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. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 9838022 |
| CHEMBL ID | 1201776 |
| CHEBI ID | 135935 |
| SCHEMBL ID | 116924 |
| MeSH ID | M0515162 |
| Synonym |
|---|
| cg-5503 |
| bn-200 |
| tapentadol |
| tapentadol (usan/inn) |
| D06007 |
| 175591-23-8 |
| CHEBI:135935 |
| 3-((1r,2r)-3-(dimethylamino)-1-ethyl-2-methylpropyl)phenol |
| BCP9000118 |
| nsc-759619 |
| bdbm50386381 |
| (r,r)-tapentadol |
| AKOS015951190 |
| CHEMBL1201776 |
| cg5503 ir |
| unii-h8a007m585 |
| hsdb 8309 |
| h8a007m585 , |
| bn 200 |
| cg5503 |
| cg 5503 |
| bn 200 (base) |
| phenol, 3-((1r,2r)-3-(dimethylamino)-1-ethyl-2-methylpropyl)- |
| dea no. 9780 |
| tapentadol [usan:inn] |
| cg5503 (base) |
| nsc 759619 |
| 3-((2r,3r)-1-(dimethylamino)-2-methylpentan-3-yl)phenol |
| tapentadol [who-dd] |
| tapentadol [mi] |
| tapentadol [vandf] |
| 3-[(1r,2r)-3-(dimethylamino)-1-ethyl-2-methylpropyl]phenol |
| tapentadol [mart.] |
| tapentadol [inn] |
| tapentadol [usan] |
| DB06204 |
| CS-M0020 |
| (1r,2r)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol |
| 3-[(2r,3r)-1-(dimethylamino)-2-methylpentan-3-yl]phenol |
| KWTWDQCKEHXFFR-SMDDNHRTSA-N |
| SCHEMBL116924 |
| 3-[(2r,3r)-1-dimethylamino-2-methylpentan-3-yl]phenol |
| gtpl7477 |
| DTXSID30170003 , |
| phenol, 3-[(1r,2r)-3-(dimethylamino)-1-ethyl-2-methylpropyl]- |
| Q414463 |
| FT-0699883 |
| 3-[3-(dimethylamino)-1-ethyl-2-methylpropyl]phenol |
| AR-270/43507984 |
| A26964 |
| dtxcid1092494 |
| tapentadolum |
| tapentadol (mart.) |
Tapentadol is an atypical opioid with mu-receptor affinity and noradrenaline reuptake inhibition approved for use in Australia in 2011. It is a centrally acting analgesic prescribed for the treatment of moderate to severe pain.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Tapentadol is a centrally acting analgesic with a dual mechanism of action. " | ( Tapentadol shows lower intrinsic efficacy at µ receptor than morphine and oxycodone. Connor, M; Manandhar, P; Santiago, M, 2022) | 3.61 |
| "Tapentadol is a centrally acting opioid analgesic prescribed for the treatment of moderate to severe pain. " | ( Characteristics of fatal tapentadol-related toxicity in Australia. Darke, S; Duflou, J; Farrell, M; Lappin, J; Peacock, A, 2022) | 2.47 |
| "Tapentadol is an atypical opioid with mu-receptor affinity and noradrenaline reuptake inhibition approved for use in Australia in 2011. " | ( Tapentadol exposures and poisonings in Australia. Allen, K; Berling, I; Brown, J; Chan, BS; Chiew, AL; Isbister, G; Isoardi, K; Mirabella, J, 2022) | 3.61 |
| "Tapentadol is an analgesic compound that acts centrally to attenuate pain. " | ( Tapentadol: A Review of Experimental Pharmacology Studies, Clinical Trials, and Recent Findings. Alshehri, FS, 2023) | 3.8 |
| "Tapentadol is an opioid that has less stomach/gut side effects, causes less sleepiness, is less likely to cause serious breathing impairment, may have less symptoms when stopping the medication and less chance of long-term (more than 3 months) use compared with a more commonly used opioid (oxycodone)." | ( Considerations for perioperative opioid analgesic stewardship in Australia: a focus on tapentadol. Ternel Lebret, SC, 2023) | 1.85 |
| "Tapentadol is a molecule incorporating mu opioid receptor agonism and norepinephrine reuptake inhibition to provide analgesia, with the potential for a lower incidence of gastrointestinal side effects than full mu opioid agonists. " | ( Evaluation of Abuse and Route of Administration of Extended-Release Tapentadol Among Treatment-Seeking Individuals, as Captured by the Addiction Severity Index-Multimedia Version (ASI-MV). Beaumont, J; Butler, SF; Dailey-Govoni, ST; Green, JL; Vosburg, SK, 2020) | 2.24 |
| "Tapentadol is an innovative drug for the treatment of chronic severe pain, with a dual mechanism of action combining µ-opioid receptors agonism and noradrenaline re-uptake inhibition (NRI)." | ( Efficacy of tapentadol prolonged release for pre- and post-operative low back pain: a prospective observational study. Bagaphou, TC; Cerotto, V; Gori, F, 2019) | 1.61 |
| "Tapentadol is an innovative dual-acting analgesic molecule, which combines two mechanisms of action, namely MOR agonism and NRI." | ( Tapentadol prolonged release in the treatment of musculoskeletal pain: an innovative pharmacological option. Evangelista, M; Finco, G; Marinangeli, F, 2019) | 2.68 |
| "Tapentadol is a synthetic opioid analgesic available in India since 2011. " | ( Tapentadol abuse and dependence in India. Benegal, V; Chand, P; Kandasamy, A; Mahadevan, J; Mukherjee, D; Murthy, P; Saha, P; Shukla, L, 2020) | 3.44 |
| "Tapentadol is a central analgesic with an improved tolerability profile that may be particularly beneficial to the elderly CLBP." | ( Efficacy and tolerability of tapentadol for the treatment of chronic low back pain in elderly patients. Ambrosio, F; Freo, U; Furnari, M; Navalesi, P, 2021) | 1.63 |
| "Tapentadol is a dual-acting mu-opioid receptor agonist and noradrenaline reuptake inhibitor with non-inferior analgesic efficacy to oxycodone and better gastrointestinal tolerability than full mu-opioid receptor agonists. " | ( Tapentadol is effective in the management of moderate-to-severe cancer-related pain in opioid-naïve and opioid-tolerant patients: a retrospective study. Koitabashi, T; Sazuka, S, 2020) | 3.44 |
| "Tapentadol is an opioid, which acts as a μ-opioid receptor agonist and inhibits noradrenaline reuptake in the central nervous system. " | ( Tapentadol versus oxycodone analgesia and side effects after laparoscopic hysterectomy: A randomised controlled trial. Comelon, M; Drægni, T; Lenz, H; Lieng, M; Raeder, J, 2021) | 3.51 |
| "Tapentadol is a combined opioid agonist and norepinephrine reuptake inhibitor with fewer gastrointestinal side effects at equianalgesic doses compared with classical strong opioids. " | ( Tapentadol results in less deterioration of gastrointestinal function and symptoms than standard opioid therapy in healthy male volunteers. Drewes, AM; Frøkjaer, JB; Hansen, TM; Krogh, K; Mark, EB; Nedergaard, RB; Nissen, TD; Scott, SM, 2021) | 3.51 |
| "Tapentadol is a centrally acting analgesic that has been available for the management of acute and chronic pain in routine clinical practice since 2009." | ( Review of Post-Marketing Safety Data on Tapentadol, a Centrally Acting Analgesic. Elling, C; Heisig, F; Sohns, M; Stollenwerk, A; von Zabern, D, 2018) | 2.19 |
| "Tapentadol is a new drug that has a dual mechanism as both an opioid agonist and noradrenalin reuptake inhibitor." | ( Efficacy of tapentadol for first-line opioid-resistant neuropathic pain in Japan. Akechi, T; Kataoka, T; Kimura, K; Kondo, Y; Naiki, T; Sakamoto, N; Sato, N; Sugiyama, Y; Tasaki, Y, 2018) | 1.58 |
| "Tapentadol is an analgesic that acts as an agonist of µ opioid receptors (MOR) and that inhibits noradrenaline reuptake. " | ( Opioid and noradrenergic contributions of tapentadol to the inhibition of locus coeruleus neurons in the streptozotocin rat model of polyneuropathic pain. Berrocoso, E; Borges, GDS; Mico, JA; Torres-Sanchez, S, 2018) | 2.19 |
| "Tapentadol is a novel drug of opioid pain reliever, which is extensively metabolized primarily through conjugation. " | ( [A simple method for quantification of tapentadol in dog plasma by liquid chromatography-tandem mass spectrometry and evaluation of the effects of conjugated metabolites on tapentadol]. Chen, XY; Dai, XJ; Liang, G; Lu, YM; Qin, MJ; Zhong, DF, 2016) | 2.15 |
| "Tapentadol is a centrally acting opioid analgesic which has partial opioid agonistic and norepinephrine reuptake inhibitor action similar to its nearest congener and tramadol though with a relatively higher μ-affinity. " | ( Is tapentadol a potential Trojan horse in the postdextropropoxyphene era in India? Basu, A; Chand, PK; Ithal, D; Mahadevan, J; Murthy, P; Selvaraj, S, ) | 2.2 |
| "Tapentadol is a centrally acting synthetic analgesic which is prescribed for the treatment of a range of chronic pain conditions. " | ( The Increasing Use and Abuse of Tapentadol and Its Incorporation Into a Validated Quantitative Method. Charlwood, C; Kostakis, C; Nash, C; Partridge, E; Scott, T; Teoh, E, 2018) | 2.21 |
| "Tapentadol is a centrally acting analgesic with a dual mode of action as a μ-opioid receptor (MOR) agonist and a noradrenaline reuptake inhibitor (NRI). " | ( Tapentadol - A representative of a new class of MOR-NRI analgesics. Kocot-Kępska, M; Leppert, W; Mika, J; Przewłocka, B; Wordliczek, J; Zajączkowska, R, 2018) | 3.37 |
| "Tapentadol is a dual-acting analgesic drug μ-opioid receptor (MOR) agonist/norepinephrine reuptake inhibitor, carrying a lower risk for opioid withdrawal symptoms and opioid-related adverse effects in comparison to potent opioid drugs." | ( Long-term, prolonged-release oral tapentadol for the treatment of refractory chronic low back pain: a single-center, observational study. Deidda, C; Demelas, I; Evangelista, M; Finco, G; Mura, P; Musu, M; Saba, M; Sardo, S, 2018) | 1.48 |
| "Tapentadol is a novel atypical opioid. " | ( Toxicity of tapentadol: a systematic review. Channell, JS; Schug, S, 2018) | 2.3 |
| "Tapentadol is an orally active analgesic with a similar structure to tramadol. " | ( Quantitation of Tapentadol by Liquid Chromatography: Tandem Mass Spectrometry. Handy, RP; Jones, GR, 2019) | 2.3 |
| "Tapentadol is a centrally acting analgesic with μ-agonistic activity combined with noradrenaline reuptake inhibition. " | ( Cornea nerve fibre state determines analgesic response to tapentadol in fibromyalgia patients without effective endogenous pain modulation. Dahan, A; Niesters, M; van de Donk, T; van Velzen, M, 2019) | 2.2 |
| "Tapentadol is a novel analgesic that activates mu-opioid receptors and blocks norepinephrine reuptake. " | ( Miotic and subject-rated effects of therapeutic doses of tapentadol, tramadol, and hydromorphone in occasional opioid users. Glaser, PE; Rush, CR; Stoops, WW, 2013) | 2.08 |
| "Tapentadol is a novel centrally acting drug that combines mu-opioid receptor (MOR) agonism and noradrenaline reuptake inhibition (NRI), producing analgesic effects in various painful conditions. " | ( Effect of tapentadol on neurons in the locus coeruleus. Alba-Delgado, C; Berrocoso, E; Llorca-Torralba, M; Mico, JA; Torres-Sanchez, S, 2013) | 2.23 |
| "Tapentadol hydrochloride is a synthetic opioid used as a centrally acting analgesic and effective in both experimental and clinical pain." | ( Application of design of experiment for floating drug delivery of tapentadol hydrochloride. Jagdale, SC; Kuchekar, BS; Patil, S, 2013) | 1.35 |
| "Tapentadol is a dual action molecule with mu opioid agonist and norepinephrine (NE) reuptake blocking activity that has recently been introduced for the treatment of moderate to severe pain. " | ( Opioid and noradrenergic contributions of tapentadol in experimental neuropathic pain. Badghisi, H; Meske, DS; Ossipov, MH; Oyarzo, J; Porreca, F; Xie, JY, 2014) | 2.11 |
| "Tapentadol is a μ-opioid receptor (MOR) agonist and norepinephrine reuptake inhibitor (NRI) with established efficacy in neuropathic pain in patients and intrinsic synergistic interaction of both mechanisms as demonstrated in rodents. " | ( Spinal-supraspinal and intrinsic μ-opioid receptor agonist-norepinephrine reuptake inhibitor (MOR-NRI) synergy of tapentadol in diabetic heat hyperalgesia in mice. Christoph, T; De Vry, J; Schröder, W; Tallarida, RJ; Tzschentke, TM, 2013) | 2.04 |
| "Tapentadol is a µ -opioid receptors agonist as well as an inhibitor of noradrenaline reuptake. " | ( [Polyneuropathic pain therapy with a patient suffering from generalized castrate- resistant prostate cancer - clinical case report]. Fiala, O; Fínek, J; Holubec, L; Matějka, VM; Mrázková, P, 2013) | 1.83 |
| "Tapentadol-ER is an opioid analgesic commonly used for the treatment of moderate-to-severe chronic pain that contains a unique dual mechanism acting as both a weak mu-opiod receptor agonist and norepinephine-reuptake inhibitor." | ( Tapentadol-ER for the treatment of diabetic peripheral neuropathy. Games, G; Hutchison, A, 2013) | 2.55 |
| "Tapentadol is a novel analgesic that combines moderate μ-opioid receptor agonism and noradrenaline reuptake inhibition in a single molecule. " | ( μ-Opioid receptor activation and noradrenaline transport inhibition by tapentadol in rat single locus coeruleus neurons. Christie, MJ; Sadeghi, M; Tzschentke, TM, 2015) | 2.09 |
| "Tapentadol is a new partial µ-receptor opioid agonist with a combined action on norepinephrine-induced analgesia, representing a promising drug in terms of less side effects at equianalgesic doses compared with pure agonists." | ( Opioids in the treatment of postoperative pain: old drugs with new options? Raeder, J, 2014) | 1.12 |
| "Tapentadol is a novel, centrally-acting analgesic drug, with an analgesic efficacy comparable to that of strong opioids such as oxycodone and morphine. " | ( The mu-opioid receptor agonist/noradrenaline reuptake inhibition (MOR-NRI) concept in analgesia: the case of tapentadol. Christoph, T; Kögel, BY; Tzschentke, TM, 2014) | 2.06 |
| "Tapentadol is an analgesic agent for treatment of acute and chronic pain that activates the µ-opioid receptor combined with inhibition of neuronal norepinephrine reuptake. " | ( Tapentadol potentiates descending pain inhibition in chronic pain patients with diabetic polyneuropathy. Aarts, L; Dahan, A; Drewes, AM; Niesters, M; Proto, PL; Sarton, EY, 2014) | 3.29 |
| "Tapentadol is a novel dual-action drug, both stimulating inhibitory μ-opioid receptors (MOR) and mediating noradrenaline reuptake inhibition (NRI) leading to activation of the inhibitory α-2 adrenoceptor." | ( Spinal neuronal correlates of tapentadol analgesia in cancer pain: a back-translational approach. Dickenson, AH; Falk, S; Heegaard, A; Mercadante, S; Patel, R, 2015) | 1.43 |
| "Tapentadol is an opioid similar to tramadol." | ( Tapentadol. Acute or chronic pain: no therapeutic advance. , 2014) | 2.57 |
| "Tapentadol (Nucynta) is a centrally acting opioid analgesic prescribed for the treatment of moderate to severe acute pain. " | ( Case report of a fatal intoxication by Nucynta. Ali, Z; Fowler, DR; Franco, DM; Levine, B; Middleberg, RA, 2014) | 1.85 |
| "Tapentadol is a newer molecule that produces analgesia in various pain models through two inhibitory mechanisms, namely central μ-opioid receptor (MOR) agonism and noradrenaline reuptake inhibition." | ( The influence of μ-opioid and noradrenaline reuptake inhibition in the modulation of pain responsive neurones in the central amygdala by tapentadol in rats with neuropathy. Dickenson, AH; Friend, LV; Gonçalves, L, 2015) | 1.34 |
| "Tapentadol is a novel, centrally acting analgesic with 2 mechanisms of action, MOR agonism and noradrenaline (NA) reuptake inhibition in a single molecule. " | ( Determination of tapentadol and tapentadol-O-glucuronide in human serum samples by UPLC-MS/MS. de Vries, R; Hillewaert, V; Langhans, M; Pusecker, K; Sips, L; Terlinden, R; Timmerman, P; Verhaeghe, T, 2015) | 2.2 |
| "Tapentadol is an opioid and norepinephrine re-uptake inhibitor, which may cause a lower incidence (and severity) of adverse effects compared to other strong opioids." | ( Tapentadol for chronic musculoskeletal pain in adults. Alarcão, J; Costa, J; Fareleira, F; Santos, J; Vaz-Carneiro, A, 2015) | 2.58 |
| "Tapentadol is a relatively new analgesic. " | ( Comparison of tapentadol with tramadol for analgesia after cardiac surgery. Iyer, SK; Mohan, G; Ramakrishnan, S; Theodore, S, ) | 1.93 |
| "Tapentadol is a novel, centrally acting analgesic medicine acting at the μ-opioid receptor and inhibiting noradrenaline reuptake." | ( Oral tapentadol for cancer pain. Bell, RF; Derry, S; Naessens, K; Wiffen, PJ, 2015) | 1.65 |
| "Tapentadol is a novel, centrally acting analgesic that has been recently commercialized for the treatment of chronic pain." | ( Chronic pain: the burden of disease and treatment innovations. Caporali, R; Monti, S, 2015) | 1.14 |
| "Tapentadol is a centrally acting analgesic with two mechanisms of action, µ-opioid receptor agonism and noradrenaline reuptake inhibition. " | ( Population Pharmacokinetic Modeling of Tapentadol Extended Release (ER) in Healthy Subjects and Patients with Moderate or Severe Chronic Pain. Drenth, HJ; Huntjens, DR; Liefaard, LC; Nandy, P; Vermeulen, A, 2016) | 2.15 |
| "Tapentadol(TP)is a new strong opioid analgesicthat has both m-opioid receptor(MOR)effects and norepinephrine reuptake inhibitor(NRI)effects. " | ( [Clinical Utility of Tapentadol]. Hiratsuka, R; Ikeda, H; Ishigure, H; Kanazawa, K; Shimoda, A; Yoshizawa, A; Yoshizawa, T, 2015) | 2.18 |
| "Tapentadol ER is a recently approved centrally acting analgesic with synergistic mechanisms of action: μ-opioid receptor agonism and inhibition of norepinephrine reuptake." | ( Diversion and Illicit Sale of Extended Release Tapentadol in the United States. Bebarta, VS; Brownstein, JS; Burke, JJ; Dart, RC; Dasgupta, N; Freifeld, CC; Kurtz, SP; Le Lait, MC; Stivers, Y; Surratt, HL, 2016) | 1.41 |
| "Tapentadol (TAP) is an analgesic agent indicated for the management of different types of pain. " | ( A tapentadol related fatality: Case report with postmortem concentrations. Aldridge, L; Cantrell, FL; Mallett, P; McIntyre, IM; Verilhac, K, 2016) | 2.6 |
| "Tapentadol is an analgesic drug with a dual synergistic mechanism of action: µ-opioid receptor agonism and noradrenaline reuptake inhibition." | ( Effect of Tapentadol on Splenic Cytokine Production in Mice. Amodeo, G; Franchi, S; Gandolla, M; Moschetti, G; Panerai, AE; Sacerdote, P, 2017) | 1.58 |
| "Tapentadol is a new, centrally acting analgesic with two mechanisms of action, combining μ-opioid agonism and norepinephrine reuptake inhibition in a single molecule. " | ( The efficacy and tolerability of multiple-dose tapentadol immediate release for the relief of acute pain following orthopedic (bunionectomy) surgery . Daniels, S; Okamoto, A; Stegmann, JU; Steup, A; Upmalis, D; Weber, H, 2008) | 2.05 |
| "Tapentadol is a novel, centrally acting analgesic with two modes of action, combining mu-opioid agonism and norepinephrine reuptake inhibition in a single molecule. " | ( Single dose analgesic efficacy of tapentadol in postsurgical dental pain: the results of a randomized, double-blind, placebo-controlled study. Black, P; Desjardins, P; Goldberg, J; Kleinert, R; Lange, C; Steup, A, 2008) | 2.07 |
| "Tapentadol is a novel, centrally acting analgesic with two mechanisms of action, mu-opioid receptor agonism and norepinephrine reuptake inhibition, in a single molecule. " | ( Tolerability of tapentadol immediate release in patients with lower back pain or osteoarthritis of the hip or knee over 90 days: a randomized, double-blind study. Hale, M; Lange, C; Okamoto, A; Rauschkolb, C; Upmalis, D, 2009) | 2.14 |
| "Tapentadol (Nucynta) is a centrally acting oral analgesic with opioid and adrenergic activity." | ( Tapentadol (Nucynta)--a new analgesic. , 2009) | 2.52 |
| "Tapentadol is a novel, centrally acting analgesic with two mechanisms of action: micro-opioid receptor agonism and norepinephrine reuptake inhibition. " | ( Tapentadol immediate release for the relief of moderate-to-severe acute pain. Hartrick, CT, 2009) | 3.24 |
| "Tapentadol is a novel analgesic with two modes of action, mu-opioid receptor (MOR) agonism and noradrenaline (NA) reuptake inhibition." | ( Tapentadol, but not morphine, selectively inhibits disease-related thermal hyperalgesia in a mouse model of diabetic neuropathic pain. Christoph, T; De Vry, J; Tzschentke, TM, 2010) | 2.52 |
| "Tapentadol hydrochloride is a centrally acting oral analgesic approved by the US Food and Drug Administration in November 2008 for the treatment of moderate to severe acute pain. " | ( Tapentadol hydrochloride: a centrally acting oral analgesic. Spruill, WJ; Wade, WE, 2009) | 3.24 |
| "Tapentadol appears to be a well-tolerated and effective analgesic for the treatment of moderate to severe acute pain. " | ( Tapentadol hydrochloride: a centrally acting oral analgesic. Spruill, WJ; Wade, WE, 2009) | 3.24 |
| "Tapentadol is a novel, centrally acting analgesic combining micro-opioid receptor (MOR) agonism and noradrenaline (NA) reuptake inhibition in a single molecule. " | ( In vitro and in vivo characterization of tapentadol metabolites. Englberger, W; Kogel, BY; Terlinden, R; Tzschentke, TM, ) | 1.84 |
| "Tapentadol is a novel opioid agent with a dual mode of analgesic action. " | ( Tapentadol immediate-release for acute pain. Hartrick, CT, 2010) | 3.25 |
| "Tapentadol is a novel, centrally acting analgesic with mu-opioid receptor agonist and norepinephrine reuptake inhibitor activity." | ( Efficacy and safety of Tapentadol extended release compared with oxycodone controlled release for the management of moderate to severe chronic pain related to osteoarthritis of the knee: a randomized, double-blind, placebo- and active-controlled phase III Afilalo, M; Etropolski, MS; Haeussler, J; Kelly, K; Kuperwasser, B; Lange, B; Okamoto, A; Rauschkolb, C; Steup, A; Van Hove, I, 2010) | 2.11 |
| "Tapentadol is a novel, centrally acting analgesic with 2 mechanisms of action: µ-opioid receptor agonism and norepinephrine reuptake inhibition. " | ( Long-term safety and tolerability of tapentadol extended release for the management of chronic low back pain or osteoarthritis pain. Etropolski, MS; Gilbert, J; Grond, S; Häufel, T; Kuperwasser, B; Lange, B; Lange, R; McCann, B; Rauschkolb, C; Steup, A; Wild, JE, ) | 1.85 |
| "Tapentadol (Nucynta) is an orally active, centrally acting synthetic analgesic that is thought to exert its analgesic effects via two mechanisms of action (mu-opioid receptor agonism and norepinephrine reuptake inhibition). " | ( Tapentadol immediate release: a review of its use in the treatment of moderate to severe acute pain. Frampton, JE, 2010) | 3.25 |
| "Tapentadol is a new, centrally active analgesic agent with two modes of action--mu opioid receptor agonism and norepinephrine reuptake inhibition--and the immediate-release (IR) formulation is approved in the US for the relief of moderate to severe acute pain. " | ( Population pharmacokinetics of tapentadol immediate release (IR) in healthy subjects and patients with moderate or severe pain. Lin, R; Nandy, P; Smit, JW; Stuyckens, K; Terlinden, R; Xu, XS, 2010) | 2.09 |
| "Tapentadol HCI is an opioid (narcotic) analgesic, which also inhibits norepinephrine reuptake. " | ( Analgesic update: tapentadol hydrochloride. Golubic, S; Hersh, EV; Moore, PA, 2010) | 2.14 |
| "Tapentadol is a newly approved novel analgesic drug with a dual mode of action: a mu-opioid agonist and an inhibitor of norepinephrine reuptake (MOR-NRI). " | ( Tapentadol for pain: a treatment evaluation. Hartrick, CT; Rodríguez Hernandez, JR, 2012) | 3.26 |
| "Tapentadol is a μ-opioid receptor (MOR) agonist and noradrenaline reuptake inhibitor (NRI)." | ( Tapentadol increases levels of noradrenaline in the rat spinal cord as measured by in vivo microdialysis. De Vry, J; Flik, G; Folgering, JH; Tzschentke, TM, 2012) | 2.54 |
| "Tapentadol is an oral mu-opioid receptor agonist and a noradrenaline reuptake inhibitor developed by Ortho-McNeil Janssen Pharmaceuticals and approved by the Food and Drug Administration in November 2008 for the treatment of moderate-to-severe acute pain in adult patients and for chronic pain in August 2011 in an extended release form." | ( Pharmacology update: tapentadol for neuropathic pain. Pierce, DM; Shipstone, E, 2012) | 1.42 |
| "Tapentadol is a mu-opioid receptor agonist and norepinephrine reuptake inhibitor. " | ( A randomised, placebo-controlled trial comparing the effects of tapentadol and oxycodone on gastrointestinal and colonic transit in healthy humans. Boldingh, A; Burton, D; Busciglio, I; Camilleri, M; Iturrino, J; Jeong, ID; Rhoten, D; Ryks, M; Shin, A; Zinsmeister, AR, 2012) | 2.06 |
| "Tapentadol is a new centrally acting analgesic with a dual mode of action as an agonist of the µ-opioid receptor and as a norepinephrine reuptake inhibitor. " | ( [Undesired side effects of tapentadol in comparison to oxycodone. A meta-analysis of randomized controlled comparative studies]. Dinges, G; Koch, T; Kranke, P; Merker, M; Morin, AM, 2012) | 2.12 |
| "Tapentadol is a novel, centrally acting analgesic with two mechanisms of action--μ-opioid receptor agonism and norepinephrine reuptake inhibition--in a single molecule." | ( Clinical efficacy and safety of tapentadol immediate release in the postoperative setting. Daniels, SE; Golf, M, ) | 1.14 |
| "Tapentadol (Nucynta®) is a synthetic mu-opioid receptor agonist that also has norepinephrine reuptake inhibitor action." | ( Postmortem distribution of tapentadol and N-desmethyltapentadol. Bayard, C; Larson, SJ; Pestaner, J; Pierre-Louis, M; Prashar, SK; Zarwell, LW, 2012) | 1.4 |
| "Tapentadol (TAP) is a novel opioid pain reliever drug that is unusual in its possession of dual mechanism of action (mu opioid-receptor agonist and noradrenaline reuptake inhibitor), this feature makes the active ingredient an attractive potential progenitor of a new pharmacological class. " | ( Quantification of tapentadol in canine plasma by HPLC with spectrofluorimetric detection: development and validation of a new methodology. Giorgi, M; Meizler, A; Mills, PC, ) | 1.91 |
| "Tapentadol (TAP) is a novel opioid pain reliever drug with a dual mechanism of action (mu opioid receptor agonist and noradrenaline reuptake inhibitor). " | ( Pharmacokinetics of the novel atypical opioid tapentadol following oral and intravenous administration in dogs. Giorgi, M; Meizler, A; Mills, PC, 2012) | 2.08 |
| "Tapentadol is a novel, centrally acting oral analgesic with a dual mode of action that has demonstrated efficacy in preclinical and clinical models of pain relief. " | ( Absorption, metabolism, and excretion of 14C-labeled tapentadol HCl in healthy male subjects. Fliegert, F; Göhler, K; Lange, C; Ossig, J; Terlinden, R, ) | 1.82 |
Tapentadol has a double mechanism of action, as a μ-opioid receptor agonism (MOR) and noradrenaline reuptake inhibitor (NRI), contributing synergistically to its analgesic efficacy on both nociceptive and neuropathic pain. The drug has a good safety profile and no evidence of acquired tolerance from the long-term data.
Tapentadol has been studied for use in nociceptive pain but few studies have yet been done to assess its efficacy in the treatment of neuropathic pain. It has been reported to provide an improved adverse-events (AE) profile compared with other potent opioid analgesics at similar levels of analgesia.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Tapentadol has a double mechanism of action, as a μ-opioid receptor agonism (MOR) and noradrenaline reuptake inhibitor (NRI), contributing synergistically to its analgesic efficacy on both nociceptive and neuropathic pain." | ( Tapentadol prolonged release in association with analgesic radiofrequency for the treatment of chronic lumbar radicular pain: an observational, prospective study. Del Gaudio, A; Mastroluca, A; Varano, L; Visconti, C, 2019) | 2.68 |
| "Tapentadol PR has a good safety profile and no evidence of acquired tolerance from the long-term data so far collected." | ( Tapentadol Prolonged Release for Chronic Pain: A Review of Clinical Trials and 5 Years of Routine Clinical Practice Data. Baron, R; Eberhart, L; Kern, KU; Regner, S; Rolke, R; Simanski, C; Tölle, T, 2017) | 2.62 |
| "Tapentadol has been shown to be at least as effective as morphine and oxycodone in five randomized (two of which were multicenter and double-blind) and a range of nonrandomized trials, although caution is needed when interpreting these results. " | ( Tapentadol for the management of cancer pain in adults: an update. Boland, JW, 2023) | 3.8 |
| "Tapentadol has been shown in a range of studies to be an effective analgesic and thus should be considered as an alternative to morphine and oxycodone, especially when opioid toxicities are an issue." | ( Tapentadol for the management of cancer pain in adults: an update. Boland, JW, 2023) | 3.8 |
| "Tapentadol has been studied for use in nociceptive pain but few studies have yet been done to assess its efficacy in the treatment of neuropathic pain." | ( Pharmacology update: tapentadol for neuropathic pain. Pierce, DM; Shipstone, E, 2012) | 1.42 |
| "Tapentadol has been reported to provide an improved adverse-events (AE) profile compared with other potent opioid analgesics at similar levels of analgesia." | ( Cost-effectiveness of tapentadol in severe chronic pain in Spain: a cost analysis of data from RCTs. Antoñanzas, F; Gálvez, R; Hertel, N; Ikenberg, R; Liedgens, H; Obradovic, M, 2012) | 1.41 |
| "Tapentadol ER treatment has been associated with better gastrointestinal tolerability and compliance with therapy than oxycodone CR, which suggests that tapentadol ER may be a better option for the long-term management of chronic pain." | ( Efficacy of tapentadol ER for managing moderate to severe chronic pain. Afilalo, M; Morlion, B, 2013) | 1.49 |
Tapentadol ER had lower rates of past 30-day abuse than ADF ER and non-ADF ER opioid comparators, both at a population level and when adjusted for drug utilization. Tapentadols may have a lower abuse risk than other opioids because it has a relatively low affinity for the mu-opioid receptor.
Tapentadol (and placebo) treatment resulted in more bowel movements and softer stool consistency as compared with oxycodone. The opioid sparing effects result in less water absorption from the gut lumen. Tapentadl ER treatment was associated with significant reductions in pain intensity from baseline to week 15.
The identification and characteristics of these cases indicate that the adverse event profile of tapentadol needs to be considered in the setting of polypharmacy. The study also looked at the relationship between the risk of opioid-related gastrointestinal adverse effects (AEs) and exposure to tapentads.
The aim of this analysis was to develop a population pharmacokinetic model for tapentadol IR in healthy subjects and patients following single and multiple dosing. The objective was to identify covariates that might explain variability in exposure following oral administration.
Absolute bioavailability for both tapentadol IR and tapENTadol PR was ~ 32% under fasted conditions. Study 1 and 2 determined the absolute bioavailability and pharmacokinetics of oral tapentdol IR 86 mg and tapentads PR 86 mg.
tapentadol prolonged release (PR) is commercially available in Germany as Palexia retard; Grünenthal GmbH, Aachen. The dosage form is administered in doses of 50 to 100 mg every four to six hours (dose and dosing interval being selected on the basis of pain intensity)
| Excerpt | Relevance | Reference |
|---|---|---|
| " This phase III, randomized, double-blind, active-controlled study evaluated the tolerability of tapentadol immediate release (IR) and oxycodone IR for low back pain or osteoarthritis pain (hip or knee), using flexible dosing over 90 days." | ( Tolerability of tapentadol immediate release in patients with lower back pain or osteoarthritis of the hip or knee over 90 days: a randomized, double-blind study. Hale, M; Lange, C; Okamoto, A; Rauschkolb, C; Upmalis, D, 2009) | 0.92 |
| "No clinically relevant changes were noted in the serum concentrations of tapentadol, and accordingly, no dosage adjustments with respect to the investigated pharmacokinetic mechanism of interaction are warranted for the administration of tapentadol given concomitantly with acetaminophen, naproxen, or acetylsalicylic acid." | ( Effects of acetaminophen, naproxen, and acetylsalicylic acid on tapentadol pharmacokinetics: results of two randomized, open-label, crossover, drug-drug interaction studies. Mangold, B; Oh, C; Ravenstijn, PG; Rengelshausen, J; Smit, JW; Terlinden, R; Upmalis, D; Wang, SS, 2010) | 0.83 |
| " Oral tapentadol HCI is administered in doses of 50 to 100 mg every four to six hours (dose and dosing interval being selected on the basis of pain intensity)." | ( Is tapentadol an advance on tramadol? Guay, DR, 2009) | 1.46 |
| " Dose-response curves of tapentadol (intravenous) were determined in combination with vehicle or a fixed dose (intraperitoneal) of the mu-opioid receptor antagonist naloxone (1mg/kg), the alpha2-adrenoceptor antagonist yohimbine (2." | ( Differential contribution of opioid and noradrenergic mechanisms of tapentadol in rat models of nociceptive and neuropathic pain. Christoph, T; Jahnel, U; Schröder, W; Tzschentke, TM; Vry, JD, 2010) | 0.9 |
| " Dose-response curves were generated in rats for tapentadol alone or in combination with the opioid antagonist naloxone or the α(2)-adrenoceptor antagonist yohimbine." | ( Synergistic interaction between the two mechanisms of action of tapentadol in analgesia. Christoph, T; De Vry, J; Jahnel, U; Schröder, W; Tallarida, RJ; Terlinden, R; Tzschentke, TM, 2011) | 0.86 |
| "Urine specimens from pain management patients dosed with Nucynta (Tapentadol) were confirmed for the presence of tapentadol and N-desmethyltapentadol using ultra-performance liquid chromatography-tandem mass spectrometry to minimize sample preparation and urine volume requirements." | ( Determination of tapentadol (Nucynta®) and N-desmethyltapentadol in authentic urine specimens by ultra-performance liquid chromatography-tandem mass spectrometry. Backer, RC; Bourland, JA; Chester, SA; Collins, AA; Ramachandran, S, 2010) | 0.94 |
| " Sensitivity analyses consider the impact of real-world dosing patterns for LAO on treatment costs." | ( Clinical simulation model of long-acting opioids for treatment of chronic non-cancer pain in the United States. Merchant, S; Mody, SH; Neil, N; Ogden, K; Provenzano, D, 2013) | 0.39 |
| " In sensitivity analyses, tapentadol ER becomes a dominant strategy when real-world dosing patterns are considered." | ( Clinical simulation model of long-acting opioids for treatment of chronic non-cancer pain in the United States. Merchant, S; Mody, SH; Neil, N; Ogden, K; Provenzano, D, 2013) | 0.69 |
| " Overall, the pharmacokinetic characteristics of tapentadol PR enable a twice-daily dosing regimen to be used; such a regimen is expected to improve patient compliance during chronic use." | ( Comparative pharmacokinetics and bioavailability of tapentadol following oral administration of immediate- and prolonged-release formulations. Brett, M; Göhler, K; Rengelshausen, J; Smit, JW; Terlinden, R, 2013) | 0.89 |
| "In a head-to-head study of up to 10 days in duration, the analgesic efficacy and tolerability of tapentadol immediate release (IR) versus oxycodone IR using a flexible dosing regimen were compared in patients with acute low back pain (LBP) and associated radicular leg pain." | ( Tapentadol immediate release versus oxycodone immediate release for treatment of acute low back pain. Benson, C; Biondi, D; Etropolski, M; Moskovitz, B; Rauschkolb, C; Xiang, J, ) | 1.79 |
| "This head-to-head study demonstrated that tapentadol IR had comparable analgesic efficacy and overall safety to that of oxycodone IR for the relief of moderate to severe, acute LBP and associated radicular leg pain when using flexible dosing regimens that reflect typical use in clinical practice; however, tapentadol IR demonstrated a better gastrointestinal tolerability profile, particularly for the common opioid-related TEAEs of vomiting and constipation." | ( Tapentadol immediate release versus oxycodone immediate release for treatment of acute low back pain. Benson, C; Biondi, D; Etropolski, M; Moskovitz, B; Rauschkolb, C; Xiang, J, ) | 1.84 |
| "This noninterventional, prospective study investigated the administration of tapentadol prolonged release (PR; the dosage form described in this article is commercially available in Germany as Palexia retard; Grünenthal GmbH, Aachen) for severe chronic pain in routine clinical practice over a 3-month period." | ( Tapentadol prolonged release for severe chronic pain: results of a noninterventional study involving general practitioners and internists. Litzenburger, BC; Schumann, C; Schwenke, K; Schwittay, A, 2013) | 2.06 |
| " Trough tapentadol concentrations increased during repeat dosing until reaching steady-state by the third dose." | ( Pharmacokinetic evaluation of tapentadol extended-release tablets in healthy subjects. Etropolski, MS; Hillewaert, VM; Smit, JW; Stahlberg, HJ; Wenge, B; Zannikos, PN, ) | 0.85 |
| " The study findings may be limited by study drug dosing every 4 to 6 hours and frequent monitoring during treatment, neither of which mimic pain treatment in clinical practice." | ( Acute postoperative pain relief with immediate-release tapentadol: randomized, double-blind, placebo-controlled study conducted in South Korea. Karcher, K; Ko, JS; Lee, EJ; Lee, HS; Lee, YK; Li, H; Rhim, HY; Shapiro, D, 2014) | 0.65 |
| "001; n = 373), using a final average daily dosage of 252." | ( [Tapentadol prolonged release improves analgesia, functional impairment and quality of life in patients with chronic pain who have previously received oxycodone/naloxone]. Kern, KU; Krings, D; Waldmann-Rex, S, 2014) | 1.31 |
| "8 points (NRS-11, 11-point pain scale, n = 96) at the end of observation, using an average dosage of 218." | ( [Conversion to tapentadol PR improves analgesia and quality of life in patients with severe and chronic pain despite using tramadol > 300 mg/d]. Lehmann, U; Richter, U; Waldmann-Rex, S, 2015) | 0.77 |
| " A limitation of this study may possibly include more controlled patient monitoring through 4-6 hour dosing intervals, which reflects optimal conditions and thus may not approximate real-world clinical practice." | ( Tapentadol immediate-release for acute postbunionectomy pain: a phase 3, randomized, double-blind, placebo-controlled, parallel-group study in Taiwan. Chen, YJ; Chiang, CC; Huang, J; Huang, PJ; Karcher, K; Li, H, 2015) | 1.86 |
| "Tapentadol PR was administered at the moment of pain onset in opioid-naive patients at the dosage of 50 mg BID." | ( Effectiveness of tapentadol prolonged release for the management of painful mucositis in head and neck cancers during intensity modulated radiation therapy. Alba, F; Filippo, A; Francesco, R; Maurizio, N; Niccolò, GL; Rosario, M; Sergio, A; Sergio, F; Stefania, G, 2016) | 2.22 |
| " The degree of disability and TP dosage assumption were evaluated at baseline and after 6 months." | ( The beneficial use of ultramicronized palmitoylethanolamide as add-on therapy to Tapentadol in the treatment of low back pain: a pilot study comparing prospective and retrospective observational arms. Aurilio, C; Barbarisi, M; Fierro, D; Fiore, M; Pace, MC; Passavanti, MB; Pota, V; Sansone, P, 2017) | 0.68 |
| "Statistical analysis performed with generalized linear mixed model on 55 patients (30 in the prospective group and 25 in the retrospective group) demonstrated that um-PEA as add-on treatment to TP in patients with chronic LBP, in comparison to TP alone, led to a significantly higher reduction in pain intensity, in the neuropathic component, the degree of disability and TP dosage assumption." | ( The beneficial use of ultramicronized palmitoylethanolamide as add-on therapy to Tapentadol in the treatment of low back pain: a pilot study comparing prospective and retrospective observational arms. Aurilio, C; Barbarisi, M; Fierro, D; Fiore, M; Pace, MC; Passavanti, MB; Pota, V; Sansone, P, 2017) | 0.68 |
| " Dose-response curves were generated for tapentadol, diclofenac, and their combination in the acetic acid-induced writhing test in mice." | ( Assessment of the antinociceptive and ulcerogenic activity of the tapentadol-diclofenac combination in rodents. Alonso-Castro, ÁJ; Granados-Soto, V; Isiordia-Espinoza, MA; Sánchez-Enriquez, S; Zapata-Morales, JR, 2018) | 0.98 |
| " Four weeks after inducing diabetes, tapentadol dose-response curves were obtained from animals pre-treated with RX821002 or naloxone (alpha2-adrenoceptors and opioid receptors antagonists, respectively)." | ( Opioid and noradrenergic contributions of tapentadol to the inhibition of locus coeruleus neurons in the streptozotocin rat model of polyneuropathic pain. Berrocoso, E; Borges, GDS; Mico, JA; Torres-Sanchez, S, 2018) | 1.02 |
| "However, depending on the dosage form and presence of swallowing disorders, the administration should be considered carefully." | ( [Retrospective Examination of Usefulness and Adverse Effects of Tapentadol in Patients with Cancer Pain during Anticancer Treatment]. Asonuma, S; Emi, Y; Fujii, M; Kajiwara, M; Kometani, T; Miyazaki, S; Mori, M; Noda, Y; Ochiai, T; Shikada, Y, 2019) | 0.75 |
| " Further studies are needed to assess dosing regimens which may lead to effective treatment of acute pain and long-term use." | ( Effectiveness of tapentadol hydrochloride for treatment of orthopedic pain in dogs: A pilot study. Aarnes, TK; Howard, J; Kieves, NR; Lakritz, J; Lerche, P, 2020) | 0.9 |
| " Dose-response curves were carried out for dexketoprofen, tapentadol, and dexketoprofen-tapentadol combinations in the acetic acid-induced writhing test in mice." | ( Antinociception and less gastric injury with the dexketoprofen-tapentadol combination in mice. Alonso-Castro, ÁJ; Franco de la-Torre, L; Granados-Soto, V; Isiordia-Espinoza, MA; Partida-Castellanos, EM; Rivas-Carrillo, JD; Vidaurrazaga-Lugo, J; Zapata-Morales, JR, 2021) | 1.11 |
| "Eligible patients started the extension trial on the tapentadol PR dosage optimized for them in the preceding trial; dose adjustments were permitted throughout the extension." | ( Long-Term Effectiveness and Tolerability of Pain Treatment with Tapentadol Prolonged Release. Bernal, DS; Escobar, AE; Ferri, CM; Mateos, RG; Morera, LMT, 2021) | 1.11 |
| "Proportions of BZD coprescribing, BZD dosing patterns in matched patients, and the esti-mated number of lives potentially saved by the opioid treatment switch." | ( Concomitant use of benzodiazepines in chronic pain patients adherent to extended-release tapentadol or oxycodone treatment-A retrospective claims analysis. DeGeorge, M; Imro, M; Passik, SD; Tatovic, S; Vukicevic, D; Zah, V, ) | 0.35 |
| " The mechanism of action of tapentadol involving norepinephrine reuptake inhibition affecting the central nervous system, higher dosage and drug interactions with other home medications likely contributed to her sleepwalking." | ( Tapentadol and Sleepwalking: A Case Report. Ko, EYJ; Tupper, MW, 2022) | 2.46 |
| "This case highlights the importance of adhering to the recommended dosage of a medication and if it is clinically warranted to exceed the maximum recommended dose, the importance of diligent monitoring for any adverse effects." | ( Tapentadol and Sleepwalking: A Case Report. Ko, EYJ; Tupper, MW, 2022) | 2.16 |
| "During dosing with tapentadol, gastrointestinal side effects and motility parameters were on placebo level." | ( Tapentadol results in less deterioration of gastrointestinal function and symptoms than standard opioid therapy in healthy male volunteers. Drewes, AM; Frøkjaer, JB; Hansen, TM; Krogh, K; Mark, EB; Nedergaard, RB; Nissen, TD; Scott, SM, 2021) | 2.39 |
| " The flow chart can be easily tailored to individual patient characteristics, duration of tapentadol treatment, response to progressive dosage reduction, and likelihood of withdrawal symptom occurrence." | ( Appropriate use of tapentadol: focus on the optimal tapering strategy. Fornasari, D; Vellucci, R, 2023) | 1.46 |
| " The effect of treatment was assessed using a Pain Numeric Rating Scale (NRS) and determined by changes in medication dosage and quality of life at day 7 and 3 months." | ( Cryoneurolysis of alveolar nerves for chronic dental pain: A new technique and a case series. Broome, M; Cachemaille, M; Geering, S, 2023) | 0.91 |
| Class | Description |
|---|---|
| alkylbenzene | A monocyclic arene that is benzene substituted with one or more alkyl groups. |
| [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 | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Solute carrier family 22 member 1 | Homo sapiens (human) | IC50 (µMol) | 21.8900 | 0.2100 | 5.5537 | 10.0000 | AID1526751 |
| Proteinase-activated receptor 1 | Homo sapiens (human) | Ki | 0.1600 | 0.0011 | 0.0287 | 0.1600 | AID669684 |
| Mu-type opioid receptor | Homo sapiens (human) | Ki | 0.1600 | 0.0000 | 0.4197 | 10.0000 | AID669684 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Proteinase-activated receptor 1 | Homo sapiens (human) | EC50 (µMol) | 0.6700 | 0.0037 | 0.5234 | 1.3000 | AID669685 |
| Mu-type opioid receptor | Homo sapiens (human) | EC50 (µMol) | 0.6700 | 0.0000 | 0.3263 | 9.4000 | AID669685 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1346971 | Human NET (Monoamine transporter subfamily) | 2007 | The Journal of pharmacology and experimental therapeutics, Oct, Volume: 323, Issue:1 | (-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol hydrochloride (tapentadol HCl): a novel mu-opioid receptor agonist/norepinephrine reuptake inhibitor with broad-spectrum analgesic properties. |
| AID1346364 | Human mu receptor (Opioid receptors) | 2007 | The Journal of pharmacology and experimental therapeutics, Oct, Volume: 323, Issue:1 | (-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol hydrochloride (tapentadol HCl): a novel mu-opioid receptor agonist/norepinephrine reuptake inhibitor with broad-spectrum analgesic properties. |
| AID1526732 | Substrate activity at human OCT1 expressed in HEK293 cells assessed as increase in compound uptake at 0.1 uM incubated for 2 mins by LC-MS/MS analysis relative to control empty vector transfected cells | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21 | Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1. |
| AID1526758 | Ratio of unbound maximal portal vein concentration in human at 80 mg, po dosed as immediate release formulation to inhibition of human OCT1 expressed in HEK293 cells assessed as reduction in ASP+ substrate uptake by microplate reader based analysis | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21 | Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1. |
| AID1526761 | Ratio of unbound maximal portal vein concentration in human at 34 mg, iv to inhibition of human OCT1 expressed in HEK293 cells assessed as reduction in ASP+ substrate uptake by microplate reader based analysis | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21 | Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1. |
| AID1526752 | Passive membrane permeability by LC-MS/MS analysis based PAMPA | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21 | Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1. |
| AID1526733 | Substrate activity at human OCT1 expressed in HEK293 cells assessed as increase in compound uptake at 0.5 uM incubated for 2 mins by LC-MS/MS analysis relative to control empty vector transfected cells | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21 | Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1. |
| AID1526755 | Unbound Cmax in human at 80 mg, po dosed as immediate release formulation | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21 | Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1. |
| 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. |
| AID1526751 | Inhibition of human OCT1 expressed in HEK293 cells assessed as reduction in ASP+ substrate uptake by microplate reader based analysis | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21 | Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1. |
| AID1526731 | Substrate activity at human OCT1 expressed in HEK293 cells assessed as increase in compound uptake at 0.05 uM incubated for 2 mins by LC-MS/MS analysis relative to control empty vector transfected cells | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21 | Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1. |
| AID1526754 | Cmax in human at 80 mg, po dosed as immediate release formulation | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21 | Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1. |
| AID1526756 | Unbound maximal portal vein concentration of in human at 80 mg, po dosed as immediate release formulation | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21 | Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1. |
| AID1526757 | Ratio of unbound Cmax in human at 80 mg, po dosed as immediate release formulation to inhibition of human OCT1 expressed in HEK293 cells assessed as reduction in ASP+ substrate uptake by microplate reader based analysis | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21 | Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1. |
| AID1526763 | Ratio of unbound Cmax in human at 34 mg, iv to inhibition of human OCT1 expressed in HEK293 cells assessed as reduction in ASP+ substrate uptake by microplate reader based analysis | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21 | Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1. |
| AID1526770 | Cmax in human at 86 mg, po dosed as prolonged release formulation | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21 | Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1. |
| AID669685 | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assay | 2012 | ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3 | NOpiates: Novel Dual Action Neuronal Nitric Oxide Synthase Inhibitors with μ-Opioid Agonist Activity. |
| AID669684 | Displacement of [3H]DAMGO from human mu opioid receptor expressed in HEK-293 cells by scintillation counting | 2012 | ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3 | NOpiates: Novel Dual Action Neuronal Nitric Oxide Synthase Inhibitors with μ-Opioid Agonist Activity. |
| AID1526769 | Unbound maximal portal vein concentration of in human at 86 mg, po dosed as prolonged release formulation | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21 | Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1. |
| AID1526768 | Unbound Cmax in human at 86 mg, po dosed as prolonged release formulation | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21 | Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1. |
| AID1526767 | Ratio of unbound Cmax in human at 86 mg, po dosed as prolonged release formulation to inhibition of human OCT1 expressed in HEK293 cells assessed as reduction in ASP+ substrate uptake by microplate reader based analysis | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21 | Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1. |
| AID1526762 | Unbound maximal portal vein concentration of in human at 34 mg, iv | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21 | Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1. |
| AID1526765 | Unbound Cmax in human at 34 mg, iv | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21 | Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1. |
| AID1526764 | Cmax in human at 34 mg, iv | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21 | Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1. |
| 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. |
| AID1526766 | Ratio of unbound maximal portal vein concentration in human at 86 mg, po dosed as prolonged release formulation to inhibition of human OCT1 expressed in HEK293 cells assessed as reduction in ASP+ substrate uptake by microplate reader based analysis | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21 | Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1. |
| [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 | 15 (4.09) | 29.6817 |
| 2010's | 273 (74.39) | 24.3611 |
| 2020's | 79 (21.53) | 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 (106.58) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 87 (21.48%) | 5.53% |
| Reviews | 79 (19.51%) | 6.00% |
| Case Studies | 26 (6.42%) | 4.05% |
| Observational | 19 (4.69%) | 0.25% |
| Other | 194 (47.90%) | 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 | ||
|---|---|---|---|---|---|---|---|
| Open-Label Evaluation of the Pharmacokinetic Profile and Safety of Tapentadol Oral Solution for the Treatment of Postsurgical Pain in Children and Adolescents Aged From 6 to Less Than 18 Years [NCT01134536] | Phase 2 | 45 participants (Actual) | Interventional | 2011-10-31 | Completed | ||
| Investigation of the Effect on the QT/QTc Interval After Multiple Dose Oral Administration (100 and 200 mg Bid) of CG5503 PR in a Randomised, Double-blind, Double-dummy Placebo- and Moxifloxacin-controlled 4- Way Cross-over Phase I Study in 48 Healthy Mal [NCT03951402] | Phase 1 | 48 participants (Actual) | Interventional | 2003-03-31 | Completed | ||
| Safety and Efficacy of Pre-emptive Tapentadol vs Pregabalin in Post Operative Pain Following Unilateral Total Knee Arthroplasty- A Randomised, Double Blind, Active Control, Clinical Trial [NCT03604354] | Phase 4 | 95 participants (Actual) | Interventional | 2018-08-01 | Completed | ||
| A One-Year, Randomized, Open-Label, Parallel-Group, Multiple-Dose Long-Term Safety Study With Controlled Adjustment of Dose of Tapentadol Extended-Release (ER) and Oxycodone Controlled-Release (CR) in Subjects With Chronic, Painful Diabetic Peripheral Neu [NCT01063868] | Phase 3 | 47 participants (Actual) | Interventional | 2010-01-31 | Terminated(stopped due to Business decision) | ||
| A Single-Dose, Open-Label, Randomized, Four-Way Crossover Study to Assess the Dose-Proportionality of the Pharmacokinetics of Tapentadol, Given as Tamper-Resistant Tablets, in Healthy Japanese and Korean Male Subjects [NCT01309425] | Phase 1 | 52 participants (Actual) | Interventional | 2011-02-28 | Completed | ||
| A Comparison of Analgesic and Respiratory Effects From Tapentadol Versus Oxycodone After Laparoscopic Hysterectomy. [NCT03314792] | Phase 4 | 86 participants (Actual) | Interventional | 2017-12-04 | Completed | ||
| An Evaluation of the Efficacy and Safety of Tapentadol Oral Solution in the Treatment of Post-operative Acute Pain Requiring Opioid Treatment in Pediatric Subjects Aged From Birth to Less Than 18 Years Old [NCT02081391] | Phase 3 | 216 participants (Actual) | Interventional | 2015-02-19 | Completed | ||
| A Randomized, Double-Blind, Active-Control, Parallel-Group, 90-Day Safety Study of CG5503 Immediate Release (IR) or Oxycodone IR in Subjects With Chronic Pain From Low Back Pain or Osteoarthritis of the Hip or Knee [NCT00364546] | Phase 3 | 877 participants (Actual) | Interventional | 2006-07-31 | Completed | ||
| A Randomized, Double-Blind, Active- and Placebo-Controlled, Parallel Group, Multicenter Study to Evaluate the Efficacy and Safety of Multiple Doses of CG5503 Immediate Release Formulation in Subjects Awaiting Primary Joint Replacement Surgery for End-Stag [NCT00361582] | Phase 3 | 669 participants (Actual) | Interventional | 2006-10-31 | Completed | ||
| A Randomized, Open-Label, Parallel-Arm, Optimal Dose-Titration, Multicenter Study to Evaluate the Safety and Efficacy of Oral JNS024 Extended-Release (ER) in Japanese Subjects Treated With Around-the-Clock Opioid Analgesics for Their Moderate to Severe Ch [NCT01309386] | Phase 3 | 100 participants (Actual) | Interventional | 2010-08-31 | Completed | ||
| Open-label, Single-arm, Flexible Dosing, Phase III Trial, With Oral Tapentadol Prolonged Release (PR) in Subjects With Chronic Malignant Tumor-related Pain Who Have Completed the Maintenance Period of the KF5503/15 Trial. [NCT01264887] | Phase 3 | 31 participants (Actual) | Interventional | 2011-03-31 | Terminated(stopped due to Administrative reasons) | ||
| 4-Week Randomized Multicenter DB, Placebo- and Active-controlled, Parallel-group, Forced-titration Phase 2B Study of Efficacy and Safety With CG5503 Prolonged Release (PR) to 233 mg BID and Oxycodone PR to 20 mg BID vs Placebo in Subjects With Moderate to [NCT00745069] | Phase 2 | 670 participants (Actual) | Interventional | 2004-07-31 | Completed | ||
| Depot-opioids for Pre- and Postoperative Pain Relief After Primary Knee Arthroplasty. A Double Blinded Randomized Controlled Study. Tapentadol vs Oxycodone vs Placebo [NCT02604446] | Phase 3 | 134 participants (Actual) | Interventional | 2015-09-30 | Completed | ||
| A Randomized Double-Blind, Placebo- and Active-Control, Parallel-arm, Phase III Trial With Controlled Adjustment of Dose to Evaluate the Efficacy and Safety of CG5503 Extended-Release (ER) in Subjects With Moderate to Severe Chronic Low Back Pain [NCT00449176] | Phase 3 | 981 participants (Actual) | Interventional | 2007-02-28 | Completed | ||
| A One-Year, Randomized, Open-Label, Parallel-Arm, Phase 3 Long-Term Safety Trial, With Controlled Adjustment of Dose, of Multiple Doses of CG5503 PR and Oxycodone CR in Subjects With Chronic Pain [NCT00361504] | Phase 3 | 1,123 participants (Actual) | Interventional | 2006-11-30 | Completed | ||
| A Randomized, Double-Blind, 2-Period, Crossover Study to Establish the Dose Equivalence and Direct Conversion Between Immediate Release (IR) and Extended-Release (ER) CG5503 in Subjects With Moderate-to-Severe, Chronic Low Back Pain [NCT00594516] | Phase 3 | 117 participants (Actual) | Interventional | 2007-12-31 | Completed | ||
| A Randomized, Double-Blind, Active- and Placebo-Controlled, Parallel Group, Multicenter Study to Evaluate the Efficacy and Safety of Multiple Doses of CG5503 Immediate Release Formulation in the Treatment of Acute Pain From Total Hip Replacement Surgery F [NCT00364533] | Phase 3 | 367 participants (Actual) | Interventional | 2006-10-31 | Terminated(stopped due to Slow enrollment) | ||
| A Randomized-Withdrawal Phase 3 Study Evaluating the Safety and Efficacy of CG5503 Extended Release (ER) in Subjects With Painful Diabetic Peripheral Neuropathy [NCT00455520] | Phase 3 | 395 participants (Actual) | Interventional | 2007-04-30 | Completed | ||
| Open-Label Extension, Single-Arm, Flexible-Dosing, Phase 3 Trial With CG5503 Extended-Release (ER) in Patients With Moderate to Severe Chronic Pain [NCT00487435] | Phase 3 | 1,166 participants (Actual) | Interventional | 2007-06-30 | Completed | ||
| A Randomized Double-blind, Placebo- and Active-control, Parallel-arm, Phase III Trial With Controlled Adjustment of Dose to Evaluate the Efficacy and Safety of CG5503 Prolonged Release (PR) in Subjects With Moderate to Severe Chronic Pain Due to Osteoarth [NCT00486811] | Phase 3 | 990 participants (Actual) | Interventional | 2007-06-30 | Completed | ||
| Phase II Study of JNS024PR in Cancer Pain Patients [NCT00805142] | Phase 2 | 78 participants (Actual) | Interventional | 2008-11-30 | Completed | ||
| A Randomized, Double-Blind, Placebo- and Oxycodone Immediate Release (IR)-Controlled Study of Tapentadol IR for the Treatment of Acute Pain Caused by Vertebral Compression Fractures Associated With Osteoporosis [NCT00771758] | Phase 3 | 108 participants (Actual) | Interventional | 2008-09-30 | Completed | ||
| A Randomized, Double-Blind, Multi-Center, Parallel-Group Study of Tapentadol Immediate Release (IR) Versus Oxycodone IR for the Treatment of Subjects With Acute Post-Operative Pain Following Elective Arthroscopic Shoulder Surgery [NCT00814580] | Phase 3 | 382 participants (Actual) | Interventional | 2008-12-31 | Completed | ||
| A Randomized, Double-Blind, Placebo- and Active-Controlled, Parallel-Arm, Multicenter Study in Subjects With End-Stage Joint Disease to Compare the Frequency of Constipation Symptoms in SubjectsTreated With Tapentadol IR and Oxycodone IR Using a Bowel Fun [NCT00784277] | Phase 3 | 597 participants (Actual) | Interventional | 2008-10-31 | Completed | ||
| A Randomized, Double-Blind, Parallel-Arm, Placebo and Active Controlled Dose-Ranging Study of the Efficacy and Safety of Multiple Doses of CG5503 (Tapentadol) IR for Postoperative Pain Following Bunionectomy Surgery [NCT00806247] | Phase 2 | 480 participants (Actual) | Interventional | 2005-01-31 | Completed | ||
| A Randomized, Double-Blind, Active- and Placebo-Controlled, Parallel-Group, Multicenter Study to Evaluate the Efficacy and Safety of Tapentadol Immediate-Release Formulation in the Treatment of Acute Pain From Bunionectomy [NCT00613938] | Phase 3 | 901 participants (Actual) | Interventional | 2008-02-29 | Completed | ||
| An Open-Label, Two-Way Crossover, Drug-Interaction Study to Determine the Effect of Omeprazole on the Pharmacokinetics of an Immediate-Release Capsule of CG5503 in Healthy Subjects [NCT03979989] | Phase 1 | 32 participants (Actual) | Interventional | 2005-09-28 | Completed | ||
| A Randomized Double-Blind, Placebo- and Active-Control, Parallel-arm, Phase III Trial With Controlled Adjustment of Dose to Evaluate the Efficacy and Safety of CG5503 Extended-Release (ER) in Patients With Moderate to Severe Chronic Pain Due to Osteoarthr [NCT00421928] | Phase 3 | 1,030 participants (Actual) | Interventional | 2007-01-31 | Completed | ||
| Investigation of the Pharmacokinetic Characteristics of Two New CG5503 Formulations as Compared to CG5503 PR Tablets and Exploration of the Effect of Food on the Bioavailability of the Two New CG5503 Formulations Following Single Oral Administration of 11 [NCT03956134] | Phase 1 | 10 participants (Actual) | Interventional | 2005-04-30 | Completed | ||
| An Open-Label, Sequential Treatment Study to Assess the Single and Multiple Dose Pharmacokinetics of a New Tapentadol Prolonged-Release 250 mg Formulation in Healthy Subjects [NCT01877226] | Phase 1 | 18 participants (Actual) | Interventional | 2008-09-30 | Completed | ||
| A Single-Dose, Open-Label, Randomized, 2-Way Crossover Pivotal Study to Assess Bio-equivalence of a New Tapentadol Extended-Release (TRF) 50-mg Tablet With Respect to a Tapentadol Extended-Release (PR2) 50-mg Tablet Under Fasted Conditions in Healthy Subj [NCT01900587] | Phase 1 | 64 participants (Actual) | Interventional | 2010-07-31 | Completed | ||
| A Post-Marketing Surveillance (PMS) Study on the Safety and Effectiveness of Prolonged Release Tapentadol Hydrochloride Among Adult Filipino Patients With Moderate To Severe Chronic Non-Cancer Pain [NCT01719588] | 0 participants (Actual) | Observational | 2014-10-31 | Withdrawn(stopped due to The company decided to cancel this study in conformity with PH FDA Circular 2013-004) | |||
| A Randomized Withdrawal, Active- and Placebo-controlled, Double-blind, Multi-center Phase III Trial Assessing Safety and Efficacy of Oral CG5503 (Tapentadol) PR* in Subjects With Moderate to Severe Chronic Malignant Tumor-related Pain [NCT00472303] | Phase 3 | 622 participants (Actual) | Interventional | 2007-07-31 | Completed | ||
| Prospective Longitudinal Observational Study to Evaluate the Clinical Characteristics and Opioids Treatments in Patients With Breakthrough Cancer Pain [NCT01946555] | 150 participants (Actual) | Observational | 2013-09-30 | Completed | |||
| A Single-Dose, Open-Label, Randomized, 2-Way Crossover Pivotal Study to Assess Bioequivalence of a New Tapentadol Extended-Release (TRF) 250-mg Tablet With Respect to a Tapentadol Extended-Release (PR2) 250-mg Tablet Under Fasted Conditions in Healthy Sub [NCT01981278] | Phase 1 | 63 participants (Actual) | Interventional | 2010-07-31 | Completed | ||
| A Single-Dose, Open-Label, Randomized, 2-Way Crossover Pivotal Study to Assess Bioequivalence of a New Tapentadol Extended-Release (TRF) 100-mg Tablet With Respect to a Tapentadol Extended-Release (PR2) 100-mg Tablet Under Fasted Conditions in Healthy Sub [NCT02019485] | Phase 1 | 64 participants (Actual) | Interventional | 2010-07-31 | Completed | ||
| A Randomized, Double-blind, Parallel-arm, Placebo- and Comparator- Controlled Trial of the Efficacy and Safety of Multiple Doses of Immediate-release (IR) CG5503 for Postoperative Pain Following Abdominal Hysterectomy [NCT00478023] | Phase 3 | 854 participants (Actual) | Interventional | 2007-05-31 | Completed | ||
| Phase II Study of JNS024ER in Japanese Subjects With Chronic Pain Due to Diabetic Neuropathic Pain or Postherpetic Neuralgia [NCT01124617] | Phase 2 | 91 participants (Actual) | Interventional | 2010-06-30 | Completed | ||
| An Evaluation of the Effectiveness and Tolerability of Tapentadol Hydrochloride Prolonged Release, and Tapentadol Hydrochloride Immediate Release on Demand, in Subjects With Uncontrolled Severe Chronic Nociceptive, Mixed or Neuropathic Low Back Pain Takin [NCT00983385] | Phase 3 | 208 participants (Actual) | Interventional | 2009-09-30 | Completed | ||
| "A Randomized Withdrawal, Active- and Placebo-controlled, Double-blind, Multi-center Phase III Trial Assessing Safety and Efficacy of Oral CG5503 (Tapentadol) Prolonged Release (PR*) in Subjects With Moderate to Severe Chronic Malignant Tumor-related Pain [NCT00505414] | Phase 3 | 136 participants (Actual) | Interventional | 2007-06-30 | Terminated(stopped due to Recall of rescue medication, alternative rescue medication availability issues.) | ||
| Phase II Study of JNS024ER in Japanese Subjects With Chronic Pain Due to Osteoarthritis of the Knee or Low Back Pain [NCT01124604] | Phase 2 | 91 participants (Actual) | Interventional | 2010-04-30 | Completed | ||
| An Evaluation of the Effectiveness and Tolerability of Tapentadol Hydrochloride Prolonged Release, and Tapentadol Hydrochloride Immediate Release on Demand, in Subjects With Uncontrolled Severe Chronic Pain Due to Osteoarthritis of the Knee Taking Either [NCT00983073] | Phase 3 | 224 participants (Actual) | Interventional | 2009-09-30 | Completed | ||
| Efficacy, Safety, and Tolerability of GRT6005 in Subjects With Moderate to Severe Chronic Low Back Pain. [NCT01725087] | Phase 2 | 1,089 participants (Actual) | Interventional | 2012-11-30 | Completed | ||
| A Single-Dose, Open-Label, Randomized, Two-Way Crossover Study to Assess the Bioequivalence of Tapentadol Given as Two 25-mg Extended-Release Tamper-Resistant Formulation (TRF) Tablets Relative to One 50-mg Extended-Release TRF Tablet in Healthy Japanese [NCT01273506] | Phase 1 | 30 participants (Actual) | Interventional | 2010-12-31 | Completed | ||
| A Comparative Study Between Intranasal Tapentadol Versus Intravenous Paracetamol for Post-operative Analgesia in Lower Limb Orthopedic Surgeries Under Spinal Anaesthesia' [NCT05999890] | Phase 4 | 74 participants (Actual) | Interventional | 2021-07-05 | Completed | ||
| Risk of Shopping Behavior of Tapentadol IR Immediate-Release (IR) Compared to Oxycodone IR Immediate-Release (IR) [NCT01545778] | 646,620 participants (Actual) | Observational | 2010-02-28 | Completed | |||
| A Randomized-Withdrawal, Placebo-Controlled, Study Evaluating the Efficacy, Safety, and Tolerability of Tapentadol Extended-Release (ER) in Subjects With Chronic, Painful Diabetic Peripheral Neuropathy (DPN) [NCT01041859] | Phase 3 | 460 participants (Actual) | Interventional | 2009-12-31 | Completed | ||
| An Evaluation of the Effectiveness and Tolerability of Tapentadol Hydrochloride Prolonged Release, and Tapentadol Hydrochloride Immediate Release on Demand, in Subjects With Severe Chronic Nociceptive, Mixed or Neuropathic Low Back Pain Taking WHO Step II [NCT00986258] | Phase 3 | 136 participants (Actual) | Interventional | 2009-10-30 | Terminated(stopped due to This clinical trial was terminated early, due to slow recruitment and study drug shortages.) | ||
| An Open-label, Multi-center, Single-arm, Phase IV Clinical Trial Assessing Conversion From Hydrocodone, Oxycodone CR or Morphine SR to Tapentadol ER in Subjects With Moderate to Severe Chronic Low Back or OA Pain of the Hip or Knee [NCT01631513] | Phase 4 | 0 participants (Actual) | Interventional | 2012-08-31 | Withdrawn(stopped due to It was a business decision to cancel this study in Aug. 2012.) | ||
| A Post-Marketing Surveillance (PMS) Study on the Safety and Effectiveness of Immediate Release Tapentadol Hydrochloride Among Adult Filipino Patients With Moderate to Severe Acute Non-Cancer Pain [NCT01719601] | 0 participants (Actual) | Observational | 2014-10-31 | Withdrawn(stopped due to The company decided to cancel this study in conformity with PH FDA Circular 2013-004) | |||
| A Randomized, Double-Blind, Active- and Placebo-Controlled, Parallel-Group, Multicenter Study to Evaluate the Efficacy and Safety of Multiple Doses of CG5503 Immediate-Release Formulation in the Treatment of Acute Pain From Bunionectomy Followed by a Volu [NCT00364247] | Phase 3 | 602 participants (Actual) | Interventional | Completed | |||
| Evaluation of the Effectiveness, Safety, and Tolerability of Tapentadol PR Versus Oxycodone/Naloxone PR in Non-opioid Pre-treated Subjects With Uncontrolled Severe Chronic Low Back Pain With a Neuropathic Pain Component. [NCT01838616] | Phase 4 | 367 participants (Actual) | Interventional | 2013-04-30 | Completed | ||
| A Randomized, Double-Blind, Placebo-Controlled, Parallel-Group, Multicenter Study to Evaluate the Efficacy and Safety of Tapentadol Immediate-Release Formulation in the Treatment of Acute Pain From Bunionectomy [NCT01813890] | Phase 3 | 60 participants (Actual) | Interventional | 2013-01-31 | Completed | ||
| A Randomized, Double-blind, Placebo-controlled Parallel Group, Multicenter Trial to Evaluate the Efficacy and Safety of Multiple Dose Administration of an Intravenous Formulation of Tapentadol in the Treatment of Acute Pain Following Bunionectomy. [NCT01435577] | Phase 2 | 177 participants (Actual) | Interventional | 2011-09-30 | Completed | ||
| An Evaluation of the Effectiveness and Tolerability of Tapentadol Hydrochloride Prolonged Release, and Tapentadol Hydrochloride Immediate Release on Demand, in Subjects With Severe Chronic Pain Due to Osteoarthritis of the Knee Taking WHO Step III Analges [NCT00982280] | Phase 3 | 82 participants (Actual) | Interventional | 2009-09-30 | Terminated(stopped due to Slow Recruitment and supply of Investigational Medicinal Product Issues) | ||
| Preemptive Tapentadol on Post-operative Analgesia Following Total Knee Arthroplasty: A Randomized Double Blind Placebo-controlled Trial. [NCT03351517] | 90 participants (Actual) | Interventional | 2017-11-01 | Completed | |||
| Open-label Evaluation of the Population Pharmacokinetic Profile, Safety, Tolerability, and Efficacy of Tapentadol Oral Solution for the Treatment of Post-surgical Pain in Children Aged From Birth to Less Than 2 Years [NCT02221674] | Phase 2 | 40 participants (Actual) | Interventional | 2014-11-05 | Terminated | ||
| Comparison of the Effects of Tapentadol and Oxycodone on Gastrointestinal and Colonic Transit in Humans [NCT01500317] | Phase 4 | 38 participants (Actual) | Interventional | 2011-05-31 | Completed | ||
| An Open-label Trial, Enrolling Subjects Aged 6 Years to Less Than 18 Years Suffering From Pain Requiring Prolonged Release Opioid Treatment, to Evaluate the Safety and Efficacy of Tapentadol PR Versus Morphine PR, Followed by an Open-label Extension [NCT02151682] | Phase 2/Phase 3 | 73 participants (Actual) | Interventional | 2015-04-29 | Completed | ||
| Evaluation of the Antihyperalgesic Effect of Tapentadol in Two Human Experimental Models of: 1) Cold and Mechanical Hyperalgesia Evoked by Topical High-concentration Menthol , 2) Heat and Mechanical Hyperalgesia by Capsaicin. [NCT01615510] | Phase 1 | 24 participants (Actual) | Interventional | 2012-10-31 | Terminated | ||
| A Randomized, Double-Blind, Placebo-Controlled, Parallel-Group, Multicenter Study to Evaluate the Efficacy and Safety of Tapentadol Immediate-Release Formulation in the Treatment of Acute Pain From Bunionectomy; Bridging Study for Korea [NCT01516008] | Phase 3 | 353 participants (Actual) | Interventional | 2012-01-31 | Completed | ||
| A Single-Dose, Open-Label, Randomized, Two-Way Crossover Study to Assess the Bioequivalence of Tapentadol Given as Two 50-mg Extended-Release, Tamper-Resistant Formulation (TRF) Tablets Relative to One 100-mg Extended-Release TRF Tablet in Healthy Japanes [NCT01273532] | Phase 1 | 30 participants (Actual) | Interventional | 2010-12-31 | Completed | ||
| Phase 4 Study of Tapentadol vs Oxycodone in Neuropathic Pain [NCT01458015] | Phase 4 | 5 participants (Actual) | Interventional | 2011-10-31 | Terminated | ||
| Open-label Evaluation of the Pharmacokinetic Profile, Safety, and Efficacy of Tapentadol Oral Solution for the Treatment of Post-surgical Pain in Children and Adolescents Aged From 2 Years to Less Than 18 Years. [NCT01729728] | Phase 2 | 86 participants (Actual) | Interventional | 2012-11-30 | Completed | ||
| Evaluation of the Effectiveness, Safety, and Tolerability of Tapentadol PR Versus a Combination of Tapentadol PR and Pregabalin in Subjects With Severe Chronic Low Back Pain With a Neuropathic Pain Component [NCT01352741] | Phase 4 | 622 participants (Actual) | Interventional | 2011-03-31 | Completed | ||
| Opioid Induced Gait Variability [NCT03121547] | Phase 1/Phase 2 | 24 participants (Actual) | Interventional | 2015-05-19 | Completed | ||
| Management of Postsurgical Pain After Cardiac Operations: Comparison of Tapentadol and Tramadol Analgesia [NCT04718116] | 90 participants (Anticipated) | Interventional | 2022-11-01 | Recruiting | |||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||
"The Participants indicated the average level of pain experienced, at each study visit, over the previous 24 hours on an 11-point Numerical Rating Scale (NRS) where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine. Baseline was the average pain intensity scores measured prior to randomization (At Week 1). At Week 52 again the average pain intensity scores were collected and the change in scores at Week 52 from the baseline scores was considered as the change from baseline in average pain intensity scores at Week 52." (NCT00361504)
Timeframe: Baseline, Week 52
| Intervention | Scores on a Scale (Mean) |
|---|---|
| Tapentadol (CG5503) | -3.22 |
| Oxycodone | -3.14 |
The number of participants who reported a TEAE during the treatment period. TEAE was defined as any adverse event that started or worsened on or after the start of the study medication and up to 3 days after the discontinuation of the study medication. (NCT00361504)
Timeframe: 52 weeks
| Intervention | Participants (Number) |
|---|---|
| Tapentadol (CG5503) | 766 |
| Oxycodone | 202 |
The SPID score incorporates the cumulative analgesic effects of tapentadol IR on pain intensity over an extended period (48 hours) allowing for an evaluation of multiple doses of drug, even when dosing frequency may vary. Scoring is derived from the Numerical Rating Scale (NRS) from 0 = No pain to 11 = Pain as bad as you can imagine. (NCT00364533)
Timeframe: 48 hours
| Intervention | score on a scale (Mean) |
|---|---|
| Tapentadol IR Fixed Dose 50 mg | 73.9 |
| Tapentadol IR Fixed Dose 75 mg | 54.4 |
| Tapentadol IR Fixed Dose 100 mg | 49.3 |
| Oxycodone HCL IR Fixed Dose 10 mg | 57.6 |
| Placebo Fixed Dose | -18.6 |
"Defined by the percentage of subjects achieving at least 50% improvement from baseline in the primary endpoint based on the 11-point NRS at week 12. For this twice daily pain assessment, the subjects were to indicate the level of pain experienced over the previous 12 hours on an 11-point Numerical Rating Scale (NRS) where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine." (NCT00421928)
Timeframe: Baseline and Week 12
| Intervention | Percentage of participants (Number) |
|---|---|
| Tapentadol (CG5503) | 32.0 |
| Oxycodone | 17.3 |
| Placebo | 24.3 |
Change from baseline to Week 12 of WOMAC Global Score: WOMAC is measure with a Likert ordinal scale from 0-4 with lower scores indicating lower levels of symptoms or physical disability (NCT00421928)
Timeframe: Baseline and 12 week endpoint
| Intervention | Scores on a scale (Mean) |
|---|---|
| Tapentadol (CG5503) | -1.2 |
| Oxycodone | -1.1 |
| Placebo | -0.9 |
Ordinal measure indicating change from start of treatment (on a scale of 7 = Very much worse to 1 = Very much improved) (NCT00421928)
Timeframe: Baseline and 12 week endpoint
| Intervention | percentage of participants (Number) |
|---|---|
| Tapentadol (CG5503) | 51.1 |
| Oxycodone | 37.7 |
| Placebo | 32.4 |
"For this twice daily pain assessment, the subjects were to indicate the level of pain experienced over the previous 12 hours on an 11-point Numerical Rating Scale (NRS) where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine." (NCT00421928)
Timeframe: Baseline and 12 weeks (Primary endpoint is the average pain intensity score during the last week of the maintenance period).
