Influence of Sample Site on Blood Concentrations of Ici 35 868

Major, E.; Aun, C. S. T.; Yate, P.M.; Savege, T. M.; Verniquet, Andrew; Adam, H. K.; Douglas, Elaine

doi:10.1093/bja/55.5.371

Cited by 31 publications

(13 citation statements)

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“…For phases in his profiles were often uninterpretable, the reason for which, we think, is venous sampling. The propofol, Major et al [28] measured significantly higher arterial than venous concentrations directly after bolus half-life of the additional early distribution phase in our study ranged from 0.1 to 0.6 min which is in agreement injection, which turned into the reverse after 1 min. Wang et al [29] found similar differences in an infusion with the findings of Adam et al [25], describing in some of the patients a half-life of this additional phase ranging setting.…”

Section: Induction Of Anaesthesia Pharmacokinetic Analysissupporting

confidence: 86%

“…In general, arterial sampling is preferred when pharmacokinetic parameters are studied of drugs which are rapidly distributed, because the steeper arterial concentration profile provides a more sensitive measure for the detection of early distribution phases [ 26, 27]. For propofol, Major et al [ 28] measured significantly higher arterial than venous concentrations directly after bolus injection, which turned into the reverse after 1 min. Wang et al [ 29] found similar differences in an infusion setting.…”

Section: Discussionmentioning

confidence: 99%

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Pharmacokinetics, induction of anaesthesia and safety characteristics of Propofol 6% SAZN vs Propofol 1% SAZN and Diprivan^®‐10 after bolus injection

Knibbe¹,

Voortman²,

Aarts³

et al. 1999

Brit J Clinical Pharma

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Aims In order to avoid the potential for elevated serum lipid levels as a consequence of long term sedation with propofol, a formulation of propofol 6% in LipofundinA MCT/LCT 10% (Propofol 6% SAZN) has been developed. The pharmacokinetics, induction of anaesthesia and safety characteristics of this new formulation were investigated after bolus injection and were compared with the commercially available product ( propofol 1% in IntralipidA 10%, DiprivanA-10) and propofol 1% in LipofundinA MCT/LCT 10% (Propofol 1% SAZN). Methods In a randomised double-blind study, 24 unpremedicated female patients received an induction dose of propofol of 2.5 mg kg −1 over 60 s which was followed by standardized balanced anaesthesia. The patients were randomized to receive propofol as Propofol 6% SAZN, Propofol 1% SAZN or DiprivanA-10. Results For all formulations the pharmacokinetics were adequately described by a tri-exponential equation, as the propofol concentrations collected early after the injection suggested an additional initial more rapid phase. The average values for clearance (CL), volume of distribution at steady-state ( V d,ss ), elimination half-life (t 1/2,z ) and distribution half-life (t 1/2,l2 ) observed in the three groups were 32±1.5 ml kg −1 min −1 , 2.0±0.18 l kg −1 , 95±5.6 min and 3.4±0.20 min, respectively (mean±s.e.mean, n=24) and no significant differences were noted between the three formulations ( P >0.05). The half-life of the additional initial distribution phase (t 1/2,l1 ) in all subjects ranged from 0.1 to 0.6 min. Anaesthesia was induced successfully and uneventfully in all cases, and the quality of induction was adequate in all 24 patients. The induction time did not vary between the three formulations and the average induction time observed in the three groups was 51±1.3 s which corresponded to an induction dose of propofol of 2.1±0.06 mg kg −1 (mean±s.e.mean, n=24). The percentage of patients reporting any pain on injection did not vary between the formulations and was 17% for the three groups. No postoperative phlebitis or other venous sequelae of the vein used for injection occurred in any of the patients at recovery of anaesthesia nor after 24 h. Conclusions From the above results, we conclude that the alteration of the type of emulsion and the higher concentration of propofol in the new parenteral formulation of propofol does not affect the pharmacokinetics and induction characteristics of propofol, compared with the currently available product. Propofol 6% SAZN can be administered safely and has the advantage of a reduction of the load of fat and emulsifier which may be preferable when long term administration of propofol is required.

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Section: Induction Of Anaesthesia Pharmacokinetic Analysissupporting

confidence: 86%

Section: Discussionmentioning

confidence: 99%

Pharmacokinetics, induction of anaesthesia and safety characteristics of Propofol 6% SAZN vs Propofol 1% SAZN and Diprivan^®‐10 after bolus injection

Knibbe¹,

Voortman²,

Aarts³

et al. 1999

Brit J Clinical Pharma

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“…Major et al . [18] found that there was no significant difference between arterial, central venous, and peripheral venous concentrations of propofol at sampling time beyond one minute.…”

