Sulfonylurea

In 1942, the first sulfonylurea (SU) VK 57 was investigated in the Section of Infectious Diseases, Montpellier Hospital, France [9]. A few years later, that compound was shown to induce neoformation of insulin granules in rat beta cells. Since 1954 SUs (Fig. 1) have been available in the USA [10] and for many years they have been remained the most popular pharmacological drug in the treatment of diabetes mellitus. First-generation SUs include chlorpropamide, tolbutamide, tolazamide and acetohexamide and are now rarely used. They have a lower binding affinity to the sulfonylurea receptor and must therefore be given in higher doses than second-generation SUs like glibenclamide (=glyburide), glipizide, gliquidone, glimepiride and gliclazide (Table 1). In addition, the major side effect - hypoglycaemia - occurs more frequently in the longer-acting first-generation SUs [10-14].

Most guidelines like the 1999 IDF [15], the 2004 American Diabetes Association [16] as well as European national guidelines recommend SUs as first-choice monotherapy as well as combination-therapy with other antidiabetic drugs. As second-generation SUs seem to be safer, but essentially of equal efficacy [17], they have been preferred in most countries during the last years.

Fig. 1. Common chemical structure of sulfonylureas.

Table 1. Overview of first- and second-generation sulfonylureas as well as non-SU secretagogues.

Daily dosage

Duratio zn of action

Drug

(mg)

Ingestion per day

(h)

First-generation sulfonylureas

Chlorpropamide

100-500

Once

60

Tolbutamide

500-2,000

Once

6-12

Tolazamide

100-1,000

Once

12-24

Acetohexamide

250-1,500

Once

12-18

Second-generation sulfonylureas

Glibenclamide

2.5-20

Twice (or three times)

16-24

Glipizide

5-20 (40)

Once

12-24

Gliquidone

15-180

Twice

12-16

Glimepiride

1-8

Once (twice)

16-24

Gliclazide

40-240

Once (twice)

16-24

Gliclazide MR

30-120

Once

16-24

Non-SU secretagogues

Repaglinide

1.5-12

Three times

1-2

Nateglinide

180-540

Three times

1-2

Supplements For Diabetics

Supplements For Diabetics

All you need is a proper diet of fresh fruits and vegetables and get plenty of exercise and you'll be fine. Ever heard those words from your doctor? If that's all heshe recommends then you're missing out an important ingredient for health that he's not telling you. Fact is that you can adhere to the strictest diet, watch everything you eat and get the exercise of amarathon runner and still come down with diabetic complications. Diet, exercise and standard drug treatments simply aren't enough to help keep your diabetes under control.

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