| Intervention | Scores on a scale (Mean) |
|---|---|
| Tapentadol (CG5503) | -3.0 |
| Oxycodone | -2.6 |
| Placebo | -2.2 |
"A Sleep Questionniare addressed the following question: How long after bedtime/lights out did you fall asleep last night (hours)? 12 week endpoint-mean changes from baseline at endpoint for sleep latency. Decrease in time(hours) indicates improvement." (NCT00421928)
Timeframe: Baseline and 12 week endpoint
| Intervention | Hours (Mean) |
|---|---|
| Tapentadol (CG5503) | 0.2 |
| Oxycodone | 0.1 |
| Placebo | 0.3 |
"Change from baseline to end point in EuroQol-5 (EQ-5D) Dimension Questionnaire. A higher score indicates an improvement in health in the Health Status Index. The EQ-5D is a five dimensional health state classification. Each dimension is assessed on a 3-point ordinal scale (1=no problems, 2=some problems, 3=extreme problems). The responses to the five EQ-5D dimensions were scored using a utility-weighted algorithm to derive an EQ-5D health status index score between 0 to 1, with 1.00 indicating full health and 0 representing dead" (NCT00421928)
Timeframe: Baseline and 12 week endpoint
| Intervention | scores on a scale (Mean) |
|---|---|
| Tapentadol (CG5503) | 0.6 |
| Oxycodone | 0.5 |
| Placebo | 0.5 |
"Defined by the proportion of subjects achieving at least 50% improvement from baseline in the primary endpoint of change from baseline of the average pain intensity based on the 11-point Numerical Rating Scale (NRS) at week 12. The subjects were to indicate the level of pain experienced over the previous 12 hours on an 11-point NRS where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine." (NCT00449176)
Timeframe: Baseline and Week 12
| Intervention | Percentage of participants (Number) |
|---|---|
| Tapentadol ER | 27.0 |
| Oxycodone CR | 23.3 |
| Placebo | 18.9 |
Ordinal measure indicating change from start of treatment (On a scale of 7 = Very much Worse to 1 = very much improved) (NCT00449176)
Timeframe: Baseline and 12 week endpoint
| Intervention | percentage of participants (Number) |
|---|---|
| Tapentadol ER | 55.5 |
| Oxycodone CR | 60 |
| Placebo | 32.7 |
The number of participants who discontinued due to lack of efficacy from baseline to endpoint (NCT00449176)
Timeframe: Baseline and 12 weeks
| Intervention | participants (Number) |
|---|---|
| Tapentadol ER | 18 |
| Oxycodone CR | 9 |
| Placebo | 64 |
"For this twice daily pain assessment, the subjects were to indicate the level of pain experienced over the previous 12 hours on an 11-point Numerical Rating Scale (NRS) where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine." (NCT00449176)
Timeframe: Baseline and 12 weeks
| Intervention | scores on a scale (Mean) |
|---|---|
| Tapentadol ER | -2.9 |
| Oxycodone CR | -2.9 |
| Placebo | -2.1 |
"A Sleep Questionnaire addressed the following question: How long after bedtime/lights out did you fall asleep last night (hours)? 12 week endpoint-mean changes from baseline at endpoint for sleep latency. Decrease in time(hours) indicates improvement." (NCT00449176)
Timeframe: Baseline and 12 week endpoint
| Intervention | hours (Mean) |
|---|---|
| Tapentadol ER | -0.2 |
| Oxycodone CR | -0.2 |
| Placebo | -0.1 |
"Total pain score where zero equals no pain to ten equals pain as bad as you can imagine from 12 week endpoint vs baseline." (NCT00449176)
Timeframe: Baseline and 12 week endpoint
| Intervention | scores on a scale (Mean) |
|---|---|
| Tapentadol ER | -2.3 |
| Oxycodone CR | -2.1 |
| Placebo | -1.6 |
"Change from baseline to end point in EuroQol-5 Dimension Questionnaire. A higher score indicates an improvement in health in the Health Status Index. The EuroQol-5 is a five dimensional health state classification. Each dimension is assessed on a 3-point ordinal scale (1=no problems, 2=some problems, 3=extreme problems). The responses to the five EQ-5D dimensions were scored using a utility-weighted algorithm to derive an EQ-5D health status index score between 0 to 1, with 1.00 indicating full health and 0 representing dead." (NCT00449176)
Timeframe: Baseline and 12 week endpoint
| Intervention | scores on a scale (Mean) |
|---|---|
| Tapentadol ER | 0.2 |
| Oxycodone CR | 0.2 |
| Placebo | 0.1 |
The number of patients achieving at least 30% improvement in pain score at Week 12 of the double-blind maintenance period on an 11-point numerical rating scale compared with the start of the open-label period. (NCT00455520)
Timeframe: Start of Open Label and at 12 weeks of Double Blind
| Intervention | participants (Number) |
|---|---|
| Tapentadol ER | 105 |
| Placebo | 81 |
Percentage of patients who reported very much improved (1) or much improved (2) based on an ordinal measure indicating change from start of double blind treatment (on a scale of 7 = Very much worse to 1 = Very much improved) (NCT00455520)
Timeframe: 12 week endpoint
| Intervention | percentage of patients (Number) |
|---|---|
| Tapentadol ER | 64 |
| Placebo | 38 |
"For this twice daily pain assessment, the subjects were to indicate the level of pain experienced over the previous 12 hours on an 11-point Numerical Rating Scale (NRS) where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine." (NCT00455520)
Timeframe: Baseline and 12 weeks
| Intervention | scores on a scale (Mean) |
|---|---|
| Tapentadol ER | -0.1 |
| Placebo | 1.3 |
"Total pain score where zero equals no pain to ten equals pain as bad as you can imagine from 12 week endpoint vs baseline." (NCT00455520)
Timeframe: Baseline and12 week endpoint
| Intervention | Scores on a scale (Mean) |
|---|---|
| Tapentadol ER | -3.1 |
| Placebo | -2.2 |
"Change from baseline to end point in EuroQol-5 Dimension Questionnaire. A higher score indicates an improvement in health in the Health Status Index. The EuroQol-5 is a five dimensional health state classification. Each dimension is assessed on a 3-point ordinal scale (1=no problems, 2=some problems, 3=extreme problems). The responses to the five EQ-5D dimensions were scored using a utility-weighted algorithm to derive an EQ-5D health status index score between 0 to 1, with 1.00 indicating full health and 0 representing dead." (NCT00455520)
Timeframe: 12 week endpoint (change from baseline)
| Intervention | scores on a scale (Mean) |
|---|---|
| Tapentadol ER | 0.7 |
| Placebo | 0.6 |
"A Sleep Questionnaire addressed the following question: How long after bedtime/lights out did you fall asleep last night (hours)? 12 week endpoint-mean changes from baseline at endpoint for sleep latency. Decrease in time (hours) indicates improvement." (NCT00455520)
Timeframe: Baseline and 12 week endpoint
| Intervention | Hours (Mean) |
|---|---|
| Tapentadol ER | -0.2 |
| Placebo | -0.59 |
Mean total daily dose of rescue medication morphine sulphate immediate release tablets in milligrams per day (mg/day). (NCT00472303)
Timeframe: Day 1 (Start of Titration Phase) through Day 43 (End of Maintenance Phase)
| Intervention | milligrams per day of morphine rescue (Mean) |
|---|---|
| Tapentadol Prolonged Release (Titration Phase) | 13.31 |
| Morphine Controlled Release Titration Phase | 8.87 |
| Tapentadol Prolonged Release (Maintenance Phase) | 11.2 |
| Matching Placebo After Tapentadol in Titration Phase | 13.65 |
| Morphine Controlled Release Maintenance Phase | 8.91 |
Participants were issued morphine 10 mg immediate release medication. The number of participants using rescue medication morphine sulfate immediate release 10 mg tablets in the maintenance phase were counted. This use of morphine immediate release was captured in each participant's electronic diary. (NCT00472303)
Timeframe: Day 15 through Day 43 (End of Maintenance Phase)
| Intervention | participants (Number) |
|---|---|
| Tapentadol Prolonged Release | 75 |
| Morphine Controlled Release | 67 |
| Matching Placebo After Tapentadol in Titration Phase | 80 |
"A responder is a participant in the study that:~completed 28 days of the maintenance phase~had a numeric rating scale score below 5 on the 11 point scale (where 0 indicates no pain and 10 indicates worst possible pain. This twice daily current pain score was averaged over Day 18 to Day 43.~did not use more than 20 mg of rescue medication per day on average in the 28 day maintenance period (from Day 18 to Day 43).~A participant that met all 3 of the above-mentioned criteria is counted as a responder, in other words the participant benefited from the assigned drug treatment. A participant that failed to meet only 1 of the 3 criteria is not counted as a responder." (NCT00472303)
Timeframe: Day 18 through Day 43 (End of Maintenance Phase)
| Intervention | participants (Number) |
|---|---|
| Tapentadol Prolonged Release (Maintenance Phase) | 65 |
| Morphine Controlled Release (Maintenance Phase) | 75 |
| Matching Placebo After Tapentadol in Titration Phase | 55 |
EuroQoL-5D Health State Visual Analog Scale (VAS) is a participant rated questionnaire to assess health-related quality of life in terms of a single index value. The VAS component rates current health state on a scale from 0 (worst imaginable health state) to 100 (best imaginable health state); higher scores indicate better health. The values indicated represent the change from Day 1, a positive value indicates an improvement since the start of treatment. (NCT00472303)
Timeframe: Day 1 (Start of Titration); Day 14 (End of Titration Phase)
| Intervention | units on a scale (Mean) |
|---|---|
| Tapentadol Prolonged Release | 3.8 |
| Morphine Controlled Release | 5.6 |
"The participant scores the EuroQol-5D. The EuroQoL-5D is a five dimensional health state classification. Each dimension is assessed on a 3-point ordinal scale (1 = no problems, 2 = some problems, 3 = extreme problems).~The responses to the five EQ-5D dimensions are scored using a utility-weighted algorithm to derive an EQ-5D health status index score between 0 to 1, with 1.00 indicating full health and 0 representing dead. A negative change in the mean indicates a worsening in health status since the beginning of the maintenance phase. A positive change indicates an improvement in health. The minimal important difference in the Health Status Index is 0.074 (range -0.011 to 0.140)." (NCT00472303)
Timeframe: Day 15 (Start of Maintenance); Day 43 (End of Maintenance Phase)
| Intervention | units on a scale (Mean) |
|---|---|
| Tapentadol Prolonged Release | -0.0626 |
| Matching Placebo After Tapentadol in Titration Phase | -0.058 |
"The participant scores the EuroQol-5D. The EuroQoL-5D is a five dimensional health state classification. Each dimension is assessed on a 3-point ordinal scale (1 = no problems, 2 = some problems, 3 = extreme problems).~The responses to the five EQ-5D dimensions are scored using a utility-weighted algorithm to derive an EQ-5D health status index score between 0 to 1, with 1.00 indicating full health and 0 representing dead. A positive change in the mean indicates that during this phase the health status improved. A positive change indicates an improvement in health. The minimal important difference is 0.074 (range -0.011 to 0.140)." (NCT00472303)
Timeframe: Day 1 (Start of Titration); Day 14 (End of Titration Phase)
| Intervention | units on a scale (Mean) |
|---|---|
| Tapentadol Prolonged Release | 0.093 |
| Morphine Controlled Release | 0.131 |
"Participants were asked to record their current pain intensity in the morning and evening. Average pain scores are the averages of all scores recorded during the 3 days prior to re-randomization or during each week. The participant scored their pain intensity on an 11-point Numerical Rating Scale (NRS) where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine." (NCT00472303)
Timeframe: Day 15 through Day 43 (End of Maintenance Phase)
| Intervention | units on a scale (Mean) | ||||
|---|---|---|---|---|---|
| Prior to start of maintenance phase | End of Week 1 | End of Week 2 | End of Week 3 | End of Week 4 | |
| Matching Placebo After Tapentadol in the Titration Phase | 2.8686 | 3.0073 | 2.8683 | 2.9122 | 2.9220 |
| Morphine Controlled Release | 2.832 | 2.780 | 2.790 | 2.733 | 2.728 |
| Tapentadol Prolonged Release (Maintenance Phase) | 3.1444 | 3.0869 | 3.1148 | 3.0137 | 3.0002 |
"Participants were asked to record their current pain intensity in the morning and evening. Average pain scores are the averages of all scores recorded during the during each week. The participant scored their pain intensity on an 11-point Numerical Rating Scale (NRS) where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine." (NCT00472303)
Timeframe: Day 1 through Day 14 (End of Titration Phase)
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| Start of Titration | End of Week 1 | End of Week 2 | |
| Morphine Controlled Release (Titration Phase) | 6.258 | 4.937 | 3.690 |
"Participants were asked to record their current pain intensity in the morning and evening. Average pain scores are the averages of all scores recorded during each week. The participant scored their pain intensity on an 11-point Numerical Rating Scale (NRS) where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine." (NCT00472303)
Timeframe: Day 1 through Day 14 (End of Titration Phase)
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| Start of Titration | End of Week 1 | End of Week 2 | |
| Tapentadol Prolonged Release (Titration Phase) | 6.344 | 5.326 | 4.049 |
"In the Patient Global Impression of Change (PGIC) the participant is asked Since I began study treatment, my overall status is. The participant is asked to circle one of seven categories. Scores range from very much improved to very much worse. The question was asked at the end of the maintenance phase with reference to the start of the maintenance phase where the participant continued at the dose that was effective at the end of the Titration Phase." (NCT00472303)
Timeframe: Day 43 (End of Maintenance Phase)
| Intervention | participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Very Much Improved | Much Improved | Minimally Improved | No Change | Minimally Worse | Much Worse | Very Much Worse | |
| Matching Placebo After Tapentadol in Titration Phase | 6 | 31 | 38 | 11 | 9 | 7 | 1 |
| Morphine Controlled Release | 6 | 23 | 38 | 12 | 6 | 12 | 0 |
| Tapentadol Prolonged Release | 4 | 29 | 33 | 10 | 10 | 7 | 1 |
"Participants were asked the following question: Please rate the overall quality of your sleep last night? The quality of sleep from the start of maintenance to the completion of treatment is reported. The participant could choose one of the following options: Excellent, good, fair and poor." (NCT00472303)
Timeframe: Day 15 (Start of Maintenance); Day 43 (End of Maintenance Phase)
| Intervention | participants (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| Excellent at start of maintenance phase | Excellent at the end of maintenance phase | Good at start of maintenance phase | Good at the end of maintenance phase | Fair at start of maintenance phase | Fair at the end of maintenance phase | Poor at start of maintenance phase | Poor at the end of maintenance phase | |
| Matching Placebo After Tapentadol in Titration Phase | 4 | 8 | 60 | 49 | 42 | 37 | 4 | 13 |
| Morphine Controlled Release | 2 | 9 | 51 | 40 | 50 | 53 | 5 | 5 |
| Tapentadol Prolonged Release | 8 | 8 | 55 | 43 | 35 | 38 | 7 | 14 |
"Participants were asked the following question: Please rate the overall quality of your sleep last night? The quality of sleep from the start of the titration phase to the end of the titration phase was measured. The participant could choose one of the following options: Excellent, good, fair and poor." (NCT00472303)
Timeframe: Day 1 (Start of Titration); Day 14 (end of Titration Phase)
| Intervention | participants (Number) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Excellent at the start of the titration phase | Excellent at the end of the titration phase | Good at the start of the titration phase | Good at the end of the titration phase | Fair at the start of the titration phase | Fair at the end of the titration phase | Poor at the start of the titration phase | Poor at the end of the titration phase | Not completed at the start of titration | Not completed at the end of the titration | |
| Morphine Controlled Release | 4 | 3 | 47 | 64 | 51 | 61 | 41 | 14 | 15 | 16 |
| Tapentadol Prolonged Release | 9 | 12 | 77 | 139 | 142 | 121 | 74 | 37 | 36 | 29 |
EuroQoL-5D Health State Visual Analog Scale (VAS) is a participant rated questionnaire to assess health-related quality of life in terms of a single index value. The VAS component rates current health state on a scale from 0 (worst imaginable health state) to 100 (best imaginable health state); higher scores indicate a better health state. The values indicated represent the change from Day 15, a negative mean value indicates a worsening of health-related quality of life since the start of the maintenance phase. (NCT00472303)
Timeframe: Day 15 (Start of Maintenance); Day 43 (End of Maintenance Phase)
| Intervention | units on a scale (Mean) |
|---|---|
| Tapentadol Prolonged Release | -2.1 |
| Morphine Controlled Release | -0.6 |
| Matching Placebo After Tapentadol in the Titration Phase | -1.5 |
"Participants were asked to record their average pain over the last 24 hours pain intensity each evening. Average pain scores are the averages of all scores recorded during each week. The participant scored their pain intensity on an 11-point Numerical Rating Scale (NRS) where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine." (NCT00472303)
Timeframe: Day 1 through Day 14 (End of Titration Phase)
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| Prior to start of the Titration Phase | End of Week 1 of the Titration Phase | End of Week 2 of the Titration Phase | |
| Morphine Controlled Release | 6.162 | 4.906 | 3.669 |
"Participants were asked to record their average pain over the last 24 hours pain intensity each evening. Average pain scores are the averages of all scores recorded during each week. The participant scored their pain intensity on an 11-point Numerical Rating Scale (NRS) where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine." (NCT00472303)
Timeframe: Day 1 through Day 14 (End of Titration Phase)
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| Prior to start of the Titration Phase | End of Week 1 of the Titration Phase | End of Week 2 of the Titration Phase | |
| Tapentadol Prolonged Release | 6.315 | 5.324 | 4.021 |
"The number of participants using rescue medication morphine sulfate immediate release 10 mg tablets in the titration phase were counted. This data was captured in an electronic diary.~During the trial, morphine immediate release 10 mg was allowed as required without a maximum dose defined. However, participants were only re-randomized if their mean consumption of rescue medication was less or equal to 2 doses (20 mg) per day during the last 3 days of the titration phase)." (NCT00472303)
Timeframe: Day 1 through Day 14 (End of Titration Phase)
| Intervention | participants (Number) |
|---|---|
| Tapentadol Prolonged Release | 241 |
| Morphine Controlled Release | 91 |
"The Constipation Assessment (PAC-SYM) is a 12-item self-report questionnaire that assesses the severity of symptoms of constipation. Participants are asked How severe have each of these symptoms been in the last two weeks? e.g. Pain in your stomach. There are 3 subscales: 4 questions on Abdominal symptoms, 3 questions on rectal symptoms and 5 questions on stool symptoms. Responses are rated on a 5-point Likert Scale ranging from 0 (absence of symptom) to 4 (very severe symptoms). The changes in overall mean and in each of the mean sub-scores vary theoretically from -4 to +4 (where a change of +4 would indicate a change from not present to very severe symptom). If the changes in the overall or subscale mean scores are positive then there is a worsening in symptoms associated with constipation from the start to the end of the maintenance phase. A negative mean change indicates an improvement." (NCT00472303)
Timeframe: Day 15 (Start of Maintenance); Day 43 (End of Maintenance Phase)
| Intervention | units on a scale (Mean) | |||
|---|---|---|---|---|
| Overall abdominal subscale | Overall rectal subscale | Overall stool subscale | Overall PAC-SYM score | |
| Matching Placebo After Tapentadol in Titration Phase | -0.075 | -0.033 | -0.03 | -0.048 |
| Morphine Controlled Release | 0.026 | 0.014 | 0.03 | 0.024 |
| Tapentadol Prolonged Release | -0.105 | 0.017 | -0.07 | -0.059 |
"This instrument was developed by the National Institute on Drug Abuse. The physical components of withdrawal are primarily evaluated and based on questions and clinical observations. The possible opioid withdrawal effects are assessed using the Clinical Opioid Withdrawal Score (COWS). The COWS is a clinician rated 11-item scale that primarily evaluates the physical components of opioid withdrawal and is based on questions and clinical observations. Responses are rated on a Likert-type scale ranging from 0 to 4 or 5 depending on the item. The total COWS score is the sum of all individual items.~The following withdrawal categories are based on the total COWS score:~None: total score below 5;~Mild: total score from 5 to 12;~Moderate: total score 13 to 24;~Moderately Severe: total score 25 to 36;~Severe: total score above 36. The investigator completes the COWS after participants discontinued trial medication 2 to less than 5 days after last intake of trial medication." (NCT00472303)
Timeframe: Day 14 (End of Titration Phase)
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| None | Mild | Moderate | Moderately Severe | Severe | |
| Matching Placebo After Tapentadol in Titration Phase | 8 | 1 | 0 | 0 | 0 |
| Morphine Controlled Release | 5 | 1 | 0 | 0 | 0 |
| Tapentadol Prolonged Release | 7 | 0 | 0 | 0 | 0 |
The Short Form 36 (SF-36) includes several brief questions on 8 aspects, (physical functioning, role physical, bodily pain, general health, vitality, social functioning, role-emotional and mental health) that a participant was asked to score over the last week. Low scores on the Physical Component Summary measure indicate limitations in physical functioning, e.g. a high degree of bodily pain and physical limitations etc. For the Mental Component Summary measure, a low score is indicative of frequent psychological distress, social and role disability due to emotional problems etc. The theoretical range for the physical component score is 12.3279 to 59.6503. The theoretical range for the mental component score is 13.5313 to 59.6503. Positive values for changes in the component scores indicate an improvement. (NCT00472303)
Timeframe: Day 1 (Start of Titration); Day 14 (End of Titration Phase)
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Mental Component Summary | Physical Component Summary | |
| Morphine Controlled Release | 1.1 | 3.1 |
| Tapentadol Prolonged Release | 1.3 | 2.0 |
The Short Form 36 (SF-36) includes several brief questions on 8 aspects, (physical functioning, role physical, bodily pain, general health, vitality, social functioning, role-emotional and mental health) that a participant was asked to score over the last week. Low scores on the Physical Component Summary measure indicate limitations in physical functioning, e.g. a high degree of bodily pain and physical limitations etc. For the Mental Component Summary measure, a low score is indicative of frequent psychological distress, social and role disability due to emotional problems etc. The theoretical range for the physical component score is 12.3279 to 59.6503. The theoretical range for the mental component score is 13.5313 to 59.6503. Positive values for changes in the component scores indicate an improvement. (NCT00472303)
Timeframe: Day 15 (Start of Maintenance); Day 43 (End of Maintenance Phase)
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Mental Component Summary | Physical Component Summary | |
| Matching Placebo After Tapentadol in Titration Phase | -1.5 | -0.9 |
| Morphine Controlled Release | -2.164 | -0.671 |
| Tapentadol Extended Release | -0.4 | -1.1 |
"The Constipation Assessment (PAC-SYM) is a 12-item self-report questionnaire that assesses the severity of symptoms of constipation. Participants are asked How severe have each of these symptoms been in the last two weeks? e.g. Pain in your stomach. There are 3 subscales: 4 questions on Abdominal symptoms, 3 questions on rectal symptoms and 5 questions on stool symptoms. Responses are rated on a 5-point Likert Scale ranging from 0 (absence of symptom) to 4 (very severe symptoms). The changes in overall mean and in each of the mean sub-scores vary theoretically from -4 to +4 (where a change of +4 would indicate a change from not present to very severe symptom). If the changes in the overall or subscale mean scores are positive then there is a worsening in symptoms associated with constipation from the start to the end of the titration phase." (NCT00472303)
Timeframe: Day 1 (Start of Titration); Day 14 (End of Titration Phase)
| Intervention | units on a scale (Mean) | |||
|---|---|---|---|---|
| Overall abdominal subscale | Overall rectal subscale | Overall stool subscale | Overall PAC-SYM score | |
| Morphine Controlled Release | -0.076 | -0.006 | 0.13 | 0.027 |
| Tapentadol Prolonged Release | -0.062 | 0.059 | 0.02 | 0.003 |
"This instrument was developed by the National Institute on Drug Abuse. The physical components of withdrawal are primarily evaluated and based on questions and clinical observations. The possible opioid withdrawal effects are assessed using the Clinical Opioid Withdrawal Score (COWS). The COWS is a clinician rated 11-item scale that primarily evaluates the physical components of opioid withdrawal and is based on questions and clinical observations. Responses are rated on a Likert-type scale ranging from 0 to 4 or 5 depending on the item. The total COWS score is the sum of all individual items.~The following withdrawal categories are based on the total COWS score:~None: total score below 5;~Mild: total score from 5 to 12;~Moderate: total score 13 to 24;~Moderately Severe: total score 25 to 36;~Severe: total score above 36. The investigator completes the COWS after participants discontinued trial medication 2 to less than 5 days after last intake of trial medication." (NCT00472303)
Timeframe: Day 43 (End of Maintenance Phase)
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| None | Mild | Moderate | Moderately Severe | Severe | |
| Matching Placebo After Tapentadol in Titration Phase | 21 | 8 | 0 | 0 | 0 |
| Morphine Controlled Release | 23 | 6 | 0 | 0 | 0 |
| Tapentadol Prolonged Release | 19 | 7 | 0 | 0 | 0 |
"Participants were asked to record their average pain over the last 24 hours pain intensity each evening. Average pain scores are the averages of all scores recorded during each week. The participant scored their pain intensity on an 11-point Numerical Rating Scale (NRS) where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine." (NCT00472303)
Timeframe: Day 18 through Day 43 (End of Maintenance Phase)
| Intervention | units on a scale (Mean) | ||||
|---|---|---|---|---|---|
| Prior to start of Maintenance Phase | End of Week 1 of the Maintenance Phase | End of Week 2 of the Maintenance Phase | End of Week 3 of the Maintenance Phase | End of Week 4 of the Maintenance Phase | |
| Matching Placebo After Tapentadol in the Titration Phase | 2.928 | 3.115 | 3.005 | 3.055 | 3.095 |
| Morphine Controlled Release | 2.928 | 2.903 | 2.858 | 2.775 | 2.768 |
| Tapentadol Prolonged Release (Maintenance Phase) | 3.198 | 3.220 | 3.248 | 3.129 | 3.121 |
"Pain Intensity assessed at predefined time points over a 24 hour period using an 11-point Numeric Rating Scale (NRS) where a score of zero indicates no pain and a score of ten indicates pain as bad as you can imagine. Differences calculated as [baseline-post baseline] at each predefined time point. The theoretical maximum range of Sum of pain intensity differences (SPID24) is from -240 (indicative of an increase in pain) to 240 (indicative of a decrease in pain, assuming patients start with a baseline value of 10 and all subsequent values will be 0)." (NCT00478023)
Timeframe: Baseline to 24 hours after first intake of study drug
| Intervention | units on scale (Mean) |
|---|---|
| Morphine | 48.8 |
| CG5503 50mg | 49.0 |
| CG5503 75mg | 52.4 |
| CG5503 100mg | 52.9 |
| Placebo | 29.0 |
"Pain Intensity assessed at predefined time points over a 48 hour period using an 11-point Numeric Rating Scale (NRS) where a score of zero indicates no pain and a score of ten indicates pain as bad as you can imagine. Differences calculated as [baseline-post baseline] at each predefined time point. The theoretical maximum range of Sum of pain intensity differences (SPID48) is from -480 (indicative of an increase in pain) to 480 (indicative of a decrease in pain, assuming patients start with a baseline value of 10 and all subsequent values will be 0)." (NCT00478023)
Timeframe: Baseline value to 48 hours after first study drug intake.
