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ATC Group: A10B Blood glucose lowering drugs, excl. insulins

Anatomical Therapeutic Chemical Classification System

Hierarchical Position

Level
Code
Title
1
A
Alimentary tract and metabolism
2
A10
Drugs used in diabetes
3
A10B
Blood glucose lowering drugs, excl. insulins

Contents

Code
Title
A10BA
Biguanides
A10BB
Sulfonamides, urea derivatives
A10BC
Sulfonamides (heterocyclic)
A10BD
Combinations of oral blood glucose lowering drugs
A10BF
Alpha glucosidase inhibitors
A10BG
Thiazolidinediones
A10BH
Dipeptidyl peptidase 4 (DPP-4) inhibitors
A10BJ
Glucagon-like peptide-1 (GLP-1) analogues
A10BK
Sodium-glucose co-transporter 2 (SGLT2) inhibitors
A10BX
Other blood glucose lowering drugs, excl. insulins

Active Ingredients

Chemical substance
Description
Acarbose

Acarbose is an alpha-glucosidase inhibitors, used in the treatment of diabetes. Inhibitors of a-glucosidase retard the breakdown of carbohydrates in the food and reduce the increase in blood glucose levels, which occurs after each meal.

Alogliptin

Alogliptin is a potent and highly selective inhibitor of DPP-4, >10,000-fold more selective for DPP-4 than other related enzymes including DPP-8 and DPP-9. Alogliptin improves glycaemic control via a glucose-dependent mechanism, whereby insulin release is enhanced and glucagon levels are suppressed when glucose levels are high.

Canagliflozin

Canagliflozin is an orally-active inhibitor of SGLT2. The SGLT2 transporter, expressed in the proximal renal tubules, is responsible for the majority of the reabsorption of filtered glucose from the tubular lumen. By inhibiting SGLT2, canagliflozin reduces reabsorption of filtered glucose and lowers the renal threshold for glucose (RTG).

Chlorpropamide

Chlorpropamide is a sulfonylurea hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. It appears to lower the blood glucose acutely by stimulating the release of insulin from the pancreas, an effect dependent upon functioning beta cells in the pancreatic islets. The mechanism by which chlorpropamide lowers blood glucose during long-term administration has not been clearly established.

Dapagliflozin

Dapagliflozin is a highly potent, selective and reversible inhibitor of SGLT2. SGLT2 is the predominant transporter responsible for reabsorption of glucose from the glomerular filtrate back into the circulation. Dapagliflozin improves both fasting and post-prandial plasma glucose levels by reducing renal glucose reabsorption leading to urinary glucose excretion.

Dulaglutide

Dulaglutide is a long-acting glucagon-like peptide 1 (GLP-1) receptor agonist. In contrast to native GLP-1, dulaglutide is resistant to degradation by DPP-4, and has a large size that slows absorption and reduces renal clearance. Dulaglutide improves glycaemic control through the sustained effects of lowering fasting, pre-meal and postprandial glucose concentrations in patients with type 2 diabetes.

Empagliflozin

Empagliflozin is a reversible, highly potent (IC50 of 1.3 nmol) and selective competitive inhibitor of sodium-glucose co-transporter 2 (SGLT2). Empagliflozin improves glycaemic control in patients with type 2 diabetes by reducing renal glucose reabsorption.

Ertugliflozin

Ertugliflozin helps to lower blood glucose by making the patient pass out glucose in the urine. It does this by blocking a protein in the kidneys (called SGLT2) that normally takes glucose back into the blood from the kidneys.

Exenatide

Exenatide is a glucagon-like peptide-1 (GLP-1) receptor agonist that exhibits several antihyperglycaemic actions of glucagon-like peptide-1 (GLP-1). The amino acid sequence of exenatide partially overlaps that of human GLP-1. Exenatide has been shown to bind to and activate the known human GLP-1 receptor in vitro, its mechanism of action mediated by cyclic AMP and/or other intracellular signalling pathways. Exenatide increases, on a glucose-dependent basis, the secretion of insulin from pancreatic beta cells.

Glibenclamide

Glibenclamide, a second-generation, short half-life sulphonylurea, is a hypoglycaemic agent that reduces blood-glucose by stimulating insulin release by the pancreas.

Gliclazide

Gliclazide is a hypoglycaemic sulfonylurea antidiabetic active substance. Gliclazide reduces blood glucose levels by stimulating insulin secretion from the β-cells of the islets of Langerhans.

