Pharmacokinetics and pharmacodynamics of propofol with or without 2% benzyl alcohol following a single induction dose administered intravenously in cats
Gregg M. GriffenhagenMarlis L. RezendeDaniel L. GustafsonRyan J. HansenPaul J. LunghoferKhursheed R. Mama
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Keywords:
Pharmacodynamics
Benzyl alcohol
Crossover study
This study was performed to compare the pharmacological characteristics of propofol in an emulsion of both medium- and long-chain triglycerides (MCT/LCT) with those of propofol in an LCT emulsion, by measuring the sedative level and the plasma concentration of propofol during sedation using a target-controlled infusion (TCI) technique. Forty ASA 1 or 2 adult patients who required spinal anaesthesia for surgery were enrolled in this study. The patients were divided into two groups: a propofol LCT group (n=20) and a propofol MCT/LCT group (n=20). Propofol was injected intravenously at target blood concentrations of 2.0, 3.0 and 4.0 μg.ml –1 . The bispectral (BIS ® ) index was recorded, and arterial blood was drawn to measure the actual plasma concentrations of propofol at each predicted concentration. Propofol was assayed by high-performance liquid chromatography. Propofol MCT/LCT was associated with significantly less pain than propofol LCT (P<0.05). There were no significant differences between the two groups in BIS® index or in plasma concentration of propofol at each predicted concentration. Computer-generated TCI of propofol MCT/LCT during sedation is comparable with that of propofol LCT with respect to pharmacokinetics and pharmacodynamics. The formulation of MCT/LCT has a beneficial effect with respect to less pain on injection.
Bispectral index
Pharmacodynamics
Arterial blood
Lipid emulsion
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목적: 최근 대장 질환의 발생 빈도가 증가함에 따라 환자가 두려움 없이 편안하게 검사를 받을 수 있으면서 시술 의사가 안심하고 검사할 수 있는 수면 대장내시경이 요구되고 있다. 저자는 수면 대장내시경에서 propofol 단독요법과 midazolam, propofol 병합요법을 서로 비교하여 보다 좋은 전처치법을 개발하고자 하였다. 대상 및 방법: 2004년 8월부터 2005년 5월까지 한림대성심병원에서 수면유도법에 의한 대장내시경을 시행한 환자를 대상으로 propofol 단독요법군(108예)과 midazolam, propofol 병합요법군(102예)으로 나누어 연구를 시행하였다. 단독요법군은 propofol을 2-2.5 ml/kg/hr로 정주하였고, 병합요법군은 midazolam 3 mg을 정주 후 propofol을 2-2.5 ml/kg/hr로 정주하였다. 검사 중 지속적으로 심전도, 혈압, 맥박, 산소포화도 등을 감시하였다. 진정상태까지의 propofol 용량, 전체 propofol 용량, 수면유도시간, 내시경소요시간, 회복시간, 환자만족도, 시술자 만족도를 측정하여 두 군 간의 결과를 비교하였다. 결과: 시술 전과 시술 중의 혈압, 분당 심박수, 호흡횟수, 산소포화도 변화에 있어서 두 군간에 유의한 차이는 없었다. 진정상태까지의 propofol 용량과 전체 propofol 용량은 병합요법군에서 단독요법군에 비해 유의하게 적었다(p＜0.001). 수면유도시간은 병합요법군에서 단독요법군에 비해 유의하게 짧았다(p＜0.001). 회복시간과 환자 만족도에서 두 군간에 유의한 차이는 없었다. 시술자만족도는 병합요법군에서 유의하게 높았다(p=0.04). 두 군 모두에서 치명적인 부작용을 보인 예는 없었다. 결론: 수면 대장내시경에서 midazolam, propofol 병합요법은 propofol 단독요법에 비해 propofol 용량을 줄일 수 있었고, 부작용 발생의 증가없이 수면유도시간을 단축할 수 있었다.
