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

Diabetes Mellitus Type 2: Causes and Treatment

Symptoms The possible acute symptoms of type 2 diabetes include: Thirst (polydipsia) and hunger (polyphagia). Increased urination (polyuria). Visual disturbances Weight loss Fatigue, exhaustion, declining performance. Poor wound healing, infectious diseases. Skin lesions, itching Acute complications: Hyperacidity (ketoacidosis), hyperosmolar hyperglycemic syndrome. Untreated diabetes is far from harmless and can lead in the longer term to … Diabetes Mellitus Type 2: Causes and Treatment

Glibenclamide

Products Glibenclamide is commercially available in tablet form (Daonil, generics). It has been approved in many countries since 1970 and is also used in fixed combination with metformin (Glucovance). Structure and properties Glibenclamide (C23H28ClN3O5S, Mr = 494.0 g/mol) is a sulfonylurea. It exists as a white crystalline powder that is practically insoluble in water. Effects … Glibenclamide

Gliclazide

Products Gliclazide has been commercially available in sustained-release tablet form and approved in many countries since 1978. The sustained-release dosage forms entered the market in 2001. In addition to the original Diamicron MR, sustained-release generics have been available since 2008. Sales of the non-retarded Diamicron 80 mg were discontinued in 2012. Structure and properties Gliclazide … Gliclazide

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

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