Glimepiride

Glimepiride is an orally active hypoglycaemic substance belonging to the sulphonylurea group. It may be used in non-insulin dependent (type 2) diabetes mellitus. Glimepiride acts mainly by stimulating insulin release from pancreatic beta cells.

Glipizide

Glipizide is an oral blood-glucose-lowering drug of the sulfonylurea class. The primary mode of action of glipizide is the stimulation of insulin secretion from the beta-cells of pancreatic islet tissue.

Gliquidone

Gliquidone is an anti-diabetic drug in the sulfonylurea class. It is used in the treatment of diabetes mellitus type 2. It is an ATP-dependent K+ (KATP) channel blocker. This block causes a depolarization which leads to activation of voltage-dependent Ca channels and Ca2+ influx, and eventually increases insulin release.

Linagliptin

Linagliptin is an inhibitor of the enzyme DPP-4 (dipeptidyl peptidase 4, EC 3.4.14.5) an enzyme which is involved in the inactivation of the incretin hormones GLP-1 and GIP (glucagon-like peptide1, glucose-dependent insulinotropic polypeptide). These hormones are rapidly degraded by the enzyme DPP-4. Both incretin hormones are involved in the physiological regulation of glucose homeostasis.

Liraglutide

Liraglutide is a GLP-1 analogue with 97% sequence homology to human GLP-1 that binds to and activates the GLP-1 receptor. The GLP-1 receptor is the target for native GLP-1, an endogenous incretin hormone that potentiates glucose-dependent insulin secretion from the pancreatic beta cells. Unlike native GLP-1, liraglutide has a pharmacokinetic and pharmacodynamic profile in humans suitable for once daily administration.

Lixisenatide

Lixisenatide is a selective GLP-1 receptor agonist. The GLP-1 receptor is the target for native GLP-1, an endogenous incretin hormone that potentiates glucose-dependent insulin secretion from the pancreatic beta cells.

Metformin

Metformin is a biguanide with antihyperglycaemic effects, lowering both basal and postprandial plasma glucose. It does not stimulate insulin secretion and therefore does not produce hypoglycaemia.

Miglitol

Miglitol is a reversible inhibitor of intestinal alpha-glucosidases. Under the influence of miglitol, the digestion of complex carbohydrates into absorbable monosaccharides in the small intestine is dosedependently delayed. Administration of miglitol thus leads to reduced postprandial hyperglycaemia and a smoothing effect on fluctuations in the daily blood glucose profile.

Nateglinide

Nateglinide is an amino acid (phenylalanine) derivative, which is chemically and pharmacologically distinct from other antidiabetic agents. Nateglinide is a rapid, short-acting oral insulin secretagogue. Its effect is dependent on functioning beta cells in the pancreas islets.

Phenformin

Phenformin is a biguanide hypoglycemic agent with actions and uses similar to those of metformin. It activates AMP-activated protein kinase (AMPK) and inhibits mTORC1 signaling. Phenformin used for the treatment of diabetes. Phenformin exerts potential anti-neoplastic action.

Pioglitazone

Pioglitazone effects may be mediated by a reduction of insulin resistance. Pioglitazone appears to act via activation of specific nuclear receptors (peroxisome proliferator activated receptor gamma) leading to increased insulin sensitivity of liver, fat and skeletal muscle cells in animals. Treatment with pioglitazone has been shown to reduce hepatic glucose output and to increase peripheral glucose disposal in the case of insulin resistance.

Pramlintide

Pramlintide is an analog of human amylin. In human studies, pramlintide, acting as an amylin analog, slows gastric emptying, reduces the postprandial rise in plasma glucagon, and modulates satiety leading to decreased caloric intake.

Repaglinide

Repaglinide is a short-acting oral secretagogue. Repaglinide lowers the blood glucose levels acutely by stimulating the release of insulin from the pancreas, an effect dependent upon functioning β-cells in the pancreatic islets.

Rosiglitazone

Rosiglitazone is a selective agonist at the PPARγ (peroxisomal proliferator activated receptor gamma) nuclear receptor and is a member of the thiazolidinedione class of anti-diabetic agents. It reduces glycaemia by reducing insulin resistance at adipose tissue, skeletal muscle and liver.

Saxagliptin

Saxagliptin is a highly potent (Ki: 1.3 nM), selective, reversible, competitive, DPP4 inhibitor. Saxagliptin improves glycaemic control by reducing fasting and postprandial glucose concentrations in patients with type 2 diabetes.

