Pharmacokinetics and Pharmacodynamics of Propofol in a New Solvent

Doenicke, Α.; Roizen, Michael F.; Rau, Jens; OʼConnor, Michael; Kugler, J.; Klotz, Ulrich; Babl, Juergen

doi:10.1213/00000539-199712000-00040

Cited by 99 publications

(57 citation statements)

References 18 publications

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“…Alternatively, the decrease in pain when using LCT/MCT propofol is considered to be attributed to the lipid solvent that decreases the propofol concentration in the aqueous phase. [12][13][14][15] Association between the aqueous phase propofol concentration and injection pain has also been reported in some studies. 23,24 Thus, it is possible that a reduction in either bradykinin generation or the aqueous phase propofol concentration decreases the pain on injection with propofol.…”

Section: Bradykinin Generation and Complement Activationmentioning

confidence: 97%

“…It was suggested that this can be attributed to a decreased concentration of the aqueous phase propofol. [12][13][14][15] According to the above reports, reduction of bradykinin generation or propofol concentration in the aqueous phase may be the main reasons for reduced pain on injection with propofol emulsified in LCT/MCT. Although a decrease in the aqueous phase propofol in this emulsion has been demonstrated, 16 the effect on bradykinin generation has not been examined.…”

Section: Résultatsmentioning

confidence: 99%

See 1 more Smart Citation

Mechanism of injection pain with long and longmedium chain triglyceride emulsive propofol

Ohmizo

Obara

Iwama

2005

Can J Anesth/J Can Anesth

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P Pu ur rp po os se e: : t has been suggested that long-medium chain triglyceride (LCT/MCT) emulsive propofol causes less injection pain than long chain triglyceride (LCT) emulsive propofol because of the decreased propofol concentration in the aqueous phase. Alternatively, LCT propofol generates bradykinin causing the injection pain and activates complement, but these effects when using LCT/MCT propofol have not been examined. To identify the mechanism for reduced pain with LCT/MCT propofol, injection pain, bradykinin generation and complement activation with use of both propofol products were compared.M Me et th ho od ds s: : Two hundred adult patients randomly allocated to two groups were given 1.5 mg·kg -1 iv of either LCT propofol or LCT/MCT propofol at a rate of 200 mg·min -1 in a double-blind manner and were asked to grade pain scores. In another study, bradykinin and activated complement 3 (C3a) concentrations were measured using blood obtained from 13 healthy volunteers mixed with saline, LCT propofol or LCT/MCT propofol.R Re es su ul lt ts s: : There was a significant difference in pain scores between groups, showing a lower incidence of injection pain in the LCT/MCT propofol group. The bradykinin concentrations in blood mixed with LCT and LCT/MCT propofol were significantly higher than in blood mixed with saline. The C3a concentrations showed similar results.C Co on nc cl lu us si io on ns s: : LCT/MCT propofol causes less pain on injection compared with LCT propofol. Bradykinin generation and complement activation are similar with both LCT and LCT/MCT propofol. Thus, the reason for less pain on injection with LCT/MCT propofol may be attributed to a decreased concentration of propofol in the aqueous phase. Objectif : On a pensé qu'une émulsion de propofol avec une chaîne mi-longue de triglycéride (CLT/CMT) cause moins de douleur à l'injection qu'une émulsion à chaîne longue (CLT) parce que la concentration de propofol diminue pendant la phase aqueuse. Aussi, le propofol avec CLT génère de la bradykinine, causant de la douleur à l'injection, et active le complément, mais ces effets n'ont pas été étudiés avec le propofol CLT/CMT. Pour définir le mécanisme qui réduit la douleur avec le propofol CLT/CMT, nous avons comparé la douleur à l'injection, la génération de bradykinine et l'activation du complément avec l'usage des deux produits de propofol. Méthode : Deux cents patients adultes ont été répartis au hasard en deux groupes et ont reçu 1,5 mg·kg -1 iv de propofol CLT ou CLT/CMT

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Section: Bradykinin Generation and Complement Activationmentioning

confidence: 97%

Section: Résultatsmentioning

confidence: 99%

Mechanism of injection pain with long and longmedium chain triglyceride emulsive propofol

Ohmizo

Obara

Iwama

2005

Can J Anesth/J Can Anesth

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“…These adverse reactions have motivated attempts to develop new, safer propofol formulations. There are several reformulations of propofol, including: 1. the basic presentation with the addition of ethylene diamine tetraacetic acid or sulfite to minimize the bacterial growth 12 ; 2. emulsion containing different longand medium-chain triglycerides to reduce the amount of serum lipids 13,14,15 ; 3. propofol prodrug 16 ; 4. water-soluble analogues of propofol 17,18 and 5. non-lipid cyclodextrinbased formulation of propofol 6,19,20 .…”

Section: Discussionmentioning

confidence: 99%

Caracterização anestésica da nanoemulsão não lipídica de propofol

Sudo¹,

Bonfá²,

Trachez³

et al. 2010

Rev. Bras. Anestesiol.

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Summary: Sudo RT, Bonfá L, Trachez MM, Debom R, Rizzi MDR, Zapata-Sudo G -Anesthetic Profile of a Non-lipid Propofol Nanoemulsion. Background and objectives:The clinical use of a lipid propofol formulation causes pain during injection, allergic reactions, and bacterial growth. Propofol has been reformulated in different non-lipid presentations to reduce the incidence of adverse effects, but those changes can modify its pharmacokinetics and pharmacodynamics. In the present study, we investigate the pharmacology and toxicology of lipid propofol (CLP) and the non-lipid nanoemulsion (NLP).

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“…Free concentrations of propofol release brandikinin by activating the kinin-kallikrein system with a direct irritation to vessel endothelium (particularly tunica media and intima), thus venous dilatation generates a hyper permeability and this causes pain by providing more contact from propofol to nerve endings [3][4][5][6][7].…”

Section: Introductionmentioning

confidence: 99%