fesoterodine: a muscarinic antagonist for treatment of overactive bladder [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 6918558 |
| CHEMBL ID | 1201764 |
| CHEBI ID | 135920 |
| SCHEMBL ID | 121127 |
| MeSH ID | M0518591 |
| Synonym |
|---|
| AB01274866-01 |
| AKOS015841710 |
| fesoterodine (inn) |
| D07226 |
| CHEBI:135920 |
| fesoterodine |
| feso |
| DB06702 |
| [2-[(1r)-3-[di(propan-2-yl)amino]-1-phenylpropyl]-4-(hydroxymethyl)phenyl] 2-methylpropanoate |
| 621g617227 , |
| fesoterodine [inn:ban] |
| unii-621g617227 |
| propanoic acid, 2-methyl-, 2-((1r)-3-(bis(1-methylethyl)amino)-1-phenylpropyl)-4-(hydroxymethyl)phenyl ester |
| 286930-02-7 |
| DCCSDBARQIPTGU-HSZRJFAPSA-N |
| CHEMBL1201764 |
| NCGC00346540-01 |
| fesoterodine [vandf] |
| fesoterodine [who-dd] |
| fesoterodine [mi] |
| fesoterodine [mart.] |
| fesoterodine [inn] |
| CS-M2392 |
| SCHEMBL121127 |
| [2-[(1r)-3-(di(propan-2-yl)amino)-1-phenylpropyl]-4-(hydroxymethyl)phenyl] 2-methylpropanoate |
| gtpl7473 |
| AC-32493 |
| AB01274866_02 |
| DTXSID80182853 , |
| 2-[(1r)-3-[bis(propan-2-yl)amino]-1-phenylpropyl]-4-(hydroxymethyl)phenyl 2-methylpropanoate |
| (r) fesoterodine |
| NCGC00346540-02 |
| Q4482372 |
| (r)-2-(3-(diisopropylamino)-1-phenylpropyl)-4-(hydroxymethyl)phenyl isobutyrate |
| HY-70053 |
| NCGC00346540-03 |
| STARBLD0000599 |
| dtxcid20105344 |
| fesoterodinum |
| g04bd11 |
| fesoterodine (mart.) |
| fesoterodina |
| EN300-25668967 |
Fesoterodine is a muscarinic receptor antagonist approved for the treatment of overactive bladder (OAB) in adults and neurogenic detrusor overactivity (NDO) in pediatric patients. The drug is a prodrug that is structurally and functionally associated with tolterodine and it is the novel drug for OAB treatment.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Fesoterodine has a favorable benefit-risk profile in 6‒<18-year-old patients with NDO and may represent an additional option for pediatric NDO treatment." | ( Fesoterodine treatment of pediatric patients with neurogenic detrusor overactivity: A 24-week, randomized, open-label, phase 3 study. Crook, TJ; Darekar, A; Jones, P; Kitta, T; Lindsay, M; Malhotra, B; Mallen, S; Nieto, A; Shahin, MH, 2023) | 3.8 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Fesoterodine was found to produce significant improvements in the treatment of overactive bladder symptoms compared with placebo." | ( Fesoterodine for the treatment of overactive bladder. Dolder, C; Olin, JL; Tzefos, M, 2009) | 2.52 |
Fesoterodine treatment had slightly higher total costs than mirabegron (3,296€vs. 3,300€) Treatment led to clinically meaningful improvements across all included patient reported outcomes.
Fesoterodine was well tolerated, with common adverse events such as headache and dry mouth recognized as antimuscarinic class effects. Incidence of treatment-related adverse events with fesoteradine was similar in women with hypertension (39%)
Fesoterodine demonstrated a pharmacokinetic (PK) profile that was favorable for once-daily dosing. Tolterodine, and not 5-HMT, was the principal source of variability.
| Excerpt | Reference | Relevance |
|---|---|---|
| " The mean Cmax and AUC0-t in PMs were approximately twice those observed in EMs." | ( Pharmacokinetic profile of fesoterodine. Gandelman, K; Guan, Z; Malhotra, B; Wood, N, 2008) | 0.64 |
| "Fesoterodine demonstrated a pharmacokinetic (PK) profile that was favorable for once-daily dosing." | ( Pharmacokinetic profile of fesoterodine. Gandelman, K; Guan, Z; Malhotra, B; Wood, N, 2008) | 2.09 |
| " 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) | 0.87 |
| " 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) | 0.64 |
| "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) | 0.84 |
| " The median time of observed maximum drug concentration (5-6 hours) and mean terminal half-life (6-7 hours) of 5-HMT are unaffected by renal impairment." | ( Assessment of the effects of renal impairment on the pharmacokinetic profile of fesoterodine. Gandelman, K; Malhotra, B; Sachse, R; Wood, N, 2009) | 0.58 |
| " time to maximum plasma concentration terminal elimination half-life and mean residence time), did not differ markedly between the fed and fasted states." | ( Influence of food on the pharmacokinetic profile of fesoterodine. Malhotra, B; Sachse, R; Wood, N, 2009) | 0.6 |
| " Pharmacodynamic variables included spontaneous salivary secretion (Studies 1 and 2) and residual urine volume (Study 2 only)." | ( Influence of age, gender, and race on pharmacokinetics, pharmacodynamics, and safety of fesoterodine. Malhotra, BK; Sachse, R; Wood, N, 2009) | 0.58 |
| "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) | 0.85 |
| " Pharmacokinetic endpoints were area under the plasma concentration-time curve from time 0 to infinity (AUC(0,∞)), maximum plasma concentration (C(max)), AUC from time 0 to the time of the last quantifiable concentration (AUC(0,last)), time to C(max) (t(max) ), and half-life (t(1/2)) for S- and R-warfarin." | ( Effects of fesoterodine on the pharmacokinetics and pharmacodynamics of warfarin in healthy volunteers. Alvey, C; Duczynski, G; Gandelman, K; Gong, J; Li, X; Malhotra, B, 2011) | 0.76 |
| "Across all pharmacokinetic and pharmacodynamic comparisons, the point estimates of treatment ratio (warfarin co-administered with fesoterodine vs." | ( Effects of fesoterodine on the pharmacokinetics and pharmacodynamics of warfarin in healthy volunteers. Alvey, C; Duczynski, G; Gandelman, K; Gong, J; Li, X; Malhotra, B, 2011) | 0.96 |
| " PK endpoints, including the area under the plasma concentration-time curve from 0 to infinity (AUC(0,∞)), maximum plasma concentration (C(max) ), time to C(max) (t(max) ), and half-life (t(1/2) ), were assessed for 5-hydroxymethyl tolterodine (5-HMT), the active moiety of fesoterodine." | ( Effects of the moderate CYP3A4 inhibitor, fluconazole, on the pharmacokinetics of fesoterodine in healthy subjects. Alvey, C; Dickins, M; Duczynski, G; Gandelman, K; Jumadilova, Z; Li, X; Malhotra, B, 2011) | 0.77 |
| " This study aimed to evaluate the safety profile and pharmacokinetic characteristics of multiple oral doses of sustained-release fesoterodine (fesoterodine SR) in healthy Korean males." | ( Multiple-dose pharmacokinetics of fesoterodine sustained-release in healthy Korean volunteers. Cho, JY; Jang, IJ; Lee, S; Lim, KS; Shin, D; Shin, KH; Shin, SG; Yu, KS, 2012) | 0.86 |
| " The CYP2D6 genotype was analyzed using polymerase chain reaction (PCR) methods to assess the effect of genetic polymorphisms on the pharmacokinetic parameters." | ( Multiple-dose pharmacokinetics of fesoterodine sustained-release in healthy Korean volunteers. Cho, JY; Jang, IJ; Lee, S; Lim, KS; Shin, D; Shin, KH; Shin, SG; Yu, KS, 2012) | 0.66 |
| " The mean AUCτ and Cmax of 5-HMT increased in approximately the same proportion as the dose increased." | ( Multiple-dose pharmacokinetics of fesoterodine sustained-release in healthy Korean volunteers. Cho, JY; Jang, IJ; Lee, S; Lim, KS; Shin, D; Shin, KH; Shin, SG; Yu, KS, 2012) | 0.66 |
| " Ten pharmacokinetic studies and three efficacy/safety studies in overactive bladder (OAB) patients were pooled for the population pharmacokinetic analysis." | ( Population pharmacokinetics of the 5-hydroxymethyl metabolite of tolterodine after administration of fesoterodine sustained release tablet in Western and East Asian populations. Malhotra, B; Oishi, M; Tomono, Y; Yamagami, H, 2014) | 0.62 |
| " Potential drug-drug interactions (DDIs) following coadministration of these 2 overactive bladder treatments were estimated using physiologically based pharmacokinetic models, developed and verified by comparing predicted and observed pharmacokinetic profiles from clinical studies." | ( Physiologically Based Pharmacokinetic Modeling Suggests Limited Drug-Drug Interaction for Fesoterodine When Coadministered With Mirabegron. Goosen, TC; Lin, J; Malhotra, B; Tse, S; Yamagami, H, 2019) | 0.74 |
| "A one-compartment model with first-order absorption and a lag time, which included the effects of body weight, sex, cytochrome (CYP) 2D6 metabolizer status and fesoterodine formulation on pharmacokinetic parameters, best described the 5-HMT pharmacokinetics." | ( Population Pharmacokinetic and Pharmacodynamic Modeling of Fesoterodine in Pediatric Patients with Neurogenic Detrusor Overactivity. Darekar, A; Malhotra, BK; Sano, Y; Shahin, M; Shoji, S; Sweeney, K, 2023) | 1.35 |
| " Population pharmacokinetic and pharmacokinetic/pharmacodynamic models were developed for 5-HMT based on data from two pediatric clinical trials that included 142 patients of age ≥ 6 years with OAB or NDO." | ( Population Pharmacokinetic and Pharmacodynamic Modeling of Fesoterodine in Pediatric Patients with Neurogenic Detrusor Overactivity. Darekar, A; Malhotra, BK; Sano, Y; Shahin, M; Shoji, S; Sweeney, K, 2023) | 1.15 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "To assess drug-drug interactions of fesoterodine with cytochrome P450 (CYP) 3A4 inhibitor (ketoconazole), inducer (rifampicin), and substrates (ethinylestradiol and levonorgestrel)." | ( Evaluation of drug-drug interactions with fesoterodine. Malhotra, B; Sachse, R; Wood, N, 2009) | 0.89 |
| " Potential drug-drug interactions (DDIs) following coadministration of these 2 overactive bladder treatments were estimated using physiologically based pharmacokinetic models, developed and verified by comparing predicted and observed pharmacokinetic profiles from clinical studies." | ( Physiologically Based Pharmacokinetic Modeling Suggests Limited Drug-Drug Interaction for Fesoterodine When Coadministered With Mirabegron. Goosen, TC; Lin, J; Malhotra, B; Tse, S; Yamagami, H, 2019) | 0.74 |
Fesoterodine delivers 5-HMT consistently, regardless of CYP2D6 status, with up to 40% higher bioavailability compared with tolterodine.
The study was a randomized, open-label, two-period, two treatment crossover, single-dose study. Subjects received fesoterodine 4 mg once daily for 4 weeks; thereafter, daily dosage was maintained at 4 mg or increased to 8 mg based on the subject's and physician's subjective assessment of efficacy and tolerability.
| Excerpt | Relevance | Reference |
|---|---|---|
| "05) except micturition frequency, demonstrating a dose-response relationship." | ( Fesoterodine dose response in subjects with overactive bladder syndrome. Dmochowski, R; Guan, Z; Khullar, V; Nitti, V; Rovner, ES; Wang, J, 2008) | 1.79 |
| " 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) | 0.89 |
| "Fesoterodine dosage should not exceed 4 mg once daily when taken concomitantly with potent CYP3A4 inhibitors." | ( Evaluation of drug-drug interactions with fesoterodine. Malhotra, B; Sachse, R; Wood, N, 2009) | 2.06 |
| " Subjects received fesoterodine 4 mg once daily for 4 weeks; thereafter, daily dosage was maintained at 4 mg or increased to 8 mg based on the subject's and physician's subjective assessment of efficacy and tolerability." | ( Effects of flexible-dose fesoterodine on overactive bladder symptoms and treatment satisfaction: an open-label study. Choo, MS; Goldfischer, ER; Gong, J; Guan, Z; Morrow, JD; Tseng, LJ; Wyndaele, JJ, 2009) | 0.98 |
| "Subject demographics, such as age, gender, and race, do not have a clinically meaningful effect on 5-HMT pharmacokinetics or pharmacodynamics after single-dose administration of fesoterodine 8 mg; thus, no dosage adjustment is required for fesoterodine based on age, gender, or race." | ( Influence of age, gender, and race on pharmacokinetics, pharmacodynamics, and safety of fesoterodine. Malhotra, BK; Sachse, R; Wood, N, 2009) | 0.77 |
| " 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) | 0.84 |
| "Overall, there were linear dose-response relationships for placebo and the fesoterodine groups for the reduction in the number of voids/24 h and UUI episodes/week." | ( Response to fesoterodine in patients with an overactive bladder and urgency urinary incontinence is independent of the urodynamic finding of detrusor overactivity. Bavendam, T; Nitti, VW; Rovner, ES, 2010) | 0.97 |
| "In this randomized, open-label, two-period, two-treatment crossover, single-dose study, healthy subjects received daytime and nighttime oral dosing of fesoterodine 8-mg sustained-release tablets, separated by a minimum 60-h washout period." | ( The pharmacokinetic profile of fesoterodine 8 mg with daytime or nighttime dosing. Crownover, PH; Glue, P; LaBadie, R; MacDiarmid, SA; Malhotra, BK, 2010) | 0.85 |
| " The 21% reduction in the C(max) for nighttime dosing is unlikely to be clinically relevant." | ( The pharmacokinetic profile of fesoterodine 8 mg with daytime or nighttime dosing. Crownover, PH; Glue, P; LaBadie, R; MacDiarmid, SA; Malhotra, BK, 2010) | 0.65 |
| "Data from subjects enrolled in double-blind, placebo-controlled phase II and III trials were used for developing longitudinal dose-response models." | ( Modeling dose-response relationships of the effects of fesoterodine in patients with overactive bladder. Cardozo, L; El-Tahtawy, A; Guan, Z; Khullar, V; Malhotra, B; Staskin, D, 2010) | 0.61 |
| " The dose-response models can be used to predict outcomes for doses not studied or for patient subgroups underrepresented in clinical trials." | ( Modeling dose-response relationships of the effects of fesoterodine in patients with overactive bladder. Cardozo, L; El-Tahtawy, A; Guan, Z; Khullar, V; Malhotra, B; Staskin, D, 2010) | 0.61 |
| " Based on the results, a drug degradation pathway was proposed, and the validated LC method was successfully applied to the quantitative analysis of fesoterodine in tablet dosage forms, helping to improve quality control and to assure therapeutic efficacy." | ( Fesoterodine stress degradation behavior by liquid chromatography coupled to ultraviolet detection and electrospray ionization mass spectrometry. Sangoi, MS; Steppe, M; Todeschini, V, 2011) | 2.01 |
| "Available data suggest that fesoterodine dosage should not exceed 4 mg once daily when taken concomitantly with potent CYP3A4 inhibitors, such as ketoconazole." | ( Effects of the moderate CYP3A4 inhibitor, fluconazole, on the pharmacokinetics of fesoterodine in healthy subjects. Alvey, C; Dickins, M; Duczynski, G; Gandelman, K; Jumadilova, Z; Li, X; Malhotra, B, 2011) | 0.89 |
| "It is concluded that fesoterodine has the added advantage of flexible dosing over some other antimuscarinics." | ( Review of fesoterodine. Cardozo, L; Vella, M, 2011) | 1.09 |
| " Its once-daily dosing regime and the flexibility to increase the dose are appealing factors." | ( Fesoterodine in randomised clinical trials: an updated systematic clinical review of efficacy and safety. Bhide, A; Dell'Utri, C; Digesu, GA; Khullar, V, 2012) | 1.82 |
| " The mean (SD) areas under the plasma concentration-time curves during the dosing interval (AUCτ) of the 4 mg and 8 mg dose groups were 26." | ( Multiple-dose pharmacokinetics of fesoterodine sustained-release in healthy Korean volunteers. Cho, JY; Jang, IJ; Lee, S; Lim, KS; Shin, D; Shin, KH; Shin, SG; Yu, KS, 2012) | 0.66 |
| "Participants were randomized to fesoterodine or placebo for 12 weeks, with stratification according to age (>75 vs ≤ 75) and dosing time (morning vs evening)." | ( Flexible-dose fesoterodine in elderly adults with overactive bladder: results of the randomized, double-blind, placebo-controlled study of fesoterodine in an aging population trial. Bitoun, CE; Darekar, A; Khullar, V; Marschall-Kehrel, D; Michel, MC; Oelke, M; Osterloh, I; Wagg, A; Weinstein, D, 2013) | 1.03 |
| "Data from flexible-dose studies provide strong evidence that fesoterodine provides treatment benefit to individual subjects with OAB because of its true dose-response effect." | ( Flexible dosing with fesoterodine 4 and 8 mg: a systematic review of data from clinical trials. Arumi, D; MacDiarmid, S; Schneider, T; Scholfield, D; Wyndaele, JJ, 2014) | 0.96 |
| "0% changed the dosage (84." | ( Profile of oab patient on treatment with flexible-dose antimuscarinic drugs in daily clinical practice. Arumi, D; García-Mediero, JM; Lizarraga, I; Sánchez-Ballester, F; Sobrón-Bustamante, M, 2016) | 0.43 |
| " We also found that increasing value of total payment and increasing frequency of payments were both independently associated with increased odds of prescribing with a dose-response effect." | ( The Receipt of Industry Payments is Associated With Prescribing Promoted Alpha-blockers and Overactive Bladder Medications. Chang, SL; Dupree, JM; Kirk, PS; Modi, PK; Singer, EA; Wang, Y, 2018) | 0.48 |
| "Fesoterodine at a dosage of 4 mg for 12 weeks reduced the severity of symptoms of AD in patients with SCI and NBD, which was manifested by the stabilization of blood pressure and a decrease in the number of episodes of AD, which significantly improved the quality of life." | ( [Efficacy of fesoterodine for prevention of autonomic dysreflexia in patients with neurogenic dysfunction of the bladder after spinal cord injury]. Chalyi, ME; Frolova, MV; Kamalov, AA; Okhobotov, DA; Salyukov, RV, 2023) | 2.72 |
| Class | Description |
|---|---|
| diarylmethane | Any compound containing two aryl groups connected by a single C atom. |
| [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 | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 33.1734 | 0.0013 | 10.1577 | 42.8575 | AID1259256 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 29.4964 | 0.0096 | 10.5250 | 35.4813 | AID1479145; AID1479148 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| virion membrane | Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
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| AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1474167 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status | 2016 | Drug discovery today, Apr, Volume: 21, Issue:4 | DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
| AID1474166 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index | 2016 | Drug discovery today, Apr, Volume: 21, Issue:4 | DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 24 (12.06) | 29.6817 |
| 2010's | 143 (71.86) | 24.3611 |
| 2020's | 32 (16.08) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
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.
| This Compound (75.31) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 79 (38.73%) | 5.53% |
| Reviews | 32 (15.69%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 6 (2.94%) | 0.25% |
| Other | 87 (42.65%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
|---|---|---|---|---|---|---|---|
| Prevention of Fall in Older Adults With Overactive Bladdar [NCT03946124] | Phase 4 | 74 participants (Actual) | Interventional | 2015-07-25 | Completed | ||
| Treatment Persistence Among Patients With Overactive Bladder: A Retrospective Secondary Data Analysis in Asia Oceania [NCT03602508] | 5,589 participants (Actual) | Observational | 2018-07-20 | Completed | |||
| A Novel Stable Iron Isotope Method to Define Iron Needs and Improve Iron Nutrition in HIV+ and HIV- Children [NCT03572010] | 180 participants (Actual) | Interventional | 2018-09-27 | Completed | |||
| Open-label, Single-dose, Randomized, Crossover Study To Estimate The Relative Bioavailability Compared To Commercial Extended-release Tablet Formulation And The Effects Of Food Or Sprinkling On Applesauce For Fesoterodine Sustained-release Beads-in-capsul [NCT02160158] | Phase 1 | 24 participants (Anticipated) | Interventional | 2014-07-31 | Completed | ||
| Randomized Cross-Over Study of Fesoterodine on Urgency Episodes in Parkinson's Disease Population [NCT02385500] | Phase 4 | 5 participants (Actual) | Interventional | 2016-09-30 | Terminated(stopped due to Insufficient or untimely patient recruitment) | ||
| The Effect of Apo- and Holo-Lactoferrin and Dosing Regimen on Iron Absorption From a Maize-based Porridge in Kenyan Infants [NCT03617575] | 25 participants (Actual) | Interventional | 2018-12-11 | Completed | |||
| Efficacy and Tolerability of Fesoterodine and Oxybutynin XL for Overactive Bladder Syndrome in Children: a Comparative Study. [NCT02327936] | Phase 3 | 62 participants (Actual) | Interventional | 2014-12-31 | Completed | ||
| Comparative Urine Proteomic Studies of Overactive Bladder in Humans [NCT01367886] | 21 participants (Actual) | Interventional | 2010-08-31 | Completed | |||
| A Randomized Double-blinded Trial Comparing DEsmopressin to FEsoterodine in the Treatment of Severe Nocturia in Women Aged 65 and olDer: The DEFEND Trial [NCT02262936] | Phase 2/Phase 3 | 4 participants (Actual) | Interventional | 2015-07-31 | Terminated(stopped due to Poor recruitment) | ||
| A 12-Week, Multicenter, Open-Label, Single-Arm Study To Evaluate The Effects Of Fesoterodine On Treatment Satisfaction And Symptom Relief In Overactive Bladder Patients. [NCT00425100] | Phase 3 | 516 participants (Actual) | Interventional | 2007-01-31 | Completed | ||
| A 14 Week Randomized Parallel Group Placebo-Controlled Double-Blind Multicentre Study Of Fesoterodine 8 Mg In Overactive Bladder Patients With Sub-Optimal Response To Tolterodine 4 Mg Extended Release (ER). [NCT01302054] | Phase 4 | 990 participants (Actual) | Interventional | 2011-05-31 | Completed | ||
| A PHASE 1, OPEN-LABEL, SINGLE-DOSE, CROSSOVER STUDY TO ASSESS THE BIOEQUIVALENCE UNDER FED AND FASTED CONDITIONS OF FESOTERODINE BEADS-IN-CAPSULE SR7 AND SR4 FORMULATIONS, THE EFFECT OF FOOD ON THE PHARMACOKINETICS OF THE BEADS-IN-CAPSULE SR7 FORMULATION [NCT04452838] | Phase 1 | 37 participants (Actual) | Interventional | 2020-06-26 | Completed | ||
| The Effect of Encapsulation Material and Encapsulated Micronutrients on Iron Absorption in Iron Depleted Women Consuming Iron Fortified Bread. [NCT03332602] | 24 participants (Actual) | Interventional | 2018-04-04 | Completed | |||
| A Local, Multicentre, Open-Label, Extension Trial To Evaluate The Efficacy And Safety Of Fesoterodine Flexible Dose Regimen In Elderly Patients With Overactive Bladder [NCT01054222] | Phase 4 | 31 participants (Actual) | Interventional | 2010-05-31 | Completed | ||
| Observational Study In Patients With Overactive Bladder (OAB) Treated With Toviaz® After Failure Of Previous Antimuscarinic Therapy Due To Ineffectivity Or Intolerance. [NCT00691093] | 823 participants (Actual) | Observational | 2008-07-31 | Completed | |||
| A 12-Week, Randomized, Double-Blind, Placebo-Controlled, Parallel-Group, Multicenter Trial To Evaluate The Efficacy And Safety Of Fesoterodine Flexible Dose Regimen In Vulnerable Elderly Patients With Overactive Bladder. [NCT00928070] | Phase 4 | 566 participants (Actual) | Interventional | 2009-09-30 | Completed | ||
| Evaluating the Effect of Polyphenols on the Iron Bioavailability From Iron Chlorophyllin in Young Women Using the Iron Stable Isotopic Method [NCT04849832] | 40 participants (Actual) | Interventional | 2021-06-21 | Completed | |||
| A Prospective, Non-interventional, Registry Study of Patients Initiating Pharmacologic Therapy for Overactive Bladder in Taiwan, Korea and China [NCT03572231] | 805 participants (Actual) | Observational | 2018-07-19 | Completed | |||
| Inflammation in Women With Urgency Urinary Incontinence Treated With Anticholinergics [NCT04090190] | Phase 4 | 20 participants (Actual) | Interventional | 2019-10-30 | Completed | ||
| Neuropathic Investigation and Anticholinergic Treatment of Bladder Dysfunction in Diabetes and Stroke Patients [NCT00713921] | Early Phase 1 | 0 participants (Actual) | Interventional | 2009-09-15 | Withdrawn(stopped due to Lack of enrollment and loss of funding) | ||
| A 12-Week, Randomized, Double-Blind, Placebo-Controlled, Parallel-Group, Multicenter Trial To Evaluate The Efficacy And Safety Of A Fesoterodine Flexible Dose Regimen In Patients With Overactive Bladder. [NCT00536484] | Phase 3 | 896 participants (Actual) | Interventional | 2007-08-31 | Completed | ||
| An Open-Label, Randomized, Two-Way Crossover Study To Evaluate The Steady-State Effect Of Fesoterodine On The Pharmacokinetics And Pharmacodynamics Of A Single Supratherapeutic Dose Of Warfarin In Healthy Subjects. [NCT00914667] | Phase 1 | 14 participants (Anticipated) | Interventional | 2009-07-31 | Completed | ||
| An Open-Label, Randomized, Two-Way Crossover Study To Evaluate The Effect Of Fluconazole, A Moderate CYP3A4 Inhibitor, On The Single-Dose Pharmacokinetics Of Fesoterodine In Healthy Subjects. [NCT00911235] | Phase 1 | 28 participants (Actual) | Interventional | 2009-05-31 | Completed | ||
| "A Randomized, Double-Blind, Placebo-Controlled Study To Evaluate The Efficacy And Safety Of Fesoterodine As An Add-On Therapy In Men With Persistent Overactive Bladder Symptoms Under Monotherapy Of Alpha Blocker For Lower Urinary Tract Symptoms." [NCT00546637] | Phase 3 | 947 participants (Actual) | Interventional | 2007-11-30 | Completed | ||
| An Open-Label, Randomized, Single-Dose, Two-Way Crossover Bioequivalence Study Of 8 Mg Fesoterodine Extended-Release Tablets (Toviaz™), Manufactured At Zwickau Versus Vega Baja, In Healthy Subjects. [NCT00902681] | Phase 1 | 36 participants (Anticipated) | Interventional | 2009-06-30 | Completed | ||
| Post Marketing Surveillance Study To Observe Safety And Efficacy Of Toviaz (Registered) [NCT00879398] | 3,000 participants (Actual) | Observational | 2009-11-30 | Completed | |||
| A Randomized, Double Blind, Placebo Controlled, Parallel Group, Multiple Dose Study To Investigate The Effects Of 8 Mg Fesoterodine SR Tablets And 10 Mg Solifenacin Tablet On Gastrointestinal Transit In Healthy Female Subjects. [NCT00832650] | Phase 1 | 60 participants (Actual) | Interventional | 2009-04-30 | Terminated(stopped due to Protocol A0221057 was terminated on December 25, 2009 for futility. There were no safety concerns related to this decision.) | ||
| A 24-Week, Multi-Centre Trial, Comprising A 12-Week, Randomised, Double-Blind, Placebo-Controlled, Parallel-Group Phase Followed By A 12-Week Open-Label Phase, To Evaluate The Efficacy And Safety Of A Fesoterodine Flexible Dose Regimen In Elderly Patients [NCT00798434] | Phase 4 | 794 participants (Actual) | Interventional | 2008-06-30 | Completed | ||
| An Open-Label, Multicenter, Long Term Study to Evaluate the Safety, Tolerability and Efficacy of Fesoterodine in Patients With Overactive Bladder. [NCT00658684] | Phase 3 | 153 participants (Actual) | Interventional | 2008-02-29 | Completed | ||
| A Phase 1, Open-Label, Randomized, Single-Dose, 2-Cohort, 3-Way Crossover Study To Determine Bioequivalence Of 4 Mg And 8 Mg Fesoterodine SR Tablet Of Commercial Formulation And 8 Mg Fesoterodine SR Tablet Between Formulation E(1) And Formulation F And In [NCT00807118] | Phase 1 | 108 participants (Anticipated) | Interventional | 2008-10-31 | Completed | ||
| 12-Week, Randomized, Double-Blind, Double-Dummy,Placebo-Controlled, Parallel-Group, Multicenter Trial To Evaluate The Efficacy And Safety Of Fesoterodine In Comparison To Tolterodine ER In Patients With Overactive Bladder (OAB) [NCT00444925] | Phase 3 | 1,712 participants (Actual) | Interventional | 2007-04-30 | Completed | ||
| 12-Week, Randomized, Double-Blind, Double-Dummy, Placebo-Controlled, Parallel-Group, Multicenter Trial To Evaluate The Efficacy And Safety Of Fesoterodine In Comparison To Tolterodine ER In Patients With Overactive Bladder. [NCT00611026] | Phase 3 | 2,417 participants (Actual) | Interventional | 2008-02-29 | Completed | ||
| A Phase 2, Randomized, Double-Blind, Multi-Dose, Placebo-Controlled Crossover Study Of The Efficacy Of Fesoterodine In Increasing Urethral Pressure In Stress Urinary Incontinence Patients. [NCT01042236] | Phase 2 | 22 participants (Actual) | Interventional | 2009-01-31 | Completed | ||
| An Open-Label, Randomized, Single-Dose, Two-Way Crossover Bioequivalence Study Of 4 Mg Fesoterodine Extended-Release Tablets (Toviaz™), Manufactured At Zwickau Versus Vega Baja, In Healthy Subjects. [NCT00902187] | Phase 1 | 36 participants (Actual) | Interventional | 2009-05-31 | Completed | ||
| An Open Label Study to Measure the Efficacy of Fesoterodine (Toviaz) on Continued Detrusor Overactivity in Patients That Have Undergone Treatment for Bladder Outlet Obstruction [NCT00605319] | Phase 4 | 17 participants (Actual) | Interventional | 2010-01-31 | Completed | ||
| An Open-Label, Dose-Escalating Study Of The Pharmacokinetics, Safety And Tolerability Of Fesoterodine In Pediatric Overactive Bladder Patients Aged 8-17 Years. [NCT00857896] | Phase 2 | 21 participants (Actual) | Interventional | 2009-03-31 | Completed | ||
| A Phase 1, Open-Label, Randomized, Single-Dose, 2-Way Crossover Study To Determine Bioequivalence Of 4 Mg Fesoterodine SR Tablet Between Formulation D And Formulation E(1) In Healthy Subjects. [NCT00786240] | Phase 1 | 37 participants (Actual) | Interventional | 2009-01-31 | Completed | ||
| A 12 Week, Multi-centre, Open Label Study To Evaluate The Efficacy, Tolerability And Safety Of A Fesoterodine Flexible Dose Regimen In Patients With Overactive Bladder. [NCT00806494] | Phase 4 | 331 participants (Actual) | Interventional | 2009-02-28 | Completed | ||
| The Effect of Ovotransferrin and Lactoferrin on Iron Absorption From Ferrous Sulfate in Adult Women With Non-anemic Iron Deficiency: Stable Isotope Study [NCT05233709] | 35 participants (Actual) | Interventional | 2022-04-25 | Completed | |||
| Evaluation of Iron Bioavailability From Iron Chlorophyllin in Young Women Using the Iron Stable Isotopic Method [NCT04602247] | 55 participants (Actual) | Interventional | 2020-10-26 | Completed | |||
| A 4 Way Placebo And Active Controlled Study To Evaluate The Effects Of Fesoterodine On Cognitive Function In Healthy Elderly Subjects [NCT01161472] | Phase 1 | 20 participants (Actual) | Interventional | 2010-07-31 | Completed | ||
| A 12-Week, Randomized, Double-Blind, Placebo-Controlled, Parallel-Group, Multicenter, Dose-Finding Study To Evaluate The Efficacy, Tolerability And Safety Of Fesoterodine In Comparison To Placebo In Patients With Overactive Bladder. [NCT00561951] | Phase 2 | 951 participants (Actual) | Interventional | 2007-11-30 | Completed | ||
| Efficacy and Tolerability of Fesoterodine for Overactive Bladder Syndrome in Children: an Extension Study. [NCT02614482] | Phase 3 | 26 participants (Actual) | Interventional | 2015-10-31 | Completed | ||
| Facts Study (Fakten-studie): Non-interventional Study to Investigate Whether Information Provided to Patients Influences Satisfaction With Toviaz Therapy As Perceived by the Patient [NCT01091519] | 781 participants (Actual) | Observational | 2010-12-31 | Terminated(stopped due to See termination reason in detailed description.) | |||
| A Phase II, Open-Label Exploratory Study Investigating the Efficacy of Toviaz for Treatment of Adult Patients With Spinal Cord Injury With Neurogenic Detrusor Overactivity for Amelioration of Autonomic Dysreflexia(PIIR-AK-TOVIAZ-AD) [NCT02676154] | Phase 2 | 15 participants (Actual) | Interventional | 2016-02-25 | Completed | ||
| A Randomized, Double Blind, Placebo Controlled, Parallel Group, Multicenter Trial To Evaluate The Efficacy And Safety Of A Fesoterodine Flexible Dose Regimen In Patients With Symptoms Of Overactive Bladder Including Nocturnal Urinary Urgency. [NCT00911937] | Phase 4 | 963 participants (Actual) | Interventional | 2009-08-31 | Completed | ||
| Phase IV Study to Evaluate the Efficacy and Safety Imidafenacin Versus Fesoterodine in Patients With Overactive Bladder [NCT01578304] | Phase 4 | 207 participants (Actual) | Interventional | 2010-12-31 | Completed | ||
| Solifenacin Succinate vs. Fesoterodine A Comparison Trial for the Treatment of Bothersome Urgency Symptoms [NCT01595152] | 60 participants (Anticipated) | Interventional | 2012-05-31 | Recruiting | |||
| A 12-Week, Randomized, Double-Blind, Placebo Controlled, Parallel Group, Multicenter Trial In Overactive Bladder Subjects To Confirm The Efficacy Of 8 Mg Fesoterodine Compared To 4 Mg Fesoterodine. [NCT01302067] | Phase 4 | 2,012 participants (Actual) | Interventional | 2011-05-31 | Completed | ||
| A Phase IV, Randomized, Double-Blind, Placebo-Controlled, Single-Center Study of the Effects of Fesoterodine in Men at High Risk for Overactive Bladder/Detrusor Overactivity Post Robotic-Assisted Laparoscopic Prostatectomy ) [NCT01661166] | Phase 4 | 3 participants (Actual) | Interventional | 2012-01-31 | Completed | ||
| An Open-Label, Single-Dose, Randomized, Cross-Over Study To Estimate The Bioavailability And Food Effect Of 4 Mg Fesoterodine Extended Release Beads-In-Capsule Formulations Compared To Commercial Tablet Formulation In Healthy Volunteers [NCT01286454] | Phase 1 | 20 participants (Actual) | Interventional | 2010-12-31 | Completed | ||
| "A 13-Week, Single-Arm, Open-Label, Multicenter Study To Evaluate Refill Adherence And Satisfaction With Fesoterodine Plus Your Way Patient Support Plan In Patients With Symptoms Of Overactive Bladder." [NCT00943735] | 774 participants (Actual) | Observational | 2009-07-31 | Completed | |||
| Post Marketing Surveillance To Assess The Safety And Efficacy Of Fesoterodine (Toviaz) On Filipino Patients Diagnosed With Over-Active Bladder [NCT01260311] | 508 participants (Actual) | Observational | 2011-02-28 | Completed | |||
| DRUG USE INVESTIGATION FOR TOVIAZ [NCT01936870] | 2,521 participants (Actual) | Observational | 2013-10-01 | Completed | |||
| A Multi-center, Randomized, Placebo-controlled Clinical Trial Comparing Fesoterodine to Placebo in Women Diagnosed With Urge Urinary Incontinence by the 3 Incontinence Questions (3IQ). Followed by a Multi-center Open Label Clinical Cohort Study of Long-te [NCT00862745] | Phase 4 | 645 participants (Actual) | Interventional | 2009-01-31 | Completed | ||
| Urinary NGF, PGE2 and ATP: Potential Biomarkers for Diagnosis and Prediction of Treatment Efficacy in Overactive Bladder Patients [NCT01499069] | 191 participants (Actual) | Interventional | 2010-02-28 | Completed | |||
| Understanding the Response to Fesoterodine Through Genetic Evaluation in the Elderly [NCT01786967] | Phase 3 | 61 participants (Actual) | Interventional | 2012-09-30 | Completed | ||
| A Double Blind, Randomized Four Way Cross Over Study to Compare the Effect of Fesoterodine 4mg and 8mg Once Daily and Oxybutynin 5mg Twice Daily After Steady State Dosing Versus Placebo on Cognitive Function in Subjects With Overactive Bladder, Over the A [NCT02240459] | Phase 2 | 47 participants (Actual) | Interventional | 2016-08-31 | Completed | ||
| Validation of Instruments for Pragmatic Clinical Trials for Overatcive Bladder [NCT01925456] | Phase 1 | 75 participants (Actual) | Interventional | 2011-05-31 | Completed | ||
| Open-Label, Single-Dose, Randomized, Crossover Study To Estimate The Effects Of Food On The Pharmacokinetics Of Two Fesoterodine Sustained-Release Beads-In-Capsule Formulations And To Estimate The Relative Bioavailability Of One Or Both Formulations Compa [NCT01566760] | Phase 1 | 24 participants (Actual) | Interventional | 2012-05-31 | Completed | ||
| Iron Bioavailability From Salt Fortified With Ferrous Sulphate, Zinc Sulphate and Ascorbic Acid Encapsulated in a Polymer Jacket [NCT02353325] | 20 participants (Actual) | Interventional | 2016-03-31 | Completed | |||
| AN OPEN-LABEL, RANDOMIZED, SINGLE-DOSE, 4 PERIOD, 4 TREATMENT, 2 SEQUENCE, TWO 2 WAY CROSSOVER, BIOEQUIVALENCE STUDY IN HEALTHY PARTICIPANTS COMPARING 4 MG AND 8 MG FESOTERODINE EXTENDED RELEASE TABLETS (TOVIAZ(TM)), MANUFACTURED AT ZWICKAU VERSUS FREIBUR [NCT04478357] | Phase 1 | 18 participants (Actual) | Interventional | 2019-11-12 | Completed | ||
| Assessment of the Bioavailability of Iron in Iron Fortified Bouillon Cubes in Healthy Women [NCT02327299] | 24 participants (Actual) | Interventional | 2014-10-31 | Completed | |||
| LONG-TERM EXTENSION STUDY TO EVALUATE THE SAFETY OF FESOTERODINE IN JAPANESE PEDIATRIC SUBJECTS WITH SYMPTOMS OF DETRUSOR OVERACTIVITY ASSOCIATED WITH A NEUROLOGICAL CONDITION (NEUROGENIC DETRUSOR OVERACTIVITY) WHO HAVE COMPLETED 24 WEEKS TREATMENT IN STU [NCT02501928] | Phase 3 | 12 participants (Actual) | Interventional | 2015-06-05 | Completed | ||
| Prospective Randomized Trial of Percutaneous Tibial Nerve Stimulation (PTNS) Versus PTNS and Fesoterodine Fumarate [NCT01605617] | Phase 4 | 4 participants (Actual) | Interventional | 2012-06-30 | Terminated(stopped due to Low recruitment rate, and study patients were removed prior to completion) | ||
| A 24-WEEK RANDOMIZED, OPEN-LABEL, STUDY TO EVALUATE THE SAFETY AND EFFICACY OF FESOTERODINE IN SUBJECTS AGED 6 TO 17 YEARS WITH SYMPTOMS OF DETRUSOR OVERACTIVITY ASSOCIATED WITH A NEUROLOGICAL CONDITION (NEUROGENIC DETRUSOR OVERACTIVITY) [NCT01557244] | Phase 3 | 181 participants (Actual) | Interventional | 2012-07-02 | Completed | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||
Each item rated by subject on a Likert scale 1 (most favorable) to 6 (least favorable). Raw scores were transformed to a score from 0 to 100. Once transformed, higher scores represent more favorable outcome. (NCT00425100)
Timeframe: Baseline and Week 12
| Intervention | scores on a scale (Mean) |
|---|---|
| Open Label Baseline | 71.3 |
| Open Label Week 12 | 88.1 |
Module coded on scale (1-very satisfied to 5-very dissatisfied). Coding reversed algorithmically & results transformed: total score range 0-100. Higher final response value associated with better satisfaction. Satisfied on TSQ = very or somewhat satisfied; Not satisfied on TSQ =very or somewhat dissatisfied or neither dissatisfied nor satisfied. (NCT00425100)
Timeframe: Week 12
| Intervention | scores on a scale (Mean) | ||
|---|---|---|---|
| All Subjects (N=473) | Subjects satisfied on TSQ (n=377) | Subjects not satisfied on TSQ (n=96) | |
| Open Label Week 12 | 74.7 | 82.7 | 43.6 |
Number of Participants who responded satisfied = (very satisfied or somewhat satisfied) and dissatisfied = (somewhat dissatisfied or very dissatisfied) to the treatment satisfaction question. (NCT00425100)
Timeframe: Week 12
| Intervention | participants (Number) | ||
|---|---|---|---|
| Satisfied (very satisfied or somewhat satisfied) | Neither dissatisfied nor satisfied | Dissatisfied (somewhat or very dissatisfied) | |
| Open Label Week 12 | 378 | 42 | 54 |
Improvement: negative score change; No change: score change=0; Deterioration: positive score change (NCT00425100)
Timeframe: Baseline and Week 12
| Intervention | participants (Number) | ||
|---|---|---|---|
| Improvement | No change | Deterioration | |
| Open Label Week 12 | 405 | 72 | 10 |
Number of participants who responded satisfied = (very satisfied or somewhat satisfied) or dissatisfied = (somewhat dissatisfied or very dissatisfied) to the treatment satisfaction question at Week 12 in the safety set. (NCT00425100)
Timeframe: Week 12
| Intervention | participants (Number) | |||
|---|---|---|---|---|
| Satisfied (very satisfied or somewhat satisfied) | Neither Dissatisfied nor Satisfied | Dissatisfied (somewhat or very dissatisfied) | Missing Response (imputed as dissatisfied) | |
| Open Label Week 12 | 378 | 42 | 54 | 42 |
The mean number of micturitions per 24 hours is calculated as the total number of micturitions divided by the total number of diary days collected at that visit. (NCT00425100)
Timeframe: Baseline and Week 12
| Intervention | number of episodes (Mean) |
|---|---|
| Open Label Baseline | 12.7 |
| Open Label Week 12 | 9.7 |
The mean number of urgency episodes per 24 hours is calculated as the total number of micturitions with Bladder Sensation Scale (BSS) >= 3 divided by the total number of diary days collected at that visit. BSS: 5 point scale measuring need to urinate from 1=no urgency to 5=unable to hold; leak urine. (NCT00425100)
Timeframe: Baseline and Week 12
| Intervention | number of episodes (Mean) |
|---|---|
| Open Label Baseline | 10.0 |
| Open Label Week 12 | 5.0 |
The mean number of UUI episodes per 24 hours is calculated as the total number of micturitions with Bladder Sensation Scale (BSS) = 5 divided by the total number of diary days collected at that visit. BSS: 5 point scale measuring need to urinate from 1=no urgency to 5=unable to hold; leak urine. (NCT00425100)
Timeframe: Baseline and Week 12
| Intervention | number of episodes (Mean) |
|---|---|
| Open Label Baseline | 2.3 |
| Open Label Week 12 | 0.6 |
"The mean rating was calculated as the sum of rating scores on the Urinary Sensation Scale divided by the total number of micturitions with non-missing rating at that visit. The scale ranges from 1 no feeling of urgency to 5 unable to hold; leak urine." (NCT00425100)
Timeframe: Baseline and Week 12
| Intervention | scores on a scale (Mean) |
|---|---|
| Open Label Baseline | 3.2 |
| Open Label Week 12 | 2.5 |
"Nocturnal micturitions (synonymous with the term nighttime micturitions) were those recorded in the bedtime section of the bladder diary." (NCT00425100)
Timeframe: Baseline and Week 12
| Intervention | number of nocturnal micturitions (Mean) |
|---|---|
| Open Label Baseline | 2.6 |
| Open Label Week 12 | 1.8 |
Each item rated by subject on a Likert scale 1 (most favorable) to 6 (least favorable). Raw scores were transformed to a score from 0 to 100. Once transformed, higher scores represent more favorable outcome. (NCT00425100)
Timeframe: Baseline and Week 12
| Intervention | scores on a scale (Mean) |
|---|---|
| Open Label Baseline | 50.5 |
| Open Label Week 12 | 79.1 |
Each item rated by subject on a Likert scale 1 (most favorable) to 6 (least favorable). Raw scores were transformed to a score from 0 to 100. Once transformed, higher scores represent more favorable outcome. (NCT00425100)
Timeframe: Baseline and Week 12
| Intervention | scores on a scale (Mean) |
|---|---|
| Open Label Baseline | 44.7 |
| Open Label Week 12 | 75.3 |
Each item rated by subject on a Likert scale 1 (most favorable) to 6 (least favorable). Raw scores were transformed to a score from 0 to 100. Once transformed, higher scores represent more favorable outcome. (NCT00425100)
Timeframe: Baseline and Week 12
| Intervention | scores on a scale (Mean) |
|---|---|
| Open Label Baseline | 47.4 |
| Open Label Week 12 | 72.3 |
Improvement: positive score change; No improvement: zero or negative score change (NCT00425100)
Timeframe: Baseline and Week 12
| Intervention | participants (Number) | |
|---|---|---|
| Improvement | No improvement | |
| Open Label Week 12 | 237 | 248 |
Each item rated by subject on a Likert scale 1 (least symptom bother) to 6 (most symptom bother). Raw scores were transformed to a score from 0 to 100. Once transformed, higher scores represent less favorable outcome. (NCT00425100)
Timeframe: Baseline and Week 12
| Intervention | scores on a scale (Mean) |
|---|---|
| Open Label Baseline | 57.4 |
| Open Label Week 12 | 28.6 |
Each item rated by subject on a Likert scale 1 (most favorable) to 6 (least favorable). Raw scores were transformed to a score from 0 to 100. Once transformed, higher scores represent more favorable outcome. (NCT00425100)
Timeframe: Baseline and Week 12
| Intervention | scores on a scale (Mean) |
|---|---|
| Open Label Baseline | 52.2 |
| Open Label Week 12 | 78.3 |
"The PPBC score ranges from 1 no problems at all to 6 many severe problems." (NCT00425100)
Timeframe: Baseline and Week 12
| Intervention | scores on a scale (Mean) |
|---|---|
| Open Label Baseline | 4.9 |
| Open Label Week 12 | 3.1 |
Severe urgency episodes defined as Urinary Sensation Scale (USS) rating ≥4. Subjects rated the feeling of urgency associated with each micturition episode using USS provided in the bladder diary. Scale ranges from 1=no feeling of urgency to 5=unable to hold; leak urine; decrease indicates an improvement with respect to urgency symptoms. (NCT00425100)
Timeframe: Baseline and Week 12
| Intervention | number of episodes (Mean) |
|---|---|
| Open Label Baseline | 5.0 |
| Open Label Week 12 | 1.5 |
"The sum rating per 24 hours was calculated as the mean rating score on the Urinary Sensation Scale multiplied by the mean number of micturitions per 24 hours at that visit. The scale ranges from 1 no feeling of urgency to 5 unable to hold; leak urine." (NCT00425100)
Timeframe: Baseline and Week 12
| Intervention | scores on a scale (Mean) |
|---|---|
| Open Label Baseline | 40.4 |
| Open Label Week 12 | 25.2 |
"UPS scores range from 0 (I am usually not able to hold urine) to 2 (I am usually able to finish what I am doing before going to the toilet [without leaking])." (NCT00425100)
Timeframe: Baseline and Week 12
| Intervention | scores on a scale (Mean) |
|---|---|
| Open Label Baseline | 0.8 |
| Open Label Week 12 | 1.4 |
Percent change calculated as change in severe urgency episodes (USS rating >= to 4 in diary ) per 24 hours at that visit divided by the baseline number of severe urgency episodes per 24 hours, multiplied by 100. USS is 5-item scale measuring urinary urgency; range is 1 (no feeling of urgency) to 5 (unable to hold; leak urine). (NCT00444925)
Timeframe: Baseline, Week 1, Week 4, Week 12
| Intervention | percent change (Median) | ||
|---|---|---|---|
| Week 1 (n=306, 618, 618) | Week 4 [LOCF] (n=311, 630, 624) | Week 12 [LOCF] (n=311, 630, 625) | |
| Fesoterodine | -25.0 | -54.5 | -71.4 |
| Placebo | -9.4 | -25.0 | -48.0 |
| Tolterodine ER | -25.0 | -45.8 | -63.4 |
Percent change of urgency episodes (USS rating >= to 3 in diary) per 24 hours calculated as change in 24-hour mean at that visit divided by the baseline 24-hour mean multiplied by 100. USS: 5-item scale measuring urinary urgency; range is 1 (no feeling of urgency) to 5 (unable to hold; leak urine). (NCT00444925)
Timeframe: Baseline, Week 1, Week 4, Week 12
| Intervention | percent change (Median) | ||
|---|---|---|---|
| Week 1 (n=306, 619, 621) | Week 4 [LOCF] (n=311,631, 627) | Week 12 [LOCF] (n=311, 631, 628) | |
| Fesoterodine | -9.7 | -26.9 | -37.9 |
| Placebo | -5.6 | -11.4 | -17.6 |
| Tolterodine ER | -12.5 | -23.1 | -30.8 |
UUI episodes per 24 hours calculated as total number of micturitions with USS of 5 in diary. USS is 5-item scale measuring urinary urgency; range is 1 (no feeling of urgency) to 5 (unable to hold; leak urine). Change calculated as UUI episodes per 24 hours at observation divided by baseline number of UUI episodes per 24 hours, multiplied by 100. (NCT00444925)
Timeframe: Baseline, Week 1, Week 4, Week 12
| Intervention | percent change (Median) | ||
|---|---|---|---|
| Week 1 (n=302, 614, 612) | Week 4 [LOCF] (n=307, 626, 618) | Week 12 [LOCF] (n=307, 626, 619) | |
| Fesoterodine | -53.6 | -93.2 | -100.0 |
| Placebo | -28.6 | -60.0 | -82.1 |
| Tolterodine ER | -55.1 | -85.7 | -100.0 |
UUI per 24 hours: total number of micturitions with Urinary Sensation Scale (USS) of 5 divided by total number of diary days collected at visit. USS: 5-item scale to measure urinary urgency; range: 1 (no feeling of urgency) to 5 (unable to hold; leak urine). Change: mean at observation minus mean at baseline. (NCT00444925)
Timeframe: Baseline, Week 12
| Intervention | number of episodes per 24 hours (Mean) |
|---|---|
| Placebo | -1.46 |
| Tolterodine ER | -1.61 |
| Fesoterodine | -1.72 |
Percent change of micturitions per 24 hours was calculated as change in 24-hour mean at that visit divided by the baseline 24-hour mean multiplied by 100 (ie, 100% *(Week 12 or 4 - baseline)/baseline). (NCT00444925)
Timeframe: Baseline, Week 1, Week 4, Week 12
| Intervention | percent change (Median) | ||
|---|---|---|---|
| Week 1 (n=307, 622, 623) | Week 4 [LOCF] (n=313, 634, 627) | Week 12 [LOCF] (n=313, 634, 628) | |
| Fesoterodine | -7.9 | -14.8 | -18.9 |
| Placebo | -2.7 | -10.3 | -12.1 |
| Tolterodine ER | -7.7 | -15.0 | -16.2 |
Percent change of nocturnal micturitions per 24 hours was calculated as change in 24-hour mean at that visit divided by the baseline 24-hour mean multiplied by 100 (ie, 100% *(Week 12 or 4 - baseline)/baseline). Nocturnal (Bedtime) was defined as the time the subject went to bed until he/she arose to start the next day. (NCT00444925)
Timeframe: Baseline, Week 1, Week 4, Week 12
| Intervention | percent change (Median) | ||
|---|---|---|---|
| Week 1 (n=288, 584, 596) | Week 4 [LOCF] (n=293, 596, 600) | Week 12 [LOCF] (n=293, 596, 601) | |
| Fesoterodine | 0.0 | -20.0 | -28.6 |
| Placebo | -10.0 | -22.2 | -25.0 |
| Tolterodine ER | -12.5 | -25.0 | -27.9 |
Diary dry rate: number of subjects with no urgency urinary incontinence episode reported in the 3 day diary at the respective time-point; based on USS: 5-item scale measuring urinary urgency; range is 1 (no feeling of urgency) to 5 (unable to hold; leak urine). (NCT00444925)
Timeframe: Week 1, Week 4, Week 12
| Intervention | participants (Number) | ||
|---|---|---|---|
| Week 1 | Week 4 | Week 12 | |
| Fesoterodine | 159 | 306 | 396 |
| Placebo | 54 | 97 | 138 |
| Tolterodine ER | 153 | 290 | 358 |
Symptom bother score derived as sum of scores for questions 1-8; lowest possible raw score: 8; highest possible score: 48. Data analyzed based on transformation of the score to a 0 to 100 scale [(Actual total raw score - lowest possible value of raw score)/by raw score range * 100]. Higher transformed scores indicative of greater symptom bother. Negative change in Symptom Bother score indicates improvement. Change calculated as score at observation minus score at baseline. (NCT00444925)
Timeframe: Baseline, Week 12
| Intervention | score on scale (Least Squares Mean) |
|---|---|
| Placebo | -16.3 |
| Tolterodine ER | -22.5 |
| Fesoterodine | -27.1 |
UUI episodes per 24 hours calculated as total number of micturitions with Urinary Sensation Scale (USS) of 5 divided by total number of diary days collected at visit. USS is 5-item scale measuring urinary urgency; range is 1 (no feeling of urgency) to 5 (unable to hold; leak urine). Change calculated as mean at observation minus mean at baseline. (NCT00444925)
Timeframe: Baseline, Week 1, Week 4
| Intervention | number of episodes per 24 hours (Mean) | |
|---|---|---|
| Week 1 (n=302, 614, 612) | Week 4 [LOCF] (n=307, 626, 618) | |
| Fesoterodine | -0.95 | -1.52 |
| Placebo | -0.54 | -1.06 |
| Tolterodine ER | -0.92 | -1.40 |
Frequency-Urgency Sum rating per 24 hours calculated as mean rating scores on the USS multiplied by the mean number of micturitions per 24 hours at that visit. USS is 5-item scale measuring urinary urgency; range is 1 (no feeling of urgency) to 5 (unable to hold; leak urine). Change calculated as mean at observation minus mean at baseline. (NCT00444925)
Timeframe: Baseline, Week 1, Week 4, Week 12
| Intervention | score on scale (Least Squares Mean) | ||
|---|---|---|---|
| Week 1 (n=306, 619, 621) | Week 4 [LOCF] (n=311,631, 627) | Week 12 [LOCF] (n=311, 631, 628) | |
| Fesoterodine | -5.5 | -10.5 | -13.2 |
| Placebo | -2.4 | -5.7 | -8.2 |
| Tolterodine ER | -5.7 | -9.7 | -12.1 |
The mean number of micturitions was calculated as the sum of all micturitions divided by the total number of diary days collected at that visit. Change calculated as mean at observation minus mean at baseline. (NCT00444925)
Timeframe: Baseline, Week 1, Week 4, Week 12
| Intervention | number of micturitions per 24 hours (Least Squares Mean) | ||
|---|---|---|---|
| Week 1 (n=307, 622, 623) | Week 4 [LOCF] (n= 313, 634, 627) | Week 12 [LOCF] (n= 313, 634, 628) | |
| Fesoterodine | -1.0 | -1.9 | -2.2 |
| Placebo | -0.5 | -1.2 | -1.5 |
| Tolterodine ER | -1.0 | -1.8 | -2.1 |
Mean number of nocturnal micturitions per 24 hours was calculated as the sum of all micturitions divided by the total number of diary days collected at that visit. Nocturnal (Bedtime) was defined as the time the subject went to bed until he/she arose to start the next day. (NCT00444925)
Timeframe: Baseline, Week 1, Week 4, Week 12
| Intervention | nocturnal micturitions per 24 hours (Least Squares Mean) | ||
|---|---|---|---|
| Week 1 (n=288, 584, 596) | Week 4 [LOCF] (n=293, 596, 600) | Week 12 [LOCF] (n=293, 596, 601) | |
| Fesoterodine | -0.2 | -0.5 | -0.6 |
| Placebo | -0.1 | -0.4 | -0.5 |
| Tolterodine ER | -0.3 | -0.5 | -0.6 |
Mean number of severe urgency episodes (USS rating >= to 4 in diary ) per 24 hours: sum of all micturitions divided by total number of diary days collected at that visit. USS: 5-item scale to measure urinary urgency; range: 1 (no feeling of urgency) to 5 (unable to hold; leak urine). Change calculated as mean at observation minus mean at baseline. (NCT00444925)
Timeframe: Baseline, Week 1, Week 4, Week 12
| Intervention | severe urgency episodes per 24 hours (Least Squares Mean) | ||
|---|---|---|---|
| Week 1 (n=306, 618, 618) | Week 4 [LOCF] (n=311, 630, 624) | Week 12 [LOCF] (n=311, 630, 625) | |
| Fesoterodine | -1.2 | -2.4 | -3.0 |
| Placebo | -0.4 | -1.2 | -1.9 |
| Tolterodine ER | -1.3 | -2.2 | -2.8 |
Mean number urgency episodes (USS rating >= to 3 in diary) per 24 hours calculated as sum of all micturitions divided by total number of diary days collected at visit. USS: 5-item scale measuring urinary urgency; range is 1 (no feeling of urgency) to 5 (unable to hold; leak urine). Change calculated as mean at observation minus mean at baseline. (NCT00444925)
Timeframe: Baseline, Week 1, Week 4, Week 12
| Intervention | urgency episodes per 24 hours (Least Squares Mean) | ||
|---|---|---|---|
| Week 1 (n=306, 619, 621) | Week 4 [LOCF] (n=311, 631, 627) | Week 12 [LOCF] (n=311, 631, 628) | |
| Fesoterodine | -1.1 | -2.6 | -3.5 |
| Placebo | -0.4 | -1.2 | -2.0 |
| Tolterodine ER | -1.3 | -2.4 | -3.1 |
Mean USS rating calculated as the sum of rating scores on USS per 24 hours divided by the mean number of micturitions per 24 hours at that visit. USS is 5-item scale measuring urinary urgency; range is 1 (no feeling of urgency) to 5 (unable to hold; leak urine). Change calculated as mean at observation minus mean at baseline. (NCT00444925)
Timeframe: Baseline, Week 1, Week 4, Week 12
| Intervention | score on scale (Least Squares Mean) | ||
|---|---|---|---|
| Week 1 (n=306, 619, 621) | Week 4 [LOCF] (n=311, 631, 627) | Week 12 [LOCF] (n=311, 631, 628) | |
| Fesoterodine | -0.2 | -0.5 | -0.7 |
| Placebo | -0.1 | -0.2 | -0.4 |
| Tolterodine ER | -0.2 | -0.4 | -0.6 |
Mean voided volume calculated as sum of voided volume divided by the total number of micturition episodes with a recorded voided volume greater than 0 in the 3-day diary at that visit. (NCT00444925)
Timeframe: Baseline, Week 1, Week 4, Week 12
| Intervention | voided volume per micturition (Least Squares Mean) | ||
|---|---|---|---|
| Week 1 (n=306, 622, 623) | Week 4 [LOCF] (n=313, 633, 625) | Week 12 [LOCF] (n=313, 633, 626) | |
| Fesoterodine | 18.7 | 30.5 | 32.9 |
| Placebo | 11.0 | 14.0 | 16.8 |
| Tolterodine ER | 19.2 | 25.7 | 23.5 |
HRQL domain and total raw score derived as sum of scores (6-point scale: 1=not at all/none of the time; 6=a very great deal/all of the time). Transformed score (Total HRQL or domain)=[(Highest possible raw score-Actual total raw score)/Raw score range]x100. Higher transformed scores indicative of better HRQL. Positive change in HRQL scores indicates improvement. Change: score at observation minus score at baseline. (NCT00444925)
Timeframe: Baseline, Week 12
| Intervention | score on scale (Least Squares Mean) | ||||
|---|---|---|---|---|---|
| HRQL concern domain (n=289, 589, 572) | HRQL coping domain (n=289, 589, 572) | HRQL sleep domain (n=289, 589, 572) | HRQL social interaction domain (n=289, 588, 572) | HRQL scale score total (n=289, 588, 572) | |
| Fesoterodine | 22.6 | 22.6 | 17.3 | 11.6 | 19.3 |
| Placebo | 13.4 | 14.0 | 12.2 | 6.8 | 12.0 |
| Tolterodine ER | 19.3 | 18.5 | 15.1 | 9.4 | 16.3 |
Number of subjects in 4-point category: >= to 2 points improvement [major improvement]; 1 point improvement [minor improvement]; no change; deterioration, based on PPBC score (rated on 6-point scale: 1=no problems at all; 6=many severe problems). Score change: score at observation minus score at baseline; re-scaled to 4-point categorical variables. (NCT00444925)
Timeframe: Baseline, Week 1, Week, 4, Week 12
| Intervention | participants (Number) | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Week 1 (n=309, 625, 623), >=2 points improvement | Week 1, 1-point improvement | Week 1, no change | Week 1, deterioration | Week 4 (n=313, 632, 629), >=2 points improvement | Week 4, 1-point improvement | Week 4, no change | Week 4, deterioration | Week 12 (n=313, 632, 630), >=2 points improvement | Week 12, 1-point improvement | Week 12, no change | Week 12, deterioration | |
| Fesoterodine | 102 | 186 | 286 | 49 | 196 | 224 | 176 | 33 | 254 | 198 | 148 | 30 |
| Placebo | 32 | 94 | 147 | 36 | 57 | 95 | 127 | 34 | 67 | 102 | 111 | 33 |
| Tolterodine ER | 79 | 181 | 306 | 59 | 169 | 201 | 203 | 59 | 210 | 189 | 171 | 62 |
Number of subjects in 3-point category: improvement [>=1-point improvement]; no change; deterioration [>=1-point decrease], based on UPS score (rated on 3-point scale: 1=not able to hold urine; 3=able to finish what I am doing). Score change calculated as score at observation minus score at baseline; re-scaled to 3-point categorical variables. (NCT00444925)
Timeframe: Baseline, Week 1, Week 4, Week 12
| Intervention | participants (Number) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Week 1 (n=309, 627, 624), improvement | Week 1, no change | Week 1, deterioration | Week 4 (n=313, 633, 629), improvement | Week 4, no change | Week 4, deterioration | Week 12 (n=313, 633, 630), improvement | Week 12, no change | Week 12, deterioration | |
| Fesoterodine | 171 | 413 | 40 | 256 | 348 | 25 | 291 | 314 | 25 |
| Placebo | 68 | 218 | 23 | 98 | 194 | 21 | 112 | 181 | 20 |
| Tolterodine ER | 162 | 438 | 27 | 238 | 362 | 33 | 254 | 344 | 35 |
"The urgency severity VAS Scale records the subject's assessment of the severity of urgency. VAS scale ranges from 1 'Very Mild' to 10 'Very Severe'. Negative change indicated improvement.~Change: mean at observation minus mean at baseline." (NCT00536484)
Timeframe: Baseline, Week 2, Week 6 and Week 12
| Intervention | scores on a scale (Least Squares Mean) | ||
|---|---|---|---|
| Week 2 (n=441; n=432) | Week 6 (n=443; n=434) | Week 12 (n=443; n=434) | |
| Fesoterodine | -1.4 | -2.2 | -2.4 |
| Placebo | -0.8 | -1.4 | -1.4 |
"The number of micturitions per 24 hours was calculated as the sum of all micturitions divided by the total number of diary days collected at that visit.~Change: mean at Week 12 minus mean at Baseline" (NCT00536484)
Timeframe: Baseline and Week 12
| Intervention | number of episodes per 24 hours (Least Squares Mean) |
|---|---|
| Placebo | -2.1 |
| Fesoterodine | -2.9 |
"Each item rated by subject on a Likert scale 1 (least symptom bother) to 6 (most symptom bother). Raw scores were transformed to a score from 0 to 100. Once transformed a negative change indicates improvement.~Change: mean at Week 12 minus mean at baseline" (NCT00536484)
Timeframe: Baseline and Week 12
| Intervention | scores on a scale (Least Squares Mean) |
|---|---|
| Placebo | -20.0 |
| Fesoterodine | -27.8 |
PPBC scale range: 1='does not cause me any problems at all' to 6='causes me many severe problems'. Major improvement=negative score change of 2 or more from baseline; minor improvement=negative score change of 1 or more from baseline; no change=0 score change from baseline; Deterioration=positive score change from baseline (NCT00536484)
Timeframe: Baseline, Week 2, Week 6 and Week 12
| Intervention | percentage of participants (Number) | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Week 2 (n=440; n=434): major improvement | Week 2: minor improvement | Week 2: no change | Week 2: deterioration | Week 6 (n=442; n=435): major improvement | Week 6: minor improvement | Week 6: no change | Week 6: deterioration | Week 12 (n=442; n=435): major improvement | Week 12: minor improvement | Week 12: no change | Week 12: deterioration | |
| Fesoterodine | 16.6 | 39.4 | 39.4 | 4.6 | 32.4 | 35.9 | 27.8 | 3.9 | 36.8 | 34.5 | 25.5 | 3.2 |
| Placebo | 13.2 | 34.8 | 45.2 | 6.8 | 24.7 | 34.8 | 33.5 | 7.0 | 29.2 | 31.0 | 33.0 | 6.8 |
"UPS scores range from 0 (I am usually not able to hold urine) to 2 (I am usually able to finish what I am doing before going to the toilet [without leaking]). Improvement: positive score change; No change: score change=0; Deterioration: negative score change" (NCT00536484)
Timeframe: Baseline, Week 2, Week 6 and Week 12
| Intervention | percentage of participants (Number) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Week 2 (n=441; n=434): improvement | Week 2: no change | Week 2: deterioration | Week 6 (n=443; n=435): improvement | Week 6: no change | Week 6: deterioration | Week 12 (n=443; n=435): improvement | Week 12: no change | Week 12: deterioration | |
| Fesoterodine | 29.3 | 64.5 | 6.2 | 37.5 | 58.6 | 3.9 | 41.8 | 52.4 | 5.7 |
| Placebo | 22.9 | 69.2 | 7.9 | 30.2 | 65.0 | 4.7 | 30.9 | 62.3 | 6.8 |
Change in frequency urgency sum is total urinary sensation scale (USS) ratings recorded for all micturitions in 24-hour day. Number of USS ratings per 24 hours is sum of all USS ratings divided by the total diary days collected at that visit. USS scale: 1=No feeling of urgency to 5=Unable to hold:leak urine. Numerical decrease indicates improvement (NCT00536484)
Timeframe: Baseline, Week 2, Week 6 and Week 12
| Intervention | scores on a scale (Least Squares Mean) | ||
|---|---|---|---|
| Week 2 (n=431; n=427) | Week 6 (n=434; n=428) | Week 12 (n=434; n=428) | |
| Fesoterodine | -8.3 | -12.5 | -13.6 |
| Placebo | -6.5 | -9.8 | -10.3 |
"Each item rated by subject on a Likert scale 1 (least symptom bother) to 6 (most symptom bother). Raw scores were transformed to a score from 0 to 100. Once transformed a positive change indicates improvement.~Change: mean at Week 12 minus mean at baseline." (NCT00536484)
Timeframe: Baseline and Week 12
| Intervention | scores on a scale (Least Squares Mean) | ||||
|---|---|---|---|---|---|
| HRQL concern domain (n=383; n=372) | HRQL coping domain (n=383; n=372) | HRQL sleep domain (n=383; n=372) | HRQL social interaction domain (n=380; n=372) | HRQL scale score total (n=380; n=372) | |
| Fesoterodine | 29.3 | 27.2 | 25.9 | 15.3 | 25.1 |
| Placebo | 20.9 | 20.2 | 21.2 | 11.6 | 18.9 |
"The number of micturitions per 24 hours was calculated as the sum of all micturitions divided by the total number of diary days collected at that visit.~Change: mean at observation minus mean at baseline" (NCT00536484)
Timeframe: Baseline, Week 2 and Week 6
| Intervention | number of episodes per 24 hours (Least Squares Mean) | |
|---|---|---|
| Week 2 (n=431; n=427) | Week 6 (n=434; n=428) | |
| Fesoterodine | -1.8 | -2.7 |
| Placebo | -1.3 | -2.0 |
Change in number of nocturnal micturitions (NM) recorded in the bladder diary. NM were defined as micturitions that occurred between the time the subject went to bed and the time he or she arose to start the next day. The number of NM per 24 hours was calculated as the sum of all NM divided by the total number of diary days collected at that visit. (NCT00536484)
Timeframe: Baseline, Week 2, Week 6 and Week 12
| Intervention | number of episodes per 24 hours (Least Squares Mean) | ||
|---|---|---|---|
| Week 2 (n=420; n=417) | Week 6 (n=423; n=418) | Week 12 (n=423; n=418) | |
| Fesoterodine | -0.5 | -0.7 | -0.8 |
| Placebo | -0.5 | -0.7 | -0.7 |
Change in number of nocturnal urgency episodes (NUE) recorded in bladder diary. NUE had urinary sensation scale (USS) rating of 3 or more that occurred between time subject went to bed and time he or she arose to start next day. Number of NUE per 24 hours was calculated as sum of all NUE divided by total number of diary days collected at that visit (NCT00536484)
Timeframe: Baseline, Week 2, Week 6 and Week 12
| Intervention | number of episodes per 24 hours (Least Squares Mean) | ||
|---|---|---|---|
| Week 2 (n=411; n=408) | Week 6 (n=414; n=409) | Week 12 (n=414; n=409) | |
| Fesoterodine | -0.6 | -0.9 | -1.0 |
| Placebo | -0.6 | -0.8 | -0.9 |
Change in number of severe urgency episodes (urinary sensation scale [USS] rating of 4 or more) recorded in the bladder diary. Scale: 0=no feeling of urgency to 5=unable to hold; leak urine. Number of severe urgency episodes per 24 hours calculated as sum of all severe urgency episodes divided by total number of diary days collected at that visit. (NCT00536484)
Timeframe: Baseline, Week 2, Week 6 and Week 12
| Intervention | number of episodes per 24 hours (Least Squares Mean) | ||
|---|---|---|---|
| Week 2 (n=393; n=403) | Week 6 (n=396; n=404) | Week 12 (n=396; n=404) | |
| Fesoterodine | -1.8 | -2.6 | -2.9 |
| Placebo | -1.6 | -2.2 | -2.2 |
Change in number of urgency episodes (urinary sensation scale [USS] rating of 3 or more) recorded in the bladder diary. Scale: 0=no feeling of urgency to 5=unable to hold; leak urine. The number of urgency episodes per 24 hours was calculated as the sum of all urgency episodes divided by the total number of diary days collected at that visit. (NCT00536484)
Timeframe: Baseline, Week 2, Week 6 and Week 12
| Intervention | number of episodes per 24 hours (Least Squares Mean) | ||
|---|---|---|---|
| Week 2 (n=431; n=427) | Week 6 (n=434; n=428) | Week 12 (n=434; n=428) | |
| Fesoterodine | -2.3 | -3.5 | -4.0 |
| Placebo | -1.9 | -2.9 | -3.0 |
Change in number of UUI episodes (urinary sensation scale [USS] rating of 5) recorded in the bladder diary. Scale: 0=no feeling of urgency to 5=unable to hold; leak urine (NCT00536484)
Timeframe: Baseline, Week 2, Week 6 and Week 12
| Intervention | number of episodes per 24 hours (Least Squares Mean) | ||
|---|---|---|---|
| Week 2 (n=255; n=251) | Week 6 (n=257; n=251) | week 12 (n=257; n=251) | |
| Fesoterodine | -1.1 | -1.5 | -1.5 |
| Placebo | -0.9 | -1.2 | -1.2 |
"PPBC: self-administered, single-item, validated questionnaire. Rated on a 6-point scale: subject was asked: Which of the following statements describes your bladder condition best at the moment? 1=no problems at all; 2=some very minor problems; 3=some minor problems; 4=some moderate problems; 5=severe problems; 6=many severe problems. A post-baseline vs baseline variable with ordinal values was derived: 1=Deterioration=Difference in scores was positive; 2=No Change=Difference in scores was 0; 3=Minor Improvement=Difference in scores was -1; 4=Major Improvement=Difference in scores was ≤ 2." (NCT00546637)
Timeframe: Baseline, Week 12
| Intervention | participants (Number) | |||
|---|---|---|---|---|
| Major Improvement | Minor Improvement | No Change | Deterioration | |
| Fesoterodine 4mg or 8mg | 124 | 166 | 148 | 21 |
| Placebo | 130 | 138 | 170 | 21 |
"PPBC: self-administered, single-item, validated questionnaire. Rated on a 6-point scale: subject was asked: Which of the following statements describes your bladder condition best at the moment? 1=no problems at all; 2=some very minor problems; 3=some minor problems; 4=some moderate problems; 5=severe problems; 6=many severe problems. A post-baseline vs baseline variable with ordinal values was derived: 1=Deterioration=Difference in scores was positive; 2=No Change=Difference in scores was 0; 3=Minor Improvement=Difference in scores was -1; 4=Major Improvement=Difference in scores was ≤ 2." (NCT00546637)
Timeframe: Baseline, Week 4
| Intervention | participants (Number) | |||
|---|---|---|---|---|
| Major Improvement | Minor Improvement | No Change | Deterioration | |
| Fesoterodine 4mg or 8mg | 83 | 171 | 180 | 25 |
| Placebo | 63 | 160 | 212 | 22 |
All micturitions with USS rating 1 to 5. USS rating: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. The mean number of micturitions per 24 hours was calculated as the total number of micturitions divided by the total number of diary days collected at that visit. Numeric change of micturitions per 24 hours at Week 4 and 12 relative to Baseline. (NCT00546637)
Timeframe: Baseline, Week 4 and 12
| Intervention | number of micturitions (Least Squares Mean) | |
|---|---|---|
| Week 4 (n=445, n=451) | Week 12 (n=446, n=452) | |
| Fesoterodine 4mg or 8mg | -1.3 | -1.9 |
| Placebo | -0.8 | -1.5 |
Number of participants experiencing serious and non-serious adverse events related to increased voiding difficulty (ie, Dysuria, Urinary retention regardless of catheterization, Urine flow decreased, Residual urine volume, Residual urine volume increased, Residual urine, and Urinary hesitation) (NCT00546637)
Timeframe: Baseline, Week 12
| Intervention | participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Dysuria | Urinary retention (Regardless of catheterization) | Urine flow decreased | Residual urine volume | Residual urine volume increased | Residual urine | Urinary hesitation | |
| Fesoterodine 4mg or 8mg | 16 | 11 | 4 | 1 | 1 | 1 | 0 |
| Placebo | 4 | 2 | 0 | 0 | 0 | 0 | 2 |
HRQL domain and total raw score derived as sum of scores (6-point scale: 1 = not at all/none of the time; 6 = a very great deal/all of the time). Transformed score range 0 to 100 (Total HRQL or domain)=[(Highest possible raw score-Actual total raw score)/Raw score range]x100. Higher transformed scores indicative of better HRQL. Positive change in HRQL scores indicates improvement. Change: score at observation minus score at baseline. (NCT00546637)
Timeframe: Baseline, Week 4 and 12
| Intervention | scores on scale (Least Squares Mean) | |
|---|---|---|
| Week 4 (n=459, n=458) | Week 12 (n=459, n=459) | |
| Fesoterodine 4mg or 8mg | 8.7 | 11.5 |
| Placebo | 6.9 | 10.0 |
The HRQL social interaction domain; range was 0-100. The transformed score for HRQL was calculated based on the following formula: Transformed score (HRQL) = [(Highest possible score - Actual raw score)/ Range]*100, where range was the raw score range. Positive change in HRQL Score indicates improvement. (NCT00546637)
Timeframe: Baseline, Week 4 and Week 12
| Intervention | scores on a scale (Least Squares Mean) | |
|---|---|---|
| Week 4 (n=459, n=458) | Week 12 (n=459, n=459) | |
| Fesoterodine 4mg or 8mg | 5.2 | 6.3 |
| Placebo | 3.7 | 6.0 |
The HRQL sleep domain; range was 0-100. The transformed score for HRQL was calculated based on the following formula: Transformed score (HRQL) = [(Highest possible score - Actual raw score)/ Range]*100, where range was the raw score range. Positive change in HRQL Score indicates improvement. (NCT00546637)
Timeframe: Baseline, Week 4 and Week 12
| Intervention | scores on a scale (Least Squares Mean) | |
|---|---|---|
| Week 4 (n=459, n=458) | Week 12 (n=459, n=459) | |
| Fesoterodine 4mg or 8mg | 9.6 | 13.8 |
| Placebo | 7.6 | 11.5 |
The HRQL coping domain; range was 0-100. The transformed score for HRQL was calculated based on the following formula: Transformed score (HRQL) = [(Highest possible score - Actual raw score)/ Range]*100, where range was the raw score range. Positive change in HRQL Score indicates improvement. (NCT00546637)
Timeframe: Baseline, Week 4 and Week 12
| Intervention | scores on a scale (Least Squares Mean) | |
|---|---|---|
| Week 4 (n=459, n=458) | Week 12 (n=459, n=459) | |
| Fesoterodine 4mg or 8mg | 9.6 | 12.5 |
| Placebo | 7.5 | 10.6 |
The HRQL concern domain; range was 0-100. The transformed score for HRQL was calculated based on the following formula: Transformed score (HRQL) = [(Highest possible score - Actual raw score)/ Range]*100, where range was the raw score range. Positive change in HRQL Score indicates improvement. (NCT00546637)
Timeframe: Baseline, Week 4 and 12
| Intervention | scores on scale (Least Squares Mean) | |
|---|---|---|
| Week 4 (n=459, n=458) | Week 12 (n=459, n=459) | |
| Fesoterodine 4mg or 8mg | 9.7 | 12.4 |
| Placebo | 8.0 | 11.1 |
Post-void residual volume measurement was measured by an ultrasound at Baseline, and at Weeks 4, 8 and 12. (NCT00546637)
Timeframe: Baseline, Week 4, 8 and 12
| Intervention | ml (Median) | ||
|---|---|---|---|
| Week 4 | Week 8 | Week 12 | |
| Fesoterodine 4mg or 8mg | 0.0 | 0.0 | 3.5 |
| Placebo | 0.0 | 0.0 | 0.0 |
OAB-q is a self-administered, 33-item, validated questionnaire that assesses how much the subject has been bothered by selected bladder symptoms during the previous week. Each item rated by subject on Likert scale 1 (least symptom bother) to 6 (most symptom bother). Raw scores were transformed to a score from 0-100. Once transformed, higher scores represent less favorable outcome. (NCT00546637)
Timeframe: Baseline, Week 4 and 12
| Intervention | scores on scale (Least Squares Mean) | |
|---|---|---|
| Week 4 (n=459, n=458) | Week 12 (n=459, n=459) | |
| Fesoterodine 4mg or 8mg | -11.6 | -15.2 |
| Placebo | -8.9 | -12.4 |
The IPSS Total Score is obtained by combining the scores of the responses to 1 though 7 component questions. Each question is scored from 0-5. Total IPSS range = 0-35 points; higher numerical scores from the IPSS questionnaire represent greater severity of symptoms. Sum of Q1, Q3, Q5, and Q6 range = 0-20 points. (NCT00546637)
Timeframe: Baseline, Week 4 and 12
| Intervention | scores on scale (Least Squares Mean) | |
|---|---|---|
| Week 4 (n=454, n=455) | Week 12 (n=455, n=457) | |
| Fesoterodine 4mg or 8mg | -1.6 | -2.1 |
| Placebo | -1.7 | -2.3 |
The IPSS Total Score is obtained by combining the scores of the responses to 1 though 7 component questions. Each question is scored from 0-5. Total IPSS range = 0-35 points; higher numerical scores from the IPSS questionnaire represent greater severity of symptoms. Sum of Q2, Q4, and Q7 range = 0-15 points. (NCT00546637)
Timeframe: Baseline, Week 4 and 12
| Intervention | scores on scale (Least Squares Mean) | |
|---|---|---|
| Week 4 (n=456, n=457) | Week 12 (n=456, n=458) | |
| Fesoterodine 4mg or 8mg | -1.8 | -2.4 |
| Placebo | -1.4 | -2.1 |
The IPSS Total Score is obtained by combining the scores of the responses to 1 though 7 component questions. Each question is scored from 0-5. Total IPSS range = 0-35 points; higher numerical scores from the IPSS questionnaire represent greater severity of symptoms. Score of Q8 range = 0-5 points. (NCT00546637)
Timeframe: Baseline, Week 4 and 12
| Intervention | scores on scale (Least Squares Mean) | |
|---|---|---|
| Week 4 (n=455, n=455) | Week 12 (n=455, 457) | |
| Fesoterodine 4mg or 8mg | -0.6 | -1.0 |
| Placebo | -0.5 | -1.0 |
The IPSS Total Score is obtained by combining the scores of the responses to 1 though 7 component questions. Each question is scored from 0-5 for an IPSS range of 0-35 points; higher numerical scores from the IPSS questionnaire represent greater severity of symptoms. (NCT00546637)
Timeframe: Baseline, Week 12
| Intervention | scores on scale (Least Squares Mean) | ||||||
|---|---|---|---|---|---|---|---|
| Q1 (sensation of not emptying bladder?) | Q2 (urinate less than two hours after urination?) | Q3 (stop and start several times during urination? | Q4 (difficulty postponing urination?) | Q5 (weak urinary stream?) | Q6 (strain to begin urination?) | Q7 (urinate at night?) | |
| Fesoterodine 4mg or 8mg | -0.7 | -0.9 | -0.5 | -0.9 | -0.6 | -0.3 | -0.5 |
| Placebo | -0.8 | -0.8 | -0.6 | -0.8 | -0.6 | -0.3 | -0.6 |
The IPSS Total Score is obtained by combining the scores of the responses to 1 though 7 component questions. Each question is scored from 0-5. Total IPSS range = 0-35 points; higher numerical scores from the IPSS questionnaire represent greater severity of symptoms. (NCT00546637)
Timeframe: Baseline, Week 4
| Intervention | scores on scale (Least Squares Mean) | ||||||
|---|---|---|---|---|---|---|---|
| Q1 (sensation of not emptying bladder?) | Q2 (urinate less than two hours after urination?) | Q3 (stop and start several times during urination? | Q4 (difficulty postponing urination?) | Q5 (weak urinary stream?) | Q6 (strain to begin urination?) | Q7 (urinate at night?) | |
| Fesoterodine 4mg or 8mg | -0.6 | -0.8 | -0.4 | -0.7 | -0.5 | -0.2 | -0.3 |
| Placebo | -0.6 | -0.5 | -0.4 | -0.6 | -0.4 | -0.3 | -0.3 |
The mean number of micturition-related urgency episodes per 24 hours was calculated as the total number of micturitions with USS Scale >= 3 divided by the total number of days that diary data was collected at that visit. USS total range 1 to 5: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. (NCT00546637)
Timeframe: Baseline, Week 12
| Intervention | number of episodes (Least Squares Mean) |
|---|---|
| Fesoterodine 4mg or 8mg | -3.2 |
| Placebo | -2.9 |
Nocturnal micturition-related urgency episodes were defined as micturition-related urgency episodes with USS ratings 3-5 that occurred between the time the subject went to bed and the time he or she arose to start the next day. USS rating: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. The percentage change at Week 4 or 12 was calculated as: 100* (Nocturnal Micturition-Related Urgency Episodes at Week 4 or 12 - Baseline)/Baseline (NCT00546637)
Timeframe: Baseline, Week 4 and 12
| Intervention | percent change (Median) | |
|---|---|---|
| Week 4 (n=424, n=433) | Week 12 (n=425, n=434) | |
| Fesoterodine 4mg or 8mg | -33.3 | -50.0 |
| Placebo | -25.0 | -40.0 |
Nocturnal micturitions were defined as micturitions with USS rating 1-5 that occurred between the time the subject went to bed and the time he or she arose to start the next day. USS rating: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. The percentage change at Week 4 or 12 was calculated as: 100* (Nocturnal micturitions at Week 4 or 12 - Baseline)/Baseline (NCT00546637)
Timeframe: Baseline, Week 4 and 12
| Intervention | percent change (Median) | |
|---|---|---|
| Week 4 (n=438, n=441) | Week 12 (n=439, n=442) | |
| Fesoterodine 4mg or 8mg | -16.7 | -25.0 |
| Placebo | -11.1 | -16.7 |
Severe micturition-related urgency episodes are defined as those with a USS rating ≥4 marked for the corresponding micturition in the bladder diary. USS rating: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. The percentage change at Week 4 or 12 was calculated as: 100* (Severe Micturition-Related Urgency Episodes at Week 4 or 12 - Baseline)/Baseline (NCT00546637)
Timeframe: Baseline, Week 4 and 12
| Intervention | percent change (Median) | |
|---|---|---|
| Week 4 (n=310, n=339) | Week 12 (n=311, n=340) | |
| Fesoterodine 4mg or 8mg | -78.6 | -100.0 |
| Placebo | -60.0 | -88.4 |
UUI episodes are defined as those micturitions with a USS rating of 5 in the bladder diary in subjects with UUI at baseline. USS rating 5: Unable to hold; leak urine. The percentage change at Week 4 or 12 was calculated as: 100* (UUI Episodes at Week 4 or 12 - Baseline)/Baseline (NCT00546637)
Timeframe: Baseline, Week 4 and 12
| Intervention | percent change (Median) | |
|---|---|---|
| Week 4 (n=103, n=104) | Week 12 (n=103, n=104) | |
| Fesoterodine 4mg or 8mg | -100.0 | -100.0 |
| Placebo | -100.0 | -100.0 |
Number of participants in 3-point category: improvement [>=1-point improvement]; no change; deterioration [>=1-point decrease], based on UPS score (rated on 3-point scale: 1=not able to hold urine; 3=able to finish what I am doing). Score change calculated as score at observation minus score at baseline; re-scaled to 3-point categorical variables. (NCT00546637)
Timeframe: Baseline, Week 12
| Intervention | participants (Number) | ||
|---|---|---|---|
| Improvement | No Change | Deterioration | |
| Fesoterodine 4mg or 8mg | 132 | 290 | 37 |
| Placebo | 129 | 299 | 31 |
The IPSS Total Score is obtained by combining the scores of the responses to 1 though 7 component questions. Each question is scored from 0-5 for an IPSS range of 0-35 points; higher numerical scores from the IPSS questionnaire represent greater severity of symptoms. (NCT00546637)
Timeframe: Baseline, Week 4 and 12
| Intervention | scores on a scale (Least Squares Mean) | |
|---|---|---|
| Week 4 (n=453, n=454) | Week 12 (n=454, n=456) | |
| Fesoterodine 4mg or 8mg | -3.4 | -4.4 |
| Placebo | -3.1 | -4.4 |
All micturitions with USS rating 1 to 5. USS rating: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. The percentage change at Week 4 or 12 was calculated as: 100* (Micturitions at Week 4 or 12 - Baseline)/Baseline (NCT00546637)
Timeframe: Baseline, Week 4 and 12
| Intervention | percent change (Median) | |
|---|---|---|
| Week 4 (n=445, n=451) | Week 12 (n=446, n=452) | |
| Fesoterodine 4mg or 8mg | -12.0 | -14.9 |
| Placebo | -7.3 | -12.5 |
The mean number of micturition-related urgency episodes per 24 hours was calculated as the total number of micturitions with USS Scale >= 3 divided by the total number of days that diary data was collected at that visit. USS total range 1 to 5: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. (NCT00546637)
Timeframe: Baseline, Week 4
| Intervention | number of episodes (Least Squares Mean) |
|---|---|
| Fesoterodine 4mg or 8mg | -2.3 |
| Placebo | -1.9 |
Maximum urinary flow rate (Qmax) was recorded at Baseline and Week 12 visit. (NCT00546637)
Timeframe: Baseline, Week 12
| Intervention | ml/sec (Median) |
|---|---|
| Fesoterodine 4mg or 8mg | 0.0 |
| Placebo | 0.0 |
Number of participants experiencing serious and non-serious adverse events of acute urinary retention requiring catheterization. (NCT00546637)
Timeframe: Baseline, Week 12
| Intervention | participants (Number) |
|---|---|
| Fesoterodine 4mg or 8mg | 1 |
| Placebo | 1 |
"Micturition-related urgency episodes per 24 hours were defined as those with USS Scale rating of >= 3 marked for the corresponding micturition in the diary. USS total range 1 to 5: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. The percentage change at Week 4 or 12 was calculated as:~100* (Micturition-Related Urgency Episodes at Week 4 or 12 - Baseline)/Baseline" (NCT00546637)
Timeframe: Baseline, Week 4 and 12
| Intervention | percent change (Median) | |
|---|---|---|
| Week 4 (n=445, 450) | Week 12 (n=446, n=451) | |
| Fesoterodine 4mg or 8mg | -30.8 | -43.8 |
| Placebo | -20.7 | -35.7 |
The USS sum rating was defined as the total of USS ratings recorded for all micturitions over the course of a day in the bladder diary. USS rating: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. USS Sum rating per 24 hours was calculated as the mean rating scores on the USS multiplied by the mean number of micturitions per 24 hours at that visit. (NCT00546637)
Timeframe: Baseline, Week 4 and 12
| Intervention | USS Sum rating per 24 hours (Least Squares Mean) | |
|---|---|---|
| Week 4 (n=445, n=451) | Week 12 (n=446, n=452) | |
| Fesoterodine 4mg or 8mg | -6.4 | -8.9 |
| Placebo | -4.7 | -7.8 |
UUI episodes were defined as those micturitions with USS rating of 5 in the diary in subjects with UUI at baseline. USS rating 5: Unable to hold; leak urine. (NCT00546637)
Timeframe: Baseline, Week 4 and Week 12
| Intervention | number of episodes (Median) | |
|---|---|---|
| Week 4 (n=103, n=104) | Week 12 (n=103, n=104) | |
| Fesoterodine 4mg or 8mg | -0.3 | -0.7 |
| Placebo | -0.7 | -0.7 |
Severe micturition related urgency episodes were defined as those micturitions with USS rating >=4 marked for the corresponding micturition in the diary. USS: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. (NCT00546637)
Timeframe: Baseline, Week 4 and 12
| Intervention | number of episodes (Median) | |
|---|---|---|
| Week 4 (n=310, n=339) | Week 12 (n=311, n=340) | |
| Fesoterodine 4mg or 8mg | -1.0 | -1.3 |
| Placebo | -1.0 | -1.0 |
Nocturnal micturitions were defined as micturitions with USS rating 1-5 that occurred between the time the subject went to bed and the time he or she arose to start the next day. USS rating: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. The mean number of nocturnal micturitions per 24 hours was calculated as the total number of nocturnal micturitions divided by the total number of diary days collected at that visit. (NCT00546637)
Timeframe: Baseline, Week 4 and 12
| Intervention | number of micturitions (Least Squares Mean) | |
|---|---|---|
| Week 4 (n=438, n=441) | Week 12 (n=439, n=442) | |
| Fesoterodine 4mg or 8mg | -0.4 | -0.6 |
| Placebo | -0.3 | -0.5 |
Nocturnal micturition-related urgency episodes were defined as micturition-related urgency episodes with USS ratings 3-5 that occurred between the time the subject went to bed and the time he or she arose to start the next day. USS rating: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. (NCT00546637)
Timeframe: Baseline, Week 4 and 12
| Intervention | number of episodes (Least Squares Mean) | |
|---|---|---|
| Week 4 (n= 424, n=433) | Week 12 (n=425, n=434) | |
| Fesoterodine 4mg or 8mg | -0.7 | -0.9 |
| Placebo | -0.6 | -0.9 |
Number of participants in 3-point category: improvement [>=1-point improvement]; no change; deterioration [>=1-point decrease], based on UPS score (rated on 3-point scale: 1=not able to hold urine; 3=able to finish what I am doing). Score change calculated as score at observation minus score at baseline; re-scaled to 3-point categorical variables. (NCT00546637)
Timeframe: Baseline, Week 4
| Intervention | participants (Number) | ||
|---|---|---|---|
| Improvement | No Change | Deterioration | |
| Fesoterodine 4mg or 8mg | 111 | 306 | 41 |
| Placebo | 98 | 326 | 34 |
"Number of urgency episodes was measured by the 3-day micturition diary completed for 3 consecutive days during the 7 days prior to each visit.~Urgency is the complaint of a sudden compelling desire to pass urine which is difficult to defer.~Change: mean at Week 12 minus mean at Baseline." (NCT00561951)
Timeframe: Baseline to Week 12
| Intervention | Urgency Episodes (Least Squares Mean) |
|---|---|
| Placebo | -1.00 |
| Fesoterodine 4 mg | -1.65 |
| Fesoterodine 8 mg | -1.66 |
"Number of Night-Time Micturitions was measured by the 3-day micturition diary completed for 3 consecutive days during the 7 days prior to each visit.~Change: mean at Week 12 minus mean at Baseline." (NCT00561951)
Timeframe: Baseline to Week 12
| Intervention | Night-Time Micturitions (Least Squares Mean) |
|---|---|
| Placebo | -0.18 |
| Fesoterodine 4 mg | -0.21 |
| Fesoterodine 8 mg | -0.29 |
"Number of micturitions was measured by the 3-day micturition diary completed for 3 consecutive days during the 7 days prior to each visit.~Change: mean at Week 12 minus mean at Baseline." (NCT00561951)
Timeframe: Baseline to Week 12
| Intervention | Micturitions (Least Squares Mean) |
|---|---|
| Placebo | -0.59 |
| Fesoterodine 4 mg | -1.15 |
| Fesoterodine 8 mg | -1.25 |
"Patient Perception of Bladder Condition (PPBC) score is rated on a 6-point scale as follows:~No problems at all~Some very minor problems~Some minor problems~Some moderate problems~Severe problems~Many severe problems~Change: mean at Week 12 minus mean at Baseline." (NCT00561951)
Timeframe: Baseline to Week 12
| Intervention | score on scale (Mean) |
|---|---|
| Placebo | -1.57 |
| Fesoterodine 4 mg | -1.83 |
| Fesoterodine 8 mg | -1.76 |
"Number of incontinence episodes was measured by the 3-day micturition diary completed for 3 consecutive days during the 7 days prior to each visit.~Incontinence is the complaint of any involuntary leakage of urine.~Change: mean at Week 12 minus mean at Baseline." (NCT00561951)
Timeframe: Baseline to Week 12
| Intervention | Incontinence Episodes (Least Squares Mean) |
|---|---|
| Placebo | -0.88 |
| Fesoterodine 4 mg | -1.27 |
| Fesoterodine 8 mg | -1.15 |
"Voided volume per micturition was measured by the 3-day micturition diary completed for 3 consecutive days during the 7 days prior to each visit.~Change: mean at each visit minus mean at Baseline." (NCT00561951)
Timeframe: Baseline to Weeks 2, 4, 8, and 12
| Intervention | mL (Mean) | |||
|---|---|---|---|---|
| Week 2 (n=308, 314, 304) | Week 4 (n=301, 303, 296) | Week 8 (n=289, 289, 287) | Week 12 (n=284, 284, 281) | |
| Fesoterodine 4 mg | 13.63 | 21.62 | 22.05 | 24.52 |
| Fesoterodine 8 mg | 21.52 | 27.41 | 30.94 | 33.40 |
| Placebo | 5.06 | 9.23 | 10.75 | 13.28 |
"Number of urgency urinary incontinence (UUI) episodes was measured by the 3-day micturition diary completed for 3 consecutive days during the 7 days prior to each visit.~Urgency urinary incontinence is the complaint of involuntary leakage accompanied by or immediately preceded by urgency. Urgency is the complaint of a sudden compelling desire to pass urine which is difficult to defer.~Change: mean at each visit minus mean at Baseline." (NCT00561951)
Timeframe: Baseline to Weeks 2, 4, 8, and 12
| Intervention | UUI Episodes (Mean) | |||
|---|---|---|---|---|
| Week 2 (n=308, 314, 305) | Week 4 (n=301, 303, 296) | Week 8 (n=289, 289, 287) | Week 12 (n=284, 284, 281) | |
| Fesoterodine 4 mg | -1.10 | -1.48 | -1.61 | -1.76 |
| Fesoterodine 8 mg | -1.12 | -1.49 | -1.65 | -1.87 |
| Placebo | -0.79 | -1.15 | -1.45 | -1.49 |
"Number of urgency episodes was measured by the 3-day micturition diary completed for 3 consecutive days during the 7 days prior to each visit.~Urgency is the complaint of a sudden compelling desire to pass urine which is difficult to defer.~Change: mean at each visit minus mean at Baseline." (NCT00561951)
Timeframe: Baseline to Weeks 2, 4, 8, and 12
| Intervention | Urgency Episodes (Mean) | |||
|---|---|---|---|---|
| Week 2 (n=308, 314, 305) | Week 4 (n=301, 303, 296) | Week 8 (n=289, 289, 287) | Week 12 (n=284, 284, 281) | |
| Fesoterodine 4 mg | -1.37 | -2.16 | -2.50 | -2.89 |
| Fesoterodine 8 mg | -1.59 | -2.16 | -2.71 | -3.05 |
| Placebo | -0.79 | -1.60 | -2.34 | -2.37 |
"Number of Night-Time Micturitions was measured by the 3-day micturition diary completed for 3 consecutive days during the 7 days prior to each visit.~Change: mean at each visit minus mean at Baseline." (NCT00561951)
Timeframe: Baseline to Weeks 2, 4, 8, and 12
| Intervention | Night-Time Micturitions (Mean) | |||
|---|---|---|---|---|
| Week 2 (n=242, 256, 256) | Week 4 (n=236, 246, 248) | Week 8 (n=224, 232, 241) | Week 12 (n=220, 229, 236) | |
| Fesoterodine 4 mg | -0.24 | -0.30 | -0.45 | -0.48 |
| Fesoterodine 8 mg | -0.34 | -0.46 | -0.58 | -0.63 |
| Placebo | -0.25 | -0.30 | -0.41 | -0.44 |
"Number of micturitions was measured by the 3-day micturition diary completed for 3 consecutive days during the 7 days prior to each visit.~Change: mean at each visit minus mean at Baseline." (NCT00561951)
Timeframe: Baseline to Weeks 2, 4, 8, and 12
| Intervention | Micturitions (Mean) | |||
|---|---|---|---|---|
| Week 2 (n=308, 314, 305) | Week 4 (n=301, 303, 296) | Week 8 (n=289, 289, 287) | Week 12 (n=284, 284, 281) | |
| Fesoterodine 4 mg | -0.94 | -1.33 | -1.81 | -2.13 |
| Fesoterodine 8 mg | -1.06 | -1.60 | -2.15 | -2.17 |
| Placebo | -0.47 | -0.85 | -1.36 | -1.36 |
"Number of incontinence episodes was measured by the 3-day micturition diary completed for 3 consecutive days during the 7 days prior to each visit.~Incontinence is the complaint of any involuntary leakage of urine.~Change: mean at each visit minus mean at Baseline." (NCT00561951)
Timeframe: Baseline to Weeks 2, 4, 8, and 12
| Intervention | Incontinence Episodes (Mean) | |||
|---|---|---|---|---|
| Week 2 (n=308, 314, 305) | Week 4 (n=301, 303, 296) | Week 8 (n=289, 289, 287) | Week 12 (n=284, 284, 281) | |
| Fesoterodine 4 mg | -1.11 | -1.61 | -1.76 | -1.97 |
| Fesoterodine 8 mg | -1.06 | -1.50 | -1.73 | -1.86 |
| Placebo | -0.80 | -1.22 | -1.56 | -1.59 |
