rapacuronium: 16-N-allyl-17-beta-propionate analog of vecuronium; structure given in first source
ID Source | ID |
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PubMed CID | 5311399 |
CHEMBL ID | 1201352 |
CHEBI ID | 135845 |
SCHEMBL ID | 16977930 |
MeSH ID | M0366636 |
Synonym |
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rapacuronium |
DB04834 |
CHEBI:135845 |
[(2s,3s,5s,8r,9s,10s,13s,14s,16s,17r)-3-acetyloxy-10,13-dimethyl-2-piperidin-1-yl-16-(1-prop-2-enylpiperidin-1-ium-1-yl)-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-17-yl] propanoate |
CHEMBL1201352 |
rapacuronium ion |
rapacuronium [vandf] |
1-allyl-1-(3.alpha.,17.beta.-dihydroxy-2.beta.-piperidino-5.alpha.-androstan-16.beta.-yl)piperidinium, 3-acetate 17-propionate |
androstane-3,17-diol, 2-(1-piperidinyl)-16-(1-(2-propenyl)-1-piperidiniumyl)-, 3-acetate 17-propanoate, (2.beta.,3.alpha.,5.alpha.,16.beta.,17.beta.)- |
rapacuronium cation |
465499-11-0 |
gg1lbm463s , |
unii-gg1lbm463s |
SCHEMBL16977930 |
DTXSID80861419 |
Rapacuronium is an aminosteroidal nondepolarising neuromuscular blocking agent. It is a rapid-onset and short- to intermediate-acting muscle relaxant.
Rapacuronium has an active metabolite that is at least as potent as the parent compound. It has a mild to moderate effect on heart rate and arterial blood pressure in ASA physical status I and II patients.
Rapacuronium has a rapid onset, and a bolus dose has a short duration of action. It has a mild to moderate effect on heart rate and arterial blood pressure in ASA physical status I and II patients.
Excerpt | Reference | Relevance |
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"Rapacuronium has an active metabolite that is at least as potent as the parent compound and is eliminated much less efficiently." | ( Pharmacokinetics and pharmacodynamics of rapacuronium bromide. Wight, WJ; Wright, PM, 2002) | 1.3 |
"Rapacuronium has a rapid onset, and a bolus dose has a short duration of action." | ( Clinical pharmacokinetics of the newer neuromuscular blocking drugs. Atherton, DP; Hunter, JM, 1999) | 1.02 |
"Rapacuronium has an onset profile that is not different from that previously reported for succinylcholine." | ( Dose-response and onset/offset characteristics of rapacuronium. Flores, F; Ghori, K; Klewicka, MM; Kopman, AF; Neuman, GG, 2000) | 1.28 |
"Rapacuronium has a mild to moderate effect on heart rate and arterial blood pressure in ASA physical status I and II patients." | ( The hemodynamic effects of rapacuronium in patients with coronary artery disease: succinylcholine and vecuronium compared. Delboy, NJ; Shields, JA; Tomichek, RC, 2002) | 1.33 |
"Rapacuronium has an active metabolite that is at least as potent as the parent compound and is eliminated much less efficiently." | ( Pharmacokinetics and pharmacodynamics of rapacuronium bromide. Wight, WJ; Wright, PM, 2002) | 1.3 |
"Rapacuronium has a rapid onset, and a bolus dose has a short duration of action." | ( Clinical pharmacokinetics of the newer neuromuscular blocking drugs. Atherton, DP; Hunter, JM, 1999) | 1.02 |
"Rapacuronium has an onset profile that is not different from that previously reported for succinylcholine." | ( Dose-response and onset/offset characteristics of rapacuronium. Flores, F; Ghori, K; Klewicka, MM; Kopman, AF; Neuman, GG, 2000) | 1.28 |
"Rapacuronium has been accepted wherever rapid onset and short duration of action are advantageous." | ( Rapacuronium: first experience in clinical practice. Bartkowski, RR; Witkowski, TA, 2001) | 2.47 |
"Rapacuronium has a mild to moderate effect on heart rate and arterial blood pressure in ASA physical status I and II patients." | ( The hemodynamic effects of rapacuronium in patients with coronary artery disease: succinylcholine and vecuronium compared. Delboy, NJ; Shields, JA; Tomichek, RC, 2002) | 1.33 |
Rapacuronium is a muscle relaxant with rapid onset and offset. The time course of a single bolus dose of 1.5 mg can be explained from its pharmacokinetic and pharmacodynamic characteristics.
