Sulfonylureas: Drug Effects, Side Effects, Dosage and Uses

Effects Sulfonylureas (ATC A10BB) have antidiabetic, antihyperglycemic, and insulin secretagogue properties. Active Ingredients 1st generation: Tolbutamide, acetohexamide, tolazamide (all off-label). Chlorpropamide (Diabiformin, out of commerce). 2nd generation: Glibenclamide (Daonil, generic). Glibornuride (Glutril, off label). Glipizide (Glibenese, out of trade) Gliclazide (Diamicron /-MR, generic). 3rd generation: Glimepiride (Amaryl, generic). Cf. Diabetes mellitus type 2, glinides

Glimepiride

Products Glimepiride is commercially available in tablet form (Amaryl, generic). It has been approved in many countries since 1995. Structure and properties Glimepiride (C24H34N4O5S, Mr = 490.62 g/mol) exists as a white to yellowish-white, crystalline and odorless powder that is practically insoluble in water. It belongs structurally to the sulfonylureas. Effects Glimepiride (ATC A10BB12) has … Glimepiride

Thiazolidinediones (Glitazones)

Effects Glitazones are antidiabetic, antihyperglycemic, and antihyperglycemic, i.e., they decrease insulin resistance. Glitazones are selective and potent agonists at nuclear PPAR-γ. They improve glycemic control by enhancing insulin sensitivity in adipose tissue, skeletal muscle, and liver. Indications Type 2 diabetes mellitus Active ingredients Pioglitazone (Actos) Rosiglitazone (Avandia, off label). Troglitazone (Rezulin, out of commerce, liver … Thiazolidinediones (Glitazones)

Antidiabetics

Active ingredients Insulins substitute for endogenous insulin: Human insulin Insulin analogues Biguanides reduce hepatic glucose formation: Metformin (Glucophage, generic). Sulfonylureas promote insulin secretion from beta cells: Glibenclamide (Daonil, generic). Glibornuride (Glutril, off label). Gliclazide (Diamicron, generic). Glimepiride (Amaryl, generics) Glinides promote insulin secretion from beta cells: Repaglinide (NovoNorm, generic). Nateglinide (Starlix) Glitazones decrease peripheral insulin … Antidiabetics

Sulfonylureas

Synonyms Drugs Diabetes mellitus, diabetes drugs, glibenclamide (e.g. Euglucon ®N), glimepiride (e.g. Amaryl®), gliquidone (e.g. Glurenorm®) How do sulfonylureas work? Sulfonylureas stimulate the pancreas to release more insulin. The prerequisite for this, however, is that the beta cells of the pancreas are still capable of producing insulin themselves. When the pancreas is no longer able … Sulfonylureas

When should sulfonylureas not be taken ? | Sulfonylureas

When should sulfonylureas not be taken ? Sulfonylureas must not be taken in case of hypersensitivity to drugs of the sulfonamide type. These include antibiotics used for urinary tract infections (Cotrimoxazole). Some medicines for high blood pressure (diuretics) have a similar origin and have been discontinued by some people due to hypersensitivity. Your doctor will … When should sulfonylureas not be taken ? | Sulfonylureas

Rosiglitazone

Products Rosiglitazone was commercially available in tablet form (Avandia). It had been approved since 1999 and was also commercially available in fixed combination with the biguanide metformin (Avandamet). The combination with the sulfonylurea glimepiride (Avaglim, EU, off-label) was not approved in many countries. A publication in on possible cardiovascular risks led to a controversy about … Rosiglitazone

Amaryl®

Glimepiride, antidiabetic, sulfonylureaAmaryl® is a so-called antidiabetic and is used to lower permanently high blood sugar levels. It should only be used when a suitable diet, additional exercise and weight loss are not sufficient to lower blood sugar levels adequately. Amaryl® contains the active ingredient glimepiride and is suitable exclusively for type 2 diabetics, as … Amaryl®