"The overactive bladder questionnaire (OAB-q) is used to assess the extent of participants who had been bothered by selected bladder symptoms and to assess the effect on their health-related quality of life (HRQL).~The each domain score ranges from 0 to 100 is a calculated value, where 0=minimal symptom severity and 100=greatest symptom severity for Symptom Bother Score, and where 0=worst HRQL outcome/response and 100=best HRQL outcome/response for HRQL domains including total score of HROL domain.~Change: mean at Week 12 minus mean at Baseline." (NCT00561951)
Timeframe: Baseline to Week 12
| Intervention | score on scale (Mean) | |||||
|---|---|---|---|---|---|---|
| Symptom Bother Score | Total Score of HRQL domain | Coping Score of HRQL domain | Concern Score of HRQL domain | Sleep Score of HRQL domain | Social Score of HRQL domain | |
| Fesoterodine 4 mg | -26.61 | 17.84 | 21.01 | 20.05 | 16.16 | 11.35 |
| Fesoterodine 8 mg | -26.35 | 17.29 | 21.48 | 19.10 | 15.35 | 9.98 |
| Placebo | -18.25 | 12.88 | 16.54 | 13.25 | 12.03 | 7.37 |
"Patient Perception of Bladder Condition (PPBC) score is rated on a 6-point scale as follows:~No problems at all~Some very minor problems~Some minor problems~Some moderate problems~Severe problems~Many severe problems" (NCT00561951)
Timeframe: Baseline to Week 12
| Intervention | participants (Number) | |
|---|---|---|
| Baseline | Week 12 | |
| Fesoterodine 4 mg | 97 | 12 |
| Fesoterodine 8 mg | 83 | 19 |
| Placebo | 82 | 28 |
"Voided volume per micturition was measured by the 3-day micturition diary completed for 3 consecutive days during the 7 days prior to each visit.~Voided volume was recorded during any 1 day of 3-day diary period through the first micturition of the next day.~Change: mean at Week 12 minus mean at Baseline." (NCT00561951)
Timeframe: Baseline to Week 12
| Intervention | mL (Mean) |
|---|---|
| Placebo | 13.07 |
| Fesoterodine 4 mg | 22.80 |
| Fesoterodine 8 mg | 32.77 |
"Number of urgency urinary incontinence episodes was measured by the 3-day micturition diary completed for 3 consecutive days during the 7 days prior to each visit.~Urgency urinary incontinence is the complaint of involuntary leakage accompanied by or immediately preceded by urgency. Urgency is the complaint of a sudden compelling desire to pass urine which is difficult to defer.~Change: mean at Week 12 minus mean at Baseline." (NCT00561951)
Timeframe: Baseline to Week 12
| Intervention | UUI Episodes (Least Squares Mean) |
|---|---|
| Placebo | -1.01 |
| Fesoterodine 4 mg | -1.35 |
| Fesoterodine 8 mg | -1.40 |
"King's Health Questionnaire(KHQ) is used to assess the impact of bladder problems on quality of life. The each domain score was calculated valued and ranged from 0 to 100, where 0=best outcome/response and 100=worst outcome/response.~Change: mean at Week 12 minus mean at Baseline." (NCT00561951)
Timeframe: Baseline to Week12
| Intervention | score on scale (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| General Health Perceptions (n=285, 283, 283) | Impact on Life (n=285, 283, 283) | Role Limitations (n=285, 283, 283) | Physical Limitations (n=285, 283, 283) | Social Limitations (n=285, 283, 283) | Personal Relationships (n=214, 210, 202) | Emotions (n=285, 283, 283) | Sleep/Energy (n=285, 283, 283) | Incontinence Severity Measures (n=285, 283, 283) | |
| Fesoterodine 4 mg | -9.36 | -27.33 | -27.92 | -23.50 | -17.92 | -16.11 | -24.70 | -19.08 | -17.67 |
| Fesoterodine 8 mg | -6.10 | -25.09 | -25.97 | -25.97 | -18.53 | -9.98 | -24.89 | -18.02 | -18.59 |
| Placebo | -7.02 | -22.46 | -20.47 | -18.65 | -14.44 | -8.33 | -18.01 | -12.51 | -13.75 |
IPSS Quality of Life (QoL) is one question used to assess how the patient's symptoms affect their quality of life. A score ranges from 1 to 6, with 6 being the worse outcome. (NCT00605319)
Timeframe: screening (Month 0), 2-months, 3-months, 7-months
| Intervention | units on a scale (Mean) | |||
|---|---|---|---|---|
| Time Screening Month-0 | Time Month-2 | Time Month-3 | Time Month-7 | |
| IPSS QoL | 4.2 | 3.8 | 3.5 | 3.5 |
International Prostate Symptom Score (IPSS) -is a 7 point scale used to screen, track and manage symptoms associated with BPH for obstructive, irritative, nocturia. The symptoms questions include feeling of incomplete bladder emptying, frequency, intermittency, urgency, weak stream, straining and nocturia. Scores range from 1 to 5 for a total of maximum 35 points (0-7 Mildly symptomatic, 8-19 Moderately symptomatic, 20-35 Severely symptomatic). This measure was taken for patients with irritative symptoms which includes frequency, urgency, nocturia and urge incontinence (NCT00605319)
Timeframe: screening (Month 0), 2-months, 3-months, 7-months
| Intervention | units on a scale (Mean) | |||
|---|---|---|---|---|
| Time Screening Month-0 | Time Month-2 | Time Month-3 | Time Month-7 | |
| IPSS Irritative | 6.6 | 5.6 | 5.1 | 4.4 |
International Prostate Symptom Score (IPSS) -is a 7 point scale used to screen, track and manage symptoms associated with BPH for obstructive, irritative, nocturia. The symptoms questions include feeling of incomplete bladder emptying, frequency, intermittency, urgency, weak stream, straining and nocturia. Scores range from 1 to 5 for a total of maximum 35 points (0-7 Mildly symptomatic, 8-19 Moderately symptomatic, 20-35 Severely symptomatic). This measure was taken for patients with nocturia meaning individuals who wake up during sleeping hours to urinate. (NCT00605319)
Timeframe: screening (Month 0), 2-months, 3-months, 7-months
| Intervention | units on a scale (Mean) | |||
|---|---|---|---|---|
| Time Screening Month-0 | Time Month-2 | Time Month-3 | Time Month-7 | |
| IPSS Nocturia | 3.2 | 2.8 | 2.6 | 2.6 |
International Prostate Symptom Score (IPSS) -is a 7 point scale used to screen, track and manage symptoms associated with BPH for obstructive, irritative, nocturia. The symptoms questions include feeling of incomplete bladder emptying, frequency, intermittency, urgency, weak stream, straining and nocturia. Scores range from 1 to 5 for a total of maximum 35 points (0-7 Mildly symptomatic, 8-19 Moderately symptomatic, 20-35 Severely symptomatic). This measure was taken for patients with obstructive symptoms which includes hesitancy or difficulty initiating the stream, straining to void, a reduced flow, an intermittent stream or a sensation of incomplete emptying. (NCT00605319)
Timeframe: screening (Month 0), 2-months, 3-months, 7-months
| Intervention | units on a scale (Mean) | |||
|---|---|---|---|---|
| Time Screening Month-0 | Time Month-2 | Time Month-3 | Time Month-7 | |
| IPSS Obstructive | 9.1 | 7.5 | 8.4 | 7.9 |
Urodynamics was used to meause maximum flow rate (Qmax) which is the maximum recorded flow rate of urinary (NCT00605319)
Timeframe: screening (Month 0), 2-months, 3-months, 7-months
| Intervention | mL/s (Mean) | |||
|---|---|---|---|---|
| Time Screening Month-0 | Time Month-2 | Time Month-3 | Time Month-7 | |
| Qmax | 15.3 | 10.2 | 10.6 | 10.5 |
Postvoid residual volume (PVR) is the volume of fluid remaining in the bladder immediately after the completion of micturition. (NCT00605319)
Timeframe: screening (Month 0), 2-months, 3-months, 7-months
| Intervention | mL (Mean) | |||
|---|---|---|---|---|
| Time Screening Month-0 | Time Month-2 | Time Month-3 | Time Month-7 | |
| Post-void Residual Volume (PVR) | 42.9 | 33.1 | 48.2 | 55.2 |
Average (mean) flow rate (Qavg) is the the volume of urine voided divided by the continuous flow time (NCT00605319)
Timeframe: screening (Month 0), 2-months, 3-months, 7-months
| Intervention | mL/s (Mean) | |||
|---|---|---|---|---|
| Time Screening Month-0 | Time Month-2 | Time Month-3 | Time Month-7 | |
| QAvg | NA | 5.1 | 6.1 | 6.2 |
UUI per 24 hours: total number of micturitions with Urinary Sensation Scale (USS) of 5 divided by total number of diary days collected at visit. USS: 5-item scale to measure urinary urgency; range: 1 (no feeling of urgency) to 5 (unable to hold; leak urine). (NCT00611026)
Timeframe: Baseline, Week 12
| Intervention | episodes per 24 hours (Mean) |
|---|---|
| Placebo | -1.62 |
| Tolterodine ER | -1.74 |
| Fesoterodine | -1.95 |
Symptom bother score derived as sum of scores for questions 1-8; lowest possible raw score: 8; highest possible score: 48. Data analyzed based on transformation of the score to a 0 to 100 scale [(Actual total raw score - lowest possible value of raw score)/range]*100. Higher scores values indicative of greater symptom bother. Negative change in Symptom Bother Score indicates improvement. (NCT00611026)
Timeframe: Baseline, Week 12
| Intervention | scores on a scale (Least Squares Mean) |
|---|---|
| Placebo | -21.8 |
| Tolterodine ER | -24.3 |
| Fesoterodine | -28.9 |
Frequency-Urgency Sum per 24 hours calculated as mean rating scores on the USS multiplied by the mean number of micturitions per 24 hours at that visit. USS is 5-item scale measuring urinary urgency; range is 1 (no feeling of urgency) to 5 (unable to hold; leak urine). (NCT00611026)
Timeframe: Baseline, Week 1, Week 4, Week 12
| Intervention | scores on a scale (Least Squares Mean) | ||
|---|---|---|---|
| Week 1 (n=447, 918, 906) | Week 4 [LOCF] (n=453, 929, 915) | Week 12 [LOCF] (n=453, 933, 915) | |
| Fesoterodine | -5.5 | -12.0 | -15.6 |
| Placebo | -4.0 | -8.1 | -12.0 |
| Tolterodine ER | -4.8 | -10.1 | -13.2 |
Mean number of nocturnal micturitions per 24 hours was calculated as the total number of all micturitions divided by the total number of diary days collected at that visit. Nocturnal micturitions are those recorded in the Bedtime section of the diary. Nocturnal (Bedtime) was defined as the time the participant went to bed until he/she arose to start the next day. (NCT00611026)
Timeframe: Baseline, Week 1, Week 4, Week 12
| Intervention | nocturnal micturitions per 24 hours (Least Squares Mean) | ||
|---|---|---|---|
| Week 1 (n=432, 879, 871) | Week 4 [LOCF] (n=437, 888, 879) | Week 12 [LOCF] (n=437, 892, 879) | |
| Fesoterodine | -0.3 | -0.5 | -0.7 |
| Placebo | -0.2 | -0.4 | -0.5 |
| Tolterodine ER | -0.3 | -0.5 | -0.6 |
Mean number of severe urgency episodes (USS rating ≥4 in diary ) per 24 hours calculated as the total number of micturitions with USS ≥4 divided by total number of diary days collected at that visit. USS: 5-item scale to measure urinary urgency; range: 1 (no feeling of urgency) to 5 (unable to hold; leak urine). (NCT00611026)
Timeframe: Baseline, Week 1, Week 4, Week 12
| Intervention | severe urgency episodes per 24 hours (Mean) | ||
|---|---|---|---|
| Week 1 (n=446, 915, 902) | Week 4 [LOCF] (n=452, 926, 911) | Week 12 [LOCF] (n=452, 930, 911) | |
| Fesoterodine | -1.58 | -3.21 | -4.08 |
| Placebo | -1.14 | -2.14 | -3.01 |
| Tolterodine ER | -1.34 | -2.71 | -3.39 |
Urgency Urinary episodes per 24 hours: total number of micturitions with Urinary Sensation Scale (USS) of ≥3 divided by total number of diary days collected at visit. USS: 5-item scale to measure urinary urgency; range: 1 (no feeling of urgency) to 5 (unable to hold; leak urine). (NCT00611026)
Timeframe: Baseline, Week 1, Week 4, Week 12
| Intervention | episodes per 24 hours (Least Squares Mean) | ||
|---|---|---|---|
| Week 1 (n=447, 918, 906) | Week 4 [LOCF] (n=453, 929, 915) | Week 12 [LOCF] (n=453, 933, 915) | |
| Fesoterodine | -1.2 | -3.1 | -4.2 |
| Placebo | -0.8 | -1.9 | -3.2 |
| Tolterodine ER | -1.0 | -2.5 | -3.5 |
UUI episodes per 24 hours calculated as total number of micturitions with Urinary Sensation Scale (USS) of 5 divided by total number of diary days collected at visit. USS is 5-item scale measuring urinary urgency; range is 1 (no feeling of urgency) to 5 (unable to hold; leak urine). (NCT00611026)
Timeframe: Baseline, Week 1, Week 4
| Intervention | episodes per 24 hours (Mean) | |
|---|---|---|
| Week 1 (n=442, 911, 899) | Week 4 [LOCF] (n=448, 922, 908) | |
| Fesoterodine | -1.03 | -1.68 |
| Placebo | -0.80 | -1.31 |
| Tolterodine ER | -0.95 | -1.52 |
Mean USS rating calculated as the sum of rating scores on USS per 24 hours divided by the total number of micturitions per 24 hours with non-missing rating at that visit. USS is 5-item scale measuring urinary urgency; range is 1 (no feeling of urgency) to 5 (unable to hold; leak urine). (NCT00611026)
Timeframe: Baseline, Week 1, Week 4, Week 12
| Intervention | scores on a scale (Least Squares Mean) | ||
|---|---|---|---|
| Week 1 (n=447, 918, 906) | Week 4 [LOCF] (n=453, 929, 915) | Week 12 [LOCF] (n=453, 933, 915) | |
| Fesoterodine | -0.2 | -0.5 | -0.7 |
| Placebo | -0.2 | -0.3 | -0.6 |
| Tolterodine ER | -0.2 | -0.4 | -0.6 |
Mean voided volume in milliliters (mL) calculated as sum of voided volume divided by the total number of micturition episodes with a recorded voided volume greater than 0 in the 3-day diary at that visit. (NCT00611026)
Timeframe: Baseline, Week 1, Week 4, Week 12
| Intervention | mL (Mean) | ||
|---|---|---|---|
| Week 1 (n=447, 917, 895) | Week 4 [LOCF] (n=452, 927, 909) | Week 12 [LOCF] (n=452, 930, 912) | |
| Fesoterodine | 18.63 | 32.26 | 34.47 |
| Placebo | 9.80 | 14.27 | 17.34 |
| Tolterodine ER | 15.65 | 26.43 | 28.43 |
"HRQL domain and total raw score derived as sum of scores (6-point scale:~1=not at all/none of the time; 6=a very great deal/all of the time). Transformed score (Total HRQL or domain)=[(Highest possible raw score- Actual total raw score)/Raw score range] * 100. Higher transformed scores indicative of better HRQL. Positive change in HRQL Score indicates improvement." (NCT00611026)
Timeframe: Baseline, Week 12
| Intervention | scores on a scale (Least Squares Mean) | ||||
|---|---|---|---|---|---|
| HRQL scale score total (n=431, 892, 873) | HRQL concern domain (n=434, 894, 875) | HRQL coping domain (n=433, 892, 875) | HRQL sleep domain (n=433, 894, 875) | HRQL social interaction domain (n=435, 894, 873) | |
| Fesoterodine | 22.9 | 26.8 | 25.9 | 21.0 | 13.9 |
| Placebo | 17.2 | 20.2 | 19.0 | 16.6 | 10.8 |
| Tolterodine ER | 19.5 | 22.5 | 22.0 | 18.7 | 12.0 |
Number of participants in 4-point category: ≥2 points improvement (major improvement; negative change from baseline); 1 point improvement (minor improvement); no change; deterioration (positive change from baseline), based on PPBC score (rated on 6-point scale: 1=no problems at all; 6=many severe problems). Score change: score at observation minus score at baseline; re-scaled to 4-point categorical variables. (NCT00611026)
Timeframe: Baseline, Week 1, Week, 4, Week 12
| Intervention | participants (Number) | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Week 1 (n=452, 931, 913) ≥2 points improvement | Week 1: 1-point improvement | Week 1: no change | Week 1: deterioration | Week 4 (n=455, 937, 918) ≥2 points improvement | Week 4: 1-point improvement | Week 4: no change | Week 4: deterioration | Week 12 (n=455, 937, 918) ≥2 points improvement | Week 12: 1-point improvement | Week 12: no change | Week 12: deterioration | |
| Fesoterodine | 144 | 280 | 428 | 61 | 334 | 280 | 250 | 54 | 440 | 236 | 189 | 53 |
| Placebo | 43 | 144 | 210 | 55 | 111 | 124 | 172 | 48 | 166 | 106 | 133 | 50 |
| Tolterodine ER | 138 | 278 | 434 | 81 | 290 | 298 | 285 | 64 | 379 | 250 | 249 | 59 |
Number of participants in 3-point category: improvement [≥1-point improvement]; no change; deterioration [≥1-point decrease], based on UPS score (rated on 3-point scale: 1=not able to hold urine; 3=able to finish what I am doing). Score change calculated as score at observation minus score at baseline; re-scaled to 3-point categorical variables. (NCT00611026)
Timeframe: Baseline, Week 1, Week, 4, Week 12
| Intervention | participants (Number) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Week 1 (n=452, 932, 913) improvement | Week 1: no change | Week 1: deterioration | Week 4 (n=455, 938, 918) improvement | Week 4: no change | Week 4: deterioration | Week 12 (n=455, 938, 918) improvement | Week 12: no change | Week 12: deterioration | |
| Fesoterodine | 267 | 609 | 37 | 421 | 467 | 30 | 495 | 393 | 30 |
| Placebo | 97 | 326 | 29 | 161 | 271 | 23 | 183 | 239 | 33 |
| Tolterodine ER | 264 | 619 | 49 | 376 | 511 | 51 | 440 | 455 | 43 |
Diary dry rate: percentage of participants with no urgency urinary incontinence episode reported in the 3 day diary at the respective time-point; based on USS: 5-item scale measuring urinary urgency; range is 1 (no feeling of urgency) to 5 (unable to hold; leak urine). (NCT00611026)
Timeframe: Week 1, Week 4, Week 12
| Intervention | percentage of participants (Number) | ||
|---|---|---|---|
| Week 1 (n=422, 911, 899) | Week 4 [LOCF] (n=448, 922, 908) | Week 12 [LOCF] (n=448, 926, 908) | |
| Fesoterodine | 25.1 | 51.1 | 63.2 |
| Placebo | 17.6 | 39.5 | 53.8 |
| Tolterodine ER | 24.5 | 46.7 | 58.1 |
Percent change from baseline in mean number of Urgency Urinary episodes per 24 hours (Urinary Sensation Scale ≥3 in the diary). Change calculated as UUI episodes per 24 hours at observation divided by baseline number of UUI episodes per 24 hours, multiplied by 100. (NCT00611026)
Timeframe: Baseline, Week 1, Week 4, Week 12
| Intervention | percent change (Median) | ||
|---|---|---|---|
| Week 1 (n=447, 918, 906) | Week 4 [LOCF] (n=453, 929, 915) | Week 12 [LOCF] (n=453, 933, 915) | |
| Fesoterodine | -11.8 | -32.1 | -45.5 |
| Placebo | -9.4 | -17.2 | -31.0 |
| Tolterodine ER | -12.0 | -26.3 | -37.5 |
Percent change of micturitions per 24 hours was calculated as change in 24-hour mean at that visit divided by the baseline 24-hour mean multiplied by 100 (ie, 100%*(Week 1 or 4 or 12 - baseline)/baseline). (NCT00611026)
Timeframe: Baseline, Week 1, Week 4, Week 12
| Intervention | percent change (Median) | ||
|---|---|---|---|
| Week 1 (n=448, 921, 908) | Week 4 [LOCF] (n=454, 931, 916) | Week 12 [LOCF] (n=454, 935, 916) | |
| Fesoterodine | -9.0 | -18.9 | -23.5 |
| Placebo | -7.1 | -13.4 | -18.2 |
| Tolterodine ER | -9.4 | -16.7 | -20.8 |
Percent change of nocturnal micturitions per 24 hours was calculated as change in 24-hour mean at that visit divided by the baseline 24-hour mean multiplied by 100 (ie, 100%*(Week 1 or 4 or 12 - baseline)/baseline). Nocturnal micturitions are those recorded in the Bedtime section of the diary. Nocturnal (Bedtime) was defined as the time the participant went to bed until he/she arose to start the next day. (NCT00611026)
Timeframe: Baseline, Week 1, Week 4, Week 12
| Intervention | percent change (Median) | ||
|---|---|---|---|
| Week 1 (n=432, 879, 871) | Week 4 [LOCF] (n=437, 888, 879) | Week 12 [LOCF] (n=437, 892, 879) | |
| Fesoterodine | -12.5 | -25.0 | -33.3 |
| Placebo | -7.7 | -20.0 | -27.3 |
| Tolterodine ER | -14.3 | -25.0 | -33.3 |
Percent change calculated as change in severe urgency episodes (USS rating ≥4 in diary ) per 24 hours at that visit divided by the baseline number of severe urgency episodes per 24 hours, multiplied by 100. USS is 5-item scale measuring urinary urgency; range is 1 (no feeling of urgency) to 5 (unable to hold; leak urine). (NCT00611026)
Timeframe: Baseline, Week 1, Week 4, Week 12
| Intervention | percent change (Median) | ||
|---|---|---|---|
| Week 1 (n=446, 915, 902) | Week 4 [LOCF] (n=452, 926, 911) | Week 12 [LOCF] (n=452, 930, 911) | |
| Fesoterodine | -25.0 | -61.1 | -79.3 |
| Placebo | -19.7 | -41.7 | -61.0 |
| Tolterodine ER | -24.1 | -55.6 | -69.2 |
"UUI episodes per 24 hours calculated as total number of micturitions with USS of 5 in diary. USS is 5-item scale measuring urinary urgency; range is~1 (no feeling of urgency) to 5 (unable to hold; leak urine). Change calculated as UUI episodes per 24 hours at observation divided by baseline number of UUI episodes per 24 hours, multiplied by 100." (NCT00611026)
Timeframe: Baseline, Week 1, Week 4, Week 12
| Intervention | percent change (Median) | ||
|---|---|---|---|
| Week 1 (n=442, 911, 899) | Week 4 [LOCF] (n=448, 922, 908) | Week 12 [LOCF] (n=448, 926, 908) | |
| Fesoterodine | -50.0 | -100.0 | -100.0 |
| Placebo | -40.8 | -75.0 | -100.0 |
| Tolterodine ER | -50.0 | -88.9 | -100.0 |
An adverse event is any untoward medical occurrence in a clinical investigation in which the participant was administered a product or medical device; the event does not necessarily need to have a causal relationship with the treatment or usage. (NCT00611026)
Timeframe: Baseline up to Week 12
| Intervention | events (Number) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Constipation | Fingers tingling | Finger numbness | Hypertension | Diabetes mellitus | Abdominal distension and discomfort | Tina pedis | Tingling sensation/decreased sensation of fingers | Dyspepsia | Abdominal bloating | |
| Fesoterodine | 0 | 1 | 1 | 2 | 2 | 1 | 1 | 1 | 1 | 1 |
| Tolterodine ER | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
The mean number of micturitions was calculated as the total number of micturitions divided by the total number of diary days collected at that visit. (NCT00611026)
Timeframe: Baseline, Week 1, Week 4, Week 12
| Intervention | micturitions per 24 hours (Least Squares Mean) | ||
|---|---|---|---|
| Week 1 (n=448, 921, 908) | Week 4 [LOCF] (n=454, 931, 916) | Week 12 [LOCF] (n=454, 935, 916) | |
| Fesoterodine | -1.0 | -2.1 | -2.6 |
| Placebo | -0.8 | -1.5 | -2.0 |
| Tolterodine ER | -1.0 | -1.8 | -2.3 |
"The number of urgency episodes was measured by the 3-day micturition diary completed for 3 consecutive days during the 7 days prior to each visit.~The mean number of urgency episodes per 24 hours was calculated as the total number of urgency episodes for valid diary days divided by the total number of valid diary days collected at that visit.~Change: mean at Week 4, 8, 28 and 52 minus mean at Baseline" (NCT00658684)
Timeframe: Week 4, 8, 28 and 52
| Intervention | Number of episodes (Mean) | |||||
|---|---|---|---|---|---|---|
| Baseline (n=150, 97, 25, 28) | Week 4 (n=150, 97, 25, 28) | Week 8 (n=148, 95, 25, 28) | Week 28 (n=137, 87, 23, 27) | Week 52 (n=133, 84, 22, 27) | Week 52 (LOCF) (n=150, 97, 25, 28) | |
| 4 mg | 3.9 | -1.77 | -2.32 | -2.41 | -2.55 | -2.30 |
| 4 mg > 8 mg | 5.1 | -1.37 | -2.70 | -2.46 | -3.37 | -3.40 |
| 4 mg > 8 mg > 4 mg | 6.2 | -1.75 | -2.59 | -3.12 | -2.80 | -2.93 |
| Total | 4.5 | -1.69 | -2.44 | -2.54 | -2.76 | -2.61 |
"The number of micturitions was measured by the 3-day micturition diary completed for 3 consecutive days during the 7 days prior to each visit.~The mean number of micturitions per 24 hours was calculated as the total number of micturitions for valid diary days divided by the total number of valid diary days collected at that visit.~Change: mean at Week 4, 8, 28 and 52 minus mean at Baseline" (NCT00658684)
Timeframe: Week 4, 8, 28 and 52
| Intervention | Number of micturitions (Mean) | |||||
|---|---|---|---|---|---|---|
| Baseline (n=150, 97, 25, 28) | Week 4 (n=150, 97, 25, 28) | Week 8 (n=148, 95, 25, 28) | Week 28 (n=137, 87, 23, 27) | Week 52 (n=133, 84, 22, 27) | Week 52 (LOCF) (n=150, 97, 25, 28) | |
| 4 mg | 11.0 | -1.73 | -2.03 | -2.18 | -2.48 | -2.35 |
| 4 mg > 8 mg | 12.3 | -0.45 | -2.63 | -3.02 | -3.44 | -3.36 |
| 4 mg > 8 mg > 4 mg | 11.2 | -1.28 | -1.81 | -2.06 | -2.21 | -2.04 |
| Total | 11.3 | -1.42 | -2.11 | -2.33 | -2.63 | -2.49 |
"The number of incontinence episodes was measured by the 3-day micturition diary completed for 3 consecutive days during the 7 days prior to each visit.~The mean number of incontinence episodes per 24 hours was calculated as the total number of incontinence episodes for valid diary days divided by the total number of valid diary days collected at that visit.~Change: mean at Week 4, 8, 28 and 52 minus mean at Baseline" (NCT00658684)
Timeframe: Week 4, 8, 28 and 52
| Intervention | Number of episodes (Mean) | |||||
|---|---|---|---|---|---|---|
| Baseilne (n=103, 62, 17,24) | Week 4 (n=103, 62, 17,24) | Week 8 (n=102, 61, 17, 24) | Week 28 (n= 97, 58, 16, 23) | Week 52 (n=94, 56, 15, 23) | Week 52 (LOCF) (n=103, 62, 17,24) | |
| 4 mg | 1.6 | -0.99 | -1.16 | -1.26 | -1.26 | -1.24 |
| 4 mg > 8 mg | 2.5 | -0.49 | -1.28 | -1.77 | -1.75 | -1.86 |
| 4 mg > 8 mg > 4 mg | 1.8 | -0.80 | -1.43 | -1.31 | -1.16 | -1.20 |
| Total | 1.8 | -0.84 | -1.23 | -1.39 | -1.37 | -1.38 |
"The PPBC assessment was rated on a 6-point scale as follows:~no problems at all~some very minor problems~some minor problems~some moderate problems~severe problems~many severe problems~Change: mean at Week 28 and 52 minus mean at baseline A negative change indicates improvement." (NCT00658684)
Timeframe: Week 28 and 52
| Intervention | Scores on a scale (Mean) | ||
|---|---|---|---|
| Baseline (n=150, 97, 25, 28) | Week 28 (n=137, 87, 23, 27) | Week 52 (n=134, 85, 22, 27) | |
| 4 mg | 4.2 | -1.74 | -1.85 |
| 4 mg > 8 mg | 4.4 | -1.26 | -1.70 |
| 4 mg > 8 mg > 4 mg | 4.5 | -1.83 | -1.59 |
| Total | 4.3 | -1.66 | -1.78 |
"The number of subjects whose perception of bladder condition improved at least by one grade on PPBC from baseline at Week 28 and 52. The PPBC was rated on a 6-point scale as follows:~no problems at all~some very minor problems~some minor problems~some moderate problems~severe problems~many severe problems" (NCT00658684)
Timeframe: Week 28 and 52
| Intervention | Number of subjects (Number) | |
|---|---|---|
| Week 28 (n=137, 87, 23, 27) | Week 52 (n=134, 85, 22, 27) | |
| 4 mg | 75 | 75 |
| 4 mg > 8 mg | 19 | 23 |
| 4 mg > 8 mg > 4 mg | 21 | 18 |
| Total | 115 | 116 |
The number of subjects who experienced AEs (all causality and treatment-related ) based on safety assessment during the study were summarized. The severity and seriousness of treatment-emergent AEs as well as discontinuations, dose reductions and temporary discontinuations (DR/TD) due to treatment-emergent AEs were also summarized. (NCT00658684)
Timeframe: 52 Weeks
| Intervention | Number of subjects (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| All-causality AEs | Treatment-related AEs | Serious AEs | Severe AEs | Discontinuations due to all-causlity AEs | Discontinuations due to treatment-related AEs | DR/TD due to all-causality AEs | DR/TD due to treatment-related AEs | |
| 4 mg | 91 | 61 | 1 | 0 | 8 | 6 | 6 | 0 |
| 4 mg > 8 mg | 22 | 16 | 0 | 0 | 0 | 0 | 1 | 0 |
| 4 mg > 8 mg > 4 mg | 25 | 25 | 0 | 0 | 2 | 1 | 23 | 23 |
| Total | 138 | 102 | 1 | 0 | 10 | 7 | 30 | 23 |
"OAB-q was used to assess the extent of subjects who had been botehred by selected bladder symptoms and to assess the effect on their health-related quality of life (HRQL). OAB-q consists of the symptom bother score(SBS), the HRQL total score and subscale scores (Coping, Concern, Sleep and Social). The SBS ranges from 0 to 100, where 0=minimal severity and 100=greatest severity (negative change indicates improvement). The HRQL scores range from 0 to 100, where 0=worst outcome and 100=best outcome (positive change indicates improvement).~Change: mean at Week 28 and 52 minus mean at baseline" (NCT00658684)
Timeframe: Week 28 and 52
| Intervention | Scores on a scale (Mean) | |||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| SBS: Baseline (n=150, 97, 25, 28) | SBS: Week 28 (n=137, 87, 23, 27) | SBS: Week 52 (n=134, 85, 22, 27) | HRQL-Total: Baseline (n=150, 97, 25, 28) | HRQL-Total: Week 28 (n=137, 87, 23, 27) | HRQL-Total: Week 52 (n=134, 85, 22, 27) | HRQL-Coping: Baseline (n=150, 97, 25, 28) | HRQL-Coping: Week 28 (n=137, 87, 23, 27) | HRQL-Coping: Week 52 (n=134, 85, 22, 27) | HRQL-Concern: Baseline (n=150, 97, 25, 28) | HRQL-Concern: Week 28 (n=137, 87, 23, 27) | HRQL-Concern: Week 52 (n=134, 85, 22, 27) | HRQL-Sleep: Baseline (n=150, 97, 25, 28) | HRQL-Sleep: Week 28 (n=137, 87, 23, 27) | HRQL-Sleep: Week 52 (n=134, 85, 22, 27) | HRQL-Social: Baseline (n=150, 97, 25, 28) | HRQ- Social: Week 28 (n=137, 87, 23, 27) | HRQL-Social: Week 52 (n=134, 85, 22, 27) | |
| 4 mg | 37.4 | -22.30 | -22.41 | 73.9 | 14.26 | 15.99 | 65.6 | 19.66 | 20.91 | 73.9 | 16.95 | 19.23 | 69.9 | 11.13 | 13.32 | 91.2 | 5.01 | 6.26 |
| 4 mg > 8 mg | 58.7 | -32.59 | -37.41 | 58.4 | 19.88 | 22.76 | 45.1 | 27.04 | 29.91 | 59.5 | 21.06 | 24.13 | 55.6 | 15.85 | 21.33 | 81.0 | 10.81 | 10.81 |
| 4 mg > 8 mg > 4 mg | 45.2 | -27.07 | -21.25 | 72.2 | 16.00 | 13.35 | 64.6 | 18.15 | 15.00 | 72.5 | 21.24 | 16.49 | 65.8 | 13.22 | 13.09 | 90.6 | 8.00 | 6.55 |
| Total | 42.7 | -25.13 | -25.24 | 70.7 | 15.66 | 16.92 | 61.6 | 20.86 | 21.75 | 71.0 | 18.48 | 19.77 | 66.5 | 12.41 | 14.90 | 89.2 | 6.66 | 7.22 |
"KHQ was used to assess the impact of bladder problems on quality of life. The scores ranged from 0 to 100, where 0=best outcome/response and 100=worst outcome/response. A negative change indicates improvement.~KHQ consists of the following domains:~General health perceptions (GHP)~Impact on life~Role limitations~Physical limitations~Social limitations~Personal relationships (PR)~Emotions~Sleep/energy~Incontinence severity measures (ISM)~Change: mean at Week 28 and 52 minus mean at Baseline" (NCT00658684)
Timeframe: Week 28 and 52
| Intervention | Scores on a ascle (Mean) | ||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| GHP: Baseline (n=150, 97, 25, 28) | GHP: Week 28 (n=137, 87, 23, 27) | GHP: Week 52 (n=134, 85, 22, 27) | Impact on life: Baseline (n=150, 97, 25, 28) | Impact on life: Week 28 (n=137, 87, 23, 27) | Impact on life: Week 52 (n=134, 85, 22, 27) | Role limitations: Baseline (n=150, 97, 25, 28) | Role limitations: Week 28 (n=137, 87, 23, 27) | Role limitations: Week 52 (n=134, 85, 22, 27) | Physical limitations: Baseline (n=150, 97, 25, 28 | Physical limitations: Week 28 (n=137, 87, 23, 27) | Physical limitations: Week 52 (n=134, 85, 22, 27) | Social limitations: Baseline (n=150, 97, 25, 28) | Social limitations: Week 28 (n=137, 87, 23, 27) | Social limitations: Week 52 (n=134, 85, 22, 27) | PR: Baseline (n=124, 82, 18, 24) | PR: Week 28 (n=110, 71, 16, 23) | PR: Week 52 (n=109, 70, 16, 23) | Emotions: Baseline (n=150, 97, 25, 28) | Emotions: Week 28 (n=137, 87, 23, 27) | Emotions: Week 52 (n=134, 85, 22, 27) | Sleep/energy: Baseline (n=150, 97, 25, 28) | Sleep/energy: Week 28 (n=137, 87, 23, 27) | Sleep/energy: Week 52 (n=134, 85, 22, 27) | ISM: Baseline (n=150, 97, 25, 28) | ISM: Week 28 (n=137, 87, 23, 27) | ISM: Week 52 (n=134, 85, 22, 27) | |
| 4 mg | 37.1 | -0.57 | -5.88 | 61.2 | -32.18 | -32.94 | 46.0 | -28.16 | -30.98 | 49.8 | -26.63 | -32.16 | 27.5 | -17.37 | -20.72 | 17.3 | -11.74 | -13.57 | 49.1 | -27.84 | -32.42 | 33.2 | -17.43 | -20.59 | 32.6 | -14.87 | -18.43 |
| 4 mg > 8 mg | 39.3 | -9.26 | -2.78 | 70.2 | -30.86 | -34.57 | 50.6 | -23.46 | -25.31 | 57.1 | -25.93 | -25.31 | 39.3 | -24.28 | -25.51 | 29.2 | -19.57 | -19.57 | 57.5 | -26.34 | -26.75 | 50.0 | -22.84 | -27.78 | 45.7 | -20.25 | -24.44 |
| 4 mg > 8 mg > 4 mg | 37.0 | 0.00 | -5.68 | 68.0 | -37.68 | -31.82 | 52.0 | -33.33 | -31.06 | 54.0 | -31.16 | -28.03 | 31.1 | -22.71 | -24.75 | 16.7 | -10.42 | -12.50 | 52.0 | -27.54 | -26.26 | 37.3 | -18.12 | -15.91 | 31.5 | -16.81 | -14.55 |
| Total | 37.5 | -2.19 | -5.22 | 64.0 | -32.85 | -33.08 | 47.9 | -28.10 | -29.85 | 51.9 | -27.25 | -30.10 | 30.3 | -19.63 | -22.35 | 19.5 | -13.18 | -14.68 | 51.2 | -27.49 | -30.27 | 37.0 | -18.61 | -21.27 | 34.8 | -16.25 | -19.00 |
"The number of nighttime micturitions was measured by the 3-day micturition diary completed for 3 consecutive days during the 7 days prior to each visit.~The mean number of nighttime micturitions per 24 hours was calculated as the total number of nighttime micturitions for valid diary days divided by the total number of valid diary days collected at that visit.~Change: mean at Week 4, 8, 28 and 52 minus mean at Baseline" (NCT00658684)
Timeframe: Week 4, 8, 28 and 52
| Intervention | Number of micturitions (Mean) | |||||
|---|---|---|---|---|---|---|
| Baseline (n=116, 69, 23, 24) | Week 4 (n=116, 69, 23, 24) | Week 8 (n=115, 68, 23, 24) | Week 28 (n=106, 62, 21, 23) | Week 52 (n=103, 60, 20, 23) | Week 52 (LOCF) (n=116, 69, 23, 24) | |
| 4 mg | 1.2 | -0.34 | -0.33 | -0.36 | -0.46 | -0.38 |
| 4 mg > 8 mg | 1.6 | -0.08 | -0.60 | -0.71 | -0.75 | -0.71 |
| 4 mg > 8 mg > 4 mg | 1.6 | -0.45 | -0.55 | -0.56 | -0.68 | -0.62 |
| Total | 1.4 | -0.31 | -0.43 | -0.47 | -0.57 | -0.50 |
"Voided volume per micturition was measured by the 3-day micturition diary completed for 3 consecutive days during the 7 days prior to each visit.~The mean voided volume per micturitions was calculated as the total voided volume for valid diary days divided by the total number of valid diary days collected at that visit.~Change: mean at Week 4, 8, 28 and 52 minus mean at Baseline" (NCT00658684)
Timeframe: Week 4, 8, 28 and 52
| Intervention | mL (Mean) | |||||
|---|---|---|---|---|---|---|
| Baseline (n=150, 97, 25, 28) | Week 4 (n=150, 97, 25, 28) | Week 8 (n=148, 95, 25, 28) | Week 28 (n=137, 87, 23, 27) | Week 52 (n=133, 84, 22, 27) | Week 52 (LOCF) (n=150, 97, 25, 28) | |
| 4 mg | 162.8 | 20.58 | 21.86 | 31.98 | 40.21 | 37.08 |
| 4 mg > 8 mg | 143.6 | 7.16 | 23.37 | 28.10 | 24.95 | 25.38 |
| 4 mg > 8 mg > 4 mg | 156.1 | 12.18 | 23.00 | 40.20 | 33.02 | 28.22 |
| Total | 158.1 | 16.67 | 22.34 | 32.59 | 35.92 | 33.42 |
"The number of UUI episodes was measured by the 3-day micturition diary completed for 3 consecutive days during the 7 days prior to each visit.~The mean number of UUI episodes per 24 hours was calculated as the total number of UUI episodes for valid diary days divided by the total number of valid diary days collected at that visit.~Change: mean at Week 4, 8, 28 and 52 minus mean at Baseline" (NCT00658684)
Timeframe: Week 4, 8, 28 and 52
| Intervention | Number of episodes (Mean) | |||||
|---|---|---|---|---|---|---|
| Baseline (n=101, 60, 17, 24) | Week 4 (n=101, 60, 17, 24) | Week 8 (n=100, 59, 17, 24) | Week 28 (n=95, 56, 16, 23) | Week 52 (n= 92, 54, 15, 23) | Week 52 (LOCF) (n=101, 60, 17, 24) | |
| 4 mg | 1.4 | -0.99 | -1.16 | -1.24 | -1.23 | -1.19 |
| 4 mg > 8 mg | 2.1 | -0.63 | -1.00 | -1.41 | -1.71 | -1.82 |
| 4 mg > 8 mg > 4 mg | 1.7 | -0.73 | -1.31 | -1.25 | -1.18 | -1.22 |
| Total | 1.6 | -0.86 | -1.15 | -1.28 | -1.34 | -1.35 |
Symptom severity/bother score: sub-section of the OAB-q consists of 8 questions. Each item assessed on ordinal scale (0=Not at all to 5=a very great deal). Score=sum of scores for items 1 to 8 and a further 2 points were added if subject was male. Lowest possible score=0 and highest=42. Data were transformed onto a 0 to 100 scale and analyzed based on the transformed score: Transformed Symptom Bother Score=[(Actual Total Raw Score minus Lowest possible value of raw score) divided by Range] multiplied by 100. Higher scores=greater symptom severity or bother and lower=minimal symptom severity. (NCT00691093)
Timeframe: Baseline, Month 3 or ET
| Intervention | scores on a scale (Mean) |
|---|---|
| Fesoterodine 4 mg | -34.101 |
| Fesoterodine 8 mg | -34.318 |
| Increase of Dose From 4 mg to 8 mg Due to Lack of Efficacy | -32.018 |
Overall Treatment Effect Scale: 3 questions from which a numeric score was derived. If a subject answered '(2) About the same' to question 1 then a score of 0 was given. If a subject answered '(1) Worse' to question 1, then a score between -7=a very great deal worse to -1=Almost the same, hardly worse at all was given depending on severity of their symptoms (determined from answer to question 2). If a subject answered '(3) Better' to question 1, then a score ranging from 1=Almost the same, hardly better at all to 7=A very great deal better, depending on their answer to question 3, was given. (NCT00691093)
Timeframe: Month 3 or ET
| Intervention | scores on a scale (Mean) |
|---|---|
| Fesoterodine 4 mg | 5.661 |
| Fesoterodine 8 mg | 5.818 |
| Increase of Dose From 4 mg to 8 mg Due to Lack of Efficacy | 4.702 |
Participant's perception of treatment response assessment since the previous visit was noted at each visit. Time to onset of response was calculated in weeks from start of treatment. (NCT00691093)
Timeframe: Month 1, Month 2, Month 3 or ET
| Intervention | weeks (Median) |
|---|---|
| Fesoterodine 4 mg | 3.0 |
| Fesoterodine 8 mg | 3.0 |
| Increase of Dose From 4 mg to 8 mg Due to Lack of Efficacy | 3.0 |
Micturition frequency: mean number of 'day time' (i.e., the time the participant was awake) micturitions per 24 hours and calculated as the total number of 'day time' urinations, divided by the total diary days collected at that visit. (NCT00691093)
Timeframe: Baseline, Month 1, Month 2, Month 3 or Early Termination (ET)
| Intervention | episodes (Mean) | |||
|---|---|---|---|---|
| Baseline | Visit 2 (Month 1) | Visit 3 (Month 2) | Visit 4 (Month 3 or ET) | |
| Fesoterodine 4 mg | 11.661 | -2.306 | -3.482 | -4.180 |
| Fesoterodine 8 mg | 10.636 | -2.303 | -2.848 | -4.000 |
| Increase of Dose From 4 mg to 8 mg Due to Lack of Efficacy | 12.664 | -1.566 | -3.160 | -4.031 |
Nocturnal frequency: mean number of 'night time' (the time the participant was asleep and the urge to urinate woke him/her up) micturitions and calculated as the total number of 'night time' urinations, divided by the total diary days collected at that visit. (NCT00691093)
Timeframe: Baseline, Month 1, Month 2, Month 3 or ET
| Intervention | episodes (Mean) | |||
|---|---|---|---|---|
| Baseline | Visit 2 (Month 1) | Visit 3 (Month 2) | Visit 4 (Month 3 or ET) | |
| Fesoterodine 4 mg | 3.027 | -1.104 | -1.621 | -1.914 |
| Fesoterodine 8 mg | 4.000 | -1.212 | -1.848 | -2.030 |
| Increase of Dose From 4 mg to 8 mg Due to Lack of Efficacy | 3.528 | -0.915 | -1.613 | -2.072 |
The PVR urine volume: measured by an ultrasound scan. (NCT00691093)
Timeframe: Baseline, Month 1, Month 2, Month 3 or ET
| Intervention | ml (Mean) | |||
|---|---|---|---|---|
| Baseline | Visit 2 (Month 1) | Visit 3 (Month 2) | Visit 4 (Month 3 or ET) | |
| Fesoterodine 4 mg | 27.932 | -6.650 | -9.864 | -12.800 |
| Fesoterodine 8 mg | 42.000 | -12.800 | -18.700 | -21.000 |
| Increase of Dose From 4 mg to 8 mg Due to Lack of Efficacy | 24.867 | -2.364 | -5.791 | -7.415 |
The mean number of UUI episodes: total number of UUI episodes, divided by the total diary days collected at that visit. (NCT00691093)
Timeframe: Baseline, Month 1, Month 2, Month 3 or ET
| Intervention | episodes (Mean) | |||
|---|---|---|---|---|
| Baseline | Visit 2 (Month 1) | Visit 3 (Month 2) | Visit 4 (Month 3 or ET) | |
| Fesoterodine 4 mg | 2.601 | -1.209 | -1.806 | -2.065 |
| Fesoterodine 8 mg | 2.933 | -1.067 | -1.583 | -1.733 |
| Increase of Dose From 4 mg to 8 mg Due to Lack of Efficacy | 3.467 | -1.190 | -1.781 | -2.362 |
UEF: mean number of micturition related urgency episodes per 24 hours and calculated as the total number of 'urgency' urinations (i.e., sudden urges to urinate and problems to delay micturition) divided by 3 (or if data for 3 days were not available, over the total number of diary days collected at that visit). (NCT00691093)
Timeframe: Baseline, Month 1, Month 2, Month 3 or ET
| Intervention | episodes (Mean) | |||
|---|---|---|---|---|
| Baseline | Visit 2 (Month 1) | Visit 3 (Month 2) | Visit 4 (Month 3 or ET) | |
| Fesoterodine 4 mg | 4.412 | -1.890 | -2.736 | -3.127 |
| Fesoterodine 8 mg | 4.697 | -1.697 | -2.182 | -2.636 |
| Increase of Dose From 4 mg to 8 mg Due to Lack of Efficacy | 5.587 | -1.650 | -2.895 | -3.814 |
Clinical global evaluation of study medication was assessed via the question 'how would you rate the study medication the patient received for overactive bladder?,' and was assessed on the four point categorical scale, ranging from 'Poor' to 'Excellent.' (NCT00691093)
Timeframe: 12 weeks
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| Excellent | Good | Fair | Poor | Missing | |
| All Subjects | 513 | 274 | 24 | 9 | 3 |
Symptom severity/bother score: sub-section of the OAB-q consists of 8 questions. Each item assessed on ordinal scale (0=Not at all to 5=a very great deal). Score=sum of scores for items 1 to 8 and a further 2 points were added if subject was male. Lowest possible score=0 and highest=42. Data were transformed onto a 0 to 100 scale and analyzed based on the transformed score: Transformed Symptom Bother Score=[(Actual Total Raw Score minus Lowest possible value of raw score) divided by Range] multiplied by 100. Higher scores=greater symptom severity or bother and lower=minimal symptom severity. (NCT00691093)
Timeframe: Baseline, Month 3 or ET
| Intervention | scores on a scale (Mean) | |
|---|---|---|
| Baseline | Visit 4 (Month 3 or ET) | |
| Fesoterodine 4 mg | 59.263 | 25.147 |
| Fesoterodine 8 mg | 70.000 | 35.682 |
| Increase of Dose From 4 mg to 8 mg Due to Lack of Efficacy | 64.737 | 32.719 |
The patients global evaluation of study medication was assessed via the question 'how would you rate your overall response to the study medication?' and was assessed on the four point categorical scale, ranging from 'Poor' to 'Excellent'. (NCT00691093)
Timeframe: Baseline, Month 3 or ET
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| Excellent | Good | Fair | Poor | Missing | |
| All Subjects | 536 | 252 | 22 | 10 | 3 |
Possible change in the dose and the reasons for the change were collected and documented. (NCT00691093)
Timeframe: Month 3 or ET
| Intervention | participants (Number) | |||||
|---|---|---|---|---|---|---|
| Inefectivity, Not Sufficient Effectivity | Infectivity | Insufficient (efficiency) effect | Insufficient response | Poor overall response | Missing | |
| All Subjects | 22 | 29 | 1 | 1 | 1 | 4 |
Number of subjects that changed doses throughout the study period. (NCT00691093)
Timeframe: Month 3 or ET
| Intervention | participants (Number) | |||
|---|---|---|---|---|
| Increased | Stayed the same | Decreased | Fluctuated | |
| All Subjects | 57 | 766 | 0 | 0 |
Nocturnal micturitions defined as micturitions with USS rating 1-5 that occurred between time participant went to bed and time he or she arose to start the next day. USS rating: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. Change = observation minus baseline, where lower scores were an improvement/decrease in nocturnal micturitions. (NCT00798434)
Timeframe: Baseline and Weeks 4, 8, and 12
| Intervention | Percent change (Median) | ||
|---|---|---|---|
| Change at Week 4 (n=366, 356) | Change at Week 8 (n=349, 331) | Change at Week 12 (n=359, 338) | |
| Fesoterodine | -0.3 | -0.7 | -0.7 |
| Placebo | -0.3 | -0.3 | -0.3 |
Severe micturition-related urgency episodes defined as those with USS rating >=4. USS rating of 4: Severe feeling of urgency and 5: Unable to hold; leak urine. Change = observation minus baseline, where lower scores were an improvement/decrease in severity of micturition-related urgency. (NCT00798434)
Timeframe: Baseline and Weeks 4, 8, and 12
| Intervention | Percent change (Median) | ||
|---|---|---|---|
| Change at Week 4 (n=365, 356) | Change at Week 8 (n=349, 331) | Change at Week 12 (n=356, 338) | |
| Fesoterodine | -1.3 | -1.7 | -2.0 |
| Placebo | -0.7 | -1.0 | -1.3 |
Percentage of participants who had at least 1 UUI episode during baseline period and were dry (no UUI episodes) in the 3 days prior to study visits at week 8 and 12. UUI episodes defined as those with USS rating of 5 (unable to hold; leak urine) in the diary. (NCT00798434)
Timeframe: Weeks 8 to 12
| Intervention | Percentage of participants (Number) |
|---|---|
| Placebo | 45.0 |
| Fesoterodine | 53.2 |
UUI episodes defined as those with the USS rating of 5 (unable to hold; leak urine)in the diary. Change = observation minus baseline, where lower scores were an improvement/decrease in UUI episodes. (NCT00798434)
Timeframe: Baseline and Weeks 4, 8, and 12
| Intervention | Percent change (Median) | ||
|---|---|---|---|
| Change at Week 4 (n=365, 356) | Change at Week 8 (n=349, 331) | Change at Week 12 (n=356, 338) | |
| Fesoterodine | 0.0 | 0.0 | 0.0 |
| Placebo | 0.0 | 0.0 | 0.0 |
Micturitions include episodes of voluntary micturition and episodes of UUI. UUI episodes defined as those micturitions with USS rating of 5 (unable to hold; leak urine) in the diary in participants with UUI at baseline. Change = observation minus baseline, where lower scores were an improvement/decrease in micturitions. (NCT00798434)
Timeframe: Baseline and Week 24
| Intervention | Micturitions per 24 hours (Mean) |
|---|---|
| Placebo/Fesoterodine | -2.28 |
| Fesoterodine/Fesoterodine | -2.36 |
Severe micturition-related urgency episodes defined as those with the USS rating >=4. USS rating of 4: Severe feeling of urgency and 5: Unable to hold; leak urine. Change = observation minus baseline, where lower scores were an improvement/decrease in micturition-related urgency episodes. (NCT00798434)
Timeframe: Baseline and Week 24
| Intervention | Episodes per 24 hours (Mean) |
|---|---|
| Placebo/Fesoterodine | -2.57 |
| Fesoterodine/Fesoterodine | -2.41 |
UUI episodes defined as those with USS rating of 5 (unable to hold; leak urine) in the diary. Change = observation minus baseline, where lower scores were an improvement/decrease in UUI episodes. (NCT00798434)
Timeframe: Baseline and Week 24
| Intervention | Episodes per 24 hours (Median) |
|---|---|
| Placebo/Fesoterodine | 0.0 |
| Fesoterodine/Fesoterodine | 0.0 |
Number of micturition-related urgency episodes per 24 hours calculated as number of micturitions with USS rating of >=3 divided by number of days that diary data was collected at that visit. USS rating of 3: Moderate feeling of urgency, 4: Severe feeling of urgency, 5: Unable to hold; leak urine). Change = observation minus baseline, where lower scores were an improvement/decrease in micturition-related urgency episodes. (NCT00798434)
Timeframe: Baseline and Week 24
| Intervention | Episodes per 24 hours (Mean) |
|---|---|
| Placebo/Fesoterodine | -4.24 |
| Fesoterodine/Fesoterodine | -4.07 |
Nocturnal micturitions were defined as micturitions with USS rating 1-5 that occurred between the time the participant went to bed and the time he or she arose to start the next day. USS rating: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. Calculated as number of nocturnal micturitions divided by number of diary days collected at that visit. Change = observation minus baseline, where lower scores were an improvement/decrease in nocturnal micturitions. (NCT00798434)
Timeframe: Baseline and Week 24
| Intervention | Micturitions per 24 hours (Mean) |
|---|---|
| Placebo/Fesoterodine | -0.60 |
| Fesoterodine/Fesoterodine | -0.67 |
"Patient Treatment Benefit Scale (PTBS): single-item scale assessed fesoterodine efficacy and safety in participants with overactive bladder. Participants asked to compare their present condition with their condition before start of trial: My condition has been: 1=Greatly Improved; 2=Improved; 3=Not Changed; 4=Worsened, During Treatment. Improvement was defined as a rating of 1 or 2." (NCT00798434)
Timeframe: Week 12
| Intervention | Percentage of participants (Number) |
|---|---|
| Placebo | 42.9 |
| Fesoterodine | 67.7 |
USS total range 1 to 5 (1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine). Change = observation minus baseline, where lower scores were an improvement/decrease in urinary sensation. (NCT00798434)
Timeframe: Baseline and Weeks 4, 8, and 12
| Intervention | Scores on a scale (Mean) | |||
|---|---|---|---|---|
| Baseline (n=381, 374) | Change at Week 4 (n=365, 356) | Change at Week 8 (n=349, 331) | Change at Week 12 (n=356, 338) | |
| Fesoterodine | 36.07 | -8.52 | -10.81 | -11.59 |
| Placebo | 37.55 | -4.35 | -6.53 | -7.33 |
EQ-5D: participant rated questionnaire to assess HRQL in terms of single index value. Visual Analogue Scale (VAS) component rated current health state on scale from 0 (worst imaginable health state) to 100 (best imaginable health state). For each question, scores categorized into 3 levels of response, level 1=no health problems, 2=some problems and 3= extreme problems, and health state profile utility score derived from these, which could range from 1 prefect health to -0.594 worst possible health. Change = observation minus baseline, where higher scores indicated a better health state. (NCT00798434)
Timeframe: Baseline and Week 12
| Intervention | Scores on a scale (Mean) | |
|---|---|---|
| Baseline (n=381, 373) | Change at Week 12 (n=362, 346) | |
| Fesoterodine | 0.8092 | 0.0064 |
| Placebo | 0.7825 | 0.0230 |
KHQ: self-administered questionnaire contained 21 questions scored in 9 domains (general health perception, incontinence impact, role limitations, physical limitations, social limitations, personal relationships, emotions, sleep/energy, severity of urinary symptoms). Range: 0-100, where 0=best outcome/response and 100=worst outcome/response. Change = observation minus baseline, where lower scores indicated better outcome/response. (NCT00798434)
Timeframe: Baseline and Week 12
| Intervention | Scores on a scale (Mean) | |||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline General Health Perception (n=23, 32) | Change at Week 12 General Hlth Perception n=21, 29 | Baseline Incontinence Impact (n=23, 32) | Change at Week 12 Incontinence Impact (n=21, 29) | Baseline Role Limitations (n=22, 32) | Change at Week 12 Role Limitations (n=20, 29) | Baseline Physical Limitations (n=22, 32) | Change at Week 12 Physical Limitations (n=20, 29) | Baseline Social Limitations (n=22, 32) | Change at Week 12 Social Limitations (n=20, 29) | Baseline Personal Relationships (n=16,17) | Change at Week 12 Personal Relationship (n=11, 14) | Baseline Emotions (n=22, 32) | Change at Week 12 Emotions (n=20, 29) | Baseline Sleep/Energy (n=22, 32) | Change at Week 12 Sleep/Energy (n=20, 29) | Baseline Severity USS (n=22, 32) | Change at Week 12 Severity USS (n=20, 29) | |
| Fesoterodine | 25.00 | 2.59 | 73.96 | -16.09 | 46.35 | -12.64 | 44.79 | -13.79 | 29.86 | -8.62 | 19.61 | -5.95 | 32.64 | -6.51 | 57.29 | -11.49 | 44.38 | -8.51 |
| Placebo | 35.87 | -2.38 | 75.36 | -12.70 | 48.48 | -10.83 | 50.76 | -13.33 | 24.75 | -7.50 | 15.63 | 4.55 | 32.32 | -2.78 | 46.97 | -8.33 | 43.94 | -2.00 |
Micturitions included episodes of voluntary micturition and episodes of UUI, defined as those micturitions with USS rating of 5 (unable to hold; leak urine) in the diary of participants with UUI at baseline. Change = observation minus baseline, where lower scores were an improvement/decrease in micturitions. (NCT00798434)
Timeframe: Baseline and Weeks 4, 8, and 12
| Intervention | Micturitions per 24 hours (Mean) | |||
|---|---|---|---|---|
| Baseline (n=382, 374) | Change at Week 4 (n=366, 356) | Change at Week 8 (n=349, 331) | Change at Week 12 (n=359, 338) | |
| Fesoterodine | 11.89 | -1.47 | -1.95 | -2.09 |
| Placebo | 12.10 | -0.69 | -1.11 | -1.15 |
Severe micturition-related urgency episodes defined as those with the USS rating >=4. USS rating of 4: Severe feeling of urgency and 5: Unable to hold; leak urine. Change = observation minus baseline, where lower scores were an improvement/decrease in severity of micturition-related urgency episodes. (NCT00798434)
Timeframe: Baseline and Weeks 4, 8, and 12
| Intervention | Episodes per 24 hours (Mean) | |||
|---|---|---|---|---|
| Baseline (n=381, 374) | Change at Week 4 (n=365, 356) | Change at Week 8 (n=349, 331) | Change at Week 12 (n=356, 338) | |
| Fesoterodine | 3.53 | -1.81 | -2.12 | -2.43 |
| Placebo | 4.11 | -0.96 | -1.53 | -1.78 |
MMSE measured general cognitive functioning: orientation, memory, attention, calculation, language, visuospatial functions. Total score derived from sub-scores; total ranged from 0 - 30, higher score indicated better cognitive state. Change = observation minus baseline where higher scores indicated better cognitive functioning. (NCT00798434)
Timeframe: Baseline and Week 12
| Intervention | Scores on a scale (Mean) | |
|---|---|---|
| Baseline | Change at Week 12 | |
| Fesoterodine | 28.20 | 0.24 |
| Placebo | 28.09 | 0.23 |
Number of micturition-related urgency episodes per 24 hours calculated as number of micturitions with USS rating of greater than or equal to (>=) 3 divided by number of days that diary data was collected at that visit. USS ranged 1 to 5 (1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine). Change = observation minus baseline, where lower scores were an improvement/decrease in micturition-related urgency episodes. (NCT00798434)
Timeframe: Baseline and Week 12
| Intervention | Episodes per 24 hours (Mean) | |
|---|---|---|
| Baseline (n=381, 374) | Change at Week 12 (n=356, 338) | |
| Fesoterodine | 8.48 | -3.84 |
| Placebo | 8.80 | -2.48 |
Nocturnal micturitions defined as micturitions with USS rating 1-5 that occurred between time participant went to bed and time he or she arose to start the next day. USS rating: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. Calculated as number of nocturnal micturitions divided by number of diary days collected at that visit. Change = observation minus baseline, where lower scores were an improvement/decrease in nocturnal micturitions. (NCT00798434)
Timeframe: Baseline and Weeks 4, 8, and 12
| Intervention | Micturitions per 24 hours (Mean) | |||
|---|---|---|---|---|
| Baseline (n=382, 374) | Change at Week 4 (n=366, 356) | Change at Week 8 (n=349, 331) | Change at Week 12 (n=359, 338) | |
| Fesoterodine | 2.80 | -0.38 | -0.51 | -0.55 |
| Placebo | 2.92 | -0.22 | -0.30 | -0.33 |
Skin protective agents included incontinence pads, barrier creams, and powders. Change = observation minus baseline, where lower scores were an improvement/decrease in protective skin agents used. (NCT00798434)
Timeframe: Baseline and Weeks 4, 8, and 12
| Intervention | Skin protective agents (Mean) | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Incontinence pads at Baseline (n=374, 369) | Incontinence pads Change at Week 4 (n=360, 350) | Incontinence pads Change at Week 8 (n=342, 326) | Incontinence pads Change at Week 12 (n=350, 332) | Creams at Baseline (n=374, 368) | Creams Change at Week 4 (n=360, 349) | Creams Change at Week 8 (n=342, 325) | Creams Change at Week 12 (n=350, 331) | Powder at Baseline (n=374, 368) | Powder Change at Week 4 (n=360, 349) | Powder Change at Week 8 (n=342, 325) | Powder Change at Week 12 (n=350, 331) | |
| Fesoterodine | 1.35 | -0.27 | -0.38 | -0.50 | 0.16 | -0.02 | -0.03 | -0.03 | 0.02 | -0.02 | -0.01 | -0.02 |
| Placebo | 1.49 | -0.20 | -0.15 | -0.16 | 0.12 | -0.01 | 0.06 | 0.04 | 0.03 | 0.03 | 0.03 | 0.03 |
UUI episodes defined as those with USS rating of 5 (unable to hold; leak urine) in the diary. Change = observation minus baseline, where lower scores were an improvement/decrease in UUI episodes. (NCT00798434)
Timeframe: Baseline and Weeks 4, 8, and 12
| Intervention | Episodes per 24 hours (Median) | |||
|---|---|---|---|---|
| Baseline (n=381, 374) | Change at Week 4 (n=365, 356) | Change at Week 8 (n=349, 331) | Change at Week 12 (n=356, 338) | |
| Fesoterodine | 0.0 | 0.0 | 0.0 | 0.0 |
| Placebo | 0.0 | 0.0 | 0.0 | 0.0 |
OAB-q: self-administered, 33-item, questionnaire assessed how much participant bothered by bladder symptoms during previous week. Each item rated by participant on Likert scale 1 (least symptom bother) to 6 (most symptom bother). Raw scores transformed to 0-100 score where higher scores were less favorable outcome. Questions 1-8 constituted symptom severity/bother score. Questions 9-33 constitute HRQL component, which included domains of coping, concern, sleep, and social function. Change = observation minus baseline and higher scores were an improvement. (NCT00798434)
Timeframe: Baseline and Weeks 4, 8, 12, and 24
| Intervention | Scores on a scale (Mean) | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Coping at Baseline (n=380, 374) | Coping Change at Week 4 (n=368, 358) | Coping Change at Week 8 (n=348, 329) | Coping Change at Week 12 (n=365, 358) | Coping Change at Week 24 | Concern at Baseline (n=380, 374) | Concern Change at Week 4 (n=368, 358) | Concern Change at Week 8 (n=348, 329) | Concern Change at Week 12 (n=365, 358) | Concern Change at Week 24 | Sleep at Baseline (n=380, 374) | Sleep Change at Week 4 (n=368, 358) | Sleep Change at Week 8 (n=348, 329) | Sleep Change at Week 12 (n=365, 358) | Sleep Change at Week 24 | Social at Baseline (n=380, 374) | Social Change at Week 4 (n=368, 355) | Social Change at Week 8 (n=349, 328) | Social Change at Week 12 (n=364, 357) | Social Change at Week 24 | |
| Fesoterodine/Fesoterodine | 58.31 | 11.90 | 14.98 | 15.65 | NA | 64.67 | 11.88 | 15.39 | 15.48 | NA | 57.52 | 9.07 | 10.87 | 11.99 | NA | 81.02 | 6.25 | 8.17 | 7.02 | NA |
| Placebo/Fesoterodine | 57.52 | 8.35 | 10.46 | 10.60 | NA | 62.10 | 7.96 | 10.88 | 11.25 | NA | 53.79 | 7.31 | 9.01 | 9.36 | NA | 79.10 | 4.41 | 5.84 | 5.29 | NA |
OAB-q: self-administered, 33-item, questionnaire assessed how much participant was bothered by selected bladder symptoms during previous week. Each item rated by participant on Likert scale 1 (least symptom bother) to 6 (most symptom bother). Raw scores transformed to a score from 0-100 where higher scores represented less favorable outcome. Change = baseline minus observation and higher scores were an improvement. (NCT00798434)
Timeframe: Baseline and Weeks 4, 8, 12, and 24
| Intervention | Scores on a scale (Mean) | ||||
|---|---|---|---|---|---|
| Baseline (n=381, 373) | Change at Week 4 (n=369, 358) | Change at Week 8 (n=349, 328) | Change at Week 12 (n=366, 357) | Change at Week 24 | |
| Fesoterodine/Fesoterodine | 50.58 | -14.05 | -18.03 | -18.37 | NA |
| Placebo/Fesoterodine | 52.90 | -9.03 | -12.86 | -12.16 | NA |
OAB-q: self-administered, 33-item, questionnaire assessed how much participant was bothered by selected bladder symptoms during previous week. Each item rated by participant on Likert scale 1 (least symptom bother) to 6 (most symptom bother). Raw scores transformed to a score from 0-100 where higher scores represented less favorable outcome. Change = observation minus baseline and higher scores were an improvement. (NCT00798434)
Timeframe: Baseline and Weeks 4, 8, 12, and 24
| Intervention | Scores on a scale (Mean) | ||||
|---|---|---|---|---|---|
| Baseline (n=373, 379) | Change at Week 4 (n=367, 354) | Change at Week 8 (n=348, 328) | Change at Week 12 (n=363, 357) | Change at Week 24 | |
| Fesoterodine/Fesoterodine | 64.42 | 10.24 | 12.96 | 13.19 | NA |
| Placebo/Fesoterodine | 62.45 | 7.28 | 9.36 | 9.56 | NA |
PPBC: self-administered, single-item, questionnaire that asked participants to describe their perception of their bladder-related problems. PPBC assessment rated on a 6-point scale: 1=no problems at all, 2=some very minor problems, 3=some minor problems, 4=moderate problems, 5=severe problems, 6=many severe problems. Change = observation minus baseline. Results categorized as Deterioration (score difference ≥1), No Change (score difference=0), Improvement (score difference less than [<]0). (NCT00798434)
Timeframe: Baseline and Week 4
| Intervention | Participants (Number) | ||
|---|---|---|---|
| Improvement | No Change | Deterioration | |
| Fesoterodine | 192 | 168 | 16 |
| Placebo | 168 | 202 | 40 |
PPBC: self-administered, single-item, questionnaire that asked participants to describe their perception of their bladder-related problems. PPBC assessment rated on a 6-point scale: 1=no problems at all, 2=some very minor problems, 3=some minor problems, 4=moderate problems, 5=severe problems, 6=many severe problems. Change = observation minus baseline. Results categorized as Deterioration (score difference ≥1), No Change (score difference=0), Improvement (score difference <0). (NCT00798434)
Timeframe: Baseline and Week 12
| Intervention | Participants (Number) | ||
|---|---|---|---|
| Improvement | No Change | Deterioration | |
| Fesoterodine | 256 | 104 | 17 |
| Placebo | 204 | 164 | 33 |
PPBC: self-administered, single-item, questionnaire that asked participants to describe their perception of their bladder-related problems. PPBC assessment rated on a 6-point scale: 1=no problems at all, 2=some very minor problems, 3=some minor problems, 4=moderate problems, 5=severe problems, 6=many severe problems. Change = observation minus baseline. Results categorized as Deterioration (score difference ≥1), No Change (score difference=0), Improvement (score difference <0). (NCT00798434)
Timeframe: Baseline and Week 8
| Intervention | Participants (Number) | ||
|---|---|---|---|
| Improvement | No Change | Deterioration | |
| Fesoterodine | 210 | 119 | 13 |
| Placebo | 185 | 166 | 22 |
PPUS: self-administered, single-item, questionnaire that measured the participant's perception of urinary urgency. It was sensitive to changes in perceptions of urinary urgency over time. Scale of 0 (usually not able to hold urine), 1 (usually able to hold urine [without leaking] until reaching toilet if go to toilet immediately), or 2 (usually able to finish what he/she was doing before going to toilet [without leaking]). Change = observation minus baseline. Improvement in PPUS defined as increase of 1 or more points in difference of scores relative to baseline. (NCT00798434)
Timeframe: Baseline and Week 12
| Intervention | Participants (Number) | ||
|---|---|---|---|
| Improvement | No Change | Deterioration | |
| Fesoterodine | 133 | 200 | 28 |
| Placebo | 109 | 226 | 32 |
PPUS: self-administered, single-item, questionnaire that measured the participant's perception of urinary urgency. It was sensitive to changes in perceptions of urinary urgency over time. Scale of 0 (usually not able to hold urine), 1 (usually able to hold urine [without leaking] until reaching toilet if go to toilet immediately), or 2 (usually able to finish what he/she was doing before going to toilet [without leaking]). Change = observation minus baseline. Improvement in PPUS defined as increase of 1 or more points in difference of scores relative to baseline. (NCT00798434)
Timeframe: Baseline and Week 8
| Intervention | Participants (Number) | ||
|---|---|---|---|
| Improvement | No Change | Deterioration | |
| Fesoterodine | 111 | 194 | 25 |
| Placebo | 95 | 224 | 32 |
PPUS: self-administered, single-item, questionnaire that measured the participant's perception of urinary urgency. It was sensitive to changes in perceptions of urinary urgency over time. Scale of 0 (usually not able to hold urine), 1 (usually able to hold urine [without leaking] until reaching toilet if go to toilet immediately), or 2 (usually able to finish what he/she was doing before going to toilet [without leaking]). Change = observation minus baseline. Improvement in PPUS defined as increase of 1 or more points in difference of scores relative to baseline. (NCT00798434)
Timeframe: Baseline and Weeks 4
| Intervention | Participants (Number) | ||
|---|---|---|---|
| Improvement | No Change | Deterioration | |
| Fesoterodine | 90 | 250 | 21 |
| Placebo | 74 | 263 | 33 |
OAB-S: evaluated OAB medication expectations, daily life with OAB, and satisfaction with OAB medication. Included 3 stand-alone items that assessed overall expectation, satisfaction, and willingness to continue treatment. Medication expectation coded on scale 1=Greatly exceeds my expectations to 5=Does not meet my expectations at all. Coding reversed by subtracting initial response value from 6, so higher final response value associated with better fulfilment of OAB medication expectations. (NCT00798434)
Timeframe: Weeks 12 and 24
| Intervention | Scores on a scale (Mean) | |
|---|---|---|
| Week 12 | Change at Week 24 | |
| Fesoterodine/Fesoterodine | 2.85 | 0.17 |
| Placebo/Fesoterodine | 2.21 | 0.74 |
OAB-S: validated self-administered instrument that evaluated OAB medication expectations, daily life with OAB, and satisfaction with OAB medication and included 3 stand-alone items that assessed overall expectation, satisfaction, and willingness to continue treatment. Satisfaction coded on scale of 1-5: (1-very satisfied to 5-very dissatisfied). Coding reversed algorithmically and results transformed: total score range 0-100. Higher final response value associated with better satisfaction. Change = score at Week 24 minus score at Week 12 where higher scores indicated better satisfaction. (NCT00798434)
Timeframe: Weeks 12 and 24
| Intervention | Scores on a scale (Mean) | |
|---|---|---|
| Week 12 | Change at Week 24 | |
| Fesoterodine/Fesoterodine | 63.01 | 3.58 |
| Placebo/Fesoterodine | 44.97 | 21.22 |
Micturition-related urgency episodes per 24 hours defined as those with USS Scale rating of >=3 marked for corresponding micturition in diary. USS rating of 3: Moderate feeling of urgency, 4: Severe feeling of urgency, 5: Unable to hold; leak urine. Percent change calculated as: 100* (Urgency Episode at Week x - baseline)/baseline. Change = observation minus baseline, where lower scores were an improvement/decrease in micturition-related urgency episodes. (NCT00798434)
Timeframe: Baseline and Weeks 4, 8, and 12
| Intervention | Percent change (Median) | ||
|---|---|---|---|
| Change at Week 4 (n=365, 356) | Change at Week 8 (n=349, 331) | Change at Week 12 (n=356, 338) | |
| Fesoterodine | 5.3 | 4.3 | 3.7 |
| Placebo | 6.7 | 5.7 | 5.3 |
Micturitions included episodes of voluntary micturition and episodes of UUI. Change = observation minus baseline, where lower scores were an improvement/decrease in micturitions. (NCT00798434)
Timeframe: Baseline and Weeks 4, 8, and 12
| Intervention | Percent change (Median) | ||
|---|---|---|---|
| Change at Week 4 (n=366, 356) | Change at Week 8 (n=349, 331) | Change at Week 12 (n=359, 338) | |
| Fesoterodine | -1.3 | -1.7 | -2.0 |
| Placebo | -0.7 | -1.0 | -1.3 |
KHQ: Self-administered questionnaire containing 21 questions scored in 9 domains (general health perception, incontinence impact, role limitations, physical limitations, social limitations, personal relationships, emotions, sleep/energy, severity of urinary symptoms). Each domain was a categorical scale that was converted to a numeric score. All domains transformed to a range of 0 to 100, where 0=best outcome/response and 100=worst outcome/response. Change=mean score at Week 12 minus mean score at baseline, negative change from baseline=improvement. (NCT00806494)
Timeframe: Baseline, Week 12
| Intervention | Score on Scale (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| General Health Perception (n=311) | Incontinence Impact (n=309) | Role Limitations (n=311) | Physical Limitations (n=311) | Social Limitations (n=310) | Personal Relationships (n=220) | Emotions (n=308) | Sleep/Energy (n=311) | Severity of Urinary Symptoms (n=311) | |
| Fesoterodine | -2.57 | -29.69 | -41.16 | -36.60 | -25.22 | -15.23 | -25.78 | -21.38 | -21.92 |
The mean number of incontinence pads used per 24 hours was calculated as the total number of incontinence pads used divided by the total number of diary days collected at that visit. Change=mean at observation minus mean at baseline. Negative change, ie, decrease in number of incontinence pads used relative to baseline=improvement. (NCT00806494)
Timeframe: Baseline, Week 4 and Week 12
| Intervention | Number of Incontinence Pads (Mean) | |
|---|---|---|
| Week 4 (n=304) | Week 12 (n=316) | |
| Fesoterodine | -0.49 | -0.64 |
Nocturnal micturitions were defined as those occurring between the time the subject went to bed and the time he or she arose to start the next day. The mean number of nocturnal micturitions per 24 hours was calculated as the total number of nocturnal micturitions divided by the total number of diary days collected at that visit. Change=mean at observation minus mean at baseline. Negative change, ie, decrease in number of nocturnal micturitions relative to baseline=improvement. (NCT00806494)
Timeframe: Baseline, Week 4 and Week 12
| Intervention | Number of episodes (Mean) | |
|---|---|---|
| Week 4 (n=297) | Week 12 (n=309) | |
| Fesoterodine | -0.61 | -0.78 |
"NUEs were defined as those with a USS rating of >=3 in the diary, occurring between the time the participant goes to bed and the time he/she arises to start the next day. USS: 5-item scale to measure urinary urgency; range: 1 (no feeling of urgency) to 5 (unable to hold; leak urine).~Mean number of NUEs per 24 hours was calculated as total number of NUEs divided by total number of diary days collected at that visit. Change=mean at observation minus mean at baseline. Negative change, ie, decrease in number of NUEs relative to baseline=improvement." (NCT00806494)
Timeframe: Baseline, Week 4 and Week 12
| Intervention | Number of Episodes (Mean) | |
|---|---|---|
| Week 4 (n=284) | Week 12 (n=297) | |
| Fesoterodine | -0.95 | -1.16 |
OAB-q symptom bother scale (8 items) is part of the OAB-q. Symptom bother score=sum of scores for items 1 to 8 (each symptom bother item measured on 6-point Likert scale ranging from 1 (not at all) to 6 (a very great deal). Lowest possible raw score=8; highest possible score=48. Data analyzed based on transformation of score to a 0 to 100 scale: (Actual total raw score - lowest possible value of raw score)/raw score range * 100. 0=no symptom bother, 100=high symptom bother. Change=mean score at observation minus mean score at baseline, negative change in score=improvement. (NCT00806494)
Timeframe: Baseline, Week 4 and Week 12
| Intervention | Score on Scale (Mean) | |
|---|---|---|
| Week 4 (n=300) | Week 12 (n=319) | |
| Fesoteridine | -27.95 | -37.25 |
PPBC: self-administered, single-item, questionnaire to describe perception of participants bladder-related problems (rated on 6-point scale: 1=no problems at all, 2=some very minor, 3=some minor, 4=some moderate, 5=severe, 6=many severe problems). Score change=score at observation minus score at baseline; re-scaled to 4-point categorical variables (major improvement [score difference <=-2]; minor improvement [score difference =-1]; no change [score difference = 0]; deterioration [score difference >=1]), based on PPBC score. (NCT00806494)
Timeframe: Baseline, Week 4 and Week 12
| Intervention | Participants (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| Major Improvement (Week 4), n=307 | Minor Improvement (Week 4), n=307 | No Change (Week 4), n=307 | Deterioration (Week 4), n=307 | Major Improvement (Week 12), n=322 | Minor Improvement (Week 12), n=322 | No Change (Week 12), n=322 | Deterioration (Week 12), n=322 | |
| Fesoterodine | 86 | 121 | 93 | 7 | 160 | 94 | 64 | 4 |
UPS: self-administered, single-item questionnaire to measure participant's perception of urinary urgency (rated on 3-point scale: 1=usually not able to hold urine; 3=usually able to finish what I am doing before going to toilet without leaking). Score change=score at observation minus score at baseline; re-scaled to 3-point categorical variables (improvement [Increase of 1 or more points in difference of scores]; no change [score difference=0]; deterioration [Negative difference of scores], based on UPS score, with number of participants in each of the 3-point categories. (NCT00806494)
Timeframe: Baseline, Week 4 and Week 12
| Intervention | Participants (Number) | |||||
|---|---|---|---|---|---|---|
| Improvement (Week 4), n=307 | No Change (Week 4), n=307 | Deterioration (Week 4), n=307 | Improvement (Week 12), n=321 | No Change (Week 12), n=321 | Deterioration (Week 12), n=321 | |
| Fesoterodine | 105 | 189 | 13 | 154 | 159 | 8 |
BSW: 3-item questionnaire to assess participants perception of effect of treatment in terms of treatment benefit, satisfaction with treatment, and participants willingness to continue treatment. Response to each item recorded in dichotomous fashion (Benefit: yes/no, yes - little benefit/much benefit; Satisfaction: yes/no, yes - a little satisfied/very satisfied, no - a little dissatisfied/very dissatisfied; Willingness to continue: yes/no, yes - a little bit willing/very willing, no - a little unwilling/very unwilling). (NCT00806494)
Timeframe: Week 12 (or Early Withdrawal)
| Intervention | Participants (Number) | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Benefit from Treatment - Much Benefit | Benefit from Treatment - Little Benefit | Benefit from Treatment - No | Satisfied with Treatment - Yes | Satisfied with Treatment - No | Satisfied with Treatment - Yes (Very Satisfied) | Satisfied with Treatment - Yes (Little Satisfied) | Satisfied with Treatment - No(Little Dissatisfied) | Satisfied with Treatment - No (Very Dissatisfied) | Willingness to Continue - Yes | Willingness to Continue - No | Willingness to Continue - Yes (Very Willing) | Willingness to Continue - Yes (Little Bit Willing) | Willingness to Continue - No (Little Unwilling) | Willingness to Continue - No (Very Unwilling) | |
| Fesoterodine | 188 | 82 | 36 | 253 | 54 | 184 | 69 | 30 | 24 | 248 | 61 | 203 | 45 | 23 | 36 |
Percentage change from baseline in nocturnal micturitions was calculated as change in mean number of nocturnal micturitions per 24 hours at that visit divided by the baseline mean number of nocturnal micturitions per 24 hours, multiplied by 100. (NCT00806494)
Timeframe: Baseline, Week 4 and Week 12
| Intervention | Percentage Change (Mean) | |
|---|---|---|
| Week 4 (n=297) | Week 12 (n=309) | |
| Fesoterodine | -15.18 | -23.35 |
Percentage change from baseline in NUEs was calculated as change in mean number of NUEs per 24 hours at that visit divided by the baseline mean number of NUEs per 24 hours, multiplied by 100. (NCT00806494)
Timeframe: Baseline, Week 4 and Week 12
| Intervention | Percentage Change (Mean) | |
|---|---|---|
| Week 4 (n=284) | Week 12 (n=297) | |
| Fesoterodine | -38.71 | -44.78 |
The number of micturitions was measured by the 3-day bladder diary completed for the 3 consecutive days preceding each clinic visit. The mean number of micturitions per 24 hours was calculated as the sum of all micturitions recorded in the diary divided by the number of days the diary was completed at that visit. Change=mean at observation minus mean at baseline. Negative change, ie, decrease in number of micturitions relative to baseline=improvement. (NCT00806494)
Timeframe: Baseline, Week 4
| Intervention | Number of Episodes (Mean) |
|---|---|
| Fesoterodine | -2.55 |
Percentage change from baseline in SUEs was calculated as the change in mean number of SUEs per 24 hours at that visit divided by the baseline mean number of SUEs per 24 hours, multiplied by 100. (NCT00806494)
Timeframe: Baseline, Week 4 and Week 12
| Intervention | Percentage Change (Mean) | |
|---|---|---|
| Week 4 (n=268) | Week 12 (n=278) | |
| Fesoterodine | -57.37 | -69.14 |
The number of micturitions was measured by the 3-day bladder diary completed for the 3 consecutive days preceding each clinic visit. The mean number of micturitions per 24 hours was calculated as the sum of all micturitions recorded in the diary divided by the number of days the diary was completed at that visit. Change=mean at observation minus mean at baseline. Negative change, more specifically (ie), a decrease in number of micturitions relative to baseline=improvement. (NCT00806494)
Timeframe: Baseline, Week 12
| Intervention | Number of Episodes (Mean) |
|---|---|
| Fesoterodine | -3.26 |
Percentage change from baseline in UUI episodes was calculated as change in mean number of UUI episodes per 24 hours at that visit divided by the baseline mean number of episodes per 24 hours, multiplied by 100. (NCT00806494)
Timeframe: Baseline, Week 4 and Week 12
| Intervention | Percentage Change (Mean) | |
|---|---|---|
| Week 4 (n=125) | Week 12 (n=127) | |
| Fesoterodine | -59.11 | -79.30 |
Percentage change from baseline in urgency episodes was calculated as change in mean number of urgency episodes per 24 hours at that visit divided by the baseline mean number of urgency episodes per 24 hours, multiplied by 100. (NCT00806494)
Timeframe: Baseline, Week 4 and Week 12
| Intervention | Percentage Change (Mean) | |
|---|---|---|
| Week 4 (n=303) | Week 12 (n=317) | |
| Fesoterodine | -40.69 | -51.75 |
"UUI episodes were defined as those with a Urinary Sensation Scale (USS) rating of 5 in the diary. USS: 5-item scale to measure urinary urgency; range: 1 (no feeling of urgency) to 5 (unable to hold; leak urine).~Mean number of UUI episodes per 24 hours was calculated as total number of micturitions with USS rating of 5 divided by total number of diary days collected at that visit. Change=mean at observation minus mean at baseline. Negative change, ie, decrease in number of UUI episodes relative to baseline=improvement." (NCT00806494)
Timeframe: Baseline, Week 4 and Week 12
| Intervention | Number of Episodes (Mean) | |
|---|---|---|
| Week 4 (n=125) | Week 12 (n=127) | |
| Fesoterodine | -1.19 | -1.64 |
Urgency episodes were defined as those with a USS rating of >=3 in the diary. USS: 5-item scale to measure urinary urgency; range: 1 (no feeling of urgency) to 5 (unable to hold; leak urine). Mean number of urgency episodes per 24 hours was calculated as total number of urgency episodes divided by total number of diary days collected at that visit. Change=mean at observation minus mean at baseline. Negative change, ie, decrease in number of urgency episodes relative to baseline=improvement. (NCT00806494)
Timeframe: Baseline, Week 4 and Week 12
| Intervention | Number of Episodes (Mean) | |
|---|---|---|
| Week 4 (n=303) | Week 12 (n=317) | |
| Fesoterodine | -3.94 | -5.10 |
SUEs were defined as those with a USS rating of >=4 in the diary. USS: 5-item scale to measure urinary urgency; range: 1 (no feeling of urgency) to 5 (unable to hold; leak urine). Mean number of SUEs per 24 hours was calculated as total number of SUEs divided by total number of diary days collected at that visit. Change=mean at observation minus mean at baseline. Negative change, ie, decrease in number of SUEs relative to baseline=improvement. (NCT00806494)
Timeframe: Baseline, Week 4 and Week 12
| Intervention | Number of Episodes (Mean) | |
|---|---|---|
| Week 4 (n=268) | Week 12 (n=278) | |
| Fesoterodine | -2.31 | -2.93 |
TSQ: Independent component of the overactive bladder TSQ. Self- administered, 1-item measure of participant satisfaction for participants receiving treatment for OAB. The 5 categorical responses were grouped to 'Satisfied' (including 'very satisfied' and 'somewhat satisfied') and 'Dissatisfied' (including 'very dissatisfied','somewhat dissatisfied', and 'neither dissatisfied nor satisfied'). Percentage of participants reporting satisfaction included those with categorical responses of 'very satisfied' and 'somewhat satisfied'. (NCT00806494)
Timeframe: Week 12 (or Early Withdrawal)
| Intervention | Percentage of Participants (Number) |
|---|---|
| Fesoterodine | 73.6 |
Percentage change from baseline in micturitions was calculated as change in mean number of micturitions per 24 hours at that visit divided by the baseline mean number of micturitions per 24 hours, multiplied by 100. (NCT00806494)
Timeframe: Baseline, Week 4 and Week 12
| Intervention | Percentage Change (Mean) | |
|---|---|---|
| Week 4 (n=305) | Week 12 (n=317) | |
| Fesoterodine | -18.69 | -23.61 |
ICIQ-SF: self-administered questionnaire for assessment and quantification of incontinence and its impact on quality of life. ICIQ score=sum of the responses to 3 questions: How often do you leak urine? (range: 0=never to 5=all the time); How much urine do you usually leak? (range: 0=none to 6=a large amount); Overall, how much does leaking urine interfere with your everyday life? (range: 0=not at all to 10=a great deal). Score range=0 (low bother from urine leakage) to 21 (maximum bother). Negative change (decrease) from baseline in score value=reduced level of bother. (NCT00806494)
Timeframe: Baseline, Week 12
| Intervention | Score on Scale (Mean) |
|---|---|
| Fesoterodine | -5.13 |
Ascending colon emptying t½ was estimated by power exponential analysis of the proportionate emptying over time of counts from the colon. (NCT00832650)
Timeframe: Day 12: 2 hours, 4 hours
| Intervention | minutes (Mean) |
|---|---|
| Fesoterodine | 145.00 |
| Placebo | 112.92 |
| Solifenacin | 127.47 |
Estimated by power exponential analysis of the proportionate emptying over time of counts from the colon. (NCT00832650)
Timeframe: Day 12 to 14
| Intervention | hours (Mean) |
|---|---|
| Fesoterodine | 21.06 |
| Placebo | 14.79 |
| Solifenacin | 19.23 |
Calculated by averaging the values of the stool form given at each visit to the toilet on each notional day. Mean of 3 days. Range of possible scores: 1 (hard lumps) to 7 (watery). (NCT00832650)
Timeframe: Day 11 to 13
| Intervention | score on a scale (Mean) |
|---|---|
| Fesoterodine | 3.66 |
| Placebo | 3.29 |
| Solifenacin | 3.02 |
"The number of stools with satisfaction of Yes divided by the total number of stools passed on each notional day. Mean of 3 days." (NCT00832650)
Timeframe: Day 11 to 13
| Intervention | mean proportion (Mean) |
|---|---|
| Fesoterodine | 0.88 |
| Placebo | 0.81 |
| Solifenacin | 0.93 |
Number of stools passed on each notional day where each visit to the toilet counts as one stool (only) unless nothing is passed. Mean of 3 days. (NCT00832650)
Timeframe: Day 11 to 13
| Intervention | stools (Mean) |
|---|---|
| Fesoterodine | 0.93 |
| Placebo | 1.06 |
| Solifenacin | 1.11 |
Colonic transit: Geometric centre at 48 hours (GC48) was estimated using geometric mean of counts in ascending (AC), transverse (TC), descending (DC) and rectosigmoid (RS) colon and stool (weighted by factors of 1 to 5 respectively). To calculate the geometric centre, the proportion of colonic counts in each colonic region was multiplied by its weighing factor: (% AC *1 + % TC *2 + % DC *3 + % RS *4 + % stool * 5 ) divided by 100. (NCT00832650)
Timeframe: Day 14 (Day 12 48 hours post-meal)
| Intervention | counts (Mean) |
|---|---|
| Fesoterodine | 3.55 |
| Placebo | 3.67 |
| Solifenacin | 3.14 |
Colonic transit: Geometric centre at 24 hours (GC24) was estimated using geometric mean of counts in ascending (AC), transverse (TC), descending (DC) and rectosigmoid (RS) colon and stool (weighted by factors of 1 to 5 respectively). To calculate the geometric centre, the proportion of colonic counts in each colonic region was multiplied by its weighing factor: (% AC *1 + % TC *2 + % DC *3 + % RS *4 + % stool * 5 ) divided by 100. (NCT00832650)
Timeframe: Day 13 (Day 12 24 hours post-meal)
| Intervention | counts (Mean) |
|---|---|
| Fesoterodine | 1.98 |
| Placebo | 2.51 |
| Solifenacin | 1.91 |
A surrogate marker of small bowel transit time. (NCT00832650)
Timeframe: Day 12
| Intervention | percentage (Mean) |
|---|---|
| Fesoterodine | 7.84 |
| Placebo | 69.58 |
| Solifenacin | 24.06 |
Calculated by averaging the values given for the ease of passage at each visit to the toilet on each notional day. Mean of 3 days. Range of possible scores: 1 (Manual disimpaction) to 7 (Incontinent). (NCT00832650)
Timeframe: Day 11 to 13
| Intervention | score on a scale (Mean) |
|---|---|
| Fesoterodine | 3.90 |
| Placebo | 3.97 |
| Solifenacin | 3.83 |
Volume of urine remaining in the bladder immediately after urination. (NCT00857896)
Timeframe: Baseline, Week 4, and Week 8 post-dose
| Intervention | mL (Median) | ||
|---|---|---|---|
| Baseline (n=10) | Week 4 (n=12) | Week 8 (n=8) | |
| Fesoterodine | 6.00 | 4.00 | 25.00 |
(NCT00857896)
Timeframe: Day 28 and Day 56
| Intervention | 1/hour (hr) (Mean) |
|---|---|
| Fesoterodine | 0.44 |
Clearance of a drug is a measure of the rate at which a drug is metabolized or eliminated by normal biological processes. Clearance obtained after oral dose (apparent oral clearance) is influenced by the fraction of the dose absorbed. Clearance was estimated using non linear mixed effect modeling. Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the blood. (NCT00857896)
Timeframe: Day 28 and Day 56
| Intervention | L/hr (Mean) |
|---|---|
| Fesoterodine | 86.70 |
The volume necessary to account for the total amount of drug in the body if it were present throughout the body at the same concentration found in the blood. Estimated using non linear mixed effect modeling. (NCT00857896)
Timeframe: Day 28 and Day 56
| Intervention | Liters (L) (Mean) |
|---|---|
| Fesoterodine | 1010.00 |
(NCT00862745)
Timeframe: Baseline and Week 12
| Intervention | episodes (Mean) |
|---|---|
| Fesoterodine | -2.5 |
| Placebo | -1.8 |
"Participants who were assessed as having improved from their baseline condition in the final efficacy assessment were considered as effective. Baseline and treatment characteristics included: geriatric status (<65 years or ≥65 years), age categories, gender, weight categories, height categories, allergic history, duration of disease, past overactive bladder (OAB) treatment history, medical history, kidney and liver disorders, concomitant medication, total administration period of Toviaz, completion status, daily dose of Toviaz, and long term administration of Toviaz (<274 days and ≥274 days) ." (NCT00879398)
Timeframe: At the end of study treatment
| Intervention | Percentage of Participants (Number) | |||||||||||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| All Participants | Geriatric Status: <65 years | Geriatric Status: ≥65 years | Age Category: <50 years | Age Category: 50 to 59 years | Age Category: 60 to 69 years | Age Category: 70 to 79 years | Age Category: ≥80 years | Gender: Male | Gender: Female | Weight Category: <50 kg | Weight Category: 50 to <60 kg | Weight Category: 60 to <70 kg | Weight Category: ≥70 kg | Height Category: <160 cm | Height Category: 160 to 170 cm | Height Category: ≥170 cm | Allergic History: Yes | Allergic History: No | Duration of Disease: <1 week | Duration of Disease: 1 to <8 weeks | Duration of Disease: 8 to <16 weeks | Duration of Disease: ≥16 weeks | Past OAB Treatment History: Yes | Past OAB Treatment History: No | Existence for Medical History of Past Disease: Yes | Existence for Medical History of Past Disease: No | Medical History of Present Disease: Yes | Medical History of Present Disease: No | Kidney Disease: Yes | Kidney Disease: No | Liver Disorder: Yes | Liver Disorder: No | Administration Period of Toviaz: <2 months | Administration Period of Toviaz: 2 to <4 months | Administration Period Of Toviaz: ≥ 4 months | Daily Dose of Toviaz: 3 mg | Daily Dose of Toviaz: 4 mg | Daily Dose of Toviaz: >4 to <8 mg | Daily Dose of Toviaz: 8 mg | Completion | Discontinuation | Total Administration Period <274 days | Total Administration Period ≥274 days | Existence for Concurrent Medication: Yes | Existence for Concurrent Medication: No | |
| Toviaz | 90.13 | 90.86 | 89.20 | 91.27 | 91.08 | 89.29 | 89.45 | 89.27 | 88.98 | 91.36 | 89.73 | 91.64 | 90.32 | 88.82 | 89.99 | 90.32 | 90.35 | 82.22 | 90.25 | 92.40 | 89.42 | 89.05 | 84.33 | 85.30 | 91.79 | 87.96 | 90.47 | 87.96 | 92.46 | 90.00 | 90.13 | 92.31 | 90.12 | 85.22 | 92.44 | 92.33 | 66.67 | 90.65 | 85.25 | 90.25 | 92.28 | 80.72 | 90.16 | 87.50 | 88.48 | 92.08 |
Participant perception of bladder condition was recorded in the CRF by the investigator. Participants were asked at baseline (BL) and at the end of study treatment (EOT) if the extent to which their bladder condition caused them problems. The possible responses were: No Problem, Very Minor Problems, Minor Problems, Moderate Problems, Severe Problems, or Many Severe Problems. (NCT00879398)
Timeframe: Baseline and at the end of study treatment
| Intervention | Participants (Number) | |||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| BL: No Problem/EOT: No problem | BL: No Problem/EOT: Very Minor Problems | BL: No Problem/EOT: Minor Problems | BL: No Problem/EOT: Moderate Problems | BL: No Problem/EOT: Severe Problems | BL: No Problem/EOT: Many Severe Problems | BL: Very Minor Problems/EOT:No Problem | BL:Very Minor Problems/EOT: Very Minor Problems | BL: Very Minor Problems/EOT: Minor Problems | BL: Very Minor Problems/EOT: Moderate Problems | BL: Very Minor Problems/EOT: Severe Problems | BL: Very Minor Problems/EOT: Many Severe Problems | BL: Minor Problems/EOT: No Problem | BL: Minor Problems/EOT: Very Minor Problems | BL: Minor Problems/EOT: Minor Problems | BL: Minor Problems/EOT:Moderate Problems | BL: Minor Problems/EOT: Severe Problems | BL: Minor Problems/EOT: Many Severe Problems | BL: Moderate Problems/EOT: No Problem | BL: Moderate Problems/EOT: Very Minor Problems | BL: Moderate Problems/EOT: Minor Problems | BL: Moderate Problems/EOT: Moderate Problems | BL: Moderate Problems/EOT: Severe Problems | BL: Moderate Problems/EOT: Many Severe Problems | BL: Severe Problems/EOT: No Problem | BL: Severe Problems/EOT: Very Minor Problems | BL: Severe Problems/EOT: Minor Problems | BL: Severe Problems/EOT: Moderate Problems | BL: Severe Problems/EOT: Severe Problems | BL: Severe Problems/EOT: Many Severe Problems | BL: Many Severe Problems/EOT: No Problem | BL: Many Severe Problems/EOT: Very Minor Problems | BL: Many Severe Problems/EOT: Minor Problems | BL: Many Severe Problems/EOT: Moderate Problems | BL: Many Severe Problems/EOT: Severe Problems | BL: Many Severe Problems/EOT: Many Severe Problems | |
| Toviaz | 0 | 0 | 0 | 1 | 0 | 0 | 29 | 33 | 0 | 0 | 0 | 0 | 105 | 134 | 42 | 1 | 0 | 0 | 224 | 447 | 171 | 116 | 3 | 1 | 188 | 456 | 227 | 97 | 49 | 0 | 105 | 195 | 148 | 97 | 51 | 19 |
The final efficacy assessment included improvement, no change, aggravation, and unevaluable evaluated by the investigator based on the subject's symptoms of frequent micturition, urgency, and urgency urinary incontinence (UUI). (NCT00879398)
Timeframe: At the end of study treatment
| Intervention | Percentage of Participants (Number) | ||
|---|---|---|---|
| Improvement | No Change | Aggravation | |
| Toviaz | 90.13 | 9.50 | 0.37 |
The number of UUI episodes per 24 hours was recorded in the CRF by the investigator. Baseline was defined as data collected within 1 week prior to the first visit. (NCT00879398)
Timeframe: Baseline and at the end of study treatment
| Intervention | Number of Episodes per 24 Hours (Mean) | ||
|---|---|---|---|
| Baseline (n=2800) | End of study treatment (n=2800) | Change from baseline (n=2800) | |
| Toviaz | 1.07 | 0.27 | -0.80 |
The number of urgency episodes per 24 hours was recorded in the CRF by the investigator. Baseline was defined as data collected within 1 week prior to the first visit. (NCT00879398)
Timeframe: Baseline and at the end of study treatment
| Intervention | Number of Episodes per 24 Hours (Mean) | ||
|---|---|---|---|
| Baseline (n=2724) | End of Study Treatment (n=2724) | Change from Baseline (n=2724) | |
| Toviaz | 3.65 | 1.27 | -2.37 |
The number of micturitions per 24 hours was recorded in the case report form (CRF) by the investigator. Baseline was defined as data collected within 1 week prior to the first visit. (NCT00879398)
Timeframe: Baseline and at the end of study treatment
| Intervention | Number of Episodes per 24 Hours (Mean) | ||
|---|---|---|---|
| Baseline (n=2718) | End of Study Treatment (n=2718) | Change from Baseline (n=2718) | |
| Toviaz | 12.05 | 8.04 | -4.02 |
An AE was any untoward medical occurrence in a clinical investigation subject administered a product or medical device; the event was not necessarily had a causal relationship with the treatment or usage. All AEs reported after start of administration of Toviaz were considered as TEAEs. (NCT00879398)
Timeframe: From the time that the participant signed data privacy statement through and including 28 calendar days after the last administration of the study drug.
