Anti-diabetes Drugs

The new anti-diabetes drug GLP-1 receptor agonists

March 31, 2012 Diabetes, Drug Informatics, Pharmacology 1 comment , , ,

A GLP-1R agonist Exenatide approved by FDA.

This article comes from references available on internet. It is about a new drug called Glucagon-like Peptide-1 [GLP-1] Receptor Agonists.

So GLP-1R Agonists is analog of human glucagon-like peptide-1, and it acts as GLP-1 receptor agonist to increase insulin secretion in the presence of elevated blood glucose. Also it delays gastric emptying to decrease postprandial glucose and decreases glucagon secretion.

So what is Glucagon-like Peptide-1 [GLP-1]?

GLP-1 is one kind of native human hormones called Incretins, which is produced by the proglucagon gene in L-cells of the small intestine. GLP-1 decreases and control blood glucose by various mechanism including: [1].Liver: reduces hepatic glucose output by inhibiting glucagon release. [2]. Alpha cell: inhibits glucagon secretion. [3].CNS: promotes satiety. [4].Stomach: slows gastric emptying. [5].Beta cell: stimulates glucose-dependent insulin secretion and beta-cell differentiation and proliferation.

Thus, modulating GLP-1 levels and GLP-1 activity through administration of the native hormone, analogs, and mimetics or by inhibiting its degradation has become a major focus of investigation for treating type 2 diabetes over the past decade.

Another important thing, where can we find the receptor of GLP-1?

The receptor is found on pancreatic periductal cells and β-cells and in the kidney, heart, stomach, and brain. GLP-1 receptor (GLP-1R) knockout mice have fasting hyperglycemia and abnormal glucose tolerance but are not obese.


[1].Medscape: Guideline Discusses Oral Pharmacotherapy for Type 2 Diabetes. Full reference:
[2].Glucagon-Like Peptide 1-Based Therapies for Type 2 Diabetes: A Focus on Exenatide. Full reference:
[3].Glucagon-Like Peptide-1 Receptor Agonists Promote Weight Loss. Full reference:

Guideline discusses oral pharmacotherapy for Type 2 diabetes

March 29, 2012 Diabetes, Pharmacology, Therapeutics No comments , ,

In this article the author disscuss several oral anti-diabetes drugs, including:

  • Metformin
  • Sulfonylureas
  • Meglitinides
  • Thiazolidinediones
  • Dipeptidyl Peptidase-4 [DPP-4] inhibitors
  • Glucagon-like Peptide-1 [GLP-1] Receptor Antagonists Note: According relative references I think Medscape have made a mistake. It should be Agonists instead of Antagonists.

I reviewed my pharmacology textbooks (a very old version) and found there were only four types of oral anti-diabetes drugs. They are Biguanides, Sulfonylureas, and α-glucosidase inhibitor. I searched on Medscape for the other types of oral anti-diabetes drug and what I found nothing. So I tried to serach on WebMD and Medscape for “Meglitinides” “Thiazolidinediones” “Dipeptidyl Peptidase-4 [DPP-4] inhibitors” “Glucagon-like Peptide-1 [GLP-1] Receptor Antagonists“. Note: It should be Agonists here

Oral anti-diabetes drugs.

Here is what I found on WebMD and Medscape:

Meglitinides includes Nateglinide and Repaglinide. Meglitinides works via increasing the amount of insulin produced by the pancreas. It’s similar to the way sulfonylureas works.

Thiazolidinediones includes Pioglitazone and Rosiglitazone. How dose Thiazolidinediones work is not well understood so far. But we do know that it works via improving the way cells in the body respond to insulin (or lowering insulin resistance). By the way Pioglitazone may help in the treatment of high cholesterol by reducing triglycerides and increasing high-density lipoproteins (HDL) in the blood. Rosiglitazone increases high-density lipoproteins (HDL) and slightly increases low-density lipoproteins (LDL).

Dipeptidyl Peptidase-4 [DPP-4] inhibitors includes Saxagliptin and Sitagliptin. They work via helping your body make more insulin after a meal. They also reduce blood sugar your body makes. They can make these effects by increasing and prolonging incretin hormone activity which are inactivated by DPP-4 enzyme.

PS: Incretins increase insulin release and synthesis from pancreatic beta cells and reduce glucagon secretion pancreatic alpha cells.

About Glucagon-like Peptide-1 [GLP-1] Receptor Antagonists, Note: It should be Agonists here there are some different opinions on internet. So I do not post the information about GLP-1 Receptor Antagonists. Maybe one key word was typed mistakenly. I have sent tweets to my friend for confirming. (more…)