at Steady State (Swing) of Guaifenesin

Pharmacokinetic Parameter Swing is Calculated as (Cmax,ss - Cmin,ss) / Cmin,ss. (NCT03643575)
Timeframe: 0 (Pre-dose), 0.5, 0.75, 1, 1.5, 2, 3, 4, 4.5, 4.75, 5, 5.5, 6, 7, 8, 8.5, 8.75, 9, 9.5, 10, 11, 12, 14 and 16 hours

InterventionPercentage (Mean)
Treatment A16.19
Treatment B15.62
Treatment C0.750

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Observed Plasma Concentration at the End of Dosing Interval at Steady State (Cmin,ss) of Guaifenesin Following the Third Dose

Observed plasma concentration at the end of the dosing interval following the third dose (that is, 4 hours following the third dose). (NCT03643575)
Timeframe: 0 (Pre-dose), 0.5, 0.75, 1, 1.5, 2, 3, 4, 4.5, 4.75, 5, 5.5, 6, 7, 8, 8.5, 8.75, 9, 9.5, 10, 11, 12, 14 and 16 hours

Interventionng/mL (Mean)
Treatment A60.3
Treatment B55.1
Treatment C73.6

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Maximum Observed Plasma Concentration (Cmax) of Guaifenesin

Pharmacokinetic Parameter Cmax is the Maximum observed plasma concentration. (NCT03643575)
Timeframe: 0 (Pre-dose), 0.5, 0.75, 1, 1.5, 2, 3, 4, 4.5, 4.75, 5, 5.5, 6, 7, 8, 8.5, 8.75, 9, 9.5, 10, 11, 12, 14 and 16 hours

Interventionng/mL (Mean)
Treatment A1730
Treatment B1230
Treatment C1110

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Maximum Measured Plasma Concentration at Steady State (Cmax,ss) of Guaifenesin Following the Third Dose

Pharmacokinetic Parameter Cmax,ss is the Maximum observed plasma concentration following the third dose. (NCT03643575)
Timeframe: 0 (Pre-dose), 0.5, 0.75, 1, 1.5, 2, 3, 4, 4.5, 4.75, 5, 5.5, 6, 7, 8, 8.5, 8.75, 9, 9.5, 10, 11, 12, 14 and 16 hours

Interventionng/mL (Mean)
Treatment A876
Treatment B765
Treatment C796

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Degree of Fluctuation (DF) of Guaifenesin

DF is the Degree of Fluctuation Index, calculated as (Cmax,ss - Cmin,ss) / Cav. (NCT03643575)
Timeframe: 0 (Pre-dose), 0.5, 0.75, 1, 1.5, 2, 3, 4, 4.5, 4.75, 5, 5.5, 6, 7, 8, 8.5, 8.75, 9, 9.5, 10, 11, 12, 14 and 16 hours

InterventionPercent fluctuation in concentration (Mean)
Treatment A2.220
Treatment B2.312
Treatment C2.463

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Average Plasma Concentration (Cav) of Guaifenesin Following the Third Dose

"Average plasma concentration (Cav) following the third dose, calculated as AUC(8-12) divided by the dosing interval, 4.~Cav is calculated as AUC(8-12) / dosing interval, 4" (NCT03643575)
Timeframe: 8, 8.5, 8.75, 9, 9.5, 10, 11 and 12 hours

Interventionng/mL (Mean)
Treatment A357
Treatment B313
Treatment C300

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Area Under the Plasma Concentration Versus Time Curve From Time 0 to the Time of the Last Measurable Concentration [AUC(0-t)] of Guaifenesin

AUC(0-t) is the area under the plasma concentration versus time curve from time 0 to the time of the last measurable concentration, as calculated by the linear trapezoidal method. (NCT03643575)
Timeframe: 0 (Pre-dose), 0.5, 0.75, 1, 1.5, 2, 3, 4, 4.5, 4.75, 5, 5.5, 6, 7, 8, 8.5, 8.75, 9, 9.5, 10, 11, 12, 14 and 16 hours