| Intervention | Percentage of Participants (Number) |
|---|---|
| Toviaz | 8.53 |
Micturitions include episodes of voluntary micturition and episodes of UUI. UUI episodes were defined as those micturitions with USS rating of 5 in the diary in participants with UUI at baseline. USS rating 5: Unable to hold; leak urine. (NCT00911937)
Timeframe: Baseline, Week 4 and 12
| Intervention | micturitions per 24 hours (Least Squares Mean) | |
|---|---|---|
| Change at Week 4 | Change at Week 12 | |
| Fesoterodine | -1.35 | -2.42 |
| Placebo | -0.90 | -1.86 |
OAB-q: self-administered, 33-item, questionnaire, assesses how much participant has been bothered by selected bladder symptoms. Each item rated on Likert scale 1 (least symptom bother) to 6 (most symptom bother). Questions 9 to 33 constitute HRQL, includes domains: concern, coping, sleep, and social function. HRQL domain and total raw score derived as sum of scores. Transformed score range 0 to 100 (Total HRQL or domain) = [(Highest possible raw score-Actual total raw score)/Raw score range]*100. Higher transformed scores indicative of better HRQL. (NCT00911937)
Timeframe: Baseline, Week 4 and 12
| Intervention | units on a scale (Least Squares Mean) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Change at Week 4: concern domain | Change at Week 4: coping domain | Change at Week 4: sleep domain | Change at Week 4: social interaction domain | Change at Week 4: total | Change at Week 12: concern domain | Change at Week 12: coping domain | Change at Week 12: sleep domain | Change at Week 12: social interaction domain | Change at Week 12: total | |
| Fesoterodine | NA | NA | NA | NA | NA | 18.05 | 18.32 | 22.45 | 10.13 | 17.42 |
| Placebo | NA | NA | NA | NA | NA | 14.63 | 15.17 | 18.97 | 8.27 | 14.39 |
Frequency-urgency sum is total USS ratings recorded for all micturitions in 24-hour day. Number of USS ratings per 24 hours is sum of all USS ratings divided by the total diary days collected at that visit. USS scale: 1=No feeling of urgency to 5=Unable to hold: leak urine. Numerical decrease indicates improvement. (NCT00911937)
Timeframe: Baseline, Week 4 and 12
| Intervention | units on a scale (Least Squares Mean) | |
|---|---|---|
| Change at Week 4 | Change at Week 12 | |
| Fesoterodine | -6.44 | -11.12 |
| Placebo | -4.88 | -8.69 |
OAB-q: a self-administered, 33-item, questionnaire that assesses how much the participant has been bothered by selected bladder symptoms. Each item rated by participant on Likert scale 1 (least symptom bother) to 6 (most symptom bother). Symptom bother score derived as sum of scores for questions 1-8; lowest possible raw score: 8; highest possible score: 48. Data analyzed based on transformation of the score to a 0 to 100 scale [(Actual total raw score - lowest possible value of raw score)/range]*100. Higher scores values indicative of greater symptom bother. (NCT00911937)
Timeframe: Baseline
| Intervention | units on a scale (Mean) |
|---|---|
| Placebo | 50.46 |
| Fesoterodine | 48.84 |
UUI episodes were defined as those with the USS rating of 5 in the diary. USS total range 1 to 5: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. (NCT00911937)
Timeframe: Baseline
| Intervention | episodes per 24 hours (Mean) |
|---|---|
| Placebo | 2.23 |
| Fesoterodine | 2.20 |
Nocturnal micturitions were defined as micturitions with USS rating 1-5 that occurred between the time the participant went to bed and the time he or she arose to start the next day. USS rating: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. The mean number of nocturnal micturitions per 24 hours was calculated as the total number of nocturnal micturitions divided by the total number of diary days collected at that visit. (NCT00911937)
Timeframe: Baseline
| Intervention | micturitions per 24 hours (Mean) |
|---|---|
| Placebo | 3.19 |
| Fesoterodine | 3.15 |
The mean number of micturition-related urgency episodes per 24 hours was calculated as the total number of micturitions with USS rating of greater than or equal to 3 divided by the total number of days that diary data was collected at that visit. USS total range 1 to 5: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. (NCT00911937)
Timeframe: Baseline
| Intervention | episodes per 24 hours (Mean) |
|---|---|
| Placebo | 10.04 |
| Fesoterodine | 9.84 |
Frequency-urgency sum is total USS ratings recorded for all nocturnal micturitions in 24-hour day. Number of USS ratings per 24 hours is sum of all USS ratings divided by the total diary days collected at that visit. USS scale: 1=No feeling of urgency to 5=Unable to hold: leak urine. Numerical decrease indicates improvement. (NCT00911937)
Timeframe: Baseline
| Intervention | units on a scale (Mean) |
|---|---|
| Placebo | 10.91 |
| Fesoterodine | 10.60 |
Micturition-related nocturnal urgency episodes had USS rating of 3 or more that occurred between time participant went to bed and time he or she arose to start next day. Number of nocturnal micturition-related urgency episodes per 24 hours was calculated as sum of all nocturnal micturition-related urgency episodes divided by total number of diary days collected at that visit. (NCT00911937)
Timeframe: Baseline and Week 12
| Intervention | episodes per 24 hours (Least Squares Mean) |
|---|---|
| Placebo | -1.06 |
| Fesoterodine | -1.29 |
Percent change of micturition-related urgency episodes per 24 hours was calculated as change in 24-hour mean at that visit divided by the baseline 24-hour mean multiplied by 100 (100*(Week 4 or 12 - baseline)/baseline). (NCT00911937)
Timeframe: Baseline, Week 4 and 12
| Intervention | percent change (Mean) | |
|---|---|---|
| Change at Week 4 | Change at Week 12 | |
| Fesoterodine | -20.0 | -34.2 |
| Placebo | -14.9 | -25.7 |
Nocturnal micturitions were defined as micturitions with USS rating 1-5 that occurred between the time the participant went to bed and the time he or she arose to start the next day. USS rating: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. The mean number of nocturnal micturitions per 24 hours was calculated as the total number of nocturnal micturitions divided by the total number of diary days collected at that visit. (NCT00911937)
Timeframe: Baseline, Week 4 and 12
| Intervention | micturitions per 24 hours (Least Squares Mean) | |
|---|---|---|
| Change at Week 4 | Change at Week 12 | |
| Fesoterodine | -0.59 | -1.02 |
| Placebo | -0.48 | -0.84 |
Frequency-urgency sum is total USS ratings recorded for all micturitions in 24-hour day. Number of USS ratings per 24 hours is sum of all USS ratings divided by the total diary days collected at that visit. USS scale: 1=No feeling of urgency to 5=Unable to hold: leak urine. (NCT00911937)
Timeframe: Baseline
| Intervention | units on a scale (Mean) |
|---|---|
| Placebo | 39.54 |
| Fesoterodine | 38.73 |
Mean voided volume per nocturnal micturition was calculated as sum of voided volume during bedtime divided by the total number of bedtime micturition episodes with a recorded voided volume greater than 0 at that visit. (NCT00911937)
Timeframe: Baseline and Week 12
| Intervention | mL (Least Squares Mean) |
|---|---|
| Placebo | 15.49 |
| Fesoterodine | 16.81 |
Mean voided volume per micturition was calculated as sum of voided volume divided by the total number of total micturition episodes with a recorded voided volume greater than 0 at that visit. (NCT00911937)
Timeframe: Baseline and Week 12
| Intervention | mL (Least Squares Mean) |
|---|---|
| Placebo | 5.51 |
| Fesoterodine | 4.65 |
Micturition-related nocturnal urgency episodes had USS rating of 3 or more that occurred between time participant went to bed and time he or she arose to start next day. Number of micturition-related nocturnal urgency episodes per 24 hours was calculated as sum of all nocturnal micturition-related urgency episodes divided by total number of diary days collected at that visit. (NCT00911937)
Timeframe: Baseline and Week 4
| Intervention | episodes per 24 hours (Least Squares Mean) |
|---|---|
| Placebo | -0.70 |
| Fesoterodine | -0.83 |
The mean number of micturition-related urgency episodes per 24 hours was calculated as the total number of micturitions with USS rating of greater than or equal to 3 divided by the total number of days that diary data was collected at that visit. USS total range 1 to 5: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. (NCT00911937)
Timeframe: Baseline, Week 4 and 12
| Intervention | episodes per 24 hours (Least Squares Mean) | |
|---|---|---|
| Change at Week 4 | Change at Week 12 | |
| Fesoterodine | -2.18 | -3.50 |
| Placebo | -1.59 | -2.72 |
Frequency-urgency sum is total USS ratings recorded for all nocturnal micturitions in 24-hour day. Number of USS ratings per 24 hours is sum of all USS ratings divided by the total diary days collected at that visit. USS scale: 1=No feeling of urgency to 5=Unable to hold: leak urine. Numerical decrease indicates improvement. (NCT00911937)
Timeframe: Baseline, Week 4 and 12
| Intervention | units on a scale (Least Squares Mean) | |
|---|---|---|
| Change at Week 4 | Change at Week 12 | |
| Fesoterodine | -2.46 | -4.08 |
| Placebo | -2.07 | -3.36 |
Percent change of UUI episodes per 24 hours was calculated as change in 24-hour mean at that visit divided by the baseline 24-hour mean multiplied by 100 (100*(Week 4 or 12 - baseline)/baseline). (NCT00911937)
Timeframe: Baseline, Week 4 and 12
| Intervention | percent change (Mean) | |
|---|---|---|
| Change at Week 4 | Change at Week 12 | |
| Fesoterodine | -34.8 | -59.2 |
| Placebo | -34.2 | -58.2 |
Percent change of nocturnal micturitions per 24 hours was calculated as change in 24-hour mean at that visit divided by the baseline 24-hour mean multiplied by 100 (100*(Week 4 or 12 - baseline)/baseline). (NCT00911937)
Timeframe: Baseline, Week 4 and 12
| Intervention | percent change (Mean) | |
|---|---|---|
| Change at Week 4 | Change at Week 12 | |
| Fesoterodine | -18.9 | -32.2 |
| Placebo | -15.1 | -26.2 |
Percent change of micturitions per 24 hours was calculated as change in 24-hour mean at that visit divided by the baseline 24-hour mean multiplied by 100 (100*(Week 4 or 12 - baseline)/baseline). (NCT00911937)
Timeframe: Baseline, Week 4 and 12
| Intervention | percent change (Mean) | |
|---|---|---|
| Change at Week 4 | Change at Week 12 | |
| Fesoterodine | -10.3 | -18.7 |
| Placebo | -6.7 | -14.2 |
Percent change of micturition-related nocturnal urgency episodes per 24 hours was calculated as change in 24-hour mean at that visit divided by the baseline 24-hour mean multiplied by 100 (100*(Week 4 or 12 - baseline)/baseline). (NCT00911937)
Timeframe: Baseline, Week 4 and 12
| Intervention | percent change (Mean) | |
|---|---|---|
| Change at Week 4 | Change at Week 12 | |
| Fesoterodine | -28.4 | -44.5 |
| Placebo | -24.1 | -36.2 |
OAB-q: self-administered, 33-item, questionnaire, assesses how much participant has been bothered by selected bladder symptoms. Each item rated on Likert scale 1 (least symptom bother) to 6 (most symptom bother). Questions 9 to 33 constitute HRQL, includes domains: concern, coping, sleep, and social function. HRQL domain and total raw score derived as sum of scores. Transformed score range 0 to 100 (Total HRQL or domain) = [(Highest possible raw score-Actual total raw score)/Raw score range]*100. Higher transformed scores indicative of better HRQL. (NCT00911937)
Timeframe: Baseline
| Intervention | units on a scale (Mean) | ||||
|---|---|---|---|---|---|
| Concern domain | Coping domain | Sleep domain | Social interaction domain | Total | |
| Fesoterodine | 64.30 | 62.26 | 49.65 | 82.48 | 64.37 |
| Placebo | 63.29 | 62.19 | 47.45 | 82.22 | 63.56 |
OAB-q: a self-administered, 33-item, questionnaire that assesses how much the participant has been bothered by selected bladder symptoms. Each item rated by participant on Likert scale 1 (least symptom bother) to 6 (most symptom bother). Symptom bother score derived as sum of scores for questions 1-8; lowest possible raw score: 8; highest possible score: 48. Data analyzed based on transformation of the score to a 0 to 100 scale [(Actual total raw score - lowest possible value of raw score)/range]*100. Higher scores values indicative of greater symptom bother. (NCT00911937)
Timeframe: Baseline, Week 4 and 12
| Intervention | units on a scale (Least Squares Mean) | |
|---|---|---|
| Change at Week 4 | Change at Week 12 | |
| Fesoterodine | NA | -20.28 |
| Placebo | NA | -15.91 |
Mean voided volume per nocturnal micturition was calculated as sum of voided volume during bedtime divided by the total number of bedtime micturition episodes with a recorded voided volume greater than 0 at that visit. (NCT00911937)
Timeframe: Baseline
| Intervention | milliliter (mL) (Mean) |
|---|---|
| Placebo | 172.53 |
| Fesoterodine | 173.14 |
Mean voided volume per micturition was calculated as sum of voided volume divided by the total number of total micturition episodes with a recorded voided volume greater than 0 at that visit. (NCT00911937)
Timeframe: Baseline
| Intervention | mL (Mean) |
|---|---|
| Placebo | 154.56 |
| Fesoterodine | 158.38 |
Micturitions include episodes of voluntary micturition and episodes of Urgency Urinary Incontinence [UUI]. UUI episodes were defined as those micturitions with USS rating of 5 in the diary in participants with UUI at baseline. USS rating 5: Unable to hold; leak urine. (NCT00911937)
Timeframe: Baseline
| Intervention | micturitions per 24 hours (Mean) |
|---|---|
| Placebo | 12.33 |
| Fesoterodine | 12.30 |
UUI episodes were defined as those with the USS rating of 5 in the diary. USS total range 1 to 5: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. (NCT00911937)
Timeframe: Baseline, Week 4 and 12
| Intervention | episodes per 24 hours (Least Squares Mean) | |
|---|---|---|
| Change at Week 4 | Change at Week 12 | |
| Fesoterodine | -0.90 | -1.26 |
| Placebo | -0.76 | -1.08 |
Micturition-related nocturnal urgency episodes had urinary sensation scale (USS) rating of 3 or more that occurred between time participant went to bed and time he or she arose to start next day. Number of nocturnal micturition-related urgency episodes per 24 hours was calculated as sum of all nocturnal micturition-related urgency episodes divided by total number of diary days collected at that visit. (NCT00911937)
Timeframe: Baseline
| Intervention | episodes per 24 hours (Mean) |
|---|---|
| Placebo | 2.93 |
| Fesoterodine | 2.91 |
Micturitions include episodes of voluntary micturition and episodes of UUI. UUI episodes were defined as those micturitions with USS rating of 5 in the diary in participants with UUI at baseline. USS rating 5: Unable to hold; leak urine. (NCT00928070)
Timeframe: Baseline
| Intervention | micturitions per 24 hours (Mean) |
|---|---|
| Placebo | 12.22 |
| Fesoterodine | 12.11 |
The mean number of micturition-related urgency episodes per 24 hours was calculated as the total number of micturitions with USS rating of greater than or equal to (>=) 3 divided by the total number of days that diary data was collected at that visit. USS total range 1 to 5: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. (NCT00928070)
Timeframe: Baseline
| Intervention | episodes per 24 hours (Mean) |
|---|---|
| Placebo | 10.30 |
| Fesoterodine | 10.02 |
Nocturnal micturition-related urgency episodes had USS rating of 3 or more that occurred between time participant went to bed and time he or she arose to start next day. Number of nocturnal micturition-related urgency episodes per 24 hours was calculated as sum of all nocturnal micturition-related urgency episodes divided by total number of diary days collected at that visit. (NCT00928070)
Timeframe: Baseline
| Intervention | episodes per 24 hours (Mean) |
|---|---|
| Placebo | 2.87 |
| Fesoterodine | 2.69 |
UUI episodes were defined as those with the Urinary Sensation Scale (USS) rating of 5 in the diary. USS total range 1 to 5: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. (NCT00928070)
Timeframe: Baseline
| Intervention | episodes per 24 hours (Mean) |
|---|---|
| Placebo | 3.93 |
| Fesoterodine | 4.07 |
MMSE measured general cognitive functioning: orientation, memory, attention, calculation, language, visuospatial functions. Total score derived from sub-scores; total ranges from 0 to 30, higher score indicates better cognitive state. (NCT00928070)
Timeframe: Screening
| Intervention | units on a scale (Mean) |
|---|---|
| Placebo | 28.04 |
| Fesoterodine | 28.16 |
OAB-q: a self-administered, 33-item, questionnaire that assesses how much the participant has been bothered by selected bladder symptoms. Each item rated by participant on Likert scale 1 (least symptom bother) to 6 (most symptom bother). Symptom bother score derived as sum of scores for questions 1-8; lowest possible raw score: 8; highest possible score: 48. Data analyzed based on transformation of the score to a 0 to 100 scale [(Actual total raw score - lowest possible value of raw score)/range]*100. Higher scores values indicative of greater symptom bother. (NCT00928070)
Timeframe: Baseline
| Intervention | units on a scale (Mean) |
|---|---|
| Placebo | 67.67 |
| Fesoterodine | 67.25 |
Micturitions include episodes of voluntary micturition and episodes of UUI. UUI episodes were defined as those micturitions with USS rating of 5 in the diary in participants with UUI at baseline. USS rating 5: Unable to hold; leak urine. (NCT00928070)
Timeframe: Baseline, Week 4, 12
| Intervention | micturitions per 24 hours (Least Squares Mean) | |
|---|---|---|
| Change at Week 4 | Change at Week 12 | |
| Fesoterodine | -1.64 | -2.34 |
| Placebo | -0.77 | -1.50 |
Frequency-urgency sum is total USS ratings recorded for all micturitions in 24-hour day. Number of USS ratings per 24 hours is sum of all USS ratings divided by the total diary days collected at that visit. USS scale: 1=No feeling of urgency to 5=Unable to hold: leak urine. (NCT00928070)
Timeframe: Baseline
| Intervention | units on a scale (Mean) |
|---|---|
| Placebo | 45.33 |
| Fesoterodine | 44.92 |
"Participant's response to question, overall, how satisfied are you with your OAB medication? was obtained on a 5 point scale, 1- very satisfied, 2- somewhat satisfied, 3- neither dissatisfied nor satisfied, 4- somewhat dissatisfied and 5- very dissatisfied. Response values 1 and 2 were combined into satisfied, and 4 and 5 were combined into dissatisfied." (NCT00928070)
Timeframe: Week 12
| Intervention | percentage of participants (Number) | ||
|---|---|---|---|
| Not satisfied | Neither dissatisfied nor satisfied | Satisfied | |
| Fesoterodine | 18.9 | 9.3 | 71.8 |
| Placebo | 37.5 | 15.2 | 47.3 |
PPBC: a self-administered, single-item, questionnaire that asks participants to describe their perception of their bladder-related problems. The PPBC assessment is rated on a 6-point scale: 1=no problems at all, 2=some very minor problems, 3=some minor problems, 4=moderate problems, 5=severe problems, 6=many severe problems. Deterioration=score difference is greater than 0; no change=score difference is 0; minor improvement=score difference is -1; major difference=score difference is less than or equal to -2. (NCT00928070)
Timeframe: Screening, Week 4, 12
| Intervention | percentage of participants (Number) | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline: No problems at all | Baseline: Some very minor problems | Baseline: Some minor problems | Baseline: Moderate problems | Baseline: Severe problems | Baseline: Many severe problems | Change at Week 4: Deterioration | Change at Week 4: No change | Change at Week 4: Minor improvement | Change at Week 4: Major improvement | Change at Week 12: Deterioration | Change at Week 12: No change | Change at Week 12: Minor improvement | Change at Week 12: Major improvement | |
| Fesoterodine | 0.0 | 0.0 | 0.0 | 44.5 | 44.2 | 11.3 | 9.5 | 29.8 | 27.5 | 33.2 | 7.2 | 27.2 | 26.8 | 38.9 |
| Placebo | 0.0 | 0.0 | 0.0 | 44.7 | 43.9 | 11.4 | 12.3 | 42.5 | 25.3 | 19.9 | 12.1 | 33.7 | 25.0 | 29.2 |
Percent change of UUI episodes per 24 hours was calculated as change in 24-hour mean at that visit divided by the baseline 24-hour mean multiplied by 100 (i.e., 100*(Week 4 or 12 - baseline)/baseline). (NCT00928070)
Timeframe: Baseline, Week 4, 12
| Intervention | percent change (Mean) | |
|---|---|---|
| Change at Week 4 | Change at Week 12 | |
| Fesoterodine | -57.2 | -71.2 |
| Placebo | -39.2 | -55.4 |
Percent change of nocturnal micturition-related urgency episodes per 24 hours was calculated as change in 24-hour mean at that visit divided by the baseline 24-hour mean multiplied by 100 (i.e., 100*(Week 4 or 12 - baseline)/baseline). (NCT00928070)
Timeframe: Baseline, Week 4, 12
| Intervention | percent change (Mean) | |
|---|---|---|
| Change at Week 4 | Change at Week 12 | |
| Fesoterodine | -18.0 | -31.2 |
| Placebo | -4.9 | -15.5 |
Percent change of micturitions per 24 hours was calculated as change in 24-hour mean at that visit divided by the baseline 24-hour mean multiplied by 100 (i.e., 100*(Week 4 or 12 - baseline)/baseline). (NCT00928070)
Timeframe: Baseline, Week 4, 12
| Intervention | percent change (Mean) | |
|---|---|---|
| Change at Week 4 | Change at Week 12 | |
| Fesoterodine | -12.7 | -17.8 |
| Placebo | -5.1 | -10.4 |
Percent change of micturition-related urgency episodes per 24 hours was calculated as change in 24-hour mean at that visit divided by the baseline 24-hour mean multiplied by 100 (i.e., 100*(Week 4 or 12 - baseline)/baseline). (NCT00928070)
Timeframe: Baseline, Week 4, 12
| Intervention | percent change (Mean) | |
|---|---|---|
| Change at Week 4 | Change at Week 12 | |
| Fesoterodine | -26.2 | -39.7 |
| Placebo | -12.7 | -23.9 |
OAB-q: self-administered, 33-item, questionnaire, assesses how much participant has been bothered by selected bladder symptoms. Each item rated on Likert scale 1 (least symptom bother) to 6 (most symptom bother). Questions 9 to 33 constitute HRQL, includes domains: concern, coping, sleep, and social function. HRQL domain and total raw score derived as sum of scores. Transformed score range 0 to 100 (Total HRQL or domain) = [(Highest possible raw score-Actual total raw score)/Raw score range]*100. Higher transformed scores indicative of better HRQL. (NCT00928070)
Timeframe: Baseline
| Intervention | units on a scale (Mean) | ||||
|---|---|---|---|---|---|
| Concern domain | Coping domain | Sleep domain | Social interaction domain | Total | |
| Fesoterodine | 46.57 | 44.74 | 43.41 | 72.70 | 50.58 |
| Placebo | 45.89 | 44.72 | 40.19 | 72.05 | 49.61 |
PVR volume is defined as volume of urine remaining in the bladder immediately after urination. (NCT00928070)
Timeframe: Baseline, Week 4, 12
| Intervention | mL (Mean) | ||
|---|---|---|---|
| Baseline | Change at Week 4 | Change at Week 12 | |
| Fesoterodine | 25.69 | 13.43 | 13.58 |
| Placebo | 26.51 | 1.83 | -2.98 |
OAB-q: a self-administered, 33-item, questionnaire that assesses how much the participant has been bothered by selected bladder symptoms. Each item rated by participant on Likert scale 1 (least symptom bother) to 6 (most symptom bother). Symptom bother score derived as sum of scores for questions 1-8; lowest possible raw score: 8; highest possible score: 48. Data analyzed based on transformation of the score to a 0 to 100 scale [(Actual total raw score - lowest possible value of raw score)/range]*100. Higher scores values indicative of greater symptom bother. (NCT00928070)
Timeframe: Baseline, Week 4, 12
| Intervention | units on a scale (Least Squares Mean) | |
|---|---|---|
| Change at Week 4 | Change at Week 12 | |
| Fesoterodine | -22.96 | -28.08 |
| Placebo | -13.81 | -20.48 |
Protective Undergarments included pads, protective padding, protective underwear (pull up), and briefs (diaper). The mean number of undergarments changed per 24 hours was calculated as the total number of undergarments changed divided by the total number of diary days collected at that visit. Change from baseline values were reported at week 4 for subsets of population with baseline values less than or equal to (=<) 3.5 and more than (>) 3.5 undergarments/day and at Week 12 for subsets of population with baseline values =< 2.5 and > 2.5 undergarments/day. (NCT00928070)
Timeframe: Baseline, Week 4, 12
| Intervention | undergarments (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Baseline: =<3.5 undergarments (n=193,184) | Baseline: >3.5 undergarments (n=12,19) | Baseline: =<2.5 undergarments (n=172,169) | Baseline: >2.5 undergarments (n=35,35) | Change at Week 4: =<3.5 undergarments(n=193,184) | Change at Week 4: >3.5 undergarments(n=12,19) | Change at Week 12: =<2.5 undergarments(n=172,169) | Change at Week 12: >2.5 undergarments(n=35,35) | |
| Fesoterodine | 1.49 | 4.81 | 1.35 | 3.94 | -0.61 | -2.11 | -0.72 | -1.98 |
| Placebo | 1.41 | 4.97 | 1.21 | 3.71 | -0.27 | -2.56 | -0.31 | -2.14 |
Nocturnal micturition-related urgency episodes had USS rating of 3 or more that occurred between time participant went to bed and time he or she arose to start next day. Number of nocturnal micturition-related urgency episodes per 24 hours was calculated as sum of all nocturnal micturition-related urgency episodes divided by total number of diary days collected at that visit. (NCT00928070)
Timeframe: Baseline, Week 4, 12
| Intervention | episodes per 24 hours (Least Squares Mean) | |
|---|---|---|
| Change at Week 4 | Change at Week 12 | |
| Fesoterodine | -0.58 | -0.97 |
| Placebo | -0.44 | -0.68 |
The mean number of micturition-related urgency episodes per 24 hours was calculated as the total number of micturitions with USS rating of greater than or equal to (>=) 3 divided by the total number of days that diary data was collected at that visit. USS total range 1 to 5: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. (NCT00928070)
Timeframe: Baseline, Week 4, 12
| Intervention | episodes per 24 hours (Least Squares Mean) | |
|---|---|---|
| Change at Week 4 | Change at Week 12 | |
| Fesoterodine | -2.74 | -4.15 |
| Placebo | -1.64 | -2.75 |
OAB-q: self-administered, 33-item, questionnaire, assesses how much participant has been bothered by selected bladder symptoms. Each item rated on Likert scale 1 (least symptom bother) to 6 (most symptom bother). Questions 9 to 33 constitute HRQL, includes domains: concern, coping, sleep, and social function. HRQL domain and total raw score derived as sum of scores. Transformed score range 0 to 100 (Total HRQL or domain) = [(Highest possible raw score-Actual total raw score)/Raw score range]*100. Higher transformed scores indicative of better HRQL. (NCT00928070)
Timeframe: Baseline, Week 4, 12
| Intervention | units on a scale (Least Squares Mean) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Change at Week 4: concern domain | Change at Week 4: coping domain | Change at Week 4: sleeping domain | Change at Week 4: social interaction domain | Change at Week 4: total | Change at Week 12: concern domain | Change at Week 12: coping domain | Change at Week 12: sleeping domain | Change at Week 12: social interaction domain | Change at Week 12: total | |
| Fesoterodine | 20.51 | 19.86 | 17.33 | 11.22 | 17.80 | 26.24 | 25.66 | 23.10 | 14.47 | 23.08 |
| Placebo | 12.35 | 12.90 | 13.33 | 8.77 | 12.00 | 17.20 | 20.34 | 19.05 | 12.12 | 17.55 |
Frequency-urgency sum is total USS ratings recorded for all micturitions in 24-hour day. Number of USS ratings per 24 hours is sum of all USS ratings divided by the total diary days collected at that visit. USS scale: 1=No feeling of urgency to 5=Unable to hold: leak urine. Numerical decrease indicates improvement. (NCT00928070)
Timeframe: Baseline, Week 4, 12
| Intervention | units on a scale (Least Squares Mean) | |
|---|---|---|
| Change at Week 4 | Change at Week 12 | |
| Fesoterodine | -11.62 | -16.50 |
| Placebo | -6.95 | -11.53 |
OAB-S: a validated self-administered instrument that evaluates OAB medication expectations, daily life with AB, and satisfaction with OAB medication and includes 3 stand-alone items that assess overall expectation, satisfaction, and willingness to continue treatment. Satisfaction coded on scale of 1 to 5: (1=very satisfied to 5=very dissatisfied). Coding reversed algorithmically and results transformed: total score range 0 to100. Higher final response value associated with better satisfaction. (NCT00928070)
Timeframe: Week 12
| Intervention | units on a scale (Mean) |
|---|---|
| Placebo | 52.98 |
| Fesoterodine | 68.89 |
UUI episodes were defined as those with the USS rating of 5 in the diary. USS total range 1 to 5: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. (NCT00928070)
Timeframe: Baseline, Week 12
| Intervention | episodes per 24 hours (Least Squares Mean) |
|---|---|
| Placebo | -2.20 |
| Fesoterodine | -2.84 |
UUI episodes were defined as those with the USS rating of 5 in the diary. USS total range 1 to 5: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. (NCT00928070)
Timeframe: Baseline, Week 4
| Intervention | episodes per 24 hours (Least Squares Mean) |
|---|---|
| Placebo | -1.54 |
| Fesoterodine | -2.36 |
MMSE measured general cognitive functioning: orientation, memory, attention, calculation, language, visuospatial functions. Total score derived from sub-scores; total ranges from 0 to 30, higher score indicates better cognitive state. Change: mean score at Week X minus mean score at baseline (NCT00928070)
Timeframe: Screening, Week 12
| Intervention | units on a scale (Least Squares Mean) |
|---|---|
| Placebo | 0.33 |
| Fesoterodine | 0.15 |
The use of the YourWay plan was optional but was available to all participants and included healthy bladder behaviors such as setting and maintaining personal goals and choice of bladder-friendly food and drinks. (NCT00943735)
Timeframe: Baseline up to 90 days
| Intervention | percentage of participants (Number) |
|---|---|
| Fesoterodine 4 mg or 8 mg | 85.3 |
(NCT00943735)
Timeframe: Baseline up to 90 days
| Intervention | percentage of participants (Number) |
|---|---|
| Fesoterodine 4 mg or 8 mg | 89.6 |
(NCT00943735)
Timeframe: Baseline up to 90 days
| Intervention | percentage of participants (Number) |
|---|---|
| Fesoterodine 4 mg or 8 mg | 91.9 |
(NCT00943735)
Timeframe: Baseline up to 90 days
| Intervention | percentage of participants (Number) |
|---|---|
| Fesoterodine 4 mg or 8 mg | 95.5 |
YourWay participants received 6 telephone calls from an automated speech-recognition system over a period of approximately 11 weeks. The calls included reinforcement of treatment participation, treatment expectations, compliance, general health messages regarding OAB, review of training materials, optional weekly email communication, and a wrap-up call which included a summary of lessons learned from each of the Core 4 lessons calls and guidance to find additional information about medication and lifestyle tips to support management of OAB symptoms. (NCT00943735)
Timeframe: Baseline up to 90 days
| Intervention | percentage of participants (Number) |
|---|---|
| Fesoterodine 4 mg or 8 mg | 81.7 |
(NCT00943735)
Timeframe: Baseline up to 90 days
| Intervention | percentage of participants (Number) |
|---|---|
| Fesoterodine 4 mg or 8 mg | 79.9 |
(NCT00943735)
Timeframe: Baseline up to 90 days
| Intervention | percentage of participants (Number) |
|---|---|
| Fesoterodine 4 mg or 8 mg | 3.0 |
"The use of the YourWay plan was optional but was available to all participants and included bladder training techniques such as to urinate each day when getting up and before going to bed, gradually increasing the amount of time between urinating, staying with timing goals whether there was a need to urinate or not, and bladder control tips (such as pelvic floor muscle squeeze, sit down and take 5 deep breaths, or stating I'm the boss - not my bladder)." (NCT00943735)
Timeframe: Baseline up to 90 days
| Intervention | percentage of participants (Number) |
|---|---|
| Fesoterodine 4 mg or 8 mg | 86.6 |
The use of the YourWay plan was optional but was available to all participants and included guidance for food and drink choices, bladder training, treatment compliance, and use of a daily tracker. (NCT00943735)
Timeframe: Baseline up to 90 days
| Intervention | percentage of participants (Number) |
|---|---|
| Fesoterodine 4 mg or 8 mg | 85.3 |
(NCT00943735)
Timeframe: Enrollment (Day 0) up to 90 days
| Intervention | percentage of participants (Number) | |
|---|---|---|
| Good understanding at enrollment (n=500) | Good understanding at end of study (n=335) | |
| Fesoterodine 4 mg or 8 mg | 78.4 | 89.6 |
YourWay plan was available and accessible to all participants prescribed fesoterodine, but was not defined as an explicit or required component. Plan included motivational support for taking fesoterodine and behavioral interventions shown in clinical studies to improve participants' Overactive Bladder (OAB) outcomes. Objectives included intervening quickly after treatment initiation, before participants had an opportunity to discontinue medication, reinforcing the treatable nature of OAB, and setting appropriate expectations for onset of action with therapy and degree of symptom improvement. (NCT00943735)
Timeframe: Baseline up to 90 days
| Intervention | percentage of participants (Number) |
|---|---|
| Fesoterodine 4 mg or 8 mg | 28.8 |
(NCT00943735)
Timeframe: Baseline up to 90 days
| Intervention | percentage of participants (Number) |
|---|---|
| Fesoterodine 4 mg or 8 mg | 93.4 |
"Treatment goals and bladder symptoms progress trackers were incorporated in the 12 Week Tracker which included a participant determined weekly goal, a reminder to fill the prescription (if appropriate interval), participant reported progress in response to this week I did well at, and a 7-day Daily Core 4 Tracker checklist (food and drink, teach your bladder, daily fesoterodine, and track your progress)." (NCT00943735)
Timeframe: Baseline up to 90 days
| Intervention | percentage of participants (Number) |
|---|---|
| Fesoterodine 4 mg or 8 mg | 74.1 |
The prototypical pattern was to fill 3 separate prescriptions, each for a 30-day supply, between the enrollment date and Day 90 of the study period; these prescription fills could happen as early as Day 0, 30, and 60 of the study period. At enrollment, the Investigator provided participants with a prescription for fesoterodine 4mg or 8mg to be filled at a pharmacy of their choice. The first refill indicated that 2 fesoterodine prescriptions had been filled. (NCT00943735)
Timeframe: Enrollment (Day 0) up to 90 days
| Intervention | percentage of participants (Number) |
|---|---|
| Fesoterodine 4 mg or 8 mg | 13.4 |
The prototypical pattern was to fill 3 separate prescriptions, each for a 30-day supply, between the enrollment date and Day 90 of the study period; these prescription fills could happen as early as Day 0, 30, and 60 of the study period. Primary adherence was met if the participant filled at least 1 fesoterodine prescription during the study period. (NCT00943735)
Timeframe: Enrollment (Day 0) up to 90 days
| Intervention | percentage of participants (Number) |
|---|---|
| Fesoterodine 4 mg or 8 mg | 26.2 |
Prototypical pattern for meeting primary endpoint was to fill 3 separate prescriptions (Rx), each for a 30-day supply between enrollment and Day 90. Rx fills could happen as early as Day 0, 30, and 60 of the study period. Participants could also have chosen to wait until their 14-day medication sample was exhausted before receiving their first fill. Investigators received no prescribing restrictions, but were advised not to write Rx for a 90-day supply of fesoterodine at enrollment visit. Participants whose first observed Rx was for a ≥90-day supply were non-evaluable for the primary endpoint. (NCT00943735)
Timeframe: Enrollment (Day 0) up to 90 days
| Intervention | percentage of participants (Number) |
|---|---|
| Fesoterodine 4 mg or 8 mg | 10.4 |
(NCT00943735)
Timeframe: Baseline up to 90 days
| Intervention | percentage of participants (Number) |
|---|---|
| Fesoterodine 4 mg or 8 mg | 81.6 |
Product indication and safety information was provided to all participants by the investigator and / or within the YourWay plan program information. (NCT00943735)
Timeframe: Baseline up to 90 days
| Intervention | percentage of participants (Number) |
|---|---|
| Fesoterodine 4 mg or 8 mg | 88.2 |
(NCT00943735)
Timeframe: Baseline up to 90 days
| Intervention | percentage of participants (Number) |
|---|---|
| Fesoterodine 4 mg or 8 mg | 93.8 |
(NCT00943735)
Timeframe: Baseline up to 90 days
| Intervention | percentage of participants (Number) |
|---|---|
| Fesoterodine 4 mg or 8 mg | 87.0 |
(NCT00943735)
Timeframe: Baseline up to 90 days
| Intervention | percentage of participants (Number) |
|---|---|
| Fesoterodine 4 mg or 8 mg | 72.4 |
(NCT00943735)
Timeframe: Baseline up to 90 days
| Intervention | percentage of participants (Number) |
|---|---|
| Fesoterodine 4 mg or 8 mg | 86.9 |
YourWay participants received 6 telephone calls from an automated speech-recognition system over a period of approximately 11 weeks. The calls included reinforcement of treatment participation, treatment expectations, compliance, general health messages regarding OAB, review of training materials, optional weekly email communication, and a wrap-up call which included a summary of lessons learned from each of the Core 4 lessons calls and guidance to find additional information about medication and lifestyle tips to support management of OAB symptoms. (NCT00943735)
Timeframe: Baseline up to 90 days
| Intervention | percentage of participants (Number) |
|---|---|
| Fesoterodine 4 mg or 8 mg | 78.5 |
"For each week, the 12 Week Tracker included a participant determined weekly goal, a reminder to fill the prescription (if appropriate interval), participant reported progress in response to this week I did well at, and a 7-day Daily Core 4 Tracker checklist (food and drink, teach your bladder, daily fesoterodine, and track your progress)." (NCT00943735)
Timeframe: Baseline up to 90 days
| Intervention | percentage of participants (Number) |
|---|---|
| Fesoterodine 4 mg or 8 mg | 57.4 |
(NCT00943735)
Timeframe: Baseline up to 90 days
| Intervention | percentage of participants (Number) |
|---|---|
| Fesoterodine 4 mg or 8 mg | 93.9 |
"YourWay Daily Core 4 Tracker to track daily progress in the 4 core areas of food and drink (make more informed choices), teach your bladder (train your bladder to wait), daily Toviaz® (always take as directed), and keep track (share with your doctor)." (NCT00943735)
Timeframe: Baseline up to 90 days
| Intervention | percentage of participants (Number) |
|---|---|
| Fesoterodine 4 mg or 8 mg | 56.8 |
(NCT00943735)
Timeframe: Baseline up to 90 days
| Intervention | percentage of participants (Number) |
|---|---|
| Fesoterodine 4 mg or 8 mg | 69.2 |
The use of the YourWay plan was optional but was available to all participants and included bladder-friendly food and drink choices and recipes as well as information for maintaining hydration and avoidance of potential bladder irritants (such as caffeine, citrus fruits and juices, artificial sweeteners, tomato-based foods, soda, alcohol, and spicy foods). (NCT00943735)
Timeframe: Baseline up to 90 days
| Intervention | percentage of participants (Number) |
|---|---|
| Fesoterodine 4 mg or 8 mg | 82.4 |
Participants were recruited for study participation when they presented with OAB symptoms during regularly-scheduled physician visits; screening and enrollment occurred during the same visit. Follow-up visits could be scheduled per standard clinical practice. (NCT00943735)
Timeframe: Baseline up to 90 days
| Intervention | percentage of participants (Number) |
|---|---|
| Fesoterodine 4 mg or 8 mg | 56.6 |
"YourWay plan included a starter pack with a 14-day supply of 4 mg or 8 mg fesoterodine; guidebook for YourWay plan components and lifestyle modification tips; plan progress tracker with additional lifestyle tips; plan enrollment form. About 1 week after plan enrollment, participants received a resource kit by mail which included: a cover letter; brochures for Core 4 elements (food and drink, teach your bladder, daily fesoterodine, and track your progress); bladder diary and track your progress brochure; and recipes using bladder-friendly foods." (NCT00943735)
Timeframe: Baseline up to 90 days
| Intervention | percentage of participants (Number) |
|---|---|
| Fesoterodine 4 mg or 8 mg | 97.3 |
Stress Incontinence Component of the daily IEF calculated as the average daily number of stress leakage episodes that occurred during the 3 days prior to randomization and the end of each treatment period. Day 7 mean for each treatment period was calculated as the mean daily episode frequency based on the diary completed in the final three days of each treatment period. (NCT01042236)
Timeframe: Baseline, Day 7 of each period
| Intervention | Episodes per 24 hours. (Mean) | ||
|---|---|---|---|
| Baseline | Absolute value at Day 7 | Change at Day 7 | |
| Fesoterodine (4 mg) | 1.44 | 0.69 | -0.75 |
| Fesoterodine (8 mg) | 1.44 | 0.98 | -0.46 |
| Placebo | 1.44 | 0.82 | -0.62 |
Closing urethral pressure measured by urethral reflectometry calculated as the mean of each of the closing urethral pressure measurements obtained in triplicate at each time point for each participant. Day 7 mean for each treatment period was calculated as the mean of the three measurements taken post-dose on Day 7 of each treatment period separately. (NCT01042236)
Timeframe: Baseline, Day 7 of each period
| Intervention | cmH20 (Mean) | ||
|---|---|---|---|
| Baseline | Absolute value at Day 7 | Mean change at Day 7 | |
| Fesoterodine (4 mg) | 40.62 | 37.84 | -2.78 |
| Fesoterodine (8 mg) | 40.62 | 38.75 | -1.88 |
| Placebo | 40.62 | 38.66 | -1.96 |
Closing urethral elastance measured by urethral reflectometry calculated as the mean of each of the closing urethral pressure measurements obtained in triplicate at each time point for each participant. Day 7 mean for each treatment period was calculated as the mean of the three measurements taken post-dose on Day 7 of each treatment period separately. (NCT01042236)
Timeframe: Baseline, Day 7 of each period
| Intervention | cmH2O/mm^2 (Mean) | ||
|---|---|---|---|
| Baseline | Absolue value at Day 7 | Mean change at Day 7 | |
| Fesoterodine (4 mg) | 1.85 | 1.56 | -0.28 |
| Fesoterodine (8 mg) | 1.85 | 1.74 | -0.10 |
| Placebo | 1.85 | 1.75 | -0.09 |
Urgency Urinary Incontinence Component of the daily IEF calculated as the average daily number of urgency leakage episodes that occurred during the 3 days prior to randomization and the end of each treatment period. Day 7 mean for each treatment period was calculated as the mean daily episode frequency based on the diary completed in the final three days of each treatment period. (NCT01042236)
Timeframe: Baseline, Day 7 of each period
| Intervention | Percent (Median) |
|---|---|
| Fesoterodine (4 mg) | -50.00 |
| Fesoterodine (8 mg) | -100.00 |
| Placebo | -100.00 |
OUP measured by urethral reflectometry calculated as the mean of all of the OUP measurements obtained in triplicate at each time point for each participant. Day 7 mean for each treatment period was calculated as the mean of the three measurements taken post-dose on Day 7 of each treatment period separately. (NCT01042236)
Timeframe: Baseline, Day 7 of each period
| Intervention | centimeter of water (cmH2O) (Mean) | ||
|---|---|---|---|
| Baseline | Absolute value at Day 7 | Mean change at Day 7 | |
| Fesoterodine (4 mg) | 49.86 | 47.92 | -1.94 |
| Fesoterodine (8 mg) | 49.86 | 49.16 | -0.70 |
| Placebo | 49.86 | 48.53 | -1.34 |
Stress Incontinence Component of the daily IEF calculated as the average daily number of stress leakage episodes that occurred during the 3 days prior to randomization and the end of each treatment period. Day 7 mean for each treatment period was calculated as the mean daily episode frequency based on the diary completed in the final three days of each treatment period. (NCT01042236)
Timeframe: Baseline, Day 7 of each period
| Intervention | Percent (Median) |
|---|---|
| Fesoterodine (4 mg) | -66.67 |
| Fesoterodine (8 mg) | -55.56 |
| Placebo | -60.00 |
Incontinence Episode Frequency (IEF) calculated as the average daily total incontinence episodes (stress or urgency) that occurred during the 3 days prior to randomization and the end of each treatment period. Day 7 mean for each treatment period was calculated as the mean daily episode frequency based on the diary completed in the final three days of each treatment period. (NCT01042236)
Timeframe: Baseline, Day 7 of each period
| Intervention | Percent (Median) |
|---|---|
| Fesoterodine (4 mg) | -66.67 |
| Fesoterodine (8 mg) | -55.56 |
| Placebo | -60.00 |
Opening urethral elastance measured by urethral reflectometry calculated as the mean of each of the opening urethral pressure measurements obtained in triplicate at each time point for each participant. Day 7 mean for each treatment period was calculated as the mean of the three measurements taken post-dose on Day 7 of each treatment period separately. (NCT01042236)
Timeframe: Baseline, Day 7 of each period
| Intervention | cmH2O/millimeter(mm)^2 (Mean) | ||
|---|---|---|---|
| Baseline | Absolue value at Day 7 | Mean Change at Day 7 | |
| Fesoterodine (4 mg) | 1.93 | 1.66 | -0.27 |
| Fesoterodine (8 mg) | 1.93 | 1.85 | -0.08 |
| Placebo | 1.93 | 1.83 | -0.10 |
Incontinence Episode Frequency (IEF) calculated as the average daily total incontinence episodes (stress or urgency) that occurred during the 3 days prior to randomization and the end of each treatment period. Day 7 mean for each treatment period was calculated as the mean daily episode frequency based on the diary completed in the final three days of each treatment period. (NCT01042236)
Timeframe: Baseline, Day 7 of each period
| Intervention | Episodes per 24 hours. (Mean) | ||
|---|---|---|---|
| Baseline | Absolute value at Day 7 | Change at Day 7 | |
| Fesoterodine (4 mg) | 1.52 | 0.71 | -0.81 |
| Fesoterodine (8 mg) | 1.52 | 0.98 | -0.54 |
| Placebo | 1.52 | 0.82 | -0.70 |
Plasma 5-HMT concentration data pre and post reflectometry following multiple doses of fesoterodine 4 mg OD and fesoterodine 8 mg OD. Day 7 mean for each treatment period was calculated as the mean of the three measurements taken post-dose on Day 7 of each treatment period separately. Summary statistics were to be calculated by setting concentration values below the lower limit of quantification (LLQ = 0.02 ng/mL) to zero. Summary statistics were not to be presented if number of observations above lower limit of quantification (NALQ) = 0. (NCT01042236)
Timeframe: Baseline, Day 7 of each period
| Intervention | nanogram/milliliter (ng/mL) (Mean) | |
|---|---|---|
| Pre-Reflectometry (n=18, 18) | Post-Reflectometry (n=18, 17) | |
| Fesoterodine (4 mg) | 2.303 | 2.185 |
| Fesoterodine (8 mg) | 4.902 | 4.971 |
Urgency Urinary Incontinence Component of the daily IEF calculated as the average daily number of urgency leakage episodes that occurred during the 3 days prior to randomization and the end of each treatment period. Day 7 mean for each treatment period was calculated as the mean daily episode frequency based on the diary completed in the final three days of each treatment period. (NCT01042236)
Timeframe: Baseline, Day 7 of each period
| Intervention | Episodes per 24 hours. (Mean) | ||
|---|---|---|---|
| Baseline | Absolute value at Day 7 | Change at Day 7 | |
| Fesoterodine (4 mg) | 0.08 | 0.02 | -0.06 |
| Fesoterodine (8 mg) | 0.08 | 0.00 | -0.08 |
| Placebo | 0.08 | 0.00 | -0.08 |
The mean number of micturition-related urgency episodes per 24 hours was calculated as the total number of micturitions with USS rating of greater than or equal to 3 divided by the total number of days that diary data was collected at that visit. USS total range 1 to 5: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. (NCT01054222)
Timeframe: Baseline, Month 3, 6, 9, 12, 15, 18
| Intervention | episodes per 24 hours (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| Baseline (n= 28) | Month 3 (n= 25) | Month 6 (n= 28) | Month 9 (n= 28) | Month 12 (n= 28) | Month 15 (n= 27) | Month 18 (n= 24) | |
| Fesoterodine | 10.49 | 5.28 | 6.37 | 4.98 | 5.15 | 5.09 | 5.22 |
The mean number of micturition-related urgency episodes per 24 hours was calculated as the total number of micturitions with Urinary Sensation Scale (USS) rating of greater than or equal to (>=) 3 divided by the total number of days that diary data was collected at that visit. USS total range 1 to 5: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. (NCT01054222)
Timeframe: End of Treatment (up to Week 82)
| Intervention | episodes per 24 hours (Mean) |
|---|---|
| Fesoterodine | 5.48 |
UUI episodes were defined as those with the urinary sensation scale (USS) rating of 5 in the diary. USS total range 1 to 5: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. (NCT01054222)
Timeframe: Baseline
| Intervention | Percentage of Participants (Number) |
|---|---|
| Fesoterodine | 58.1 |
OAB-q: self-administered, 33-item, questionnaire, assesses how much participant has been bothered by selected bladder symptoms. Each item rated on Likert scale 1 (least symptom bother) to 6 (most symptom bother). Questions 9 to 33 constitute HRQL, includes domains: concern, coping, sleep, and social function. HRQL domain and total raw score derived as sum of scores. Transformed score range 0 to 100 (Total HRQL or domain) = [(Highest possible raw score-Actual total raw score)/Raw score range]*100. Higher transformed scores indicative of better HRQL. (NCT01054222)
Timeframe: Baseline, Month 3, 6, 9, 12, 15, 18, End of Treatment (Week 82)
| Intervention | units on a scale (Mean) | |||||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Coping Domain: Baseline (n= 28) | Coping Domain: Month 3 (n= 27) | Coping Domain: Month 6 (n= 28) | Coping Domain: Month 9 (n= 28) | Coping Domain: Month 12 (n= 28) | Coping Domain: Month 15 (n= 27) | Coping Domain: Month 18 (n= 24) | Coping Domain: End of Treatment (n= 28) | Concern Domain: Baseline (n= 28) | Concern Domain: Month 3 (n= 27) | Concern Domain: Month 6 (n= 28) | Concern Domain: Month 9 (n= 28) | Concern Domain: Month 12 (n= 28) | Concern Domain: Month 15 (n= 27) | Concern Domain: Month 18 (n= 24) | Concern Domain: End of Treatment (n= 28) | Sleep Domain: Baseline (n= 28) | Sleep Domain: Month 3 (n= 27) | Sleep Domain: Month 6 (n= 28) | Sleep Domain: Month 9 (n= 28) | Sleep Domain: Month 12 (n= 28) | Sleep Domain: Month 15 (n= 27) | Sleep Domain: Month 18 (n= 24) | Sleep Domain: End of Treatment (n= 28) | Social Interaction Domain: Baseline (n= 28) | Social Interaction Domain: Month 3 (n= 27) | Social Interaction Domain: Month 6 (n= 28) | Social Interaction Domain: Month 9 (n= 28) | Social Interaction Domain: Month 12 (n= 28) | Social Interaction Domain: Month 15 (n= 27) | Social Interaction Domain: Month 18 (n= 24) | Social Interaction Domain: End of Treatment (n=28) | Total: Baseline (n= 28) | Total: Month 3 (n= 27) | Total: Month 6 (n= 28) | Total: Month 9 (n= 28) | Total: Month 12 (n= 28) | Total: Month 15 (n= 27) | Total: Month 18 (n= 24) | Total: End of Treatment (n= 28) | |
| Fesoterodine | 77.77 | 78.28 | 77.14 | 79.55 | 76.70 | 74.54 | 79.69 | 79.29 | 71.04 | 72.80 | 70.51 | 74.49 | 71.33 | 69.63 | 72.50 | 72.35 | 71.00 | 73.93 | 73.86 | 77.04 | 74.71 | 73.93 | 74.33 | 73.57 | 90.57 | 88.26 | 87.25 | 87.11 | 84.82 | 84.41 | 86.79 | 86.25 | 77.09 | 77.87 | 76.65 | 79.14 | 76.42 | 75.01 | 78.02 | 77.59 |
KHQ: self-administered questionnaire contained 21 questions scored in 9 domains (general health perception, incontinence impact, role limitations, physical limitations, social limitations, personal relationships, emotions, sleep/energy, and severity of urinary symptoms). Each domain score ranged: 0-100, where 0=best outcome/response and 100=worst outcome/response. (NCT01054222)
Timeframe: Baseline, End of Treatment (EOT) (Week 82)
| Intervention | units on a scale (Mean) | |||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| General Health Perception: Baseline (n=28) | General Health Perception: EOT (n=20) | Incontinence Impact: Baseline (n=27) | Incontinence Impact: EOT (n=20) | Role Limitations: Baseline (n=27) | Role Limitations: EOT (n=20) | Physical Limitations: Baseline (n=27) | Physical Limitations: EOT (n=20) | Social Limitations: Baseline (n=27) | Social Limitations: EOT (n=20) | Personal Relationships: Baseline (n=11) | Personal Relationships: EOT (n=10) | Emotions: Baseline (n=27) | Emotions: EOT (n=20) | Sleep/Energy: Baseline (n=27) | Sleep/Energy: EOT (n=20) | Severity of Urinary Symptoms: Baseline (n=27) | Severity of Urinary Symptoms: EOT (n=20) | |
| Fesoterodine | 43.75 | 38.75 | 50.62 | 41.67 | 31.48 | 35.00 | 37.04 | 34.17 | 13.99 | 20.56 | 1.52 | 11.67 | 35.80 | 32.78 | 34.57 | 35.00 | 44.69 | 42.33 |
Micturitions include episodes of voluntary micturition and episodes of Urgency Urinary Incontinence (UUI). UUI episodes were defined as those micturitions with USS rating of 5 in the diary in participants with UUI at baseline. USS total range 1 to 5: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. (NCT01054222)
Timeframe: Baseline, Month 3, 6, 9, 12, 15, 18, End of Treatment (Week 82)
| Intervention | micturitions per 24 hours (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Baseline (n= 28) | Month 3 (n= 25) | Month 6 (n= 28) | Month 9 (n= 28) | Month 12 (n= 28) | Month 15 (n= 27) | Month 18 (n= 24) | End of Treatment (n= 28) | |
| Fesoterodine | 13.44 | 10.97 | 10.98 | 10.44 | 10.51 | 10.67 | 10.60 | 10.38 |
Nocturnal micturitions were defined as micturitions with USS rating 1-5 that occurred between the time the participant went to bed and the time he or she arose to start the next day. USS rating: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. The mean number of nocturnal micturitions per 24 hours was calculated as the total number of nocturnal micturitions divided by the total number of diary days collected at that visit. (NCT01054222)
Timeframe: Baseline, Month 3, 6, 9, 12, 15, 18, End of Treatment (Week 82)
| Intervention | micturitions per 24 hours (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Baseline (n= 28) | Month 3 (n= 25) | Month 6 (n= 28) | Month 9 (n= 28) | Month 12 (n= 28) | Month 15 (n= 27) | Month 18 (n= 24) | End of Treatment (n= 28) | |
| Fesoterodine | 3.45 | 3.08 | 3.25 | 3.07 | 2.88 | 3.00 | 2.95 | 2.95 |
The mean number of severe micturition-related urgency episodes per 24 hours was calculated as the total number of micturitions with USS rating of greater than or equal to (>=) 4 divided by the total number of days that diary data was collected at that visit. USS total range 1 to 5: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. (NCT01054222)
Timeframe: Baseline, Month 3, 6, 9, 12, 15, 18, End of Treatment (Week 82)
| Intervention | episodes per 24 hours (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Baseline (n= 28) | Month 3 (n= 25) | Month 6 (n= 28) | Month 9 (n= 28) | Month 12 (n= 28) | Month 15 (n= 27) | Month 18 (n= 24) | End of Treatment (n= 28) | |
| Fesoterodine | 6.35 | 3.36 | 2.40 | 2.52 | 2.23 | 2.67 | 2.44 | 2.29 |
UUI episodes were defined as those with the USS rating of 5 in the diary. USS total range 1 to 5: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. (NCT01054222)
Timeframe: Baseline, Month 3, 6, 9, 12, 15, 18, End of Treatment (Week 82)
| Intervention | episodes per 24 hours (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Baseline (n= 28) | Month 3 (n= 25) | Month 6 (n= 28) | Month 9 (n= 28) | Month 12 (n= 28) | Month 15 (n= 27) | Month 18 (n= 24) | End of Treatment (n= 28) | |
| Fesoterodine | 2.64 | 2.27 | 1.54 | 1.36 | 1.29 | 1.83 | 1.65 | 1.49 |
The mean number of urinary incontinence pads (IP), barrier creams (BC) and powder used per 24 hours is calculated as the total number of IP, BC and powder used divided by the total number of diary days collected at that visit. (NCT01054222)
Timeframe: Baseline, Month 3, 6, 9, 12, 15, 18, End of Treatment (Week 82)
| Intervention | Units per 24 hours (Mean) | |||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline: IP (n= 18) | Baseline: BC (n= 18) | Baseline: Powder (n= 18) | Month 3: IP (n= 16) | Month 3: BC (n= 16) | Month 3: Powder (n= 16) | Month 6: IP (n= 18) | Month 6: BC (n= 18) | Month 6: Powder (n= 18) | Month 9: IP (n= 18) | Month 9: BC (n= 18) | Month 9: Powder (n= 18) | Month 12: IP (n= 18) | Month 12: BC (n= 18) | Month 12: Powder (n= 18) | Month 15: IP (n= 17) | Month 15: BC (n= 17) | Month 15: Powder (n= 17) | Month 18: IP (n= 15) | Month 18: BC (n= 15) | Month 18: Powder (n= 15) | End of Treatment: IP (n= 18) | End of Treatment: BC (n= 18) | End of Treatment: Powder (n= 18) | |
| Fesoterodine | 3.69 | 0.48 | 0.24 | 3.15 | 0.79 | 0.19 | 3.02 | 0.43 | 0.20 | 2.56 | 0.33 | 0.17 | 2.52 | 0.13 | 0.31 | 2.45 | 0.18 | 0.00 | 2.49 | 0.18 | 0.00 | 2.31 | 0.15 | 0.00 |
PPBC: self-administered, single-item, questionnaire that asked participants to describe their perception of their bladder-related problems. PPBC assessment rated on a 6-point scale: 1=no problems at all, 2=some very minor problems, 3=some minor problems, 4=moderate problems, 5=severe problems, 6=many severe problems. Change = observation minus baseline. Results categorized as Deterioration (score difference ≥1), No Change (score difference=0), Improvement (score difference less than [<]0). (NCT01054222)
Timeframe: Baseline, Month 3, 6, 9, 12, 15, 18, End of Treatment (Week 82)
| Intervention | Participants (Number) | ||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline: No Problems at all (n= 28) | Baseline: Some Very Minor Problems (n= 28) | Baseline: Some Minor Problems (n= 28) | Baseline: Some Moderate Problems (n= 28) | Baseline: Severe Problems (n= 28) | Baseline: Many Severe Problems (n= 28) | Change at Month 3: Deterioration (n= 27) | Change at Month 3: No Change (n= 27) | Change at Month 3: Improvement (n= 27) | Change at Month 6: Deterioration (n= 28) | Change at Month 6: No Change (n= 28) | Change at Month 6: Improvement (n= 28) | Change at Month 9: Deterioration (n= 28) | Change at Month 9: No Change (n= 28) | Change at Month 9: Improvement (n= 28) | Change at Month 12: Deterioration (n= 28) | Change at Month 12: No Change (n= 28) | Change at Month 12: Improvement (n= 28) | Change at Month 15: Deterioration (n= 27) | Change at Month 15: No Change (n= 27) | Change at Month 15: Improvement (n= 27) | Change at Month 18: Deterioration (n= 24) | Change at Month 18: No Change (n= 24) | Change at Month 18: Improvement (n= 24) | Change at EOT: Deterioration (n= 28) | Change at EOT: No Change (n= 28) | Change at EOT: Improvement (n= 28) | |
| Fesoterodine | 0 | 2 | 11 | 11 | 4 | 0 | 6 | 9 | 12 | 6 | 12 | 10 | 6 | 12 | 10 | 5 | 12 | 11 | 6 | 10 | 11 | 6 | 6 | 12 | 6 | 9 | 13 |
PPUS: self-administered, single-item, questionnaire that measured the participant's perception of urinary urgency. It was sensitive to changes in perceptions of urinary urgency over time. Score of 0 (usually not able to hold urine), 1 (usually able to hold urine [without leaking] until reaching toilet if go to toilet immediately), or 2 (usually able to finish what he/she was doing before going to toilet [without leaking]). Change = observation minus baseline. Deterioration: negative difference of scores; improvement: increase of 1 or more points in difference of scores, relative to baseline. (NCT01054222)
Timeframe: Baseline, Month 3, 6, 9, 12, 15, 18, End of Treatment (Week 82)
| Intervention | Participants (Number) | |||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline: Score 0, Unable to hold urine (n= 28) | Baseline: Score 1, Able to hold urine (n= 28) | Baseline:Score 2,Able to finish ongoing task(n=28) | Change at Month 3: Deterioration (n= 27) | Change at Month 3: No Change (n= 27) | Change at Month 3: Improvement (n= 27) | Change at Month 6: Deterioration (n= 28) | Change at Month 6: No Change (n= 28) | Change at Month 6: Improvement (n= 28) | Change at Month 9: Deterioration (n= 28) | Change at Month 9: No Change (n= 28) | Change at Month 9: Improvement (n= 28) | Change at Month 12: Deterioration (n= 28) | Change at Month 12: No Change (n= 28) | Change at Month 12: Improvement (n= 28) | Change at Month 15: Deterioration (n= 27) | Change at Month 15: No Change (n= 27) | Change at Month 15: Improvement (n= 27) | Change at Month 18: Deterioration (n= 24) | Change at Month 18: No Change (n= 24) | Change at Month 18: Improvement (n= 24) | Change at EOT: Deterioration (n= 28) | Change at EOT: No Change (n= 28) | Change at EOT: Improvement (n= 28) | |
| Fesoterodine | 3 | 12 | 13 | 5 | 17 | 5 | 9 | 13 | 6 | 7 | 19 | 2 | 7 | 17 | 4 | 5 | 19 | 3 | 6 | 12 | 6 | 6 | 16 | 6 |
OAB-q: a self-administered, 33-item, questionnaire that assesses how much the participant has been bothered by selected bladder symptoms. Each item rated by participant on Likert scale 1 (least symptom bother) to 6 (most symptom bother). Symptom bother score derived as sum of scores for questions 1-8; lowest possible raw score: 8; highest possible score: 48. Data analyzed based on transformation of the score to a 0 to 100 scale [(Actual total raw score - lowest possible value of raw score)/range]*100. Higher scores values indicative of greater symptom bother. (NCT01054222)
Timeframe: Baseline, Month 3, 6, 9, 12, 15, 18, End of Treatment (Week 82)
| Intervention | units on a scale (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Baseline (n= 28) | Month 3 (n= 27) | Month 6 (n= 28) | Month 9 (n= 28) | Month 12 (n= 28) | Month 15 (n= 27) | Month 18 (n= 24) | End of Treatment (n= 28) | |
| Fesoterodine | 35.54 | 33.29 | 32.95 | 33.93 | 29.55 | 31.30 | 31.46 | 32.59 |
The daily sum rating was calculated as the mean rating score on the USS multiplied by the mean number of micturitions per 24 hours at that visit. USS total range 1 to 5: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. Numerical decrease indicates improvement. (NCT01054222)
Timeframe: Baseline, Month 3, 6, 9, 12, 15, 18, End of Treatment (Week 82)
| Intervention | Units on a Scale (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Baseline (n= 28) | Month 3 (n= 25) | Month 6 (n= 28) | Month 9 (n= 28) | Month 12 (n= 28) | Month 15 (n= 27) | Month 18 (n= 24) | End of Treatment (n= 28) | |
| Fesoterodine | 45.63 | 31.60 | 31.39 | 28.29 | 27.63 | 28.67 | 29.01 | 28.60 |
UUI episodes were defined as those with the urinary sensation scale (USS) rating of 5 in the diary. USS total range 1 to 5: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. (NCT01054222)
Timeframe: Month 3, 6, 9, 12, 15, 18, End of Treatment (Week 82)
| Intervention | Percentage of Participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Month 3 (n= 16) | Month 6 (n= 18) | Month 9 (n= 18) | Month 12 (n= 18) | Month 15 (n= 17) | Month 18 (n= 15) | End of Treatment (n= 18) | |
| Fesoterodine | 81.3 | 77.8 | 77.8 | 77.8 | 64.7 | 66.7 | 66.7 |
"OAB-s assessed OAB medication expectations, daily life with OAB, and satisfaction with OAB medication. Question (Q) 5 evaluates OAB medication expectations (exceeds/meets or does not meet expectation). Q9 to 11 assessed satisfaction with OAB medication's ability to allow reaching bathroom without urine loss (Q9), decrease: sudden urgencies to urinate (Q10a), urine loss due to urgency (Q10b), waking up at night to urinate (Q10c) and urination during day (Q10d), and improve control of urine loss (Q11a) and need to urinate (Q11b). Q9 to 11 were answered as 'very satisfied', 'somewhat satisfied', 'neither dissatisfied nor satisfied', 'somewhat dissatisfied', and 'very dissatisfied'. The results for Q9 to 11 are reported as satisfied (participants who answered 'very satisfied' or 'somewhat satisfied' for all 7 questions) or not satisfied (participants who answered 'neither dissatisfied nor satisfied' or 'somewhat dissatisfied' or 'very dissatisfied' for all 7 questions)." (NCT01054222)
Timeframe: Baseline, Month 3, 6, 9, 12, 15, 18, End of Treatment (EOT) (Week 82)
| Intervention | participants (Number) | |||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline, Q5: Exceeding/meeting expectations(n=26) | Baseline, Q5: Does not meet expectations (n= 26) | Month 3, Q5: Exceeding/meeting expectations(n=27) | Month 3, Q5: Does not meet expectations (n= 27) | Month 6, Q5: Exceeding/meeting expectations(n=28) | Month 6, Q5: Does not meet expectations (n= 28) | Month 9, Q5: Exceeding/meeting expectations(n=28) | Month 9, Q5: Does not meet expectations (n= 28) | Month 12, Q5: Exceeding/meeting expectations(n=28) | Month 12, Q5: Does not meet expectations (n= 28) | Month 15, Q5: Exceeding/meeting expectations(n=27) | Month 15, Q5: Does not meet expectations (n= 27) | Month 18, Q5: Exceeding/meeting expectations(n=24) | Month 18, Q5: Does not meet expectations (n= 24) | EOT, Q5: Exceeding/meeting expectations(n=28) | EOT, Q5: Does not meet expectations (n= 28) | Baseline; Q9, 10a-10d, 11a-11b: Satisfied (n=27) | Baseline; Q9,10a-10d,11a-11b: Not Satisfied (n=27) | Month 3; Q9, 10a-10d, 11a-11b: Satisfied (n=26) | Month 3; Q9,10a-10d,11a-11b: Not Satisfied (n=26) | Month 6; Q9, 10a-10d, 11a-11b: Satisfied (n=27) | Month 6; Q9,10a-10d,11a-11b: Not Satisfied (n=27) | Month 9; Q9, 10a-10d, 11a-11b: Satisfied (n=27) | Month 9; Q9,10a-10d,11a-11b: Not Satisfied (n=27) | Month 12; Q9, 10a-10d, 11a-11b: Satisfied (n=27) | Month 12; Q9,10a-10d,11a-11b: Not Satisfied (n=27) | Month 15; Q9, 10a-10d, 11a-11b: Satisfied (n=26) | Month 15; Q9,10a-10d,11a-11b: Not Satisfied (n=26) | Month 18; Q9, 10a-10d, 11a-11b: Satisfied (n=24) | Month 18; Q9,10a-10d,11a-11b: Not Satisfied (n=24) | EOT; Q9, 10a-10d, 11a-11b: Satisfied (n=27) | EOT; Q9,10a-10d,11a-11b: Not Satisfied (n=27) | |
| Fesoterodine | 22 | 4 | 22 | 5 | 25 | 3 | 25 | 3 | 24 | 4 | 23 | 4 | 19 | 5 | 23 | 5 | 19 | 8 | 17 | 9 | 15 | 12 | 16 | 11 | 16 | 11 | 17 | 9 | 16 | 8 | 18 | 9 |
"PPBC: single-item, self-administered validated questionnaire. Rated on a 6-point scale: participant was asked: Which of the following statements describes your bladder condition best at the moment? 1=no problems at all; 2=some very minor problems; 3=some minor problems; 4=some moderate problems; 5=severe problems; 6=many severe problems. Change from baseline results categorized as deterioration (Positive change from baseline); no Change (scores change=0); minor Improvement (negative score change in magnitude of 1); major improvement (negative score change in magnitude of >=2)." (NCT01091519)
Timeframe: Baseline, Week 4, Month 4
| Intervention | participants (Number) | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline: No problem at all (n=266, 368) | Baseline: Some very minor problems (n=266, 368) | Baseline: Some minor problems (n=266, 368) | Baseline: Some moderate problems (n=266, 368) | Baseline: Severe problems (n=266, 368) | Baseline: Many severe problems (n=266, 368) | Change at Week 4: Deterioration (n=266, 368) | Change at Week 4: No change (n=266, 368) | Change at Week 4: Minor improvement (n=266, 368) | Change at Week 4: Major improvement (n=266, 368) | Change at Month 4: Deterioration (n=252, 330) | Change at Month 4: No change (n=252, 330) | Change at Month 4: Minor improvement (n=252, 330) | Change at Month 4: Major improvement (n=252, 330) | |
| Fesoterodine With Educational Materials | 1 | 2 | 15 | 75 | 145 | 28 | 12 | 57 | 90 | 107 | 7 | 32 | 49 | 164 |
| Fesoterodine Without Educational Materials | 0 | 3 | 16 | 122 | 179 | 48 | 14 | 93 | 107 | 154 | 4 | 43 | 82 | 201 |
"Participant's response to treatment was based on treatment satisfaction questionnaires (TSQ). Participants answered: overall, how satisfied are you with your OAB medication? and were asked to rate this question on 5 point scale as 1=very satisfied, 2=somewhat satisfied, 3= neither dissatisfied nor satisfied, 4=somewhat dissatisfied and 5=very dissatisfied. Five categorical responses were grouped to satisfied (including very satisfied and somewhat satisfied) and dissatisfied (including very dissatisfied, somewhat dissatisfied, and neither dissatisfied nor satisfied)." (NCT01091519)
Timeframe: Month 4
| Intervention | percentage of participants (Number) |
|---|---|
| Fesoterodine With Educational Materials | 79.6 |
| Fesoterodine Without Educational Materials | 76.1 |
"Participant's response to the treatment was based on treatment satisfaction questionnaires (TSQ). TSQ was rated on a 5-point scale, participant was asked: overall how satisfied are you with your over active bladder (OAB) medication? 1=very satisfied, 2=somewhat satisfied, 3=neither dissatisfied nor satisfied, 4=somewhat dissatisfied, 5=very dissatisfied. Change from baseline results categorized as deterioration (Positive change from baseline);no change (scores change=0);minor improvement (negative score change in magnitude of 1);major improvement (negative score change in magnitude of >=2)." (NCT01091519)
Timeframe: Baseline, Week 4, Month 4
| Intervention | participants (Number) | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline: Very Satisfied (n=144, 203) | Baseline: Somewhat Satisfied (n=144, 203) | Baseline:Neither Dissatisfied/Satisfied(n=144,203) | Baseline: Somewhat Dissatisfied (n=144, 203) | Baseline: Very Dissatisfied (n=144, 203) | Change at Week 4: Deterioration (n=144, 203) | Change at Week 4: No Change (n=144, 203) | Change at Week 4: Minor Improvement (n=144, 203) | Change at Week 4: Major Improvement (n=144, 203) | Change at Month 4: Deterioration (n=143, 179) | Change at Month 4: No Change (n=143, 179) | Change at Month 4: Minor Improvement (n=143, 179) | Change at Month 4: Major Improvement (n=143, 179) | |
| Fesoterodine With Educational Materials | 2 | 20 | 47 | 60 | 15 | 6 | 45 | 42 | 51 | 2 | 33 | 51 | 57 |
| Fesoterodine Without Educational Materials | 4 | 29 | 54 | 95 | 21 | 16 | 56 | 56 | 75 | 10 | 38 | 48 | 83 |
"PPUS: single-item, self-administered validated questionnaire. Rated on a 3-point scale: participant was asked: Which of the following would typically describe your experience when you have a desire to urinate? 1=usually not able to hold urine; 2=usually able to hold urine (without leaking) until I reach a toilet if I go to the toilet immediately; 3= usually able to finish what I am doing before going to the toilet (without leaking). Change from baseline results categorized as deterioration (Negative change); no change (Score change=0); improvement (Positive change)." (NCT01091519)
Timeframe: Baseline, Week 4, Month 4
| Intervention | participants (Number) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Baseline: Usually not able hold urine (n=252, 351) | Baseline: Usually able to hold urine (n=252, 351) | Baseline: Usually able to finish (n=252, 351) | Change at Week 4: Deterioration (n=252, 351) | Change at Week 4: No Change (n=252, 351) | Change at Week 4: Improvement (n=252, 351) | Change at Month 4: Deterioration (n=238, 311) | Change at Month 4: No Change (n=238, 311) | Change at Month 4: Improvement (n=238, 311) | |
| Fesoterodine With Educational Materials | 75 | 157 | 20 | 19 | 130 | 103 | 29 | 85 | 124 |
| Fesoterodine Without Educational Materials | 116 | 186 | 49 | 28 | 174 | 149 | 32 | 109 | 170 |
GMLT: a cognitive test which assessed executive function. Participant was shown a 10 x 10 grid of tiles on a computer touch screen. A 28-step pathway was hidden among 100 possible locations. The participant was instructed to move 1 step from the start location and then continue 1 tile at a time, toward the end to find the pathway. The outcome measure was total number of errors made in attempting to learn the same hidden pathway on 5 consecutive trials at a single session. Lower scores meant a better performance. (NCT01161472)
Timeframe: Baseline
| Intervention | Errors (Mean) |
|---|---|
| Fesoterodine 4 mg | 53.72 |
| Fesoterodine 8 mg | 58.39 |
| Aplrazolam 1 mg | 56.83 |
| Placebo | 52.28 |
GMLT: a cognitive test which assessed executive function. Participant was shown a 10 x 10 grid of tiles on a computer touch screen. A 28-step pathway was hidden among 100 possible locations. The participant was instructed to move 1 step from the start location and then continue 1 tile at a time, toward the end to find the pathway. The outcome measure was total number of errors made in attempting to learn the same hidden pathway on 5 consecutive trials at a single session. Lower scores meant a better performance. (NCT01161472)
Timeframe: Baseline and Day 6
| Intervention | Errors (Least Squares Mean) |
|---|---|
| Fesoterodine 4 mg | -4.1399 |
| Fesoterodine 8 mg | -5.7717 |
| Aplrazolam 1 mg | 24.7115 |
| Placebo | -4.1467 |
One card learning: a cognitive test which assessed visual learning. Participants were to remember which cards were previously shown in a task. The outcome measure was accuracy of performance; arcsine transformation of the square root (sqrt) of the proportion of correct responses. Higher scores meant a better performance. (NCT01161472)
Timeframe: Baseline and Day 6
| Intervention | Arcsine [(sqrt) proportion correct] (Least Squares Mean) |
|---|---|
| Fesoterodine 4 mg | -0.0094 |
| Fesoterodine 8 mg | 0.0151 |
| Aplrazolam 1 mg | -0.0880 |
| Placebo | -0.0058 |
CPAL: a cognitive test which assessed visual episodic learning. Participant was to learn and remember picture locations on the screen and was to tap the target on the central location to begin. As each picture was revealed, the participant was to remember where the picture was located and tap that location. The outcome measure was the number of errors made in correctly placing each of the 4 patterns in their location 4 times. Lower scores meant a better performance. (NCT01161472)
Timeframe: Baseline and Day 6
| Intervention | Errors (Least Squares Mean) |
|---|---|
| Fesoterodine 4 mg | 6.7933 |
| Fesoterodine 8 mg | -16.7905 |
| Aplrazolam 1 mg | 58.2002 |
| Placebo | 3.1304 |
Detection speed: a cognitive test which assessed psychomotor function. A playing card was presented face up in the center of the screen. As soon as this happened, the participant was to press the 'Yes' key. The outcome measure was speed of performance; mean of the log10 transformed reaction time for correct responses [measured in log10 milliseconds (MS)]. Lower scores meant a better performance. (NCT01161472)
Timeframe: Baseline and Day 6
| Intervention | Log10 MS (Least Squares Mean) |
|---|---|
| Fesoterodine 4 mg | -0.0201 |
| Fesoterodine 8 mg | -0.0119 |
| Aplrazolam 1 mg | 0.0684 |
| Placebo | 0.0084 |
CPAL: a cognitive test which assessed visual episodic learning. Participant was to learn and remember picture locations on the screen and was to tap the target on the central location to begin. As each picture was revealed, the participant was to remember where the picture was located and tap that location. The outcome measure was the number of errors made in correctly placing each of the 4 patterns in their location 4 times. Lower scores meant a better performance. (NCT01161472)
Timeframe: Baseline
| Intervention | Errors (Mean) |
|---|---|
| Fesoterodine 4 mg | 96.33 |
| Fesoterodine 8 mg | 99.83 |
| Aplrazolam 1 mg | 89.50 |
| Placebo | 107.44 |
Identification speed: a cognitive test which assessed visual attention. A playing card was presented face up in the center of the screen. As soon as this happened, the participant had to decide whether the card was red or not. The outcome measure was speed of performance; mean of the log10 transformed reaction time for correct responses (measured in log10 MS). Lower scores meant a better performance. (NCT01161472)
Timeframe: Baseline
| Intervention | Log10 MS (Mean) |
|---|---|
| Fesoterodine 4 mg | 2.7540 |
| Fesoterodine 8 mg | 2.7672 |
| Aplrazolam 1 mg | 2.7577 |
| Placebo | 2.7457 |
Identification speed: a cognitive test which assessed visual attention. A playing card was presented face up in the center of the screen. As soon as this happened, the participant had to decide whether the card was red or not. The outcome measure was speed of performance; mean of the log10 transformed reaction time for correct responses (measured in log10 MS). Lower scores meant a better performance. (NCT01161472)
Timeframe: Baseline and Day 6
| Intervention | Log10 MS (Least Squares Mean) |
|---|---|
| Fesoterodine 4 mg | 0.0105 |
| Fesoterodine 8 mg | 0.0057 |
| Aplrazolam 1 mg | 0.0817 |
| Placebo | 0.0142 |
RAVLT evaluates a wide diversity of functions: short-term auditory-verbal memory, rate of learning, learning strategies, retroactive, and proactive interference, presence of confabulation of confusion in memory processes, retention of information, and differences between learning and retrieval. Assessment of RAVLT is between 10 to 15 minutes; Performance variable: the sum of the number of words recalled successfully on the delayed recall trial. Higher score meant a better performance. (NCT01161472)
Timeframe: Baseline
| Intervention | Words Recalled (Mean) |
|---|---|
| Fesoterodine 4 mg | 6.50 |
| Fesoterodine 8 mg | 6.67 |
| Aplrazolam 1 mg | 7.22 |
| Placebo | 6.33 |
RAVLT evaluates a wide diversity of functions: short-term auditory-verbal memory, rate of learning, learning strategies, retroactive, and proactive interference, presence of confabulation of confusion in memory processes, retention of information, and differences between learning and retrieval. Assessment of RAVLT is between 10 to 15 minutes; Performance variable: the sum of the number of words recalled successfully on the delayed recall trial. Higher score meant a better performance. (NCT01161472)
Timeframe: Baseline and Day 6
| Intervention | Words Recalled (Least Squares Mean) |
|---|---|
| Fesoterodine 4 mg | 0.1565 |
| Fesoterodine 8 mg | -0.1780 |
| Aplrazolam 1 mg | -3.9222 |
| Placebo | -0.1119 |
Detection speed: a cognitive test which assessed psychomotor function. A playing card was presented face up in the center of the screen. As soon as this happened, the participant was to press the 'Yes' key. The outcome measure was speed of performance; mean of the log10 transformed reaction time for correct responses [measured in log10 milliseconds (MS)]. Lower scores meant a better performance. (NCT01161472)
Timeframe: Baseline
| Intervention | Log10 MS (Mean) |
|---|---|
| Fesoterodine 4 mg | 2.6333 |
| Fesoterodine 8 mg | 2.5971 |
| Aplrazolam 1 mg | 2.6103 |
| Placebo | 2.5842 |
One card learning: a cognitive test which assessed visual learning. Participants were to remember which cards were previously shown in a task. The outcome measure was accuracy of performance; arcsine transformation of the square root (sqrt) of the proportion of correct responses. Higher scores meant a better performance. (NCT01161472)
Timeframe: Baseline
| Intervention | Arcsine [(sqrt) proportion correct] (Mean) |
|---|---|
| Fesoterodine 4 mg | 0.9585 |
| Fesoterodine 8 mg | 0.9421 |
| Aplrazolam 1 mg | 0.9531 |
| Placebo | 0.9302 |
Counts of participants who had treatment-emergent AEs (TEAEs), defined as newly occurring or worsening after first dose. Relatedness to fesoterodine fumarate (Toviaz) was assessed by the investigator. Participants with multiple occurrences of an AE within a category were counted once within the category. Seriousness of an AE was assessed under the criteria of serious adverse event (SAE). AE was assessed according to severity; mild (not causing any significant problem, dose adjustment not required), moderate (caused problem that does not interfere significantly with usual activities or the clinical status, dose adjustment needed due to AE) and severe (caused problem that interferes significantly with usual activities or the clinical status, study drug stopped due to AE). (NCT01260311)
Timeframe: Baseline up to 28 days after last dose
| Intervention | participants (Number) | |||||
|---|---|---|---|---|---|---|
| Participants with AEs, all-causality | Participants with AEs, treatment-related | Participants with serious AEs, all-causality | Participants with serious AEs, treatment-related | Participants with severe AEs, all-causality | Participants with severe AEs, treatment-related | |
| Fesoterodine Fumarate | 21 | 19 | 0 | 0 | 2 | 2 |
(NCT01286454)
Timeframe: 0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 15, 24, 30, 36 and 48 hrs post dose
| Intervention | ng/mL (Geometric Mean) |
|---|---|
| Fesoterodine 4 mg IR-BIC Fasted | 5.830 |
| Fesoterodine 4 mg 10% ER-BIC Fasted | 3.030 |
| Fesoterodine 4 mg 15% ER-BIC Fasted | 1.092 |
| Fesoterodine 4 mg 20% ER-BIC Fasted | 0.323 |
| Fesoterodine 4 mg ER Tablet Fasted | 2.247 |
| Fesoterodine 4 mg 10% ER-BIC Fed | 5.183 |
Plasma decay half-life is the time measured for the plasma concentration to decrease by one half. (NCT01286454)
Timeframe: 0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 15, 24, 30, 36 and 48 hrs post dose
| Intervention | hr (Mean) |
|---|---|
| Fesoterodine 4 mg IR-BIC Fasted | 5.56 |
| Fesoterodine 4 mg 10% ER-BIC Fasted | 7.22 |
| Fesoterodine 4 mg 15% ER-BIC Fasted | 10.89 |
| Fesoterodine 4 mg 20% ER-BIC Fasted | NA |
| Fesoterodine 4 mg ER Tablet Fasted | 7.54 |
| Fesoterodine 4 mg 10% ER-BIC Fed | 4.59 |
(NCT01286454)
Timeframe: 0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 15, 24, 30, 36 and 48 hrs post dose
| Intervention | hr (Median) |
|---|---|
| Fesoterodine 4 mg IR-BIC Fasted | 1.0 |
| Fesoterodine 4 mg 10% ER-BIC Fasted | 6.0 |
| Fesoterodine 4 mg 15% ER-BIC Fasted | 6.0 |
| Fesoterodine 4 mg 20% ER-BIC Fasted | 8.0 |
| Fesoterodine 4 mg ER Tablet Fasted | 5.0 |
| Fesoterodine 4 mg 10% ER-BIC Fed | 4.0 |
AUC (0 - ∞) = Area under the plasma concentration versus time curve (AUC) from time zero to extrapolated infinite time (0 - ∞). It is obtained from AUC (0 - t) plus AUC (t - ∞). (NCT01286454)
Timeframe: 0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 15, 24, 30, 36 and 48 hours (hrs) post dose
| Intervention | ng*hr/mL (Geometric Mean) |
|---|---|
| Fesoterodine 4 mg IR-BIC Fasted | 30.48 |
| Fesoterodine 4 mg 10% ER-BIC Fasted | 28.24 |
| Fesoterodine 4 mg 15% ER-BIC Fasted | 19.64 |
| Fesoterodine 4 mg 20% ER-BIC Fasted | NA |
| Fesoterodine 4 mg ER Tablet Fasted | 27.40 |
| Fesoterodine 4 mg 10% ER-BIC Fed | 32.07 |
Area under the plasma concentration time-curve from zero to the last measured concentration (AUClast) of 5-HMT. (NCT01286454)
Timeframe: 0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 15, 24, 30, 36 and 48 hrs post dose
| Intervention | ng*hr/mL (Geometric Mean) |
|---|---|
| Fesoterodine 4 mg IR-BIC Fasted | 30.23 |
| Fesoterodine 4 mg 10% ER-BIC Fasted | 27.79 |
| Fesoterodine 4 mg 15% ER-BIC Fasted | 17.92 |
| Fesoterodine 4 mg 20% ER-BIC Fasted | 7.59 |
| Fesoterodine 4 mg ER Tablet Fasted | 26.80 |
| Fesoterodine 4 mg 10% ER-BIC Fed | 31.88 |
UUI episodes were defined as those with the urinary sensation scale (USS) rating of 5 in the diary. USS range from 1 to 5: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. (NCT01302054)
Timeframe: Baseline, Week 12
| Intervention | episodes per 24 hours (Mean) | |
|---|---|---|
| Baseline | Change at Week 12 | |
| Fesoterodine | 3.93 | -2.32 |
| Placebo | 3.83 | -1.76 |
UUI episodes were defined as those with the urinary sensation scale (USS) rating of 5 in the diary. USS range from 1 to 5: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. (NCT01302054)
Timeframe: Week 4, Week 12
| Intervention | percentage of participants (Number) | |
|---|---|---|
| Week 4 | Week 12 | |
| Fesoterodine | 25.4 | 39.0 |
| Placebo | 17.7 | 32.3 |
"UPS: single-item, self-administered validated questionnaire. Participant answered: Which of the following would typically describe your experience when you have a desire to urinate? on a 3-point scale, 1=usually not able to hold urine; 2=usually able to hold urine (without leaking) until I reach a toilet if I go to the toilet immediately; 3= usually able to finish what I am doing before going to the toilet (without leaking). Change = observation minus baseline. Results categorized as Deterioration (Negative change); no change (Score change=0); improvement (Positive change)." (NCT01302054)
Timeframe: Baseline, Week 12
| Intervention | participants (Number) | |||||
|---|---|---|---|---|---|---|
| Baseline: Not able to hold urine | Baseline:Able to hold urine until I reach a toilet | Baseline:Able to finish what I am doing | Change at Week 12: Deterioration | Change at Week 12: No Change | Change at Week 12: Improvement | |
| Fesoterodine | 126 | 158 | 7 | 17 | 167 | 107 |
| Placebo | 99 | 157 | 11 | 31 | 158 | 78 |
UUI episodes were defined as those with the urinary sensation scale (USS) rating of 5 in the diary. USS range from 1 to 5: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. (NCT01302054)
Timeframe: Baseline, Week 12
| Intervention | episodes per 24 hours (Mean) |
|---|---|
| Fesoterodine: Double-Blind Baseline | 3.93 |
| Fesoterodine: Double-Blind Week 12 | 1.60 |
UUI episodes were defined as those with the urinary sensation scale (USS) rating of 5 in the diary. USS range from 1 to 5: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. (NCT01302054)
Timeframe: Baseline, Week 12
| Intervention | percentage of participants (Number) |
|---|---|
| Fesoterodine | 69.9 |
| Placebo | 57.0 |
UUI episodes were defined as those with the urinary sensation scale (USS) rating of 5 in the diary. USS range from 1 to 5: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. (NCT01302054)
Timeframe: Week -2, Week 12
| Intervention | percentage of participants (Number) |
|---|---|
| Fesoterodine | 72.8 |
| Placebo | 59.6 |
OAB-q: self-administered, 33-item, questionnaire, assesses how much participant has been bothered by selected bladder symptoms. Each item rated on Likert scale 1 (not at all) to 6 (a very great deal). Questions 9 to 33 constitute HRQL, includes domains: concern, coping, sleep, and social function. HRQL domain and total raw score derived as sum of scores. Transformed score range 0 to 100 (Total HRQL or domain) = [(Highest possible raw score-Actual total raw score)/Raw score range]*100. Higher transformed scores indicative of better HRQL. (NCT01302054)
Timeframe: Baseline, Week 12
| Intervention | units on a scale (Mean) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Concern Subscale: Baseline | Concern Subscale: Change at Week 12 | Coping Subscale: Baseline | Coping Subscale: Change at Week 12 | Sleep Subscale: Baseline | Sleep Subscale: Change at Week 12 | Social Interaction Subscale: Baseline | Social Interaction Subscale: Change at Week 12 | Total HRQL Score: Baseline | Total HRQL Score: Change at Week 12 | |
| Fesoterodine | 43.63 | 23.11 | 38.74 | 23.70 | 41.38 | 20.85 | 65.03 | 14.47 | 45.90 | 21.12 |
| Placebo | 44.25 | 13.83 | 41.15 | 15.07 | 40.69 | 14.79 | 68.40 | 8.85 | 47.38 | 13.42 |
The mean number of micturition-related urgency episodes per 24 hours was calculated as the total number of micturitions with USS rating of greater than or equal to 3 divided by the total number of days that diary data was collected at that visit. USS range from 1 to 5: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. (NCT01302054)
Timeframe: Baseline, Week 12
| Intervention | episodes per 24 hours (Mean) | |
|---|---|---|
| Baseline | Change at Week 12 | |
| Fesoterodine | 11.38 | -3.33 |
| Placebo | 11.26 | -2.52 |
"PPBC: single-item, self-administered validated questionnaire. Participant answered: Which of the following statements describes your bladder condition best at the moment? on a 6-point scale, 1=no problems at all; 2=some very minor problems; 3=some minor problems; 4=some moderate problems; 5=severe problems; 6=many severe problems. Change=observation minus baseline. Results categorized as Deterioration (Positive change from baseline); No Change (scores change=0); Minor Improvement (negative score change in magnitude of 1); Major Improvement (negative score change in magnitude of >=2)." (NCT01302054)
Timeframe: Baseline, Week 12
| Intervention | participants (Number) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Baseline: No Problems at all | Baseline: Some Very Minor Problems | Baseline: Some Minor Problems | Baseline: Some Moderate Problems | Baseline: Severe Problems | Baseline: Many Severe Problems | Change at Week 12: Deterioration | Change at Week 12: No Change | Change at Week 12: Minor Improvement | Change at Week 12: Major Improvement | |
| Fesoterodine | 0 | 4 | 15 | 60 | 147 | 65 | 17 | 80 | 84 | 110 |
| Placebo | 0 | 6 | 9 | 75 | 141 | 36 | 32 | 95 | 83 | 57 |
OAB-q: a self-administered, 33-item, questionnaire that assesses how much the participant has been bothered by selected bladder symptoms. Each item rated by participant on Likert scale 1 (not at all) to 6 (a very great deal). Symptom bother score derived as sum of scores for questions 1-8; lowest possible raw score: 8; highest possible score: 48. Data analyzed based on transformation of the score to a 0 to 100 scale [(Actual total raw score - lowest possible value of raw score)/range]*100. Higher scores values indicative of greater symptom bother. Change=observation minus baseline. (NCT01302054)
Timeframe: Baseline, Week 12
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Baseline | Change at Week 12 | |
| Fesoterodine | 66.67 | -24.61 |
| Placebo | 64.74 | -15.99 |
Micturitions include episodes of voluntary micturition and episodes of Urgency Urinary Incontinence (UUI). UUI episodes were defined as those micturitions with USS rating of 5 in the diary in participants with UUI at baseline. USS rating 5: Unable to hold; leak urine. (NCT01302054)
Timeframe: Baseline, Week 12
| Intervention | micturitions per 24 hours (Mean) | |
|---|---|---|
| Baseline | Change at Week 12 | |
| Fesoterodine | 12.44 | -1.94 |
| Placebo | 12.48 | -1.57 |
"UPS: single-item, self-administered validated questionnaire. Participant answered: Which of the following would typically describe your experience when you have a desire to urinate? on a 3-point scale, 1=usually not able to hold urine; 2=usually able to hold urine (without leaking) until I reach a toilet if I go to the toilet immediately; 3= usually able to finish what I am doing before going to the toilet (without leaking). Change = observation minus baseline. Results categorized as Deterioration (Negative change); no change (Score change=0); improvement (Positive change)." (NCT01302067)
Timeframe: Week 12
| Intervention | Participants (Number) | ||
|---|---|---|---|
| Deterioration | No change | Improvement | |
| Fesoterodine 4 Milligram (mg) | 37 | 361 | 302 |
| Fesoterodine 8 mg | 30 | 305 | 342 |
| Placebo | 23 | 193 | 132 |
PPBC: a self-administered, single-item, questionnaire that asks participants to describe their perception of their bladder-related problems. The PPBC assessment is rated on a 6-point scale: 1=no problems at all, 2=some very minor problems, 3=some minor problems, 4=moderate problems, 5=severe problems, 6=many severe problems. Improvement is defined as negative change from baseline. (NCT01302067)
Timeframe: Week 12
| Intervention | Participants (Number) | |||
|---|---|---|---|---|
| Deterioration | No Change | Minor improvement | Major improvement | |
| Fesoterodine 4 Milligram (mg) | 38 | 172 | 210 | 280 |
| Fesoterodine 8 mg | 27 | 151 | 170 | 329 |
| Placebo | 25 | 122 | 105 | 96 |
Percentage of participants with no UUI episode for the three day diary, the numerator being the number of participants with no UUI at a visit and the denominator the total number of participants with UUI>0 at baseline. UUI episodes defined as those with USS rating of 5 (unable to hold; leak urine) in the diary (NCT01302067)
Timeframe: Week 4
| Intervention | Percentage of participants (Number) |
|---|---|
| Fesoterodine 4 Milligram (mg) | 35.5 |
| Placebo | 26.4 |
| Fesoterodine 8 mg | 36.2 |
Percentage of participants with no UUI episode for the three day diary, the numerator being the number of participants with no UUI at a visit and the denominator the total number of participants with UUI >0 at baseline. UUI episodes defined as those with USS rating of 5 (unable to hold; leak urine) in the diary. (NCT01302067)
Timeframe: Week 12
| Intervention | Percentage of participants (Number) |
|---|---|
| Fesoterodine 4 Milligram (mg) | 49.2 |
| Placebo | 39.5 |
| Fesoterodine 8 mg | 57.8 |
UUI episodes were defined as those with the USS rating of 5 in the diary. USS total range 1 to 5: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. (NCT01302067)
Timeframe: Week 4
| Intervention | Episodes per 24 hours (Median) |
|---|---|
| Fesoterodine 4 Milligram (mg) | -77.78 |
| Placebo | -60.50 |
| Fesoterodine 8 mg | -82.48 |
UUI episodes were defined as those with the USS rating of 5 in the diary. USS total range 1 to 5: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. (NCT01302067)
Timeframe: Week 12
| Intervention | Episodes per 24 hours (Median) |
|---|---|
| Fesoterodine 4 Milligram (mg) | -93.75 |
| Placebo | -78.89 |
| Fesoterodine 8 mg | -100.00 |
Micturitions include episodes of voluntary micturition and episodes of UUI. (NCT01302067)
Timeframe: Week 4
| Intervention | Episodes per 24 hours (Median) |
|---|---|
| Fesoterodine 4 Milligram (mg) | -14.58 |
| Placebo | -9.01 |
| Fesoterodine 8 mg | -17.24 |
Micturitions include episodes of voluntary micturition and episodes of UUI. (NCT01302067)
Timeframe: Week 12
| Intervention | Episodes per 24 hours (Median) |
|---|---|
| Fesoterodine 4 Milligram (mg) | -19.74 |
| Placebo | -12.16 |
| Fesoterodine 8 mg | -24.14 |
The mean number of micturition-related urgency episodes per 24 hours was calculated as the total number of micturitions with USS rating of greater than or equal to (>=) 3 divided by the total number of days that diary data was collected at that visit. USS total range 1 to 5: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. (NCT01302067)
Timeframe: Week 4
| Intervention | Participant (Median) |
|---|---|
| Fesoterodine 4 Milligram (mg) | -23.26 |
| Placebo | -14.70 |
| Fesoterodine 8 mg | -27.27 |
The mean number of micturition-related urgency episodes per 24 hours was calculated as the total number of micturitions with USS rating of greater than or equal to (>=) 3 divided by the total number of days that diary data was collected at that visit. USS total range 1 to 5: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. (NCT01302067)
Timeframe: Week 12
| Intervention | Participant (Median) |
|---|---|
| Fesoterodine 4 Milligram (mg) | -34.88 |
| Placebo | -22.73 |
| Fesoterodine 8 mg | -44.29 |
The mean number of micturition-related urgency episodes per 24 hours was calculated as the total number of micturitions with USS rating of greater than or equal to (>=) 3 divided by the total number of days that diary data was collected at that visit. USS total range 1 to 5: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. (NCT01302067)
Timeframe: Week 4
| Intervention | Episodes per 24 hours (Least Squares Mean) |
|---|---|
| Fesoterodine 4 Milligram (mg) | -2.89 |
| Placebo | -1.85 |
| Fesoterodine 8 mg | -3.40 |
The mean number of micturition-related urgency episodes per 24 hours was calculated as the total number of micturitions with USS rating of greater than or equal to (>=) 3 divided by the total number of days that diary data was collected at that visit. USS total range 1 to 5: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. (NCT01302067)
Timeframe: Week 12
| Intervention | Episodes per 24 hours (Least Squares Mean) |
|---|---|
| Fesoterodine 4 Milligram (mg) | -4.23 |
| Placebo | -2.99 |
| Fesoterodine 8 mg | -5.01 |
OAB-q: self-administered, 33-item, questionnaire, assesses how much participant has been bothered by selected bladder symptoms. Each item rated on Likert scale 1 (not at all) to 6 (a very great deal). Questions 9 to 33 constitute HRQL, includes domains: concern, coping, sleep, and social function. HRQL domain and total raw score derived as sum of scores. Transformed score range 0 to 100 (Total HRQL or domain) = [(Highest possible raw score-Actual total raw score)/Raw score range]*100. Higher transformed scores indicative of better HRQL. (NCT01302067)
Timeframe: Week 12
| Intervention | Scores on a scale (Least Squares Mean) |
|---|---|
| Fesoterodine 4 Milligram (mg) | 23.70 |
| Placebo | 18.57 |
| Fesoterodine 8 mg | 27.94 |
OAB-q: self-administered, 33-item, questionnaire, assesses how much participant has been bothered by selected bladder symptoms. Each item rated on Likert scale 1 (not at all) to 6 (a very great deal). Questions 9 to 33 constitute HRQL, includes domains: concern, coping, sleep, and social function. HRQL domain and total raw score derived as sum of scores. Transformed score range 0 to 100 (Total HRQL or domain) = [(Highest possible raw score-Actual total raw score)/Raw score range]*100. Higher transformed scores indicative of better HRQL. (NCT01302067)
Timeframe: Week 12
| Intervention | Scores on a scale (Least Squares Mean) |
|---|---|
| Fesoterodine 4 Milligram (mg) | 16.43 |
| Placebo | 12.61 |
| Fesoterodine 8 mg | 20.11 |
OAB-q: self-administered, 33-item, questionnaire, assesses how much participant has been bothered by selected bladder symptoms. Each item rated on Likert scale 1 (not at all) to 6 (a very great deal). Questions 9 to 33 constitute HRQL, includes domains: concern, coping, sleep, and social function. HRQL domain and total raw score derived as sum of scores. Transformed score range 0 to 100 (Total HRQL or domain) = [(Highest possible raw score-Actual total raw score)/Raw score range]*100. Higher transformed scores indicative of better HRQL. (NCT01302067)
Timeframe: Week 12
| Intervention | Scores on a scale (Least Squares Mean) |
|---|---|
| Fesoterodine 4 Milligram (mg) | 21.97 |
| Placebo | 18.25 |
| Fesoterodine 8 mg | 25.71 |
OAB-q: self-administered, 33-item, questionnaire, assesses how much participant has been bothered by selected bladder symptoms. Each item rated on Likert scale 1 (not at all) to 6 (a very great deal). Questions 9 to 33 constitute HRQL, includes domains: concern, coping, sleep, and social function. HRQL domain and total raw score derived as sum of scores. Transformed score range 0 to 100 (Total HRQL or domain) = [(Highest possible raw score-Actual total raw score)/Raw score range]*100. Higher transformed scores indicative of better HRQL. (NCT01302067)
Timeframe: Week 12
| Intervention | Scores on a scale (Least Squares Mean) |
|---|---|
| Fesoterodine 4 Milligram (mg) | 26.69 |
| Placebo | 20.91 |
| Fesoterodine 8 mg | 31.38 |
OAB-q: self-administered, 33-item, questionnaire, assesses how much participant has been bothered by selected bladder symptoms. Each item rated on Likert scale 1 (not at all) to 6 (a very great deal). Questions 9 to 33 constitute HRQL, includes domains: concern, coping, sleep, and social function. HRQL domain and total raw score derived as sum of scores. Transformed score range 0 to 100 (Total HRQL or domain) = [(Highest possible raw score-Actual total raw score)/Raw score range]*100. Higher transformed scores indicative of better HRQL. (NCT01302067)
Timeframe: Week 12
| Intervention | Scores on a scale (Least Squares Mean) |
|---|---|
| Fesoterodine 4 Milligram (mg) | 26.82 |
| Placebo | 20.27 |
| Fesoterodine 8 mg | 31.18 |
UUI episodes were defined as those with the USS rating of 5 in the diary. USS total range 1 to 5: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. (NCT01302067)
Timeframe: Week 4
| Intervention | Episodes per 24 hours (Least Squares Mean) |
|---|---|
| Fesoterodine 4 Milligram (mg) | -2.55 |
| Placebo | -1.99 |
| Fesoterodine 8 mg | -2.75 |
UUI episodes were defined as those with the Urinary Sensation Scale (USS) rating of 5 in the diary. USS total range 1 to 5: 1. No feeling of urgency, 2. Mild feeling of urgency, 3. Moderate feeling of urgency, 4. Severe feeling of urgency, 5. Unable to hold; leak urine. (NCT01302067)
Timeframe: Week 12
| Intervention | Episodes per 24 hours (Least Squares Mean) |
|---|---|
| Fesoterodine 4 Milligram (mg) | -2.85 |
| Placebo | -2.22 |
| Fesoterodine 8 mg | -3.12 |
Micturitions include episodes of voluntary micturition and episodes of UUI. (NCT01302067)
Timeframe: Week 4
| Intervention | Episodes per 24 hours (Least Squares Mean) |
|---|---|
| Fesoterodine 4 Milligram (mg) | -1.95 |
| Placebo | -1.19 |
| Fesoterodine 8 mg | -2.33 |
Micturitions include episodes of voluntary micturition and episodes of UUI. (NCT01302067)
Timeframe: Week 12
| Intervention | Episodes per 24 hours (Least Squares Mean) |
|---|---|
| Fesoterodine 4 Milligram (mg) | -2.45 |
| Placebo | -1.58 |
| Fesoterodine 8 mg | -2.97 |
OAB-q: a self-administered, 33-item, questionnaire that assesses how much the participant has been bothered by selected bladder symptoms. Each item rated by participant on Likert scale 1 (not at all) to 6 (a very great deal). Symptom bother score derived as sum of scores for questions 1-8; lowest possible raw score: 8; highest possible score: 48. Data analyzed based on transformation of the score to a 0 to 100 scale [(Actual total raw score - lowest possible value of raw score)/range]*100. Higher scores values indicative of greater symptom bother. (NCT01302067)
Timeframe: Week 12
| Intervention | Scores on a scale (Least Squares Mean) |
|---|---|
| Fesoterodine 4 Milligram (mg) | -30.19 |
| Placebo | -22.41 |
| Fesoterodine 8 mg | -34.88 |
Overactive Bladder subjects answered the Overactive Bladder Questionnaire (OAB-q) before starting Fesoterodine and at the end of taking 6 weeks of Fesoterodine. The OAB-q consists of 8 questions asking how bothered subject was in the past 4 weeks. Questions # 1 (Frequent urination during the daytime hours?); #5 (Nighttime urination?) and #6 (Waking up at night because you have to urinate?) are asking about frequency. Choices of answers are: 1 (Not at all); 2 (A little bit); 3 (Somewhat); 4 (Quite a bit); 5 (A great deal) 6 (A very great deal). Multiple responses to the questionnaire were averaged for each participant at baseline and at 6 weeks and then all participants' answers were totaled and averaged at baseline and at 6 weeks. (NCT01367886)
Timeframe: Outcome measure was assessed at baseline and after the 6 week visit.
| Intervention | scores on a scale (Mean) | |
|---|---|---|
| OAB-q to assess bother from frequency at baseline | OAB-q to assess bother from frequency at 6 weeks | |
| Fesoterodine | 4.89 | 3.50 |
Overactive bladder subjects answered the Overactive Bladder questionnaire (OAB-q) before starting Fesoterodine and at the end of taking 6 weeks of Fesoterodine. The OAB-q consists of 8 questions asking how bothered subject was in the past 4 weeks. Questions #2 (An uncomfortable urge to urinate?); #3 (A sudden urge to urinate with little or no warning?); #4 (Accidental loss of small amounts of urine?); #7 (An uncontrollable urge to urinate?); #8 (Urine loss associated with a strong desire to urinate?) are asking about urgency. Choices for answers are: 1 (Not at all); 2 (A little bit); 3 (Somewhat); 4 (Quite a bit); 5 (A great deal); 6 (A very great deal). Multiple responses to the questionnaire was averaged per participant at baseline and at 6 weeks and then all participants answers were totaled and then averaged at baseline and at 6 weeks. (NCT01367886)
Timeframe: Outcome measures were assessed at baseline and after the 6 week visit.
| Intervention | scores on a scale (Mean) | |
|---|---|---|
| OAB-q to measure bother from urgency at baseline | OAB-q to measure bther from urgency at 6 weeks | |
| Fesoterodine | 4.52 | 3.14 |
The Urinary Sensation Scale found in the bladder diary given to subjects was used to assess urinary urgency. The Urinary Sensation Scale was filled out by the subject for 3 days before starting Fesoterodine and filled out again for 3 days at the end of taking 6 weeks of Fesoterodine. The scale ranges from 1 (no feeling of urgency), 2 (mild), 3 (moderate), 4 (severe) to 5 (unable to hold; leak urine). The urgency scale with the most check marks per day over a period of 3 days before start of medication was averaged for each subject. The urgency scale with the most check marks per day over a period of 3 days at the end of taking 6 weeks of medication was averaged for each subject. Then, the average before start of medication for all subjects and the average at the end of taking 6 weeks of medication for all subjects were compared. (NCT01367886)
Timeframe: Outcome measure was assesses at baseline and at the end of the 6-week treatment period.
