blood glucose-lowering

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

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

Inhalable Insulin

Products An inhalable insulin preparation containing a rapid-acting human insulin was approved in the United States in 2014 (Afrezza, powder inhalation). The drug has not yet been registered in many countries. Pfizer’s first inhalable insulin Exubera was withdrawn from the market in 2007 for commercial reasons; see Exubera. Structure and properties Human insulin (C257H383N65O77S6, Mr … Inhalable Insulin

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

Empagliflozin

Products Empagliflozin is commercially available in the form of film-coated tablets. It was approved in the EU, the United States, and many countries in 2014 (Jardiance). Empagliflozin is also combined fixed with metformin (Jardiance Met) as well as with linagliptin (Glyxambi). Trijardy XR is a fixed combination of empagliflozin, linagliptin, and metformin. Structure and properties … Empagliflozin

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

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

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)

Tofogliflozin

Products Tofogliflozin was approved in Japan in 2014 (initial registration, Apleway, Deberza). The drug is not currently registered in many countries. Structure and properties Tofogliflozin (C22H26O6, Mr = 386.4 g/mol) Effects Tofogliflozin has antidiabetic and antihyperglycemic properties. It is a selective inhibitor of sodium–glucose co-transporter 2 (SGLT2). This transporter is responsible for the reabsorption of … Tofogliflozin

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 Degludec

Products Insulin degludec is commercially available as a solution for injection (Tresiba). It is also combined fixed with insulin aspart (Ryzodeg, see under IDegAsp). It was newly approved in many countries in March 2013. In 2014, a fixed combination with liraglutide was registered (Xultophy); see under IDegLira. Structure and properties Insulin degludec has essentially the … Insulin Degludec