Page last updated: 2024-12-11

morphinans

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Description

Morphinans: Compounds based on a partially saturated iminoethanophenanthrene, which can be described as ethylimino-bridged benzo-decahydronaphthalenes. They include some of the OPIOIDS found in PAPAVER that are used as ANALGESICS. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

FloraRankFlora DefinitionFamilyFamily Definition
PapavergenusA genus of Eurasian herbaceous plants, the poppies (family PAPAVERACEAE of the dicotyledon class Magnoliopsida), that yield OPIUM from the latex of the unripe seed pods.[MeSH]PapaveraceaeThe poppy plant family of the order Papaverales, subclass Magnoliidae, class Magnoliopsida. These have bisexual, regular, cup-shaped flowers with one superior pistil and many stamens; 2 or 3 conspicuous, separate sepals and a number of separate petals. The fruit is a capsule. Leaves are usually deeply cut or divided into leaflets.[MeSH]

Cross-References

ID SourceID
PubMed CID6857497
CHEBI ID35649
SCHEMBL ID41785
MeSH IDM0014063

Synonyms (21)

Synonym
morphinan
CHEBI:35649
468-10-0
SCHEMBL41785
(9beta,13beta,14beta)-morphinan
(4ar-(4aalpha,10alpha,10aalpha))-1,3,4,9,10,10a-hexahydro-2h-10,4a-(iminoethano)phenanthrene
unii-o97t9o1050
morphinans
unii-oj66wl736g
OJ66WL736G ,
morphinan, (+/-)-
O97T9O1050 ,
(4ar-(4a.alpha.,10.alpha.,10a.alpha.))-1,3,4,9,10,10a-hexahydro-2h-10,4a-(iminoethano)phenanthrene
(4asr,10sr,10asr)-1,3,4,9,10,10a-hexahydro-2h-10,4a-(iminoethano)phenanthrene
(-)-morphinan
(4ar,10r,10ar)-1,3,4,9,10,10a-hexahydro-2h-10,4a-(iminoethano)phenanthrene
morphinan [mi]
(9.beta.,13.beta.,14.beta.)-morphinan
morphinan, (-)-
morphinane
1215192-09-8

Research Excerpts

Overview

Aminomorphinans are a relatively young class of opioid drugs among which substances of high in vitro efficacy and favorable in vivo action are found. Morphinans contain the basic structure of morphine.

ExcerptReferenceRelevance
"The morphinans are an important class of structurally fascinating and physiologically important natural products as exemplified by the famous opium alkaloids of the morphine family. "( Synthesis of Morphinans through Anodic Aryl-Aryl Coupling.
Geske, L; Opatz, T; Sato, E; Vierengel, N, 2021
)
1.55
"Aminomorphinans are a relatively young class of opioid drugs among which substances of high in vitro efficacy and favorable in vivo action are found. "( Novel 6β-acylaminomorphinans with analgesic activity.
Grinnell, SG; Hosztafi, S; Le Rouzic, V; Majumdar, S; Noszál, B; Pasternak, GW; Tóth, G; Urai, Á; Váradi, A, 2013
)
1.24
"Morphinans are a class of compounds containing the basic structure of morphine. "( Neuropsychopharmacological understanding for therapeutic application of morphinans.
Hong, JS; Kim, HC; Shin, EJ, 2010
)
2.04
"Morphinans are a class of compounds containing the basic morphine structure."( Morphinan neuroprotection: new insight into the therapy of neurodegeneration.
Block, ML; Hong, JS; Kim, HC; Zhang, W, 2004
)
1.04

Toxicity

ExcerptReferenceRelevance
"Using the systemically active, non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist dextrorphan, we explored the role of the NMDA receptor-calcium channel complex in the toxic mechanism of action of 3,4-methylenedioxymethamphetamine (MDMA)."( The N-methyl-D-aspartate (NMDA) receptor antagonist, dextrorphan, prevents the neurotoxic effects of 3,4-methylenedioxymethamphetamine (MDMA) in rats.
Finnegan, KT; Irwin, I; Langston, JW; Skratt, JJ, 1989
)
0.28
" DX also antagonized morphological and chemical (lactate dehydrogenase efflux) evidence of cortical neuronal cell injury produced by toxic bath exposure to NMDA, quinolinate or glutamate, but did not affect toxic exposure to quisqualate or kainate."( Dextrorphan and levorphanol selectively block N-methyl-D-aspartate receptor-mediated neurotoxicity on cortical neurons.
Choi, DW; Peters, S; Viseskul, V, 1987
)
0.27
"05 mg/kg to provide a safe outpatient intravenous sedative technique."( Nalbuphine combined with midazolam for outpatient sedation. An assessment of safety in volunteers.
Cole, PV; Sury, MR, 1988
)
0.27
" Adverse effects, such as dizziness, nausea, thirst, numbness of the hands etc, observed in 5 patients were transient and required no medication."( [Clinical trial of butorphanol tartrate in cancer patients: evaluation for analgesic effects and safety on the basis of long term administration].
Ebina, A; Hayashi, I; Ito, T; Konno, K; Nagai, K; Nakai, Y; Sato, M, 1983
)
0.27
"The narcotic antagonist TR5379M had po LD50 values of 365 and 750 mg/kg and iv LD50 values of 35."( Preclinical toxicity and teratogenicity studies with the narcotic antagonist analgesic drug TR5379M.
Bare, JJ; Clemens, GR; Halliwell, WE; Hartnagel, RE; Kitchen, DN; Kowalski, RL; Porter, MC,
)
0.13
"This open-label study examined the effects and adverse drug reactions (ADRs) of 52-week oral administration of nalfurafine hydrochloride (5 µg/day) in 211 hemodialysis patients with a treatment-resistant itch."( Efficacy and safety of a novel ĸ-agonist for managing intractable pruritus in dialysis patients.
Ebata, T; Kumagai, H; Kurihara, M; Miyasato, K; Muramatsu, T; Nakamoto, H; Suzuki, H; Takamori, K; Yanagita, T, 2012
)
0.38
" This is the first study to demonstrate that the novel δ opioid receptor agonist KNT-127 produces distinct anxiolytic-like effects in rats, without producing the adverse effects associated with benzodiazepines."( The novel δ opioid receptor agonist KNT-127 produces distinct anxiolytic-like effects in rats without producing the adverse effects associated with benzodiazepines.
Inagaki, M; Nagase, H; Oka, J; Saitoh, A; Sugiyama, A; Yamada, M, 2013
)
0.39
"Opioid-induced constipation (OIC) is a common adverse effect of opioid therapy."( Randomised clinical trial: the long-term safety and tolerability of naloxegol in patients with pain and opioid-induced constipation.
Chey, WD; Diva, U; Lappalainen, J; Sostek, M; Tack, J; Webster, L, 2014
)
0.4
" Frequency of adverse events (AEs) was 81."( Randomised clinical trial: the long-term safety and tolerability of naloxegol in patients with pain and opioid-induced constipation.
Chey, WD; Diva, U; Lappalainen, J; Sostek, M; Tack, J; Webster, L, 2014
)
0.4
"In patients with noncancer pain and opioid-induced constipation, naloxegol 25 mg/day up to 52 weeks was generally safe and well tolerated."( Randomised clinical trial: the long-term safety and tolerability of naloxegol in patients with pain and opioid-induced constipation.
Chey, WD; Diva, U; Lappalainen, J; Sostek, M; Tack, J; Webster, L, 2014
)
0.4
" The most common adverse events were somnolence, dizziness, headache, and nausea."( Safety, tolerability, pharmacokinetics, and pharmacodynamic effects of naloxegol at peripheral and central nervous system receptors in healthy male subjects: A single ascending-dose study.
Bui, K; Butler, K; Eldon, MA; Kugler, AR; Medve, RA; Sostek, M, 2015
)
0.42
"Opioid-induced constipation (OIC) is the most common and often a treatment-limiting adverse event (AE) of opioid therapy for chronic pain."( Safety, tolerability, and pharmacokinetics of multiple ascending doses of naloxegol.
Bui, K; Butler, K; Eldon, MA; Kugler, AR; Medve, RA; Sostek, M, 2015
)
0.42
"Naloxegol was generally safe and well tolerated in this 12-week extension study in patients with noncancer pain and OIC."( A 12-week extension study to assess the safety and tolerability of naloxegol in patients with noncancer pain and opioid-induced constipation.
Diva, U; Lappalainen, J; Tummala, R; Webster, L,
)
0.13
" Often the only therapeutic option is to use class 2 or 3 analgesic opioids in the WHO classification, as class 1 analgesics may be toxic or of limited efficacy."( [Management of adverse effects of opioid therapy].
Wirz, S, 2017
)
0.46
"Compared to MTX, SIN had better clinical efficacy and relatively fewer adverse events\ in treatment of RA, especially when it was used together with MTX."( Effects and safety of Sinomenine in treatment of rheumatoid arthritis contrast to methotrexate: a systematic review and Meta-analysis.
Ji, W; Liu, W; Lu, Y; Qian, X; Wang, Y; Wei, G, 2016
)
0.43
" Adverse event incidences were generally comparable across treatment groups, regardless of opioid dose or duration of therapy but were numerically higher with some specific baseline opioids."( Efficacy and safety of naloxegol for opioid-induced constipation assessed by specific opioid medication, opioid dose, and duration of opioid use.
Coyne, K; Datto, C; Gudin, J; Hu, Y; Nalamachu, S; Poon, JL,
)
0.13
" Safety assessments included adverse event documentation, measurements of opioid withdrawal, and clinical laboratory tests."( Long-term Safety and Tolerability of NKTR-181 in Patients with Moderate to Severe Chronic Low Back Pain or Chronic Noncancer Pain: A Phase 3 Multicenter, Open-Label, 52-Week Study (SUMMIT-08 LTS).
Agaiby, E; Argoff, C; Doberstein, SK; Gimbel, J; Gudin, J; Hale, M; Katz, N; Lu, L; Markman, J; Potts, J; Rauck, R; Siddhanti, S; Tagliaferri, M; Wild, J, 2020
)
0.56
" The most frequently reported treatment-emergent adverse events (TEAEs) were constipation (26%) and nausea (12%)."( Long-term Safety and Tolerability of NKTR-181 in Patients with Moderate to Severe Chronic Low Back Pain or Chronic Noncancer Pain: A Phase 3 Multicenter, Open-Label, 52-Week Study (SUMMIT-08 LTS).
Agaiby, E; Argoff, C; Doberstein, SK; Gimbel, J; Gudin, J; Hale, M; Katz, N; Lu, L; Markman, J; Potts, J; Rauck, R; Siddhanti, S; Tagliaferri, M; Wild, J, 2020
)
0.56
"The study results support the premise that NKTR-181 is a safe and effective option for patients with moderate to severe CLBP or CNP."( Long-term Safety and Tolerability of NKTR-181 in Patients with Moderate to Severe Chronic Low Back Pain or Chronic Noncancer Pain: A Phase 3 Multicenter, Open-Label, 52-Week Study (SUMMIT-08 LTS).
Agaiby, E; Argoff, C; Doberstein, SK; Gimbel, J; Gudin, J; Hale, M; Katz, N; Lu, L; Markman, J; Potts, J; Rauck, R; Siddhanti, S; Tagliaferri, M; Wild, J, 2020
)
0.56
" Thus, sinomenine inhibits amyloid beta-induced production of toxic factors from astrocytes, and confers protection to hippocampal neuronal cells as well as human neurons against indirect toxicity."( Sinomenine inhibits amyloid beta-induced astrocyte activation and protects neurons against indirect toxicity.
Agrawal, A; Pandey, HS; Seth, P; Sharma, SK; Singal, CMS; Singh, D, 2020
)
0.56
" The frequency of adverse reactions were reduced compared with that in the control group(P<0."( [Meta-analysis of efficacy and safety of sinomenine combined with methotrexate in treatment of rheumatoid arthritis].
Li, X; Shuai, YF; Zeng, C, 2021
)
0.62