| Intervention | scores on Urinary Sensation Scale (Mean) | |
|---|---|---|
| USS to assess baseline urgency | USS to assess 6 week urgency | |
| Fesoterodine | 2.84 | 2.50 |
Overactive bladder subjects filled out a 3-day bladder diary before starting Fesoterodine and another 3-day bladder diary at the end of taking 6 weeks of Fesoterodine. The bladder diary was used to assess urinary frequency. The average number of urinations (frequency) per day over a period of 3 days before the start of medication and at the end of 6 weeks of medication were compared for each subject and then as a group. (NCT01367886)
Timeframe: Outcome measure was assessed at baseline and at the end of the 6-week treatment
| Intervention | urinations/day (Mean) | |
|---|---|---|
| Average number of urinations/day after 6 weeks | Average number of urinations/day at baseline | |
| Fesoterodine | 12.32 | 10.79 |
Maximum cystometric bladder capacity (in milliliter) was defined as maximal tolerable cystometric capacity, until voiding or leaking begins or at a pressure of >=40 centimeter (cm) water (H2O). (NCT01557244)
Timeframe: Baseline, Week 12
| Intervention | milliliter (Least Squares Mean) |
|---|---|
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg | 58.12 |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg Then 8 mg | 83.36 |
| Cohort 1, Active Comparator Phase: Oxybutynin | 87.17 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg | 23.49 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg Then 4 mg | 40.17 |
The mean number of catheterizations per 24 hours were calculated as the total number of catheterizations divided by the total number of diary days collected at the assessment time point. Number of diary days collected at the assessment time point = number of calendar days when the diary was completed on; even if it was not a full 24 hours period. This outcome measure was only calculated for participants with >0 catheterizations at Baseline. (NCT01557244)
Timeframe: Baseline, Week 12
| Intervention | catheterizations per 24 hours (Least Squares Mean) |
|---|---|
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg | -0.30 |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg Then 8 mg | -0.32 |
| Cohort 1, Active Comparator Phase: Oxybutynin | -0.34 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg | -0.10 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg Then 4 mg | -0.22 |
The mean number of incontinence episodes per 24 hours were calculated as the total number of incontinence episodes divided by the total number of diary days collected at the assessment time point. Number of diary days collected at the assessment time point = number of calendar days when the diary was completed; even if it was not a full 24 hours period. This outcome measure was only calculated for participants with >0 incontinence episodes at Baseline. (NCT01557244)
Timeframe: Baseline, Week 12
| Intervention | incontinence episodes per 24 hours (Least Squares Mean) |
|---|---|
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg | -0.46 |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg Then 8 mg | -0.89 |
| Cohort 1, Active Comparator Phase: Oxybutynin | -1.01 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg | -0.38 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg Then 4 mg | -0.69 |
The mean number of micturitions or catheterizations combined per 24 hours were calculated as the total number of micturitions and catheterizations combined divided by the total number of diary days collected at the assessment point. Number of diary days collected at the assessment time point = number of calendar days when the diary was completed; even if it was not a full 24 hour (hrs) period. This outcome was evaluated in those participants who had micturitions or catheterizations >0 at Baseline. (NCT01557244)
Timeframe: Baseline, Week 12
| Intervention | micturitions and catheterizations/24 hrs (Least Squares Mean) |
|---|---|
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg | -0.61 |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg Then 8 mg | -0.60 |
| Cohort 1, Active Comparator Phase: Oxybutynin | -0.75 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg | -0.24 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg Then 4 mg | -0.28 |
The mean number of micturitions per 24 hours were calculated as the total number of micturitions divided by the total number of diary days collected at the assessment time point. Number of diary days collected at the assessment time point = number of calendar days when the diary was completed on, even if it was not a full 24 hour period. This outcome measure was only calculated for participants with >0 micturitions at Baseline. (NCT01557244)
Timeframe: Baseline, Week 12
| Intervention | micturitions per 24 hours (Least Squares Mean) |
|---|---|
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg | -1.07 |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg Then 8 mg | -0.68 |
| Cohort 1, Active Comparator Phase: Oxybutynin | -0.97 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg | -0.37 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg Then 4 mg | -0.70 |
The mean number of urgency episodes per 24 hours were calculated as the total number of urgency episodes divided by the total number of diary days collected at the assessment time point. Number of diary days collected at the assessment time point = number of calendar days when the diary was completed; even if it was not a full 24 hours period. Urgency episodes were defined as urgency marked as 'yes' in the diary. This outcome measure was only calculated for participants with >0 urgency episodes at Baseline. (NCT01557244)
Timeframe: Baseline, Week 12
| Intervention | urgency episodes per 24 hours (Least Squares Mean) |
|---|---|
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg | -0.62 |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg Then 8 mg | -0.50 |
| Cohort 1, Active Comparator Phase: Oxybutynin | -0.14 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg | -0.23 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg Then 4 mg | -0.62 |
The mean voided volume per micturition was calculated as sum of voided volume divided by the total number of micturition episodes with a recorded voided volume greater than 0. (NCT01557244)
Timeframe: Baseline, Week 12
| Intervention | milliliter per micturition (Least Squares Mean) |
|---|---|
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg | 4.10 |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg Then 8 mg | 19.21 |
| Cohort 1, Active Comparator Phase: Oxybutynin | 4.15 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg | -12.72 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg Then 4 mg | -8.41 |
The mean voided volume per micturition or catheterization was calculated as sum of voided volume divided by the total number of micturition or catheterization episodes with a recorded voided volume greater than 0. This outcome was evaluated in those participants who had micturitions or catheterizations >0 at Baseline. (NCT01557244)
Timeframe: Baseline, Week 12
| Intervention | mL per micturition or catheterization (Least Squares Mean) |
|---|---|
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg | 18.45 |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg Then 8 mg | 55.55 |
| Cohort 1, Active Comparator Phase: Oxybutynin | 36.69 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg | 7.12 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg Then 4 mg | -2.65 |
Post-void residual volume measurement was measured by an ultrasound. PVR volume was only assessed for participants who did not perform clean intermittent catheterization or in any participants who had >1 UTI during the study. (NCT01557244)
Timeframe: Baseline, Week 24
| Intervention | milliliter (Mean) |
|---|---|
| Cohort 1, Safety Extension Phase: Fesoterodine 4 mg | 11.50 |
| Cohort 1, Safety Extension Phase: Fesoterodine 8 mg | 11.60 |
| Cohort 1, SEP: Oxybutynin Then Fesoterodine 4 mg | 18.00 |
| Cohort 1, SEP: Oxybutynin Then Fesoterodine 4 mg Then 8 mg | 36.67 |
| Cohort 2, Safety Extension Phase: Fesoterodine 2 mg | 21.67 |
| Cohort 2, Safety Extension Phase: Fesoterodine 4 mg | 2.75 |
Hematology: hemoglobin, hematocrit, erythrocytes <0.8*lower limit of normal (LLN), platelets<0.5*LLN>1.75*upper limit of normal (ULN), leukocytes <0.6*LLN>1.5*ULN, lymphocytes, neutrophils, <0.8*LLN >1.2*ULN, basophils, eosinophils, monocytes monocytes/leukocytes >1.2*ULN. Clinical chemistry: bilirubin, direct, bilirubin >1.5*ULN, aspartate aminotransferase (AT), alanine AT, gamma glutamyl transferase, lactate dehydrogenase, alkaline phosphatase>3.0*ULN, protein, albumin, phosphate <0.8*LLN >1.2*ULN, blood urea nitrogen, creatinine >1.3*ULN, urate >1.2*ULN, sodium<0.95*LLN>1.05*ULN, potassium, chloride, calcium bicarbonate<0.9*LLN>1.1*ULN, glucose<0.6*LLN>1.5*ULN, creatine kinase >2.0*ULN. Urinalysis: specific gravity <1.003>1.030, pH <4.5>8, urine glucose, ketones, urine protein, urine hemoglobin, urine bilirubin, nitrite, >=1, urine erythrocytes, urine leukocytes >=20, epithelial cells >=6, bacteria >20. (NCT01557244)
Timeframe: Week 1 up to Week 12
| Intervention | Participants (Count of Participants) |
|---|---|
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg | 30 |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg Then 8 mg | 29 |
| Cohort 1, Active Comparator Phase: Oxybutynin | 27 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg | 19 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg Then 4 mg | 19 |
Hematology: hemoglobin, hematocrit, erythrocytes <0.8*lower limit of normal (LLN), platelets<0.5*LLN>1.75*upper limit of normal (ULN), leukocytes <0.6*LLN>1.5*ULN, lymphocytes, neutrophils, <0.8*LLN >1.2*ULN, basophils, eosinophils, monocytes monocytes/leukocytes >1.2*ULN. Clinical chemistry: bilirubin, direct, bilirubin >1.5*ULN, aspartate aminotransferase (AT), alanine AT, gamma glutamyl transferase, lactate dehydrogenase, alkaline phosphatase>3.0*ULN, protein, albumin, phosphate <0.8*LLN >1.2*ULN, blood urea nitrogen, creatinine >1.3*ULN, urate >1.2*ULN, sodium<0.95*LLN>1.05*ULN, potassium, chloride, calcium bicarbonate<0.9*LLN>1.1*ULN, glucose<0.6*LLN>1.5*ULN, creatine kinase >2.0*ULN. Urinalysis: specific gravity <1.003>1.030, pH <4.5>8, urine glucose, ketones, urine protein, urine hemoglobin, urine bilirubin, nitrite, >=1, urine erythrocytes, urine leukocytes >=20, epithelial cells >=6, bacteria >20. (NCT01557244)
Timeframe: Week 12 up to Week 26
| Intervention | Participants (Count of Participants) |
|---|---|
| Cohort 1, Safety Extension Phase: Fesoterodine 4 mg | 19 |
| Cohort 1, Safety Extension Phase: Fesoterodine 8 mg | 22 |
| Cohort 1, SEP: Oxybutynin Then Fesoterodine 4 mg | 7 |
| Cohort 1, SEP: Oxybutynin Then Fesoterodine 4 mg Then 8 mg | 12 |
| Cohort 2, Safety Extension Phase: Fesoterodine 2 mg | 15 |
| Cohort 2, Safety Extension Phase: Fesoterodine 4 mg | 21 |
Physical examination included assessment of the general appearance and the skin, head, ears, eyes, nose, mouth, throat, respiratory, cardiovascular, gastrointestinal, musculoskeletal and neurological systems. Clinically relevant changes in physical findings were assessed by the investigator. (NCT01557244)
Timeframe: Baseline up to Week 12
| Intervention | Participants (Count of Participants) |
|---|---|
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg | 2 |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg Then 8 mg | 1 |
| Cohort 1, Active Comparator Phase: Oxybutynin | 1 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg | 1 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg Then 4 mg | 0 |
Physical examination included assessment of the general appearance and the skin, head, ears, eyes, nose, mouth, throat, respiratory, cardiovascular, gastrointestinal, musculoskeletal and neurological systems. Clinically relevant changes in physical findings were assessed by the investigator. (NCT01557244)
Timeframe: Baseline up to Week 24
| Intervention | Participants (Count of Participants) |
|---|---|
| Cohort 1, Safety Extension Phase: Fesoterodine 4 mg | 3 |
| Cohort 1, Safety Extension Phase: Fesoterodine 8 mg | 2 |
| Cohort 1, SEP: Oxybutynin Then Fesoterodine 4 mg | 0 |
| Cohort 1, SEP: Oxybutynin Then Fesoterodine 4 mg Then 8 mg | 0 |
| Cohort 2, Safety Extension Phase: Fesoterodine 2 mg | 0 |
| Cohort 2, Safety Extension Phase: Fesoterodine 4 mg | 2 |
Clinically significant UTI, counted as an adverse event was defined as: positive urine culture with a uropathogen (defined as >=10^5 colony forming unit per milliliter [CFU/mL]) and the presence of symptoms, or pyuria (defined as >50 white blood cells [WBC] per high-pass filter [hpf]) and the presence of symptoms, or positive urine culture with a uropathogen (defined as >=10^5 CFU/mL) with or without symptoms in a participant with a documented history of vesicoureteral reflux (VUR). (NCT01557244)
Timeframe: Week 1 up to Week 12
| Intervention | Participants (Count of Participants) |
|---|---|
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg | 4 |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg Then 8 mg | 1 |
| Cohort 1, Active Comparator Phase: Oxybutynin | 4 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg | 3 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg Then 4 mg | 4 |
Clinically significant UTI, counted as an adverse event was defined as: positive urine culture with a uropathogen (defined as >=10^5 CFU/mL) and the presence of symptoms, or pyuria (defined as >50 WBC per hpf and the presence of symptoms, or positive urine culture with a uropathogen (defined as >=10^5 CFU/mL) with or without symptoms in a participants with a documented history of VUR. (NCT01557244)
Timeframe: Week 12 up to Week 26
| Intervention | Participants (Count of Participants) |
|---|---|
| Cohort 1, Safety Extension Phase: Fesoterodine 4 mg | 0 |
| Cohort 1, Safety Extension Phase: Fesoterodine 8 mg | 1 |
| Cohort 1, SEP: Oxybutynin Then Fesoterodine 4 mg | 2 |
| Cohort 1, SEP: Oxybutynin Then Fesoterodine 4 mg Then 8 mg | 0 |
| Cohort 2, Safety Extension Phase: Fesoterodine 2 mg | 1 |
| Cohort 2, Safety Extension Phase: Fesoterodine 4 mg | 5 |
Volume of distribution is defined as the theoretical volume in which the total amount of drug would need to be uniformly distributed to produce the desired plasma concentration of a drug. PK analysis was not done separately for each dose of fesoterodine in respective cohorts and were combined for PK analysis using PK modelling approach. (NCT01557244)
Timeframe: Week 4, Day 1: pre-dose (when dose administered at clinic) or if dose taken at home up to 3 hours before coming to the clinic, sampling just after arrival at clinic, 5 hours post-dose, 8-10 hours post-dose (if participants remained at clinic)
| Intervention | liter (Mean) |
|---|---|
| Fesoterodine Pooled | 68.1 |
CBCL: 120 items questionnaire answered by parent/caregiver of child to assess a child's behavioral, emotional problems. Scale for each item: 0= not true, 1= somewhat/sometimes true, 2= very true/often true. Out of 120 items, 103 were categorized into 8 domains; aggressive behavior, anxious/depressed, attention problems, rule-breaking behavior, social problems, somatic complaints, thought problems, withdrawn. Summary scores: Internalizing problems=anxious/depressed + withdrawn + somatic complaints; Externalizing problems=rule-breaking + aggressive behavior. Total problems=8 domains + other 17 items. Raw scores for each domain, summary and total problems=sum of scores of related items. Using Assessment Data Manager (ADM) tool raw scores transformed/derived into standard T-scores, range: each domain=50 to 100, internalizing problems=34 to 100, externalizing problems=33 to 100, total problems=24 to 100. Lower T-score for each 8 domains, 2 summary and total problems scores=better outcomes. (NCT01557244)
Timeframe: Baseline, Week 12
| Intervention | T score (Mean) | |||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Aggressive behavior: Baseline | Aggressive behavior: Change at Week 12 | Anxious/depressed: Baseline | Anxious/depressed: Change at Week 12 | Attention problems: Baseline | Attention problems: Change at week 12 | Rule-breaking behavior: Baseline | Rule-breaking behavior: Change at Week 12 | Social problems : Baseline | Social problems : Change at Week 12 | Somatic complaints: Baseline | Somatic complaints: Change at Week 12 | Thought problems: Baseline | Thought problems: Change at Week 12 | Withdrawn: Baseline | Withdrawn: Change at Week 12 | Externalizing: Baseline | Externalizing: Change at Week 12 | Internalizing: Baseline | Internalizing: Change at Week 12 | Total Problems: Baseline | Total Problems: Change at Week 12 | |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg | 53.86 | -1.03 | 56.07 | -1.73 | 56.29 | -1.97 | 53.26 | -0.92 | 57.52 | -1.35 | 61.14 | -0.46 | 55.00 | -0.92 | 54.60 | 0.35 | 49.48 | -2.08 | 56.45 | -2.14 | 55.05 | -2.51 |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg Then 8 mg | 54.32 | -0.95 | 57.00 | -1.38 | 56.66 | -1.40 | 53.80 | -0.88 | 58.54 | -2.55 | 60.46 | -1.28 | 53.54 | -0.48 | 57.54 | -1.25 | 49.46 | -2.33 | 55.93 | -2.35 | 53.61 | -3.23 |
| Cohort 1, Active Comparator Phase: Oxybutynin | 54.58 | -1.28 | 56.75 | -1.92 | 56.30 | -1.28 | 53.43 | -0.72 | 57.95 | -0.67 | 60.58 | -0.87 | 56.73 | -1.59 | 58.25 | -1.92 | 50.10 | -1.95 | 57.25 | -3.05 | 55.45 | -2.36 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg | 54.9 | -1.29 | 55.5 | -0.79 | 55.4 | -1.29 | 54.5 | -1.71 | 57.9 | -2.21 | 57.1 | -0.38 | 51.9 | -0.42 | 55.7 | -1.75 | 51.1 | -2.63 | 53.9 | -1.96 | 53.4 | -2.17 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg Then 4 mg | 52.8 | -0.03 | 56.3 | -3.21 | 55.3 | -1.45 | 52.3 | -0.10 | 55.8 | -1.10 | 58.4 | -1.69 | 54.9 | -1.38 | 55.0 | -0.59 | 48.0 | -1.45 | 54.6 | -3.52 | 52.7 | -3.38 |
CBCL: 120 items questionnaire answered by parent/caregiver of child to assess a child's behavioral, emotional problems. Scale for each item: 0= not true, 1= somewhat/sometimes true, 2= very true/often true. Out of 120 items, 103 were categorized into 8 domains; aggressive behavior, anxious/depressed, attention problems, rule-breaking behavior, social problems, somatic complaints, thought problems, withdrawn. Summary scores: Internalizing problems=anxious/depressed + withdrawn + somatic complaints; Externalizing problems=rule-breaking + aggressive behavior. Total problems=8 domains + other 17 items. Raw scores for each domain, summary and total problems=sum of scores of related items. Using Assessment Data Manager (ADM) tool raw scores transformed/derived into standard T-scores, range: each domain=50 to 100, internalizing problems=34 to 100, externalizing problems=33 to 100, total problems=24 to 100. Lower T-score for each 8 domains, 2 summary and total problems scores=better outcomes. (NCT01557244)
Timeframe: Baseline, Week 24
| Intervention | T score (Mean) | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Aggressive behavior: Change at Week 24 | Anxious/depressed: Change at Week 24 | Attention problems: Change at Week 24 | Rule-breaking behavior: Change at Week 24 | Social problems : Change at Week 24 | Somatic complaints: Change at Week 24 | Thought problems: Change at Week 24 | Withdrawn: Change at Week 24 | Externalizing: Change at Week 24 | Internalizing: Change at Week 24 | Total Problems: Change at Week 24 | |
| Cohort 1, Safety Extension Phase: Fesoterodine 4 mg | -1.59 | -3.45 | -2.21 | -1.59 | -2.83 | -4.38 | -3.10 | -0.69 | -5.21 | -7.69 | -7.03 |
| Cohort 1, Safety Extension Phase: Fesoterodine 8 mg | -1.31 | -2.31 | -2.64 | -1.47 | -2.56 | -2.64 | -1.03 | -1.50 | -2.89 | -4.14 | -4.44 |
| Cohort 1, SEP: Oxybutynin Then Fesoterodine 4 mg | -1.25 | -1.50 | -3.38 | -1.31 | -3.19 | -1.69 | -3.25 | -2.19 | -1.81 | -3.25 | -3.69 |
| Cohort 1, SEP: Oxybutynin Then Fesoterodine 4 mg Then 8 mg | -2.40 | -3.25 | -1.70 | -0.90 | -2.65 | -1.50 | -2.30 | -4.35 | -4.15 | -5.35 | -4.90 |
| Cohort 2, Safety Extension Phase: Fesoterodine 2 mg | -1.70 | -2.60 | -1.50 | -2.15 | -3.90 | -0.60 | -1.40 | -1.80 | -4.20 | -4.40 | -5.20 |
| Cohort 2, Safety Extension Phase: Fesoterodine 4 mg | -1.86 | -3.89 | -1.71 | -0.36 | -2.36 | -1.96 | -1.75 | -0.43 | -4.21 | -4.32 | -5.25 |
CBCL: It consisted of 120 items on behavior and emotional problems. Parent/caregiver of child answered 120 items, each on scale: 0= not true, 1= somewhat/sometimes true, 2= very/often true. 103 items were classified in 8 domains: aggressive behavior: total score range (TSR)= 0 to 36, anxious/depressed: TSR= 0 to 26, attention problems: TSR= 0 to 20, rule-breaking behavior: TSR= 0 to 34, social problems: TSR= 0 to 22, somatic complaints: TSR= 0 to 22, thought problems: TSR= 0 to 30, withdrawn (TSR)= 0 to 16. Rule-breaking and aggressive behavior summarized to externalizing problems with a TSR= 0 to 70. Anxious/depressed, withdrawn, somatic complaints summarized to internalizing problems with a TSR= 0 to 64. All 103 items of 8 domains and other 17 remaining items were combined to give total problems TSR = 0 to 240. TSR for each domain, summary and total problems was sum of scores of related items respectively. Lower scores for each domain, summary and total problems= better outcomes. (NCT01557244)
Timeframe: Baseline, Week 12
| Intervention | units on a scale (Mean) | |||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Aggressive behavior: Baseline | Aggressive behavior: Change at Week 12 | Anxious/depressed: Baseline | Anxious/depressed: Change at Week 12 | Attention problems: Baseline | Attention problems: Change at Week 12 | Rule-breaking behavior: Baseline | Rule-breaking behavior: Change at Week 12 | Social problems: Baseline | Social problems: Change at Week 12 | Somatic complaints: Baseline | Somatic complaints: Change at Week 12 | Thought problems: Baseline | Thought problems: Change at Week 12 | Withdrawn: Baseline | Withdrawn: Change at Week 12 | Externalizing: Baseline | Externalizing: Change at Week 12 | Internalizing: Baseline | Internalizing: Change at Week 12 | Total Problems: Baseline | Total Problems: Change at Week 12 | |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg | 4.19 | -0.62 | 3.83 | -0.97 | 4.79 | -1.05 | 1.64 | -0.43 | 3.60 | -0.54 | 3.40 | -0.05 | 2.05 | -0.46 | 1.52 | 0.14 | 5.83 | -1.05 | 8.76 | -0.89 | 31.52 | -4.92 |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg Then 8 mg | 4.66 | -0.90 | 4.20 | -0.73 | 4.49 | -0.73 | 1.66 | -0.30 | 4.07 | -1.13 | 3.46 | -0.53 | 1.46 | -0.10 | 2.49 | -0.35 | 6.32 | -1.20 | 10.15 | -1.70 | 31.88 | -5.83 |
| Cohort 1, Active Comparator Phase: Oxybutynin | 4.88 | -0.97 | 4.10 | -1.05 | 4.85 | -0.77 | 1.70 | -0.38 | 3.80 | -0.26 | 3.40 | -0.51 | 2.58 | -0.51 | 2.75 | -0.64 | 6.53 | -1.31 | 10.25 | -2.21 | 34.18 | -5.85 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg | 5.1 | -0.92 | 3.8 | -0.58 | 4.2 | -0.71 | 1.9 | -0.63 | 3.9 | -0.83 | 2.1 | -0.04 | 1.0 | -0.21 | 1.7 | -0.50 | 6.9 | -1.54 | 7.5 | -1.13 | 29.5 | -5.33 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg Then 4 mg | 3.5 | -0.17 | 4.0 | -1.48 | 3.9 | -0.83 | 1.0 | 0.52 | 3.2 | -0.62 | 2.6 | -0.55 | 2.0 | -0.45 | 1.6 | -0.17 | 4.5 | -0.31 | 8.2 | -2.21 | 27.0 | -5.10 |
CBCL: It consisted of 120 items on behavior and emotional problems. Parent/caregiver of child answered 120 items, each on scale: 0= not true, 1= somewhat/sometimes true, 2= very/often true. 103 items were classified in 8 domains: aggressive behavior: total score range (TSR)= 0 to 36, anxious/depressed: TSR= 0 to 26, attention problems: TSR= 0 to 20, rule-breaking behavior: TSR= 0 to 34, social problems: TSR= 0 to 22, somatic complaints: TSR= 0 to 22, thought problems: TSR= 0 to 30, withdrawn (TSR)= 0 to 16. Rule-breaking and aggressive behavior summarized to externalizing problems with a TSR= 0 to 70. Anxious/depressed, withdrawn, somatic complaints summarized to internalizing problems with a TSR= 0 to 64. All 103 items of 8 domains and other 17 remaining items were combined to give total problems TSR = 0 to 240. TSR for each domain, summary and total problems was sum of scores of related items respectively. Lower scores for each domain, summary and total problems= better outcomes. (NCT01557244)
Timeframe: Baseline, Week 24
| Intervention | units on a scale (Mean) | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Aggressive behavior: Change at Week 24 | Anxious/depressed: Change at Week 24 | Attention problems: Change at Week 24 | Rule-breaking behavior: Change at Week 24 | Social problems: Change at Week 24 | Somatic complaints: Change at Week 24 | Thought problems: Change at Week 24 | Withdrawn: Change at Week 24 | Externalizing: Change at Week 24 | Internalizing: Change at Week 24 | Total Problems: Change at Week 24 | |
| Cohort 1, Safety Extension Phase: Fesoterodine 4 mg | -1.34 | -1.93 | -1.41 | -0.62 | -1.28 | -1.34 | -1.31 | -0.24 | -1.97 | -3.52 | -10.90 |
| Cohort 1, Safety Extension Phase: Fesoterodine 8 mg | -1.17 | -1.28 | -1.36 | -0.50 | -1.19 | -0.89 | -0.36 | -0.44 | -1.67 | -2.61 | -8.58 |
| Cohort 1, SEP: Oxybutynin Then Fesoterodine 4 mg | -0.81 | -1.06 | -1.94 | -0.50 | -1.13 | -0.88 | -1.06 | -0.69 | -1.19 | -2.63 | -9.00 |
| Cohort 1, SEP: Oxybutynin Then Fesoterodine 4 mg Then 8 mg | -1.75 | -1.60 | -1.25 | -0.55 | -1.20 | -0.45 | -0.90 | -1.35 | -2.30 | -3.40 | -10.10 |
| Cohort 2, Safety Extension Phase: Fesoterodine 2 mg | -1.40 | -1.70 | -1.15 | -0.80 | -1.65 | -0.15 | -0.65 | -0.45 | -2.20 | -2.30 | -9.45 |
| Cohort 2, Safety Extension Phase: Fesoterodine 4 mg | -1.57 | -1.75 | -0.89 | -0.18 | -1.14 | -0.68 | -0.64 | -0.14 | -1.79 | -2.57 | -8.39 |
The grooved pegboard test was a manipulative dexterity test that assessed psychomotor speed, fine motor control, and rapid-visual motor coordination. It consisted of a small board of 25 holes with randomly positioned slots. Pegs with a key along one side must be rotated to match the hole before they can be inserted. Participants were asked to insert 10 grooved pegs into the holes within the given time limit (up to 300 seconds). In this outcome measure number of pegs dropped while putting in the holes were measured. The task needs to be completed once for each hand; firstly, using the dominant hand followed by the non-dominant hand. (NCT01557244)
Timeframe: Baseline, Week 12
| Intervention | pegs (Mean) | |||
|---|---|---|---|---|
| Dominant hand: Baseline | Dominant hand: Change at Week 12 | Non-dominant hand: Baseline | Non-dominant hand: Change at Week 12 | |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg | 0.11 | 0.29 | 0.44 | 0.43 |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg Then 8 mg | 0.75 | 0.57 | 1.22 | 1.00 |
| Cohort 1, Active Comparator Phase: Oxybutynin | 0.29 | -0.17 | 0.00 | 0.17 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg | 0.39 | 0.00 | 0.35 | 0.00 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg Then 4 mg | 0.10 | 0.05 | 0.76 | 0.60 |
The grooved pegboard test was a manipulative dexterity test that assessed psychomotor speed, fine motor control, and rapid-visual motor coordination. It consisted of a small board of 25 holes with randomly positioned slots. Pegs with a key along one side must be rotated to match the hole before they can be inserted. Participants were asked to insert 10 grooved pegs into the holes within the given time limit (up to 300 seconds). In this outcome measure number of pegs dropped while putting in the holes were measured. The task needs to be completed once for each hand; firstly, using the dominant hand followed by the non-dominant hand. (NCT01557244)
Timeframe: Baseline, Week 24
| Intervention | pegs (Mean) | |
|---|---|---|
| Dominant hand: Change at week 24 | Non-dominant hand: Change at week 24 | |
| Cohort 1, Safety Extension Phase: Fesoterodine 4 mg | 0.33 | 1.33 |
| Cohort 1, Safety Extension Phase: Fesoterodine 8 mg | 0.43 | 0.00 |
| Cohort 1, SEP: Oxybutynin Then Fesoterodine 4 mg | 0.00 | 0.50 |
| Cohort 1,SEP: Oxybutynin Then Fesoterodine 8 mg | -0.33 | 0.00 |
| Cohort 2, Safety Extension Phase: Fesoterodine 2 mg | -0.27 | -0.36 |
| Cohort 2, Safety Extension Phase: Fesoterodine 4 mg | -0.06 | 0.11 |
The grooved pegboard test was a manipulative dexterity test that assessed psychomotor speed, fine motor control, and rapid-visual motor coordination. It consisted of a small board of 25 holes with randomly positioned slots. Pegs with a key along one side must be rotated to match the hole before they can be inserted. Participants were asked to insert 25 grooved pegs into the holes within the given time limit (up to 300 seconds). In this outcome measure number of pegs dropped while putting in the holes were measured. The task needs to be completed once for each hand; firstly, using the dominant hand followed by the non-dominant hand. (NCT01557244)
Timeframe: Baseline, Week 24
| Intervention | pegs (Mean) | |
|---|---|---|
| Dominant hand: Change at Week 24 | Non-dominant hand: Change at Week 24 | |
| Cohort 1, Safety Extension Phase: Fesoterodine 4 mg | 0.00 | -0.28 |
| Cohort 1, Safety Extension Phase: Fesoterodine 8 mg | 0.63 | 0.68 |
| Cohort 1, SEP: Oxybutynin Then Fesoterodine 4 mg | 0.14 | 0.00 |
| Cohort 1, SEP: Oxybutynin Then Fesoterodine 4 mg Then 8 mg | 0.25 | 0.27 |
| Cohort 2, Safety Extension Phase: Fesoterodine 2 mg | 0.00 | 0.60 |
| Cohort 2, Safety Extension Phase: Fesoterodine 4 mg | 0.44 | -0.13 |
The grooved pegboard test was a manipulative dexterity test that assessed psychomotor speed, fine motor control, and rapid-visual motor coordination. It consisted of a small board of 25 holes with randomly positioned slots. Pegs with a key along one side must be rotated to match the hole before they can be inserted. Participants were asked to insert 10 grooved pegs into the holes within the given time limit (up to 300 seconds). In this outcome measure number of pegs placed correctly while putting in the holes were measured. The task needs to be completed once for each hand; firstly, using the dominant hand followed by the non-dominant hand. (NCT01557244)
Timeframe: Baseline, Week 12
| Intervention | pegs (Mean) | |||
|---|---|---|---|---|
| Dominant hand: Baseline | Dominant hand: Change at Week 12 | Non-dominant hand: Baseline | Non-dominant hand: Change at Week 12 | |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg | 9.56 | -0.29 | 9.56 | -0.57 |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg Then 8 mg | 9.38 | 0.00 | 9.00 | 0.00 |
| Cohort 1, Active Comparator Phase: Oxybutynin | 10.00 | 0.00 | 10.00 | 0.00 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg | 9.89 | 0.00 | 9.82 | -0.07 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg Then 4 mg | 10.0 | -0.11 | 9.62 | 0.00 |
The grooved pegboard test was a manipulative dexterity test that assessed psychomotor speed, fine motor control, and rapid-visual motor coordination. It consisted of a small board of 25 holes with randomly positioned slots. Pegs with a key along one side must be rotated to match the hole before they can be inserted. Participants were asked to insert 10 grooved pegs into the holes within the given time limit (up to 300 seconds). In this outcome measure number of pegs placed correctly while putting in the holes were measured. The task needs to be completed once for each hand; firstly, using the dominant hand followed by the non-dominant hand. (NCT01557244)
Timeframe: Baseline, Week 24
| Intervention | pegs (Mean) | |
|---|---|---|
| Dominant hand: Change at Week 24 | Non-dominant hand: Change at Week 24 | |
| Cohort 1, Safety Extension Phase: Fesoterodine 4 mg | -0.33 | -1.33 |
| Cohort 1, Safety Extension Phase: Fesoterodine 8 mg | 0.00 | 0.00 |
| Cohort 1, SEP: Oxybutynin Then Fesoterodine 4 mg | 0.00 | 0.00 |
| Cohort 1, SEP: Oxybutynin Then Fesoterodine 4 mg Then 8 mg | 0.00 | 0.00 |
| Cohort 2, Safety Extension Phase: Fesoterodine 2 mg | 0.07 | 0.14 |
| Cohort 2, Safety Extension Phase: Fesoterodine 4 mg | 0.00 | 0.21 |
The grooved pegboard test was a manipulative dexterity test that assessed psychomotor speed, fine motor control, and rapid-visual motor coordination. It consisted of a small board of 25 holes with randomly positioned slots. Pegs with a key along one side must be rotated to match the hole before they can be inserted. Participants were asked to insert 25 grooved pegs into the holes within the given time limit (up to 300 seconds). In this outcome measure number of pegs placed correctly while putting in the holes were measured. The task needs to be completed once for each hand; firstly, using the dominant hand followed by the non-dominant hand. (NCT01557244)
Timeframe: Baseline, Week 12
| Intervention | pegs (Mean) | |||
|---|---|---|---|---|
| Dominant hand: Baseline | Dominant hand: Change at Week 12 | Non-dominant hand: Baseline | Non-dominant hand: Change at Week 12 | |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg | 25.00 | -0.07 | 24.45 | 0.53 |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg Then 8 mg | 24.56 | 0.42 | 24.75 | 0.26 |
| Cohort 1, Active Comparator Phase: Oxybutynin | 25.00 | -0.12 | 24.88 | 0.03 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg | 25.00 | -0.13 | 24.50 | 0.63 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg Then 4 mg | 23.22 | 0.11 | 24.25 | -0.63 |
The grooved pegboard test was a manipulative dexterity test that assessed psychomotor speed, fine motor control, and rapid-visual motor coordination. It consisted of a small board of 25 holes with randomly positioned slots. Pegs with a key along one side must be rotated to match the hole before they can be inserted. Participants were asked to insert 25 grooved pegs into the holes within the given time limit (up to 300 seconds). In this outcome measure number of pegs placed correctly while putting in the holes were measured. The task needs to be completed once for each hand; firstly, using the dominant hand followed by the non-dominant hand. (NCT01557244)
Timeframe: Baseline, Week 24
| Intervention | pegs (Mean) | |
|---|---|---|
| Dominant hand: Change at Week 24 | Non-dominant hand: Change at Week 24 | |
| Cohort 1, Safety Extension Phase: Fesoterodine 4 mg | 0.00 | 0.60 |
| Cohort 1, Safety Extension Phase: Fesoterodine 8 mg | 0.50 | 0.21 |
| Cohort 1, SEP: Oxybutynin Then Fesoterodine 4 mg | 0.00 | 0.14 |
| Cohort 1, SEP: Oxybutynin Then Fesoterodine 4 mg Then 8 mg | 0.00 | 0.00 |
| Cohort 2, Safety Extension Phase: Fesoterodine 2 mg | 0.00 | 0.60 |
| Cohort 2, Safety Extension Phase: Fesoterodine 4 mg | 0.11 | -0.50 |
Post-void residual volume measurement was measured by an ultrasound. PVR volume was only assessed for participants who did not perform clean intermittent catheterization or in any participants who had >1 UTI during the study. (NCT01557244)
Timeframe: Baseline, Week 4, 12
| Intervention | milliliter (Mean) | ||
|---|---|---|---|
| Baseline | Change at Week 4 | Change at Week 12 | |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg | 7.00 | 5.40 | 25.60 |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg Then 8 mg | 9.57 | -7.33 | -4.00 |
| Cohort 1, Active Comparator Phase: Oxybutynin | 5.78 | 19.11 | 12.86 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg | 14.7 | -2.00 | 2.50 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg Then 4 mg | 10.7 | 10.25 | 0.75 |
The grooved pegboard test was a manipulative dexterity test that assessed psychomotor speed, fine motor control, and rapid-visual motor coordination. It consisted of a small board of 25 holes with randomly positioned slots. Pegs with a key along one side must be rotated to match the hole before they can be inserted. In this outcome measure participants were asked to insert 10 grooved pegs into the holes within the given time limit (up to 300 seconds). The task needs to be completed once for each hand; firstly, using the dominant hand followed by the non-dominant hand. Time taken to complete the test was inversely correlated to the cognitive ability. (NCT01557244)
Timeframe: Baseline, Week 12
| Intervention | seconds (Mean) | |||
|---|---|---|---|---|
| Dominant hand: Baseline | Dominant hand: Change at Week 12 | Non-dominant hand: Baseline | Non-dominant hand: Change at Week 12 | |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg | 61.11 | -7.71 | 80.44 | -21.71 |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg Then 8 mg | 56.50 | 10.14 | 114.00 | 15.33 |
| Cohort 1, Active Comparator Phase: Oxybutynin | 46.43 | -5.33 | 48.00 | -2.00 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg | 69.56 | -11.20 | 91.29 | -19.36 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg Then 4 mg | 52.20 | -10.26 | 76.29 | -3.25 |
The grooved pegboard test was a manipulative dexterity test that assessed psychomotor speed, fine motor control, and rapid-visual motor coordination. It consisted of a small board of 25 holes with randomly positioned slots. Pegs with a key along one side must be rotated to match the hole before they can be inserted. In this outcome measure participants were asked to insert 10 grooved pegs into the holes within the given time limit (up to 300 seconds). The task needs to be completed once for each hand; firstly, using the dominant hand followed by the non-dominant hand. Time taken to complete the test was inversely correlated to the cognitive ability. (NCT01557244)
Timeframe: Baseline, Week 24
| Intervention | seconds (Mean) | |
|---|---|---|
| Dominant hand: Change at Week 24 | Non-dominant hand: Change at Week 24 | |
| Cohort 1, Safety Extension Phase: Fesoterodine 4 mg | -11.33 | -2.00 |
| Cohort 1, Safety Extension Phase: Fesoterodine 8 mg | -3.71 | -4.00 |
| Cohort 1, SEP: Oxybutynin Then Fesoterodine 4 mg | -2.00 | 1.50 |
| Cohort 1, SEP: Oxybutynin Then Fesoterodine 4 mg Then 8 mg | -6.33 | -11.00 |
| Cohort 2, Safety Extension Phase: Fesoterodine 2 mg | -7.07 | -9.14 |
| Cohort 2, Safety Extension Phase: Fesoterodine 4 mg | -15.00 | -18.47 |
The grooved pegboard test was a manipulative dexterity test that assessed psychomotor speed, fine motor control, and rapid-visual motor coordination. It consisted of a small board of 25 holes with randomly positioned slots. Pegs with a key along one side must be rotated to match the hole before they can be inserted. In this outcome measure participants were asked to insert 25 grooved pegs into the holes within the given time limit (up to 300 seconds). The task needs to be completed once for each hand; firstly, using the dominant hand followed by the non-dominant hand. Time taken to complete the test was inversely correlated to the cognitive ability. (NCT01557244)
Timeframe: Baseline, Week 12
| Intervention | seconds (Mean) | |||
|---|---|---|---|---|
| Dominant hand: Baseline | Dominant hand: Change at Week 12 | Non-dominant hand: Baseline | Non-dominant hand: Change at Week 12 | |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg | 88.85 | -5.40 | 110.61 | -9.10 |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg Then 8 mg | 92.15 | -8.88 | 109.00 | -4.10 |
| Cohort 1, Active Comparator Phase: Oxybutynin | 82.64 | 1.21 | 92.94 | -1.97 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg | 106.7 | -14.38 | 130.30 | -13.50 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg Then 4 mg | 124.7 | -18.44 | 126.1 | -12.50 |
The grooved pegboard test was a manipulative dexterity test that assessed psychomotor speed, fine motor control, and rapid-visual motor coordination. It consisted of a small board of 25 holes with randomly positioned slots. Pegs with a key along one side must be rotated to match the hole before they can be inserted. In this outcome measure participants were asked to insert 25 grooved pegs into the holes within the given time limit (up to 300 seconds). The task needs to be completed once for each hand; firstly, using the dominant hand followed by the non-dominant hand. Time taken to complete the test was inversely correlated to the cognitive ability. (NCT01557244)
Timeframe: Baseline, Week 24
| Intervention | seconds (Mean) | |
|---|---|---|
| Dominant hand: Change at Week 24 | Non-dominant hand: Change at Week 24 | |
| Cohort 1, Safety Extension Phase: Fesoterodine 4 mg | -8.20 | -9.24 |
| Cohort 1, Safety Extension Phase: Fesoterodine 8 mg | -12.27 | -8.46 |
| Cohort 1, SEP: Oxybutynin Then Fesoterodine 4 mg | -5.71 | -3.79 |
| Cohort 1, SEP: Oxybutynin Then Fesoterodine 4 mg Then 8 mg | -7.00 | -11.87 |
| Cohort 2, Safety Extension Phase: Fesoterodine 2 mg | -38.20 | -38.00 |
| Cohort 2, Safety Extension Phase: Fesoterodine 4 mg | -17.00 | -15.50 |
The visual accommodation was the distance for each eye at which vision became blurred and was calculated as the mean of triplicate measurements. The participants focused on a single letter of the 20/40 line of an eye chart and chart was moved slowly towards the participant until letter was blurred. At this point, the distance from eye to letter was measured for each eye. In this outcome measure data have been reported for right and left eye separately. (NCT01557244)
Timeframe: Baseline, Week 12
| Intervention | centimeter (Mean) | |||
|---|---|---|---|---|
| Right Eye: Baseline | Right Eye: Change at Week 12 | Left Eye: Baseline | Left Eye: Change at Week 12 | |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg | 11.88 | 1.74 | 12.31 | 0.27 |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg Then 8 mg | 15.94 | 7.77 | 15.83 | 5.79 |
| Cohort 1, Active Comparator Phase: Oxybutynin | 9.59 | 0.50 | 9.69 | 0.81 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg | 9.67 | -1.04 | 8.81 | -1.45 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg Then 4 mg | 8.17 | 1.02 | 8.04 | 0.90 |
The visual accommodation is the distance for each eye at which vision became blurred and was calculated as the mean of triplicate measurements. The participants focused on a single letter of the 20/40 line of an eye chart and chart was moved slowly towards the participant until letter was blurred. At this point, the distance from eye to letter was measured for each eye. In this outcome measure data have been reported for right and left eye separately. (NCT01557244)
Timeframe: Baseline, Week 24
| Intervention | centimeter (Mean) | |
|---|---|---|
| Right Eye: Change at Week 24 | Left Eye: Change at Week 24 | |
| Cohort 1, Safety Extension Phase: Fesoterodine 4 mg | 0.73 | 0.90 |
| Cohort 1, Safety Extension Phase: Fesoterodine 8 mg | 4.33 | 3.79 |
| Cohort 1, SEP: Oxybutynin Then Fesoterodine 4 mg | 1.50 | 1.66 |
| Cohort 1, SEP: Oxybutynin Then Fesoterodine 4 mg Then 8 mg | 0.50 | 0.58 |
| Cohort 2, Safety Extension Phase: Fesoterodine 2 mg | -1.35 | 0.43 |
| Cohort 2, Safety Extension Phase: Fesoterodine 4 mg | 0.96 | 1.12 |
Visual acuity (VA) was assessed using the Snellen method, where logarithm of minimum angle of resolution (logMAR) units were derived from the Snellen ratios. Participants had to read letters from the chart at a distance of 20 feet/6 meter or 4 meter. VA/Snellen ratio = distance between the chart and participant, divided by the distance at which participant was able to see or read chart without impairment; expressed as decimal. logMAR = log10 (1/decimal VA). In this outcome measure data have been reported for right and left eye separately. (NCT01557244)
Timeframe: Baseline, Week 12
| Intervention | logMAR unit (Mean) | |||
|---|---|---|---|---|
| Right Eye: Baseline | Right Eye: Change at Week 12 | Left Eye: Baseline | Left Eye: Change at Week 12 | |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg | 0.09 | 0.01 | 0.08 | 0.00 |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg Then 8 mg | 0.11 | -0.01 | 0.10 | -0.01 |
| Cohort 1, Active Comparator Phase: Oxybutynin | 0.03 | 0.02 | 0.02 | 0.00 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg | 0.15 | 0.03 | 0.16 | -0.02 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg Then 4 mg | 0.10 | -0.00 | 0.14 | 0.00 |
VA was assessed using the Snellen method, where logMAR units were derived from the Snellen ratios. Participants had to read letters from the chart at a distance of 20 feet/6 meter or 4 meter. VA/Snellen ratio = distance between the chart and participant, divided by the distance at which participant was able to see or read chart without impairment; expressed as decimal. logMAR = log10 (1/decimal VA). In this outcome measure data have been reported for right and left eye separately. (NCT01557244)
Timeframe: Baseline, Week 24
| Intervention | logMAR unit (Mean) | |
|---|---|---|
| Right Eye: Change at Week 24 | Left Eye: Change at Week 24 | |
| Cohort 1, Safety Extension Phase: Fesoterodine 4 mg | 0.04 | 0.01 |
| Cohort 1, Safety Extension Phase: Fesoterodine 8 mg | -0.02 | -0.01 |
| Cohort 1, SEP: Oxybutynin Then Fesoterodine 4 mg | -0.01 | 0.00 |
| Cohort 1, SEP: Oxybutynin Then Fesoterodine 4 mg Then 8 mg | 0.02 | -0.04 |
| Cohort 2, Safety Extension Phase: Fesoterodine 2 mg | 0.00 | -0.02 |
| Cohort 2, Safety Extension Phase: Fesoterodine 4 mg | 0.01 | 0.03 |
Pre-defined criteria for vital signs: 1) a) systolic blood pressure (SBP) of <90 millimeter of mercury (mmHg), b) change >=30 mmHg increase, c) change >=30 mmHg decrease; 2) a) diastolic blood pressure (DBP) of <50 mmHg, b) change >=20 mmHg increase, c) change >=20 mmHg decrease; 3) a) pulse rate value of <40 beats per minute (bpm), b) pulse rate value >120 bpm. (NCT01557244)
Timeframe: Baseline up to Week 12
| Intervention | Participants (Count of Participants) | |||||||
|---|---|---|---|---|---|---|---|---|
| SBP: <90 mmHg | SBP: Change >=30 mmHg increase | SBP: Change >=30 mmHg decrease | DBP: <50 mmHg | DBP: Change >=20 mmHg increase | DBP: Change >=20 mmHg decrease | Pulse rate: <40 bpm | Pulse rate: >120 bpm | |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg | 2 | 1 | 1 | 2 | 1 | 1 | 0 | 2 |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg Then 8 mg | 2 | 2 | 0 | 1 | 2 | 1 | 0 | 4 |
| Cohort 1, Active Comparator Phase: Oxybutynin | 0 | 1 | 0 | 2 | 1 | 1 | 0 | 0 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg | 7 | 0 | 0 | 3 | 3 | 2 | 0 | 2 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg Then 4 mg | 4 | 1 | 0 | 1 | 4 | 0 | 0 | 3 |
Pre-defined criteria for vital signs: 1) a) systolic blood pressure (SBP) of <90 millimeter of mercury (mmHg), b) change >=30 mmHg increase, c) change >=30 mmHg decrease; 2) a) diastolic blood pressure (DBP) of <50 mmHg, b) change >=20 mmHg increase, c) change >=20 mmHg decrease; 3) a) pulse rate value of <40 beats per minute (bpm), b) pulse rate value >120 bpm. (NCT01557244)
Timeframe: Baseline up to Week 24
| Intervention | Participants (Count of Participants) | |||||||
|---|---|---|---|---|---|---|---|---|
| SBP: <90 mmHg | SBP: Change >=30 mmHg increase | SBP: Change >=30 mmHg decrease | DBP: <50 mmHg | DBP: Change >=20 mmHg increase | DBP: Change >=20 mmHg decrease | Pulse rate: <40 bpm | Pulse rate: >120 bpm | |
| Cohort 1, Safety Extension Phase: Fesoterodine 4 mg | 0 | 1 | 0 | 0 | 1 | 1 | 0 | 0 |
| Cohort 1, Safety Extension Phase: Fesoterodine 8 mg | 3 | 0 | 1 | 2 | 0 | 0 | 0 | 0 |
| Cohort 1, SEP: Oxybutynin Then Fesoterodine 4 mg | 2 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Cohort 1, SEP: Oxybutynin Then Fesoterodine 4 mg Then 8 mg | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Cohort 2, Safety Extension Phase: Fesoterodine 2 mg | 4 | 0 | 0 | 2 | 1 | 0 | 0 | 0 |
| Cohort 2, Safety Extension Phase: Fesoterodine 4 mg | 2 | 0 | 0 | 0 | 2 | 0 | 0 | 1 |
In this outcome measure, shift data have been reported using 4 categories: (1) number of participants who did not have IDC at Baseline and at Week 12, (2) number of participants who did not have IDC at Baseline but had IDC at Week 12, (3) number of participants who had IDC at Baseline but no IDC at Week 12, and (4) number of participants who had IDC at Baseline and at Week 12. (NCT01557244)
Timeframe: Baseline, Week 12
| Intervention | Participants (Count of Participants) | |||
|---|---|---|---|---|
| Baseline IDC = No; Week 12 IDC = No | Baseline IDC = No; Week 12 IDC = Yes | Baseline IDC = Yes; Week 12 IDC = No | Baseline IDC = Yes; Week 12 IDC = Yes | |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg | 12 | 2 | 9 | 18 |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg Then 8 mg | 4 | 1 | 18 | 18 |
| Cohort 1, Active Comparator Phase: Oxybutynin | 6 | 0 | 14 | 18 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg | 0 | 0 | 6 | 19 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg Then 4 mg | 1 | 0 | 11 | 16 |
An AE was any untoward medical occurrence in a participant who received investigational product without regard to possibility of causal relationship. SAE was an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly; medically important events. A treatment emergent AE was defined as an event that emerged during the treatment period that was absent before treatment, or worsened during the treatment period relative to the pretreatment state. AEs included both all serious and non-serious adverse events. (NCT01557244)
Timeframe: Baseline up to Week 12
| Intervention | Participants (Count of Participants) | |
|---|---|---|
| Treatment Emergent AEs | Treatment Emergent SAEs | |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg | 26 | 3 |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg Then 8 mg | 20 | 2 |
| Cohort 1, Active Comparator Phase: Oxybutynin | 30 | 1 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg | 19 | 2 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg Then 4 mg | 18 | 2 |
The grooved pegboard test was a manipulative dexterity test that assessed psychomotor speed, fine motor control, and rapid-visual motor coordination. It consisted of a small board of 25 holes with randomly positioned slots. Pegs with a key along one side must be rotated to match the hole before they can be inserted. Participants were asked to insert 25 grooved pegs into the holes within the given time limit (up to 300 seconds). In this outcome measure number of pegs dropped while putting in the holes were measured. The task needs to be completed once for each hand; firstly, using the dominant hand followed by the non-dominant hand. (NCT01557244)
Timeframe: Baseline, Week 12
| Intervention | pegs (Mean) | |||
|---|---|---|---|---|
| Dominant hand: Baseline | Dominant hand: Change at Week 12 | Non-dominant hand: Baseline | Non-dominant hand: Change at Week 12 | |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg | 0.45 | 0.00 | 0.91 | -0.33 |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg Then 8 mg | 0.24 | -0.18 | 0.28 | 0.06 |
| Cohort 1, Active Comparator Phase: Oxybutynin | 0.24 | 0.09 | 0.36 | 0.21 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg | 0.10 | 0.00 | 0.40 | 0.13 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg Then 4 mg | 0.11 | 0.44 | 0.13 | 0.00 |
The mean volume per catheterization was calculated as sum of voided volume divided by the total number of catheterization, with a recorded voided volume greater than 0. (NCT01557244)
Timeframe: Baseline, Week 12
| Intervention | milliliter per catheterization (Least Squares Mean) |
|---|---|
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg | 29.47 |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg Then 8 mg | 47.18 |
| Cohort 1, Active Comparator Phase: Oxybutynin | 45.90 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg | 11.50 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg Then 4 mg | 1.74 |
An AE was any untoward medical occurrence in a participant who received investigational product without regard to possibility of causal relationship. SAE was an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly; medically important events. A treatment emergent AE was defined as an event that emerged during the treatment period that was absent before treatment, or worsened during the treatment period relative to the pretreatment state. AEs included both all serious and non-serious adverse events. (NCT01557244)
Timeframe: Week 12 up to Week 26 (including 2 weeks of follow up after last dose)
| Intervention | Participants (Count of Participants) | |
|---|---|---|
| Treatment emergent AEs | Treatment emergent SAEs | |
| Cohort 1, Safety Extension Phase (SEP): Fesoterodine 8 mg | 13 | 2 |
| Cohort 1, Safety Extension Phase: Fesoterodine 4 mg | 14 | 0 |
| Cohort 1, SEP: Oxybutynin Then Fesoterodine 4 mg | 9 | 0 |
| Cohort 1, SEP: Oxybutynin Then Fesoterodine 4 mg Then 8 mg | 11 | 0 |
| Cohort 2, Safety Extension Phase: Fesoterodine 2 mg | 11 | 0 |
| Cohort 2, Safety Extension Phase: Fesoterodine 4 mg | 16 | 2 |
Absorption rate constant is used to determine rate at which drug is entering into body. Pharmacokinetic (PK) analysis was not done separately for each dose of fesoterodine in respective cohorts and were combined for PK analysis using PK modelling approach. (NCT01557244)
Timeframe: Week 4, Day 1: pre-dose (when dose administered at clinic) or if dose taken at home up to 3 hours before coming to the clinic, sampling just after arrival at clinic, 5 hours post-dose, 8-10 hours post-dose (if participants remained at clinic)
| Intervention | per hour (Mean) |
|---|---|
| Fesoterodine Pooled | 0.0897 |
Clearance determines the rate at which a drug is metabolized or eliminated by normal biological processes. PK analysis was not done separately for each dose of fesoterodine in respective cohorts and were combined for PK analysis using PK modelling approach. (NCT01557244)
Timeframe: Week 4, Day 1: pre-dose (when dose administered at clinic) or if dose taken at home up to 3 hours before coming to the clinic, sampling just after arrival at clinic, 5 hours post-dose, 8-10 hours post-dose (if participants remained at clinic)
| Intervention | liter per hour (Mean) |
|---|---|
| Fesoterodine Pooled | 71.6 |
Bladder compliance was defined as change in bladder volume in milliliter (mL) divided by change in bladder pressure in cm H2O (during the same time when change in bladder volume was estimated). (NCT01557244)
Timeframe: Baseline, Week 12
| Intervention | mL per cm H2O (Least Squares Mean) |
|---|---|
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg | 6.40 |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg Then 8 mg | 5.41 |
| Cohort 1, Active Comparator Phase: Oxybutynin | 11.36 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg | 12.44 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg Then 4 mg | 16.44 |
Bladder volume (in milliliter) at first IDC was measured using urodynamic testing. (NCT01557244)
Timeframe: Baseline, Week 12
| Intervention | milliliter (Least Squares Mean) |
|---|---|
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg | 30.53 |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg Then 8 mg | 26.06 |
| Cohort 1, Active Comparator Phase: Oxybutynin | 41.31 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg | 23.80 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg Then 4 mg | 31.26 |
Detrusor pressure (in cm H2O) at maximum urinary bladder capacity was measured using urodynamic testing. (NCT01557244)
Timeframe: Baseline, Week 12
| Intervention | cm H2O (Least Squares Mean) |
|---|---|
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg | -2.86 |
| Cohort 1, Active Comparator Phase: Fesoterodine 4 mg Then 8 mg | -1.57 |
| Cohort 1, Active Comparator Phase: Oxybutynin | -2.39 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg | -2.74 |
| Cohort 2, Efficacy Phase: Fesoterodine 2 mg Then 4 mg | -9.73 |
Outcome was defined as moderate to severe anticipated adverse events (AE) based on the NCI Common Terminology Criteria for Adverse Events (CTCAE). Each AE is graded 1-5 with Grade 1=mild AE, Grade 2=moderate AE, Grade 3=severe AE, Grade 4=life-threatening or disabling AE, grade 5=Death-related to AE. Any side effect grade >= 2 considered a moderate to severe AE. Anticipated AEs included dizziness, somnolence, insomnia, confusion, cognitive impairment, dry eyes, blurry vision, dry mouth, constipation, nausea, dyspepsia and urinary retention. Example: dry mouth grades per CTCAE: Grade 1=symptomatic without significant dietary alteration; unstimulated saliva flow > 0.2 mL/min; Grade 2=symptomatic and significant oral intake alteration; unstimulated saliva flow 0.1 to 0.2 mL/min; Grade 3=symptoms leading to inability to adequately aliment orally; IV fluids, tube feedings or total parenteral nutrition indicated; unstimulated saliva < 0.1 mL/min. (NCT01786967)
Timeframe: 4 weeks
| Intervention | percentage of participants (Number) |
|---|---|
| Extensive Metabolizers | 14.8 |
| Poor Metabolizers | 0.0 |
"Treatment Success (Yes/No) was defined by the Treatment Benefit Scale (TBS). TBS is a 4-point scale which was dichotomized into Yes/No for the Treatment Success outcome. The scale asks participants to rate My condition has been improved: 1= greatly improved, 2=improved, 3=not changed, 4= worsened. If a participant responded 1 (greatly improved) or 2 (improved), they were considered as a Yes for Treatment Success. If a participant responded 3 (not changed) or 4 (worsened), then they were considered as a No for Treatment Success." (NCT01786967)
Timeframe: 4 weeks
| Intervention | percentage of participants (Number) |
|---|---|
| Extensive Metabolizers | 74.1 |
| Poor Metabolizers | 75.0 |
A treatment-related adverse event was any untoward medical occurrence attributed to fesoterodine fumarate in a participant who received fesoterodine fumarate. Expectedness of the adverse event was determined according to the Japanese package insert. Relatedness to fesoterodine fumarate was assessed by the investigator. (NCT01936870)
Timeframe: 12 Weeks
| Intervention | Participants (Count of Participants) |
|---|---|
| Fesoterodine Fumarate | 27 |
A treatment-related adverse event was any untoward medical occurrence attributed to fesoterodine fumarate in a participant who received fesoterodine fumarate. Relatedness to fesoterodine fumarate was assessed by the investigator. (NCT01936870)
Timeframe: 12 Weeks
| Intervention | Participants (Count of Participants) | ||
|---|---|---|---|
| From 4 mg to 8 mg | 4 mg | 8 mg | |
| Fesoterodine Fumarate | 53 | 330 | 32 |
Mini-Mental State Examination (MMSE) measured general cognitive functioning: orientation, memory, attention, concentration, naming, repetition, comprehension, and ability to create a sentence and to copy two intersecting polygons. Total score derived from sub-scores; total ranged from 0 to 30, higher score indicates better cognitive state. Mean change from baseline in the MMSE score at 12 weeks was presented along with the corresponding standard deviation. (NCT01936870)
Timeframe: Baseline, 12 Weeks
| Intervention | Scale (Mean) |
|---|---|
| Fesoterodine Fumarate | 0.4 |
Overactive Bladder Symptom Score (OABSS) was defined as the sum score (0 to 15) of the following four OAB symptoms: daytime frequency (2 at maximum), nighttime frequency (3 at maximum), urgency (5 at maximum), and urgency incontinence (5 at maximum). Higher score indicates worse symptoms. Mean change from baseline in the OABSS at 12 weeks was presented along with the corresponding standard deviation. (NCT01936870)
Timeframe: Baseline, 12 Weeks
| Intervention | Scale (Mean) |
|---|---|
| Fesoterodine Fumarate | -3.4 |
Clinical efficacy rate, which was defined as the percentage of participants who achieved clinical effectiveness over the total number of assessable effectiveness analysis population, was presented along with the corresponding 2-sided 95% CI. Overall effectiveness of fesoterodine fumarate was determined by the investigator based on clinical symptoms and examinations. Clinical effectiveness was assessed according to the following categories: (1) effective, (2) ineffective, or (3) unassessable at week 12 of the treatment. (NCT01936870)
Timeframe: 12 Weeks
| Intervention | Percentage of participants (Number) |
|---|---|
| Fesoterodine Fumarate | 74.8 |
An adverse event was any untoward medical occurrence in a participant who received fesoterodine fumarate without regard to possibility of causal relationship. Adverse events related to cognitive function disorder were identified by broad searches on the Standard MedDRA Queries (SMQ). (NCT01936870)
Timeframe: 12 Weeks
| Intervention | Participants (Count of Participants) |
|---|---|
| Fesoterodine Fumarate | 2 |
A treatment-related adverse event was any untoward medical occurrence attributed to fesoterodine fumarate in a participant who received fesoterodine fumarate. Relatedness to fesoterodine fumarate was assessed by the investigator. (NCT01936870)
Timeframe: 12 Weeks
| Intervention | Participants (Count of Participants) |
|---|---|
| Fesoterodine Fumarate | 415 |
A treatment-related adverse event was any untoward medical occurrence attributed to fesoterodine fumarate in a participant who received fesoterodine fumarate. A treatment-related serious adverse event was a treatment-related adverse event resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; lifethreatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly. Relatedness to fesoterodine fumarate was assessed by the investigator. (NCT01936870)
Timeframe: 12 Weeks
| Intervention | Participants (Count of Participants) |
|---|---|
| Fesoterodine Fumarate | 8 |
Satisfaction rate, which was defined as the percentage of participants who were satisfied by fesoterodine fumarate treatment over the total number of assessable effectiveness analysis population, was presented along with the corresponding 2-sided 95% CI. Satisfaction scale was assessed by the participants according to the following categories: (1) satisfied, (2) unsatisfied, (3) uncertain, or (4) unconfirmed. (NCT01936870)
Timeframe: 12 Weeks
| Intervention | Percentage of participants (Number) |
|---|---|
| Fesoterodine Fumarate | 59.0 |
Cytochrome P450 2D6 (CYP2D6) inhibitors included quinidine and paroxetine. A treatment-related adverse event was any untoward medical occurrence attributed to fesoterodine fumarate in a participant who received fesoterodine fumarate. Relatedness to fesoterodine fumarate was assessed by the investigator. (NCT01936870)
Timeframe: 12 Weeks
| Intervention | Participants (Count of Participants) | |
|---|---|---|
| Received Concomitant CYP2D6 Inhibitors | Not Received Concomitant CYP2D6 Inhibitors | |
| Fesoterodine Fumarate | 11 | 404 |
Cytochrome P450 3A4 (CYP3A4) inhibitors included atazanavir, clarithromycin, indinavir, itraconazole, nelfinavir, ritonavir, saquinavir, and telithromycin. (NCT01936870)
Timeframe: 12 Weeks
| Intervention | Participants (Count of Participants) | |
|---|---|---|
| Received Concomitant CYP3A4 Inhibitors | Not Received Concomitant CYP3A4 Inhibitors | |
| Fesoterodine Fumarate | 6 | 409 |
The visual accommodation was the minimum focusing distance for each eye at which vision became blurred - the mean of triplicate measurements. The participants focused on a single letter of the 20/40 line of an eye chart and chart was moved slowly towards the participant until letter was blurred. At this point, the distance from eye to letter was measured for each eye. In this outcome measure data have been reported for right and left eye separately. Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Week 12
| Intervention | centimeter (Mean) | |||
|---|---|---|---|---|
| Right Eye: Baseline | Right Eye: Change at Week 12 | Left Eye: Baseline | Left Eye: Change at Week 12 | |
| Fesoterodine 2 mg Capsule | 8.62 | 5.86 | 9.86 | 3.24 |
| Fesoterodine 4 mg Capsule | 5.56 | 6.67 | 4.83 | 16.17 |
| Fesoterodine 8 mg Tablet | 9.33 | 2.50 | 14.00 | -1.83 |
The visual accommodation was the minimum focusing distance for each eye at which vision became blurred - the mean of triplicate measurements. The participants focused on a single letter of the 20/40 line of an eye chart and chart was moved slowly towards the participant until letter was blurred. At this point, the distance from eye to letter was measured for each eye. In this outcome measure data have been reported for right and left eye separately. Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Week 28
| Intervention | centimeter (Mean) | |
|---|---|---|
| Right Eye | Left Eye | |
| Fesoterodine 2 mg Capsule | 0.78 | -0.39 |
| Fesoterodine 4 mg Capsule | -0.11 | 0.50 |
| Fesoterodine 8 mg Tablet | 5.17 | 3.17 |
Pulse rate was evaluated for examination of vital signs. Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Final visit (Week 28 for participants who completed the study or in case of early withdrawal the last assessment before Week 28 was considered to be the final visit)
| Intervention | beats per minute (Mean) |
|---|---|
| Fesoterodine 8 mg Tablet | -3.5 |
| Fesoterodine 2 mg Capsule | -1.4 |
| Fesoterodine 4 mg Capsule | -3.7 |
The mean number of micturitions and catheterizations combined per 24 hours were calculated as the total number of micturitions and catheterizations combined divided by the total number of diary days collected at the assessment point. Number of diary days collected at the assessment time point = number of calendar days when the diary was completed, even if it was not a full 24 hour (hr) period. This outcome measure was only calculated for participants with >0 micturitions or catheterizations at Baseline. Data was summarized for each cohort, each treatment group and total of treatment groups, using the merged data of studies A0221047 and A0221109 as planned. (NCT02501928)
Timeframe: Study A0221047: Baseline, Week 12; Study A0221109: Week 28, Final Visit (Week 28 for participants who completed the study or in case of early withdrawal the last assessment before Week 28 was considered to be the final visit)
| Intervention | micturitions or catheterizations/24 hr (Mean) | |||
|---|---|---|---|---|
| Baseline | Change at Week 12 | Change at Week 28 | Change at Final Visit | |
| Cohort 1 | 5.33 | 0.00 | 0.33 | 0.33 |
| Cohort 2 | 6.30 | -0.55 | -0.57 | -0.55 |
| Fesoterodine 2 mg Capsule | 6.86 | -0.83 | -0.92 | -0.83 |
| Fesoterodine 4 mg Capsule | 5.00 | 0.11 | 0.11 | 0.11 |
| Fesoterodine 8 mg Tablet | 5.33 | 0.00 | 0.33 | 0.33 |
| Total of Treatment Groups | 6.14 | -0.46 | -0.41 | -0.40 |
Pulse rate was evaluated for examination of vital signs. Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Week 12
| Intervention | beats per minute (Mean) |
|---|---|
| Fesoterodine 8 mg Tablet | 0.0 |
| Fesoterodine 2 mg Capsule | 2.4 |
| Fesoterodine 4 mg Capsule | -8.0 |
Pulse rate was evaluated for examination of vital signs. Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Week 28
| Intervention | beats per minute (Mean) |
|---|---|
| Fesoterodine 8 mg Tablet | -3.5 |
| Fesoterodine 2 mg Capsule | -2.7 |
| Fesoterodine 4 mg Capsule | -3.7 |
UTI data were summarized for each cohort, each treatment group and the total of treatment groups, using the merged data of studies A0221047 and A0221109 as planned. (NCT02501928)
Timeframe: Up to a maximum of 56 weeks (24 weeks of treatment in A0221047 and 32 weeks [28 weeks treatment + 4 weeks follow up post last dose] in A0221109)
| Intervention | Participants (Count of Participants) |
|---|---|
| Cohort 1 | 0 |
| Cohort 2 | 1 |
| Fesoterodine 8 mg Tablet | 0 |
| Fesoterodine 2 mg Capsule | 1 |
| Fesoterodine 4 mg Capsule | 0 |
| Total of Treatment Groups | 1 |
Hematology: hemoglobin, hematocrit, erythrocytes <0.8*lower limit of normal (LLN); platelets<0.5*LLN>1.75*upper limit of normal (ULN); leukocytes <0.6*LLN>1.5*ULN; lymphocytes, neutrophils <0.8*LLN >1.2*UL; basophils, eosinophils, monocytes >1.2*ULN. Clinical chemistry: bilirubin, direct bilirubin >1.5*ULN; aspartate aminotransferase (AT), alanine AT, gamma glutamyl transferase, lactate dehydrogenase, alkaline phosphatase >3.0*ULN; protein, albumin <0.8*LLN >1.2*ULN; blood urea nitrogen, creatinine >1.3*ULN; urate >1.2*ULN, sodium<0.95*LLN>1.05*ULN; potassium, chloride, bicarbonate <0.9*LLN>1.1*ULN; glucose <0.6*LLN>1.5*ULN; creatine kinase >2.0*ULN. Urinalysis: specific gravity <1.003>1.030, pH <4.5>8, glucose, ketones, protein, hemoglobin, nitrite, leukocyte esterase >=1; erythrocytes, leukocytes >=20; epithelial cells >=6, bacteria >20, hyaline casts >1. Data for this outcome was planned to be analysed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline to 28 weeks
| Intervention | Participants (Count of Participants) |
|---|---|
| Fesoterodine 8 mg Tablet | 2 |
| Fesoterodine 2 mg Capsule | 6 |
| Fesoterodine 4 mg Capsule | 2 |
Bladder compliance was defined as change in bladder volume in milliliter (mL) divided by change in bladder pressure in cm H2O (during the same time when change in bladder volume was estimated). Bladder Compliance was summarized for each cohort, each treatment group and total of treatment groups, using the merged data of studies A0221047 and A0221109 as planned. (NCT02501928)
Timeframe: Study A0221047: Baseline, Week 12; Study A0221109: Week 28, Final Visit (Week 28 for participants who completed the study or in case of early withdrawal the last assessment before Week 28 was considered to be the final visit)
| Intervention | milliliter per cm H2O (Mean) | |||
|---|---|---|---|---|
| Baseline | Change at Week 12 | Change at Week 28 | Change at Final Visit | |
| Cohort 1 | 7.00 | 9.00 | 8.65 | 8.65 |
| Cohort 2 | 6.97 | 20.06 | 13.22 | 13.22 |
| Fesoterodine 2 mg Capsule | 8.16 | 23.34 | 13.18 | 13.18 |
| Fesoterodine 4 mg Capsule | 4.20 | 12.40 | 13.30 | 13.30 |
| Fesoterodine 8 mg Tablet | 7.00 | 9.00 | 8.65 | 8.65 |
| Total of Treatment Groups | 6.98 | 18.22 | 12.39 | 12.39 |
Bladder volume at first IDC was measured using urodynamic testing. Bladder volume at first IDC was summarized for each cohort, each treatment group and total of treatment groups, using the merged data of studies A0221047 and A0221109 as planned. (NCT02501928)
Timeframe: Study A0221047: Baseline, Week 12; Study A0221109: Week 28, Final Visit (Week 28 for participants who completed the study or in case of early withdrawal the last assessment before Week 28 was considered to be the final visit)
| Intervention | milliliter (Mean) |
|---|---|
| Baseline | |
| Cohort 1 | 175.0 |
| Fesoterodine 8 mg Tablet | 175.0 |
Bladder volume at first IDC was measured using urodynamic testing. Bladder volume at first IDC was summarized for each cohort, each treatment group and total of treatment groups, using the merged data of studies A0221047 and A0221109 as planned. (NCT02501928)
Timeframe: Study A0221047: Baseline, Week 12; Study A0221109: Week 28, Final Visit (Week 28 for participants who completed the study or in case of early withdrawal the last assessment before Week 28 was considered to be the final visit)
| Intervention | milliliter (Mean) | |||
|---|---|---|---|---|
| Baseline | Change at Week 12 | Change at Week 28 | Change at Final Visit | |
| Cohort 2 | 48.8 | 95.0 | 50.4 | 50.4 |
| Fesoterodine 2 mg Capsule | 48.1 | 113.8 | 38.6 | 38.6 |
| Fesoterodine 4 mg Capsule | 50.3 | 70.0 | 70.0 | 70.0 |
| Total of Treatment Groups | 60.3 | 95.0 | 50.4 | 50.4 |
CBCL: assessed child's behavioral and emotional problems. Parent/caregiver of child answered 120 items, each on scale: 0=not true, 1=somewhat/sometimes true, 2=very/often true. 103 items were categorized in 8 domains: aggressive behavior, anxious/depressed, attention problems, rule-breaking behavior, social problems, somatic complaints, thought problems, withdrawn. Summary scores: Internalizing problems =anxious/depressed+withdrawn+somatic complaints; Externalizing problems =rule-breaking+aggressive behavior. Total problems =8 domains+other 17 items. Raw scores for each domain, summary and total problems =sum of scores of related items. Using ADM tool raw scores transformed/derived into standard T-scores, range: each domain=50-100, internalizing problems=34-100, externalizing problems=33-100, total problems=24-100. Lower T-score (8 domain,2 summary,total problems)=better outcomes. Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Final visit (Week 28 for participants who completed the study or in case of early withdrawal the last assessment before Week 28 was considered to be the final visit)
| Intervention | units on a scale (Mean) | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Aggressive behavior | Anxious/depressed | Attention problems | Rule-breaking behavior | Social problems | Somatic complaints | Thought problems | Withdrawn | Externalizing problems | Internalizing problems | Total problems | |
| Fesoterodine 2 mg Capsule | -1.9 | -0.6 | -0.9 | -0.9 | 0.3 | 1.0 | -0.1 | -1.7 | -3.0 | -2.1 | -1.4 |
| Fesoterodine 4 mg Capsule | -0.3 | 0.3 | 0.0 | 1.3 | 1.0 | -2.3 | -0.3 | 0.0 | 0.0 | -2.7 | 1.0 |
| Fesoterodine 8 mg Tablet | 0.0 | 0.0 | 0.0 | -0.5 | 0.0 | 0.0 | 0.0 | 0.0 | -3.0 | 0.0 | -2.5 |
CBCL: assessed child's behavioral and emotional problems. Parent/caregiver of child answered 120 items, each on scale: 0=not true, 1=somewhat/sometimes true, 2=very/often true. 103 items were categorized in 8 domains: aggressive behavior, anxious/depressed, attention problems, rule-breaking behavior, social problems, somatic complaints, thought problems, withdrawn. Summary scores: Internalizing problems =anxious/depressed+withdrawn+somatic complaints; Externalizing problems =rule-breaking+aggressive behavior. Total problems =8 domains+other 17 items. Raw scores for each domain, summary and total problems =sum of scores of related items. Using ADM tool raw scores transformed/derived into standard T-scores, range: each domain=50-100, internalizing problems=34-100, externalizing problems=33-100, total problems=24-100. Lower T-score (8 domain,2 summary,total problems)=better outcomes. Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Week 12
| Intervention | units on a scale (Mean) | |||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Aggressive behavior: Baseline | Aggressive behavior: Change at Week 12 | Anxious/depressed: Baseline | Anxious/depressed: Change at Week 12 | Attention problems: Baseline | Attention problems: Change at week 12 | Rule-breaking behavior: Baseline | Rule-breaking behavior: Change at Week 12 | Social problems: Baseline | Social problems: Change at Week 12 | Somatic complaints: Baseline | Somatic complaints: Change at Week 12 | Thought problems: Baseline | Thought problems: Change at Week 12 | Withdrawn: Baseline | Withdrawn: Change at Week 12 | Externalizing problems: Baseline | Externalizing problems: Change at Week 12 | Internalizing problems: Baseline | Internalizing problems: Change at Week 12 | Total problems: Baseline | Total problems: Change at Week 12 | |
| Fesoterodine 2 mg Capsule | 52.6 | -0.1 | 52.1 | 0.7 | 53.6 | -1.1 | 52.4 | -0.3 | 52.4 | 0.0 | 53.4 | 0.9 | 50.9 | 0.3 | 53.4 | -1.7 | 47.6 | -0.3 | 49.0 | 0.4 | 49.1 | -1.1 |
| Fesoterodine 4 mg Capsule | 50.7 | 0.0 | 50.7 | -0.7 | 53.3 | 0.0 | 53.3 | 0.0 | 54.3 | 0.7 | 55.7 | -2.3 | 53.0 | 0.0 | 52.7 | 0.0 | 44.0 | 0.0 | 47.7 | -4.0 | 46.7 | 0.3 |
| Fesoterodine 8 mg Tablet | 50.0 | 0.0 | 50.0 | 0.0 | 50.0 | 0.0 | 50.5 | 0.0 | 50.0 | 0.0 | 51.5 | 1.5 | 50.0 | 0.0 | 50.0 | 0.0 | 37.0 | 0.0 | 36.0 | 3.0 | 30.5 | 3.0 |
CBCL: assessed child's behavioral and emotional problems. Parent/caregiver of child answered 120 items, each on scale: 0=not true, 1=somewhat/sometimes true, 2=very/often true. 103 items were categorized in 8 domains: aggressive behavior, anxious/depressed, attention problems, rule-breaking behavior, social problems, somatic complaints, thought problems, withdrawn. Summary scores: Internalizing problems =anxious/depressed+withdrawn+somatic complaints; Externalizing problems =rule-breaking+aggressive behavior. Total problems =8 domains+other 17 items. Raw scores for each domain, summary and total problems =sum of scores of related items. Using ADM tool raw scores transformed/derived into standard T-scores, range: each domain=50-100, internalizing problems=34-100, externalizing problems=33-100, total problems=24-100. Lower T-score (8 domain,2 summary,total problems)=better outcomes. Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Week 28
| Intervention | units on a scale (Mean) | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Aggressive behavior | Anxious/depressed | Attention problems | Rule-breaking behavior | Social problems | Somatic complaints | Thought problems | Withdrawn | Externalizing problems | Internalizing problems | Total problems | |
| Fesoterodine 2 mg Capsule | -2.2 | -0.7 | -1.0 | -1.0 | 0.3 | 1.2 | -0.2 | -2.0 | -3.5 | -2.5 | -1.7 |
| Fesoterodine 4 mg Capsule | -0.3 | 0.3 | 0.0 | 1.3 | 1.0 | -2.3 | -0.3 | 0.0 | 0.0 | -2.7 | 1.0 |
| Fesoterodine 8 mg Tablet | 0.0 | 0.0 | 0.0 | -0.5 | 0.0 | 0.0 | 0.0 | 0.0 | -3.0 | 0.0 | -2.5 |
CBCL:assessed child's behavioral and emotional problems. Parent/caregiver of child answered 120 items, each on scale:0=not true, 1=somewhat/sometimes true, 2=very/often true. 103 items were classified in 8 domains: aggressive behavior, total score range (TSR) =0-36; anxious/depressed,TSR=0-26; attention problems,TSR=0-20; rule-breaking behavior, TSR=0-34; social problems, TSR=0-22; somatic complaints, TSR=0-22; thought problems, TSR=0-30; withdrawn, TSR=0-16. Summary scores: externalizing problems combined rule-breaking and aggressive behavior,TSR=0-70; internalizing problems combined anxious/depressed, withdrawn and somatic complaints, TSR=0-64. Total problems combined 8 domains and 17 remaining items,TSR=0-240. TSR for each domain, summary and total problems was sum of scores of related items respectively. Lower scores for each domain, summary, total problems = better outcomes.Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Final visit (Week 28 for participants who completed the study or in case of early withdrawal the last assessment before Week 28 was considered to be the final visit)
| Intervention | units on a scale (Mean) | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Aggressive behavior | Anxious/depressed | Attention problems | Rule-breaking behavior | Social problems | Somatic complaints | Thought problems | Withdrawn | Externalizing problems | Internalizing problems | Total problems | |
| Fesoterodine 2 mg Capsule | -1.6 | -0.3 | -0.4 | -0.1 | 0.1 | 0.3 | -0.1 | -0.4 | -1.7 | -0.4 | -2.3 |
| Fesoterodine 4 mg Capsule | -0.3 | 0.0 | 0.0 | 0.3 | 0.3 | -0.7 | -0.3 | 0.0 | 0.0 | -0.7 | 0.7 |
| Fesoterodine 8 mg Tablet | 0.0 | 0.0 | 0.0 | -0.5 | 0.0 | 0.0 | 0.0 | 0.0 | -0.5 | 0.0 | -0.5 |
CBCL:assessed child's behavioral and emotional problems. Parent/caregiver of child answered 120 items, each on scale:0=not true, 1=somewhat/sometimes true, 2=very/often true. 103 items were classified in 8 domains: aggressive behavior, total score range (TSR) =0-36; anxious/depressed,TSR=0-26; attention problems,TSR=0-20; rule-breaking behavior, TSR=0-34; social problems, TSR=0-22; somatic complaints, TSR=0-22; thought problems, TSR=0-30; withdrawn, TSR=0-16. Summary scores: externalizing problems combined rule-breaking and aggressive behavior,TSR=0-70; internalizing problems combined anxious/depressed, withdrawn and somatic complaints, TSR=0-64. Total problems combined 8 domains and 17 remaining items,TSR=0-240. TSR for each domain, summary and total problems was sum of scores of related items respectively. Lower scores for each domain, summary, total problems = better outcomes.Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Week 12
| Intervention | units on a scale (Mean) | |||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Aggressive behavior: Baseline | Aggressive behavior: Change at Week 12 | Anxious/depressed: Baseline | Anxious/depressed: Change at Week 12 | Attention problems: Baseline | Attention problems: Change at week 12 | Rule-breaking behavior: Baseline | Rule-breaking behavior: Change at Week 12 | Social problems: Baseline | Social problems: Change at Week 12 | Somatic complaints: Baseline | Somatic complaints: Change at Week 12 | Thought problems: Baseline | Thought problems: Change at Week 12 | Withdrawn: Baseline | Withdrawn: Change at Week 12 | Externalizing problems: Baseline | Externalizing problems: Change at Week 12 | Internalizing problems: Baseline | Internalizing problems: Change at Week 12 | Total problems: Baseline | Total problems: Change at Week 12 | |
| Fesoterodine 2 mg Capsule | 3.4 | -0.1 | 1.9 | 0.3 | 3.6 | -0.6 | 1.3 | -0.1 | 1.6 | 0.0 | 1.0 | 0.3 | 0.6 | -0.1 | 0.9 | -0.4 | 4.7 | -0.3 | 3.7 | 0.1 | 19.1 | -1.3 |
| Fesoterodine 4 mg Capsule | 2.0 | 0.0 | 1.3 | -0.7 | 3.0 | 0.0 | 1.3 | 0.0 | 2.3 | 0.3 | 1.7 | -0.7 | 1.3 | 0.0 | 0.7 | 0.0 | 3.3 | 0.0 | 3.7 | -1.3 | 18.0 | -0.3 |
| Fesoterodine 8 mg Tablet | 0.0 | 0.0 | 0.0 | 0.0 | 0.0 | 0.0 | 0.5 | 0.0 | 0.0 | 0.0 | 0.5 | 0.5 | 0.0 | 0.0 | 0.0 | 0.0 | 0.5 | 0.0 | 0.5 | 0.5 | 1.5 | 1.0 |
CBCL:assessed child's behavioral and emotional problems. Parent/caregiver of child answered 120 items, each on scale:0=not true, 1=somewhat/sometimes true, 2=very/often true. 103 items were classified in 8 domains: aggressive behavior, total score range (TSR) =0-36; anxious/depressed,TSR=0-26; attention problems,TSR=0-20; rule-breaking behavior, TSR=0-34; social problems, TSR=0-22; somatic complaints, TSR=0-22; thought problems, TSR=0-30; withdrawn, TSR=0-16. Summary scores: externalizing problems combined rule-breaking and aggressive behavior,TSR=0-70; internalizing problems combined anxious/depressed, withdrawn and somatic complaints, TSR=0-64. Total problems combined 8 domains and 17 remaining items,TSR=0-240. TSR for each domain, summary and total problems was sum of scores of related items respectively. Lower scores for each domain, summary, total problems = better outcomes.Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Week 28
| Intervention | units on a scale (Mean) | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Aggressive behavior | Anxious/depressed | Attention problems | Rule-breaking behavior | Social problems | Somatic complaints | Thought problems | Withdrawn | Externalizing problems | Internalizing problems | Total problems | |
| Fesoterodine 2 mg Capsule | -1.8 | -0.3 | -0.5 | -0.2 | 0.2 | 0.3 | -0.2 | -0.5 | -2.0 | -0.5 | -2.7 |
| Fesoterodine 4 mg Capsule | -0.3 | 0.0 | 0.0 | 0.3 | 0.3 | -0.7 | -0.3 | 0.0 | 0.0 | -0.7 | 0.7 |
| Fesoterodine 8 mg Tablet | 0.0 | 0.0 | 0.0 | -0.5 | 0.0 | 0.0 | 0.0 | 0.0 | -0.5 | 0.0 | -0.5 |
Detrusor pressure (cm H2O) at maximum urinary bladder capacity was measured using urodynamic testing. Detrusor pressure was summarized for each cohort, each treatment group and total of treatment groups, using the merged data of studies A0221047 and A0221109 as planned. (NCT02501928)
Timeframe: Study A0221047: Baseline, Week 12; Study A0221109: Week 28, Final Visit (Week 28 for participants who completed the study or in case of early withdrawal the last assessment before Week 28 was considered to be the final visit)
| Intervention | cm H2O (Mean) | |||
|---|---|---|---|---|
| Baseline | Change at Week 12 | Change at Week 28 | Change at Final Visit | |
| Cohort 1 | 29.0 | -5.5 | -7.0 | -7.0 |
| Cohort 2 | 40.2 | -13.7 | -4.3 | -4.3 |
| Fesoterodine 2 mg Capsule | 32.4 | -6.0 | -2.8 | -2.8 |
| Fesoterodine 4 mg Capsule | 58.3 | -31.7 | -7.3 | -7.3 |
| Fesoterodine 8 mg Tablet | 29.0 | -5.5 | -7.0 | -7.0 |
| Total of Treatment Groups | 38.3 | -12.3 | -4.8 | -4.8 |
The grooved pegboard test was a manipulative dexterity test that assessed psychomotor speed, fine motor control, and rapid-visual motor coordination. Participants were asked to insert 10 grooved pegs into the holes within the given time limit up to 300 seconds. The task needs to be completed once for each hand; firstly, using the dominant hand followed by the non-dominant hand. Number of pegs dropped while putting in the holes were measured. Participants were assigned to either a 10 or 25-peg assessment based on their age. 10-peg assessment was done on participants below age of 9 years. In this outcome measure data for dominant and non-dominant hand have been reported separately. Data for this outcome measure was planned to be analyzed for each treatment group of Study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, final visit (Week 28 for participants who completed the study or in case of early withdrawal the last assessment before Week 28 was considered to be the final visit)
| Intervention | pegs (Mean) | |
|---|---|---|
| Dominant hand | Non-dominant hand | |
| Fesoterodine 2 mg Capsule | 0.2 | 0.0 |
| Fesoterodine 4 mg Capsule | 0.0 | 0.0 |
The grooved pegboard test was a manipulative dexterity test that assessed psychomotor speed, fine motor control, and rapid-visual motor coordination. Participants were asked to insert 10 grooved pegs into the holes within the given time limit (up to 300 seconds). The task needs to be completed once for each hand; firstly, using the dominant hand followed by the non-dominant hand. Number of pegs placed correctly in hole was measured. Participants were assigned to either a 10 or 25-peg assessment based on their age. 10-peg assessment was done on participants below age of 9 years. In this outcome measure data for dominant and non-dominant hand have been reported separately. Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Final visit (Week 28 for participants who completed the study or in case of early withdrawal the last assessment before Week 28 was considered to be the final visit)
| Intervention | pegs (Mean) | |
|---|---|---|
| Dominant hand | Non-dominant hand | |
| Fesoterodine 2 mg Capsule | 0.0 | 0.0 |
| Fesoterodine 4 mg Capsule | 0.0 | 0.0 |
The grooved pegboard test was a manipulative dexterity test that assessed psychomotor speed, fine motor control, and rapid-visual motor coordination. Participants were asked to insert 10 grooved pegs into holes within the given time limit up to 300 seconds. The task needs to be completed once for each hand; firstly, using the dominant hand followed by the non-dominant hand. Time taken to complete the test was inversely correlated to the cognitive ability. Participants were assigned to either a 10 or 25-peg assessment based on their age. 10-peg assessment was done on participants below age of 9 years. In this outcome measure data for dominant and non-dominant hand have been reported separately. Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Final visit (Week 28 for participants who completed the study or in case of early withdrawal the last assessment before Week 28 was considered to be the final visit)
| Intervention | seconds (Mean) | |
|---|---|---|
| Dominant hand | Non-dominant hand | |
| Fesoterodine 2 mg Capsule | 0.8 | 4.4 |
| Fesoterodine 4 mg Capsule | 3.7 | -7.7 |
The grooved pegboard test was a manipulative dexterity test that assessed psychomotor speed, fine motor control, and rapid-visual motor coordination. Participants were asked to insert 10 grooved pegs into the holes within the given time limit up to 300 seconds. The task needs to be completed once for each hand; firstly, using the dominant hand followed by the non-dominant hand. Number of pegs dropped while putting in the holes were measured. Participants were assigned to either a 10 or 25-peg assessment based on their age. 10-peg assessment was done on participants below age of 9 years. In this outcome measure data for dominant and non-dominant hand have been reported separately. Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Week 12
| Intervention | pegs (Mean) | |||
|---|---|---|---|---|
| Dominant hand: Baseline | Dominant hand: Change at Week 12 | Non-dominant hand: Baseline | Non-dominant hand: Change at Week 12 | |
| Fesoterodine 2 mg Capsule | 0.2 | 0.2 | 0.0 | 0.6 |
| Fesoterodine 4 mg Capsule | 0.0 | 0.0 | 0.0 | 0.0 |
The grooved pegboard test was a manipulative dexterity test that assessed psychomotor speed, fine motor control, and rapid-visual motor coordination. Participants were asked to insert 10 grooved pegs into the holes within the given time limit up to 300 seconds. The task needs to be completed once for each hand; firstly, using the dominant hand followed by the non-dominant hand. Number of pegs placed correctly in hole was measured. Participants were assigned to either a 10 or 25-peg assessment based on their age. 10-peg assessment was done on participants below age of 9 years. In this outcome measure data for dominant and non-dominant hand have been reported separately. Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Week 12
| Intervention | pegs (Mean) | |||
|---|---|---|---|---|
| Dominant hand: Baseline | Dominant hand: Change at Week 12 | Non-dominant hand: Baseline | Non-dominant hand: Change at Week 12 | |
| Fesoterodine 2 mg Capsule | 10.0 | 0.0 | 10.0 | 0.0 |
| Fesoterodine 4 mg Capsule | 10.0 | 0.0 | 10.0 | 0.0 |
The grooved pegboard test was a manipulative dexterity test that assessed psychomotor speed, fine motor control, and rapid-visual motor coordination. Participants were asked to insert 10 grooved pegs into holes within the given time limit up to 300 seconds. The task needs to be completed once for each hand; firstly, using the dominant hand followed by the non-dominant hand. Time taken to complete the test was inversely correlated to the cognitive ability. Participants were assigned to either a 10 or 25-peg assessment based on their age. 10-peg assessment was done on participants below age of 9 years. In this outcome measure data for dominant and non-dominant hand have been reported separately. Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Week 12
| Intervention | seconds (Mean) | |||
|---|---|---|---|---|
| Dominant hand: Baseline | Dominant hand: Change at Week 12 | Non-dominant hand: Baseline | Non-dominant hand: Change at Week 12 | |
| Fesoterodine 2 mg Capsule | 43.0 | 0.8 | 33.4 | 8.2 |
| Fesoterodine 4 mg Capsule | 39.3 | -0.3 | 52.0 | -1.3 |
The grooved pegboard test was a manipulative dexterity test that assessed psychomotor speed, fine motor control, and rapid-visual motor coordination. Participants were asked to insert 10 grooved pegs into the holes within the given time limit up to 300 seconds. The task needs to be completed once for each hand; firstly, using the dominant hand followed by the non-dominant hand. Number of pegs dropped while putting in the holes were measured. Participants were assigned to either a 10 or 25-peg assessment based on their age. 10-peg assessment was done on participants below age of 9 years. In this outcome measure data for dominant and non-dominant hand have been reported separately. Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Week 28
| Intervention | pegs (Mean) | |
|---|---|---|
| Dominant hand | Non-dominant hand | |
| Fesoterodine 2 mg Capsule | 0.3 | 0.0 |
| Fesoterodine 4 mg Capsule | 0.0 | 0.0 |
The grooved pegboard test was a manipulative dexterity test that assessed psychomotor speed, fine motor control, and rapid-visual motor coordination. Participants were asked to insert 10 grooved pegs into the holes within the given time limit up to 300 seconds. The task needs to be completed once for each hand; firstly, using the dominant hand followed by the non-dominant hand. Number of pegs placed correctly in hole was measured. Participants were assigned to either a 10 or 25-peg assessment based on their age. 10-peg assessment was done on participants below age of 9 years. In this outcome measure data for dominant and non-dominant hand have been reported separately. Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Week 28
| Intervention | pegs (Mean) | |
|---|---|---|
| Dominant hand | Non-dominant hand | |
| Fesoterodine 2 mg Capsule | 0.0 | 0.0 |
| Fesoterodine 4 mg Capsule | 0.0 | 0.0 |
The grooved pegboard test was a manipulative dexterity test that assessed psychomotor speed, fine motor control, and rapid-visual motor coordination. Participants were asked to insert 10 grooved pegs into holes within the given time limit (up to 300 seconds). The task needs to be completed once for each hand; firstly, using the dominant hand followed by the non-dominant hand. Time taken to complete the test was inversely correlated to the cognitive ability. Participants were assigned to either a 10 or 25-peg assessment based on their age. 10-peg assessment was done on participants below age of 9 years. In this outcome measure data for dominant and non-dominant hand have been reported separately. Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Week 28
| Intervention | seconds (Mean) | |
|---|---|---|
| Dominant hand | Non-dominant hand | |
| Fesoterodine 2 mg Capsule | 4.5 | 6.3 |
| Fesoterodine 4 mg Capsule | 3.7 | -7.7 |
VA was assessed for each eye using the Snellen method, where logMAR units were derived from the Snellen ratios. Participants had to read letters from the chart at a distance of 20 feet/6 meter or 4 meter. VA (Snellen ratio) = distance between the chart and participant, divided by distance at which participant was able to see/read chart without impairment; expressed as decimal. logMAR = log10 (1/decimal VA). In this outcome measure, data have been reported for right and left eye separately. Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Final visit (Week 28 for participants who completed the study or in case of early withdrawal the last assessment before Week 28 was considered to be the final visit)
| Intervention | LogMAR (Mean) | |
|---|---|---|
| Right Eye | Left Eye | |
| Fesoterodine 2 mg Capsule | 0.02 | 0.04 |
| Fesoterodine 4 mg Capsule | 0.02 | 0.16 |
| Fesoterodine 8 mg Tablet | 0.00 | 0.31 |
Visual acuity (VA) was assessed for each eye using the Snellen method, where logarithm of minimum angle of resolution (logMAR) units were derived from the Snellen ratios. Participants had to read letters from the chart at a distance of 20 feet/6 meter or 4 meter. VA (Snellen ratio) = distance between the chart and participant, divided by distance at which participant was able to see/read chart without impairment; expressed as decimal. logMAR = log10 (1/decimal VA). In this outcome measure, data have been reported for right and left eye separately. Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Week 12
| Intervention | LogMAR (Mean) | |||
|---|---|---|---|---|
| Right Eye: Baseline | Right Eye: Change at Week 12 | Left Eye: Baseline | Left Eye: Change at Week 12 | |
| Fesoterodine 2 mg Capsule | 0.04 | -0.03 | 0.04 | 0.03 |
| Fesoterodine 4 mg Capsule | 0.28 | 0.04 | 0.63 | 0.07 |
| Fesoterodine 8 mg Tablet | 0.27 | 0.14 | 0.45 | 0.03 |
VA was assessed for each eye using the Snellen method, where logMAR units were derived from the Snellen ratios. Participants had to read letters from the chart at a distance of 20 feet/6 meter or 4 meter. VA (Snellen ratio) = distance between the chart and participant, divided by distance at which participant was able to see/read chart without impairment; expressed as decimal. logMAR = log10 (1/decimal VA). In this outcome measure, data have been reported for right and left eye separately. Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Week 28
| Intervention | LogMAR (Mean) | |
|---|---|---|
| Right Eye | Left Eye | |
| Fesoterodine 2 mg Capsule | 0.03 | 0.05 |
| Fesoterodine 4 mg Capsule | 0.02 | 0.16 |
| Fesoterodine 8 mg Tablet | 0.00 | 0.31 |
Systolic and diastolic blood pressure were evaluated for examination of vital signs. Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Final visit (Week 28 for participants who completed the study or in case of early withdrawal the last assessment before Week 28 was considered to be the final visit)
| Intervention | millimeter of mercury (Mean) | |
|---|---|---|
| Systolic blood pressure | Diastolic blood pressure | |
| Fesoterodine 2 mg Capsule | 5.1 | 4.6 |
| Fesoterodine 4 mg Capsule | 9.7 | 10.7 |
| Fesoterodine 8 mg Tablet | 8.5 | 12.0 |
Systolic and diastolic blood pressure were evaluated for examination of vital signs. Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Week 12
| Intervention | millimeter of mercury (Mean) | |
|---|---|---|
| Systolic blood pressure | Diastolic blood pressure | |
| Fesoterodine 2 mg Capsule | 2.1 | -0.9 |
| Fesoterodine 4 mg Capsule | 5.0 | 6.3 |
| Fesoterodine 8 mg Tablet | 6.0 | 10.5 |
Systolic and diastolic blood pressure were evaluated for examination of vital signs. Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Week 28
| Intervention | millimeter of mercury (Mean) | |
|---|---|---|
| Systolic blood pressure | Diastolic blood pressure | |
| Fesoterodine 2 mg Capsule | 5.7 | 5.3 |
| Fesoterodine 4 mg Capsule | 9.7 | 10.7 |
| Fesoterodine 8 mg Tablet | 8.5 | 12.0 |
Participants with presence of IDC was summarized for each cohort, each treatment group and total of treatment groups, using the merged data of studies A0221047 and A0221109 as planned. (NCT02501928)
Timeframe: Study A0221047: Baseline, Week 12; Study A0221109: Week 28, Final Visit (Week 28 for participants who completed the study or in case of early withdrawal the last assessment before Week 28 was considered to be the final visit)
| Intervention | Participants (Count of Participants) | |||
|---|---|---|---|---|
| Baseline | Week 12 | Week 28 | Final Visit | |
| Cohort 1 | 1 | 0 | 0 | 0 |
| Cohort 2 | 10 | 7 | 8 | 8 |
| Fesoterodine 2 mg Capsule | 7 | 4 | 5 | 5 |
| Fesoterodine 4 mg Capsule | 3 | 3 | 3 | 3 |
| Fesoterodine 8 mg Tablet | 1 | 0 | 0 | 0 |
| Total of Treatment Groups | 11 | 7 | 8 | 8 |
An AE was any untoward medical occurrence in a participant who received investigational product without regard to possibility of causal relationship. SAE was an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly; medically important events. A treatment emergent AE was defined as an event that emerged during the treatment period that was absent before treatment, or worsened during the treatment period relative to the pretreatment state. AEs included both serious and non-serious adverse events. TEAEs were summarized for each cohort (Cohort 1 and Cohort 2, irrespective of treatment received), each treatment group and the total of treatment groups, using the merged data of studies A0221047 and A0221109 as planned. (NCT02501928)
Timeframe: Up to a maximum of 56 weeks (24 weeks of treatment in A0221047 and 32 weeks [28 weeks treatment + 4 weeks follow up post last dose] in A0221109)
| Intervention | Participants (Count of Participants) | |
|---|---|---|
| Participants with AEs | Participants with SAEs | |
| Cohort 1 | 2 | 0 |
| Cohort 2 | 9 | 1 |
| Fesoterodine 2 mg Capsule | 6 | 1 |
| Fesoterodine 4 mg Capsule | 3 | 0 |
| Fesoterodine 8 mg Tablet | 2 | 0 |
| Total of Treatment Groups | 11 | 1 |
The grooved pegboard test was a manipulative dexterity test that assessed psychomotor speed, fine motor control, and rapid-visual motor coordination. Participants were asked to insert 25 grooved pegs into the holes within the given time limit up to 300 seconds. The task needs to be completed once for each hand; firstly, using the dominant hand followed by the non-dominant hand. Number of pegs dropped while putting in the holes were measured. Participants were assigned to either a 10 or 25-peg assessment based on their age. 25-peg assessment was done on participants of age 9 years and above. In this outcome measure data for dominant and non-dominant hand have been reported separately. Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Week 12
| Intervention | pegs (Mean) | |||
|---|---|---|---|---|
| Dominant hand: Baseline | Dominant hand: Change at Week 12 | Non-dominant hand: Baseline | Non-dominant hand: Change at Week 12 | |
| Fesoterodine 2 mg Capsule | 0.5 | -0.5 | 0.5 | -0.5 |
| Fesoterodine 8 mg Tablet | 0.0 | 0.0 | 0.0 | 0.0 |
The grooved pegboard test was a manipulative dexterity test that assessed psychomotor speed, fine motor control, and rapid-visual motor coordination. Participants were asked to insert 25 grooved pegs into the holes within the given time limit up to 300 seconds. The task needs to be completed once for each hand; firstly, using the dominant hand followed by the non-dominant hand. Number of pegs dropped while putting in the holes were measured. Participants were assigned to either a 10- or 25-peg assessment based on their age. 25-peg assessment was done on participants of age 9 years and above. In this outcome measure data for dominant and non-dominant hand have been reported separately. Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Final visit (Week 28 for participants who completed the study or in case of early withdrawal the last assessment before Week 28 was considered to be the final visit)
| Intervention | pegs (Mean) | |
|---|---|---|
| Dominant hand | Non-dominant hand | |
| Fesoterodine 2 mg Capsule | 0.0 | -0.5 |
| Fesoterodine 8 mg Tablet | 0.0 | 0.0 |
The grooved pegboard test was a manipulative dexterity test that assessed psychomotor speed, fine motor control, and rapid-visual motor coordination. Participants were asked to insert 25 grooved pegs into the holes within the given time limit up to 300 seconds. The task needs to be completed once for each hand; firstly, using the dominant hand followed by the non-dominant hand. Number of pegs placed correctly in hole was measured. Participants were assigned to either a 10 or 25-peg assessment based on their age. 25-peg assessment was done on participants of age 9 years and above. In this outcome measure data for dominant and non-dominant hand have been reported separately. Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Final visit (Week 28 for participants who completed the study or in case of early withdrawal the last assessment before Week 28 was considered to be the final visit)
| Intervention | pegs (Mean) | |
|---|---|---|
| Dominant hand | Non-dominant hand | |
| Fesoterodine 2 mg Capsule | 0.0 | 0.0 |
| Fesoterodine 8 mg Tablet | 0.0 | 0.0 |
The grooved pegboard test was a manipulative dexterity test that assessed psychomotor speed, fine motor control, and rapid-visual motor coordination. Participants were asked to insert 25 grooved pegs into holes within the given time limit up to 300 seconds. The task needs to be completed once for each hand; firstly, using the dominant hand followed by the non-dominant hand. Time taken to complete the test was inversely correlated to the cognitive ability. Participants were assigned to either a 10 or 25-peg assessment based on their age. 25-peg assessment was done on participants of age 9 years and above. In this outcome measure data for dominant and non-dominant hand have been reported separately. Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Week 12
| Intervention | seconds (Mean) | |||
|---|---|---|---|---|
| Dominant hand: Baseline | Dominant hand: Change at Week 12 | Non-dominant hand: Baseline | Non-dominant hand: Change at Week 12 | |
| Fesoterodine 2 mg Capsule | 107.5 | -11.5 | 145.5 | -2.0 |
| Fesoterodine 8 mg Tablet | 59.5 | 0.0 | 60.5 | -0.5 |
The grooved pegboard test was a manipulative dexterity test that assessed psychomotor speed, fine motor control, and rapid-visual motor coordination. Participants were asked to insert 25 grooved pegs into the holes within the given time limit up to 300 seconds. The task needs to be completed once for each hand; firstly, using the dominant hand followed by the non-dominant hand. Number of pegs dropped while putting in the holes were measured. Participants were assigned to either a 10 or 25-peg assessment based on their age. 25-peg assessment was done on participants of age 9 years and above. In this outcome measure data for dominant and non-dominant hand have been reported separately. Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Week 28
| Intervention | pegs (Mean) | |
|---|---|---|