| Intervention | units on scale (Mean) |
|---|---|
| Morphine | 116.6 |
| CG5503 50mg | 112.4 |
| CG5503 75mg | 120.6 |
| CG5503 100mg | 123.5 |
| Placebo | 71.1 |
"The Constipation Assessment (PAC-SYM) is a 12-item self-report questionnaire that assesses the severity of symptoms of constipation. Participants are asked How severe have each of these symptoms been in the last two weeks? e.g. Pain in your stomach. There are 3 subscales: 4 questions on Abdominal symptoms, 3 on rectal symptoms and 5 on stool symptoms. Responses are rated on a 5-point Likert scale ranging from 0 (absence of symptom) to 4 (very severe symptoms). If the changes in the overall or subscale scores are positive then there is a worsening in symptoms associated with constipation." (NCT00486811)
Timeframe: Change from Baseline to Week 12 of the Maintenance Period
| Intervention | Units on a scale (Mean) | |||
|---|---|---|---|---|
| Overall abdominal subscale change | Overall rectal subscale change | Overall stool subscale change | Overall PAC-SYM score change | |
| Oxycodone CR | 0.3 | 0.4 | 0.6 | 0.4 |
| Placebo Matching | -0.1 | 0.0 | 0.0 | 0.0 |
| Tapentadol ER | 0.1 | 0.1 | 0.2 | 0.1 |
In the Patient Global Impression of Change (PGIC) the participant indicates the perceived change over the treatment period. The participant is requested to choose one of seven categories. Scores range from very much improved to very much worse. (NCT00486811)
Timeframe: Baseline; End of 12 week maintenance period
| Intervention | participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Very Much Improved | Much Improved | Minimally Improved | No Change | Minimally Worse | Much Worse | Very Much Worse | |
| Oxycodone CR | 25 | 65 | 51 | 30 | 19 | 19 | 3 |
| Placebo Matching | 33 | 94 | 76 | 59 | 15 | 14 | 3 |
| Tapentadol ER | 40 | 99 | 61 | 22 | 9 | 14 | 3 |
"The Sleep Questionnaire addressed the following question: How many times did you wake up during the night?. Sleep was assessed by the subject once a week during the entire double-blind treatment period. Reported are the baseline and end of maintenance period. Generally the less the number of awakenings the better the sleep." (NCT00486811)
Timeframe: Week 12 of the maintenance period compared with baseline
| Intervention | participants (Number) | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| No awakening during night baseline | No awakening during night end point | 1 awakening per night baseline | 1 awakening per night end point | 2 awakening per night baseline | 2 awakening per night end point | 3 awakening per night baseline | 3 awakening per night end point | 4 awakening per night baseline | 4 awakening per night end point | 5 or more awakenings per night baseline | 5 or more awakenings per night end point | |
| Oxycodone CR | 29 | 46 | 57 | 67 | 85 | 89 | 77 | 61 | 38 | 42 | 28 | 23 |
| Placebo Matching | 32 | 55 | 56 | 89 | 102 | 84 | 82 | 66 | 33 | 21 | 22 | 22 |
| Tapentadol ER | 33 | 44 | 53 | 92 | 88 | 94 | 66 | 46 | 39 | 22 | 26 | 21 |
Change from baseline to week 12 of Western Ontario McMaster Questionnaire (WOMAC) Global Score: WOMAC is measured with a Likert ordinal scale (the participant gives one of 5 possible answers) from 0 to 4. Higher scores indicate that a symptom is bothersome and physically disabling. (NCT00486811)
Timeframe: Change from baseline to week 12 of the maintenance period
| Intervention | units on a scale (Mean) |
|---|---|
| Placebo Matching | -1.0 |
| Tapentadol ER | -1.0 |
| Oxycodone CR | -1.1 |
"The twice daily pain assessments were averaged. The participants were to indicate their pain on an 11-point Numerical Rating Scale (NRS) where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine. The lower the value the less pain intensity." (NCT00486811)
Timeframe: Change from Baseline to Week 12 of the Maintenance Period
| Intervention | Units on a scale (Mean) |
|---|---|
| Placebo Matching | -2.5 |
| Tapentadol ER | -2.7 |
| Oxycodone CR | -2.3 |
"For this twice daily pain assessment, the participants were required to indicate the level of pain experienced over the previous 12 hours on an 11-point Numeric Rating Scale (NRS) where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine. The lower the value the less pain in the treatment group. Negative values indicate a reduction in pain." (NCT00486811)
Timeframe: Change from baseline over the 12 week Maintenance Period
| Intervention | Units on a scale (Mean) |
|---|---|
| Placebo Matching | -2.2 |
| Tapentadol ER | -2.5 |
| Oxycodone CR | -2.1 |
"The participant scored the EuroQol-5. This is a five dimensional health state classification. Each dimension is assessed on a 3-point ordinal scale (1=no problems, 2=some problems, 3=extreme problems). The responses to the five EQ-5D dimensions were scored using a utility-weighted algorithm to derive an EQ-5D health status index score between 0 to 1, with 1.00 indicating full health and 0 representing dead. The positive values indicate that during the study the health status improved." (NCT00486811)
Timeframe: Comparison of Baseline to Week 12 of the Maintenance Period
| Intervention | Index value (Mean) |
|---|---|
| Placebo Matching | 0.2 |
| Tapentadol ER | 0.2 |
| Oxycodone CR | 0.1 |
"The Sleep Questionnaire addressed the following question: How long did you sleep last night?. The mean change for the number of hours slept during the night before from baseline to 12 weeks was studied." (NCT00486811)
Timeframe: Baseline to Week 12 of the maintenance period
| Intervention | hours (Mean) |
|---|---|
| Placebo Matching | 0.2 |
| Tapentadol ER | 0.2 |
| Oxycodone CR | 0.3 |
"The Sleep Questionnaire addressed the following question: How long after bedtime/lights out did you fall asleep last night(hours)?. The mean change from baseline to 12 weeks was studied. Decrease in time, measured in hours, indicates an improvement." (NCT00486811)
Timeframe: Week 12 of the maintenance period compared to baseline
| Intervention | hours (Mean) |
|---|---|
| Placebo Matching | 0.4 |
| Tapentadol ER | 0.2 |
| Oxycodone CR | 0.2 |
The Scores Form 36 (SF-36) includes several brief board questions on 8 aspects, (physical functioning, role physical, bodily pain, general health, vitality, social functioning, role-emotional and mental health) that a participant was asked to score over the last week. A higher score indicates an improvement in health. All domains are scored on a scale from 0 (negative health) to 100 (positive health), with 100 representing the best possible health state. (NCT00486811)
Timeframe: Change From Baseline to Week 12 of the Maintenance Period
| Intervention | units on a scale (Least Squares Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Physical Functioning | Role-Physical | Bodily Pain | General Health | Vitality | Social Functioning | Role-Emotional | Mental Health | |
| Oxycodone CR | 9.5 | 13.8 | 13.9 | 4.8 | 3.8 | 4.9 | 5.0 | 2.7 |
| Placebo Matching | 11.1 | 18.7 | 15.4 | 6.8 | 6.8 | 7.5 | 7.9 | 6.3 |
| Tapentadol ER | 11.70 | 20.8 | 19.1 | 6.8 | 7.1 | 9.2 | 11.1 | 3.7 |
"The Sleep Questionnaire addressed the following question: Please rate the overall quality of your sleep last night? The quality of sleep at baseline and prior to completion of treatment are reported. The participant can choose one of the following options: Excellent, good, fair and poor." (NCT00486811)
Timeframe: Week 12 of the maintenance period compared to baseline
| Intervention | participants (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| Excellent at baseline | Excellent at end point | Good at baseline | Good at end point | Fair at baseline | Fair at end point | Poor at baseline | Poor at end point | |
| Oxycodone CR | 5 | 19 | 118 | 158 | 151 | 125 | 40 | 26 |
| Placebo Matching | 11 | 10 | 134 | 174 | 146 | 124 | 36 | 29 |
| Tapentadol ER | 8 | 15 | 122 | 177 | 138 | 107 | 37 | 20 |
The number of subjects who reported a TEAE during the treatment period. TEAE was defined as any adverse event that started or worsened on or after the start of the study medication and up to 3 days after the discontinuation of the study medication. (NCT00487435)
Timeframe: 52 weeks
| Intervention | participants (Number) |
|---|---|
| Tapentadol (CG5503) Extended Release (ER) | 907 |
"The subjects indicated the average level of pain experienced, at each study visit, over the previous 24 hours on an 11-point Numerical Rating Scale (NRS) where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine." (NCT00487435)
Timeframe: Baseline, 52 weeks
| Intervention | Scores on a Scale (Mean) |
|---|---|
| Tapentadol (CG5503) Extended Release (ER) | -0.26 |
The Patient Global Impression of Change (PGIC) is an instrument where the participant indicates their perceived change at the end of a treatment phase. The overall participant status assessed using Patient Global Impression of Change (PGIC) self-assessment questionnaire which was used by participants to report on 7 categories listed as follows; Very Much Improved, Much Improved, Minimally Improved, No Change, Minimally Worse, Much Worse and Very Much Worse in tapentadol and morphine at Day 15 (Start of Maintenance Phase) and repeated in participants completing the Maintenance Phase in the Matching Placebo, Tapentadol and Morphine (Day 43). (NCT00505414)
Timeframe: Day 15 corresponds with PGIC at end of titration phase; Day 43 corresponds with PGIC at end of maintenance phase
| Intervention | participants (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| Very Much Improved | Much Improved | Minimally Improved | No Change | Minimally Worse | Much Worse | Very Much Worse | Missing | |
| Matching Placebo (Maintenance Phase) | 0 | 2 | 4 | 1 | 0 | 2 | 0 | 5 |
| Morphine (Maintenance Phase) | 1 | 3 | 4 | 4 | 0 | 1 | 0 | 5 |
| Morphine (Titration Phase) | 0 | 1 | 4 | 2 | 0 | 0 | 0 | 24 |
| Tapentadol (Maintenance Phase) | 0 | 8 | 4 | 1 | 1 | 1 | 0 | 0 |
| Tapentadol (Titration Phase) | 0 | 5 | 8 | 3 | 4 | 2 | 0 | 40 |
"A responder is a participant in the study that:~completed 28 days of the maintenance phase~had a numeric rating scale score below 5 on the 11 point scale (where 0 indicates no pain and 10 indicates worst possible pain. This twice daily current pain score was averaged over Day 18 to Day 43.~did not use more than 30 mg of rescue medication per day on average in the 28 day (excluding the first 3 days) maintenance period (from Day 18 to Day 43).~A participant that met all 3 of the above-mentioned criteria is counted as a responder, in other words the participant benefited from the assigned drug treatment. A participant that fails to meet at least 1 of the 3 criteria is not counted as a responder." (NCT00505414)
Timeframe: End of the 4 week Maintenance Phase (Day 43)
| Intervention | participants (Number) |
|---|---|
| Morphine (Maintenance Phase) | 6 |
| Tapentadol (Maintenance Phase) | 8 |
| Matching Placebo (Maintenance Phase) | 3 |
Average total daily dose (TDD) of tapentadol ER during the double-blind treatment period. (NCT00594516)
Timeframe: 14 days for each treatment period
| Intervention | mg (Mean) |
|---|---|
| Tapentadol | 330.4 |
Average total daily dose (TDD) of tapentadol IR during the double blind treatment period (NCT00594516)
Timeframe: 14-day for each DB treatment period
| Intervention | mg (Mean) |
|---|---|
| Tapentadol | 331.0 |
(NCT00594516)
Timeframe: 14 days for each cross-over period
| Intervention | participants (Number) |
|---|---|
| Tapentadol | 24 |
(NCT00594516)
Timeframe: 14 days for each cross-over period
| Intervention | participants (Number) |
|---|---|
| Tapentadol | 29 |
"For this twice daily pain assessment, the subjects were to indicate the level of average pain experienced over the previous 12 hours on an 11-point Numerical Rating Scale (NRS) where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine." (NCT00594516)
Timeframe: 14 days for each cross-over period
| Intervention | Units on a scale (Least Squares Mean) |
|---|---|
| Tapentadol | 0.1 |
Total Pain Relief (TOTPAR48) was defined as the weighted sum over all pain relief scores(PAR) from 0.5 hour to Hour 48, with the actual time elapsed from the previous PAR observation as the weight. A higher value in TOTPAR indicates greater pain relief. (NCT00613938)
Timeframe: 48 hours
| Intervention | scores on a scale (Mean) |
|---|---|
| Placebo | 68.2 |
| Tapentadol 50mg Fixed Dose | 96.6 |
| Tapentadol 75mg Fixed Dose | 107.5 |
| Oxycodone 10mg Fixed Dose | 105.2 |
The SPID score incorporates the cumulative analgesic effects of tapentadol IR on pain intensity over an extended period (12 to 72 hours) allowing for an evaluation of multiple doses of drug, even when dosing frequency may vary. Scoring is derived from the Numerical Rating Scale (NRS) from 0 = No pain to 11 = Pain as bad as you can imagine. A positive difference between the mean SPID12 for an active study drug and placebo would indicate a numerically larger analgesic effect for subjects dosed with active study drug than in the placebo group. A higher value in SPID indicates greater pain relief. (NCT00613938)
Timeframe: 12 hours
| Intervention | Scores on a scale (Mean) |
|---|---|
| Placebo | 7.5 |
| Tapentadol 50mg Fixed Dose | 21.1 |
| Tapentadol 75mg Fixed Dose | 26.0 |
| Oxycodone 10mg Fixed Dose | 24.9 |
The SPID score incorporates the cumulative analgesic effects of tapentadol IR on pain intensity over an extended period (48 hours) allowing for an evaluation of multiple doses of drug, even when dosing frequency may vary. Scoring is derived from the Numerical Rating Scale (NRS) from 0 = No pain to 11 = Pain as bad as you can imagine. A positive difference between the mean SPID48 for an active study drug and placebo would indicate a numerically larger analgesic effect for subjects dosed with active study drug than in the placebo group. A higher value in SPID indicates greater pain relief. (NCT00613938)
Timeframe: 48 hours
| Intervention | Scores on a scale (Mean) |
|---|---|
| Placebo | 54.1 |
| Tapentadol 50mg Fixed Dose | 122.2 |
| Tapentadol 75mg Fixed Dose | 143.7 |
| Oxycodone 10mg Fixed Dose | 140.3 |
The SPID score incorporates the cumulative analgesic effects of tapentadol IR on pain intensity over an extended period (12 to 72 hours) allowing for an evaluation of multiple doses of drug, even when dosing frequency may vary. Scoring is derived from the Numerical Rating Scale (NRS) from 0 = No pain to 11 = Pain as bad as you can imagine. A positive difference between the mean SPID24 for an active study drug and placebo would indicate a numerically larger analgesic effect for subjects dosed with active study drug than in the placebo group. A higher value in SPID indicates greater pain relief. (NCT00613938)
Timeframe: 24 hours
| Intervention | Scores on a scale (Mean) |
|---|---|
| Placebo | 12.1 |
| Tapentadol 50mg Fixed Dose | 45.4 |
| Tapentadol 75mg Fixed Dose | 58.1 |
| Oxycodone 10mg Fixed Dose | 53.8 |
Ordinal measure indicating change from the start of treatment (On a scale of 7 = Very much Worse to 1 = very much improved) to endpoint at Day 3 (NCT00613938)
Timeframe: Baseline and 3 days
| Intervention | percentage of participants (Number) |
|---|---|
| Placebo | 65.2 |
| Tapentadol 50mg Fixed Dose | 83.2 |
| Tapentadol 75mg Fixed Dose | 87.8 |
| Oxycodone 10mg Fixed Dose | 86.0 |
The 30% responder rate was defined as the proportion of participants with a value of percentage change greater than or equal to the 30% from baseline in pain intensity at Day 3 (average of Day 3 PM and Day 4 AM). (NCT00771758)
Timeframe: Day 3
| Intervention | percentage of participants (Number) |
|---|---|
| Tapentadol IR | 36.1 |
| Oxycodone IR | 39.0 |
| Placebo | 50.0 |
The 30% responder rate was defined as the proportion of participants with a value of percentage change greater than or equal to the 30% from baseline in pain intensity at Day 5 (average of Day 5 PM and Day 6 AM). (NCT00771758)
Timeframe: Day 5
| Intervention | percentage of participants (Number) |
|---|---|
| Tapentadol IR | 44.4 |
| Oxycodone IR | 48.8 |
| Placebo | 35.0 |
The 50% responder rate was defined as the proportion of participants with a value of percentage change greater than or equal to the 50% from baseline in pain intensity at Day 10 (average of Day 9 PM and Day 10 AM). (NCT00771758)
Timeframe: Day 10
| Intervention | percentage of participants (Number) |
|---|---|
| Tapentadol IR | 30.6 |
| Oxycodone IR | 26.8 |
| Placebo | 30.0 |
The 50% responder rate was defined as the proportion of participants with a value of percentage change greater than or equal to the 50% from baseline in pain intensity at Day 3 (average of Day 3 PM and Day 4 AM). (NCT00771758)
Timeframe: Day 3
| Intervention | percentage of participants (Number) |
|---|---|
| Tapentadol IR | 25.0 |
| Oxycodone IR | 24.4 |
| Placebo | 25.0 |
The 50% responder rate was defined as the proportion of participants with a value of percentage change greater than or equal to the 50% from baseline in pain intensity at Day 5 (average of Day 5 PM and Day 6 AM). (NCT00771758)
Timeframe: Day 5
| Intervention | percentage of participants (Number) |
|---|---|
| Tapentadol IR | 25.0 |
| Oxycodone IR | 26.8 |
| Placebo | 25.0 |
The participants were assessed whether were able to rise from a chair 5 times at each visit. For those subjects who were unable to complete all 5 rises, the number of rises would be recorded. For those completed the 5 rises, 5 were recorded. The change in number of chair stands at the end of study was derived using the number of chair stands at baseline minus the number of chair stands at the end of study (Day 10). The range of change in number of chair stands is from -5 to 5. A negative value indicated better performance. (NCT00771758)
Timeframe: Day 10
| Intervention | chair stands (Mean) |
|---|---|
| Tapentadol IR | -0.1 |
| Oxycodone IR | -0.0 |
| Placebo | 0.0 |
"The time for the subject to rise from a chair 5 times was measured at baseline and the end of study.~Change = baseline - end of study. For the change in each treatment group, only subjects who were assessed at both baseline and end of study were summarized. A positive value of Change indicated performance improved." (NCT00771758)
Timeframe: Day 10
| Intervention | second (Mean) |
|---|---|
| Tapentadol IR | 3.1 |
| Oxycodone IR | 3.6 |
| Placebo | 2.6 |
The participants were assessed whether were able to walk for 4 meters at each visit. For those subjects who were unable to walk 4 meters, the distance walked would be recorded. For those completed the walk, 4 meters were recorded. The change in distance walked at the end of study was derived using the distance walked at baseline minus the distance walked at the end of study (Day 10). The range of change in distance walked is from -4 to 4. A negative value indicated better performance. (NCT00771758)
Timeframe: Day 10
| Intervention | meters (Mean) |
|---|---|
| Tapentadol IR | -0.1 |
| Oxycodone IR | 0.4 |
| Placebo | 0.0 |
The time for the subject to walk for 4 meters was measured at baseline and the end of study. Change = baseline - end of study. For the change in each treatment group, only subjects who were assessed at both baseline and end of study were summarized. A positive value of Change indicated performance improved. (NCT00771758)
Timeframe: Day 10
| Intervention | seconds (Mean) |
|---|---|
| Tapentadol IR | 0.6 |
| Oxycodone IR | 3.5 |
| Placebo | 0.6 |
Pain Intensity (PI) was assessed on 11-point numerical rating scale from 0=no pain to 10=pain as bad as you can imagine. Pain Intensity Difference (PID) was the difference between baseline PI (prior to the first dose) and current PI at assessment. Sum of Pain Intensity Difference Over 10 Days was calculated as the time-weighted Sum of PID scores up to Day 10, 8 AM. The range is from -2160 to 2160. The higher value in Sum of Pain Intensity Difference indicates greater pain relief. (NCT00771758)
Timeframe: 10 Days (216 Hours)
| Intervention | Scores on a scale (Mean) |
|---|---|
| Tapentadol IR | 505.0 |
| Oxycodone IR | 422.9 |
| Placebo | 389.9 |
Pain Intensity (PI) was assessed on 11-point numerical rating scale from 0=no pain to 10=pain as bad as you can imagine. Pain Intensity Difference (PID) was the difference between baseline PI (prior to the first dose) and current PI at assessment. SPID48 was calculated as the time-weighted Sum of PID scores over 48 hours. The range of SPID48 is from -480 to 480. The higher value in SPID indicates greater pain relief. (NCT00771758)
Timeframe: 2 Days (48 hours)
| Intervention | Scores on a scale (Mean) |
|---|---|
| Tapentadol IR | 82.1 |
| Oxycodone IR | 86.5 |
| Placebo | 67.1 |
"Pain Intensity (PI) was assessed on 11-point numerical rating scale from 0=no pain to 10=pain as bad as you can imagine. Pain Intensity Difference (PID) was the difference between baseline PI (prior to the first dose) and current PI at assessment. SPID72 was calculated as the time-weighted Sum of PID scores over 72 hours. The range of SPID72 is from -720 to 720. The higher value in SPID indicates greater pain relief.~The study was terminated prematurely due to slow enrollment after 108 of 600 subjects enrolled. Valid statistical conclusions cannot be made due to the low number of subjects." (NCT00771758)
Timeframe: 3 Days (72 hours)
| Intervention | Scores on a scale (Mean) |
|---|---|
| Tapentadol IR | 139.0 |
| Oxycodone IR | 129.4 |
| Placebo | 114.2 |
Pain Intensity (PI) was assessed on 11-point numerical rating scale from 0=no pain to 10=pain as bad as you can imagine. Pain Intensity Difference (PID) was the difference between baseline PI (prior to the first dose) and current PI at assessment. SPID120 was calculated as the time-weighted Sum of PID scores over 120 hours. The range of SPID120 is from -1200 to 1200. The higher value in SPID indicates greater pain relief. (NCT00771758)
Timeframe: 5 Days (120 hours)
| Intervention | Scores on a scale (Mean) |
|---|---|
| Tapentadol IR | 252.7 |
| Oxycodone IR | 227.1 |
| Placebo | 198.4 |
The Sum of Total Pain Relief and Sum of Pain Intensity Difference (SPRID) was derived from Sum of TOTPAR and SPID. The range of SPRID over 10 days is from -2160 to 3024. A higher value in SPRID indicated greater pain relief. (NCT00771758)
Timeframe: 10 Days
| Intervention | Scores on a scale (Mean) |
|---|---|
| Tapentadol IR | 883.8 |
| Oxycodone IR | 837.3 |
| Placebo | 781.7 |
The Sum of Total Pain Relief and Sum of Pain Intensity Difference (SPRID) was derived from Sum of TOTPAR and SPID. The range of SPRID over 2 days is from -480 to 672. A higher value in SPRID indicated greater pain relief. (NCT00771758)
Timeframe: 2 Days
| Intervention | Scores on a scale (Mean) |
|---|---|
| Tapentadol IR | 168.6 |
| Oxycodone IR | 178.9 |
| Placebo | 158.9 |
The Sum of Total Pain Relief and Sum of Pain Intensity Difference (SPRID) was derived from Sum of TOTPAR and SPID. The range of SPRID over 3 days is from -720 to 1008. A higher value in SPRID indicated greater pain relief. (NCT00771758)
Timeframe: 3 Days
| Intervention | Scores on a scale (Mean) |
|---|---|
| Tapentadol IR | 265.5 |
| Oxycodone IR | 267.7 |
| Placebo | 240.0 |
The Sum of Total Pain Relief and Sum of Pain Intensity Difference (SPRID) was derived from Sum of TOTPAR and SPID. The range of SPRID over 5 days is from -1200 to 1680. A higher value in SPRID indicated greater pain relief. (NCT00771758)
Timeframe: 5 Days
| Intervention | Scores on a scale (Mean) |
|---|---|
| Tapentadol IR | 469.5 |
| Oxycodone IR | 459.7 |
| Placebo | 419.1 |
Level of functionality assessed using a 5-point scale where 0=no difficulty and 4=impossible without help. (NCT00771758)
Timeframe: Day 10
| Intervention | percentage of participants (Number) |
|---|---|
| Tapentadol IR | 21.4 |
| Oxycodone IR | 20.8 |
| Placebo | 7.1 |
Level of functionality assessed using a 5-point scale where 0=no difficulty and 4=impossible without help. (NCT00771758)
Timeframe: Day 3
| Intervention | percentage of participants (Number) |
|---|---|
| Tapentadol IR | 16.7 |
| Oxycodone IR | 19.4 |
| Placebo | 10.5 |
Level of functionality assessed using a 5-point scale where 0=no difficulty and 4=impossible without help. (NCT00771758)
Timeframe: Day 5
| Intervention | percentage of participants (Number) |
|---|---|
| Tapentadol IR | 15.6 |
| Oxycodone IR | 14.8 |
| Placebo | 5.9 |
Level of functionality assessed using a 5-point scale where 0=no difficulty and 4=impossible without help. (NCT00771758)
Timeframe: Day 3
| Intervention | percentage of participants (Number) |
|---|---|
| Tapentadol IR | 16.7 |
| Oxycodone IR | 8.3 |
| Placebo | 10.5 |
Level of functionality assessed using a 5-point scale where 0=no difficulty and 4=impossible without help. (NCT00771758)
Timeframe: Day 10
| Intervention | percentage of participants (Number) |
|---|---|
| Tapentadol IR | 28.6 |
| Oxycodone IR | 8.3 |
| Placebo | 14.3 |
Level of functionality assessed using a 5-point scale where 0=no difficulty and 4=impossible without help. (NCT00771758)
Timeframe: Day 2
| Intervention | percentage of participants (Number) |
|---|---|
| Tapentadol IR | 20.6 |
| Oxycodone IR | 14.3 |
| Placebo | 0 |
Level of functionality assessed using a 5-point scale where 0=no difficulty and 4=impossible without help. (NCT00771758)
Timeframe: Day 5
| Intervention | percentage of participants (Number) |
|---|---|
| Tapentadol IR | 18.8 |
| Oxycodone IR | 7.4 |
| Placebo | 5.6 |
Level of functionality assessed using a 5-point scale where 0=no difficulty and 4=impossible without help. (NCT00771758)
Timeframe: Day 10
| Intervention | percentage of participants (Number) |
|---|---|
| Tapentadol IR | 28.6 |
| Oxycodone IR | 25.0 |
| Placebo | 7.1 |
Level of functionality assessed using a 5-point scale where 0=no difficulty and 4=impossible without help. (NCT00771758)
Timeframe: Day 2
| Intervention | percentage of participants (Number) |
|---|---|
| Tapentadol IR | 14.7 |
| Oxycodone IR | 8.6 |
| Placebo | 11.1 |
Level of functionality assessed using a 5-point scale where 0=no difficulty and 4=impossible without help. (NCT00771758)
Timeframe: Day 3
| Intervention | percentage of participants (Number) |
|---|---|
| Tapentadol IR | 19.4 |
| Oxycodone IR | 13.9 |
| Placebo | 15.8 |
Level of functionality assessed using a 5-point scale where 0=no difficulty and 4=impossible without help. (NCT00771758)
Timeframe: Day 5
| Intervention | percentage of participants (Number) |
|---|---|
| Tapentadol IR | 25.0 |
| Oxycodone IR | 14.8 |
| Placebo | 11.1 |
Treatment satisfaction was measured using a 7-point scale where 1 = very satisfied and 7 = very dissatisfied. (NCT00771758)
Timeframe: Day 10
| Intervention | Scores on a scale (Mean) |
|---|---|
| Tapentadol IR | 3.3 |
| Oxycodone IR | 2.5 |
| Placebo | 3.1 |
Treatment satisfaction was measured using a 7-point scale where 1 = very satisfied and 7 = very dissatisfied. (NCT00771758)
Timeframe: Day 2
| Intervention | Scores on a scale (Mean) |
|---|---|
| Tapentadol IR | 3.5 |
| Oxycodone IR | 3.0 |
| Placebo | 3.6 |
Treatment satisfaction was measured using a 7-point scale where 1 = very satisfied and 7 = very dissatisfied. (NCT00771758)
Timeframe: Day 3
| Intervention | Scores on a scale (Mean) |
|---|---|
| Tapentadol IR | 3.3 |
| Oxycodone IR | 2.8 |
| Placebo | 3.3 |
Level of functionality assessed using a 5-point scale where 0=no difficulty and 4=impossible without help. (NCT00771758)
Timeframe: Day 2
| Intervention | percentage of participants (Number) |
|---|---|
| Tapentadol IR | 11.8 |
| Oxycodone IR | 14.3 |
| Placebo | 11.1 |
Pain Relief was defined as a 5-point categorical scale of 0-4 (0=none, 1=A little, 2=Some, 3=A lot, 4=Complete). Total Pain Relief (TOTPAR) was calculated as the time-weighted sum over all pain relief up to hour 48. The range of TOTPAR over 2 days is from 0 to 192. A higher value in TOTPAR indicated greater pain relief. (NCT00771758)
Timeframe: 2 Days (48 Hours)
| Intervention | Scores on a scale (Mean) |
|---|---|
| Tapentadol IR | 84.7 |
| Oxycodone IR | 92.3 |
| Placebo | 89.5 |
Pain Relief was defined as a 5-point categorical scale of 0-4 (0=none, 1=A little, 2=Some, 3=A lot, 4=Complete). Total Pain Relief (TOTPAR) was calculated as the time-weighted sum over all pain relief up to hour 72. The range of TOTPAR over 3 days is from 0 to 288. A higher value in TOTPAR indicated greater pain relief. (NCT00771758)
Timeframe: 3 Days (72 Hours)
| Intervention | Scores on a scale (Mean) |
|---|---|
| Tapentadol IR | 126.5 |
| Oxycodone IR | 138.3 |
| Placebo | 125.8 |
Pain Relief was defined as a 5-point categorical scale of 0-4 (0=none, 1=A little, 2=Some, 3=A lot, 4=Complete). Total Pain Relief (TOTPAR) was calculated as the time-weighted sum over all pain relief up to hour 120. The range of TOTPAR over 5 days is from 0 to 480. A higher value in TOTPAR indicated greater pain relief. (NCT00771758)
Timeframe: 5 Days (120 Hours)
| Intervention | Scores on a scale (Mean) |
|---|---|
| Tapentadol IR | 216.8 |
| Oxycodone IR | 232.6 |
| Placebo | 220.7 |
Clinician Global Impression of Change (CGIC) was defined as the 7-point numeric scale, where 1=very much improved to 7=very much worse. (NCT00771758)
Timeframe: Day 10
| Intervention | percenatage of participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Very much improved | Much improved | Minimally improved | No change | Minimally worse | Much worse | Very much worse | |
| Oxycodone IR | 7.0 | 39.5 | 34.9 | 9.3 | 4.7 | 2.3 | 0 |
| Placebo | 14.3 | 23.8 | 33.3 | 19.0 | 4.8 | 0 | 4.8 |
| Tapentadol IR | 19.5 | 29.3 | 19.5 | 26.8 | 0 | 0 | 0 |
Patient Global Impression of Change (PGIC) was defined as the 7-point numeric scale, where 1=very much improved to 7=very much worse. (NCT00771758)
Timeframe: Day 10
| Intervention | percenatage of participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Very much improved | Much improved | Minimally improved | No change | Minimally worse | Much worse | Very much worse | |
| Oxycodone IR | 9.3 | 34.9 | 34.9 | 11.6 | 4.7 | 2.3 | 0 |
| Placebo | 9.5 | 23.8 | 23.8 | 28.6 | 4.8 | 0 | 4.8 |
| Tapentadol IR | 17.1 | 24.4 | 26.8 | 26.8 | 0 | 0 | 0 |
"Sleep Quality was assessed by a 4-point numeric scale (1=excellent, 2=good, 3=fair, and 4=poor). The sleep question was Please rate the overall quality of your sleep last night., which was administered via IVR system in the morning." (NCT00771758)
Timeframe: 10 days
| Intervention | participants (Number) | |||||
|---|---|---|---|---|---|---|
| Excellent - Baseline | Good - Baseline | Fair - Baseline | Poor - Baseline | Missing - Baseline | End of Study Total | |
| Baseline Total | 0 | 10 | 24 | 8 | 1 | 43 |
| Excellent - End of Study | 0 | 1 | 8 | 0 | 0 | 9 |
| Fair - End of Study | 0 | 2 | 7 | 3 | 0 | 12 |
| Good - End of Study | 0 | 6 | 6 | 1 | 0 | 13 |
| Missing - End of Study | 0 | 1 | 0 | 1 | 1 | 3 |
| Poor - End of Study | 0 | 0 | 3 | 3 | 0 | 6 |
"Sleep Quality was assessed by a 4-point numeric scale (1=excellent, 2=good, 3=fair, and 4=poor). The sleep question was Please rate the overall quality of your sleep last night., which was administered via IVR system in the morning." (NCT00771758)
Timeframe: 10 days
| Intervention | participants (Number) | |||||
|---|---|---|---|---|---|---|
| Excellent - Baseline | Good - Baseline | Fair - Baseline | Poor - Baseline | Missing - Baseline | End of Study Total | |
| Baseline Total | 0 | 5 | 9 | 7 | 0 | 21 |
| Excellent - End of Study | 0 | 2 | 1 | 1 | 0 | 4 |
| Fair - End of Study | 0 | 3 | 6 | 2 | 0 | 11 |
| Good - End of Study | 0 | 0 | 2 | 2 | 0 | 4 |
| Poor - End of Study | 0 | 0 | 0 | 2 | 0 | 2 |
"Sleep Quality was assessed by a 4-point numeric scale (1=excellent, 2=good, 3=fair, and 4=poor). The sleep question was Please rate the overall quality of your sleep last night., which was administered via Interactive Voice Response (IVR) system in the morning." (NCT00771758)
Timeframe: 10 days
| Intervention | participants (Number) | |||||
|---|---|---|---|---|---|---|
| Excellent - Baseline | Good - Baseline | Fair - Baseline | Poor - Baseline | Missing - Baseline | End of Study Total | |
| Baseline Total | 0 | 12 | 19 | 10 | 0 | 41 |
| Excellent - End of Study | 0 | 5 | 2 | 5 | 0 | 12 |
| Fair - End of Study | 0 | 2 | 8 | 3 | 0 | 13 |
| Good - End of Study | 0 | 4 | 8 | 0 | 0 | 12 |
| Missing - End of Study | 0 | 1 | 0 | 1 | 0 | 2 |
| Poor - End of Study | 0 | 0 | 1 | 1 | 0 | 2 |
"The Clinician Ease-of-Care was defined on a 6-point scale, where 0 = not at all to 5=a very great deal." (NCT00771758)
Timeframe: Day 10
| Intervention | percent of participants (Number) | |||||
|---|---|---|---|---|---|---|
| Not at all | A little bit | Somewhat | Quite a bit | A great deal | A very great deal | |
| Oxycodone IR | 53.5 | 18.6 | 9.3 | 14.0 | 2.3 | 0 |
| Placebo | 76.2 | 9.5 | 4.8 | 4.8 | 4.8 | 0 |
| Tapentadol IR | 56.1 | 17.1 | 14.6 | 7.3 | 2.4 | 0 |
"The Clinician Ease-of-Care was defined on a 6-point scale, where 0 = not at all to 5=a very great deal." (NCT00771758)
Timeframe: Day 10
| Intervention | percent of participants (Number) | |||||
|---|---|---|---|---|---|---|
| Not at all | A little bit | Somewhat | Quite a bit | A great deal | A very great deal | |
| Oxycodone IR | 51.2 | 16.3 | 16.3 | 9.3 | 4.7 | 0 |
| Placebo | 47.6 | 23.8 | 19.0 | 4.8 | 4.8 | 0 |
| Tapentadol IR | 51.2 | 19.5 | 12.2 | 12.2 | 2.4 | 0 |
Pain Relief was defined as a 5-point categorical scale of 0-4 (0=none, 1=A little, 2=Some, 3=A lot, 4=Complete). Total Pain Relief (TOTPAR) was calculated as the time-weighted sum over all pain relief up to Day 10, 8 AM. The range of TOTPAR over 10 days is from 0 to 864. A higher value in TOTPAR indicated greater pain relief. (NCT00771758)
Timeframe: 10 Days (216 Hours)
| Intervention | Scores on a scale (Mean) |
|---|---|
| Tapentadol IR | 378.8 |
| Oxycodone IR | 414.4 |
| Placebo | 391.7 |
The 30% responder rate was defined as the proportion of participants with a value of percentage change greater than or equal to the 30% from baseline in pain intensity at Day 10 (average of Day 9 PM and Day 10 AM). (NCT00771758)
Timeframe: Day 10
| Intervention | percentage of participants (Number) |
|---|---|
| Tapentadol IR | 52.8 |
| Oxycodone IR | 39.0 |
| Placebo | 55.0 |
Treatment satisfaction was measured using a 7-point scale where 1 = very satisfied and 7 = very dissatisfied. (NCT00771758)
Timeframe: Day 5
| Intervention | Scores on a scale (Mean) |
|---|---|
| Tapentadol IR | 3.5 |
| Oxycodone IR | 2.6 |
| Placebo | 3.7 |
The number of SBM over the 14-day IR treatment phase was determined from the Bowel Function Patient Diary and factored to enable a per week value to be used. An SBM is defined as any BM that has occurred without the use of a laxative, enema, suppository, or manual manipulation within the previous 24 hours. (NCT00784277)
Timeframe: Week 1 to Week 2
| Intervention | number of stools/week (Mean) |
|---|---|
| Placebo | 9.9 |
| Tapentadol 50 mg | 9.0 |
| Tapentadol 75 mg | 8.6 |
| Oxycodone | 6.7 |
"SPID5 was calculated as the weighted (weights is taken as the number of hours elapsed since the previous measurement) sum of the PID collected up to 5 days. Pain intensity (PI) score is calculated as the average PI over the past 12 hours using an 11-point (0 to 10) numerical rating scale (NRS) where 0 is no pain and 10 is pain as bad as you can imagine. The difference between baseline PI at the qualifying period and current PI is pain intensity difference (PID)." (NCT00784277)
Timeframe: Day 1 to Day 5
| Intervention | Units on a scale (Mean) |
|---|---|
| Placebo | 98.6 |
| Tapentadol 50 mg | 153.1 |
| Tapentadol 75 mg | 161.8 |
| Oxycodone | 218.4 |
Pain intensity scores were measured on 11 point NRS, where 0 = no pain and 10 = severest pain imaginable. The pain intensity at Baseline was the average of scores on two consecutive morning doses (Day -1 and Day 0) and on Day 20 only a single observation was recorded. (NCT00805142)
Timeframe: Baseline (Average of Day -1 and Day 0 morning scores), Day 20
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Baseline | Day 20 | |
| Opioid-Naive Participants (Tapentadol PR) | 4.9 | 2.4 |
| Opioid-Switch Participants (Tapentadol PR) | 1.3 | 1.7 |
Percentage of participants who achieved dose adjustment included those participants whose dose was adjusted during the titration period period and entered the fixed dose maintenance period. Titration period (3-14 days) was the duration between start of treatment to the day before the initial dose in the maintenance period. Maintenance period (15-19 days) was the duration between the first dose and the final assessment in the maintenance period. (NCT00805142)
Timeframe: Day 3 up to Day 14
| Intervention | percentage of participants (Number) |
|---|---|
| Opioid-Naive Participants Titration Period (Tapentadol PR) | 93.3 |
| Opioid-Switch Participants Titration Period (Tapentadol PR) | 80.6 |
Percentage of participants with sustained pain control for 5 day fixed dose phase were the participants who completed 5 day maintenance period, whose mean Numerical Rating Scale (NRS) score during the fixed dose phase and which was assessed immediately before giving each dose was less than 4 and the number of rescue doses per day for fixed dose phase was 2 or less. Pain intensity scores were recorded 0 to 30 minutes before dose on 11 point NRS where 0 = no pain and 10 = severest pain imaginable. (NCT00805142)
Timeframe: Day 15 up to Day 19
| Intervention | percentage of participants (Number) |
|---|---|
| Opioid-Naive Participants Maintenance Period (Tapentadol PR) | 89.7 |
| Opioid-Switch Participants Maintenance Period (Tapentadol PR) | 92.9 |
The AE is an undesirable or unwanted consequence that occurred during the course of the clinical trial, but not necessarily because of study drug.The AEs included the onset of new symptoms, worsening of the frequency or severity of the symptom compared with Baseline, and abnormal findings including abnormal laboratory test values in the diagnostic examination. The participants who discontinued because of lack of efficacy were those in which satisfactory analgesia was not maintained. (NCT00805142)
Timeframe: Baseline up to 7 days after last dose of study treatment
| Intervention | participants (Number) | |
|---|---|---|
| AEs | Lack of efficacy | |
| Opioid-Naive Participants (Tapentadol PR) | 2 | 0 |
| Opioid-Switch Participants (Tapentadol PR) | 3 | 1 |
Pain VAS assesses the pain intensity experienced by the participant on a 100 millimeter (mm) VAS, where responses range from a response of no pain (score of 0 mm) to severest pain imaginable (score of 100 mm). The participant indicated the pain by marking the applicable place with slash (/) and the investigator then measured the length from left edge to the slash. (NCT00805142)
Timeframe: Baseline and Day 19
| Intervention | mm (Mean) | |
|---|---|---|
| Baseline | Day 19 | |
| Opioid-Naive Participants (Tapentadol PR) | 44.34 | 20.33 |
| Opioid-Switch Participants (Tapentadol PR) | 10.71 | 10.30 |
PGI-C is a participant rated instrument to measure participant's change in overall status of general condition including pain on a 7-point scale; range from 1 (very much improved) to 7 (very much worse). (NCT00805142)
Timeframe: Day 19
| Intervention | participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Very much improved | Improved | Minimally improved | No change | Minimally worse | Worse | Very much worse | |
| Opioid-Naive Participants Maintenance Period (Tapentadol PR) | 1 | 13 | 10 | 5 | 0 | 0 | 0 |
| Opioid-Switch Participants Maintenance Period (Tapentadol PR) | 0 | 1 | 6 | 15 | 6 | 0 | 0 |
The immediate release (IR) oral opioids were used as rescue doses in the participants with lack of efficacy or to have relief from severe pain. In case of opioid-switching participants rescue doses were continued without any change in the preceding doses or the type throughout the study. The IR morphine HCl was used as the rescue dose for opioid-naive participants. The upper limit of rescue doses was specified for each daily dose of tapentadol PR. There was no change in the dose of rescue medication during maintenance period for opioid-naive participants. (NCT00805142)
Timeframe: Day 12, 13, 14, 15, 16, 17, 18 and 19
| Intervention | mg per day (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Day 12 | Day 13 | Day 14 | Day 15 | Day 16 | Day 17 | Day 18 | Day 19 | |
| Opioid-Naive Participants (Tapentadol PR) | 0.34 | 0.52 | 1.03 | 1.21 | 1.72 | 1.72 | 0.86 | 1.03 |
| Opioid-Switch Participants (Tapentadol PR) | 1.07 | 1.16 | 1.61 | 2.05 | 1.21 | 1.56 | 2.32 | 1.96 |
The sleep questionnaire is a 4-item questionnaire evaluating the condition of the sleep of the participant on the previous night . Participants were asked to provide the number of times they awoke at night. (NCT00805142)
Timeframe: Pre-dose (Day 1) and Day 20
| Intervention | awakenings (Mean) | |
|---|---|---|
| Pre-dose (Day 1) | Day 20 | |
| Opioid-Naive Participants (Tapentadol PR) | 2.40 | 2.20 |
| Opioid-Switch Participants (Tapentadol PR) | 3.40 | 3.80 |
The sleep questionnaire is a 4-item questionnaire evaluating the condition of the sleep of the participant on the previous night. Participants rated overall sleep quality on a scale ranging from excellent to very poor. (NCT00805142)
Timeframe: Pre-dose (Day 1) and Day 20
| Intervention | participants (Number) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Excellent: Pre-dose (Day 1) | Excellent: Day 20 | Good: Pre-dose (Day 1) | Good: Day 20 | Fair: Pre-dose (Day 1) | Fair: Day 20 | Poor: Pre-dose (Day 1) | Poor: Day 20 | Very Poor: Pre-dose (Day 1) | Very Poor: Day 20 | |
| Opioid-Naive Participants (Tapentadol PR) | 1 | 4 | 16 | 17 | 0 | 8 | 10 | 0 | 2 | 0 |
| Opioid-Switch Participants (Tapentadol PR) | 0 | 2 | 20 | 18 | 0 | 6 | 6 | 2 | 2 | 0 |
The sleep questionnaire is a 4-item questionnaire evaluating the condition of the sleep of the participant on the previous night. The participants were asked about the time taken by them to fall asleep previous night after bedtime and the total time they slept during previous night. (NCT00805142)
Timeframe: Pre-dose (Day 1) and Day 20
| Intervention | minutes (Mean) | |||
|---|---|---|---|---|
| Time to sleep: Pre-dose (Day 1) | Time to sleep: Day 20 | Total time slept: Pre-dose (Day 1) | Total time slept: Day 20 | |
| Opioid-Naive Participants (Tapentadol PR) | 47.10 | 43.10 | 371.70 | 418.40 |
| Opioid-Switch Participants Maintenance Period (Tapentadol PR) | 63.80 | 56.60 | 390.50 | 373.00 |
Treatment satisfaction was measured using a 7-point scale where 1 = very satisfied and 7 = very dissatisfied (NCT00814580)
Timeframe: 7 Days
| Intervention | percentage of participants (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| Very satisfied | Somewhat satisfied | Slightly satisfied | Neither satisfied nor dissatisfied | Slightly dissatisfied | Somewhat dissatisfied | Very dissatisfied | Missing | |
| Oxycodone IR | 48.1 | 20.4 | 5.5 | 5.0 | 3.3 | 1.7 | 14.4 | 1.7 |
| Tapentadol IR | 58.3 | 15.6 | 2.6 | 7.3 | 3.6 | 2.1 | 9.9 | 0.5 |
The 30% responder rate was defined as the proportion of participants with a value of percentage change greater than or equal to the 30% from baseline in pain intensity at Day 3 (average of Day 3 PM and Day 4 AM). If a subject has only the Day 3 PM value or Day 4 AM value, then response rate will be based on the non-missing value. If a subject withdraws or uses rescue medication before Day 3 PM then Baseline Observation Carried Forward (BOCF) will be imputed. Last Observation Carried Forward (LOCF) may be used if no value afterward. (NCT00814580)
Timeframe: Day 3
| Intervention | percentage of participants (Number) |
|---|---|
| Tapentadol IR | 33.5 |
| Oxycodone IR | 34.4 |
Pain Relief was defined as a 5-point categorical scale of 0-4 (0=none, 1=A little, 2=Some, 3=A lot, 4=Complete). Total Pain Relief (TOTPAR) was calculated as the time-weighted sum over all pain relief up to Day 7, 8 AM. The range of TOTPAR over 7 days is from 0 to 576. A higher value in TOTPAR indicated greater pain relief. (NCT00814580)
Timeframe: 7 Days
| Intervention | Scores on a scale (Mean) |
|---|---|
| Tapentadol IR | 299.1 |
| Oxycodone IR | 272.9 |
The 50% responder rate was defined as the proportion of participants with a value of percentage change greater than or equal to the 50% from baseline in pain intensity at Day 7 (average of Day 6 PM and Day 7 AM). If a subject has only the Day 6 PM value or Day 7 AM value, then response rate will be based on the non-missing value. If a subject withdraws or uses rescue medication before Day 6 PM then BOCF will be imputed. LOCF may be used if no value afterward. (NCT00814580)
Timeframe: Day 7
| Intervention | percentage of participants (Number) |
|---|---|
| Tapentadol IR | 35.4 |
| Oxycodone IR | 29.2 |
Pain Relief was defined as a 5-point categorical scale of 0-4 (0=none, 1=A little, 2=Some, 3=A lot, 4=Complete). Total Pain Relief (TOTPAR) was calculated as the time-weighted sum over all pain relief up to hour 48. The range of TOTPAR over 2 days is from 0 to 192. A higher value in TOTPAR indicated greater pain relief. (NCT00814580)
Timeframe: 2 Days (48 hours)
| Intervention | Scores on a scale (Mean) |
|---|---|
| Tapentadol IR | 97.7 |
| Oxycodone IR | 92.0 |
The Sum of Total Pain Relief and Sum of Pain Intensity Difference (SPRID) was derived from Sum of TOTPAR and SPID. The range of SPRID over 7 days is from -1440 to 2016. A higher value in SPRID indicated greater pain relief. (NCT00814580)
Timeframe: 7 Days
| Intervention | Scores on a scale (Mean) |
|---|---|
| Tapentadol IR | 435.2 |
| Oxycodone IR | 395.0 |
The Sum of Total Pain Relief and Sum of Pain Intensity Difference (SPRID) was derived from Sum of TOTPAR and SPID. The range of SPRID over 3 days is from -720 to 1008. A higher value in SPRID indicated greater pain relief. (NCT00814580)
Timeframe: 3 Days (72hours)
| Intervention | Scores on a scale (Mean) |
|---|---|
| Tapentadol IR | 186.1 |
| Oxycodone IR | 181.4 |
The Sum of Total Pain Relief and Sum of Pain Intensity Difference (SPRID) was derived from Sum of TOTPAR and SPID. The range of SPRID over 2 days is from -480 to 672. A higher value in SPRID indicated greater pain relief. (NCT00814580)
Timeframe: 2 Days (48 hours)
| Intervention | Scores on a scale (Mean) |
|---|---|
| Tapentadol IR | 108.2 |
| Oxycodone IR | 106.6 |
Pain Intensity (PI) was assessed on 11-point numerical rating scale from 0=no pain to 10=pain as bad as you can imagine. Pain Intensity Difference (PID) was the difference between baseline PI (prior to the first dose) and current PI at assessment. SPID over 7 Days was calculated as the time-weighted Sum of PID scores up to Day 7, 8 AM. The range is from -1440 to 1440. The higher value in SPID indicates greater pain relief. (NCT00814580)
Timeframe: 7 Days
| Intervention | Scores on a scale (Mean) |
|---|---|
| Tapentadol IR | 136.1 |
| Oxycodone IR | 122.1 |
Pain Relief was defined as a 5-point categorical scale of 0-4 (0=none, 1=A little, 2=Some, 3=A lot, 4=Complete). Total Pain Relief (TOTPAR) was calculated as the time-weighted sum over all pain relief up to hour 72. The range of TOTPAR over 3 days is from 0 to 288. A higher value in TOTPAR indicated greater pain relief. (NCT00814580)
Timeframe: 3 Days (72hours)
| Intervention | Scores on a scale (Mean) |
|---|---|
| Tapentadol IR | 151.3 |
| Oxycodone IR | 140.9 |
Pain Intensity (PI) was assessed on 11-point numerical rating scale from 0=no pain to 10=pain as bad as you can imagine. Pain Intensity Difference (PID) was the difference between baseline PI (prior to the first dose) and current PI at assessment. SPID72 was calculated as the time-weighted Sum of PID scores over 72 hours. The range of SPID72 is from -720 to 720. The higher value in SPID indicates greater pain relief. (NCT00814580)
Timeframe: 3 Days (72 hours)
| Intervention | Scores on a scale (Mean) |
|---|---|
| Tapentadol IR | 34.8 |
| Oxycodone IR | 40.5 |
"Over the past 7 days patients reported trouble falling asleep by using a 4-category scale (not at all, 1 to 2 days, 3 to 5 days, 6 to 7 days) at baseline and the final study visit (Day 7)." (NCT00814580)
Timeframe: Baseline and 7 Days
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| Baseline: Not at all | Baseline: 1-2 Days | Baseline: 3-5 Days | Baseline: 6-7 Days | Baseline: Miss the measurement | |
| Baseline - Total | 104 | 40 | 26 | 21 | 1 |
| End of Study: 1-2 Days | 34 | 12 | 6 | 4 | 0 |
| End of Study: 3-5 Days | 20 | 7 | 4 | 4 | 0 |
| End of Study: 6-7 Days | 16 | 5 | 6 | 8 | 0 |
| End of Study: Missing the Measurement | 0 | 1 | 2 | 0 | 0 |
| End of Study: Not at All | 34 | 15 | 8 | 5 | 1 |
"Over the past 7 days patients reported Trouble staying asleep by using a 4-category scale (not at all, 1 to 2 days, 3 to 5 days, 6 to 7 days) at baseline and the final study visit (Day 7)." (NCT00814580)
Timeframe: Baseline and 7 Days
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| Baseline: Not at all | Baseline: 1-2 Days | Baseline: 3-5 Days | Baseline: 6-7 Days | Baseline: Miss the measurement | |
| Baseline - Total | 77 | 42 | 29 | 30 | 3 |
| End of Study: 1-2 Days | 17 | 13 | 6 | 3 | 1 |
| End of Study: 3-5 Days | 12 | 8 | 7 | 7 | 0 |
| End of Study: 6-7 Days | 20 | 13 | 9 | 14 | 1 |
| End of Study: Missing the Measurement | 2 | 0 | 2 | 0 | 0 |
| End of Study: Not at All | 26 | 8 | 5 | 6 | 1 |
"Over the past 7 days patients reported Trouble staying asleep by using a 4-category scale (not at all, 1 to 2 days, 3 to 5 days, 6 to 7 days) at baseline and the final study visit (Day 7)." (NCT00814580)
Timeframe: Baseline and 7 Days
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| Baseline: Not at all | Baseline: 1-2 Days | Baseline: 3-5 Days | Baseline: 6-7 Days | Baseline: Miss the measurement | |
| Baseline - Total | 81 | 41 | 31 | 38 | 1 |
| End of Study: 1-2 Days | 24 | 13 | 3 | 7 | 0 |
| End of Study: 3-5 Days | 17 | 7 | 13 | 8 | 0 |
| End of Study: 6-7 Days | 13 | 8 | 9 | 17 | 0 |
| End of Study: Missing the Measurement | 0 | 1 | 1 | 1 | 0 |
| End of Study: Not at All | 27 | 12 | 5 | 5 | 1 |
"Over the past 7 days patients reported Wake up feeling tired and worn out by using a 4-category scale (not at all, 1 to 2 days, 3 to 5 days, 6 to 7 days) at baseline and the final study visit (Day 7)." (NCT00814580)
Timeframe: Baseline and 7 Days
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| Baseline: Not at all | Baseline: 1-2 Days | Baseline: 3-5 Days | Baseline: 6-7 Days | Baseline: Miss the measurement | |
| Baseline - Total | 82 | 48 | 24 | 25 | 2 |
| End of Study: 1-2 Days | 23 | 12 | 8 | 3 | 0 |
| End of Study: 3-5 Days | 20 | 13 | 6 | 5 | 0 |
| End of Study: 6-7 Days | 8 | 9 | 6 | 13 | 0 |
| End of Study: Missing the Measurement | 3 | 0 | 1 | 0 | 0 |
| End of Study: Not at All | 28 | 14 | 3 | 4 | 2 |
"Over the past 7 days patients reported Wake up feeling tired and worn out by using a 4-category scale (not at all, 1 to 2 days, 3 to 5 days, 6 to 7 days) at baseline and the final study visit (Day 7)." (NCT00814580)
Timeframe: Baseline and 7 Days
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| Baseline: Not at all | Baseline: 1-2 Days | Baseline: 3-5 Days | Baseline: 6-7 Days | Baseline: Miss the measurement | |
| Baseline - Total | 71 | 49 | 36 | 35 | 1 |
| End of Study: 1-2 Days | 19 | 16 | 10 | 6 | 0 |
| End of Study: 3-5 Days | 8 | 17 | 14 | 8 | 0 |
| End of Study: 6-7 Days | 9 | 6 | 8 | 15 | 0 |
| End of Study: Missing the Measurement | 0 | 2 | 0 | 1 | 0 |
| End of Study: Not at All | 35 | 8 | 4 | 5 | 1 |
"Over the past 7 days patients reported Wake up several times during night by using a 4-category scale (not at all, 1 to 2 days, 3 to 5 days, 6 to 7 days) at baseline and the final study visit (Day 7)." (NCT00814580)
Timeframe: Baseline and 7 Days
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| Baseline: Not at all | Baseline: 1-2 Days | Baseline: 3-5 Days | Baseline: 6-7 Days | Baseline: Miss the measurement | |
| Baseline - Total | 44 | 46 | 36 | 53 | 2 |
| End of Study: 1-2 Days | 14 | 7 | 11 | 3 | 1 |
| End of Study: 3-5 Days | 6 | 11 | 10 | 18 | 0 |
| End of Study: 6-7 Days | 14 | 23 | 12 | 29 | 1 |
| End of Study: Missing the Measurement | 2 | 0 | 1 | 1 | 0 |
| End of Study: Not at All | 8 | 5 | 2 | 2 | 0 |
"Over the past 7 days patients reported Wake up several times during night by using a 4-category scale (not at all, 1 to 2 days, 3 to 5 days, 6 to 7 days) at baseline and the final study visit (Day 7)." (NCT00814580)
Timeframe: Baseline and 7 Days
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| Baseline: Not at all | Baseline: 1-2 Days | Baseline: 3-5 Days | Baseline: 6-7 Days | Baseline: Miss the measurement | |
| Baseline - Total | 42 | 35 | 53 | 61 | 1 |
| End of Study: 1-2 Days | 12 | 12 | 17 | 7 | 0 |
| End of Study: 3-5 Days | 8 | 8 | 12 | 14 | 0 |
| End of Study: 6-7 Days | 12 | 13 | 21 | 33 | 0 |
| End of Study: Missing the Measurement | 1 | 0 | 0 | 2 | 0 |
| End of Study: Not at All | 9 | 2 | 3 | 5 | 1 |
Pain Intensity (PI) was assessed on 11-point numerical rating scale from 0=no pain to 10=pain as bad as you can imagine. Pain Intensity Difference (PID) was the difference between baseline PI (prior to the first dose) and current PI at assessment. SPID48 was calculated as the time-weighted Sum of PID scores over 48 hours. The range of SPID48 is from -480 to 480. The higher value in SPID indicates greater pain relief. (NCT00814580)
Timeframe: 2 Days (48 hours)
| Intervention | Scores on a scale (Mean) |
|---|---|
| Tapentadol IR | 10.6 |
| Oxycodone IR | 14.6 |
Information associated with contacts with a healthcare professional was collected by the investigator and study staff for all subjects throughout the study. (NCT00814580)
Timeframe: 7 Days
| Intervention | Number of calls (Number) | |||||
|---|---|---|---|---|---|---|
| Total number of subjects who made calls | Number of adverse event related calls | Number of pain-related calls | Number of non-medical/administrative calls | Number of other medical conditions calls | Total number of calls | |
| Oxycodone IR | 74 | 28 | 70 | 19 | 7 | 122 |
| Tapentadol IR | 69 | 39 | 46 | 16 | 10 | 105 |
Information associated with contacts with a healthcare professional was collected by the investigator and study staff for all subjects throughout the study. (NCT00814580)
Timeframe: 7 Days
| Intervention | Number of participants (Number) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Patients visited a healthcare professional | Number of patient with scheduled visits | Number of patient with unscheduled visits | Number of patient with Internist | Number of patient with Orthopedic surgeon | Number of patient with Physical therapist | Number of patient with Primary care physician | Patient with other healthcare professional | Number of patient with emergency room visit | Number of patient with hospital admissions | |
| Oxycodone IR | 89 | 85 | 6 | 1 | 87 | 0 | 1 | 1 | 6 | 2 |
| Tapentadol IR | 87 | 84 | 7 | 2 | 80 | 3 | 5 | 2 | 6 | 0 |
"Over the past 7 days patients reported Pain interferes with sleep by using a 4-category scale (not at all, 1 to 2 days, 3 to 5 days, 6 to 7 days) at baseline and the final study visit (Day 7)." (NCT00814580)
Timeframe: Baseline and 7 Days
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| Baseline: Not at all | Baseline: 1-2 Days | Baseline: 3-5 Days | Baseline: 6-7 Days | Baseline: Miss the measurement | |
| Baseline - Total | 56 | 46 | 38 | 51 | 1 |
| End of Study: 1-2 Days | 17 | 17 | 15 | 10 | 0 |
| End of Study: 3-5 Days | 13 | 9 | 10 | 14 | 0 |
| End of Study: 6-7 Days | 2 | 5 | 7 | 20 | 0 |
| End of Study: Missing the Measurement | 1 | 2 | 0 | 0 | 0 |
| End of Study: Not at All | 23 | 13 | 6 | 7 | 1 |
"Over the past 7 days patients reported Pain interferes with sleep by using a 4-category scale (not at all, 1 to 2 days, 3 to 5 days, 6 to 7 days) at baseline and the final study visit (Day 7)." (NCT00814580)
Timeframe: Baseline and 7 Days
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| Baseline: Not at all | Baseline: 1-2 Days | Baseline: 3-5 Days | Baseline: 6-7 Days | Baseline: Miss the measurement | |
| Baseline - Total | 57 | 37 | 31 | 54 | 2 |
| End of Study: 1-2 Days | 15 | 11 | 16 | 8 | 2 |
| End of Study: 3-5 Days | 15 | 15 | 6 | 14 | 0 |
| End of Study: 6-7 Days | 9 | 6 | 5 | 28 | 0 |
| End of Study: Missing the Measurement | 2 | 1 | 1 | 0 | 0 |
| End of Study: Not at All | 16 | 4 | 3 | 4 | 0 |
"Over the past 7 days patients reported Feeling well rested by using a 4-category scale (not at all, 1 to 2 days, 3 to 5 days, 6 to 7 days) at baseline and the final study visit (Day 7)." (NCT00814580)
Timeframe: Baseline and 7 Days
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| Baseline: Not at all | Baseline: 1-2 Days | Baseline: 3-5 Days | Baseline: 6-7 Days | Baseline: Miss the measurement | |
| Baseline - Total | 39 | 34 | 55 | 63 | 1 |
| End of Study: 1-2 Days | 7 | 9 | 13 | 6 | 0 |
| End of Study: 3-5 Days | 9 | 9 | 20 | 21 | 0 |
| End of Study: 6-7 Days | 11 | 7 | 14 | 26 | 1 |
| End of Study: Missing the Measurement | 1 | 0 | 1 | 1 | 0 |
| End of Study: Not at All | 11 | 9 | 7 | 9 | 0 |
"Over the past 7 days patients reported Feeling well rested by using a 4-category scale (not at all, 1 to 2 days, 3 to 5 days, 6 to 7 days) at baseline and the final study visit (Day 7)." (NCT00814580)
Timeframe: Baseline and 7 Days
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| Baseline: Not at all | Baseline: 1-2 Days | Baseline: 3-5 Days | Baseline: 6-7 Days | Baseline: Miss the measurement | |
| Baseline - Total | 27 | 32 | 50 | 70 | 2 |
| End of Study: 1-2 Days | 6 | 11 | 14 | 13 | 0 |
| End of Study: 3-5 Days | 4 | 11 | 14 | 15 | 1 |
| End of Study: 6-7 Days | 6 | 5 | 13 | 29 | 1 |
| End of Study: Missing the Measurement | 1 | 1 | 0 | 2 | 0 |
| End of Study: Not at All | 10 | 4 | 9 | 11 | 0 |
"Over the past 7 days patients reported Feeling alert during daytime hours by using a 4-category scale (not at all, 1 to 2 days, 3 to 5 days, 6 to 7 days) at baseline and the final study visit (Day 7)." (NCT00814580)
Timeframe: Baseline and 7 Days
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| Baseline: Not at all | Baseline: 1-2 Days | Baseline: 3-5 Days | Baseline: 6-7 Days | Baseline: Miss the measurement | |
| Baseline - Total | 23 | 24 | 41 | 103 | 1 |
| End of Study: 1-2 Days | 6 | 6 | 10 | 19 | 0 |
| End of Study: 3-5 Days | 3 | 8 | 14 | 38 | 0 |
| End of Study: 6-7 Days | 11 | 9 | 10 | 38 | 1 |
| End of Study: Missing the Measurement | 0 | 0 | 0 | 3 | 0 |
| End of Study: Not at All | 3 | 1 | 7 | 5 | 0 |
"Over the past 7 days patients reported Feeling alert during daytime hours by using a 4-category scale (not at all, 1 to 2 days, 3 to 5 days, 6 to 7 days) at baseline and the final study visit (Day 7)." (NCT00814580)
Timeframe: Baseline and 7 Days
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| Baseline: Not at all | Baseline: 1-2 Days | Baseline: 3-5 Days | Baseline: 6-7 Days | Baseline: Miss the measurement | |
| Baseline - Total | 25 | 20 | 34 | 100 | 2 |
| End of Study: 1-2 Days | 3 | 5 | 6 | 17 | 0 |
| End of Study: 3-5 Days | 4 | 9 | 13 | 25 | 0 |
| End of Study: 6-7 Days | 12 | 3 | 12 | 42 | 2 |
| End of Study: Missing the Measurement | 1 | 1 | 0 | 2 | 0 |
| End of Study: Not at All | 5 | 2 | 3 | 14 | 0 |
Patient Global Impression of Change (PGIC) was defined as the 7-point numeric scale, where 1=very much improved to 7=very much worse. (NCT00814580)
Timeframe: 7 Days
| Intervention | percentage of participants (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| Very much improved | Much improved | Minimally improved | No change | Minimally worse | Much worse | Very much worse | Missing | |
| Oxycodone IR | 26.0 | 42.5 | 13.3 | 7.7 | 2.2 | 0.6 | 5.5 | 2.2 |
| Tapentadol IR | 27.6 | 46.9 | 15.6 | 3.1 | 2.1 | 1.6 | 1.0 | 2.1 |
Clinician Global Impression of Change (CGIC) was defined as the 7-point numeric scale, where 1=very much improved to 7=very much worse. (NCT00814580)
Timeframe: 7 Days
| Intervention | percentage of participants (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| Very much improved | Much improved | Minimally improved | No change | Minimally worse | Much worse | Very much worse | Missing | |
| Oxycodone IR | 29.3 | 39.8 | 12.7 | 7.2 | 2.2 | 1.1 | 5.0 | 2.8 |
| Tapentadol IR | 33.3 | 47.4 | 11.5 | 3.6 | 1.0 | 1.0 | 1.0 | 1.0 |
From date of first administration of study medication to time to achieve adequate 50% reduction in pain intensity from baseline score. Censored observations included subjects who completed or discontinued from the study without a 50% reduction in pain intensity from baseline score. If a subject discontinued due to lack of efficacy (including rescue medication), the subject was censored on Day 7, 12 PM. (NCT00814580)
Timeframe: 7 Days
| Intervention | Hours (Median) |
|---|---|
| Tapentadol IR | 125.3 |
| Oxycodone IR | NA |
From date of first administration of study medication to time to achieve adequate 30% reduction in pain intensity from baseline score. Censored observations included subjects who completed or discontinued from the study without a 30% reduction in pain intensity from baseline score. If a subject discontinued due to lack of efficacy (including rescue medication), the subject was censored on Day 7, 12 PM. (NCT00814580)
Timeframe: 7 Days
| Intervention | Hours (Median) |
|---|---|
| Tapentadol IR | 73.9 |
| Oxycodone IR | 66.4 |
"Over the past 7 days patients reported trouble falling asleep by using a 4-category scale (not at all, 1 to 2 days, 3 to 5 days, 6 to 7 days) at baseline and the final study visit (Day 7)." (NCT00814580)
Timeframe: Baseline and 7 Days
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| Baseline: Not at all | Baseline: 1-2 Days | Baseline: 3-5 Days | Baseline: 6-7 Days | Baseline: Miss the measurement | |
| Baseline - Total | 105 | 34 | 24 | 16 | 2 |
| End of Study: 1-2 Days | 23 | 12 | 8 | 2 | 0 |
| End of Study: 3-5 Days | 21 | 4 | 3 | 5 | 0 |
| End of Study: 6-7 Days | 14 | 7 | 5 | 6 | 0 |
| End of Study: Missing the Measurement | 3 | 0 | 1 | 0 | 0 |
| End of Study: Not at All | 44 | 11 | 7 | 3 | 2 |
The 50% responder rate was defined as the proportion of participants with a value of percentage change greater than or equal to the 50% from baseline in pain intensity at Day 3 (average of Day 3 PM and Day 4 AM). If a subject has only the Day 3 PM value or Day 4 AM value, then response rate will be based on the non-missing value. If a subject withdraws or uses rescue medication before Day 3 PM then BOCF will be imputed. LOCF may be used if no value afterward. (NCT00814580)
Timeframe: Day 3
| Intervention | percentage of participants (Number) |
|---|---|
| Tapentadol IR | 19.0 |
| Oxycodone IR | 22.7 |
The 30% responder rate was defined as the proportion of participants with a value of percentage change greater than or equal to the 30% from baseline in pain intensity at Day 7 (average of Day 6 PM and Day 7 AM). If a subject has only the Day 6 PM value or Day 7 AM value, then response rate will be based on the non-missing value. If a subject withdraws or uses rescue medication before Day 6 PM then BOCF will be imputed. LOCF may be used if no value afterward. (NCT00814580)
Timeframe: Day 7
| Intervention | percentage of participants (Number) |
|---|---|
| Tapentadol IR | 48.1 |
| Oxycodone IR | 42.2 |
In the Patient Global Impression of Change (PGIC) the participant indicates the perceived change over the treatment period. The participant is requested to choose one of seven categories. Scores range from very much improved to very much worse. (NCT00982280)
