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At least 19 recordsLinked to original sources
PubMed2002

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

OBJECTIVES: A population pharmacokinetic and pharmacodynamic model of propofol for long-term sedation in critically ill patients is described, because limited information is available in these patients. In the models the influence of time-independent covariates, in particular, the propofol formulation (propofol 6% versus propofol 1%), and of time-dependent covariates was investigated. METHODS: Twenty critically ill, mechanically ventilated patients received propofol formulated as propofol 6% (n = 10) or propofol 1% (n = 10) during a 2- to 5-day period. The level of sedation was assessed with the Ramsay 6-point scale. The data from a short-term sedation study in 24 patients after cardiac surgery were included. Population pharmacokinetic and pharmacodynamic modeling was performed with NONMEM. RESULTS: The pharmacokinetics was adequately described by a 2-compartment model. The propofol formulation was not a significant covariate for the pharmacokinetics, whereas serum triglyceride concentration (TG) and relative body temperature (T(c)) were significant covariates for elimination clearance (CL). The population pharmacokinetic parameters were as follows: CL = 2.2 + 0.27 x T(c) - 0.049 x TG (mean, 2.1 L/min); volume of central compartment, 22.2 L; CL (distribution), 1.5 L/min; and volume of peripheral compartment, 168 L. The addition of other time-independent covariates (long-term versus short-term sedation study, as well as physiologic characteristics) or time-dependent covariates (duration of propofol infusion, additional midazolam rates, and hemodynamic parameters) to the model did not improve the quality of fit. For the pharmacodynamics, the probability that the sedation level was equal to, or more than, a specific score was described with the use of a sigmoid inverse logit of the maximal achievable probability model. The values for the inverse logit of the concentration causing half of the maximal effect for Ramsay sedation scores of 2 through 6 were 0.13 +/- 0.09, 0.31 +/- 0.17, 0.56 +/- 0.24, 0.79 +/- 0.31, and 1.78 +/- 0.65 mg/L, respectively (population mean +/- SE). Interindividual variability was high, with a coefficient of variation of 119% in the 50% effective concentration values. No covariates were identified. CONCLUSIONS: 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.

APACHE↗
PubMed2005

Propofol injection pain in children: a prospective randomized double-blind trial of a new propofol formulation versus propofol with added lidocaine.

BACKGROUND: The incidence of pain on injection of propofol remains unacceptably high in children, despite various strategies to reduce it. A new drug formulation of propofol has, in adult studies, been reported to cause less injection pain compared with other propofol solutions. The aim of the present prospective randomized double-blind clinical trial was to compare the incidence of pain-free injection following the use of this new formulation with that following the use of propofol with added lidocaine in children undergoing day case surgery. METHODS: Eighty-three children (age range 2-18 yr) were randomized to receive 3 mg kg(-1) of either Propofol-Lipuro (propofol dissolved in a mixture of medium- and long-chain triglycerides [MCT-LCT]; group pL, n=42) or Diprivan (propofol dissolved in long-chain triglycerides [LCT]) with added lidocaine (0.3 mg kg(-1)) (group pD, n=41). A specially trained nurse anaesthetist assessed the occurrence of injection pain using a four-graded pain scale. RESULTS: Significantly fewer patients had an entirely pain-free propofol injection in group pL (33.3%) than in group pD (61.0%) (P=0.016). CONCLUSIONS: A new MCT-LCT propofol formulation as a plain solution was associated with a higher incidence of injection pain than LCT propofol with added lidocaine when used for induction of anaesthesia in children.

Adolescent↗
PubMed1998

Pain on injection of propofol. A comparison of cold propofol with propofol premixed with lignocaine.

Propofol is frequently associated with pain on injection. Previous studies have suggested that chilling of the propofol decreases pain significantly. This prospective, randomised, double-blind trial was designed to assess the effectiveness of cold propofol compared with propofol premixed with lignocaine in minimising pain on injection. Patients were allocated to one of four groups: propofol + lignocaine 0.1 mg.kg-1, propofol + lignocaine 0.2 mg.kg-1, cold propofol and a control group consisting of propofol premixed with normal saline and maintained at room temperature. The results of this study show that cold propofol is associated with a very high incidence of injection pain while lignocaine 0.1 mg.kg-1 premixed with propofol significantly decreases the incidence of pain (p < 0.001). Increasing the dosage of lignocaine above 0.1 mg.kg-1, however, does not significantly decrease the incidence of pain further. The addition of lignocaine also significantly decreases the incidence of excitatory side-effects.

