Pharmacokinetics and Protein Binding of Propofol in Patients with Cirrhosis

Servln, F.; Desmonts, J. M.; Haberer, J.-P.; Cockshott, I. D.; Plummer, Greg; Farinotti, Robert

doi:10.1097/00000542-198812000-00014

Cited by 219 publications

(82 citation statements)

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“…We found that total body clearance of propofol in patients after esophagectomy was 1.76 Ϯ 0.39 l min Ϫ1 . This value was almost the same as those reported in patients receiving general anesthesia [6,14,15]. Propofol sedation by target-controlled infusion for patients at the postsurgical acute stage may be useful without significant hemodynamic instability.…”

Section: Discussionsupporting

confidence: 83%

Plasma concentration for optimal sedation and total body clearance of propofol in patients after esophagectomy

et al. 2005

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The present study investigated plasma propofol concentration for optimal sedation and total body clearance in patients who required sedation for mechanical ventilation after esophagectomy. Seven patients after esophagectomy were enrolled in this study. Plasma propofol concentrations were measured with high performance liquid chromatography. Total body clearance was calculated from the steady-state concentration. The infusion rate of propofol for achieving the sedation score of level 3 (drowsy, responds to verbal stimulation) was 1.74 +/- 0.82 mg kg(-1) h(-1) (mean +/- SD, n = 7) when the plasma propofol concentration and the total body clearance were 0.85 +/- 0.24 microg ml(-1) and 1.83 +/- 0.54 l min(-1) (mean +/- SD, n =7), respectively.

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Section: Discussionsupporting

confidence: 83%

Plasma concentration for optimal sedation and total body clearance of propofol in patients after esophagectomy

et al. 2005

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“…15 Propofol pharmacokinetic parameters were not signi®cantly in¯uenced by the presence of dexmedetomidine in this study, and these parameter values were consistent with values reported in the literature. 7,9,16,17 Propofol V SS was probably underestimated because blood samples were collected for only 8 h after termination of infusion. Studies with prolonged infusions and extended sampling have shown larger V SS and longer t 1/2 values associated with slowly equilibrating tissue compartments.…”

Section: Pharmacokineticsmentioning

confidence: 99%

Effect of dexmedetomidine on propofol requirements in healthy subjects

Dutta

Karol

Cohen³

et al. 2001

Journal of Pharmaceutical Sciences

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“…A 20-ml aliquot of the filtrate was injected into the HPLC system. 19) HPLC was carried out using an LC-6AD pump and a C-R7A plus chromatopac (Shimadzu, Kyoto, Japan) equipped with a Neopack C 18 column (4.6 mmϫ 250 mm, Nishio Industry Co., Ltd., Tokyo, Japan) and a model RF-10A XL fluorescence detector (Shimadzu) set at 276 nm of excitation and 310 nm of emission. The mobile phase was composed of acetonitrile-water-phosphoric acid (85%): 60-40-0.2 and the flow rate was set at 1.3 ml/min.…”

Section: Effect Of Penetration Enhancers On Transdermal Delivery Of Pmentioning

confidence: 99%

Effect of Penetration Enhancers on Transdermal Delivery of Propofol

Yamato

Akiyama

Tsuji

et al. 2009

Biological & Pharmaceutical Bulletin

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Transdermal therapeutic systems, intended to deliver a drug across skin for systemic activity, are receiving attention because these systems can (1) avoid hepatic first-pass metabolism, (2) maintain blood drug levels for an extended period of time by controlling the drug-release rate and (3) allow easy interruption of drug delivery.1,2) However, the stratum corneum is known to be a major barrier to drug permeation through the keratinized epithelium. Due to the poor skin permeation of drugs, transdermal administration is often limited.3) For enhancing drug delivery across the skin, the efficacy of penetration enhancers has been investigated.4) The penetration enhancers are generally classified as membraneacting types or co-solvent types. The membrane-acting types, such as fatty acid, 5-7) terpene [8][9][10] and surfactant, [11][12][13] achieve effects using small amounts by altering the condition of the lipid membrane constituting the stratum corneum. The co-solvent types, such as propylene glycol (PG), 10,14) polyethylene glycol 15) and ethanol, 8) achieve effects by improving the solubility of drugs or enhancing permeation of drugs through the skin.Propofol (PF), a lipophilic anesthetic, is widely used clinically as it (1) has a rapid onset and cessation of effects upon intravenous infusion, (2) accumulates little and induces a brief but profound anesthesia, (3) maintains a level in circulation similar to the levels achieved by inhalation anesthetics. The characteristics of PF, lipophilicity and low molecular weight (MWϭ178), is suited to the transdermal delivery. 16)Furthermore, as PF exists in the liquid state above 20°C, a high-concentration PF solution can be prepared. In the previous study, we confirmed that PF was absorbed through rat skin and induced a sedative effect in rats.17) By transdermal delivery of PF, the blood level of the drug can be maintained for an extended period of time. Hence, a possibility that PF can be developed as a transdermal dosage form of sedative or hypnotic is considered. In this study, the in vitro skin permeability and the in vivo absorbability of PF were investigated in rats using PF solutions containing various types of enhancers. Then, we estimated the effectiveness of enhancers on the transdermal delivery of PF. (Osaka, Japan) as the purest grade available. Macrogol 400 (MG) was of Japanese Pharmacopoeia (JP) grade. Sucrose fatty acid esters were obtained from MitsubishiKagaku Foods Corporation (Tokyo, Japan). We used four kinds of sucrose fatty acid esters (L595, L1695, O1570 and S1570). L, O and S indicate lauric acid, oleic acid and stearic acid, respectively. The hydrophilic lipophilic balance (HLB) values of L595, L1695, O1570 and S1570 were 5, 16, 15 and 15, respectively. All other chemicals were obtained commercially as the purest grade available. MATERIALS AND METHODS MaterialsAnimals Male Sprague-Dawley rats weighing approximately 200-220 g were purchased from Tokyo Laboratory Animals Science Co., Ltd. (Tokyo, Japan). The experimental protocol was approved by the...

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Pharmacokinetics and Protein Binding of Propofol in Patients with Cirrhosis

Cited by 219 publications

References 0 publications

Plasma concentration for optimal sedation and total body clearance of propofol in patients after esophagectomy

Plasma concentration for optimal sedation and total body clearance of propofol in patients after esophagectomy

Effect of dexmedetomidine on propofol requirements in healthy subjects

Effect of Penetration Enhancers on Transdermal Delivery of Propofol

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