| Dominant hand | Non-dominant hand | |
| Fesoterodine 2 mg Capsule | 0.0 | -0.5 |
| Fesoterodine 8 mg Tablet | 0.0 | 0.0 |
The grooved pegboard test was a manipulative dexterity test that assessed psychomotor speed, fine motor control, and rapid-visual motor coordination. Participants were asked to insert 25 grooved pegs into the holes within the given time limit (up to 300 seconds). The task needs to be completed once for each hand; firstly, using the dominant hand followed by the non-dominant hand. Number of pegs placed correctly in hole was measured. Participants were assigned to either a 10 or 25-peg assessment based on their age. 25-peg assessment was done on participants of age 9 years and above. In this outcome measure data for dominant and non-dominant hand have been reported separately. Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Week 28
| Intervention | pegs (Mean) | |
|---|---|---|
| Dominant hand | Non-dominant hand | |
| Fesoterodine 2 mg Capsule | 0.0 | 0.0 |
| Fesoterodine 8 mg Tablet | 0.0 | 0.0 |
The grooved pegboard test was a manipulative dexterity test that assessed psychomotor speed, fine motor control, and rapid-visual motor coordination. Participants were asked to insert 25 grooved pegs into the holes within the given time limit (up to 300 seconds). The task needs to be completed once for each hand; firstly, using the dominant hand followed by the non-dominant hand. Time taken to complete the test was inversely correlated to the cognitive ability. Participants were assigned to either a 10 or 25-peg assessment based on their age. 25-peg assessment was done on participants of age 9 years and above. In this outcome measure data for dominant and non-dominant hand have been reported separately. Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Week 28
| Intervention | seconds (Mean) | |
|---|---|---|
| Dominant hand | Non-dominant hand | |
| Fesoterodine 2 mg Capsule | -14.0 | -35.0 |
| Fesoterodine 8 mg Tablet | 2.0 | -1.0 |
Maximum cystometric bladder capacity was defined as maximal tolerable cystometric capacity, until voiding or leaking begins or at a pressure of >=40 centimeter (cm) water (H2O). Maximum cystometric bladder capacity was summarized for each cohort, each treatment group and total of treatment groups, using the merged data of studies A0221047 and A0221109 as planned. (NCT02501928)
Timeframe: Study A0221047: Baseline, Week 12; Study A0221109: Week 28, Final Visit (Week 28 for participants who completed the study or in case of early withdrawal the last assessment before Week 28 was considered to be the final visit)
| Intervention | milliliter (Mean) | |||
|---|---|---|---|---|
| Baseline | Change at Week 12 | Change at Week 28 | Change at Final Visit | |
| Cohort 1 | 181.0 | 153.0 | 121.5 | 121.5 |
| Cohort 2 | 135.5 | 42.9 | 37.9 | 37.9 |
| Fesoterodine 2 mg Capsule | 149.7 | 37.6 | 32.8 | 32.8 |
| Fesoterodine 4 mg Capsule | 102.3 | 55.3 | 48.0 | 48.0 |
| Fesoterodine 8 mg Tablet | 181.0 | 153.0 | 121.5 | 121.5 |
| Total of Treatment Groups | 143.1 | 61.3 | 53.1 | 53.1 |
The mean number of catheterizations per 24 hours were calculated as the total number of catheterizations divided by the total number of diary days collected at the assessment time point. Number of diary days collected at the assessment time point = number of calendar days when the diary was completed, even if it was not a full 24 hour period. This outcome measure was only calculated for participants with >0 catheterizations at Baseline. Data was summarized for each cohort, each treatment group and total of treatment groups, using the merged data of studies A0221047 and A0221109 as planned. (NCT02501928)
Timeframe: Study A0221047: Baseline, Week 12; Study A0221109: Week 28, Final Visit (Week 28 for participants who completed the study or in case of early withdrawal the last assessment before Week 28 was considered to be the final visit)
| Intervention | catheterizations per 24 hours (Mean) | |||
|---|---|---|---|---|
| Baseline | Change at Week 12 | Change at Week 28 | Change at Final Visit | |
| Cohort 1 | 5.33 | 0.00 | 0.33 | 0.33 |
| Cohort 2 | 4.47 | 0.05 | -0.09 | -0.12 |
| Fesoterodine 2 mg Capsule | 4.24 | 0.03 | -0.19 | -0.21 |
| Fesoterodine 4 mg Capsule | 5.00 | 0.11 | 0.11 | 0.11 |
| Fesoterodine 8 mg Tablet | 5.33 | 0.00 | 0.33 | 0.33 |
| Total of Treatment Groups | 4.61 | 0.04 | -0.02 | -0.04 |
The mean number of incontinence episodes per 24 hours were calculated as the total number of incontinence episodes divided by the total number of diary days collected at the assessment time point. Number of diary days collected at the assessment time point = number of calendar days when the diary was completed, even if it was not a full 24 hour period. This outcome measure was only calculated for participants with >0 incontinence episodes at Baseline. Data was summarized for each cohort, each treatment group and total of treatment groups, using the merged data of studies A0221047 and A0221109 as planned. (NCT02501928)
Timeframe: Study A0221047: Baseline, Week 12; Study A0221109: Week 28, Final Visit (Week 28 for participants who completed the study or in case of early withdrawal the last assessment before Week 28 was considered to be the final visit)
| Intervention | incontinence episodes per 24 hours (Mean) | |||
|---|---|---|---|---|
| Baseline | Change at Week 12 | Change at Week 28 | Change at Final Visit | |
| Cohort 1 | 1.17 | 0.50 | 1.83 | 1.83 |
| Cohort 2 | 3.60 | -0.18 | -0.31 | 0.08 |
| Fesoterodine 2 mg Capsule | 3.48 | -0.26 | -0.42 | 0.17 |
| Fesoterodine 4 mg Capsule | 3.89 | 0.00 | -0.11 | -0.11 |
| Fesoterodine 8 mg Tablet | 1.17 | 0.50 | 1.83 | 1.83 |
| Total of Treatment Groups | 3.19 | -0.07 | 0.08 | 0.38 |
The grooved pegboard test was a manipulative dexterity test that assessed psychomotor speed, fine motor control, and rapid-visual motor coordination. Participants were asked to insert 25 grooved pegs into the holes within the given time limit up to 300 seconds. The task needs to be completed once for each hand; firstly, using the dominant hand followed by the non-dominant hand. Time taken to complete the test was inversely correlated to the cognitive ability. Participants were assigned to either a 10 or 25-peg assessment based on their age. 25-peg assessment was done on participants of age 9 years and above. In this outcome measure data for dominant and non-dominant hand have been reported separately. Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Final visit (Week 28 for participants who completed the study or in case of early withdrawal the last assessment before Week 28 was considered to be the final visit)
| Intervention | seconds (Mean) | |
|---|---|---|
| Dominant hand | Non-dominant hand | |
| Fesoterodine 2 mg Capsule | -14.0 | -35.0 |
| Fesoterodine 8 mg Tablet | 2.08 | -1.0 |
The mean number of micturitions per 24 hours were calculated as the total number of micturitions divided by the total number of diary days collected at the assessment time point. Number of diary days collected at the assessment time point = number of calendar days when the diary was completed on, even if it was not a full 24 hour period. This outcome measure was only calculated for participants with >0 micturitions at Baseline. Data was summarized for each cohort, each treatment group and total of treatment groups, using the merged data of studies A0221047 and A0221109 as planned. (NCT02501928)
Timeframe: Study A0221047: Baseline, Week 12; Study A0221109: Week 28, Final Visit (Week 28 for participants who completed the study or in case of early withdrawal the last assessment before Week 28 was considered to be the final visit)
| Intervention | micturitions per 24 hours (Mean) | |||
|---|---|---|---|---|
| Baseline | Change at Week 12 | Change at Week 28 | Change at Final Visit | |
| Cohort 2 | 4.58 | -1.50 | -1.08 | -1.08 |
| Fesoterodine 2 mg Capsule | 4.58 | -1.50 | -1.08 | -1.08 |
| Total of Treatment Groups | 4.58 | -1.50 | -1.08 | -1.08 |
The grooved pegboard test was a manipulative dexterity test that assessed psychomotor speed, fine motor control, and rapid-visual motor coordination. Participants were asked to insert 25 grooved pegs into the holes within the given time limit up to 300 seconds. The task needs to be completed once for each hand; firstly, using the dominant hand followed by the non-dominant hand. Number of pegs placed correctly in hole was measured. Participants were assigned to either a 10 or 25-peg assessment based on their age. 25-peg assessment was done on participants of age 9 years and above. In this outcome measure data for dominant and non-dominant hand have been reported separately. Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Week 12
| Intervention | pegs (Mean) | |||
|---|---|---|---|---|
| Dominant hand: Baseline | Dominant hand: Change at Week 12 | Non-dominant hand: Baseline | Non-dominant hand: Change at Week 12 | |
| Fesoterodine 2 mg Capsule | 25.0 | 0.0 | 25.0 | 0.0 |
| Fesoterodine 8 mg Tablet | 25.0 | 0.0 | 25.0 | 0.0 |
The mean number of urgency episodes per 24 hours were calculated as the total number of urgency episodes divided by the total number of diary days collected at the assessment time point. Number of diary days collected at the assessment time point = number of calendar days when the diary was completed, even if it was not a full 24 hour period. Urgency episodes were defined as urgency marked as 'yes' in the diary. This outcome measure was only calculated for sensate participants with >0 urgency episodes at Baseline. Data was summarized for each cohort, each treatment group and total of treatment groups, using the merged data of studies A0221047 and A0221109 as planned. (NCT02501928)
Timeframe: Study A0221047: Baseline, Week 12; Study A0221109: Week 28, Final Visit (Week 28 for participants who completed the study or in case of early withdrawal the last assessment before Week 28 was considered to be the final visit)
| Intervention | urgency episodes per 24 hours (Mean) | |||
|---|---|---|---|---|
| Baseline | Change at Week 12 | Change at Week 28 | Change at Final Visit | |
| Cohort 2 | 0.61 | -0.61 | -0.61 | -0.61 |
| Fesoterodine 2 mg Capsule | 0.75 | -0.75 | -0.75 | -0.75 |
| Fesoterodine 4 mg Capsule | 0.33 | -0.33 | -0.33 | -0.33 |
| Total of Treatment Groups | 0.61 | -0.61 | -0.61 | -0.61 |
The mean volume per catheterization was calculated as sum of voided volume divided by the total number of catheterization, with a recorded voided volume >0. This outcome measure included only participants who actually had the records of volume voided per catherization. Data was summarized for each cohort, each treatment group and total of treatment groups, using the merged data of studies A0221047 and A0221109 as planned. (NCT02501928)
Timeframe: Study A0221047: Baseline, Week 12; Study A0221109: Week 28, Final Visit (Week 28 for participants who completed the study or in case of early withdrawal the last assessment before Week 28 was considered to be the final visit)
| Intervention | milliliter per catheterization (Mean) | |||
|---|---|---|---|---|
| Baseline | Change at Week 12 | Change at Week 28 | Change at Final Visit | |
| Cohort 1 | 198.75 | -0.92 | -29.42 | -29.42 |
| Cohort 2 | 58.31 | 20.66 | 11.58 | 11.58 |
| Fesoterodine 2 mg Capsule | 48.76 | 17.90 | 8.72 | 8.72 |
| Fesoterodine 4 mg Capsule | 80.58 | 27.08 | 17.28 | 17.28 |
| Fesoterodine 8 mg Tablet | 198.75 | -0.92 | -29.42 | -29.42 |
| Total of Treatment Groups | 81.72 | 17.06 | 4.12 | 4.12 |
The mean voided volume per micturition was calculated as sum of voided volume divided by the total number of micturition episodes with a recorded voided volume >0. This outcome measure included only participants who actually had the records of volume voided per micturition. Data was summarized for each cohort, each treatment group and total of treatment groups, using the merged data of studies A0221047 and A0221109 as planned. (NCT02501928)
Timeframe: Study A0221047: Baseline, Week 12; Study A0221109: Week 28, Final Visit (Week 28 for participants who completed the study or in case of early withdrawal the last assessment before Week 28 was considered to be the final visit)
| Intervention | milliliter per micturition (Mean) | |||
|---|---|---|---|---|
| Baseline | Change at Week 12 | Change at Week 28 | Change at Final Visit | |
| Cohort 2 | 73.42 | 15.77 | 4.75 | 4.75 |
| Fesoterodine 2 mg Capsule | 73.42 | 15.77 | 4.75 | 4.75 |
| Total of Treatment Groups | 73.42 | 15.77 | 4.75 | 4.75 |
The mean voided volume per micturition or catheterization was calculated as sum of voided volume divided by the total number of micturition or catheterization episodes with a recorded voided volume >0. Data was summarized for each cohort, each treatment group and total of treatment groups, using the merged data of studies A0221047 and A0221109 as planned. (NCT02501928)
Timeframe: Study A0221047: Baseline, Week 12; Study A0221109: Week 28, Final Visit (Week 28 for participants who completed the study or in case of early withdrawal the last assessment before Week 28 was considered to be the final visit)
| Intervention | mL per micturition or catheterization (Mean) | |||
|---|---|---|---|---|
| Baseline | Change at Week 12 | Change at Week 28 | Change at Final Visit | |
| Cohort 1 | 198.75 | -0.92 | -29.42 | -29.42 |
| Cohort 2 | 65.68 | 17.88 | 12.34 | 12.34 |
| Fesoterodine 2 mg Capsule | 59.29 | 13.94 | 9.86 | 9.86 |
| Fesoterodine 4 mg Capsule | 80.58 | 27.08 | 17.28 | 17.28 |
| Fesoterodine 8 mg Tablet | 198.75 | -0.92 | -29.42 | -29.42 |
| Total of Treatment Groups | 87.86 | 14.75 | 4.75 | 4.75 |
The visual accommodation was the minimum focusing distance for each eye at which vision became blurred - the mean of triplicate measurements. The participants focused on a single letter of the 20/40 line of an eye chart and chart was moved slowly towards the participant until letter was blurred. At this point, the distance from eye to letter was measured for each eye. In this outcome measure data have been reported for right and left eye separately. Data for this outcome measure was planned to be analyzed for each treatment group of study A0221109 only. (NCT02501928)
Timeframe: A0221109: Baseline, Final visit (Week 28 for participants who completed the study or in case of early withdrawal the last assessment before Week 28 was considered to be the final visit)
| Intervention | centimeter (Mean) | |
|---|---|---|
| Right Eye | Left Eye | |
| Fesoterodine 2 mg Capsule | 4.38 | 2.86 |
| Fesoterodine 4 mg Capsule | -0.11 | 0.50 |
| Fesoterodine 8 mg Tablet | 5.17 | 3.17 |
Physical activity was measured by using accelerometer worn over the course of a week at follow up. Average daily step counts were derived from this weeklong measurement. (NCT03946124)
Timeframe: 1 week
| Intervention | steps per day (Median) |
|---|---|
| Fesoterodine | 1634.19 |
Statistical testing was used to determine if there was a difference in inflammatory markers in the urine of patients between baseline visit and 6 week visit. 7 markers were chosen and compared, all inflammatory markers present in urine. (NCT04090190)
Timeframe: Baseline and 6 weeks
| Intervention | pg/mL (Median) | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline CRP | Follow-up CRP | Baseline IL-12/IL-23p40 | Follow-up IL-12/IL-23p40 | Baseline MCP-1 | Follow-up MCP-1 | Baseline GM-CSF | Follow-up GM CSF | Baseline IL-1B | Follow-up IL-1B | Baseline IL-6 | Follow-up IL-6 | Baseline IL-8 | Follow-up IL-8 | |
| Standard of Care Anticholinergic Treatment | 2.192 | 2.565 | 2.192 | 2.565 | 75.49 | 65.02 | 0.102 | 0.203 | 0.203 | 0.415 | 0.667 | 0.967 | 7.211 | 6.116 |
The change in g_lactobacillus from Baseline to Follow-up (6 weeks), which corresponds to before and after anticholinergic treatment. (NCT04090190)
Timeframe: At the 6 week mark
| Intervention | pg/mL (Median) |
|---|---|
| Standard of Care Anticholinergic Treatment | 0.001131599 |
| Substance | Relationship Strength | Studies | Trials | Classes | Roles |
|---|---|---|---|---|---|
| benzyl alcohol Benzyl Alcohol: A colorless liquid with a sharp burning taste and slight odor. It is used as a local anesthetic and to reduce pain associated with LIDOCAINE injection. Also, it is used in the manufacture of other benzyl compounds, as a pharmaceutic aid, and in perfumery and flavoring.. hydroxytoluene : Any member of the class of toluenes carrying one or more hydroxy substituents.. benzyl alcohol : An aromatic alcohol that consists of benzene bearing a single hydroxymethyl substituent.. aromatic alcohol : Any alcohol in which the alcoholic hydroxy group is attached to a carbon which is itself bonded to an aromatic ring.. aromatic primary alcohol : Any primary alcohol in which the alcoholic hydroxy group is attached to a carbon which is itself bonded to an aromatic ring. | 2.05 | 1 | 0 | benzyl alcohols | antioxidant; fragrance; metabolite; solvent |
| betaine glycine betaine : The amino acid betaine derived from glycine. | 3.23 | 1 | 0 | amino-acid betaine; glycine derivative | fundamental metabolite |
| bupropion Bupropion: A propiophenone-derived antidepressant and antismoking agent that inhibits the uptake of DOPAMINE.. bupropion : An aromatic ketone that is propiophenone carrying a tert-butylamino group at position 2 and a chloro substituent at position 3 on the phenyl ring. | 3.23 | 1 | 0 | aromatic ketone; monochlorobenzenes; secondary amino compound | antidepressant; environmental contaminant; xenobiotic |
| aminocaproic acid Aminocaproic Acid: An antifibrinolytic agent that acts by inhibiting plasminogen activators which have fibrinolytic properties.. 6-aminohexanoic acid : An epsilon-amino acid comprising hexanoic acid carrying an amino substituent at position C-6. Used to control postoperative bleeding, and to treat overdose effects of the thrombolytic agents streptokinase and tissue plasminogen activator. | 3.23 | 1 | 0 | amino acid zwitterion; epsilon-amino acid; omega-amino fatty acid | antifibrinolytic drug; hematologic agent; metabolite |
| niacin Niacin: A water-soluble vitamin of the B complex occurring in various animal and plant tissues. It is required by the body for the formation of coenzymes NAD and NADP. It has PELLAGRA-curative, vasodilating, and antilipemic properties.. vitamin B3 : Any member of a group of vitamers that belong to the chemical structural class called pyridines that exhibit biological activity against vitamin B3 deficiency. Vitamin B3 deficiency causes a condition known as pellagra whose symptoms include depression, dermatitis and diarrhea. The vitamers include nicotinic acid and nicotinamide (and their ionized and salt forms).. nicotinic acid : A pyridinemonocarboxylic acid that is pyridine in which the hydrogen at position 3 is replaced by a carboxy group. | 3.23 | 1 | 0 | pyridine alkaloid; pyridinemonocarboxylic acid; vitamin B3 | antidote; antilipemic drug; EC 3.5.1.19 (nicotinamidase) inhibitor; Escherichia coli metabolite; human urinary metabolite; metabolite; mouse metabolite; plant metabolite; vasodilator agent |
| pyrazinamide pyrazinecarboxamide : A monocarboxylic acid amide resulting from the formal condensation of the carboxy group of pyrazinoic acid (pyrazine-2-carboxylic acid) with ammonia. A prodrug for pyrazinoic acid, pyrazinecarboxamide is used as part of multidrug regimens for the treatment of tuberculosis. | 3.23 | 1 | 0 | monocarboxylic acid amide; N-acylammonia; pyrazines | antitubercular agent; prodrug |
| pyridoxine 4,5-bis(hydroxymethyl)-2-methylpyridin-3-ol: structure in first source. vitamin B6 : Any member of the group of pyridines that exhibit biological activity against vitamin B6 deficiency. Vitamin B6 deficiency is associated with microcytic anemia, electroencephalographic abnormalities, dermatitis with cheilosis (scaling on the lips and cracks at the corners of the mouth) and glossitis (swollen tongue), depression and confusion, and weakened immune function. Vitamin B6 consists of the vitamers pyridoxine, pyridoxal, and pyridoxamine and their respective 5'-phosphate esters (and includes their corresponding ionized and salt forms). | 3.23 | 1 | 0 | hydroxymethylpyridine; methylpyridines; monohydroxypyridine; vitamin B6 | cofactor; Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite |
| thiamine thiamine(1+) : A primary alcohol that is 1,3-thiazol-3-ium substituted by (4-amino-2-methylpyrimidin-5-yl)methyl, methyl and 2-hydroxyethyl groups at positions 3, 4 and 5, respectively. | 3.23 | 1 | 0 | primary alcohol; vitamin B1 | Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite |
| phenytoin [no description available] | 3.23 | 1 | 0 | imidazolidine-2,4-dione | anticonvulsant; drug allergen; sodium channel blocker; teratogenic agent |
| acebutolol Acebutolol: A cardioselective beta-1 adrenergic antagonist with little effect on the bronchial receptors. The drug has stabilizing and quinidine-like effects on cardiac rhythm, as well as weak inherent sympathomimetic action.. acebutolol : An ether that is the 2-acetyl-4-(butanoylamino)phenyl ether of the primary hydroxy group of 3-(propan-2-ylamino)propane-1,2-diol. | 3.23 | 1 | 0 | aromatic amide; ethanolamines; ether; monocarboxylic acid amide; propanolamine; secondary amino compound | anti-arrhythmia drug; antihypertensive agent; beta-adrenergic antagonist; sympathomimetic agent |
| acetaminophen Acetaminophen: Analgesic antipyretic derivative of acetanilide. It has weak anti-inflammatory properties and is used as a common analgesic, but may cause liver, blood cell, and kidney damage.. paracetamol : A member of the class of phenols that is 4-aminophenol in which one of the hydrogens attached to the amino group has been replaced by an acetyl group. | 3.23 | 1 | 0 | acetamides; phenols | antipyretic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; cyclooxygenase 3 inhibitor; environmental contaminant; ferroptosis inducer; geroprotector; hepatotoxic agent; human blood serum metabolite; non-narcotic analgesic; non-steroidal anti-inflammatory drug; xenobiotic |
| acetazolamide Acetazolamide: One of the CARBONIC ANHYDRASE INHIBITORS that is sometimes effective against absence seizures. It is sometimes useful also as an adjunct in the treatment of tonic-clonic, myoclonic, and atonic seizures, particularly in women whose seizures occur or are exacerbated at specific times in the menstrual cycle. However, its usefulness is transient often because of rapid development of tolerance. Its antiepileptic effect may be due to its inhibitory effect on brain carbonic anhydrase, which leads to an increased transneuronal chloride gradient, increased chloride current, and increased inhibition. (From Smith and Reynard, Textbook of Pharmacology, 1991, p337) | 3.23 | 1 | 0 | monocarboxylic acid amide; sulfonamide; thiadiazoles | anticonvulsant; diuretic; EC 4.2.1.1 (carbonic anhydrase) inhibitor |
| acetohydroxamic acid acetohydroxamic acid: urease inhibitor. oxime : Compounds of structure R2C=NOH derived from condensation of aldehydes or ketones with hydroxylamine. Oximes from aldehydes may be called aldoximes; those from ketones may be called ketoximes.. N-hydroxyacetimidic acid : A carbohydroximic acid consisting of acetimidic acid having a hydroxy group attached to the imide nitrogen.. acetohydroxamic acid : A member of the class of acetohydroxamic acids that is acetamide in which one of the amino hydrogens has been replaced by a hydroxy group. | 3.23 | 1 | 0 | acetohydroxamic acids; carbohydroximic acid | algal metabolite; EC 3.5.1.5 (urease) inhibitor |
| alaproclate alaproclate: specific 5-hydroxytryptamine uptake inhibitors; RN given refers to (DL)-isomer | 3.23 | 1 | 0 | alpha-amino acid ester | |
| albendazole [no description available] | 3.23 | 1 | 0 | aryl sulfide; benzimidazoles; benzimidazolylcarbamate fungicide; carbamate ester | anthelminthic drug; microtubule-destabilising agent; tubulin modulator |
| albuterol Albuterol: A short-acting beta-2 adrenergic agonist that is primarily used as a bronchodilator agent to treat ASTHMA. Albuterol is prepared as a racemic mixture of R(-) and S(+) stereoisomers. The stereospecific preparation of R(-) isomer of albuterol is referred to as levalbuterol.. albuterol : A member of the class of phenylethanolamines that is 4-(2-amino-1-hydroxyethyl)-2-(hydroxymethyl)phenol having a tert-butyl group attached to the nirogen atom. It acts as a beta-adrenergic agonist used in the treatment of asthma and chronic obstructive pulmonary disease (COPD). | 3.23 | 1 | 0 | phenols; phenylethanolamines; secondary amino compound | beta-adrenergic agonist; bronchodilator agent; environmental contaminant; xenobiotic |
| alendronate alendronic acid : A 1,1-bis(phosphonic acid) that is methanebis(phosphonic acid) in which the two methylene hydrogens are replaced by hydroxy and 3-aminopropyl groups. | 3.23 | 1 | 0 | 1,1-bis(phosphonic acid); primary amino compound | bone density conservation agent; EC 2.5.1.1 (dimethylallyltranstransferase) inhibitor |
| alfuzosin alfuzosin: structure given in first source | 3.23 | 1 | 0 | monocarboxylic acid amide; quinazolines; tetrahydrofuranol | alpha-adrenergic antagonist; antihypertensive agent; antineoplastic agent |
| alosetron alosetron : A pyrido[4,3-b]indole compound having a 5-methyl-1H-imidazol-4-ylmethyl group at the 2-position. | 3.23 | 1 | 0 | imidazoles; pyridoindole | antiemetic; gastrointestinal drug; serotonergic antagonist |
| alprazolam Alprazolam: A triazolobenzodiazepine compound with antianxiety and sedative-hypnotic actions, that is efficacious in the treatment of PANIC DISORDERS, with or without AGORAPHOBIA, and in generalized ANXIETY DISORDERS. (From AMA Drug Evaluations Annual, 1994, p238). alprazolam : A member of the class of triazolobenzodiazepines that is 4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine carrying methyl, phenyl and chloro substituents at positions 1, 6 and 8 respectively. Alprazolam is only found in individuals that have taken this drug. | 4.99 | 2 | 1 | organochlorine compound; triazolobenzodiazepine | anticonvulsant; anxiolytic drug; GABA agonist; muscle relaxant; sedative; xenobiotic |
| altretamine Altretamine: A hexamethyl-2,4,6-triamine derivative of 1,3,5-triazine. | 3.23 | 1 | 0 | triamino-1,3,5-triazine | |
| amantadine amant: an antiviral compound consisting of an adamantane derivative chemically linked to a water-solube polyanioic matrix; structure in first source | 3.23 | 1 | 0 | adamantanes; primary aliphatic amine | analgesic; antiparkinson drug; antiviral drug; dopaminergic agent; NMDA receptor antagonist; non-narcotic analgesic |
| ambenonium ambenonium : A symmetrical oxalamide-based bis-quaternary ammonium ion having ethyl and 2-chlorobenzyl groups attached to the nitrogens. | 3.23 | 1 | 0 | quaternary ammonium ion | EC 3.1.1.8 (cholinesterase) inhibitor |
| diatrizoic acid Diatrizoate: A commonly used x-ray contrast medium. As DIATRIZOATE MEGLUMINE and as Diatrizoate sodium, it is used for gastrointestinal studies, angiography, and urography.. amidotrizoic acid : A member of the class of benzoic acids that is benzoic acid having iodo substituents at the 2-, 4- and 6-positions and acetamido substituents at the 3- and 5-positions. It is used, mainly as its N-methylglucamine and sodium salts, as an X-ray contrast medium in gastrointestinal studies, angiography, and urography. | 3.23 | 1 | 0 | acetamides; benzoic acids; organoiodine compound | environmental contaminant; radioopaque medium; xenobiotic |
| amifostine anhydrous Amifostine: A phosphorothioate proposed as a radiation-protective agent. It causes splenic vasodilation and may block autonomic ganglia.. amifostine : An organic thiophosphate that is the S-phospho derivative of 2-[(3-aminopropyl)amino]ethanethiol. A prodrug for the free thiol, WR-1065, which is used as a cytoprotectant in cancer chemotherapy and radiotherapy. | 3.23 | 1 | 0 | diamine; organic thiophosphate | antioxidant; prodrug; radiation protective agent |
| p-aminohippuric acid p-Aminohippuric Acid: The glycine amide of 4-aminobenzoic acid. Its sodium salt is used as a diagnostic aid to measure effective renal plasma flow (ERPF) and excretory capacity.. p-aminohippurate : A hippurate that is the conjugate base of p-aminohippuric acid, arising from deprotonation of the carboxy group.. p-aminohippuric acid : An N-acylglycine that is the 4-amino derivative of hippuric acid; used as a diagnostic agent in the measurement of renal plasma flow. | 3.23 | 1 | 0 | N-acylglycine | Daphnia magna metabolite |
| theophylline [no description available] | 3.23 | 1 | 0 | dimethylxanthine | adenosine receptor antagonist; anti-asthmatic drug; anti-inflammatory agent; bronchodilator agent; drug metabolite; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; fungal metabolite; human blood serum metabolite; immunomodulator; muscle relaxant; vasodilator agent |
| amiodarone Amiodarone: An antianginal and class III antiarrhythmic drug. It increases the duration of ventricular and atrial muscle action by inhibiting POTASSIUM CHANNELS and VOLTAGE-GATED SODIUM CHANNELS. There is a resulting decrease in heart rate and in vascular resistance.. amiodarone : A member of the class of 1-benzofurans that is 1-benzofuran substituted by a butyl group at position 2 and a 4-[2-(diethylamino)ethoxy]-3,5-diiodobenzoyl group at position 3. It is a cardiovascular drug used for the treatment of cardiac dysrhythmias. | 3.23 | 1 | 0 | 1-benzofurans; aromatic ketone; organoiodine compound; tertiary amino compound | cardiovascular drug |
| amitriptyline Amitriptyline: Tricyclic antidepressant with anticholinergic and sedative properties. It appears to prevent the re-uptake of norepinephrine and serotonin at nerve terminals, thus potentiating the action of these neurotransmitters. Amitriptyline also appears to antagonize cholinergic and alpha-1 adrenergic responses to bioactive amines.. amitriptyline : An organic tricyclic compound that is 10,11-dihydro-5H-dibenzo[a,d][7]annulene substituted by a 3-(dimethylamino)propylidene group at position 5. | 3.23 | 1 | 0 | carbotricyclic compound; tertiary amine | adrenergic uptake inhibitor; antidepressant; environmental contaminant; tropomyosin-related kinase B receptor agonist; xenobiotic |
| amlodipine Amlodipine: A long-acting dihydropyridine calcium channel blocker. It is effective in the treatment of ANGINA PECTORIS and HYPERTENSION.. amlodipine : A fully substituted dialkyl 1,4-dihydropyridine-3,5-dicarboxylate derivative, which is used for the treatment of hypertension, chronic stable angina and confirmed or suspected vasospastic angina. | 3.23 | 1 | 0 | dihydropyridine; ethyl ester; methyl ester; monochlorobenzenes; primary amino compound | antihypertensive agent; calcium channel blocker; vasodilator agent |
| amoxapine Amoxapine: The N-demethylated derivative of the antipsychotic agent LOXAPINE that works by blocking the reuptake of norepinephrine, serotonin, or both; it also blocks dopamine receptors. Amoxapine is used for the treatment of depression.. amoxapine : A dibenzooxazepine compound having a chloro substituent at the 2-position and a piperazin-1-yl group at the 11-position. | 3.23 | 1 | 0 | dibenzooxazepine | adrenergic uptake inhibitor; antidepressant; dopaminergic antagonist; geroprotector; serotonin uptake inhibitor |
| anastrozole [no description available] | 3.23 | 1 | 0 | nitrile; triazoles | antineoplastic agent; EC 1.14.14.14 (aromatase) inhibitor |
| aspirin Aspirin: The prototypical analgesic used in the treatment of mild to moderate pain. It has anti-inflammatory and antipyretic properties and acts as an inhibitor of cyclooxygenase which results in the inhibition of the biosynthesis of prostaglandins. Aspirin also inhibits platelet aggregation and is used in the prevention of arterial and venous thrombosis. (From Martindale, The Extra Pharmacopoeia, 30th ed, p5). acetylsalicylate : A benzoate that is the conjugate base of acetylsalicylic acid, arising from deprotonation of the carboxy group.. acetylsalicylic acid : A member of the class of benzoic acids that is salicylic acid in which the hydrogen that is attached to the phenolic hydroxy group has been replaced by an acetoxy group. A non-steroidal anti-inflammatory drug with cyclooxygenase inhibitor activity. | 3.23 | 1 | 0 | benzoic acids; phenyl acetates; salicylates | anticoagulant; antipyretic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; drug allergen; EC 1.1.1.188 (prostaglandin-F synthase) inhibitor; geroprotector; non-narcotic analgesic; non-steroidal anti-inflammatory drug; plant activator; platelet aggregation inhibitor; prostaglandin antagonist; teratogenic agent |
| atenolol Atenolol: A cardioselective beta-1 adrenergic blocker possessing properties and potency similar to PROPRANOLOL, but without a negative inotropic effect.. atenolol : An ethanolamine compound having a (4-carbamoylmethylphenoxy)methyl group at the 1-position and an N-isopropyl substituent. | 3.23 | 1 | 0 | ethanolamines; monocarboxylic acid amide; propanolamine | anti-arrhythmia drug; antihypertensive agent; beta-adrenergic antagonist; environmental contaminant; sympatholytic agent; xenobiotic |
| azathioprine Azathioprine: An immunosuppressive agent used in combination with cyclophosphamide and hydroxychloroquine in the treatment of rheumatoid arthritis. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), this substance has been listed as a known carcinogen. (Merck Index, 11th ed). azathioprine : A thiopurine that is 6-mercaptopurine in which the mercapto hydrogen is replaced by a 1-methyl-4-nitroimidazol-5-yl group. It is a prodrug for mercaptopurine and is used as an immunosuppressant, prescribed for the treatment of inflammatory conditions and after organ transplantation and also for treatment of Crohn's didease and MS. | 3.23 | 1 | 0 | aryl sulfide; C-nitro compound; imidazoles; thiopurine | antimetabolite; antineoplastic agent; carcinogenic agent; DNA synthesis inhibitor; hepatotoxic agent; immunosuppressive agent; prodrug |
| baclofen [no description available] | 3.23 | 1 | 0 | amino acid zwitterion; gamma-amino acid; monocarboxylic acid; monochlorobenzenes; primary amino compound | central nervous system depressant; GABA agonist; muscle relaxant |
| bendazac bendazac : A monocarboxylic acid that is glycolic acid in which the hydrogen attached to the 2-hydroxy group is replaced by a 1-benzyl-1H-indazol-3-yl group. Although it has anti-inflammatory, antinecrotic, choleretic and antilipidaemic properties and has been used for the treatment of various inflammatory skin disorders, its principal effect is to inhibit the denaturation of proteins. Its lysine salt is used in the management of cataracts. | 3.23 | 1 | 0 | indazoles; monocarboxylic acid | non-steroidal anti-inflammatory drug; radical scavenger |
| bendroflumethiazide Bendroflumethiazide: A thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE. It has been used in the treatment of familial hyperkalemia, hypertension, edema, and urinary tract disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p810). bendroflumethiazide : A sulfonamide consisting of 7-sulfamoyl-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide in which the hydrogen at position 6 is substituted by a trifluoromethyl group and that at position 3 is substituted by a benzyl group. | 3.23 | 1 | 0 | benzothiadiazine; sulfonamide | antihypertensive agent; diuretic |
| benzbromarone Benzbromarone: Uricosuric that acts by increasing uric acid clearance. It is used in the treatment of gout.. benzbromarone : 1-Benzofuran substituted at C-2 and C-3 by an ethyl group and a 3,5-dibromo-4-hydroxybenzoyl group respectively. An inhibitor of CYP2C9, it is used as an anti-gout medication. | 3.23 | 1 | 0 | 1-benzofurans; aromatic ketone | uricosuric drug |
| betaxolol [no description available] | 3.23 | 1 | 0 | propanolamine | antihypertensive agent; beta-adrenergic antagonist; sympatholytic agent |
| bethanechol Bethanechol: A slowly hydrolyzing muscarinic agonist with no nicotinic effects. Bethanechol is generally used to increase smooth muscle tone, as in the GI tract following abdominal surgery or in urinary retention in the absence of obstruction. It may cause hypotension, HEART RATE changes, and BRONCHIAL SPASM.. bethanechol : The carbamic acid ester of 2-methylcholine. A slowly hydrolysed muscarinic agonist with no nicotinic effects, it is used as its chloride salt to increase smooth muscle tone, as in the gastrointestinal tract following abdominal surgery, treatment of gastro-oesophageal reflux disease, and as an alternative to catheterisation in the treatment of non-obstructive urinary retention. | 3.23 | 1 | 0 | carbamate ester; quaternary ammonium ion | muscarinic agonist |
| bicalutamide bicalutamide: approved for treatment of advanced prostate cancer. N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide : A member of the class of (trifluoromethyl)benzenes that is 4-amino-2-(trifluoromethyl)benzonitrile in which one of the amino hydrogens is substituted by a 3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanoyl group.. bicalutamide : A racemate comprising of equal amounts of (R)-bicalutamide and (S)-bicalutamide. It is an oral non-steroidal antiandrogen used in the treatment of prostate cancer and hirsutism. | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; monocarboxylic acid amide; monofluorobenzenes; nitrile; sulfone; tertiary alcohol | |
| biperiden Biperiden: A muscarinic antagonist that has effects in both the central and peripheral nervous systems. It has been used in the treatment of arteriosclerotic, idiopathic, and postencephalitic parkinsonism. It has also been used to alleviate extrapyramidal symptoms induced by phenothiazine derivatives and reserpine.. biperiden : A member of the class of piperidines that is N-propylpiperidine in which the methyl hydrogens have been replaced by hydroxy, phenyl, and 5-norbornen-2-yl groups. A muscarinic antagonist affecting both the central and peripheral nervous systems, it is used in the treatment of all forms of Parkinson's disease. | 3.23 | 1 | 0 | piperidines; tertiary alcohol; tertiary amino compound | antidote to sarin poisoning; antidyskinesia agent; antiparkinson drug; muscarinic antagonist; parasympatholytic |
| bisacodyl Bisacodyl: A diphenylmethane stimulant laxative used for the treatment of CONSTIPATION and for bowel evacuation. (From Martindale, The Extra Pharmacopoeia, 30th ed, p871) | 3.23 | 1 | 0 | diarylmethane | |
| bisoprolol Bisoprolol: A cardioselective beta-1 adrenergic blocker. It is effective in the management of HYPERTENSION and ANGINA PECTORIS. | 3.23 | 1 | 0 | secondary alcohol; secondary amine | anti-arrhythmia drug; antihypertensive agent; beta-adrenergic antagonist; sympatholytic agent |
| bumetanide [no description available] | 3.23 | 1 | 0 | amino acid; benzoic acids; sulfonamide | diuretic; EC 3.6.3.49 (channel-conductance-controlling ATPase) inhibitor |
| buspirone Buspirone: An anxiolytic agent and serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. Its structure is unrelated to those of the BENZODIAZAPINES, but it has an efficacy comparable to DIAZEPAM.. buspirone : An azaspiro compound that is 8-azaspiro[4.5]decane-7,9-dione substituted at the nitrogen atom by a 4-(piperazin-1-yl)butyl group which in turn is substituted by a pyrimidin-2-yl group at the N(4) position. | 3.23 | 1 | 0 | azaspiro compound; N-alkylpiperazine; N-arylpiperazine; organic heteropolycyclic compound; piperidones; pyrimidines | anxiolytic drug; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; sedative; serotonergic agonist |
| busulfan [no description available] | 3.23 | 1 | 0 | methanesulfonate ester | alkylating agent; antineoplastic agent; carcinogenic agent; insect sterilant; teratogenic agent |
| secbutabarbital secbutabarbital: Butabarbital (a synonym for Secbutabarbital) should be distinguished from Butobarbital | 3.23 | 1 | 0 | barbiturates | |
| caffeine [no description available] | 3.23 | 1 | 0 | purine alkaloid; trimethylxanthine | adenosine A2A receptor antagonist; adenosine receptor antagonist; adjuvant; central nervous system stimulant; diuretic; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; environmental contaminant; food additive; fungal metabolite; geroprotector; human blood serum metabolite; mouse metabolite; mutagen; plant metabolite; psychotropic drug; ryanodine receptor agonist; xenobiotic |
| verapamil Verapamil: A calcium channel blocker that is a class IV anti-arrhythmia agent.. verapamil : A racemate comprising equimolar amounts of dexverapamil and (S)-verapamil. An L-type calcium channel blocker of the phenylalkylamine class, it is used (particularly as the hydrochloride salt) in the treatment of hypertension, angina pectoris and cardiac arrhythmia, and as a preventive medication for migraine.. 2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile : A tertiary amino compound that is 3,4-dimethoxyphenylethylamine in which the hydrogens attached to the nitrogen are replaced by a methyl group and a 4-cyano-4-(3,4-dimethoxyphenyl)-5-methylhexyl group. | 3.23 | 1 | 0 | aromatic ether; nitrile; polyether; tertiary amino compound | |
| candesartan candesartan: a nonpeptide angiotensin II receptor antagonist. candesartan : A benzimidazolecarboxylic acid that is 1H-benzimidazole-7-carboxylic acid substituted by an ethoxy group at position 2 and a ({2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl}methyl) group at position 1. It is a angiotensin receptor antagonist used for the treatment of hypertension. | 3.23 | 1 | 0 | benzimidazolecarboxylic acid; biphenylyltetrazole | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| carbamazepine Carbamazepine: A dibenzazepine that acts as a sodium channel blocker. It is used as an anticonvulsant for the treatment of grand mal and psychomotor or focal SEIZURES. It may also be used in the management of BIPOLAR DISORDER, and has analgesic properties.. carbamazepine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine carrying a carbamoyl substituent at the azepine nitrogen, used as an anticonvulsant. | 3.23 | 1 | 0 | dibenzoazepine; ureas | analgesic; anticonvulsant; antimanic drug; drug allergen; EC 3.5.1.98 (histone deacetylase) inhibitor; environmental contaminant; glutamate transporter activator; mitogen; non-narcotic analgesic; sodium channel blocker; xenobiotic |
| carbinoxamine carbinoxamine: Note: tradenames that start with Histex refer to more than one drug. carbinoxamine : An organochlorine compound that is 2-(4-chlorobenzyl)pyridine in which one of the benzylic hydrogens is substituted by 2-(dimethylamino)ethoxy group. It is an ethanolamine-type antihistamine, used as its maleate salt for treating hay fever, as well as mild cases of Parkinson's disease. | 3.23 | 1 | 0 | monochlorobenzenes; pyridines; tertiary amino compound | anti-allergic agent; antiparkinson drug; H1-receptor antagonist; muscarinic antagonist |
| carisoprodol Carisoprodol: A centrally acting skeletal muscle relaxant whose mechanism of action is not completely understood but may be related to its sedative actions. It is used as an adjunct in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1202). carisoprodol : A carbamate ester that is the mono-N-isopropyl derivative of meprobamate (which is a significant metabolite). Carisoprodol interrupts neuronal communication within the reticular formation and spinal cord, resulting in sedation and alteration in pain perception. It is used as a muscle relaxant in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm. | 3.23 | 1 | 0 | carbamate ester | muscle relaxant |
| carvedilol [no description available] | 3.23 | 1 | 0 | carbazoles; secondary alcohol; secondary amino compound | alpha-adrenergic antagonist; antihypertensive agent; beta-adrenergic antagonist; cardiovascular drug; vasodilator agent |
| celecoxib [no description available] | 3.23 | 1 | 0 | organofluorine compound; pyrazoles; sulfonamide; toluenes | cyclooxygenase 2 inhibitor; geroprotector; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| cetirizine Cetirizine: A potent second-generation histamine H1 antagonist that is effective in the treatment of allergic rhinitis, chronic urticaria, and pollen-induced asthma. Unlike many traditional antihistamines, it does not cause drowsiness or anticholinergic side effects.. cetirizine : A member of the class of piperazines that is piperazine in which the hydrogens attached to nitrogen are replaced by a (4-chlorophenyl)(phenyl)methyl and a 2-(carboxymethoxy)ethyl group respectively. | 3.23 | 1 | 0 | ether; monocarboxylic acid; monochlorobenzenes; piperazines | anti-allergic agent; environmental contaminant; H1-receptor antagonist; xenobiotic |
| chlorambucil Chlorambucil: A nitrogen mustard alkylating agent used as antineoplastic for chronic lymphocytic leukemia, Hodgkin's disease, and others. Although it is less toxic than most other nitrogen mustards, it has been listed as a known carcinogen in the Fourth Annual Report on Carcinogens (NTP 85-002, 1985). (Merck Index, 11th ed). chlorambucil : A monocarboxylic acid that is butanoic acid substituted at position 4 by a 4-[bis(2-chloroethyl)amino]phenyl group. A chemotherapy drug that can be used in combination with the antibody obinutuzumab for the treatment of chronic lymphocytic leukemia. | 3.23 | 1 | 0 | aromatic amine; monocarboxylic acid; nitrogen mustard; organochlorine compound; tertiary amino compound | alkylating agent; antineoplastic agent; carcinogenic agent; drug allergen; immunosuppressive agent |
| chlorcyclizine chlorcyclizine: was heading 1964-94 (Prov 1964-73); CHLOROCYCLIZINE & HISTACHLORAZINE were see CHLORCYCLIZINE 1977-94; use PIPERAZINES to search CHLORCYCLIZINE 1966-94; histamine H1-blocker used both orally and topically in allergies and also for the prevention of motion sickness | 3.23 | 1 | 0 | diarylmethane | |
| chlordiazepoxide Chlordiazepoxide: An anxiolytic benzodiazepine derivative with anticonvulsant, sedative, and amnesic properties. It has also been used in the symptomatic treatment of alcohol withdrawal.. chlordiazepoxide : A benzodiazepine that is 3H-1,4-benzodiazepine 4-oxide substituted by a chloro group at position 7, a phenyl group at position 5 and a methylamino group at position 2. | 3.23 | 1 | 0 | benzodiazepine | |
| chlormezanone Chlormezanone: A non-benzodiazepine that is used in the management of anxiety. It has been suggested for use in the treatment of muscle spasm.. chlormezanone : A 1,3-thiazine that is 1,3-thiazinan-4-one S,S-dioxide in which a hydrogen at position 2 is substituted by a 4-chlorophenyl group and the hydrogen attached to the nitrogen is substituted by methyl. A non-benzodiazepine muscle relaxant, it was used in the management of anxiety and in the treatment of muscle spasms until being discontinued worldwide by its manufacturer in 1996, due to rare but serious cutaneous reactions. | 3.23 | 1 | 0 | 1,3-thiazine; lactam; monochlorobenzenes; sulfone | antipsychotic agent; anxiolytic drug; muscle relaxant |
| chloroquine Chloroquine: The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses.. chloroquine : An aminoquinoline that is quinoline which is substituted at position 4 by a [5-(diethylamino)pentan-2-yl]amino group at at position 7 by chlorine. It is used for the treatment of malaria, hepatic amoebiasis, lupus erythematosus, light-sensitive skin eruptions, and rheumatoid arthritis. | 3.23 | 1 | 0 | aminoquinoline; organochlorine compound; secondary amino compound; tertiary amino compound | anticoronaviral agent; antimalarial; antirheumatic drug; autophagy inhibitor; dermatologic drug |
| chlorothiazide Chlorothiazide: A thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p812). thiazide : Heterocyclic compound with sulfur and nitrogen in the ring.. chlorothiazide : 4H-1,2,4-benzothiadiazine 1,1-dioxide in which the hydrogen at position is substituted by chlorine and that at position 7 is substituted by a sulfonamide group. A diuretic, it is used for treatment of oedema and hypertension. | 3.23 | 1 | 0 | benzothiadiazine | antihypertensive agent; diuretic |
| chlorpheniramine Chlorpheniramine: A histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria, and asthma. It has also been used in veterinary applications. One of the most widely used of the classical antihistaminics, it generally causes less drowsiness and sedation than PROMETHAZINE.. chlorphenamine : A tertiary amino compound that is propylamine which is substituted at position 3 by a pyridin-2-yl group and a p-chlorophenyl group and in which the hydrogens attached to the nitrogen are replaced by methyl groups. A histamine H1 antagonist, it is used to relieve the symptoms of hay fever, rhinitis, urticaria, and asthma. | 3.23 | 1 | 0 | monochlorobenzenes; pyridines; tertiary amino compound | anti-allergic agent; antidepressant; antipruritic drug; H1-receptor antagonist; histamine antagonist; serotonin uptake inhibitor |
| chlorpromazine Chlorpromazine: The prototypical phenothiazine antipsychotic drug. Like the other drugs in this class chlorpromazine's antipsychotic actions are thought to be due to long-term adaptation by the brain to blocking DOPAMINE RECEPTORS. Chlorpromazine has several other actions and therapeutic uses, including as an antiemetic and in the treatment of intractable hiccup.. chlorpromazine : A substituted phenothiazine in which the ring nitrogen at position 10 is attached to C-3 of an N,N-dimethylpropanamine moiety. | 3.23 | 1 | 0 | organochlorine compound; phenothiazines; tertiary amine | anticoronaviral agent; antiemetic; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; phenothiazine antipsychotic drug |
| chlorpropamide Chlorpropamide: A sulfonylurea hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. (From Martindale, The Extra Pharmacopoeia, 30th ed, p277). chlorpropamide : An N-sulfonylurea that is urea in which a hydrogen attached to one of the nitrogens is substituted by 4-chlorobenzenesulfonyl group and a hydrogen attached to the other nitrogen is substituted by propyl group. Chlorpropamide is a hypoglycaemic agent used in the treatment of type 2 (non-insulin-dependent) diabetes mellitus not responding to dietary modification. | 3.23 | 1 | 0 | monochlorobenzenes; N-sulfonylurea | hypoglycemic agent; insulin secretagogue |
| chlorthalidone Chlorthalidone: A benzenesulfonamide-phthalimidine that tautomerizes to a BENZOPHENONES form. It is considered a thiazide-like diuretic. | 3.23 | 1 | 0 | isoindoles; monochlorobenzenes; sulfonamide | |
| chlorzoxazone Chlorzoxazone: A centrally acting central muscle relaxant with sedative properties. It is claimed to inhibit muscle spasm by exerting an effect primarily at the level of the spinal cord and subcortical areas of the brain. (From Martindale, The Extra Pharmacopoea, 30th ed, p1202). chlorzoxazone : A member of the class of 1,3-benzoxazoles that is 1,3-benzoxazol-2-ol in which the hydrogen atom at position 5 is substituted by chlorine. A centrally acting muscle relaxant with sedative properties, it is used for the symptomatic treatment of painful muscle spasm. | 3.23 | 1 | 0 | 1,3-benzoxazoles; heteroaryl hydroxy compound; organochlorine compound | muscle relaxant; sedative |
| cilostazol [no description available] | 3.23 | 1 | 0 | lactam; tetrazoles | anticoagulant; bronchodilator agent; EC 3.1.4.17 (3',5'-cyclic-nucleotide phosphodiesterase) inhibitor; fibrin modulating drug; neuroprotective agent; platelet aggregation inhibitor; vasodilator agent |
| cimetidine Cimetidine: A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.. cimetidine : A member of the class of guanidines that consists of guanidine carrying a methyl substituent at position 1, a cyano group at position 2 and a 2-{[(5-methyl-1H-imidazol-4-yl)methyl]sulfanyl}ethyl group at position 3. It is a H2-receptor antagonist that inhibits the production of acid in stomach. | 3.23 | 1 | 0 | aliphatic sulfide; guanidines; imidazoles; nitrile | adjuvant; analgesic; anti-ulcer drug; H2-receptor antagonist; P450 inhibitor |
| ciprofloxacin Ciprofloxacin: A broad-spectrum antimicrobial carboxyfluoroquinoline.. ciprofloxacin : A quinolone that is quinolin-4(1H)-one bearing cyclopropyl, carboxylic acid, fluoro and piperazin-1-yl substituents at positions 1, 3, 6 and 7, respectively. | 3.23 | 1 | 0 | aminoquinoline; cyclopropanes; fluoroquinolone antibiotic; N-arylpiperazine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone; zwitterion | antibacterial drug; antiinfective agent; antimicrobial agent; DNA synthesis inhibitor; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; environmental contaminant; topoisomerase IV inhibitor; xenobiotic |
| citalopram Citalopram: A furancarbonitrile that is one of the serotonin uptake inhibitors used as an antidepressant. The drug is also effective in reducing ethanol uptake in alcoholics and is used in depressed patients who also suffer from TARDIVE DYSKINESIA in preference to tricyclic antidepressants, which aggravate dyskinesia.. citalopram : A racemate comprising equimolar amounts of (R)-citalopram and its enantiomer, escitalopram. It is used as an antidepressant, although only escitalopram is active.. 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile : A nitrile that is 1,3-dihydro-2-benzofuran-5-carbonitrile in which one of the hydrogens at position 1 is replaced by a p-fluorophenyl group, while the other is replaced by a 3-(dimethylamino)propyl group. | 3.23 | 1 | 0 | 2-benzofurans; cyclic ether; nitrile; organofluorine compound; tertiary amino compound | |
| clofibrate angiokapsul: contains clofibrate & insoitolnicotinate | 3.23 | 1 | 0 | aromatic ether; ethyl ester; monochlorobenzenes | anticholesteremic drug; antilipemic drug; geroprotector; PPARalpha agonist |
| clomiphene [no description available] | 3.23 | 1 | 0 | tertiary amine | estrogen antagonist; estrogen receptor modulator |
| clomipramine Clomipramine: A tricyclic antidepressant similar to IMIPRAMINE that selectively inhibits the uptake of serotonin in the brain. It is readily absorbed from the gastrointestinal tract and demethylated in the liver to form its primary active metabolite, desmethylclomipramine.. clomipramine : A dibenzoazepine that is 10,11-dihydro-5H-dibenzo[b,f]azepine which is substituted by chlorine at position 3 and in which the hydrogen attached to the nitrogen is replaced by a 3-(dimethylamino)propyl group. One of the more sedating tricyclic antidepressants, it is used as the hydrochloride salt for the treatment of depression as well as obsessive-compulsive disorder and phobias. | 3.23 | 1 | 0 | dibenzoazepine | anticoronaviral agent; antidepressant; EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor; serotonergic antagonist; serotonergic drug; serotonin uptake inhibitor |
| clonazepam Clonazepam: An anticonvulsant used for several types of seizures, including myotonic or atonic seizures, photosensitive epilepsy, and absence seizures, although tolerance may develop. It is seldom effective in generalized tonic-clonic or partial seizures. The mechanism of action appears to involve the enhancement of GAMMA-AMINOBUTYRIC ACID receptor responses.. clonazepam : 1,3-Dihydro-2H-1,4-benzodiazepin-2-one in which the hydrogens at positions 5 and 7 are substituted by 2-chlorophenyl and nitro groups, respectively. It is used in the treatment of all types of epilepsy and seizures, as well as myoclonus and associated abnormal movements, and panic disorders. However, its use can be limited by the development of tolerance and by sedation. | 3.23 | 1 | 0 | 1,4-benzodiazepinone; monochlorobenzenes | anticonvulsant; anxiolytic drug; GABA modulator |
| clonidine Clonidine: An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.. clonidine (amino form) : A clonidine that is 4,5-dihydro-1H-imidazol-2-amine in which one of the amino hydrogens is replaced by a 2,6-dichlorophenyl group. | 3.23 | 1 | 0 | clonidine; imidazoline | |
| chlorazepate clorazepic acid : A 1,4-benzodiazepinone in which the oxo group is at position 2, and which is substituted at positions 3, 5, and 7 by carboxy, phenyl and chloro groups, respectively. | 3.23 | 1 | 0 | 1,4-benzodiazepinone | anticonvulsant; anxiolytic drug; GABA modulator; prodrug |
| clotrimazole [no description available] | 3.23 | 1 | 0 | conazole antifungal drug; imidazole antifungal drug; imidazoles; monochlorobenzenes | antiinfective agent; environmental contaminant; xenobiotic |
| cyclobenzaprine cyclobenzaprine: RN given refers to parent cpd; Lisseril is synonymous for HCl; structure. cyclobenzaprine : 5-Methylidene-5H-dibenzo[a,d]cycloheptene in which one of the hydrogens of the methylidene group is substituted by a 2-(dimethylamino)ethyl group. A centrally acting skeletal muscle relaxant, it is used as its hydrochloride salt in the symptomatic treatment of painful muscle spasm. | 3.23 | 1 | 0 | carbotricyclic compound | antidepressant; muscle relaxant; tranquilizing drug |
| cyclofenil Cyclofenil: A gonadal stimulant and inducer of ovulation. It is used in the treatment of infertility and amenorrhea, but is thought to be less effective than CLOMIPHENE. | 3.23 | 1 | 0 | organic molecular entity | |
| cyproheptadine Cyproheptadine: A serotonin antagonist and a histamine H1 blocker used as antipruritic, appetite stimulant, antiallergic, and for the post-gastrectomy dumping syndrome, etc.. cyproheptadine : The product resulting from the formal oxidative coupling of position 5 of 5H-dibenzo[a,d]cycloheptene with position 4 of 1-methylpiperidine resulting in the formation of a double bond between the two fragments. It is a sedating antihistamine with antimuscarinic and calcium-channel blocking actions. It is used (particularly as the hydrochloride sesquihydrate) for the relief of allergic conditions including rhinitis, conjunctivitis due to inhalant allergens and foods, urticaria and angioedema, and in pruritic skin disorders. Unlike other antihistamines, it is also a seratonin receptor antagonist, making it useful in conditions such as vascular headache and anorexia. | 3.23 | 1 | 0 | piperidines; tertiary amine | anti-allergic agent; antipruritic drug; gastrointestinal drug; H1-receptor antagonist; serotonergic antagonist |
| dapsone [no description available] | 3.23 | 1 | 0 | substituted aniline; sulfone | anti-inflammatory drug; antiinfective agent; antimalarial; leprostatic drug |
| deferoxamine Deferoxamine: Natural product isolated from Streptomyces pilosus. It forms iron complexes and is used as a chelating agent, particularly in the mesylate form.. desferrioxamine B : An acyclic desferrioxamine that is butanedioic acid in which one of the carboxy groups undergoes formal condensation with the primary amino group of N-(5-aminopentyl)-N-hydroxyacetamide and the second carboxy group undergoes formal condensation with the hydroxyamino group of N(1)-(5-aminopentyl)-N(1)-hydroxy-N(4)-[5-(hydroxyamino)pentyl]butanediamide. It is a siderophore native to Streptomyces pilosus biosynthesised by the DesABCD enzyme cluster as a high affinity Fe(III) chelator. | 3.23 | 1 | 0 | acyclic desferrioxamine | bacterial metabolite; ferroptosis inhibitor; iron chelator; siderophore |
| desipramine Desipramine: A tricyclic dibenzazepine compound that potentiates neurotransmission. Desipramine selectively blocks reuptake of norepinephrine from the neural synapse, and also appears to impair serotonin transport. This compound also possesses minor anticholinergic activity, through its affinity to muscarinic receptors.. desipramine : A dibenzoazepine consisting of 10,11-dihydro-5H-dibenzo[b,f]azepine substituted on nitrogen with a 3-(methylamino)propyl group. | 3.23 | 1 | 0 | dibenzoazepine; secondary amino compound | adrenergic uptake inhibitor; alpha-adrenergic antagonist; antidepressant; cholinergic antagonist; drug allergen; EC 3.1.4.12 (sphingomyelin phosphodiesterase) inhibitor; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; H1-receptor antagonist; serotonin uptake inhibitor |
| amphetamine Amphetamine: A powerful central nervous system stimulant and sympathomimetic. Amphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulation of release of monamines, and inhibiting monoamine oxidase. Amphetamine is also a drug of abuse and a psychotomimetic. The l- and the d,l-forms are included here. The l-form has less central nervous system activity but stronger cardiovascular effects. The d-form is DEXTROAMPHETAMINE.. 1-phenylpropan-2-amine : A primary amine that is isopropylamine in which a hydrogen attached to one of the methyl groups has been replaced by a phenyl group.. amphetamine : A racemate comprising equimolar amounts of (R)-amphetamine (also known as levamphetamine or levoamphetamine) and (S)-amphetamine (also known as dexamfetamine or dextroamphetamine. | 3.23 | 1 | 0 | primary amine | |
| diazepam Diazepam: A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity.. diazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a methyl group at position 1 and a phenyl group at position 5. | 3.23 | 1 | 0 | 1,4-benzodiazepinone; organochlorine compound | anticonvulsant; anxiolytic drug; environmental contaminant; sedative; xenobiotic |
| diazoxide Diazoxide: A benzothiadiazine derivative that is a peripheral vasodilator used for hypertensive emergencies. It lacks diuretic effect, apparently because it lacks a sulfonamide group.. diazoxide : A benzothiadiazine that is the S,S-dioxide of 2H-1,2,4-benzothiadiazine which is substituted at position 3 by a methyl group and at position 7 by chlorine. A peripheral vasodilator, it increases the concentration of glucose in the plasma and inhibits the secretion of insulin by the beta- cells of the pancreas. It is used orally in the management of intractable hypoglycaemia and intravenously in the management of hypertensive emergencies. | 3.23 | 1 | 0 | benzothiadiazine; organochlorine compound; sulfone | antihypertensive agent; beta-adrenergic agonist; bronchodilator agent; cardiotonic drug; diuretic; K-ATP channel agonist; sodium channel blocker; sympathomimetic agent; vasodilator agent |
| diclofenac Diclofenac: A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt.. diclofenac : A monocarboxylic acid consisting of phenylacetic acid having a (2,6-dichlorophenyl)amino group at the 2-position. | 3.23 | 1 | 0 | amino acid; aromatic amine; dichlorobenzene; monocarboxylic acid; secondary amino compound | antipyretic; drug allergen; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; environmental contaminant; non-narcotic analgesic; non-steroidal anti-inflammatory drug; xenobiotic |
| dichlorphenamide Dichlorphenamide: A carbonic anhydrase inhibitor that is used in the treatment of glaucoma.. diclofenamide : A sulfonamide that is benzene-1,3-disulfonamide in which the hydrogens at positions 4 and 5 are substituted by chlorine. An oral carbonic anhydrase inhibitor, it partially suppresses the secretion (inflow) of aqueous humor in the eye and so reduces intraocular pressure. It is used for the treatment of glaucoma. | 3.23 | 1 | 0 | dichlorobenzene; sulfonamide | antiglaucoma drug; EC 4.2.1.1 (carbonic anhydrase) inhibitor; ophthalmology drug |
| dicyclomine Dicyclomine: A muscarinic antagonist used as an antispasmodic and in urinary incontinence. It has little effect on glandular secretion or the cardiovascular system. It does have some local anesthetic properties and is used in gastrointestinal, biliary, and urinary tract spasms.. dicyclomine : The ester resulting from the formal condensation of 1-cyclohexylcyclohexanecarboxylic acid with 2-(diethylamino)ethanol. An anticholinergic, it is used as the hydrochloride to treat or prevent spasm in the muscles of the gastrointestinal tract, particularly that associated with irritable bowel syndrome. | 3.23 | 1 | 0 | carboxylic ester; tertiary amine | antispasmodic drug; muscarinic antagonist; parasympatholytic |
| pentetic acid Pentetic Acid: An iron chelating agent with properties like EDETIC ACID. DTPA has also been used as a chelator for other metals, such as plutonium. | 3.23 | 1 | 0 | pentacarboxylic acid | copper chelator |
| diflunisal Diflunisal: A salicylate derivative and anti-inflammatory analgesic with actions and side effects similar to those of ASPIRIN.. diflunisal : An organofluorine compound comprising salicylic acid having a 2,4-difluorophenyl group at the 5-position. | 3.23 | 1 | 0 | monohydroxybenzoic acid; organofluorine compound | non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| dimercaprol Dimercaprol: An anti-gas warfare agent that is effective against Lewisite (dichloro(2-chlorovinyl)arsine) and formerly known as British Anti-Lewisite or BAL. It acts as a chelating agent and is used in the treatment of arsenic, gold, and other heavy metal poisoning.. dimercaprol : A dithiol that is propane-1,2-dithiol in which one of the methyl hydrogens is replaced by a hydroxy group. a chelating agent originally developed during World War II as an experimental antidote against the arsenic-based poison gas Lewisite, it has been used clinically since 1949 for the treatment of poisoning by arsenic, mercury and gold. It can also be used for treatment of poisoning by antimony, bismuth and possibly thallium, and (with sodium calcium edetate) in cases of acute leaad poisoning. Administration is by (painful) intramuscular injection of a suspension of dimercaprol in peanut oil, typically every 4 hours for 2-10 days depending on the toxicity. In the past, dimercaprol was also used for the treatment of Wilson's disease, a severely debilitating genetic disorder in which the body tends to retain copper, with resultant liver and brain injury. | 3.23 | 1 | 0 | dithiol; primary alcohol | chelator |
| diphenhydramine Diphenhydramine: A histamine H1 antagonist used as an antiemetic, antitussive, for dermatoses and pruritus, for hypersensitivity reactions, as a hypnotic, an antiparkinson, and as an ingredient in common cold preparations. It has some undesired antimuscarinic and sedative effects.. diphenhydramine : An ether that is the benzhydryl ether of 2-(dimethylamino)ethanol. It is a H1-receptor antagonist used as a antipruritic and antitussive drug.. antitussive : An agent that suppresses cough. Antitussives have a central or a peripheral action on the cough reflex, or a combination of both. Compare with expectorants, which are considered to increase the volume of secretions in the respiratory tract, so facilitating their removal by ciliary action and coughing, and mucolytics, which decrease the viscosity of mucus, facilitating its removal by ciliary action and expectoration. | 3.23 | 1 | 0 | ether; tertiary amino compound | anti-allergic agent; antidyskinesia agent; antiemetic; antiparkinson drug; antipruritic drug; antitussive; H1-receptor antagonist; local anaesthetic; muscarinic antagonist; oneirogen; sedative |
| dipyridamole Dipyridamole: A phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells. Dipyridamole also potentiates the antiaggregating action of prostacyclin. (From AMA Drug Evaluations Annual, 1994, p752). dipyridamole : A pyrimidopyrimidine that is 2,2',2'',2'''-(pyrimido[5,4-d]pyrimidine-2,6-diyldinitrilo)tetraethanol substituted by piperidin-1-yl groups at positions 4 and 8 respectively. A vasodilator agent, it inhibits the formation of blood clots. | 3.23 | 1 | 0 | piperidines; pyrimidopyrimidine; tertiary amino compound; tetrol | adenosine phosphodiesterase inhibitor; EC 3.5.4.4 (adenosine deaminase) inhibitor; platelet aggregation inhibitor; vasodilator agent |
| disopyramide Disopyramide: A class I anti-arrhythmic agent (one that interferes directly with the depolarization of the cardiac membrane and thus serves as a membrane-stabilizing agent) with a depressant action on the heart similar to that of guanidine. It also possesses some anticholinergic and local anesthetic properties.. disopyramide : A monocarboxylic acid amide that is butanamide substituted by a diisopropylamino group at position 4, a phenyl group at position 2 and a pyridin-2-yl group at position 2. It is used as a anti-arrhythmia drug. | 3.23 | 1 | 0 | monocarboxylic acid amide; pyridines; tertiary amino compound | anti-arrhythmia drug |
| disulfiram [no description available] | 3.23 | 1 | 0 | organic disulfide; organosulfur acaricide | angiogenesis inhibitor; antineoplastic agent; apoptosis inducer; EC 1.2.1.3 [aldehyde dehydrogenase (NAD(+))] inhibitor; EC 3.1.1.1 (carboxylesterase) inhibitor; EC 3.1.1.8 (cholinesterase) inhibitor; EC 5.99.1.2 (DNA topoisomerase) inhibitor; ferroptosis inducer; fungicide; NF-kappaB inhibitor |
| valproic acid Valproic Acid: A fatty acid with anticonvulsant and anti-manic properties that is used in the treatment of EPILEPSY and BIPOLAR DISORDER. The mechanisms of its therapeutic actions are not well understood. It may act by increasing GAMMA-AMINOBUTYRIC ACID levels in the brain or by altering the properties of VOLTAGE-GATED SODIUM CHANNELS.. valproic acid : A branched-chain saturated fatty acid that comprises of a propyl substituent on a pentanoic acid stem. | 3.23 | 1 | 0 | branched-chain fatty acid; branched-chain saturated fatty acid | anticonvulsant; antimanic drug; EC 3.5.1.98 (histone deacetylase) inhibitor; GABA agent; neuroprotective agent; psychotropic drug; teratogenic agent |
| donepezil Donepezil: An indan and piperidine derivative that acts as a selective and reversible inhibitor of ACETYLCHOLINESTERASE. Donepezil is highly selective for the central nervous system and is used in the management of mild to moderate DEMENTIA in ALZHEIMER DISEASE.. donepezil : A racemate comprising equimolar amounts of (R)- and (S)-donepezil. A centrally acting reversible acetylcholinesterase inhibitor, its main therapeutic use is in the treatment of Alzheimer's disease where it is used to increase cortical acetylcholine.. 2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxyindan-1-one : A member of the class of indanones that is 5,6-dimethoxyindan-1-one which is substituted at position 2 by an (N-benzylpiperidin-4-yl)methyl group. | 3.23 | 1 | 0 | aromatic ether; indanones; piperidines; racemate | EC 3.1.1.7 (acetylcholinesterase) inhibitor; EC 3.1.1.8 (cholinesterase) inhibitor; nootropic agent |
| doxapram Doxapram: A central respiratory stimulant with a brief duration of action. (From Martindale, The Extra Pharmocopoeia, 30th ed, p1225). doxapram : A member of the class of pyrrolidin-2-ones that is N-ethylpyrrolidin-2-one in which both of the hydrogens at the 3 position (adjacent to the carbonyl group) are substituted by phenyl groups, and one of the hydrogens at the 4 position is substituted by a 2-(morpholin-4-yl)ethyl group. A central and respiratory stimulant with a brief duration of action, it is used (generally as the hydrochloride or the hydrochloride hydrate) as a temporary treatment of acute respiratory failure, particularly when superimposed on chronic obstructive pulmonary disease, and of postoperative respiratory depression. It has also been used for treatment of postoperative shivering. | 3.23 | 1 | 0 | morpholines; pyrrolidin-2-ones | central nervous system stimulant |
| doxazosin Doxazosin: A prazosin-related compound that is a selective alpha-1-adrenergic blocker.. doxazosin : A member of the class of quinazolines that is quinazoline substituted by an amino group at position 4, methoxy groups at positions 6 and 7 and a piperazin-1-yl group at position 2 which in turn is substituted by a 2,3-dihydro-1,4-benzodioxin-2-ylcarbonyl group at position 4. An antihypertensive agent, it is used in the treatment of high blood pressure. | 3.86 | 3 | 0 | aromatic amine; benzodioxine; monocarboxylic acid amide; N-acylpiperazine; N-arylpiperazine; quinazolines | alpha-adrenergic antagonist; antihyperplasia drug; antihypertensive agent; antineoplastic agent; vasodilator agent |
| doxepin Doxepin: A dibenzoxepin tricyclic compound. It displays a range of pharmacological actions including maintaining adrenergic innervation. Its mechanism of action is not fully understood, but it appears to block reuptake of monoaminergic neurotransmitters into presynaptic terminals. It also possesses anticholinergic activity and modulates antagonism of histamine H(1)- and H(2)-receptors.. doxepin : A dibenzooxepine that is 6,11-dihydrodibenzo[b,e]oxepine substituted by a 3-(dimethylamino)propylidene group at position 11. It is used as an antidepressant drug. | 3.23 | 1 | 0 | dibenzooxepine; tertiary amino compound | antidepressant |
| doxylamine Doxylamine: Histamine H1 antagonist with pronounced sedative properties. It is used in allergies and as an antitussive, antiemetic, and hypnotic. Doxylamine has also been administered in veterinary applications and was formerly used in PARKINSONISM. | 3.23 | 1 | 0 | pyridines; tertiary amine | anti-allergic agent; antiemetic; antitussive; cholinergic antagonist; H1-receptor antagonist; histamine antagonist; sedative |
| droperidol Droperidol: A butyrophenone with general properties similar to those of HALOPERIDOL. It is used in conjunction with an opioid analgesic such as FENTANYL to maintain the patient in a calm state of neuroleptanalgesia with indifference to surroundings but still able to cooperate with the surgeon. It is also used as a premedicant, as an antiemetic, and for the control of agitation in acute psychoses. (From Martindale, The Extra Pharmacopoeia, 29th ed, p593). droperidol : An organofluorine compound that is haloperidol in which the hydroxy group has been eliminated with the introduction of a double bond in the piperidine ring, and the 4-chlorophenyl group has been replaced by a benzimidazol-2-on-1-yl group. It is used in the management of chemotherapy-induced nausea and vomiting, and in conjunction with an opioid analgesic such as fentanyl to maintain the patient in a calm state of neuroleptanalgesia with indifference to surroundings but still able to cooperate with the surgeon. | 3.23 | 1 | 0 | aromatic ketone; benzimidazoles; organofluorine compound | anaesthesia adjuvant; antiemetic; dopaminergic antagonist; first generation antipsychotic |
| dyphylline Dyphylline: A THEOPHYLLINE derivative with broncho- and vasodilator properties. It is used in the treatment of asthma, cardiac dyspnea, and bronchitis.. dyphylline : An oxopurine that is theophylline bearing a 2,3-dihydroxypropyl group at the 7 position. It has broncho- and vasodilator properties, and is used in the treatment of asthma, cardiac dyspnea, and bronchitis. It is also an ingredient in preparations that have been promoted for coughs. | 3.23 | 1 | 0 | oxopurine; propane-1,2-diols | bronchodilator agent; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; muscle relaxant; vasodilator agent |
| edrophonium Edrophonium: A rapid-onset, short-acting cholinesterase inhibitor used in cardiac arrhythmias and in the diagnosis of myasthenia gravis. It has also been used as an antidote to curare principles.. edrophonium : A quaternary ammonium ion that is N-ethyl-N,N-dimethylanilinium in which one of the meta positions is substituted by a hydroxy group. It is a reversible inhibitor of cholinesterase, with a rapid onset (30-60 seconds after injection) but a short duration of action (5-15 minutes). The chloride salt is used in myasthenia gravis both diagnostically and to distinguish between under- or over-treatment with other anticholinesterases. It has also been used for the reversal of neuromuscular blockade in anaesthesia, and for the management of poisoning due to tetrodotoxin, a neuromuscular blocking toxin found in puffer fish and other marine animals. | 3.23 | 1 | 0 | phenols; quaternary ammonium ion | antidote; diagnostic agent; EC 3.1.1.8 (cholinesterase) inhibitor |
| estazolam Estazolam: A benzodiazepine with anticonvulsant, hypnotic, and muscle relaxant properties. It has been shown in some cases to be more potent than DIAZEPAM or NITRAZEPAM.. estazolam : A triazolo[4,3-a][1,4]benzodiazepine having a phenyl group at position 6 and a chloro substituent at position 8. A short-acting benzodiazepine with general properties similar to diazepam, it is given by mouth as a hypnotic in the short-term management of insomnia. | 3.23 | 1 | 0 | triazoles; triazolobenzodiazepine | anticonvulsant; anxiolytic drug; GABA modulator |
| ethacrynic acid Ethacrynic Acid: A compound that inhibits symport of sodium, potassium, and chloride primarily in the ascending limb of Henle, but also in the proximal and distal tubules. This pharmacological action results in excretion of these ions, increased urinary output, and reduction in extracellular fluid. This compound has been classified as a loop or high ceiling diuretic.. etacrynic acid : An aromatic ether that is phenoxyacetic acid in which the phenyl ring is substituted by chlorines at positions 2 and 3, and by a 2-methylidenebutanoyl group at position 4. It is a loop diuretic used to treat high blood pressure resulting from diseases such as congestive heart failure, liver failure, and kidney failure. It is also a glutathione S-transferase (EC 2.5.1.18) inhibitor. | 3.23 | 1 | 0 | aromatic ether; aromatic ketone; dichlorobenzene; monocarboxylic acid | EC 2.5.1.18 (glutathione transferase) inhibitor; ion transport inhibitor; loop diuretic |
| ethosuximide Ethosuximide: An anticonvulsant especially useful in the treatment of absence seizures unaccompanied by other types of seizures.. ethosuximide : A dicarboximide that is pyrrolidine-2,5-dione in which the hydrogens at position 3 are substituted by one methyl and one ethyl group. An antiepileptic, it is used in the treatment of absence seizures and may be used for myoclonic seizures, but is ineffective against tonic-clonic seizures. | 3.23 | 1 | 0 | dicarboximide; pyrrolidinone | anticonvulsant; geroprotector; T-type calcium channel blocker |
| ethotoin ethotoin: was heading 1966-94 (see under HYDANTOINS 1966-90); use HYDANTOINS to search ETHOTOIN 1966-94. ethotoin : An imidazolidine-2,4-dione that is hydantoin substituted by ethyl and phenyl at positions 3 and 5, respectively. An antiepileptic, it is less toxic than phenytoin but also less effective. | 3.23 | 1 | 0 | imidazolidine-2,4-dione | anticonvulsant |
| etidronate Etidronic Acid: A diphosphonate which affects calcium metabolism. It inhibits ectopic calcification and slows down bone resorption and bone turnover.. etidronic acid : A 1,1-bis(phosphonic acid) that is (ethane-1,1-diyl)bis(phosphonic acid) having a hydroxy substituent at the 1-position. It inhibits the formation, growth, and dissolution of hydroxyapatite crystals by chemisorption to calcium phosphate surfaces. | 3.23 | 1 | 0 | 1,1-bis(phosphonic acid) | antineoplastic agent; bone density conservation agent; chelator |
| etodolac Etodolac: A non-steroidal anti-inflammatory agent and cyclooxygenase-2 (COX-2) inhibitor with potent analgesic and anti-arthritic properties. It has been shown to be effective in the treatment of OSTEOARTHRITIS; RHEUMATOID ARTHRITIS; ANKYLOSING SPONDYLITIS; and in the alleviation of postoperative pain (PAIN, POSTOPERATIVE).. etodolac : A monocarboxylic acid that is acetic acid in which one of the methyl hydrogens is substituted by a 1,8-diethyl-1,3,4,9-tetrahydropyrano[3,4-b]indol-1-yl moiety. A preferential inhibitor of cyclo-oxygenase 2 and non-steroidal anti-inflammatory, it is used for the treatment of rheumatoid arthritis and osteoarthritis, and for the alleviation of postoperative pain. Administered as the racemate, only the (S)-enantiomer is active. | 3.23 | 1 | 0 | monocarboxylic acid; organic heterotricyclic compound | antipyretic; cyclooxygenase 2 inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| brl 42810 [no description available] | 3.23 | 1 | 0 | 2-aminopurines; acetate ester | antiviral drug; prodrug |
| felbamate Felbamate: A PEGylated phenylcarbamate derivative that acts as an antagonist of NMDA RECEPTORS. It is used as an anticonvulsant, primarily for the treatment of SEIZURES in severe refractory EPILEPSY.. felbamate : The bis(carbamate ester) of 2-phenylpropane-1,3-diol. An anticonvulsant, it is used in the treatment of epilepsy. | 3.23 | 1 | 0 | carbamate ester | anticonvulsant; neuroprotective agent |
| felodipine Felodipine: A dihydropyridine calcium antagonist with positive inotropic effects. It lowers blood pressure by reducing peripheral vascular resistance through a highly selective action on smooth muscle in arteriolar resistance vessels.. felodipine : The mixed (methyl, ethyl) diester of 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid. A calcium-channel blocker, it lowers blood pressure by reducing peripheral vascular resistance through a highly selective action on smooth muscle in arteriolar resistance vessels. It is used in the management of hypertension and angina pectoris. | 3.23 | 1 | 0 | dichlorobenzene; dihydropyridine; ethyl ester; methyl ester | anti-arrhythmia drug; antihypertensive agent; calcium channel blocker; vasodilator agent |
| fenofibrate Pharmavit: a polyvitamin product, comprising vitamins A, D2, B1, B2, B6, C, E, nicotinamide, & calcium pantothene; may be a promising agent for application to human populations exposed to carcinogenic and genetic hazards of ionizing radiation; RN from CHEMLINE | 3.23 | 1 | 0 | aromatic ether; chlorobenzophenone; isopropyl ester; monochlorobenzenes | antilipemic drug; environmental contaminant; geroprotector; xenobiotic |
| fenoldopam Fenoldopam: A dopamine D1 receptor agonist that is used as an antihypertensive agent. It lowers blood pressure through arteriolar vasodilation. | 3.23 | 1 | 0 | benzazepine | alpha-adrenergic agonist; antihypertensive agent; dopamine agonist; dopaminergic antagonist; vasodilator agent |
| fenoprofen Fenoprofen: A propionic acid derivative that is used as a non-steroidal anti-inflammatory agent.. fenoprofen : A monocarboxylic acid that is propanoic acid in which one of the hydrogens at position 2 is substituted by a 3-phenoxyphenyl group. A non-steroidal anti-inflammatory drug, the dihydrate form of the calcium salt is used for the management of mild to moderate pain and for the relief of pain and inflammation associated with disorders such as arthritis. It is pharmacologically similar to aspirin, but causes less gastrointestinal bleeding. | 3.23 | 1 | 0 | monocarboxylic acid | antipyretic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; drug allergen; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| fexofenadine fexofenadine: a second generation antihistamine; metabolite of the antihistaminic drug terfenadine; structure in first source; RN refers to HCl. fexofenadine : A piperidine-based anti-histamine compound. | 3.23 | 1 | 0 | piperidines; tertiary amine | anti-allergic agent; H1-receptor antagonist |
| fipexide fipexide: regulates dopaminergic systems at macromolecular level | 3.23 | 1 | 0 | benzodioxoles | |
| flavoxate Flavoxate: A drug that has been used in various urinary syndromes and as an antispasmodic. Its therapeutic usefulness and its mechanism of action are not clear. It may have local anesthetic activity and direct relaxing effects on smooth muscle as well as some activity as a muscarinic antagonist.. flavoxate : A carboxylic ester resulting from the formal condensation of 3-methylflavone-8-carboxylic acid with 2-(1-piperidinyl)ethanol. | 3.23 | 1 | 0 | carboxylic ester; flavones; piperidines; tertiary amino compound | antispasmodic drug; muscarinic antagonist; parasympatholytic |
| flecainide Flecainide: A potent anti-arrhythmia agent, effective in a wide range of ventricular and atrial ARRHYTHMIAS and TACHYCARDIAS.. flecainide : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 2,5-bis(2,2,2-trifluoroethoxy)benzoic acid with the primary amino group of piperidin-2-ylmethylamine. An antiarrhythmic agent used (in the form of its acetate salt) to prevent and treat tachyarrhythmia (abnormal fast rhythm of the heart). | 3.23 | 1 | 0 | aromatic ether; monocarboxylic acid amide; organofluorine compound; piperidines | anti-arrhythmia drug |
| fluconazole Fluconazole: Triazole antifungal agent that is used to treat oropharyngeal CANDIDIASIS and cryptococcal MENINGITIS in AIDS.. fluconazole : A member of the class of triazoles that is propan-2-ol substituted at position 1 and 3 by 1H-1,2,4-triazol-1-yl groups and at position 2 by a 2,4-difluorophenyl group. It is an antifungal drug used for the treatment of mucosal candidiasis and for systemic infections including systemic candidiasis, coccidioidomycosis, and cryptococcosis. | 9.98 | 2 | 1 | conazole antifungal drug; difluorobenzene; tertiary alcohol; triazole antifungal drug | environmental contaminant; P450 inhibitor; xenobiotic |
| flucytosine Flucytosine: A fluorinated cytosine analog that is used as an antifungal agent.. flucytosine : An organofluorine compound that is cytosine that is substituted at position 5 by a fluorine. A prodrug for the antifungal 5-fluorouracil, it is used for the treatment of systemic fungal infections. | 3.23 | 1 | 0 | aminopyrimidine; nucleoside analogue; organofluorine compound; pyrimidine antifungal drug; pyrimidone | prodrug |
| fluphenazine [no description available] | 3.23 | 1 | 0 | N-alkylpiperazine; organofluorine compound; phenothiazines | anticoronaviral agent; dopaminergic antagonist; phenothiazine antipsychotic drug |
| flumazenil Flumazenil: A potent benzodiazepine receptor antagonist. Since it reverses the sedative and other actions of benzodiazepines, it has been suggested as an antidote to benzodiazepine overdoses.. flumazenil : An organic heterotricyclic compound that is 5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted at positions 3, 5, 6, and 8 by ethoxycarbonyl, methyl, oxo, and fluoro groups, respectively. It is used as an antidote to benzodiazepine overdose. | 3.23 | 1 | 0 | ethyl ester; imidazobenzodiazepine; organofluorine compound | antidote to benzodiazepine poisoning; GABA antagonist |
| fluorescite fluorescein (acid form) : A xanthene dye that is highly fluorescent and commonly used as a fluorescent tracer. | 3.23 | 1 | 0 | benzoic acids; cyclic ketone; hydroxy monocarboxylic acid; organic heterotricyclic compound; phenols; xanthene dye | fluorescent dye; radioopaque medium |
| fluorouracil Fluorouracil: A pyrimidine analog that is an antineoplastic antimetabolite. It interferes with DNA synthesis by blocking the THYMIDYLATE SYNTHETASE conversion of deoxyuridylic acid to thymidylic acid.. 5-fluorouracil : A nucleobase analogue that is uracil in which the hydrogen at position 5 is replaced by fluorine. It is an antineoplastic agent which acts as an antimetabolite - following conversion to the active deoxynucleotide, it inhibits DNA synthesis (by blocking the conversion of deoxyuridylic acid to thymidylic acid by the cellular enzyme thymidylate synthetase) and so slows tumour growth. | 3.23 | 1 | 0 | nucleobase analogue; organofluorine compound | antimetabolite; antineoplastic agent; environmental contaminant; immunosuppressive agent; radiosensitizing agent; xenobiotic |
| fluoxetine Fluoxetine: The first highly specific serotonin uptake inhibitor. It is used as an antidepressant and often has a more acceptable side-effects profile than traditional antidepressants.. fluoxetine : A racemate comprising equimolar amounts of (R)- and (S)-fluoxetine. A selective serotonin reuptake inhibitor (SSRI), it is used (generally as the hydrochloride salt) for the treatment of depression (and the depressive phase of bipolar disorder), bullimia nervosa, and obsessive-compulsive disorder.. N-methyl-3-phenyl-3-[4-(trifluoromethyl)phenoxy]propan-1-amine : An aromatic ether consisting of 4-trifluoromethylphenol in which the hydrogen of the phenolic hydroxy group is replaced by a 3-(methylamino)-1-phenylpropyl group. | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; aromatic ether; secondary amino compound | |
| flurazepam Flurazepam: A benzodiazepine derivative used mainly as a hypnotic.. flurazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a 2-(diethylamino)ethyl group, 2-fluorophenyl group and chloro group at positions 1, 5 and 7, respectively. It is a partial agonist of GABAA receptors and used for the treatment of insomnia. | 3.23 | 1 | 0 | 1,4-benzodiazepinone; monofluorobenzenes; organochlorine compound; tertiary amino compound | anticonvulsant; anxiolytic drug; GABAA receptor agonist; sedative |
| flurbiprofen Flurbiprofen: An anti-inflammatory analgesic and antipyretic of the phenylalkynoic acid series. It has been shown to reduce bone resorption in periodontal disease by inhibiting CARBONIC ANHYDRASE.. flurbiprofen : A monocarboxylic acid that is a 2-fluoro-[1,1'-biphenyl-4-yl] moiety linked to C-2 of propionic acid. A non-steroidal anti-inflammatory, analgesic and antipyretic, it is used as a pre-operative anti-miotic as well as orally for arthritis or dental pain. | 3.23 | 1 | 0 | fluorobiphenyl; monocarboxylic acid | antipyretic; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| flutamide Flutamide: An antiandrogen with about the same potency as cyproterone in rodent and canine species. | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; monocarboxylic acid amide | androgen antagonist; antineoplastic agent |
| fomepizole Fomepizole: A pyrazole and competitive inhibitor of ALCOHOL DEHYDROGENASE that is used for the treatment of poisoning by ETHYLENE GLYCOL or METHANOL.. fomepizole : A member of the class of pyrazoles that is 1H-pyrazole substituted by a methyl group at position 4. | 3.23 | 1 | 0 | pyrazoles | antidote; EC 1.1.1.1 (alcohol dehydrogenase) inhibitor; protective agent |
| foscarnet Foscarnet: An antiviral agent used in the treatment of cytomegalovirus retinitis. Foscarnet also shows activity against human herpesviruses and HIV.. phosphonoformic acid : Phosphoric acid in which one of the hydroxy groups is replaced by a carboxylic acid group. It is used as the trisodium salt as an antiviral agent in the treatment of cytomegalovirus retinitis (CMV retinitis, an inflamation of the retina that can lead to blindness) and as an alternative to ganciclovir for AIDS patients who require concurrent antiretroviral therapy but are unable to tolerate ganciclovir due to haematological toxicity. | 3.23 | 1 | 0 | carboxylic acid; one-carbon compound; phosphonic acids | antiviral drug; geroprotector; HIV-1 reverse transcriptase inhibitor; sodium-dependent Pi-transporter inhibitor |
| furosemide Furosemide: A benzoic-sulfonamide-furan. It is a diuretic with fast onset and short duration that is used for EDEMA and chronic RENAL INSUFFICIENCY.. furosemide : A chlorobenzoic acid that is 4-chlorobenzoic acid substituted by a (furan-2-ylmethyl)amino and a sulfamoyl group at position 2 and 5 respectively. It is a diuretic used in the treatment of congestive heart failure. | 3.23 | 1 | 0 | chlorobenzoic acid; furans; sulfonamide | environmental contaminant; loop diuretic; xenobiotic |
| gabapentin Gabapentin: A cyclohexane-gamma-aminobutyric acid derivative that is used for the treatment of PARTIAL SEIZURES; NEURALGIA; and RESTLESS LEGS SYNDROME.. gabapentin : A gamma-amino acid that is cyclohexane substituted at position 1 by aminomethyl and carboxymethyl groups. Used for treatment of neuropathic pain and restless legs syndrome. | 3.23 | 1 | 0 | gamma-amino acid | anticonvulsant; calcium channel blocker; environmental contaminant; xenobiotic |
| gemfibrozil [no description available] | 3.23 | 1 | 0 | aromatic ether | antilipemic drug |
| glafenine Glafenine: An anthranilic acid derivative with analgesic properties used for the relief of all types of pain.. glafenine : A carboxylic ester that is 2,3-dihydroxypropyl anthranilate in which the amino group is substituted by a 7-chloroquinolin-4-yl group. A non-steroidal anti-inflammatory drug, glafenine and its hydrochloride salt were used for the relief of all types of pain, but high incidence of anaphylactic reactions resulted in their withdrawal from the market. | 3.23 | 1 | 0 | aminoquinoline; carboxylic ester; glycol; organochlorine compound; secondary amino compound | inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| glimepiride glimepiride: structure given in first source | 3.23 | 1 | 0 | sulfonamide | |
| glipizide Glipizide: An oral hypoglycemic agent which is rapidly absorbed and completely metabolized.. glipizide : An N-sulfonylurea that is glyburide in which the (5-chloro-2-methoxybenzoyl group is replaced by a (5-methylpyrazin-2-yl)carbonyl group. An oral hypoglycemic agent, it is used in the treatment of type 2 diabetes mellitus. | 3.23 | 1 | 0 | aromatic amide; monocarboxylic acid amide; N-sulfonylurea; pyrazines | EC 2.7.1.33 (pantothenate kinase) inhibitor; hypoglycemic agent; insulin secretagogue |
| glyburide Glyburide: An antidiabetic sulfonylurea derivative with actions like those of chlorpropamide. glyburide : An N-sulfonylurea that is acetohexamide in which the acetyl group is replaced by a 2-(5-chloro-2-methoxybenzamido)ethyl group. | 3.23 | 1 | 0 | monochlorobenzenes; N-sulfonylurea | anti-arrhythmia drug; EC 2.7.1.33 (pantothenate kinase) inhibitor; EC 3.6.3.49 (channel-conductance-controlling ATPase) inhibitor; hypoglycemic agent |
| 2-cyclopentyl-2-hydroxy-2-phenylacetic acid (1,1-dimethyl-3-pyrrolidin-1-iumyl) ester [no description available] | 3.23 | 1 | 0 | benzenes | |
| granisetron [no description available] | 3.23 | 1 | 0 | aromatic amide; indazoles | |
| guaifenesin Guaifenesin: An expectorant that also has some muscle relaxing action. It is used in many cough preparations. | 3.23 | 1 | 0 | methoxybenzenes | |
| guanethidine Guanethidine: An antihypertensive agent that acts by inhibiting selectively transmission in post-ganglionic adrenergic nerves. It is believed to act mainly by preventing the release of norepinephrine at nerve endings and causes depletion of norepinephrine in peripheral sympathetic nerve terminals as well as in tissues.. guanethidine : A member of the class of guanidines in which one of the hydrogens of the amino group has been replaced by a 2-azocan-1-ylethyl group.. guanethidine sulfate : A organic sulfate salt composed of two molecules of guanethidine and one of sulfuric acid. | 3.23 | 1 | 0 | azocanes; guanidines | adrenergic antagonist; antihypertensive agent; sympatholytic agent |
| guanfacine Guanfacine: A centrally acting antihypertensive agent with specificity towards ADRENERGIC ALPHA-2 RECEPTORS. | 3.23 | 1 | 0 | acetamides | |
| guanidine Guanidine: A strong organic base existing primarily as guanidium ions at physiological pH. It is found in the urine as a normal product of protein metabolism. It is also used in laboratory research as a protein denaturant. (From Martindale, the Extra Pharmacopoeia, 30th ed and Merck Index, 12th ed) It is also used in the treatment of myasthenia and as a fluorescent probe in HPLC.. guanidine : An aminocarboxamidine, the parent compound of the guanidines. | 3.23 | 1 | 0 | carboxamidine; guanidines; one-carbon compound | |
| haloperidol Haloperidol: A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279). haloperidol : A compound composed of a central piperidine structure with hydroxy and p-chlorophenyl substituents at position 4 and an N-linked p-fluorobutyrophenone moiety. | 3.23 | 1 | 0 | aromatic ketone; hydroxypiperidine; monochlorobenzenes; organofluorine compound; tertiary alcohol | antidyskinesia agent; antiemetic; dopaminergic antagonist; first generation antipsychotic; serotonergic antagonist |
| hydralazine Hydralazine: A direct-acting vasodilator that is used as an antihypertensive agent.. hydralazine : The 1-hydrazino derivative of phthalazine; a direct-acting vasodilator that is used as an antihypertensive agent. | 3.23 | 1 | 0 | azaarene; hydrazines; ortho-fused heteroarene; phthalazines | antihypertensive agent; vasodilator agent |
| hydrochlorothiazide Hydrochlorothiazide: A thiazide diuretic often considered the prototypical member of this class. It reduces the reabsorption of electrolytes from the renal tubules. This results in increased excretion of water and electrolytes, including sodium, potassium, chloride, and magnesium. It is used in the treatment of several disorders including edema, hypertension, diabetes insipidus, and hypoparathyroidism.. hydrochlorothiazide : A benzothiadiazine that is 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide substituted by a chloro group at position 6 and a sulfonamide at 7. It is diuretic used for the treatment of hypertension and congestive heart failure. | 3.23 | 1 | 0 | benzothiadiazine; organochlorine compound; sulfonamide | antihypertensive agent; diuretic; environmental contaminant; xenobiotic |
| hydroflumethiazide Hydroflumethiazide: A thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p822). hydroflumethiazide : A benzothiadiazine consisting of a 3,4-dihydro-HH-1,2,4-benzothiadiazine bicyclic system dioxygenated on sulfur and carrying trifluoromethyl and aminosulfonyl groups at positions 6 and 7 respectively. A diuretic with actions and uses similar to those of hydrochlorothiazide. | 3.23 | 1 | 0 | benzothiadiazine; thiazide | antihypertensive agent; diuretic |
| hydroxychloroquine Hydroxychloroquine: A chemotherapeutic agent that acts against erythrocytic forms of malarial parasites. Hydroxychloroquine appears to concentrate in food vacuoles of affected protozoa. It inhibits plasmodial heme polymerase. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p970). hydroxychloroquine : An aminoquinoline that is chloroquine in which one of the N-ethyl groups is hydroxylated at position 2. An antimalarial with properties similar to chloroquine that acts against erythrocytic forms of malarial parasites, it is mainly used as the sulfate salt for the treatment of lupus erythematosus, rheumatoid arthritis, and light-sensitive skin eruptions. | 3.23 | 1 | 0 | aminoquinoline; organochlorine compound; primary alcohol; secondary amino compound; tertiary amino compound | anticoronaviral agent; antimalarial; antirheumatic drug; dermatologic drug |
| hydroxyurea [no description available] | 3.23 | 1 | 0 | one-carbon compound; ureas | antimetabolite; antimitotic; antineoplastic agent; DNA synthesis inhibitor; EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor; genotoxin; immunomodulator; radical scavenger; teratogenic agent |
| hydroxyzine Hydroxyzine: A histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness. It is also effective as an antiemetic, for relief of anxiety and tension, and as a sedative.. hydroxyzine : A N-alkylpiperazine that is piperzine in which the nitrogens atoms are substituted by 2-(2-hydroxyethoxy)ethyl and (4-chlorophenyl)(phenyl)methyl groups respectively. | 3.23 | 1 | 0 | hydroxyether; monochlorobenzenes; N-alkylpiperazine | anticoronaviral agent; antipruritic drug; anxiolytic drug; dermatologic drug; H1-receptor antagonist |
| ibuprofen Midol: combination of cinnamedrine, phenacetin, aspirin & caffeine | 3.23 | 1 | 0 | monocarboxylic acid | antipyretic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; drug allergen; environmental contaminant; geroprotector; non-narcotic analgesic; non-steroidal anti-inflammatory drug; radical scavenger; xenobiotic |
| phenelzine Phenelzine: One of the MONOAMINE OXIDASE INHIBITORS used to treat DEPRESSION; PHOBIC DISORDERS; and PANIC. | 3.23 | 1 | 0 | primary amine | |
| lidocaine Lidocaine: A local anesthetic and cardiac depressant used as an antiarrhythmia agent. Its actions are more intense and its effects more prolonged than those of PROCAINE but its duration of action is shorter than that of BUPIVACAINE or PRILOCAINE.. lidocaine : The monocarboxylic acid amide resulting from the formal condensation of N,N-diethylglycine with 2,6-dimethylaniline. | 3.23 | 1 | 0 | benzenes; monocarboxylic acid amide; tertiary amino compound | anti-arrhythmia drug; drug allergen; environmental contaminant; local anaesthetic; xenobiotic |
| ifosfamide [no description available] | 3.23 | 1 | 0 | ifosfamides | alkylating agent; antineoplastic agent; environmental contaminant; immunosuppressive agent; xenobiotic |
| imipramine Imipramine: The prototypical tricyclic antidepressant. It has been used in major depression, dysthymia, bipolar depression, attention-deficit disorders, agoraphobia, and panic disorders. It has less sedative effect than some other members of this therapeutic group.. imipramine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine substituted by a 3-(dimethylamino)propyl group at the nitrogen atom. | 3.23 | 1 | 0 | dibenzoazepine | adrenergic uptake inhibitor; antidepressant; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor |
| amrinone Amrinone: A positive inotropic cardiotonic (CARDIOTONIC AGENTS) with vasodilator properties, phosphodiesterase 3 inhibitory activity, and the ability to stimulate calcium ion influx into the cardiac cell.. amrinone : A 3,4'-bipyridine substituted at positions 5 and 6 by an amino group and a keto function respectively. A pyridine phosphodiesterase 3 inhibitor, it is a drug that may improve the prognosis in patients with congestive heart failure. | 3.23 | 1 | 0 | bipyridines | EC 3.1.4.* (phosphoric diester hydrolase) inhibitor |
| indapamide Indapamide: A benzamide-sulfonamide-indole derived DIURETIC that functions by inhibiting SODIUM CHLORIDE SYMPORTERS.. indapamide : A sulfonamide formed by condensation of the carboxylic group of 4-chloro-3-sulfamoylbenzoic acid with the amino group of 2-methyl-2,3-dihydro-1H-indol-1-amine. | 3.23 | 1 | 0 | indoles; organochlorine compound; sulfonamide | antihypertensive agent; diuretic |
| indomethacin Indomethacin: A non-steroidal anti-inflammatory agent (NSAID) that inhibits CYCLOOXYGENASE, which is necessary for the formation of PROSTAGLANDINS and other AUTACOIDS. It also inhibits the motility of POLYMORPHONUCLEAR LEUKOCYTES.. indometacin : A member of the class of indole-3-acetic acids that is indole-3-acetic acid in which the indole ring is substituted at positions 1, 2 and 5 by p-chlorobenzoyl, methyl, and methoxy groups, respectively. A non-steroidal anti-inflammatory drug, it is used in the treatment of musculoskeletal and joint disorders including osteoarthritis, rheumatoid arthritis, gout, bursitis and tendinitis. | 3.23 | 1 | 0 | aromatic ether; indole-3-acetic acids; monochlorobenzenes; N-acylindole | analgesic; drug metabolite; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; environmental contaminant; gout suppressant; non-steroidal anti-inflammatory drug; xenobiotic metabolite; xenobiotic |
| ioversol [no description available] | 3.23 | 1 | 0 | amidobenzoic acid | |
| iproniazid [no description available] | 3.23 | 1 | 0 | carbohydrazide; pyridines | |
| avapro Irbesartan: A spiro compound, biphenyl and tetrazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION, and in the treatment of kidney disease.. irbesartan : A biphenylyltetrazole that is an angiotensin II receptor antagonist used mainly for the treatment of hypertension. | 3.23 | 1 | 0 | azaspiro compound; biphenylyltetrazole | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| isocarboxazid Isocarboxazid: An MAO inhibitor that is effective in the treatment of major depression, dysthymic disorder, and atypical depression. It also is useful in the treatment of panic disorder and the phobic disorders. (From AMA, Drug Evaluations Annual, 1994, p311) | 3.23 | 1 | 0 | benzenes | |
| isoniazid Hydra: A genus of freshwater polyps in the family Hydridae, order Hydroida, class HYDROZOA. They are of special interest because of their complex organization and because their adult organization corresponds roughly to the gastrula of higher animals.. hydrazide : Compounds derived from oxoacids RkE(=O)l(OH)m (l =/= 0) by replacing -OH by -NRNR2 (R groups are commonly H). (IUPAC). | 3.23 | 1 | 0 | carbohydrazide | antitubercular agent; drug allergen |