Adolescent↗
PubMed2002

Intravenous magnesium sulfate administration reduces propofol infusion requirements during maintenance of propofol-N2O anesthesia: part I: comparing propofol requirements according to hemodynamic responses: part II: comparing bispectral index in control and magnesium groups.

BACKGROUND: The authors investigated whether an intravenous administration of magnesium sulfate reduces propofol infusion requirements during maintenance of propofol-N2O anesthesia. METHODS: Part I study: 54 patients undergoing total abdominal hysterectomy were randomly divided into two groups (n = 27 per group). The patients in the control group received 0.9% sodium chloride solution, whereas the patients in the magnesium group received magnesium (50 mg/kg as a bolus, then 8 mg x kg(-1) x h(-1)). To maintain mean arterial blood pressure (MAP) and heart rate (HR) at baseline value, the propofol infusion rate was changed when the MAP or the HR changed. The amount of propofol infused excluding the bolus dosage was divided by patient's body weight and total infusion time. Part II study: Another 20 patients were randomly divided into two groups (n = 10 per group). When the MAP and HR had been maintained at baseline value and the propofol infusion rate had been maintained at 80 microg x kg(-1) x min(-1) (magnesium group) and 160 microg x kg(-1) x min(-1) (control group), bispectral index (BIS) values were measured. RESULTS: Part I: The mean propofol infusion rate in the magnesium group (81.81 +/- 13.09 microg x kg(-1) x min(-1)) was significantly less than in the control group (167.57 +/- 47.27). Part II: BIS values in the control group (40.70 +/- 3.89) were significantly less than those in the magnesium group (57.80 +/- 7.32). CONCLUSION: Intravenous administration of magnesium sulfate reduces propofol infusion requirements. These results suggest that magnesium administration may have an effect on anesthesia or analgesia and may be a useful adjunct to propofol anesthesia.

Adult↗
PubMed1991

Effect of prior administration of cold saline on pain during propofol injection. A comparison with cold propofol and propofol with lignocaine.

A single-blind, randomised, controlled study was undertaken to compare the efficacy of three methods of preventing pain during injection of propofol on induction of anaesthesia. Patients were allocated randomly to receive unmodified propofol, propofol with 0.05% lignocaine, propofol at 4 degrees C and unmodified propofol preceded by 10 ml of 0.9% saline at 4 degrees C. Prior injection of cold saline reduced the incidence of pain and discomfort significantly (22%) compared with unmodified propofol (75%; p less than 0.005) and was similar to that after cold propofol (33%) and propofol with lignocaine (44%). There was no significant difference between the treatment groups.

Adult↗
PubMed2004

Propofol-induced injection pain: comparison of a modified propofol emulsion to standard propofol with premixed lidocaine.

Propofol is well known for its association with pain on injection. The most frequently used method to reduce this pain is premixture with lidocaine. Recently, a modified lipid emulsion of propofol containing medium-chain triglycerides (MCT) with long-chain triglycerides (LCT), in contrast to the usual LCT formulation, has been advocated to alleviate pain. In a randomized, prospective, controlled, double-blind study on 222 surgical patients, we compared the effect of the two solutions on the incidence and intensity of injection pain. Patients were randomly allocated to receive either propofol MCT/LCT (group M; n = 109) or standard propofol LCT with the addition of 20 mg of lidocaine (2 mL of lidocaine 1%) to 200 mg of propofol (group L; n = 113). Pain scores were assessed using a verbal analog scale (VAS) ranging from 0-10. Group L was found to have significantly less pain on the injection of propofol (mean VAS, 2.5 +/- 2.9) (mean +/- sd) than group M (mean VAS, 3.8 +/- 3.2; P = 0.002). Regarding postoperative recall of pain on injection, patients in group L indicated significantly less pain (mean VAS, 2.2 +/- 2.4) than patients in group M (mean VAS, 3.0 +/- 2.7; P = 0.02). Premixing of 20 mg of lidocaine (2 mL of lidocaine 1%) to 200 mg of standard propofol LCT causes less pain on injection than propofol MCT/LCT and thus increases patient comfort.