Section: Discussionmentioning

confidence: 99%

Propofol pharmacokinetics in young healthy Indian subjects

et al. 2012

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Objectives:To analyze population pharmacokinetics of Propofol in Indian patients after single bolus dose of Propofol using WINNONLIN program.Materials and Methods:Population pharmacokinetics of Propofol was investigated in Indian subjects in 26 elective surgical patients (14 males and 12 females) following single bolus dose of 2 mg/kg propofol. A total of 364 samples were estimated by High Performance Liquid Chromatography and pharmacokinetic parameters were derived using WINNONLIN (5.2). The effect of demographic characters of the study population on pharmacokinetic parameters was investigated.Results:Three-compartment model was used to describe the pharmacokinetic data of Propofol in Indian subjects. Initial volume of distribution (V1) clearance (Cl) and steady state volume of distribution (Vdss) was 13.5 ± 3.3 l, 1.08 ± 0.42 l/min, and 77.69 ± 48.0 l, respectively. Body weight best described the volume of central compartment (V1) as well as elimination clearance (P<0.01).Conclusion:Pharmacokinetics of Propofol in young healthy Indian subjects show lower volume of distribution and clearance as compared with most of the western data. Body weight best describes the V1, Vdss, and Clearance in this group.

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“…And also, to be mixed instantaneously was a little difficult for high concentrations. [14] Therefore, high concentrations were still unable to predict ideal values. Maybe propofol at high concentration may follow nonlinear pharmacokinetics.…”

Section: Discussionmentioning

confidence: 99%

Propofol pharmacokinetics in China: A multicentric study

Rui

et al. 2012

Indian J Pharmacol

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Objective:A multicenter population pharmacokinetics study of propofol was performed to establish a new population model.Materials and Methods:Three thousand two hundred and fifty-nine blood samples of 220 participants were measured by HPLC-UV or HPLC-FLU or GC-MS. Target-controlled infusion after single bolus or continuous infusion was applied for propofol anesthesia. The samples were taken from 2 to 1500 min. The concentration-time profiles were analyzed by nonlinear mixed effect model (NONMEM) with first order estimation method. The inter-individual variability and the residual variability were described by exponential model and constant coefficient variation model. The stepwise modeling strategy using PsN was applied for covariate modeling. The criteria of forward addition and backward elimination were (α = 0.01 and α = 0.005, χ2, df = 1). The final model was evaluated by bootstrap using PDx and visual predictive check using PsN. 500 bootstraps and 1000 simulation were run.Result:The propofol population model was described by 3-compartment model with inter-individual variability of CL, V1, Q2, and Q3 describing by exponential model. The inter-individual variability of V2, V3 were not included because it is reported that the parameter was near its boundary. The typical value of CL, V1, Q2, V2, Q3 and V3 were 1.28 L · min-1, 10.1 × (age/44)-0.465 × (1 + 0.352 × sex) L, 0.819 L · min-1, 36.0 L, 0.405 × (bodyweight/60)1.58 L · min-1 and 272 L, respectively. Coefficients of inter-individual variability of CL, V1, Q2 and Q3 were 30.5%, 35.6%, 43.7% and 66.9%, respectively, and the coefficients of variation of HPLC-UV, GC-MS and HPLC-FLU were 13.3%, 16.9% and 24.2%, respectively. The bootstrap evaluation showed that the final model parameter estimates were within ± 3.39% compared with bootstrap median. The curves of observations percentiles were distributed within the corresponding 95 prediction percentiles by the visual predictive check.Conclusion:The three-compartment model with first-order elimination could describe the pharmacokinetics of propofol fairly well. The involved fixed effects are age, body weight and sex. The population model was evaluated to be stable by bootstrap and visual predictive check.

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Influence of Sample Site on Blood Concentrations of Ici 35 868

Cited by 31 publications

References 1 publication

Pharmacokinetics, induction of anaesthesia and safety characteristics of Propofol 6% SAZN vs Propofol 1% SAZN and Diprivan^®‐10 after bolus injection

Pharmacokinetics, induction of anaesthesia and safety characteristics of Propofol 6% SAZN vs Propofol 1% SAZN and Diprivan^®‐10 after bolus injection

Propofol pharmacokinetics in young healthy Indian subjects

Propofol pharmacokinetics in China: A multicentric study

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Influence of Sample Site on Blood Concentrations of Ici 35 868

Cited by 31 publications

References 1 publication

Pharmacokinetics, induction of anaesthesia and safety characteristics of Propofol 6% SAZN vs Propofol 1% SAZN and Diprivan®‐10 after bolus injection

Pharmacokinetics, induction of anaesthesia and safety characteristics of Propofol 6% SAZN vs Propofol 1% SAZN and Diprivan®‐10 after bolus injection

Propofol pharmacokinetics in young healthy Indian subjects

Propofol pharmacokinetics in China: A multicentric study

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Pharmacokinetics, induction of anaesthesia and safety characteristics of Propofol 6% SAZN vs Propofol 1% SAZN and Diprivan^®‐10 after bolus injection

Pharmacokinetics, induction of anaesthesia and safety characteristics of Propofol 6% SAZN vs Propofol 1% SAZN and Diprivan^®‐10 after bolus injection