| isoproterenol Isoproterenol: Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.. isoprenaline : A secondary amino compound that is noradrenaline in which one of the hydrogens attached to the nitrogen is replaced by an isopropyl group. A sympathomimetic acting almost exclusively on beta-adrenergic receptors, it is used (mainly as the hydrochloride salt) as a bronghodilator and heart stimulant for the management of a variety of cardiac disorders. | 3.23 | 1 | 0 | catechols; secondary alcohol; secondary amino compound | beta-adrenergic agonist; bronchodilator agent; cardiotonic drug; sympathomimetic agent |
| isoxsuprine Isoxsuprine: A beta-adrenergic agonist that causes direct relaxation of uterine and vascular smooth muscle. Its vasodilating actions are greater on the arteries supplying skeletal muscle than on those supplying skin. It is used in the treatment of peripheral vascular disease and in premature labor. | 3.23 | 1 | 0 | alkylbenzene | |
| isradipine Isradipine: A potent antagonist of CALCIUM CHANNELS that is highly selective for VASCULAR SMOOTH MUSCLE. It is effective in the treatment of chronic stable angina pectoris, hypertension, and congestive cardiac failure. | 3.23 | 1 | 0 | benzoxadiazole; dihydropyridine; isopropyl ester; methyl ester | |
| itraconazole [no description available] | 3.23 | 1 | 0 | piperazines | |
| ketamine Ketamine: A cyclohexanone derivative used for induction of anesthesia. Its mechanism of action is not well understood, but ketamine can block NMDA receptors (RECEPTORS, N-METHYL-D-ASPARTATE) and may interact with sigma receptors.. ketamine : A member of the class of cyclohexanones in which one of the hydrogens at position 2 is substituted by a 2-chlorophenyl group, while the other is substituted by a methylamino group. | 3.23 | 1 | 0 | cyclohexanones; monochlorobenzenes; secondary amino compound | analgesic; environmental contaminant; intravenous anaesthetic; neurotoxin; NMDA receptor antagonist; xenobiotic |
| ketoconazole 1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine : A dioxolane that is 1,3-dioxolane which is substituted at positions 2, 2, and 4 by imidazol-1-ylmethyl, 2,4-dichlorophenyl, and [para-(4-acetylpiperazin-1-yl)phenoxy]methyl groups, respectively. | 11.26 | 5 | 2 | dichlorobenzene; dioxolane; ether; imidazoles; N-acylpiperazine; N-arylpiperazine | |
| ketoprofen Ketoprofen: An IBUPROFEN-type anti-inflammatory analgesic and antipyretic. It is used in the treatment of rheumatoid arthritis and osteoarthritis.. ketoprofen : An oxo monocarboxylic acid that consists of propionic acid substituted by a 3-benzoylphenyl group at position 2. | 3.23 | 1 | 0 | benzophenones; oxo monocarboxylic acid | antipyretic; drug allergen; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; environmental contaminant; non-steroidal anti-inflammatory drug; xenobiotic |
| ketorolac Ketorolac: A pyrrolizine carboxylic acid derivative structurally related to INDOMETHACIN. It is an NSAID and is used principally for its analgesic activity. (From Martindale The Extra Pharmacopoeia, 31st ed). ketorolac : A racemate comprising equimolar amounts of (R)-(+)- and (S)-(-)-5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid. While only the (S)-(-) enantiomer is a COX1 and COX2 inhibitor, the (R)-(+) enantiomer exhibits potent analgesic activity. A non-steroidal anti-inflammatory drug, ketorolac is mainly used (generally as the tromethamine salt) for its potent analgesic properties in the short-term management of post-operative pain, and in eye drops to relieve the ocular itching associated with seasonal allergic conjunctivitis. It was withdrawn from the market in many countries in 1993 following association with haemorrhage and renal failure.. 5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid : A member of the class of pyrrolizines that is 2,3-dihydro-1H-pyrrolizine which is substituted at positions 1 and 5 by carboxy and benzoyl groups, respectively. | 3.23 | 1 | 0 | amino acid; aromatic ketone; monocarboxylic acid; pyrrolizines; racemate | analgesic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug |
| labetalol Labetalol: A salicylamide derivative that is a non-cardioselective blocker of BETA-ADRENERGIC RECEPTORS and ALPHA-1 ADRENERGIC RECEPTORS.. labetalol : A diastereoisomeric mixture of approximately equal amounts of all four possible stereoisomers ((R,S)-labetolol, (S,R)-labetolol, (S,S)-labetalol and (R,R)-labetalol). It is an adrenergic antagonist used to treat high blood pressure.. 2-hydroxy-5-{1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl}benzamide : A member of the class of benzamides that is benzamide substituted by a hydroxy group at position 2 and by a 1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl group at position 5. | 3.23 | 1 | 0 | benzamides; benzenes; phenols; primary carboxamide; salicylamides; secondary alcohol; secondary amino compound | |
| lamotrigine [no description available] | 3.23 | 1 | 0 | 1,2,4-triazines; dichlorobenzene; primary arylamine | anticonvulsant; antidepressant; antimanic drug; calcium channel blocker; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; environmental contaminant; excitatory amino acid antagonist; geroprotector; non-narcotic analgesic; xenobiotic |
| lansoprazole Lansoprazole: A 2,2,2-trifluoroethoxypyridyl derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS. Lansoprazole is a racemic mixture of (R)- and (S)-isomers. | 3.23 | 1 | 0 | benzimidazoles; pyridines; sulfoxide | anti-ulcer drug; EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor |
| leflunomide Leflunomide: An isoxazole derivative that inhibits dihydroorotate dehydrogenase, the fourth enzyme in the pyrimidine biosynthetic pathway. It is used an immunosuppressive agent in the treatment of RHEUMATOID ARTHRITIS and PSORIATIC ARTHRITIS.. leflunomide : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 5-methyl-1,2-oxazole-4-carboxylic acid with the anilino group of 4-(trifluoromethyl)aniline. The prodrug of teriflunomide. | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; isoxazoles; monocarboxylic acid amide | antineoplastic agent; antiparasitic agent; EC 1.3.98.1 [dihydroorotate oxidase (fumarate)] inhibitor; EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor; hepatotoxic agent; immunosuppressive agent; non-steroidal anti-inflammatory drug; prodrug; pyrimidine synthesis inhibitor; tyrosine kinase inhibitor |
| letrozole [no description available] | 3.23 | 1 | 0 | nitrile; triazoles | antineoplastic agent; EC 1.14.14.14 (aromatase) inhibitor |
| lomefloxacin lomefloxacin: structure given in first source. lomefloxacin : A fluoroquinolone antibiotic, used (generally as the hydrochloride salt) to treat bacterial infections including bronchitis and urinary tract infections. It is also used to prevent urinary tract infections prior to surgery. | 3.23 | 1 | 0 | fluoroquinolone antibiotic; N-arylpiperazine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone | antimicrobial agent; antitubercular agent; photosensitizing agent |
| lomustine [no description available] | 3.23 | 1 | 0 | N-nitrosoureas; organochlorine compound | alkylating agent; antineoplastic agent |
| loperamide Loperamide: One of the long-acting synthetic ANTIDIARRHEALS; it is not significantly absorbed from the gut, and has no effect on the adrenergic system or central nervous system, but may antagonize histamine and interfere with acetylcholine release locally.. loperamide : A synthetic piperidine derivative, effective against diarrhoea resulting from gastroenteritis or inflammatory bowel disease. | 3.23 | 1 | 0 | monocarboxylic acid amide; monochlorobenzenes; piperidines; tertiary alcohol | anticoronaviral agent; antidiarrhoeal drug; mu-opioid receptor agonist |
| loratadine Loratadine: A second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (HISTAMINE H1 ANTAGONISTS) it lacks central nervous system depressing effects such as drowsiness.. loratadine : A benzocycloheptapyridine that is 6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine substituted by a chloro group at position 8 and a 1-(ethoxycarbonyl)piperidin-4-ylidene group at position 11. It is a H1-receptor antagonist commonly employed in the treatment of allergic disorders. | 3.23 | 1 | 0 | benzocycloheptapyridine; ethyl ester; N-acylpiperidine; organochlorine compound; tertiary carboxamide | anti-allergic agent; cholinergic antagonist; geroprotector; H1-receptor antagonist |
| lorazepam Lorazepam: A benzodiazepine used as an anti-anxiety agent with few side effects. It also has hypnotic, anticonvulsant, and considerable sedative properties and has been proposed as a preanesthetic agent. | 3.23 | 1 | 0 | benzodiazepine | |
| losartan Losartan: An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.. losartan : A biphenylyltetrazole where a 1,1'-biphenyl group is attached at the 5-position and has an additional trisubstituted imidazol-1-ylmethyl group at the 4'-position | 3.23 | 1 | 0 | biphenylyltetrazole; imidazoles | angiotensin receptor antagonist; anti-arrhythmia drug; antihypertensive agent; endothelin receptor antagonist |
| loxapine Loxapine: An antipsychotic agent used in SCHIZOPHRENIA. | 3.23 | 1 | 0 | dibenzooxazepine | antipsychotic agent; dopaminergic antagonist |
| maprotiline Maprotiline: A bridged-ring tetracyclic antidepressant that is both mechanistically and functionally similar to the tricyclic antidepressants, including side effects associated with its use. | 3.23 | 1 | 0 | anthracenes | |
| mebendazole Mebendazole: A benzimidazole that acts by interfering with CARBOHYDRATE METABOLISM and inhibiting polymerization of MICROTUBULES.. mebendazole : A carbamate ester that is methyl 1H-benzimidazol-2-ylcarbamate substituted by a benzoyl group at position 5. | 3.23 | 1 | 0 | aromatic ketone; benzimidazoles; carbamate ester | antinematodal drug; microtubule-destabilising agent; tubulin modulator |
| mecamylamine Mecamylamine: A nicotinic antagonist that is well absorbed from the gastrointestinal tract and crosses the blood-brain barrier. Mecamylamine has been used as a ganglionic blocker in treating hypertension, but, like most ganglionic blockers, is more often used now as a research tool. | 3.23 | 1 | 0 | primary aliphatic amine | |
| mechlorethamine nitrogen mustard : Compounds having two beta-haloalkyl groups bound to a nitrogen atom, as in (X-CH2-CH2)2NR. | 3.23 | 1 | 0 | nitrogen mustard; organochlorine compound | alkylating agent |
| meclizine Meclizine: A histamine H1 antagonist used in the treatment of motion sickness, vertigo, and nausea during pregnancy and radiation sickness. | 3.23 | 1 | 0 | diarylmethane | |
| meclofenamic acid Meclofenamic Acid: A non-steroidal anti-inflammatory agent with antipyretic and antigranulation activities. It also inhibits prostaglandin biosynthesis.. meclofenamic acid : An aminobenzoic acid that is anthranilic acid in which one of the hydrogens attached to the nitrogen is replaced by a 2,6-dichloro-3-methylphenyl group. A non-steroidal anti-inflammatory drug, it is used as the sodium salt for the treatment of dysmenorrhoea (painful periods), osteoarthritis and rheumatoid arthritis. | 3.23 | 1 | 0 | aminobenzoic acid; organochlorine compound; secondary amino compound | analgesic; anticonvulsant; antineoplastic agent; antipyretic; antirheumatic drug; EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-steroidal anti-inflammatory drug |
| mefenamic acid Mefenamic Acid: A non-steroidal anti-inflammatory agent with analgesic, anti-inflammatory, and antipyretic properties. It is an inhibitor of cyclooxygenase.. mefenamic acid : An aminobenzoic acid that is anthranilic acid in which one of the hydrogens attached to the nitrogen is replaced by a 2,3-dimethylphenyl group. Although classed as a non-steroidal anti-inflammatory drug, its anti-inflammatory properties are considered to be minor. It is used to relieve mild to moderate pain, including headaches, dental pain, osteoarthritis and rheumatoid arthritis. | 3.23 | 1 | 0 | aminobenzoic acid; secondary amino compound | analgesic; antipyretic; antirheumatic drug; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; environmental contaminant; non-steroidal anti-inflammatory drug; xenobiotic |
| memantine [no description available] | 3.23 | 1 | 0 | adamantanes; primary aliphatic amine | antidepressant; antiparkinson drug; dopaminergic agent; neuroprotective agent; NMDA receptor antagonist |
| mepenzolate mepenzolic acid: anticholinergic, antispasmodic agent; RN given refers to parent cpd; structure | 3.23 | 1 | 0 | diarylmethane | |
| meperidine Meperidine: A narcotic analgesic that can be used for the relief of most types of moderate to severe pain, including postoperative pain and the pain of labor. Prolonged use may lead to dependence of the morphine type; withdrawal symptoms appear more rapidly than with morphine and are of shorter duration.. pethidine : A piperidinecarboxylate ester that is piperidine which is substituted by a methyl group at position 1 and by phenyl and ethoxycarbonyl groups at position 4. It is an analgesic which is used for the treatment of moderate to severe pain, including postoperative pain and labour pain. | 3.23 | 1 | 0 | ethyl ester; piperidinecarboxylate ester; tertiary amino compound | antispasmodic drug; kappa-opioid receptor agonist; mu-opioid receptor agonist; opioid analgesic |
| mephenytoin Mephenytoin: An anticonvulsant effective in tonic-clonic epilepsy (EPILEPSY, TONIC-CLONIC). It may cause blood dyscrasias.. mephenytoin : An imidazolidine-2,4-dione (hydantoin) in which the imidazolidine nucleus carries a methyl group at N-3 and has ethyl and phenyl substituents at C-5. An anticonvulsant, it is no longer available in the USA or the UK but is still studied largely because of its interesting hydroxylation polymorphism. | 3.23 | 1 | 0 | imidazolidine-2,4-dione | anticonvulsant |
| mepivacaine Mepivacaine: A local anesthetic that is chemically related to BUPIVACAINE but pharmacologically related to LIDOCAINE. It is indicated for infiltration, nerve block, and epidural anesthesia. Mepivacaine is effective topically only in large doses and therefore should not be used by this route. (From AMA Drug Evaluations, 1994, p168). mepivacaine : A piperidinecarboxamide in which N-methylpipecolic acid and 2,6-dimethylaniline have combined to form the amide bond. It is used as a local amide-type anaesthetic. | 3.23 | 1 | 0 | piperidinecarboxamide | drug allergen; local anaesthetic |
| meprobamate Meprobamate: A carbamate with hypnotic, sedative, and some muscle relaxant properties, although in therapeutic doses reduction of anxiety rather than a direct effect may be responsible for muscle relaxation. Meprobamate has been reported to have anticonvulsant actions against petit mal seizures, but not against grand mal seizures (which may be exacerbated). It is used in the treatment of ANXIETY DISORDERS, and also for the short-term management of INSOMNIA but has largely been superseded by the BENZODIAZEPINES. (From Martindale, The Extra Pharmacopoeia, 30th ed, p603) | 3.23 | 1 | 0 | organic molecular entity | |
| mesalamine Mesalamine: An anti-inflammatory agent, structurally related to the SALICYLATES, which is active in INFLAMMATORY BOWEL DISEASE. It is considered to be the active moiety of SULPHASALAZINE. (From Martindale, The Extra Pharmacopoeia, 30th ed). mesalamine : A monohydroxybenzoic acid that is salicylic acid substituted by an amino group at the 5-position. | 3.23 | 1 | 0 | amino acid; aromatic amine; monocarboxylic acid; monohydroxybenzoic acid; phenols | non-steroidal anti-inflammatory drug |
| mesoridazine Mesoridazine: A phenothiazine antipsychotic with effects similar to CHLORPROMAZINE.. mesoridazine : A phenothiazine substituted at position 2 (para to the S atom) by a methylsulfinyl group, and on the nitrogen by a 2-(1-methylpiperidin-2-yl)ethyl group. | 3.23 | 1 | 0 | phenothiazines; sulfoxide; tertiary amino compound | dopaminergic antagonist; first generation antipsychotic |
| metaproterenol Metaproterenol: A beta-2 adrenergic agonist used in the treatment of ASTHMA and BRONCHIAL SPASM.. orciprenaline : A racemate composed of equimolar amounts of (R)- and (S)-orciprenaline. Used (as its sulfate salt) to relax the airway muscles and improve breathing for patients suffering from asthma or bronchitis.. 5-[1-hydroxy-2-(isopropanylamino)ethyl]benzene-1,3-diol : A member of the class of resorcinols bearing an additional 1-hydroxy-2-(isopropanylamino)ethyl substituent at position 5 of resorcinol itself. | 3.23 | 1 | 0 | aralkylamino compound; phenylethanolamines; resorcinols; secondary alcohol; secondary amino compound | |
| metformin Metformin: A biguanide hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. Metformin improves glycemic control by improving insulin sensitivity and decreasing intestinal absorption of glucose. (From Martindale, The Extra Pharmacopoeia, 30th ed, p289). metformin : A member of the class of guanidines that is biguanide the carrying two methyl substituents at position 1. | 3.23 | 1 | 0 | guanidines | environmental contaminant; geroprotector; hypoglycemic agent; xenobiotic |
| methadone Methadone: A synthetic opioid that is used as the hydrochloride. It is an opioid analgesic that is primarily a mu-opioid agonist. It has actions and uses similar to those of MORPHINE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1082-3). methadone : A racemate comprising equimolar amounts of dextromethadone and levomethadone. It is a opioid analgesic which is used as a painkiller and as a substitute for heroin in the treatment of heroin addiction.. 6-(dimethylamino)-4,4-diphenylheptan-3-one : A ketone that is heptan-3-one substituted by a dimethylamino group at position 6 and two phenyl groups at position 4. | 3.23 | 1 | 0 | benzenes; diarylmethane; ketone; tertiary amino compound | |
| methazolamide Methazolamide: A carbonic anhydrase inhibitor that is used as a diuretic and in the treatment of glaucoma. | 3.23 | 1 | 0 | sulfonamide; thiadiazoles | |
| methocarbamol Methocarbamol: A centrally acting muscle relaxant whose mode of action has not been established. It is used as an adjunct in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1206). methocarbamol : A racemate comprising equimolar amounts of (R)- and (S)-methocarbamol. A centrally acting skeletal muscle relaxant, it is used as an adjunct in the short-term symptomatic treatment of painful muscle spasm. The (R)-enantiomer is more active than the (S)-enantiomer.. 2-hydroxy-3-(2-methoxyphenoxy)propyl carbamate : A carbamate ester that is glycerol in which one of the primary alcohol groups has been converted to its 2-methoxyphenyl ether while the other has been converted to the corresponding carbamate ester. | 3.23 | 1 | 0 | aromatic ether; carbamate ester; secondary alcohol | |
| methoxsalen Methoxsalen: A naturally occurring furocoumarin compound found in several species of plants, including Psoralea corylifolia. It is a photoactive substance that forms DNA ADDUCTS in the presence of ultraviolet A irradiation.. methoxsalen : A member of the class of psoralens that is 7H-furo[3,2-g]chromen-7-one in which the 9 position is substituted by a methoxy group. It is a constituent of the fruits of Ammi majus. Like other psoralens, trioxsalen causes photosensitization of the skin. It is administered topically or orally in conjunction with UV-A for phototherapy treatment of vitiligo and severe psoriasis. | 3.23 | 1 | 0 | aromatic ether; psoralens | antineoplastic agent; cross-linking reagent; dermatologic drug; photosensitizing agent; plant metabolite |
| methyclothiazide Methyclothiazide: A thiazide diuretic with properties similar to those of HYDROCHLOROTHIAZIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p825) | 3.23 | 1 | 0 | benzothiadiazine | |
| methylphenidate Methylphenidate: A central nervous system stimulant used most commonly in the treatment of ATTENTION DEFICIT DISORDER in children and for NARCOLEPSY. Its mechanisms appear to be similar to those of DEXTROAMPHETAMINE. The d-isomer of this drug is referred to as DEXMETHYLPHENIDATE HYDROCHLORIDE.. methylphenidate : A racemate comprising equimolar amounts of the two threo isomers of methyl phenyl(piperidin-2-yl)acetate. A central stimulant and indirect-acting sympathomimetic, is used (generally as the hydrochloride salt) in the treatment of hyperactivity disorders in children and for the treatment of narcolepsy.. methyl phenyl(piperidin-2-yl)acetate : A amino acid ester that is methyl phenylacetate in which one of the hydrogens alpha to the carbonyl group is replaced by a piperidin-2-yl group. | 3.23 | 1 | 0 | beta-amino acid ester; methyl ester; piperidines | |
| metoclopramide Metoclopramide: A dopamine D2 antagonist that is used as an antiemetic.. metoclopramide : A member of the class of benzamides resulting from the formal condensation of 4-amino-5-chloro-2-methoxybenzoic acid with the primary amino group of N,N-diethylethane-1,2-diamine. | 3.23 | 1 | 0 | benzamides; monochlorobenzenes; substituted aniline; tertiary amino compound | antiemetic; dopaminergic antagonist; environmental contaminant; gastrointestinal drug; xenobiotic |
| metolazone Metolazone: A quinazoline-sulfonamide derived DIURETIC that functions by inhibiting SODIUM CHLORIDE SYMPORTERS.. metolazone : A quinazoline that consists of 1,2,3,4-tetrahydroquinazolin-4-one bearing additional methyl, 2-tolyl, sulfamyl and chloro substituents at positions 2, 3, 6 and 7 respectively. A quinazoline diuretic, with properties similar to thiazide diuretics. | 3.23 | 1 | 0 | organochlorine compound; quinazolines; sulfonamide | antihypertensive agent; diuretic; ion transport inhibitor |
| metoprolol Metoprolol: A selective adrenergic beta-1 blocking agent that is commonly used to treat ANGINA PECTORIS; HYPERTENSION; and CARDIAC ARRHYTHMIAS.. metoprolol : A propanolamine that is 1-(propan-2-ylamino)propan-2-ol substituted by a 4-(2-methoxyethyl)phenoxy group at position 1. | 3.23 | 1 | 0 | aromatic ether; propanolamine; secondary alcohol; secondary amino compound | antihypertensive agent; beta-adrenergic antagonist; environmental contaminant; geroprotector; xenobiotic |
| metronidazole Metronidazole: A nitroimidazole used to treat AMEBIASIS; VAGINITIS; TRICHOMONAS INFECTIONS; GIARDIASIS; ANAEROBIC BACTERIA; and TREPONEMAL INFECTIONS.. metronidazole : A member of the class of imidazoles substituted at C-1, -2 and -5 with 2-hydroxyethyl, nitro and methyl groups respectively. It has activity against anaerobic bacteria and protozoa, and has a radiosensitising effect on hypoxic tumour cells. It may be given by mouth in tablets, or as the benzoate in an oral suspension. The hydrochloride salt can be used in intravenous infusions. Metronidazole is a prodrug and is selective for anaerobic bacteria due to their ability to intracellularly reduce the nitro group of metronidazole to give nitroso-containing intermediates. These can covalently bind to DNA, disrupting its helical structure, inducing DNA strand breaks and inhibiting bacterial nucleic acid synthesis, ultimately resulting in bacterial cell death. | 3.23 | 1 | 0 | C-nitro compound; imidazoles; primary alcohol | antiamoebic agent; antibacterial drug; antimicrobial agent; antiparasitic agent; antitrichomonal drug; environmental contaminant; prodrug; radiosensitizing agent; xenobiotic |
| metyrapone Metyrapone: An inhibitor of the enzyme STEROID 11-BETA-MONOOXYGENASE. It is used as a test of the feedback hypothalamic-pituitary mechanism in the diagnosis of CUSHING SYNDROME.. metyrapone : An aromatic ketone that is 3,3-dimethylbutan-2-one in which the methyl groups at positions 1 and 4 are replaced by pyridin-3-yl groups. A steroid 11beta-monooxygenase (EC 1.14.15.4) inhibitor, it is used in the diagnosis of adrenal insufficiency. | 3.23 | 1 | 0 | aromatic ketone | antimetabolite; diagnostic agent; EC 1.14.15.4 (steroid 11beta-monooxygenase) inhibitor |
| mexiletine Mexiletine: Antiarrhythmic agent pharmacologically similar to LIDOCAINE. It may have some anticonvulsant properties.. mexiletine : An aromatic ether which is 2,6-dimethylphenyl ether of 2-aminopropan-1-ol. | 3.23 | 1 | 0 | aromatic ether; primary amino compound | anti-arrhythmia drug |
| midazolam Midazolam: A short-acting hypnotic-sedative drug with anxiolytic and amnestic properties. It is used in dentistry, cardiac surgery, endoscopic procedures, as preanesthetic medication, and as an adjunct to local anesthesia. The short duration and cardiorespiratory stability makes it useful in poor-risk, elderly, and cardiac patients. It is water-soluble at pH less than 4 and lipid-soluble at physiological pH.. midazolam : An imidazobenzodiazepine that is 4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted by a methyl, 2-fluorophenyl and chloro groups at positions 1, 6 and 8, respectively. | 3.23 | 1 | 0 | imidazobenzodiazepine; monofluorobenzenes; organochlorine compound | anticonvulsant; antineoplastic agent; anxiolytic drug; apoptosis inducer; central nervous system depressant; GABAA receptor agonist; general anaesthetic; muscle relaxant; sedative |
| midodrine Midodrine: An ethanolamine derivative that is an adrenergic alpha-1 agonist. It is used as a vasoconstrictor agent in the treatment of HYPOTENSION.. midodrine : An aromatic ether that is 1,4-dimethoxybenzene which is substituted at position 2 by a 2-(glycylamino)-1-hydroxyethyl group. A direct-acting sympathomimetic with selective alpha-adrenergic agonist activity, it is used (generally as its hydrochloride salt) as a peripheral vasoconstrictor in the treatment of certain hypotensive states. The main active moiety is its major metabolite, deglymidodrine. | 3.23 | 1 | 0 | amino acid amide; aromatic ether; secondary alcohol | alpha-adrenergic agonist; prodrug; sympathomimetic agent; vasoconstrictor agent |
| milrinone [no description available] | 3.23 | 1 | 0 | bipyridines; nitrile; pyridone | cardiotonic drug; EC 3.1.4.17 (3',5'-cyclic-nucleotide phosphodiesterase) inhibitor; platelet aggregation inhibitor; vasodilator agent |
| minoxidil Minoxidil: A potent direct-acting peripheral vasodilator (VASODILATOR AGENTS) that reduces peripheral resistance and produces a fall in BLOOD PRESSURE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p371). minoxidil : A pyrimidine N-oxide that is pyrimidine-2,4-diamine 3-oxide substituted by a piperidin-1-yl group at position 6. | 3.23 | 1 | 0 | dialkylarylamine; tertiary amino compound | |
| mirtazapine Mirtazapine: A piperazinoazepine tetracyclic compound that enhances the release of NOREPINEPHRINE and SEROTONIN through blockage of presynaptic ALPHA-2 ADRENERGIC RECEPTORS. It also blocks both 5-HT2 and 5-HT3 serotonin receptors and is a potent HISTAMINE H1 RECEPTOR antagonist. It is used for the treatment of depression, and may also be useful for the treatment of anxiety disorders. | 3.23 | 1 | 0 | benzazepine; tetracyclic antidepressant | alpha-adrenergic antagonist; anxiolytic drug; H1-receptor antagonist; histamine antagonist; oneirogen; serotonergic antagonist |
| mitotane Mitotane: A derivative of the insecticide DICHLORODIPHENYLDICHLOROETHANE that specifically inhibits cells of the adrenal cortex and their production of hormones. It is used to treat adrenocortical tumors and causes CNS damage, but no bone marrow depression. | 3.23 | 1 | 0 | diarylmethane | |
| mitoxantrone Mitoxantrone: An anthracenedione-derived antineoplastic agent.. mitoxantrone : A dihydroxyanthraquinone that is 1,4-dihydroxy-9,10-anthraquinone which is substituted by 6-hydroxy-1,4-diazahexyl groups at positions 5 and 8. | 3.23 | 1 | 0 | dihydroxyanthraquinone | analgesic; antineoplastic agent |
| modafinil Modafinil: A benzhydryl acetamide compound, central nervous system stimulant, and CYP3A4 inducing agent that is used in the treatment of NARCOLEPSY and SLEEP WAKE DISORDERS.. modafinil : A racemate comprising equimolar amounts of armodafinil and (S)-modafinil. A central nervous system stimulant, it is used for the treatment of sleeping disorders such as narcolepsy, obstructive sleep apnoea, and shift-work sleep disorder. The optical enantiomers of modafinil have similar pharmacological actions in animals.. 2-[(diphenylmethyl)sulfinyl]acetamide : A sulfoxide that is dimethylsulfoxide in which two hydrogens attached to one of the methyl groups are replaced by phenyl groups, while one hydrogen attached to the other methyl group is replaced by a carbamoyl (aminocarbonyl) group. | 3.23 | 1 | 0 | monocarboxylic acid amide; sulfoxide | |
| moxisylyte Moxisylyte: An alpha-adrenergic blocking agent that is used in Raynaud's disease. It is also used locally in the eye to reverse the mydriasis caused by phenylephrine and other sympathomimetic agents. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1312) | 3.23 | 1 | 0 | monoterpenoid | |
| nabumetone Nabumetone: A butanone non-steroidal anti-inflammatory drug and cyclooxygenase-2 (COX2) inhibitor that is used in the management of pain associated with OSTEOARTHRITIS and RHEUMATOID ARTHRITIS.. nabumetone : A methyl ketone that is 2-butanone in which one of the methyl hydrogens at position 4 is replaced by a 6-methoxy-2-naphthyl group. A prodrug that is converted to the active metabolite, 6-methoxy-2-naphthylacetic acid, following oral administration. It is shown to have a slightly lower risk of gastrointestinal side effects than most other non-steroidal anti-inflammatory drugs. | 3.23 | 1 | 0 | methoxynaphthalene; methyl ketone | cyclooxygenase 2 inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug; prodrug |
| nadolol [no description available] | 3.23 | 1 | 0 | tetralins | |
| nalidixic acid [no description available] | 3.23 | 1 | 0 | 1,8-naphthyridine derivative; monocarboxylic acid; quinolone antibiotic | antibacterial drug; antimicrobial agent; DNA synthesis inhibitor |
| naratriptan naratriptan: structure given in first source | 3.23 | 1 | 0 | heteroarylpiperidine; sulfonamide; tryptamines | serotonergic agonist; vasoconstrictor agent |
| nefazodone nefazodone: may be useful as an opiate adjunct | 3.23 | 1 | 0 | aromatic ether; monochlorobenzenes; N-alkylpiperazine; N-arylpiperazine; triazoles | alpha-adrenergic antagonist; analgesic; antidepressant; serotonergic antagonist; serotonin uptake inhibitor |
| nevirapine Nevirapine: A potent, non-nucleoside reverse transcriptase inhibitor used in combination with nucleoside analogues for treatment of HIV INFECTIONS and AIDS.. nevirapine : A dipyridodiazepine that is 5,11-dihydro-6H-dipyrido[3,2-b:2',3'-e][1,4]diazepine which is substituted by methyl, oxo, and cyclopropyl groups at positions 4, 6, and 11, respectively. A non-nucleoside reverse transcriptase inhibitor with activity against HIV-1, it is used in combination with other antiretrovirals for the treatment of HIV infection. | 3.23 | 1 | 0 | cyclopropanes; dipyridodiazepine | antiviral drug; HIV-1 reverse transcriptase inhibitor |
| nialamide Nialamide: An MAO inhibitor that is used as an antidepressive agent. | 3.23 | 1 | 0 | organonitrogen compound; organooxygen compound | |
| nicardipine Nicardipine: A potent calcium channel blockader with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardiodepressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents.. nicardipine : A racemate comprising equimolar amounts of (R)- and (S)-nicardipine. It is a calcium channel blocker which is used to treat hypertension.. 2-[benzyl(methyl)amino]ethyl methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate : A dihydropyridine that is 1,4-dihydropyridine substituted by a methyl, {2-[benzyl(methyl)amino]ethoxy}carbonyl, 3-nitrophenyl, methoxycarbonyl and methyl groups at positions 2, 3, 4, 5 and 6, respectively. | 3.23 | 1 | 0 | benzenes; C-nitro compound; diester; dihydropyridine; methyl ester; tertiary amino compound | |
| nifedipine Nifedipine: A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure. | 3.23 | 1 | 0 | C-nitro compound; dihydropyridine; methyl ester | calcium channel blocker; human metabolite; tocolytic agent; vasodilator agent |
| nilutamide [no description available] | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; C-nitro compound; imidazolidinone | androgen antagonist; antineoplastic agent |
| nimesulide nimesulide: structure. nimesulide : An aromatic ether having phenyl and 2-methylsulfonamido-5-nitrophenyl as the two aryl groups. | 3.23 | 1 | 0 | aromatic ether; C-nitro compound; sulfonamide | cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug |
| nimodipine Nimodipine: A calcium channel blockader with preferential cerebrovascular activity. It has marked cerebrovascular dilating effects and lowers blood pressure.. nimodipine : A dihydropyridine that is 1,4-dihydropyridine which is substituted by methyl groups at positions 2 and 6, a (2-methoxyethoxy)carbonyl group at position 3, a m-nitrophenyl group at position 4, and an isopropoxycarbonyl group at position 5. An L-type calcium channel blocker, it acts particularly on cerebral circulation, and is used both orally and intravenously for the prevention and treatment of subarachnoid hemorrhage from ruptured intracranial aneurysm. | 3.23 | 1 | 0 | 2-methoxyethyl ester; C-nitro compound; dicarboxylic acids and O-substituted derivatives; diester; dihydropyridine; isopropyl ester | antihypertensive agent; calcium channel blocker; cardiovascular drug; vasodilator agent |
| nisoldipine Nisoldipine: A dihydropyridine calcium channel antagonist that acts as a potent arterial vasodilator and antihypertensive agent. It is also effective in patients with cardiac failure and angina.. nisoldipine : A racemate consisting of equimolar amounts of (R)- and (S)-nisoldipine. A calcium channel blocker, it is used in the treatment of hypertension and angina pectoris.. methyl 2-methylpropyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate : A dihydropyridine that is 1,4-dihydropyridine which is substituted by methyl groups at positions 2 and 6, a methoxycarbonyl group at position 3, an o-nitrophenyl group at position 4, and an isobutoxycarbonyl group at position 5. The racemate, a calcium channel blocker, is used in the treatment of hypertension and angina pectoris. | 3.23 | 1 | 0 | C-nitro compound; dicarboxylic acids and O-substituted derivatives; diester; dihydropyridine; methyl ester | |
| nitroglycerin Nitroglycerin: A volatile vasodilator which relieves ANGINA PECTORIS by stimulating GUANYLATE CYCLASE and lowering cytosolic calcium. It is also sometimes used for TOCOLYSIS and explosives.. nitroglycerol : A nitrate ester that is glycerol in which nitro group(s) replace the hydrogen(s) attached to one or more of the hydroxy groups.. nitroglycerin : A nitroglycerol that is glycerol in which the hydrogen atoms of all three hydroxy groups are replaced by nitro groups. It acts as a prodrug, releasing nitric oxide to open blood vessels and so alleviate heart pain. | 3.23 | 1 | 0 | nitroglycerol | explosive; muscle relaxant; nitric oxide donor; prodrug; tocolytic agent; vasodilator agent; xenobiotic |
| nizatidine [no description available] | 3.23 | 1 | 0 | 1,3-thiazoles; C-nitro compound; carboxamidine; organic sulfide; tertiary amino compound | anti-ulcer drug; cholinergic drug; H2-receptor antagonist |
| nomifensine Nomifensine: An isoquinoline derivative that prevents dopamine reuptake into synaptosomes. The maleate was formerly used in the treatment of depression. It was withdrawn worldwide in 1986 due to the risk of acute hemolytic anemia with intravascular hemolysis resulting from its use. In some cases, renal failure also developed. (From Martindale, The Extra Pharmacopoeia, 30th ed, p266). nomifensine : An N-methylated tetrahydroisoquinoline carrying phenyl and amino substituents at positions C-4 and C-8, respectively. | 3.23 | 1 | 0 | isoquinolines | dopamine uptake inhibitor |
| norfloxacin Norfloxacin: A synthetic fluoroquinolone (FLUOROQUINOLONES) with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin inhibits bacterial DNA GYRASE.. norfloxacin : A quinolinemonocarboxylic acid with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase. | 3.23 | 1 | 0 | fluoroquinolone antibiotic; N-arylpiperazine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone | antibacterial drug; DNA synthesis inhibitor; environmental contaminant; xenobiotic |
| nortriptyline Nortriptyline: A metabolite of AMITRIPTYLINE that is also used as an antidepressive agent. Nortriptyline is used in major depression, dysthymia, and atypical depressions.. nortriptyline : An organic tricyclic compound that is 10,11-dihydro-5H-dibenzo[a,d][7]annulene substituted by a 3-(methylamino)propylidene group at position 5. It is an active metabolite of amitriptyline. | 3.23 | 1 | 0 | organic tricyclic compound; secondary amine | adrenergic uptake inhibitor; analgesic; antidepressant; antineoplastic agent; apoptosis inducer; drug metabolite |
| ofloxacin Ofloxacin: A synthetic fluoroquinolone antibacterial agent that inhibits the supercoiling activity of bacterial DNA GYRASE, halting DNA REPLICATION.. 9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid : An oxazinoquinoline that is 2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinolin-7-one substituted by methyl, carboxy, fluoro, and 4-methylpiperazin-1-yl groups at positions 3, 6, 9, and 10, respectively.. ofloxacin : A racemate comprising equimolar amounts of levofloxacin and dextrofloxacin. It is a synthetic fluoroquinolone antibacterial agent which inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication. | 3.23 | 1 | 0 | 3-oxo monocarboxylic acid; N-arylpiperazine; N-methylpiperazine; organofluorine compound; oxazinoquinoline | |
| omeprazole Omeprazole: A 4-methoxy-3,5-dimethylpyridyl, 5-methoxybenzimidazole derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits an H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS.. omeprazole : A racemate comprising equimolar amounts of (R)- and (S)-omeprazole.. 5-methoxy-2-{[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl}-1H-benzimidazole : A member of the class of benzimidazoles that is 1H-benzimidazole which is substituted by a [4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl group at position 2 and a methoxy group at position 5. | 3.23 | 1 | 0 | aromatic ether; benzimidazoles; pyridines; sulfoxide | |
| ondansetron Ondansetron: A competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties. | 3.23 | 1 | 0 | carbazoles | |
| orphenadrine Orphenadrine: A muscarinic antagonist used to treat drug-induced parkinsonism and to relieve pain from muscle spasm.. orphenadrine : A tertiary amino compound which is the phenyl-o-tolylmethyl ether of 2-(dimethylamino)ethanol. | 3.23 | 1 | 0 | ether; tertiary amino compound | antidyskinesia agent; antiparkinson drug; H1-receptor antagonist; muscarinic antagonist; muscle relaxant; NMDA receptor antagonist; parasympatholytic |
| oxaprozin Oxaprozin: An oxazole-propionic acid derivative, cyclooxygenase inhibitor, and non-steroidal anti-inflammatory drug that is used in the treatment of pain and inflammation associated with of OSTEOARTHRITIS; RHEUMATOID ARTHRITIS; and ARTHRITIS, JUVENILE.. oxaprozin : A monocarboxylic acid that is a propionic acid derivative having a 4,5-diphenyl-1,3-oxazol-2-yl substituent at position 3. It is non-steroidal anti-inflammatory drug commonly used to relieve the pain and inflammatory responses associated with osteoarthritis and rheumatoid arthritis. | 3.23 | 1 | 0 | 1,3-oxazoles; monocarboxylic acid | analgesic; non-steroidal anti-inflammatory drug |
| oxazepam Oxazepam: A benzodiazepine used in the treatment of anxiety, alcohol withdrawal, and insomnia.. oxazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a hydroxy group at position 3 and phenyl group at position 5. | 3.23 | 1 | 0 | 1,4-benzodiazepinone; organochlorine compound | anxiolytic drug; environmental contaminant; xenobiotic |
| oxybutynin oxybutynin: RN given refers to parent cpd. oxybutynin : A racemate comprising equimolar amounts of (R)-oxybutynin and esoxybutynin. An antispasmodic used for the treatment of overactive bladder. | 10.49 | 17 | 2 | acetylenic compound; carboxylic ester; racemate; tertiary alcohol; tertiary amino compound | antispasmodic drug; calcium channel blocker; local anaesthetic; muscarinic antagonist; muscle relaxant; parasympatholytic |
| aminosalicylic acid Aminosalicylic Acid: An antitubercular agent often administered in association with ISONIAZID. The sodium salt of the drug is better tolerated than the free acid.. 4-aminosalicylic acid : An aminobenzoic acid that is salicylic acid substituted by an amino group at position 4. | 3.23 | 1 | 0 | aminobenzoic acid; phenols | antitubercular agent |
| pamidronate [no description available] | 3.23 | 1 | 0 | phosphonoacetic acid | |
| pantoprazole Pantoprazole: 2-pyridinylmethylsulfinylbenzimidazole proton pump inhibitor that is used in the treatment of GASTROESOPHAGEAL REFLUX and PEPTIC ULCER.. pantoprazole : A member of the class of benzimidazoles that is 1H-benzimidazole substituted by a difluoromethoxy group at position 5 and a [(3,4-dimethoxypyridin-2-yl)methyl]sulfinyl group at position 2. | 3.23 | 1 | 0 | aromatic ether; benzimidazoles; organofluorine compound; pyridines; sulfoxide | anti-ulcer drug; EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor; environmental contaminant; xenobiotic |
| papaverine Papaverine: An alkaloid found in opium but not closely related to the other opium alkaloids in its structure or pharmacological actions. It is a direct-acting smooth muscle relaxant used in the treatment of impotence and as a vasodilator, especially for cerebral vasodilation. The mechanism of its pharmacological actions is not clear, but it apparently can inhibit phosphodiesterases and it may have direct actions on calcium channels.. papaverine : A benzylisoquinoline alkaloid that is isoquinoline substituted by methoxy groups at positions 6 and 7 and a 3,4-dimethoxybenzyl group at position 1. It has been isolated from Papaver somniferum. | 3.23 | 1 | 0 | benzylisoquinoline alkaloid; dimethoxybenzene; isoquinolines | antispasmodic drug; vasodilator agent |
| pemoline Pemoline: A central nervous system stimulant used in fatigue and depressive states and to treat hyperkinetic disorders in children.. pemoline : A member of the class of 1,3-oxazoles that is 1,3-oxazol-4(5H)-one which is substituted by an amino group at position 2 and by a phenyl group at position 5. A central nervous system stimulant, it was used to treat hyperactivity disorders in children, but withdrawn from use following reports of serious hepatotoxicity. | 3.23 | 1 | 0 | 1,3-oxazoles | central nervous system stimulant |
| pentamidine Pentamidine: Antiprotozoal agent effective in trypanosomiasis, leishmaniasis, and some fungal infections; used in treatment of PNEUMOCYSTIS pneumonia in HIV-infected patients. It may cause diabetes mellitus, central nervous system damage, and other toxic effects.. pentamidine : A diether consisting of pentane-1,5-diol in which both hydroxyl hydrogens have been replaced by 4-amidinophenyl groups. A trypanocidal drug that is used for treatment of cutaneous leishmaniasis and Chagas disease. | 3.23 | 1 | 0 | aromatic ether; carboxamidine; diether | anti-inflammatory agent; antifungal agent; calmodulin antagonist; chemokine receptor 5 antagonist; EC 2.3.1.48 (histone acetyltransferase) inhibitor; NMDA receptor antagonist; S100 calcium-binding protein B inhibitor; trypanocidal drug; xenobiotic |
| pentobarbital Pentobarbital: A short-acting barbiturate that is effective as a sedative and hypnotic (but not as an anti-anxiety) agent and is usually given orally. It is prescribed more frequently for sleep induction than for sedation but, like similar agents, may lose its effectiveness by the second week of continued administration. (From AMA Drug Evaluations Annual, 1994, p236). pentobarbital : A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by ethyl and sec-pentyl groups. | 3.23 | 1 | 0 | barbiturates | GABAA receptor agonist |
| pentoxifylline [no description available] | 3.23 | 1 | 0 | oxopurine | |
| perhexiline Perhexiline: 2-(2,2-Dicyclohexylethyl)piperidine. Coronary vasodilator used especially for angina of effort. It may cause neuropathy and hepatitis. | 3.23 | 1 | 0 | piperidines | cardiovascular drug |
| perphenazine Perphenazine: An antipsychotic phenothiazine derivative with actions and uses similar to those of CHLORPROMAZINE.. perphenazine : A phenothiazine derivative in which the phenothiazine tricycle carries a chloro substituent at the 2-position and a 3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl group at N-10. | 3.23 | 1 | 0 | N-(2-hydroxyethyl)piperazine; N-alkylpiperazine; organochlorine compound; phenothiazines | antiemetic; dopaminergic antagonist; phenothiazine antipsychotic drug |
| phenobarbital Phenobarbital: A barbituric acid derivative that acts as a nonselective central nervous system depressant. It potentiates GAMMA-AMINOBUTYRIC ACID action on GABA-A RECEPTORS, and modulates chloride currents through receptor channels. It also inhibits glutamate induced depolarizations.. phenobarbital : A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by ethyl and phenyl groups. | 3.23 | 1 | 0 | barbiturates | anticonvulsant; drug allergen; excitatory amino acid antagonist; sedative |
| phenoxybenzamine Phenoxybenzamine: An alpha-adrenergic antagonist with long duration of action. It has been used to treat hypertension and as a peripheral vasodilator. | 3.23 | 1 | 0 | aromatic amine | |
| phentermine Phentermine: A central nervous system stimulant and sympathomimetic with actions and uses similar to those of DEXTROAMPHETAMINE. It has been used most frequently in the treatment of obesity. | 3.23 | 1 | 0 | primary amine | adrenergic agent; appetite depressant; central nervous system drug; central nervous system stimulant; dopaminergic agent; sympathomimetic agent |
| 4-phenylbutyric acid 4-phenylbutyric acid: RN refers to the parent cpd. 4-phenylbutyric acid : A monocarboxylic acid the structure of which is that of butyric acid substituted with a phenyl group at C-4. It is a histone deacetylase inhibitor that displays anticancer activity. It inhibits cell proliferation, invasion and migration and induces apoptosis in glioma cells. It also inhibits protein isoprenylation, depletes plasma glutamine, increases production of foetal haemoglobin through transcriptional activation of the gamma-globin gene and affects hPPARgamma activation. | 3.23 | 1 | 0 | monocarboxylic acid | antineoplastic agent; apoptosis inducer; EC 3.5.1.98 (histone deacetylase) inhibitor; prodrug |
| pindolol Pindolol: A moderately lipophilic beta blocker (ADRENERGIC BETA-ANTAGONISTS). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638). pindolol : A member of the class of indols which is the 2-hydroxy-3-(isopropylamino)propyl ether derivative of 1H-indol-4-ol. | 3.23 | 1 | 0 | indoles; secondary amine | antiglaucoma drug; antihypertensive agent; beta-adrenergic antagonist; serotonergic antagonist; vasodilator agent |
| pioglitazone Pioglitazone: A thiazolidinedione and PPAR GAMMA agonist that is used in the treatment of TYPE 2 DIABETES MELLITUS.. pioglitazone : A member of the class of thiazolidenediones that is 1,3-thiazolidine-2,4-dione substituted by a benzyl group at position 5 which in turn is substituted by a 2-(5-ethylpyridin-2-yl)ethoxy group at position 4 of the phenyl ring. It exhibits hypoglycemic activity. | 3.23 | 1 | 0 | aromatic ether; pyridines; thiazolidinediones | antidepressant; cardioprotective agent; EC 2.7.1.33 (pantothenate kinase) inhibitor; EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor; ferroptosis inhibitor; geroprotector; hypoglycemic agent; insulin-sensitizing drug; PPARgamma agonist; xenobiotic |
| polythiazide [no description available] | 3.23 | 1 | 0 | benzothiadiazine | |
| duodote duodote: consists of atropine and pralidoxime chloride; for treating those exposed to organophosphorus-containing nerve agents | 3.23 | 1 | 0 | pyridinium ion | antidote to organophosphate poisoning; antidote to sarin poisoning; cholinergic drug; cholinesterase reactivator |
| praziquantel azinox: Russian drug | 3.23 | 1 | 0 | isoquinolines | |
| prazosin Prazosin: A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.. prazosin : A member of the class of piperazines that is piperazine substituted by a furan-2-ylcarbonyl group and a 4-amino-6,7-dimethoxyquinazolin-2-yl group at positions 1 and 4 respectively. | 3.23 | 1 | 0 | aromatic ether; furans; monocarboxylic acid amide; piperazines; quinazolines | alpha-adrenergic antagonist; antihypertensive agent; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor |
| primaquine Primaquine: An aminoquinoline that is given by mouth to produce a radical cure and prevent relapse of vivax and ovale malarias following treatment with a blood schizontocide. It has also been used to prevent transmission of falciparum malaria by those returning to areas where there is a potential for re-introduction of malaria. Adverse effects include anemias and GI disturbances. (From Martindale, The Extra Pharmacopeia, 30th ed, p404). primaquine : An N-substituted diamine that is pentane-1,4-diamine substituted by a 6-methoxyquinolin-8-yl group at the N(4) position. It is a drug used in the treatment of malaria and Pneumocystis pneumonia. | 3.23 | 1 | 0 | aminoquinoline; aromatic ether; N-substituted diamine | antimalarial |
| primidone Primidone: A barbiturate derivative that acts as a GABA modulator and anti-epileptic agent. It is partly metabolized to PHENOBARBITAL in the body and owes some of its actions to this metabolite.. primidone : A pyrimidone that is dihydropyrimidine-4,6(1H,5H)-dione substituted by an ethyl and a phenyl group at position 5. It is used as an anticonvulsant for treatment of various types of seizures. | 3.23 | 1 | 0 | pyrimidone | anticonvulsant; environmental contaminant; xenobiotic |
| probenecid Probenecid: The prototypical uricosuric agent. It inhibits the renal excretion of organic anions and reduces tubular reabsorption of urate. Probenecid has also been used to treat patients with renal impairment, and, because it reduces the renal tubular excretion of other drugs, has been used as an adjunct to antibacterial therapy.. probenecid : A sulfonamide in which the nitrogen of 4-sulfamoylbenzoic acid is substituted with two propyl groups. | 3.23 | 1 | 0 | benzoic acids; sulfonamide | uricosuric drug |
| procainamide Procainamide: A class Ia antiarrhythmic drug that is structurally-related to PROCAINE.. procainamide : A benzamide that is 4-aminobenzamide substituted on the amide N by a 2-(diethylamino)ethyl group. It is a pharmaceutical antiarrhythmic agent used for the medical treatment of cardiac arrhythmias. | 3.23 | 1 | 0 | benzamides | anti-arrhythmia drug; platelet aggregation inhibitor; sodium channel blocker |
| procarbazine Procarbazine: An antineoplastic agent used primarily in combination with mechlorethamine, vincristine, and prednisone (the MOPP protocol) in the treatment of Hodgkin's disease.. procarbazine : A benzamide obtained by formal condensation of the carboxy group of 4-[(2-methylhydrazino)methyl]benzoic acid with the amino group of isopropylamine. An antineoplastic chemotherapy drug used for treatment of Hodgkin's lymphoma. Metabolism yields azo-procarbazine and hydrogen peroxide, which results in the breaking of DNA strands. | 3.23 | 1 | 0 | benzamides; hydrazines | antineoplastic agent |
| prochlorperazine Prochlorperazine: A phenothiazine antipsychotic used principally in the treatment of NAUSEA; VOMITING; and VERTIGO. It is more likely than CHLORPROMAZINE to cause EXTRAPYRAMIDAL DISORDERS. (From Martindale, The Extra Pharmacopoeia, 30th ed, p612). prochlorperazine : A member of the class of phenothiazines that is 10H-phenothiazine having a chloro substituent at the 2-position and a 3-(4-methylpiperazin-1-yl)propyl group at the N-10 position. | 3.23 | 1 | 0 | N-alkylpiperazine; N-methylpiperazine; organochlorine compound; phenothiazines | alpha-adrenergic antagonist; antiemetic; cholinergic antagonist; dopamine receptor D2 antagonist; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; first generation antipsychotic |
| procyclidine Procyclidine: A muscarinic antagonist that crosses the blood-brain barrier and is used in the treatment of drug-induced extrapyramidal disorders and in parkinsonism.. procyclidine : A tertiary alcohol that consists of propan-1-ol substituted by a cyclohexyl and a phenyl group at position 1 and a pyrrolidin-1-yl group at position 3. | 3.23 | 1 | 0 | pyrrolidines; tertiary alcohol | antidyskinesia agent; antiparkinson drug; muscarinic antagonist |
| promethazine Promethazine: A phenothiazine derivative with histamine H1-blocking, antimuscarinic, and sedative properties. It is used as an antiallergic, in pruritus, for motion sickness and sedation, and also in animals.. promethazine : A tertiary amine that is a substituted phenothiazine in which the ring nitrogen at position 10 is attached to C-3 of an N,N-dimethylpropan-2-amine moiety. | 3.23 | 1 | 0 | phenothiazines; tertiary amine | anti-allergic agent; anticoronaviral agent; antiemetic; antipruritic drug; H1-receptor antagonist; local anaesthetic; sedative |
| propafenone Propafenone: An antiarrhythmia agent that is particularly effective in ventricular arrhythmias. It also has weak beta-blocking activity.. propafenone : An aromatic ketone that is 3-(propylamino)propane-1,2-diol in which the hydrogen of the primary hydroxy group is replaced by a 2-(3-phenylpropanoyl)phenyl group. It is a class 1C antiarrhythmic drug with local anesthetic effects, and is used as the hydrochloride salt in the management of supraventricular and ventricular arrhythmias. | 3.23 | 1 | 0 | aromatic ketone; secondary alcohol; secondary amino compound | anti-arrhythmia drug |
| propantheline Propantheline: A muscarinic antagonist used as an antispasmodic, in rhinitis, in urinary incontinence, and in the treatment of ulcers. At high doses it has nicotinic effects resulting in neuromuscular blocking. | 3.23 | 1 | 0 | xanthenes | |
| propiverine propiverine: anticholinergic used for overactive bladder syndrome | 12.94 | 5 | 1 | diarylmethane | |
| propofol Propofol: An intravenous anesthetic agent which has the advantage of a very rapid onset after infusion or bolus injection plus a very short recovery period of a couple of minutes. (From Smith and Reynard, Textbook of Pharmacology, 1992, 1st ed, p206). Propofol has been used as ANTICONVULSANTS and ANTIEMETICS.. propofol : A phenol resulting from the formal substitution of the hydrogen at the 2 position of 1,3-diisopropylbenzene by a hydroxy group. | 3.23 | 1 | 0 | phenols | anticonvulsant; antiemetic; intravenous anaesthetic; radical scavenger; sedative |
| propranolol Propranolol: A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs.. propranolol : A propanolamine that is propan-2-ol substituted by a propan-2-ylamino group at position 1 and a naphthalen-1-yloxy group at position 3. | 3.23 | 1 | 0 | naphthalenes; propanolamine; secondary amine | anti-arrhythmia drug; antihypertensive agent; anxiolytic drug; beta-adrenergic antagonist; environmental contaminant; human blood serum metabolite; vasodilator agent; xenobiotic |
| protriptyline Protriptyline: Tricyclic antidepressant similar in action and side effects to IMIPRAMINE. It may produce excitation. | 3.23 | 1 | 0 | carbotricyclic compound | antidepressant |
| pyridostigmine [no description available] | 3.23 | 1 | 0 | pyridinium ion | |
| pyrimethamine Maloprim: contains above 2 cpds | 3.23 | 1 | 0 | aminopyrimidine; monochlorobenzenes | antimalarial; antiprotozoal drug; EC 1.5.1.3 (dihydrofolate reductase) inhibitor |
| sch 16134 quazepam: structure given in first source | 3.23 | 1 | 0 | benzodiazepine | |
| quetiapine [no description available] | 3.23 | 1 | 0 | dibenzothiazepine; N-alkylpiperazine; N-arylpiperazine | adrenergic antagonist; dopaminergic antagonist; histamine antagonist; second generation antipsychotic; serotonergic antagonist |
| rabeprazole Rabeprazole: A 4-(3-methoxypropoxy)-3-methylpyridinyl derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS. | 3.23 | 1 | 0 | benzimidazoles; pyridines; sulfoxide | anti-ulcer drug; EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor |
| raloxifene raloxifene : A member of the class of 1-benzothiophenes that is 1-benzothiophene in which the hydrogens at positions 2, 3, and 6 have been replaced by p-hydroxyphenyl, p-[2-(piperidin-1-yl)ethoxy]benzoyl, and hydroxy groups, respectively. | 3.23 | 1 | 0 | 1-benzothiophenes; aromatic ketone; N-oxyethylpiperidine; phenols | bone density conservation agent; estrogen antagonist; estrogen receptor modulator |
| riluzole Riluzole: A glutamate antagonist (RECEPTORS, GLUTAMATE) used as an anticonvulsant (ANTICONVULSANTS) and to prolong the survival of patients with AMYOTROPHIC LATERAL SCLEROSIS. | 3.23 | 1 | 0 | benzothiazoles | |
| rimantadine Rimantadine: An RNA synthesis inhibitor that is used as an antiviral agent in the prophylaxis and treatment of influenza. | 3.23 | 1 | 0 | alkylamine | |
| risperidone Risperidone: A selective blocker of DOPAMINE D2 RECEPTORS and SEROTONIN 5-HT2 RECEPTORS that acts as an atypical antipsychotic agent. It has been shown to improve both positive and negative symptoms in the treatment of SCHIZOPHRENIA.. risperidone : A member of the class of pyridopyrimidines that is 2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one carrying an additional 2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl group at position 2. | 3.23 | 1 | 0 | 1,2-benzoxazoles; heteroarylpiperidine; organofluorine compound; pyridopyrimidine | alpha-adrenergic antagonist; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; H1-receptor antagonist; psychotropic drug; second generation antipsychotic; serotonergic antagonist |
| rizatriptan rizatriptan: structure given in first source; RN given refers to benzoate | 3.23 | 1 | 0 | tryptamines | anti-inflammatory drug; serotonergic agonist; vasoconstrictor agent |
| ropinirole [no description available] | 3.23 | 1 | 0 | indolones; tertiary amine | antidyskinesia agent; antiparkinson drug; central nervous system drug; dopamine agonist |
| salicylsalicylic acid salicylsalicylic acid: structure. salsalate : A dimeric benzoate ester obtained by intermolecular condensation between the carboxy of one molecule of salicylic acid with the phenol group of a second. It is a prodrug for salycylic acid that is used for treatment of rheumatoid arthritis and osteoarthritis and also shows activity against type II diabetes. | 3.23 | 1 | 0 | benzoate ester; benzoic acids; phenols; salicylates | antineoplastic agent; antirheumatic drug; EC 3.5.2.6 (beta-lactamase) inhibitor; hypoglycemic agent; non-narcotic analgesic; non-steroidal anti-inflammatory drug; prodrug |
| secobarbital Secobarbital: A barbiturate that is used as a sedative. Secobarbital is reported to have no anti-anxiety activity.. secobarbital : A member of the class of barbiturates that is barbituric acid in which the hydrogens at position 5 are substituted by prop-2-en-1-yl and pentan-2-yl groups. | 3.23 | 1 | 0 | barbiturates | anaesthesia adjuvant; GABA modulator; sedative |
| sibutramine sibutramine: serotonin and norepinephrine transporter inhibitor; Meridia is tradename for sibutramine hydrochloride | 3.23 | 1 | 0 | organochlorine compound; tertiary amino compound | anti-obesity agent; serotonin uptake inhibitor |
| sulfadiazine Sulfadiazine: One of the short-acting SULFONAMIDES used in combination with PYRIMETHAMINE to treat toxoplasmosis in patients with acquired immunodeficiency syndrome and in newborns with congenital infections.. sulfadiazine : A sulfonamide consisting of pyrimidine with a 4-aminobenzenesulfonamido group at the 2-position.. diazine : The parent structure of the diazines. | 3.23 | 1 | 0 | pyrimidines; substituted aniline; sulfonamide antibiotic; sulfonamide | antiinfective agent; antimicrobial agent; antiprotozoal drug; coccidiostat; drug allergen; EC 1.1.1.153 [sepiapterin reductase (L-erythro-7,8-dihydrobiopterin forming)] inhibitor; EC 2.5.1.15 (dihydropteroate synthase) inhibitor; environmental contaminant; xenobiotic |
| risedronic acid Risedronic Acid: A pyridine and diphosphonic acid derivative that acts as a CALCIUM CHANNEL BLOCKER and inhibits BONE RESORPTION. | 3.23 | 1 | 0 | pyridines | |
| sotalol Sotalol: An adrenergic beta-antagonist that is used in the treatment of life-threatening arrhythmias.. sotalol : A sulfonamide that is N-phenylmethanesulfonamide in which the phenyl group is substituted at position 4 by a 1-hydroxy-2-(isopropylamino)ethyl group. It has both beta-adrenoreceptor blocking (Vaughan Williams Class II) and cardiac action potential duration prolongation (Vaughan Williams Class III) antiarrhythmic properties. It is used (usually as the hydrochloride salt) for the management of ventricular and supraventricular arrhythmias. | 3.23 | 1 | 0 | ethanolamines; secondary alcohol; secondary amino compound; sulfonamide | anti-arrhythmia drug; beta-adrenergic antagonist; environmental contaminant; xenobiotic |
| imatinib [no description available] | 3.23 | 1 | 0 | aromatic amine; benzamides; N-methylpiperazine; pyridines; pyrimidines | antineoplastic agent; apoptosis inducer; tyrosine kinase inhibitor |
| vorinostat Vorinostat: A hydroxamic acid and anilide derivative that acts as a HISTONE DEACETYLASE inhibitor. It is used in the treatment of CUTANEOUS T-CELL LYMPHOMA and SEZARY SYNDROME.. vorinostat : A dicarboxylic acid diamide comprising suberic (octanedioic) acid coupled to aniline and hydroxylamine. A histone deacetylase inhibitor, it is marketed under the name Zolinza for the treatment of cutaneous T cell lymphoma (CTCL). | 3.23 | 1 | 0 | dicarboxylic acid diamide; hydroxamic acid | antineoplastic agent; apoptosis inducer; EC 3.5.1.98 (histone deacetylase) inhibitor |
| succinylcholine Succinylcholine: A quaternary skeletal muscle relaxant usually used in the form of its bromide, chloride, or iodide. It is a depolarizing relaxant, acting in about 30 seconds and with a duration of effect averaging three to five minutes. Succinylcholine is used in surgical, anesthetic, and other procedures in which a brief period of muscle relaxation is called for.. succinylcholine : A quaternary ammonium ion that is the bis-choline ester of succinic acid. | 3.23 | 1 | 0 | quaternary ammonium ion; succinate ester | drug allergen; muscle relaxant; neuromuscular agent |
| sulfamethizole Sulfamethizole: A sulfathiazole antibacterial agent.. sulfamethizole : A sulfonamide consisting of a 1,3,4-thiadiazole nucleus with a methyl substituent at C-5 and a 4-aminobenzenesulfonamido group at C-2. | 3.23 | 1 | 0 | sulfonamide antibiotic; sulfonamide; thiadiazoles | antiinfective agent; antimicrobial agent; drug allergen; EC 2.5.1.15 (dihydropteroate synthase) inhibitor |
| sulfasalazine Sulfasalazine: A drug that is used in the management of inflammatory bowel diseases. Its activity is generally considered to lie in its metabolic breakdown product, 5-aminosalicylic acid (see MESALAMINE) released in the colon. (From Martindale, The Extra Pharmacopoeia, 30th ed, p907). sulfasalazine : An azobenzene consisting of diphenyldiazene having a carboxy substituent at the 4-position, a hydroxy substituent at the 3-position and a 2-pyridylaminosulphonyl substituent at the 4'-position. | 3.23 | 1 | 0 | ||
| sulfathiazole Sulfathiazole: A sulfathiazole compound that is used as a short-acting anti-infective agent. It is no longer commonly used systemically due to its toxicity, but may still be applied topically in combination with other drugs for the treatment of vaginal and skin infections, and is still used in veterinary medicine.. sulfathiazole : A 1,3-thiazole compound having a 4-aminobenzenesulfonamido group at the 2-position. | 3.23 | 1 | 0 | 1,3-thiazoles; substituted aniline; sulfonamide antibiotic; sulfonamide | antiinfective agent; drug allergen; EC 2.5.1.15 (dihydropteroate synthase) inhibitor; environmental contaminant; xenobiotic |
| 2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol [no description available] | 3.23 | 1 | 0 | alkylbenzene | |
| sumatriptan Sumatriptan: A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of MIGRAINE DISORDERS.. sumatriptan : A sulfonamide that consists of N,N-dimethyltryptamine bearing an additional (N-methylsulfamoyl)methyl substituent at position 5. Selective agonist for a vascular 5-HT1 receptor subtype (probably a member of the 5-HT1D family). Used (in the form of its succinate salt) for the acute treatment of migraine with or without aura in adults. | 3.23 | 1 | 0 | sulfonamide; tryptamines | serotonergic agonist; vasoconstrictor agent |
| temazepam Temazepam: A benzodiazepine that acts as a GAMMA-AMINOBUTYRIC ACID modulator and anti-anxiety agent. | 3.23 | 1 | 0 | benzodiazepine | |
| temozolomide [no description available] | 3.23 | 1 | 0 | imidazotetrazine; monocarboxylic acid amide; triazene derivative | alkylating agent; antineoplastic agent; prodrug |
| terazosin Terazosin: induces decreased blood pressure; used in the treatment of benign prostatic hyperplasia | 3.23 | 1 | 0 | furans; piperazines; primary amino compound; quinazolines | alpha-adrenergic antagonist; antihypertensive agent; antineoplastic agent |
| terbutaline Terbutaline: A selective beta-2 adrenergic agonist used as a bronchodilator and tocolytic.. terbutaline : A member of the class of phenylethanolamines that is catechol substituted at position 5 by a 2-(tert-butylamino)-1-hydroxyethyl group. | 3.23 | 1 | 0 | phenylethanolamines; resorcinols | anti-asthmatic drug; beta-adrenergic agonist; bronchodilator agent; EC 3.1.1.7 (acetylcholinesterase) inhibitor; hypoglycemic agent; sympathomimetic agent; tocolytic agent |
| thalidomide Thalidomide: A piperidinyl isoindole originally introduced as a non-barbiturate hypnotic, but withdrawn from the market due to teratogenic effects. It has been reintroduced and used for a number of immunological and inflammatory disorders. Thalidomide displays immunosuppressive and anti-angiogenic activity. It inhibits release of TUMOR NECROSIS FACTOR-ALPHA from monocytes, and modulates other cytokine action.. thalidomide : A racemate comprising equimolar amounts of R- and S-thalidomide.. 2-(2,6-dioxopiperidin-3-yl)-1H-isoindole-1,3(2H)-dione : A dicarboximide that is isoindole-1,3(2H)-dione in which the hydrogen attached to the nitrogen is substituted by a 2,6-dioxopiperidin-3-yl group. | 3.23 | 1 | 0 | phthalimides; piperidones | |
| thiabendazole Tresaderm: dermatologic soln containing dexamethasone, thiabendazole & neomycin sulfate | 3.23 | 1 | 0 | 1,3-thiazoles; benzimidazole fungicide; benzimidazoles | antifungal agrochemical; antinematodal drug |
| thioridazine Thioridazine: A phenothiazine antipsychotic used in the management of PHYCOSES, including SCHIZOPHRENIA.. thioridazine : A phenothiazine derivative having a methylsulfanyl subsitituent at the 2-position and a (1-methylpiperidin-2-yl)ethyl] group at the N-10 position. | 3.23 | 1 | 0 | phenothiazines; piperidines | alpha-adrenergic antagonist; dopaminergic antagonist; EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; first generation antipsychotic; H1-receptor antagonist; serotonergic antagonist |
| thiotepa Thiotepa: A very toxic alkylating antineoplastic agent also used as an insect sterilant. It causes skin, gastrointestinal, CNS, and bone marrow damage. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), thiotepa may reasonably be anticipated to be a carcinogen (Merck Index, 11th ed). | 3.23 | 1 | 0 | aziridines | |
| ticlopidine Ticlopidine: An effective inhibitor of platelet aggregation commonly used in the placement of STENTS in CORONARY ARTERIES.. ticlopidine : A thienopyridine that is 4,5,6,7-tetrahydrothieno[3,2-c]pyridine in which the hydrogen attached to the nitrogen is replaced by an o-chlorobenzyl group. | 3.23 | 1 | 0 | monochlorobenzenes; thienopyridine | anticoagulant; fibrin modulating drug; hematologic agent; P2Y12 receptor antagonist; platelet aggregation inhibitor |
| tinidazole Tinidazole: A nitroimidazole alkylating agent that is used as an antitrichomonal agent against TRICHOMONAS VAGINALIS; ENTAMOEBA HISTOLYTICA; and GIARDIA LAMBLIA infections. It also acts as an antibacterial agent for the treatment of BACTERIAL VAGINOSIS and anaerobic bacterial infections.. tinidazole : 1H-imidazole substituted at C-1 by a (2-ethylsulfonyl)ethyl group, at C-2 by a methyl group and at C-5 by a nitro group. It is used as an antiprotozoal, antibacterial agent. | 3.23 | 1 | 0 | imidazoles | antiamoebic agent; antibacterial drug; antiparasitic agent; antiprotozoal drug |
| tiopronin Tiopronin: Sulfhydryl acylated derivative of GLYCINE. | 3.23 | 1 | 0 | N-acyl-amino acid | |
| tizanidine tizanidine: RN given refers to parent cpd; structure. tizanidine : 2,1,3-Benzothiadiazole substituted at C-4 by a Delta(1)-imidazolin-2-ylamino group and at C-4 by a chloro group. It is an agonist at alpha2-adrenergic receptor sites. | 3.23 | 1 | 0 | benzothiadiazole; imidazoles | alpha-adrenergic agonist; muscle relaxant |
| tolazamide Tolazamide: A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE.. tolazamide : An N-sulfonylurea that is 1-tosylurea in which a hydrogen attached to the nitrogen at position 3 is replaced by an azepan-1-yl group. A hypoglycemic agent, it is used for the treatment of type 2 diabetes mellitus. | 3.23 | 1 | 0 | N-sulfonylurea | hypoglycemic agent; potassium channel blocker |
| tolbutamide Tolbutamide: A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p290). tolbutamide : An N-sulfonylurea that consists of 1-butylurea having a tosyl group attached at the 3-position. | 3.23 | 1 | 0 | N-sulfonylurea | human metabolite; hypoglycemic agent; insulin secretagogue; potassium channel blocker |
| tolmetin Tolmetin: A non-steroidal anti-inflammatory agent (ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL) similar in mode of action to INDOMETHACIN.. tolmetin : A monocarboxylic acid that is (1-methylpyrrol-2-yl)acetic acid substituted at position 5 on the pyrrole ring by a 4-methylbenzoyl group. Used in the form of its sodium salt dihydrate as a nonselective nonsteroidal anti-inflammatory drug. | 3.23 | 1 | 0 | aromatic ketone; monocarboxylic acid; pyrroles | EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-steroidal anti-inflammatory drug |
| ultram 2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol : A tertiary alcohol that is cyclohexanol substituted at positions 1 and 2 by 3-methoxyphenyl and dimethylaminomethyl groups respectively. | 3.23 | 1 | 0 | aromatic ether; tertiary alcohol; tertiary amino compound | |
| tranexamic acid Tranexamic Acid: Antifibrinolytic hemostatic used in severe hemorrhage. | 3.23 | 1 | 0 | amino acid | |
| trazodone Trazodone: A serotonin uptake inhibitor that is used as an antidepressive agent. It has been shown to be effective in patients with major depressive disorders and other subsets of depressive disorders. It is generally more useful in depressive disorders associated with insomnia and anxiety. This drug does not aggravate psychotic symptoms in patients with schizophrenia or schizoaffective disorders. (From AMA Drug Evaluations Annual, 1994, p309). trazodone : An N-arylpiperazine in which one nitrogen is substituted by a 3-chlorophenyl group, while the other is substituted by a 3-(3-oxo[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)propyl group. | 3.23 | 1 | 0 | monochlorobenzenes; N-alkylpiperazine; N-arylpiperazine; triazolopyridine | adrenergic antagonist; antidepressant; anxiolytic drug; H1-receptor antagonist; sedative; serotonin uptake inhibitor |
| triamterene Triamterene: A pteridinetriamine compound that inhibits SODIUM reabsorption through SODIUM CHANNELS in renal EPITHELIAL CELLS.. triamterene : Pteridine substituted at positions 2, 4 and 7 with amino groups and at position 6 with a phenyl group. A sodium channel blocker, it is used as a diuretic in the treatment of hypertension and oedema. | 3.23 | 1 | 0 | pteridines | diuretic; sodium channel blocker |
| triazolam Triazolam: A short-acting benzodiazepine used in the treatment of insomnia. Some countries temporarily withdrew triazolam from the market because of concerns about adverse reactions, mostly psychological, associated with higher dose ranges. Its use at lower doses with appropriate care and labeling has been reaffirmed by the FDA and most other countries. | 3.23 | 1 | 0 | triazolobenzodiazepine | sedative |
| trifluoperazine [no description available] | 3.23 | 1 | 0 | N-alkylpiperazine; N-methylpiperazine; organofluorine compound; phenothiazines | antiemetic; calmodulin antagonist; dopaminergic antagonist; EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor; EC 5.3.3.5 (cholestenol Delta-isomerase) inhibitor; phenothiazine antipsychotic drug |
| trihexyphenidyl Trihexyphenidyl: One of the centrally acting MUSCARINIC ANTAGONISTS used for treatment of PARKINSONIAN DISORDERS and drug-induced extrapyramidal movement disorders and as an antispasmodic. | 3.23 | 1 | 0 | amine | |
| trimethadione Trimethadione: An anticonvulsant effective in absence seizures, but generally reserved for refractory cases because of its toxicity. (From AMA Drug Evaluations Annual, 1994, p378). trimethadione : An oxazolidinone that is 1,3-oxazolidine-2,4-dione substituted by methyl groups at positions 3, 5 and 5. It is an antiepileptic agent. | 3.23 | 1 | 0 | oxazolidinone | anticonvulsant; geroprotector |
| trimethobenzamide trimethobenzamide: major descriptor (64-84); on-line search BENZAMIDES (64-84); Index Medicus search TRIMETHOBENZAMIDE (64-84); RN given refers to parent cpd. trimethobenzamide : The amide obtained by formal condensation of 3,4,5-trihydroxybenzoic acid with 4-[2-(N,N-dimethylamino)ethoxy]benzylamine. It is used to prevent nausea and vomitting in humans. | 3.23 | 1 | 0 | benzamides; tertiary amino compound | antiemetic |
| trimethoprim Trimethoprim: A pyrimidine inhibitor of dihydrofolate reductase, it is an antibacterial related to PYRIMETHAMINE. It is potentiated by SULFONAMIDES and the TRIMETHOPRIM, SULFAMETHOXAZOLE DRUG COMBINATION is the form most often used. It is sometimes used alone as an antimalarial. TRIMETHOPRIM RESISTANCE has been reported.. trimethoprim : An aminopyrimidine antibiotic whose structure consists of pyrimidine 2,4-diamine and 1,2,3-trimethoxybenzene moieties linked by a methylene bridge. | 3.23 | 1 | 0 | aminopyrimidine; methoxybenzenes | antibacterial drug; diuretic; drug allergen; EC 1.5.1.3 (dihydrofolate reductase) inhibitor; environmental contaminant; xenobiotic |
| trimetrexate Trimetrexate: A nonclassical folic acid inhibitor through its inhibition of the enzyme dihydrofolate reductase. It is being tested for efficacy as an antineoplastic agent and as an antiparasitic agent against PNEUMOCYSTIS PNEUMONIA in AIDS patients. Myelosuppression is its dose-limiting toxic effect. | 3.23 | 1 | 0 | ||
| trimipramine Trimipramine: Tricyclic antidepressant similar to IMIPRAMINE, but with more antihistaminic and sedative properties.. trimipramine : A dibenzoazepine that is 10,11-dihydro-5H-dibenzo[b,f]azepine substituted by a 3-(dimethylamino)-2-methylpropyl group at the nitrogen atom. It is used as an antidepressant. | 3.23 | 1 | 0 | dibenzoazepine; tertiary amino compound | antidepressant; environmental contaminant; xenobiotic |
| troglitazone Troglitazone: A chroman and thiazolidinedione derivative that acts as a PEROXISOME PROLIFERATOR-ACTIVATED RECEPTORS (PPAR) agonist. It was formerly used in the treatment of TYPE 2 DIABETES MELLITUS, but has been withdrawn due to hepatotoxicity. | 3.23 | 1 | 0 | chromanes; thiazolidinone | anticoagulant; anticonvulsant; antineoplastic agent; antioxidant; EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor; ferroptosis inhibitor; hypoglycemic agent; platelet aggregation inhibitor; vasodilator agent |
| tyramine [no description available] | 3.23 | 1 | 0 | monoamine molecular messenger; primary amino compound; tyramines | EC 3.1.1.8 (cholinesterase) inhibitor; Escherichia coli metabolite; human metabolite; mouse metabolite; neurotransmitter |
| delavirdine Delavirdine: A potent, non-nucleoside reverse transcriptase inhibitor with activity specific for HIV-1.. delavirdine : The amide resulting from the formal condensation of 5-[(methylsulfonyl)amino]-1H-indole-2-carboxylic acid and 4-amino group of 1-[3-(isopropylamino)pyridin-2-yl]piperazine, delavirdine is a non-nucleoside reverse transcriptase inhibitor with activity specific for HIV-1. Viral resistance emerges rapidly when delavirdine is used alone, so it is therefore used (as the methanesulfonic acid salt) with other antiretrovirals for combination therapy of HIV infection. | 3.23 | 1 | 0 | aminopyridine; indolecarboxamide; N-acylpiperazine; sulfonamide | antiviral drug; HIV-1 reverse transcriptase inhibitor |
| venlafaxine venlafaxine : A tertiary amino compound that is N,N-dimethylethanamine substituted at position 1 by a 1-hydroxycyclohexyl and 4-methoxyphenyl group. | 3.23 | 1 | 0 | cyclohexanols; monomethoxybenzene; tertiary alcohol; tertiary amino compound | adrenergic uptake inhibitor; analgesic; antidepressant; dopamine uptake inhibitor; environmental contaminant; serotonin uptake inhibitor; xenobiotic |
| vigabatrin [no description available] | 3.23 | 1 | 0 | gamma-amino acid | anticonvulsant; EC 2.6.1.19 (4-aminobutyrate--2-oxoglutarate transaminase) inhibitor |
| ici 204,219 zafirlukast: a leukotriene D4 receptor antagonist | 3.23 | 1 | 0 | carbamate ester; indoles; N-sulfonylcarboxamide | anti-asthmatic agent; leukotriene antagonist |
| zaleplon zaleplon: an azabicyclo(4.3.0)nonane; a nonbenzodiazepine; one of the so-called of Z drugs (zopiclone, eszopiclone, zolpidem, and zaleplon) for which there is some correlation with tumors; a hypnotic with less marked effect on psychomotor functions compared to lorazepam. zaleplon : A pyrazolo[1,5-a]pyrimidine having a nitrile group at position 3 and a 3-(N-ethylacetamido)phenyl substituent at the 7-position. | 3.23 | 1 | 0 | nitrile; pyrazolopyrimidine | anticonvulsant; anxiolytic drug; central nervous system depressant; sedative |
| zolpidem Zolpidem: An imidazopyridine derivative and short-acting GABA-A receptor agonist that is used for the treatment of INSOMNIA.. zolpidem : An imidazo[1,2-a]pyridine compound having a 4-tolyl group at the 2-position, an N,N-dimethylcarbamoylmethyl group at the 3-position and a methyl substituent at the 6-position. | 3.23 | 1 | 0 | imidazopyridine | central nervous system depressant; GABA agonist; sedative |
| zonisamide Zonisamide: A benzisoxazole and sulfonamide derivative that acts as a CALCIUM CHANNEL blocker. It is used primarily as an adjunctive antiepileptic agent for the treatment of PARTIAL SEIZURES, with or without secondary generalization.. zonisamide : A 1,2-benzoxazole compound having a sulfamoylmethyl substituent at the 3-position. | 3.23 | 1 | 0 | 1,2-benzoxazoles; sulfonamide | anticonvulsant; antioxidant; central nervous system drug; protective agent; T-type calcium channel blocker |
| cortisone acetate Cortisone Acetate: The acetate ester of cortisone that is used mainly for replacement therapy in adrenocortical insufficiency and in the treatment of many allergic and inflammatory disorders. | 3.23 | 1 | 0 | corticosteroid hormone | |
| mitomycin Mitomycin: An antineoplastic antibiotic produced by Streptomyces caespitosus. It is one of the bi- or tri-functional ALKYLATING AGENTS causing cross-linking of DNA and inhibition of DNA synthesis.. mitomycin : A family of aziridine-containing natural products isolated from Streptomyces caespitosus or Streptomyces lavendulae. | 3.23 | 1 | 0 | mitomycin | alkylating agent; antineoplastic agent |
| prednisolone Prednisolone: A glucocorticoid with the general properties of the corticosteroids. It is the drug of choice for all conditions in which routine systemic corticosteroid therapy is indicated, except adrenal deficiency states.. prednisolone : A glucocorticoid that is prednisone in which the oxo group at position 11 has been reduced to the corresponding beta-hydroxy group. It is a drug metabolite of prednisone. | 3.23 | 1 | 0 | 11beta-hydroxy steroid; 17alpha-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; C21-steroid; glucocorticoid; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone | adrenergic agent; anti-inflammatory drug; antineoplastic agent; drug metabolite; environmental contaminant; immunosuppressive agent; xenobiotic |
| reserpine Reserpine: An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. Reserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It has been used as an antihypertensive and an antipsychotic as well as a research tool, but its adverse effects limit its clinical use.. reserpine : An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. | 3.23 | 1 | 0 | alkaloid ester; methyl ester; yohimban alkaloid | adrenergic uptake inhibitor; antihypertensive agent; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; environmental contaminant; first generation antipsychotic; plant metabolite; xenobiotic |
| phentolamine Phentolamine: A nonselective alpha-adrenergic antagonist. It is used in the treatment of hypertension and hypertensive emergencies, pheochromocytoma, vasospasm of RAYNAUD DISEASE and frostbite, clonidine withdrawal syndrome, impotence, and peripheral vascular disease.. phentolamine : A substituted aniline that is 3-aminophenol in which the hydrogens of the amino group are replaced by 4-methylphenyl and 4,5-dihydro-1H-imidazol-2-ylmethyl groups respectively. An alpha-adrenergic antagonist, it is used for the treatment of hypertension. | 3.23 | 1 | 0 | imidazoles; phenols; substituted aniline; tertiary amino compound | alpha-adrenergic antagonist; vasodilator agent |
| sorbitol D-glucitol : The D-enantiomer of glucitol (also known as D-sorbitol). | 3.23 | 1 | 0 | glucitol | cathartic; Escherichia coli metabolite; food humectant; human metabolite; laxative; metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite; sweetening agent |
| thyroxine Thyroxine: The major hormone derived from the thyroid gland. Thyroxine is synthesized via the iodination of tyrosines (MONOIODOTYROSINE) and the coupling of iodotyrosines (DIIODOTYROSINE) in the THYROGLOBULIN. Thyroxine is released from thyroglobulin by proteolysis and secreted into the blood. Thyroxine is peripherally deiodinated to form TRIIODOTHYRONINE which exerts a broad spectrum of stimulatory effects on cell metabolism.. thyroxine : An iodothyronine compound having iodo substituents at the 3-, 3'-, 5- and 5'-positions. | 3.23 | 1 | 0 | 2-halophenol; iodophenol; L-phenylalanine derivative; non-proteinogenic L-alpha-amino acid; thyroxine zwitterion; thyroxine | antithyroid drug; human metabolite; mouse metabolite; thyroid hormone |
| dextroamphetamine Dextroamphetamine: The d-form of AMPHETAMINE. It is a central nervous system stimulant and a sympathomimetic. It has also been used in the treatment of narcolepsy and of attention deficit disorders and hyperactivity in children. Dextroamphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulating release of monamines, and inhibiting monoamine oxidase. It is also a drug of abuse and a psychotomimetic.. (S)-amphetamine : A 1-phenylpropan-2-amine that has S configuration. | 3.23 | 1 | 0 | 1-phenylpropan-2-amine | adrenergic agent; adrenergic uptake inhibitor; dopamine uptake inhibitor; dopaminergic agent; neurotoxin; sympathomimetic agent |
| spironolactone Spironolactone: A potassium sparing diuretic that acts by antagonism of aldosterone in the distal renal tubules. It is used mainly in the treatment of refractory edema in patients with congestive heart failure, nephrotic syndrome, or hepatic cirrhosis. Its effects on the endocrine system are utilized in the treatments of hirsutism and acne but they can lead to adverse effects. (From Martindale, The Extra Pharmacopoeia, 30th ed, p827). spironolactone : A steroid lactone that is 17alpha-pregn-4-ene-21,17-carbolactone substituted by an oxo group at position 3 and an alpha-acetylsulfanyl group at position 7. | 3.23 | 1 | 0 | 3-oxo-Delta(4) steroid; oxaspiro compound; steroid lactone; thioester | aldosterone antagonist; antihypertensive agent; diuretic; environmental contaminant; xenobiotic |
| penicillamine Penicillamine: 3-Mercapto-D-valine. The most characteristic degradation product of the penicillin antibiotics. It is used as an antirheumatic and as a chelating agent in Wilson's disease.. penicillamine : An alpha-amino acid having the structure of valine substituted at the beta position with a sulfanyl group. | 3.23 | 1 | 0 | non-proteinogenic alpha-amino acid; penicillamine | antirheumatic drug; chelator; copper chelator; drug allergen |
| cysteine [no description available] | 3.23 | 1 | 0 | cysteine zwitterion; cysteine; L-alpha-amino acid; proteinogenic amino acid; serine family amino acid | EC 4.3.1.3 (histidine ammonia-lyase) inhibitor; flour treatment agent; human metabolite |
| prednisone Prednisone: A synthetic anti-inflammatory glucocorticoid derived from CORTISONE. It is biologically inert and converted to PREDNISOLONE in the liver.. prednisone : A synthetic glucocorticoid drug that is particularly effective as an immunosuppressant, and affects virtually all of the immune system. Prednisone is a prodrug that is converted by the liver into prednisolone (a beta-hydroxy group instead of the oxo group at position 11), which is the active drug and also a steroid. | 3.23 | 1 | 0 | 11-oxo steroid; 17alpha-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; C21-steroid; glucocorticoid; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone | adrenergic agent; anti-inflammatory drug; antineoplastic agent; immunosuppressive agent; prodrug |
| estrone Hydroxyestrones: Estrone derivatives substituted with one or more hydroxyl groups in any position. They are important metabolites of estrone and other estrogens. | 3.23 | 1 | 0 | 17-oxo steroid; 3-hydroxy steroid; phenolic steroid; phenols | antineoplastic agent; bone density conservation agent; estrogen; human metabolite; mouse metabolite |
| oxandrolone Oxandrolone: A synthetic hormone with anabolic and androgenic properties. | 3.23 | 1 | 0 | 17beta-hydroxy steroid; 3-oxo steroid; anabolic androgenic steroid; oxa-steroid | anabolic agent; androgen |
| penicillin g Penicillin G: A penicillin derivative commonly used in the form of its sodium or potassium salts in the treatment of a variety of infections. It is effective against most gram-positive bacteria and against gram-negative cocci. It has also been used as an experimental convulsant because of its actions on GAMMA-AMINOBUTYRIC ACID mediated synaptic transmission.. benzylpenicillin : A penicillin in which the substituent at position 6 of the penam ring is a phenylacetamido group. | 3.23 | 1 | 0 | penicillin allergen; penicillin | antibacterial drug; drug allergen; epitope |
| pilocarpine Pilocarpine: A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma.. (+)-pilocarpine : The (+)-enantiomer of pilocarpine. | 3.23 | 1 | 0 | pilocarpine | antiglaucoma drug |
| triiodothyronine Triiodothyronine: A T3 thyroid hormone normally synthesized and secreted by the thyroid gland in much smaller quantities than thyroxine (T4). Most T3 is derived from peripheral monodeiodination of T4 at the 5' position of the outer ring of the iodothyronine nucleus. The hormone finally delivered and used by the tissues is mainly T3.. 3,3',5-triiodo-L-thyronine : An iodothyronine compound having iodo substituents at the 3-, 3'- and 5-positions. Although some is produced in the thyroid, most of the 3,3',5-triiodo-L-thyronine in the body is generated by mono-deiodination of L-thyroxine in the peripheral tissues. Its metabolic activity is about 3 to 5 times that of L-thyroxine. The sodium salt is used in the treatment of hypothyroidism. | 3.23 | 1 | 0 | 2-halophenol; amino acid zwitterion; iodophenol; iodothyronine | human metabolite; mouse metabolite; thyroid hormone |
| chloramphenicol Amphenicol: Chloramphenicol and its derivatives. | 3.23 | 1 | 0 | C-nitro compound; carboxamide; diol; organochlorine compound | antibacterial drug; antimicrobial agent; Escherichia coli metabolite; geroprotector; Mycoplasma genitalium metabolite; protein synthesis inhibitor |
| glutamine Glutamine: A non-essential amino acid present abundantly throughout the body and is involved in many metabolic processes. It is synthesized from GLUTAMIC ACID and AMMONIA. It is the principal carrier of NITROGEN in the body and is an important energy source for many cells.. L-glutamine : An optically active form of glutamine having L-configuration.. glutamine : An alpha-amino acid that consists of butyric acid bearing an amino substituent at position 2 and a carbamoyl substituent at position 4. | 3.23 | 1 | 0 | amino acid zwitterion; glutamine family amino acid; glutamine; L-alpha-amino acid; polar amino acid zwitterion; proteinogenic amino acid | EC 1.14.13.39 (nitric oxide synthase) inhibitor; Escherichia coli metabolite; human metabolite; metabolite; micronutrient; mouse metabolite; nutraceutical; Saccharomyces cerevisiae metabolite |
| vincristine [no description available] | 3.23 | 1 | 0 | acetate ester; formamides; methyl ester; organic heteropentacyclic compound; organic heterotetracyclic compound; tertiary alcohol; tertiary amino compound; vinca alkaloid | antineoplastic agent; drug; microtubule-destabilising agent; plant metabolite; tubulin modulator |
| physostigmine Physostigmine: A cholinesterase inhibitor that is rapidly absorbed through membranes. It can be applied topically to the conjunctiva. It also can cross the blood-brain barrier and is used when central nervous system effects are desired, as in the treatment of severe anticholinergic toxicity. | 3.23 | 1 | 0 | carbamate ester; indole alkaloid | antidote to curare poisoning; EC 3.1.1.8 (cholinesterase) inhibitor; miotic |
| apomorphine Apomorphine: A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use. | 3.23 | 1 | 0 | aporphine alkaloid | alpha-adrenergic drug; antidyskinesia agent; antiparkinson drug; dopamine agonist; emetic; serotonergic drug |
| methyltestosterone Methyltestosterone: A synthetic hormone used for androgen replacement therapy and as an hormonal antineoplastic agent (ANTINEOPLASTIC AGENTS, HORMONAL).. methyltestosterone : A 17beta-hydroxy steroid that is testosterone bearing a methyl group at the 17alpha position. | 3.23 | 1 | 0 | 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; enone | anabolic agent; androgen; antineoplastic agent |
| tetrabenazine 9,10-dimethoxy-3-isobutyl-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-one : A benzoquinolizine that is 1,2,3,4,4a,9,10,10a-octahydrophenanthrene in which the carbon at position 10a is replaced by a nitrogen and which is substituted by an isobutyl group at position 2, an oxo group at position 3, and methoxy groups at positions 6 and 7. | 3.23 | 1 | 0 | benzoquinolizine; cyclic ketone; tertiary amino compound | |
| kanamycin a Kanamycin: Antibiotic complex produced by Streptomyces kanamyceticus from Japanese soil. Comprises 3 components: kanamycin A, the major component, and kanamycins B and C, the minor components.. kanamycin : Kanamycin is a naturally occurring antibiotic complex from Streptomyces kanamyceticus that consists of several components: kanamycin A, the major component (also usually designated as kanamycin), and kanamycins B, C, D and X the minor components. | 3.23 | 1 | 0 | kanamycins | bacterial metabolite |
| edetic acid Edetic Acid: A chelating agent that sequesters a variety of polyvalent cations such as CALCIUM. It is used in pharmaceutical manufacturing and as a food additive. | 3.23 | 1 | 0 | ethylenediamine derivative; polyamino carboxylic acid; tetracarboxylic acid | anticoagulant; antidote; chelator; copper chelator; geroprotector |
| cysteamine Cysteamine: A mercaptoethylamine compound that is endogenously derived from the COENZYME A degradative pathway. The fact that cysteamine is readily transported into LYSOSOMES where it reacts with CYSTINE to form cysteine-cysteamine disulfide and CYSTEINE has led to its use in CYSTINE DEPLETING AGENTS for the treatment of CYSTINOSIS.. cysteamine : An amine that consists of an ethane skeleton substituted with a thiol group at C-1 and an amino group at C-2. | 3.23 | 1 | 0 | amine; thiol | geroprotector; human metabolite; mouse metabolite; radiation protective agent |
| acetylcholine chloride acetylcholine chloride : The chloride salt of acetylcholine, and a parasympatomimetic drug. | 3.23 | 1 | 0 | quaternary ammonium salt | |
| mepazine mepazine: major descriptor (66-85); on-line search PHENOTHIAZINES (66-85); Index Medicus search MEPAZINE (66-85); RN given refers to parent cpd. pacatal : A phenothiazine derivative in which 10H-phenothiazine has an N-methylpiperidin-4-ylmethyl substituent at the N-10 position. | 3.23 | 1 | 0 | phenothiazines | |
| cloxacillin Cloxacillin: A semi-synthetic antibiotic that is a chlorinated derivative of OXACILLIN.. cloxacillin : A semisynthetic penicillin antibiotic carrying a 3-(2-chlorophenyl)-5-methylisoxazole-4-carboxamido group at position 6. | 3.23 | 1 | 0 | penicillin allergen; penicillin; semisynthetic derivative | antibacterial agent; antibacterial drug |
| calcium acetate calcium acetate: a principal compound used as phosphate binders in patients with chronic renal failure; used like sevelamer. calcium acetate : The calcium salt of acetic acid. It is used, commonly as a hydrate, to treat hyperphosphataemia (excess phosphate in the blood) in patients with kidney disease: the calcium ion combines with dietary phosphate to form (insoluble) calcium phosphate, which is excreted in the faeces. | 3.23 | 1 | 0 | calcium salt | chelator |
| methionine Methionine: A sulfur-containing essential L-amino acid that is important in many body functions.. methionine : A sulfur-containing amino acid that is butyric acid bearing an amino substituent at position 2 and a methylthio substituent at position 4. | 3.23 | 1 | 0 | aspartate family amino acid; L-alpha-amino acid; methionine zwitterion; methionine; proteinogenic amino acid | antidote to paracetamol poisoning; human metabolite; micronutrient; mouse metabolite; nutraceutical |
| colchicine (S)-colchicine : A colchicine that has (S)-configuration. It is a secondary metabolite, has anti-inflammatory properties and is used to treat gout, crystal-induced joint inflammation, familial Mediterranean fever, and many other conditions. | 3.23 | 1 | 0 | alkaloid; colchicine | anti-inflammatory agent; gout suppressant; mutagen |
| mebanazine mebanazine: RN given refers to parent cpd without isomeric designation; structure | 3.23 | 1 | 0 | benzenes | |
| oxacillin Oxacillin: An antibiotic similar to FLUCLOXACILLIN used in resistant staphylococci infections.. oxacillin : A penicillin antibiotic carrying a 5-methyl-3-phenylisoxazole-4-carboxamide group at position 6beta. | 3.23 | 1 | 0 | penicillin | antibacterial agent; antibacterial drug |
| cycloserine Cycloserine: Antibiotic substance produced by Streptomyces garyphalus.. D-cycloserine : A 4-amino-1,2-oxazolidin-3-one that has R configuration. It is an antibiotic produced by Streptomyces garyphalus or S. orchidaceus and is used as part of a multi-drug regimen for the treatment of tuberculosis when resistance to, or toxicity from, primary drugs has developed. An analogue of D-alanine, it interferes with bacterial cell wall synthesis in the cytoplasm by competitive inhibition of L-alanine racemase (which forms D-alanine from L-alanine) and D-alanine--D-alanine ligase (which incorporates D-alanine into the pentapeptide required for peptidoglycan formation and bacterial cell wall synthesis). | 3.23 | 1 | 0 | 4-amino-1,2-oxazolidin-3-one; organonitrogen heterocyclic antibiotic; organooxygen heterocyclic antibiotic; zwitterion | antiinfective agent; antimetabolite; antitubercular agent; metabolite; NMDA receptor agonist |
| benziodarone benziodarone: minor descriptor (75-89); on-line & INDEX MEDICUS search BENZOFURANS (68-89) & IODOBENZOATES (74) | 3.23 | 1 | 0 | aromatic ketone | |
| ampicillin Ampicillin: Semi-synthetic derivative of penicillin that functions as an orally active broad-spectrum antibiotic.. ampicillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-amino-2-phenylacetamido group. | 3.23 | 1 | 0 | beta-lactam antibiotic; penicillin allergen; penicillin | antibacterial drug |
| mannitol [no description available] | 3.23 | 1 | 0 | mannitol | allergen; antiglaucoma drug; compatible osmolytes; Escherichia coli metabolite; food anticaking agent; food bulking agent; food humectant; food stabiliser; food thickening agent; hapten; metabolite; osmotic diuretic; sweetening agent |
| cytarabine [no description available] | 3.23 | 1 | 0 | beta-D-arabinoside; monosaccharide derivative; pyrimidine nucleoside | antimetabolite; antineoplastic agent; antiviral agent; immunosuppressive agent |
| arginine Arginine: An essential amino acid that is physiologically active in the L-form.. arginine : An alpha-amino acid that is glycine in which the alpha-is substituted by a 3-guanidinopropyl group. | 3.23 | 1 | 0 | arginine; glutamine family amino acid; L-alpha-amino acid; proteinogenic amino acid | biomarker; Escherichia coli metabolite; micronutrient; mouse metabolite; nutraceutical |
| perflutren Definity: a fluorocarbon-filled ultrasonic contrast agent; Definity is tradename. octafluoropropane : A fluorocarbon that is propane in which all of the hydrogens have been replaced by fluorines. | 3.23 | 1 | 0 | fluoroalkane; fluorocarbon | |
| fluoxymesterone Fluoxymesterone: An anabolic steroid that has been used in the treatment of male HYPOGONADISM, delayed puberty in males, and in the treatment of breast neoplasms in women. | 3.23 | 1 | 0 | 11beta-hydroxy steroid; 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; anabolic androgenic steroid; fluorinated steroid | anabolic agent; antineoplastic agent |
| methsuximide methsuximide: anticonvulsant effective in petit mal & psychomotor epilepsy; has a number of unpleasant & toxic side effects; minor descriptor (75-86); on-line & INDEX MEDICUS search SUCCINIMIDES (75-86); RN given refers to parent cpd without isomeric designation | 3.23 | 1 | 0 | organic molecular entity | |
| tromethamine Tromethamine: An organic amine proton acceptor. It is used in the synthesis of surface-active agents and pharmaceuticals; as an emulsifying agent for cosmetic creams and lotions, mineral oil and paraffin wax emulsions, as a biological buffer, and used as an alkalizer. (From Merck, 11th ed; Martindale, The Extra Pharmacopoeia, 30th ed, p1424) | 3.23 | 1 | 0 | primary amino compound; triol | buffer |
| methylprednisolone Methylprednisolone: A PREDNISOLONE derivative with similar anti-inflammatory action.. 6alpha-methylprednisolone : The 6alpha-stereoisomer of 6-methylprednisolone. | 3.23 | 1 | 0 | 6-methylprednisolone; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone | adrenergic agent; anti-inflammatory drug; antiemetic; environmental contaminant; neuroprotective agent; xenobiotic |
| brompheniramine Brompheniramine: Histamine H1 antagonist used in treatment of allergies, rhinitis, and urticaria.. brompheniramine : Pheniramine in which the hydrogen at position 4 of the phenyl substituent is substituted by bromine. A histamine H1 receptor antagonist, brompheniramine is used (commonly as its maleate salt) for the symptomatic relief of allergic conditions, including rhinitis and conjunctivitis. | 3.23 | 1 | 0 | organobromine compound; pyridines | anti-allergic agent; H1-receptor antagonist |
| penicillin v Penicillin V: A broad-spectrum penicillin antibiotic used orally in the treatment of mild to moderate infections by susceptible gram-positive organisms.. phenoxymethylpenicillin : A penicillin compound having a 6beta-(phenoxyacetyl)amino side-chain. | 3.23 | 1 | 0 | penicillin allergen; penicillin | |
| isosorbide dinitrate Isosorbide Dinitrate: A vasodilator used in the treatment of ANGINA PECTORIS. Its actions are similar to NITROGLYCERIN but with a slower onset of action. | 3.23 | 1 | 0 | glucitol derivative; nitrate ester | nitric oxide donor; vasodilator agent |
| pseudoephedrine Pseudoephedrine: A phenethylamine that is an isomer of EPHEDRINE which has less central nervous system effects and usage is mainly for respiratory tract decongestion.. pseudoephedrine : A member of the class of the class of phenylethanolamines that is (1S)-2-(methylamino)-1-phenylethan-1-ol in which the pro-S hydrogen at position 2 is replaced by a methyl group. | 3.23 | 1 | 0 | phenylethanolamines; secondary alcohol; secondary amino compound | anti-asthmatic drug; bronchodilator agent; central nervous system drug; nasal decongestant; plant metabolite; sympathomimetic agent; vasoconstrictor agent; xenobiotic |
| diethylpropion Diethylpropion: A appetite depressant considered to produce less central nervous system disturbance than most drugs in this therapeutic category. It is also considered to be among the safest for patients with hypertension. (From AMA Drug Evaluations Annual, 1994, p2290). diethylpropion : An aromatic ketone that is propiophenone in which one of the hydrogens alpha- to the carbonyl is substituted by a diethylamino group. A central stimulant and indirect-acting sympathomimetic, it is an appetite depressant and is used as the hydrochloride as an anoretic in the short term management of obesity. | 3.23 | 1 | 0 | aromatic ketone; tertiary amine | appetite depressant |
| quinuclidines Quinuclidines: A class of organic compounds which contain two rings that share a pair of bridgehead carbon atoms and contains an amine group. | 8.16 | 10 | 1 | quinuclidines; saturated organic heterobicyclic parent | |
| benzonatate benzonatate: structure in Merck Index, 9th ed, #1107. benzonatate : The ester obtained by formal condensation of 4-butylaminobenzoic acid with nonaethylene glycol monomethyl ether. Structurally related to procaine and benzocaine, it has an anaesthetic effect on the stretch sensors in the lungs, and is used as a non-narcotic cough suppressant. | 3.23 | 1 | 0 | benzoate ester; secondary amino compound; substituted aniline | anaesthetic; antitussive |
| methylergonovine Methylergonovine: A homolog of ERGONOVINE containing one more CH2 group. (Merck Index, 11th ed) | 3.23 | 1 | 0 | ergoline alkaloid | |
| cinchophen cinchophen: was heading 1963-94; ACIPHENOCHINOLIUM was see CHINOPHEN 1978-94; use QUINOLINES to search CINCHOPHEN 1966-94 | 3.23 | 1 | 0 | quinolines | |
| nafcillin Nafcillin: A semi-synthetic antibiotic related to penicillin.. nafcillin : A penicillin in which the substituent at position 6 of the penam ring is a (2-ethoxy-1-naphthoyl)amino group. | 3.23 | 1 | 0 | penicillin allergen; penicillin | antibacterial drug |
| methohexital Methohexital: An intravenous anesthetic with a short duration of action that may be used for induction of anesthesia.. methohexital : A barbiturate, the structure of which is that of barbituric acid substituted at N-1 by a methyl group and at C-5 by allyl and 1-methylpent-2-ynyl groups. | 3.23 | 1 | 0 | acetylenic compound; barbiturates | drug allergen; intravenous anaesthetic |