Pharmacokinetics

ExcerptReferenceRelevance
" No differences were found between treatments in mean Cmax and AUC values of oxycodone which varied from 34 to 38 ng ml-1 and from 208 to 245 ng ml-1 h, respectively."( The pharmacokinetics and metabolism of oxycodone after intramuscular and oral administration to healthy subjects.
Kalso, E; Olkkola, KT; Pöyhiä, R; Seppälä, T, 1992
)
0.28
" injection of 20 mg/kg of sinomenine to rabbits, the pharmacokinetic characteristics were found to fit a two-compartment open model."( [Pharmacokinetics of sinomenine by HPLC].
Cai, H; Lou, S; Pan, X; Zhang, X, 1992
)
0.28
" The half-life time in plasma was slightly shorter than in other studies, while the peak plasma concentrations were comparable with other results in the literature."( [Cumulative pharmacokinetics and clinical effects of nalbuphine in patients in the postoperative phase. An open multicenter study].
, 1989
)
0.28
" Elimination half-life (t1/2) was significantly shorter in group I (0."( Pharmacokinetics of nalbuphine in infants, young healthy volunteers, and elderly patients.
Bergnieres, J; Blondel, Y; Gardin, ME; Grippat, JC; Jaillon, P; Lecocq, B; Meignan, S; Richard, MO; Vergnoux, O, 1989
)
0.28
"40 liters/kg), distribution half-life (7."( Influence of age on the pharmacokinetics of butorphanol.
Higbee, M; Maesner, J; Ramsey, R; Wood, J, 1988
)
0.27
" After administration, serum concentrations of nalbuphine were measured for 12 h using a high pressure liquid chromatography assay, and pharmacokinetic parameters were derived using a three compartment model."( The pharmacokinetics of oral and intravenous nalbuphine in healthy volunteers.
Achola, KJ; Aitkenhead, AR; Lin, ES, 1988
)
0.27
" No therapeutically significant differences were detected between the three preparations tested, and there were no great differences between the pharmacokinetic profiles of dextromethorphan and dextrorphan."( Pharmacokinetics of dextromethorphan and dextrorphan: a single dose comparison of three preparations in human volunteers.
Hänninen, U; Karttunen, P; Kokkonen, P; Nykänen, S; Silvasti, M; Tukiainen, H, 1987
)
0.27
" Mean Cmax values after 20 mg doses were 60 and 56 ng/ml."( The pharmacokinetics of intravenous, intramuscular, and subcutaneous nalbuphine in healthy subjects.
Lee, FH; Lo, MW; Schary, WL; Whitney, CC, 1987
)
0.27
" AUC values were also calculated for the pharmacodynamic variable "drug effect," scored on a 100 mm visual analog scale."( Pharmacokinetic-pharmacodynamic relationships of controlled-release oxycodone.
Benziger, DP; Burke, BE; Fitzmartin, RD; Goldenheim, PD; Kaiko, RF; Reder, RF, 1996
)
0.29
" Mean elimination half-life was prolonged in uremic patients due to increased volume of distribution and reduced clearance."( The pharmacokinetics of oxycodone in uremic patients undergoing renal transplantation.
Kirvela, M; Lindgren, L; Olkkola, KT; Seppala, T, 1996
)
0.29
" Studies on pharmacokinetic interaction between the active constituents of these two herbs (paeoniflorin and sinomenine, respectively) provide empirical evidence to support their clinical practice."( Influence of co-administrated sinomenine on pharmacokinetic fate of paeoniflorin in unrestrained conscious rats.
Cai, X; Chan, K; Jiang, ZH; Liu, L; Liu, ZQ; Wong, YF; Xie, Y; Xu, HX; Zhou, H, 2005
)
0.33
" The results demonstrated that oral administration with a single dosage at a rate of 90 mg sinomenine/kg in rats achieved about 80% bioavailability, while most of the other pharmacokinetic parameters were similar to the data from the animals treated intravenously."( The pharmacokinetics and tissue distribution of sinomenine in rats and its protein binding ability in vitro.
Chan, K; Jiang, ZH; Liu, L; Liu, ZQ; Wong, YF; Xu, HX; Zhou, H, 2005
)
0.33
" From a pharmacokinetic standpoint, the 24-h SM."( Impact of release characteristics of sinomenine hydrochloride dosage forms on its pharmacokinetics in beagle dogs.
Gao, K; He, ZG; Li, B; Mao, JJ; Shi, JM; Sun, J; Sun, YH; Zhang, TH, 2005
)
0.33
"The in vitro release properties of the dosage forms strongly affect their pharmacokinetic behavior in vivo."( Impact of release characteristics of sinomenine hydrochloride dosage forms on its pharmacokinetics in beagle dogs.
Gao, K; He, ZG; Li, B; Mao, JJ; Shi, JM; Sun, J; Sun, YH; Zhang, TH, 2005
)
0.33
", paeoniflorin and sinomenine, in pharmacokinetic parameters, tissues distribution, and protein binding ability could provide empirical data to support their clinical application."( Pharmacokinetic interaction of paeoniflorin and sinomenine: pharmacokinetic parameters and tissue distribution characteristics in rats and protein binding ability in vitro.
Bian, ZX; Chan, K; Jiang, ZH; Liu, L; Liu, ZQ; Wong, YF; Xu, HX; Zhou, H, 2005
)
0.33
" In this report a liquid chromatography-electrospray mass spectrometry (LC-ESI-MS) method with in vivo microdialysis for the pharmacokinetic study of free-form sinomenine in rat skin has been developed."( Pharmacokinetic study of free-form sinomenine in rat skin by microdialysis coupled with liquid chromatography-electrospray mass spectrometry.
Hu, JH; Shi, LF; Zheng, H, 2007
)
0.34
" Oral administration of oxycodone to the SD rat is a poor model of the human for the study of the pharmacodynamic effects of oxycodone."( Sex differences in the pharmacokinetics, oxidative metabolism and oral bioavailability of oxycodone in the Sprague-Dawley rat.
Chan, S; Edwards, SR; Smith, MT; Wyse, BD, 2008
)
0.35
"To study pharmacokinetic parameters and absolute bioavailability for oral use of sinomenine tablet in beagle dogs."( [Study on pharmacokinetics and absolute bioavailability of sinomenine in beagle dogs].
Chen, W; Feng, X; Kang, J; Li, Q; Zhou, Y, 2009
)
0.35
" The pharmacokinetic parameters were calculated by 3P97 pharmacokinetic program."( [Study on pharmacokinetics and absolute bioavailability of sinomenine in beagle dogs].
Chen, W; Feng, X; Kang, J; Li, Q; Zhou, Y, 2009
)
0.35
" Plasma concentrations of oxycodone and its oxidative metabolites were measured for 48 h, and pharmacodynamic effects were evaluated."( Effects of itraconazole on the pharmacokinetics and pharmacodynamics of intravenously and orally administered oxycodone.
Grönlund, J; Hagelberg, NM; Laine, K; Neuvonen, M; Neuvonen, PJ; Olkkola, KT; Saari, TI, 2010
)
0.36
" Most of the pharmacokinetic changes in oral oxycodone were seen in the elimination phase, with modest effects by itraconazole on its peak concentration, which was increased by 45% (P=0."( Effects of itraconazole on the pharmacokinetics and pharmacodynamics of intravenously and orally administered oxycodone.
Grönlund, J; Hagelberg, NM; Laine, K; Neuvonen, M; Neuvonen, PJ; Olkkola, KT; Saari, TI, 2010
)
0.36
" We performed a three-way, placebo-controlled, double-blind cross-over study to assess the pharmacokinetic and pharmacodynamic consequences of drug interactions with oxycodone."( Effect of the inhibition of CYP3A4 or CYP2D6 on the pharmacokinetics and pharmacodynamics of oxycodone.
Drewe, J; Hammann, F; Krähenbühl, S; Kummer, O; Moser, C; Schaller, O, 2011
)
0.37
"Inhibition of CYP3A4 by ketoconazole increases the exposure and some pharmacodynamic effects of oxycodone."( Effect of the inhibition of CYP3A4 or CYP2D6 on the pharmacokinetics and pharmacodynamics of oxycodone.
Drewe, J; Hammann, F; Krähenbühl, S; Kummer, O; Moser, C; Schaller, O, 2011
)
0.37
"To explore the pharmacokinetic of Sinomenine transdermal patch."( [The pharmacokinetics study on Sinomenine transdermal patch on anaesthetized Beagle dogs].
Yu, Y; Zhang, YF; Zhou, LL, 2010
)
0.36
" There were no significant sex-related differences in any of the pharmacokinetic parameters."( Elimination of intravenous oxycodone in the elderly: a pharmacokinetic study in postoperative orthopaedic patients of different age groups.
Aantaa, R; Kuusniemi, K; Liukas, A; Neuvonen, M; Neuvonen, PJ; Olkkola, KT; Virolainen, P, 2011
)
0.37
" We may conclude that pharmacokinetic studies of complex herbal products are not only necessary but also feasible by using representative bioactive chemicals as indicators of establishing quality control standards and of determining pharmacokinetic behavior of herbal medicines."( The pharmacokinetic study of sinomenine, paeoniflorin and paeonol in rats after oral administration of a herbal product Qingfu Guanjiesu capsule by HPLC.
Jiang, ZH; Liu, L; Liu, ZQ; Ma, WZ; Wong, YF; Xie, Y; Zhou, H, 2014
)
0.4