Interventionng*hr/mL (Mean)
Treatment A5588.99
Treatment B4369.98
Treatment C4223.74

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Area Under Plasma Concentration Versus Time Curve From Time 8 to 12 Hours [AUC(8-12)] of Guaifenesin

AUC(8-12) is the area under the plasma concentration versus time curve from time 8 to 12 hours postdose (relative to first dose), as calculated by the linear trapezoidal method. (NCT03643575)
Timeframe: 8, 8.5, 8.75, 9, 9.5, 10, 11 and 12 hours

Interventionng*hr/mL (Mean)
Treatment A1427.70
Treatment B1253.09
Treatment C1198.55

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Area Under Plasma Concentration Versus Time Curve From Time 0 to Infinity [AUC(0-inf)] of Guaifenesin

AUC(0-inf) is the area under the plasma concentration versus time curve from time 0 to infinity, calculated as AUC(0-t) + Ct/Kel, where Ct was the last measurable concentration and Kel is the apparent first-order terminal elimination rate constant. (NCT03643575)
Timeframe: 0 (Pre-dose), 0.5, 0.75, 1, 1.5, 2, 3, 4, 4.5, 4.75, 5, 5.5, 6, 7, 8, 8.5, 8.75, 9, 9.5, 10, 11, 12, 14 and 16 hours

Interventionng*hr/mL (Mean)
Treatment A5596.33
Treatment B4427.06
Treatment C4232.61

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Area Under Plasma Concentration Versus Time Curve From 0 to 4 Hours [AUC(0-4)] of Guaifenesin

AUC(0-4) is the area under the plasma concentration versus time curve from time 0 to 4 hours post dose (relative to first dose), as calculated by the linear trapezoidal method. (NCT03643575)
Timeframe: 0 (Pre-dose), 0.5, 0.75, 1, 1.5, 2, 3 and 4 hours

Interventionng*hr/mL (Mean)
Treatment A2013.16
Treatment B1490.15
Treatment C1414.18

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Area Under Plasma Concentration Curve Ratio (AUCR) of Guaifenesin

Pharmacokinetic Parameter AUCR is the Ratio of AUC(0-t) to AUC(0-inf). AUCR = AUC(0-t) / AUC(0-inf). (NCT03643575)
Timeframe: 0 (Pre-dose), 0.5, 0.75, 1, 1.5, 2, 3, 4, 4.5, 4.75, 5, 5.5, 6, 7, 8, 8.5, 8.75, 9, 9.5, 10, 11, 12, 14 and 16 hours

InterventionRatio (Mean)
Treatment A0.9986
Treatment B0.9982
Treatment C0.9978

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Apparent First-order Terminal Elimination Half-life (T1/2) of Guaifenesin

T1/2 is the apparent first-order terminal elimination half-life, calculated as ln(2)/Kel. (NCT03643575)
Timeframe: 0 (Pre-dose), 0.5, 0.75, 1, 1.5, 2, 3, 4, 4.5, 4.75, 5, 5.5, 6, 7, 8, 8.5, 8.75, 9, 9.5, 10, 11, 12, 14 and 16 hours

Interventionhr (Mean)
Treatment A0.961
Treatment B1.04
Treatment C0.941

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Accumulation Index (AI) of Guaifenesin

AI is the accumulation index, calculated as AUC(8-12) / AUC(0-4). (NCT03643575)
Timeframe: 0 (Pre-dose), 0.5, 0.75, 1, 1.5, 2, 3, 4 hours and 8, 8.5, 8.75, 9, 9.5, 10, 11, 12 hours

InterventionRatio (Mean)
Treatment A0.7056
Treatment B0.8420
Treatment C0.8592

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Apparent First-order Terminal Elimination Rate Constant (Kel) of Guaifenesin