Midazolam
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Pharmacodynamics
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The pharmacodynamic profile of bucainide dimaleate (RHC G-233) in dogs has been studied. The first observed pharmacologic effect was a change in the ECG pattern (T-wave duration and amplitude) that occurred after an average intravenous dose of 2.7 mg/kg. The average plasma concentration of bucainide was approximately 350 ng/ml. Analysis of data from dogs that received a dual infusion of bucainide indicated that bucainide has an extensive volume of distribution, with an average value of approximately 26 l/kg. An average terminal half-life of 89 minutes was observed. Studies with the radiolabeled drug in rats and dogs also demonstrated the drug's large volume of distribution, and its initial rapid disappearance from the blood. Tissue distribution studies in the rat after administration of the radiolabeled drug showed that bucainide is rapidly taken up by the tissues.
Pharmacodynamics
Distribution Volume
Plasma clearance
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Objective To observe the outcomes of anesthesia with target-controlled infusion(TCI) of propofol and remifentanel in the elderly undergoing gestroendoscopy.Methods A total of 200 patients aged more than 70 years old was equally assigned into two groups.Group T was given TCI with target concentrtions of propofol 0.5-1.8 μg/ml and remifentanel 0.5-1.0 ng/ml.Group P was conventionally injected propofol 1.5-2.0 mg/kg,which was followed by 4 mg/s and supplemental injection of propofol if necessary.SBP,DBP,HR,RR and SpO2 were monitored.Propofol consumption and awakening time were compared.Results Anesthesia was more stable in group T than that in group P.Propofol consumption was less in group T than that in group P [(61.5±21.3) mg vs.(98.4±31.2) mg] and awakening time was earlier in group T than that in group P[(62±38) s vs.(426±57) s](P0.05).There was no case with severe respiratory depression in both groups.ConclusionCompared to propofol alone,anesthesia with TCI of propofol and remifentanel is better with less requirement of propofol and earlier awakening after surgery in the elderly undergoing gestroendoscopy.
Target controlled infusion
Group B
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Pharmacodynamics
Intravenous bolus
Bolus (digestion)
Elimination rate constant
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The pharmacokinetics and protein binding of propofol were studied in ten patients with cirrhosis and in ten control patients undergoing elective surgery. All patients received 2.5 mg.kg-1 propofol as an intravenous bolus injection for the induction of anesthesia. Whole blood propofol concentrations were measured at intervals up to 12 h, using a high-performance liquid chromatography (HPLC) technique. Propofol protein binding was estimated by equilibrium dialysis 10 min after injection of propofol. Individual propofol profiles for all patients were best described by a three-compartment open mammillary model. Rapid and slow propofol distribution half-times were observed, followed by an elimination phase with a half-time of 4-5 h. Propofol total body clearance was reduced (1.99 +/- 0.68 l.min-1) in the patients with cirrhosis but did not differ significantly from that in the control patients (2.30 +/- 0.61 l.min-1). The apparent volume of distribution at steady state (Vdss) was similar in the two groups. No significant difference in elimination half-life was observed between the two groups. Propofol was extensively bound (mean: 97-98%) to the plasma protein of both cirrhotic and control groups. This study shows that propofol pharmacokinetics and protein binding of propofol following a single intravenous bolus dose were not markedly affected by uncomplicated cirrhosis of the liver.
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Objective To study the relationship between BIS value and propofol blood concentration in patients with different age during TCI of propofol.Methods Sixty patients of ASA class Ⅰ or Ⅱ,admitted upper abdominal surgey,were divided into adult group(n=30) and elderly group(n=30).Anesthesia was induced with TCI of remifentanil and propofol in two groups.Blood target concentration of remifentanil was set at 7 μg/L and propofol 3 mg/L.When lost consciousness,the patients were given vencuroium 0.1 mg/kg and intubated. Mechanical ventilation was maintained in all patients.After intubation,the blood target concentration of remifentanil was kept unchanged and of propofol reduced to 2.5 mg/L.The propofol infusion rate was adjusted to maintain a BIS value between 45 and 55 during surgery.Two millilitres of arterial blood samples were drawn for detecting propofol plasma concentration after TCI propofol for 5 min.Results There was no correlation between plasma propofol concentration and BIS values in adult group,but there was a high inverse correlation between the measured propofol concentration and BIS value in elderly group(r=-0.64816).Conclusion There is a good correlation between blood concentration of propofol and BIS value in elderly patients,which is not in adult paients.Therefore blood concentration of propofol in elderly patients can be applied to sedation assessment.
Bispectral index
Arterial blood
Blood concentration
Target controlled infusion
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