High-performance liquid chromatographic determination and preliminary pharmacokinetics of propofol and its metabolites in human plasma and urine

Vree, T. B.; Baars, A. M.; Grood, P.M.R.M. de

doi:10.1016/0378-4347(87)80145-7

Cited by 53 publications

(24 citation statements)

References 2 publications

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“…According to Vree et.al. [12] the quinol glucuronide amounts to 20-50% of the dose. Quantification of propofol in 3 different hair segments showed an increase in the concentrations towards the scalp i.e.…”

Section: Resultsmentioning

confidence: 99%

“…The last half-life corresponds to the elimination from adipose tissue [10], but being insignificant due to the rapid metabolism of propofol. Propofol is maily metabolised by two pathways: either direct glucronide conjugation or p-hydroxylation with subsequent glucuronidation (or sulphation) [11] where quinol glucuronide amounts to 20-50% of the dose [12]. Only very small amounts are aliminated without being metabolised [10,11].…”

Section: Introductionmentioning

confidence: 99%

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Death after excessive propofol abuse

Iwersen‐Bergmann

Rösner

Kühnau

et al. 2001

International Journal of Legal Medicine

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Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Death after excessive propofol abuse

Iwersen‐Bergmann

Rösner

Kühnau

et al. 2001

International Journal of Legal Medicine

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“…Most systemic clearance estimates of propofol, a drug eliminated almost entirely by metabolism (Vree et al, 1987), exceed the commonly accepted value for human hepatic blood flow. This has promoted speculation that there may be significant extrahepatic metabolism of this drug (Servin et al, 1986;Kay et al, 1986;Schuttler et al, 1986;Cockshott et al, 1987).…”

Section: Methodsmentioning

confidence: 97%

Extended blood collection period required to define distribution and elimination kinetics of propofol.

Campbell

Morgan

Kumar

et al. 1988

Brit J Clinical Pharma

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The pharmacokinetics of propofol were investigated following bolus intravenous administration of 2-3 mg kg-1 of drug to eight surgical patients. Apparent elimination half-life, volume of distribution and systemic blood clearance of propofol correlated strongly with the sampling period, which ranged from 8 to 52 h, depending on the time taken for the propofol concentration to reach the detection limit of the assay. In the three patients in whom the sampling period exceeded 42 h, apparent elimination half-life (55.6 h) and apparent volume of distribution (13701) greatly exceeded previously published estimates and systemic blood clearance (1020 ml min-1) was much less than previous estimates. This suggests that previous estimates were biased by the relatively short duration of blood collection in those studies (8 to 12 h).

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“…Key words propofol; pharmacokinetic; total intravenous anesthesia propofol was measured using HPLC equipped with a fluorescence detector, as described by Vree et al 6) Propofol was kindly supplied by Astra Zeneca (Osaka, Japan). Methanol and acetonitrile were of HPLC grade.…”

Section: Pharmacokinetics Of Propofol In Elderly Coronary Artery Bypamentioning

confidence: 99%

Pharmacokinetics of Propofol in Elderly Coronary Artery Bypass Graft Patients under Total Intravenous Anesthesia.

Morikawa

Oishi

Takeyama

et al. 2002

Biological & Pharmaceutical Bulletin

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Intravenous infusion of propofol induces a rapid and smooth onset and clearing of anesthesia, and has minimal accumulation in the body over long-term administration. 1)Propofol anesthesia enables the smooth maintenance of unconsciousness devoid of excitatory problems.2-4) Propofol is increasingly used for cardiac anesthesia and postoperative sedation. Since pharmacokinetic parameters vary among distinct patient populations, rational drug dosing for cardiac surgery patients is dependent on the characterization of the drug's pharmacokinetic parameters in coronary artery bypass graft. The pharmacokinetic profile of propofol, with its short elimination half-life and high total body clearance makes it ideally suited for administration as an infusion. However, many factors (age, weight, drug interaction, and pre-existing disease) alter propofol's pharmacokinetic properties. Of these, age is one of the most important factors. There have been reports of the pharmacokinetics of propofol infusion in Japanese patients. 5) However, there have been few reports of the pharmacokinetics of propofol in elderly patients with coronary diseases under surgery. In this study, we investigated the pharmacokinetics of propofol in two elderly patients with angina pectoris undergoing coronary artery bypass graft.Case Reports A 78-year-old Japanese man (164 cm, 64 kg, patient A) with unstable angina pectoris was operated on in an off pump coronary artery bypass graft under total intravenous anesthesia with propofol after written informed consent was obtained. The liver function was normal (GOT: 22.0, GPT: 22.7) before the operation. Propofol (Diprivan ® injection) was purchased from Astra Zeneca Co., Ltd. (Osaka, Japan). For the induction of anesthesia, 1.5 mg/kg propofol (96 mg) was administered as a single bolus infusion. From 20 min after the end of the bolus infusion, anesthesia was maintained using the step-down infusion regimens of propofol with an infusion pump, at 10 mg/kg/h for 10 min, 8 mg/kg/h for 10 min, 6 mg/kg/h for 5 min, 4 mg/kg/h for 30 min, 8 mg/kg/h for 10 min, 6 mg/kg/h for 50 min, 4 mg/kg/h for 190 min, and 3 mg/kg/h for 40 min until the end of the surgical procedure (total 1792 mg of propofol). Blood samples were collected at 5 min from the end of the bolus infusion, and at 60, 120, 195, 240, 300, 365, 395, 425 and 725 min.A 76-year-old Japanese man (162 cm, 64.1 kg, patient B) with unstable angina pectoris was operated on in a minimally invasive direct coronary artery bypass graft under total intravenous anesthesia with propofol after written informed consent was obtained. The liver function was normal (GOT : 23.5, GPT : 20.1) before the operation. For the induction of anesthesia, 1.5 mg/kg propofol (100 mg) was administered as a single bolus infusion. Anesthesia was maintained using the step-down infusion regimens of propofol using the infusion pump, at 10 mg/kg/h for 20 min, 8 mg/kg/h for 10 min, 6 mg/kg/h for 10 min, 4 mg/kg/h for 30 min, 6 mg/kg/h for 20 min, 4 mg/kg/h for 165 min, and 3 mg/kg/h for 20 min until...

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High-performance liquid chromatographic determination and preliminary pharmacokinetics of propofol and its metabolites in human plasma and urine

Cited by 53 publications

References 2 publications

Death after excessive propofol abuse

Death after excessive propofol abuse

Extended blood collection period required to define distribution and elimination kinetics of propofol.

Pharmacokinetics of Propofol in Elderly Coronary Artery Bypass Graft Patients under Total Intravenous Anesthesia.

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