Kel is the apparent first-order terminal elimination rate constant calculated from a semi-log plot of the plasma concentration versus time curve. The parameter was calculated by linear least-squares (LS) regression analysis using the maximum number of points (e.g., 3 or more non-zero plasma concentrations) in the terminal log-linear phase. (NCT03643575)
Timeframe: 0 (Pre-dose), 0.5, 0.75, 1, 1.5, 2, 3, 4, 4.5, 4.75, 5, 5.5, 6, 7, 8, 8.5, 8.75, 9, 9.5, 10, 11, 12, 14 and 16 hours

Intervention1/hr (Mean)
Treatment A0.729
Treatment B0.677
Treatment C0.750

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Number of Participants With Adverse Events (AEs)

"Intensity was determined by the Investigator. For symptomatic Adverse Events (AEs) the following definitions were applied.~Mild = AE did not limit usual activities; subject may have experienced slight discomfort.~Moderate = AE resulted in some limitation of usual activities; subject may have experienced significant discomfort.~Severe = AE resulted in an inability to carry out usual activities; subject may have experienced intolerable discomfort/pain.~Relationship to Investigational Medicinal Products (IMP)~Unlikely = Slight, but remote, chance that AE was caused by IMP. Possible = Reasonable suspicion that the AE was caused by IMP. Probable = Most likely that AE was caused by IMP." (NCT03643575)
Timeframe: Up to day 2 (Period 3)

,,
Interventionparticipants (Number)
TEAE by severity: MildTEAE by severity: ModerateTEAE by severity: SevereRelationship to IMP - UnlikelyRelationship to IMP - PossibleRelationship to IMP - Probable
Treatment A520510
Treatment B100100
Treatment C410220

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Time to Maximum Observed Plasma Concentration at Steady State (Tmax,ss) of Guaifenesin Following the Third Dose

Pharmacokinetic Parameter Tmax, ss is the time of the maximum observed plasma concentration following the third dose. (NCT03643575)
Timeframe: 0 (Pre-dose), 0.5, 0.75, 1, 1.5, 2, 3, 4, 4.5, 4.75, 5, 5.5, 6, 7, 8, 8.5, 8.75, 9, 9.5, 10, 11, 12, 14 and 16 hours

Interventionhr (Mean)
Treatment A8.70
Treatment B8.67
Treatment C9.02

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Apparent Terminal Elimination Rate Constant (Kel) of Guaifenesin

Apparent first-order terminal elimination rate constant calculated from a semi-log plot of the plasma concentration versus time curve. The parameter was calculated by linear least-squares (LS) regression analysis using the maximum number of points (e.g. 3 or more non-zero plasma concentrations) in the terminal log-linear phase. (NCT03644095)
Timeframe: 0 (pre-dose), 0.5, 0.75, 1, 1.5, 2, 3, 4, 4.5, 4.75, 5, 5.5, 6, 7, 8, 8.5, 8.75, 9, 9.5, 10, 11, 12, 14, 16 and 24 hours (post-dose) on Day 1 and 2

Intervention1/hr (Mean)
Test (Treatment A)0.373
Reference (Treatment B)0.716

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Area Under Plasma Concentration Curve Ratio (AUCR) of Guaifenesin

Pharmacokinetic Parameter AUCR is the ratio of AUC(0-t) to AUC(0-inf). AUCR = AUC(0-t) / AUC(0-inf) (NCT03644095)
Timeframe: 0 (pre-dose), 0.5, 0.75, 1, 1.5, 2, 3, 4, 4.5, 4.75, 5, 5.5, 6, 7, 8, 8.5, 8.75, 9, 9.5, 10, 11, 12, 14, 16 and 24 hours (post-dose) on Day 1 and 2

InterventionRatio (Mean)
Test (Treatment A)0.988
Reference (Treatment B)0.998

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Area Under Plasma Concentration-time Curve From Time 0 to Infinity (AUC(0-inf)) of Guaifenesin