Timeframe: Baseline; End of Week 12 (12 Weeks)
| Intervention | participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Very much improved | Much improved | Minimally improved | No change | Minimally worse | Much worse | Very much worse | |
| Tapentadol PR | 3 | 17 | 11 | 1 | 0 | 0 | 0 |
Participants were requested to rate their previous analgesic medication on a 5-point scale. Previous medication was rated as excellent, very good, good, fair and poor. (NCT00982280)
Timeframe: Baseline
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| Excellent | Very Good | Good | Fair | Poor | |
| Tapentadol PR | 0 | 0 | 1 | 46 | 15 |
Participants were requested to rate their tapentadol (new) analgesic medication on a 5-point scale. The medication was rated as excellent, very good, good, fair and poor. (NCT00982280)
Timeframe: After 6 weeks
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| Excellent | Very Good | Good | Fair | Poor | |
| Tapentadol PR | 3 | 27 | 21 | 4 | 0 |
Participants were requested to rate their tapentadol (new) analgesic medication on a 5-point scale. The medication was rated as excellent, very good, good, fair and poor. (NCT00982280)
Timeframe: After 12 weeks
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| Excellent | Very Good | Good | Fair | Poor | |
| Tapentadol PR | 3 | 16 | 12 | 1 | 0 |
In the Clinical Global Impression of Change (CGIC) the clinician indicates the perceived change over the treatment period. The clinician is requested to choose one of seven categories. Scores range from very much improved to very much worse. (NCT00982280)
Timeframe: Baseline; End of Week 6 (6 Weeks)
| Intervention | participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Very much improved | Much improved | Minimally improved | No change | Minimally worse | Much worse | Very much worse | |
| Tapentadol PR | 6 | 28 | 18 | 1 | 2 | 0 | 0 |
In the Clinical Global Impression of Change (CGIC) the clinician indicates the perceived change over the treatment period. The clinician is requested to choose one of seven categories. Scores range from very much improved to very much worse. (NCT00982280)
Timeframe: Baseline; End of Week 12 (12 Weeks)
| Intervention | participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Very much improved | Much improved | Minimally improved | No change | Minimally worse | Much worse | Very much worse | |
| Tapentadol PR | 3 | 17 | 11 | 1 | 0 | 0 | 0 |
Participants were considered responders if they reported the same or less average pain intensity over a 3 day period after 6 weeks of tapentadol PR treatment as with their previous analgesic treatment. (NCT00982280)
Timeframe: 6 weeks
| Intervention | Participants (Number) |
|---|---|
| Tapentadol PR | 50 |
Tapentadol was compared to Oxycodone with Oxycodone set to 1. The average total daily dose of Tapentadol at which a pain score equivalent or below to the pain score at the end of observation period under Oxycodone was reached was documented as the equipotent or equianalgesic dose to the total daily dose of the previously used Oxycodone. (NCT00982280)
Timeframe: Baseline; End of Week 6 (6 Weeks)
| Intervention | Ratio (Number) |
|---|---|
| Tapentadol | 4.6 |
EuroQoL-5D Health State Visual Analog Scale (VAS) is a participant rated questionnaire to assess health-related quality of life in terms of a single index value. The VAS component rates current health state on a scale from 0 (worst imaginable health state) to 100 (best imaginable health state); higher scores indicate a better health state. The values indicated represent the change from the baseline, a positive value indicates an improvement. (NCT00982280)
Timeframe: 6 Weeks
| Intervention | Units on a scale (Mean) |
|---|---|
| Tapentadol PR | 29.6 |
Tapentadol was compared to Transdermal Buprenorphine with Buprenorphine set to 1. The average total daily dose of Tapentadol at which a pain score equivalent or below to the pain score at the end of observation period under Transdermal Buprenorphine was reached was documented as the equipotent or equianalgesic dose to the total daily dose of the previously used Transdermal Buprenorphine. (NCT00982280)
Timeframe: Baseline; End of Week 6 (6 Weeks)
| Intervention | Ratio (Number) |
|---|---|
| Tapentadol | 281.1 |
"The participant scored the EuroQol-5. This is a five dimensional health state classification. Each dimension is assessed on a 3-point ordinal scale (1=no problems, 2=some problems, 3=extreme problems). The responses to the five EQ-5D dimensions were scored using a utility-weighted algorithm to derive an EQ-5D health status index score between 0 to 1, with 1.00 indicating full health and 0 representing dead. The positive values indicate that during the study the health status improved." (NCT00982280)
Timeframe: 6 weeks
| Intervention | Units on a scale (Median) |
|---|---|
| Tapentadol PR | 0.201 |
"The participant scored the EuroQol-5. This is a five dimensional health state classification. Each dimension is assessed on a 3-point ordinal scale (1=no problems, 2=some problems, 3=extreme problems). The responses to the five EQ-5D dimensions were scored using a utility-weighted algorithm to derive an EQ-5D health status index score between 0 to 1, with 1.00 indicating full health and 0 representing dead. The positive values indicate that during the study the health status improved." (NCT00982280)
Timeframe: 12 weeks
| Intervention | Units on a scale (Median) |
|---|---|
| Tapentadol PR | 0.155 |
EuroQoL-5D Health State Visual Analog Scale (VAS) is a participant rated questionnaire to assess health-related quality of life in terms of a single index value. The VAS component rates current health state on a scale from 0 (worst imaginable health state) to 100 (best imaginable health state); higher scores indicate a better health state. The values indicated represent the change from the baseline, a positive value indicates an improvement. (NCT00982280)
Timeframe: 12 Weeks
| Intervention | Units on a scale (Mean) |
|---|---|
| Tapentadol PR | 34.6 |
"For this pain assessment, the participant was to indicate the level of average pain experienced over the previous 3 days on an 11-point Numerical Rating Scale(NRS) where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine. The value indicates the change from the baseline value on the 0 to 10 scale. A Negative value indicates a reduction in pain intensity from the baseline average pain intensity." (NCT00982280)
Timeframe: Baseline; Week 6 (6 weeks)
| Intervention | Units on a scale (Mean) |
|---|---|
| Tapentadol PR | -2.2 |
The WOMAC is a self-administered questionnaire and has 24 questions: Pain, Stiffness and Physical Function. The possible scores range from 0-20 for pain, 0-8 for stiffness, 0-68 for physical function and these are then summed 0-96 for the global score. The negative value indicates that there has been an improvement since baseline, the higher the value the greater the change since baseline. (NCT00982280)
Timeframe: 6 weeks
| Intervention | Units on a scale (Mean) |
|---|---|
| Tapentadol PR | -24.5 |
The WOMAC is a self-administered questionnaire and has 24 questions: Pain, Stiffness and Physical Function. The possible scores range from 0-20 for pain, 0-8 for stiffness, 0-68 for physical function and these are then summed 0-96 for the global score. The negative value indicates that there has been an improvement since baseline, the higher the value the greater the change since baseline. (NCT00982280)
Timeframe: 12 weeks
| Intervention | Units on a scale (Mean) |
|---|---|
| Tapentadol PR | -25.1 |
"For this pain assessment, the participant was to indicate the level of average pain experienced over the previous 3 days on an 11-point Numerical Rating Scale(NRS) where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine." (NCT00982280)
Timeframe: Baseline
| Intervention | units on a scale (Mean) |
|---|---|
| Tapentadol PR | 4.7 |
Western Ontario McMaster Questionnaire (WOMAC) Global Score: WOMAC is measured with a Likert ordinal scale (the participant gives one of 5 possible answers) A higher score indicate that a symptom is bothersome or disabling. The WOMAC is a self-administered questionnaire and has 24 questions: Pain, Stiffness and Physical Function. The possible scores range from 0-20 for pain, 0-8 for stiffness, 0-68 for physical function and these are then summed 0-96 for the global score. A lower score indicates a lower level of symptoms and or disability. (NCT00982280)
Timeframe: Baseline
| Intervention | Units on a scale (Mean) |
|---|---|
| Tapentadol PR | 54.2 |
In the Patient Global Impression of Change (PGIC) the participant indicates the perceived change over the treatment period. The participant is requested to choose one of seven categories. Scores range from very much improved to very much worse. (NCT00982280)
Timeframe: Baseline; End of Week 6 (6 Weeks)
| Intervention | participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Very much improved | Much improved | Minimally improved | No change | Minimally worse | Much worse | Very much worse | |
| Tapentadol PR | 6 | 28 | 18 | 1 | 2 | 0 | 0 |
"For this pain assessment, the participant was to indicate the level of average pain experienced over the previous 3 days on an 11-point Numerical Rating Scale(NRS) where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine. The value indicates the change from the baseline value on the 0 to 10 scale. A Negative value indicates a reduction in pain intensity from the baseline average pain intensity." (NCT00982280)
Timeframe: Baseline; Week 12 (12 weeks)
| Intervention | Units on a scale (Mean) |
|---|---|
| Tapentadol PR | -2.7 |
In the Patient Global Impression of Change (PGIC) the participant indicates the perceived change over the treatment period. The participant is requested to choose one of seven categories. Scores range from very much improved to very much worse. (NCT00983073)
Timeframe: Baseline; End of Week 6 (6 Weeks)
| Intervention | Participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Very Much Improved | Much Improved | Minimally Improved | No Change | Minimally Worse | Much Worse | Very Much Worse | |
| Tapentadol PR | 14 | 75 | 58 | 8 | 2 | 2 | 0 |
The WOMAC is a self-administered questionnaire and has 24 questions: Pain, Stiffness and Physical Function. The possible scores range from 0-20 for pain, 0-8 for stiffness, 0-68 for physical function and these are then summed 0-96 for the global score. The negative value indicates that there has been an improvement since baseline, the higher the value the greater the change since baseline. (NCT00983073)
Timeframe: Baseline; End of Week 12 (12 Weeks)
| Intervention | units on a scale (Mean) |
|---|---|
| Tapentadol PR | -27.6 |
The WOMAC is a self-administered questionnaire and has 24 questions: Pain, Stiffness and Physical Function. The possible scores range from 0-20 for pain, 0-8 for stiffness, 0-68 for physical function and these are then summed 0-96 for the global score. The negative value indicates that there has been an improvement since baseline, the higher the value the greater the change since baseline. (NCT00983073)
Timeframe: Baseline; End of Week 6 (6 Weeks)
| Intervention | units on a scale (Mean) |
|---|---|
| Tapentadol PR | -21.0 |
"For this pain assessment, the participant was to indicate the level of average pain experienced over the previous 3 days on an 11-point Numerical Rating Scale(NRS) where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine. The value indicates the change from the baseline value on the 0 to 10 scale. A Negative value indicates a reduction in pain intensity from the baseline average pain intensity." (NCT00983073)
Timeframe: Baseline; End of Week 12 (12 Weeks)
| Intervention | units on a scale (Mean) |
|---|---|
| Tapentadol PR | -4.4 |
"For this pain assessment, the participant was to indicate the level of average pain experienced over the previous 3 days on an 11-point Numerical Rating Scale(NRS) where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine. The value indicates the change from the baseline value on the 0 to 10 scale. A Negative value indicates a reduction in pain intensity from the baseline average pain intensity." (NCT00983073)
Timeframe: Baseline; End of Week 6 (6 Weeks)
| Intervention | units on a scale (Mean) |
|---|---|
| Tapentadol PR | -3.8 |
EuroQoL-5D Health State Visual Analog Scale (VAS) is a participant rated questionnaire to assess health-related quality of life in terms of a single index value. The VAS component rates current health state on a scale from 0 (worst imaginable health state) to 100 (best imaginable health state); higher scores indicate a better health state. The values indicated represent the change from the baseline, a positive value indicates an improvement. (NCT00983073)
Timeframe: Baseline, End of Week 12 (12 Weeks)
| Intervention | Units on a scale (Mean) |
|---|---|
| Tapentadol PR | 19.5 |
EuroQoL-5D Health State Visual Analog Scale (VAS) is a participant rated questionnaire to assess health-related quality of life in terms of a single index value. The VAS component rates current health state on a scale from 0 (worst imaginable health state) to 100 (best imaginable health state); higher scores indicate a better health state. The values indicated represent the change from the baseline, a positive value indicates an improvement. (NCT00983073)
Timeframe: Baseline; End of Week 6 (6 Weeks)
| Intervention | Units on a scale (Mean) |
|---|---|
| Tapentadol PR | 15.8 |
"The participant scored the EuroQol-5. This is a five dimensional health state classification. Each dimension is assessed on a 3-point ordinal scale (1=no problems, 2=some problems, 3=extreme problems). The responses to the five EQ-5D dimensions were scored using a utility-weighted algorithm to derive an EQ-5D health status index score between 0 to 1, with 1.00 indicating full health and 0 representing dead. The positive values indicate that during the study the health status improved." (NCT00983073)
Timeframe: Baseline; End of Week 12 (12 Weeks)
| Intervention | Units on a scale (Mean) |
|---|---|
| Tapentadol PR | 0.27 |
"The participant scored the EuroQol-5. This is a five dimensional health state classification. Each dimension is assessed on a 3-point ordinal scale (1=no problems, 2=some problems, 3=extreme problems). The responses to the five EQ-5D dimensions were scored using a utility-weighted algorithm to derive an EQ-5D health status index score between 0 to 1, with 1.00 indicating full health and 0 representing dead. The positive values indicate that during the study the health status improved." (NCT00983073)
Timeframe: Baseline; End of Week 6 (6 Weeks)
| Intervention | Units on a scale (Mean) |
|---|---|
| Tapentadol PR | 0.23 |
Participants were requested to rate their tapentadol (new) analgesic medication on a 5-point scale. The medication was rated as excellent, very good, good, fair and poor. (NCT00983073)
Timeframe: Baseline; End of Week 12 (12 Weeks)
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| Excellent | Very Good | Good | Fair | Poor | |
| Tapentadol PR | 16 | 45 | 54 | 9 | 1 |
Western Ontario McMaster Questionnaire (WOMAC) Global Score: WOMAC is measured with a Likert ordinal scale (the participant gives one of 5 possible answers) A higher score indicate that a symptom is bothersome or disabling. The WOMAC is a self-administered questionnaire and has 24 questions: Pain, Stiffness and Physical Function. The possible scores range from 0-20 for pain, 0-8 for stiffness, 0-68 for physical function and these are then summed 0-96 for the global score. A lower score indicates a lower level of symptoms and or disability. (NCT00983073)
Timeframe: Baseline
| Intervention | units on a scale (Mean) |
|---|---|
| Tapentadol PR | 53.6 |
Participants were requested to rate their tapentadol (new) analgesic medication on a 5-point scale. The medication was rated as excellent, very good, good, fair and poor. (NCT00983073)
Timeframe: Baseline; End of Week 6 (6 Weeks)
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| Excellent | Very Good | Good | Fair | Poor | |
| Tapentadol PR | 16 | 39 | 88 | 17 | 0 |
"For this pain assessment, the participant was to indicate the level of average pain experienced over the previous 3 days on an 11-point Numerical Rating Scale(NRS) where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine. The value indicates the change from the baseline value on the 0 to 10 scale. A Negative value indicates a reduction in pain intensity from the baseline average pain intensity." (NCT00983073)
Timeframe: Baseline to end of week 6
| Intervention | Units on a scale (Mean) |
|---|---|
| Tapentadol PR | -3.4 |
In the Clinical Global Impression of Change (CGIC) the clinician indicates the perceived change over the treatment period. The clinician is requested to choose one of seven categories. Scores range from very much improved to very much worse. (NCT00983073)
Timeframe: Baseline; End of Week 12 (12 Weeks)
| Intervention | Participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Very Much Improved | Much Improved | Minimally Improved | No Change | Minimally Worse | Much Worse | Very Much Worse | |
| Tapentadol PR | 28 | 68 | 27 | 2 | 0 | 0 | 0 |
In the Patient Global Impression of Change (PGIC) the participant indicates the perceived change over the treatment period. The participant is requested to choose one of seven categories. Scores range from very much improved to very much worse. (NCT00983073)
Timeframe: Baseline; End of Week 12 (12 Weeks)
| Intervention | Participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Very Much Improved | Much Improved | Minimally Improved | No Change | Minimally Worse | Much Worse | Very Much Worse | |
| Tapentadol PR | 23 | 64 | 33 | 5 | 0 | 0 | 0 |
Participants were requested to rate their previous analgesic medication on a 5-point scale. Previous medication was rated as excellent, very good, good, fair and poor. (NCT00983073)
Timeframe: Baseline
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| Excellent | Very Good | Good | Fair | Poor | |
| Tapentadol PR | 0 | 0 | 4 | 132 | 62 |
In the Clinical Global Impression of Change (CGIC) the clinician indicates the perceived change over the treatment period. The clinician is requested to choose one of seven categories. Scores range from very much improved to very much worse. (NCT00983073)
Timeframe: Baseline; End of Week 6 (6 Weeks)
| Intervention | Participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Very Much Improved | Much Improved | Minimally Improved | No Change | Minimally Worse | Much Worse | Very Much Worse | |
| Tapentadol PR | 14 | 88 | 47 | 7 | 2 | 1 | 1 |
"For this pain assessment, the participant was to indicate the level of average pain experienced over the previous 3 days on an 11-point Numerical Rating Scale (NRS)where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine." (NCT00983073)
Timeframe: Baseline
| Intervention | units on a scale (Mean) |
|---|---|
| Tapentadol PR | 7.5 |
Change in mean score NPSI, questionnaire evaluates symptoms of neuropathic pain. Ten pain descriptors questions are answered on an 11-point scale 0 (no pain)-10 (most intense pain imaginable). The NPSI derives a total intensity score calculated from the subscores. A negative value indicates improvement in neuropathic symptoms. (NCT00983385)
Timeframe: Baseline; End of Week 12 (12 Weeks)
| Intervention | units on a scale (Mean) |
|---|---|
| Tapentadol | -0.296 |
Change in mean score NPSI, questionnaire evaluates symptoms of neuropathic pain. Ten pain descriptors questions are answered on an 11-point scale 0 (no pain)-10 (most intense pain imaginable). The NPSI derives a total intensity score calculated from the subscores. A negative value indicates improvement in neuropathic symptoms. (NCT00983385)
Timeframe: Baseline; End of Week 6 (6 Weeks)
| Intervention | Units on a scale (Mean) |
|---|---|
| Tapentadol | -0.224 |
"The painDETECT questionnaire was used to determine the possibility of the presence of a neuropathic pain component. It is a participant completed questionnaire. A total score is calculated. Participants with a score between 0 and 12 are scored as being negative (no neuropathic pain component). Value between 19 and 38 as being positive (presence of neuropathic component). Values from 13 to 18 are scored as being unclear." (NCT00983385)
Timeframe: Baseline
| Intervention | units on a scale (Mean) |
|---|---|
| Baseline painDETECT Negative Group | 7.1 |
| Baseline painDETECT Unclear Group | 13.2 |
| Baseline painDETECT Positive Group | 21.4 |
"The baseline painDETECT score was reassessed at the end of Week 12.~It is a participant completed questionnaire. A total score is calculated. Participants with a score between 0 and 12 are scored as being negative (no neuropathic pain component). Value between 19 and 38 as being positive (presence of neuropathic component). Values from 13 to 18 are scored as being unclear." (NCT00983385)
Timeframe: End of Week 12
| Intervention | units on a scale (Mean) |
|---|---|
| Baseline painDETECT Negative Group | 5.7 |
| Baseline painDETECT Unclear Group | 7.1 |
| Baseline painDETECT Positive Group | 11.2 |
"The baseline painDETECT score was reassessed at the end of Week 6.~It is a participant completed questionnaire. A total score is calculated. Participants with a score between 0 and 12 are scored as being negative (no neuropathic pain component). Value between 19 and 38 as being positive (presence of neuropathic component). Values from 13 to 18 are scored as being unclear." (NCT00983385)
Timeframe: End of Week 6
| Intervention | units on a scale (Mean) |
|---|---|
| Baseline painDETECT Negative Group | 5.5 |
| Baseline painDETECT Unclear Group | 9.8 |
| Baseline painDETECT Positive Group | 14.4 |
"For this pain assessment, the participant was to indicate the level of average pain experienced over the previous 3 days on an 11-point Numerical Rating Scale(NRS) where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine. The value indicates the change from the baseline participant assessment on the 0 to 10 scale. A negative value indicates a reduction in pain intensity." (NCT00983385)
Timeframe: Baseline; End of Week 6 (6 Weeks)
| Intervention | Units on a scale (Mean) |
|---|---|
| Tapentadol | -2.8 |
"For this pain assessment, the participant was to indicate the level of average pain experienced over the previous 3 days on an 11-point Numerical Rating Scale(NRS) where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine." (NCT00983385)
Timeframe: Baseline
| Intervention | Units on a scale (Mean) | |
|---|---|---|
| Negative painDETECT participants | Unclear and positive painDETECT participants | |
| Tapentadol | 7.3 | 7.4 |
"For this pain assessment, the participant was to indicate the level of average pain experienced over the previous 3 days on an 11-point Numerical Rating Scale(NRS) where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine." (NCT00983385)
Timeframe: Baseline
| Intervention | Units on a scale (Mean) | |
|---|---|---|
| Negative painDETECT participants | Unclear and positive painDETECT participants | |
| Tapentadol | 6.7 | 7.6 |
EuroQoL-5D Health State Visual Analog Scale (VAS) is a participant rated questionnaire to assess health-related quality of life in terms of a single index value. The VAS component rates current health state on a scale from 0 (worst imaginable health state) to 100 (best imaginable health state); higher scores indicate a better health state. The values indicated represent the change from the baseline, a positive value indicates an improvement. (NCT00983385)
Timeframe: Baseline; End of Week 12 (12 weeks)
| Intervention | Units on a scale (Mean) | ||
|---|---|---|---|
| All participants | Participants painDETECT negative | Participant painDETECT unclear or positive | |
| Tapentadol | 20.0 | 14.7 | 21.8 |
The Scores Form 36 (SF-36) includes several brief board questions on 8 aspects, (physical functioning, role physical, bodily pain, general health, vitality, social functioning, role-emotional and mental health) that a participant was asked to score over the last week. A higher score indicates an improvement in health. All domains are scored on a scale from 0 (negative health) to 100 (positive health), with 100 representing the best possible health state. A positive mean value indicates an improvement from baseline. (NCT00983385)
Timeframe: Baseline; End of Week 12 (12 weeks)
| Intervention | Units on a scale (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Physical Functioning | Bodily Pain | General Health | Vitality | Social Functioning | Role Emotional | Mental Health | Role Physical | |
| Tapentadol | 15.7 | 24.4 | 10.3 | 9.5 | 13.2 | 18.6 | 12.0 | 29.2 |
The Scores Form 36 (SF-36) includes several brief board questions on 8 aspects, (physical functioning, role physical, bodily pain, general health, vitality, social functioning, role-emotional and mental health) that a participant was asked to score over the last week. A higher score indicates an improvement in health. All domains are scored on a scale from 0 (negative health) to 100 (positive health), with 100 representing the best possible health state. A positive mean value indicates an improvement from baseline. (NCT00983385)
Timeframe: Baseline; End of Week 6 (6 weeks)
| Intervention | Units on a scale (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Physical Functioning | Bodily Pain | General Health | Vitality | Social Functioning | Role Emotional | Mental Health | Role Physical | |
| Tapentadol | 14.1 | 21.7 | 6.3 | 8.0 | 10.7 | 14.8 | 7.5 | 25.0 |
In the Clinical Global Impression of Change (CGIC) the clinician indicates the perceived change over the treatment period. The clinician is requested to choose one of seven categories. Scores range from very much improved to very much worse. (NCT00983385)
Timeframe: Baseline; End of Week 12 (12 weeks)
| Intervention | participants (Number) | |||
|---|---|---|---|---|
| Very much improved | Much improved | Minimally improved | No change | |
| Tapentadol | 17 | 45 | 22 | 5 |
In the Clinical Global Impression of Change (CGIC) the clinician indicates the perceived change over the treatment period. The clinician is requested to choose one of seven categories. Scores range from very much improved to very much worse. (NCT00983385)
Timeframe: Baseline; End of Week 6 (6 weeks)
| Intervention | participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Very much improved | Much improved | Minimally improved | No change | Minimally worse | Much worse | Very much worse | |
| Tapentadol | 17 | 53 | 49 | 11 | 2 | 1 | 1 |
"The participant scored the EuroQol-5. This is a five dimensional health state classification. Each dimension is assessed on a 3-point ordinal scale (1=no problems, 2=some problems, 3=extreme problems). The responses to the five EQ-5D dimensions were scored using a utility-weighted algorithm to derive an EQ-5D health status index score between 0 to 1, with 1.00 indicating full health and 0 representing dead. The positive values indicate that during the study the health status improved." (NCT00983385)
Timeframe: Baseline; End of Week 12 (12 weeks)
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| All participants | Participants painDETECT negative | Participants painDETECT unclear or positive | |
| Tapentadol | 0.282 | 0.182 | 0.316 |
"The participant scored the EuroQol-5. This is a five dimensional health state classification. Each dimension is assessed on a 3-point ordinal scale (1=no problems, 2=some problems, 3=extreme problems). The responses to the five EQ-5D dimensions were scored using a utility-weighted algorithm to derive an EQ-5D health status index score between 0 to 1, with 1.00 indicating full health and 0 representing dead. The positive values indicate that during the study the health status improved." (NCT00983385)
Timeframe: Baseline; End of Week 6 (6 weeks)
| Intervention | Units on a scale (Mean) | ||
|---|---|---|---|
| All participants | Participants painDETECT negative | Participant painDETECT unclear or positive | |
| Tapentadol | 0.244 | 0.229 | 0.249 |
Tapentadol hydrochloride PR dose after 5 weeks of titration which was to be kept stable during the remained of the trial. (NCT00983385)
Timeframe: Week 6
| Intervention | milligrams (mg) (Mean) | ||
|---|---|---|---|
| Negative painDETECT participants | Unclear painDETECT participants | Positive painDETECT participants | |
| Tapentadol | 336.4 | 293.3 | 268.2 |
"Anxiety Scale - 7 items scored for each individual question from 0 = best and 3 = worst.~HADS is a self-assessment scale for the symptom severity of anxiety disorders and depression. It comprises of 14 items. Seven statements describe anxiety. Each answer is scored on a four-point scale (0-3). All seven answers are summed to a total score with a maximum score of 21 points.~A negative value indicates that there has been an improvement." (NCT00983385)
Timeframe: Baseline
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| All participants | Negative painDETECT participants | Unclear and positive painDETECT participants | |
| Tapentadol | 7.8 | 6.2 | 8.4 |
"Anxiety Scale - 7 items scored for each individual question from 0 = best and 3 = worst.~HADS is a self-assessment scale for the symptom severity of anxiety disorders and depression. It comprises of 14 items. Seven statements describe anxiety. Each answer is scored on a four-point scale (0-3). All seven answers are summed to a total score with a maximum score of 21 points.~A negative value indicates that there has been an improvement." (NCT00983385)
Timeframe: Baseline; End of Week 12 (12 Weeks)
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| All participants | Negative painDETECT participants | Unclear and positive painDETECT participants | |
| Tapentadol | -2.1 | -0.8 | -2.5 |
"Anxiety Scale - 7 items scored for each individual question from 0 = best and 3 = worst.~HADS is a self-assessment scale for the symptom severity of anxiety disorders and depression. It comprises of 14 items. Seven statements describe anxiety. Each answer is scored on a four-point scale (0-3). All seven answers are summed to a total score with a maximum score of 21 points.~A negative value indicates that there has been an improvement." (NCT00983385)
Timeframe: Baseline; End of Week 6 (6 weeks)
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| All participants | Negative painDETECT participants | Unclear and positive painDETECT participants | |
| Tapentadol | -1.2 | -0.3 | -1.5 |
"Depression Scale - 7 items scored for each individual question from 0 = best and 3 = worst.~HADS is a self-assessment scale for the symptom severity of anxiety disorders and depression. It comprises of 14 items. Seven statements describe depression. Each answer is scored on a four-point scale (0-3). All seven answers are summed to a total score with a maximum score of 21 points.~A negative value indicates that there has been an improvement." (NCT00983385)
Timeframe: Baseline; End of Week 12 (12 Weeks)
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| All participants | Negative painDETECT participants | Unclear and positive painDETECT participants | |
| Tapentadol | -1.6 | -0.5 | -2.0 |
"Depression Scale - 7 items scored for each individual question from 0 = best and 3 = worst.~HADS is a self-assessment scale for the symptom severity of anxiety disorders and depression. It comprises of 14 items. Seven statements describe depression. Each answer is scored on a four-point scale (0-3). All seven answers are summed to a total score with a maximum score of 21 points.~A negative value indicates that there has been an improvement." (NCT00983385)
Timeframe: Baseline; End of Week 6 (6 weeks)
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| All participants | Negative painDETECT participants | Unclear and positive painDETECT participants | |
| Tapentadol | -1.2 | -1.0 | -1.3 |
"Depression Scale - 7 items scored for each individual question from 0 = best and 3 = worst.~HADS is a self-assessment scale for the symptom severity of anxiety disorders and depression. It comprises of 14 items. Seven statements describe anxiety. Each answer is scored on a four-point scale (0-3). All seven answers are summed to a total score with a maximum score of 21 points.~A negative value indicates that there has been an improvement." (NCT00983385)
Timeframe: Baseline
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| All participants | Negative painDETECT participants | Unclear and positive painDETECT participants | |
| Tapentadol | 7.9 | 6.5 | 8.5 |
Mean score NPSI (Neuropathic Pain Symptom Inventory). The participant rates their symptoms of neuropathic pain. Ten pain questions are answered on an 11-point scale 0 (no pain) to 10 (most intense pain imaginable). Two items related to temporal pain assessed on 5-point scales. (NCT00983385)
Timeframe: Baseline Visit
| Intervention | units on a scale (Mean) | |||||
|---|---|---|---|---|---|---|
| Sub-score burning pain | Sub-score pressing pain | Sub-score paroxysmal pain | Sub-score evoked pain | Sub-score paresthesia / dysthesia | Overall score | |
| Tapentadol | 0.470 | 0.549 | 0.575 | 0.391 | 0.539 | 0.497 |
Mean score NPSI (Neuropathic Pain Symptom Inventory). The participant rates their symptoms of neuropathic pain. Ten pain questions are answered on an 11-point scale 0 (no pain) to 10 (most intense pain imaginable). Two items related to temporal pain assessed on 5-point scales. (NCT00983385)
Timeframe: End of Week 12
| Intervention | units on a scale (Mean) | |||||
|---|---|---|---|---|---|---|
| Sub-score burning pain | Sub-score pressing pain | Sub-score paroxysmal pain | Sub-score evoked pain | Sub-score paresthesia / dysthesia | Overall score | |
| Tapentadol | 0.180 | 0.235 | 0.211 | 0.175 | 0.231 | 0.206 |
Mean score NPSI (Neuropathic Pain Symptom Inventory). The participant rates their symptoms of neuropathic pain. Ten pain questions are answered on an 11-point scale 0 (no pain) to 10 (most intense pain imaginable). Two items related to temporal pain assessed on 5-point scales. (NCT00983385)
Timeframe: End of Week 6
| Intervention | units on a scale (Mean) | |||||
|---|---|---|---|---|---|---|
| Sub-score burning pain | Sub-score pressing pain | Sub-score paroxysmal pain | Sub-score evoked pain | Sub-score paresthesia / dysthesia | Overall score | |
| Tapentadol | 0.260 | 0.316 | 0.293 | 0.230 | 0.303 | 0.278 |
"For this pain assessment, the participant was to indicate the level of average pain experienced over the previous 3 days on an 11-point Numerical Rating Scale(NRS) where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine." (NCT00983385)
Timeframe: End of Week 12
| Intervention | Units on a scale (Mean) | |
|---|---|---|
| Negative painDETECT participants | Unclear and positive painDETECT participants | |
| Tapentadol | 3.4 | 3.2 |
"For this pain assessment, the participant was to indicate the level of average pain experienced over the previous 3 days on an 11-point Numerical Rating Scale(NRS) where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine." (NCT00983385)
Timeframe: End of Week 6
| Intervention | Units on a scale (Mean) | |
|---|---|---|
| Negative painDETECT participants | Unclear and positive painDETECT participants | |
| Tapentadol | 4.2 | 4.4 |
"For this pain assessment, the participant was to indicate the level of average pain experienced over the previous 3 days on an 11-point Numerical Rating Scale(NRS) where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine." (NCT00983385)
Timeframe: End of Week 12
| Intervention | Units on a scale (Mean) | |
|---|---|---|
| Negative painDETECT participants | Unclear and positive painDETECT participants | |
| Tapentadol | 3.1 | 3.4 |
"For this pain assessment, the participant was to indicate the level of average pain experienced over the previous 3 days on an 11-point Numerical Rating Scale(NRS) where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine." (NCT00983385)
Timeframe: End of Week 6
| Intervention | Units on a scale (Mean) | |
|---|---|---|
| Negative painDETECT participants | Unclear and positive painDETECT participants | |
| Tapentadol | 4.0 | 4.1 |
Participants were requested to rate their tapentadol (new) analgesic medication on a 5-point scale. The medication was rated as excellent, very good, good, fair and poor. (NCT00983385)
Timeframe: End of Week 12
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| Excellent | Very Good | Good | Fair | Poor | |
| Tapentadol | 10 | 38 | 28 | 11 | 2 |
Participants were requested to rate their tapentadol (new) analgesic medication on a 5-point scale. The medication was rated as excellent, very good, good, fair and poor. (NCT00983385)
Timeframe: End of Week 6
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| Excellent | Very Good | Good | Fair | Poor | |
| Tapentadol | 12 | 29 | 64 | 22 | 7 |
Participants were requested to rate their tapentadol (new) analgesic medication on a 5-point scale. The medication was rated as excellent, very good, good, fair and poor. (NCT00983385)
Timeframe: End of Week 8
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| Excellent | Very Good | Good | Fair | Poor | |
| Tapentadol | 14 | 30 | 58 | 17 | 3 |
Participants were requested to rate their previous analgesic medication on a 5-point scale. Previous analgesic medication was rated as excellent, very good, good, fair and poor. (NCT00983385)
Timeframe: Baseline
| Intervention | participants (Number) | ||
|---|---|---|---|
| Good | Fair | Poor | |
| Tapentadol | 2 | 98 | 75 |
In the Patient Global Impression of Change (PGIC) the participant indicates the perceived change over the treatment period. The participant is requested to choose one of seven categories. Scores range from very much improved to very much worse. (NCT00983385)
Timeframe: Baseline; End of Week 12 (12 weeks)
| Intervention | participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Very much improved | Much improved | Minimally improved | No change | Minimally worse | Much worse | Very much worse | |
| Tapentadol | 19 | 42 | 23 | 5 | 0 | 0 | 0 |
In the Patient Global Impression of Change (PGIC) the participant indicates the perceived change over the treatment period. The participant is requested to choose one of seven categories. Scores range from very much improved to very much worse. (NCT00983385)
Timeframe: Baseline; End of Week 6 (6 Weeks)
| Intervention | participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Very much improved | Much improved | Minimally improved | No change | Minimally worse | Much worse | Very much worse | |
| Tapentadol | 12 | 55 | 49 | 10 | 5 | 2 | 1 |
EuroQoL-5D Health State Visual Analog Scale (VAS) is a participant rated questionnaire to assess health-related quality of life in terms of a single index value. The VAS component rates current health state on a scale from 0 (worst imaginable health state) to 100 (best imaginable health state); higher scores indicate a better health state. The values indicated represent the change from the baseline, a positive value indicates an improvement. (NCT00983385)
Timeframe: Baseline; End of Week 6 (6 weeks)
| Intervention | Units on a scale (Mean) | ||
|---|---|---|---|
| All participants | Participants painDETECT negative | Participant painDETECT unclear or positive | |
| Tapentadol | 12.2 | 7.6 | 13.8 |
Tapentadol was compared to Oxycodone with Oxycodone set to 1. The average total daily dose of Tapentadol at which a pain score equivalent or below to the pain score at the end of observation period under Oxycodone was reached was documented as the equipotent or equianalgesic dose to the total daily dose of the previously used Oxycodone. (NCT00986258)
Timeframe: Baseline; End of Week 6 (6 Weeks)
| Intervention | Ratio (Number) |
|---|---|
| Tapentadol | 5.3 |
"For this pain assessment, the participant was to indicate the level of average pain experienced over the previous 3 days on an 11-point Numerical Rating Scale (NRS) where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine." (NCT00986258)
Timeframe: Baseline
| Intervention | units on a scale (Mean) |
|---|---|
| Tapentadol Prolonged Release | 4.8 |
In the Patient Global Impression of Change (PGIC) the participant indicates the perceived change over the treatment period. The participant is requested to choose one of seven categories. Scores range from very much improved to very much worse. (NCT00986258)
Timeframe: Baseline; End of Week 6 (6 Weeks)
| Intervention | participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Very much improved | Much improved | Minimally improved | No change | Minimally worse | Much worse | Very much worse | |
| Tapentadol Prolonged Release | 5 | 29 | 47 | 11 | 6 | 3 | 0 |
Tapentadol was compared to Hydromorphone with Hydromorphone set to 1. The average total daily dose of Tapentadol at which a pain score equivalent or below to the pain score at the end of observation period under Hydromorphone was reached was documented as the equipotent or equianalgesic dose to the total daily dose of the previously used Hydromorphone. (NCT00986258)
Timeframe: Baseline; End of Week 6 (6 Weeks)
| Intervention | Ratio (Number) |
|---|---|
| Tapentadol | 10.5 |
Tapentadol was compared to Morphine with Morphine set to 1. The average total daily dose of Tapentadol at which a pain score equivalent or below to the pain score at the end of observation period under Morphine was reached was documented as the equipotent or equianalgesic dose to the total daily dose of the previously used Morphine. (NCT00986258)
Timeframe: Baseline; End of Week 6 (6 Weeks)
| Intervention | Ratio (Number) |
|---|---|
| Tapentadol | 3.0 |
Tapentadol was compared to Transdermal Fentanyl with Fentanyl set to 1. The average total daily dose of Tapentadol at which a pain score equivalent or below to the pain score at the end of observation period under Transdermal Fentanyl was reached was documented as the equipotent or equianalgesic dose to the total daily dose of the previously used Fentanyl. (NCT00986258)
Timeframe: Baseline; End of Week 6 (6 Weeks)
| Intervention | Ratio (Number) |
|---|---|
| Tapentadol | 250.7 |
Participants were considered responders if they reported the same or less average pain intensity over a 3 day period (NRS-3) after 6 weeks of tapentadol prolonged release treatment compared to their previous analgesic treatment (over a 3 day period on the Numeric Rating Scale) at Week 6 compared with Week-1. (NCT00986258)
Timeframe: 6 weeks
| Intervention | participants (Number) |
|---|---|
| Tapentadol Prolonged Release | 76 |
"The painDETECT questionnaire was used to determine the possibility of the presence of a neuropathic pain component. It is a participant completed questionnaire. A total score is calculated. Participants with a score between 0 and 12 are scored as being negative (no neuropathic pain component). Value between 19 and 38 as being positive (presence of neuropathic component). Values from 13 to 18 are scored as being unclear." (NCT00986258)
Timeframe: Baseline
| Intervention | units on a scale (Mean) |
|---|---|
| Baseline painDETECT Negative Group | 6.5 |
| Baseline painDETECT Unclear Group | 14.7 |
| Baseline painDETECT Positive Group | 21.1 |
"The baseline painDETECT score was reassessed at the end of Week 12.~It is a participant completed questionnaire. A total score is calculated. Participants with a score between 0 and 12 are scored as being negative (no neuropathic pain component). Value between 19 and 38 as being positive (presence of neuropathic component). Values from 13 to 18 are scored as being unclear." (NCT00986258)
Timeframe: End of Week 12
| Intervention | units on a scale (Mean) |
|---|---|
| Baseline painDETECT Negative Group | 6.8 |
| Baseline painDETECT Unclear Group | 8.6 |
| Baseline painDETECT Positive Group | 16.5 |
"The baseline painDETECT score was reassessed at the end of Week 6.~It is a participant completed questionnaire. A total score is calculated. Participants with a score between 0 and 12 are scored as being negative (no neuropathic pain component). Value between 19 and 38 as being positive (presence of neuropathic component). Values from 13 to 18 are scored as being unclear." (NCT00986258)
Timeframe: End of Week 6
| Intervention | units on a scale (Mean) |
|---|---|
| Baseline painDETECT Negative Group | 7.5 |
| Baseline painDETECT Unclear Group | 10.5 |
| Baseline painDETECT Positive Group | 17.4 |
The Scores Form 36 (SF-36) includes several brief questions on 8 aspects, (physical functioning, role physical, bodily pain, general health, vitality, social functioning, role-emotional and mental health) that a participant was asked to score over the last week. A higher score indicates an improvement in health. All domains are scored on a scale from 0 (negative health) to 100 (positive health), with 100 representing the best possible health state. A positive mean value indicates an improvement from baseline. (NCT00986258)
Timeframe: Baseline; End of Week 12 (12 Weeks)
| Intervention | units on a scale (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Physical Functioning | Bodily Pain | General Health | Vitality | Social Functioning | Role Emotional | Mental Health | Role Physical | |
| Tapentadol Prolonged Release | 10.5 | 14.1 | 5.7 | 12.0 | 11.7 | 13.9 | 9.8 | 10.7 |
The Scores Form 36 (SF-36) includes several brief questions on 8 aspects, (physical functioning, role physical, bodily pain, general health, vitality, social functioning, role-emotional and mental health) that a participant was asked to score over the last week. A higher score indicates an improvement in health. All domains are scored on a scale from 0 (negative health) to 100 (positive health), with 100 representing the best possible health state. A positive mean value indicates an improvement from baseline. (NCT00986258)
Timeframe: Baseline; End of Week 6 (6 Weeks)
| Intervention | units on a scale (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Physical Functioning | Bodily Pain | General Health | Vitality | Social Functioning | Role Emotional | Mental Health | Role Physical | |
| Tapentadol Prolonged Release | 8.4 | 11.6 | 5.9 | 9.2 | 8.0 | -1.4 | 5.1 | 6.9 |
"All participants were requested to complete the NPSI (Neuropathic Pain Symptom Inventory) questionnaire at this visit. Each participant rated their own neuropathic pain symptoms by answering ten questions relating to neuropathic symptoms on an 11-point scale 0 (not present) to 10 (worst imaginable) for each question. The higher the score for a question (sub-scale) the more bothersome the symptom is for the participant.~Results are reported as the mean (average) for each neuropathic symptom in a sub-scale.~The mean score is reported on a scale of 0 (not present in the group) to 1 (symptom has the maximum imaginable intensity for the whole group)." (NCT00986258)
Timeframe: End of Week 12
| Intervention | units on a scale (Mean) | |||||
|---|---|---|---|---|---|---|
| Sub-score burning pain | Sub-score pressing pain | Sub-score paroxysmal pain | Sub-score evoked pain | Sub-score paresthesia / dysthesia | Overall score | |
| Tapentadol Prolonged Release | 0.27 | 0.302 | 0.254 | 0.273 | 0.299 | 0.280 |
"All participants were requested to complete the NPSI (Neuropathic Pain Symptom Inventory) questionnaire at this visit. Each participant rated their own neuropathic pain symptoms by answering ten questions relating to neuropathic symptoms on an 11-point scale 0 (not present) to 10 (worst imaginable) for each question. The higher the score for a question (sub-scale) the more bothersome the symptom is for the participant.~Results are reported as the mean for each neuropathic symptom in a sub-scale. The mean score is reported on a scale of 0 (not present in the group) to 1 (symptom has the maximum imaginable intensity for the whole group)." (NCT00986258)
Timeframe: End of Week 6
| Intervention | units on a scale (Mean) | |||||
|---|---|---|---|---|---|---|
| Sub-score burning pain | Sub-score pressing pain | Sub-score paroxysmal pain | Sub-score evoked pain | Sub-score paresthesia / dysthesia | Overall score | |
| Tapentadol Prolonged Release | 0.32 | 0.322 | 0.271 | 0.274 | 0.302 | 0.297 |
"All participants were requested to complete the NPSI (Neuropathic Pain Symptom Inventory) questionnaire at this visit. Each participant rated their own neuropathic pain symptoms by answering ten questions relating to neuropathic symptoms on an 11-point scale 0 (not present) to 10 (worst imaginable) for each question. The higher the score for a question (sub-scale) the more bothersome the symptom is for the participant.~Results are reported as the mean for each neuropathic symptom in the sub-scale. The mean score is reported on a scale of 0 (not present in the group) to 1 (symptom has the maximum imaginable intensity for the whole group)." (NCT00986258)
Timeframe: Baseline
| Intervention | units on a scale (Mean) | |||||
|---|---|---|---|---|---|---|
| Sub-score burning pain | Sub-score pressing pain | Sub-score paroxysmal pain | Sub-score evoked pain | Sub-score paresthesia / dysthesia | Overall score | |
| Tapentadol Prolonged Release | 0.41 | 0.405 | 0.422 | 0.385 | 0.424 | 0.408 |
In the Patient Global Impression of Change (PGIC) the participant indicates the perceived change over the treatment period. The participant is requested to choose one of seven categories. Scores range from very much improved to very much worse. (NCT00986258)
Timeframe: Baseline; End of Week 12 (12 Weeks)
| Intervention | participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Very much improved | Much improved | Minimally improved | No change | Minimally worse | Much worse | Very much worse | |
| Tapentadol Prolonged Release | 9 | 34 | 38 | 9 | 2 | 1 | 0 |
"For this pain assessment, the participant was to indicate the level of average pain experienced over the previous 3 days on an 11-point Numerical Rating Scale(NRS) where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine. The value indicates the change from the baseline value on the 0 to 10 scale. A Negative value indicates a reduction in pain intensity from the baseline average pain intensity." (NCT00986258)
Timeframe: Baseline; End of Week 12 (12 weeks)
| Intervention | units on a scale (Mean) |
|---|---|
| Tapentadol Prolonged Release | -1.3 |
"For this pain assessment, the participant was to indicate the level of average pain experienced over the previous 3 days on an 11-point Numerical Rating Scale(NRS) where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine. The value indicates the change from the baseline value on the 0 to 10 scale. A negative value indicates a reduction in pain intensity from the baseline average pain intensity." (NCT00986258)
Timeframe: Baseline; End of Week 6 (6 weeks)
| Intervention | units on a scale (Mean) |
|---|---|
| Tapentadol Prolonged Release | -0.9 |
Tapentadol was compared to Buprenorphine with Buprenorphine set to 1. The average total daily dose of Tapentadol at which a pain score equivalent or below to the pain score at the end of observation period under Buprenorphine was reached was documented as the equipotent or equianalgesic dose to the total daily dose of the previously used Buprenorphine. (NCT00986258)
Timeframe: Baseline; End of Week 6 (6 Weeks)
| Intervention | Ratio (Number) |
|---|---|
| Tapentadol | 210.0 |
"The NRS was a twice-daily pain assessment in which patients were to indicate the level of pain experienced over the previous 12 hours on an 11-point scale with a score of 0 indicating no pain and a score of 10 indicating pain as bad as you can imagine." (NCT01041859)
Timeframe: Open-label Baseline and End of Double-Blind Treatment at 15 Weeks (3 weeks open-label plus 12 weeks double-blind)
| Intervention | percentage of participants (Number) |
|---|---|
| DB Tapentadol ER | 40.4 |
| DB Placebo | 28.9 |
"For this twice daily pain assessment, the patients were to indicate the level of pain experienced over the previous 12 hours on an 11-point Numerical Rating Scale (NRS) where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine." (NCT01041859)
Timeframe: Double-Blind Baseline and 12 weeks (Primary endpoint is the average pain intensity score during the last week of the maintenance period)
| Intervention | units on a scale (Mean) |
|---|---|
| DB Tapentadol ER | 0.28 |
| DB Placebo | 1.3 |
The BPI is a 12-item questionnaire to evaluate the intensity of pain and the degree to which pain interferes with function. It includes 4 items assessing current pain intensity and pain at its worst, least, and on average over the past day using an 11-point scale from 0 = no pain to 10 = pain as bad as you can imagine. The pain intensity subscale score is defined as the mean of the scores from these 4 items. (NCT01041859)
Timeframe: Open-label Baseline and End of Double-Blind Treatment at 15 Weeks (3 weeks open-label plus 12 weeks double-blind)
| Intervention | units on a scale (Mean) |
|---|---|
| DB Tapentadol ER | -3.0 |
| DB Placebo | -2.3 |
EQ-5D has 5 items (mobility, self-care, usual activities, pain/discomfort, anxiety/depression) rated on a categorical scale of 1-3 with 1=no problems, 2=some problems, 3=extreme problems. The health state index is a weighted combination of the 5 items. It has a range of 0 to 1, with 0=deceased and 1=full health. (NCT01041859)
Timeframe: Double-blind Baseline and End of Double-Blind Treatment at 12 Weeks
| Intervention | units on a scale (Mean) |
|---|---|
| DB Tapentadol ER | 0.00 |
| DB Placebo | -0.10 |
Patient Global Impression of Change (PGIC) is a patient-rated assessment of overall neuropathic pain since the start of treatment using a categorical scale 1-7, where 1 is 'very much improved' and 7 is 'very much worse' (NCT01041859)
Timeframe: End of Double-Blind Treatment at 12 Weeks
| Intervention | percentage of participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Very much improved | Much improved | Minimally improved | Not changed | Minimally worse | Much worse | Very much worse | |
| DB Placebo | 14.4 | 30.9 | 20.9 | 18.7 | 5.0 | 7.9 | 2.2 |
| DB Tapentadol ER | 28.7 | 37.3 | 21.3 | 8.0 | 2.0 | 1.3 | 1.3 |
The number of participants who reported a TEAE during the treatment period. TEAE was defined as any adverse event that started or worsened on or after the start of the study medication and up to 3 days after the discontinuation of the study medication. (NCT01063868)
Timeframe: Entire Study
| Intervention | participants (Number) |
|---|---|
| Tapentadol ER | 23 |
| Oxycodone CR | 11 |
The PGIC is a 7-point scale that requires the participants to assess how much their illness has improved or worsened relative to a Baseline state at the beginning of the intervention. The response options are 1 = very much improved, 2 = much improved, 3 = minimally improve, 4 = no change, 5 = minimally worse, 6 = much worse, and 7 = very much worse. (NCT01124604)
Timeframe: Week 8, Week 12
| Intervention | Participants (Number) | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Week 8; Very Much Improved (n = 47, 29) | Week 8; Much Improved (n = 47, 29) | Week 8; Minimally Improved (n = 47, 29) | Week 8; No Change (n = 47, 29) | Week 8; Minimally Worse (n = 47, 29) | Week 8; Much Worse (n = 47, 29) | Week 12; Very Much Improved (n = 45, 29) | Week 12; Much Improved (n = 45, 29) | Week 12; Minimally Improved (n = 45, 29) | Week 12; No Change (n = 45, 29) | Week 12 ; Minimally Worse (n = 45, 29) | Week 12; Much Worse (n = 45, 29) | |
| Placebo | 5 | 9 | 9 | 4 | 2 | 0 | 5 | 9 | 8 | 5 | 2 | 0 |
| Tapentadol Hydrochloride | 13 | 17 | 12 | 2 | 1 | 2 | 14 | 16 | 9 | 4 | 0 | 2 |
"Number of awakenings was addressed by the question: How many times did you wake up during the night?'' and lesser number signified better sleep." (NCT01124604)
Timeframe: Baseline, Week 12
| Intervention | Participants (Number) | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline; 0 awakening (n=60,31) | Baseline; 1 awakening (n=60,31) | Baseline; 2 awakenings (n=60,31) | Baseline; 3 awakenings (n=60,31) | Baseline; 4 awakenings (n=60,31) | Baseline; >= 5 awakenings (n=60,31) | Week 12; 0 awakening (n=45,29) | Week 12; 1 awakening (n=45,29) | Week 12; 2 awakenings (n=45,29) | Week 12; 3 awakenings (n=45,29) | Week 12; 4 awakenings (n=45,29) | Week 12; >=5 awakenings (n=45,29) | |
| Placebo | 6 | 6 | 10 | 7 | 1 | 1 | 6 | 9 | 6 | 7 | 1 | 0 |
| Tapentadol Hydrochloride | 10 | 18 | 16 | 10 | 2 | 4 | 9 | 20 | 9 | 3 | 2 | 2 |
BPI-sf is a self-evaluated pain assessment form consisting of 15 items (item 1 - presence of pain, item 2 - pain location, items 3 to 6 - pain severity, item 7 - status of pain treatment, item 8 - efficacy of pain treatment, and items 9a to 9g - interference of pain with daily life). Item 8 for efficacy of pain treatment assesses number of participants with at least 50 percent pain relief during the last 24 hours on a scale ranging from 0 percent (no relief) to 100 percent (complete relief). (NCT01124604)
Timeframe: Baseline, Week 12
| Intervention | Participants (Number) | |
|---|---|---|
| Baseline (n=60, 31) | Week 12 (n=45, 29) | |
| Placebo | 7 | 4 |
| Tapentadol Hydrochloride | 9 | 10 |
WOMAC is a self administered 24-item questionnaire used to evaluate participants with osteoarthritis of the knee. It consists of 3 subscales: pain (5 items), joint stiffness (2 items), and physical function (17 items). Each item is assessed on a 5-point scale from 0 to 4. The global score assesses pain, disability and joint stiffness and ranges from 0 to 96. Higher scores indicate that a symptom is bothersome and physically disabling. (NCT01124604)
Timeframe: Baseline, Week 12
| Intervention | Units on a scale (Mean) | |
|---|---|---|
| Global Score; Baseline (n=27, 13) | Global Score; Change at Week 12 (n=20, 13) | |
| Placebo | 1.7 | -0.4 |
| Tapentadol Hydrochloride | 1.9 | -0.9 |
SF-36v2 is 36-item form related to 8 health concepts (physical functioning, role physical, role emotional, general health, social functioning, bodily pain, vitality, mental health) and 2 summary scores (physical and mental component summary). Physical functioning, role physical and bodily pain contribute to physical component; role emotional, social functioning and mental health contribute to mental component; and social functioning, vitality, and general health contribute to both. All scores are based on a scale from 0 to 100, with higher scores defining more favorable health state. (NCT01124604)
Timeframe: Baseline, Week 12
| Intervention | Units on a scale (Mean) | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Physical Functioning; Baseline (n=60, 31) | Physical Functioning; Change at Week 12 (n=45, 29) | Role-Physical; Baseline (n=60, 31) | Role-Physical; Change at Week 12 (n=45, 29) | Bodily Pain; Baseline (n=60, 31) | Bodily Pain; Change at Week 12 (n=45, 29) | General Health; Baseline (n=60, 31) | General Health; Change at Week 12 (n=45, 29) | Vitality; Baseline (n=60, 31) | Vitality; Change at Week 12 (n=45, 29) | Social Functioning; Baseline (n=60, 31) | Social Functioning; Change at Week 12 (n=45, 29) | Role-Emotional; Baseline (n=60, 31) | Role-Emotional; Change at Week 12 (n=45, 29) | Mental Health; Baseline (n=60, 31) | Mental Health; Change at Week 12 (n=45, 29) | Mental Summary; Baseline (n=60, 31) | Mental Summary; Change at Week 12 (n=45, 29) | Physical Summary; Baseline (n=60, 31) | Physical Summary; Change at Week 12 (n=45, 29) | |
| Placebo | 51.9 | 3.4 | 57.1 | -0.4 | 34.3 | 15.1 | 47.8 | 4.7 | 51.4 | 3.7 | 66.1 | 5.2 | 61.0 | 2.6 | 59.7 | 6.4 | 48.6 | 3.6 | 25.2 | 1.3 |
| Tapentadol Hydrochloride | 48.9 | 12.1 | 57.8 | 9.6 | 34.7 | 19.4 | 47.6 | 9.1 | 46.4 | 7.6 | 66.5 | 12.5 | 63.6 | 10.7 | 58.7 | 7.4 | 47.5 | 3.6 | 25.5 | 7.9 |
"Overall quality of sleep was addressed by the question: Please rate the overall quality of your sleep last night and participants could choose one of the following options: excellent, good, fair or poor." (NCT01124604)
Timeframe: Baseline, Week 12
| Intervention | Participants (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| Baseline; Excellent (n=60, 31) | Baseline; Good (n=60, 31) | Baseline; Fair (n=60, 31) | Baseline; Poor (n=60, 31) | Week 12; Excellent (n=45, 29) | Week 12; Good (n=45, 29) | Week 12; Fair (n=45, 29) | Week 12; Poor (n=45, 29) | |
| Placebo | 1 | 17 | 13 | 0 | 0 | 21 | 7 | 1 |
| Tapentadol Hydrochloride | 1 | 37 | 19 | 3 | 2 | 30 | 9 | 4 |
(NCT01124604)
Timeframe: Week 2, 4, 8, 12
| Intervention | nanogram per milliliter (Mean) | |||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Tapentadol Hydrochloride 25 mg Week 2, n=11 | Tapentadol Hydrochloride 50 mg Week 2, n=48 | Tapentadol Hydrochloride 100 mg Week 2, n=1 | Tapentadol Hydrochloride 150 mg Week 2, n=0 | Tapentadol Hydrochloride 200 mg Week 2, n=0 | Tapentadol Hydrochloride 250 mg Week 2, n=0 | Tapentadol Hydrochloride 25 mg Week 4, n=4 | Tapentadol Hydrochloride 50 mg Week 4, n=10 | Tapentadol Hydrochloride 100 mg Week 4, n=28 | Tapentadol Hydrochloride 150 mg Week 4, n=16 | Tapentadol Hydrochloride 200 mg Week 4, n=0 | Tapentadol Hydrochloride 250 mg Week 4, n=0 | Tapentadol Hydrochloride 25 mg Week 8, n=3 | Tapentadol Hydrochloride 50 mg Week 8, n=8 | Tapentadol Hydrochloride 100 mg Week 8, n=16 | Tapentadol Hydrochloride 150 mg Week 8, n=13 | Tapentadol Hydrochloride 200 mg Week 8, n=4 | Tapentadol Hydrochloride 250 mg Week 8, n=4 | Tapentadol Hydrochloride 25 mg Week 12, n=3 | Tapentadol Hydrochloride 50 mg Week 12, n=8 | Tapentadol Hydrochloride 100 mg Week 12, n=14 | Tapentadol Hydrochloride 150 mg Week 12, n=12 | Tapentadol Hydrochloride 200 mg Week 12, n=4 | Tapentadol Hydrochloride 250 mg Week 12, n=4 | |
| Tapentadol Hydrochloride | 14.1 | 29.7 | 47.9 | NA | NA | NA | 22.8 | 23.6 | 59.0 | 76.2 | NA | NA | 25.1 | 22.7 | 57.7 | 83.2 | 87.8 | 147 | 29.2 | 25.1 | 49.1 | 40.4 | 119 | 130 |
BPI-sf consists of 15 items (item 1 - presence of pain, item 2 - pain location, items 3 to 6 - pain severity, item 7 - status of pain treatment, item 8 - efficacy of pain treatment, and items 9a to 9g - interference of pain with daily life). Total score is defined as the mean scores from items 3, 4, 5, 6 and 9 recorded on an 11-point scale where 0 = no pain and 10 = pain as bad as you can imagine. Negative change indicates an improvement in pain. (NCT01124604)
Timeframe: Baseline, Week 12
| Intervention | Units on a scale (Mean) | |
|---|---|---|
| Total Score; Baseline (n=60, 31) | Total Score; Change at Week 12 (n=45, 29) | |
| Placebo | 5.7 | -2.3 |
| Tapentadol Hydrochloride | 5.4 | -2.4 |
Participants were asked to assess the average pain intensity on a 11-point NRS ranging from 0 (no pain) to 10 (maximum pain imaginable) by selecting a number applicable to their pain on the scale. The mean pain intensity during the past 74 hours (3 days) was evaluated at Baseline and the mean pain intensity during the past 12 hours was evaluated at subsequent study visits. (NCT01124604)
Timeframe: Baseline, Week 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11
| Intervention | Units on a scale (Mean) | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Change at Week 1 | Change at Week 2 | Change at Week 3 | Change at Week 4 | Change at Week 5 | Change at Week 6 | Change at Week 7 | Change at Week 8 | Change at Week 9 | Change at Week 10 | Change at Week 11 | |