"The aim of this study is to evaluate the pharmacokinetic profile of oxycodone and three of its metabolites, noroxycodone, oxymorphone and noroxymorphone after intravenous administration in Chinese patients with pain."( Pharmacokinetics of oxycodone hydrochloride and three of its metabolites after intravenous administration in Chinese patients with pain.
Dong, RH; Gao, HZ; Hao, GT; Li, YY; Liang, YG; Liu, ZY; Qu, HY; Wang, XF; Zhang, LJ; Zhou, HY, 2014
)
0.4
"Pharmacokinetic parameters showed that mean values of C(max), AUC(0-t) and AUC(0-∞) of oxycodone were dose dependent, whereas Tmax and t(1/2) were not."( Pharmacokinetics of oxycodone hydrochloride and three of its metabolites after intravenous administration in Chinese patients with pain.
Dong, RH; Gao, HZ; Hao, GT; Li, YY; Liang, YG; Liu, ZY; Qu, HY; Wang, XF; Zhang, LJ; Zhou, HY, 2014
)
0.4
" Time to Cmax was shorter in patients with moderate impairment (0."( The effects of mild or moderate hepatic impairment on the pharmacokinetics, safety, and tolerability of naloxegol.
Bui, K; She, F; Sostek, M, 2014
)
0.4
" Overall exposures in ESRD patients were similar and Cmax was 29% lower versus normal subjects."( The effects of renal impairment on the pharmacokinetics, safety, and tolerability of naloxegol.
Bui, K; She, F; Sostek, M, 2014
)
0.4
" Pharmacokinetic parameters for sinomenine were processed by non-compartmental analysis."( Comparative pharmacokinetics study of sinomenine in rats after oral administration of sinomenine monomer and Sinomenium acutum extract.
Han, L; Jiang, KY; Lu, XY; Meng, SN; Wang, X; Zhang, MF; Zhao, Y; Zuo, L, 2014
)
0.4
" Data were evaluated from 24 subjects in two pharmacokinetic studies who received an oral dose of 40 mg of dimemorfan syrup (n = 12) or dimemorfan tablet (n = 12) after providing written informed consent and being divided into three groups: subjects with CYP2D6*10 CC (n = 5), CYP2D6*10 CT (n = 11) and CYP2D6*10 TT (n = 8)."( Cytochrome P450 2D6*10 genotype affects the pharmacokinetics of dimemorfan in healthy Chinese subjects.
Liu, L; Liu, S; Pei, Q; Peng, J; Tan, H; Yang, G; Yang, L; Yang, X; Yuan, H, 2015
)
0.42
" Finally, the developed method was successfully applied for the determination of dimemorfan in a pharmacokinetic study using healthy Chinese subjects."( Simple and sensitive LC-MS/MS-based assay for the quantification of dimemorfan in human plasma for use in a pharmacokinetic study.
Chen, J; Guo, C; Hua, Y; Pei, Q; Peng, J; Tan, H; Yang, G; Yang, L; Yuan, H, 2015
)
0.42
" However, the pharmacokinetic and penetration into synovial fluid (SF) of sinomenine have not been reported."( Pharmacokinetics and penetration into synovial fluid of systemical and electroporation administered sinomenine to rabbits.
Cai, HL; Deng, Y; Jiang, P; Li, HD; Yan, H; Yan, M, 2015
)
0.42
" In both studies, samidorphan was rapidly absorbed, with a Tmax of 1 hour, and AUC increased with increasing dose."( Single- and multiple-dose pharmacokinetics of samidorphan, a novel opioid antagonist, in healthy volunteers.
DiPetrillo, L; Ehrich, E; Silverman, B; Turncliff, R, 2015
)
0.42
"In these single- and multiple-dose studies in healthy volunteers, samidorphan exhibited a pharmacokinetic profile consistent with once-daily dosing."( Single- and multiple-dose pharmacokinetics of samidorphan, a novel opioid antagonist, in healthy volunteers.
DiPetrillo, L; Ehrich, E; Silverman, B; Turncliff, R, 2015
)
0.42
" The aim of the study was to develop a population pharmacokinetic model describing the concentration vs."( Population pharmacokinetics of naloxegol in a population of 1247 healthy subjects and patients.
Al-Huniti, N; Bui, KH; Chapel, S; Sostek, M; Xu, H, 2016
)
0.43
" Pharmacokinetic analysis used the non-linear mixed effects modelling program."( Population pharmacokinetics of naloxegol in a population of 1247 healthy subjects and patients.
Al-Huniti, N; Bui, KH; Chapel, S; Sostek, M; Xu, H, 2016
)
0.43
" Phase of study, gender, race, concomitant strong or moderate CYP3A4 inhibitors, strong CYP3A4 inducers, P-glycoprotein inhibitors or inducers, naloxegol formulation, baseline creatinine clearance and baseline opioid dose had a significant effect on at least one pharmacokinetic parameter."( Population pharmacokinetics of naloxegol in a population of 1247 healthy subjects and patients.
Al-Huniti, N; Bui, KH; Chapel, S; Sostek, M; Xu, H, 2016
)
0.43
" Rapid absorption, linear pharmacokinetics up to 1000 mg, and low to moderate between-subject pharmacokinetic variability was observed."( Safety, tolerability, pharmacokinetics, and pharmacodynamic effects of naloxegol at peripheral and central nervous system receptors in healthy male subjects: A single ascending-dose study.
Bui, K; Butler, K; Eldon, MA; Kugler, AR; Medve, RA; Sostek, M, 2015
)
0.42
" By integrating in silico, preclinical, and clinical pharmacokinetic (PK) findings, minimal and full physiologically based pharmacokinetic (PBPK) models were developed to predict the drug-drug interaction (DDI) potential for naloxegol."( Simulation and Prediction of the Drug-Drug Interaction Potential of Naloxegol by Physiologically Based Pharmacokinetic Modeling.
Al-Huniti, N; Bui, K; Sostek, M; Zhou, D, 2016
)
0.43
" Preterm neonates were found to have the highest pharmacokinetic variability out of the study population."( Maturation of oxycodone pharmacokinetics in neonates and infants: Oxycodone and its metabolites in plasma and urine.
Hautajärvi, H; Heikkinen, M; Hokkanen, J; Kokki, H; Kokki, M; Pitkänen, H; Ranta, VP; Sankilampi, U; Välitalo, P, 2017
)
0.46
"Oxycodone elimination is slower and pharmacokinetic variability more pronounced in neonates when compared to older infants."( Maturation of oxycodone pharmacokinetics in neonates and infants: Oxycodone and its metabolites in plasma and urine.
Hautajärvi, H; Heikkinen, M; Hokkanen, J; Kokki, H; Kokki, M; Pitkänen, H; Ranta, VP; Sankilampi, U; Välitalo, P, 2017
)
0.46
" single supratherapeutic doses up to 1000 mg in healthy volunteers), the pharmacokinetic properties of naloxegol appear to be time- and dose-independent."( Clinical Pharmacokinetics and Pharmacodynamics of Naloxegol, a Peripherally Acting µ-Opioid Receptor Antagonist.
Al-Huniti, N; Bui, K; Floettmann, E; Xu, H; Zhou, D, 2017
)
0.46
"Investigate the pharmacokinetic properties of the antitussive dimemorfan phosphate tablets in healthy male and female Chinese volunteers after single and multiple-dose administration; and to evaluate the food-effect on pharmacokinetics of dimemorfan."( Pharmacokinetics of dimemorfan phosphate tablets in healthy Chinese volunteers.
Luo, Z; Miao, J; Shen, Y; Wang, Y; Xiang, J; Yu, Q, 2017
)
0.46
" The HPLC-MS/MS method was developed and fully validated for determination of SND-117 in rat plasma, and the pharmacokinetic differences were investigated after different administration routes."( A selective HPLC-MS/MS method for quantification of SND-117 in rat plasma and its application to a pharmacokinetic study.
Bao, BH; Di, LQ; Kang, A; Li, JS; Li, JX; Shen, Q; Zhao, Y, 2017
)
0.46
" This study was to investigate whether and how CV drugs affect the pharmacokinetic profile of sinomenine."( Co-administration with simvastatin or lovastatin alters the pharmacokinetic profile of sinomenine in rats through cytochrome P450-mediated pathways.
Dai, Y; Jin, Y; Wang, M; Wang, Y; Xia, Y; Yun, X, 2018
)
0.48
" The pharmacokinetics including the relatively short half-life of oxycodone in patients with ESRD with or without haemodialysis and the absence of unconjugated active metabolites indicate that oxycodone can be used at usual doses in patients requiring dialysis."( Pharmacokinetics of oxycodone/naloxone and its metabolites in patients with end-stage renal disease during and between haemodialysis sessions.
Amico, P; Dickenmann, M; Duthaler, U; Hammann, F; Haschke, M; Jehle, AW; Kalbermatter, S; Krähenbühl, S; Lenherr, C; Leuppi-Taegtmeyer, A; Liechti, ME; Meyer Zu Schwabedissen, HE; Schmid, Y, 2019
)
0.51
"The method was validated with respect to sensitivity, specificity, linearity, precision, accuracy and especially the stability of analytes under various conditions, and was successfully applied in evaluating the pharmacokinetic profiles of SN in the joint cavity."( Evaluation of pharmacokinetics and pharmaco-dynamics of sinomenine-hyaluronic acid conjugate after intra-articular administration for osteoarthritis treatment.
Chen, J; Cheng, Y; Fang, S; Ling, P; Liu, J; Shao, H, 2019
)
0.51