Adolescent↗
PubMed2004

Comparison of Propofol-Lipuro with propofol mixed with lidocaine 10 mg on propofol injection pain.

A common drawback of propofol is pain on injection and lidocaine is commonly mixed with propofol to reduce its incidence and severity. We conducted a randomised, prospective, double-blind study to compare injection pain following the administration of two different formulations of propofol in 200 unpremedicated ASA I-III adult patients scheduled for elective surgery under general anaesthesia. Patients were allocated randomly into two groups to receive either Propofol-Lipuro without added lidocaine or Diprivan mixed with lidocaine 10 mg. Five ml of the study solution was injected at a constant rate over 15 s and patients graded any associated pain or discomfort using a four-point verbal rating scale. The incidence of propofol injection pain was virtually identical in both study groups with 37/98 (38%) patients experiencing pain or discomfort following Propofol-Lipuro compared with 35/98 (36%) after Diprivan (p = 0.88). We observed no significant difference in pain scores between the groups (p = 0.67). Moderate or severe injection pain was experienced by 12/98 (12%) patients given Propofol-Lipuro compared with 8/98 (8%) given Diprivan (p = 0.48).

Adolescent↗
PubMed2005

Randomized double-blind comparison of ketamine-propofol, fentanyl-propofol and propofol-saline on haemodynamics and laryngeal mask airway insertion conditions.

The aim of this prospective, double-blind, randomized, placebo-controlled clinical trial was to investigate whether the administration of ketamine before induction with propofol improves its associated haemodynamic profile and laryngeal mask airway (LMA) insertion conditions. Ninety adult patients were randomly allocated to receive either ketamine 0.5 mg x kg(-1) (n = 30), fentanyl 1 microg x kg(-1) (n = 30) or normal saline (n = 30), before induction of anaesthesia with propofol 2.5 mg x kg(-1). Insertion of the LMA was performed 60s after injection of propofol. Arterial blood pressure and heart rate were measured before induction (baseline), immediately after induction, immediately before LMA insertion, immediately after LMA insertion and every minute for three minutes after LMA insertion. Following LMA insertion, the following six subjective endpoints were graded by a blinded anaesthestist using ordinal scales graded 1 to 3: mouth opening, gagging, swallowing, movement, laryngospasm and ease of insertion. Systolic blood pressure was significantly higher following ketamine than either fentanyl (P = 0.010) or saline (P = 0.0001). The median (interquartile range) summed score describing the overall insertion conditions were similar in the ketamine [median 7.0, interquartile range (6.0-8.0)] and fentanyl groups [median 7.0, interquartile range (6.0-8.0)]. Both appeared significantly better than the saline group [median 8.0, interquartile range (6.75-9.25); P = 0.024]. The incidence of prolonged apnoea (> 120s) was higher in the fentanyl group [23.1% (7/30)] compared with the ketamine [6.3% (2/30)] and saline groups [3.3% (1/30)]. We conclude that the addition of ketamine 0.5 mg x kg(-1) improves haemodynamics when compared to fentanyl 1 microg x kg(-1), with less prolonged apnoea, and is associated with better LMA insertion conditions than placebo (saline).

Adjuvants, Anesthesia↗
PubMed1998

[Clinical indication of propofol for pediatric patients--pharmacokinetics of propofol and ketamine during and after total intravenous anesthesia with propofol, fentanyl and ketamine (PFK) in a neonate].

A 60-day-old neonate boy received hepatic portojejunostomy for biliary atresia under PFK. Pharmacokinetics of propofol and ketamine during and after PFK was also studied. Plasma levels of propofol (Cp) and ketamine (Ck) were maintained at 2 to 3 micrograms ml-1 and at 200 to 300 ng ml-1 during surgery, respectively. Both Cp and Ck decreased quickly after the end of infusions. From the pharmacokinetic point of view, PFK may be safely applied even for neonates.