Semaglutide

Semaglutide is a GLP-1 receptor agonist. It acts in the same way as GLP-1 (a hormone produced in the gut) by increasing the amount of insulin that the pancreas releases in response to food. This helps with the control of blood glucose levels.

Sitagliptin

Sitagliptin is a member of a class of oral anti-hyperglycaemic agents called dipeptidyl peptidase 4 (DPP-4) inhibitors. The improvement in glycaemic control observed with this medicinal product may be mediated by enhancing the levels of active incretin hormones.

Sotagliflozin

Sotagliflozin is a dual inhibitor of sodium glucose cotransporter type 1 (SGLT1) and SGLT2. Local intestinal inhibition of SGLT1, the major transporter for glucose absorption, delays and reduces glucose absorption in the proximal intestine, resulting in a blunting and delay of postprandial hyperglycaemia.

Tolbutamide

Tolbutamide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). It is structurally similar to acetohexamide, chlorpropamide and tolazamide and belongs to the sulfonylurea class of insulin secretagogues, which act by stimulating β cells of the pancreas to release insulin.

Vildagliptin

Vildagliptin enhances the sensitivity of beta cells to glucose, resulting in improved glucose-dependent insulin secretion by increasing the endogenous levels of these incretin hormones. The administration of vildagliptin results in a rapid and complete inhibition of DPP-4 activity, resulting in increased fasting and postprandial endogenous levels of the incretin hormones GLP-1 (glucagon-like peptide 1) and GIP (glucose-dependent insulinotropic polypeptide).

Monographs

Monograph
Type
Country
ACTOS Tablet
MPI, US: SPL/PLR
US
AMARYL Tablet
MPI, US: SPL/PLR
US
AMGLIDIA Oral suspension
MPI, EU: SmPC
UK
AVANDIA Film-coated tablet
MPI, US: SPL/PLR
US
BYETTA Solution for injection
MPI, EU: SmPC
COMPETACT Film-coated tablet
MPI, EU: SmPC
EUCREAS Film-coated tablet
MPI, EU: SmPC
FORXIGA Film-coated tablets
MPI, EU: SmPC
GLICLAZIDE Tablets
MPI, EU: SmPC
UK
GLUCOBAY 50mg Tablet
MPI, EU: SmPC
UK
GLUCOPHAGE / GLUCOPHAGE XR Tablet / Extended-release tablet
MPI, US: SPL/PLR
US
GLUCOTROL Tablet
MPI, US: SPL/Old
US
GLUCOTROL XL Extended-release tablet
MPI, US: SPL/PLR
US
GLUMETZA Film coated tablet, extended release
MPI, US: SPL/PLR
US
INVOKANA Film-coated tablets
MPI, EU: SmPC
JALRA Tablet
MPI, EU: SmPC
JANUMET Film-coated tablet
MPI, EU: SmPC
JANUVIA Film-coated tablets
MPI, EU: SmPC
JARDIANCE Film-coated tablets
MPI, EU: SmPC
JENTADUETO Film-coated tablet
MPI, EU: SmPC
KOMBOGLYZE Film-coated tablet
MPI, EU: SmPC
LYXUMIA Solution for injection
MPI, EU: SmPC
METFORMIN Oral Solution
MPI, EU: SmPC
UK
NESINA Film-coated tablet
MPI, US: SPL/PLR
US
ONGLYZA Film-coated tablets
MPI, EU: SmPC
OZEMPIC Solution for injection
MPI, EU: SmPC
PIOGLITAZONE ACCORD Tablet
MPI, EU: SmPC
UK
PRANDIN Tablet
MPI, US: SPL/PLR
US
QTERN Film-coated tablets
MPI, EU: SmPC
REPAGLINIDE Tablet
MPI, EU: SmPC
UK
RYBELSUS Tablet
MPI, US: SPL/PLR
US
STARLIX Film-coated tablets
MPI, EU: SmPC
STEGLATRO Film-coated tablet
MPI, EU: SmPC
TRAJENTA Film-coated tablets
MPI, EU: SmPC
TRULICITY Solution for injection
MPI, EU: SmPC
VICTOZA Solution for injection
MPI, EU: SmPC
VIPIDIA Film-coated tablets
MPI, EU: SmPC
ZYNQUISTA Film-coated tablet
MPI, EU: SmPC