Area under the plasma concentration versus time curve from time 0 to infinity, calculated as AUC 0-t + C last/kel, where C last is the last measurable concentration and kel is the apparent first-order terminal elimination rate constant. (NCT03644095)
Timeframe: 0 (pre-dose), 0.5, 0.75, 1, 1.5, 2, 3, 4, 4.5, 4.75, 5, 5.5, 6, 7, 8, 8.5, 8.75, 9, 9.5, 10, 11, 12, 14, 16 and 24 hours (post-dose) on Day 1 and 2

Interventionng*hr/mL (Mean)
Test (Treatment A)3442.0
Reference (Treatment B)4456.4

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Area Under Plasma Concentration-time Curve From Time 0 to the Last Measurable Concentration (AUC(0-t)) of Guaifenesin

Area under the plasma concentration versus time curve from time 0 to the time of the last measurable concentration, as calculated by the linear trapezoidal method. (NCT03644095)
Timeframe: 0 (pre-dose), 0.5, 0.75, 1, 1.5, 2, 3, 4, 4.5, 4.75, 5, 5.5, 6, 7, 8, 8.5, 8.75, 9, 9.5, 10, 11, 12, 14, 16 and 24 hours (post-dose) on Day 1 and 2

Interventionng*hr/mL (Mean)
Test (Treatment A)3404.7
Reference (Treatment B)4447.1

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Maximum Observed Plasma Concentration (Cmax) of Guaifenesin

Pharmacokinetic Parameter (Cmax) Maximum observed plasma concentration. (NCT03644095)
Timeframe: 0 (pre-dose), 0.5, 0.75, 1, 1.5, 2, 3, 4, 4.5, 4.75, 5, 5.5, 6, 7, 8, 8.5, 8.75, 9, 9.5, 10, 11, 12, 14, 16 and 24 hours (post-dose) on Day 1 and 2

Interventionng/mL (Mean)
Test (Treatment A)857
Reference (Treatment B)1390

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Time to Maximum Observed Concentration (Tmax) of Guaifenesin

Pharmacokinetic Parameter (Tmax) Time of the maximum observed plasma concentration. (NCT03644095)
Timeframe: 0 (pre-dose), 0.5, 0.75, 1, 1.5, 2, 3, 4, 4.5, 4.75, 5, 5.5, 6, 7, 8, 8.5, 8.75, 9, 9.5, 10, 11, 12, 14, 16 and 24 hours (post-dose) on Day 1 and 2

Interventionhr (Mean)
Test (Treatment A)0.885
Reference (Treatment B)3.05

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Number of Adverse Events (AE) of Participants

Mild = AE does not limit usual activities;subject may experience slight discomfort; Moderate = AE results in some limitation of usual activities; subject may experience significant discomfort; Severe = AE results in an inability to carry out usual activities; Probable = Most likely that the AE was caused by study drug; Possible = Reasonable suspicion that the AE was caused by the study drug; Unlikely = Slight but remote chance that the AE was caused by study drug but the balance of judgment is that it was most likely not due to the study drug. (NCT03644095)
Timeframe: Upto Day 2

,
InterventionEvents (Number)
TEAE by severity: MildTEAE by severity: ModerateTEAE by severity: SevereRelationship to Drug: ProbableRelationship to Drug: PossibleRelationship to Drug: Unlikely
Reference (Treatment B)800035
Test (Treatment A)700061

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Apparent Terminal Elimination Half-life (t1/2) of Guaifenesin

Apparent first-order terminal elimination half-life, calculated as ln(2)/kel. (NCT03644095)
Timeframe: 0 (pre-dose), 0.5, 0.75, 1, 1.5, 2, 3, 4, 4.5, 4.75, 5, 5.5, 6, 7, 8, 8.5, 8.75, 9, 9.5, 10, 11, 12, 14, 16 and 24 hours (post-dose) on Day 1 and 2

Interventionhr (Mean)
Test (Treatment A)2.26
Reference (Treatment B)0.989

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