Compound-Compound Interactions

ExcerptReferenceRelevance
"The sedative effects of the low dose of butorphanol combined with diazepam during spinal-epidural (H-type) anesthesia were studied in 20 urological or gynecological patients of ASA class I or II."( [The sedative effects of a low dose of butorphanol combined with diazepam during spinal-epidural anesthesia (H-type anesthesia)].
Abe, Y; Hanaoka, K; Hiraishi, T; Ide, Y; Sugiyama, A; Yajima, C, 1989
)
0.28
"This study compared the analgesic efficacy, sedative, and amnesic properties, and side effects of nalbuphine versus meperidine as intravenous premedicants in combination with intravenous diazepam for the treatment of outpatients undergoing the removal of impacted third molars with alveolar nerve block anesthesia."( A double-blind comparison of nalbuphine and meperidine hydrochloride as intravenous analgesics in combination with diazepam for oral surgery outpatients.
Scott, RF, 1987
)
0.27
" These results are similar to previous results obtained with tripelennamine and pentazocine suggesting that nalbuphine may have abuse potential if combined with tripelennamine."( Effects of nalbuphine alone and in combination with tripelennamine on rewarding brain stimulation thresholds in the rat.
Kornetsky, C; Unterwald, EM, 1986
)
0.27
"A xylazine and butorphanol drug combination produced minimal and transient hemodynamic effects and no significant respiratory depression when administered to 6 healthy horses."( A new analgesic drug combination in the horse.
Muir, WW; Robertson, JT, 1983
)
0.27
" Its antiproliferative effect on human mononuclear cells in combination with different immunosuppressive drugs was further analysed in vitro."( Synergistic effects of the alkaloid sinomenine in combination with the immunosuppressive drugs tacrolimus and mycophenolic acid.
Kaever, V; Resch, K; Vieregge, B, 1999
)
0.3
"To investigate the inhibitory effects of sinomenine (SIN) combined with 5-fluorouracil (5-FU) on esophageal carcinoma in vitro and in vivo."( Cooperative inhibitory effect of sinomenine combined with 5-fluorouracil on esophageal carcinoma.
Dong, WG; Guo, XF; Qiu, S; Song, J; Wang, J; Yang, ZR; Zhang, JX, 2013
)
0.39
"The combined effects of SIN and 5-FU on esophageal carcinoma were superior to those of the individual compounds, and the drug combination did not increase the side effects of chemotherapy."( Cooperative inhibitory effect of sinomenine combined with 5-fluorouracil on esophageal carcinoma.
Dong, WG; Guo, XF; Qiu, S; Song, J; Wang, J; Yang, ZR; Zhang, JX, 2013
)
0.39
" The permeability of nalfurafine across human P-glycoprotein (P-gp)-expressing LLC-PK1 cells was investigated to evaluate drug-drug interactions (DDI) involving the P-gp efflux transporter of nalfurafine."( Drug-Drug Interactions of a Novel κ-Opioid Receptor Agonist, Nalfurafine Hydrochloride, Involving the P-Glycoprotein.
Ando, A; Miyamoto, Y; Ohzone, Y; Sasago, S, 2016
)
0.43
" By integrating in silico, preclinical, and clinical pharmacokinetic (PK) findings, minimal and full physiologically based pharmacokinetic (PBPK) models were developed to predict the drug-drug interaction (DDI) potential for naloxegol."( Simulation and Prediction of the Drug-Drug Interaction Potential of Naloxegol by Physiologically Based Pharmacokinetic Modeling.
Al-Huniti, N; Bui, K; Sostek, M; Zhou, D, 2016
)
0.43
" Here, we further investigated whether NFF alone (1-10 μg/kg) or in combination with naltrexone (NTX, mu-opioid receptor [MOP-r] antagonist) altered alcohol relapse-like drinking using a mouse alcohol deprivation effect (ADE) paradigm to mimic the relapse episodes in human alcoholics."( Clinically utilized kappa-opioid receptor agonist nalfurafine combined with low-dose naltrexone prevents alcohol relapse-like drinking in male and female mice.
Kreek, MJ; Zhou, Y, 2019
)
0.51
" In addition, both in vitro and in vivo studies indicated that the SIN-TSL combined with microwave hyperthermia exhibited superior anti-rheumatoid arthritis effect."( Sinomenine hydrochloride loaded thermosensitive liposomes combined with microwave hyperthermia for the treatment of rheumatoid arthritis.
Du, Y; Qi, J; Shen, Q; Shu, G; Ying, X; Zhang, X, 2020
)
0.56
"To systemically evaluate the efficacy and safety of sinomenine combined with methotrexate(SIN+MTX) in the treatment of rheumatoid arthritis(RA)."( [Meta-analysis of efficacy and safety of sinomenine combined with methotrexate in treatment of rheumatoid arthritis].
Li, X; Shuai, YF; Zeng, C, 2021
)
0.62

