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

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