Water-soluble propofol analogues with intravenous anaesthetic activity

Cooke, Andrew; Anderson, Alison; Buchanan, Kirsteen; Byford, Alan; Gemmell, David K.; Hamilton, Niall M.; McPhail, Petula; Miller, Stephen R.; Sundaram, Hardy; Vijn, Peter

doi:10.1016/s0960-894x(01)00088-9

Cited by 23 publications

(20 citation statements)

References 9 publications

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“…As shown in Table V, a similar HD 50 value was observed for both propofol for- (macroemulsion, 10.5 mg/kg and microemulsion, 11.6 mg/kg). These values are analogous to the results previously reported, 11.8 mg/kg (Adam et al, 1980) and 12.1 mg/kg (Cooke et al, 2001). Therapeutic index was calculated from the ratio of LD 50 to HD 50 (Banaszczy et al, 2002).…”

Section: In Vivo Toxicity and Anesthetic Activitysupporting

confidence: 85%

“…Thus, it might accelerate the onset of sedation state and full recovery from anesthesia as well as reduce risk of psychomotor function damage (Adam et al, 1980;Kay and Stephenson, 1980). Several studies have reported that propofol might cause fewer occurrences of side effects such as headache, nausea and vomiting (Langley and Heel, 1988;Trappni et al, 2000;Cooke et al, 2001). Due to these clinical advantages, propofol has been widely used for inducing and maintaining general anesthesia and local analgesic adjuvant (Smint et al, 1994).…”

Section: Introductionmentioning

confidence: 99%

“…Due to these clinical advantages, propofol has been widely used for inducing and maintaining general anesthesia and local analgesic adjuvant (Smint et al, 1994). Additionally, this drug can be administrated to some patients who are in an intensive care unit or have respiratory disorders (Cooke et al, 2001).…”

Section: Introductionmentioning

confidence: 99%

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Formulation and evaluation of an alternative triglyceride-free propofol microemulsion

Cho

Lee

et al. 2010

Arch. Pharm. Res.

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A new triglyceride-free propofol microemulsion for intravenous injection was formulated using nonionic surfactants, poloxamers and polyethylene glycol 660 hydroxystearate. The aim of this investigation was to evaluate the formulation for storage stability, antimicrobial activity, toxicity and preclinical efficacy. The results were compared to the characteristics obtained for the most commonly used formulation of propofol (Diprivan®). The mean particle diameter of the microemulsion was less than 100 nm so that it could be readily sterilized using a 0.22 μm membrane at room temperature. The microemulsion formulation demonstrated enhanced stability compared to the marketed macroemulsion formulation. In a stress storage condition, it was physicochemically stable for at least 40 months. This new formulation showed higher antimicrobial activity, lower risk of hyperlipidemia and better tolerability than Diprivan®. In preclinical studies, the efficacy and pharmacokinetic profile of the microemulsion were similar to those of Diprivan®. Nevertheless, the administration of the microemulsion caused considerably low histamine release compared to the macroemulsion. Based on these results, the newly developed microemulsion of propofol appeared to have several advantages and, thus, could be an alternative to the fat macroemulsions of propofol.

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Section: In Vivo Toxicity and Anesthetic Activitysupporting

confidence: 85%

Section: Introductionmentioning

confidence: 99%

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Formulation and evaluation of an alternative triglyceride-free propofol microemulsion

Cho

Lee

et al. 2010

Arch. Pharm. Res.

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“…Water-soluble propofol analogs have been tested for their hypnotic effect in mice and rats, but hemodynamic effects were not reported [13] . DSB is not water soluble.…”

Section: Resultsmentioning

confidence: 99%

Hemodynamic Effects of Di-Sec-Butyl Phenol, an Anesthetic Substituted Phenol

Deau

Heerdt²,

Wang³

2006

Pharmacology

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Dose- and age-related hemodynamic effects were determined for an anesthetic substituted phenol, 2,6-di-sec-butyl phenol (DSB). DSB, 7.5 mg/kg, induced hypnosis in young rabbits and increased mean blood pressure to 170 ± 14% and heart rate to 150 ± 21% of control values. In elderly rabbits, 7.5 mg/kg DSB induced hypnosis, had no effect on blood pressure, but increased the heart rate to 130 ± 2% of control. After ganglionic blockade with hexamethonium, 7.5 mg/kg DSB caused a decline in mean blood pressure (71 ± 5% of control) without change in heart rate. DSB increased norepinephrine release from SH-SY5Y cells, a human neuroblastoma cell line (5.4 ± 1.7% vs. 3.5 ± 0.3%). DSB produced age-dependent elevation of mean blood pressure in rabbits, probably by causing release of catecholamines from the sympathetic nervous system.

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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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Water-soluble propofol analogues with intravenous anaesthetic activity

Cited by 23 publications

References 9 publications

Formulation and evaluation of an alternative triglyceride-free propofol microemulsion

Formulation and evaluation of an alternative triglyceride-free propofol microemulsion

Hemodynamic Effects of Di-Sec-Butyl Phenol, an Anesthetic Substituted Phenol

Caracterização anestésica da nanoemulsão não lipídica de propofol

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