| thiazoles [no description available] | 8.84 | 17 | 2 | 1,3-thiazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene | |
| ephedrine Ephedrine: A phenethylamine found in EPHEDRA SINICA. PSEUDOEPHEDRINE is an isomer. It is an alpha- and beta-adrenergic agonist that may also enhance release of norepinephrine. It has been used for asthma, heart failure, rhinitis, and urinary incontinence, and for its central nervous system stimulatory effects in the treatment of narcolepsy and depression. It has become less extensively used with the advent of more selective agonists.. (-)-ephedrine : A phenethylamine alkaloid that is 2-phenylethanamine substituted by a methyl group at the amino nitrogen and a methyl and a hydroxy group at position 2 and 1 respectively. | 3.23 | 1 | 0 | phenethylamine alkaloid; phenylethanolamines | bacterial metabolite; environmental contaminant; nasal decongestant; plant metabolite; sympathomimetic agent; vasoconstrictor agent; xenobiotic |
| aminophylline Aminophylline: A drug combination that contains THEOPHYLLINE and ethylenediamine. It is more soluble in water than theophylline but has similar pharmacologic actions. It's most common use is in bronchial asthma, but it has been investigated for several other applications.. aminophylline : A mixture comprising of theophylline and ethylenediamine in a 2:1 ratio. | 3.23 | 1 | 0 | mixture | bronchodilator agent; cardiotonic drug |
| azacitidine Azacitidine: A pyrimidine analogue that inhibits DNA methyltransferase, impairing DNA methylation. It is also an antimetabolite of cytidine, incorporated primarily into RNA. Azacytidine has been used as an antineoplastic agent.. 5-azacytidine : An N-glycosyl-1,3,5-triazine that is 4-amino-1,3,5-triazin-2(1H)-one substituted by a beta-D-ribofuranosyl residue via an N-glycosidic linkage. An antineoplastic agent, it is used in the treatment of myeloid leukaemia. | 3.23 | 1 | 0 | N-glycosyl-1,3,5-triazine; nucleoside analogue | antineoplastic agent |
| galantamine Galantamine: A benzazepine derived from norbelladine. It is found in GALANTHUS and other AMARYLLIDACEAE. It is a cholinesterase inhibitor that has been used to reverse the muscular effects of GALLAMINE TRIETHIODIDE and TUBOCURARINE and has been studied as a treatment for ALZHEIMER DISEASE and other central nervous system disorders.. galanthamine : A benzazepine alkaloid isolated from certain species of daffodils. | 3.23 | 1 | 0 | benzazepine alkaloid fundamental parent; benzazepine alkaloid; organic heterotetracyclic compound; tertiary amino compound | antidote to curare poisoning; cholinergic drug; EC 3.1.1.7 (acetylcholinesterase) inhibitor; EC 3.1.1.8 (cholinesterase) inhibitor; plant metabolite |
| nandrolone decanoate Nandrolone Decanoate: Decanoic acid ester of nandrolone that is used as an anabolic agent to prevent or treat WASTING SYNDROME associated with severe chronic illness or HIV infection (HIV WASTING SYNDROME). It may also be used in the treatment of POSTMENOPAUSAL OSTEOPOROSIS. | 3.23 | 1 | 0 | steroid ester | |
| dextropropoxyphene Dextropropoxyphene: A narcotic analgesic structurally related to METHADONE. Only the dextro-isomer has an analgesic effect; the levo-isomer appears to exert an antitussive effect.. propoxyphene : A racemate of the (1R,2R)- and (1S,2R)- diastereoisomers.. dextropropoxyphene : The (1S,2R)-(+)-diastereoisomer of propoxyphene. | 3.23 | 1 | 0 | 1-benzyl-3-(dimethylamino)-2-methyl-1-phenylpropyl propanoate | mu-opioid receptor agonist; opioid analgesic |
| chenodeoxycholic acid Chenodeoxycholic Acid: A bile acid, usually conjugated with either glycine or taurine. It acts as a detergent to solubilize fats for intestinal absorption and is reabsorbed by the small intestine. It is used as cholagogue, a choleretic laxative, and to prevent or dissolve gallstones.. chenodeoxycholic acid : A dihydroxy-5beta-cholanic acid that is (5beta)-cholan-24-oic acid substituted by hydroxy groups at positions 3 and 7 respectively.. chenodeoxycholate : Conjugate base of chenodeoxycholic acid; major species at pH 7.3. | 3.23 | 1 | 0 | bile acid; C24-steroid; dihydroxy-5beta-cholanic acid | human metabolite; mouse metabolite |
| phenylpropanolamine 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.. 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.. (-)-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. | 12.02 | 28 | 9 | amphetamines; phenethylamine alkaloid | plant metabolite |
| 4-hydroxybutyric acid 4-hydroxybutyric acid: was an entry term to Sodium Oxybate (74-98). 4-hydroxybutyric acid : A 4-hydroxy monocarboxylic acid that is butyric acid in which one of the hydrogens at position 4 is replaced by a hydroxy group. | 3.23 | 1 | 0 | 4-hydroxy monocarboxylic acid; hydroxybutyric acid | general anaesthetic; GHB receptor agonist; neurotoxin; sedative |
| dihydroergotamine Dihydroergotamine: A 9,10alpha-dihydro derivative of ERGOTAMINE. It is used as a vasoconstrictor, specifically for the therapy of MIGRAINE DISORDERS.. dihydroergotamine : Ergotamine in which a single bond replaces the double bond between positions 9 and 10. A semisynthetic ergot alkaloid with weaker oxytocic and vasoconstrictor properties than ergotamine, it is used (as the methanesulfonic or tartaric acid salts) for the treatment of migraine and orthostatic hypotension. | 3.23 | 1 | 0 | ergot alkaloid; semisynthetic derivative | dopamine agonist; non-narcotic analgesic; serotonergic agonist; sympatholytic agent; vasoconstrictor agent |
| medroxyprogesterone [no description available] | 3.23 | 1 | 0 | 17alpha-hydroxy steroid; 20-oxo steroid; 3-oxo-Delta(4) steroid; tertiary alpha-hydroxy ketone | contraceptive drug; progestin; synthetic oral contraceptive |
| dimenhydrinate gravinol: has antioxidant and ant-inflammatory activities; structure in first source | 3.23 | 1 | 0 | diarylmethane | |
| methamphetamine Methamphetamine: A central nervous system stimulant and sympathomimetic with actions and uses similar to DEXTROAMPHETAMINE. The smokable form is a drug of abuse and is referred to as crank, crystal, crystal meth, ice, and speed.. methamphetamine : A member of the class of amphetamines in which the amino group of (S)-amphetamine carries a methyl substituent. | 3.23 | 1 | 0 | amphetamines; secondary amine | central nervous system stimulant; environmental contaminant; neurotoxin; psychotropic drug; xenobiotic |
| levocarnitine (R)-carnitine : The (R)-enantiomer of carnitine. | 3.23 | 1 | 0 | carnitine | antilipemic drug; nootropic agent; nutraceutical; Saccharomyces cerevisiae metabolite; water-soluble vitamin (role) |
| sulfanilylurea sulfanilylurea: antimicrobial agent; structure | 3.23 | 1 | 0 | benzenes; sulfonamide | |
| lactulose [no description available] | 3.23 | 1 | 0 | glycosylfructose | gastrointestinal drug; laxative |
| pamabrom [no description available] | 3.23 | 1 | 0 | ||
| acetylcysteine N-acetyl-L-cysteine : An N-acetyl-L-amino acid that is the N-acetylated derivative of the natural amino acid L-cysteine. | 3.23 | 1 | 0 | acetylcysteine; L-cysteine derivative; N-acetyl-L-amino acid | antidote to paracetamol poisoning; antiinfective agent; antioxidant; antiviral drug; ferroptosis inhibitor; geroprotector; human metabolite; mucolytic; radical scavenger; vulnerary |
| erythromycin Erythromycin: A bacteriostatic antibiotic macrolide produced by Streptomyces erythreus. Erythromycin A is considered its major active component. In sensitive organisms, it inhibits protein synthesis by binding to 50S ribosomal subunits. This binding process inhibits peptidyl transferase activity and interferes with translocation of amino acids during translation and assembly of proteins.. erythromycin : Any of several wide-spectrum macrolide antibiotics obtained from actinomycete Saccharopolyspora erythraea (formerly known as Streptomyces erythraeus).. erythromycin A : An erythromycin that consists of erythronolide A having 2,6-dideoxy-3-C-methyl-3-O-methyl-alpha-L-ribo-hexopyranosyl and 3,4,6-trideoxy-3-(dimethylamino)-beta-D-xylo-hexopyranosyl residues attahced at positions 4 and 6 respectively. | 3.23 | 1 | 0 | cyclic ketone; erythromycin | |
| levonorgestrel Levonorgestrel: A synthetic progestational hormone with actions similar to those of PROGESTERONE and about twice as potent as its racemic or (+-)-isomer (NORGESTREL). It is used for contraception, control of menstrual disorders, and treatment of endometriosis. | 3.23 | 1 | 0 | 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; terminal acetylenic compound | contraceptive drug; female contraceptive drug; progestin; synthetic oral contraceptive |
| diphenoxylate Diphenoxylate: A MEPERIDINE congener used as an antidiarrheal, usually in combination with ATROPINE. At high doses, it acts like morphine. Its unesterified metabolite difenoxin has similar properties and is used similarly. It has little or no analgesic activity.. diphenoxylate : A piperidinecarboxylate ester that is the ethyl ester of difenoxin. | 3.23 | 1 | 0 | ethyl ester; nitrile; piperidinecarboxylate ester; tertiary amine | antidiarrhoeal drug |
| ethambutol Ethambutol: An antitubercular agent that inhibits the transfer of mycolic acids into the cell wall of the tubercle bacillus. It may also inhibit the synthesis of spermidine in mycobacteria. The action is usually bactericidal, and the drug can penetrate human cell membranes to exert its lethal effect. (From Smith and Reynard, Textbook of Pharmacology, 1992, p863). ethambutol : An ethylenediamine derivative that is ethane-1,2-diamine in which one hydrogen attached to each of the nitrogens is sutstituted by a 1-hydroxybutan-2-yl group (S,S-configuration). It is a bacteriostatic antimycobacterial drug, effective against Mycobacterium tuberculosis and some other mycobacteria. It is used (as the dihydrochloride salt) in combination with other antituberculous drugs in the treatment of pulmonary and extrapulmonary tuberculosis; resistant strains of M. tuberculosis are readily produced if ethambutol is used alone. | 3.23 | 1 | 0 | ethanolamines; ethylenediamine derivative | antitubercular agent; environmental contaminant; xenobiotic |
| vancomycin Vancomycin: Antibacterial obtained from Streptomyces orientalis. It is a glycopeptide related to RISTOCETIN that inhibits bacterial cell wall assembly and is toxic to kidneys and the inner ear.. vancomycin : A complex glycopeptide from Streptomyces orientalis. It inhibits a specific step in the synthesis of the peptidoglycan layer in the Gram-positive bacteria Staphylococcus aureus and Clostridium difficile. | 3.23 | 1 | 0 | glycopeptide | antibacterial drug; antimicrobial agent; bacterial metabolite |
| d-alpha tocopherol Vitamin E: A generic descriptor for all TOCOPHEROLS and TOCOTRIENOLS that exhibit ALPHA-TOCOPHEROL activity. By virtue of the phenolic hydrogen on the 2H-1-benzopyran-6-ol nucleus, these compounds exhibit varying degree of antioxidant activity, depending on the site and number of methyl groups and the type of ISOPRENOIDS.. tocopherol : A collective name for a group of closely related lipids that contain a chroman-6-ol nucleus substituted at position 2 by a methyl group and by a saturated hydrocarbon chain consisting of three isoprenoid units. They are designated as alpha-, beta-, gamma-, and delta-tocopherol depending on the number and position of additional methyl substituents on the aromatic ring. Tocopherols occur in vegetable oils and vegetable oil products, almost exclusively with R,R,R configuration. Tocotrienols differ from tocopherols only in having three double bonds in the hydrocarbon chain.. vitamin E : Any member of a group of fat-soluble chromanols that exhibit biological activity against vitamin E deficiency. The vitamers in this class consists of a chroman-6-ol core which is substituted at position 2 by a methyl group and (also at position 2) either a saturated or a triply-unsaturated hydrocarbon chain consisting of three isoprenoid units. The major function of vitamin E is to act as a natural antioxidant by scavenging free radicals and molecular oxygen.. (R,R,R)-alpha-tocopherol : An alpha-tocopherol that has R,R,R configuration. The naturally occurring stereoisomer of alpha-tocopherol, it is found particularly in sunflower and olive oils. | 3.23 | 1 | 0 | alpha-tocopherol | algal metabolite; antiatherogenic agent; anticoagulant; antioxidant; antiviral agent; EC 2.7.11.13 (protein kinase C) inhibitor; immunomodulator; micronutrient; nutraceutical; plant metabolite |
| ibufenac ibufenac: used in the treatment of rheumatism; also possesses antipyretic properties; minor descriptor (75-84); on-line & Index Medicus search PHENYLACETATES (75-84); RN given refers to parent cpd. ibufenac : A monocarboxylic acid that is acetic acid in which one of the methyl hydrogens is replaced by a 4-isobutylphenyl group. Although it was shown to be effective in treatment of rheumatoid arthritis, the clinical use of ibufenac was discontinued due to hepatotoxic side-effects. | 3.23 | 1 | 0 | monocarboxylic acid | EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; hepatotoxic agent; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| metaxalone [no description available] | 3.23 | 1 | 0 | aromatic ether | |
| spectinomycin Spectinomycin: An antibiotic produced by Streptomyces spectabilis. It is active against gram-negative bacteria and used for the treatment of GONORRHEA.. spectinomycin dihydrochloride : A hydrochloride obtained by combining spectinomycin with two molar equivalents of hydrochloric acid. An antibiotic that is active against gram-negative bacteria and used (as its pentahydrate) to treat gonorrhea.. spectinomycin : A pyranobenzodioxin and antibiotic that is active against gram-negative bacteria and used (as its dihydrochloride pentahydrate) to treat gonorrhea. It is produced by the bacterium Streptomyces spectabilis. | 3.23 | 1 | 0 | cyclic acetal; cyclic hemiketal; cyclic ketone; pyranobenzodioxin; secondary alcohol; secondary amino compound | antibacterial drug; antimicrobial agent; bacterial metabolite |
| dronabinol Dronabinol: A psychoactive compound extracted from the resin of Cannabis sativa (marihuana, hashish). The isomer delta-9-tetrahydrocannabinol (THC) is considered the most active form, producing characteristic mood and perceptual changes associated with this compound.. Delta(9)-tetrahydrocannabinol : A diterpenoid that is 6a,7,8,10a-tetrahydro-6H-benzo[c]chromene substituted at position 1 by a hydroxy group, positions 6, 6 and 9 by methyl groups and at position 3 by a pentyl group. The principal psychoactive constituent of the cannabis plant, it is used for treatment of anorexia associated with AIDS as well as nausea and vomiting associated with cancer chemotherapy. | 3.23 | 1 | 0 | benzochromene; diterpenoid; phytocannabinoid; polyketide | cannabinoid receptor agonist; epitope; hallucinogen; metabolite; non-narcotic analgesic |
| amiloride Amiloride: A pyrazine compound inhibiting SODIUM reabsorption through SODIUM CHANNELS in renal EPITHELIAL CELLS. This inhibition creates a negative potential in the luminal membranes of principal cells, located in the distal convoluted tubule and collecting duct. Negative potential reduces secretion of potassium and hydrogen ions. Amiloride is used in conjunction with DIURETICS to spare POTASSIUM loss. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p705). amiloride : A member of the class of pyrazines resulting from the formal monoacylation of guanidine with the carboxy group of 3,5-diamino-6-chloropyrazine-2-carboxylic acid. | 3.23 | 1 | 0 | aromatic amine; guanidines; organochlorine compound; pyrazines | diuretic; sodium channel blocker |
| pimozide Pimozide: A diphenylbutylpiperidine that is effective as an antipsychotic agent and as an alternative to HALOPERIDOL for the suppression of vocal and motor tics in patients with Tourette syndrome. Although the precise mechanism of action is unknown, blockade of postsynaptic dopamine receptors has been postulated. (From AMA Drug Evaluations Annual, 1994, p403). pimozide : A member of the class of benzimidazoles that is 1,3-dihydro-2H-benzimidazol-2-one in which one of the nitrogens is substituted by a piperidin-4-yl group, which in turn is substituted on the nitrogen by a 4,4-bis(p-fluorophenyl)butyl group. | 3.23 | 1 | 0 | benzimidazoles; heteroarylpiperidine; organofluorine compound | antidyskinesia agent; dopaminergic antagonist; first generation antipsychotic; H1-receptor antagonist; serotonergic antagonist |
| dexbrompheniramine dexbrompheniramine : The (pharmacologically active) (S)-(+)-enantiomer of brompheniramine. A histamine H1 receptor antagonist, it is used (commonly as its maleate salt) for the symptomatic relief of allergic conditions, including rhinitis and conjunctivitis. | 3.23 | 1 | 0 | brompheniramine | anti-allergic agent; H1-receptor antagonist |
| stavudine Stavudine: A dideoxynucleoside analog that inhibits reverse transcriptase and has in vitro activity against HIV.. stavudine : A nucleoside analogue obtained by formal dehydration across positions 2 and 3 of thymidine. An inhibitor of HIV-1 reverse transcriptase | 3.23 | 1 | 0 | dihydrofuran; nucleoside analogue; organic molecular entity | antimetabolite; antiviral agent; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor |
| dicloxacillin Dicloxacillin: One of the PENICILLINS which is resistant to PENICILLINASE.. dicloxacillin : A penicillin that is 6-aminopenicillanic acid in which one of the amino hydrogens is replaced by a 3-(2,6-dichlorophenyl)-5-methyl-1,2-oxazol-4-yl]formyl group. | 3.23 | 1 | 0 | dichlorobenzene; penicillin | antibacterial drug |
| megestrol Megestrol: A progestational hormone used most commonly as the acetate ester. As the acetate, it is more potent than progesterone both as a progestagen and as an ovulation inhibitor. It has also been used in the palliative treatment of breast cancer.. megestrol : A 3-oxo Delta(4)-steroid that is pregna-4,6-diene-3,20-dione substituted by a methyl group at position 6 and a hydroxy group at position 17. | 3.23 | 1 | 0 | 17alpha-hydroxy steroid; 20-oxo steroid; 3-oxo-Delta(4) steroid; tertiary alpha-hydroxy ketone | antineoplastic agent; appetite enhancer; contraceptive drug; progestin; synthetic oral contraceptive |
| streptomycin [no description available] | 3.23 | 1 | 0 | antibiotic antifungal drug; antibiotic fungicide; streptomycins | antibacterial drug; antifungal agrochemical; antimicrobial agent; antimicrobial drug; bacterial metabolite; protein synthesis inhibitor |
| cladribine [no description available] | 3.23 | 1 | 0 | organochlorine compound; purine 2'-deoxyribonucleoside | antineoplastic agent; immunosuppressive agent |
| carbenicillin Carbenicillin: Broad-spectrum semisynthetic penicillin derivative used parenterally. It is susceptible to gastric juice and penicillinase and may damage platelet function.. carbenicillin : A penicillin antibiotic having a 6beta-2-carboxy-2-phenylacetamido side-chain. | 3.23 | 1 | 0 | penicillin allergen; penicillin | antibacterial drug |
| clomacran clomacran: RN given refers to parent cpd; structure | 3.23 | 1 | 0 | acridines | |
| methenamine hippurate methenamine hippurate: both parts of molecule contribute to its antibacterial action | 3.23 | 1 | 0 | N-acylglycine | |
| olsalazine olsalazine: cpd with 2 salicylate molecules linked together by an azo bond. olsalazine : An azobenzene that consists of two molecules of 4-aminosalicylic acid joined by an azo linkage. A prodrug for mesalazine, an anti-inflammatory drug, it is used (as the disodium salt) in the treatment of inflammatory bowel disease. | 3.23 | 1 | 0 | azobenzenes; dicarboxylic acid | non-steroidal anti-inflammatory drug; prodrug |
| iridium Iridium: A metallic element with the atomic symbol Ir, atomic number 77, and atomic weight 192.22. | 2.11 | 1 | 0 | cobalt group element atom; platinum group metal atom | |
| sodium thiosulfate sodium thiosulfate: do not confuse synonym sodium hyposulfite with sodium hyposulfite, synonym for di-Na salt of dithionous acid. sodium thiosulfate : An inorganic sodium salt composed of sodium and thiosulfate ions in a 2:1 ratio. | 3.23 | 1 | 0 | inorganic sodium salt | antidote to cyanide poisoning; antifungal drug; nephroprotective agent |
| selegiline Selegiline: A selective, irreversible inhibitor of Type B monoamine oxidase that is used for the treatment of newly diagnosed patients with PARKINSON DISEASE, and for the treatment of depressive disorders. The compound without isomeric designation is Deprenyl. | 3.23 | 1 | 0 | selegiline; terminal acetylenic compound | geroprotector |
| clemastine Clemastine: A histamine H1 antagonist used as the hydrogen fumarate in hay fever, rhinitis, allergic skin conditions, and pruritus. It causes drowsiness.. clemastine : 2-[(2R)-1-Methylpyrrolidin-2-yl]ethanol in which the hydrogen of the hydroxy group is substituted by a 1-(4-chlorophenyl)-1-phenylethyl group (R configuration). An antihistamine with antimuscarinic and moderate sedative properties, it is used as its fumarate salt for the symptomatic relief of allergic conditions such as rhinitis, urticaria, conjunctivitis and in pruritic (severe itching) skin conditions. | 3.23 | 1 | 0 | monochlorobenzenes; N-alkylpyrrolidine | anti-allergic agent; antipruritic drug; H1-receptor antagonist; muscarinic antagonist |
| cephalexin Cephalexin: A semisynthetic cephalosporin antibiotic with antimicrobial activity similar to that of CEPHALORIDINE or CEPHALOTHIN, but somewhat less potent. It is effective against both gram-positive and gram-negative organisms.. cephalexin : A semisynthetic first-generation cephalosporin antibiotic having methyl and beta-(2R)-2-amino-2-phenylacetamido groups at the 3- and 7- of the cephem skeleton, respectively. It is effective against both Gram-negative and Gram-positive organisms, and is used for treatment of infections of the skin, respiratory tract and urinary tract. | 3.23 | 1 | 0 | beta-lactam antibiotic allergen; cephalosporin; semisynthetic derivative | antibacterial drug |
| danazol Danazol: A synthetic steroid with antigonadotropic and anti-estrogenic activities that acts as an anterior pituitary suppressant by inhibiting the pituitary output of gonadotropins. It possesses some androgenic properties. Danazol has been used in the treatment of endometriosis and some benign breast disorders. | 3.23 | 1 | 0 | 17beta-hydroxy steroid; terminal acetylenic compound | anti-estrogen; estrogen antagonist; geroprotector |
| fenclozic acid fenclozic acid: an analgesic & antipyretic with anti-inflammatory properties; minor descriptor (75-86); on-line & INDEX MEDICUS search THIAZOLES (75-86); RN given refers to parent cpd | 3.23 | 1 | 0 | ||
| laxagetten 4,4'-diacetoxydiphenylpyridylemethane [no description available] | 3.23 | 1 | 0 | ||
| daunorubicin Daunorubicin: A very toxic anthracycline aminoglycoside antineoplastic isolated from Streptomyces peucetius and others, used in treatment of LEUKEMIA and other NEOPLASMS.. anthracycline : Anthracyclines are polyketides that have a tetrahydronaphthacenedione ring structure attached by a glycosidic linkage to the amino sugar daunosamine.. daunorubicin : A natural product found in Actinomadura roseola. | 3.23 | 1 | 0 | aminoglycoside antibiotic; anthracycline; p-quinones; tetracenequinones | antineoplastic agent; bacterial metabolite |
| fludarabine phosphate fludarabine phosphate: structure given in first source. fludarabine phosphate : A purine arabinonucleoside monophosphate having 2-fluoroadenine as the nucleobase. A prodrug, it is rapidly dephosphorylated to 2-fluoro-ara-A and then phosphorylated intracellularly by deoxycytidine kinase to the active triphosphate, 2-fluoro-ara-ATP. Once incorporated into DNA, 2-fluoro-ara-ATP functions as a DNA chain terminator. It is used for the treatment of adult patients with B-cell chronic lymphocytic leukemia (CLL) who have not responded to, or whose disease has progressed during, treatment with at least one standard alkylating-agent containing regimenas. | 3.23 | 1 | 0 | nucleoside analogue; organofluorine compound; purine arabinonucleoside monophosphate | antimetabolite; antineoplastic agent; antiviral agent; DNA synthesis inhibitor; immunosuppressive agent; prodrug |
| alclofenac alclofenac: was heading 1975-94 (was see under PHENYLACETATES 1975-90); use PHENYLACETATES to search ALCLOFENAC 1975-94; an anti-inflammatory agent used in the treatment of rheumatoid arthritis; acts also as an analgesic and an antipyretic. alclofenac : An aromatic ether in which the ether oxygen links an allyl group to the 4-position of (3-chlorophenyl)acetic acid.A non-steroidal anti-inflammatory drug, it was withdrawn from the UK market in 1979 due to concerns with its association with vasculitis and rash. | 3.23 | 1 | 0 | aromatic ether; monocarboxylic acid; monochlorobenzenes | drug allergen; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| bromocriptine Bromocriptine: A semisynthetic ergotamine alkaloid that is a dopamine D2 agonist. It suppresses prolactin secretion. | 3.23 | 1 | 0 | indole alkaloid | antidyskinesia agent; antiparkinson drug; dopamine agonist; hormone antagonist |
| oxyphenisatin [no description available] | 3.23 | 1 | 0 | indoles | |
| fludrocortisone Fludrocortisone: A synthetic mineralocorticoid with anti-inflammatory activity. | 3.23 | 1 | 0 | 11beta-hydroxy steroid; 17alpha-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(4) steroid; C21-steroid; fluorinated steroid; mineralocorticoid | adrenergic agent; anti-inflammatory drug |
| ursodeoxycholic acid Ursodeoxycholic Acid: An epimer of chenodeoxycholic acid. It is a mammalian bile acid found first in the bear and is apparently either a precursor or a product of chenodeoxycholate. Its administration changes the composition of bile and may dissolve gallstones. It is used as a cholagogue and choleretic.. ursodeoxycholic acid : A bile acid found in the bile of bears (Ursidae) as a conjugate with taurine. Used therapeutically, it prevents the synthesis and absorption of cholesterol and can lead to the dissolution of gallstones.. ursodeoxycholate : A bile acid anion that is the conjugate base of ursodeoxycholic acid, obtained by deprotonation of the carboxy group; major species at pH 7.3. | 3.23 | 1 | 0 | bile acid; C24-steroid; dihydroxy-5beta-cholanic acid | human metabolite; mouse metabolite |
| dexchlorpheniramine dexchlorpheniramine: RN given refers to parent cpd(S)-isomer | 3.23 | 1 | 0 | chlorphenamine | |
| clometacin clometacin: structure | 3.23 | 1 | 0 | N-acylindole | |
| cefazolin Cefazolin: A semisynthetic cephalosporin analog with broad-spectrum antibiotic action due to inhibition of bacterial cell wall synthesis. It attains high serum levels and is excreted quickly via the urine.. cefazolin : A first-generation cephalosporin compound having [(5-methyl-1,3,4-thiadiazol-2-yl)sulfanyl]methyl and (1H-tetrazol-1-ylacetyl)amino side-groups at positions 3 and 7 respectively. | 3.23 | 1 | 0 | beta-lactam antibiotic allergen; cephalosporin; tetrazoles; thiadiazoles | antibacterial drug |
| amoxicillin Amoxicillin: A broad-spectrum semisynthetic antibiotic similar to AMPICILLIN except that its resistance to gastric acid permits higher serum levels with oral administration.. amoxicillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-amino-2-(4-hydroxyphenyl)acetamido group. | 3.23 | 1 | 0 | penicillin allergen; penicillin | antibacterial drug |
| timolol (S)-timolol (anhydrous) : The (S)-(-) (more active) enantiomer of timolol. A beta-adrenergic antagonist, both the hemihydrate and the maleate salt are used in the mangement of glaucoma, hypertension, angina pectoris and myocardial infarction, and for the prevention of migraine. | 3.23 | 1 | 0 | timolol | anti-arrhythmia drug; antiglaucoma drug; antihypertensive agent; beta-adrenergic antagonist |
| oxcarbazepine Oxcarbazepine: A carbamazepine derivative that acts as a voltage-gated sodium channel blocker. It is used for the treatment of PARTIAL SEIZURES with or without secondary generalization. It is also an inducer of CYTOCHROME P-450 CYP3A4.. oxcarbazepine : A dibenzoazepine derivative, having a carbamoyl group at the ring nitrogen, substituted with an oxo group at C-4 of the azepeine ring which is also hydrogenated at C-4 and C-5. It is a anticholinergic anticonvulsant and mood stabilizing drug, used primarily in the treatment of epilepsy. | 3.23 | 1 | 0 | cyclic ketone; dibenzoazepine | anticonvulsant; drug allergen |
| carbidopa carbidopa (anhydrous) : 3-(3,4-Dihydroxyphenyl)propanoic acid in which the hydrogens alpha- to the carboxyl group are substituted by hydrazinyl and methyl groups (S-configuration). Carbidopa is a dopa decarboxylase inhibitor, so prevents conversion of levodopa to dopamine. It has no antiparkinson activity by itself, but is used (commonly as its hydrate) in the management of Parkinson's disease to reduce peripheral adverse effects of levodopa. | 3.23 | 1 | 0 | catechols; hydrazines; monocarboxylic acid | antiparkinson drug; dopaminergic agent; EC 4.1.1.28 (aromatic-L-amino-acid decarboxylase) inhibitor |
| moricizine Moricizine: An antiarrhythmia agent used primarily for ventricular rhythm disturbances.. moricizine : A phenothiazine substituted on the nitrogen by a 3-(morpholin-4-yl)propanoyl group, and at position 2 by an (ethoxycarbonyl)amino group. | 3.23 | 1 | 0 | carbamate ester; morpholines; phenothiazines | anti-arrhythmia drug |
| amineptin amineptin: used in treatment of neuroses with psychoasthenic, anxio-phobic & depressive manifestations; synonym S 1694 refers to HCl; structure. amineptine : A carbocyclic fatty acid that is 5-aminoheptanoic acid in which one of the hydrogens attached to the nitrogen is replaced by a 10,11-dihydro-5H-dibenzo[a,d][7]annulen-5-yl group. A tricyclic antidepressant, it was never approved in the US and was withdrawn from the French market in 1999 due to concerns over abuse, dependence and severe acne. | 3.23 | 1 | 0 | amino acid; carbocyclic fatty acid; carbotricyclic compound; secondary amino compound | antidepressant; dopamine uptake inhibitor |
| zidovudine Zidovudine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by an azido group. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA during reverse transcription. It improves immunologic function, partially reverses the HIV-induced neurological dysfunction, and improves certain other clinical abnormalities associated with AIDS. Its principal toxic effect is dose-dependent suppression of bone marrow, resulting in anemia and leukopenia.. zidovudine : A pyrimidine 2',3'-dideoxyribonucleoside compound having a 3'-azido substituent and thymine as the nucleobase. | 3.23 | 1 | 0 | azide; pyrimidine 2',3'-dideoxyribonucleoside | antimetabolite; antiviral drug; HIV-1 reverse transcriptase inhibitor |
| pirprofen pirprofen: anti-inflammatory agent used in therapy of rheumatoid arthritis; prostaglandin synthetase inhibitor; more potent than indomethacin; structure | 3.23 | 1 | 0 | pyrroline | |
| paclitaxel Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL). | 3.23 | 1 | 0 | taxane diterpenoid; tetracyclic diterpenoid | antineoplastic agent; human metabolite; metabolite; microtubule-stabilising agent |
| etoposide [no description available] | 3.23 | 1 | 0 | beta-D-glucoside; furonaphthodioxole; organic heterotetracyclic compound | antineoplastic agent; DNA synthesis inhibitor |
| dobutamine Dobutamine: A catecholamine derivative with specificity for BETA-1 ADRENERGIC RECEPTORS. It is commonly used as a cardiotonic agent after CARDIAC SURGERY and during DOBUTAMINE STRESS ECHOCARDIOGRAPHY.. dobutamine : A catecholamine that is 4-(3-aminobutyl)phenol in which one of the hydrogens attached to the nitrogen is substituted by a 2-(3,4-dihydroxyphenyl)ethyl group. A beta1-adrenergic receptor agonist that has cardiac stimulant action without evoking vasoconstriction or tachycardia, it is used as the hydrochloride to increase the contractility of the heart in the management of acute heart failure. | 3.23 | 1 | 0 | catecholamine; secondary amine | beta-adrenergic agonist; cardiotonic drug; sympathomimetic agent |
| penbutolol Penbutolol: A nonselective beta-blocker used as an antihypertensive and an antianginal agent. | 3.23 | 1 | 0 | ethanolamines | |
| ribavirin Rebetron: Rebetron is tradename | 3.23 | 1 | 0 | 1-ribosyltriazole; aromatic amide; monocarboxylic acid amide; primary carboxamide | anticoronaviral agent; antiinfective agent; antimetabolite; antiviral agent; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor |
| amikacin Amikacin: A broad-spectrum antibiotic derived from KANAMYCIN. It is reno- and oto-toxic like the other aminoglycoside antibiotics.. amikacin : An amino cyclitol glycoside that is kanamycin A acylated at the N-1 position by a 4-amino-2-hydroxybutyryl group. | 3.23 | 1 | 0 | alpha-D-glucoside; amino cyclitol glycoside; aminoglycoside; carboxamide | antibacterial drug; antimicrobial agent; nephrotoxin |
| cephradine Cephradine: A semi-synthetic cephalosporin antibiotic.. cephradine : A first-generation cephalosporin antibiotic with a methyl substituent at position 3, and a (2R)-2-amino-2-cyclohexa-1,4-dien-1-ylacetamido substituent at position 7, of the cephem skeleton. | 3.23 | 1 | 0 | beta-lactam antibiotic allergen; cephalosporin | antibacterial drug |
| ticrynafen Ticrynafen: A novel diuretic with uricosuric action. It has been proposed as an antihypertensive agent.. tienilic acid : An aromatic ketone that is 2,3-dichlorophenoxyacetic acid in which the hydrogen at position 4 on the benzene ring is replaced by a thiophenecarbonyl group. A loop diuretic used to treat hypertension, it was withdrawn from the market in 1982 due to links with hepatitis. | 3.23 | 1 | 0 | aromatic ether; aromatic ketone; dichlorobenzene; monocarboxylic acid; thiophenes | antihypertensive agent; hepatotoxic agent; loop diuretic |
| methyldopa Methyldopa: An alpha-2 adrenergic agonist that has both central and peripheral nervous system effects. Its primary clinical use is as an antihypertensive agent.. alpha-methyl-L-dopa : A derivative of L-tyrosine having a methyl group at the alpha-position and an additional hydroxy group at the 3-position on the phenyl ring. | 3.23 | 1 | 0 | L-tyrosine derivative; non-proteinogenic L-alpha-amino acid | alpha-adrenergic agonist; antihypertensive agent; hapten; peripheral nervous system drug; sympatholytic agent |
| diltiazem Diltiazem: A benzothiazepine derivative with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions.. diltiazem : A 5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate in which both stereocentres have S configuration. A calcium-channel blocker and vasodilator, it is used as the hydrochloride in the management of angina pectoris and hypertension. | 3.23 | 1 | 0 | 5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate | antihypertensive agent; calcium channel blocker; vasodilator agent |
| vecuronium vecuronium : A 5alpha-androstane compound having 3alpha-acetoxy-, 17beta-acetoxy-, 2beta-piperidino- and 16beta-N-methylpiperidinium substituents. | 3.23 | 1 | 0 | acetate ester; androstane; quaternary ammonium ion | drug allergen; muscle relaxant; neuromuscular agent; nicotinic antagonist |
| benoxaprofen benoxaprofen: RN given refers to parent cpd; structure. benoxaprofen : A monocarboxylic acid that is propionic acid substituted at position 2 by a 2-(4-chlorophenyl)-1,3-benzoxazol-5-yl group. It was used as a non-steroidal anti-inflammatory drug until 1982 when it was withdrawn from the market due to adverse side-effects including liver necrosis, photosensitivity, and carcinogenicity in animals. | 3.23 | 1 | 0 | 1,3-benzoxazoles; monocarboxylic acid; monochlorobenzenes | antipsoriatic; antipyretic; EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor; hepatotoxic agent; nephrotoxin; non-narcotic analgesic; non-steroidal anti-inflammatory drug; protein kinase C agonist |
| exifone [no description available] | 3.23 | 1 | 0 | benzophenones | |
| mefloquine (-)-(11S,2'R)-erythro-mefloquine : An optically active form of [2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol having (-)-(11S,2'R)-erythro-configuration. An antimalarial agent, used in racemic form, which acts as a blood schizonticide; its mechanism of action is unknown. | 3.23 | 1 | 0 | [2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol | antimalarial |
| nitazoxanide nitazoxanide: a 5-nitrothiazolyl derivative used for a broad range of intestinal parasitic infections including CRYPTOSPORIDIUM and GIARDIA; it is a redox-active nitrothiazolyl-salicylamide prodrug | 3.23 | 1 | 0 | benzamides; carboxylic ester | |
| sufentanil Sufentanil: An opioid analgesic that is used as an adjunct in anesthesia, in balanced anesthesia, and as a primary anesthetic agent.. sufentanil : An anilide resulting from the formal condensation of the aryl amino group of 4-(methoxymethyl)-N-phenyl-1-[2-(2-thienyl)ethyl]piperidin-4-amine with propanoic acid. | 3.23 | 1 | 0 | anilide; ether; piperidines; thiophenes | anaesthesia adjuvant; intravenous anaesthetic; mu-opioid receptor agonist; opioid analgesic |
| acarbose [no description available] | 3.23 | 1 | 0 | tetrasaccharide derivative | EC 3.2.1.1 (alpha-amylase) inhibitor; EC 3.2.1.20 (alpha-glucosidase) inhibitor; geroprotector; hypoglycemic agent |
| torsemide Torsemide: A pyridine and sulfonamide derivative that acts as a sodium-potassium chloride symporter inhibitor (loop diuretic). It is used for the treatment of EDEMA associated with CONGESTIVE HEART FAILURE; CHRONIC RENAL INSUFFICIENCY; and LIVER DISEASES. It is also used for the management of HYPERTENSION.. torasemide : An N-sulfonylurea obtained by formal condensation of [(3-methylphenyl)amino]pyridine-3-sulfonic acid with the free amino group of N-isopropylurea. It is a potent loop diuretic used for the treatment of hypertension and edema in patients with congestive heart failure. | 3.23 | 1 | 0 | aminopyridine; N-sulfonylurea; secondary amino compound | antihypertensive agent; loop diuretic |
| epirubicin Epirubicin: An anthracycline which is the 4'-epi-isomer of doxorubicin. The compound exerts its antitumor effects by interference with the synthesis and function of DNA. | 3.23 | 1 | 0 | aminoglycoside; anthracycline antibiotic; anthracycline; deoxy hexoside; monosaccharide derivative; p-quinones; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone | antimicrobial agent; antineoplastic agent; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor |
| idarubicin Idarubicin: An orally administered anthracycline antineoplastic. The compound has shown activity against BREAST NEOPLASMS; LYMPHOMA; and LEUKEMIA. | 3.23 | 1 | 0 | anthracycline antibiotic; deoxy hexoside; monosaccharide derivative | |
| piperacillin Piperacillin: Semisynthetic, broad-spectrum, AMPICILLIN derived ureidopenicillin antibiotic proposed for PSEUDOMONAS infections. It is also used in combination with other antibiotics.. piperacillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-[(4-ethyl-2,3-dioxopiperazin-1-yl)carboxamido]-2-phenylacetamido group. | 3.23 | 1 | 0 | penicillin allergen; penicillin | antibacterial drug |
| paroxetine Paroxetine: A serotonin uptake inhibitor that is effective in the treatment of depression.. paroxetine : A benzodioxole that consists of piperidine bearing 1,3-benzodioxol-5-yloxy)methyl and 4-fluorophenyl substituents at positions 3 and 4 respectively; the (3S,4R)-diastereomer. Highly potent and selective 5-HT uptake inhibitor that binds with high affinity to the serotonin transporter (Ki = 0.05 nM). Ki values are 1.1, 350 and 1100 nM for inhibition of [3H]-5-HT, [3H]-l-NA and [3H]-DA uptake respectively. Displays minimal affinity for alpha1-, alpha2- or beta-adrenoceptors, 5-HT2A, 5-HT1A, D2 or H1 receptors at concentrations below 1000 nM, however displays weak affinity for muscarinic ACh receptors (Ki = 42 nM). Antidepressant and anxiolytic in vivo. | 3.23 | 1 | 0 | aromatic ether; benzodioxoles; organofluorine compound; piperidines | antidepressant; anxiolytic drug; hepatotoxic agent; P450 inhibitor; serotonin uptake inhibitor |
| captopril Captopril: A potent and specific inhibitor of PEPTIDYL-DIPEPTIDASE A. It blocks the conversion of ANGIOTENSIN I to ANGIOTENSIN II, a vasoconstrictor and important regulator of arterial blood pressure. Captopril acts to suppress the RENIN-ANGIOTENSIN SYSTEM and inhibits pressure responses to exogenous angiotensin.. captopril : A L-proline derivative in which L-proline is substituted on nitrogen with a (2S)-2-methyl-3-sulfanylpropanoyl group. It is used as an anti-hypertensive ACE inhibitor drug. | 3.23 | 1 | 0 | alkanethiol; L-proline derivative; N-acylpyrrolidine; pyrrolidinemonocarboxylic acid | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor |
| cefoperazone Cefoperazone: Semisynthetic broad-spectrum cephalosporin with a tetrazolyl moiety that is resistant to beta-lactamase. It may be used to treat Pseudomonas infections.. cefoperazone : A semi-synthetic parenteral cephalosporin with a tetrazolyl moiety that confers beta-lactamase resistance. | 3.23 | 1 | 0 | cephalosporin | antibacterial drug |
| atracurium Atracurium: A non-depolarizing neuromuscular blocking agent with short duration of action. Its lack of significant cardiovascular effects and its lack of dependence on good kidney function for elimination provide clinical advantage over alternate non-depolarizing neuromuscular blocking agents.. atracurium : A diester compound consisting of pentane-1,5-diol with both hydroxyls bearing 3-[1-(3,4-dimethoxybenzyl)-6,7-dimethoxy-2-methyl-3,4-dihydroisoquinolinium-2(1H)-yl]propanoyl groups. | 3.23 | 1 | 0 | diester; quaternary ammonium ion | muscle relaxant; nicotinic antagonist |
| pergolide Pergolide: A long-acting dopamine agonist which has been used to treat PARKINSON DISEASE and HYPERPROLACTINEMIA but withdrawn from some markets due to potential for HEART VALVE DISEASES.. pergolide : A diamine that is ergoline in which the beta-hydrogen at position 8 is replaced by a (methylthio)methyl group and the hydrogen attached to the piperidine nitrogen (position 6) is replaced by a propyl group. A dopamine D2 receptor agonist which also has D1 and D2 agonist properties, it is used as the mesylate salt in the management of Parkinson's disease, although it was withdrawn from the U.S. and Canadian markets in 2007 due to an increased risk of cardiac valve dysfunction. | 3.23 | 1 | 0 | diamine; methyl sulfide; organic heterotetracyclic compound | antiparkinson drug; dopamine agonist |
| cefadroxil anhydrous Cefadroxil: Long-acting, broad-spectrum, water-soluble, CEPHALEXIN derivative.. cefadroxil : A cephalosporin bearing methyl and (2R)-2-amino-2-(4-hydroxyphenyl)acetamido groups at positions 3 and 7, respectively, of the cephem skeleton. | 3.23 | 1 | 0 | cephalosporin | antibacterial drug |
| fialuridine [no description available] | 3.23 | 1 | 0 | ||
| cefaclor anhydrous Cefaclor: Semisynthetic, broad-spectrum antibiotic derivative of CEPHALEXIN.. cefaclor : A cephalosporin bearing chloro and (R)-2-amino-2-phenylacetamido groups at positions 3 and 7, respectively, of the cephem skeleton. | 3.23 | 1 | 0 | cephalosporin | antibacterial drug; drug allergen |
| alfentanil Alfentanil: A short-acting opioid anesthetic and analgesic derivative of FENTANYL. It produces an early peak analgesic effect and fast recovery of consciousness. Alfentanil is effective as an anesthetic during surgery, for supplementation of analgesia during surgical procedures, and as an analgesic for critically ill patients.. alfentanil : A member of the class of piperidines that is piperidine having a 2-(4-ethyl-5-oxo-4,5-dihydro-1H-tetrazol-1-yl)ethyl group at the 1-position as well as N-phenylpropanamido- and methoxymethyl groups at the 4-position. | 3.23 | 1 | 0 | monocarboxylic acid amide; piperidines | central nervous system depressant; intravenous anaesthetic; mu-opioid receptor agonist; opioid analgesic; peripheral nervous system drug |
| miglustat miglustat: a glucosylceramide synthase inhibitor. miglustat : A hydroxypiperidine that is deoxynojirimycin in which the amino hydrogen is replaced by a butyl group. | 3.23 | 1 | 0 | piperidines; tertiary amino compound | anti-HIV agent; EC 2.4.1.80 (ceramide glucosyltransferase) inhibitor |
| haloperidol decanoate [no description available] | 3.23 | 1 | 0 | organic molecular entity | |
| cefotetan Cefotetan: A semisynthetic cephamycin antibiotic that is administered intravenously or intramuscularly. The drug is highly resistant to a broad spectrum of beta-lactamases and is active against a wide range of both aerobic and anaerobic gram-positive and gram-negative microorganisms.. cefotetan : A semi-synthetic second-generation cephamycin antibiotic with [(1-methyl-1H-tetrazol-5-yl)sulfanyl]methyl, methoxy and {[4-(2-amino-1-carboxy-2-oxoethylidene)-1,3-dithietan-2-yl]carbonyl}amino groups at the 3, 7alpha, and 7beta positions, respectively, of the cephem skeleton. It is resistant to a wide range of beta-lactamases and is active against a broad spectrum of aerobic and anaerobic Gram-positive and Gram-negative microorganisms. | 3.23 | 1 | 0 | ||
| lovastatin Lovastatin: A fungal metabolite isolated from cultures of Aspergillus terreus. The compound is a potent anticholesteremic agent. It inhibits 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It also stimulates the production of low-density lipoprotein receptors in the liver.. lovastatin : A fatty acid ester that is mevastatin carrying an additional methyl group on the carbobicyclic skeleton. It is used in as an anticholesteremic drug and has been found in fungal species such as Aspergillus terreus and Pleurotus ostreatus (oyster mushroom). | 3.23 | 1 | 0 | delta-lactone; fatty acid ester; hexahydronaphthalenes; polyketide; statin (naturally occurring) | anticholesteremic drug; antineoplastic agent; Aspergillus metabolite; prodrug |
| tolrestat tolrestat: RN & structure given in first source | 3.23 | 1 | 0 | naphthalenes | EC 1.1.1.21 (aldehyde reductase) inhibitor |
| simvastatin Simvastatin: A derivative of LOVASTATIN and potent competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It may also interfere with steroid hormone production. Due to the induction of hepatic LDL RECEPTORS, it increases breakdown of LDL CHOLESTEROL.. simvastatin : A member of the class of hexahydronaphthalenes that is lovastatin in which the 2-methylbutyrate ester moiety has been replaced by a 2,2-dimethylbutyrate ester group. It is used as a cholesterol-lowering and anti-cardiovascular disease drug. | 3.23 | 1 | 0 | delta-lactone; fatty acid ester; hexahydronaphthalenes; statin (semi-synthetic) | EC 1.1.1.34/EC 1.1.1.88 (hydroxymethylglutaryl-CoA reductase) inhibitor; EC 3.4.24.83 (anthrax lethal factor endopeptidase) inhibitor; ferroptosis inducer; geroprotector; prodrug |
| balsalazide balsalazide: a mesalamine 5-aminosalicylate prodrug; 99% of ingested drug remains intact through the stomach and is delivered to and activated in the colon; used for inflammatory bowel disease, ulcerative colitis and radiation-induced proctosigmoiditis but avoided in patients with known hypersensitivity reaction to salicylates or mesalamine; structure in first source. balsalazide : A monohydroxybenzoic acid consisting of 5-aminosalicylic acid (mesalazine) linked to 4-aminobenzoyl-beta-alanine via an azo bond. | 3.23 | 1 | 0 | ||
| pravastatin Pravastatin: An antilipemic fungal metabolite isolated from cultures of Nocardia autotrophica. It acts as a competitive inhibitor of HMG CoA reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES).. pravastatin : A carboxylic ester resulting from the formal condensation of (S)-2-methylbutyric acid with the hydroxy group adjacent to the ring junction of (3R,5R)-7-[(1S,2S,6S,8S,8aR)-6,8-dihydroxy-2-methyl-1,2,6,7,8,8a-hexahydronaphthalen-1-yl]-3,5-dihydroxyheptanoic acid. Derived from microbial transformation of mevastatin, pravastatin is a reversible inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA). The sodium salt is used for lowering cholesterol and preventing cardiovascular disease. It is one of the lower potency statins, but has the advantage of fewer side effects compared with lovastatin and simvastatin. | 3.23 | 1 | 0 | 3-hydroxy carboxylic acid; carbobicyclic compound; carboxylic ester; hydroxy monocarboxylic acid; secondary alcohol; statin (semi-synthetic) | anticholesteremic drug; environmental contaminant; metabolite; xenobiotic |
| cabergoline Cabergoline: An ergoline derivative and dopamine D2-agonist that inhibits PROLACTIN secretion. It is used in the management of HYPERPROLACTINEMIA, and to suppress lactation following childbirth for medical reasons. Cabergoline is also used in the management of PARKINSON DISEASE.. cabergoline : An N-acylurea that is (8R)-ergoline-8-carboxamide in which the hydrogen attached to the piperidine nitrogen (position 6) is substituted by an allyl group and the hydrogens attached to the carboxamide nitrogen are substituted by a 3-(dimethylamino)propyl group and an N-ethylcarbamoyl group. A dopamine D2 receptor agonist, cabergoline is used in the management of Parkinson's disease and of disorders associated with hyperprolactinaemia. | 3.23 | 1 | 0 | N-acylurea | antineoplastic agent; antiparkinson drug; dopamine agonist |
| atomoxetine atomoxetine : A secondary amino compound having methyl and 3-(2-methylphenoxy)-3-phenylpropan-1-yl substituents. | 3.23 | 1 | 0 | aromatic ether; secondary amino compound; toluenes | adrenergic uptake inhibitor; antidepressant; environmental contaminant; xenobiotic |
| quinapril Quinapril: A tetrahydroisoquinoline derivative and ANGIOTENSIN CONVERTING ENZYME inhibitor that is used in the treatment of HYPERTENSION and HEART FAILURE.. quinapril : A member of the class of isoquinolines that is (3S)-2-L-alanyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid in which the alpha-amino group of the alanyl residue has been substituted by a 1-ethoxycarbonyl-4-phenylbutan-2-yl group (the all-S isomer). A prodrug for quinaprilat (by hydrolysis of the ethyl ester to the corresponding carboxylic acid), it is used as an angiotensin-converting enzyme inhibitor (ACE inhibitor) used (generally as the hydrochloride salt) for the treatment of hypertension and congestive heart failure. | 3.23 | 1 | 0 | dicarboxylic acid monoester; ethyl ester; isoquinolines; tertiary carboxamide | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; prodrug |
| alpidem [no description available] | 3.23 | 1 | 0 | imidazoles | |
| mifepristone Mifepristone: A progestational and glucocorticoid hormone antagonist. Its inhibition of progesterone induces bleeding during the luteal phase and in early pregnancy by releasing endogenous prostaglandins from the endometrium or decidua. As a glucocorticoid receptor antagonist, the drug has been used to treat hypercortisolism in patients with nonpituitary CUSHING SYNDROME. | 3.23 | 1 | 0 | 3-oxo-Delta(4) steroid; acetylenic compound; tertiary amino compound | abortifacient; contraceptive drug; hormone antagonist; synthetic oral contraceptive |
| fosphenytoin fosphenytoin: structure given in first & second source | 3.23 | 1 | 0 | imidazolidine-2,4-dione | |
| ranolazine Ranolazine: An acetanilide and piperazine derivative that functions as a SODIUM CHANNEL BLOCKER and prevents the release of enzymes during MYOCARDIAL ISCHEMIA. It is used in the treatment of ANGINA PECTORIS.. N-(2,6-dimethylphenyl)-2-{4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl}acetamide : An aromatic amide obtained by formal condensation of the carboxy group of 2-{4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl}acetic acid with the amino group of 2,6-dimethylaniline.. ranolazine : A racemate comprising equal amounts of (R)- and (S)-ranolazine. Used for treatment of chronic angina. | 3.23 | 1 | 0 | aromatic amide; monocarboxylic acid amide; monomethoxybenzene; N-alkylpiperazine; secondary alcohol | |
| finasteride Finasteride: An orally active 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE inhibitor. It is used as a surgical alternative for treatment of benign PROSTATIC HYPERPLASIA.. finasteride : An aza-steroid that is a synthetic drug for the treatment of benign prostatic hyperplasia. | 3.23 | 1 | 0 | 3-oxo steroid; aza-steroid; delta-lactam | androgen antagonist; antihyperplasia drug; EC 1.3.1.22 [3-oxo-5alpha-steroid 4-dehydrogenase (NADP(+))] inhibitor |
| esmolol methyl 3-{4-[2-hydroxy-3-(propan-2-ylamino)propoxy]phenyl}propanoate : A methyl ester that is methyl 3-(4-hydroxyphenyl)propanoate in which the hydrogen attached to the phenolic hydroxy group is substituted by a 2-hydroxy-3-(isopropylamino)propyl group.. esmolol : A racemate comprising equimolar amounts of (R)- and (S)-esmolol. A cardioselective and short-acting beta1 receptor blocker with rapid onset but lacking intrinsic sympathomimetic and membrane-stabilising properties, it is used as the hydrochloride salt in the management of supraventricular arrhythmias, and for the control of hypertension and tachycardia during surgery. While the S enantiomer possesses all of the heart rate control, both enantiomers contribute to lowering blood pressure. | 3.23 | 1 | 0 | aromatic ether; ethanolamines; methyl ester; secondary alcohol; secondary amino compound | |
| adefovir adefovir: inhibitor of African swine fever virus. adefovir(1-) : A organophosphonate oxoanion obtained by removal of a proton from the phosphonate group of adefovir, a nucleoside reverse transcriptase inhibitor. It is the major microspecies at pH 7.3 (according to Marvin v 6.2.0.).. adefovir : A member of the class of phosphonic acids that is methylphosphonic acid in which one of the methyl hydrogens has been replaced by a 2-(6-amino-9H-purin-9-yl)ethoxy group. An inhibitor of HIV-1 reverse transcriptase, the bis(t-butoxycarbonyloxymethyl) ester (dipivoxil ester) prodrug is used to treat chronic hepatitis B viral infection. | 3.23 | 1 | 0 | 6-aminopurines; ether; phosphonic acids | antiviral drug; DNA synthesis inhibitor; drug metabolite; HIV-1 reverse transcriptase inhibitor; nephrotoxic agent |
| aromasil [no description available] | 3.23 | 1 | 0 | 17-oxo steroid; 3-oxo-Delta(1),Delta(4)-steroid | antineoplastic agent; EC 1.14.14.14 (aromatase) inhibitor; environmental contaminant; xenobiotic |
| zileuton [no description available] | 3.23 | 1 | 0 | 1-benzothiophenes; ureas | anti-asthmatic drug; EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor; ferroptosis inhibitor; leukotriene antagonist; non-steroidal anti-inflammatory drug |
| clopidogrel Clopidogrel: A ticlopidine analog and platelet purinergic P2Y receptor antagonist that inhibits adenosine diphosphate-mediated PLATELET AGGREGATION. It is used to prevent THROMBOEMBOLISM in patients with ARTERIAL OCCLUSIVE DISEASES; MYOCARDIAL INFARCTION; STROKE; or ATRIAL FIBRILLATION.. clopidogrel : A thienopyridine that is 4,5,6,7-tetrahydrothieno[3,2-c]pyridine in which the hydrogen attached to the nitrogen is replaced by an o-chlorobenzyl group, the methylene hydrogen of which is replaced by a methoxycarbonyl group (the S enantiomer). A P2Y12 receptor antagonist, it is used to inhibit blood clots and prevent heart attacks. | 3.23 | 1 | 0 | methyl ester; monochlorobenzenes; thienopyridine | anticoagulant; P2Y12 receptor antagonist; platelet aggregation inhibitor |
| cidofovir anhydrous Cidofovir: An acyclic nucleoside phosphonate that acts as a competitive inhibitor of viral DNA polymerases. It is used in the treatment of RETINITIS caused by CYTOMEGALOVIRUS INFECTIONS and may also be useful for treating HERPESVIRUS INFECTIONS.. cidofovir anhydrous : Cytosine substituted at the 1 position by a 3-hydroxy-2-(phosphonomethoxy)propyl group (S configuration). A nucleoside analogue, it is an injectable antiviral used for the treatment of cytomegalovirus (CMV) retinitis in AIDS patients. | 3.23 | 1 | 0 | phosphonic acids; pyrimidone | anti-HIV agent; antineoplastic agent; antiviral drug; photosensitizing agent |
| tiagabine Tiagabine: A nipecotic acid derivative that acts as a GABA uptake inhibitor and anticonvulsant agent. It is used in the treatment of EPILEPSY, for refractory PARTIAL SEIZURES.. tiagabine : A piperidinemonocarboxylic acid that is (R)-nipecotic acid in which the hydrogen attached to the nitrogen has been replaced by a 1,1-bis(3-methyl-2-thienyl)but-1-en-4-yl group. A GABA reuptake inhibitor, it is used (generally as the hydrochloride salt) for the treatment of epilepsy. | 3.23 | 1 | 0 | beta-amino acid; piperidinemonocarboxylic acid; tertiary amino compound; thiophenes | anticonvulsant; GABA reuptake inhibitor |
| topotecan Topotecan: An antineoplastic agent used to treat ovarian cancer. It works by inhibiting DNA TOPOISOMERASES, TYPE I.. topotecan : A pyranoindolizinoquinoline used as an antineoplastic agent. It is a derivative of camptothecin and works by binding to the topoisomerase I-DNA complex and preventing religation of these 328 single strand breaks. | 3.23 | 1 | 0 | pyranoindolizinoquinoline | antineoplastic agent; EC 5.99.1.2 (DNA topoisomerase) inhibitor |
| bromfenac bromfenac: bromfenac sodium is the active cpd; structure in first source. bromfenac : Amfenac in which the the hydrogen at the 4 position of the benzoyl group is substituted by bromine. It is used for the management of ocular pain and treatment of postoperative inflammation in patients who have undergone cataract extraction. It was withdrawn from the US market in 1998, following concerns over off-label abuse and hepatic failure. | 3.23 | 1 | 0 | aromatic amino acid; benzophenones; organobromine compound; substituted aniline | non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| gemcitabine gemcitabine : A 2'-deoxycytidine having geminal fluoro substituents in the 2'-position. An inhibitor of ribonucleotide reductase, gemcitabine is used in the treatment of various carcinomas, particularly non-small cell lung cancer, pancreatic cancer, bladder cancer and breast cancer. | 3.23 | 1 | 0 | organofluorine compound; pyrimidine 2'-deoxyribonucleoside | antimetabolite; antineoplastic agent; antiviral drug; DNA synthesis inhibitor; EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor; environmental contaminant; immunosuppressive agent; photosensitizing agent; prodrug; radiosensitizing agent; xenobiotic |
| ibutilide ibutilide: RN & structure in first source; RN refers to the fumarate salt | 3.23 | 1 | 0 | benzenes; organic amino compound | |
| aripiprazole Aripiprazole: A piperazine and quinolone derivative that is used primarily as an antipsychotic agent. It is a partial agonist of SEROTONIN RECEPTOR, 5-HT1A and DOPAMINE D2 RECEPTORS, where it also functions as a post-synaptic antagonist, and an antagonist of SEROTONIN RECEPTOR, 5-HT2A. It is used for the treatment of SCHIZOPHRENIA and BIPOLAR DISORDER, and as an adjunct therapy for the treatment of depression.. aripiprazole : An N-arylpiperazine that is piperazine substituted by a 4-[(2-oxo-1,2,3,4-tetrahydroquinolin-7-yl)oxy]butyl group at position 1 and by a 2,3-dichlorophenyl group at position 4. It is an antipsychotic drug used for the treatment of Schizophrenia, and other mood disorders. | 3.23 | 1 | 0 | aromatic ether; delta-lactam; dichlorobenzene; N-alkylpiperazine; N-arylpiperazine; quinolone | drug metabolite; H1-receptor antagonist; second generation antipsychotic; serotonergic agonist |
| remifentanil Remifentanil: A piperidine-propionate derivative and opioid analgesic structurally related to FENTANYL. It functions as a short-acting MU OPIOID RECEPTOR agonist, and is used as an analgesic during induction or maintenance of general anesthesia, following surgery, during childbirth, and in mechanically ventilated patients under intensive care.. remifentanil : A piperidinecarboxylate ester that is methyl piperidine-4-carboxylate in which the hydrogen attached to the nitrogen is substituted by a 3-methoxy-3-oxopropyl group and the hydrogen at position 4 is substituted the nitrogen of N-propanoylaniline. | 3.23 | 1 | 0 | alpha-amino acid ester; anilide; monocarboxylic acid amide; piperidinecarboxylate ester | intravenous anaesthetic; mu-opioid receptor agonist; opioid analgesic; sedative |
| atorvastatin [no description available] | 3.23 | 1 | 0 | aromatic amide; dihydroxy monocarboxylic acid; monofluorobenzenes; pyrroles; statin (synthetic) | environmental contaminant; xenobiotic |
| lamivudine [no description available] | 3.23 | 1 | 0 | monothioacetal; nucleoside analogue; oxacycle; primary alcohol | allergen; anti-HBV agent; antiviral drug; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor; HIV-1 reverse transcriptase inhibitor; prodrug |
| duloxetine [no description available] | 3.23 | 1 | 0 | duloxetine | |
| irinotecan [no description available] | 3.23 | 1 | 0 | carbamate ester; delta-lactone; N-acylpiperidine; pyranoindolizinoquinoline; ring assembly; tertiary alcohol; tertiary amino compound | antineoplastic agent; apoptosis inducer; EC 5.99.1.2 (DNA topoisomerase) inhibitor; prodrug |
| valsartan Valsartan: A tetrazole derivative and ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to treat HYPERTENSION.. valsartan : A monocarboxylic acid amide consisting of L-valine in which the amino hydrogens have been replaced by a pentanoyl and a [2'-(1H-tetrazol-5-yl)biphenyl]-4-yl]methyl group. It exhibits antihypertensive activity. | 3.23 | 1 | 0 | biphenylyltetrazole; monocarboxylic acid amide; monocarboxylic acid | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| ibandronic acid Ibandronic Acid: Aminobisphosphonate that is a potent inhibitor of BONE RESORPTION. It is used in the treatment of HYPERCALCEMIA associated with malignancy, for the prevention of fracture and bone complications in patients with breast cancer and bone metastases, and for the treatment and prevention of POSTMENOPAUSAL OSTEOPOROSIS. | 3.23 | 1 | 0 | ||
| ziprasidone ziprasidone: a benzisothiazoylpiperazine derivative; has combined dopamine and serotonin receptor antagonist activity; structurally related to tiospirone. ziprasidone : A piperazine compound having 1,2-benzothiazol-3-yl- and 2-(6-chloro-1,3-dihydro-2-oxindol-5-yl)ethyl substituents attached to the nitrogen atoms. | 3.23 | 1 | 0 | 1,2-benzisothiazole; indolones; organochlorine compound; piperazines | antipsychotic agent; dopaminergic antagonist; histamine antagonist; muscarinic antagonist; psychotropic drug; serotonergic antagonist |
| zolmitriptan zolmitriptan: an antimigraine compound; a serotonin (5HT)-1D receptor agonist. zolmitriptan : A member of the class of tryptamines that is N,N-dimethyltryptamine in which the hydrogen at position 5 of the indole ring has been replaced by a [(4S)-2-oxo-1,3-oxazolidin-4-yl]methyl group. A serotonin 5-HT1 B and D receptor agonist, it is used for the treatment of migraine. | 3.23 | 1 | 0 | oxazolidinone; tryptamines | anti-inflammatory drug; serotonergic agonist; vasoconstrictor agent |
| emtricitabine Emtricitabine: A deoxycytidine analog and REVERSE TRANSCRIPTASE INHIBITOR with antiviral activity against HIV-1 and HEPATITIS B viruses. It is used to treat HIV INFECTIONS.. emtricitabine : An organofluorine compound that is 5-fluorocytosine substituted at the 1 position by a 2-(hydroxymethyl)-1,3-oxathiolan-5-yl group (2R,5S configuration). It is used in combination therapy for the treatment of HIV-1 infection. | 3.23 | 1 | 0 | monothioacetal; nucleoside analogue; organofluorine compound; pyrimidone | antiviral drug; HIV-1 reverse transcriptase inhibitor |
| tasosartan tasosartan: angiotensin II antagonist; structure given in first source | 3.23 | 1 | 0 | biphenyls | |
| tiludronic acid tiludronic acid: a bone resorption inhibitor; an antihypercalcemic agent; used in the tratment of Paget's disease; used in the treatment and prevention of osteoporosis; structure given in first source | 3.23 | 1 | 0 | organochlorine compound | |
| tirofiban Tirofiban: Tyrosine analog and PLATELET GLYCOPROTEIN GPIIB-IIIA COMPLEX antagonist that inhibits PLATELET AGGREGATION and is used in the treatment of ACUTE CORONARY SYNDROME.. tirofiban : A member of the class of piperidines that is L-tyrosine in which a hydrogen attached to the amino group is replaced by a butylsulfonyl group and in which the hydrogen attached to the phenolic hydroxy group is replaced by a 4-(piperidin-4-yl)butyl group. | 3.23 | 1 | 0 | L-tyrosine derivative; piperidines; sulfonamide | anticoagulant; fibrin modulating drug; platelet glycoprotein-IIb/IIIa receptor antagonist |
| capecitabine Capecitabine: A deoxycytidine derivative and fluorouracil PRODRUG that is used as an ANTINEOPLASTIC ANTIMETABOLITE in the treatment of COLON CANCER; BREAST CANCER and GASTRIC CANCER.. capecitabine : A carbamate ester that is cytidine in which the hydrogen at position 5 is replaced by fluorine and in which the amino group attached to position 4 is converted into its N-(penyloxy)carbonyl derivative. Capecitabine is a antineoplastic agent used in the treatment of cancers. | 3.23 | 1 | 0 | carbamate ester; cytidines; organofluorine compound | antimetabolite; antineoplastic agent; prodrug |
| adenosine quinquefolan B: isolated from roots of Panax quinquefolium L.; RN not in Chemline 10/87; RN from Toxlit | 3.23 | 1 | 0 | adenosines; purines D-ribonucleoside | analgesic; anti-arrhythmia drug; fundamental metabolite; human metabolite; vasodilator agent |
| trovafloxacin trovafloxacin: a trifluoronaphthyridone derivative of 7-(3-azabicyclo(3.1.0)hexyl)naphthyridone; has antineoplastic activity. trovafloxacin : A 1,8-naphthyridine derivative that is 4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid bearing additional 2,4-difluorophenyl, fluoro and 6-amino-3-azabicyclo[3.1.0]hex-3-yl substituents at positions 1, 6 and 7 respectively. A broad-spectrum antibiotic that was withdrawn from the market due to risk of liver failure. | 3.23 | 1 | 0 | ||
| cefprozil [no description available] | 3.23 | 1 | 0 | cephalosporin; semisynthetic derivative | antibacterial drug |
| efavirenz efavirenz: HIV-1 reverse transcriptase inhibitor. efavirenz : 1,4-Dihydro-2H-3,1-benzoxazin-2-one substituted at the 4 position by cyclopropylethynyl and trifluoromethyl groups (S configuration) and at the 6 position by chlorine. A non-nucleoside reverse transcriptase inhibitor with activity against HIV, it is used with other antiretrovirals for combination therapy of HIV infection. | 3.23 | 1 | 0 | acetylenic compound; benzoxazine; cyclopropanes; organochlorine compound; organofluorine compound | antiviral drug; HIV-1 reverse transcriptase inhibitor |
| nelfinavir Nelfinavir: A potent HIV protease inhibitor. It is used in combination with other antiviral drugs in the treatment of HIV in both adults and children.. nelfinavir : An aryl sulfide that is used (as its mesylate salt) for treatment of HIV and also exhibits some anticancer properties. | 3.23 | 1 | 0 | aryl sulfide; benzamides; organic heterobicyclic compound; phenols; secondary alcohol; tertiary amino compound | antineoplastic agent; HIV protease inhibitor |
| fenofibric acid fenofibric acid: RN given refers to parent cpd without isomeric designation; structure. fenofibric acid : A monocarboxylic acid that is 2-methylpropanoic acid substituted by a 4-(4-chlorobenzoyl)phenoxy group at position 2. It is a metabolite of the drug fenofibrate. | 3.23 | 1 | 0 | aromatic ketone; chlorobenzophenone; monocarboxylic acid | drug metabolite; marine xenobiotic metabolite |
| plerixafor plerixafor: a bicyclam derivate, highly potent & selective inhibitor of HIV-1 & HIV-2. plerixafor : An azamacrocycle consisting of two cyclam rings connected by a 1,4-phenylenebis(methylene) linker. It is a CXCR4 chemokine receptor antagonist and a hematopoietic stem cell mobilizer. It is used in combination with grulocyte-colony stimulating factor (G-CSF) to mobilize hematopoietic stem cells to the perpheral blood for collection and subsequent autologous transplantation in patients with non-Hodgkin's lymphoma and multiple myeloma. | 3.59 | 2 | 0 | azacycloalkane; azamacrocycle; benzenes; crown amine; secondary amino compound; tertiary amino compound | anti-HIV agent; antineoplastic agent; C-X-C chemokine receptor type 4 antagonist; immunological adjuvant |
| amprenavir [no description available] | 3.23 | 1 | 0 | carbamate ester; sulfonamide; tetrahydrofuryl ester | antiviral drug; HIV protease inhibitor |
| oseltamivir Oseltamivir: An acetamido cyclohexene that is a structural homolog of SIALIC ACID and inhibits NEURAMINIDASE.. oseltamivir : A cyclohexenecarboxylate ester that is the ethyl ester of oseltamivir acid. An antiviral prodrug (it is hydrolysed to the active free carboxylic acid in the liver), it is used to slow the spread of influenza. | 3.23 | 1 | 0 | acetamides; amino acid ester; cyclohexenecarboxylate ester; primary amino compound | antiviral drug; EC 3.2.1.18 (exo-alpha-sialidase) inhibitor; environmental contaminant; prodrug; xenobiotic |
| histamine phosphate histamine phosphate : A phosphate salt that is the diphosphate salt of histamine. | 3.23 | 1 | 0 | phosphate salt | histamine agonist |
| tilbroquinol [no description available] | 3.23 | 1 | 0 | organohalogen compound; quinolines | |
| bendamustine [no description available] | 3.23 | 1 | 0 | benzimidazoles | |
| droxicam droxicam: structure given in first source. droxicam : An organic heterotricyclic compound that is 2H,5H-[1,3]oxazino[5,6-c][1,2]benzothiazine-2,4(3H)-dione 6,6-dioxide substituted at positions 3 and 5 by pyridin-2-yl and methyl groups respectively. A prodrug of piroxicam, it is used for the relief of pain and inflammation in musculoskeletal disorders such as rheumatoid arthritis and osteoarthritis. | 3.23 | 1 | 0 | organic heterotricyclic compound; pyridines | cyclooxygenase 1 inhibitor; hepatotoxic agent; non-narcotic analgesic; non-steroidal anti-inflammatory drug; platelet aggregation inhibitor; prodrug |
| milnacipran Milnacipran: A cyclopropanecarboxamide serotonin and norepinephrine reuptake inhibitor (SNRI) that is used in the treatment of FIBROMYALGIA. | 2.05 | 1 | 0 | acetamides | |
| ebrotidine ebrotidine: an H2-receptor antagonist and gastric mucosa protector | 3.23 | 1 | 0 | sulfonamide | |
| repaglinide [no description available] | 3.23 | 1 | 0 | piperidines | |
| telmisartan Telmisartan: A biphenyl compound and benzimidazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION.. telmisartan : A member of the class of benzimidazoles used widely in the treatment of hypertension. | 3.23 | 1 | 0 | benzimidazoles; biphenyls; carboxybiphenyl | angiotensin receptor antagonist; antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; environmental contaminant; xenobiotic |
| triazoles Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms. | 2.05 | 1 | 0 | 1,2,3-triazole | |
| sertraline Sertraline: A selective serotonin uptake inhibitor that is used in the treatment of depression.. sertraline : A member of the class of tetralins that is tetralin which is substituted at positions 1 and 4 by a methylamino and a 3,4-dichlorophenyl group, respectively (the S,S diastereoisomer). A selective serotonin-reuptake inhibitor (SSRI), it is administered orally as the hydrochloride salt as an antidepressant for the treatment of depression, obsessive-compulsive disorder, panic disorder and post-traumatic stress disorder. | 3.23 | 1 | 0 | dichlorobenzene; secondary amino compound; tetralins | antidepressant; serotonin uptake inhibitor |
| zoledronic acid Zoledronic Acid: An imidobisphosphonate inhibitor of BONE RESORPTION that is used for the treatment of malignancy-related HYPERCALCEMIA; OSTEITIS DEFORMANS; and OSTEOPOROSIS.. zoledronic acid : An imidazole compound having a 2,2-bis(phosphono)-2-hydroxyethane-1-yl substituent at the 1-position. | 3.23 | 1 | 0 | 1,1-bis(phosphonic acid); imidazoles | bone density conservation agent |
| acamprosate Acamprosate: Structural analog of taurine that is used for the prevention of relapse in individuals with ALCOHOLISM.. acamprosate : An organosulfonic acid that is propane-1-sulfonic acid substituted by an acetylamino group at position 3. | 3.23 | 1 | 0 | acetamides; organosulfonic acid | environmental contaminant; neurotransmitter agent; xenobiotic |
| isaxonine isaxonine: promotes nerve growth | 3.23 | 1 | 0 | aminopyrimidine | |
| nebivolol 2,2'-iminobis[1-(6-fluoro-3,4-dihydro-2H-chromen-2-yl)ethanol] : A member of the class of chromanes that is 2,2'-iminodiethanol in which one hydrogen attached to each hydroxy-bearing carbon is replaced by a 6-fluorochroman-2-yl group. | 3.23 | 1 | 0 | chromanes; diol; organofluorine compound; secondary alcohol; secondary amino compound | |
| uk 68798 [no description available] | 3.23 | 1 | 0 | aromatic ether; sulfonamide; tertiary amino compound | anti-arrhythmia drug; potassium channel blocker |
| hp 873 iloperidone: an atypical, negative symptom antipsychotic agent. iloperidone : A member of the class of piperidines that is the 4-acetyl-2-methoxyphenyl ether of 3-(piperidin-1-yl)propan-1-ol which is substituted at position 4 of the piperidine ring by a 6-fluoro-1,2-benzoxazol-3-yl group. A member of the group of second generation antipsychotics (also known as an atypical antipsychotics), it is used for the treatment of schizophrenia. | 3.23 | 1 | 0 | 1,2-benzoxazoles; aromatic ether; aromatic ketone; methyl ketone; monoamine; organofluorine compound; piperidines; tertiary amino compound | dopaminergic antagonist; second generation antipsychotic; serotonergic antagonist |
| dexrazoxane Dexrazoxane: The (+)-enantiomorph of razoxane. | 3.23 | 1 | 0 | razoxane | antineoplastic agent; cardiovascular drug; chelator; immunosuppressive agent |
| fenoxypropazine [no description available] | 3.23 | 1 | 0 | aromatic ether | |
| voriconazole Voriconazole: A triazole antifungal agent that specifically inhibits STEROL 14-ALPHA-DEMETHYLASE and CYTOCHROME P-450 CYP3A.. voriconazole : A triazole-based antifungal agent used for the treatment of esophageal candidiasis, invasive pulmonary aspergillosis, and serious fungal infections caused by Scedosporium apiospermum and Fusarium spp. It is an inhibitor of cytochrome P450 2C9 (CYP2C9) and CYP3A4. | 3.23 | 1 | 0 | conazole antifungal drug; difluorobenzene; pyrimidines; tertiary alcohol; triazole antifungal drug | P450 inhibitor |
| aceclofenac [no description available] | 3.23 | 1 | 0 | amino acid; carboxylic ester; dichlorobenzene; monocarboxylic acid; secondary amino compound | EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| nitrefazole [no description available] | 3.23 | 1 | 0 | imidazoles | |
| doripenem Doripenem: A carbapenem derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of infections such as HOSPITAL-ACQUIRED PNEUMONIA, and complicated intra-abdominal or urinary-tract infections, including PYELONEPHRITIS. | 3.23 | 1 | 0 | carbapenems | |
| atovaquone Atovaquone: A hydroxynaphthoquinone that has antimicrobial activity and is being used in antimalarial protocols.. atovaquone : A naphthoquinone compound having a 4-(4-chlorophenyl)cyclohexyl group at the 2-position and a hydroxy substituent at the 3-position. | 3.23 | 1 | 0 | hydroxy-1,2-naphthoquinone | |
| rivastigmine [no description available] | 3.23 | 1 | 0 | carbamate ester; tertiary amino compound | cholinergic drug; EC 3.1.1.8 (cholinesterase) inhibitor; neuroprotective agent |
| frovatriptan [no description available] | 3.23 | 1 | 0 | carbazoles | |
| eletriptan eletriptan: 5-HT(1B/1D) receptor agonist; structure in first source. eletriptan : An N-alkylpyrrolidine, that is N-methylpyrrolidine in which the pro-R hydrogen at position 2 is replaced by a {5-[2-(phenylsulfonyl)ethyl]-1H-indol-3-yl}methyl group. | 3.23 | 1 | 0 | indoles; N-alkylpyrrolidine; sulfone | non-steroidal anti-inflammatory drug; serotonergic agonist; vasoconstrictor agent |
| rosiglitazone [no description available] | 3.23 | 1 | 0 | aminopyridine; thiazolidinediones | EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor; ferroptosis inhibitor; insulin-sensitizing drug |
| bexarotene [no description available] | 3.23 | 1 | 0 | benzoic acids; naphthalenes; retinoid | antineoplastic agent |
| clarithromycin Clarithromycin: A semisynthetic macrolide antibiotic derived from ERYTHROMYCIN that is active against a variety of microorganisms. It can inhibit PROTEIN SYNTHESIS in BACTERIA by reversibly binding to the 50S ribosomal subunits. This inhibits the translocation of aminoacyl transfer-RNA and prevents peptide chain elongation.. clarithromycin : The 6-O-methyl ether of erythromycin A, clarithromycin is a macrolide antibiotic used in the treatment of respiratory-tract, skin and soft-tissue infections. It is also used to eradicate Helicobacter pylori in the treatment of peptic ulcer disease. It prevents bacteria from growing by interfering with their protein synthesis. | 3.23 | 1 | 0 | macrolide antibiotic | antibacterial drug; environmental contaminant; protein synthesis inhibitor; xenobiotic |
| moexipril [no description available] | 3.23 | 1 | 0 | peptide | |
| mci 9038 [no description available] | 3.23 | 1 | 0 | peptide | |
| fulvestrant Fulvestrant: An estradiol derivative and estrogen receptor antagonist that is used for the treatment of estrogen receptor-positive, locally advanced or metastatic breast cancer.. fulvestrant : A 3-hydroxy steroid that is 17beta-estradiol in which the 7alpha hydrogen has been replaced by a nonyl group in which one of the hydrogens of the terminal methyl has been replaced by a (4,4,5,5,5-pentafluoropentyl)sulfinyl group. An estrogen receptor antagonist, it is used in the treatment of breast cancer. | 3.23 | 1 | 0 | 17beta-hydroxy steroid; 3-hydroxy steroid; organofluorine compound; sulfoxide | antineoplastic agent; estrogen antagonist; estrogen receptor antagonist |
| bosentan anhydrous Bosentan: A sulfonamide and pyrimidine derivative that acts as a dual endothelin receptor antagonist used to manage PULMONARY HYPERTENSION and SYSTEMIC SCLEROSIS. | 3.23 | 1 | 0 | primary alcohol; pyrimidines; sulfonamide | antihypertensive agent; endothelin receptor antagonist |
| perindopril Perindopril: An angiotensin-converting enzyme inhibitor. It is used in patients with hypertension and heart failure.. perindopril : An alpha-amino acid ester that is the ethyl ester of N-{(2S)-1-[(2S,3aS,7aS)-2-carboxyoctahydro-1H-indol-1-yl]-1-oxopropan-2-yl}-L-norvaline | 3.23 | 1 | 0 | alpha-amino acid ester; dicarboxylic acid monoester; ethyl ester; organic heterobicyclic compound | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor |
| tadalafil [no description available] | 10.01 | 2 | 1 | benzodioxoles; pyrazinopyridoindole | EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor; vasodilator agent |
| paliperidone 3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one : A member of the class of pyridopyrimidines that is 9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one carrying an additional 2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl group at position 2.. paliperidone : A racemate comprising equimolar amounts of (R)- and (S)-paliperidone. Paliperidone is the primary active metabolite of the older antipsychotic risperidone and is used for treatment of schizophrenia. | 3.23 | 1 | 0 | 1,2-benzoxazoles; heteroarylpiperidine; organofluorine compound; pyridopyrimidine; secondary alcohol | |
| nitisinone [no description available] | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; C-nitro compound; cyclohexanones; mesotrione | EC 1.13.11.27 (4-hydroxyphenylpyruvate dioxygenase) inhibitor |
| clofarabine [no description available] | 3.23 | 1 | 0 | adenosines; organofluorine compound | antimetabolite; antineoplastic agent |
| pramipexole Pramipexole: A benzothiazole derivative and dopamine agonist with antioxidant properties that is used in the treatment of PARKINSON DISEASE and RESTLESS LEGS SYNDROME.. pramipexole : A member of the class of benzothiazoles that is 4,5,6,7-tetrahydro-1,3-benzothiazole in which the hydrogens at the 2 and 6-pro-S-positions are substituted by amino and propylamino groups, respectively. | 3.23 | 1 | 0 | benzothiazoles; diamine | antidyskinesia agent; antiparkinson drug; dopamine agonist; radical scavenger |
| valdecoxib [no description available] | 3.23 | 1 | 0 | isoxazoles; sulfonamide | antipyretic; antirheumatic drug; cyclooxygenase 2 inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| almotriptan almotriptan : An indole compound having a 2-(dimethylamino)ethyl group at the 3-position and a (pyrrolidin-1-ylsulfonyl)methyl group at the 5-position. | 3.23 | 1 | 0 | indoles; sulfonamide; tertiary amine | non-steroidal anti-inflammatory drug; serotonergic agonist; vasoconstrictor agent |
| gefitinib [no description available] | 3.23 | 1 | 0 | aromatic ether; monochlorobenzenes; monofluorobenzenes; morpholines; quinazolines; secondary amino compound; tertiary amino compound | antineoplastic agent; epidermal growth factor receptor antagonist |
| desloratadine desloratadine: major metabolite of loratadine. desloratadine : Loratadine in which the ethoxycarbonyl group attached to the piperidine ring is replaced by hydrogen. The major metabolite of loratidine, desloratadine is an antihistamine which is used for the symptomatic relief of allergic conditions including rhinitis and chronic urticaria. It does not readily enter the central nervous system, so does not cause drowsiness. | 3.23 | 1 | 0 | benzocycloheptapyridine | anti-allergic agent; cholinergic antagonist; drug metabolite; H1-receptor antagonist |
| desvenlafaxine O-desmethylvenlafaxine : A tertiary amino compound that is N,N-dimethylethanamine substituted at position 1 by a 1-hydroxycyclohexyl and 4-hydroxyphenyl group. It is a metabolite of the drug venlafaxine. | 3.23 | 1 | 0 | cyclohexanols; phenols; tertiary amino compound | antidepressant; drug metabolite; marine xenobiotic metabolite |
| methotrexate [no description available] | 3.23 | 1 | 0 | dicarboxylic acid; monocarboxylic acid amide; pteridines | abortifacient; antimetabolite; antineoplastic agent; antirheumatic drug; dermatologic drug; DNA synthesis inhibitor; EC 1.5.1.3 (dihydrofolate reductase) inhibitor; immunosuppressive agent |
| tamsulosin [no description available] | 10.91 | 2 | 1 | 5-(2-{[2-(2-ethoxyphenoxy)ethyl]amino}propyl)-2-methoxybenzenesulfonamide | alpha-adrenergic antagonist; antineoplastic agent |
| rufinamide rufinamide: for treatment of Lennox-Gastaut syndrome; structure in first source | 3.59 | 2 | 0 | aromatic amide; heteroarene | |
| olmesartan medoxomil Olmesartan Medoxomil: An ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to manage HYPERTENSION. | 3.23 | 1 | 0 | biphenyls | |
| dexpanthenol dexpanthenol: The alcohol of pantothenic acid | 3.23 | 1 | 0 | amino alcohol; monocarboxylic acid amide | cholinergic drug; provitamin |
| fosamprenavir fosamprenavir: a prodrug of the protease inhibitor amprenavir. fosamprenavir : A sulfonamide with a structure based on that of sulfanilamide substituted on the sulfonamide nitrogen by a (2R,3S)-4-phenyl-2-(phosphonooxy)-3-({[(3S)-tetrahydrofuran-3-yloxy]carbonyl}amino)butyl group. It is a pro-drug of the HIV protease inhibitor and antiretroviral drug amprenavir. | 3.23 | 1 | 0 | sulfonamide | prodrug |
| febuxostat Febuxostat: A thiazole derivative and inhibitor of XANTHINE OXIDASE that is used for the treatment of HYPERURICEMIA in patients with chronic GOUT.. febuxostat : A 1,3-thiazolemonocarboxylic acid that is 4-methyl-1,3-thiazole-5-carboxylic acid which is substituted by a 3-cyano-4-(2-methylpropoxy)phenyl group at position 2. It is an orally-active, potent, and selective xanthine oxidase inhibitor used for the treatment of chronic hyperuricaemia in patients with gout. | 3.59 | 2 | 0 | 1,3-thiazolemonocarboxylic acid; aromatic ether; nitrile | EC 1.17.3.2 (xanthine oxidase) inhibitor |
| escitalopram Escitalopram: S-enantiomer of CITALOPRAM. Belongs to a class of drugs known as SELECTIVE SEROTONIN REUPTAKE INHIBITORS, used to treat depression and generalized anxiety disorder.. escitalopram : A 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile that has S-configuration at the chiral centre. It is the active enantiomer of citalopram. | 3.23 | 1 | 0 | 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile | antidepressant; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor |
| 10-propargyl-10-deazaaminopterin 10-propargyl-10-deazaaminopterin: structure in first source. pralatrexate : A pteridine that is the N-4-[1-(2,4-diaminopteridin-6-yl)pent-4-yn-2-yl]benzoyl derivative of L-glutamic acid. Used for treatment of Peripheral T-Cell Lymphoma, an aggressive form of non-Hodgkins lymphoma. | 3.23 | 1 | 0 | N-acyl-L-glutamic acid; pteridines; terminal acetylenic compound | antimetabolite; antineoplastic agent; EC 1.5.1.3 (dihydrofolate reductase) inhibitor |
| docetaxel anhydrous Docetaxel: A semisynthetic analog of PACLITAXEL used in the treatment of locally advanced or metastatic BREAST NEOPLASMS and NON-SMALL CELL LUNG CANCER.. docetaxel anhydrous : A tetracyclic diterpenoid that is paclitaxel with the N-benzyloxycarbonyl group replaced by N-tert-butoxycarbonyl, and the acetoxy group at position 10 replaced by a hydroxy group. | 3.23 | 1 | 0 | secondary alpha-hydroxy ketone; tetracyclic diterpenoid | antimalarial; antineoplastic agent; photosensitizing agent |
| atazanavir atazanavir : A heavily substituted carbohydrazide that is an antiretroviral drug of the protease inhibitor (PI) class used to treat infection of human immunodeficiency virus (HIV). | 3.23 | 1 | 0 | carbohydrazide | antiviral drug; HIV protease inhibitor |
| levofloxacin Levofloxacin: The L-isomer of Ofloxacin.. levofloxacin : An optically active form of ofloxacin having (S)-configuration; an inhibitor of bacterial topoisomerase IV and DNA gyrase. | 3.23 | 1 | 0 | 9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid; fluoroquinolone antibiotic; quinolone antibiotic | antibacterial drug; DNA synthesis inhibitor; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; topoisomerase IV inhibitor |
| ezetimibe Ezetimibe: An azetidine derivative and ANTICHOLESTEREMIC AGENT that inhibits intestinal STEROL absorption. It is used to reduce total CHOLESTEROL; LDL CHOLESTEROL, and APOLIPOPROTEINS B in the treatment of HYPERLIPIDEMIAS.. ezetimibe : A beta-lactam that is azetidin-2-one which is substituted at 1, 3, and 4 by p-fluorophenyl, 3-(p-fluorophenyl)-3-hydroxypropyl, and 4-hydroxyphenyl groups, respectively (the 3R,3'S,4S enantiomer). | 3.23 | 1 | 0 | azetidines; beta-lactam; organofluorine compound | anticholesteremic drug; antilipemic drug; antimetabolite |
| ertapenem Ertapenem: A carbapenem derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of Gram-positive and Gram-negative bacterial infections including intra-abdominal infections, acute gynecological infections, complicated urinary tract infections, skin infections, and respiratory tract infections. It is also used to prevent infection in colorectal surgery.. ertapenem : Meropenem in which the one of the two methyl groups attached to the amide nitrogen is replaced by hydrogen while the other is replaced by a 3-carboxyphenyl group. The sodium salt is used for the treatment of moderate to severe susceptible infections including intra-abdominal and acute gynaecological infections, pneumonia, and infections of the skin and of the urinary tract. | 3.23 | 1 | 0 | carbapenemcarboxylic acid; pyrrolidinecarboxamide | antibacterial drug |
| cox 189 lumiracoxib: a COX-2 inhibitor. lumiracoxib : An amino acid that is phenylacetic acid which is substituted at position 2 by the nitrogen of 2-chloro-6-fluoroaniline and at position 5 by a methyl group. A highly selective cyclooxygenase 2 inhibitor, it was briefly used for the treatment of osteoarthritis, but was withdrawn due to concersns of hepatotoxicity. | 3.23 | 1 | 0 | amino acid; monocarboxylic acid; organochlorine compound; organofluorine compound; secondary amino compound | cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug |
| conivaptan conivaptan : The amide resulting from the formal condensation of 4-[(biphenyl-2-ylcarbonyl)amino]benzoic acid with the benzazepine nitrogen of 2-methyl-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepine. It is an antagonist for two of the three types of arginine vasopressin (AVP) receptors, V1a and V2. It is used as its hydrochloride salt for the treatment of hyponatraemia (low blood sodium levels) caused by syndrome of inappropriate antidiuretic hormone (SIADH). | 3.23 | 1 | 0 | benzazepine | aquaretic; vasopressin receptor antagonist |
| moxifloxacin Moxifloxacin: A fluoroquinolone that acts as an inhibitor of DNA TOPOISOMERASE II and is used as a broad-spectrum antibacterial agent.. moxifloxacin : A quinolone that consists of 4-oxo-1,4-dihydroquinoline-3-carboxylic acid bearing a cyclopropyl substituent at position 1, a fluoro substitiuent at position 6, a (4aS,7aS)-octahydro-6H-pyrrolo[3,4-b]pyridin-6-yl group at position 7 and a methoxy substituent at position 8. A member of the fluoroquinolone class of antibacterial agents. | 4.97 | 2 | 1 | aromatic ether; cyclopropanes; fluoroquinolone antibiotic; pyrrolidinopiperidine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone | antibacterial drug |
| pralnacasan pralnacasan: NSAID, ICE inhibitor & metastasis inhibitor; RN & structure in first source | 3.23 | 1 | 0 | ||
| clevidipine clevidipine: a calcium channel blocker and antihypertensive agent; structure in first source | 3.23 | 1 | 0 | dihydropyridine | |
| solifenacin [no description available] | 3.23 | 1 | 0 | isoquinolines | |
| dexmethylphenidate dexmethylphenidate : A methyl phenyl(piperidin-2-yl)acetate in which both stereocentres have R configuration. It is the active enantiomer in the racemic drug methylphenidate. | 3.23 | 1 | 0 | methyl phenyl(piperidin-2-yl)acetate | adrenergic agent |
| naproxen Naproxen: An anti-inflammatory agent with analgesic and antipyretic properties. Both the acid and its sodium salt are used in the treatment of rheumatoid arthritis and other rheumatic or musculoskeletal disorders, dysmenorrhea, and acute gout.. naproxen : A methoxynaphthalene that is 2-methoxynaphthalene substituted by a carboxy ethyl group at position 6. Naproxen is a non-steroidal anti-inflammatory drug commonly used for the reduction of pain, fever, inflammation and stiffness caused by conditions such as osteoarthritis, kidney stones, rheumatoid arthritis, psoriatic arthritis, gout, ankylosing spondylitis, menstrual cramps, tendinitis, bursitis, and for the treatment of primary dysmenorrhea. It works by inhibiting both the COX-1 and COX-2 enzymes. | 3.23 | 1 | 0 | methoxynaphthalene; monocarboxylic acid | antipyretic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; drug allergen; environmental contaminant; gout suppressant; non-narcotic analgesic; non-steroidal anti-inflammatory drug; xenobiotic |
| cinacalcet cinacalcet : A secondary amino compound that is (1R)-1-(naphthalen-1-yl)ethanamine in which one of the hydrogens attached to the nitrogen is substituted by a 3-[3-(trifluoromethyl)phenyl]propyl group. | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; naphthalenes; secondary amino compound | calcimimetic; P450 inhibitor |
| lubiprostone [no description available] | 3.23 | 1 | 0 | ||
| telbivudine [no description available] | 3.23 | 1 | 0 | pyrimidine 2'-deoxyribonucleoside | antiviral drug; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor |
| paromomycin Paromomycin: An aminoglycoside antibacterial and antiprotozoal agent produced by species of STREPTOMYCES.. paromomycin : An amino cyclitol glycoside that is the 1-O-(2-amino-2-deoxy-alpha-D-glucopyranoside) and the 3-O-(2,6-diamino-2,6-dideoxy-beta-L-idopyranosyl)-beta-D-ribofuranoside of 4,6-diamino-2,3-dihydroxycyclohexane (the 1R,2R,3S,4R,6S diastereoisomer). It is obtained from various Streptomyces species. A broad-spectrum antibiotic, it is used (generally as the sulfate salt) for the treatment of acute and chronic intestinal protozoal infections, but is not effective for extraintestinal protozoal infections. It is also used as a therapeutic against visceral leishmaniasis. | 3.23 | 1 | 0 | amino cyclitol glycoside; aminoglycoside antibiotic | anthelminthic drug; antibacterial drug; antiparasitic agent; antiprotozoal drug |
| anidulafungin Anidulafungin: Echinocandin antifungal agent that is used in the treatment of CANDIDEMIA and CANDIDIASIS.. anidulafungin : A semisynthetic echinocandin anti-fungal drug. It is active against Aspergillus and Candida species and is used for the treatment of invasive candidiasis. | 3.23 | 1 | 0 | antibiotic antifungal drug; azamacrocycle; echinocandin; heterodetic cyclic peptide; semisynthetic derivative | |
| 17 alpha-hydroxyprogesterone caproate 17 alpha-Hydroxyprogesterone Caproate: Hydroxyprogesterone derivative that acts as a PROGESTIN and is used to reduce the risk of recurrent MISCARRIAGE and of PREMATURE BIRTH. It is also used in combination with ESTROGEN in the management of MENSTRUATION DISORDERS. | 3.23 | 1 | 0 | corticosteroid hormone | |
| varenicline Varenicline: A benzazepine derivative that functions as an ALPHA4-BETA2 NICOTINIC RECEPTOR partial agonist. It is used for SMOKING CESSATION.. varenicline : An organic heterotetracyclic compound that acts as a partial agonist for nicotinic cholinergic receptors and is used (in the form of its tartate salt) as an aid to giving up smoking. | 3.23 | 1 | 0 | ||
| fiduxosin fiduxosin: fiduxosin (ABT-980) is the (3aR,9bR)-isomer; structure in first source | 3.23 | 1 | 0 | ||
| atropine tropan-3alpha-yl 3-hydroxy-2-phenylpropanoate : A tropane alkaloid that is (1R,5)-8-methyl-8-azabicyclo[3.2.1]octane substituted by a (3-hydroxy-2-phenylpropanoyl)oxy group at position 3. | 3.23 | 1 | 0 | ||
| erlotinib [no description available] | 3.23 | 1 | 0 | aromatic ether; quinazolines; secondary amino compound; terminal acetylenic compound | antineoplastic agent; epidermal growth factor receptor antagonist; protein kinase inhibitor |
| etravirine [no description available] | 3.23 | 1 | 0 | aminopyrimidine; aromatic ether; dinitrile; organobromine compound | antiviral agent; HIV-1 reverse transcriptase inhibitor |
| dronedarone Dronedarone: A non-iodinated derivative of amiodarone that is used for the treatment of ARRHYTHMIA.. dronedarone : A member of the class of 1-benzofurans used for the treatment of cardiac arrhythmias. | 3.23 | 1 | 0 | 1-benzofurans; aromatic ether; aromatic ketone; sulfonamide; tertiary amino compound | anti-arrhythmia drug; environmental contaminant; xenobiotic |
| ramelteon ramelteon: melatonin MT1/MT2 receptor agonist | 3.23 | 1 | 0 | indanes | |
| lapatinib [no description available] | 3.23 | 1 | 0 | furans; organochlorine compound; organofluorine compound; quinazolines | antineoplastic agent; tyrosine kinase inhibitor |
| darunavir Darunavir: An HIV PROTEASE INHIBITOR that is used in the treatment of AIDS and HIV INFECTIONS. Due to the emergence of ANTIVIRAL DRUG RESISTANCE when used alone, it is administered in combination with other ANTI-HIV AGENTS.. darunavir : An N,N-disubstituted benzenesulfonamide bearing an unsubstituted amino group at the 4-position, used for the treatment of HIV infection. A second-generation HIV protease inhibitor, darunavir was designed to form robust interactions with the protease enzyme from many strains of HIV, including those from treatment-experienced patients with multiple resistance mutations to other protease inhibitors. | 3.23 | 1 | 0 | carbamate ester; furofuran; sulfonamide | antiviral drug; HIV protease inhibitor |
| deferasirox Deferasirox: A triazole and benzoate derivative that acts as a selective iron chelator. It is used in the management of chronic IRON OVERLOAD due to blood transfusion or non-transfusion dependent THALASSEMIA.. deferasirox : A member of the class of triazoles, deferasirox is 1,2,4-triazole substituted by a 4-carboxyphenyl group at position 1 and by 2-hydroxyphenyl groups at positions 3 and 5. An orally active iron chelator, it is used to manage chronic iron overload in patients receiving long-term blood transfusions. | 3.23 | 1 | 0 | benzoic acids; monocarboxylic acid; phenols; triazoles | iron chelator |
| tbc-11251 sitaxsentan: endothelin A receptor antagonist; structure in first source | 3.23 | 1 | 0 | benzodioxoles | |
| tolvaptan [no description available] | 3.59 | 2 | 0 | benzazepine; benzenedicarboxamide | aquaretic; vasopressin receptor antagonist |
| sorafenib [no description available] | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; aromatic ether; monochlorobenzenes; phenylureas; pyridinecarboxamide | angiogenesis inhibitor; anticoronaviral agent; antineoplastic agent; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; ferroptosis inducer; tyrosine kinase inhibitor |
| lenalidomide [no description available] | 3.23 | 1 | 0 | aromatic amine; dicarboximide; isoindoles; piperidones | angiogenesis inhibitor; antineoplastic agent; immunomodulator |
| solifenacin succinate Solifenacin Succinate: A quinuclidine and tetrahydroisoquinoline derivative and selective M3 MUSCARINIC ANTAGONIST. It is used as a UROLOGIC AGENT in the treatment of URINARY INCONTINENCE. | 11.48 | 27 | 3 | isoquinolines | |
| regadenoson [no description available] | 3.23 | 1 | 0 | purine nucleoside | |
| lacosamide Lacosamide: An acetamide derivative that acts as a blocker of VOLTAGE-GATED SODIUM CHANNELS. It is used as an anticonvulsant, for adjunctive or monotherapy, in the treatment of PARTIAL SEIZURES. | 3.59 | 2 | 0 | N-acyl-amino acid | |
| vincaleukoblastine [no description available] | 3.23 | 1 | 0 | acetate ester; indole alkaloid fundamental parent; methyl ester; organic heteropentacyclic compound; organic heterotetracyclic compound; tertiary alcohol; tertiary amino compound; vinca alkaloid | antineoplastic agent; immunosuppressive agent; microtubule-destabilising agent; plant metabolite |
| benzofurans Benzofurans: Compounds that contain a BENZENE ring fused to a furan ring. | 8.84 | 12 | 1 | ||
| benzarone benzarone: antihemorrhagic agent; structure | 3.23 | 1 | 0 | 1-benzofurans | |
| estramustine Estramustine: A nitrogen mustard linked to estradiol, usually as phosphate; used to treat prostatic neoplasms; also has radiation protective properties.. estramustine : A carbamate ester obtained by the formal condensation of the hydroxy group of 17beta-estradiol with the carboxy group of bis(2-chloroethyl)carbamic acid. | 3.23 | 1 | 0 | 17beta-hydroxy steroid; carbamate ester; organochlorine compound | alkylating agent; antineoplastic agent; radiation protective agent |
| bortezomib [no description available] | 3.23 | 1 | 0 | amino acid amide; L-phenylalanine derivative; pyrazines | antineoplastic agent; antiprotozoal drug; protease inhibitor; proteasome inhibitor |
| ritonavir Ritonavir: An HIV protease inhibitor that works by interfering with the reproductive cycle of HIV. It also inhibits CYTOCHROME P-450 CYP3A.. ritonavir : An L-valine derivative that is L-valinamide in which alpha-amino group has been acylated by a [(2-isopropyl-1,3-thiazol-4-yl)methyl]methylcarbamoyl group and in which a hydrogen of the carboxamide amino group has been replaced by a (2R,4S,5S)-4-hydroxy-1,6-diphenyl-5-{[(1,3-thiazol-5-ylmethoxy)carbonyl]amino}hexan-2-yl group. A CYP3A inhibitor and antiretroviral drug from the protease inhibitor class used to treat HIV infection and AIDS, it is often used as a fixed-dose combination with another protease inhibitor, lopinavir. Also used in combination with dasabuvir sodium hydrate, ombitasvir and paritaprevir (under the trade name Viekira Pak) for treatment of chronic hepatitis C virus genotype 1 infection as well as cirrhosis of the liver. | 3.23 | 1 | 0 | 1,3-thiazoles; carbamate ester; carboxamide; L-valine derivative; ureas | antiviral drug; environmental contaminant; HIV protease inhibitor; xenobiotic |
| oxytocin Oxytocin: A nonapeptide hormone released from the neurohypophysis (PITUITARY GLAND, POSTERIOR). It differs from VASOPRESSIN by two amino acids at residues 3 and 8. Oxytocin acts on SMOOTH MUSCLE CELLS, such as causing UTERINE CONTRACTIONS and MILK EJECTION.. oxytocin : A cyclic nonapeptide hormone with amino acid sequence CYIQNCPLG that also acts as a neurotransmitter in the brain; the principal uterine-contracting and milk-ejecting hormone of the posterior pituitary. Together with the neuropeptide vasopressin, it is believed to influence social cognition and behaviour. | 3.23 | 1 | 0 | heterodetic cyclic peptide; peptide hormone | oxytocic; vasodilator agent |
| pentostatin Pentostatin: A potent inhibitor of ADENOSINE DEAMINASE. The drug induces APOPTOSIS of LYMPHOCYTES, and is used in the treatment of many lymphoproliferative malignancies, particularly HAIRY CELL LEUKEMIA. It is also synergistic with some other antineoplastic agents and has immunosuppressive activity.. pentostatin : A member of the class of coformycins that is coformycin in which the hydroxy group at position 2' is replaced with a hydrogen. It is a drug used for the treatment of hairy cell leukaemia. | 3.23 | 1 | 0 | coformycins | antimetabolite; antineoplastic agent; Aspergillus metabolite; bacterial metabolite; EC 3.5.4.4 (adenosine deaminase) inhibitor |
| quinidine Quinidine: An optical isomer of quinine, extracted from the bark of the CHINCHONA tree and similar plant species. This alkaloid dampens the excitability of cardiac and skeletal muscles by blocking sodium and potassium currents across cellular membranes. It prolongs cellular ACTION POTENTIALS, and decreases automaticity. Quinidine also blocks muscarinic and alpha-adrenergic neurotransmission.. quinidine : A cinchona alkaloid consisting of cinchonine with the hydrogen at the 6-position of the quinoline ring substituted by methoxy. | 3.23 | 1 | 0 | cinchona alkaloid | alpha-adrenergic antagonist; anti-arrhythmia drug; antimalarial; drug allergen; EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor; EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor; muscarinic antagonist; P450 inhibitor; potassium channel blocker; sodium channel blocker |
| meropenem Meropenem: A thienamycin derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of bacterial infections, including infections in immunocompromised patients.. meropenem : A carbapenemcarboxylic acid in which the azetidine and pyrroline rings carry 1-hydroxymethyl and in which the azetidine and pyrroline rings carry 1-hydroxymethyl and 5-(dimethylcarbamoyl)pyrrolidin-3-ylthio substituents respectively. | 3.23 | 1 | 0 | alpha,beta-unsaturated monocarboxylic acid; carbapenemcarboxylic acid; organic sulfide; pyrrolidinecarboxamide | antibacterial agent; antibacterial drug; drug allergen |
| griseofulvin Griseofulvin: An antifungal agent used in the treatment of TINEA infections.. griseofulvin : An oxaspiro compound produced by Penicillium griseofulvum. It is used by mouth as an antifungal drug for infections involving the scalp, hair, nails and skin that do not respond to topical treatment. | 3.23 | 1 | 0 | 1-benzofurans; antibiotic antifungal drug; benzofuran antifungal drug; organochlorine compound; oxaspiro compound | antibacterial agent; Penicillium metabolite |
| cefoxitin Cefoxitin: A semisynthetic cephamycin antibiotic resistant to beta-lactamase.. cefoxitin : A semisynthetic cephamycin antibiotic which, in addition to the methoxy group at the 7alpha position, has 2-thienylacetamido and carbamoyloxymethyl side-groups. It is resistant to beta-lactamase. | 3.23 | 1 | 0 | beta-lactam antibiotic allergen; cephalosporin; cephamycin; semisynthetic derivative | antibacterial drug |