Excerpt | Reference | Relevance |
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" Terminal half-life and mean residence time were 71." | ( Pharmacodynamics and pharmacokinetics of an infusion of Org 9487, a new short-acting steroidal neuromuscular blocking agent. Proost, JH; Smeulers, NJ; van den Broek, L; Wierda, JM, 1994) | 0.29 |
" To determine whether similar differences exist for rapacuronium, a muscle relaxant with rapid onset and offset, the authors determined its pharmacodynamic characteristics." | ( A pharmacodynamic explanation for the rapid onset/offset of rapacuronium bromide. Brown, R; Fisher, DM; Lau, M; Wright, PM, 1999) | 0.8 |
" A semiparametric effect compartment pharmacodynamic model was fit to values for rapacuronium plasma concentrations and twitch tension of the adductor pollicis and laryngeal adductors." | ( A pharmacodynamic explanation for the rapid onset/offset of rapacuronium bromide. Brown, R; Fisher, DM; Lau, M; Wright, PM, 1999) | 0.77 |
" Pharmacokinetic parameters were determined using mixed-effects modeling." | ( Influence of renal failure on the pharmacokinetics and neuromuscular effects of a single dose of rapacuronium bromide. Brown, R; Caldwell, JE; Fisher, DM; Lau, M; Luks, AM; Szenohradszky, J; Wright, PM, 1999) | 0.52 |
" In this study, the pharmacokinetic behavior (n = 7) of this metabolite and the pharmacokinetic/pharmacodynamic (PK/PD) relationship of rapacuronium (n = 10) and Org 9488 (n = 7) were investigated in humans." | ( Pharmacokinetics and pharmacokinetic-dynamic relationship between rapacuronium (Org 9487) and its 3-desacetyl metabolite (Org 9488). Proost, JH; Schiere, S; Schuringa, M; Wierda, JM, 1999) | 0.74 |
" As part of a study to determine its neuromuscular effects, the authors sampled plasma sparsely to determine the influence of age, gender, and other covariates on its pharmacokinetic characteristics." | ( Factors affecting the pharmacokinetic characteristics of rapacuronium. Angst, MS; Bevan, D; Bikhazi, G; Fisher, DM; Fragen, RJ; Kahwaji, R; Matteo, RS; Ornstein, E, 1999) | 0.55 |
" Pharmacokinetic analysis was performed using a population approach (mixed-effects modeling) to determine the influence of demographic characteristics and preoperative laboratory values on the pharmacokinetic parameters." | ( Factors affecting the pharmacokinetic characteristics of rapacuronium. Angst, MS; Bevan, D; Bikhazi, G; Fisher, DM; Fragen, RJ; Kahwaji, R; Matteo, RS; Ornstein, E, 1999) | 0.55 |
" Rapacuronium's weight-normalized pharmacokinetic parameters were not influenced by age, gender, or other covariates examined." | ( Factors affecting the pharmacokinetic characteristics of rapacuronium. Angst, MS; Bevan, D; Bikhazi, G; Fisher, DM; Fragen, RJ; Kahwaji, R; Matteo, RS; Ornstein, E, 1999) | 1.46 |
" This finding contrasts to an age-related decrease in plasma clearance observed in a study of 10 healthy volunteers and in a pooled analysis of the pharmacokinetic data from 206 adults in multiple clinical studies." | ( Factors affecting the pharmacokinetic characteristics of rapacuronium. Angst, MS; Bevan, D; Bikhazi, G; Fisher, DM; Fragen, RJ; Kahwaji, R; Matteo, RS; Ornstein, E, 1999) | 0.55 |
" Pipecuronium resembles pancuronium in its pharmacokinetic and neuromuscular blocking profile, but is devoid of cardiovascular effects." | ( Clinical pharmacokinetics of the newer neuromuscular blocking drugs. Atherton, DP; Hunter, JM, 1999) | 0.3 |
" The elimination half-life was 88 (77-102) min in controls and 90 (76-117) min in patients with cirrhosis." | ( Pharmacokinetics and pharmacodynamics of rapacuronium in patients with cirrhosis. Duvaldestin, P; Rebufat, Y; Slavov, V, 1999) | 0.57 |
" A three-compartment pharmacokinetic model was justified." | ( Antagonism of rapacuronium using edrophonium or neostigmine: pharmacodynamics and pharmacokinetics. Danjoux, G; Hing, JP; Hunter, JM; Mills, KG; Pollard, BJ; Scott, JM; Wright, PM, 1999) | 0.66 |
" In the current study, the authors determined its pharmacokinetic characteristics in children." | ( Pharmacokinetics of rapacuronium in infants and children with intravenous and intramuscular administration. Brown, R; Fisher, DM; Hsu, J; Infosino, A; Reynolds, LM, 2000) | 0.63 |
" A mixed-effects population pharmacokinetic analysis was applied to these values to determine bioavailability, absorption rate constant, and time to peak plasma concentration with intramuscular administration." | ( Pharmacokinetics of rapacuronium in infants and children with intravenous and intramuscular administration. Brown, R; Fisher, DM; Hsu, J; Infosino, A; Reynolds, LM, 2000) | 0.63 |
" Rapacuronium's pharmacokinetic parameters were determined using mixed-effects modeling." | ( Effect of renal failure and cirrhosis on the pharmacokinetics and neuromuscular effects of rapacuronium administered by bolus followed by infusion. Abengochea, A; Atherton, DP; Brown, R; Dempsey, GA; Fisher, DM; Hunter, JM, 2000) | 1.44 |
