Acarbose Effects and Side Effects

Products Acarbose is commercially available in tablet form (Glucobay). It is usually combined with other agents such as metformin, insulin, or sulfonylureas to enhance the antidiabetic effect. Acarbose has been approved in many countries since 1986. Structure and properties Acarbose (C25H43NO18, Mr = 645.60 g/mol) is a pseudotetrasaccharide obtained from the bacterium by fermentation. It … Acarbose Effects and Side Effects

GLP-1 Receptor Agonists

Products The first agent in the GLP-1 receptor agonist group to be approved was exenatide (Byetta) in the United States in 2005 and in many countries and the EU in 2006. In the meantime, several other drugs have been registered (see below). These drugs are also known as incretin mimetics. They are commercially available as … GLP-1 Receptor Agonists

Exenatide

Products Exenatide is commercially available as an injectable (Byetta, Bydureon). It was approved in the United States in 2005 as the first agent in the GLP-1 receptor agonist group (Byetta). In many countries, the drug was registered a year later. The long-acting Bydureon Pen was approved in many countries in 2012, with additional approval as … Exenatide

Lixisenatide

Products Lixisenatide was approved as a subcutaneous solution for injection in the EU in 2012, in the United States in 2016, and in many countries in 2017 (Lyxumia). Lixisenatide is also combined with insulin glargine; see iGlarLixi (Suliqua). Structure and properties Lixisenatide is a peptide and GLP1 analog of 44 amino acids that, like exenatide, … Lixisenatide

Liraglutide

Products Liraglutide was approved in many countries in 2009 as a solution for injection in a prefilled pen (Victoza). In 2014, a fixed-dose combination with insulin degludec was released (Xultophy); see IDegLira. In 2016, Saxenda was registered for the treatment of overweight and obesity. Its related successor, semaglutide, unlike liraglutide, only needs to be injected … Liraglutide

Repaglinide

Products Repaglinide is commercially available in tablet form (NovoNorm, generic). It was approved in many countries in 1999. Structure and properties Repaglinide (C27H36N2O4, Mr = 452.6 g/mol) is a meglitinide and carbamoylmethylbenzoic acid derivative without sulfonylurea structure. It is a white, odorless powder that is practically insoluble in water due to its lipophilicity. In drugs, … Repaglinide

Glibornuride

Products Glibornuride was commercially available in tablet form (Glutril, originally Roche, later MEDA Pharma). It was approved in many countries since 1971. It was discontinued in 2019. Structure and properties Glibornuride (C18H26N2O4S, Mr = 366.48 g/mol) is a sulfonylurea. Effects Glibornuride (ATC A10BB04) has antihyperglycemic and antidiabetic properties. The effects are due to the promotion … Glibornuride

Glinides (Meglitinides): Diabetes Drugs

Products Glinides are commercially available in tablet form. Repaglinide (NovoNorm, USA: 1997) was the first to be approved in many countries in 1999, and nateglinide (Starlix) was approved a year later in 2000. Structure and properties The glinides differ structurally from the sulfonylureas. They are also referred to as meglitinide analogs. Repaglinide is a carbamoylmethylbenzoic … Glinides (Meglitinides): Diabetes Drugs

Glipizide

Products Glibenese is no longer commercially available in many countries. Numerous other sulfonylureas and antidiabetic agents are available as alternatives. Structure and properties Glipizide (C21H27N5O4S, Mr = 445.54 g/mol) is a white to almost white crystalline powder that is practically insoluble in water. Effects Glipizide (ATC A10BB07) is antidiabetic; see under sulfonylureas. Indications Type II … Glipizide

Glitazare

Effects Glitazars combine the lipid-lowering effects of fibrates (lower triglycerides and LDL, increase HDL) with the antidiabetic effect of glitazones, which increase tissue sensitivity to insulin. Mechanism of action Glitazars have a dual mechanism of action. On the one hand, they activate the nuclear receptor PPAR-alpha, the drug target of fibrates, and on the other … Glitazare

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)

Nateglinide

Products Nateglinide is commercially available in the form of film-coated tablets (Starlix, Starlix mite). It has been approved in many countries since 2000. Structure and properties Nateglinide (C19H27NO3, Mr = 317.42 g/mol) is a cyclohexane derivative of the amino acid phenylalanine. It is a white powder that is practically insoluble in water. Effects Nateglinide (ATC … Nateglinide