Bioavailability

ExcerptReferenceRelevance
" The bioavailability of dextromethorphan hydrobromide after 30 mg po, as measured by the concentration of total (free and conjugated) dextrorphan in the plasma, was determined in six human volunteers with this procedure."( Determination of dextrorphan in plasma and evaluation of bioavailability of dextromethorphan hydrobromide in humans.
Emele, JF; Ramachander, G; Williams, FD, 1977
)
0.26
" Absolute bioavailability of nalbuphine increased from F = 12% in group II to 46."( Pharmacokinetics of nalbuphine in infants, young healthy volunteers, and elderly patients.
Bergnieres, J; Blondel, Y; Gardin, ME; Grippat, JC; Jaillon, P; Lecocq, B; Meignan, S; Richard, MO; Vergnoux, O, 1989
)
0.28
" The disposition of (-)17-(cyclobutylmethyl)-4,5 alpha-epoxymorphinan-3,6 alpha, 14-triol (Nalbuphine, Nubain) and its 3-acetylsalicylate ester has been studied in rat and dog to determine whether this analogue can improve the oral bioavailability of nalbuphine."( Species variation in the disposition of nalbuphine and its acetylsalicylate ester analogue.
Harrelson, JC; Wong, YJ, 1988
)
0.27
" Bioavailability of the oral preparation was 11."( The pharmacokinetics of oral and intravenous nalbuphine in healthy volunteers.
Achola, KJ; Aitkenhead, AR; Lin, ES, 1988
)
0.27
" Absolute bioavailability of the orally administered forms of nalbuphine ranged from 16."( The disposition and bioavailability of intravenous and oral nalbuphine in healthy volunteers.
Lo, MW; Schary, WL; Whitney, CC, 1987
)
0.27
" The mean absolute bioavailability was 81% and 83% for the 10 and 20 mg intramuscular doses, respectively, and 79% and 76% following 10 and 20 mg of subcutaneous nalbuphine."( The pharmacokinetics of intravenous, intramuscular, and subcutaneous nalbuphine in healthy subjects.
Lee, FH; Lo, MW; Schary, WL; Whitney, CC, 1987
)
0.27
" Gastric emptying in the immediate postoperative period was also assessed in each patient by measuring the rate of absorption of orally administered paracetamol."( Analgesic and gastrointestinal effects of nalbuphine--a comparison with pethidine.
Couch, RA; Mark, A; Slattery, PJ, 1986
)
0.27
" In both species nalbuphine had high systemic clearance and low oral bioavailability as a result of extensive first-pass metabolism."( Oral and rectal nalbuphine bioavailability: first-pass metabolism in rats and dogs.
Aungst, BJ; Lam, G; Shefter, E,
)
0.13
"The systemic bioavailability of buprenorphine has been studied in female rats following single doses (200 microgram kg-1) administered by one of six different routes."( The systemic bioavailability of buprenorphine by various routes of administration.
Brewster, D; Humphrey, MJ; Mcleavy, MA, 1981
)
0.26
" Comparison of areas under the plasma concentration versus time curves to 24 hours after dosing showed the mean bioavailability of buprenorphine from the intramuscular doses was 70% of that from the reference intravenous doses."( Plasma concentration and disposition of buprenorphine after intravenous and intramuscular doses to baboons.
Biggs, SR; Henson, R; Lloyd-Jones, JG; Robinson, P; Taylor, T, 1980
)
0.26
" The variation in plasma morphine concentrations was higher than that of oxycodone, consistent with the lower bioavailability of morphine."( Morphine or oxycodone in cancer pain?
Heiskanen, TE; Kalso, EA; Ruismäki, PM; Seppälä, TA, 2000
)
0.31
"Due to low central nervous system (CNS) bioavailability of delta-opioid peptides, little is known about the effect of systemic administration of delta-opioid receptor ligands."( Spinal delta-opioid receptors mediate suppression of systemic SNC80 on excitability of the flexor reflex in normal and inflamed rat.
Cao, CQ; Dray, A; Hong, Y; Perkins, M, 2001
)
0.31
" morphine-induced systemic skin scratching and is more readily absorbed intragastrically than is U-50488H, resulting in high bioavailability in the intragastric route."( Inhibitory effects of TRK-820 on systemic skin scratching induced by morphine in rhesus monkeys.
Endoh, T; Fujiwara, A; Nagase, H; Okano, K; Tanaka, T; Umeuchi, H; Wakasa, Y, 2004
)
0.32
" These results indicate that sinomenine hydrochloride at 90 mg/kg significantly improved the bioavailability of paeoniflorin in rats."( Influence of co-administrated sinomenine on pharmacokinetic fate of paeoniflorin in unrestrained conscious rats.
Cai, X; Chan, K; Jiang, ZH; Liu, L; Liu, ZQ; Wong, YF; Xie, Y; Xu, HX; Zhou, H, 2005
)
0.33
" Our previous studies demonstrated that sinomenine could significantly improve the bioavailability of paeoniflorin in rats, but the underlying mechanisms remain unknown."( The effects of sinomenine on intestinal absorption of paeoniflorin by the everted rat gut sac model.
Chan, K; Jiang, ZH; Liu, L; Liu, ZQ; Wong, YF; Xu, HX; Zhou, H, 2006
)
0.33
"Poor permeation, p-gp-mediated efflux, and hydrolysis via a glucosidase contributed to the poor bioavailability of paeoniflorin."( Mechanisms responsible for poor oral bioavailability of paeoniflorin: Role of intestinal disposition and interactions with sinomenine.
Hu, M; Jiang, ZH; Liu, L; Liu, ZQ, 2006
)
0.33
" Microdialysis can be used to study bioavailability and bioequivalence of different preparation."( [Bioequivalence study of sinomenine patch by microdialysis].
Ling, JJ; Wang, Y; Xie, B; Zhou, LL, 2008
)
0.35
"To study pharmacokinetic parameters and absolute bioavailability for oral use of sinomenine tablet in beagle dogs."( [Study on pharmacokinetics and absolute bioavailability of sinomenine in beagle dogs].
Chen, W; Feng, X; Kang, J; Li, Q; Zhou, Y, 2009
)
0.35
" The absolute bioavailability for oral use was (30."( [Study on pharmacokinetics and absolute bioavailability of sinomenine in beagle dogs].
Chen, W; Feng, X; Kang, J; Li, Q; Zhou, Y, 2009
)
0.35
"The absolute bioavailability of sinomenine is low, and the elimination of sinomenine tablet is fast."( [Study on pharmacokinetics and absolute bioavailability of sinomenine in beagle dogs].
Chen, W; Feng, X; Kang, J; Li, Q; Zhou, Y, 2009
)
0.35
" Finally, SN significantly improved the absolute OCT bioavailability in rats and the transport rate in Caco-2 cell monolayers."( A novel perspective and approach to intestinal octreotide absorption: sinomenine-mediated reversible tight junction opening and its molecular mechanism.
Duan, Z; Li, Y; Liu, Z; Tian, Y; Wang, Q, 2013
)
0.39
"The current review emphasizes on the herbal bioenhancers which themselves do not possess inherent pharmacological activity of their own but when co-administered with Active Pharmaceutical Ingredients (API), enhances their bioavailability and efficacy."( Role of herbal bioactives as a potential bioavailability enhancer for Active Pharmaceutical Ingredients.
Alexander, A; Kumari, L; Qureshi, A; Saraf, S; Sharma, M; Vaishnav, P, 2014
)
0.4
" However, the discrepancy between low oral bioavailability and higher minimal effective concentration made its action mode mysterious."( Sinomenine suppresses collagen-induced arthritis by reciprocal modulation of regulatory T cells and Th17 cells in gut-associated lymphoid tissues.
Dai, Y; Dou, Y; Kong, L; Tong, B; Wang, T; Wu, X; Xia, Y; Yu, J, 2015
)
0.42
"99 times higher than that of SH-G, and the relative bioavailability value was 199."( Sinomenine hydrochloride-loaded dissolving microneedles enhanced its absorption in rabbits.
Cao, Y; Chen, L; Chen, Y; Gui, S; Ma, P; Wu, X; Yin, D, 2016
)
0.43
" Food increases the bioavailability of naloxegol, and the relative bioavailability of the tablet formulation was not limited by dissolution."( Clinical Pharmacokinetics and Pharmacodynamics of Naloxegol, a Peripherally Acting µ-Opioid Receptor Antagonist.
Al-Huniti, N; Bui, K; Floettmann, E; Xu, H; Zhou, D, 2017
)
0.46
" Compared with naloxegol commercial tablets, the relative bioavailability of naloxegol using 3 alternative methods of administration was approximately 100%."( An Open-Label, Randomized Bioavailability Study of Alternative Methods of Oral Administration of Naloxegol in Healthy Subjects.
Berger, B; Birmingham, B; Bui, K; Diva, U, 2017
)
0.46
"The use of plant‑based compounds derived from traditional medicine to improve human diseases has been gaining momentum, due to their high bioavailability and moderate adverse effects."( Sinomenine hydrochloride sensitizes cervical cancer cells to ionizing radiation by impairing DNA damage response.
Dong, Y; Han, S; Hegde, ML; Qian, Y; Wang, H; Zhang, D; Zhao, Y; Zhou, C, 2018
)
0.48
"The local bioavailability of SN in joint cavity was improved significantly after conjugated with HA."( Evaluation of pharmacokinetics and pharmaco-dynamics of sinomenine-hyaluronic acid conjugate after intra-articular administration for osteoarthritis treatment.
Chen, J; Cheng, Y; Fang, S; Ling, P; Liu, J; Shao, H, 2019
)
0.51
"The aim of this study was to investigate the release behaviors of sinomenine hydrochloride loaded via in situ hexagonal liquid crystal (ISH), and its potential to improve the local bioavailability in knee joints of sinomenine hydrochloride (SMH) after intra-articular administration."( In situ hexagonal liquid crystal for intra-articular delivery of sinomenine hydrochloride.
Chen, Y; Gui, S; Liang, X; Maharjan, A; Regmi, B; Wu, L; Zhang, J, 2019
)
0.51
" To do so, we prepared a mixture of SIN and exosomes (Exo-SIN) to improve the bioavailability of SIN to treat liver cancer."( A Natural Membrane Vesicle Exosome-based Sinomenine Delivery Platform for Hepatic Carcinoma Therapy.
Li, M; Liang, L; Wang, Y; Yu, X; Yuan, W; Zhao, L, 2021
)
0.62