| Placebo | -0.7 | -1.3 | -1.6 | -1.8 | -2.0 | -2.3 | -2.6 | -2.6 | -2.7 | -2.8 | -2.9 |
| Tapentadol Hydrochloride | -0.6 | -1.1 | -1.5 | -1.9 | -2.4 | -2.7 | -2.7 | -2.8 | -2.9 | -2.9 | -3.0 |
"Time slept was addressed by the question: How long did you sleep last night? and the change from Baseline in time slept was reported." (NCT01124604)
Timeframe: Baseline, Week 12
| Intervention | Hours (Mean) |
|---|---|
| Tapentadol Hydrochloride | 0.1 |
| Placebo | 0.2 |
"Sleep Latency was addressed by the question: How long after bedtime/lights out did you fall asleep last night? and the change from Baseline in sleep latency was reported. Decrease in time indicated improvement." (NCT01124604)
Timeframe: Baseline, Week 12
| Intervention | Minutes (Mean) |
|---|---|
| Tapentadol Hydrochloride | 1.0 |
| Placebo | 1.2 |
Percentage of participants with improvement in mean NRS score by greater than or equal to 30 percent or 50 percent in the last week from Baseline were considered as responders. Participants were asked to assess the average pain intensity on a 11-point NRS ranging from 0 (no pain) to 10 (maximum pain imaginable) by selecting a number applicable to their pain on the scale. (NCT01124604)
Timeframe: Week 12
| Intervention | Percentage of participants (Number) | |
|---|---|---|
| Greater than or equal to 30 percent improvement | Greater than or equal to 50 percent improvement | |
| Placebo | 61.3 | 48.4 |
| Tapentadol Hydrochloride | 55.0 | 40.0 |
"Physician's Global Assessment Scale assesses the therapeutic efficacy (effectiveness) of the study drug for pain control on a 2-point scale of effective and not effective." (NCT01124604)
Timeframe: Week 8, Week 12
| Intervention | Participants (Number) | |||
|---|---|---|---|---|
| Week 8; Effective (n=47, 29) | Week 8; Not effective (n=47, 29) | Week 12; Effective (n=45, 29) | Week 12; Not effective (n=45, 29) | |
| Placebo | 24 | 5 | 21 | 8 |
| Tapentadol Hydrochloride | 41 | 6 | 40 | 5 |
COWS is an 11-item questionnaire for clinical assessment of withdrawal symptoms. Total score is calculated by adding the scores of all the 11-items. The severity of withdrawal symptoms is categorized using values of total score as: 0-4 = no withdrawal, 5-12 = mild, 13-24 = moderate, 25-36 = moderately severe, and 37-48 = severe withdrawal. (NCT01124604)
Timeframe: Week 12
| Intervention | Participants (Number) | ||||
|---|---|---|---|---|---|
| No Withdrawal | Mild | Moderate | Moderately Severe | Severe Withdrawal | |
| Placebo | 31 | 0 | 0 | 0 | 0 |
| Tapentadol Hydrochloride | 60 | 0 | 0 | 0 | 0 |
Participants were asked to assess the average pain intensity on a 11-point NRS ranging from 0 (no pain) to 10 (maximum pain imaginable) by selecting a number applicable to their pain on the scale. The mean pain intensity during the past 74 hours (3 days) was evaluated at Baseline and the mean pain intensity during the past 12 hours was evaluated at subsequent study visits. (NCT01124604)
Timeframe: Baseline, Week 12
| Intervention | Units on a scale (Mean) | |
|---|---|---|
| Baseline | Change at Week 12 | |
| Placebo | 6.9 | -2.9 |
| Tapentadol Hydrochloride | 6.9 | -3.0 |
"BPI-sf is a self-evaluated pain assessment form consisting of 15 items (item 1 - presence of pain, item 2 - pain location, items 3 to 6 - pain severity, item 7 - status of pain treatment, item 8 - efficacy of pain treatment, and items 9a to 9g - interference of pain with daily life). Item 1 for presence of pain assesses the question: Do you have any pain today other than everyday kinds of pain? on a 2-point scale of yes or no." (NCT01124604)
Timeframe: Baseline, Week 12
| Intervention | Participants (Number) | |
|---|---|---|
| Baseline (n=60,31) | Week 12 (n=45, 29) | |
| Placebo | 25 | 21 |
| Tapentadol Hydrochloride | 46 | 25 |
"RDQ scale is used to assess the impact of low back pain on daily activities by participants. The scale consists of 24 item questionnaire with options as Yes/No where Yes is counted as 1 point. The total score ranged from 0 to 24, with higher scores indicating greater disability." (NCT01124604)
Timeframe: Baseline, Week 12
| Intervention | Units on a scale (Mean) | |
|---|---|---|
| Baseline (n=33, 18) | Change at Week 12 (n=25, 16) | |
| Placebo | 12.7 | -1.8 |
| Tapentadol Hydrochloride | 11.7 | -3.3 |
The PGIC is a 7-point scale that requires the participants to assess how much their illness has improved or worsened relative to a Baseline state at the beginning of the intervention. The response options are 1 = very much improved, 2 = much improved, 3 = minimally improve, 4 = no change, 5 = minimally worse, 6 = much worse, and 7 = very much worse. (NCT01124617)
Timeframe: Week 8 and Week 12
| Intervention | Participants (Number) | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Week 8: Very Much Improved (n = 46, 26) | Week 8: Much Improved (n = 46, 26) | Week 8: Minimally Improved (n = 46, 26) | Week 8: No Change (n = 46, 26) | Week 8: Minimally Worse (n = 46, 26) | Week 8: Much Worse (n = 46, 26) | Week 8: Very Much Worse (n = 46, 26) | Week 12: Very Much Improved (n = 40, 25) | Week 12 : Much Improved (n = 40, 25) | Week 12 : Minimally Improved (n = 40, 25) | Week 12 : No Change (n = 40, 25) | Week 12 : Minimally Worse (n = 40, 25) | Week 12 : Much Worse (n = 40, 25) | Week 12 : Very Much Worse (n = 40, 25) | |
| Placebo | 4 | 7 | 10 | 2 | 2 | 1 | 0 | 2 | 9 | 11 | 2 | 0 | 1 | 0 |
| Tapentadol | 7 | 16 | 16 | 6 | 1 | 1 | 0 | 6 | 18 | 13 | 2 | 0 | 1 | 0 |
"Physician's Global Assessment Scale assesses the therapeutic efficacy (effectiveness) of the study drug for pain control on a 2-point scale of effective and ineffective." (NCT01124617)
Timeframe: Week 8 and Week 12
| Intervention | Participants (Number) | |||
|---|---|---|---|---|
| Week 8: Effective (n = 46, 26) | Week 8: Ineffective (n = 46, 26) | Week 12: Effective (n = 40, 25) | Week 12 : Ineffective (n = 40, 25) | |
| Placebo | 19 | 7 | 20 | 5 |
| Tapentadol | 41 | 5 | 35 | 5 |
Participants rated the overall quality of sleep last night as excellent, good, fair and poor. (NCT01124617)
Timeframe: Baseline and Week 12
| Intervention | Participants (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| Baseline: Excellent (n=60,31) | Baseline: Good (n=60,31) | Baseline: Fair (n=60,31) | Baseline: Poor (n=60,31) | Week 12 : Excellent (n=60,31) | Week 12 : Good (n=40,25) | Week 12 : Fair (n=40,25) | Week 12 : Poor (n=40,25) | |
| Placebo | 1 | 12 | 16 | 2 | 0 | 17 | 8 | 0 |
| Tapentadol | 0 | 35 | 22 | 3 | 4 | 28 | 6 | 2 |
Percentage of participants with treatment response in mean NRS score by greater than equal to 30 or 50 percent (%) in the last week from baseline were considered as responders. Participants were asked to assess the average pain intensity on an 11-point NRS ranging from 0 (no pain) to 10 (maximum pain imaginable) by selecting a number applicable to their pain on the scale. (NCT01124617)
Timeframe: Week 12
| Intervention | Percentage of participants (Number) | |
|---|---|---|
| Greater than or equal to 30% treatment response | Greater than or equal to 50% treatment response | |
| Placebo | 41.9 | 38.7 |
| Tapentadol | 48.3 | 33.3 |
The SF-36v2 is 36-item form related to 8 health concepts (physical functioning, role physical, role emotional, general health, social functioning, bodily pain, vitality, mental health) and 2 summary scores (physical and mental component summary). Physical functioning, role physical and bodily pain contribute to physical component; role emotional, social functioning and mental health contribute to mental component; and social functioning, vitality, and general health contribute to both. All scores are based on a scale from 0 to 100, with higher scores defining more favorable health state. (NCT01124617)
Timeframe: Baseline and Week 12
| Intervention | Units on a scale (Mean) | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Physical Functioning: Baseline (n=60,31) | Role-Physical: Baseline (n=60,31) | Bodily Pain: Baseline (n=60,31) | General Health: Baseline (n=60,31) | Vitality: Baseline (n=60,31) | Social Functioning: Baseline (n=60,31) | Role-Emotional: Baseline (n=60,31) | Mental Health: Baseline (n=60,31) | Mental Summary: Baseline (n=60,31) | Physical Summary: Baseline (n=60,31) | Physical Functioning: Change at Week 12 (n=40,25) | Role-Physical: Change at Week 12 (n=40,25) | Bodily Pain: Change at Week 12 (n=40,25) | General Health: Change at Week 12 (n=40,25) | Vitality: Change at Week 12 (n=40,25) | Social Functioning: Change at Week 12 (n=40,25) | Role-Emotional: Change at Week 12 (n=40,25) | Mental Health: Change at Week 12 (n=40,25) | Mental Summary: Change at Week 12 (n=40,25) | Physical Summary: Change at Week 12 (n=40,25) | |
| Placebo | 61.0 | 64.3 | 38.8 | 44.7 | 50.4 | 80.2 | 68.5 | 61.8 | 47.6 | 31.7 | 4.8 | 4.8 | 7.0 | 0.2 | 6.8 | 2.0 | 5.7 | 9.0 | 3.3 | 2.8 |
| Tapentadol | 68.6 | 70.1 | 36.2 | 45.7 | 48.8 | 72.9 | 68.9 | 57.6 | 43.9 | 36.0 | 5.4 | 6.6 | 10.5 | -0.4 | 9.4 | 8.1 | 6.0 | 7.8 | 4.5 | 4.4 |
Participants were asked to assess the average pain intensity on an 11-point NRS ranging from 0 (no pain) to 10 (maximum pain imaginable) by selecting a number on the scale applicable to their pain. Baseline pain score is defined as the average pain intensity score over the last 3 days prior to the randomization. Change from Baseline in NRS score is the mean NRS score at corresponding week minus mean NRS score at Baseline. (NCT01124617)
Timeframe: Baseline, Week 1, 2, 3, 4, 5, 6, 7, 8, 9, 10 and 11
| Intervention | Units on a scale (Mean) | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Change at Week 1 | Change at Week 2 | Change at Week 3 | Change at Week 4 | Change at Week 5 | Change at Week 6 | Change at Week 7 | Change at Week 8 | Change at Week 9 | Change at Week 10 | Change at Week 11 | |
| Placebo | -0.2 | -0.9 | -1.1 | -1.6 | -1.7 | -2.0 | -2.2 | -2.4 | -2.4 | -2.6 | -2.4 |
| Tapentadol | -0.7 | -1.1 | -1.5 | -1.8 | -2.1 | -2.3 | -2.3 | -2.4 | -2.5 | -2.6 | -2.6 |
Participants were asked to assess the average pain intensity on an 11-point NRS ranging from 0 (no pain) to 10 (maximum pain imaginable) by selecting a number on the scale applicable to their pain. Baseline pain score is defined as the average pain intensity score over the last 3 days prior to the randomization. Change from Baseline in NRS score is the mean NRS score at Week 12 minus mean NRS score at Baseline. (NCT01124617)
Timeframe: Baseline and Week 12
| Intervention | Units on a scale (Mean) | |
|---|---|---|
| Baseline | Change at Week 12 | |
| Placebo | 6.9 | -2.6 |
| Tapentadol | 6.7 | -2.6 |
The BPI-sf consists of 15 Items (Item 1:presence of pain; Item 2:pain location; Items 3 to 6:pain severity; Item 7:status of pain treatment; Item 8:efficacy of pain treatment; and Items 9a to 9g: interference of pain with daily life). Total score is defined as the mean scores from Items 3, 4, 5, 6 and 9 recorded on an 11-point scale where 0 = no pain and 10 = pain as bad as you can imagine. Lower score indicates an improvement in pain. (NCT01124617)
Timeframe: Baseline and Week 12
| Intervention | Units on a scale (Mean) | |
|---|---|---|
| Baseline (n=60,31) | Change at Week 12 (n=40,25) | |
| Placebo | 5.2 | -2.3 |
| Tapentadol | 5.2 | -2.7 |
The BPI-sf consists of 15 Items (Item 1:presence of pain; Item 2:pain location; Items 3 to 6:pain severity; Item 7:status of pain treatment; Item 8:efficacy of pain treatment; and Items 9a to 9g: interference of pain with daily life). Pain interference sub-scale score ranges from 0 (do not interfere) to 10 (completely interferes). Higher scores indicates worsening. Total score is defined as the mean scores from Items 3, 4, 5, 6 and 9 recorded on an 11-point scale where 0 = no pain and 10 = pain as bad as you can imagine. Lower score indicates an improvement in pain. (NCT01124617)
Timeframe: Baseline and Week 12
| Intervention | Units on a scale (Mean) | |
|---|---|---|
| Baseline (n=60, 31) | Week 12 (n=25,40) | |
| Placebo | 4.6 | -2.1 |
| Tapentadol | 4.7 | -2.6 |
The BPI-sf consists of 15 Items (Item 1:presence of pain; Item 2:pain location; Items 3 to 6:pain severity; Item 7:status of pain treatment; Item 8:efficacy of pain treatment; and Items 9a to 9g: interference of pain with daily life). Pain Sub-scale score ranges from 0 (absent [no pain]) to 10 (extreme [pain as bad as you can image]). Higher scores indicates worsening. Total score is defined as the mean scores from Items 3, 4, 5, 6 and 9 recorded on an 11-point scale where 0 = no pain and 10 = pain as bad as you can imagine. Lower score indicates an improvement in pain. (NCT01124617)
Timeframe: Baseline and Week 12
| Intervention | Units on a scale (Mean) | |
|---|---|---|
| Baseline (n=60, 31) | Week 12 (n=25,40) | |
| Placebo | 6.3 | -2.6 |
| Tapentadol | 6.2 | -3.0 |
"Sleep Latency was related to How long after bedtime or lights out did the participant fall asleep last night . Decrease in time indicates an improvement." (NCT01124617)
Timeframe: Baseline and Week 12
| Intervention | Minutes (Mean) | |
|---|---|---|
| Baseline (n=60, 30) | Change at Week 12 (n=40, 24) | |
| Placebo | 34.7 | -3.1 |
| Tapentadol | 45.4 | -11.1 |
"Time slept was related to How long did the participant sleep last night. The mean change for the time in hours slept during the last night was reported." (NCT01124617)
Timeframe: Baseline and Week 12
| Intervention | Hours (Mean) | |
|---|---|---|
| Baseline (n=60, 31) | Change at Week 12 (n=40,25) | |
| Placebo | 6.4 | 0.3 |
| Tapentadol | 5.8 | 0.3 |
"Number of awakenings was related to How many times did the participant wake up during the night. Lesser number signifies better sleep." (NCT01124617)
Timeframe: Baseline and Week 12
| Intervention | Participants (Number) | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline: 0 awakening (n=60,30) | Baseline: 1 awakening (n=60,30) | Baseline: 2 awakenings (n=60,30) | Baseline: 3 awakenings (n=60,30) | Baseline: 4 awakenings (n=60,30) | Baseline: > or = 5 awakenings (n=60,30) | Week 12 : 0 awakening (n=40,25) | Week 12 : 1 awakening (n=40,25) | Week 12 : 2 awakenings (n=40,25) | Week 12 : 3 awakenings (n=40,25) | Week 12 : 4 awakenings (n=40,25) | Week 12 : > or = 5 awakenings (n=40,25) | |
| Placebo | 3 | 9 | 10 | 6 | 1 | 1 | 3 | 8 | 7 | 4 | 2 | 1 |
| Tapentadol | 17 | 16 | 10 | 8 | 5 | 4 | 12 | 14 | 9 | 1 | 3 | 1 |
Participant-based analysis of treatment emergent adverse events (TEAEs) regarding countermeasure to the study drug (tapentadol). The TEAEs were reported by the participants or were captured by the investigator. The countermeasure taken by the investigator were reported. (NCT01264887)
Timeframe: Day 1; up to 144 weeks
| Intervention | participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| All Treatment Emergent Events | No Treatment Emergent Adverse Events | No countermeasures taken | Countermeasures with Medication | Trial Discontinued Countermeasure | Other Countermeasure due to Somnolence | Other Countermeasure due to Migraine | |
| Tapentadol Prolonged Release | 30 | 1 | 5 | 17 | 6 | 1 | 1 |
The number of days that participants took tapentadol prolonged release. The extent of exposure was categorized into 2 periods, less than 90 days and more than 90 days (up to 144 weeks). (NCT01264887)
Timeframe: Day 1; up to 144 weeks
| Intervention | participants (Number) | |
|---|---|---|
| 0 to 90 days | more than 90 days | |
| Tapentadol Prolonged Release | 11 | 20 |
"The participant scored their pain intensity on an 11-point Numerical Rating Scale (NRS) where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine.~Average pain intensity score is the average of pain experienced for previous 24 hours as rated on an 11-point NRS at each visit. Calculations are based on 3 consecutive planned (at 4-weekly intervals) visits.~All available data of a participant was used; if a participant dropped-out or had incomplete data during a 12-week period no imputations were performed for the missing values." (NCT01264887)
Timeframe: Day 1; up to Week 144
| Intervention | units on a scale (Mean) | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline | Week 1 to 12 | Week 13 to 24 | Week 25 to 36 | Week 37 to 48 | Week 49 to 60 | Week 61 to 72 | Week 73 to 84 | Week 85 to 96 | Week 97 to 108 | Week 109 to 120 | Week 121 to 132 | Week 133 to 144 | |
| Tapentadol Prolonged Release | 3.3 | 3.1 | 3.1 | 2.1 | 2.0 | 2.0 | 2.0 | 2.4 | 3.1 | 3.1 | 3.3 | 1.0 | 1.0 |
The Total Daily Dose (TDD) on any given day is the sum of the morning and evening intake amounts. The average TDD is an individuals average over the trial period. (NCT01264887)
Timeframe: Day 1; up to 144 weeks
| Intervention | mg per day (Mean) |
|---|---|
| Tapentadol Prolonged Release | 360 |
Summary of the modal total daily dose during the treatment period. The modal dose was based on assessment of the consecutive morning and evening intake amounts on each day and evaluation of the total daily dose. (NCT01264887)
Timeframe: Day 1; up to 144 weeks
| Intervention | participants (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| less than 200 mg/day | 200 to less than 250 mg/day | 250 to less than 300 mg/day | 300 to less than 350 mg/day | 350 to less than 400 mg/day | 400 to less than 450 mg/day | 450 to less than 500 mg/day | 500 mg/day | |
| Tapentadol Prolonged Release | 0 | 3 | 1 | 8 | 0 | 11 | 0 | 8 |
"Participant-based analysis of treatment emergent adverse events (TEAEs) regarding the relationship to the study drug (tapentadol). The TEAEs were reported by the participants or were captured by the investigator. The relationship was rated by the investigator. The categorization of relatedness into one of the two categories was based on the following: Related included possible, probable/likely, and certain; whilst unrelated treatment emergent adverse events include those rated by the investigator as unlikely, conditional/unclassified, un-assessable/unclassifiable, and not related." (NCT01264887)
Timeframe: Day 1; up to 144 weeks
| Intervention | participants (Number) | |||
|---|---|---|---|---|
| No Treatment Emergent Adverse Events | All Treatment Emergent Adverse Events | Investigator-rated Related | Investigator-rated Not Related | |
| Tapentadol Prolonged Release | 1 | 30 | 6 | 24 |
"The severity of treatment emergent adverse events was any untoward medical occurrence in a patient administered tapentadol. An adverse event can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding, for example), symptom, or disease temporally associated with the use of the (investigational) medicinal product whether or not related to the use of tapentadol.~The clinical intensity of adverse event were classified as:~Mild: signs and symptoms which can be easily tolerated. Symptoms could be ignored and disappeared when the participant is distracted.~Moderate: symptoms caused discomfort but were tolerable, they could not be ignored and affect concentration.~Severe: symptoms affected the usual daily activity." (NCT01264887)
Timeframe: Day 1; up to 144 weeks
| Intervention | participants (Number) | ||
|---|---|---|---|
| mild intensity | moderate intensity | severe intensity | |
| Number of Treatment Emergent Adverse Events | 3 | 15 | 12 |
Average pain intensity was assessed using an 11-point NRS to measure the pain level for the past 24-hours where 0=no pain to 10=pain as bad as you can imagine. (NCT01309386)
Timeframe: Baseline, Week 1, 2, 3, 4, 5, 6, 7, 8
| Intervention | Unit on scale (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Change at Week 1 (n = 50, 50) | Change at Week 2 (n = 45, 44) | Change at Week 3 (n= 41, 41) | Change at Week 4 (n = 38, 37) | Change at Week 5 (n = 36, 34) | Change at Week 6 (n = 36, 32) | Change at Week 7 (n = 34, 29) | Change at Week 8 (n = 29, 29) | |
| Morphine SR | -0.2 | -0.3 | -0.1 | -0.3 | -0.1 | 0.1 | 0.1 | 0.0 |
| Tapentadol ER | 0.4 | 0.3 | 0.1 | 0.1 | 0.1 | 0.2 | 0.1 | 0.0 |
Total number of days of rescue medication over time were assessed. Rescue medications are medicines that are administered to the participants when the efficacy of the study drug is not satisfactory, or the effect of the study drug is too great and is likely to cause a hazard to the participant, or to manage an emergency situation. Supplemental analgesics (drug used to control pain) were used as rescue medication. (NCT01309386)
Timeframe: Baseline up to Week 8
| Intervention | Days (Mean) |
|---|---|
| Tapentadol ER | 15.9 |
| Morphine SR | 9.2 |
Pain control was considered to be achieved for participants who met both of the following criteria for any consecutive 3 days during the first week of treatment period: a) Change from baseline of mean 24 hour numerical rating scale (NRS) (an 11-point NRS is used to measure the pain level where 0=no pain to 10=pain as bad as you can imagine) score less than +1.5, and b) when the frequency of rescue medication was twice or less per day. (NCT01309386)
Timeframe: Week 1
| Intervention | Percentage of Participants (Number) |
|---|---|
| Tapentadol ER | 84.0 |
| Morphine SR | 98.0 |
Number of participants who discontinued the treatment due to lack of efficacy were assessed throughout the study. (NCT01309386)
Timeframe: Baseline up to Week 8
| Intervention | Participants (Number) |
|---|---|
| Tapentadol ER | 3 |
| Morphine SR | 1 |
Number of doses of rescue medication over time were assessed. Rescue medications are medicines that are administered to the participants when the efficacy of the study drug is not satisfactory, or the effect of the study drug is too great and is likely to cause a hazard to the participant, or to manage an emergency situation. Supplemental analgesics (drug used to control pain) were used as rescue medication. (NCT01309386)
Timeframe: Baseline up to Week 8
| Intervention | Morphine-equivalent doses (Mean) |
|---|---|
| Tapentadol ER | 0.7 |
| Morphine SR | 0.4 |
Rescue medications are medicines that are administered to the participants when the efficacy of the study drug is not satisfactory, or the effect of the study drug is too great and is likely to cause a hazard to the participant, or to manage an emergency situation. Supplemental analgesics (drug used to control pain) were used as rescue medication. Average amount was the averages of all doses recorded during the baseline period or during each week (Week 1, 2, 3, 4, 5, 6, 7 and 8). (NCT01309386)
Timeframe: Baseline, Week 1, 2, 3, 4, 5, 6, 7, 8
| Intervention | Milligram (mg) (Mean) |
|---|---|
| Tapentadol ER | 3.02 |
| Morphine SR | -0.15 |
"The PGIC is a single-item questionnaire designed to provide an overall assessment of treatment from the participant's perspective since the start of the study. It is measured on a 7-point scale, where 1=very much improved and 7=very much worse. A participant is considered a responder if they have a response of very much improved or much improved." (NCT01309386)
Timeframe: Week 1, 4 and 8
| Intervention | Participants (Number) | ||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Week 1 (very much improved) (n=48,48) | Week 1 (much improved) (n=48,48) | Week 1 (minimally improved) (n=48,48) | Week 1 (not changed) (n=48,48) | Week 1 (minimally worse) (n=48,48) | Week 1 (much worse) (n=48,48) | Week 1 (very much worse) (n=48,48) | Week 4 (very much improved) (n=37,37) | Week 4 (much improved) (n=37,37) | Week 4 (minimally improved) (n=37,37) | Week 4 (not changed) (n=37,37) | Week 4 (minimally worse) (n=37,37) | Week 4 (much worse) (n=37,37) | Week 4 (very much worse) (n=37,37) | Week 8 (very much improved) (n=28,28) | Week 8 (much improved) (n=28,28) | Week 8 (minimally improved) (n=28,28) | Week 8 (not changed) (n=28,28) | Week 8 (minimally worse) (n=28,28) | Week 8 (much worse) (n=28,28) | Week 8 (very much worse) (n=28,28) | |
| Morphine SR | 2 | 4 | 7 | 29 | 6 | 0 | 0 | 3 | 5 | 7 | 19 | 3 | 0 | 0 | 3 | 2 | 4 | 13 | 4 | 2 | 0 |
| Tapentadol ER | 1 | 1 | 11 | 24 | 9 | 2 | 0 | 1 | 2 | 9 | 22 | 3 | 0 | 0 | 0 | 3 | 8 | 15 | 2 | 0 | 0 |
The sleep evaluation questionnaire was completed by the participant. The participant was asked: How long after bedtime/lights out did you fall asleep last night [hours]? The values are for the night prior to the visits. The negative change from baseline indicates that the time to falling asleep decreased from baseline in a treatment group. (NCT01352741)
Timeframe: Baseline Visit (Day 1); Randomization Visit (Day 22) to Final Evaluation Visit (Day 77)
| Intervention | hours (Mean) | |
|---|---|---|
| Change from baseline visit | Change from randomization visit | |
| Tapentadol Prolonged Release | -0.3 | 0.2 |
| Tapentadol Prolonged Release and Pregabalin | -0.3 | -0.2 |
"The sleep evaluation questionnaire was completed by the participant. The questionnaire measures 4 main concepts: 1 of the 4 main concepts being the number of awakenings.~The participant was asked: How long did you sleep last night? [Answered in hours and minutes]." (NCT01352741)
Timeframe: Enrollment Visit (Day-12); Baseline Visit (Day 1); Randomization Visit (Day 22)
| Intervention | hours (Mean) |
|---|---|
| Enrollment Visit (Day -12) | 5.8 |
| Baseline Visit (Day 1) | 5.3 |
| Randomization Visit (Day 22) | 6.4 |
"The sleep evaluation questionnaire was completed by the participant. The questionnaire measures 4 main concepts: 1 of the 4 main concepts being the number of awakenings.~How many times did you wake up during the night? The values were calculated from the data that participants self-reported for the night prior to their Randomization Visit (Baseline), for the night prior to the Baseline Visit (Day 1) and the night prior to the Randomization Visit (Day 22).~The participant was asked at each visit: How many times did you wake up during the night?" (NCT01352741)
Timeframe: Enrollment Visit (Day-12); Baseline Visit (Day 1); Randomization Visit (Day 22)
| Intervention | Number of Awakenings (Mean) |
|---|---|
| Enrollment Visit (Day -12) | 3.3 |
| Baseline Visit (Day 1) | 3.9 |
| Randomization Visit (Day 22) | 2.5 |
"The sleep evaluation questionnaire was completed by the participant. The questionnaire measures 4 main concepts: 1 of the 4 main concepts being the sleep latency.~To assess latency the participant was asked: How long after bedtime/lights out did you fall asleep last night [hours]?" (NCT01352741)
Timeframe: Enrollment Visit (Day-12); Baseline Visit (Day 1); Randomization Visit (Day 22)
| Intervention | hours (Mean) |
|---|---|
| Enrollment Visit (Day -12) | 1.2 |
| Baseline Visit (Day 1) | 1.5 |
| Randomization Visit (Day 22) | 1.3 |
"The recalled average pain intensity score on the NRS-3 was assessed using an 11-point Numeric Rating Scale (NRS). This scale recalls the average pain intensity during the last 3 days. The participant was asked: Please rate your pain intensity by assessing the one number that best describes your pain on average during the last 3 days (the last 72 hours prior to the visit). Where 0 = no pain and 10 indicates pain as bad as you can imagine." (NCT01352741)
Timeframe: Final Evaluation Visit (Day 77)
| Intervention | units on a scale (Mean) |
|---|---|
| Tapentadol Prolonged Release After Tapentadol | 4.4 |
| Tapentadol Prolonged Release After Tapentadol and Pregabalin | 4.5 |
"The recalled worst pain intensity during the last 24 hours was assessed using an 11-point Numeric rating scale, where 0 = no pain and 10 = pain as bad as you can imagine.~The participant was asked: Please rate your pain intensity by assessing the one number that best describes your worst pain during the last 24 hours prior to the visit.~A negative change indicates that the pain intensity decreased from the start of the trial." (NCT01352741)
Timeframe: Randomization Visit (Day 22); Final Evaluation Visit (Day 77)
| Intervention | units on a scale (Mean) |
|---|---|
| Tapentadol Prolonged Release | -1.7 |
| Tapentadol Prolonged Release and Pregabalin | -1.8 |
"The sleep evaluation questionnaire was completed by the participant. The questionnaire measures 4 main concepts: 1 of the 4 main concepts being the overall quality of sleep.~The participant rated this categorically as being one of the following: excellent, good, fair or poor." (NCT01352741)
Timeframe: Enrollment Visit (Day-12); Baseline Visit (Day 1); Randomization Visit (Day 22)
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| Excellent | Good | Fair | Poor | Missing | |
| Baseline Visit (Day 1) | 5 | 76 | 149 | 210 | 5 |
| Enrollment Visit (Day -12) | 9 | 110 | 171 | 148 | 7 |
| Randomization Visit (Day 22) | 21 | 173 | 127 | 56 | 68 |
"NRS-3 pain intensity score (recalled average pain intensity score during the last 3 days on 11-point NRS, where 0 is the no pain and 10 is pain as bad as you can imagine) for radiating pain (pain radiating into or towards the leg, typically of shooting, radiating character, usually radiating below the knee towards the foot).~The value reported represents the change from the randomization visit (i.e., the last 3 days in the titration period) to the end of the double-blind comparative period (i.e., the last 3 days in the comparative period). The theoretical values range from -10 to 10. A negative sign indicates a decrease in pain from the start of treatment. The higher the absolute values, the greater the change since the start of treatment (baseline visit)." (NCT01352741)
Timeframe: Randomization Visit (Day 22); End of Evaluation Visit (Day 77)
| Intervention | units on a scale (Mean) |
|---|---|
| Tapentadol Prolonged Release | -1.5 |
| Tapentadol Prolonged Release and Pregabalin | -1.9 |
"The recalled worst pain intensity during the last 24 hours was assessed using an 11-point Numeric rating scale, where 0 = no pain and 10 = pain as bad as you can imagine.~The participant was asked: Please rate your pain intensity by assessing the one number that best describes your worst pain during the last 24 hours prior to the visit." (NCT01352741)
Timeframe: Enrollment Visit (Day -14); Baseline Visit (Day 1); Randomization Visit (Day 22)
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| Enrollment Visit (N=438) | Baseline Visit (N=440) | Randomization Visit (N=377) | |
| Tapentadol Prolonged Release | 7.6 | 8.5 | 5.8 |
"The primary endpoint is defined as the comparison of tapentadol prolonged release (PR) 300 mg plus 200 mg per day and the combination of tapentadol PR 300 mg per day and pregabalin 300 mg per day regarding the change in NRS-3 pain intensity scores (recalled average pain intensity score during the last 3 days on 11-point NRS, where 0 is the no pain and 10 is pain as bad as you can imagine) from the randomization visit to the final evaluation visit.~Theoretically a maximum decrease of -10 and an increase of +4 in the pain intensity would have been possible. A negative sign indicates a decrease in pain intensity from the start of treatment. The higher the absolute values, the greater the change since the start of treatment (Baseline visit)." (NCT01352741)
Timeframe: Randomization (Day 22); Final Evaluation Visit (Day 77)
| Intervention | units on a scale (Mean) |
|---|---|
| Tapentadol Prolonged Release | -1.6 |
| Tapentadol Prolonged Release and Pregabalin | -1.7 |
"The Short Form Health Survey (SF-12) has several brief broad questions on 8 aspects of health (physical functioning, role physical, bodily pain, general health, vitality, social functioning, role-emotional and mental health) that a participant was asked to score over the last week. The physical summary scores were calculated from the individual responses to those questions covering physical health. A higher score indicates a better participant perceived state of health. All domains were scored on a scale from 0 (lowest level of health) to 100 (highest level of health), with 100 representing the best possible health state.~The change in the SF-12 score shows an improvement in health from baseline if the values are positive. The higher the value the greater the improvement." (NCT01352741)
Timeframe: Baseline Visit (Day 1); Randomization Visit (Day 22); Final Evaluation Visit (Day 77)
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Change from Baseline Visit | Change from Randomization Visit | |
| Tapentadol Prolonged Release | 12.3 | 6.2 |
| Tapentadol Prolonged Release and Pregabalin | 11.1 | 5.6 |
"Participants rated their satisfaction with the study drug (IMPs) by answering the following question on a 5-point rating scale:~How would you rate your overall satisfaction with your current pain treatment?: Excellent, Very Good, Good, Fair and Poor." (NCT01352741)
Timeframe: End of Open-label Titration Period at Randomization Visit (Day 22)
| Intervention | participants (Number) | |||||
|---|---|---|---|---|---|---|
| Poor | Fair | Good | Very Good | Excellent | Missing | |
| Tapentadol Prolonged Release | 12 | 119 | 178 | 58 | 11 | 67 |
"The sleep evaluation questionnaire was completed by the participant. The questionnaire measures 4 main concepts: 1 of the 4 main concepts being the overall quality of sleep.~The participant rated this categorically as being one of the following: excellent, good, fair or poor." (NCT01352741)
Timeframe: Randomization Visit (Day 22)
| Intervention | participants (Number) | |||
|---|---|---|---|---|
| Excellent | Good | Fair | Poor | |
| Tapentadol Prolonged Release | 7 | 62 | 48 | 22 |
| Tapentadol Prolonged Release and Pregabalin | 8 | 59 | 56 | 26 |
"The sleep evaluation questionnaire was completed by the participant. The questionnaire measures 4 main concepts: 1 of the 4 main concepts being the overall quality of sleep.~The participant rated this categorically as being one of the following: excellent, good, fair or poor." (NCT01352741)
Timeframe: Enrollment Visit (Day-12)
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| Excellent | Good | Fair | Poor | Missing | |
| Tapentadol Prolonged Release | 1 | 37 | 42 | 58 | 1 |
| Tapentadol Prolonged Release and Pregabalin | 5 | 30 | 61 | 53 | 0 |
"The sleep evaluation questionnaire was completed by the participant. The questionnaire measures 4 main concepts: 1 of the 4 main concepts being the overall quality of sleep.~The participant rated this categorically as being one of the following: excellent, good, fair or poor." (NCT01352741)
Timeframe: Baseline Visit (Day 1)
| Intervention | participants (Number) | |||
|---|---|---|---|---|
| Excellent | Good | Fair | Poor | |
| Tapentadol Prolonged Release | 2 | 23 | 42 | 72 |
| Tapentadol Prolonged Release and Pregabalin | 1 | 17 | 49 | 82 |
"The participants were requested to answer the following question:~How long did you sleep last night [hours]? The values were calculated from the data that participants self-reported for the night prior to their Randomization Visit (Baseline) and for the night prior to the End of the Continuation Visit (12 weeks after randomization)." (NCT01352741)
Timeframe: Enrollment Visit (Day -12); Baseline Visit (Day 1); Randomization Visit (Day 22)
| Intervention | hours (Mean) | ||
|---|---|---|---|
| Enrollment Visit (N=138, N=149) | Baseline Visit (N=139, N=149) | Randomization Visit (N=139, N=149) | |
| Tapentadol Prolonged Release | 5.8 | 5.3 | 6.2 |
| Tapentadol Prolonged Release and Pregabalin | 5.7 | 5.2 | 6.4 |
The sleep evaluation questionnaire was completed by the participant. The participant was asked: How long after bedtime/lights out did you fall asleep last night [hours]? The values are for the night prior to the Randomization Visit (Baseline) and for the night prior to the Final Evaluation Visit (12 weeks after randomization). The higher the value the longer it took to fall asleep. Sleep evaluation questionnaire (SQ) items (NCT01352741)
Timeframe: Enrollment Visit (Day -12); Baseline Visit (Day 1); Randomization Visit (Day 22)
| Intervention | hours (Mean) | ||
|---|---|---|---|
| Enrollment Visit (N=138, N=149) | Baseline Visit (N=139, N=149) | Randomization Visit (N=139, N=149) | |
| Tapentadol Prolonged Release | 1.3 | 1.5 | 1.1 |
| Tapentadol Prolonged Release and Pregabalin | 1.3 | 1.5 | 1.4 |
"The sleep evaluation questionnaire was completed by the participant. The questionnaire measures 4 main concepts: 1 of the 4 main concepts being the number of awakenings.~How many times did you wake up during the night? The values were calculated from the data that participants self-reported for the night prior to their Randomization Visit (Baseline), for the night prior to the Baseline Visit (Day 1) and the night prior to the Randomization Visit (Day 22).~The participant was asked at each visit: How many times did you wake up during the night?" (NCT01352741)
Timeframe: Enrollment Visit (Day-12); Baseline Visit (Day 1); Randomization Visit (Day 22)
| Intervention | Number of Awakenings (Mean) | ||
|---|---|---|---|
| Enrollment Visit (N=138; N=149) | Baseline Visit (N=139; N=149) | Randomization Visit (N=139; N=149) | |
| Tapentadol Prolonged Release | 3.2 | 3.6 | 2.5 |
| Tapentadol Prolonged Release and Pregabalin | 3.4 | 4.6 | 2.7 |
The NRS-3 pain intensity score at the visits in the open-label titration period for the two comparative double-blind period treatment groups analyzed is reported. NRS-3 pain intensity score (recalled average pain intensity score during the last 3 days on an 11-point NRS) for radiating pain (pain radiating into or towards the leg, typically of shooting, radiating character, usually radiating below the knee towards the foot) is reported. Where 0 = no pain and 10 indicates pain as bad as you can imagine. (NCT01352741)
Timeframe: Enrollment Visit (Day -14); Baseline Visit (Day 1); Randomization Visit (Day 22)
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| Enrollment Visit (N=438) | Baseline Visit (N=440) | Randomization Visit (N=377) | |
| Tapentadol Prolonged Release | 7.0 | 8.0 | 5.3 |
The NRS-3 pain intensity score at the visits in the open-label titration period for the two comparative double-blind period treatment groups analyzed is reported. NRS-3 pain intensity score (recalled average pain intensity score during the last 3 days on an 11-point NRS) for radiating pain (pain radiating into or towards the leg, typically of shooting, radiating character, usually radiating below the knee towards the foot) is reported. Where 0 = no pain and 10 indicates pain as bad as you can imagine. (NCT01352741)
Timeframe: Enrollment Visit (Day -14); Baseline Visit (Day 1); Randomization Visit (Day 22)
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| Enrollment Visit (N=138; N=149) | Baseline Visit (N=139; N=149) | Randomization Visit (N=139; N=149) | |
| Tapentadol Prolonged Release | 7.1 | 8.1 | 5.6 |
| Tapentadol Prolonged Release and Pregabalin | 6.9 | 8.1 | 5.7 |
"The painDETECT was a participant completed questionnaire. The questionnaire consists of 14 questions in four domains. Based on these questions a final assessment score was calculated. The minimum score ranged from zero to a maximum of 38. Participants with a score between 0 and 12 were scored as being negative (had no neuropathic pain component). A value between 19 and 38 was rated as being positive (neuropathic component present). Values from 13 to 18 were scored as being unclear." (NCT01352741)
Timeframe: Enrollment Visit (Day-12); Baseline Visit (Day 1); Randomization Visit (Day 22)
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| Enrollment Visit (N=438) | Baseline Visit (N=440) | Randomization Visit (N=377) | |
| Tapentadol Prolonged Release | 21.4 | 22.7 | 16.9 |
In the Neuropathic Pain Symptom Inventory (NPSI) the participant rated their symptoms of neuropathic pain. Ten pain questions were answered on an 11-point scale; from 0 (symptom not present) to 10 (symptom at its worst imaginable intensity, e.g. worst burning imaginable). The overall NPSI score was calculated by the summation of all ten responses and ranges between 0 and 100. For pain descriptions burning, pressing, paroxysmal (pain like electric shocks or stabbing), evoked (due to touch) and paresthesia (sensation that is not unpleasant) or dysesthesia (unpleasant) sub-scores are reported. The overall values reported for all participants that completed the questionnaire are shown. A symptom was absent if the value is 0, the symptom was present in all participants and all participants rated it at its worst possible intensity if a value is 100. (NCT01352741)
Timeframe: Enrollment Visit; Baseline Visit (Day 1); Randomization Visit (Day 22); Final Evaluation Visit (Day 77)
| Intervention | units on a scale (Mean) | |||
|---|---|---|---|---|
| Overall Score Enrollment Visit (N=138, N=149) | Overall Score Baseline Visit (N=139, N=149) | Overall Score Randomization Visit (N=139, N=149) | Overall Score Final Evaluation Visit(N=131, N=143) | |
| Tapentadol Prolonged Release | 54.8 | 62.8 | 45.2 | 28.9 |
| Tapentadol Prolonged Release and Pregabalin | 57.6 | 65.4 | 46.5 | 30.5 |
In the Neuropathic Pain Symptom Inventory (NPSI) the participant rated their symptoms of neuropathic pain. Ten pain questions were answered on an 11-point scale; from 0 (symptom not present) to 10 (symptom at its worst imaginable intensity, e.g. worst burning imaginable). The overall NPSI score was calculated by the summation of all ten responses and ranges between 0 and 100. For pain descriptions burning, pressing, paroxysmal (pain like electric shocks or stabbing), evoked (due to touch) and paresthesia (sensation that is not unpleasant) or dysesthesia (unpleasant) sub-scores are reported. The overall values reported for all participants that completed the questionnaire are shown. A symptom was absent if the value is 0, the symptom was present in all participants and all participants rated it at its worst possible intensity if a value is 100. (NCT01352741)
Timeframe: Enrollment Visit; Baseline Visit (Day 1); Randomization Visit (Day 22)
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| Overall Score Enrollment Visit (N=438) | Overall Score Baseline Visit (N=440) | Overall Score Randomization Visit (N=377) | |
| Tapentadol Prolonged Release | 55.2 | 62.7 | 42.0 |
The Hospital Anxiety and Depression Scale (HADS) is a self-assessment scale for the symptom severity of anxiety disorders and depression. It comprises 14 items. Seven statements describe depression. Each answer is scored on a four-point scale (0-3). All seven answers are summed to a total score with a maximum score of 21 points. A score below 7 is not considered to indicate depression. A score of 11 or above is considered to be a case of depression. A decrease in values over time indicates that there has been an improvement. (NCT01352741)
Timeframe: Enrollment Visit (Day-12); Baseline Visit (Day 1); Randomization Visit (Day 22)
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| Enrollment Visit (N=138; N=149) | Baseline Visit (N=139; N=149) | Randomization Visit (N=139; N=149) | |
| Tapentadol Prolonged Release | 6.9 | 7.6 | 6.0 |
| Tapentadol Prolonged Release and Pregabalin | 7.8 | 8.6 | 6.8 |
"The Hospital Anxiety and Depression Scale (HADS) is a self-assessment scale for the symptom severity of anxiety disorders and depression. It comprises 14 items. Seven statements describe anxiety. Each answer is scored on a four-point scale (0-3). All seven answers are summed to a total score with a maximum score of 21 points. A score below 7 is not considered to indicate anxiety. A score of 11 or above is considered to be a case of anxiety.~A decrease in values over the trial period indicate that there has been an improvement." (NCT01352741)
Timeframe: Enrollment Visit (Day-12); Baseline Visit (Day 1); Randomization Visit (Day 22)
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| Enrollment Visit (N=138; N=149) | Baseline Visit (N=139; N=149) | Randomization Visit (N=139; N=149) | |
| Tapentadol Prolonged Release | 7.4 | 7.7 | 5.8 |
| Tapentadol Prolonged Release and Pregabalin | 8.6 | 9.0 | 7.1 |
"The participant scored the EuroQol-5 questionnaire. The EuroQol-5 questionnaire uses a health state classification with 5 dimensions. Each dimension was assessed on a 3-point ordinal scale (1=no problems, 2=some problems, 3=extreme problems). The responses to the five EQ-5D dimensions were scored using a utility-weighted algorithm to derive an EQ-5D health status index score between 0 to 1 (with 1 indicating full health and 0 representing dead). The higher the values (the closer the value is to 1) the better the health status in a treatment group." (NCT01352741)
Timeframe: Enrollment Visit (day-12); Baseline Visit (Day 1); Randomization Visit (Day 22)
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| Enrollment Visit (N=138; N=149) | Baseline Visit (N=139; N=149) | Randomization Visit (N=139; N=149) | |
| Tapentadol Prolonged Release | 0.32 | 0.29 | 0.55 |
| Tapentadol Prolonged Release and Pregabalin | 0.33 | 0.18 | 0.52 |
"The recalled worst pain intensity during the last 24 hours was assessed using an 11-point Numeric Rating Scale (NRS), where 0 = no pain and 10 = pain as bad as you can imagine.~The participant was asked : Please rate your pain intensity by assessing the one number that best describes your worst pain during the past 24 hours prior to the visit." (NCT01352741)
Timeframe: Enrollment Visit (Day-12); Baseline Visit (day 1); Randomization Visit (Day 22)
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| Enrollment Visit (N=138; N=149) | Baseline Visit (N=139; N=149) | Randomization Visit (N=139; N=149) | |
| Tapentadol Prolonged Release | 7.8 | 8.5 | 6.3 |
| Tapentadol Prolonged Release and Pregabalin | 7.5 | 8.7 | 6.4 |
The Short Form Health Survey (SF-12) has several brief broad questions on 8 aspects of health (physical functioning, role physical, bodily pain, general health, vitality, social functioning, role-emotional and mental health) that a participant was asked to score over the last week. The physical and mental summary scores were calculated from the individual responses. A higher score indicates a better perceived state of health. All domains were scored on a scale from 0 (lowest level of health) to 100 (highest level of health), with 100 representing the best possible health state. (NCT01352741)
Timeframe: Enrollment Visit; Baseline Visit (Day 1); Randomization Visit (Day 22)
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| Enrollment Visit (N=138; N=149) | Baseline Visit (N=139; N=149) | Randomization Visit (N=139; N=149) | |
| Tapentadol Prolonged Release | 29.9 | 28.2 | 34.1 |
| Tapentadol Prolonged Release and Pregabalin | 29.8 | 28.5 | 34.1 |
The Short Form Health Survey (SF-12) has several brief broad questions on 8 aspects of health (physical functioning, role physical, bodily pain, general health, vitality, social functioning, role-emotional and mental health) that a participant was asked to score over the last week. The mental health summary scores were calculated from the individual responses to two of the 12 questions. A higher score indicates a better participant perceived state of health. All domains were scored on a scale from 0 (lowest level of health) to 100 (highest level of health), with 100 representing the best possible mental health. (NCT01352741)
Timeframe: Enrollment Visit; Baseline Visit (Day 1); Randomization Visit (Day 22)
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| Enrollment Visit (N=138; N=149) | Baseline Visit (N=139; N=149) | Randomization Visit (N=139; N=149) | |
| Tapentadol Prolonged Release | 46.1 | 45.4 | 49.2 |
| Tapentadol Prolonged Release and Pregabalin | 44.8 | 43.2 | 47.3 |
"The painDETECT was a participant completed questionnaire. The questionnaire consists of 14 questions in four domains. Based on these questions a final assessment score was calculated. The minimum score ranged from zero to a maximum of 38. Participants with a score between 0 and 12 were scored as being negative (had no neuropathic pain component). A value between 19 and 38 was rated as being positive (neuropathic component present). Values from 13 to 18 were scored as being unclear." (NCT01352741)
Timeframe: Enrollment Visit (Day-12); Baseline Visit (Day 1); Randomization Visit (Day 22)
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| Enrollment Visit (N=138; N=149) | Baseline Visit (N=139; N=149) | Randomization Visit (N=138; N=149) | |
| Tapentadol Prolonged Release | 21.6 | 22.4 | 17.6 |
| Tapentadol Prolonged Release and Pregabalin | 21.7 | 23.8 | 18.4 |
"The recalled average pain intensity score on the NRS-3 was assessed using an 11-point Numeric Rating Scale (NRS). This scale recalls the average pain intensity during the last 3 days. The participant was asked: Please rate your pain intensity by assessing the one number that best describes your pain on average during the last 3 days (the last 72 hours prior to the visit). Where 0 = no pain and 10 indicates pain as bad as you can imagine. This is the treatment period prior to the primary outcome period." (NCT01352741)
Timeframe: Enrollment (Day -14); Baseline Visit (Day 1); Randomization Visit (Day 22)
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| Enrollment Visit (N=438) | Baseline Visit (N=440) | Randomization Visit (N=377) | |
| Tapentadol Prolonged Release | 7.2 | 8.3 | 5.4 |
"The recalled average pain intensity score on the NRS-3 was assessed using an 11-point Numeric Rating Scale (NRS). This scale recalls the average pain intensity during the last 3 days. The participant was asked: Please rate your pain intensity by assessing the one number that best describes your pain on average during the last 3 days (the last 72 hours prior to the visit). Where 0 = no pain and 10 indicates pain as bad as you can imagine." (NCT01352741)
Timeframe: Enrollment (Day -14); Baseline Visit (Day 1); Randomization Visit (Day 22); Final Evaluation Visit (Day 77)
| Intervention | units on a scale (Mean) | |||
|---|---|---|---|---|
| Enrollment Visit (N=56) | Baseline Visit (N=57) | Randomization Visit (N=57) | Final Evaluation Visit (N=59) | |
| Tapentadol Prolonged Release | 7.3 | 7.9 | 2.6 | 2.6 |
"Participants rated their satisfaction with the study drug (IMPs) by answering the following question on a 5-point rating scale:~How would you rate your overall satisfaction with your current pain treatment?: Excellent, Very Good, Good, Fair and Poor." (NCT01352741)
Timeframe: End of Comparative Period at Final Evaluation Visit (Day 77)
| Intervention | participants (Number) | |||||
|---|---|---|---|---|---|---|
| Poor | Fair | Good | Very Good | Excellent | Missing | |
| Tapentadol and Pregabalin in the Comparative Period | 6 | 28 | 43 | 43 | 23 | 6 |
| Tapentadol in the Comparative Period | 3 | 32 | 43 | 32 | 21 | 8 |
The sleep evaluation questionnaire was completed by the participant. The answer was in response to the question: Sleep evaluation: How long did you sleep last night [hours]? The value reported is the change in the number of hours of sleep from baseline. The positive value indicates that there was an increase in the number of hours of sleep in a treatment group. (NCT01352741)
Timeframe: Baseline Visit (Day -12); Randomization Visit (Day 1); Final Evaluation Visit (Day 77)
| Intervention | hours (Mean) | |
|---|---|---|
| Change from baseline visit | Change from randomization visit | |
| Tapentadol Prolonged Release | 1.2 | 0.3 |
| Tapentadol Prolonged Release and Pregabalin | 1.6 | 0.3 |
The sleep evaluation questionnaire was completed by the participant. The questionnaire measures 4 main concepts: 1 of the 4 main concepts being the number of awakenings. Participants were asked: How many times did you wake up during the night? The change in the Number of Awakenings was calculated from the data that participants self-reported for the night prior to their Randomization Visit (Baseline), for the night prior to the Baseline Visit (Day 1) and the night prior to the Final Evaluation Visit (Day 77). A negative change indicates that the number of awakenings in a treatment group have gone down since the Baseline or Randomization Visit. In general pain can interfere with sleep, one potential indicator is the number of awakenings. (NCT01352741)
Timeframe: Baseline Visit (Day 1); Randomization Visit (Day 22) to Final Evaluation Visit (Day 77)
| Intervention | Number of Awakenings (Mean) | |
|---|---|---|
| Change from Baseline Visit | Change from Randomization Visit | |
| Tapentadol Prolonged Release | -1.4 | -0.2 |
| Tapentadol Prolonged Release and Pregabalin | -2.5 | -0.8 |
"In the Patient Global Impression of Change (PGIC) the participant indicated the perceived change over the treatment period. PGIC is a 7 point scale where the patient's rates overall improvement. Patients rate their change as very much improved, much improved, minimally improved, no change, minimally worse, much worse, or very much worse." (NCT01352741)
Timeframe: Randomization Visit (Day 22) to Final Evaluation Visit (Day 77)
| Intervention | participants (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| Very much improved | Much improved | Minimally improved | No change | Minimally worse | Much worse | Very much worse | Missing | |
| Tapentadol Prolonged Release | 28 | 44 | 51 | 10 | 5 | 4 | 0 | 10 |
| Tapentadol Prolonged Release and Pregabalin | 32 | 66 | 31 | 10 | 5 | 5 | 1 | 7 |
"In the Clinician Global Impression of Change (CGIC) the clinician indicated the perceived change over the treatment period. The clinician was requested to choose one of seven categories for each participant. The Clinician rated the participants change as very much improved, much improved, minimally improved, no change, minimally worse, much worse, or very much worse." (NCT01352741)
Timeframe: Randomization Visit (Day 22) to Final Evaluation Visit (Day 77)
| Intervention | participants (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| Very much improved | Much improved | Minimally improved | No change | Minimally worse | Much worse | Very much worse | Missing | |
| Tapentadol Prolonged Release | 26 | 54 | 46 | 8 | 3 | 5 | 0 | 10 |
| Tapentadol Prolonged Release and Pregabalin | 30 | 82 | 19 | 10 | 2 | 5 | 2 | 7 |
"The sleep evaluation questionnaire was completed by the participant. The questionnaire measures 4 main concepts: 1 of the 4 main concepts being the overall quality of sleep.~The improvement, no change or worsening is reported based on the replies scored by the participants given at their End of Continuation Visit." (NCT01352741)
Timeframe: Randomization Visit (Day 22) to Final Evaluation (Day 77)
| Intervention | participants (Number) | |||
|---|---|---|---|---|
| Improvement | No change | Worsening | Missing | |
| Tapentadol Prolonged Release | 39 | 63 | 21 | 16 |
| Tapentadol Prolonged Release and Pregabalin | 58 | 59 | 20 | 12 |
The Short Form Health Survey (SF-12) has several brief broad questions on 8 aspects of health (physical functioning, role physical, bodily pain, general health, vitality, social functioning, role-emotional and mental health) that a participant was asked to score over the last week. The mental health summary scores were calculated from the individual responses to two of the 12 questions. A higher score indicates a better participant perceived state of health. All domains were scored on a scale from 0 (lowest level of health) to 100 (highest level of health), with 100 representing the best possible mental health. (NCT01352741)
Timeframe: Baseline Visit (Day 1); Randomization Visit (Day 22); Final Evaluation Visit (Day 77)
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Change from Baseline Visit (N=131; N=143) | Change from Randomization Visit (N=131; N=143) | |
| Tapentadol Prolonged Release | 3.9 | 0.1 |
| Tapentadol Prolonged Release and Pregabalin | 6.5 | 2.5 |
"The painDETECT was a participant completed questionnaire. The questionnaire consists of 14 questions in four domains. Based on these questions a final assessment score was calculated. The minimum score ranged from zero to a maximum of 38. Participants with a score between 0 and 12 were scored as being negative (had no neuropathic pain component). A value between 19 and 38 was rated as being positive (neuropathic component present). Values from 13 to 18 were scored as being unclear. The theoretical range of change in this trial ranged from -38 to 19. A negative change indicated a decrease in their neuropathic component of pain." (NCT01352741)
Timeframe: Baseline Visit (Day 1); Randomization Visit (Day 22); Final Evaluation Visit (Day 77)
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Change from Baseline | Change from Randomization | |
| Tapentadol Prolonged Release | -10.2 | -6.0 |
| Tapentadol Prolonged Release and Pregabalin | -11.0 | -5.9 |
In the Neuropathic Pain Symptom Inventory (NPSI) the participant rated their symptoms of neuropathic pain. Ten pain questions were answered on an 11-point scale, from 0 (symptom not present) to 10 (symptom at its worst imaginable intensity, e.g. Spontaneous Pressing Pain Subscore). The overall NPSI score was calculated by the summation of all ten responses and ranges between 0 and 100. For pain descriptions burning, pressing, paroxysmal (pain like electric shocks or stabbing), evoked (due to touch) and paresthesia (sensation that is not unpleasant) or dysesthesia (unpleasant) subscores are reported. The overall values reported for all participants that completed the questionnaire are shown. A symptom was absent if the value is 0, the symptom was present in all participants and all participants rated it at its worst possible intensity if a value is 10 (100 for the overall score) . A negative change indicates that the intensity of the symptom has decreased since the start of treatment. (NCT01352741)
Timeframe: Randomization Visit (Day 22); Final Evaluation Visit (Day 77)
| Intervention | units on a scale (Mean) | |||||
|---|---|---|---|---|---|---|
| Overall Score | Subscore: Superficial Spontaneous Burning | Subscore: Deep Sponatenous Pressing Pain | Subscore: Paroxysmal Pain | Subscore: Evoked Pain | Subscore: Parasthesia/Dysesthesia | |
| Tapentadol Prolonged Release | -16.8 | -1.9 | -1.4 | -2.0 | -1.8 | -1.4 |
| Tapentadol Prolonged Release and Pregabalin | -16.6 | -2.3 | -1.4 | -1.6 | -1.7 | -1.5 |
The Hospital Anxiety and Depression Scale (HADS) is a self-assessment scale for the symptom severity of anxiety disorders and depression. It comprises 14 items. Seven statements describe depression. Each answer is scored on a four-point scale (0-3). All seven answers are summed to a total score with a maximum score of 21 points. A score below 7 is not considered to indicate depression. A score of 11 or above is considered to be a case of depression. A decrease in values over time indicates that there has been an improvement. A negative change value indicates a decrease in the depression score since the start of treatment. (NCT01352741)
Timeframe: Baseline Visit (Day 1); Randomization Visit (Day 22); Final Evaluation Visit (Day 77)
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Change from Baseline Visit | Change from Randomization Visit | |
| Tapentadol Prolonged Release | -2.0 | -0.4 |
| Tapentadol Prolonged Release and Pregabalin | -3.1 | -1.3 |
"The Hospital Anxiety and Depression Scale (HADS) is a self-assessment scale for the symptom severity of anxiety disorders and depression. It comprises 14 items. Seven statements describe anxiety. Each answer is scored on a four-point scale (0-3). All seven answers are summed to a total score with a maximum score of 21 points. A score below 7 is not considered to indicate anxiety. A score of 11 or above is considered to be a case of anxiety.~A negative sign indicates that there has been a decrease in anxiety since the start of treatment." (NCT01352741)
Timeframe: Baseline Visit (Day 1); Randomization Visit (Day 22); Final Evaluation Visit (Day 77)
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Change from Baseline Visit | Change from Randomization Visit | |
| Tapentadol Prolonged Release | -2.2 | -0.3 |
| Tapentadol Prolonged Release and Pregabalin | -3.1 | -1.2 |
"The participant scored the EuroQol-5 questionnaire. The EuroQol-5 questionnaire uses a health state classification with 5 dimensions. Each dimension was assessed on a 3-point ordinal scale (1=no problems, 2=some problems, 3=extreme problems). The responses to the five EQ-5D dimensions were scored using a utility-weighted algorithm to derive an EQ-5D health status index score between 0 to 1 (with 1 indicating full health and 0 representing dead). The higher the values (the closer the value is to 1) the better the health status in a treatment group." (NCT01352741)
Timeframe: Enrollment Visit (Day-12); Baseline Visit (Day 1); Randomization Visit (Day 22)
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Change from Baseline Visit | Change from Randomization Visit | |
| Tapentadol Prolonged Release | 0.34 | 0.09 |
| Tapentadol Prolonged Release and Pregabalin | 0.43 | 0.09 |
Pain Intensity (PI) was assessed on 11-point numerical rating scale from 0 = no pain to 10 = pain as bad as you can imagine. Pain Intensity Difference (PID) was the difference between the PI after fixed times after first dose and the baseline PI (prior to the first dose). The Sum of Pain Intensity Differences over 8 hours was calculated. If the values are negative (then the baseline pain intensity was greater than the pain intensity measured after dosing). (NCT01435577)
Timeframe: Baseline value to 8 hours after first study drug administration
| Intervention | units on a scale (Mean) |
|---|---|
| Tapentadol Intravenous | -9.9 |
| Matching Placebo Intravenous | 9.74 |
Individual participant response. Number of participants that reported a 30% or more reduction in pain intensity from the administration of the first dose to 12 hours after the first study drug administration are counted as having a response if their pain intensity decreased by 30% from their baseline value. (NCT01435577)
Timeframe: Baseline value to 12 hours after first study drug administration
| Intervention | participants (Number) |
|---|---|
| Tapentadol Intravenous | 27 |
| Matching Placebo Intravenous | 1 |
Individual participant response. Number of participants that reported a 50% or more reduction in pain intensity from the administration of the first dose to 12 hours after the first study drug administration are counted as having a response if their pain intensity decreased by 50% from their baseline value. (NCT01435577)
Timeframe: Baseline value to 12 hours after first study drug administration
| Intervention | participants (Number) |
|---|---|
| Tapentadol Intravenous | 18 |
| Matching Placebo Intravenous | 1 |
Pain Intensity (PI) was assessed on 11-point numerical rating scale from 0 = no pain to 10 = pain as bad as you can imagine. Pain Intensity Difference (PID) was the difference between the PI after fixed times after first dose and the baseline PI (prior to the first dose). The Sum of Pain Intensity Differences over 60 minutes was calculated. If the values are negative (then the baseline pain intensity was greater than the pain intensity measured after dosing). (NCT01435577)
Timeframe: Baseline value to 48 hours after first study drug administration
| Intervention | units on a scale (Mean) |
|---|---|
| Tapentadol Intravenous | -122.93 |
| Matching Placebo Intravenous | 45.86 |
The pain intensity at the relative time points are the pain intensity before and one hour after study drug administration. The pain intensity was measured using the Pain Intensity (PI). Pain intensity was assessed on 11-point numerical rating scale from 0 = no pain to 10 = pain as bad as you can imagine. (NCT01435577)
