Glipizide: A Second‐generation Sulfonylurea Hypoglycemic Agent; Pharmacology, Pharmacokinetics and Clinical Use

Lebovitz, Harold E.

doi:10.1002/j.1875-9114.1985.tb03405.x

Cited by 48 publications

(14 citation statements)

References 35 publications

(17 reference statements)

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“…Overall, these results are in agreement with previous results where glibenclamide and the first generation sulfonylurea tolbutamide reverted the antinociception produced by diclofenac, but not by indomethacin (Ortiz et al, 2003;Ortiz, 2011). In the present study, we demonstrated for the first time that the antinociceptive effects of diclofenac were blocked by glipizide, a second generation sulfonylurea (Lebovitz, 1985). It is one of the most regularly prescribed drugs for the treatment of patients with noninsulin-dependent diabetes (Wysowski et al, 2003).…”

Section: Effect Of Sulfonylureas On the Antinociceptive Effects Of DIsupporting

confidence: 95%

Metformin and phenformin block the peripheral antinociception induced by diclofenac and indomethacin on the formalin test

Ortiz

2012

Life Sciences

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Section: Effect Of Sulfonylureas On the Antinociceptive Effects Of DIsupporting

confidence: 95%

Metformin and phenformin block the peripheral antinociception induced by diclofenac and indomethacin on the formalin test

Ortiz

2012

Life Sciences

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“…Glipizide is a second-generation sulfonylurea used in the treatment of Type II diabetes [1000]. First-pass metabolism of glipizide appears to be minimal, and the absolute oral bioavailability of the drug is reported to be 80-100% [1000].…”

Section: Glipizidementioning

confidence: 99%

Substrates, Inducers, Inhibitors and Structure-Activity Relationships of Human Cytochrome P450 2C9 and Implications in Drug Development

Zhou¹,

Zhou²,

Liu³

et al. 2009

CMC

146

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Cytochrome P450 2C9 (CYP2C9) is one of the most abundant CYP enzymes in the human liver. CYP2C9 metabolizes more than 100 therapeutic drugs, including tolbutamide, glyburide, diclofenac, celecoxib, torasemide, phenytoin losartan, and S-warfarin). Some natural and herbal compounds are also metabolized by CYP2C9, probably leading to the formation of toxic metabolites. CYP2C9 also plays a role in the metabolism of several endogenous compounds such as steroids, melatonin, retinoids and arachidonic acid. Many CYP2C9 substrates are weak acids, but CYP2C9 also has the capacity to metabolise neutral, highly lipophilic compounds. A number of ligand-based and homology models of CYP2C9 have been reported and this has provided insights into the binding of ligands to the active site of CYP2C9. Data from the site-directed mutagenesis studies have revealed that a number of residues (e.g. Arg97, Phe110, Val113, Phe114, Arg144, Ser286, Asn289, Asp293 and Phe476) play an important role in ligand binding and determination of substrate specificity. The resolved crystal structures of CYP2C9 have confirmed the importance of these residues in substrate recognition and ligand orientation. CYP2C9 is activated by dapsone and its analogues and R-lansoprazole in a stereo-specific and substrate-dependent manner, probably through binding to the active site and inducing positive cooperativity. CYP2C9 is subject to induction by rifampin, phenobarbital, and dexamethasone, indicating the involvement of pregnane X receptor, constitutive androstane receptor and glucocorticoid receptor in the regulation of CYP2C9. A number of compounds have been found to inhibit CYP2C9 and this may provide an explanation for some clinically important drug interactions. Tienilic acid, suprofen and silybin are mechanism-based inhibitors of CYP2C9. Given the critical role of CYP2C9 in drug metabolism and the presence of polymorphisms, it is important to identify drug candidates as potential substrates, inducer or inhibitors of CYP2C9 in drug development and drug discovery scientists should develop drugs with minimal interactions with this enzyme. Further studies are warranted to explore the molecular determinants for ligand-CYP2C9 binding and the structure-activity relationships.

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“…Even though a majority of patients show an initial 'response', in most studies, only about 50% demonstrate a clinically meaningful lowering of plasma glucose (for example, fasting glucose concentration below 7.8 mmol/L; Lebovitz 1985).…”

Section: Discussionmentioning

confidence: 99%

Continuous versus Intermittent Sulphonylurea Therapy in Non-Insulin-Dependent Diabetes Mellitus

Grunberger

1993

Drug Safety

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Although it is 50 years since the discovery of the hypoglycaemic effects of sulphonylureas, the molecular basis of their effects are still not fully understood. It has been suggested that long term sulphonylurea therapy may desensitise the pancreatic beta-cells to further drug effects, and that intermittent sulphonylurea therapy may be the best approach to maintain their effectiveness. A randomised, double-blind study has been carried out to attempt to answer the question of whether intermittent sulphonylurea therapy is more effective then continuous administration. Responders to oral glibenclamide (glyburide) went on to receive continuous or intermittent treatment (glibenclamide for 2 weeks then placebo for 2 weeks) for 16 weeks. Glycaemic control was maintained in the continuous treatment group. However, glucose levels deteriorated in the intermittent treatment group, suggesting that there is no merit to intermittent sulphonylurea treatment. Other strategies to investigate include administration on an alternate-day basis or a shorter period off the drug (e.g. 1 week). The underlying question of optimal glycaemic control with sulphonylureas warrants a definitive answer.

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Glipizide: A Second‐generation Sulfonylurea Hypoglycemic Agent; Pharmacology, Pharmacokinetics and Clinical Use

Cited by 48 publications

References 35 publications

Metformin and phenformin block the peripheral antinociception induced by diclofenac and indomethacin on the formalin test

Metformin and phenformin block the peripheral antinociception induced by diclofenac and indomethacin on the formalin test

Substrates, Inducers, Inhibitors and Structure-Activity Relationships of Human Cytochrome P450 2C9 and Implications in Drug Development

Continuous versus Intermittent Sulphonylurea Therapy in Non-Insulin-Dependent Diabetes Mellitus

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