Anesthesia, Intravenous↗
PubMed2004

[Propofol-LCT versus propofol-MCT/LCT with or without lidocaine - a comparison on pain on injection].

OBJECTIVE: A disadvantage of Propofol (commercial preparation containing long-chain triglycerides; Propofol-LCT) is pain on injection, which is reported by 54 - 100 % of the patients. Many different approaches have been used in an attempt to decrease the pain on injection of propofol. The currently most efficacious treatment is lidocaine given intravenously with a tourniquet prior to Propofol injection. In previous studies, larger concentrations of free propofol in the aqueous phase of an emulsion were associated with more pain on injection. A new formulation of propofol (a mixture of long-chain and medium-chain triglycerides in the carrier emulsion; Propofol-MCT/LCT) reduces the incidence of pain on bolus injection. This study was designed to investigate, whether the use of Propofol-MCT/LCT alleviates pain on injection to a similar degree as pretreatment with lidocaine. METHODS: Eighty patients (ASA I - III) were randomly assigned to four groups according to a double-blinded protocol, to receive either lidocaine 2 % or normal saline given iv. with a 60 seconds tourniquet time before the injection of Propofol-LCT or Propofol-MCT/LCT. (group 1: 2 ml NaCl 0,9 %, Propofol-LCT; group 2: 2 ml NaCl 0,9 %, Propofol-MCT/LCT; group 3: 2 ml lidocaine 2 %, Propofol-LCT; group 4: 2 ml lidocaine 2 %, Propofol-MCT/LCT). Assessment of pain on injection was performed after 30 % of the induction dose was given. RESULTS: Pain on injection caused by Propofol-LCT with pre-treatment of lidocaine and Propofol-MCT/LCT alone is shown to be equivalent. Comparison of Propofol-MCT/LCT with pre-treatment of lidocaine and Propofol-LCT alone shows a statistical noticeable p-value of 0.035. Propofol-MCT/LCT with pre-treatment of lidocaine suggests a tendency of causing less pain compared to Propofol-MCT/LCT. Analysis of the postoperative questionnaire supplies no significant difference. CONCLUSION: The results suggest that pain on injection is reduced equivalent using either Propofol-MCT/LCT alone or Propofol-LCT with pre-treatment of lidocaine. Pre-treatment with lidocaine before Propofol-MCT/LCT seems to have an additional effect.

Adult↗
PubMed2001

[Less pain on injection by a new formulation of propofol? A comparison with propofol LCT].

BACKGROUND: Pain on injection is a major disadvantage of propofol, experienced by the vast majority of patients. Since the traditional formulation has almost normal osmolality and pH, it is hypothesised that the concentration of free propofol in the aqueous phase of the emulsion is responsible for the pain and that reducing the amount of free propofol would also reduce the frequency and intensity of pain on injection. This study was designed to investigate whether pain on injection can be reduced in frequency and intensity by a new formulation of propofol. METHODS: We performed a monocentre, controlled, randomised, double-blind study to compare the pain produced by intravenous injection of a new propofol preparation (propofol-MCT/LCT) with standard propofol in patients undergoing elective surgical procedures. A total of 184 non-premedicated patients received either 1% propofol prepared in a mixture of medium and long chain triglycerides (Propofol-MCT/LCT, Propofol- Lipuro, B. Braum Melsungen AG) or standard 1% propofol prepared exclusively in long chain triglycerides (Propofol-LCT; Disoprivan, AstraZeneca) into a vein of the dorsal hand for induction of anaesthesia. Anaesthesia was maintained by TIVA with propofol and remifentanil. Pain on injection was recorded and graded as none, mild, moderate or severe. RESULTS: Patients receiving propofol-MCT/LCT had a significantly lower incidence of pain on injection compared to the standard propofol group (37% vs 64%) with the intensity of pain also being less severe. There were no differences between both groups in propofol dosage for induction (3.2 +/- 0.8 mg/kg vs 3.3 +/- 0.9 mg/kg) and maintenance of anaesthesia (3.4 +/- 0.6 mg/kg/h vs 3.2 +/- 0.5 mg/kg/h), remifentanil dosage (25 +/- 6 micrograms/kg/h vs. 24 +/- 6 micrograms/kg/h), intraoperative hemodynamics, recovery parameters and postoperative patient satisfaction. Postoperative thrombophlebitis at the injection site for propofol was not observed in any of the patients. CONCLUSIONS: Propofol-MCT/LCT produced significantly less pain on injection when compared to standard propofol in ASA I and II patients undergoing elective surgery. Pain was also significantly less severe, with both effects presumably being due to the lower concentration of free propofol in the MCT/LCT-preparation. With regard to injection pain propofol-MCT/LCT offers significant a advantage over standard propofol.