"The rapid onset and offset of rapacuronium can be explained from its pharmacokinetic and pharmacodynamic characteristics." | ( A pharmacokinetic-dynamic explanation of the rapid onset-offset of rapacuronium. Proost, JH; Wright, PM, 2001) | 0.84 |
" Pharmacokinetic parameters do not appear to differ markedly in hepatic insufficiency, but clearance is reduced by approximately 30% in renal failure." | ( Pharmacokinetics and pharmacodynamics of rapacuronium bromide. Wight, WJ; Wright, PM, 2002) | 0.58 |
"To test the suitability of an Iterative Two-Stage Bayesian (ITSB) technique for population pharmacokinetic analysis of rich data sets, and to compare ITSB with Standard Two-Stage (STS) analysis and nonlinear Mixed Effect Modeling (MEM)." | ( Performance of an iterative two-stage bayesian technique for population pharmacokinetic analysis of rich data sets. Eleveld, DJ; Proost, JH, 2006) | 0.33 |
"ITSB is a suitable technique for population pharmacokinetic analysis of rich data sets, and in the presented data set it is superior to STS and MEM." | ( Performance of an iterative two-stage bayesian technique for population pharmacokinetic analysis of rich data sets. Eleveld, DJ; Proost, JH, 2006) | 0.33 |
Excerpt | Reference | Relevance |
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" A mixed-effects population pharmacokinetic analysis was applied to these values to determine bioavailability, absorption rate constant, and time to peak plasma concentration with intramuscular administration." | ( Pharmacokinetics of rapacuronium in infants and children with intravenous and intramuscular administration. Brown, R; Fisher, DM; Hsu, J; Infosino, A; Reynolds, LM, 2000) | 0.63 |
" Intramuscular bioavailability averaged 56%." | ( Pharmacokinetics of rapacuronium in infants and children with intravenous and intramuscular administration. Brown, R; Fisher, DM; Hsu, J; Infosino, A; Reynolds, LM, 2000) | 0.63 |
" After intramuscular administration, bioavailability is 56%, and plasma rapacuronium concentrations peak within 4 or 5 min." | ( Pharmacokinetics of rapacuronium in infants and children with intravenous and intramuscular administration. Brown, R; Fisher, DM; Hsu, J; Infosino, A; Reynolds, LM, 2000) | 0.86 |
We analysed raw data for succinylcholine, rocuronium, rapacuronium, and cisatracurium from previously published studies using both LRA and NLR. We determined the ED(50) and ED(95) values and the respective slopes of the dose-response relationships.
Excerpt | Relevance | Reference |
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" However, the decreased clearance of rapacuronium and its potent metabolite in renal failure suggests that repeated dosing of rapacuronium may lead to prolonged effects in patients with renal failure." | ( Influence of renal failure on the pharmacokinetics and neuromuscular effects of a single dose of rapacuronium bromide. Brown, R; Caldwell, JE; Fisher, DM; Lau, M; Luks, AM; Szenohradszky, J; Wright, PM, 1999) | 0.79 |
"A rigorous study of the dose-response relation of rapacuronium has, to our knowledge, yet to be performed." | ( Dose-response and onset/offset characteristics of rapacuronium. Flores, F; Ghori, K; Klewicka, MM; Kopman, AF; Neuman, GG, 2000) | 0.81 |
" By dosing to maintain target twitch depression, recovery was not prolonged." | ( Effect of renal failure and cirrhosis on the pharmacokinetics and neuromuscular effects of rapacuronium administered by bolus followed by infusion. Abengochea, A; Atherton, DP; Brown, R; Dempsey, GA; Fisher, DM; Hunter, JM, 2000) | 0.53 |
" Some statisticians now consider this approach outmoded and assert that non-linear regression (NLR) is the preferred way to analyse sigmoidal dose-response relationships." | ( Determining the potency of neuromuscular blockers: are traditional methods flawed? Kopman, AF; Lien, CA; Naguib, M, 2010) | 0.36 |
"We analysed raw data for succinylcholine, rocuronium, rapacuronium, and cisatracurium from previously published studies using both LRA and NLR to determine the ED(50) and ED(95) values and the respective slopes of the dose-response relationships." | ( Determining the potency of neuromuscular blockers: are traditional methods flawed? Kopman, AF; Lien, CA; Naguib, M, 2010) | 0.61 |
Class | Description |
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steroid ester | |
[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] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 36 (32.73) | 18.2507 |
2000's | 70 (63.64) | 29.6817 |
2010's | 2 (1.82) | 24.3611 |
2020's | 2 (1.82) | 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 moderate demand-to-supply ratio for research on this compound.
| This Compound (28.99) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 40 (36.04%) | 5.53% |
Reviews | 16 (14.41%) | 6.00% |
Case Studies | 10 (9.01%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 45 (40.54%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |