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

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

Gliptine

Products Gliptins are commercially available in the form of film-coated tablets. Sitagliptin (Januvia) was the first representative to be approved in the United States in 2006. Today, various active ingredients and combination products are commercially available (see below). They are also called dipeptidyl peptidase-4 inhibitors. Structure and properties Some gliptins have a proline-like structure because … Gliptine

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

Insulin Aspart

Products Insulin aspart is marketed as an injectable (NovoRapid, USA: NovoLog). It has been approved in many countries since 1999. The fixed combination IDegAsp (insulin aspart + insulin degludec, Ryzodeg) was registered in many countries and in the EU in 2013. In 2017, Fiasp ultra-fast-acting, a very fast-acting insulin aspart, was also approved. With the … Insulin Aspart

Insulin Detemir

Products Insulin detemir is commercially available as an injectable (Levemir). It has been approved in many countries since 2003. Structure and properties Insulin detemir (C267H402O76N64S6, Mr = 5916.9 g/mol) has an identical primary sequence to human insulin except for the removed threonine at position B30 of the B chain and an added molecule of myristic … Insulin Detemir

Insulin Glargine

Products Insulin glargine is commercially available as an injectable (Lantus). It has been approved in many countries since 2002. The biosimilar Abasaglar (LY2963016) was approved in the EU in 2014 and in many countries in 2015. The drugs must be stored between 2 to 8°C in a refrigerator. In 2015, Toujeo was additionally approved in … Insulin Glargine

Insulin Glulisine

Products Insulin glulisine is commercially available as an injectable and is usually administered with an insulin pen (Apidra). It has been approved in many countries since 2005. The brand name Apidra is derived from English (fast), and the active ingredient name glulisine is derived from the exchanged amino acids glutamic acid and lysine. Structure and … Insulin Glulisine

Insulin Lispro

Products Insulin lispro is commercially available as an injectable (Humalog). It has been approved in many countries since 1995. Biosimilars are available in some countries. In 2021, Lyumjev was approved in many countries, a new formulation that is characterized by an (even) faster onset of action and a slightly shorter duration of action. Structure and … Insulin Lispro