Timeframe: Baseline; for the first 6 administrations
| Intervention | units on a scale (Mean) | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Prior to first dose | 1 hour after first dose | prior to second dose | 1 hour after second dose | prior to third dose | 1 hour after third dose | prior to fourth dose | 1 hour after fourth dose | prior to fifth dose | 1 hour after fifth dose | prior to sixth dose | 1 hour after sixth dose | |
| Matching Placebo Intravenous | 7.3 | 7.8 | 8.4 | 8.6 | 7.9 | 7.9 | 7.3 | 7.1 | 5.8 | 5.2 | 5.7 | 4.8 |
The pain intensity at the relative time points are the pain intensity before and one hour after study drug administration. The pain intensity was measured using the Pain Intensity (PI). Pain intensity was assessed on 11-point numerical rating scale from 0 = no pain to 10 = pain as bad as you can imagine. (NCT01435577)
Timeframe: Baseline; for the first 6 administrations
| Intervention | units on a scale (Mean) | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Prior to first dose (n = 64) | 1 hour after first dose (n = 64) | prior to second dose | 1 hour after second dose | prior to third dose | 1 hour after third dose | prior to fourth dose | 1 hour after fourth dose | prior to fifth dose | 1 hour after fifth dose | prior to sixth dose | |
| Tapentadol Intravenous | 7.2 | 3.6 | 7.3 | 4.7 | 7.2 | 6.1 | 6.6 | 4.1 | 4.9 | 2.7 | 4.5 |
"Responders are those participants with Patient Global Impression of Change (PGIC) values Much improved, or Very much improved. Participants with missing value are considered non-responders." (NCT01435577)
Timeframe: Fixed time points at 12, 24 and 48 hours after baseline
| Intervention | participants (Number) | ||
|---|---|---|---|
| Responders 12 hours after first dose | Responders 24 hours after first dose | Responders 48 hours after first dose | |
| Matching Placebo Intravenous | 1 | 5 | 10 |
| Tapentadol Intravenous | 31 | 39 | 43 |
Pain Intensity (PI) was assessed on 11-point numerical rating scale from 0 = no pain to 10 = pain as bad as you can imagine. Pain Intensity Difference (PID) was the difference between baseline pain intensity (prior to the first dose) and the pain intensity at the time. A negative number indicates a decrease in pain in the whole treatment group. The greater the negative pain intensity difference value the greater the pain relief in the treatment arm. A score of 0 indicates that there has been no change in pain in a treatment group. A positive value indicates an increase in pain in the treatment group. (NCT01435577)
Timeframe: Starting at 15 minutes and up to 48 hours after first drug administration
| Intervention | units on a scale (Mean) | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 0.25 hours after first administration | 0.5 hours after first administration | 1 hour after first administration | 2 hours after first administration | 4 hours after first dose administration | 6 hours after first dose administration | 8 hours after first dose administration | 12 hours after first dose administration | 16 hours after first dose administration | 20 hours after first dose administration | 24 hours after first dose administration | 36 hours after first dose administration | 48 hours after first dose administration | |
| Matching Placebo Intravenous | -0.2 | 0.1 | 0.5 | 1.2 | 1.4 | 1.4 | 1.3 | 1.2 | 0.9 | 0.7 | 0.9 | 0.8 | 0.8 |
| Tapentadol Intravenous | -3.5 | -4.1 | -3.5 | -1.3 | -1.0 | -0.9 | -0.7 | -2.0 | -3.4 | -3.5 | -3.1 | -3.2 | -2.9 |
In the Patient Global Impression of Change (PGIC) the participant indicates the perceived change over the treatment period. The participant verbally rated their impression of overall status with 1 of 7 possible responses (very much improved, much improved, minimally improved, no change, minimally worse, much worse, very much worse). (NCT01435577)
Timeframe: Baseline value to 12 hours after first study drug administration
| Intervention | participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Very Much Improved | Much Improved | Minimally Improved | No Change | Minimally Worse | Much Worse | Very Much Worse | |
| Matching Placebo Intravenous | 0 | 1 | 9 | 4 | 1 | 0 | 0 |
| Tapentadol Intravenous | 11 | 20 | 14 | 5 | 4 | 0 | 0 |
In the Patient Global Impression of Change (PGIC) the participant indicates the perceived change over the treatment period. The participant verbally rated their impression of overall status with 1 of 7 possible responses (very much improved, much improved, minimally improved, no change, minimally worse, much worse, very much worse). (NCT01435577)
Timeframe: Baseline value to 48 hours after first study drug administration
| Intervention | participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Very Much Improved | Much Improved | Minimally Improved | No Change | Minimally Worse | Much Worse | Very Much Worse | |
| Matching Placebo Intravenous | 2 | 8 | 2 | 1 | 0 | 0 | 0 |
| Tapentadol Intravenous | 19 | 24 | 4 | 0 | 0 | 0 | 0 |
Tapentadol concentrations were measured in participants in the tapentadol treatment arm. Serum was analyzed by means of liquid chromatography coupled to tandem mass spectrometry with a lower limit of quantification (LLOQ) at 0.2 ng/mL. (NCT01435577)
Timeframe: 15 minutes to 20 hours after first drug administration
| Intervention | ng/mL (Mean) | |||||
|---|---|---|---|---|---|---|
| 15 minutes after first infusion | 30 minutes after first infusion | 60 minutes after first infusion | 4 hours after end of first infusion | 3.5 hours after end of fifth infusion | 4 hours after end of fifth infusion | |
| Tapentadol Intravenous | 201.2 | 99.5 | 76.4 | 38.2 | 73.2 | 70.3 |
"Tapentadol-O-glucuronide is the metabolite of tapentadol. Metabolites are sometimes referred to as breakdown products. The body alters the administered medication to a metabolite so that can be more easily or quickly removed from the body. Tapentadol-O-glucuronide concentrations were measured in participants in the tapentadol treatment arm. Serum was analyzed by means of liquid chromatography coupled to tandem mass spectrometry with a lower limit of quantification (LLOQ) at 0.2 ng/mL." (NCT01435577)
Timeframe: 15 minutes to 20 hours after first drug administration
| Intervention | ng/mL (Mean) | |||||
|---|---|---|---|---|---|---|
| 15 minutes after first infusion | 30 minutes after first infusion | 60 minutes after first infusion | 4 hours after end of first infusion | 3.5 hours after end of fifth infusion | 4 hours after end of fifth infusion | |
| Tapentadol Intravenous | 26.4 | 290.4 | 488.2 | 452.4 | 1048.7 | 945.1 |
Individual participant response. Number of participants that reported a 50% or more reduction in pain intensity from the administration of the first dose to 48 hours after the first study drug administration are counted as having a response if their pain intensity decreased by 50% from their baseline value. (NCT01435577)
Timeframe: Baseline value to 48 hours after first study drug administration
| Intervention | participants (Number) |
|---|---|
| Tapentadol Intravenous | 6 |
| Matching Placebo Intravenous | 0 |
"Pain Intensity assessed at predefined time points (at 0.25, 0.5, 1, 2, 4, 6, 8, 12, 16, 20 and 24 hours after first drug administration) over a 24 hour period using an 11-point Numeric Rating Scale (NRS) where a score of zero indicates no pain and a score of ten indicates pain as bad as you can imagine. Pain Intensity Differences at each predefined time point (calculated as post-baseline NRS values - baseline NRS values) were analyzed. Negative SPID24 values indicate a decrease in pain intensity and positive values indicate an increase in pain intensity since baseline." (NCT01435577)
Timeframe: Baseline value; up to 24 hours after first study drug administration
| Intervention | units on a scale (Least Squares Mean) |
|---|---|
| Tapentadol Intravenous | -51.23 |
| Matching Placebo Intravenous | 25.46 |
Individual participants response. Number of participants that reported a 30% or more reduction in pain intensity from the administration of the first dose to 48 hours after the first study drug administration are counted as having a response if their pain intensity decreased by 30% from their baseline value. (NCT01435577)
Timeframe: Baseline value to 48 hours after first study drug administration
| Intervention | participants (Number) |
|---|---|
| Tapentadol Intravenous | 8 |
| Matching Placebo Intravenous | 1 |
Pain Intensity (PI) was assessed on 11-point numerical rating scale from 0 = no pain to 10 = pain as bad as you can imagine. Pain Intensity Difference (PID) was the difference between the PI after fixed times after first dose and the baseline PI (prior to the first dose). The Sum of Pain Intensity Differences over 12 hours was calculated. If the values are negative (then the baseline pain intensity was greater than the pain intensity measured after dosing). (NCT01435577)
Timeframe: Baseline value to 12 hours after first study drug administration
| Intervention | units on a scale (Mean) |
|---|---|
| Tapentadol Intravenous | -14.98 |
| Matching Placebo Intravenous | 14.82 |
Pain Intensity (PI) was assessed on 11-point numerical rating scale from 0 = no pain to 10 = pain as bad as you can imagine. Pain Intensity Difference (PID) was the difference between the PI after fixed times after first dose and the baseline PI (prior to the first dose). The Sum of Pain Intensity Differences over 4 hours was calculated. If the values are negative (then the baseline pain intensity was greater than the pain intensity measured after dosing). (NCT01435577)
Timeframe: Baseline value to 4 hours after first study drug intake
| Intervention | units on a scale (Mean) |
|---|---|
| Tapentadol Intravenous | -6.76 |
| Matching Placebo Intravenous | 4.22 |
Individual participant response. Number of participants that reported a 50% or more reduction in pain intensity from the administration of the first dose to 24 hours after the first study drug administration are counted as having a response if their pain intensity decreased by 50% from their baseline value. (NCT01435577)
Timeframe: Baseline value to 24 hours after first study drug administration
| Intervention | participants (Number) |
|---|---|
| Tapentadol Intravenous | 24 |
| Matching Placebo Intravenous | 1 |
Pain Intensity (PI) was assessed on 11-point numerical rating scale from 0 = no pain to 10 = pain as bad as you can imagine. Pain Intensity Difference (PID) was the difference between the PI after fixed times after first dose and the baseline PI (prior to the first dose). The Sum of Pain Intensity Differences over 60 minutes was calculated. If the value is negative then the baseline pain intensity was greater than the pain intensity measured after dosing. (NCT01435577)
Timeframe: Baseline value to 60 minutes after first study drug administration
| Intervention | units on a scale (Mean) |
|---|---|
| Tapentadol Intravenous | -3.65 |
| Matching Placebo Intravenous | 0.26 |
In the Patient Global Impression of Change (PGIC) the participant indicates the perceived change over the treatment period. The participant verbally rated their impression of overall status with 1 of 7 possible responses (very much improved, much improved, minimally improved, no change, minimally worse, much worse, very much worse). (NCT01435577)
Timeframe: Baseline value to 24 hours after study drug administration
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| Very Much Improved | Much Improved | Minimally Improved | No Change | Minimally Worse | |
| Matching Placebo Intravenous | 0 | 5 | 6 | 2 | 2 |
| Tapentadol Intravenous | 13 | 26 | 11 | 1 | 1 |
The median time to first rescue medication intake (600 mg ibuprofen) in hours. (NCT01435577)
Timeframe: up to 48 hours
| Intervention | hours (Median) |
|---|---|
| Tapentadol Intravenous | 5.4 |
| Matching Placebo Intravenous | 2.1 |
The participant was instructed to stop the stopwatch when they had meaningful pain relief. That is, when the pain relief made a real difference, after the first drug administration. (NCT01435577)
Timeframe: up to 48 hours
| Intervention | hours (Median) |
|---|---|
| Tapentadol Intravenous | 0.3 |
When the participant began to feel any pain-relieving effect after the administration of the first dose they were requested to stop the first stopwatch. The time was noted. This measured when the participant first felt any difference in the pain. (NCT01435577)
Timeframe: up to 48 hours
| Intervention | hours (Median) |
|---|---|
| Tapentadol Intravenous | 0.2 |
The mean pain intensity at fixed time points in the trial for all participants is listed. The pain intensity was measured using the Pain Intensity (PI). Pain intensity was assessed on 11-point numerical rating scale from 0 = no pain to 10 = pain as bad as you can imagine. (NCT01435577)
Timeframe: Baseline; up to 48 hours
| Intervention | units on a scale (Mean) | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline (before first study drug administration) | 0.25 hours after first dose | 0.5 hour after first dose | 1 hour after first dose | 2 hours after first dose | 4 hours after first dose | 6 hours after first dose | 8 hours after first dose | 12 hours after first dose | 16 hours after first dose | 20 hours after first dose | 24 hours after first dose | 36 hours after first dose | 48 hours after first dose | |
| Matching Placebo Intravenous | 7.3 | 7.1 | 7.4 | 7.8 | 8.5 | 8.6 | 8.7 | 8.6 | 8.5 | 8.2 | 8.0 | 8.1 | 8.0 | 8.1 |
| Tapentadol Intravenous | 7.2 | 3.7 | 3.1 | 3.6 | 5.8 | 6.1 | 6.3 | 6.5 | 5.2 | 3.8 | 3.7 | 4.1 | 3.9 | 4.3 |
Individual participant response. Number of participants that reported a 30% or more reduction in pain intensity from the administration of the first dose to 24 hours after the first study drug administration are counted as having a response if their pain intensity decreased by 30% from their baseline value. (NCT01435577)
Timeframe: Baseline value to 24 hours after first study drug administration
| Intervention | participants (Number) |
|---|---|
| Tapentadol Intravenous | 31 |
| Matching Placebo Intravenous | 4 |
Percent of the radio-labeled meal that reached the colon at 6 hours, indirectly reflecting small bowel transit time. (NCT01500317)
Timeframe: 6 hours
| Intervention | percentage of radio-labeled meal (Mean) |
|---|---|
| Tapentadol | 35.55 |
| Oxycodone | 38.6 |
| Placebo | 65.54 |
The scintigraphic method is used to measure colonic transit. An isotope is adsorbed on activated charcoal particles and delivered to the colon in a delayed release capsule. Anterior and posterior gamma images are taken hourly. The geometric center (GC) is the weighted average of counts in the different colonic regions. The scale ranges from 1 to 5; a high GC implies faster colonic transit, a GC of 1 implies all isotope is in the ascending colon, and a GC of 5 implies all isotope is in the stool. (NCT01500317)
Timeframe: 24 hours
| Intervention | units on a scale (Mean) |
|---|---|
| Tapentadol | 2.06 |
| Oxycodone | 2.07 |
| Placebo | 2.17 |
(NCT01500317)
Timeframe: 24 hours
| Intervention | minutes (Mean) |
|---|---|
| Tapentadol | 159.2 |
| Oxycodone | 155.2 |
| Placebo | 124.7 |
The scintigraphic method is used to measure colonic transit. An isotope is adsorbed on activated charcoal particles and delivered to the colon in a delayed release capsule. Anterior and posterior gamma images are taken hourly. The geometric center (GC) is the weighted average of counts in the different colonic regions. The scale ranges from 1 to 5; a high GC implies faster colonic transit, a GC of 1 implies all isotope is in the ascending colon, and a GC of 5 implies all isotope is in the stool. (NCT01500317)
Timeframe: 8 hours, 48 hours
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Colonic geometric center at 8 hr | Colonic geometric center at 48 hr | |
| Oxycodone | 0.75 | 3.51 |
| Placebo | 0.79 | 3.742 |
| Tapentadol | 0.78 | 3.59 |
Ascending colon emptying t1/2 will be estimated by power exponential analysis of the proportionate emptying over time of counts from the colon. The primary data for this analysis will be the proportion of decay and depth-corrected counts in the ascending colon on the hourly scans on the first day of transit measurement and the 24 hour data. (NCT01500317)
Timeframe: Over the first 24 hours after ingestion of the radioisotopically labeled charcoal particles
| Intervention | hours (Mean) |
|---|---|
| Tapentadol | 21.92 |
| Oxycodone | 19.3 |
| Placebo | 17.88 |
Participants rated pain relief rated on 5-point categorical scale of 0-4 (0=none, 1=A little, 2=Some, 3=A lot, 4=Complete). Total Pain Relief (TOTPAR) was calculated as the time-weighted sum of pain relief scores up to Hour 12, 24, 48, and 72 hours. Total score ranges from 0 (worst) to 48 (best) for TOTPAR12, 0 (worst) to 96 (best) for TOTPAR24, 0 (worst) to 192 (best) for TOTPAR48, and 0 (worst) to 288 (best) for TOTPAR72. A higher value of TOTPAR indicated greater pain relief. (NCT01516008)
Timeframe: 12, 24, 48, and 72 hours
| Intervention | Scores on a scale (Mean) | |||
|---|---|---|---|---|
| 12 hours | 24 hours | 48 hours | 72 hours | |
| Placebo | 7.8 | 19.4 | 53.8 | 94.7 |
| Tapentadol IR 50 mg | 15.0 | 34.5 | 88.4 | 151.3 |
| Tapentadol IR 75 mg | 15.1 | 35.1 | 87.6 | 148.5 |
Pain Intensity (PI) was assessed on an 11-point numerical rating scale from 0=no pain to 10=pain as bad as you can imagine. PID was the difference between baseline PI (prior to the first dose) and current PI at assessment. SPID was calculated as the time-weighted Sum of PID scores over 12, 24, and 72 hours. Total score ranges from -120 (worst) to 120 (best) for SPID12, -240 (worst) to 240 (best) for SPID24, -720 (worst) to 720 (best) for SPID72. A higher value of SPID indicates greater pain relief. (NCT01516008)
Timeframe: 12, 24, and 72 hours
| Intervention | Scores on a scale (Mean) | ||
|---|---|---|---|
| 12 hours | 24 hours | 72 hours | |
| Placebo | 5.7 | 17.7 | 127.9 |
| Tapentadol IR 50 mg | 20.4 | 48.1 | 234.5 |
| Tapentadol IR 75 mg | 24.6 | 60.1 | 264.1 |
Response rate was defined as the percentage of participants with a 50 percent or greater reduction in pain intensity from baseline to 12, 24, 48, and 72 hours. Pain intensity was assessed on a 11-point numerical rating scale from 0=no pain to 10=pain as bad as you can imagine. Participants with no assessment at the given time point, who used an analgesic medication prior to the time point, or who had worse pain intensity at the time point compared to baseline were assigned a percent reduction of 0 percent. (NCT01516008)
Timeframe: 12, 24, 48, and 72 hours
| Intervention | Percentage of participants (Number) | |||
|---|---|---|---|---|
| 12 hours | 24 hours | 48 hours | 72 hours | |
| Placebo | 11.4 | 31.6 | 48.2 | 56.1 |
| Tapentadol IR 50 mg | 28.9 | 46.3 | 71.1 | 79.3 |
| Tapentadol IR 75 mg | 32.5 | 54.7 | 70.1 | 76.9 |
Response rate was defined as the percentage of participants with a 30 percent or greater reduction in pain intensity from baseline to 12, 24, 48, and 72 hours. Pain intensity was assessed on a 11-point numerical rating scale from 0=no pain to 10=pain as bad as you can imagine. Participants with no assessment at the given time point, who used an analgesic medication prior to the time point, or who had worse pain intensity at the time point compared to baseline were assigned a percent reduction of 0 percent. (NCT01516008)
Timeframe: 12, 24, 48, and 72 hours
| Intervention | Percentage of participants (Number) | |||
|---|---|---|---|---|
| 12 hours | 24 hours | 48 hours | 72 hours | |
| Placebo | 27.2 | 39.5 | 53.5 | 57.9 |
| Tapentadol IR 50 mg | 47.9 | 68.6 | 79.3 | 81.8 |
| Tapentadol IR 75 mg | 49.6 | 70.9 | 76.9 | 80.3 |
Pain intensity was assessed on a 11-point numerical rating scale from 0=no pain to 10=pain as bad as you can imagine. Participants with no assessment at the given time point, who used an analgesic medication prior to the time point, or who had worse pain intensity at the time point compared to baseline were assigned a percent reduction of 0 percent. (NCT01516008)
Timeframe: Baseline (Day 1) and 12, 24, 48, and 72 hours
| Intervention | Percentage Reduction (Median) | |||
|---|---|---|---|---|
| 12 hours | 24 hours | 48 hours | 72 hours | |
| Placebo | 0.0 | 20.0 | 41.4 | 60.0 |
| Tapentadol IR 50 mg | 28.6 | 44.4 | 66.7 | 77.8 |
| Tapentadol IR 75 mg | 28.6 | 50.0 | 70.0 | 80.0 |
Rescue medication was defined as any analgesic medication used for participants discontinued due to lack of efficacy (including those started at time of discontinuation) or analgesic medication used during the double-blind period for completed participants. (NCT01516008)
Timeframe: Up to 48 hours
| Intervention | Hours (Median) |
|---|---|
| Placebo | NA |
| Tapentadol IR 50 mg | NA |
| Tapentadol IR 75 mg | NA |
The PGI-C is a 7-point scale that requires the patients to assess how much their illness has improved or worsened relative to a baseline state at the beginning of the intervention. The response options are: 1=very much improved; 2=much improved; 3=minimally improved; 4=no change; 5=minimally worse; 6=much worse; and 7=very much worse. Higher scores indicate worsening. (NCT01516008)
Timeframe: Baseline (Day 1) and 72 hours
| Intervention | Percentage of participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Very Much Improved | Much Improved | Minimally Improved | No Change | Minimally Worse | Much Worse | Very Much Worse | |
| Placebo | 28.9 | 23.7 | 11.4 | 21.1 | 7.9 | 6.1 | 0.9 |
| Tapentadol IR 50 mg | 44.6 | 36.4 | 8.3 | 5.0 | 3.3 | 0.8 | 1.7 |
| Tapentadol IR 75 mg | 46.2 | 37.6 | 6.0 | 6.0 | 1.7 | 1.7 | 0.9 |
Participants rated pain relief rated on 5-point categorical scale of 0-4 (0=none, 1=A little, 2=Some, 3=A lot, 4=Complete). Pain Intensity (PI) was assessed on an 11-point numerical rating scale from 0=no pain to 10=pain as bad as you can imagine. PID was the difference between baseline PI (prior to the first dose) and current PI at assessment. PRID is the sum of pain relief and PID at the same assessment time. SPRID was calculated as the time-weighted Sum of PRID scores over 12, 24, 48, and 72 hours. Total score ranges from -120 (worst) to 168 (best) for SPRID12, -240 (worst) to 336 (best) for SPRID24, -480 (worst) to 672 (best) for SPRID48, and -720 (worst) to 1008 (best) for SPRID72. A higher value of SPRID indicates greater pain relief. (NCT01516008)
Timeframe: 12, 24, 48, and 72 hours
| Intervention | Scores on a scale (Mean) | |||
|---|---|---|---|---|
| 12 hours | 24 hours | 48 hours | 72 hours | |
| Placebo | 13.6 | 37.1 | 119.1 | 222.6 |
| Tapentadol IR 50 mg | 35.4 | 82.6 | 220.2 | 385.7 |
| Tapentadol IR 75 mg | 39.7 | 95.2 | 242.1 | 412.6 |
Pain Intensity (PI) was assessed on an 11-point numerical rating scale from 0=no pain to 10=pain as bad as you can imagine. PID was the difference between baseline PI (prior to the first dose) and current PI at assessment. SPID was calculated as the time-weighted Sum of PID scores over 48 hours. Total score ranges from -480 (worst) to 480 (best) for SPID48. A higher value of SPID indicates greater pain relief. (NCT01516008)
Timeframe: 48 hours
| Intervention | Scores on a scale (Mean) |
|---|---|
| Placebo | 65.3 |
| Tapentadol IR 50 mg | 131.7 |
| Tapentadol IR 75 mg | 154.5 |
Pain intensity assessments were with a 0 (no pain) to 10 (worst pain) scored McGrath color analog scale (CAS) in participants aged 6 years to less than 18 years, i.e. in Adolescents and Older Children. Participants were presented with the CAS and instructed to place the sliding bar on the color that best represented their pain intensity level at the time of assessment. The CAS is a pocket size tool used to measure the self-reported pain intensity of the older participants. The CAS consists of a 145 mm long triangular shaped strip of plastic, varying in width and hue from 1 mm wide and light pink hue at the bottom (and text no pain), to 3 mm wide and deep red hue at the top (most pain). This instrument includes 2 sides. One side shows the color pain intensity scale as described and the other shows a graduated scale, which provides a specific numeric value for the participant-reported level of pain. (NCT01729728)
Timeframe: Baseline; 15 hours post-dose
| Intervention | units on a scale (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Pre-dose | 15 minutes post-dose | 30 minutes after dosing | 1 hour post-dose | 2 hours post-dose | 4 hours post-dose | 6 hours post-dose | 11 hours post-dose | 15 hours post-dose | |
| McGrath Color Analog Scale: Adolescents | 6.643 | 6.131 | 5.262 | 4.393 | 3.475 | 4.200 | 3.438 | 3.350 | 3.288 |
| McGrath Color Analog Scale: Older Children | 4.670 | 3.071 | 2.571 | 2.407 | 2.292 | 2.341 | 2.636 | 3.352 | 3.568 |
"At predefined times after investigational medicinal product administration, participants were asked to rate their pain on a 100 mm line (visual analog scale - VAS) by marking a point on the line in response to:~My pain at this time is. The mark was scored between no pain and pain as bad as it could be. The distance was then measured by a clinician and reported.~A value of 0 indicates no pain. A value of 100 indicates pain as bad as it could be." (NCT01729728)
Timeframe: Baseline; 15 hours
| Intervention | units on a scale (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Pre-dose | 15 minutes post-dose | 30 minutes post-dose | 1 hour post-dose | 2 hours post-dose | 4 hours post-dose | 6 hours post-dose | 11 hours post-dose | 15 hours post-dose | |
| Visual Analog Scale: Adolescents | 71.5 | 63.6 | 53.2 | 46.3 | 34.0 | 43.5 | 34.8 | 32.7 | 33.4 |
Mean and Standard Deviation of Serum Concentrations of Tapentadol. Serum was analyzed by means of liquid chromatography coupled to tandem mass spectrometry with a lower limit of quantification (LLOQ) at 0.2 ng/mL. (NCT01729728)
Timeframe: up to 15 hours
| Intervention | nanogram per milliliter (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| 15 minutes post-dose | 30 minutes post-dose | 1 hour post-dose | 2 hours post-dose | 4 hours post-dose | 6 hours post-dose | 11 hours post-dose | 15 hours post-dose | |
| Tapentadol Serum Concentrations: Adolescents | 23.2 | 45.6 | 49.4 | 43.1 | 32.8 | 22.3 | 8.14 | 3.66 |
Mean and Standard Deviation of Serum Concentrations of Tapentadol. Serum was analyzed by means of liquid chromatography coupled to tandem mass spectrometry with a lower limit of quantification (LLOQ) at 0.2 ng/mL. (NCT01729728)
Timeframe: up to 15 hours
| Intervention | nanogram per milliliter (Mean) | |||
|---|---|---|---|---|
| 1.25 hours post-dose | 3 hours post-dose | 5 hours post-dose | 8 hours post-dose | |
| Tapentadol Serum Concentrations: Very Young Children | 19.9 | 37.7 | 23.4 | 10.0 |
Mean and Standard Deviation of Serum Concentrations of Tapentadol. Serum was analyzed by means of liquid chromatography coupled to tandem mass spectrometry with a lower limit of quantification (LLOQ) at 0.2 ng/mL. (NCT01729728)
Timeframe: up to 15 hours
| Intervention | nanogram per milliliter (Mean) | |
|---|---|---|
| 15 minutes to 1 hour post-dose (N = 11) | 4 to 11 hours post-dose (N=11) | |
| Tapentadol Serum Concentrations: Younger Children | 30.1 | 26.4 |
"Mean and Standard Deviation of Serum Concentrations of Tapentadol-O-glucuronide. Tapentadol-O-glucuronide is the metabolite of tapentadol. Metabolites are sometimes referred to as breakdown products. The body alters the administered medication to a metabolite so that it can be more easily or quickly removed from the body. Tapentadol-O-glucuronide concentrations were measured in participants. Serum was analyzed by means of liquid chromatography coupled to tandem mass spectrometry with a lower limit of quantification (LLOQ) at 10 ng/mL." (NCT01729728)
Timeframe: up to 15 hours
| Intervention | nanogram per milliliter (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| 15 minutes post-dose | 30 minutes post-dose | 1 hour post-dose | 2 hours post-dose | 4 hours post-dose | 6 hours post-dose | 11 hours post-dose | 15 hours post-dose | |
| Tapentadol-O-glucuronide Serum Concentrations: Adolescents | 404 | 855 | 1424 | 1202 | 824 | 497 | 150 | 66.9 |
"Mean and Standard Deviation of Serum Concentrations of Tapentadol-O-glucuronide. Tapentadol-O-glucuronide is the metabolite of tapentadol. Metabolites are sometimes referred to as breakdown products. The body alters the administered medication to a metabolite so that it can be more easily or quickly removed from the body. Tapentadol-O-glucuronide concentrations were measured in participants. Serum was analyzed by means of liquid chromatography coupled to tandem mass spectrometry with a lower limit of quantification (LLOQ) at 10 ng/mL." (NCT01729728)
Timeframe: up to 15 hours
| Intervention | nanogram per milliliter (Mean) | |||
|---|---|---|---|---|
| 15 minutes to 1 hour post-dose | 1 to 4 hours post-dose | 4 to 11 hours post-dose | 11 to 15 hours post-dose | |
| Tapentadol-O-glucuronide Serum Concentrations: Older Children | 676 | 900 | 321 | 86.3 |
"Mean and Standard Deviation of Serum Concentrations of Tapentadol-O-glucuronide. Tapentadol-O-glucuronide is the metabolite of tapentadol. Metabolites are sometimes referred to as breakdown products. The body alters the administered medication to a metabolite so that it can be more easily or quickly removed from the body. Tapentadol-O-glucuronide concentrations were measured in participants. Serum was analyzed by means of liquid chromatography coupled to tandem mass spectrometry with a lower limit of quantification (LLOQ) at 10 ng/mL." (NCT01729728)
Timeframe: up to 15 hours
| Intervention | nanogram per milliliter (Mean) | |||
|---|---|---|---|---|
| 1.25 hours after administration | 3 hours after administration | 5 hours after administration | 8 hours after administration | |
| Tapentadol-O-glucuronide Concentrations: Very Young Children | 497 | 938 | 624 | 253 |
"Mean and Standard Deviation of Serum Concentrations of Tapentadol-O-glucuronide. Tapentadol-O-glucuronide is the metabolite of tapentadol. Metabolites are sometimes referred to as breakdown products. The body alters the administered medication to a metabolite so that it can be more easily or quickly removed from the body. Tapentadol-O-glucuronide concentrations were measured in participants. Serum was analyzed by means of liquid chromatography coupled to tandem mass spectrometry with a lower limit of quantification (LLOQ) at 10 ng/mL." (NCT01729728)
Timeframe: up to 15 hours
| Intervention | nanogram per milliliter (Mean) | |
|---|---|---|
| 15 minutes to 1 hour post-dose | 4 to 11 hours post-dose | |
| Tapentadol-O-glucuronide Serum Concentrations Younger Children | 494 | 504 |
"Respiratory rate assessments were performed at pre-defined times during the 15 hour period following investigational medicinal product intake.~Pre-surgery data for these participants is also given from the enrollment Visit (Visit 1)." (NCT01729728)
Timeframe: Enrollment Visit; 15 hours post-dose
| Intervention | breaths per minute (Mean) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Visit 1 | Pre-dose | 15 minutes post-dose | 30 minutes post-dose | 1 hours post-dose | 2 hours post-dose | 4 hours post-dose | 6 hours post-dose | 11 hours post-dose | 15 hours post-dose | |
| Respiratory Rates: Adolescents | 17.8 | 16.4 | 16.8 | 17.5 | 15.9 | 17.3 | 16.4 | 16.9 | 17.4 | 16.1 |
| Respiratory Rates: Older Children | 18.4 | 19.2 | 19.7 | 19.4 | 19.0 | 19.3 | 19.5 | 19.0 | 18.4 | 17.3 |
| Respiratory Rates: Young and Very Young Children | 25.1 | 25.1 | 24.0 | 22.6 | 21.8 | 22.5 | 22.5 | 22.1 | 22.4 | 21.1 |
"Different pain intensity assessment tools were used in the different age groups. Therefore the sum of pain intensities were calculated and are reported for each age group based on the tool used.~Adolescents - Age 12 to Less Than 18 Years.~Older Children - Age 6 to Less Than 12 Years.~Young Children - Age 3 to Less Than 6 Years.~Very Young Children - Age 2 to Less Than 3 Years.~CAS (McGrath color analog scale) [Theoretical Range: -40 to + 40],~VAS (100 mm Visual Analog Scale) [Theoretical Range: -400 to + 400],~FPS-R (6-point Faces Pain Scale - Revised) [Theoretical Range: -40 to + 40],~FLACC (Face, Legs, Activity, Cry, and Consolability score) [Theoretical Range: -40 to + 40].~A mean score of zero indicates that there was no pain intensity change over the 4 hours.~The positive values indicate that in the group as a whole the sum of all pain intensity values over the first 4 hours lead to a reduction in pain in the time period." (NCT01729728)
Timeframe: Baseline; 4 hours post-dose
| Intervention | units on a scale (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| Adolescents SPID for VAS | Adolescents SPID for CAS | Older Children SPID for CAS | Older Children SPID for FPS-R | Young Children SPID for FPS-R | Young Children SPID for FLACC | Very Young Children SPID for FLACC | |
| Sum of Pain Intensity Differences | 106.282 | 8.925 | 9.698 | 8.724 | 17.646 | 11.614 | 12.483 |
"Systolic and Diastolic blood pressure assessments were performed at pre-defined times during the 15 hour period following investigational medicinal product intake.~Pre-surgery data for these participants is also given from the enrollment Visit (Visit 1)." (NCT01729728)
Timeframe: Enrollment Visit; 15 hours post-dose
| Intervention | mmHg (Mean) | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Visit 1 Enrollment Systolic blood pressure | Pre-dose Systolic Blood Pressure | 15 minutes post-dose Systolic Blood Pressure | 30 minutes post-dose Systolic Blood Pressure | 1 hour post-dose Systolic Blood Pressure | 2 hours post-dose Systolic Blood Pressure | 4 hours post-dose Systolic Blood Pressure | 6 hours post-dose Systolic Blood Pressure | 11 hours post-dose Systolic Blood Pressure | 15 hours post-dose Systolic Blood Pressure | Visit 1 Enrollment Diastolic blood pressure | Pre-dose Diastolic blood pressure | 15 minutes post-dose Diastolic blood pressure | 30 minutes post-dose Diastolic blood pressure | 1 hour post-dose Diastolic blood pressure | 2 hours post-dose Diastolic blood pressure | 4 hours post-dose Diastolic blood pressure | 6 hours post-dose Diastolic blood pressure | 11 hours post-dose Diastolic blood pressure | 15 hours post-dose Diastolic blood pressure | |
| Blood Pressure: Adolescents | 110.2 | 122.9 | 126.9 | 126.8 | 127.0 | 124.9 | 122.8 | 116.8 | 115.1 | 113.8 | 66.5 | 74.8 | 78.9 | 76.1 | 77.6 | 74.7 | 73.2 | 66.0 | 65.4 | 67.1 |
| Blood Pressure: Older Children | 103.8 | 107.1 | 104.1 | 104.1 | 104.0 | 103.9 | 104.8 | 106.7 | 102.0 | 100.3 | 66.3 | 64.2 | 62.4 | 61.3 | 61.1 | 59.7 | 60.0 | 59.0 | 54.6 | 56.8 |
| Blood Pressure: Young and Very Young Children | 98.7 | 105.1 | 101.8 | 100.1 | 97.6 | 98.4 | 100.1 | 102.0 | 99.4 | 93.3 | 62.8 | 65.6 | 62.4 | 60.2 | 59.6 | 59.7 | 58.7 | 58.8 | 57.3 | 57.0 |
"The intensity of all treatment emergent adverse events (TEAEs) were scored by the investigator. Treatment emergent adverse events were those adverse events documented from the time of investigational medicinal product (IMP), study drug, up to 48 hours post dosing.~The clinical intensity of an adverse event was classified as:~Mild: Signs and symptoms that can be easily tolerated. Symptoms can be ignored and disappear when the subject is distracted.~Moderate: Symptoms cause discomfort but are tolerable; they cannot be ignored and affect concentration.~Severe: Symptoms which affect usual daily activity.~For adverse events where the intensity changes over time, the maximum intensity observed was documented." (NCT01729728)
Timeframe: Baseline; 48 hours post dosing
| Intervention | number of events (Number) | ||
|---|---|---|---|
| Total number of TEAEs | Total number of mild TEAEs | Total number of moderate TEAEs | |
| Number of TEAEs: Adolescents | 22 | 10 | 12 |
| Number of TEAEs: Older Children | 33 | 16 | 17 |
| Number of TEAEs: Young and Very Young Children | 11 | 10 | 1 |
Mean and Standard Deviation of Serum Concentrations of Tapentadol. Serum was analyzed by means of liquid chromatography coupled to tandem mass spectrometry with a lower limit of quantification (LLOQ) at 0.2 ng/mL. (NCT01729728)
Timeframe: up to 15 hours
| Intervention | nanogram per milliliter (Mean) | |||
|---|---|---|---|---|
| 15 minutes to 1 hour post-dose (N=22) | 1 to 4 hours post-dose (N=22) | 4 to 11 hours post-dose (N=22) | 11 to 15 hours post-dose (N=22) | |
| Tapentadol Serum Concentrations: Older Children | 36.5 | 36.5 | 13.5 | 3.71 |
Potassium is a mineral that the body needs to work normally. In the study there were 3 planned safety blood draws for routine blood tests: at Visit 1 (during the enrollment period, including surgery), at Visit 2 (prior to study drug administration) and at Visit 3 (prior to discharge from the hospital). The discharge visit was as per standard of care. (NCT01729728)
Timeframe: Enrollment Visit; Visit 2 and Discharge Visit
| Intervention | mmol/L (Mean) | ||
|---|---|---|---|
| Visit 1 | Visit 2 | Visit 3 | |
| Blood Potassium Concentration: Adolescents | 4.20 | 3.90 | 3.94 |
| Blood Potassium Concentration: Older Children | 4.20 | 3.83 | 3.93 |
| Blood Potassium Concentration: Young and Very Young Children | 4.09 | 4.04 | 3.93 |
"12-lead Electrocardiograms (ECG) were part of the planned safety assessments. 12-lead Electrocardiograms were performed prior at the enrollment visit after informed consent and at the discharge visit. The discharge visit was as per standard of care.~The changes in heart rate (beats per minute) parameters are reported per treatment group between the visits.~A positive value indicates that the heart rate was higher at discharge than at enrollment." (NCT01729728)
Timeframe: Enrollment; Discharge Visit
| Intervention | beats per minute (Mean) |
|---|---|
| ECG Heart Rate Change: Adolescents | 2.0 |
| ECG Heart Rate Change: Older Children | 4.3 |
| ECG Heart Rate Change: Young and Very Young Children | 10.7 |
"Serum samples for pharmacokinetic analysis were obtained using frequent sampling techniques in participants 12 years to less than 18 years of age.~Serum samples (frequent sampling) were drawn at 0.25, 0.5, 1, 2, 4, 6, 11, and 15 hours.~The Area Under the Curve (AUC) from dose to 15 hours (AUC 0-15) is a summary measure of data from each pharmacokinetic blood sample taken over the 15 hour time period.~The area is that below the line fitted to the data points." (NCT01729728)
Timeframe: up to 15 hours
| Intervention | ng*hr/mL (Mean) |
|---|---|
| Tapentadol Non-Compartmental PK Parameter: AUC | 302 |
"Serum samples for pharmacokinetic analysis were obtained using frequent sampling techniques in participants 12 years to less than 18 years of age.~Serum samples (frequent sampling) were drawn at 0.25, 0.5, 1, 2, 4, 6, 11, and 15 hours. The concentration of tapentadol (active drug) is assessed during absorption and distribution.~The maximum concentration is derived from the Area Under the Curve, from dose to 15 hours (AUC 0-15). It is the highest amount of active drug observed in the blood sample." (NCT01729728)
Timeframe: up to 15 hours
| Intervention | ng*hr/mL (Mean) |
|---|---|
| Tapentadol-O-glucuronide Non-Compartmental PK Parameter: AUC | 7082 |
"Serum samples for pharmacokinetic analysis were obtained using frequent sampling techniques in participants 12 years to less than 18 years of age.~Serum samples (frequent sampling) were drawn at 0.25, 0.5, 1, 2, 4, 6, 11, and 15 hours. The concentration of tapentadol (active drug) is assessed during absorption and distribution.~The maximum concentration is derived from the Area Under the Curve, from dose to 15 hours (AUC 0-15). It is the highest amount of active drug observed in the blood sample" (NCT01729728)
Timeframe: up to 15 hours
| Intervention | nanograms/millilitre (Mean) |
|---|---|
| Tapentadol Non-Compartmental PK Parameter: Cmax | 67.5 |
"Tapentadol-O-glucuronide is the metabolite of tapentadol. Metabolites are sometimes referred to as breakdown products. The body alters the administered medication to a metabolite so that it can be more easily or quickly removed from the body. Serum samples (frequent sampling) were drawn at 0.25, 0.5, 1, 2, 4, 6, 11, and 15 hours. The concentration of tapentadol-O-glucuronide (metabolite) is assessed to study absorption and distribution.~The maximum concentration is derived from the Area Under the Curve, from dose to 15 hours (AUC 0-15). It is the highest amount of metabolite observed in the blood sample." (NCT01729728)
Timeframe: up to 15 hours
| Intervention | nanogramsg/millilitre (Mean) |
|---|---|
| Tapentadol-O-glucuronide Non-Compartmental PK Parameter: Cmax | 1487 |
"Serum samples for pharmacokinetic analysis were obtained using frequent sampling techniques in participants 12 years to less than 18 years of age.~The time to maximum concentration is derived from the area under the curve from dose to 15 hours (AUC 0-15). The Tmax is the time after dosing at which the maximum concentration of the tapentadol (active drug) occurs.~Serum samples (frequent sampling) were drawn at 0.25, 0.5, 1, 2, 4, 6, 11, and 15 hours." (NCT01729728)
Timeframe: up to 15 hours
| Intervention | hours (Mean) |
|---|---|
| Tapentadol Non-Compartmental PK Parameter: Tmax | 1.4 |
"Tapentadol-O-glucuronide is the metabolite of tapentadol. Metabolites are sometimes referred to as breakdown products. The body alters the administered medication to a metabolite so that it can be more easily or quickly removed from the body. Serum samples for pharmacokinetic analysis were obtained using frequent sampling techniques in participants 12 years to less than 18 years of age. The time to maximum concentration is derived from the area under the curve from dose to 15 hours (AUC 0-15). The Tmax is the time after dosing at which the maximum concentration of the tapentadol-O-glucuronide (metabolite) occurs. Serum samples (frequent sampling) were drawn at 0.25, 0.5, 1, 2, 4, 6, 11, and 15 hours." (NCT01729728)
Timeframe: up to 15 hours
| Intervention | hours (Mean) |
|---|---|
| Tapentadol-O-glucuronide Non-Compartmental PK Parameter: Tmax | 1.70 |
The Alkaline Phosphatase activity was used to detect bone or hepatobiliary disease. In the study there were 3 planned safety blood draws for routine blood tests: at Visit 1 (during the enrollment period, including surgery), at Visit 2 (prior to study drug administration) and at Visit 3 (prior to discharge from the hospital). The discharge visit was as per standard of care. (NCT01729728)
Timeframe: Enrollment Visit, Visit 2 and Discharge Visit
| Intervention | U/L (Mean) | ||
|---|---|---|---|
| Visit 1 | Visit 2 | Visit 3 | |
| ALP Activity: Adolescents | 124.7 | 114.7 | 107.6 |
| ALP Activity: Older Children | 240.0 | 207.5 | 204.1 |
| ALP Activity: Young & Very Young Children | 230.1 | 210.2 | 199.2 |
AST is considered to be one of the two most important tests to detect liver injury. During liver damage the enzyme is released into the blood. In the study there were 3 planned safety blood draws for routine blood tests: at Visit 1 (during the enrollment period, including surgery), at Visit 2 (prior to study drug administration) and at Visit 3 (prior to discharge from the hospital). The discharge visit was as per standard of care. (NCT01729728)
Timeframe: Enrollment Visit; Visit 2 and Discharge Visit
| Intervention | U/L (Mean) | ||
|---|---|---|---|
| Visit 1 | Visit 2 | Visit 3 | |
| AST Activity: Adolescents | 21.5 | 21.6 | 21.6 |
| AST Activity: Older Children | 27.9 | 29.9 | 30.2 |
| AST Activity: Young and Very Young Children | 33.4 | 37.9 | 33.8 |
All cells need calcium in order to function. In the study there were 3 planned safety blood draws for routine blood tests. In the study there were 3 planned safety blood draws for routine blood tests: at Visit 1 (during the enrollment period, including surgery), at Visit 2 (prior to study drug administration) and at Visit 3 (prior to discharge from the hospital). The discharge visit was as per standard of care. (NCT01729728)
Timeframe: Enrollment Visit; Visit 2 and Discharge Visit
| Intervention | mmol/L (Mean) | ||
|---|---|---|---|
| Visit 1 | Visit 2 | Visit 3 | |
| Blood Calcium Concentration: Adolescents | 2.455 | 2.268 | 2.359 |
| Blood Calcium Concentration: Older Children | 2.482 | 2.267 | 2.266 |
| Blood Calcium Concentration: Young and Very Young Children | 2.519 | 2.343 | 2.369 |
Chloride with other electrolytes help keep the proper balance of body fluids and maintain the body's acid-base balance. In the study there were 3 planned safety blood draws for routine blood tests: at Visit 1 (during the enrollment period, including surgery), at Visit 2 (prior to study drug administration) and at Visit 3 (prior to discharge from the hospital). The discharge visit was as per standard of care (NCT01729728)
Timeframe: Enrollment Visit; Visit 2 and Discharge Visit
| Intervention | mmol/L (Mean) | ||
|---|---|---|---|
| Visit 1 | Visit 2 | Visit 3 | |
| Blood Chloride Concentration: Adolescents | 103.3 | 106.6 | 103.0 |
| Blood Chloride Concentration: Older Children | 103.4 | 104.9 | 105.1 |
| Blood Chloride Concentration: Young and Very Young Children | 103.8 | 106.2 | 105.1 |
A blood glucose test measures the amount of a sugar called glucose in blood. In the study there were 3 planned safety blood draws for routine blood tests: at Visit 1 (during the enrollment period, including surgery), at Visit 2 (prior to study drug administration) and at Visit 3 (prior to discharge from the hospital). The discharge visit was as per standard of care. (NCT01729728)
Timeframe: Enrollment Visit; Visit 2 and Discharge Visit
| Intervention | mmol/L (Mean) | ||
|---|---|---|---|
| Visit 1 | Visit 2 | Visit 3 | |
| Blood Glucose Concentration: Adolescents | 4.77 | 5.10 | 5.51 |
| Blood Glucose Concentration: Older Children | 4.81 | 6.39 | 5.69 |
| Blood Glucose Concentration: Young and Very Young Children | 5.01 | 5.89 | 4.90 |
Phosphate is needed by the body. This test was done to see how much phosphate is in the blood. In the study there were 3 planned safety blood draws for routine blood tests: at Visit 1 (during the enrollment period, including surgery), at Visit 2 (prior to study drug administration) and at Visit 3 (prior to discharge from the hospital). The discharge visit was as per standard of care. (NCT01729728)
Timeframe: Enrollment Visit; Visit 2 and Discharge Visit
| Intervention | mmol/L (Mean) | ||
|---|---|---|---|
| Visit 1 | Visit 2 | Visit 3 | |
| Blood Phosphate Concentration: Adolescents | 1.384 | 1.234 | 1.500 |
| Blood Phosphate Concentration: Older Children | 1.560 | 1.248 | 1.535 |
| Blood Phosphate Concentration: Young and Very Young Children | 1.689 | 1.412 | 1.611 |
The test was done to verify kidney and liver function. It is done in combination with the albumin test. In the study there were 3 planned safety blood draws for routine blood tests: at Visit 1 (during the enrollment period, including surgery), at Visit 2 (prior to study drug administration) and at Visit 3 (prior to discharge from the hospital). The discharge visit was as per standard of care. (NCT01729728)
Timeframe: Enrollment Visit, Visit 2 and Discharge Visit
| Intervention | g/L (Mean) | ||
|---|---|---|---|
| Visit 1 | Visit 2 | Visit 3 | |
| Protein Concentration: Adolescents | 72.3 | 64.2 | 64.9 |
| Protein Concentration: Older Children | 73.3 | 61.8 | 62.1 |
| Protein Concentration: Young & Very Young Children | 68.6 | 62.1 | 61.8 |
Sodium is required by the body for the body to function properly. In the study there were 3 planned safety blood draws for routine blood tests: at Visit 1 (during the enrollment period, including surgery), at Visit 2 (prior to study drug administration) and at Visit 3 (prior to discharge from the hospital). The discharge visit was as per standard of care. (NCT01729728)
Timeframe: Enrollment Visit; Visit 2 and Discharge Visit
| Intervention | mmol/L (Mean) | ||
|---|---|---|---|
| Visit 1 | Visit 2 | Visit 3 | |
| Blood Sodium Concentration: Adolescents | 140.9 | 140.3 | 138.1 |
| Blood Sodium Concentration: Older Children | 140.4 | 138.4 | 138.7 |
| Blood Sodium Concentration: Young and Very Young Children | 139.3 | 139.1 | 138.8 |
This test is to measure the amount of urea nitrogen in the blood. It was used to test liver and kidney function. In the study there were 3 planned safety blood draws for routine blood tests: at Visit 1 (during the enrollment period, including surgery), at Visit 2 (prior to study drug administration) and at Visit 3 (prior to discharge from the hospital). The discharge visit was as per standard of care. (NCT01729728)
Timeframe: Enrollment Visit; Visit 2 and Discharge Visit
| Intervention | mmol/L (Mean) | ||
|---|---|---|---|
| Visit 1 | Visit 2 | Visit 3 | |
| BUN Concentration: Adolescents | 4.55 | 4.54 | 3.88 |
| BUN Concentration: Older Children | 4.47 | 4.38 | 4.31 |
| BUN Concentration: Young and Very Young Children | 5.15 | 4.19 | 4.11 |
Glomerular filtration rate (GFR) was done to check how well the kidneys are working. It estimates how much blood passes through the glomeruli in the kidney each minute. In the study there were 3 planned safety blood draws for routine blood tests: at Visit 1 (during the enrollment period, including surgery), at Visit 2 (prior to study drug administration) and at Visit 3 (prior to discharge from the hospital). The discharge visit was as per standard of care. (NCT01729728)
Timeframe: Enrollment Visit; Visit 2 and Discharge Visit
| Intervention | mL/min/1.73m^2 (Mean) | ||
|---|---|---|---|
| Visit 1 | Visit 2 | Visit 3 | |
| Glomerular Filtration Rate: Adolescents | 133.6 | 146.6 | 142.6 |
| Glomerular Filtration Rate: Older Children | 133.9 | 155.1 | 158.7 |
| Glomerular Filtration Rate: Young and Very Young Children | 141.5 | 166.9 | 164.0 |
The creatine kinase (CK) test was used to detect inflammation of muscles. The test was done in combination with other tests. In the study there were 3 planned safety blood draws for routine blood tests: at Visit 1 (during the enrollment period, including surgery), at Visit 2 (prior to study drug administration) and at Visit 3 (prior to discharge from the hospital). The discharge visit was as per standard of care. (NCT01729728)
Timeframe: Enrollment Visit, Visit 2 and Discharge Visit
| Intervention | U/L (Mean) | ||
|---|---|---|---|
| Visit 1 | Visit 2 | Visit 3 | |
| CK Activity: Adolescents | 126.0 | 186.8 | 264.6 |
| CK Activity: Older Children | 109.8 | 283.3 | 288.1 |
| CK Activity: Young & Very Young Children | 133.4 | 275.8 | 203.6 |
Creatinine is removed from the body entirely by the kidneys. If kidney function is not normal, creatinine level increases in the blood. In the study there were 3 planned safety blood draws for routine blood tests. In the study there were 3 planned safety blood draws for routine blood tests: at Visit 1 (during the enrollment period, including surgery), at Visit 2 (prior to study drug administration) and at Visit 3 (prior to discharge from the hospital). The discharge visit was as per standard of care. (NCT01729728)
Timeframe: Enrollment Visit; Visit 2 and Discharge Visit
| Intervention | µmol/L (Mean) | ||
|---|---|---|---|
| Visit 1 | Visit 2 | Visit 3 | |
| Creatinine Concentration: Adolescents | 73.3 | 67.8 | 68.6 |
| Creatinine Concentration: Older Children | 49.5 | 44.1 | 41.5 |
| Creatinine Concentration: Young and Very Young Children | 35.6 | 31.6 | 33.0 |
This test was done in combination with other tests (such as AST, ALP, and bilirubin) to diagnose and monitor the liver function. In the study there were 3 planned safety blood draws for routine blood tests. In the study there were 3 planned safety blood draws for routine blood tests: at Visit 1 (during the enrollment period, including surgery), at Visit 2 (prior to study drug administration) and at Visit 3 (prior to discharge from the hospital). The discharge visit was as per standard of care. (NCT01729728)
Timeframe: Enrollment Visit, Visit 2 and Discharge Visit
| Intervention | U/L (Mean) | ||
|---|---|---|---|
| Visit 1 | Visit 2 | Visit 3 | |
| ALT Activity: Adolescents | 16.2 | 14.1 | 14.2 |
| ALT Activity: Older Children | 15.9 | 15.7 | 15.4 |
| ALT Activity: Young & Very Young Children | 16.4 | 17.9 | 17.1 |
Old red blood cells are replaced by new blood cells every day. Bilirubin is made by the body when the old blood cells are removed. The concentration of bilirubin in the blood measures liver function. In the study there were 3 planned safety blood draws for routine blood tests: at Visit 1 (during the enrollment period, including surgery), at Visit 2 (prior to study drug administration) and at Visit 3 (prior to discharge from the hospital). The discharge visit was as per standard of care. (NCT01729728)
Timeframe: Enrollment Visit, Visit 2 and Discharge Visit
| Intervention | µmol/L (Mean) | ||
|---|---|---|---|
| Visit 1 | Visit 2 | Visit 3 | |
| Bilirubin Concentration: Adolescents | 12.0 | 10.9 | 17.8 |
| Bilirubin Concentration: Older Children | 6.8 | 6.3 | 9.3 |
| Bilirubin Concentration: Young & Very Young Children | 4.8 | 3.7 | 5.8 |
The gamma-glutamyl transferase (GGT) test was used in combination with the alkaline phosphatase (ALP) test. Both ALP and GGT can be elevated in bile duct or liver complications. In the study there were 3 planned safety blood draws for routine blood tests: at Visit 1 (during the enrollment period, including surgery), at Visit 2 (prior to study drug administration) and at Visit 3 (prior to discharge from the hospital). The discharge visit was as per standard of care. (NCT01729728)
Timeframe: Enrollment Visit, Visit 2 and Discharge Visit
| Intervention | U/L (Mean) | ||
|---|---|---|---|
| Visit 1 | Visit 2 | Visit 3 | |
| GGT Activity: Adolescents | 12.0 | 10.4 | 10.8 |
| GGT Activity: Older Children | 10.6 | 8.7 | 8.8 |
| GGT Activity: Young & Very Young Children | 9.4 | 8.6 | 8.3 |
Lactate Dehydrogenase (LDH) was used to check for tissue damage. In the study there were 3 planned safety blood draws for routine blood tests: at Visit 1 (during the enrollment period, including surgery), at Visit 2 (prior to study drug administration) and at Visit 3 (prior to discharge from the hospital). The discharge visit was as per standard of care. (NCT01729728)
Timeframe: Enrollment Visit, Visit 2 and Discharge Visit
| Intervention | U/L (Mean) | ||
|---|---|---|---|
| Visit 1 | Visit 2 | Visit 3 | |
| LDH Activity: Adolescents | 157.7 | 154.5 | 143.9 |
| LDH Activity: Older Children | 210.5 | 199.1 | 197.8 |
| LDH Activity: Young & Very Young Children | 243.8 | 256.3 | 238.6 |
Albumin is a protein made by the liver. Albumin prevents fluid leaking into the tissues. Albumin also transports many small molecules. Serum albumin was measured in the clear liquid portion of the blood called serum. In the study there were 3 planned safety blood draws for routine blood tests: at Visit 1 (during the enrollment period, including surgery), at Visit 2 (prior to study drug administration) and at Visit 3 (prior to discharge from the hospital). The discharge visit was as per standard of care. (NCT01729728)
Timeframe: Enrollment Visit; Visit 2 and Discharge Visit
| Intervention | g/L (Mean) | ||
|---|---|---|---|
| Visit 1 | Visit 2 | Visit 3 | |
| Albumin Concentration: Adolescents | 43.4 | 38.4 | 38.4 |
| Albumin Concentration: Older Children | 43.4 | 37.1 | 37.2 |
| Albumin Concentration: Young and Very Young Children | 42.6 | 38.9 | 37.5 |
A triacylglycerol lipase test was done to check for pancreatic function. In the study there were 3 planned safety blood draws for routine blood tests. In the study there were 3 planned safety blood draws for routine blood tests: at Visit 1 (during the enrollment period, including surgery), at Visit 2 (prior to investigational medicinal product administration) and at Visit 3 (prior to discharge from the hospital). The discharge visit was as per standard of care. (NCT01729728)
Timeframe: Enrollment Visit, Visit 2 and Discharge Visit
| Intervention | U/L (Mean) | ||
|---|---|---|---|
| Visit 1 | Visit 2 | Visit 3 | |
| TL Activity: Adolescents | 29.5 | 22.7 | 24.8 |
| TL Activity: Older Children | 30.3 | 22.6 | 22.2 |
| TL Activity: Young & Very Young Children | 26.3 | 19.6 | 19.3 |
Triglycerides are a group of fat. Triglycerides were measured as part of metabolic and cardiac assessments. In the study there were 3 planned safety blood draws for routine blood tests: at Visit 1 (during the enrollment period, including surgery), at Visit 2 (prior to study drug administration) and at Visit 3 (prior to discharge from the hospital). The discharge visit was as per standard of care. (NCT01729728)
Timeframe: Enrollment Visit; Visit 2 and Discharge Visit
| Intervention | mmol/L (Mean) | ||
|---|---|---|---|
| Visit 1 | Visit 2 | Visit 3 | |
| Triglycerides Concentration: Adolescents | 1.118 | 0.666 | 0.634 |
| Triglycerides Concentration: Older Children | 1.129 | 0.499 | 0.646 |
| Triglycerides Concentration: Young and Very Young Children | 1.223 | 0.556 | 0.789 |
Uric acid (urate is the salt) is a chemical created when the body breaks down substances called purines. Most urate dissolves in blood and travels to the kidneys. From there, it passes out in the urine. The test is used to determine kidney function. In the study there were 3 planned safety blood draws for routine blood tests: at Visit 1 (during the enrollment period, including surgery), at Visit 2 (prior to study drug administration) and at Visit 3 (prior to discharge from the hospital). The discharge visit was as per standard of care. (NCT01729728)
Timeframe: Enrollment Visit; Visit 2 and Discharge Visit
| Intervention | µmol/L (Mean) | ||
|---|---|---|---|
| Visit 1 | Visit 2 | Visit 3 | |
| Urate: Adolescents | 301.62 | 305.57 | 291.45 |
| Urate: Older Children | 228.32 | 225.39 | 213.68 |
| Urate: Young and Very Young Children | 214.82 | 205.65 | 195.94 |
A urine sample was tested right away. A dipstick made with a color-sensitive pad was used. The color indicated the acidity of the urine. In the study there were 2 planned safety urine collections. At Visit 1 in the enrollment period, after consent and assent obtained. The second sample was obtained at Visit 3 prior to discharge from the hospital. The discharge visit was as per standard of care. (NCT01729728)
Timeframe: Enrollment Visit and Discharge Visit
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Visit 1 | Visit 3 | |
| Urine pH: Adolescents | 6.2 | 6.1 |
| Urine pH: Older Children | 6.5 | 6.2 |
| Urine pH: Young and Very Young Children | 6.2 | 6.4 |
This test was used to test for the water balance and urine concentration. A urine sample was tested right away. A dipstick with a color-sensitive pad was used. The color the dipstick changes and the specific gravity of the urine was read off the color chart. In the study there were 2 planned safety urine collections. At Visit 1 in the enrollment period, after consent and assent obtained. The second sample was obtained at Visit 3 prior to discharge from the hospital. The discharge visit was as per standard of care. (NCT01729728)
Timeframe: Enrollment Visit and Discharge Visit
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Visit 1 | Visit 3 | |
| Specific Gravity Urine: Adolescents | 1.025 | 1.022 |
| Specific Gravity Urine: Older Children | 1.024 | 1.024 |
| Specific Gravity Urine: Young and Very Young Children | 1.021 | 1.024 |
"12-lead electrocardiograms (ECG) were part of the planned safety assessments. 12-lead Electrocardiograms were performed prior at the enrollment visit after informed consent and at the discharge visit. The discharge visit was as per standard of care.~The changes in ECG parameters are reported. Negative mean values indicate that the millisecond intervals decreased from the enrollment to the discharge visit. Positive mean values indicate that the millisecond intervals increased from the enrollment to the discharge visit. The Letters P,Q,R,S and T refer to specific medically defined points on an ECG tracing and correspond to specific heart activities." (NCT01729728)
Timeframe: Enrollment (pre-surgery); Discharge Visit
| Intervention | milliseconds (Mean) | ||||
|---|---|---|---|---|---|
| QTcF change | QT Duration change | QRS Duration change | PR Duration change | RR Duration change | |
| ECG Changes: Adolescents | -3.6 | -8.0 | 0.5 | -3.5 | -32.2 |
| ECG Changes: Older Children | 15.7 | 8.5 | -0.2 | -1.8 | -35.2 |
| ECG Changes: Young and Very Young Children | 5.6 | -4.1 | 0.5 | -2.4 | -48.1 |
Erythrocyte Mean Corpuscular volume is a measurement of the average size of Red Blood Cells (RBC). It is also referred to as Mean Corpuscular Volume. In the study there were 3 planned safety blood draws for routine blood tests: at Visit 1 (during the enrollment period, including surgery), at Visit 2 (prior to study drug administration) and at Visit 3 (prior to discharge from the hospital). The discharge visit was as per standard of care. (NCT01729728)
Timeframe: Enrollment Visit; Visit 2 and Discharge Visit
| Intervention | fL (Mean) | ||
|---|---|---|---|
| Visit 1 | Visit 2 | Visit 3 | |
| Mean Corpuscular Volume: Adolescents | 86.1 | 86.5 | 86.9 |
| Mean Corpuscular Volume: Older Children | 82.3 | 83.1 | 83.1 |
| Mean Corpuscular Volume: Young and Very Young Children | 79.6 | 81.8 | 82.7 |
Hematocrit is a blood test that measures the percentage of the volume of whole blood that is made up of red blood cells (RBC). This measurement depends on the number of red blood cells and the size of red blood cells. In the study there were 3 planned safety blood draws for routine blood tests: at Visit 1 (during the enrollment period, including surgery), at Visit 2 (prior to study drug administration) and at Visit 3 (prior to discharge from the hospital). The discharge visit was as per standard of care. (NCT01729728)
Timeframe: Enrollment Visit; Visit 2 and Discharge Visit
| Intervention | fraction of blood volume (Mean) | ||
|---|---|---|---|
| Visit 1 | Visit 2 | Visit 3 | |
| Hematocrit: Adolescents | 0.436 | 0.421 | 0.402 |
| Hematocrit: Older Children | 0.400 | 0.372 | 0.364 |
| Hematocrit: Young and Very Young Children | 0.368 | 0.363 | 0.356 |
The hemoglobin test is a commonly ordered blood test and was done as part of a complete blood count (CBC). It is routinely done before and after surgery to check for anemia, the presence of chronic kidney disease or other chronic medical problems. In the study there were 3 planned safety blood draws for routine blood tests: at Visit 1 (during the enrollment period, including surgery), at Visit 2 (prior to study drug administration) and at Visit 3 (prior to discharge from the hospital). The discharge visit was as per standard of care. (NCT01729728)
Timeframe: Enrollment Visit; Visit 2 and Discharge Visit
| Intervention | g/L (Mean) | ||
|---|---|---|---|
| Visit 1 | Visit 2 | Visit 3 | |
| Hemoglobin Concentration: Adolescents | 151.10 | 145.67 | 139.00 |
| Hemoglobin Concentration: Older Children | 140.04 | 128.64 | 126.54 |
| Hemoglobin Concentration: Young and Very Young Children | 127.47 | 121.75 | 117.00 |
Leukocytes are also called white blood cells (WBC). These were measured to assess immune function. In the study there were 3 planned safety blood draws for routine blood tests: at Visit 1 (during the enrollment period, including surgery), at Visit 2 (prior to study drug administration) and at Visit 3 (prior to discharge from the hospital). The discharge visit was as per standard of care. (NCT01729728)
