Pharmacokinetics of glimepiride and cytochrome P450 2C9 genetic polymorphisms

Wang, Rui; Chen, Kun; Wen, Siyuan; Li, Jian; Wang, Shengqi

doi:10.1016/j.clpt.2005.03.008

Cited by 42 publications

(30 citation statements)

References 5 publications

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“…On the contrary, there were no significant differences in any diclofenac pharmacokinetic parameters between *1/*1 and *1/*3 genotype groups (Shimamoto et al, 2000). In addition, the *3 heterozygotes showed a 1.3-to 2.5-fold higher mean glimepiride area under the plasma concentration-time curve than that for the wild type (Niemi et al, 2002;Wang et al, 2005;Suzuki et al, 2006), and *3-bearing patients might have an increased risk of sulfonylurea-associated severe hypoglycemia (Holstein et al, 2005).…”

Section: Discussionmentioning

confidence: 84%

Substrate-Dependent Functional Alterations of Seven CYP2C9 Variants Found in Japanese Subjects

Maekawa

Harakawa²,

Sugiyama³

et al. 2009

Drug Metab Dispos

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ABSTRACT:CYP2C9 is a polymorphic enzyme that metabolizes a number of clinically important drugs. In this study, catalytic activities of seven alleles found in Japanese individuals, CYP2C9*3 (I359L), *13 (L90P), *26 (T130R), *28 (Q214L), *30 (A477T), *33 (R132Q), and *34 (R335Q), were assessed using three substrates (diclofenac, losartan, and glimepiride). When expressed in a baculovirus-insect cell system, the holo and total (apo and holo) CYP2C9 protein expression levels were similar among the wild type (CYP2C9.1) and six variants except for CYP2C9. CYP2C9 is a polymorphic enzyme responsible for the oxidative metabolism of up to 15% of the drugs that undergo phase I metabolism (Miners and Birkett, 1998). This enzyme hydroxylates weakly acidic or neutral drugs of diverse therapeutic categories, including the hypoglycemic agents tolbutamide and glimepiride, the nonsteroidal anti-inflammatory drugs flurbiprofen and diclofenac, the antihypertensive losartan, the diuretic torsemide, the anticonvulsant phenytoin, and the anticoagulant warfarin (Rettie and Jones, 2005). To date, 34 CYP2C9 alleles located in the coding region have been reported

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Section: Discussionmentioning

confidence: 84%

Substrate-Dependent Functional Alterations of Seven CYP2C9 Variants Found in Japanese Subjects

Maekawa

Harakawa²,

Sugiyama³

et al. 2009

Drug Metab Dispos

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“…A single-dose clinical study found a 1.3-and 1.5-fold higher AUC of glimepiride in healthy Chinese volunteers with the CYP2C9*1/*3 and *3/*3 genotypes, respectively (Wang et al, 2005). In this study, the formation clearance of glimepiride to M1 (and subsequent inactive M2 metabolite) was significantly decreased in individuals harbouring the CYP2C9*1/*3 genotype.…”

Section: Diabetesmentioning

confidence: 88%

Polymorphisms of human cytochrome P450 2C9 and the functional relevance

2010

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“…Sulfonylurea Drugs. CYP2C9 is important for the metabolism of this class, with CYP2C9*3 (but not CYP2C9*2) being clearly implicated in impaired clearance of tolbutamide, glyburide, and glimepiride (Kirchheiner et al, 2002a,b;Lee et al, 2002b;Niemi et al, 2002;Shon et al, 2002;Wang et al, 2005).…”

Section: B Cyp2c9mentioning

confidence: 99%