Disease relevance of 3-[(1R,2R)-6,7-dimethoxy-2-methyl-1-veratryl-3,4-dihydro-1H-isoquinolin-2-yl]propanoic acid 5-[3-[(1R,2R)-6,7-dimethoxy-2-methyl-1-veratryl-3,4-dihydro-1H-isoquinolin-2-yl]propanoyloxy]pentyl ester

• Following a 5- to 10-sec intravenous bolus dose of cisatracurium besilate to healthy young adult surgical patients, elderly patients and patients with renal or hepatic failure, the concentration versus time profile of cisatracurium besilate is best characterised by a 2-compartment model [1].
• Anaphylactic reaction after cisatracurium [2].
• A comparison of cisatracurium (51W89) and atracurium by infusion in critically ill patients [3].
• CONCLUSION: The authors conclude that cisatracurium is equipotent in infants and children when dose is referenced to body weight during balanced anesthesia [4].
• One patient who received cisatracurium exhibited intermittent bronchospasm during and after the study period [3].

High impact information on 3-[(1R,2R)-6,7-dimethoxy-2-methyl-1-veratryl-3,4-dihydro-1H-isoquinolin-2-yl]propanoic acid 5-[3-[(1R,2R)-6,7-dimethoxy-2-methyl-1-veratryl-3,4-dihydro-1H-isoquinolin-2-yl]propanoyloxy]pentyl ester

• The in vitro degradation of cisatracurium, the R, cis-R'-isomer of atracurium, in human and rat plasma [5].
• The rapid hydrolysis of cisatracurium by rat plasma relative to human indicates a major species difference in plasma esterase(s) [5].
• Cisatracurium and the degradation products, laudanosine and the monoquaternary alcohol, were quantitated by HPLC with use of fluorescence detection [5].
• Evidence for esterase involvement at this step in the degradation of cisatracurium was based on inhibition studies with O-cresyl benzodioxaphosphorin oxide (CBDP), a specific carboxylesterase inhibitor [5].
• Clinical pharmacokinetics of cisatracurium besilate [1].

Chemical compound and disease context of 3-[(1R,2R)-6,7-dimethoxy-2-methyl-1-veratryl-3,4-dihydro-1H-isoquinolin-2-yl]propanoic acid 5-[3-[(1R,2R)-6,7-dimethoxy-2-methyl-1-veratryl-3,4-dihydro-1H-isoquinolin-2-yl]propanoyloxy]pentyl ester

• RESULTS: The population PK/PD model for cisatracurium revealed that anesthesia type, gender, age, creatinine clearance, and presence of obesity were associated with statistically significant (p < 0.01) effects on the PK/PD parameters of cisatracurium [6].
• Refractory spasms and hiccups resolved with fentanyl and cisatracurium therapy [7].
• PURPOSE: To compare recovery parameters of total intravenous anesthesia (TIVA) with remifentanil and propofol, hemodynamic responses to perioperative events, and pharmacodynamic parameters of cisatracurium in 22 end-stage renal failure and 22 normal renal function patients [8].
• Through increased serum eosinophil cationic protein, tryptase and histamine levels and IgE levels specific to cisatracurium, we demonstrated an IgE-mediated anaphylactic reaction to cisatracurium in the child's first exposure to this new neuromuscular blocking agent [9].
• Persistent anaphylactic reaction after induction with thiopentone and cisatracurium [9].

Biological context of 3-[(1R,2R)-6,7-dimethoxy-2-methyl-1-veratryl-3,4-dihydro-1H-isoquinolin-2-yl]propanoic acid 5-[3-[(1R,2R)-6,7-dimethoxy-2-methyl-1-veratryl-3,4-dihydro-1H-isoquinolin-2-yl]propanoyloxy]pentyl ester

• METHODS: Twenty-three patients aged younger than 2 yr were randomly assigned to receive either cisatracurium or vecuronium infusions postoperatively in a double-blinded fashion after undergoing congenital heart surgery [10].
• BACKGROUND: The comparative clinical pharmacology of cisatracurium and rocuronium and their combinations has not been reported [11].
• MEASUREMENTS AND RESULTS: Patients were randomly selected to receive infusions of opioid sedation during the first session (session 1) and the same sedation with muscle relaxation (cisatracurium) during the second session (session 2) [12].
• Changes in blood pressure and heart rate after the administration of cisatracurium were negligible in both age groups [13].
• These effects were ascribed to oxidative stress elicited by acrylate esters formed during cisatracurium breakdown [14].