Anesthesia, Intravenous↗
PubMed2004

Long-term sedation with propofol 60 mg ml(-1) vs. propofol 10 mg(-1) ml in critically ill, mechanically ventilated patients.

BACKGROUND: Hypertriglyceridaemia is the main cause of therapeutic failure during propofol use in long-term sedated mechanically ventilated patients. Propofol 60 mg ml(-1) has been developed to reduce fat and volume load for the critically ill patient. The purpose of the study was to compare the effectiveness of sedation, achievability of effective concentrations and the effects on serum lipid concentrations of propofol 60 mg ml(-1) vs. propofol 10 mg ml(-1) for long-term sedation in critically ill patients. METHODS: In this randomized, open, prospective study, 20 critically ill, mechanically ventilated patients who required sedation for a minimum of 48 h received propofol 60 mg ml(-1) or propofol 10 mg ml(-1) in doses as required during 2-5 days. RESULTS: No differences between propofol 60 mg ml(-1) and propofol 10 mg ml(-1) were observed in the effectiveness of sedation using the Ramsay Sedation score and the Subjective Sedation score, nor in relation to the propofol concentrations. Between the two groups, there were no significant differences in the daily propofol dose, number of daily infusion rate adjustments or need for additional sedatives. Mean serum triglyceride concentrations were higher in the propofol 10 mg ml(-1) group compared with the propofol 60 mg ml(-1) group [5.26 (3.19) vs. 3.22 (2.05) mmol l(-1), P > 0.05][mean (SD)]. Patients in the propofol 10 mg ml(-1) group received more fat from the propofol infusion than from the propofol 60 mg ml(-1) group [53.2 (29.6) vs. 10.0 (4.7) % compared with fat from nutrition, respectively]. A significant relationship was observed between the daily total fat dose and the serum triglyceride concentration (r2 = 0.32, P < 0.001), whereas there was no significant correlation between the daily propofol dose and the serum triglyceride concentration. CONCLUSION: Propofol 60 mg ml(-1) is a useful alternative to propofol 10 mg ml(-1) for the long-term sedation of critically ill patients. Sedation with propofol 60 mg ml(-1) reduces fat and volume load by 83%, which reduces the risk of hypertriglyceridaemia.

Adult↗
PubMed1999

The growth of microorganisms in propofol and mixtures of propofol and lidocaine.

UNLABELLED: Propofol emulsion supports bacterial growth. Extrinsic contamination of propofol has been implicated as an etiological event in postsurgical infections. When added to propofol, local anesthetics (e.g., lidocaine) alleviate the pain associated with injecting it. Because local anesthetics have antimicrobial activity, we determined whether lidocaine would inhibit microbial growth by comparing the growth of four microorganisms in propofol and in mixtures of propofol and lidocaine. Known quanta of Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, and Candida albicans were inoculated into solutions of 1% propofol, 0.2% lidocaine in propofol, 0.5% lidocaine in propofol, 0.5% lidocaine in isotonic sodium chloride solution, and 0.9% isotonic sodium chloride solution. All microorganisms were taken from stock cultures and incubated for 24 h. Growth of microorganisms in each solution was compared by counting the number of colony-forming units grown from a subculture of the solution at 0, 3, 6, 12 and 24 h. Propofol supported the growth of E. coli and C. albicans. Propofol maintained static levels of S. aureus and was bactericidal toward P. aeruginosa. The addition of 0.2% and 0.5% lidocaine to propofol failed to prevent the growth of the studied microorganisms. The effect of 0.5% lidocaine in isotonic sodium chloride solution did not differ from the effects of isotonic sodium chloride solution alone. We conclude that lidocaine, when added to propofol in clinically acceptable concentrations, does not exhibit antimicrobial properties. IMPLICATIONS: Local anesthetics such as lidocaine have antimicrobial activity. Propofol supports the growth of bacteria responsible for infection. Bacteria were added to propofol and propofol mixed with lidocaine. The addition of lidocaine to propofol in clinically relevant concentrations did not prevent the growth of bacteria. The addition of lidocaine to propofol cannot prevent infection from contaminated propofol.