Timeframe: Enrollment Visit; Visit 2 and Discharge Visit
| Intervention | GI/L (Mean) | ||
|---|---|---|---|
| Visit 1 | Visit 2 | Visit 3 | |
| Leukocyte Concentration: Adolescents | 6.631 | 8.537 | 10.052 |
| Leukocyte Concentration: Older Children | 7.594 | 12.509 | 14.806 |
| Leukocyte Concentration: Young and Very Young Children | 6.555 | 10.751 | 13.160 |
Platelets are cell fragments that are vital for normal blood clotting. In the study there were 3 planned safety blood draws for routine blood tests: at Visit 1 (during the enrollment period, including surgery), at Visit 2 (prior to study drug administration) and at Visit 3 (prior to discharge from the hospital). The discharge visit was as per standard of care. (NCT01729728)
Timeframe: Enrollment Visit; Visit 2 and Discharge Visit
| Intervention | GI/L (Mean) | ||
|---|---|---|---|
| Visit 1 | Visit 2 | Visit 3 | |
| Platelet Count: Adolescents | 297.0 | 266.1 | 263.9 |
| Platelet Count: Older Children | 347.1 | 303.4 | 316.9 |
| Platelet Count: Young and Very Young Children | 357.4 | 312.6 | 307.3 |
Number of participants with intakes of supplemental analgesic medication between investigational medicinal product (IMP) intake and Site Discharge grouped according to preparation taken (non-opioid/opioid). (NCT01729728)
Timeframe: Baseline; 15 hours post dosing
| Intervention | participants (Number) | ||
|---|---|---|---|
| Supplemental analgesic medication taken | Supplemental opioid analgesic taken | Supplemental non-opioid analgesic taken | |
| Adolescents With Supplementary Analgesic | 12 | 3 | 12 |
| Older Children With Supplementary Analgesic | 18 | 3 | 18 |
| Young and Very Young Children With Supplementary Analgesic | 15 | 8 | 15 |
"Oxygen saturation assessments were performed at pre-defined times during the 15 hour period following investigational medicinal product intake.~Oxygen saturation was assessed using pulse oximetry. The uppermost value is 100%.~Pre-surgery data for these participants is also given from the enrollment Visit (Visit 1)." (NCT01729728)
Timeframe: Enrollment Visit; 15 hours post-dose
| Intervention | percentage of oxygen saturation (Mean) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Visit 1 | Pre-dose | 15 minutes post-dose | 30 minutes post-dose | 1 hour post-dose | 2 hours post-dose | 4 hours post-dose | 6 hours post-dose | 11 hours post-dose | 15 hours post-dose | |
| Oxygen Saturation: Adolescents | 97.8 | 97.7 | 97.3 | 97.0 | 97.3 | 97.1 | 96.9 | 97.1 | 96.8 | 96.7 |
| Oxygen Saturation: Older Children | 97.4 | 96.7 | 96.8 | 96.4 | 96.0 | 95.8 | 96.5 | 96.7 | 96.8 | 96.5 |
| Oxygen Saturation: Young and Very Young Children | 97.4 | 96.8 | 96.5 | 96.8 | 96.2 | 95.8 | 96.5 | 96.7 | 96.4 | 97.1 |
The Face Legs Activity Cry Consolability (FLACC) Scale was developed by the Department of Anesthesiology, University of Michigan Medical School and Health Systems. The FLACC Scale is a behavioral scale for scoring postoperative pain in children between the ages of two months and seven years or in persons unable to communicate. In this trial the scale was used in the young and very young children, i.e. in participants aged 2 to less than 6 years. This tool includes five categories of pain behaviors, including facial expression, leg movement, activity, cry, and consolability. The clinician observes the participant for 5 minutes or more and scores each category with a 0, 1 or 2. The scores are added together for a total score ranging from 0 (no pain) to 10 (worst pain). The higher the total score the higher the pain. (NCT01729728)
Timeframe: Baseline; 15 hours post-dose
| Intervention | units on a scale (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Pre-dose | 15 minutes post-dose | 30 minutes post-dose | 1 hour post-dose | 2 hours post-dose | 4 hours post-dose | 6 hours post-dose | 11 hours post-dose | 15 hours post-dose | |
| Face, Legs, Activity, Cry, Consolability Scale | 4.2 | 1.8 | 1.2 | 1.1 | 0.8 | 1.5 | 0.8 | 0.9 | 0.8 |
"This assessment tool was used in 3 to less than 12 year old participants, i.e. Older Children and Young Children.~The Faces Pain Scale (Revised) [FPS-R] score as allocated to a selected face by the participant. There are 6 faces and the participant is asked to indicate on a face to express how much it hurts.~The numeric value 0 (no pain) to 10 (very much pain) is read off the reverse side of the scale by the clinician." (NCT01729728)
Timeframe: Baseline; 15 hours post-dose
| Intervention | units on a scale (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Pre-dose | 15 minutes post-dose | 30 minutes post-dose | 1 hour post-dose | 2 hours post-dose | 4 hours post-dose | 6 hours post-dose | 11 hours post-dose | 15 hours post-dose | |
| Faces Pain Scale: Older Children | 4.8 | 3.5 | 2.9 | 2.4 | 2.6 | 2.5 | 2.7 | 2.7 | 3.5 |
| Faces Pain Scale: Young Children | 6.8 | 4.5 | 2.8 | 1.8 | 1.2 | 3.5 | 1.8 | 2.3 | 2.8 |
Response rate was defined as the percentage of participants with a 50 percent or greater reduction in pain intensity from baseline to 12, 24, 48, and 72 hours. Pain intensity was assessed on a 11-point numerical rating scale from 0=no pain to 10=pain as bad as you can imagine. Participants with no assessment at the given time point, who used an analgesic medication prior to the time point, or who had worse pain intensity at the time point compared to baseline were assigned a percent reduction of 0 percent. (NCT01813890)
Timeframe: 12, 24, 48 and 72 hours
| Intervention | Percentage of Participants (Number) | |||
|---|---|---|---|---|
| 12 hours | 24 hours | 48 hours | 72 hours | |
| Placebo | 20.0 | 35.0 | 40.0 | 45.0 |
| Tapentadol IR 50 mg | 42.9 | 61.9 | 76.2 | 81.0 |
| Tapentadol IR 75 mg | 57.9 | 73.7 | 68.4 | 68.4 |
Pain Intensity (PI) was assessed on an 11-point numerical rating scale from 0=no pain to 10=pain as bad as you can imagine. PID was the difference between baseline PI (prior to the first dose) and current PI at assessment. SPID was calculated as the time-weighted Sum of PID scores over 12, 24, and 72 hours. Total score ranges from -120 (worst) to 120 (best) for SPID12, -240 (worst) to 240 (best) for SPID24, -720 (worst) to 720 (best) for SPID72. A higher value of SPID indicates greater pain relief. (NCT01813890)
Timeframe: 12, 24 and 72 hours
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| 12 hours | 24 hours | 72 hours | |
| Placebo | 7.6 | 16.7 | 91.6 |
| Tapentadol IR 50 mg | 30.3 | 67.5 | 281.3 |
| Tapentadol IR 75 mg | 34.7 | 82.0 | 316.1 |
Participants rated pain relief on 5-point categorical scale of 0-4 (0=none, 1=A little, 2=Some, 3=A lot, 4=Complete). Pain Intensity (PI) was assessed on an 11-point numerical rating scale from 0=no pain to 10=pain as bad as you can imagine. PID was the difference between baseline PI (prior to the first dose) and current PI at assessment. PRID is the sum of pain relief and PID at the same assessment time. SPRID was calculated as the time-weighted Sum of PRID scores over 12, 24, 48, and 72 hours. Total score ranges from -120 (worst) to 168 (best) for SPRID12, -240 (worst) to 336 (best) for SPRID24, -480 (worst) to 672 (best) for SPRID48, and -720 (worst) to 1008 (best) for SPRID72. A higher value of SPRID indicates greater pain relief. (NCT01813890)
Timeframe: 12, 24, 48 and 72 hours
| Intervention | units on a scale (Mean) | |||
|---|---|---|---|---|
| 12 hours | 24 hours | 48 hours | 72 hours | |
| Placebo | 20.7 | 44.7 | 119.1 | 204.3 |
| Tapentadol IR 50 mg | 52.8 | 115.7 | 284.0 | 468.6 |
| Tapentadol IR 75 mg | 59.1 | 136.0 | 318.4 | 510.2 |
Participants rated pain relief on 5-point categorical scale of 0-4 (0=none, 1=A little, 2=Some, 3=A lot, 4=Complete). Total Pain Relief (TOTPAR) was calculated as the time-weighted sum of pain relief scores up to Hour 12, 24, 48, and 72. Total score ranges from 0 (worst) to 48 (best) for TOTPAR12, 0 (worst) to 96 (best) for TOTPAR24, 0 (worst) to 192 (best) for TOTPAR48, and 0 (worst) to 288 (best) for TOTPAR72. A higher value of TOTPAR indicated greater pain relief. (NCT01813890)
Timeframe: 12, 24, 48, and 72 hours
| Intervention | units on a scale (Mean) | |||
|---|---|---|---|---|
| 12 hours | 24 hours | 48 hours | 72 hours | |
| Placebo | 13.0 | 28.0 | 68.2 | 112.6 |
| Tapentadol IR 50 mg | 22.5 | 48.2 | 115.6 | 187.3 |
| Tapentadol IR 75 mg | 24.4 | 54.1 | 123.5 | 194.1 |
Pain Intensity (PI) was assessed on an 11-point numerical rating scale from 0=no pain to 10=pain as bad as you can imagine. PID was the difference between baseline PI (prior to the first dose) and current PI at assessment. SPID was calculated as the time-weighted Sum of PID scores over 48 hours. Total score ranges from -480 (worst) to 480 (best) for SPID48. A higher value of SPID indicates greater pain relief. (NCT01813890)
Timeframe: 48 hours
| Intervention | units on a scale (Mean) |
|---|---|
| Placebo | 50.8 |
| Tapentadol IR 50 mg | 168.4 |
| Tapentadol IR 75 mg | 194.9 |
Rescue medication was defined as any analgesic medication used for participants discontinued due to lack of efficacy (including those started at time of discontinuation) or analgesic medication used during the double-blind period for completed participants. (NCT01813890)
Timeframe: up to 48 hours
| Intervention | Hours (Median) |
|---|---|
| Placebo | NA |
| Tapentadol IR 50 mg | NA |
| Tapentadol IR 75 mg | NA |
The PGI-C is a 7-point scale that requires the participants to assess how much their illness has improved or worsened relative to a baseline state at the beginning of the intervention. The response options are: 1=very much improved; 2=much improved; 3=minimally improved; 4=no change; 5=minimally worse; 6=much worse; and 7=very much worse. Higher scores indicate worsening. (NCT01813890)
Timeframe: Baseline (Day 1) and 72 hours
| Intervention | Percentage of participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Very Much Improved | Much Improved | Minimally Improved | No Change | Minimally Worse | Much Worse | Very Much Worse | |
| Placebo | 40.0 | 10.0 | 5.0 | 20.0 | 0.0 | 0.0 | 25.0 |
| Tapentadol IR 50 mg | 71.4 | 14.3 | 9.5 | 4.8 | 0.0 | 0.0 | 0.0 |
| Tapentadol IR 75 mg | 73.7 | 5.3 | 10.5 | 0.0 | 0.0 | 0.0 | 10.5 |
Response rate was defined as the percentage of participants with a 30 percent or greater reduction in pain intensity from baseline to 12, 24, 48, and 72 hours. Pain intensity was assessed on a 11-point numerical rating scale from 0=no pain to 10=pain as bad as you can imagine. Participants with no assessment at the given time point, who used an analgesic medication prior to the time point, or who had worse pain intensity at the time point compared to baseline were assigned a percent reduction of 0 percent. (NCT01813890)
Timeframe: 12, 24, 48 and 72 hours
| Intervention | Percentage of Participants (Number) | |||
|---|---|---|---|---|
| 12 hours | 24 hours | 48 hours | 72 hours | |
| Placebo | 35.0 | 40.0 | 45.0 | 45.0 |
| Tapentadol IR 50 mg | 66.7 | 66.7 | 81.0 | 81.0 |
| Tapentadol IR 75 mg | 73.7 | 73.7 | 68.4 | 68.4 |
"The participant scored the EuroQol-5 questionnaire. The EuroQol-5 questionnaire uses a health state classification with 5 dimensions. Each dimension was assessed on a 3-point ordinal scale (1=no problems, 2=some problems, 3=extreme problems). The responses to the five EQ-5D dimensions were scored using a utility-weighted algorithm to derive an EQ-5D health status index score between 0 to 1 (with 1 indicating full health and 0 representing dead). The higher the values (the closer the value is to 1) the better the health status in a treatment group." (NCT01838616)
Timeframe: Baseline (Randomization Visit); End of Continuation Period (Week 12)
| Intervention | units on a scale (Least Squares Mean) |
|---|---|
| Tapentadol Prolonged Release | 0.3395 |
| Oxycodone/Naloxone Prolonged Release | 0.2398 |
"The Hospital Anxiety and Depression Scale (HADS) is a self-assessment scale for the symptom severity of anxiety disorders and depression. It comprises 14 items. Seven statements describe anxiety. Each answer is scored on a four-point scale (0-3). All seven answers are summed to a total score with a maximum score of 21 points. A score below 7 is not considered to indicate anxiety. A score of 11 or above is considered to be a case of anxiety.~A negative sign indicates that there has been a decrease in anxiety since the start of treatment." (NCT01838616)
Timeframe: Baseline (Randomization Visit); End of Continuation Period (Week 12)
| Intervention | units on a scale (Least Squares Mean) |
|---|---|
| Tapentadol Prolonged Release | -2.1 |
| Oxycodone/Naloxone Prolonged Release | -1.1 |
The Hospital Anxiety and Depression Scale (HADS) is a self-assessment scale for the symptom severity of anxiety disorders and depression. It comprises 14 items. Seven statements describe depression. Each answer is scored on a four-point scale (0-3). All seven answers are summed to a total score with a maximum score of 21 points. A score below 7 is not considered to indicate depression. A score of 11 or above is considered to be a case of depression. A decrease in values over time indicates that there has been an improvement. A negative change value indicates a decrease in the depression score since the start of treatment. (NCT01838616)
Timeframe: Baseline (Randomization Visit); End of Continuation Period (Week 12)
| Intervention | units on a scale (Least Squares Mean) |
|---|---|
| Tapentadol Prolonged Release | -2.4 |
| Oxycodone/Naloxone Prolonged Release | -1.1 |
"The painDETECT was a participant completed questionnaire. The questionnaire consists of 14 questions in four domains. Based on these questions a final assessment score was calculated. The minimum score ranged from zero to a maximum of 38. Participants with a score between 0 and 12 were scored as being negative (had no neuropathic pain component). A value between 19 and 38 was rated as being positive (neuropathic component present). Values from 13 to 18 were scored as being unclear. The theoretical range of change in this trial ranged from -38 to 15. A negative change indicated a decrease in their neuropathic component of pain." (NCT01838616)
Timeframe: Baseline (Randomization Visit); End of Continuation Period (Week 12)
| Intervention | units on a scale (Least Squares Mean) |
|---|---|
| Tapentadol Prolonged Release | -10.8 |
| Oxycodone/Naloxone Prolonged Release | -7.9 |
"The recalled average pain intensity score on the NRS-3 was assessed using an 11-point Numeric Rating Scale (NRS), on this scale 0 indicates no pain and 10 indicates pain as bad as you can imagine. This scale recorded the average pain intensity recalled by the participant during the previous 3 days. The participant was asked: Please rate your pain intensity by assessing the one number that best describes your pain on average during the last 3 days (the last 72 hours prior to the visit). A negative sign indicates a decrease in pain from the start of treatment. The higher the absolute values, the greater the change since the start of treatment (baseline visit)." (NCT01838616)
Timeframe: Baseline (Randomization Visit); End of Continuation Period (Week 12)
| Intervention | units on a scale (Least Squares Mean) |
|---|---|
| Tapentadol Prolonged Release | -3.7 |
| Oxycodone/Naloxone Prolonged Release | -2.8 |
"For this pain assessment, the participant indicated the level of average pain experienced over the previous 3 days on an 11-point Numeric Rating Scale (NRS-3) where a score of 0 indicated no pain and a score of 10 indicated pain as bad as you can imagine. The value reported represents the change from the randomization visit (i.e., the last 3 days in the washout period prior to Investigational Medicinal Product initiation and titration) to the end of the continuation period (i.e., up to 9 weeks on the stable dose). The theoretical values range from -10 to 10. A negative sign indicates a decrease in pain from the start of treatment. The higher the absolute values, the greater the change since the start of treatment (Baseline Visit)." (NCT01838616)
Timeframe: Baseline (Randomization Visit); End of Continuation Period (Week 12)
| Intervention | units on a scale (Least Squares Mean) |
|---|---|
| Tapentadol Prolonged Release | -3.7 |
| Oxycodone/Naloxone Prolonged Release | -2.7 |
"The Constipation Assessment (PAC-SYM) is a 12-item self-report questionnaire that assessed the severity of symptoms of constipation. Participants were asked How severe have each of these symptoms been in the last two weeks? e.g. Pain in your stomach. There are 3 subscales: 4 questions on abdominal symptoms, 3 on rectal symptoms and 5 on stool symptoms. Responses were rated on a 5-point Likert scale ranging from 0 (absence of symptom) to 4 (very severe symptoms). If the changes in the overall or subscale scores are positive then there is a worsening in symptoms associated with constipation. The change in the assessment of constipation symptoms (PAC-SYM) total score from the Randomization Visit to the Final Evaluation Visit. The PAC-SYM overall score is the sum of scores of all non-missing items divided by the number of non-missing items (if at least 6 items were non-missing)." (NCT01838616)
Timeframe: Baseline (Randomization Visit); End of Continuation Period (Week 12)
| Intervention | units on a scale (Least Squares Mean) |
|---|---|
| Tapentadol Prolonged Release | 0.07 |
| Oxycodone/Naloxone Prolonged Release | 0.14 |
"The recalled worst pain intensity during the last 24 hours was assessed using an 11-point Numeric rating scale, where 0 = no pain and 10 = pain as bad as you can imagine.~The participant was asked: Please rate your pain intensity by assessing the one number that best describes your worst pain during the last 24 hours prior to the visit.~A negative change indicates that the pain intensity decreased from the start of the trial." (NCT01838616)
Timeframe: Baseline (Randomization Visit); End of Continuation Period (Week 12)
| Intervention | units on a scale (Least Squares Mean) |
|---|---|
| Tapentadol Prolonged Release | -3.7 |
| Oxycodone/Naloxone Prolonged Release | -2.8 |
"Typical dermatomal pain was defined as being pain that radiates beyond the knee towards the foot (sciatica) or pain evoked by stretching of the sciatic nerve.~Therefore, the participant was asked to rate their pain intensity over the past 3 days with regards to this particular pain characteristic.~The recalled average pain intensity during the last 24 hours was assessed using an 11-point Numeric rating scale, where 0 = no pain and 10 = pain as bad as you can imagine.~A negative sign indicates that there was a decrease in the average pain radiating towards or into the leg." (NCT01838616)
Timeframe: Baseline (Randomization Visit); End of Continuation Period (Week 12)
| Intervention | units on a scale (Least Squares Mean) |
|---|---|
| Tapentadol Prolonged Release | -3.9 |
| Oxycodone/Naloxone Prolonged Release | -2.8 |
"In this outcome measure the number of participants affected by early gastrointestinal-related treatment emergent adverse events (TEAEs). As the trial population was opioid-naïve this was considered of interest.~The composition score from participant who reported:~Mild, moderate to severe nausea and/or Mild, moderate to severe vomiting and/or Mild, moderate to severe constipation was evaluated." (NCT01838616)
Timeframe: Baseline (Randomization Visit) to End of Titration Period (End of Week 3)
| Intervention | participants (Number) |
|---|---|
| Tapentadol Prolonged Release | 42 |
| Oxycodone/Naloxone Prolonged Release | 59 |
"In this outcome measure the early gastrointestinal-related treatment emergent events (TEAEs) were evaluated. As the trial population was opioid-naïve this was considered of interest.~The composition score of reported events of Mild, moderate to severe nausea and/or Mild, moderate to severe vomiting and/or Mild, moderate to severe constipation was evaluated." (NCT01838616)
Timeframe: Baseline (Randomization Visit); End of Week 3 (End of Titration Period)
| Intervention | number of events (Number) |
|---|---|
| Tapentadol Prolonged Release | 56 |
| Oxycodone/Naloxone Prolonged Release | 81 |
The sleep evaluation questionnaire was completed by the participant. The participant was asked: How long after bedtime/lights out did you fall asleep last night [hours]? The values are for the night prior to the visits. The negative change from baseline indicates that the time to falling asleep decreased from baseline in a treatment group. (NCT01838616)
Timeframe: Baseline (Randomization Visit); End of Continuation Visit (Week 12)
| Intervention | hours (Least Squares Mean) |
|---|---|
| Tapentadol Prolonged Release | -0.300 |
| Oxycodone/Naloxone Prolonged Release | -0.177 |
The participants were requested to answer the question: How many times did you wake up during the night? The values were calculated from the data that participants self-reported. The change from baseline in the number of times of waking up during the night in a treatment group is reported. A negative symbol indicates that there was a reduction in the number of awakenings. (NCT01838616)
Timeframe: Baseline (Randomization Visit); End of Continuation Period (Week 12)
| Intervention | number of awakenings (Least Squares Mean) |
|---|---|
| Tapentadol Prolonged Release | -0.8 |
| Oxycodone/Naloxone Prolonged Release | -0.5 |
The sleep evaluation questionnaire was completed by the participant. The answer was in response to the question: Sleep evaluation: How long did you sleep last night [hours]? The value reported is the change in the number of hours of sleep from baseline. The positive value indicates that there was an increase in the number of hours of sleep in a treatment group. (NCT01838616)
Timeframe: Baseline (Randomization Visit); End of Continuation Period (Week 12)
| Intervention | hours (Least Squares Mean) |
|---|---|
| Tapentadol Prolonged Release | 0.460 |
| Oxycodone/Naloxone Prolonged Release | 0.412 |
"The participants were requested to answer the following question:~How long did you sleep last night [hours]? The values were calculated from the data that participants self-reported for the night prior to their Randomization Visit (Baseline) and for the night prior to the End of the Continuation Visit (12 weeks after randomization)." (NCT01838616)
Timeframe: Baseline (Randomization Visit); End of Continuation Period (Week 12)
| Intervention | hours (Mean) | |
|---|---|---|
| Baseline | End of Continuation Period | |
| Oxycodone/Naloxone Prolonged Release | 5.675 | 6.218 |
| Tapentadol Prolonged Release | 5.781 | 6.207 |
"The participants were requested to answer the following question:~How many times did you wake up during the night? The values were calculated from the data that participants self-reported for the night prior to their Randomization Visit (Baseline) and for the night prior to the End of the Continuation Visit (12 weeks after randomization)." (NCT01838616)
Timeframe: Baseline (Randomization Visit); End of Continuation Period (Week 12)
| Intervention | number of awakenings (Mean) | |
|---|---|---|
| Baseline | End of Continuation Period | |
| Oxycodone/Naloxone Prolonged Release | 2.6 | 2.2 |
| Tapentadol Prolonged Release | 3.0 | 2.0 |
The sleep evaluation questionnaire was completed by the participant. The participant was asked: How long after bedtime/lights out did you fall asleep last night [hours]? The values are for the night prior to the Randomization Visit (Baseline) and for the night prior to the Final Evaluation Visit (12 weeks after randomization). The higher the value the longer it took to fall asleep. (NCT01838616)
Timeframe: Baseline (Randomization Visit); End of Continuation Period (Week 12)
| Intervention | hours (Mean) | |
|---|---|---|
| Baseline | End of Continuation Period | |
| Oxycodone/Naloxone Prolonged Release | 1.203 | 0.865 |
| Tapentadol Prolonged Release | 1.047 | 0.803 |
"The sleep evaluation questionnaire was completed by the participant. The questionnaire measures 4 main concepts: 1 of the 4 main concepts being the overall quality of sleep.~The participant rated this categorically as being one of the following: excellent, good, fair or poor.~The improvement, no change or worsening is reported based on the replies scored by the participants given at their End of Continuation Visit." (NCT01838616)
Timeframe: Baseline (Randomization Visit); End of Continuation Period (Week 12)
| Intervention | participants (Number) | |||
|---|---|---|---|---|
| Improvement | No Change | Worsening | Missing | |
| Oxycodone/Naloxone Prolonged Release | 43 | 56 | 15 | 12 |
| Tapentadol Prolonged Release | 62 | 46 | 16 | 6 |
The Short Form Health Survey (SF-12) has several brief broad questions on 8 aspects of health (physical functioning, role physical, bodily pain, general health, vitality, social functioning, role-emotional and mental health) that a participant was asked to score over the last week. The physical and mental summary scores were calculated from the individual responses. A higher score indicates a better participant perceived state of health. All domains were scored on a scale from 0 (lowest level of health) to 100 (highest level of health), with 100 representing the best possible health state. (NCT01838616)
Timeframe: Baseline (Randomization Visit); End of Continuation Period (Week 12)
| Intervention | units on a scale (Mean) | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline Physical Functioning | End Continuation Period Physical functioning | Baseline Role-Physical | End Continuation Period Role-Physical | Baseline Bodily Pain | End Continuation Period Bodily Pain | Baseline General Health | End Continuation Period General Health | Baseline Vitality | End Continuation Period Vitality | Baseline Social Functioning | End Continuation Period Social Functioning | Baseline Role-Emotional | End Continuation Period Role-Emotional | Baseline Mental Health | End Continuation Period Mental health | Baseline Physical Component summary | End Continuation Period Physical component summary | Baseline Mental Component Summary | End Continuation Period Mental Component Summary | |
| Oxycodone/Naloxone Prolonged Release | 33.813 | 39.120 | 33.695 | 38.757 | 31.117 | 38.637 | 34.652 | 39.941 | 45.516 | 47.724 | 41.734 | 44.475 | 37.046 | 41.219 | 42.394 | 46.451 | 31.684 | 37.765 | 45.216 | 47.595 |
| Tapentadol Prolonged Release | 33.256 | 41.701 | 33.783 | 41.025 | 30.430 | 42.003 | 36.110 | 44.382 | 46.518 | 51.202 | 42.290 | 47.494 | 41.018 | 44.727 | 44.967 | 49.828 | 30.319 | 40.493 | 48.736 | 51.117 |
"The recalled average pain intensity score on the NRS-3 was assessed using an 11-point Numeric Rating Scale (NRS), on this scale 0 indicates no pain and 10 indicates pain as bad as you can imagine. This scale recalls the average pain intensity during the last 3 days. The participant was asked: Please rate your pain intensity by assessing the one number that best describes your pain on average during the last 3 days (the last 72 hours prior to the visit)." (NCT01838616)
Timeframe: Baseline (Randomization Visit); End of Continuation Period (Week 12)
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Baseline | End of Continuation Period | |
| Oxycodone/Naloxone Prolonged Release | 7.6 | 4.8 |
| Tapentadol Prolonged Release | 7.7 | 3.9 |
"The painDETECT was a participant completed questionnaire. The questionnaire consists of 14 questions in four domains. Based on these questions a final assessment score was calculated. The minimum score ranged from zero to a maximum of 38. Participants with a score between 0 and 12 were scored as being negative (had no neuropathic pain component). A value between 19 and 38 was rated as being positive (neuropathic component present). Values from 13 to 18 were scored as being unclear. The theoretical range of change in this trial ranged from -38 to 15. A negative change indicated a decrease in their neuropathic component of pain." (NCT01838616)
Timeframe: Baseline (Randomization Visit); End of Continuation Period (Week 12)
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Baseline | End of Continuation Period | |
| Oxycodone/Naloxone Prolonged Release | 22.5 | 14.6 |
| Tapentadol Prolonged Release | 22.3 | 11.9 |
The Hospital Anxiety and Depression Scale (HADS) is a self-assessment scale for the symptom severity of anxiety disorders and depression. It comprises 14 items. Seven statements describe depression. Each answer is scored on a four-point scale (0-3). All seven answers are summed to a total score with a maximum score of 21 points. A score below 7 is not considered to indicate depression. A score of 11 or above is considered to be a case of depression. A decrease in values over time indicates that there has been an improvement. (NCT01838616)
Timeframe: Baseline (Randomization Visit); End of Continuation Period (Week 12)
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Baseline | End of Continuation Period | |
| Oxycodone/Naloxone Prolonged Release | 8.0 | 6.5 |
| Tapentadol Prolonged Release | 7.4 | 5.1 |
"The Hospital Anxiety and Depression Scale (HADS) is a self-assessment scale for the symptom severity of anxiety disorders and depression. It comprises 14 items. Seven statements describe anxiety. Each answer is scored on a four-point scale (0-3). All seven answers are summed to a total score with a maximum score of 21 points. A score below 7 is not considered to indicate anxiety. A score of 11 or above is considered to be a case of anxiety.~A decrease in values over the trial period indicate that there has been an improvement." (NCT01838616)
Timeframe: Baseline (Randomization Visit); End of Continuation Period (Week 12)
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Baseline | End of Continuation Period | |
| Oxycodone/Naloxone Prolonged Release | 8.2 | 6.7 |
| Tapentadol Prolonged Release | 7.3 | 5.3 |
"The participant scored the EuroQol-5 questionnaire. The EuroQol-5 questionnaire uses a health state classification with 5 dimensions. Each dimension was assessed on a 3-point ordinal scale (1=no problems, 2=some problems, 3=extreme problems). The responses to the five EQ-5D dimensions were scored using a utility-weighted algorithm to derive an EQ-5D health status index score between 0 to 1 (with 1 indicating full health and 0 representing dead). The higher the values (the closer the value is to 1) the better the health status in a treatment group." (NCT01838616)
Timeframe: Baseline (Randomization Visit); End of Continuation Period (Week 12)
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Baseline | End of Continuation Period | |
| Oxycodone/Naloxone Prolonged Release | 0.3392 | 0.5745 |
| Tapentadol Prolonged Release | 0.3186 | 0.6686 |
"In the Clinician Global Impression of Change (CGIC) the clinician indicated the perceived change over the treatment period. The clinician was requested to choose one of seven categories for each participant. The Clinician rated the participants change as very much improved, much improved, minimally improved, no change, minimally worse, much worse, or very much worse." (NCT01838616)
Timeframe: Baseline (Randomization Visit); End of Continuation Period (Week 12)
| Intervention | participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Very Much Improved | Much Improved | Minimally Improved | No Change | Minimally Worse | Much Worse | Very Much Worse | |
| Oxycodone/Naloxone Prolonged Release | 18 | 25 | 37 | 26 | 7 | 9 | 1 |
| Tapentadol Prolonged Release | 32 | 44 | 22 | 21 | 6 | 3 | 0 |
"The Short Form Health Survey (SF-12) has several brief broad questions on 8 aspects of health (physical functioning, role physical, bodily pain, general health, vitality, social functioning, role-emotional and mental health) that a participant was asked to score over the last week. The physical and mental summary scores were calculated from the individual responses. A higher score indicates a better participant perceived state of health. All domains were scored on a scale from 0 (lowest level of health) to 100 (highest level of health), with 100 representing the best possible health state.~The change in the SF-12 score shows an improvement in health from baseline if the values are positive. The higher the value the greater the improvement since starting the trial." (NCT01838616)
Timeframe: Baseline (Randomization Visit); End of Continuation Period (Week 12)
| Intervention | units on a scale (Least Squares Mean) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Physical Functioning | Role-Physical | Bodily Pain | General Health | Vitality | Social Functioning | Role-Emotional | Mental Health | Physical Component Summary | Mental Component Summary | |
| Oxycodone/Naloxone Prolonged Release | 5.073 | 4.668 | 7.458 | 4.309 | 1.468 | 2.286 | 2.587 | 2.973 | 6.202 | 1.146 |
| Tapentadol Prolonged Release | 8.358 | 7.260 | 10.990 | 8.447 | 4.943 | 5.246 | 4.764 | 5.158 | 9.735 | 3.077 |
In the Neuropathic Pain Symptom Inventory (NPSI) the participant rated their symptoms of neuropathic pain. Ten pain questions were answered on an 11-point scale, from 0 (symptom not present) to 10 (symptom at its worst imaginable intensity, e.g. worst burning imaginable). The overall NPSI score was calculated by the summation of all ten responses and ranges between 0 and 1. For pain descriptions burning, pressing, paroxysmal (pain like electric shocks or stabbing), evoked (due to touch) and paresthesia (sensation that is not unpleasant) or dysesthesia (unpleasant) sub-scores are reported. The overall values reported for all participants that completed the questionnaire are shown. A symptom was absent if the value is 0, the symptom was present in all participants and all participants rated it at its worst possible intensity if a value is 1. A negative change indicates that the intensity of the symptom has decreased since the start of treatment. (NCT01838616)
Timeframe: Baseline (Randomization Visit); End of Continuation Period (Week 12)
| Intervention | units on a scale (Least Squares Mean) | |||||
|---|---|---|---|---|---|---|
| Overall Score | Sub-Score Burning Pain | Sub-Score Pressing Pain | Sub-Score Paroxysmal Pain | Sub-score Evoked Pain | Sub-Score Pare/Dysesthesia | |
| Oxycodone/Naloxone Prolonged Release | -0.248 | -0.278 | -0.226 | -0.283 | -0.225 | -0.252 |
| Tapentadol Prolonged Release | -0.353 | -0.375 | -0.331 | -0.385 | -0.334 | -0.363 |
"Typical dermatomal pain was defined as being pain that radiates beyond the knee towards the foot (sciatica) or pain evoked by stretching of the sciatic nerve.~The participant was asked to rate their pain intensity over the past 3 days with regards to this particular pain characteristic.~The recalled average pain intensity over the past 3 days for the pain radiating towards or into the leg was assessed by the participant using an 11-point Numeric rating scale, where 0 = no pain and 10 = pain as bad as you can imagine." (NCT01838616)
Timeframe: Baseline (Randomization Visit); End of Continuation Period (Week 12)
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Baseline | End of Continuation Period | |
| Oxycodone/Naloxone Prolonged Release | 7.6 | 4.7 |
| Tapentadol Prolonged Release | 7.5 | 3.7 |
"In the Patient Global Impression of Change (PGIC) the participant indicated the perceived change over the treatment period. PGIC is a 7 point scale depicting a patient's rating of overall improvement. Patients rate their change as very much improved, much improved, minimally improved, no change, minimally worse, much worse, or very much worse." (NCT01838616)
Timeframe: Baseline (Randomization Visit); End of Continuation Period (Week 12)
| Intervention | participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Very Much Improved | Much Improved | Minimally Improved | No Change | Minimally Worse | Much Worse | Very Much Worse | |
| Oxycodone/Naloxone Prolonged Release | 18 | 19 | 46 | 29 | 6 | 4 | 3 |
| Tapentadol Prolonged Release | 27 | 43 | 32 | 21 | 3 | 2 | 1 |
In the Neuropathic Pain Symptom Inventory (NPSI) the participant rated their symptoms of neuropathic pain. Ten pain questions were answered on an 11-point scale; from 0 (symptom not present) to 10 (symptom at its worst imaginable intensity, e.g. worst burning imaginable). The overall NPSI score was calculated by the summation of all ten responses and ranges between 0 and 1. For pain descriptions burning, pressing, paroxysmal (pain like electric shocks or stabbing), evoked (due to touch) and paresthesia (sensation that is not unpleasant) or dysesthesia (unpleasant) sub-scores are reported. The overall values reported for all participants that completed the questionnaire are shown. A symptom was absent if the value is 0, the symptom was present in all participants and all participants rated it at its worst possible intensity if a value is 1. (NCT01838616)
Timeframe: Baseline (Randomization Visit); End of Continuation Period (Week 12)
| Intervention | units on a scale (Mean) | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline Overall Score | End Continuation Period Overall Score | Baseline Sub-Score Burning Pain | End Continuation Period Sub-Score Burning Pain | Baseline Sub-score pressing pain | End Continuation Period Sub-Score Pressing Pain | Baseline Sub-Score Paroxysmal Pain | End Continuation Period Sub-Score Paroxysmal Pain | Baseline Sub-Score Evoked Pain | End Continuation Period Sub-Score Evoked Pain | Baseline Sub-Score Pare/Dysesthesia | End Continuation Period Sub-Score Pare/Dysesthesia | |
| Oxycodone/Naloxone Prolonged Release | 0.612 | 0.354 | 0.634 | 0.337 | 0.608 | 0.375 | 0.670 | 0.375 | 0.548 | 0.321 | 0.642 | 0.372 |
| Tapentadol Prolonged Release | 0.598 | 0.251 | 0.612 | 0.248 | 0.595 | 0.276 | 0.638 | 0.269 | 0.555 | 0.219 | 0.621 | 0.260 |
"The recalled worst pain intensity during the last 24 hours was assessed using an 11-point Numeric rating scale, where 0 = no pain and 10 = pain as bad as you can imagine.~The participant was asked: Please rate your pain intensity by assessing the one number that best describes your worst pain during the last 24 hours prior to the visit" (NCT01838616)
Timeframe: Baseline (Randomization Visit); End of Continuation Period (Week 12)
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Baseline | End of Continuation Period | |
| Oxycodone/Naloxone Prolonged Release | 8.0 | 5.2 |
| Tapentadol Prolonged Release | 8.1 | 4.3 |
The mean amount of supplemental opioid analgesic medication (SOAM) used in the Full Analysis Set subset aged from birth to less than 2 years old was determined from 0 to 12 hours and from 0 to 24 hours after first intake of IMP. SOAM use is expressed in mg/kg of morphine i.v. equivalents. (NCT02081391)
Timeframe: Up to 24 hours
| Intervention | mg/kg (Mean) | |
|---|---|---|
| 0-12 hours | 0-24 hours | |
| Placebo (From Birth to <2 Years) | 0.01 | 0.016 |
| Tapentadol (From Birth to <2 Years) | 0.03 | 0.054 |
"Palatability of IMP after the first dose was assessed in participants aged 2 years to less than 18 years using 5-point hedonic scales in combination with verbal rating. A question How does the medication taste was asked and the verbal rating was from really good, good, a bit good/a bit bad, bad, and really bad. The pictorial scale of facial expressions was co-related with verbal rating range where 5 = really good, 4 = good, 3 = a bit good/a bit bad, 2 = bad, and 1 = really bad. Higher scores represent good palatability. Responses were summarized. Missing values were not imputed.~Palatability data was not collected for participants <2 years old." (NCT02081391)
Timeframe: Up to 96 hours
| Intervention | Participants (Count of Participants) | |||||
|---|---|---|---|---|---|---|
| Really bad | Bad | A bit bad / a bit good | Good | Really good | Missing | |
| Placebo (From 2 to <18 Years) | 2 | 2 | 10 | 24 | 11 | 3 |
| Tapentadol (From 2 to <18 Years) | 13 | 28 | 36 | 24 | 6 | 1 |
The median amount of supplemental opioid analgesic medication (SOAM) used in the Full Analysis Set subset aged from birth to less than 2 years old was determined from 0 to 12 hours and from 0 to 24 hours after first intake of IMP. SOAM use is expressed in mg/kg of morphine i.v. equivalents. (NCT02081391)
Timeframe: Up to 24 hours
| Intervention | mg/kg (Median) | |
|---|---|---|
| 0-12 hours | 0-24 hours | |
| Placebo (From Birth to <2 Years) | 0.01 | 0.013 |
| Tapentadol (From Birth to <2 Years) | 0.00 | 0.016 |
"Palatability of IMP after the last dose in participants aged 2 years to less than 18 years was assessed using 5-point hedonic scales in combination with verbal rating. A question How does the medication taste was asked and the verbal rating was from really good, good, a bit good/a bit bad, bad, and really bad. The pictorial scale of facial expressions was co-related with verbal rating range with 5 = really good, 4 = good, 3 = a bit good/a bit bad, 2 = bad, and 1 = really bad. Higher scores represent good palatability. Responses were summarized. Missing values were not imputed.~Palatability data was not collected in participants <2 years old." (NCT02081391)
Timeframe: Up to 96 hours
| Intervention | Participants (Count of Participants) | |||||
|---|---|---|---|---|---|---|
| Really bad | Bad | A bit bad / a bit good | Good | Really good | Missing | |
| Placebo (From 2 to <18 Years) | 1 | 3 | 14 | 16 | 12 | 6 |
| Tapentadol (From 2 to <18 Years) | 14 | 15 | 38 | 28 | 5 | 8 |
"For children and adolescents aged 12 years to less than 18 years, pain intensity was assessed by the use of a Visual analog scale (VAS). The participant was asked to draw a single line to indicate the current level of pain intensity on a 100 mm long scale by marking a point on the line in response to: My pain right now is. The mark was scored between no pain and pain as bad as it could be. A value of 0 indicates no pain. A value of 100 indicates pain as bad as it could be. Pain intensity scores were obtained before and after first dose of IMP, and before each subsequent dose of IMP, whenever possible. Changes from baseline values were summarized descriptively for each time point." (NCT02081391)
Timeframe: Up to 96 hours
| Intervention | units on a scale (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| 30-60 mins after 1st IMP | Before 2nd dose of IMP | Before 3rd dose of IMP | Before 4th dose of IMP | Before 5th dose of IMP | Before 6th dose of IMP | Before 7th dose of IMP | Before 8th dose of IMP | At End of Treatment | |
| Placebo (12 to <18 Years) | 6.4 | 6.0 | 5.9 | 5.1 | -2.7 | 6.6 | 15.0 | 11.9 | 11.4 |
| Tapentadol (12 to <18 Years) | 8.0 | 6.5 | 13.1 | 8.8 | 13.0 | 13.0 | 10.7 | 12.2 | 11.0 |
"The time to first and time to second patient-controlled analgesia (PCA) or nurse-controlled analgesia (NCA) after the first dose of IMP were summarized descriptively using time-to-event methods and are displayed by relevant treatment groups. Participants who completed the End of Treatment Visit (scheduled for 96 hours after first IMP) before their first/second use of NCA/PCA or participants who terminated treatment before their first/second use of NCA/PCA were censored at the End of Treatment Visit.~Time-to-event variables are reported using Kaplan-Meier analyses. Therefore, values might remain missing if the survival function does not reach a respective threshold. This is indicated by not applicable (NA)." (NCT02081391)
Timeframe: Up to 96 hours
| Intervention | minutes (Median) | |
|---|---|---|
| Time to first NCA/PCA administration | Time to second NCA/PCA administration | |
| Placebo (From 2 to <18 Years) | 131.5 | 388.0 |
| Placebo (From Birth to <2 Years) | 155.0 | NA |
| Tapentadol (From 2 to <18 Years) | 183.0 | 572.0 |
| Tapentadol (From Birth to <2 Years) | 960.0 | NA |
"The total amount of supplemental opioid analgesic medication (SOAM) received was assessed in 12-hour intervals from 24 hours to 96 hours after the first dose of IMP for participants who were administered SOAM.~SOAM use was expressed in mg/kg of morphine i.v. equivalents." (NCT02081391)
Timeframe: Up to 96 hours
| Intervention | mg/kg (Mean) | |
|---|---|---|
| 24 h to 36 h | 36 h to 48 h | |
| Placebo (From Birth to <2 Years) | 0.003 | 0.000 |
| Tapentadol (From Birth to <2 Years) | 0.020 | 0.000 |
"The total amount of supplemental opioid analgesic medication (SOAM) received was assessed in 12-hour intervals from 24 hours to 96 hours after the first dose of IMP for participants who were administered SOAM.~SOAM use was expressed in mg/kg of morphine i.v. equivalents." (NCT02081391)
Timeframe: Up to 96 hours
| Intervention | mg/kg (Mean) | ||||
|---|---|---|---|---|---|
| 24 h to 36 h | 36 h to 48 h | 48 h to 60 h | 60 h to 72 h | 72 h to 84 h | |
| Placebo (From 2 to <18 Years) | 0.14 | 0.06 | 0.06 | 0.03 | 0.0 |
| Tapentadol (From 2 to <18 Years) | 0.08 | 0.06 | 0.05 | 0.06 | 0.0 |
"For children aged 6 years (if possible) to less than 12 years, pain intensity was assessed by the use of the Faces Pain Scale-Revised (FPS-R). The FPS-R is a validated self-reported 6-point scale (0, 2, 4, 6, 8, 10) with 0 representing no pain and 10 representing very much pain. Facial representations were used to indicate how much the pain hurts. Higher scores represent worse condition.~Pain intensity scores were obtained before and after first dose of IMP, and before each subsequent dose of IMP, whenever possible.~Changes from baseline pain values were summarized descriptively for each time point up to end of treatment (96 hours)." (NCT02081391)
Timeframe: Up to 96 hours
| Intervention | units on a scale (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| 30-60 mins after 1st IMP | Before 2nd dose of IMP | Before 3rd dose of IMP | Before 4th dose of IMP | Before 5th dose of IMP | Before 6th dose of IMP | Before 7th dose of IMP | Before 8th dose of IMP | At End of Treatment | |
| Placebo (6 to <12 Years) | 0.7 | 0.5 | -0.2 | -0.3 | 0 | 0.2 | 0.7 | 0.2 | 3.4 |
| Tapentadol (6 to <12 Years) | 1.0 | 1.0 | 1.0 | 1.3 | 0.8 | 0.5 | 2.0 | 1.3 | 2.8 |
"The FLACC scale was used for children from birth to less than 6 years, or in older children who were not able to report their pain using the other scales. This tool includes 5 categories of pain behaviors: facial expression (F), leg movement (L), activity (A), cry (C), and consolability (C). Each of the 5 categories is scored 0, 1 or 2. The total score between 0 and 10 is the sum of the 5 individual categories. Higher scores represent worse condition.~The Pain intensity scores were obtained before and after first dose of IMP, and before each subsequent dose of IMP, whenever possible, up to end of treatment (96 hours).~Changes from baseline values were summarized descriptively for each time point." (NCT02081391)
Timeframe: Up to 96 hours
| Intervention | score on a scale (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| 30-60 mins after 1st IMP | Before 2nd dose of IMP | Before 3rd dose of IMP | Before 4th dose of IMP | Before 5th dose of IMP | Before 6th dose of IMP | Before 7th dose of IMP | Before 8th dose of IMP | At End of Treatment | |
| Placebo (From 2 to <6 Years) | 1.9 | 1.3 | 1.6 | 1.3 | 1.9 | 2.3 | 2.1 | 2.2 | 2.0 |
| Placebo (From Birth to <2 Years) | 2.8 | 1.0 | -1.3 | 0.0 | 2.0 | 2.5 | 2.0 | -0.5 | 3.5 |
| Tapentadol (From 2 to <6 Years) | 1.1 | 1.4 | 1.7 | 1.4 | 1.8 | 1.6 | 1.6 | 1.2 | 2.4 |
| Tapentadol (From Birth to <2 Years) | 1.4 | 0.7 | 2.0 | 1.3 | 1.4 | 2.0 | 1.9 | 3.8 | 2.1 |
The primary endpoint for the United States Food and Drug Administration (US FDA) (and secondary endpoint for the Pediatric Committee of the European Medicines Agency [EU PDCO]) was the total amount of supplemental opioid analgesic medication (SOAM) used in the Full Analysis Set (from 2 years to <18 years old) within 12 hours after first intake of IMP. SOAM use is expressed in mg/kg of morphine i.v. equivalents. (NCT02081391)
Timeframe: Up to 12 hours
| Intervention | mg/kg (Least Squares Mean) |
|---|---|
| Tapentadol (From 2 to <18 Years) | 0.08 |
| Placebo (From 2 to <18 Years) | 0.13 |
The primary endpoint for the EU PDCO (and secondary endpoint for the US FDA) was the total amount of supplemental opioid analgesic medication (SOAM) used in the Full Analysis Set (from 2 years to <18 years old) within 24 hours after first intake of IMP. SOAM use is expressed in mg/kg of morphine i.v. equivalents. (NCT02081391)
Timeframe: Up to 24 hours
| Intervention | mg/kg (Least Squares Mean) |
|---|---|
| Tapentadol (From 2 to <18 Years) | 0.14 |
| Placebo (From 2 to <18 Years) | 0.24 |
"Pain intensity was assessed by scoring Pain right now using the Visual Analog Scale (VAS) as well as the Faces Pain Scale-Revised (FPS-R) at each visit. The pain intensity was first documented using the VAS and directly thereafter the FPS-R. If required, pain intensity assessments could be assisted by the legal guardian or a health care provider.~The VAS is scored from 0, equivalent to no pain, to 100, equivalent to pain as bad as it could be. The FPS-R is a validated self-reported 6-point scale with 0 representing no pain and 10 representing very much pain. Facial representations were used to indicate how much the pain hurts.~The pain right now score at the tapentadol baseline (last evaluation before or at Day 15) and at the last assessment for those subjects who completed the 12 months treatment of Part 2 were used for the calculation of the change in pain intensity from the tapentadol baseline." (NCT02151682)
Timeframe: From Day 15 to Day 379 (End of Part 2)
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Pain intensity change (FPR-S) from Day 15 | Pain intensity change (VAS) from Day 15 | |
| Tapentadol Prolonged-release (Part 2) | 0 | -11.7 |
"Pain intensity was assessed by scoring Pain right now twice daily up to Day 14 by every participant using the Visual Analog Scale (VAS) as well as the Faces Pain Scale-Revised (FPS-R) in an electronic diary. Pain intensity was first documented using the VAS and directly thereafter the FPS-R. If required, pain intensity diary entry could be assisted by the legal guardian or a health care provider.~The VAS is scored from 0, equivalent to no pain, to 100, equivalent to pain as bad as it could be.~The FPS-R is a validated self-reported 6-point scale with 0 representing no pain and 10 representing very much pain. Facial representations were used to indicate how much the pain hurts.~The pain right now scores at baseline (last evaluation before starting IMP) and the mean of last 6 assessments collected up to the time point of last IMP intake in Part 1 (i.e., Day 14 or the day of early discontinuation) were used for the calculation of the change in pain intensity from baseline." (NCT02151682)
Timeframe: From Baseline up to Day 14 (End of Part 1) or early discontinuation
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Pain intensity change from Baseline (FPS-R) | Pain intensity change from Baseline (VAS) | |
| Morphine Prolonged-release (Part 1) | -2.0 | -23.4 |
| Tapentadol Prolonged-release (Part 1) | -1.9 | -18.8 |
"Opiate withdrawal symptoms were assessed using the Subjective Opiate Withdrawal Scale (SOWS) questionnaire. The SOWS is designed to reflect common motoric, autonomic, musculoskeletal, and psychic signs and symptoms of opiate withdrawal. Each participant was requested to rate the first 15 items of the 16-item questionnaire for 7 days after last IMP intake. Participants rated the intensity of specific signs and symptoms on a scale of 0 (not at all) to 4 (extremely). The minimum overall score is 0, the maximum score is 64.~SOWS Total Score at baseline (i.e., for Part 1 = Day 14-17, for Part 2 = Day 352-380, or the day after an early termination visit (Part 1/2)), and changes from baseline 2-7 days after last intake of IMP in Part 1 (= up to Day 23) and in Part 2 (= up to Day 386) are presented." (NCT02151682)
Timeframe: From Day 1 to Day 386 (End of Part 2 + 7 days)
| Intervention | units on a scale (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| Total score at baseline | Change Day 2 after last IMP intake | Change Day 3 after last IMP intake | Change Day 4 after last IMP intake | Change Day 5 after last IMP intake | Change Day 6 after last IMP intake | Change Day 7 after last IMP intake | |
| Morphine Prolonged-release (Part 1) | 4.0 | -0.4 | -1.6 | -1.7 | -1.6 | -2.3 | -2.7 |
| Tapentadol Prolonged-release (Part 1) | 6.9 | -1.7 | -2.3 | -3.9 | -3.8 | -3.6 | -5.1 |
| Tapentadol Prolonged-release (Part 2) | 6.1 | -0.7 | -0.3 | -0.1 | 0 | -0.6 | -1.4 |
The time to discontinuation from IMP due to treatment emergent adverse events (TEAEs) was analyzed for tapentadol PR treatment in Part 2 of the study. (NCT02151682)
Timeframe: From first day in Part 2 (Day 15) to last day in Part 2 (Day 379)
| Intervention | weeks (Mean) |
|---|---|
| Tapentadol Prolonged-release (Part 2) | 5.3 |
"The proportion of participants classified as responders was assessed and compared between the treatment groups.~A participant was defined as responder if both of the following criteria were met:~Completion of the 14-day Treatment Period (Part 1).~One of the following calculated from the scheduled pain assessments (pain right now) documented during the last 3 days of the Treatment Period:~Average pain less than 50 on a visual analog scale (VAS, range 0 [no pain] to 100 [pain as bad as it could be]) for participants aged 12 years to less than 18 years; or less than 5 on the Faces Pain Scale-revised (FPS-R, range 0 [no pain] and 10 [very much pain]) for participants aged 6 years to less than 12 years.~Average reduction from baseline of pain greater than or equal to 20 on a VAS for participants aged 12 years to less than 18 years; or greater than or equal to 2 on the FPS-R for participants aged 6 years to less than 12 years." (NCT02151682)
Timeframe: From Day 1 up to Day 14 (End of Part 1)
| Intervention | Participants (Count of Participants) |
|---|---|
| Morphine Prolonged-release (Part 1) | 19 |
| Tapentadol Prolonged-release (Part 1) | 32 |
"Tapentadol serum concentrations were measured in participants in the tapentadol treatment arm (Part 1).~All participants who had quantifiable serum concentrations during the Treatment Period were included in the descriptive pharmacokinetic analysis. Data from participants who vomited within 6 hours of administration of IMP during the Treatment Period were carefully assessed to decide if the data should be included in the pharmacokinetic analysis." (NCT02151682)
Timeframe: From Day 1 to Day 14 (End of Part 1)
| Intervention | nanograms per milliliter (Mean) | |
|---|---|---|
| Day 1 | Day 14 | |
| Tapentadol Prolonged-release (12 Years to Less Than 18 Years) | 19.9 | 48.5 |
| Tapentadol Prolonged-release (6 Years to Less Than 12 Years) | 17.2 | 35.6 |
| Tapentadol Prolonged-release (All Participants) | 19.1 | 44.7 |
"Tapentadol-O-glucuronide is a metabolite of tapentadol. The body transforms tapentadol into its metabolites so that it can be more easily/quickly removed from the body. Tapentadol-O-glucuronide serum concentrations were measured in participants who received tapentadol PR in Part 1.~All participants who had quantifiable serum concentrations were included in the descriptive pharmacokinetic analysis. Data from participants who vomited within 6 hours of administration of IMP during Part 1 were carefully assessed to decide if they should be included in the pharmacokinetic analysis." (NCT02151682)
Timeframe: From Day 1 to Day 14 (End of Part1)
| Intervention | nanograms per milliliter (Mean) | |
|---|---|---|
| Day 1 | Day 14 | |
| Tapentadol Prolonged-release (12 Years to Less Than 18 Years) | 786.7 | 1700.3 |
| Tapentadol Prolonged-release (6 Years to Less Than 12 Years) | 603.2 | 1223.8 |
| Tapentadol Prolonged-release (All Participants) | 731.7 | 1557.3 |
The time to discontinuation from IMP due to lack of efficacy was analyzed for tapentadol PR treatment in Part 2 of the trial. (NCT02151682)
Timeframe: From first day in Part 2 (Day 15) to last day in Part 2 (Day 379)
| Intervention | weeks (Mean) |
|---|---|
| Tapentadol Prolonged-release (Part 2) | 30.9 |
"Morphine oral solution could be given during Part 1 as rescue medication in both treatment groups. The dose per rescue medication intake was 1/6 of the total daily dose of the scheduled tapentadol or morphine PR intakes. Rescue medication administration times and doses were recorded.~18 Participants in the morphine PR group and 27 participants in the tapentadol PR group had no documented intake of rescue medication between Day 1 and Day 14.~Summary statistics were calculated based on participants with any intake, i.e., those that took at least 1 dose of rescue medication. The mean (standard deviation) time (hours) to first dose of rescue medication following the first dose of the IMP (on Day 1) is presented." (NCT02151682)
Timeframe: From Day 1 up to Day 14 (End of Part 1)
| Intervention | hours (Mean) | |
|---|---|---|
| Participants with rescue medication intake | Participants with no rescue medication intake | |
| Morphine Prolonged-release (Part 1) | 39.7 | NA |
| Tapentadol Prolonged-release (Part 1) | 74.6 | NA |
"The time to discontinuation from IMP due to treatment emergent adverse events (TEAEs) was analyzed for both treatment arms (tapentadol PR and morphine PR) in Part 1 of the study.~Note that no participant discontinued due to a TEAE in the morphine PR arm, and 2 participants in the tapentadol PR arm." (NCT02151682)
Timeframe: From first day in Part 1 (Day 1) to last day in Part 1 (Day 14)
| Intervention | days (Mean) |
|---|---|
| Morphine Prolonged-release (Part 1) | NA |
| Tapentadol Prolonged-release (Part 1) | 3.0 |
"Tolerability was assessed by the number of participants with exactly 1 to more than 5 treatment emergent adverse events (TEAE) by treatment group during the different trial periods, on a participant level.~In addition, tolerability was assessed by the number of participants with TEAEs which were considered by the investigator to be at least possibly related to the treatment the participant received." (NCT02151682)
Timeframe: Part 1: Day 1 (Start of Part 1) to Day 14; Part 2: Day 15 to Day 379 (End of Part 2)
| Intervention | participants (Number) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Participants without any TEAE | Participants with at least 1 TEAE | Participants with exactly 1 TEAE | Participants with exactly 2 TEAEs | Participants with exactly 3 TEAEs | Participants with exactly 4 TEAEs | Participants with exactly 5 TEAEs | Participants with more than 5 TEAEs | Participants with related TEAEs | |
| Morphine Prolonged-release (Part 1) | 12 | 12 | 1 | 2 | 2 | 2 | 1 | 4 | 6 |
| Tapentadol Prolonged-release (Part 1) | 19 | 26 | 7 | 5 | 4 | 1 | 3 | 6 | 12 |
| Tapentadol Prolonged-release (Part 2) | 6 | 30 | 5 | 2 | 2 | 4 | 3 | 14 | 13 |
"Due to an overall low intake of rescue medication, it was not appropriate to present the number of doses of oral morphine solution used at different dose levels of investigational medicinal product (IMP) but the average daily dose (milligrams per kilogram body weight) for the treatment period and a modified average daily dose. Average daily dose and modified average daily dose were both calculated based on drug accountability.~For the modified average daily doses, implausible values were excluded from the analysis, i.e., the amount of rescue medication that was lost due to a broken bottle was excluded from the analysis and negative amounts of rescue medication intakes due to measurement inaccuracies for bottle weights were considered as no intake." (NCT02151682)
Timeframe: From Day 1 up to Day 14 (End of Part 1)
| Intervention | milligrams per kilogram per day (Mean) | |
|---|---|---|
| Average daily dose | Modified average daily dose | |
| Morphine Prolonged-release (Part 1) | 0.07 | 0.08 |
| Tapentadol Prolonged-release (Part 1) | 0.46 | 0.11 |
"Constipation was assessed using the modified constipation assessment scale (mCAS). This is an 8-item questionnaire where the observer has scored constipation on a nominal scale (no problem [score 0], some problem [score 1] or severe problem [score 2]). The response to an item could also be scored as unable to assess.~The Total Score can vary from 0-16; the higher the Total Score the higher the extent of constipation. A positive change from baseline to last assessment indicates a worsening, a negative change an improvement." (NCT02151682)
Timeframe: From baseline (Day 15 or switch) to last assessment (up to Day 379 of Part 2)
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| Baseline | Last assessment | Change from baseline | |
| Observation Period After Morphine in Part 1 | 2.5 | 0.4 | -1.6 |
| Observation Period After Tapentadol in Part 1 | 1.8 | 0.4 | -1.4 |
| Observation Period After Tapentadol in Part 2 | 1.5 | 0.8 | -1.4 |
| Tapentadol in Part 2 After Tapentadol or Morphine in Part 1 | 2.3 | 1.8 | -0.7 |
"Constipation was assessed using the modified constipation assessment scale (mCAS). This is an 8-item questionnaire where the observer has scored constipation on a nominal scale (no Problem [score 0], some problem [score 1] or severe Problem [score 2]). The response to an item could also be scored as unable to assess.~The Total Score can vary from 0-16; the higher the Total Score the higher the extent of constipation. A positive change from Day 1 to Day 14 indicates a worsening, a negative change an improvement." (NCT02151682)
Timeframe: From Day 1 to Day 14 (End of Part 1)
| Intervention | score on a scale (Mean) | ||
|---|---|---|---|
| Day 1 | Day 14 | Change from Day 1 | |
| Morphine Prolonged-release (Part 1) | 2.7 | 2.7 | -0.1 |
| Tapentadol Prolonged-release (Part 1) | 1.5 | 1.8 | 0.4 |
"The pharmacokinetic profile of Tapentadol and its major metabolite tapentadol-O-glucuronide was evaluated to enable data based recommendations for the use of Tapentadol in children of different ages.~Each participant had a single pharmacokinetic sample taken at up to 2 different pre-defined time points.~Serum was analyzed using liquid chromatography-tandem mass spectrometry. Mean and Standard Deviation of Serum Concentrations of tapentadol-O-glucuronide were calculated.~Summary statistics at a given time point were only determined if at least 2 participants had observations above the lower limit of quantification (LLOQ).~If overall only a single sample was available at one of the pre-defined time points, the measured value is presented and the standard deviation is given as N/A." (NCT02221674)
Timeframe: Up to 8 hours after IMP
| Intervention | nanogram per milliliter (Mean) | |||||
|---|---|---|---|---|---|---|
| 30 minutes after administration | 1 hour after administration | 2 hours after administration | 4 hours after administration | 6 hours after administration | 8 hours after administration | |
| Participants Aged 6 Months to Less Than 2 Years - PK Set | 105.7 | 430.7 | 468.0 | 348.7 | 370.2 | 285.1 |
"The pharmacokinetic profile of Tapentadol and its major metabolite tapentadol-O-glucuronide was evaluated to enable data based recommendations for the use of Tapentadol in children of different ages.~Each participant had a single pharmacokinetic sample taken at up to 2 different pre-defined time points.~Serum was analyzed using liquid chromatography-tandem mass spectrometry. Mean and Standard Deviation of Serum Concentrations of Tapentadol were calculated.~Summary statistics at a given time point were only determined if at least 2 participants had observations above the lower limit of quantification (LLOQ).~If overall only a single sample was available at one of the pre-defined time points, the measured value is presented and the standard deviation is given as N/A." (NCT02221674)
Timeframe: Up to 8 hours after IMP
| Intervention | nanogram per milliliter (Mean) | |||||
|---|---|---|---|---|---|---|
| 30 minutes after administration | 1 hour after administration | 2 hours after administration | 4 hours after administration | 6 hours after administration | 8 hours after administration | |
| Participants Aged From Birth to Less Than 1 Month - PK Set | 26.62 | 43.63 | 19.9 | 15.0 | 18.82 | 14.6 |
"The pharmacokinetic profile of Tapentadol and its major metabolite tapentadol-O-glucuronide was evaluated to enable data based recommendations for the use of Tapentadol in children of different ages.~Each participant had a single pharmacokinetic sample taken at up to 2 different pre-defined time points.~Serum was analyzed using liquid chromatography-tandem mass spectrometry. Mean and Standard Deviation of Serum Concentrations of tapentadol-O-glucuronide were calculated.~Summary statistics at a given time point were only determined if at least 2 participants had observations above the lower limit of quantification (LLOQ).~If overall only a single sample was available at one of the pre-defined time points, the measured value is presented and the standard deviation is given as N/A." (NCT02221674)
Timeframe: Up to 8 hours after IMP
| Intervention | nanogram per milliliter (Mean) | |||||
|---|---|---|---|---|---|---|
| 30 minutes after administration | 1 hour after administration | 2 hours after administration | 4 hours after administration | 6 hours after administration | 8 hours after administration | |
| Participants Aged From Birth to Less Than 1 Month - PK Set | 74.38 | 209 | 98.5 | 147.6 | 224.8 | 174.1 |
"The change from baseline in pain intensity using the Face, Legs, Activity, Cry, Consolability Scale (FLACC Scale) at 15 minutes, 30 minutes, 1 hour, 2 hours, 4 hours, 6 hours, 8 hours, 12 hours, and 15 hours after a single dose of tapentadol.~The FLACC Scale is a behavioral scale for scoring postoperative pain in young children. It includes five categories of pain behaviors, including facial expression, leg movement, activity, cry, and consolability. The scale is scored in a range of 0-10 with 0 representing no pain.~The pain intensity scores were summarized descriptively per scheduled time point." (NCT02221674)
Timeframe: Baseline; up to 15 hours after study medication
| Intervention | units on a scale (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| 15 minutes after administration | 30 minutes after administration | 1 hour after administration | 2 hours after administration | 4 hours after administration | 6 hours after administration | 8 hours after administration | 12 hours after administration | 15 hours after administration | |
| Participants Aged 1 Month to Less Than 6 Months. | -1.3 | -3.0 | -2.7 | -3.0 | -2.2 | -1.7 | -3.0 | -3.5 | -3.8 |
| Participants Aged 6 Months to Less Than 2 Years. | -0.8 | -1.1 | -2.0 | -2.8 | -1.6 | -1.9 | -2.5 | -2.4 | -2.1 |
| Participants Aged From Birth to Less Than 1 Month. | -1.6 | -1.4 | 0.0 | -0.4 | -0.4 | -0.4 | -1.2 | -1.4 | -1.0 |
"The pharmacokinetic profile of Tapentadol and its major metabolite tapentadol-O-glucuronide was evaluated to enable data based recommendations for the use of Tapentadol in children of different ages.~Each participant had a single pharmacokinetic sample taken at up to 2 different pre-defined time points.~Serum was analyzed using liquid chromatography-tandem mass spectrometry. Mean and Standard Deviation of Serum Concentrations of Tapentadol were calculated.~Summary statistics at a given time point were only determined if at least 2 participants had observations above the lower limit of quantification (LLOQ).~If overall only a single sample was available at one of the pre-defined time points, the measured value is presented and the standard deviation is given as N/A." (NCT02221674)
Timeframe: Up to 8 hours after IMP administration
| Intervention | nanogram per milliliter (Mean) | |||||
|---|---|---|---|---|---|---|
| 30 minutes after administration | 1 hour after administration | 2 hours after administration | 4 hours after administration | 6 hours after administration | 8 hours after administration | |
| Participants Aged 1 Month to Less Than 6 Months - PK Set | 8.3 | 35.27 | 27.3 | 25.9 | 32.75 | 5.6 |
"The pharmacokinetic profile of Tapentadol and its major metabolite tapentadol-O-glucuronide was evaluated to enable data based recommendations for the use of Tapentadol in children of different ages.~Each participant had a single pharmacokinetic sample taken at up to 2 different pre-defined time points.~Serum was analyzed using liquid chromatography-tandem mass spectrometry. Mean and Standard Deviation of Serum Concentrations of Tapentadol were calculated.~Summary statistics at a given time point were only determined if at least 2 participants had observations above the lower limit of quantification (LLOQ).~If overall only a single sample was available at one of the pre-defined time points, the measured value is presented and the standard deviation is given as N/A." (NCT02221674)
Timeframe: Up to 8 hours after IMP administration
| Intervention | nanogram per milliliter (Mean) | |||||
|---|---|---|---|---|---|---|
| 30 minutes after administration | 1 hour after administration | 2 hours after administration | 4 hours after administration | 6 hours after administration | 8 hours after administration | |
| Participants Aged 6 Months to Less Than 2 Years - PK Set | 9.8 | 18.79 | 32.2 | 11.1 | 14.85 | 10.7 |
"The pharmacokinetic profile of Tapentadol and its major metabolite tapentadol-O-glucuronide was evaluated to enable data based recommendations for the use of Tapentadol in children of different ages.~Each participant had a single pharmacokinetic sample taken at up to 2 different pre-defined time points.~Serum was analyzed using liquid chromatography-tandem mass spectrometry. Mean and Standard Deviation of Serum Concentrations of tapentadol-O-glucuronide were calculated.~Summary statistics at a given time point were only determined if at least 2 participants had observations above the lower limit of quantification (LLOQ).~If overall only a single sample was available at one of the pre-defined time points, the measured value is presented and the standard deviation is given as N/A." (NCT02221674)
Timeframe: Up to 8 hours after IMP
| Intervention | nanogram per milliliter (Mean) | |||||
|---|---|---|---|---|---|---|
| 30 minutes after administration | 1 hour after administration | 2 hours after administration | 4 hours after administration | 6 hours after administration | 8 hours after administration | |
| Participants Aged 1 Month to Less Than 6 Months - PK Set | 128.8 | 136.3 | 324.9 | 449.7 | 253.3 | 92.2 |
| Substance | Relationship Strength | Studies | Trials | Classes | Roles |
|---|---|---|---|---|---|
| gamma-aminobutyric acid gamma-Aminobutyric Acid: The most common inhibitory neurotransmitter in the central nervous system.. gamma-aminobutyric acid : A gamma-amino acid that is butanoic acid with the amino substituent located at C-4. | 6.01 | 4 | 0 | amino acid zwitterion; gamma-amino acid; monocarboxylic acid | human metabolite; neurotransmitter; Saccharomyces cerevisiae metabolite; signalling molecule |
| acetic acid Acetic Acid: Product of the oxidation of ethanol and of the destructive distillation of wood. It is used locally, occasionally internally, as a counterirritant and also as a reagent. (Stedman, 26th ed). acetic acid : A simple monocarboxylic acid containing two carbons. | 2.55 | 2 | 0 | monocarboxylic acid | antimicrobial food preservative; Daphnia magna metabolite; food acidity regulator; protic solvent |
| 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 |
| carbamates [no description available] | 2.58 | 2 | 0 | amino-acid anion | |
| citric acid, anhydrous Citric Acid: A key intermediate in metabolism. It is an acid compound found in citrus fruits. The salts of citric acid (citrates) can be used as anticoagulants due to their calcium chelating ability.. citric acid : A tricarboxylic acid that is propane-1,2,3-tricarboxylic acid bearing a hydroxy substituent at position 2. It is an important metabolite in the pathway of all aerobic organisms. | 2.08 | 1 | 0 | tricarboxylic acid | antimicrobial agent; chelator; food acidity regulator; 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 |
| lactic acid Lactic Acid: A normal intermediate in the fermentation (oxidation, metabolism) of sugar. The concentrated form is used internally to prevent gastrointestinal fermentation. (From Stedman, 26th ed). 2-hydroxypropanoic acid : A 2-hydroxy monocarboxylic acid that is propanoic acid in which one of the alpha-hydrogens is replaced by a hydroxy group. | 2.54 | 2 | 0 | 2-hydroxy monocarboxylic acid | algal metabolite; Daphnia magna metabolite |
| formaldehyde paraform: polymerized formaldehyde; RN given refers to parent cpd; used in root canal therapy | 2.53 | 2 | 0 | aldehyde; one-carbon compound | allergen; carcinogenic agent; disinfectant; EC 3.5.1.4 (amidase) inhibitor; environmental contaminant; Escherichia coli metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite |
| dalteparin Dalteparin: A low-molecular-weight fragment of heparin, prepared by nitrous acid depolymerization of porcine mucosal heparin. The mean molecular weight is 4000-6000 daltons. It is used therapeutically as an antithrombotic agent. (From Merck Index, 11th ed) | 2.06 | 1 | 0 | ||
| 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 |
| triphosphoric acid triphosphoric acid: used as water softener, peptizing agent, emulsifier & dispersing agent; ingredient of cleansers; meat preservative; RN given refers to parent cpd; structure | 2.15 | 1 | 0 | acyclic phosphorus acid anhydride; phosphorus oxoacid | |
| 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. | 7.75 | 7 | 1 | 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. | 3.23 | 1 | 0 | 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. | 6.37 | 4 | 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. | 4.97 | 2 | 1 | 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 |
| bupivacaine Bupivacaine: A widely used local anesthetic agent.. 1-butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamide : A piperidinecarboxamide obtained by formal condensation of the carboxy group of N-butylpipecolic acid with the amino group of 2,6-dimethylaniline.. bupivacaine : A racemate composed of equimolar amounts of dextrobupivacaine and levobupivacaine. Used (in the form of its hydrochloride hydrate) as a local anaesthetic. | 2.08 | 1 | 0 | aromatic amide; piperidinecarboxamide; tertiary amino compound | |
| 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. | 8.61 | 2 | 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 |
| nordazepam Nordazepam: An intermediate in the metabolism of DIAZEPAM to OXAZEPAM. It may have actions similar to those of diazepam.. nordazepam : A 1,4-benzodiazepinone having phenyl and chloro substituents at positions 5 and 7 respectively; it has anticonvulsant, anxiolytic, muscle relaxant and sedative properties but is used primarily in the treatment of anxiety. | 2.31 | 1 | 0 | 1,4-benzodiazepinone; organochlorine compound | anticonvulsant; anxiolytic drug; GABA modulator; human metabolite; sedative |
| 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. | 8.6 | 2 | 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. | 3.69 | 2 | 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. | 8.91 | 3 | 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. | 3.69 | 2 | 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. | 3.23 | 1 | 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 |
| berotek Fenoterol: A synthetic adrenergic beta-2 agonist that is used as a bronchodilator and tocolytic.. fenoterol : A member of the class resorcinols that is 5-(1-hydroxyethyl)benzene-1,3-diol in which one of the methyl hydrogens is replaced by a 1-(4-hydroxyphenyl)propan-2-amino group. A beta2-adrenergic agonist, it is used (as the hydrobromide salt) as a bronchodilator in the management of reversible airway obstruction. | 2.21 | 1 | 0 | resorcinols; secondary alcohol; secondary amino compound | beta-adrenergic agonist; bronchodilator agent; sympathomimetic agent; tocolytic agent |
| fentanyl Fentanyl: A potent narcotic analgesic, abuse of which leads to habituation or addiction. It is primarily a mu-opioid agonist. Fentanyl is also used as an adjunct to general anesthetics, and as an anesthetic for induction and maintenance. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1078). fentanyl : A monocarboxylic acid amide resulting from the formal condensation of the aryl amino group of N-phenyl-1-(2-phenylethyl)piperidin-4-amine with propanoic acid. | 8.76 | 12 | 1 | anilide; monocarboxylic acid amide; piperidines | adjuvant; anaesthesia adjuvant; anaesthetic; intravenous anaesthetic; mu-opioid receptor agonist; opioid analgesic |
| 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. | 3.23 | 1 | 0 | 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. | 6.37 | 4 | 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 | 6.18 | 3 | 1 | 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. | 6.37 | 4 | 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. | 3.61 | 2 | 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. | 3.23 | 1 | 0 | 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. | 8.69 | 2 | 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. | 5.58 | 4 | 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. | 8.95 | 3 | 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. | 5.94 | 9 | 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. | 8.64 | 2 | 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. | 3.62 | 2 | 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 |
| oxidopamine Oxidopamine: A neurotransmitter analogue that depletes noradrenergic stores in nerve endings and induces a reduction of dopamine levels in the brain. Its mechanism of action is related to the production of cytolytic free-radicals.. oxidopamine : A benzenetriol that is phenethylamine in which the hydrogens at positions 2, 4, and 5 on the phenyl ring are replaced by hydroxy groups. It occurs naturally in human urine, but is also produced as a metabolite of the drug DOPA (used for the treatment of Parkinson's disease). | 2.25 | 1 | 0 | benzenetriol; catecholamine; primary amino compound | drug metabolite; human metabolite; neurotoxin |
| 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. | 3.23 | 1 | 0 | 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 |
| palmidrol palmidrol: a cannabinoid receptor-inactive eCB-related molecule used as prophylactic in helping to prevent respiratory viral infection. palmitoyl ethanolamide : An N-(long-chain-acyl)ethanolamine that is the ethanolamide of palmitic (hexadecanoic) acid. | 2.15 | 1 | 0 | endocannabinoid; N-(long-chain-acyl)ethanolamine; N-(saturated fatty acyl)ethanolamine | anti-inflammatory drug; anticonvulsant; antihypertensive agent; neuroprotective 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 | |
| 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. | 3.66 | 2 | 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. | 3.6 | 2 | 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 |
| levodopa Levodopa: The naturally occurring form of DIHYDROXYPHENYLALANINE and the immediate precursor of DOPAMINE. Unlike dopamine itself, it can be taken orally and crosses the blood-brain barrier. It is rapidly taken up by dopaminergic neurons and converted to DOPAMINE. It is used for the treatment of PARKINSONIAN DISORDERS and is usually given with agents that inhibit its conversion to dopamine outside of the central nervous system.. L-dopa : An optically active form of dopa having L-configuration. Used to treat the stiffness, tremors, spasms, and poor muscle control of Parkinson's disease | 2.25 | 1 | 0 | amino acid zwitterion; dopa; L-tyrosine derivative; non-proteinogenic L-alpha-amino acid | allelochemical; antidyskinesia agent; antiparkinson drug; dopaminergic agent; hapten; human metabolite; mouse metabolite; neurotoxin; plant growth retardant; plant metabolite; prodrug |
| 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) | 3.69 | 2 | 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. | 6.15 | 3 | 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 |
| 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 |
| cyclohexanol Cyclohexanols: Monohydroxy derivatives of cyclohexanes that contain the general formula R-C6H11O. They have a camphorlike odor and are used in making soaps, insecticides, germicides, dry cleaning, and plasticizers.. cyclohexanols : An alcohol in which one or more hydroxy groups are attached to a cyclohexane skeleton. | 2.07 | 1 | 0 | cyclohexanols; secondary alcohol | solvent |
| thiophenes Thiophenes: A monocyclic heteroarene furan in which the oxygen atom is replaced by a sulfur.. thiophenes : Compounds containing at least one thiophene ring. | 2.5 | 2 | 0 | mancude organic heteromonocyclic parent; monocyclic heteroarene; thiophenes; volatile organic compound | non-polar solvent |
| 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 | |
| yohimbine Yohimbine: A plant alkaloid with alpha-2-adrenergic blocking activity. Yohimbine has been used as a mydriatic and in the treatment of ERECTILE DYSFUNCTION.. yohimbine : An indole alkaloid with alpha2-adrenoceptor antagonist activity. It is produced by Corynanthe johimbe and Rauwolfia serpentina. | 4.27 | 6 | 0 | methyl 17-hydroxy-20xi-yohimban-16-carboxylate | alpha-adrenergic antagonist; dopamine receptor D2 antagonist; serotonergic antagonist |
| 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] | 2.05 | 1 | 0 | 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 |
| 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 |
| alpha-aminopyridine alpha-aminopyridine: RN given refers to parent cpd; structure in Merck Index, 9th ed, #485. aminopyridine : Compounds containing a pyridine skeleton substituted by one or more amine groups. | 2.11 | 1 | 0 | ||
| 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 |
| clothiapine clothiapine: was heading 1975-94 (was see under DIBENZOTHIAZEPINES 1975-90); CLOTIAPINE was see CLOTHIAPINE 1978-94; use DIBENZOTHIAZEPINES to search CLOTHIAPINE 1975-94; antipsychotic similar to clozapine | 2.31 | 1 | 0 | dibenzothiazepine | |
| 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 |
| 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 |
| trolamine salicylate Arthritis: Acute or chronic inflammation of JOINTS. | 2.06 | 1 | 0 | ||
| 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 |
| eedq EEDQ: peptide coupling reagent | 2.08 | 1 | 0 | ||
| 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 |
| glutamic acid Glutamic Acid: A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.. glutamic acid : An alpha-amino acid that is glutaric acid bearing a single amino substituent at position 2. | 4.11 | 2 | 1 | glutamic acid; glutamine family amino acid; L-alpha-amino acid; proteinogenic amino acid | Escherichia coli metabolite; ferroptosis inducer; micronutrient; mouse metabolite; neurotransmitter; nutraceutical |
| 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 |
| tramadol Tramadol: A narcotic analgesic proposed for severe pain. It may be habituating.. tramadol : A racemate consisting of equal amounts of (R,R)- and (S,S)-tramadol. A centrally acting synthetic opioid analgesic, used (as the hydrochloride salt) to treat moderately severe pain. The (R,R)-enantiomer exhibits ten-fold higher analgesic potency than the (S,S)-enantiomer. Originally developed by Gruenenthal GmbH and launched in 1977, it was subsequently isolated from the root bark of the South African tree Nauclea latifolia.. (R,R)-tramadol : A 2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol in which both stereocentres have R-configuration; the (R,R)-enantiomer of the racemic opioid analgesic tramadol, it exhibits ten-fold higher analgesic potency than the (S,S)-enantiomer. | 13.27 | 33 | 4 | 2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol | adrenergic uptake inhibitor; antitussive; capsaicin receptor antagonist; delta-opioid receptor agonist; kappa-opioid receptor agonist; metabolite; mu-opioid receptor agonist; muscarinic antagonist; nicotinic antagonist; NMDA receptor antagonist; opioid analgesic; serotonergic antagonist; serotonin uptake inhibitor |
| 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 |
| meptazinol Meptazinol: A narcotic antagonist with analgesic properties. It is used for the control of moderate to severe pain. | 2.21 | 1 | 0 | azepanes | |
| 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. | 4.84 | 3 | 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 |
| flupirtine flupirtine: RN given refers to parent cpd without isomeric designation | 7.11 | 1 | 0 | aminopyridine | |
| 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 |
| idazoxan Idazoxan: A benzodioxane-linked imidazole that has alpha-2 adrenoceptor antagonist activity.. idazoxan : A benzodioxine that is 2,3-dihydro-1,4-benzodioxine in which one of the hydrogens at position 2 has been replaced by a 4,5-dihydro-1H-imidazol-2-yl group. | 2.52 | 2 | 0 | benzodioxine; imidazolines | alpha-adrenergic antagonist |
| 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 hydrochloride Duloxetine Hydrochloride: A thiophene derivative and selective NEUROTRANSMITTER UPTAKE INHIBITOR for SEROTONIN and NORADRENALINE (SNRI). It is an ANTIDEPRESSIVE AGENT and ANXIOLYTIC, and is also used for the treatment of pain in patients with DIABETES MELLITUS and FIBROMYALGIA.. (S)-duloxetine hydrochloride : A duloxetine hydrochloride in which the duloxetine moiety has S configuration. | 6.2 | 5 | 0 | duloxetine hydrochloride | antidepressant |
| 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 |
| venlafaxine hydrochloride Venlafaxine Hydrochloride: A cyclohexanol and phenylethylamine derivative that functions as a SEROTONIN AND NORADRENALINE REUPTAKE INHIBITOR (SNRI) and is used as an ANTIDEPRESSIVE AGENT. | 5.79 | 3 | 0 | hydrochloride | |
| 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 | |
| atipamezole [no description available] | 2.06 | 1 | 0 | ||
| 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 |
| rx 821002 2-methoxyidazoxan: 2-methoxy analog of idazoxan. 2-methoxyidazoxan : A benzodioxine that is idazoxan substituted at position 2 by a methoxy group. | 2.52 | 2 | 0 | benzodioxine; cyclic ketal; imidazolines | alpha-adrenergic antagonist |
| tadalafil [no description available] | 3.23 | 1 | 0 | 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 |
| reboxetine Reboxetine: A morpholine derivative that is a selective and potent noradrenaline reuptake inhibitor; it is used in the treatment of DEPRESSIVE DISORDER. | 2.1 | 1 | 0 | aromatic ether | |
| tamsulosin [no description available] | 3.23 | 1 | 0 | 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 |
| omega-n-methylarginine omega-N-Methylarginine: A competitive inhibitor of nitric oxide synthetase.. N(omega)-methyl-L-arginine : A L-arginine derivative with a N(omega)-methyl substituent. | 2.07 | 1 | 0 | amino acid zwitterion; arginine derivative; guanidines; L-arginine derivative; non-proteinogenic L-alpha-amino acid | |
| 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. | 3.61 | 2 | 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. | 3.23 | 1 | 0 | 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. | 5.29 | 3 | 1 | 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] | 4.13 | 2 | 0 | ||
| telbivudine [no description available] | 3.23 | 1 | 0 | pyrimidine 2'-deoxyribonucleoside | antiviral drug; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor |
| desmethylnaproxen desmethylnaproxen: RN given refers to cpd without isomeric designation. desmethylnaproxen : A member of the class of naphthols that is naproxen in which the 6-methoxy group has been demethylated. | 7.21 | 1 | 0 | ||
| 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 |
| dexketoprofen trometamol dexketoprofen trometamol: a water-soluble tromethamine salt of the racemic ketoprofen, rac(+-)-ketoprofen | 2.31 | 1 | 0 | ||
| 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 |
| 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. | 6.68 | 5 | 3 | 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 |
| 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 |
| norfentanyl norfentanyl: metabolite of fentanyl; RN given refers to parent cpd; structure given in first source. norfentanyl : A monocarboxylic acid amide resulting from the formal condensation of the aryl amino group of 4-(N'-phenyl)piperidin-4-amine with propanoic acid. A major metabolite of fentanyl. | 2.21 | 1 | 0 | anilide; monocarboxylic acid amide; piperidines | drug metabolite; opioid analgesic |
| 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 |
| pentazocine Pentazocine: The first mixed agonist-antagonist analgesic to be marketed. It is an agonist at the kappa and sigma opioid receptors and has a weak antagonist action at the mu receptor. (From AMA Drug Evaluations Annual, 1991, p97) | 7.31 | 1 | 0 | benzazocine | |
| 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. | 3.23 | 1 | 0 | 1-benzofurans; monocarboxylic acid amide; pyrrolidines | antispasmodic drug; muscarinic antagonist |
| betadex beta-Cyclodextrins: Cyclic GLUCANS consisting of seven (7) glucopyranose units linked by 1,4-glycosidic bonds. | 2.1 | 1 | 0 | cyclodextrin | |
| 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 |
| alpha-cyclodextrin alpha-cyclodextrin : A cycloamylose composed of six alpha-(1->4) linked D-glucopyranose units. | 2.1 | 1 | 0 | cyclodextrin | |
| 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. | 3.61 | 2 | 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 |
| dipyrone Dipyrone: A drug that has analgesic, anti-inflammatory, and antipyretic properties. It is the sodium sulfonate of AMINOPYRINE.. metamizole sodium : An organic sodium salt of antipyrine substituted at C-4 by a methyl(sulfonatomethyl)amino group, commonly used as a powerful analgesic and antipyretic. | 2.11 | 1 | 0 | organic sodium salt | anti-inflammatory agent; antipyretic; antirheumatic drug; cyclooxygenase 3 inhibitor; non-narcotic analgesic; peripheral nervous system drug; prodrug |
| 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 |
| buprenorphine Buprenorphine: A derivative of the opioid alkaloid THEBAINE that is a more potent and longer lasting analgesic than MORPHINE. It appears to act as a partial agonist at mu and kappa opioid receptors and as an antagonist at delta receptors. The lack of delta-agonist activity has been suggested to account for the observation that buprenorphine tolerance may not develop with chronic use.. buprenorphine : A morphinane alkaloid that is 7,8-dihydromorphine 6-O-methyl ether in which positions 6 and 14 are joined by a -CH2CH2- bridge, one of the hydrogens of the N-methyl group is substituted by cyclopropyl, and a hydrogen at position 7 is substituted by a 2-hydroxy-3,3-dimethylbutan-2-yl group. It is highly effective for the treatment of opioid use disorder and is also increasingly being used in the treatment of chronic pain. | 13.81 | 9 | 2 | morphinane alkaloid | delta-opioid receptor antagonist; kappa-opioid receptor antagonist; mu-opioid receptor agonist; opioid analgesic |
| 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 |
| capsaicin ALGRX-4975: an injectable capsaicin (TRPV1 receptor agonist) formulation for longlasting pain relief. capsaicinoid : A family of aromatic fatty amides produced as secondary metabolites by chilli peppers. | 8.4 | 6 | 1 | capsaicinoid | non-narcotic analgesic; TRPV1 agonist; voltage-gated sodium channel blocker |
| 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 | |
| dezocine dezocine: potent analgesic; RN given refers to ((5R-(5alpha,11alpha,13S*)))-isomer (dezocin); structure. dezocine : (7S,8S)-7-Amino-8-methyl-5,6,7,8-tetrahydronaphthalen-2-ol in which the hydrogen at position 8 and one of the hydrogens at position 6 are substituted by each end of a tetramethylene bridge. A synthetic opioid analgesic, it has mixed opiod agonist and antagonist properties. Although it is used for pain management, it can produce opioid withdrawal syndrome in patients already dependent on other opioids, and its clinical application is limited by side effects such as dizziness. | 2.69 | 2 | 0 | phenols; primary amino compound | opioid analgesic |
| 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] | 5.03 | 4 | 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 | |
| hydrocodone Hydrocodone: Narcotic analgesic related to CODEINE, but more potent and more addicting by weight. It is used also as cough suppressant.. hydrocodone : A morphinane-like compound that is a semi-synthetic opioid synthesized from codeine. | 3.11 | 4 | 0 | morphinane-like compound; organic heteropentacyclic compound | antitussive; mu-opioid receptor agonist; opioid analgesic |
| 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. | 9.45 | 12 | 2 | 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. | 12.1 | 24 | 6 | 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. | 18.33 | 101 | 39 | 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) | 10.92 | 4 | 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. | 3.23 | 1 | 0 | ||
| 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. | 12.3 | 42 | 4 | 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 |
| endomorphin 1 endomorphin 1: isolated from bovine brain | 2.13 | 1 | 0 | oligopeptide | |
| 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 | |
| mdl 100907 Serotonin 5-HT2 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT2 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT2 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more specific 5-HT2 receptor subtypes. | 2.06 | 1 | 0 | ||
| 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 | 3.59 | 2 | 0 | 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. | 9.75 | 4 | 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. | 3.66 | 2 | 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. | 3.66 | 2 | 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 |
| dextrorphan Dextrorphan: Dextro form of levorphanol. It acts as a noncompetitive NMDA receptor antagonist, among other effects, and has been proposed as a neuroprotective agent. It is also a metabolite of DEXTROMETHORPHAN. | 2.21 | 1 | 0 | morphinane alkaloid | |
| 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 |
| methylnaltrexone methylnaltrexone: RN given refers to parent cpd(5alpha)-isomer | 2.21 | 1 | 0 | phenanthrenes | |
| 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 | ||
| bleomycin [no description available] | 3.23 | 1 | 0 | bleomycin | antineoplastic agent; metabolite |
| 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 |
| 3-methoxymorphinan [no description available] | 2.21 | 1 | 0 | ||
| 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. | 10.58 | 13 | 4 | 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 | |
| noroxycodone noroxycodone: RN given for (5alpha)-isomer; metabolite of oxycodone | 2.21 | 1 | 0 | phenanthrenes | |
| 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. | 3.73 | 2 | 0 | azabicycloalkane; delta-lactam; organic heterotricyclic compound | antiemetic; serotonergic antagonist |
| 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 | ||
| netupitant netupitant: orally active neurokinin-1 receptor antagonist. netupitant : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 2-[3,5-bis(trifluoromethyl)phenyl]-2-methylpropanoic acid with the secondary amino group of N-methyl-4-(2-methylphenyl)-6-(4-methylpiperazin-1-yl)pyridin-3-amine; an antiemetic used in combination with palonosetron hydrochloride (under the trade name Akynzeo) to treat nausea and vomiting in patients undergoing cancer chemotherapy. | 2.6 | 1 | 0 | aminopyridine; monocarboxylic acid amide; N-alkylpiperazine; N-arylpiperazine; organofluorine compound; toluenes | antiemetic; neurokinin-1 receptor antagonist |
| 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 | |
| fesoterodine fesoterodine: a muscarinic antagonist for treatment of overactive bladder | 3.59 | 2 | 0 | diarylmethane | |
| 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 |
| 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 | |
| o-demethyltramadol [no description available] | 2.07 | 1 | 0 | alkylbenzene; ring assembly | |
| 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 | |
| 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 |
| buprenorphine, naloxone drug combination Buprenorphine, Naloxone Drug Combination: A pharmaceutical preparation that combines buprenorphine, an OPIOID ANALGESICS with naloxone, a NARCOTIC ANTAGONISTS to reduce the potential for NARCOTIC DEPENDENCE in the treatment of pain. It may also be used for OPIOID SUBSTITUTION THERAPY. | 2.25 | 1 | 0 | ||
| 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 | ||
| ent-dextilidine Tilidine: An opioid analgesic used similarly to MORPHINE in the control of moderate to severe pain. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1097). ent-dextilidine : An ethyl 2-(dimethylamino)-1-phenylcyclohex-3-ene-1-carboxylate that has R configuration at the carbon bearing the phenyl group and S configuration at the carbon bearing the dimethylamino group. It is the enantiomer of dextilidine; the opioid analgesic tilidine is the racemate comprising equimolar amounts of dextilidine and ent-dextilidine.. tilidine : A racemate that is an equimolar mixture of the two trans diastereoisomers of ethyl 2-(dimethylamino)-1-phenylcyclohex-3-ene-1-carboxylate, namely dextilidine and ent-dextilidine. It is used (commonly as the hydrochloride hemihydrate) as an opioid analgesic for the management of moderate to severe pain. A prodrug, it is metabolised in the body to nortilidine, which is responsible for the analgesic activity; virtually all of the opioid activity resides in the (1S,2R) isomer. | 2.21 | 1 | 0 | ethyl 2-(dimethylamino)-1-phenylcyclohex-3-ene-1-carboxylate | |
| cytochrome c-t Cytochromes c: Cytochromes of the c type that are found in eukaryotic MITOCHONDRIA. They serve as redox intermediates that accept electrons from MITOCHONDRIAL ELECTRON TRANSPORT COMPLEX III and transfer them to MITOCHONDRIAL ELECTRON TRANSPORT COMPLEX IV. | 2.13 | 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 | ||
| cellulose DEAE-Cellulose: Cellulose derivative used in chromatography, as ion-exchange material, and for various industrial applications. | 7.08 | 1 | 0 | glycoside | |
| chitosan [no description available] | 2.55 | 2 | 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 |
| mannans [no description available] | 2.08 | 1 | 0 | ||
| 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. | 3.23 | 1 | 0 | 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) | 3.23 | 1 | 0 | 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 |
|---|---|---|---|---|
| Chronic Illness [description not available] | 0 | 11.36 | 17 | 7 |
| Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases. | 0 | 7.46 | 16 | 1 |
| Ache [description not available] | 0 | 17.79 | 93 | 30 |
| Acute Disease Disease having a short and relatively severe course. | 0 | 7.55 | 6 | 2 |
| 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 | 11.36 | 17 | 7 |
| Pain An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS. | 1 | 19.79 | 93 | 30 |
| Acute Liver Injury, Drug-Induced [description not available] | 0 | 3.46 | 2 | 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 | 3.46 | 2 | 0 |
| Cancer-Associated Pain [description not available] | 0 | 9.71 | 17 | 2 |
| Benign Neoplasms [description not available] | 0 | 11.99 | 23 | 6 |
| Nerve Pain [description not available] | 0 | 15.4 | 48 | 18 |
| Cancer Pain Pain that may be caused by or related to cellular, tissue, and systemic changes that occur during NEOPLASM growth, tissue invasion, and METASTASIS. | 0 | 9.71 | 17 | 2 |
| Neoplasms New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms. | 1 | 13.99 | 23 | 6 |
| Neuralgia Intense or aching pain that occurs along the course or distribution of a peripheral or cranial nerve. | 1 | 17.4 | 48 | 18 |
| Musculoskeletal Pain Discomfort stemming from muscles, LIGAMENTS, tendons, and bones. | 0 | 7.12 | 9 | 1 |
| Nociceptive Pain Dull or sharp aching pain caused by stimulated NOCICEPTORS due to tissue injury, inflammation or diseases. It can be divided into somatic or tissue pain and VISCERAL PAIN. | 0 | 6.02 | 5 | 1 |
| Osteoarthritis of Knee [description not available] | 0 | 17.38 | 50 | 30 |
| Pain, Chronic [description not available] | 0 | 20.34 | 155 | 32 |
| Osteoarthritis, Knee Noninflammatory degenerative disease of the knee joint consisting of three large categories: conditions that block normal synchronous movement, conditions that produce abnormal pathways of motion, and conditions that cause stress concentration resulting in changes to articular cartilage. (Crenshaw, Campbell's Operative Orthopaedics, 8th ed, p2019) | 1 | 19.38 | 50 | 30 |
| Chronic Pain Aching sensation that persists for more than a few months. It may or may not be associated with trauma or disease, and may persist after the initial injury has healed. Its localization, character, and timing are more vague than with acute pain. | 1 | 22.34 | 155 | 32 |
| Acute Post-operative Pain [description not available] | 0 | 12.98 | 25 | 14 |
| Pain, Postoperative Pain during the period after surgery. | 0 | 12.98 | 25 | 14 |
| Absence Seizure [description not available] | 0 | 4.04 | 4 | 0 |
| Seizures Clinical or subclinical disturbances of cortical function due to a sudden, abnormal, excessive, and disorganized discharge of brain cells. Clinical manifestations include abnormal motor, sensory and psychic phenomena. Recurrent seizures are usually referred to as EPILEPSY or seizure disorder. | 0 | 9.04 | 4 | 0 |
| Delirium of Mixed Origin [description not available] | 0 | 2.41 | 1 | 0 |
| Delirium A disorder characterized by CONFUSION; inattentiveness; disorientation; ILLUSIONS; HALLUCINATIONS; agitation; and in some instances autonomic nervous system overactivity. It may result from toxic/metabolic conditions or structural brain lesions. (From Adams et al., Principles of Neurology, 6th ed, pp411-2) | 0 | 2.41 | 1 | 0 |
| Addiction, Opioid [description not available] | 0 | 8.33 | 23 | 1 |
| Opioid-Related Disorders Disorders related to or resulting from abuse or misuse of OPIOIDS. | 0 | 8.33 | 23 | 1 |
| Back Ache [description not available] | 0 | 5.93 | 8 | 3 |
| Back Pain Acute or chronic pain located in the posterior regions of the THORAX; LUMBOSACRAL REGION; or the adjacent regions. | 1 | 7.93 | 8 | 3 |
| Colonic Inertia Symptom characterized by the passage of stool once a week or less. | 0 | 13.81 | 25 | 15 |
| 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 | 13.81 | 25 | 15 |
| Opiate Overdose Accidental or deliberate use of an OPIOID in excess of normal dosage. It includes overdose for prescription and illicit opioids. | 0 | 2.41 | 1 | 0 |
| Drug Overdose Accidental or deliberate use of a medication or street drug in excess of normal dosage. | 0 | 3.25 | 5 | 0 |
| Drug Withdrawal Symptoms [description not available] | 0 | 7.03 | 10 | 0 |
| Substance Withdrawal Syndrome Physiological and psychological symptoms associated with withdrawal from the use of a drug after prolonged administration or habituation. The concept includes withdrawal from smoking or drinking, as well as withdrawal from an administered drug. | 0 | 7.03 | 10 | 0 |
| Neuroblastoma A common neoplasm of early childhood arising from neural crest cells in the sympathetic nervous system, and characterized by diverse clinical behavior, ranging from spontaneous remission to rapid metastatic progression and death. This tumor is the most common intraabdominal malignancy of childhood, but it may also arise from thorax, neck, or rarely occur in the central nervous system. Histologic features include uniform round cells with hyperchromatic nuclei arranged in nests and separated by fibrovascular septa. Neuroblastomas may be associated with the opsoclonus-myoclonus syndrome. (From DeVita et al., Cancer: Principles and Practice of Oncology, 5th ed, pp2099-2101; Curr Opin Oncol 1998 Jan;10(1):43-51) | 0 | 3.33 | 4 | 0 |
| Adverse Drug Event [description not available] | 0 | 11.1 | 21 | 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 | 11.1 | 21 | 0 |
| Central Nervous System Origin Vertigo [description not available] | 0 | 3.6 | 2 | 0 |
| Vertigo An illusion of movement, either of the external world revolving around the individual or of the individual revolving in space. Vertigo may be associated with disorders of the inner ear (EAR, INNER); VESTIBULAR NERVE; BRAINSTEM; or CEREBRAL CORTEX. Lesions in the TEMPORAL LOBE and PARIETAL LOBE may be associated with FOCAL SEIZURES that may feature vertigo as an ictal manifestation. (From Adams et al., Principles of Neurology, 6th ed, pp300-1) | 0 | 3.6 | 2 | 0 |
| Diabetes Mellitus, Adult-Onset [description not available] | 0 | 2.69 | 2 | 0 |
| Morbid Obesity [description not available] | 0 | 2.6 | 1 | 0 |
| Diabetes Mellitus, Type 2 A subclass of DIABETES MELLITUS that is not INSULIN-responsive or dependent (NIDDM). It is characterized initially by INSULIN RESISTANCE and HYPERINSULINEMIA; and eventually by GLUCOSE INTOLERANCE; HYPERGLYCEMIA; and overt diabetes. Type II diabetes mellitus is no longer considered a disease exclusively found in adults. Patients seldom develop KETOSIS but often exhibit OBESITY. | 0 | 2.69 | 2 | 0 |
| Obesity, Morbid The condition of weighing two, three, or more times the ideal weight, so called because it is associated with many serious and life-threatening disorders. In the BODY MASS INDEX, morbid obesity is defined as having a BMI greater than 40.0 kg/m2. | 0 | 2.6 | 1 | 0 |
| Autosomal Dominant Juvenile Parkinson Disease [description not available] | 0 | 2.25 | 1 | 0 |
| Motor Disorders Motor skills deficits that significantly and persistently interfere with ACTIVITIES OF DAILY LIVING appropriate to chronological age. (from DSM-5) | 0 | 2.25 | 1 | 0 |
| Dyskinesia, Medication-Induced [description not available] | 0 | 2.25 | 1 | 0 |
| Dyskinesia, Drug-Induced Abnormal movements, including HYPERKINESIS; HYPOKINESIA; TREMOR; and DYSTONIA, associated with the use of certain medications or drugs. Muscles of the face, trunk, neck, and extremities are most commonly affected. Tardive dyskinesia refers to abnormal hyperkinetic movements of the muscles of the face, tongue, and neck associated with the use of neuroleptic agents (see ANTIPSYCHOTIC AGENTS). (Adams et al., Principles of Neurology, 6th ed, p1199) | 0 | 2.25 | 1 | 0 |
| Parkinsonian Disorders A group of disorders which feature impaired motor control characterized by bradykinesia, MUSCLE RIGIDITY; TREMOR; and postural instability. Parkinsonian diseases are generally divided into primary parkinsonism (see PARKINSON DISEASE), secondary parkinsonism (see PARKINSON DISEASE, SECONDARY) and inherited forms. These conditions are associated with dysfunction of dopaminergic or closely related motor integration neuronal pathways in the BASAL GANGLIA. | 0 | 2.25 | 1 | 0 |
| Low Back Ache [description not available] | 0 | 17.1 | 54 | 26 |
| Low Back Pain Acute or chronic pain in the lumbar or sacral regions, which may be associated with musculo-ligamentous SPRAINS AND STRAINS; INTERVERTEBRAL DISK DISPLACEMENT; and other conditions. | 1 | 19.1 | 54 | 26 |
| Cognitive Decline [description not available] | 0 | 2.21 | 1 | 0 |
| Anxiety Feelings or emotions of dread, apprehension, and impending disaster but not disabling as with ANXIETY DISORDERS. | 0 | 7.55 | 2 | 0 |
| Depression Depressive states usually of moderate intensity in contrast with MAJOR DEPRESSIVE DISORDER present in neurotic and psychotic disorders. | 0 | 7.55 | 2 | 0 |
| Cognitive Dysfunction Diminished or impaired mental and/or intellectual function. | 0 | 2.21 | 1 | 0 |
| Nerve Root Avulsion [description not available] | 0 | 2.21 | 1 | 0 |
| Radiculopathy Disease involving a spinal nerve root (see SPINAL NERVE ROOTS) which may result from compression related to INTERVERTEBRAL DISK DISPLACEMENT; SPINAL CORD INJURIES; SPINAL DISEASES; and other conditions. Clinical manifestations include radicular pain, weakness, and sensory loss referable to structures innervated by the involved nerve root. | 0 | 2.21 | 1 | 0 |
| Debility [description not available] | 0 | 2.21 | 1 | 0 |
| Obesity A status with BODY WEIGHT that is grossly above the recommended standards, usually due to accumulation of excess FATS in the body. The standards may vary with age, sex, genetic or cultural background. In the BODY MASS INDEX, a BMI greater than 30.0 kg/m2 is considered obese, and a BMI greater than 40.0 kg/m2 is considered morbidly obese (MORBID OBESITY). | 0 | 2.21 | 1 | 0 |
| Drug Abuse, Intravenous [description not available] | 0 | 2.66 | 2 | 0 |
| Acute Pain Intensely discomforting, distressful, or agonizing sensation associated with trauma or disease, with well-defined location, character, and timing. | 0 | 12.86 | 22 | 15 |
| Chemical Dependence [description not available] | 0 | 4.61 | 5 | 0 |
| Behavior Disorders [description not available] | 0 | 2.25 | 1 | 0 |
| Hepatitis, Viral, Non-A, Non-B, Parenterally-Transmitted [description not available] | 0 | 2.25 | 1 | 0 |
| Mental Disorders Psychiatric illness or diseases manifested by breakdowns in the adaptational process expressed primarily as abnormalities of thought, feeling, and behavior producing either distress or impairment of function. | 0 | 2.25 | 1 | 0 |
| Hepatitis C INFLAMMATION of the LIVER in humans caused by HEPATITIS C VIRUS, a single-stranded RNA virus. Its incubation period is 30-90 days. Hepatitis C is transmitted primarily by contaminated blood parenterally and is often associated with transfusion and intravenous drug abuse. However, in a significant number of cases, the source of hepatitis C infection is unknown. | 0 | 2.25 | 1 | 0 |
| Substance-Related Disorders Disorders related to substance use or abuse. | 0 | 4.61 | 5 | 0 |
| ACL Injuries [description not available] | 0 | 2.25 | 1 | 0 |
| Canine Diseases [description not available] | 0 | 3.94 | 2 | 1 |
| Bone Cancer [description not available] | 0 | 3.09 | 4 | 0 |
| Allodynia [description not available] | 0 | 10.9 | 8 | 1 |
| Bone Neoplasms Tumors or cancer located in bone tissue or specific BONES. | 0 | 3.09 | 4 | 0 |
| Arthritis, Degenerative [description not available] | 0 | 6.98 | 9 | 3 |
| Osteoarthritis A progressive, degenerative joint disease, the most common form of arthritis, especially in older persons. The disease is thought to result not from the aging process but from biochemical changes and biomechanical stresses affecting articular cartilage. In the foreign literature it is often called osteoarthrosis deformans. | 1 | 8.98 | 9 | 3 |
| Asymmetric Diabetic Proximal Motor Neuropathy [description not available] | 0 | 12.4 | 20 | 6 |
| Diabetic Neuropathies Peripheral, autonomic, and cranial nerve disorders that are associated with DIABETES MELLITUS. These conditions usually result from diabetic microvascular injury involving small blood vessels that supply nerves (VASA NERVORUM). Relatively common conditions which may be associated with diabetic neuropathy include third nerve palsy (see OCULOMOTOR NERVE DISEASES); MONONEUROPATHY; mononeuropathy multiplex; diabetic amyotrophy; a painful POLYNEUROPATHY; autonomic neuropathy; and thoracoabdominal neuropathy. (From Adams et al., Principles of Neurology, 6th ed, p1325) | 1 | 17.04 | 40 | 12 |
| Bone Fractures [description not available] | 0 | 7.31 | 1 | 0 |
| Fractures, Bone Breaks in bones. | 0 | 2.31 | 1 | 0 |
| Gastric Ulcer [description not available] | 0 | 2.63 | 2 | 0 |
| Stomach Ulcer Ulceration of the GASTRIC MUCOSA due to contact with GASTRIC JUICE. It is often associated with HELICOBACTER PYLORI infection or consumption of nonsteroidal anti-inflammatory drugs (NSAIDS). | 0 | 2.63 | 2 | 0 |
| Craniofacial Pain [description not available] | 0 | 3.24 | 5 | 0 |
| Facial Pain Pain in the facial region including orofacial pain and craniofacial pain. Associated conditions include local inflammatory and neoplastic disorders and neuralgic syndromes involving the trigeminal, facial, and glossopharyngeal nerves. Conditions which feature recurrent or persistent facial pain as the primary manifestation of disease are referred to as FACIAL PAIN SYNDROMES. | 0 | 3.24 | 5 | 0 |
| Serotonin Syndrome An adverse drug interaction characterized by altered mental status, autonomic dysfunction, and neuromuscular abnormalities. It is most frequently caused by use of both serotonin reuptake inhibitors and monoamine oxidase inhibitors, leading to excess serotonin availability in the CNS at the serotonin 1A receptor. | 0 | 4.21 | 3 | 0 |
| Pyrexia [description not available] | 0 | 2.31 | 1 | 0 |
| Infections, Staphylococcal [description not available] | 0 | 2.31 | 1 | 0 |
| Infection, Postoperative Wound [description not available] | 0 | 2.31 | 1 | 0 |
| Fever An abnormal elevation of body temperature, usually as a result of a pathologic process. | 0 | 2.31 | 1 | 0 |
| Osteomyelitis INFLAMMATION of the bone as a result of infection. It may be caused by a variety of infectious agents, especially pyogenic (PUS - producing) BACTERIA. | 0 | 2.31 | 1 | 0 |
| Staphylococcal Infections Infections with bacteria of the genus STAPHYLOCOCCUS. | 0 | 2.31 | 1 | 0 |
| Bacteremia The presence of viable bacteria circulating in the blood. Fever, chills, tachycardia, and tachypnea are common acute manifestations of bacteremia. The majority of cases are seen in already hospitalized patients, most of whom have underlying diseases or procedures which render their bloodstreams susceptible to invasion. | 0 | 2.31 | 1 | 0 |
| Nocturnal Wandering [description not available] | 0 | 2.41 | 1 | 0 |
| 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 | 4.04 | 2 | 0 |
| Hepatic Failure [description not available] | 0 | 4.04 | 2 | 0 |
| Liver Failure Severe inability of the LIVER to perform its normal metabolic functions, as evidenced by severe JAUNDICE and abnormal serum levels of AMMONIA; BILIRUBIN; ALKALINE PHOSPHATASE; ASPARTATE AMINOTRANSFERASE; LACTATE DEHYDROGENASES; and albumin/globulin ratio. (Blakiston's Gould Medical Dictionary, 4th ed) | 0 | 4.04 | 2 | 0 |
| 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 | 4.04 | 2 | 0 |
| Diabetes Mellitus A heterogeneous group of disorders characterized by HYPERGLYCEMIA and GLUCOSE INTOLERANCE. | 0 | 3.33 | 1 | 0 |
| Emesis [description not available] | 0 | 12.82 | 18 | 13 |
| Nausea An unpleasant sensation in the stomach usually accompanied by the urge to vomit. Common causes are early pregnancy, sea and motion sickness, emotional stress, intense pain, food poisoning, and various enteroviruses. | 0 | 17.89 | 18 | 14 |
| Vomiting The forcible expulsion of the contents of the STOMACH through the MOUTH. | 0 | 17.82 | 18 | 13 |
| Kidney Diseases Pathological processes of the KIDNEY or its component tissues. | 0 | 2.15 | 1 | 0 |
| Proteinuria The presence of proteins in the urine, an indicator of KIDNEY DISEASES. | 0 | 2.15 | 1 | 0 |
| Emesis, Postoperative [description not available] | 0 | 4.45 | 1 | 1 |
| Postoperative Nausea and Vomiting Emesis and queasiness occurring after anesthesia. | 0 | 4.45 | 1 | 1 |
| Peripheral Nerve Diseases [description not available] | 0 | 3.45 | 2 | 0 |
| Peripheral Nervous System Diseases Diseases of the peripheral nerves external to the brain and spinal cord, which includes diseases of the nerve roots, ganglia, plexi, autonomic nerves, sensory nerves, and motor nerves. | 0 | 3.45 | 2 | 0 |
| Asystole [description not available] | 0 | 3.06 | 1 | 0 |
| Heart Arrest Cessation of heart beat or MYOCARDIAL CONTRACTION. If it is treated within a few minutes, heart arrest can be reversed in most cases to normal cardiac rhythm and effective circulation. | 0 | 3.06 | 1 | 0 |
| Acute Hypercapnic Respiratory Failure [description not available] | 0 | 3.5 | 2 | 0 |
| Respiratory Insufficiency Failure to adequately provide oxygen to cells of the body and to remove excess carbon dioxide from them. (Stedman, 25th ed) | 0 | 3.5 | 2 | 0 |
| Visceral Pain Pain originating from internal organs (VISCERA) associated with autonomic phenomena (PALLOR; SWEATING; NAUSEA; and VOMITING). It often becomes a REFERRED PAIN. | 0 | 7.55 | 2 | 0 |
| Alloxan Diabetes [description not available] | 0 | 3 | 4 | 0 |
| Breast Cancer [description not available] | 0 | 7.17 | 1 | 0 |
| Pain, Intractable Persistent pain that is refractory to some or all forms of treatment. | 0 | 2.58 | 2 | 0 |
| Breast Neoplasms Tumors or cancer of the human BREAST. | 0 | 2.17 | 1 | 0 |
| Peripheral Arterial Diseases [description not available] | 0 | 2.17 | 1 | 0 |
| Diabetic Angiopathies VASCULAR DISEASES that are associated with DIABETES MELLITUS. | 0 | 2.17 | 1 | 0 |
| Peripheral Arterial Disease Lack of perfusion in the EXTREMITIES resulting from atherosclerosis. It is characterized by INTERMITTENT CLAUDICATION, and an ANKLE BRACHIAL INDEX of 0.9 or less. | 0 | 2.17 | 1 | 0 |
| 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 | 2.83 | 3 | 0 |
| Pain, Breakthrough [description not available] | 0 | 3.09 | 1 | 0 |
| Breakthrough Pain Acute pain that comes on rapidly despite the use of pain medication. | 0 | 3.09 | 1 | 0 |
| Pregnancy The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH. | 0 | 3.59 | 1 | 1 |
| Diffuse Myofascial Pain Syndrome [description not available] | 0 | 2.21 | 1 | 0 |
| Fibromyalgia A common nonarticular rheumatic syndrome characterized by myalgia and multiple points of focal muscle tenderness to palpation (trigger points). Muscle pain is typically aggravated by inactivity or exposure to cold. This condition is often associated with general symptoms, such as sleep disturbances, fatigue, stiffness, HEADACHES, and occasionally DEPRESSION. There is significant overlap between fibromyalgia and the chronic fatigue syndrome (FATIGUE SYNDROME, CHRONIC). Fibromyalgia may arise as a primary or secondary disease process. It is most frequent in females aged 20 to 50 years. (From Adams et al., Principles of Neurology, 6th ed, p1494-95) | 0 | 7.21 | 1 | 0 |
| Dysphagia [description not available] | 0 | 3.12 | 1 | 0 |
| Deglutition Disorders Difficulty in SWALLOWING which may result from neuromuscular disorder or mechanical obstruction. Dysphagia is classified into two distinct types: oropharyngeal dysphagia due to malfunction of the PHARYNX and UPPER ESOPHAGEAL SPHINCTER; and esophageal dysphagia due to malfunction of the ESOPHAGUS. | 0 | 3.12 | 1 | 0 |
| Constricted Pupil [description not available] | 0 | 3.47 | 1 | 1 |
| Miosis Pupillary constriction. This may result from congenital absence of the dilatator pupillary muscle, defective sympathetic innervation, or irritation of the CONJUNCTIVA or CORNEA. | 0 | 3.47 | 1 | 1 |
| Phantom Limb Perception of painful and nonpainful phantom sensations that occur following the complete or partial loss of a limb. The majority of individuals with an amputated extremity will experience the impression that the limb is still present, and in many cases, painful. (From Neurol Clin 1998 Nov;16(4):919-36; Brain 1998 Sep;121(Pt 9):1603-30) | 0 | 2.08 | 1 | 0 |
| Blood Pressure, High [description not available] | 0 | 9.81 | 10 | 9 |
| 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 | 9.81 | 10 | 9 |
| Gastroenteritis INFLAMMATION of any segment of the GASTROINTESTINAL TRACT from ESOPHAGUS to RECTUM. Causes of gastroenteritis are many including genetic, infection, HYPERSENSITIVITY, drug effects, and CANCER. | 0 | 3.47 | 1 | 1 |
| Polyneuropathy, Acquired [description not available] | 0 | 2.08 | 1 | 0 |
| Cancer of Prostate [description not available] | 0 | 2.08 | 1 | 0 |
| Polyneuropathies Diseases of multiple peripheral nerves simultaneously. Polyneuropathies usually are characterized by symmetrical, bilateral distal motor and sensory impairment with a graded increase in severity distally. The pathological processes affecting peripheral nerves include degeneration of the axon, myelin or both. The various forms of polyneuropathy are categorized by the type of nerve affected (e.g., sensory, motor, or autonomic), by the distribution of nerve injury (e.g., distal vs. proximal), by nerve component primarily affected (e.g., demyelinating vs. axonal), by etiology, or by pattern of inheritance. | 0 | 2.08 | 1 | 0 |
| Prostatic Neoplasms Tumors or cancer of the PROSTATE. | 0 | 2.08 | 1 | 0 |
| Psychophysiologic Disorders A group of disorders characterized by physical symptoms that are affected by emotional factors and involve a single organ system, usually under AUTONOMIC NERVOUS SYSTEM control. (American Psychiatric Glossary, 1988) | 0 | 2.08 | 1 | 0 |
| Costen's Syndrome [description not available] | 0 | 3.01 | 1 | 0 |
| Metastase [description not available] | 0 | 7.52 | 4 | 4 |
| Neoplasm Metastasis The transfer of a neoplasm from one organ or part of the body to another remote from the primary site. | 0 | 7.52 | 4 | 4 |
| Coxarthrosis [description not available] | 0 | 15.48 | 29 | 13 |
| Osteoarthritis, Hip Noninflammatory degenerative disease of the hip joint which usually appears in late middle or old age. It is characterized by growth or maturational disturbances in the femoral neck and head, as well as acetabular dysplasia. A dominant symptom is pain on weight-bearing or motion. | 1 | 17.48 | 29 | 13 |
| Injuries, Spinal Cord [description not available] | 0 | 2.1 | 1 | 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 | 2.1 | 1 | 0 |
| Hallux Abductovalgus [description not available] | 0 | 8.09 | 5 | 5 |
| Hallux Valgus Lateral displacement of the great toe (HALLUX), producing deformity of the first METATARSOPHALANGEAL JOINT with callous, bursa, or BUNION formation over the bony prominence. | 1 | 10.09 | 5 | 5 |
| Diabetic Glomerulosclerosis [description not available] | 0 | 2.11 | 1 | 0 |
| Diabetic Nephropathies KIDNEY injuries associated with diabetes mellitus and affecting KIDNEY GLOMERULUS; ARTERIOLES; KIDNEY TUBULES; and the interstitium. Clinical signs include persistent PROTEINURIA, from microalbuminuria progressing to ALBUMINURIA of greater than 300 mg/24 h, leading to reduced GLOMERULAR FILTRATION RATE and END-STAGE RENAL DISEASE. | 0 | 2.11 | 1 | 0 |
| Bilateral Headache [description not available] | 0 | 3.03 | 1 | 0 |
| 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 | 3.03 | 1 | 0 |
| Peripheral Nerve Injury [description not available] | 0 | 2.11 | 1 | 0 |
| Peripheral Nerve Injuries Injuries to the PERIPHERAL NERVES. | 0 | 2.11 | 1 | 0 |
| Postherpetic Neuralgia [description not available] | 0 | 2.11 | 1 | 0 |
| Neuralgia, Postherpetic Pain in nerves, frequently involving facial SKIN, resulting from the activation the latent varicella-zoster virus (HERPESVIRUS 3, HUMAN). The two forms of the condition preceding the pain are HERPES ZOSTER OTICUS; and HERPES ZOSTER OPHTHALMICUS. Following the healing of the rashes and blisters, the pain sometimes persists. | 0 | 2.11 | 1 | 0 |
| Hematologic Malignancies [description not available] | 0 | 2.13 | 1 | 0 |
| Hematologic Neoplasms Neoplasms located in the blood and blood-forming tissue (the bone marrow and lymphatic tissue). The commonest forms are the various types of LEUKEMIA, of LYMPHOMA, and of the progressive, life-threatening forms of the MYELODYSPLASTIC SYNDROMES. | 0 | 2.13 | 1 | 0 |
| Necrosis The death of cells in an organ or tissue due to disease, injury or failure of the blood supply. | 0 | 2.13 | 1 | 0 |
| Cancer of Head [description not available] | 0 | 2.13 | 1 | 0 |
| Head and Neck Neoplasms Soft tissue tumors or cancer arising from the mucosal surfaces of the LIP; oral cavity; PHARYNX; LARYNX; and cervical esophagus. Other sites included are the NOSE and PARANASAL SINUSES; SALIVARY GLANDS; THYROID GLAND and PARATHYROID GLANDS; and MELANOMA and non-melanoma skin cancers of the head and neck. (from Holland et al., Cancer Medicine, 4th ed, p1651) | 0 | 2.13 | 1 | 0 |
| Mucositis An INFLAMMATION of the MUCOSA with burning or tingling sensation. It is characterized by atrophy of the squamous EPITHELIUM, vascular damage, inflammatory infiltration, and ulceration. It usually occurs at the mucous lining of the MOUTH, the GASTROINTESTINAL TRACT or the airway due to chemical irritations, CHEMOTHERAPY, or radiation therapy (RADIOTHERAPY). | 0 | 7.13 | 1 | 0 |
| Chronic Pancreatitis [description not available] | 0 | 7.15 | 1 | 0 |
| Pancreatitis, Chronic INFLAMMATION of the PANCREAS that is characterized by recurring or persistent ABDOMINAL PAIN with or without STEATORRHEA or DIABETES MELLITUS. It is characterized by the irregular destruction of the pancreatic parenchyma which may be focal, segmental, or diffuse. | 0 | 2.15 | 1 | 0 |
| Cancer of Colon [description not available] | 0 | 2.15 | 1 | 0 |
| Hepatocellular Carcinoma [description not available] | 0 | 2.15 | 1 | 0 |
| Cancer of Liver [description not available] | 0 | 2.15 | 1 | 0 |
| Colonic Neoplasms Tumors or cancer of the COLON. | 0 | 2.15 | 1 | 0 |
| Carcinoma, Hepatocellular A primary malignant neoplasm of epithelial liver cells. It ranges from a well-differentiated tumor with EPITHELIAL CELLS indistinguishable from normal HEPATOCYTES to a poorly differentiated neoplasm. The cells may be uniform or markedly pleomorphic, or form GIANT CELLS. Several classification schemes have been suggested. | 0 | 2.15 | 1 | 0 |
| Liver Neoplasms Tumors or cancer of the LIVER. | 0 | 2.15 | 1 | 0 |
| Odontalgia [description not available] | 0 | 4.75 | 2 | 1 |
| Toothache Pain in the adjacent areas of the teeth. | 0 | 4.75 | 2 | 1 |
| Disease Exacerbation [description not available] | 0 | 3.44 | 1 | 1 |
| Arthropathies [description not available] | 0 | 4.37 | 1 | 1 |
| Joint Diseases Diseases involving the JOINTS. | 1 | 6.37 | 1 | 1 |
| Polyarthritis [description not available] | 0 | 2.06 | 1 | 0 |
| Arthritis Acute or chronic inflammation of JOINTS. | 0 | 2.06 | 1 | 0 |
| Thromboembolism Obstruction of a blood vessel (embolism) by a blood clot (THROMBUS) in the blood stream. | 0 | 2.06 | 1 | 0 |
| Innate Inflammatory Response [description not available] | 0 | 2.06 | 1 | 0 |
| Inflammation A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function. | 0 | 2.06 | 1 | 0 |
| Kahler Disease [description not available] | 0 | 2.07 | 1 | 0 |
| Multiple Myeloma A malignancy of mature PLASMA CELLS engaging in monoclonal immunoglobulin production. It is characterized by hyperglobulinemia, excess Bence-Jones proteins (free monoclonal IMMUNOGLOBULIN LIGHT CHAINS) in the urine, skeletal destruction, bone pain, and fractures. Other features include ANEMIA; HYPERCALCEMIA; and RENAL INSUFFICIENCY. | 0 | 2.07 | 1 | 0 |
| Allergic Reaction [description not available] | 0 | 2.08 | 1 | 0 |
| Hypersensitivity Altered reactivity to an antigen, which can result in pathologic reactions upon subsequent exposure to that particular antigen. | 0 | 7.08 | 1 | 0 |