sglt2 inhibitors

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

Elimination

Introduction Elimination is a pharmacokinetic process that describes the irreversible removal of active pharmaceutical ingredients from the body. It is composed of biotransformation (metabolism) and excretion (elimination). The most important organs for excretion are the kidney and the liver. However, drugs can also be excreted through the respiratory tract, hair, saliva, milk, tears, and sweat. … Elimination

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

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

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

Dapagliflozin

Products Dapagliflozin is commercially available in the form of film-coated tablets (Forxiga). It was approved in the EU in 2012 and in the United States and many countries in 2014. Dapagliflozin is also combined fixed with metformin (Xigduo XR). A fixed combination with saxagliptin was approved in 2017 (Qternmet film-coated tablets). Qternmet XR is a … Dapagliflozin

Remogliflozin

Structure and properties Remogliflozin (C23H32N2O8, Mr = 464.5 g/mol) is present in drugs as remogliflozinetabonate, an ester prodrug of remogliflozin. Effects Remogliflozin 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 glucose at the proximal tubule of the nephron. Inhibition leads … Remogliflozin

Canagliflozin

Products Canagliflozin is commercially available in the form of film-coated tablets (Invokana). It was approved in the United States and EU in 2013 and in many countries in 2014. Vokanamet is a fixed combination of canagliflozin and metformin. It was also registered in many countries in 2014. Structure and properties Canagliflozin (C24H25FO5S, Mr = 444.5 … Canagliflozin

Ipragliflozin

Products Ipragliflozin is not currently registered in many countries. It was first approved in Japan in 2014 (Suglat). Structure and properties Ipragliflozin (C21H21FO5S, Mr = 404.5 g/mol) is a benzthiophene derivative. Effects Ipragliflozin has antidiabetic and antihyperglycemic properties. It is a selective inhibitor of sodium–glucose co-transporter 2 (SGLT2). This transporter is responsible for the reabsorption … Ipragliflozin

Ertugliflozin

Products Ertugliflozin was approved in the United States in 2017 and in the EU and many countries in 2018 in film-coated tablet form (Steglatro). The agent is also combined fixed with sitagliptin (Steglujan) and with metformin (Segluromet). Structure and properties Ertugliflozin (C22H25ClO7, Mr = 436.9 g/mol) is present in the drug as ertugliflozin-L-pyroglutamic acid, a … Ertugliflozin

Me-Too Drugs

Definition and examples Me-too drugs are imitators of already approved and established drugs, which differ only slightly from their predecessors. Typical drug groups with many me-too drugs are the statins (e.g., pitavastatin), the ACE inhibitors (e.g., zofenopril), the sartans (e.g., azilsartan), and the SSRIs (e.g., vortioxetine). Me-too drugs are not generics, but active ingredients with … Me-Too Drugs

Phlorizin

Products No finished drug products containing phlorizin are commercially available in many countries. Phlorizin served as a precursor to modern SGLT2 inhibitors, which are antidiabetic drugs administered to treat type 2 diabetes. Structure and properties Phlorizin (C21H24O10, Mr = 436.4 g/mol) is a natural substance from apple tree bark. Effects Unlike modern SGLT2 inhibitors, phlorizin … Phlorizin