Anesthetics, Intravenous↗
PubMed2003

The pharmacokinetics and pharmacodynamics of propofol in a modified cyclodextrin formulation (Captisol) versus propofol in a lipid formulation (Diprivan): an electroencephalographic and hemodynamic study in a porcine model.

UNLABELLED: The currently marketed propofol formulation has a number of undesirable properties that are in part a function of the lipid emulsion formulation, including pain on injection, serious allergic reactions, and the support of microbial growth. A modified cyclodextrin-based formulation of propofol (sulfobutyl ether-beta-cyclodextrin) has been developed that may mitigate some of these formulation-dependent problems. However, reformulation may alter propofol's pharmacologic behavior. Our aim in this study was to compare the pharmacokinetics and pharmacodynamics of propofol in the currently marketed lipid-based formulation with those of the novel cyclodextrin formulation. We hypothesized that the pharmacokinetics and pharmacodynamics of the propofol in cyclodextrin would be substantially similar to those of the propofol in lipid. Thirty-two isoflurane-anesthetized animals were instrumented with pulmonary artery, arterial, and IV catheters and were randomly assigned to receive either propofol in lipid or propofol in cyclodextrin by continuous infusion. Arterial blood samples for propofol assay were collected. The processed electroencephalogram, heart rate, mean arterial blood pressure, and cardiac output were measured continuously. The propofol formulations were compared by using model-independent analysis techniques. Combined kinetic/dynamic models were also constructed for simulation purposes. There were no significant differences in the pharmacokinetics or pharmacodynamics of the two propofol formulations. The simulations based on the combined pharmacokinetic/pharmacodynamic models confirmed the substantial similarity of the two formulations. The hypothesis that the propofol-in-cyclodextrin formulation would exhibit pharmacokinetic and pharmacodynamic behavior that was substantially similar to the propofol-in-lipid formulation was confirmed. IMPLICATIONS: A modified cyclodextrin-based formulation of propofol has been developed that may mitigate some of the problems associated with propofol in lipid emulsion. However, reformulation of propofol may change its clinical characteristics. This study in a pig model showed that the novel propofol formulation was substantially similar to the lipid emulsion propofol formulation.

Anesthetics, Intravenous↗
PubMed2003

[Injection pain secondary to propofol-MCT/LCT and propofol-LCT--comparison of prophylaxis with lidocaine].

OBJECTIVE: Pain on injection is one of the most described side-effects of the intravenous application of propofol. This study was designed to assess the efficacy of lidocaine 40 mg in preventing incidence and severity of injection pain for two different propofol solvents. METHODS: In a double-blind and prospective study 202 patients were enrolled and randomized to 4 different groups: group A receiving 2 ml NaCl 0.9 % and propofol-LCT (Disoprivan; AstraZeneca), group B 40 mg lidocaine and propofol-LCT, group C received 2 ml NaCl 0.9 % and propofol-MCT/LCT (Propofol-Lipuro, B. Braun Melsungen AG) and group D 40 mg lidocaine and propofol-MCT/LCT. According to the protocol, all patients were cannulated with a 18-G venous cannula at the dorsum of the hand and no other medicament was injected before the study drug. Time interval between test agents and propofol application in a dosage of 2 mg/kg was one minute. Severity of pain was evaluated during propofol injection over 30 seconds until loss of consciousness using a 4-point rating scale. RESULTS: The incidence of injection pain did not differ between propofol-LCT and propofol-MCT/LCT (64 % and 53 %). Propofol-MCT/LCT significantly reduced the severity of pain compared to propofol-LCT (p < 0.05). The application of lidocaine resulted in a significant reduction in incidence (Propofol-MCT/LCT: 16 %; Propofol-LCT: 31 %) and severity of injection pain compared to placebo. CONCLUSION: Propofol-MCT/LCT showed a significant advantage compared to propofol-LCT considering the severity of injection pain, but not in reducing the incidence of pain. The use of lidocaine resulted in a significant reduction of incidence and severity of injection pain for both propofol solvents.