Anatomical context of 3-[(1R,2R)-6,7-dimethoxy-2-methyl-1-veratryl-3,4-dihydro-1H-isoquinolin-2-yl]propanoic acid 5-[3-[(1R,2R)-6,7-dimethoxy-2-methyl-1-veratryl-3,4-dihydro-1H-isoquinolin-2-yl]propanoyloxy]pentyl ester

• Cisatracurium besilate is not associated with dose-related histamine release (at bolus doses of < or = 8 x ED95) and, consistent with this, has demonstrated cardiovascular stability in both healthy patients (< or = 8 x ED95) and those with coronary artery disease (< or = 6 x ED95) [15].
• We tested the influence of atracurium and cisatracurium (final concentrations: 0, 0.96, 3.2, 9.6, 32, and 96 microM) on proliferation of human cells (hepatoma HepG2 cells and human umbilical vein endothelial cells) in vitro [16].
• Previous reports have indicated growth-inhibitory effects of cisatracurium, but not mivacurium, on two human cell lines in vitro [14].
• Basophil activation with rocuronium, vecuronium, atracurium, cisatracurium and suxamethonium was analysed flow cytometrically by labelling with anti-CD123/anti-HLADR/anti-CD63 [17].
• The neuromuscular blocking effect of 0.1 mg x kg(-1) cisatracurium at the adducting laryngeal muscles, the diaphragm and the adductor pollicis (AP) were compared [18].

Associations of 3-[(1R,2R)-6,7-dimethoxy-2-methyl-1-veratryl-3,4-dihydro-1H-isoquinolin-2-yl]propanoic acid 5-[3-[(1R,2R)-6,7-dimethoxy-2-methyl-1-veratryl-3,4-dihydro-1H-isoquinolin-2-yl]propanoyloxy]pentyl ester with other chemical compounds

• Compared with vecuronium, cisatracurium besilate was associated with a significantly faster recovery after continuous infusion in patients in intensive care [15].
• In clinical trials, cisatracurium besilate has been used successfully to facilitate intubation (at 2 to 4 x ED95) and as a muscle relaxant during surgery and in intensive care [15].
• The 50% effective concentration (153+/-33 ng/mL) was 56% higher than that reported in patients anesthetized with volatile anesthetics, which suggests that, compared with inhaled anesthetics, a cisatracurium neuromuscular block is less enhanced by propofol [19].
• The initial drug costs were not substantially different for both Parts 1 and 2, but over time, mivacurium became the most expensive drug and cisatracurium the least expensive [20].
• The dose of neostigmine required to achieve 50% assisted recovery of the train-of-four ratio at 5 min was significantly (P < 0.05) smaller in patients who received vecuronium (29.1 [17.9-55.3] microg/kg) (mean [95% confidence interval]) compared with those who received cisatracurium (53.7 [31.6-131.5] microg/kg) [21].

Gene context of 3-[(1R,2R)-6,7-dimethoxy-2-methyl-1-veratryl-3,4-dihydro-1H-isoquinolin-2-yl]propanoic acid 5-[3-[(1R,2R)-6,7-dimethoxy-2-methyl-1-veratryl-3,4-dihydro-1H-isoquinolin-2-yl]propanoyloxy]pentyl ester

• Cisatracurium infusion rates ranged from 6.3 to 10.5 microg/kg/min, with an average of 8.0 microg/kg/min [22].
• After discontinuing cisatracurium administration, recovery to 70% TOF ratio averaged 68 +/- 13 min [23].
• One-way ANOVA showed a statistically significant difference between the cisatracurium infusion rates before, during and after CPB: A T1/T0 of 15% could be achieved with a mean infusion rate of 1.1, 0.75 and 0.98 micrograms kg-1 min-1 before, during and after CPB, respectively [24].
• The degradation products of cistracurium were identified by ESI positive-ion detection as Hofmann elimination and ester hydrolysis products of cisatracurium [25].
• Response to cisatracurium in patient with Charcot-Marie-Tooth disease [26].

Analytical, diagnostic and therapeutic context of 3-[(1R,2R)-6,7-dimethoxy-2-methyl-1-veratryl-3,4-dihydro-1H-isoquinolin-2-yl]propanoic acid 5-[3-[(1R,2R)-6,7-dimethoxy-2-methyl-1-veratryl-3,4-dihydro-1H-isoquinolin-2-yl]propanoyloxy]pentyl ester

• To augment the contribution of central command independent of force generation, on a separate day the protocol was repeated following partial neuromuscular blockade (PNB; i.v. cisatracurium) [27].
• OBJECTIVE: To evaluate and compare the safety and efficacy of cisatracurium (51W89) and atracurium administered by continuous infusion to critically ill patients requiring neuromuscular blocking agents to facilitate mechanical ventilation [3].
• We designed this study to compare the pharmacodynamics of cisatracurium in OPMD patients versus a control group [28].
• Dose requirements of infusions of cisatracurium or rocuronium during hypothermic cardiopulmonary bypass [24].
• Pharmacokinetics and pharmacodynamics of cisatracurium in patients with end-stage liver disease undergoing liver transplantation [29].

References