Dosage Studied

ExcerptRelevanceReference
"The chemistry, pharmacology, uses, side effects, pharmacokinetics and dosage of butorphanol tartrate, a narcotic analgesic with antagonist properties, are reviewed."( Drug therapy reviews: evaluation of butorphanol tartrate.
Ameer, B; Salter, FJ, 1979
)
0.26
" The log dose-response relationship for buprenorphine was curvilinear in mouse and rat tail flick tests with the antinociceptive effect decreasing at higher, non-toxic doses."( Agonist and antagonist properties of buprenorphine, a new antinociceptive agent.
Cowan, A; Lewis, JW; Macfarlane, IR, 1977
)
0.26
" In contrast, the morphine dose-response relationship was linear."( The animal pharmacology of buprenorphine, an oripavine analgesic agent.
Cowan, A; Doxey, JC; Harry, EJ, 1977
)
0.26
" The drug was found to be effective and safe for a wide range of ungulates and pachyderms and Burchell's zebra (Equus burchelli) did not react to expected dosage levels."( Immobilisation of free-ranging wild animals using a new drug.
De Vos, V, 1978
)
0.26
" The study was double-blind, and the drugs were given IM at several dosage levels."( Butorphanol and morphine: a double-blind comparison of their parenteral analgesic activity.
Caruso, FS; Corssen, G; Tavakoli, M,
)
0.13
" There were at least 50 patients in each of the five dosage groups."( Butorphanol and pentazocine in patients with severe postoperative pain.
Caruso, FS; Dobkin, AB; Eamkaow, S, 1975
)
0.25
" In addition, dose-response curves were determined for (+)- and (-)-phenylmorphan using the mouse tail-flick assay with the (+)-enantiomer found to be about 7 times more potent."( Phenylmorphans and analogues: opioid receptor subtype selectivity and effect of conformation on activity.
Froimowitz, M; Pasternak, GW; Pick, CG, 1992
)
0.28
" A dose-response curve was also made for the mu-opioid receptor agonist, morphine."( Spinal antinociception by Tyr-D-Ser(otbu)-Gly-Phe-Leu-Thr, a selective delta-opioid receptor agonist.
Dickenson, AH; Kalso, EA; McQuay, HJ; Sullivan, AF, 1992
)
0.28
" 1) In the presence of a fixed dose of DPDPE (150 nmol), there was a left shift in the dose-response curve of the mu agonist, with the magnitude of the shifts being greater than those anticipated from a simple additive interaction: PL017 (31-fold) > or = DAMGO (20-fold) > morphine (6."( Isobolographic and dose-response analyses of the interaction between intrathecal mu and delta agonists: effects of naltrindole and its benzofuran analog (NTB).
Malmberg, AB; Yaksh, TL, 1992
)
0.28
" The dextrorphan-trained birds generalized to l-cyclorphan at 10 mg/kg; naltrexone did not alter the l-cyclorphan dose-response curve for this effect."( Discriminative stimulus effects of cyclorphan: selective antagonism with naltrexone.
Bertalmio, AJ; Woods, JH, 1992
)
0.28
"3 nmol/rat of DADELT II and shifted the dose-response curve to the right, without decreasing the maximum effect."( Behavioural effects of deltorphins in rats.
Angelucci, F; Negri, L; Noviello, V, 1991
)
0.28
" morphine dose-response line was shown to be displaced progressively to the right with decreasing maximal effect (i."( Modulation of the potency and efficacy of mu-mediated antinociception by delta agonists in the mouse.
Mosberg, HI; Porreca, F; Qi, JN, 1990
)
0.28
" injection of the drug at a dosage rate of 20 micrograms/kg."( Neurochemical changes in the brain and spinal cord of sheep: a basis for the immobilizing action of etorphine.
Kania, BF, 1985
)
0.27
" Physiologic measures and subject- and observer-rated behavioral responses were measured before dosing and for 2 hr after drug administration."( Butorphanol-precipitated withdrawal in opioid-dependent human volunteers.
Bigelow, GE; Liebson, IA; Preston, KL, 1988
)
0.27
"Pharmacokinetic data and analgetic potency of nalbuphine hydrochloride (Nubain) under conditions of postoperative respiratory treatment and repeated dosage was investigated in a multicenter study."( [Cumulative pharmacokinetics and clinical effects of nalbuphine in patients in the postoperative phase. An open multicenter study].
, 1989
)
0.28
" In order to investigate the possible actions of peripheral, endogenous kappa agonists, a dose-response curve was generated in the place conditioning paradigm from separate groups of naive rats injected with various intraperitoneal doses of the specific kappa antagonist Mr2266 (0."( Kappa receptors mediate the peripheral aversive effects of opiates.
Bechara, A; van der Kooy, D, 1987
)
0.27
" Dextrorphan displayed high affinity to PCP receptors and it had weak PCP-like bioactivity, but could antagonize PCP's action dose-dependently in vitro and shift the dose-response curve to the right."( Dextrorphan: an antagonist for phencyclidine receptor.
Sun, FY; Xu, XR; Zhang, AZ; Zhang, LM; Zhu, H, 1986
)
0.27
" Dosage titration increased efficacy to 85."( Butorphanol as a dental premedication in the mentally retarded.
Fidone, G; Gorday, M; Jann, MW; Rostedt, RR, 1987
)
0.27
" The low- and high-dose nalbuphine groups clinically resembled the fentanyl group in terms of dosing frequency and patients' self-ratings of postoperative analgesia."( A comparison of clinical and psychological effects of fentanyl and nalbuphine in ambulatory gynecologic patients.
Earls, F; Garfield, FB; Garfield, JM; Philip, BK; Roaf, E, 1987
)
0.27
" In long-term dosing studies in rodents and primates buprenorphine did not produce the manifestations of physical dependence when treatment was stopped."( Buprenorphine.
Lewis, JW, 1985
)
0.27
" The agonist, bremazocine, bound (in order of decreasing affinity) to the kappa approximately equal to mu greater than delta binding sites, and it's pharmacological effects appeared in the dosage range of kappa and mu binding."( In vivo binding of benzomorphans to mu, delta and kappa opioid receptors: comparison with urine output in the rat.
Richards, ML; Sadée, W, 1985
)
0.27
" Antagonism by competition at the same site(s) is suggested from parallel shifts of the dose-response curves of etorphine or beta-endorphin in the presence of beta-endorphin-(1-27)."( Beta-endorphin-(1-27) is a naturally occurring antagonist to etorphine-induced analgesia.
Li, CH; Nicolas, P, 1985
)
0.27
" Despite high dosage in some cases (up to 200 mg in an hour) no clinically important cardiovascular or respiratory effects were observed."( On-demand nalbuphine for post-operative pain relief.
Kay, B; Krishnan, A, 1986
)
0.27
" It may be assumed, that with partial agonists the relation of agonistic and antagonistic activity may be different, depending on the dosage used and on the respective pharmacologic effect observed during investigation."( [Intra- and postoperative interactions between the 2 opioids fentanyl and buprenorphine].
Börner, U; Gerlach, H; Gips, H; Hempelmann, G; Müller, H; Richter, M, 1986
)
0.27
" The output of urine for a 2 h period after M320, administered subcutaneously to normally hydrated Long Evans rats, showed a bell-shaped dose-response relationship, the maximum effect occurring after 10 micrograms kg-1."( The effects of N-(cyclopropylmethyl)-19-isopentylnororvinol (M320), a potent agonist at kappa- and mu-opiate receptors, on urine excretion of rats.
Abrahams, JM; Boura, AL; Evans, RG; Johnston, CI; Olley, JE, 1986
)
0.27
" It had weak PCP-like bioactivity, but could antagonize PCP's action dose-dependently in vitro study with the rabbit ear artery preparation and shifted the dose-response curve of PCP to the right."( Dextrorphan: an antagonist for phencyclidine receptors.
Sun, FY; Xu, XR; Zhang, AZ; Zhang, LM; Zhu, H, 1987
)
0.27
" A tentative dosage range has been established."( Butorphanol improves CO2 response and ventilation after fentanyl anesthesia.
Bjurstrom, RL; Bowdle, TA; Greichen, SL; Schoene, RB, 1987
)
0.27
" Dose-response curves for diprenorphine and naloxone were determined prior to and following chronic administration of 10."( Diprenorphine and naloxone in squirrel monkeys with enhanced sensitivity to opioid antagonists.
Dykstra, LA; Oliveto, AH, 1988
)
0.27
"5 mg/kg) allowed for a significant reduction in the mean dosage of midazolam required to produce satisfactory sedation when compared with trials where midazolam was used alone."( New intravenous sedative combinations in oral surgery: a comparative study of nalbuphine or pentazocine with midazolam.
Hook, PC; Lavery, KM, 1988
)
0.27
" Both antagonists produced large shifts in the dose-response curves to the mu-agonists, morphine and fentanyl, confirming their mu-antagonist activity."( Reversal by beta-funaltrexamine and 16-methyl cyprenorphine of the antinociceptive effects of opioid agonists in the mouse and guinea-pig.
Birch, PJ; Hayes, AG, 1988
)
0.27
" Our data suggest that young and old subjects attain similar plasma concentrations after single doses; however, longer dosing intervals may be necessary for multiple dosing in the elderly."( Influence of age on the pharmacokinetics of butorphanol.
Higbee, M; Maesner, J; Ramsey, R; Wood, J, 1988
)
0.27
" While butorphanol had a bell-shaped dose-response relationship for elevation of DA metabolites in the striatum, it had no action on DA metabolites in the entorhinal, prefrontal, pyriform and cingulate cortices and in the olfactory tubercle."( Agonist action of the agonist/antagonist analgesic butorphanol on dopamine metabolism in the nucleus accumbens of the rat.
Iyengar, S; Kim, HS; Wood, PL, 1987
)
0.27
" Blood specimens were obtained up to 15 h after dosing for determination of nalbuphine."( The pharmacokinetics of intravenous, intramuscular, and subcutaneous nalbuphine in healthy subjects.
Lee, FH; Lo, MW; Schary, WL; Whitney, CC, 1987
)
0.27
" With increasing dosage of nalbuphine there appeared to be a limit to the extent of respiratory depression."( Respiratory function following nalbuphine and morphine in anaesthetized man.
Klepper, ID; Mapleson, WW; Rosen, M; Vickers, MD, 1986
)
0.27