English Abstract↗
PubMed1999

Pharmacokinetics, induction of anaesthesia and safety characteristics of propofol 6% SAZN vs propofol 1% SAZN and Diprivan-10 after bolus injection.

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 Lipofundin(R) 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 Intralipid(R) 10%, Diprivan-10) and propofol 1% in Lipofundin(R) 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 Diprivan-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 (Vd,ss ), elimination half-life (t1/2,z ) and distribution half-life (t1/2, lambda2) 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 (t1/2,lambda1 ) 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.

Adult↗
PubMed2006

Propofol alone titrated to deep sedation versus propofol in combination with opioids and/or benzodiazepines and titrated to moderate sedation for colonoscopy.

BACKGROUND: Propofol by nonanesthesiologists is controversial because the drug is commonly used to produce deep sedation or general anesthesia. Propofol in combination with opioids and/or benzodiazepines can be titrated to moderate sedation, which might be safer. AIM: To compare recovery time, patient satisfaction, and other end points with propofol alone titrated to deep sedation versus propofol combination therapy with opioids and/or benzodiazepines. METHOD: A randomized controlled clinical trial of propofol alone titrated to deep sedation versus fentanyl plus propofol versus midazolam plus propofol versus fentanyl plus midazolam plus propofol in 200 outpatients undergoing colonoscopy. Each combination regimen was titrated to moderate sedation. RESULTS: Patients receiving propofol alone received higher doses of propofol and had deeper sedation scores compared with combination therapy (both p < 0.001). Patients receiving combination regimens were discharged more quickly (median 13.0-14.7 versus 18.1 min) than those receiving propofol alone (p < 0.01). There were no differences in vital signs or oxygen saturations among the study arms. There were no significant differences in pain or satisfaction among the study arms in the recovery area. At a follow-up phone call, patients receiving fentanyl and propofol remembered more of the procedure than those in the other regimens (p < 0.005) and remembered more pain than those receiving propofol alone (p < 0.02). CONCLUSIONS: Propofol in combination with fentanyl and/or midazolam can be titrated to moderate levels of sedation without substantial loss of satisfaction and with shorter recovery times compared with propofol titrated to deep sedation throughout the procedure.

Adjuvants, Anesthesia↗
PubMed2001

[Injection pain from propofol-MCT-LCT in children. A comparison with propofol-LCT].

OBJECTIVES: This prospective, randomised, double-blind study was designed to compare the incidence and intensity of pain on injection of propofol formulated in a mixture of medium- and long-chain triglycerides, Propofol-MCT/LCT 1% (Propofol-Lipuro, B. Braun, Germany) with propofol in a commonly used emulsion of long-chain triglycerides, Propofol-LCT 1% (Disoprivan, Zeneca) in children undergoing elective surgical procedures. METHODS: After approval of the local ethics committee 40 children, aged 7-14 years, were enrolled in the study. Premedication was with 5-10 mg diazepam orally one hour before induction of anesthesia. In the beginning 20% of the calculated dose of Propofol for induction was injected into a separate venous cannula in a dorsal vein of the hand; patients were observed for expressing pain spontaneously during injection patients or were asked to describe the sensations after 10 s. Withdrawal of the arm during injection was also noted. RESULTS: Significantly more children reported pain on injection of propofol-LCT compared to Propofol-MCT/LCT (25% vs, 10%) and significantly more children retracted their arm during injection of propofol-LCT (40% vs. 10%). IMPLICATIONS: Propofol-MCT/LCT 1% (Propofol-Lipuro) for induction of anesthesia produced significantly less pain on injection and significantly less drawing back of the arm when compared to Propofol-LCT (Disoprivan). Thus, with respect to pain on injection Propofol-MCT/LCT appears to be superior to Propofol-LCT in children aged 7-14 years.

Adolescent↗