2002
DOI: 10.1007/s00228-002-0478-x
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Pharmacokinetics in renally impaired subjects of NXY-059, a nitrone-based, free-radical trapping agent developed for the treatment of acute stroke

Abstract: Non-renal elimination of NXY-059 appeared to be insignificant even in subjects with low renal capacity. Patients with renal impairment should have their dose of NXY-059 adjusted for renal function, conveniently assessed from serum creatinine.

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Cited by 24 publications
(19 citation statements)
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“…In contrast to STAZN and other lipophilic nitrones, hydrophilic nitrones such as NXY-059 and S-PBN are quickly eliminated unchanged in the urine and have short half-lives dependent on renal function (Marklund et al, 2001;Strid et al, 2002). Furthermore, these hydrophilic nitrones normally penetrate the blood-brain barrier poorly (Kuroda et al, 1999), although there is in vitro evidence that they may do so under hypoxic and ischemic conditions (Dehouck et al, 2002).…”
Section: Discussionmentioning
confidence: 99%
“…In contrast to STAZN and other lipophilic nitrones, hydrophilic nitrones such as NXY-059 and S-PBN are quickly eliminated unchanged in the urine and have short half-lives dependent on renal function (Marklund et al, 2001;Strid et al, 2002). Furthermore, these hydrophilic nitrones normally penetrate the blood-brain barrier poorly (Kuroda et al, 1999), although there is in vitro evidence that they may do so under hypoxic and ischemic conditions (Dehouck et al, 2002).…”
Section: Discussionmentioning
confidence: 99%
“…have been performed on NXY-059 in humans (Lees et al ., 2001;Strid et al ., 2002;Lees et al ., 2003). Low doses of NXY-059 (250 mg over 1 h followed by 85 mg h − 1 for 71 h or 500 mg over 1 h followed by 170 mg h − 1 for 71 h) were given to patients with acute stroke.…”
Section: Nitrones Are Protective In Stroke Modelsmentioning
confidence: 99%
“…Secondly, NXY-059 induces vasodilation of cerebral vessels, but does not directly promote survival of neural cells. Pharmacokinetic issues, such as the short half-life of the drug and its inability to easily cross the BBB may have also contributed to its lack of efficacy (Shuaib et al, 2007; Strid et al, 2002; Zivin, 2009). In order to confer longer lasting neuroprotection during ischemic stroke, researchers have begun focusing on therapeutics that enhances of the activity the brain’s endogenous antioxidant enzymes.…”
Section: 1 Oxidative Stress In Ischemic Strokementioning
confidence: 99%