" The urinary and fecal excretion pattern observed for a human subject following oral dosing of buprenorphine suggests enterohepatic circulation of buprenorphine."( 63Ni electron-capture gas chromatographic assay for buprenorphine and metabolites in human urine and feces.
Cone, EJ; Darwin, WD; Gorodetzky, CW; Yousefnejad, D, 1985
)
0.27
" When the scores derived from the categorized ratings 1 hour after drug dosing (generally the time of peak effect) were analyzed, there was little difference whether a parametric or nonparametric approach was taken."( Reassessment of verbal and visual analog ratings in analgesic studies.
Littman, GS; Schneider, BE; Walker, BR, 1985
)
0.27
" This increase was reversed after the test dosage was doubled from 20 mg to 40 mg nalbuphine."( [Hemodynamic effects of nalbuphine in patients with acute respiratory insufficiency].
Knoch, M; Konder, H; Lennartz, H; von Rechenberg, H, 1986
)
0.27
", oral, and rectal dosing was evaluated in rats and dogs."( Oral and rectal nalbuphine bioavailability: first-pass metabolism in rats and dogs.
Aungst, BJ; Lam, G; Shefter, E,
)
0.13
" Dose-response curves were constructed using the rat tail pressure test for analgesia which indicated a rank order of potency of buprenorphine much greater than morphine greater than butorphanol greater than xorphanol = nalbuphine."( Physical dependence induced by opiate partial agonists in the rat.
Howlett, GJ; McCarthy, PS, 1984
)
0.27
" 2 Buprenorphine revealed a bell-shaped dose-response curve for antinociception peaking at approx."( In vivo receptor binding of the opiate partial agonist, buprenorphine, correlated with its agonistic and antagonistic actions.
Dum, JE; Herz, A, 1981
)
0.26
"Agonist/antagonist (Ag/Ant) analgesics possess bell-shaped dose-response curves with regard to nigrostriatal dopamine (DA) metabolism in the rat."( Agonist/antagonist analgesics and nigrostriatal dopamine metabolism in the rat: evidence for receptor dualism.
McQuade, P; Richard, JW; Thakur, M; Wood, PL, 1983
)
0.27
" At the dosage applied no major respiratory or circulatory effects were observed in the patients."( [Mr 1268--a new furylmethyl-substituted benzomorphan. Comparison of its effects with pentazocine and placebo in a double-blind study].
Behrendt, W; Conrad, H; Richter, M; Veit, G, 1983
)
0.27
", delayed nociceptive reaction on a 55 degrees C hot-plate with a dose-response curve not readily fitting a single straight line; this effect was antagonized by high doses of naloxone."( Bremazocine induces antinociception, but prevents opioid-induced constipation and catatonia in rats and precipitates withdrawal in morphine-dependent rats.
Gambino, MC; Petrillo, P; Tavani, A, 1984
)
0.27
", dose-response curves were shifted to the right) but failed to block the effects of diprenorphine."( Effects of naloxone, diprenorphine, buprenorphine and etorphine on unpunished and punished food-reinforced responding in the squirrel monkey.
DeRossett, SE; Holtzman, SG, 1984
)
0.27
" The increasing morphine dosage was associated with progressive rightward displacements and ultimately decreases in the slope of the CO2 response curves."( Analgesic and respiratory depressant activity of nalbuphine: a comparison with morphine.
DiFazio, CA; Gal, TJ; Moscicki, J, 1982
)
0.26
" Buprenorphine showed a bell-shaped dose-response curve in the mouse D'Amour-Smith's test at high stimulus intensity."( [Analgesic and narcotic antagonist effects of buprenorphine (author's transl)].
Hiyama, T; Shintani, S; Tsutsui, M; Yasuda, Y, 1982
)
0.26
" after 30 min pretreatment produced a significant and parallel shift in OTMN's analgesic dose-response line, assessed by the hot plate test (55 degrees C)."( Some observations on the effects of enantiomers of two benzomorphan narcotic antagonists and atropine on analgesia, tremor and hypothermia produced by oxotremorine.
Ben-Sreti, MM; Sewell, RD; Upton, N, 1982
)
0.26
" The dose-response curves for both were shifted to the right in non-parallel fashion with decreased slopes and antidiuretic efficacies."( Cross tolerance to etorphine in rats tolerant to morphine-induced antidiuresis.
Fuhrman-Lane, C; Fujimoto, JM; Tseng, LF, 1982
)
0.26
" Buprenorphine showed naloxone-sensitive effects with a bell-shaped dose-response curve in the thermal test but dose-dependent activity in the pressure test."( Involvement of the median raphe nucleus in antinociception induced by morphine, buprenorphine and tilidine in the rat.
Bryant, RM; Olley, JE; Tyers, MB, 1982
)
0.26
" The patterns of analgesia were similar and without indication of increasing dosage requirements with time."( The study of analgesics following single and repeated doses.
Johnson, RP; Robinson, N; Waite, E; Wang, RI,
)
0.13
" Comparison of areas under the plasma concentration versus time curves to 24 hours after dosing showed the mean bioavailability of buprenorphine from the intramuscular doses was 70% of that from the reference intravenous doses."( Plasma concentration and disposition of buprenorphine after intravenous and intramuscular doses to baboons.
Biggs, SR; Henson, R; Lloyd-Jones, JG; Robinson, P; Taylor, T, 1980
)
0.26
" After intramuscular administration of [3H]buprenorphine to rats, dogs, rhesus monkeys and one human volunteer, most of the dosed radioactivity was excreted in the faeces, indicating biliary excretion and a possible enterohepatic circulation of the drug in these species."( Biliary excretion, metabolism and enterohepatic circulation of buprenorphine.
Brewster, D; Humphrey, MJ; McLeavy, MA, 1981
)
0.26
" Reports of high intrabiliary pressures and bizarre cholangiograms for patients under such anesthesia led us to investigate the specific effects on intrabiliary pressure of morphine sulfate, fentanyl and butorphanol tartrate, each at two different dosage levels."( Effects of butorphanol, fentanyl and morphine on the intrabiliary pressure of guinea pigs.
Aldrete, JA; Franatovic, Y; Romo-Salas, F, 1980
)
0.26
" At higher dosage levels respiratory rate was reduced to 2/minute."( Immobilization of coastal grizzly bears with etorphine hydrochloride.
Herbert, DM; Lay, DW; Turnbull, WG, 1980
)
0.26
" Once rats had acquired the discrimination an ethanol dose-response test was conducted."( The influence of opioid antagonists on the discriminative stimulus effects of ethanol.
Spanagel, R, 1996
)
0.29
"1 after titration with IR oxycodone dosed qid."( Double-blind, randomized comparison of the analgesic and pharmacokinetic profiles of controlled- and immediate-release oral oxycodone in cancer pain patients.
Davis, M; Reder, RF; Stambaugh, H; Stambaugh, JE; Stambaugh, MD, 2001
)
0.31
"Morphine-dependent rats were induced by injecting morphine on dosage increasing by degrees, then treated with medication."( [Effect of sinamine on withdrawal symptom and neurotransmitter of morphine-dependent rats].
Mo, Z; Wang, C; Wen, L; Zhu, Q, 2002
)
0.31
"For exploring the mechanism of the anti-inflammatory and anti-rheumatic effect of sinomenine (SN), the actions of different dosage of SN were observed in vitro on the expression of cytokines, tumor necrosis factor (TNF-alpha) and interleukin-1beta (IL-1beta), as well as the activity of nuclear factor-kappaB (NF-kappaB) and the inhibitory kappaB-alpha (IkappaB-alpha) protein level of peritoneal macrophages (PMs) and synoviocytes in adjuvant arthritis (AA) rats."( Effect of sinomenine on cytokine expression of macrophages and synoviocytes in adjuvant arthritis rats.
Fang, Y; Huang, W; Peng, D; Wang, M; Wang, Y; Zhong, B; Zhou, X, 2005
)
0.33
" The results demonstrated that oral administration with a single dosage at a rate of 90 mg sinomenine/kg in rats achieved about 80% bioavailability, while most of the other pharmacokinetic parameters were similar to the data from the animals treated intravenously."( The pharmacokinetics and tissue distribution of sinomenine in rats and its protein binding ability in vitro.
Chan, K; Jiang, ZH; Liu, L; Liu, ZQ; Wong, YF; Xu, HX; Zhou, H, 2005
)
0.33
"To investigate the effect of release behavior of sustained-release dosage forms of sinomenine hydrochloride (SM."( Impact of release characteristics of sinomenine hydrochloride dosage forms on its pharmacokinetics in beagle dogs.
Gao, K; He, ZG; Li, B; Mao, JJ; Shi, JM; Sun, J; Sun, YH; Zhang, TH, 2005
)
0.33
"HCl dosage forms, including commercial 12-h sustained-release tablets and 24-h sustained-release pellets prepared in our laboratory, was examined."( Impact of release characteristics of sinomenine hydrochloride dosage forms on its pharmacokinetics in beagle dogs.
Gao, K; He, ZG; Li, B; Mao, JJ; Shi, JM; Sun, J; Sun, YH; Zhang, TH, 2005
)
0.33
"HCl dosage forms was comparable and both preparations were statistically bioequivalent."( Impact of release characteristics of sinomenine hydrochloride dosage forms on its pharmacokinetics in beagle dogs.
Gao, K; He, ZG; Li, B; Mao, JJ; Shi, JM; Sun, J; Sun, YH; Zhang, TH, 2005
)
0.33
"The in vitro release properties of the dosage forms strongly affect their pharmacokinetic behavior in vivo."( Impact of release characteristics of sinomenine hydrochloride dosage forms on its pharmacokinetics in beagle dogs.
Gao, K; He, ZG; Li, B; Mao, JJ; Shi, JM; Sun, J; Sun, YH; Zhang, TH, 2005
)
0.33
" In vivo MCL-145 produced a full dose-response curve in the 55 degrees C warm water tail-flick test and was equipotent to morphine."( Characterization of a novel bivalent morphinan possessing kappa agonist and micro agonist/antagonist properties.
Bidlack, JM; Mathews, JL; Negus, SS; Neumeyer, JL; Peng, X; Xiong, W; Zhang, A, 2005
)
0.33
" The morphine-dependent model mice were established by injection on dosage increasing by degrees."( [Study on the detoxification of alcohol extracts from orientvine and its effective component on withdrawal syndromes of morphine].
Mo, ZX; Wang, CY; Zhang, GM, 2009
)
0.35