| saquinavir Saquinavir: An HIV protease inhibitor which acts as an analog of an HIV protease cleavage site. It is a highly specific inhibitor of HIV-1 and HIV-2 proteases, and also inhibits CYTOCHROME P-450 CYP3A.. saquinavir : An aspartic acid derivative obtained by formal condensation of the primary amino group of (2S,3R)-4-[(3S,4aS,8aS)-3-(tert-butylcarbamoyl)octahydroisoquinolin-2(1H)-yl]-3-hydroxy-1-phenylbutan-2-ylamine with the carboxy group of N(2)(-quinolin-2-ylcarbonyl)-L-asparagine. An inhibitor of HIV-1 protease. | 3.23 | 1 | 0 | L-asparagine derivative; quinolines | antiviral drug; HIV protease inhibitor |
| pancuronium Pancuronium: A bis-quaternary steroid that is a competitive nicotinic antagonist. As a neuromuscular blocking agent it is more potent than CURARE but has less effect on the circulatory system and on histamine release.. pancuronium : A steroid ester in which a 5alpha-androstane skeleton is C-3alpha- and C-17beta-disubstituted with acetoxy groups and 2beta- and 16beta-disubstituted with 1-methylpiperidinium-1-yl groups. It is a non-depolarizing curare-mimetic muscle relaxant. | 3.23 | 1 | 0 | acetate ester; steroid ester | cholinergic antagonist; muscle relaxant; nicotinic antagonist |
| abacavir abacavir: a carbocyclic nucleoside with potent selective anti-HIV activity. abacavir : A 2,6-diaminopurine that is (1S)-cyclopent-2-en-1-ylmethanol in which the pro-R hydrogen at the 4-position is substituted by a 2-amino-6-(cyclopropylamino)-9H-purin-9-yl group. A nucleoside analogue reverse transcriptase inhibitor (NRTI) with antiretroviral activity against HIV, it is used (particularly as the sulfate) with other antiretrovirals in combination therapy of HIV infection. | 3.23 | 1 | 0 | 2,6-diaminopurines | antiviral drug; drug allergen; HIV-1 reverse transcriptase inhibitor |
| miglitol [no description available] | 3.23 | 1 | 0 | piperidines | |
| metyrosine alpha-methyl-L-tyrosine : An L-tyrosine derivative that consists of L-tyrosine bearing an additional methyl substituent at position 2. An inhibitor of the enzyme tyrosine 3-monooxygenase, and consequently of the synthesis of catecholamines. It is used to control the symptoms of excessive sympathetic stimulation in patients with pheochromocytoma. | 3.23 | 1 | 0 | L-tyrosine derivative; non-proteinogenic L-alpha-amino acid | antihypertensive agent; EC 1.14.16.2 (tyrosine 3-monooxygenase) inhibitor |
| linezolid [no description available] | 3.23 | 1 | 0 | acetamides; morpholines; organofluorine compound; oxazolidinone | antibacterial drug; protein synthesis inhibitor |
| clindamycin phosphate [no description available] | 3.23 | 1 | 0 | ||
| eplerenone Eplerenone: A spironolactone derivative and selective ALDOSTERONE RECEPTOR antagonist that is used in the management of HYPERTENSION and CONGESTIVE HEART FAILURE, post-MYOCARDIAL INFARCTION. | 3.23 | 1 | 0 | 3-oxo-Delta(4) steroid; epoxy steroid; gamma-lactone; methyl ester; organic heteropentacyclic compound; oxaspiro compound; steroid acid ester | aldosterone antagonist; antihypertensive agent |
| tolterodine [no description available] | 3.23 | 1 | 0 | tertiary amine | antispasmodic drug; muscarinic antagonist; muscle relaxant |
| darifenacin darifenacin : 2-[(3S)-1-Ethylpyrrolidin-3-yl]-2,2-diphenylacetamide in which one of the hydrogens at the 2-position of the ethyl group is substituted by a 2,3-dihydro-1-benzofuran-5-yl group. It is a selective antagonist for the M3 muscarinic acetylcholine receptor, which is primarily responsible for bladder muscle contractions, and is used as the hydrobromide salt in the management of urinary incontinence. | 14.06 | 13 | 1 | 1-benzofurans; monocarboxylic acid amide; pyrrolidines | antispasmodic drug; muscarinic antagonist |
| tretinoin Tretinoin: An important regulator of GENE EXPRESSION during growth and development, and in NEOPLASMS. Tretinoin, also known as retinoic acid and derived from maternal VITAMIN A, is essential for normal GROWTH; and EMBRYONIC DEVELOPMENT. An excess of tretinoin can be teratogenic. It is used in the treatment of PSORIASIS; ACNE VULGARIS; and several other SKIN DISEASES. It has also been approved for use in promyelocytic leukemia (LEUKEMIA, PROMYELOCYTIC, ACUTE).. retinoic acid : A retinoid consisting of 3,7-dimethylnona-2,4,6,8-tetraenoic acid substituted at position 9 by a 2,6,6-trimethylcyclohex-1-en-1-yl group (geometry of the four exocyclic double bonds is not specified).. all-trans-retinoic acid : A retinoic acid in which all four exocyclic double bonds have E- (trans-) geometry. | 3.23 | 1 | 0 | retinoic acid; vitamin A | anti-inflammatory agent; antineoplastic agent; antioxidant; AP-1 antagonist; human metabolite; keratolytic drug; retinoic acid receptor agonist; retinoid X receptor agonist; signalling molecule |
| retinol Vitamin A: Retinol and derivatives of retinol that play an essential role in metabolic functioning of the retina, the growth of and differentiation of epithelial tissue, the growth of bone, reproduction, and the immune response. Dietary vitamin A is derived from a variety of CAROTENOIDS found in plants. It is enriched in the liver, egg yolks, and the fat component of dairy products.. vitamin A : Any member of a group of fat-soluble retinoids produced via metabolism of provitamin A carotenoids that exhibit biological activity against vitamin A deficiency. Vitamin A is involved in immune function, vision, reproduction, and cellular communication.. all-trans-retinol : A retinol in which all four exocyclic double bonds have E- (trans-) geometry.. retinol : A retinoid consisting of 3,7-dimethylnona-2,4,6,8-tetraen-1-ol substituted at position 9 by a 2,6,6-trimethylcyclohex-1-en-1-yl group (geometry of the four exocyclic double bonds is not specified). | 3.23 | 1 | 0 | retinol; vitamin A | human metabolite; mouse metabolite; plant metabolite |
| tacrolimus Tacrolimus: A macrolide isolated from the culture broth of a strain of Streptomyces tsukubaensis that has strong immunosuppressive activity in vivo and prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation in vitro.. tacrolimus (anhydrous) : A macrolide lactam containing a 23-membered lactone ring, originally isolated from the fermentation broth of a Japanese soil sample that contained the bacteria Streptomyces tsukubaensis. | 3.23 | 1 | 0 | macrolide lactam | bacterial metabolite; immunosuppressive agent |
| rosuvastatin rosuvastatin : A dihydroxy monocarboxylic acid that is (6E)-7-{4-(4-fluorophenyl)-2-[methyl(methylsulfonyl)amino]-6-(propan-2-yl)pyrimidin-5-yl} hept-6-enoic acid carrying two hydroxy substituents at positions 3 and 5 (the 3R,5S-diastereomer). | 3.23 | 1 | 0 | dihydroxy monocarboxylic acid; monofluorobenzenes; pyrimidines; statin (synthetic); sulfonamide | anti-inflammatory agent; antilipemic drug; cardioprotective agent; CETP inhibitor; environmental contaminant; xenobiotic |
| mycophenolic acid Mycophenolic Acid: Compound derived from Penicillium stoloniferum and related species. It blocks de novo biosynthesis of purine nucleotides by inhibition of the enzyme inosine monophosphate dehydrogenase (IMP DEHYDROGENASE). Mycophenolic acid exerts selective effects on the immune system in which it prevents the proliferation of T-CELLS, LYMPHOCYTES, and the formation of antibodies from B-CELLS. It may also inhibit recruitment of LEUKOCYTES to sites of INFLAMMATION.. mycophenolate : A monocarboxylic acid anion resulting from the removal of a proton from the carboxy group of mycophenolic acid.. mycophenolic acid : A member of the class of 2-benzofurans that is 2-benzofuran-1(3H)-one which is substituted at positions 4, 5, 6, and 7 by methyl, methoxy, (2E)-5-carboxy-3-methylpent-2-en-1-yl, and hydroxy groups, respectively. It is an antibiotic produced by Penicillium brevi-compactum, P. stoloniferum, P. echinulatum and related species. An immunosuppressant, it is widely used (partiularly as its sodium salt and as the 2-(morpholin-4-yl)ethyl ester prodrug, mycophenolate mofetil) to prevent tissue rejection following organ transplants and for the treatment of certain autoimmune diseases. | 3.23 | 1 | 0 | 2-benzofurans; gamma-lactone; monocarboxylic acid; phenols | anticoronaviral agent; antimicrobial agent; antineoplastic agent; EC 1.1.1.205 (IMP dehydrogenase) inhibitor; environmental contaminant; immunosuppressive agent; mycotoxin; Penicillium metabolite; xenobiotic |
| clindamycin Clindamycin: An antibacterial agent that is a semisynthetic analog of LINCOMYCIN.. clindamycin : A carbohydrate-containing antibiotic that is the semisynthetic derivative of lincomycin, a natural antibiotic. | 3.23 | 1 | 0 | ||
| fosfomycin Fosfomycin: An antibiotic produced by Streptomyces fradiae.. fosfomycin : A phosphonic acid having an (R,S)-1,2-epoxypropyl group attached to phosphorus. | 3.23 | 1 | 0 | epoxide; phosphonic acids | antimicrobial agent; EC 2.5.1.7 (UDP-N-acetylglucosamine 1-carboxyvinyltransferase) inhibitor |
| zithromax Azithromycin: A semi-synthetic macrolide antibiotic structurally related to ERYTHROMYCIN. It has been used in the treatment of Mycobacterium avium intracellulare infections, toxoplasmosis, and cryptosporidiosis.. azithromycin : A macrolide antibiotic useful for the treatment of bacterial infections. | 3.23 | 1 | 0 | macrolide antibiotic | antibacterial drug; environmental contaminant; xenobiotic |
| octreotide [no description available] | 3.23 | 1 | 0 | ||
| eptifibatide [no description available] | 3.23 | 1 | 0 | homodetic cyclic peptide; macrocycle; organic disulfide | anticoagulant; platelet aggregation inhibitor |
| decitabine [no description available] | 3.23 | 1 | 0 | 2'-deoxyribonucleoside | |
| teniposide [no description available] | 3.23 | 1 | 0 | aromatic ether; beta-D-glucoside; cyclic acetal; furonaphthodioxole; gamma-lactone; monosaccharide derivative; phenols; thiophenes | antineoplastic agent; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor |
| dactinomycin Dactinomycin: A compound composed of a two CYCLIC PEPTIDES attached to a phenoxazine that is derived from STREPTOMYCES parvullus. It binds to DNA and inhibits RNA synthesis (transcription), with chain elongation more sensitive than initiation, termination, or release. As a result of impaired mRNA production, protein synthesis also declines after dactinomycin therapy. (From AMA Drug Evaluations Annual, 1993, p2015) | 3.23 | 1 | 0 | actinomycin | mutagen |
| melphalan Melphalan: An alkylating nitrogen mustard that is used as an antineoplastic in the form of the levo isomer - MELPHALAN, the racemic mixture - MERPHALAN, and the dextro isomer - MEDPHALAN; toxic to bone marrow, but little vesicant action; potential carcinogen.. melphalan : A phenylalanine derivative comprising L-phenylalanine having [bis(2-chloroethyl)amino group at the 4-position on the phenyl ring. | 3.23 | 1 | 0 | L-phenylalanine derivative; nitrogen mustard; non-proteinogenic L-alpha-amino acid; organochlorine compound | alkylating agent; antineoplastic agent; carcinogenic agent; drug allergen; immunosuppressive agent |
| tenofovir tenofovir (anhydrous) : A member of the class of phosphonic acids that is methylphosphonic acid in which one of the methyl hydrogens is replaced by a [(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy group. An inhibitor of HIV-1 reverse transcriptase, the bis(isopropyloxycarbonyloxymethyl) ester (disoproxil ester) prodrug is used as the fumaric acid salt in combination therapy for the treatment of HIV infection. | 3.23 | 1 | 0 | nucleoside analogue; phosphonic acids | antiviral drug; drug metabolite; HIV-1 reverse transcriptase inhibitor |
| posaconazole [no description available] | 3.23 | 1 | 0 | aromatic ether; conazole antifungal drug; N-arylpiperazine; organofluorine compound; oxolanes; triazole antifungal drug; triazoles | trypanocidal drug |
| micafungin Micafungin: A cyclic lipo-hexapeptide echinocandin antifungal agent that is used for the treatment and prevention of CANDIDIASIS.. micafungin : A cyclic hexapeptide echinocandin antibiotic which exerts its effect by inhibiting the synthesis of 1,3-beta-D-glucan, an integral component of the fungal cell wall. It is used as the sodium salt for the treatment of invasive candidiasis, and of aspergillosis in patients who are intolerant of other therapy. | 3.23 | 1 | 0 | antibiotic antifungal drug; echinocandin | antiinfective agent |
| riboflavin vitamin B2 : Any member of a group of vitamers that belong to the chemical structural class called flavins that exhibit biological activity against vitamin B2 deficiency. Symptoms associated with vitamin B2 deficiency include glossitis, seborrhea, angular stomaitis, cheilosis and photophobia. The vitamers include riboflavin and its phosphate derivatives (and includes their salt, ionised and hydrate forms). | 3.23 | 1 | 0 | flavin; vitamin B2 | anti-inflammatory agent; antioxidant; cofactor; Escherichia coli metabolite; food colouring; fundamental metabolite; human urinary metabolite; mouse metabolite; photosensitizing agent; plant metabolite |
| sodium bicarbonate Sodium Bicarbonate: A white, crystalline powder that is commonly used as a pH buffering agent, an electrolyte replenisher, systemic alkalizer and in topical cleansing solutions. | 3.23 | 1 | 0 | one-carbon compound; organic sodium salt | antacid; food anticaking agent |
| arsenic trioxide Tetraarsenic Oxide: A form of As2O3 that exists as As4O6 in the solid state. It dissociates to As2O3 upon heating to the vapor phase above 800 degrees Celsius. | 3.23 | 1 | 0 | arsenic oxide | antineoplastic agent; insecticide |
| sr 90107 fondaparinux sodium : An organic sodium salt, being the decasodium salt of fondaparinux. | 3.23 | 1 | 0 | ||
| meglumine iodipamide [no description available] | 3.23 | 1 | 0 | organoammonium salt | radioopaque medium |
| thyrotropin-releasing hormone PR 546: no other info available 9/89. protirelin : A tripeptide composed of L-pyroglutamyl, L-histidyl and L-prolinamide residues joined in sequence. | 3.23 | 1 | 0 | peptide hormone; tripeptide | human metabolite |
| arginine vasopressin Arginine Vasopressin: The predominant form of mammalian antidiuretic hormone. It is a nonapeptide containing an ARGININE at residue 8 and two disulfide-linked cysteines at residues of 1 and 6. Arg-vasopressin is used to treat DIABETES INSIPIDUS or to improve vasomotor tone and BLOOD PRESSURE.. argipressin : The predominant form of mammalian vasopressin (antidiuretic hormone). It is a nonapeptide containing an arginine at residue 8 and two disulfide-linked cysteines at residues of 1 and 6. | 3.23 | 1 | 0 | vasopressin | cardiovascular drug; hematologic agent; mitogen |
| s 1033 [no description available] | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; imidazoles; pyridines; pyrimidines; secondary amino compound; secondary carboxamide | anticoronaviral agent; antineoplastic agent; tyrosine kinase inhibitor |
| propylthiouracil Propylthiouracil: A thiourea antithyroid agent. Propythiouracil inhibits the synthesis of thyroxine and inhibits the peripheral conversion of throxine to tri-iodothyronine. It is used in the treatment of hyperthyroidism. (From Martindale, The Extra Pharmacopeoia, 30th ed, p534). 6-propyl-2-thiouracil : A pyrimidinethione consisting of uracil in which the 2-oxo group is substituted by a thio group and the hydrogen at position 6 is substituted by a propyl group. | 3.23 | 1 | 0 | pyrimidinethione | antidote to paracetamol poisoning; antimetabolite; antioxidant; antithyroid drug; carcinogenic agent; EC 1.14.13.39 (nitric oxide synthase) inhibitor; hormone antagonist |
| etomidate Etomidate: Imidazole derivative anesthetic and hypnotic with little effect on blood gases, ventilation, or the cardiovascular system. It has been proposed as an induction anesthetic.. etomidate : The ethyl ester of 1-[(1R)-1-phenylethyl]-1H-imidazole-5-carboxylic acid. It is an intravenous general anaesthetic with no analgesic activity. | 3.23 | 1 | 0 | ethyl ester; imidazoles | intravenous anaesthetic; sedative |
| mercaptopurine Mercaptopurine: An antimetabolite antineoplastic agent with immunosuppressant properties. It interferes with nucleic acid synthesis by inhibiting purine metabolism and is used, usually in combination with other drugs, in the treatment of or in remission maintenance programs for leukemia.. purine-6-thiol : A thiol that is the tautomer of mercaptopurine.. mercaptopurine : A member of the class of purines that is 6,7-dihydro-1H-purine carrying a thione group at position 6. An adenine analogue, it is used in the treatment of acute lymphocytic leukemia (ALL), chronic myeloid leukemia (CML), Crohn's disease, and ulcerative colitis. | 3.23 | 1 | 0 | aryl thiol; purines; thiocarbonyl compound | anticoronaviral agent; antimetabolite; antineoplastic agent |
| pyrantel Pyrantel: A depolarizing neuromuscular-blocking agent, that causes persistent nicotinic activation resulting in spastic paralysis of susceptible nematodes. It is a drug of second-choice after benzimidazoles for treatment of ascariasis, hookworm, and pinworm infections, being effective after a single dose. (From Smith and Reynard, Textbook of Pharmacology, 1992, p920). pyrantel : A carboxamidine that is 1,4,5,6-tetrahydropyrimidine that is substituted at position 1 by a methyl group and at position 2 by an (E)-2-(2-thienyl)vinyl group. It is used, particularly as the embonate [4,4'-methylenebis(3-hydroxy-2-naphthoate)] salt, as an anthelmintic that is effective against intestinal nematodes including threadworms, roundworms and hookworms, and is included in the WHO 'Model List of Essential Medicines'. | 3.23 | 1 | 0 | 1,4,5,6-tetrahydropyrimidines; carboxamidine; thiophenes | antinematodal drug |
| thiothixene [no description available] | 3.23 | 1 | 0 | N-methylpiperazine | anticoronaviral agent |
| eszopiclone Eszopiclone: A pyridine, pyrazine, and piperazine derivative that is used as a HYPNOTIC AND SEDATIVE in the treatment of INSOMNIA.. eszopiclone : The (5S)- (active) enantiomer of zopiclone. Unlike almost all other hypnotic sedatives, which are approved only for the relief of short-term (6-8 weeks) insomnia, eszopiclone is approved by the U.S. Food and Drug Administration for long-term use. | 3.23 | 1 | 0 | zopiclone | central nervous system depressant; sedative |
| benztropine Benztropine: A centrally active muscarinic antagonist that has been used in the symptomatic treatment of PARKINSON DISEASE. Benztropine also inhibits the uptake of dopamine.. benzatropine : Tropane in which a hydrogen at position 3 is substituted by a diphenylmethoxy group (endo-isomer). An acetylcholine receptor antagonist, it is used (particularly as its methanesulphonate salt) in the treatment of Parkinson's disease, and to reduce parkinsonism and akathisia side effects of antipsychotic treatments. | 3.23 | 1 | 0 | diarylmethane | |
| methimazole Methimazole: A thioureylene antithyroid agent that inhibits the formation of thyroid hormones by interfering with the incorporation of iodine into tyrosyl residues of thyroglobulin. This is done by interfering with the oxidation of iodide ion and iodotyrosyl groups through inhibition of the peroxidase enzyme.. methimazole : A member of the class of imidazoles that it imidazole-2-thione in which a methyl group replaces the hydrogen which is attached to a nitrogen. | 3.23 | 1 | 0 | 1,3-dihydroimidazole-2-thiones | antithyroid drug |
| sulindac Sulindac: A sulfinylindene derivative prodrug whose sulfinyl moiety is converted in vivo to an active NSAID analgesic. Specifically, the prodrug is converted by liver enzymes to a sulfide which is excreted in the bile and then reabsorbed from the intestine. This helps to maintain constant blood levels with reduced gastrointestinal side effects.. sulindac : A monocarboxylic acid that is 1-benzylidene-1H-indene which is substituted at positions 2, 3, and 5 by methyl, carboxymethyl, and fluorine respectively, and in which the phenyl group of the benzylidene moiety is substituted at the para position by a methylsulfinyl group. It is a prodrug for the corresponding sulfide, a non-steroidal anti-inflammatory drug, used particularly in the treatment of acute and chronic inflammatory conditions. | 3.23 | 1 | 0 | monocarboxylic acid; organofluorine compound; sulfoxide | analgesic; antineoplastic agent; antipyretic; apoptosis inducer; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug; prodrug; tocolytic agent |
| terbinafine [no description available] | 3.23 | 1 | 0 | acetylenic compound; allylamine antifungal drug; enyne; naphthalenes; tertiary amine | EC 1.14.13.132 (squalene monooxygenase) inhibitor; P450 inhibitor; sterol biosynthesis inhibitor |
| thioguanine anhydrous Thioguanine: An antineoplastic compound which also has antimetabolite action. The drug is used in the therapy of acute leukemia.. tioguanine : A 2-aminopurine that is the 6-thiono derivative of 2-amino-1,9-dihydro-6H-purine. Incorporates into DNA and inhibits synthesis. Used in the treatment of leukaemia. | 3.23 | 1 | 0 | 2-aminopurines | anticoronaviral agent; antimetabolite; antineoplastic agent |
| succimer Succimer: A mercaptodicarboxylic acid used as an antidote to heavy metal poisoning because it forms strong chelates with them.. succimer : A sulfur-containing carboxylic acid that is succinic acid bearing two mercapto substituents at positions 2 and 3. A lead chelator used as an antedote to lead poisoning. | 3.23 | 1 | 0 | dicarboxylic acid; dithiol; sulfur-containing carboxylic acid | chelator |
| digoxin Digoxin: A cardiotonic glycoside obtained mainly from Digitalis lanata; it consists of three sugars and the aglycone DIGOXIGENIN. Digoxin has positive inotropic and negative chronotropic activity. It is used to control ventricular rate in ATRIAL FIBRILLATION and in the management of congestive heart failure with atrial fibrillation. Its use in congestive heart failure and sinus rhythm is less certain. The margin between toxic and therapeutic doses is small. (From Martindale, The Extra Pharmacopoeia, 30th ed, p666). digoxin : A cardenolide glycoside that is digitoxin beta-hydroxylated at C-12. A cardiac glycoside extracted from the foxglove plant, Digitalis lanata, it is used to control ventricular rate in atrial fibrillation and in the management of congestive heart failure with atrial fibrillation, but the margin between toxic and therapeutic doses is small. | 3.23 | 1 | 0 | cardenolide glycoside; steroid saponin | anti-arrhythmia drug; cardiotonic drug; EC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor; epitope |
| streptozocin [no description available] | 3.23 | 1 | 0 | ||
| tamoxifen [no description available] | 3.23 | 1 | 0 | stilbenoid; tertiary amino compound | angiogenesis inhibitor; antineoplastic agent; bone density conservation agent; EC 1.2.3.1 (aldehyde oxidase) inhibitor; EC 2.7.11.13 (protein kinase C) inhibitor; estrogen antagonist; estrogen receptor antagonist; estrogen receptor modulator |
| ethionamide Ethionamide: A second-line antitubercular agent that inhibits mycolic acid synthesis.. ethionamide : A thiocarboxamide that is pyridine-4-carbothioamide substituted by an ethyl group at position 2. A prodrug that undergoes metabolic activation by conversion to the corresponding S-oxide. | 3.23 | 1 | 0 | pyridines; thiocarboxamide | antilipemic drug; antitubercular agent; fatty acid synthesis inhibitor; leprostatic drug; prodrug |
| cancidas [no description available] | 3.23 | 1 | 0 | ||
| lincomycin Lincomycin: An antibiotic produced by Streptomyces lincolnensis var. lincolnensis. It has been used in the treatment of staphylococcal, streptococcal, and Bacteroides fragilis infections.. lincomycin : A carbohydrate-containing antibiotic produced by the actinomyces Streptomyces lincolnensis. | 3.23 | 1 | 0 | carbohydrate-containing antibiotic; L-proline derivative; monocarboxylic acid amide; pyrrolidinecarboxamide; S-glycosyl compound | antimicrobial agent; bacterial metabolite |
| ranitidine Ranitidine: A non-imidazole blocker of those histamine receptors that mediate gastric secretion (H2 receptors). It is used to treat gastrointestinal ulcers.. ranitidine : A member of the class of furans used to treat peptic ulcer disease (PUD) and gastroesophageal reflux disease. | 3.23 | 1 | 0 | C-nitro compound; furans; organic sulfide; tertiary amino compound | anti-ulcer drug; drug allergen; environmental contaminant; H2-receptor antagonist; xenobiotic |
| aplaviroc aplaviroc: a spiro-diketo-piperazine; a potent noncompetitive allosteric antagonist of the CCR5 receptor with concomitantly potent antiviral effects for HIV-1; structure in first source | 3.23 | 1 | 0 | ||
| hmr 3647 [no description available] | 3.23 | 1 | 0 | ||
| maraviroc [no description available] | 3.23 | 1 | 0 | tropane alkaloid | |
| toremifene Toremifene: A first generation selective estrogen receptor modulator (SERM). Like TAMOXIFEN, it is an estrogen agonist for bone tissue and cholesterol metabolism but is antagonistic on mammary and uterine tissue. | 3.23 | 1 | 0 | aromatic ether; organochlorine compound; tertiary amine | antineoplastic agent; bone density conservation agent; estrogen antagonist; estrogen receptor modulator |
| nelarabine nelarabine: prodrug of ara-G. nelarabine : A purine nucleoside in which O-methylguanine is attached to arabinofuranose via a beta-N(9)-glycosidic bond. Inhibits DNA synthesis and causes cell death; a prodrug of 9-beta-D-arabinofuranosylguanine (ara-G). | 3.23 | 1 | 0 | beta-D-arabinoside; monosaccharide derivative; purine nucleoside | antineoplastic agent; DNA synthesis inhibitor; prodrug |
| dermatan sulfate Dermatan Sulfate: A naturally occurring glycosaminoglycan found mostly in the skin and in connective tissue. It differs from CHONDROITIN SULFATE A (see CHONDROITIN SULFATES) by containing IDURONIC ACID in place of glucuronic acid, its epimer, at carbon atom 5. (from Merck, 12th ed). alpha-L-IdopA-(1->3)-beta-D-GalpNAc4S : An oligosaccharide sulfate that is 2-acetamido-2-deoxy-4-O-sulfo-beta-D-galactopyranose in which the hydroxy group at position 3 has been converted to the corresponding alpha-L-idopyranuronoside.. dermatan sulfate : Any of a group of glycosaminoglycans with repeating units consisting of variously sulfated beta1->4-linked L-iduronyl-(alpha1->3)-N-acetyl-D-galactosamine units. | 3.23 | 1 | 0 | amino disaccharide; glycosylgalactose derivative; iduronic acids; oligosaccharide sulfate | |
| dolasetron [no description available] | 3.23 | 1 | 0 | indolyl carboxylic acid | |
| orlistat Orlistat: A lactone derivative of LEUCINE that acts as a pancreatic lipase inhibitor to limit the absorption of dietary fat; it is used in the management of obesity.. orlistat : A carboxylic ester resulting from the formal condensation of the carboxy group of N-formyl-L-leucine with the hydroxy group of (3S,4S)-3-hexyl-4-[(2S)-2-hydroxytridecyl]oxetan-2-one. A pancreatic lipase inhibitor, it is used as an anti-obesity drug. | 3.23 | 1 | 0 | beta-lactone; carboxylic ester; formamides; L-leucine derivative | anti-obesity agent; bacterial metabolite; EC 2.3.1.85 (fatty acid synthase) inhibitor; EC 3.1.1.3 (triacylglycerol lipase) inhibitor |
| quinine [no description available] | 3.23 | 1 | 0 | cinchona alkaloid | antimalarial; muscle relaxant; non-narcotic analgesic |
| fospropofol [no description available] | 3.23 | 1 | 0 | alkylbenzene | |
| rasagiline [no description available] | 3.23 | 1 | 0 | indanes; secondary amine; terminal acetylenic compound | EC 1.4.3.4 (monoamine oxidase) inhibitor; neuroprotective agent |
| dasatinib N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-1,3-thiazole-5-carboxamide: a dasatinib prodrug; structure in first source. dasatinib (anhydrous) : An aminopyrimidine that is 2-methylpyrimidine which is substituted at position 4 by the primary amino group of 2-amino-1,3-thiazole-5-carboxylic acid and at position 6 by a 4-(2-hydroxyethyl)piperazin-1-yl group, and in which the carboxylic acid group has been formally condensed with 2-chloro-6-methylaniline to afford the corresponding amide. A multi-targeted kinase inhibitor, it is used, particularly as the monohydrate, for the treatment of chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia. Note that the name 'dasatinib' is used to refer to the monohydrate (USAN) as well as to anhydrous dasatinib (INN). | 3.23 | 1 | 0 | 1,3-thiazoles; aminopyrimidine; monocarboxylic acid amide; N-(2-hydroxyethyl)piperazine; N-arylpiperazine; organochlorine compound; secondary amino compound; tertiary amino compound | anticoronaviral agent; antineoplastic agent; tyrosine kinase inhibitor |
| sitagliptin sitagliptin : A triazolopyrazine that exhibits hypoglycemic activity. | 3.23 | 1 | 0 | triazolopyrazine; trifluorobenzene | EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor; environmental contaminant; hypoglycemic agent; serine proteinase inhibitor; xenobiotic |
| tolcapone Tolcapone: A benzophenone and nitrophenol compound that acts as an inhibitor of CATECHOL O-METHYLTRANSFERASE, an enzyme involved in the metabolism of DOPAMINE and LEVODOPA. It is used in the treatment of PARKINSON DISEASE in patients for whom levodopa is ineffective or contraindicated.. tolcapone : Benzophenone substituted on one of the phenyl rings at C-3 and C-4 by hydroxy groups and at C-5 by a nitro group, and on the other phenyl ring by a methyl group at C-4. It is an inhibitor of catechol O-methyltransferase. | 3.23 | 1 | 0 | 2-nitrophenols; benzophenones; catechols | antiparkinson drug; EC 2.1.1.6 (catechol O-methyltransferase) inhibitor |
| calcitriol dihydroxy-vitamin D3: as a major in vitro metabolite of 1alpha,25-dihydroxyvitamin D3, produced in primary cultures of neonatal human keratinocytes | 3.23 | 1 | 0 | D3 vitamins; hydroxycalciol; triol | antineoplastic agent; antipsoriatic; bone density conservation agent; calcium channel agonist; calcium channel modulator; hormone; human metabolite; immunomodulator; metabolite; mouse metabolite; nutraceutical |
| vitamin d 2 Ergocalciferols: Derivatives of ERGOSTEROL formed by ULTRAVIOLET RAYS breaking of the C9-C10 bond. They differ from CHOLECALCIFEROL in having a double bond between C22 and C23 and a methyl group at C24.. vitamin D2 : A vitamin D supplement and has been isolated from alfalfa. | 3.23 | 1 | 0 | hydroxy seco-steroid; seco-ergostane; vitamin D | bone density conservation agent; nutraceutical; plant metabolite; rodenticide |
| amphotericin b Amphotericin B: Macrolide antifungal antibiotic produced by Streptomyces nodosus obtained from soil of the Orinoco river region of Venezuela.. amphotericin B : A macrolide antibiotic used to treat potentially life-threatening fungal infections. | 3.23 | 1 | 0 | antibiotic antifungal drug; macrolide antibiotic; polyene antibiotic | antiamoebic agent; antiprotozoal drug; bacterial metabolite |
| pulmicort Budesonide: A glucocorticoid used in the management of ASTHMA, the treatment of various skin disorders, and allergic RHINITIS.. budesonide : A glucocorticoid steroid having a highly oxygenated pregna-1,4-diene structure. It is used mainly in the treatment of asthma and non-infectious rhinitis and for treatment and prevention of nasal polyposis. | 3.23 | 1 | 0 | 11beta-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; cyclic acetal; glucocorticoid; primary alpha-hydroxy ketone | anti-inflammatory drug; bronchodilator agent; drug allergen |
| oxymetholone Oxymetholone: A synthetic hormone with anabolic and androgenic properties. It is used mainly in the treatment of anemias. According to the Fourth Annual Report on Carcinogens (NTP 85-002), this compound may reasonably be anticipated to be a carcinogen. (From Merck Index, 11th ed). oxymetholone : A 3-oxo-5alpha- steroid that is 4,5alpha-dihydrotestosterone which is substituted by a hydroxymethylidene group at position 2 and by a methyl group at the 17alpha position. A synthetic androgen, it was mainly used for the treatment of anaemias until being replaced by treatments with fewer side effects. | 3.23 | 1 | 0 | ||
| eprosartan eprosartan: angiotensin II receptor antagonist. eprosartan : A member of the class of imidazoles and thiophenes that is an angiotensin II receptor antagonist used for the treatment of high blood pressure. | 3.23 | 1 | 0 | dicarboxylic acid; imidazoles; thiophenes | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| montelukast montelukast: a leukotriene D4 receptor antagonist | 3.23 | 1 | 0 | aliphatic sulfide; monocarboxylic acid; quinolines | anti-arrhythmia drug; anti-asthmatic drug; leukotriene antagonist |
| mivacurium Mivacurium: An isoquinoline derivative that is used as a short-acting non-depolarizing agent. | 3.23 | 1 | 0 | isoquinolines | |
| hemabate carboprost tromethamine : The tromethamine salt of carboprost. It is used as an abortifacient agent that is effective in both the first and second trimesters of pregnancy. | 3.23 | 1 | 0 | ||
| mycophenolate mofetil mycophenolate mofetil : A carboxylic ester resulting from the formal condensation between the carboxylic acid group of mycophenolic acid and the hydroxy group of 2-(morpholin-4-yl)ethanol. In the liver, it is metabolised to mycophenolic acid, an immunosuppressant for which it is a prodrug. It is widely used to prevent tissue rejection following organ transplants as well as for the treatment of certain autoimmune diseases. | 3.23 | 1 | 0 | carboxylic ester; ether; gamma-lactone; phenols; tertiary amino compound | anticoronaviral agent; EC 1.1.1.205 (IMP dehydrogenase) inhibitor; immunosuppressive agent; prodrug |
| entacapone entacapone: structure given in first source. entacapone : A monocarboxylic acid amide that is N,N-diethylprop-2-enamide in which the hydrogen at position 2 is substituted by a cyano group and the hydrogen at the 3E position is substituted by a 3,4-dihydroxy-5-nitrophenyl group. | 3.23 | 1 | 0 | 2-nitrophenols; catechols; monocarboxylic acid amide; nitrile | antidyskinesia agent; antiparkinson drug; central nervous system drug; EC 2.1.1.6 (catechol O-methyltransferase) inhibitor |
| paricalcitol [no description available] | 3.23 | 1 | 0 | hydroxy seco-steroid; seco-cholestane | antiparathyroid drug |
| 7432 s Ceftibuten: A cephalosporin antibacterial agent that is used in the treatment of infections, including urinary-tract and respiratory-tract infections.. ceftibuten : A third-generation cephalosporin antibiotic with a [(2Z)-2-(2-amino-1,3-thiazol-4-yl)-4-carboxybut-2-enoyl]amino substituent at the 7 position of the cephem skeleton. An orally-administered agent, ceftibuten is used as the dihydrate to treat urinary-tract and respiratory-tract infections. | 3.23 | 1 | 0 | cephalosporin; dicarboxylic acid | antibacterial drug |
| isotretinoin Isotretinoin: A topical dermatologic agent that is used in the treatment of ACNE VULGARIS and several other skin diseases. The drug has teratogenic and other adverse effects.. isotretinoin : A retinoic acid that is all-trans-retinoic acid in which the double bond which is alpha,beta- to the carboxy group is isomerised to Z configuration. A synthetic retinoid, it is used for the treatment of severe cases of acne and other skin diseases. | 3.23 | 1 | 0 | retinoic acid | antineoplastic agent; keratolytic drug; teratogenic agent |
| epoprostenol [no description available] | 3.23 | 1 | 0 | prostaglandins I | mouse metabolite |
| indocyanine green [no description available] | 3.23 | 1 | 0 | 1,1-diunsubstituted alkanesulfonate; benzoindole; cyanine dye | |
| triprolidine Triprolidine: Histamine H1 antagonist used in allergic rhinitis; ASTHMA; and URTICARIA. It is a component of COUGH and COLD medicines. It may cause drowsiness.. triprolidine : An N-alkylpyrrolidine that is acrivastine in which the pyridine ring is lacking the propenoic acid substituent. It is a sedating antihistamine that is used (generally as the monohydrochloride monohydrate) for the relief of the symptoms of uticaria, rhinitis, and various pruritic skin disorders. | 3.23 | 1 | 0 | N-alkylpyrrolidine; olefinic compound; pyridines | H1-receptor antagonist |
| pitavastatin pitavastatin : A dihydroxy monocarboxylic acid that is (6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]hept-6-enoic acid in which the two hydroxy groups are located at positions 3 and 5 (the 3R,5S-stereoisomer). Used as its calcium salt for treatment of hypercholesterolemia (elevated levels of cholesterol in the blood) on patients unable to sufficiently lower their cholesterol levels by diet and exercise. | 3.23 | 1 | 0 | cyclopropanes; dihydroxy monocarboxylic acid; monofluorobenzenes; quinolines; statin (synthetic) | antioxidant |
| ethamolin monoethanolamine oleate: used for treatment of pyogenic granuloma | 3.23 | 1 | 0 | long-chain fatty acid | |
| alatrofloxacin mesylate [no description available] | 3.23 | 1 | 0 | ||
| codeine [no description available] | 3.23 | 1 | 0 | morphinane alkaloid; organic heteropentacyclic compound | antitussive; drug allergen; environmental contaminant; opioid analgesic; opioid receptor agonist; prodrug; xenobiotic |
| cyclosporine ramihyphin A: one of the metabolites produced by Fusarium sp. S-435; RN given refers to cpd with unknown MF | 3.23 | 1 | 0 | homodetic cyclic peptide | anti-asthmatic drug; anticoronaviral agent; antifungal agent; antirheumatic drug; carcinogenic agent; dermatologic drug; EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor; geroprotector; immunosuppressive agent; metabolite |
| acitretin Acitretin: An oral retinoid effective in the treatment of psoriasis. It is the major metabolite of ETRETINATE with the advantage of a much shorter half-life when compared with etretinate.. acitretin : A retinoid that consists of 3,7-dimethylnona-2,4,6,8-tetraenoic acid having a 4-methoxy-2,3,6-trimethylphenyl group attached at position 9. | 3.23 | 1 | 0 | acitretin; alpha,beta-unsaturated monocarboxylic acid; retinoid | keratolytic drug |
| estropipate estropipate: used therapeutically in menopausal patients | 3.23 | 1 | 0 | piperazinium salt; steroid sulfate | |
| hydromorphone Hydromorphone: An opioid analgesic made from MORPHINE and used mainly as an analgesic. It has a shorter duration of action than morphine.. hydromorphone : A morphinane alkaloid that is a hydrogenated ketone derivative of morphine. A semi-synthetic drug, it is a centrally acting pain medication of the opioid class. | 3.23 | 1 | 0 | morphinane alkaloid; organic heteropentacyclic compound | mu-opioid receptor agonist; opioid analgesic |
| levetiracetam Levetiracetam: A pyrrolidinone and acetamide derivative that is used primarily for the treatment of SEIZURES and some movement disorders, and as a nootropic agent.. levetiracetam : A pyrrolidinone and carboxamide that is N-methylpyrrolidin-2-one in which one of the methyl hydrogens is replaced by an aminocarbonyl group, while another is replaced by an ethyl group (the S enantiomer). An anticonvulsant, it is used for the treatment of epilepsy in both human and veterinary medicine. | 3.23 | 1 | 0 | pyrrolidin-2-ones | anticonvulsant; environmental contaminant; xenobiotic |
| ly 163892 loracarbef: 1-carbacephem antibiotic; has a broad spectrum of antimicrobial activity; structure given in first source; carbacephems differ from cephalosporins in the substitution of a sulfur atom in the dihydrothiazine ring with a methylene group to form a tetrahydropyridine ring. loracarbef : A synthetic "carba" analogue of cefaclor, with carbon replacing sulfur at position 1. Used to treat a wide range of infections caused by both gram-positive and gram-negative bacteria. | 3.23 | 1 | 0 | carbacephem; zwitterion | antibacterial drug; antimicrobial agent |
| nabilone nabilone: cannabinol deriv; RN given refers to cpd without isomeric designation; structure | 3.23 | 1 | 0 | ||
| naloxone Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.. naloxone : A synthetic morphinane alkaloid that is morphinone in which the enone double bond has been reduced to a single bond, the hydrogen at position 14 has been replaced by a hydroxy group, and the methyl group attached to the nitrogen has been replaced by an allyl group. A specific opioid antagonist, it is used (commonly as its hydrochloride salt) to reverse the effects of opioids, both following their use of opioids during surgery and in cases of known or suspected opioid overdose. | 3.23 | 1 | 0 | morphinane alkaloid; organic heteropentacyclic compound; tertiary alcohol | antidote to opioid poisoning; central nervous system depressant; mu-opioid receptor antagonist |
| oxycodone Oxycodone: A semisynthetic derivative of CODEINE.. oxycodone : A semisynthetic opioid of formula C18H21NO4 that is derived from thebaine. It is a moderately potent opioid analgesic, generally used for relief of moderate to severe pain. | 3.23 | 1 | 0 | organic heteropentacyclic compound; semisynthetic derivative | antitussive; mu-opioid receptor agonist; opioid analgesic |
| oxymorphone Oxymorphone: An opioid analgesic with actions and uses similar to those of MORPHINE, apart from an absence of cough suppressant activity. It is used in the treatment of moderate to severe pain, including pain in obstetrics. It may also be used as an adjunct to anesthesia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1092) | 3.23 | 1 | 0 | morphinane alkaloid | |
| vitamin k 1 Vitamin K 1: A family of phylloquinones that contains a ring of 2-methyl-1,4-naphthoquinone and an isoprenoid side chain. Members of this group of vitamin K 1 have only one double bond on the proximal isoprene unit. Rich sources of vitamin K 1 include green plants, algae, and photosynthetic bacteria. Vitamin K1 has antihemorrhagic and prothrombogenic activity.. phylloquinone : A member of the class of phylloquinones that consists of 1,4-naphthoquinone having methyl and phytyl groups at positions 2 and 3 respectively. The parent of the class of phylloquinones. | 3.23 | 1 | 0 | phylloquinones; vitamin K | cofactor; human metabolite; plant metabolite |
| sirolimus Sirolimus: A macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to IMMUNOPHILINS. Sirolimus is a potent immunosuppressant and possesses both antifungal and antineoplastic properties.. sirolimus : A macrolide lactam isolated from Streptomyces hygroscopicus consisting of a 29-membered ring containing 4 trans double bonds, three of which are conjugated. It is an antibiotic, immunosupressive and antineoplastic agent. | 3.59 | 2 | 0 | antibiotic antifungal drug; cyclic acetal; cyclic ketone; ether; macrolide lactam; organic heterotricyclic compound; secondary alcohol | antibacterial drug; anticoronaviral agent; antineoplastic agent; bacterial metabolite; geroprotector; immunosuppressive agent; mTOR inhibitor |
| topiramate Topiramate: A sulfamate-substituted fructose analog that was originally identified as a hypoglycemic agent. It is used for the treatment of EPILEPSY and MIGRAINE DISORDERS, and may also promote weight loss.. topiramate : A hexose derivative that is 2,3:4,5-di-O-isopropylidene-beta-D-fructopyranose in which the hydroxy group has been converted to the corresponding sulfamate ester. It blocks voltage-dependent sodium channels and is used as an antiepileptic and for the prevention of migraine. | 3.23 | 1 | 0 | cyclic ketal; ketohexose derivative; sulfamate ester | anticonvulsant; sodium channel blocker |
| trospium chloride trospium chloride : An organic chloride salt of trospium. It is an antispasmodic drug used for the treatment of overactive bladder. | 5.81 | 3 | 1 | ||
| morphine Meconium: The thick green-to-black mucilaginous material found in the intestines of a full-term fetus. It consists of secretions of the INTESTINAL GLANDS; BILE PIGMENTS; FATTY ACIDS; AMNIOTIC FLUID; and intrauterine debris. It constitutes the first stools passed by a newborn. | 3.23 | 1 | 0 | morphinane alkaloid; organic heteropentacyclic compound; tertiary amino compound | anaesthetic; drug allergen; environmental contaminant; geroprotector; mu-opioid receptor agonist; opioid analgesic; plant metabolite; vasodilator agent; xenobiotic |
| benzphetamine Benzphetamine: A sympathomimetic agent with properties similar to DEXTROAMPHETAMINE. It is used in the treatment of obesity. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1222). benzphetamine : Dextroamphetamine in which the the hydrogens attached to the amino group are substituted by a methyl and a benzyl group. A sympathomimetic agent with properties similar to dextroamphetamine, it is used as its hydrochloride salt in the treatment of obesity. | 3.23 | 1 | 0 | amphetamines; tertiary amine | adrenergic uptake inhibitor; appetite depressant; dopamine uptake inhibitor; sympathomimetic agent |
| deamino arginine vasopressin Deamino Arginine Vasopressin: A synthetic analog of the pituitary hormone, ARGININE VASOPRESSIN. Its action is mediated by the VASOPRESSIN receptor V2. It has prolonged antidiuretic activity, but little pressor effects. It also modulates levels of circulating FACTOR VIII and VON WILLEBRAND FACTOR. | 3.23 | 1 | 0 | heterodetic cyclic peptide | diagnostic agent; renal agent; vasopressin receptor agonist |
| dexmedetomidine [no description available] | 3.23 | 1 | 0 | medetomidine | alpha-adrenergic agonist; analgesic; non-narcotic analgesic; sedative |
| goserelin Goserelin: A synthetic long-acting agonist of GONADOTROPIN-RELEASING HORMONE. Goserelin is used in treatments of malignant NEOPLASMS of the prostate, uterine fibromas, and metastatic breast cancer. | 3.23 | 1 | 0 | organic molecular entity | |
| nalbuphine Nalbuphine: A narcotic used as a pain medication. It appears to be an agonist at KAPPA RECEPTORS and an antagonist or partial agonist at MU RECEPTORS. | 3.23 | 1 | 0 | organic heteropentacyclic compound | mu-opioid receptor antagonist; opioid analgesic |
| nateglinide Nateglinide: A phenylalanine and cyclohexane derivative that acts as a hypoglycemic agent by stimulating the release of insulin from the pancreas. It is used in the treatment of TYPE 2 DIABETES.. nateglinide : An N-acyl-D-phenylalanine resulting from the formal condensation of the amino group of D-phenylalanine with the carboxy group of trans-4-isopropylcyclohexanecarboxylic acid. An orally-administered, rapidly-absorbed, short-acting insulinotropic agent, it is used for the treatment of type 2 diabetes mellitus. | 3.23 | 1 | 0 | phenylalanine derivative | |
| vinorelbine [no description available] | 3.23 | 1 | 0 | acetate ester; methyl ester; organic heteropentacyclic compound; organic heterotetracyclic compound; ring assembly; vinca alkaloid | antineoplastic agent; photosensitizing agent |
| silodosin silodosin: an alpha(1a)-adrenoceptor-selective antagonist; structure given in first source | 6.28 | 5 | 2 | indolecarboxamide | |
| fluvoxamine Fluvoxamine: A selective serotonin reuptake inhibitor that is used in the treatment of DEPRESSION and a variety of ANXIETY DISORDERS.. fluvoxamine : An oxime O-ether that is benzene substituted by a (1E)-N-(2-aminoethoxy)-5-methoxypentanimidoyl group at position 1 and a trifluoromethyl group at position 4. It is a selective serotonin reuptake inhibitor that is used for the treatment of obsessive-compulsive disorder. | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; 5-methoxyvalerophenone O-(2-aminoethyl)oxime | antidepressant; anxiolytic drug; serotonin uptake inhibitor |
| su 11248 [no description available] | 3.23 | 1 | 0 | monocarboxylic acid amide; pyrroles | angiogenesis inhibitor; antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; immunomodulator; neuroprotective agent; vascular endothelial growth factor receptor antagonist |
| (6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid (6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid : A dihydroxy monocarboxylic acid that is N-isopropylindole which is substituted at position 3 by a p-fluorophenyl group and at position 2 by a 6-carboxy-3,5-dihydroxyhex-1-en-1-yl group. It has four possible diastereoisomers. | 3.23 | 1 | 0 | dihydroxy monocarboxylic acid; indoles; organofluorine compound | |
| levorphanol Levorphanol: A narcotic analgesic that may be habit-forming. It is nearly as effective orally as by injection. | 3.23 | 1 | 0 | morphinane alkaloid | |
| naltrexone Naltrexone: Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.. naltrexone : An organic heteropentacyclic compound that is naloxone substituted in which the allyl group attached to the nitrogen is replaced by a cyclopropylmethyl group. A mu-opioid receptor antagonist, it is used to treat alcohol dependence. | 3.23 | 1 | 0 | cyclopropanes; morphinane-like compound; organic heteropentacyclic compound | antidote to opioid poisoning; central nervous system depressant; environmental contaminant; mu-opioid receptor antagonist; xenobiotic |
| dextromethorphan Dextromethorphan: Methyl analog of DEXTRORPHAN that shows high affinity binding to several regions of the brain, including the medullary cough center. This compound is an NMDA receptor antagonist (RECEPTORS, N-METHYL-D-ASPARTATE) and acts as a non-competitive channel blocker. It is one of the widely used ANTITUSSIVES, and is also used to study the involvement of glutamate receptors in neurotoxicity.. dextromethorphan : A 6-methoxy-11-methyl-1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthrene in which the sterocenters at positions 4a, 10 and 10a have S-configuration. It is a prodrug of dextrorphan and used as an antitussive drug for suppressing cough. | 3.23 | 1 | 0 | 6-methoxy-11-methyl-1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthrene | antitussive; environmental contaminant; neurotoxin; NMDA receptor antagonist; oneirogen; prodrug; xenobiotic |
| butorphanol Butorphanol: A synthetic morphinan analgesic with narcotic antagonist action. It is used in the management of severe pain.. butorphanol : Levorphanol in which a hydrogen at position 14 of the morphinan skeleton is substituted by hydroxy and one of the hydrogens of the N-methyl group is substituted by cyclopropyl. A semi-synthetic opioid agonist-antagonist analgesic, it is used as its (S,S)-tartaric acid salt for relief or moderate to severe pain. | 3.23 | 1 | 0 | morphinane alkaloid | antitussive; kappa-opioid receptor agonist; mu-opioid receptor agonist; opioid analgesic |
| cefixime [no description available] | 3.23 | 1 | 0 | cephalosporin | antibacterial drug; drug allergen |
| lisinopril Lisinopril: One of the ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACE inhibitors), orally active, that has been used in the treatment of hypertension and congestive heart failure. | 3.23 | 1 | 0 | dipeptide | EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor |
| benazepril benazepril: structure given in first source. benazepril : A benzazepine that is benazeprilat in which the carboxy group of the 2-amino-4-phenylbutanoic acid moiety has been converted to the corresponding ethyl ester. It is used (generally as its hydrochloride salt) as a prodrug for the angiotensin-converting enzyme inhibitor benazeprilat in the treatment of hypertension and heart failure. | 3.23 | 1 | 0 | benzazepine; dicarboxylic acid monoester; ethyl ester; lactam | EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; prodrug |
| ramipril Ramipril: A long-acting angiotensin-converting enzyme inhibitor. It is a prodrug that is transformed in the liver to its active metabolite ramiprilat.. ramipril : A dipeptide that is the prodrug for ramiprilat, the active metabolite obtained by hydrolysis of the ethyl ester group. An angiotensin-converting enzyme (ACE) inhibitor, used to treat high blood pressure and congestive heart failure.. quark : Quarks comprise one of two classes of the fundamental particles. Quarks possess fractional electric charges and are not observed in free state. The word "quark" first appears in James Joyce's Finnegans Wake and has been chosen by Murray Gell-Mann as a name for fundamental building blocks of particles. | 3.23 | 1 | 0 | azabicycloalkane; cyclopentapyrrole; dicarboxylic acid monoester; dipeptide; ethyl ester | bradykinin receptor B2 agonist; cardioprotective agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; matrix metalloproteinase inhibitor; prodrug |
| verteporfin (2R,2(1)S)-8-ethenyl-2(1),2(2)-bis(methoxycarbonyl)-17-(3-methoxy-3-oxopropyl)-2,7,12,18-tetramethyl-2,2(1)-dihydrobenzo[b]porphyrin-13-propanoic acid : The 2(1),2(2),17-trimethyl ester of (2R,2(1)S)-2(1),2(2)-dicarboxy-8-ethenyl-2,7,12,18-tetramethyl-2,2(1)-dihydrobenzo[b]porphyrin-13,17-dipropanoic acid. | 3.23 | 1 | 0 | ||
| indinavir sulfate Indinavir: A potent and specific HIV protease inhibitor that appears to have good oral bioavailability. | 3.23 | 1 | 0 | dicarboxylic acid diamide; N-(2-hydroxyethyl)piperazine; piperazinecarboxamide | HIV protease inhibitor |
| zimeldine Zimeldine: One of the SEROTONIN UPTAKE INHIBITORS formerly used for depression but was withdrawn worldwide in September 1983 because of the risk of GUILLAIN-BARRE SYNDROME associated with its use. (From Martindale, The Extra Pharmacopoeia, 29th ed, p385) | 3.23 | 1 | 0 | styrenes | |
| enalapril Enalapril: An angiotensin-converting enzyme inhibitor that is used to treat HYPERTENSION and HEART FAILURE.. enalapril : A dicarboxylic acid monoester that is ethyl 4-phenylbutanoate in which a hydrogen alpha to the carboxy group is substituted by the amino group of L-alanyl-L-proline (S-configuration). | 3.23 | 1 | 0 | dicarboxylic acid monoester; dipeptide | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; geroprotector; prodrug |
| trientine hydrochloride [no description available] | 3.23 | 1 | 0 | ||
| n-methylscopolamine bromide scopolamine methobromide : A quaternary ammonium salt resulting from the reaction of the amino group of scopolamine with methyl bromide. | 3.23 | 1 | 0 | ||
| fumarates Fumarates: Compounds based on fumaric acid.. fumarate(2-) : A C4-dicarboxylate that is the E-isomer of but-2-enedioate(2-) | 2.21 | 1 | 0 | butenedioate; C4-dicarboxylate | human metabolite; metabolite; Saccharomyces cerevisiae metabolite |
| bleomycin [no description available] | 3.23 | 1 | 0 | bleomycin | antineoplastic agent; metabolite |
| boron Boron: A trace element with the atomic symbol B, atomic number 5, and atomic weight [10.806; 10.821]. Boron-10, an isotope of boron, is used as a neutron absorber in BORON NEUTRON CAPTURE THERAPY. | 2.6 | 1 | 0 | boron group element atom; metalloid atom; nonmetal atom | micronutrient |
| enalaprilat anhydrous Enalaprilat: The active metabolite of ENALAPRIL and one of the potent, intravenously administered, ANGIOTENSIN-CONVERTING ENZYME INHIBITORS. It is an effective agent for the treatment of essential hypertension and has beneficial hemodynamic effects in heart failure. The drug produces renal vasodilation with an increase in sodium excretion.. enalaprilat dihydrate : The dihydrate form of enalaprilat, an angiotensin-converting enzyme (ACE) inhibitor that is used (often in the form of its prodrug, enalapril) in the treatment of hypertension and heart failure, for reduction of proteinuria and renal disease in patients with nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients. Unlike enalapril, enalaprilat is not absorbed by mouth but is administered by intravenous injection.. enalaprilat (anhydrous) : Enalapril in which the ethyl ester group has been hydrolysed to the corresponding carboxylic acid. Enalaprilat is an angiotensin-converting enzyme (ACE) inhibitor and is used (often in the form of its prodrug, enalapril) in the treatment of hypertension and heart failure, for reduction of proteinuria and renal disease in patients with nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients. Unlike enalapril, enalaprilat is not absorbed by mouth but is given by intravenous injection, usually as the dihydrate. | 3.23 | 1 | 0 | dicarboxylic acid; dipeptide | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor |
| ximelagatran ximelagatran: prodrug (via hydroxylation) of melagatran & a direct thrombin inhibitor; liver toxicity concerns so AZD0837 being developed to replace this. ximelagatran : A member of the class of azetidines that is melagatran in which the carboxylic acid group has been converted to the corresponding ethyl ester and in which the amidine group has been converted into the corresponding amidoxime. A prodrug for melagatran, ximelagatran was the first orally available direct thrombin inhibitor to be brought to market as an anticoagulant, but was withdrawn in 2006 following reports of it causing liver damage. | 3.23 | 1 | 0 | amidoxime; azetidines; carboxamide; ethyl ester; hydroxylamines; secondary amino compound; secondary carboxamide; tertiary carboxamide | anticoagulant; EC 3.4.21.5 (thrombin) inhibitor; prodrug; serine protease inhibitor |
| cefuroxime [no description available] | 3.23 | 1 | 0 | 3-(carbamoyloxymethyl)cephalosporin; furans; oxime O-ether | drug allergen |
| ceftriaxone [no description available] | 3.23 | 1 | 0 | 1,2,4-triazines; 1,3-thiazoles; cephalosporin; oxime O-ether | antibacterial drug; drug allergen; EC 3.5.2.6 (beta-lactamase) inhibitor |
| cefepime Cefepime: A fourth-generation cephalosporin antibacterial agent that is used in the treatment of infections, including those of the abdomen, urinary tract, respiratory tract, and skin. It is effective against PSEUDOMONAS AERUGINOSA and may also be used in the empiric treatment of FEBRILE NEUTROPENIA.. cefepime : A cephalosporin bearing (1-methylpyrrolidinium-1-yl)methyl and (2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetamido groups at positions 3 and 7, respectively, of the cephem skeleton. | 3.23 | 1 | 0 | cephalosporin; oxime O-ether | antibacterial drug |
| pafuramidine pafuramidine: a prodrug of furamidine | 3.23 | 1 | 0 | ||
| ceftazidime [no description available] | 3.23 | 1 | 0 | cephalosporin; oxime O-ether | antibacterial drug; drug allergen; EC 2.4.1.129 (peptidoglycan glycosyltransferase) inhibitor |
| trandolapril trandolapril : A heterobicylic compound that is (2S,3aR,7aS)-1-[(2S)-2-aminopropanoyl]octahydro-1H-indole-2-carboxylic acid in which the hydrogen of the amino group is substituted by a (2R)-1-ethoxy-1-oxo-4-phenylbutan-2-yl group. It is a angiotensin-converting enzyme inhibitor and a prodrug used for the treatment of hypertension. | 3.23 | 1 | 0 | dicarboxylic acid monoester; dipeptide; ethyl ester; organic heterobicyclic compound; secondary amino compound; tertiary carboxamide | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; prodrug |
| pregabalin Pregabalin: A gamma-aminobutyric acid (GABA) derivative that functions as a CALCIUM CHANNEL BLOCKER and is used as an ANTICONVULSANT as well as an ANTI-ANXIETY AGENT. It is also used as an ANALGESIC in the treatment of NEUROPATHIC PAIN and FIBROMYALGIA.. pregabalin : A gamma-amino acid that is gamma-aminobutyric acid (GABA) carrying an isobutyl substitutent at the beta-position (the S-enantiomer). Binds with high affinity to the alpha2-delta site (an auxiliary subunit of voltage-gated calcium channels) in central nervous system tissues. | 3.23 | 1 | 0 | gamma-amino acid | anticonvulsant; calcium channel blocker |
| alvimopan anhydrous alvimopan: mu opioid receptor antagonist; intended to treat constipation in patients taking opiates for pain | 3.23 | 1 | 0 | peptide | |
| aliskiren aliskiren: orally active nonpeptidic renin inhibitor. aliskiren : A monomethoxybenzene compound having a 3-methoxypropoxy group at the 2-position and a multi-substituted branched alkyl substituent at the 4-position. | 3.23 | 1 | 0 | monocarboxylic acid amide; monomethoxybenzene | antihypertensive agent |
| famotidine [no description available] | 3.23 | 1 | 0 | 1,3-thiazoles; guanidines; sulfonamide | anti-ulcer drug; H2-receptor antagonist; P450 inhibitor |
| cefotaxime Cefotaxime: Semisynthetic broad-spectrum cephalosporin.. cefotaxime : A cephalosporin compound having acetoxymethyl and [2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetyl]amino side groups. | 3.23 | 1 | 0 | 1,3-thiazoles; cephalosporin; oxime O-ether | antibacterial drug; drug allergen |
| aztreonam [no description available] | 3.23 | 1 | 0 | beta-lactam antibiotic allergen; monobactam | antibacterial drug; drug allergen; EC 2.4.1.129 (peptidoglycan glycosyltransferase) inhibitor |
| cefpodoxime [no description available] | 3.23 | 1 | 0 | carboxylic acid; cephalosporin | antibacterial drug |
| palonosetron Palonosetron: Isoquinoline and quinuclidine derivative that acts as a 5-HT3 RECEPTOR antagonist. It is used in the prevention of nausea and vomiting induced by cytotoxic chemotherapy, and for the prevention of post-operative nausea and vomiting.. palonosetron : An organic heterotricyclic compound that is an antiemetic used (as its hydrochloride salt) in combination with netupitant (under the trade name Akynzeo) to treat nausea and vomiting in patients undergoing cancer chemotherapy. | 3.23 | 1 | 0 | azabicycloalkane; delta-lactam; organic heterotricyclic compound | antiemetic; serotonergic antagonist |
| imidafenacin imidafenacin: structure in first source | 10.79 | 3 | 1 | diarylmethane | |
| rifaximin [no description available] | 3.23 | 1 | 0 | acetate ester; cyclic ketal; lactam; macrocycle; organic heterohexacyclic compound; rifamycins; semisynthetic derivative | antimicrobial agent; gastrointestinal drug; orphan drug |
| everolimus [no description available] | 3.59 | 2 | 0 | cyclic acetal; cyclic ketone; ether; macrolide lactam; primary alcohol; secondary alcohol | anticoronaviral agent; antineoplastic agent; geroprotector; immunosuppressive agent; mTOR inhibitor |
| ixabepilone [no description available] | 3.23 | 1 | 0 | 1,3-thiazoles; beta-hydroxy ketone; epoxide; lactam; macrocycle | antineoplastic agent; microtubule-destabilising agent |
| cgp-56697 Artemether, Lumefantrine Drug Combination: Drug combination of artemether and lumefantrine that is used to treat PLASMODIUM FALCIPARUM MALARIA. | 2.05 | 1 | 0 | ||
| ceftizoxime [no description available] | 3.23 | 1 | 0 | cephalosporin | antibacterial drug |
| 1-methyl-d-lysergic acid butanolamide [no description available] | 3.23 | 1 | 0 | ergot alkaloid; monocarboxylic acid amide | serotonergic antagonist; sympatholytic agent; vasoconstrictor agent |
| nitrofurantoin Nitrofurantoin: A urinary anti-infective agent effective against most gram-positive and gram-negative organisms. Although sulfonamides and antibiotics are usually the agents of choice for urinary tract infections, nitrofurantoin is widely used for prophylaxis and long-term suppression.. nitrofurantoin : An imidazolidine-2,4-dione that is hydantoin substituted at position 1 by a [(5-nitro-2-furyl)methylene]amino group. An antibiotic that damages bacterial DNA. | 3.23 | 1 | 0 | imidazolidine-2,4-dione; nitrofuran antibiotic; organonitrogen heterocyclic antibiotic; organooxygen heterocyclic antibiotic | antibacterial drug; antiinfective agent; hepatotoxic agent |
| dantrolene [no description available] | 3.23 | 1 | 0 | ||
| cefdinir [no description available] | 3.23 | 1 | 0 | cephalosporin; ketoxime | antibacterial drug |
| etonogestrel [no description available] | 3.23 | 1 | 0 | 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; terminal acetylenic compound | contraceptive drug; female contraceptive drug; progestin |
| temsirolimus [no description available] | 3.23 | 1 | 0 | macrolide lactam | |
| dutasteride Dutasteride: A 5-ALPHA-REDUCTASE INHIBITOR that is reported to inhibit both type-1 and type2 isoforms of the enzyme and is used to treat BENIGN PROSTATIC HYPERPLASIA.. dutasteride : An aza-steroid that is inasteride in which the tert-butyl group is replaced by a 2,5-bis(trifluoromethyl)phenyl group. A synthetic 4-azasteroid, dutasteride is a selective inhibitor of both the type 1 and type 2 isoforms of steroid 5alpha-reductase, an intracellular enzyme that converts testosterone to 5alpha-dihydrotestosterone. Dutasteride is used for the treatment of symptomatic benign prostatic hyperplasia in men with an enlarged prostate gland. | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; aza-steroid; delta-lactam | antihyperplasia drug; EC 1.3.1.22 [3-oxo-5alpha-steroid 4-dehydrogenase (NADP(+))] inhibitor |
| lu 208075 ambrisentan: an ET(A) receptor antagonist and antihypertensive agent; studied for use in pulmonary arterial hypertension | 3.23 | 1 | 0 | diarylmethane | |
| bibx 1382bs BIBX 1382BS: an ErbB receptor kinase inhibitor; no further information available 4/2001 | 3.23 | 1 | 0 | substituted aniline | |
| gemifloxacin Gemifloxacin: A naphthyridine and fluoroquinolone derivative antibacterial agent and DNA TOPOISOMERASE II inhibitor that is used for the treatment of community-acquired pneumonia and acute bacterial infections associated with chronic bronchitis.. gemifloxacin : A 1,4-dihydro-1,8-naphthyridine with a carboxy group at the 3-position, an oxo sustituent at the 4-position, a fluoro substituent at the 5-position and a substituted pyrrolin-1-yl group at the 7-position. | 3.23 | 1 | 0 | 1,8-naphthyridine derivative; fluoroquinolone antibiotic; monocarboxylic acid; quinolone antibiotic | antibacterial drug; antimicrobial agent; topoisomerase IV inhibitor |
| dexlansoprazole Dexlansoprazole: The R-isomer of lansoprazole that is used to treat severe GASTROESOPHAGEAL REFLUX DISEASE. | 3.23 | 1 | 0 | benzimidazoles; sulfoxide | |
| fosinopril [no description available] | 3.23 | 1 | 0 | ||
| armodafinil armodafinil : A 2-[(diphenylmethyl)sulfinyl]acetamide that has R configuration at the sulfur atom. Like its racemate, modafinil, it is used for the treatment of sleeping disorders such as narcolepsy, obstructive sleep apnoea, and shift-work sleep disorder. Peak concentration in the blood later occurs later following administration than with modafinil, so it is thought that armodafinil may be more effective than modafinil in treating people with excessive daytime sleepiness. | 3.23 | 1 | 0 | 2-[(diphenylmethyl)sulfinyl]acetamide | central nervous system stimulant; eugeroic |
| ferrihydrite ferric oxyhydroxide: an antiferromagnetic material; constitutes the core of natural ferritin; mol form 5Fe2O3.9H2O | 2.6 | 1 | 0 | ||
| pnu 200577 5-hydroxymethyl tolterodine: a metabolite of tolterodine | 8 | 12 | 6 | diarylmethane | |
| sincalide Sincalide: An octapeptide hormone present in the intestine and brain. When secreted from the gastric mucosa, it stimulates the release of bile from the gallbladder and digestive enzymes from the pancreas. | 3.23 | 1 | 0 | oligopeptide | |
| tapentadol Tapentadol: An opioid analgesic, MU OPIOID RECEPTOR agonist, and noradrenaline reuptake inhibitor that is used in the treatment of moderate to severe pain, and of pain associated with DIABETIC NEUROPATHIES. | 3.59 | 2 | 0 | alkylbenzene | |
| pentagastrin Pentagastrin: A synthetic pentapeptide that has effects like gastrin when given parenterally. It stimulates the secretion of gastric acid, pepsin, and intrinsic factor, and has been used as a diagnostic aid. | 3.23 | 1 | 0 | organic molecular entity | |
| mirabegron mirabegron: a beta3-adrenergic receptor agonist; structure in first source. mirabegron : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 2-amino-1,3-thiazol-4-ylacetic acid with the anilino group of (1R)-2-{[2-(4-aminophenyl)ethyl]amino}-1-phenylethanol. Used for the treatment of overactive bladder syndrome. | 8.92 | 18 | 2 | 1,3-thiazoles; aromatic amide; ethanolamines; monocarboxylic acid amide | beta-adrenergic agonist |
| cefditoren cefditoren: structure given in first source; RN given refers to the (6R-(3(Z),6alpha,7beta(Z)))-isomer. cefditoren : A broad spectrum, third-generation cephalosporin antibiotic with (Z)-2-(4-methyl-1,3-thiazol-5-yl)ethenyl and (2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetamido groups at positions 3 and 7, respectively, of the cephem skeleton. Generally administered as its orally absorbed pivaloyloxymethyl ester prodrug, it is used for the treatment of mild to moderate infections caused by susceptible strains of microorganisms in acute bacterial exacerbation of chronic bronchitis, community-acquired pneumonia, pharyngitis/tonsillitis, and uncomplicated skin and skin-structure infections. | 3.23 | 1 | 0 | carboxylic acid; cephalosporin | antibacterial drug |
| pazopanib pazopanib: a protein kinase inhibitor. pazopanib : A pyrimidine that is 5-(pyrimidin-2-yl}amino-2-methylbenzenesulfonamide substituted at position 4 by a (2,3-dimethylindazol-6-yl)(methyl)amino group. Used as its hydrochloride salt for treatment of kidney cancer. | 3.23 | 1 | 0 | aminopyrimidine; indazoles; sulfonamide | angiogenesis modulating agent; antineoplastic agent; tyrosine kinase inhibitor; vascular endothelial growth factor receptor antagonist |
| prasugrel hydrochloride Prasugrel Hydrochloride: A piperazine derivative and PLATELET AGGREGATION INHIBITOR that is used to prevent THROMBOSIS in patients with ACUTE CORONARY SYNDROME; UNSTABLE ANGINA and MYOCARDIAL INFARCTION, as well as in those undergoing PERCUTANEOUS CORONARY INTERVENTIONS.. prasugrel hydrochloride : A racemate comprising equal amounts of (R)- and (S)-prasugrel hydrochloride. Used to prevent blood clots in people with acute coronary syndrome who are undergoing a procedure after a recent heart attack or stroke, and in people with certain disorders of the heart or blood vessels. | 3.23 | 1 | 0 | ||
| besifloxacin [no description available] | 2.05 | 1 | 0 | quinolines | |
| baci-im [no description available] | 3.23 | 1 | 0 | homodetic cyclic peptide; polypeptide; zwitterion | antibacterial agent; antimicrobial agent |
| bms 477118 [no description available] | 3.23 | 1 | 0 | adamantanes; azabicycloalkane; monocarboxylic acid amide; nitrile; tertiary alcohol | EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor; hypoglycemic agent |
| nystatin a1 Nystatin: Macrolide antifungal antibiotic complex produced by Streptomyces noursei, S. aureus, and other Streptomyces species. The biologically active components of the complex are nystatin A1, A2, and A3.. nystatin : A heterogeneous mixture of polyene compounds produced by cultures of Streptomyces noursei. It mainly consists of three biologically active components designated nystatin A1, nystatin A2, and nystatin A3. It is used to treat oral and dermal fungal infections.. nystatin A1 : A polyene macrolide antibiotic; part of the nystatin complex produced by several Streptomyces species. It is an antifungal antibiotic used for the treatment of topical fungal infections caused by a broad spectrum of fungal pathogens comprising yeast-like and filamentous species. | 3.23 | 1 | 0 | nystatins | |
| milnacipran [no description available] | 3.23 | 1 | 0 | acetamides | |
| scopolamine hydrobromide [no description available] | 3.23 | 1 | 0 | ||
| bivalirudin bivalirudin: designed to bind to the alpha-thrombin catalytic site and anion-binding exosite for fibrin(ogen) recognition. bivalirudin : A synthetic peptide of 20 amino acids, comprising D-Phe, Pro, Arg, Pro, Gly, Gly, Gly, Gly, Asn, Gly, Asp, Phe, Glu, Glu, Ile, Pro, Glu, Glu, Tyr, and Leu in sequence. A congener of hirudin (a naturally occurring drug found in the saliva of the medicinal leech), it a specific and reversible inhibitor of thrombin, and is used as an anticoagulant. | 3.23 | 1 | 0 | polypeptide | anticoagulant; EC 3.4.21.5 (thrombin) inhibitor |
| enfuvirtide Enfuvirtide: A synthetic 36-amino acid peptide that corresponds to the heptad repeat sequence of HIV-1 gp41. It blocks HIV cell fusion and viral entry and is used with other anti-retrovirals for combination therapy of HIV INFECTIONS and AIDS.. enfuvirtide : A synthetic 36-amino acid peptide consisting of N-acetyltyrosyl, threonyl, seryl, leucyl, isoleucyl, histidyl, seryl, leucyl, isoleucyl, alpha-glutamyl, alpha-glutamyl, seryl, glutaminyl, asparaginyl, glutaminyl, glutaminyl, alpha-glutamyl, lysyl, asparaginyl, alpha-glutamyl, alpha-glutamyl, alpha-glutamyl, leucyl, leucyl, alpha-glutamyl, leucyl, alpha-aspartyl, lysyl, tryptophyl, alanyl, seryl, leucyl, tryptophyl, asparaginyl, tryptophyl, and phenylalaninamide residues joined in sequence. An HIV fusion inhibitor, it was the first of a novel class of antiretroviral drugs used in combination therapy for the treatment of HIV-1 infection. It interferes with entry of HIV into cells by binding to the gp41 sub-unit of the viral envelope glycoprotein, so inhibiting fusion of viral and cellular membranes. | 3.23 | 1 | 0 | ||
| ganirelix [no description available] | 3.23 | 1 | 0 | polypeptide | |
| teriparatide [no description available] | 3.23 | 1 | 0 | polypeptide | |
| salmon calcitonin [no description available] | 3.23 | 1 | 0 | heterodetic cyclic peptide; peptide hormone; polypeptide | bone density conservation agent; metabolite |
| ly-146032 [no description available] | 3.23 | 1 | 0 | heterodetic cyclic peptide; lipopeptide antibiotic; lipopeptide; macrocycle; macrolide | antibacterial drug; bacterial metabolite; calcium-dependent antibiotics |
| acetyl-2-naphthylalanyl-3-chlorophenylalanyl-1-oxohexadecyl-seryl-4-aminophenylalanyl(hydroorotyl)-4-aminophenylalanyl(carbamoyl)-leucyl-ilys-prolyl-alaninamide acetyl-2-naphthylalanyl-3-chlorophenylalanyl-1-oxohexadecyl-seryl-4-aminophenylalanyl(hydroorotyl)-4-aminophenylalanyl(carbamoyl)-leucyl-ILys-prolyl-alaninamide: FE-200486 is the acetate salt | 3.59 | 2 | 0 | polypeptide | |
| exenatide [no description available] | 3.23 | 1 | 0 | ||
| sodium borate borax: see also sodium borate. borax : A hydrate that is the decahydrate form of disodium tetraborate. | 2.6 | 1 | 0 | ||
| mesna Mesna: A sulfhydryl compound used to prevent urothelial toxicity by inactivating metabolites from ANTINEOPLASTIC AGENTS, such as IFOSFAMIDE or CYCLOPHOSPHAMIDE. | 3.23 | 1 | 0 | organosulfonic acid | |
| sodium lactate Sodium Lactate: The sodium salt of racemic or inactive lactic acid. It is a hygroscopic agent used intravenously as a systemic and urinary alkalizer.. sodium lactate : An organic sodium salt having lactate as the counterion. | 3.23 | 1 | 0 | lactate salt; organic sodium salt | food acidity regulator; food preservative |
| sodium iothalamate [no description available] | 3.23 | 1 | 0 | ||
| cetrorelix cetrorelix: LHRH antagonist. cetrorelix : A synthetic ten-membered oligopeptide comprising N-acetyl-3-(naphthalen-2-yl)-D-alanyl, 4-chloro-D-phenylalanyl, 3-(pyridin-3-yl)-D-alanyl, L-seryl, L-tyrosyl, N(5)-carbamoyl-D-ornithyl, L-leucyl, L-arginyl, L-prolyl, and D-alaninamide residues coupled in sequence. A gonadotrophin-releasing hormone (GnRH) antagonist, it is used for treatment of infertility and of hormone-sensitive cancers of the prostate and breast. | 3.23 | 1 | 0 | oligopeptide | antineoplastic agent; GnRH antagonist |
| tolterodine tartrate Tolterodine Tartrate: An ANTIMUSCARINIC AGENT selective for the MUSCARINIC RECEPTORS of the BLADDER that is used in the treatment of URINARY INCONTINENCE and URINARY URGE INCONTINENCE. | 13.81 | 44 | 12 | tartrate salt | |
| ascorbic acid Ascorbic Acid: A six carbon compound related to glucose. It is found naturally in citrus fruits and many vegetables. Ascorbic acid is an essential nutrient in human diets, and necessary to maintain connective tissue and bone. Its biologically active form, vitamin C, functions as a reducing agent and coenzyme in several metabolic pathways. Vitamin C is considered an antioxidant.. L-ascorbic acid : The L-enantiomer of ascorbic acid and conjugate acid of L-ascorbate.. L-ascorbate : The L-enantiomer of ascorbate and conjugate base of L-ascorbic acid, arising from selective deprotonation of the 3-hydroxy group. Required for a range of essential metabolic reactions in all animals and plants.. vitamin C : Any member of a group of vitamers that belong to the chemical structural class called butenolides that exhibit biological activity against vitamin C deficiency in animals. The vitamers include L-ascorbic acid and its salt, ionized and oxidized forms. | 3.23 | 1 | 0 | ascorbic acid; vitamin C | coenzyme; cofactor; flour treatment agent; food antioxidant; food colour retention agent; geroprotector; plant metabolite; skin lightening agent |
| raltegravir [no description available] | 3.23 | 1 | 0 | 1,2,4-oxadiazole; dicarboxylic acid amide; hydroxypyrimidine; monofluorobenzenes; pyrimidone; secondary carboxamide | antiviral drug; HIV-1 integrase inhibitor |
| tetracycline Tetracycline: A naphthacene antibiotic that inhibits AMINO ACYL TRNA binding during protein synthesis.. tetracycline : A broad-spectrum polyketide antibiotic produced by the Streptomyces genus of actinobacteria. | 3.23 | 1 | 0 | ||
| oxytetracycline, anhydrous Oxytetracycline: A TETRACYCLINE analog isolated from the actinomycete STREPTOMYCES RIMOSUS and used in a wide variety of clinical conditions.. oxytetracycline : A tetracycline used for treatment of infections caused by a variety of Gram positive and Gram negative microorganisms including Mycoplasma pneumoniae, Pasteurella pestis, Escherichia coli, Haemophilus influenzae (respiratory infections), and Diplococcus pneumoniae. | 3.23 | 1 | 0 | ||
| minocycline Minocycline: A TETRACYCLINE analog, having a 7-dimethylamino and lacking the 5 methyl and hydroxyl groups, which is effective against tetracycline-resistant STAPHYLOCOCCUS infections.. minocycline : A tetracycline analogue having a dimethylamino group at position 7 and lacking the methyl and hydroxy groups at position 5. | 3.23 | 1 | 0 | ||
| piroxicam [no description available] | 3.23 | 1 | 0 | benzothiazine; monocarboxylic acid amide; pyridines | analgesic; antirheumatic drug; cyclooxygenase 1 inhibitor; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-steroidal anti-inflammatory drug |
| mobic Meloxicam: A benzothiazine and thiazole derivative that acts as a NSAID and cyclooxygenase-2 (COX-2) inhibitor. It is used in the treatment of RHEUMATOID ARTHRITIS; OSTEOARTHRITIS; and ANKYLOSING SPONDYLITIS.. meloxicam : A benzothiazine that is piroxicam in which the pyridin-2-yl group is replaced by a 5-methyl-1,3-thiazol-2-yl group. A non-steroidal anti-inflammatory drug and selective inhibitor of COX-2, it is used particularly for the management of rheumatoid arthritis. | 3.23 | 1 | 0 | 1,3-thiazoles; benzothiazine; monocarboxylic acid amide | analgesic; antirheumatic drug; cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug |
| warfarin Warfarin: An anticoagulant that acts by inhibiting the synthesis of vitamin K-dependent coagulation factors. Warfarin is indicated for the prophylaxis and/or treatment of venous thrombosis and its extension, pulmonary embolism, and atrial fibrillation with embolization. It is also used as an adjunct in the prophylaxis of systemic embolism after myocardial infarction. Warfarin is also used as a rodenticide.. warfarin : A racemate comprising equal amounts of (R)- and (S)-warfarin. Extensively used as both an anticoagulant drug and as a pesticide against rats and mice.. 4-hydroxy-3-(3-oxo-1-phenylbutyl)-1-benzopyran-2-one : A member of the class of coumarins that is 4-hydroxycoumarin which is substituted at position 3 by a 1-phenyl-3-oxo-1-butyl group. | 9.98 | 2 | 1 | benzenes; hydroxycoumarin; methyl ketone | |
| demeclocycline Demeclocycline: A TETRACYCLINE analog having a 7-chloro and a 6-methyl. Because it is excreted more slowly than tetracycline, it maintains effective blood levels for longer periods of time.. demeclocycline : Tetracycline which lacks the methyl substituent at position 7 and in which the hydrogen para- to the phenolic hydroxy group is substituted by chlorine. Like tetracycline, it is an antibiotic, but being excreted more slowly, effective blood levels are maintained for longer. It is used (mainly as the hydrochloride) for the treatment of Lyme disease, acne and bronchitis, as well as for hyponatraemia (low blood sodium concentration) due to the syndrome of inappropriate antidiuretic hormone (SIADH) where fluid restriction alone has been ineffective. | 3.23 | 1 | 0 | ||
| tipranavir tipranavir: inhibits HIV-1 protease. tipranavir : A pyridine-2-sulfonamide substituted at C-5 by a trifluoromethyl group and at the sulfonamide nitrogen by a dihydropyrone-containing m-tolyl substituent. It is an HIV-1 protease inhibitor. | 3.23 | 1 | 0 | sulfonamide | antiviral drug; HIV protease inhibitor |
| tigecycline [no description available] | 3.23 | 1 | 0 | ||
| fertinex [no description available] | 3.23 | 1 | 0 | ||
| entecavir entecavir (anhydrous) : Guanine substituted at the 9 position by a 4-hydroxy-3-(hydroxymethyl)-2-methylidenecyclopentyl group. A synthetic analogue of 2'-deoxyguanosine, it is a nucleoside reverse transcriptase inhibitor with selective antiviral activity against hepatitis B virus. Entecavir is phosphorylated intracellularly to the active triphosphate form, which competes with deoxyguanosine triphosphate, the natural substrate of hepatitis B virus reverse transcriptase, inhibiting every stage of the enzyme's activity, although it has no activity against HIV. It is used for the treatment of chronic hepatitis B. | 3.23 | 1 | 0 | 2-aminopurines; oxopurine; primary alcohol; secondary alcohol | antiviral drug; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor |
| acyclovir Acyclovir: A GUANOSINE analog that acts as an antimetabolite. Viruses are especially susceptible. Used especially against herpes.. acyclovir : An oxopurine that is guanine substituted by a (2-hydroxyethoxy)methyl substituent at position 9. Used in the treatment of viral infections. | 3.23 | 1 | 0 | 2-aminopurines; oxopurine | antimetabolite; antiviral drug |
| folic acid folcysteine: used to promote fertility in chickens. vitamin B9 : Any B-vitamin that exhibits biological activity against vitamin B9 deficiency. Vitamin B9 refers to the many forms of folic acid and its derivatives, including tetrahydrofolic acid (the active form), methyltetrahydrofolate (the primary form found in blood), methenyltetrahydrofolate, folinic acid amongst others. They are present in abundance in green leafy vegetables, citrus fruits, and animal products. Lack of vitamin B9 leads to anemia, a condition in which the body cannot produce sufficient number of red blood cells. Symptoms of vitamin B9 deficiency include fatigue, muscle weakness, and pale skin. | 3.23 | 1 | 0 | folic acids; N-acyl-amino acid | human metabolite; mouse metabolite; nutrient |
| rifampin Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160) | 5.31 | 3 | 1 | cyclic ketal; hydrazone; N-iminopiperazine; N-methylpiperazine; rifamycins; semisynthetic derivative; zwitterion | angiogenesis inhibitor; antiamoebic agent; antineoplastic agent; antitubercular agent; DNA synthesis inhibitor; EC 2.7.7.6 (RNA polymerase) inhibitor; Escherichia coli metabolite; geroprotector; leprostatic drug; neuroprotective agent; pregnane X receptor agonist; protein synthesis inhibitor |
| clozapine Clozapine: A tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity. Agranulocytosis is a major adverse effect associated with administration of this agent.. clozapine : A benzodiazepine that is 5H-dibenzo[b,e][1,4]diazepine substituted by a chloro group at position 8 and a 4-methylpiperazin-1-yl group at position 11. It is a second generation antipsychotic used in the treatment of psychiatric disorders like schizophrenia. | 3.23 | 1 | 0 | benzodiazepine; N-arylpiperazine; N-methylpiperazine; organochlorine compound | adrenergic antagonist; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; environmental contaminant; GABA antagonist; histamine antagonist; muscarinic antagonist; second generation antipsychotic; serotonergic antagonist; xenobiotic |
| dacarbazine (E)-dacarbazine : A dacarbazine in which the N=N double bond adopts a trans-configuration. | 3.23 | 1 | 0 | dacarbazine | |
| didanosine Didanosine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. Didanosine is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA by binding to reverse transcriptase; ddI is then metabolized to dideoxyadenosine triphosphate, its putative active metabolite.. didanosine : A purine 2',3'-dideoxyribonucleoside that is inosine in which the hydroxy groups at both the 2' and the 3' positions on the sugar moiety have been replaced by hydrogen. An antiviral drug, it is used as a medication to treat HIV/AIDS. | 3.23 | 1 | 0 | purine 2',3'-dideoxyribonucleoside | antimetabolite; antiviral drug; EC 2.4.2.1 (purine-nucleoside phosphorylase) inhibitor; geroprotector; HIV-1 reverse transcriptase inhibitor |
| ganciclovir [no description available] | 3.23 | 1 | 0 | 2-aminopurines; oxopurine | antiinfective agent; antiviral drug |
| valacyclovir Valacyclovir: A prodrug of acyclovir that is used in the treatment of HERPES ZOSTER and HERPES SIMPLEX VIRUS INFECTION of the skin and mucous membranes, including GENITAL HERPES. | 3.23 | 1 | 0 | L-valyl ester | antiviral drug |
| sildenafil sildenafil : A pyrazolo[4,3-d]pyrimidin-7-one having a methyl substituent at the 1-position, a propyl substituent at the 3-position and a 2-ethoxy-5-[(4-methylpiperazin-1-yl)sulfonyl]phenyl group at the 5-position. | 3.23 | 1 | 0 | piperazines; pyrazolopyrimidine; sulfonamide | EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor; vasodilator agent |
| olanzapine Olanzapine: A benzodiazepine derivative that binds SEROTONIN RECEPTORS; MUSCARINIC RECEPTORS; HISTAMINE H1 RECEPTORS; ADRENERGIC ALPHA-1 RECEPTORS; and DOPAMINE RECEPTORS. It is an antipsychotic agent used in the treatment of SCHIZOPHRENIA; BIPOLAR DISORDER; and MAJOR DEPRESSIVE DISORDER; it may also reduce nausea and vomiting in patients undergoing chemotherapy.. olanzapine : A benzodiazepine that is 10H-thieno[2,3-b][1,5]benzodiazepine substituted by a methyl group at position 2 and a 4-methylpiperazin-1-yl group at position 4. | 3.23 | 1 | 0 | benzodiazepine; N-arylpiperazine; N-methylpiperazine | antiemetic; dopaminergic antagonist; histamine antagonist; muscarinic antagonist; second generation antipsychotic; serotonergic antagonist; serotonin uptake inhibitor |
| vardenafil vardenafil : The sulfonamide resulting from formal condensation of the sulfo group of 4-ethoxy-3-(5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(1H)-one-2-yl)benzenesulfonic acid and the secondary amino group of 4-ethylpiperazine. | 3.23 | 1 | 0 | imidazotriazine; N-alkylpiperazine; N-sulfonylpiperazine | EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; vasodilator agent |
| allopurinol Allopurinol: A XANTHINE OXIDASE inhibitor that decreases URIC ACID production. It also acts as an antimetabolite on some simpler organisms.. allopurinol : A bicyclic structure comprising a pyrazole ring fused to a hydroxy-substituted pyrimidine ring. | 3.23 | 1 | 0 | nucleobase analogue; organic heterobicyclic compound | antimetabolite; EC 1.17.3.2 (xanthine oxidase) inhibitor; gout suppressant; radical scavenger |
| citrovorum factor [no description available] | 3.23 | 1 | 0 | tetrahydrofolic acid | |
| leucovorin 5-formyltetrahydrofolic acid : A formyltetrahydrofolic acid in which the formyl group is located at position 5. | 3.23 | 1 | 0 | formyltetrahydrofolic acid | Escherichia coli metabolite; mouse metabolite |
| rifapentine rifapentine: cyclopentyl derivative of rifampicin | 3.23 | 1 | 0 | N-alkylpiperazine; N-iminopiperazine; rifamycins | antitubercular agent; leprostatic drug |
| bl 4162a anagrelide: imidazoquinazoline derivative which lowers platelet count probably by inhibiting thrombopoiesis and reduces platelet aggregation; used for thrombocythemia; structure in first source. anagrelide : A 1,5-dihydroimidazo[2,1-]quinazoline having an oxo substituent at the 2-position and chloro substituents at the 6- and 7-positions. | 3.23 | 1 | 0 | imidazoquinazoline | anticoagulant; antifibrinolytic drug; cardiovascular drug; platelet aggregation inhibitor |
| tegaserod tegaserod: a nonbenzamide 5-hydroxytryptamine(4) agonist; used in treatment of irritable bowel syndrome; marketing suspended 2007 in US due to higher incidence of MI, stroke, and unstable angina; structure given in first source | 3.23 | 1 | 0 | carboxamidine; guanidines; hydrazines; indoles | gastrointestinal drug; serotonergic agonist |
| pemetrexed pemetrexed disodium : An organic sodium salt that is the disodium salt of N-{4-[2-(2-amino-4-oxo-4,7-dihydro-1H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl}-L-glutamic acid. Inhibits thymidylate synthase (TS), 421 dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT). | 3.23 | 1 | 0 | N-acyl-L-glutamic acid; pyrrolopyrimidine | antimetabolite; antineoplastic agent; EC 1.5.1.3 (dihydrofolate reductase) inhibitor; EC 2.1.1.45 (thymidylate synthase) inhibitor; EC 2.1.2.2 (phosphoribosylglycinamide formyltransferase) inhibitor |
| valganciclovir Valganciclovir: A ganciclovir prodrug and antiviral agent that is used to treat CYTOMEGALOVIRUS RETINITIS in patients with AIDS, and for the prevention of CYTOMEGALOVIRUS INFECTIONS in organ transplant recipients who have received an organ from a CMV-positive donor.. valganciclovir : The L-valinyl ester of ganciclovir, into which it is rapidly converted by intestinal and hepatic esterases. It is a synthetic analogue of 2'-deoxyguanosine. | 3.23 | 1 | 0 | L-valyl ester; purines | antiviral drug; prodrug |
| aprepitant Aprepitant: A morpholine neurokinin-1 (NK1) receptor antagonist that is used in the management of nausea and vomiting caused by DRUG THERAPY, and for the prevention of POSTOPERATIVE NAUSEA AND VOMITING.. aprepitant : A morpholine-based antiemetic, which is or the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy. Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; cyclic acetal; morpholines; triazoles | antidepressant; antiemetic; neurokinin-1 receptor antagonist; peripheral nervous system drug; substance P receptor antagonist |
| fosaprepitant fosaprepitant: a pro-drug form of aprepitant. fosaprepitant : A morpholine derivative that is the (1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl ether of (3-{[(2R,3S)-3-(4-fluorophenyl)-2-hydroxymorpholin-4-yl]methyl}-5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl)phosphonic acid. | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; cyclic acetal; morpholines; phosphoramide; triazoles | antiemetic; neurokinin-1 receptor antagonist; prodrug |
| rifabutin [no description available] | 3.23 | 1 | 0 | ||
| levomefolate calcium levomefolate calcium: an ingredient in Contraceptives, Oral, Combined. levomefolate calcium : An organic calcium salt of (6S)-5-methyltetrahydrofolic acid. | 3.23 | 1 | 0 | organic calcium salt | antidepressant |
| Condition | Indicated | Relationship Strength | Studies | Trials |
|---|---|---|---|---|
| Acute Liver Injury, Drug-Induced [description not available] | 0 | 3.04 | 1 | 0 |
| Chemical and Drug Induced Liver Injury A spectrum of clinical liver diseases ranging from mild biochemical abnormalities to ACUTE LIVER FAILURE, caused by drugs, drug metabolites, herbal and dietary supplements and chemicals from the environment. | 0 | 3.04 | 1 | 0 |
| Congenital Zika Syndrome [description not available] | 0 | 2.25 | 1 | 0 |
| Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases. | 0 | 3.99 | 4 | 0 |
| Zika Virus Infection A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME. | 0 | 2.25 | 1 | 0 |
| Bladder, Overactive [description not available] | 0 | 21.01 | 191 | 65 |
| Bladder Disorder, Neurogenic [description not available] | 0 | 7.79 | 11 | 5 |
| MS (Multiple Sclerosis) [description not available] | 0 | 2.63 | 2 | 0 |
| Injuries, Spinal Cord [description not available] | 0 | 6.23 | 5 | 2 |
| Urinary Bladder, Neurogenic Dysfunction of the URINARY BLADDER due to disease of the central or peripheral nervous system pathways involved in the control of URINATION. This is often associated with SPINAL CORD DISEASES, but may also be caused by BRAIN DISEASES or PERIPHERAL NERVE DISEASES. | 1 | 9.79 | 11 | 5 |
| Multiple Sclerosis An autoimmune disorder mainly affecting young adults and characterized by destruction of myelin in the central nervous system. Pathologic findings include multiple sharply demarcated areas of demyelination throughout the white matter of the central nervous system. Clinical manifestations include visual loss, extra-ocular movement disorders, paresthesias, loss of sensation, weakness, dysarthria, spasticity, ataxia, and bladder dysfunction. The usual pattern is one of recurrent attacks followed by partial recovery (see MULTIPLE SCLEROSIS, RELAPSING-REMITTING), but acute fulminating and chronic progressive forms (see MULTIPLE SCLEROSIS, CHRONIC PROGRESSIVE) also occur. (Adams et al., Principles of Neurology, 6th ed, p903) | 0 | 7.63 | 2 | 0 |
| Spinal Cord Injuries Penetrating and non-penetrating injuries to the spinal cord resulting from traumatic external forces (e.g., WOUNDS, GUNSHOT; WHIPLASH INJURIES; etc.). | 0 | 6.23 | 5 | 2 |
| Urinary Bladder, Overactive Symptom of overactive detrusor muscle of the URINARY BLADDER that contracts with abnormally high frequency and urgency. Overactive bladder is characterized by the frequent feeling of needing to urinate during the day, during the night, or both. URINARY INCONTINENCE may or may not be present. | 1 | 23.01 | 191 | 65 |
| Urinary Incontinence Involuntary loss of URINE, such as leaking of urine. It is a symptom of various underlying pathological processes. Major types of incontinence include URINARY URGE INCONTINENCE and URINARY STRESS INCONTINENCE. | 1 | 13.32 | 20 | 12 |
| Urge Incontinence [description not available] | 0 | 11.81 | 22 | 10 |
| Anxiety Feelings or emotions of dread, apprehension, and impending disaster but not disabling as with ANXIETY DISORDERS. | 0 | 7.31 | 1 | 0 |
| Depression Depressive states usually of moderate intensity in contrast with MAJOR DEPRESSIVE DISORDER present in neurotic and psychotic disorders. | 0 | 7.31 | 1 | 0 |
| Urinary Incontinence, Urge Involuntary discharge of URINE that is associated with an abrupt and strong desire to void. It is usually related to the involuntary contractions of the detrusor muscle of the bladder (detrusor hyperreflexia or detrusor instability). | 0 | 11.81 | 22 | 10 |
| Amentia [description not available] | 0 | 3.68 | 2 | 0 |
| Dementia An acquired organic mental disorder with loss of intellectual abilities of sufficient severity to interfere with social or occupational functioning. The dysfunction is multifaceted and involves memory, behavior, personality, judgment, attention, spatial relations, language, abstract thought, and other executive functions. The intellectual decline is usually progressive, and initially spares the level of consciousness. | 0 | 3.68 | 2 | 0 |
| Blood Pressure, High [description not available] | 0 | 2.93 | 3 | 0 |
| Hypertension Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more. | 0 | 2.93 | 3 | 0 |
| Urinary Retention Inability to empty the URINARY BLADDER with voiding (URINATION). | 0 | 2.41 | 1 | 0 |
| Autonomic Hyperreflexia [description not available] | 0 | 5.9 | 3 | 2 |
| Autonomic Dysreflexia A syndrome associated with damage to the spinal cord above the mid thoracic level (see SPINAL CORD INJURIES) characterized by a marked increase in the sympathetic response to minor stimuli such as bladder or rectal distention. Manifestations include HYPERTENSION; TACHYCARDIA (or reflex bradycardia); FEVER; FLUSHING; and HYPERHIDROSIS. Extreme hypertension may be associated with a STROKE. (From Adams et al., Principles of Neurology, 6th ed, pp538 and 1232; J Spinal Cord Med 1997;20(3):355-60) | 1 | 7.9 | 3 | 2 |
| Lower Urinary Tract Symptom [description not available] | 0 | 5.7 | 3 | 2 |
| Idiopathic Parkinson Disease [description not available] | 0 | 4 | 2 | 1 |
| Parkinson Disease A progressive, degenerative neurologic disease characterized by a TREMOR that is maximal at rest, retropulsion (i.e. a tendency to fall backwards), rigidity, stooped posture, slowness of voluntary movements, and a masklike facial expression. Pathologic features include loss of melanin containing neurons in the substantia nigra and other pigmented nuclei of the brainstem. LEWY BODIES are present in the substantia nigra and locus coeruleus but may also be found in a related condition (LEWY BODY DISEASE, DIFFUSE) characterized by dementia in combination with varying degrees of parkinsonism. (Adams et al., Principles of Neurology, 6th ed, p1059, pp1067-75) | 0 | 4 | 2 | 1 |
| Colonic Inertia Symptom characterized by the passage of stool once a week or less. | 0 | 7.93 | 7 | 1 |
| Constipation Infrequent or difficult evacuation of FECES. These symptoms are associated with a variety of causes, including low DIETARY FIBER intake, emotional or nervous disturbances, systemic and structural disorders, drug-induced aggravation, and infections. | 0 | 7.93 | 7 | 1 |
| Sensitivity and Specificity Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed) | 0 | 3.94 | 2 | 1 |
| Cognitive Decline [description not available] | 0 | 3.23 | 1 | 0 |
| Prodromal Characteristics [description not available] | 0 | 3.23 | 1 | 0 |
| Cognitive Dysfunction Diminished or impaired mental and/or intellectual function. | 0 | 3.23 | 1 | 0 |
| Nycturia [description not available] | 0 | 6.43 | 5 | 3 |
| Nocturia Frequent URINATION at night that interrupts sleep. It is often associated with outflow obstruction, DIABETES MELLITUS, or bladder inflammation (CYSTITIS). | 0 | 11.43 | 5 | 3 |
| Alloxan Diabetes [description not available] | 0 | 2.15 | 1 | 0 |
| Impotence [description not available] | 0 | 2.15 | 1 | 0 |
| Erectile Dysfunction The inability in the male to have a PENILE ERECTION due to psychological or organ dysfunction. | 0 | 7.15 | 1 | 0 |
| Asialia [description not available] | 0 | 3.42 | 2 | 0 |
| Xerostomia Decreased salivary flow. | 0 | 3.42 | 2 | 0 |
| Diabetes Mellitus A heterogeneous group of disorders characterized by HYPERGLYCEMIA and GLUCOSE INTOLERANCE. | 0 | 2.17 | 1 | 0 |
| Electrocardiogram QT Prolonged [description not available] | 0 | 3.89 | 2 | 1 |
| Torsade de Pointes [description not available] | 0 | 2.17 | 1 | 0 |
| Long QT Syndrome A condition that is characterized by episodes of fainting (SYNCOPE) and varying degree of ventricular arrhythmia as indicated by the prolonged QT interval. The inherited forms are caused by mutation of genes encoding cardiac ion channel proteins. The two major forms are ROMANO-WARD SYNDROME and JERVELL-LANGE NIELSEN SYNDROME. | 0 | 3.89 | 2 | 1 |
| Ischemia A hypoperfusion of the BLOOD through an organ or tissue caused by a PATHOLOGIC CONSTRICTION or obstruction of its BLOOD VESSELS, or an absence of BLOOD CIRCULATION. | 0 | 7.31 | 1 | 0 |
| Symptom Cluster [description not available] | 0 | 4.61 | 3 | 0 |
| Syndrome A characteristic symptom complex. | 0 | 4.61 | 3 | 0 |
| Adenoma, Prostatic [description not available] | 0 | 6.52 | 4 | 4 |
| Prostatic Hyperplasia Increase in constituent cells in the PROSTATE, leading to enlargement of the organ (hypertrophy) and adverse impact on the lower urinary tract function. This can be caused by increased rate of cell proliferation, reduced rate of cell death, or both. | 0 | 6.52 | 4 | 4 |
| Muscle Contraction A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments. | 0 | 3.41 | 2 | 0 |
| Urinary Incontinence, Stress Involuntary discharge of URINE as a result of physical activities that increase abdominal pressure on the URINARY BLADDER without detrusor contraction or overdistended bladder. The subtypes are classified by the degree of leakage, descent and opening of the bladder neck and URETHRA without bladder contraction, and sphincter deficiency. | 0 | 4.4 | 1 | 1 |
| Long Sleeper Syndrome [description not available] | 0 | 3.48 | 1 | 1 |
| Sleep Wake Disorders Abnormal sleep-wake schedule or pattern associated with the CIRCADIAN RHYTHM which affect the length, timing, and/or rigidity of the sleep-wake cycle relative to the day-night cycle. | 0 | 3.48 | 1 | 1 |
| Liver Dysfunction [description not available] | 0 | 3.48 | 1 | 1 |
| Liver Diseases Pathological processes of the LIVER. | 0 | 3.48 | 1 | 1 |
| Intraocular Pressure The pressure of the fluids in the eye. | 0 | 3.51 | 1 | 1 |
| Aging The gradual irreversible changes in structure and function of an organism that occur as a result of the passage of time. | 0 | 5.85 | 4 | 2 |
| Mouth Diseases Diseases involving the MOUTH. | 0 | 3.51 | 1 | 1 |
| Frigidity [description not available] | 0 | 3.51 | 1 | 1 |
| Sexual Dysfunctions, Psychological Disturbances in sexual desire and the psychophysiologic changes that characterize the sexual response cycle and cause marked distress and interpersonal difficulty. (APA, DSM-IV, 1994) | 0 | 3.51 | 1 | 1 |
| Adverse Drug Event [description not available] | 0 | 2.49 | 2 | 0 |
| Drug-Related Side Effects and Adverse Reactions Disorders that result from the intended use of PHARMACEUTICAL PREPARATIONS. Included in this heading are a broad variety of chemically-induced adverse conditions due to toxicity, DRUG INTERACTIONS, and metabolic effects of pharmaceuticals. | 0 | 2.49 | 2 | 0 |
| Urination Disorders Abnormalities in the process of URINE voiding, including bladder control, frequency of URINATION, as well as the volume and composition of URINE. | 0 | 3.43 | 1 | 1 |
| Kidney Failure A severe irreversible decline in the ability of kidneys to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism. | 0 | 3.43 | 1 | 1 |
| Renal Insufficiency Conditions in which the KIDNEYS perform below the normal level in the ability to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism. Renal insufficiency can be classified by the degree of kidney damage (as measured by the level of PROTEINURIA) and reduction in GLOMERULAR FILTRATION RATE. | 0 | 3.43 | 1 | 1 |
| Urethral Obstruction Partial or complete blockage in any part of the URETHRA that can lead to difficulty or inability to empty the URINARY BLADDER. It is characterized by an enlarged, often damaged, bladder with frequent urges to void. | 0 | 2.46 | 2 | 0 |
| Bilateral Headache [description not available] | 0 | 3.44 | 1 | 1 |
| Headache The symptom of PAIN in the cranial region. It may be an isolated benign occurrence or manifestation of a wide variety of HEADACHE DISORDERS. | 0 | 3.44 | 1 | 1 |
| Hepatic Insufficiency Conditions in which the LIVER functions fall below the normal ranges. Severe hepatic insufficiency may cause LIVER FAILURE or DEATH. Treatment may include LIVER TRANSPLANTATION. | 0 | 3.45 | 1 | 1 |
| Cirrhosis, Liver [description not available] | 0 | 3.45 | 1 | 1 |
| Liver Cirrhosis Liver disease in which the normal microcirculation, the gross vascular anatomy, and the hepatic architecture have been variably destroyed and altered with fibrous septa surrounding regenerated or regenerating parenchymal nodules. | 0 | 3.45 | 1 | 1 |
| Cognition Disorders Disorders characterized by disturbances in mental processes related to learning, thinking, reasoning, and judgment. | 0 | 2.06 | 1 | 0 |
| Chronic Illness [description not available] | 0 | 2.99 | 1 | 0 |
| Chronic Disease Diseases which have one or more of the following characteristics: they are permanent, leave residual disability, are caused by nonreversible pathological alteration, require special training of the patient for rehabilitation, or may be expected to require a long period of supervision, observation, or care (Dictionary of Health Services Management, 2d ed). For epidemiological studies chronic disease often includes HEART DISEASES; STROKE; CANCER; and diabetes (DIABETES MELLITUS, TYPE 2). | 0 | 2.99 | 1 | 0 |