Sulfonylureas and meglitinides: insights into physiology and translational clinical utility

Melander, Arne

doi:10.1002/9781118387658.ch42

Cited by 3 publications

(14 citation statements)

References 189 publications

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“…Numerous studies comparing relative risks of hypoglycaemia between different SUs consistently show glibenclamide/glyburide to have the highest risk, an intermediate risk with glimepiride and glipizide, and the least risk with gliclazide . The risk of SU‐mediated hypoglycaemia is greatest in patients with T2DM who are elderly, poorly nourished, or who have cardiovascular or renal disease . As discussed, the risk of hypoglycaemia increases when SUs are used in combination with certain other drugs.…”

Section: Sulphonylureasmentioning

confidence: 97%

“…The effect of SUs is the result of the timing and magnitude of their insulin secretion and its independence on ambient glucose concentrations. They do not correct the delay in first‐phase insulin secretion, but primarily increase second‐phase insulin secretion . This, plus the independence of their stimulation of insulin secretion on glucose concentrations, are the cause of the frequently associated hypoglycaemia and weight gain.…”

Section: Sulphonylureasmentioning

confidence: 99%

“…glibenclamide (glyburide in the USA), glipizide, gliclazide and glimepiride] in the late 1960s/1970s and 1980s [80]. Just as DPP-4 inhibitors are a heterogeneous group, so too do SUs vary in their pharmacokinetic and pharmacodynamic characteristics [80]. Sulphonylyreas work by binding to the sulphonylurea receptor (SUR)-1 subunit of pancreatic -cell ATP-sensitive potassium (K ATP ) channels, leading to their closure; the resultant membrane depolarization opens voltage-dependent calcium channels, causing intracellular calcium concentrations to increase, with subsequent release of insulin [81,82].…”

Section: Sulphonylureasmentioning

confidence: 99%

“…SU-mediated hypoglycaemia is a relatively frequent occurrence and has been shown to be a cause of significant use of emergency services, emergency ward visits and hospitalizations [96,97]. Severe hypoglycaemia tends to be relatively resistant to acute glucose administration and may be recurrent for 12-72 h. Such episodes generally require medical treatment for several days [80]. Sulphonylureas are implicated with adverse effects related to the increased risk of hypoglycaemia.…”

Section: Safetymentioning

confidence: 99%

“…First generation SUs (e.g. tolbutamide and chlorpropamide), introduced during the early 1960s, are now infrequently used in current clinical practice . They were followed by second generation SUs [e.g.…”

Section: Sulphonylureasmentioning

confidence: 99%

See 4 more Smart Citations

Comparative review of dipeptidyl peptidase‐4 inhibitors and sulphonylureas

Deacon

Lebovitz

2016

Diabetes Obesity Metabolism

182

139

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Type 2 diabetes (T2DM) is a progressive disease, and pharmacotherapy with a single agent does not generally provide durable glycaemic control over the long term. Sulphonylurea (SU) drugs have a history stretching back over 60 years, and have traditionally been the mainstay choice as second-line agents to be added to metformin once glycaemic control with metformin monotherapy deteriorates; however, they are associated with undesirable side effects, including increased hypoglycaemia risk and weight gain. Dipeptidyl peptidase (DPP)-4 inhibitors are, by comparison, more recent, with the first compound being launched in 2006, but the class now globally encompasses at least 11 different compounds. DPP-4 inhibitors improve glycaemic control with similar efficacy to SUs, but do not usually provoke hypoglycaemia or weight gain, are relatively free from adverse side effects, and have recently been shown not to increase cardiovascular risk in large prospective safety trials. Because of these factors, DPP-4 inhibitors have become an established therapy for T2DM and are increasingly being positioned earlier in treatment algorithms. The present article reviews these two classes of oral antidiabetic drugs (DPP-4 inhibitors and SUs), highlighting differences and similarities between members of the same class, as well as discussing the potential advantages and disadvantages of the two drug classes. While both classes have their merits, the choice of which to use depends on the characteristics of each individual patient; however, for the majority of patients, DPP-4 inhibitors are now the preferred choice.

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Section: Sulphonylureasmentioning

confidence: 97%

Section: Sulphonylureasmentioning

confidence: 99%