Pharmacokinetics and pharmacodynamics of propofol 6% SAZN versus propofol 1% SAZN and Diprivan-10 for short-term sedation following coronary artery bypass surgery

Knibbe, Caj; Aarts, Leon; Kuks, Paul F. M.; Voortman, Henk-Jan; Lie‐A‐Huen, Loraine; Bras, Leo; Danhof, Meindert

doi:10.1007/s002280050726

Cited by 20 publications

(25 citation statements)

References 17 publications

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“…Other recent studies did not find any effect of the changing formulation on the pharmacokinetics or pharmacodynamics of propofol. [9][10][11][12] In the current study, the commercially available propofol formulation, Diprivan 2%, was compared to the newly formulated propofol 2% for bioequivalence with regard to pharmacokinetic parameters after each study drug was administered as a single 2-mg/kg bolus dose. The 90% confidence interval for the AUC ratio was included by the acceptance range for bioequivalence (80%-125%).…”

Section: Discussionmentioning

confidence: 99%

Pharmacokinetics and Pharmacodynamics of a Single Bolus of Propofol 2% in Healthy Volunteers

Abad‐Santos¹,

Gálvez-Múgica²,

Santos³

et al. 2003

The Journal of Clinical Pharma

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This study was undertaken to assess the bioequivalence between a new formulation of propofol 2% and the commercially available product Diprivan. Secondary objectives were to compare the times to onset of and emergence from hypnosis, the hemodynamic effects, and the safety profiles. Twelve healthy male volunteers were included in a randomized crossover study. Subjects were administered a 2-mg/kg single bolus injection of each formulation separated by a 7- to 10-day washout period. Plasma propofol was determined by reversed-phase liquid chromatography with fluorescence detection. Eleven subjects completed the study, and both formulations were considered bioequivalent. There were no serious or severe adverse events. The concentration-time profiles of all the subjects could adequately be described using a three-compartment model. The mean times to cessation of counting out loud (17 vs. 18 s) and to eye opening (245 vs. 244 s) were not statistically different between treatment groups. Moreover, they seem to show some degree of pharmacodynamic bioequivalence, although a higher number of subjects are necessary to unequivocally demonstrate it.

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Section: Discussionmentioning

confidence: 99%

Pharmacokinetics and Pharmacodynamics of a Single Bolus of Propofol 2% in Healthy Volunteers

Abad‐Santos¹,

Gálvez-Múgica²,

Santos³

et al. 2003

The Journal of Clinical Pharma

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“…[6] In another study, propofol formulation 6% in Lipofundin MCT/LCT 10% had a similar incidence of pain on injection as LCT propofol containing intralipid 10%. [7] Lipofundin MCT/LCT 10% is a 10% fat emulsion consisting of MCT and LCT, whereas intralipid 10% contains only LCT. [7] In several other studies, less pain is reported with MCT/LCT preparation compared to LCT preparation.…”

Section: Different Formulations Of Propofolmentioning

confidence: 99%

“…[7] Lipofundin MCT/LCT 10% is a 10% fat emulsion consisting of MCT and LCT, whereas intralipid 10% contains only LCT. [7] In several other studies, less pain is reported with MCT/LCT preparation compared to LCT preparation.…”

Section: Different Formulations Of Propofolmentioning

confidence: 99%

Pain on propofol injection: Causes and remedies

DeSousa

2016

Indian J Pharmacol

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Pain on propofol injection (POPI) is a minor problem that all anesthetists face every day. Introduction of several new formulations and hundreds of clinical trials have failed to find its remedy with just one intervention in all patients. This article highlights the causes of POPI and interventions that are used to eliminate this pain in current practice. Relevant articles from Medline and Embase databases were searched and included in this descriptive review with the following conclusions: (1) POPI is due to irritation of venous adventitia leading to release of mediators such as kininogen from kinin cascade. (2) When two or more drugs or measures are used, the incidence of POPI decreases considerably. Hence, the approach to eliminating POPI should be multimodal. (3) Any regimen that includes a drug having local anesthetic effect combined with central sedative/analgesic and rapid injection into a large vein should definitely reduce the risk of POPI to negligible levels.

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“…5,6 For this reason, a new formulation, propofol 6%, has been developed, resulting in a reduction of fat, emulsifier, and volume load by 83%. Propofol 6% has previously been studied for short-term use in clinical 11,12 and preclinical 13 studies.…”

mentioning

confidence: 99%

Population pharmacokinetic and pharmacodynamic modeling of propofol for long-term sedation in critically ill patients: A comparison between propofol 6% and propofol 1%

Knibbe

2002

Clinical Pharmacology & Therapeutics

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The population models in critically ill patients showed no differences in pharmacokinetics or pharmacodynamics between propofol 6% and propofol 1%. TG and T(c) appeared to be significant covariates for elimination clearance. For the pharmacodynamics, when propofol concentrations were between 0.75 and 1.5 mg/L, Ramsay sedation score 6 was most probable (40%-75%) and the probability for Ramsay sedation score 5 was 20% to 40%. Large pharmacodynamic variabilities were observed.

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Pharmacokinetics and pharmacodynamics of propofol 6% SAZN versus propofol 1% SAZN and Diprivan-10 for short-term sedation following coronary artery bypass surgery

Cited by 20 publications

References 17 publications

Pharmacokinetics and Pharmacodynamics of a Single Bolus of Propofol 2% in Healthy Volunteers

Pharmacokinetics and Pharmacodynamics of a Single Bolus of Propofol 2% in Healthy Volunteers

Pain on propofol injection: Causes and remedies

Population pharmacokinetic and pharmacodynamic modeling of propofol for long-term sedation in critically ill patients: A comparison between propofol 6% and propofol 1%

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