" There was a poor correlation between concentrations of both oxycodone and noroxycodone in plasma and saliva over a range of times following dosing (r (2) = 0."( Is saliva a valid substitute for plasma in pharmacokinetic studies of oxycodone and its metabolites in patients with cancer?
Anderson, H; Charles, B; Hardy, J; Norris, R; O'Shea, A, 2012
)
0.38
" The expression of COX-2 and VEGF protein in HepG2 cells treated with anti-TfR mAb alone was increased in line with increasing dosage of the agent."( Sinomenine hydrochloride enhancement of the inhibitory effects of anti-transferrin receptor antibody-dependent on the COX-2 pathway in human hepatoma cells.
Bian, J; Hong, Y; Hu, H; Lei, P; Shen, G; Shen, X; Sun, X; Tao, J; Wen, X; Yang, J; Yuan, L; Zhu, H, 2013
)
0.39
" Digital 12-lead ECGs were recorded at baseline and at 10 time points over 24 hours after dosing in each treatment period."( Evaluation of the effect of Naloxegol on cardiac repolarization: a randomized, placebo- and positive-controlled crossover thorough QT/QTc study in healthy volunteers.
Carlson, G; Gottfridsson, C; Lappalainen, J; Sostek, M, 2013
)
0.39
" Similar findings were observed using QTcB; the upper limits of the 2-sided 90% CI were <10 msec at all time points after dosing with naloxegol 25 or 150 mg."( Evaluation of the effect of Naloxegol on cardiac repolarization: a randomized, placebo- and positive-controlled crossover thorough QT/QTc study in healthy volunteers.
Carlson, G; Gottfridsson, C; Lappalainen, J; Sostek, M, 2013
)
0.39
" Plasma concentration of oxycodone and its metabolites were measured up to 8 hours after administration as follows: on day 1, CR oxycodone was administered alone; on day 2, CR oxycodone was administered with aprepitant (125 mg, at the same time of oxycodone dosing in the morning)."( Effects of aprepitant on the pharmacokinetics of controlled-release oral oxycodone in cancer patients.
Chayahara, N; Fujiwara, Y; Imamura, Y; Kiyota, N; Minami, H; Mukohara, T; Shimada, T; Toyoda, M, 2014
)
0.4
" We demonstrated that cytochrome P450 2D6*10 (100C > T, rs1065852) polymorphism can affect the pharmacokinetics of dimemorfan in humans, not dosage forms."( Cytochrome P450 2D6*10 genotype affects the pharmacokinetics of dimemorfan in healthy Chinese subjects.
Liu, L; Liu, S; Pei, Q; Peng, J; Tan, H; Yang, G; Yang, L; Yang, X; Yuan, H, 2015
)
0.42
" In summary, the PBPK models reasonably estimated interactions with various CYP3A modulators and can be used to guide dosing in clinical practice when naloxegol is coadministered with such agents."( Simulation and Prediction of the Drug-Drug Interaction Potential of Naloxegol by Physiologically Based Pharmacokinetic Modeling.
Al-Huniti, N; Bui, K; Sostek, M; Zhou, D, 2016
)
0.43
" In order to characterize the protocol-defined naloxegol responder rate, the number of daily spontaneous bowel movements (SBMs) was characterized by a longitudinal ordinal nonlinear mixed-effects logistic regression dose-response model, and the incidence of diary entry discontinuation was described by a time-to-event model."( Population Exposure-Response Modeling of Naloxegol in Patients With Noncancer-Related Pain and Opioid-Induced Constipation.
Al-Huniti, N; Cantagallo, K; Hutmacher, MM; Lappalainen, J; Nielsen, JC; Sostek, M, 2016
)
0.43
" However, there are some disadvantages, including low activity in transdermal permeation and a high dosage being clinically required."( Transdermal Permeation and Anti-Inflammation Activities of Novel Sinomenine Derivatives.
Wang, JC; Xiao, J; Zhao, C; Zhao, ZJ, 2016
)
0.43
" Modeling and simulation of naloxegol efficacy and tolerability informed selection of doses for phase III studies and provided comprehensive dosage recommendations for the naloxegol US package insert."( Pharmacometric Modeling of Naloxegol Efficacy and Safety: Impact on Dose and Label.
Aksenov, S; Al-Huniti, N; Bui, KH; Fox, R; Helmlinger, G; Stanski, D; Xu, H; Zhou, D, 2017
)
0.46
" In the rat, but not the mouse, 2-year carcinogenicity study a change in tumour pattern with an increase in testicular Leydig cell tumours (LCT) was observed after dosing at high (supra-pharmacological) concentrations."( Naloxegol, an opioid antagonist with reduced CNS penetration: Mode-of-action and human relevance for rat testicular tumours.
Andersson, H; Floettmann, E; Johnson, N; Mitchard, T, 2017
)
0.46
" In a drug control group, piglets were dosed IP with vehicle and 3 h late IM with 10 mg/kg sinomenine while those in an LPS control group were challenged with 1 mg LPS/kg (IP) and then vehicle 3 h later; naïve control piglets were administered normal saline IP and then IM only."( Protective effects of sinomenine against LPS-induced inflammation in piglets.
Chen, X; He, K; Hu, Y; Jiang, C; Yang, H, 2017
)
0.46
" The weekly probability of response defined as having ≥3/week spontaneous bowel movements (SBMs) and ≥1 SBM/week increase over baseline was characterized by a longitudinal mixed-effects logistic regression dose-response model, and the probability of time to discontinuation was modeled with a Weibull distribution function."( Population Exposure-Response Modeling Supported Selection of Naloxegol Doses in Phase III Studies in Patients With Opioid-Induced Constipation.
Aksenov, S; Al-Huniti, N; Bui, KH; Fox, R; Xu, H; Zhou, D, 2017
)
0.46
" Here, we consider the integration of both efficacy and dose-response estimation accuracy into the go/no-go decision process, using a model-based approach."( Integrating dose estimation into a decision-making framework for model-based drug development.
Al-Huniti, N; Dunyak, J; Hamrén, B; Helmlinger, G; Matcham, J; Mitchell, P; Stanski, D, 2018
)
0.48
"Haemodialysis performed 6-10 h after dosing removed ∼10% of the administered dose of oxycodone predominantly as unconjugated oxycodone and noroxycodone or conjugated oxymorphone and noroxymorphone."( Pharmacokinetics of oxycodone/naloxone and its metabolites in patients with end-stage renal disease during and between haemodialysis sessions.
Amico, P; Dickenmann, M; Duthaler, U; Hammann, F; Haschke, M; Jehle, AW; Kalbermatter, S; Krähenbühl, S; Lenherr, C; Leuppi-Taegtmeyer, A; Liechti, ME; Meyer Zu Schwabedissen, HE; Schmid, Y, 2019
)
0.51
" Adults with moderate-to-severe CLBP refractory to nonopioid analgesics achieving an analgesic NKTR-181 dosage (100-400 mg twice daily) during the open-label titration period were randomized to continued NKTR-181 treatment, double-blind, or switched to placebo."( SUMMIT-07: a randomized trial of NKTR-181, a new molecular entity, full mu-opioid receptor agonist for chronic low-back pain.
Agaiby, E; Argoff, C; Doberstein, SK; Gimbel, J; Gudin, J; Hale, M; Katz, N; Lu, L; Markman, J; Rauck, R; Rowbotham, M; Siddhanti, S; Tagliaferri, M, 2019
)
0.51
"3 and 1 mg/kg) reduced cocaine-primed reinstatement of drug-seeking behavior and caused significant downward shift of the dose-response curve in cocaine self-administration tests (0."( MP1104, a mixed kappa-delta opioid receptor agonist has anti-cocaine properties with reduced side-effects in rats.
Atigari, DV; Kivell, BM; Majumdar, S; Pasternak, GW; Uprety, R, 2019
)
0.51
" Current treatment involves intravenous administration of anti-inflammatory drugs which have limited clinical outcomes only when dosed within the early time window after injury."( Dendrimer mediated targeted delivery of sinomenine for the treatment of acute neuroinflammation in traumatic brain injury.
Chen, S; Duh, EI; Kambhampati, SP; Kannan, RM; Kannan, S; Sharma, A; Sharma, R; Tso, MOM; Zhang, Z, 2020
)
0.56
" The two compounds were characterised by an inverted U-shaped dose-response curve, and their effects were blocked by the co-administration of the antagonist MCL-117, which alone had no effect."( Behavioural and pharmacological profiles of zebrafish administrated pyrrolidinyl benzodioxanes and prolinol aryl ethers with high affinity for heteromeric nicotinic acetylcholine receptors.
Appiani, R; Bavo, F; Bolchi, C; Braida, D; Gotti, C; Moretti, M; Pallavicini, M; Ponzoni, L; Sala, M; Viani, P, 2020
)
0.56
" At inclusion, the median opioid dosage was 60 mg of oral morphine or equivalent."( Effectiveness of naloxegol in patients with cancer pain suffering from opioid-induced constipation.
Braniste, V; Lemaire, A; Narciso, B; Piloquet, FX; Pointreau, Y; Sabaté, JM, 2021
)
0.62
"Sinomenine (SIN) is an effective anti-inflammatory agent, but its therapeutic efficacy is limited by its short half-life and the high dosage required."( Novel synovial targeting peptide-sinomenine conjugates as a potential strategy for the treatment of rheumatoid arthritis.
Chang, L; Gou, S; Li, B; Liu, H; Ni, J; Ouyang, X; Yan, N; Zhang, F; Zhang, T; Zhang, Y, 2022
)
0.72
"The work aims to explore the feasibility of Raman mapping in predicting the dissolution profiles of solid oral dosage form."( Dissolution profiles prediction of sinomenine hydrochloride sustained-release tablets using Raman mapping technique.
Fang, G; Hu, Y; Li, W; Li, Z; Liu, H; Wang, L; Wu, S; Zeng, Q, 2022
)
0.72
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
morphinane alkaloidAn isoquinoline alkaloid based on a morphinan skeleton and its substituted derivatives.
isoquinoline alkaloid fundamental parent
[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]

Research

Studies (3,099)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901868 (60.28)18.7374
1990's237 (7.65)18.2507
2000's310 (10.00)29.6817
2010's513 (16.55)24.3611
2020's171 (5.52)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 34.69

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index34.69 (24.57)
Research Supply Index8.18 (2.92)
Research Growth Index4.64 (4.65)
Search Engine Demand Index56.46 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (34.69)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials307 (9.44%)5.53%
Reviews138 (4.24%)6.00%
Case Studies61 (1.88%)4.05%
Observational0 (0.00%)0.25%
Other2,745 (84.44%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]