Tuesday, August 6, 2019

Glucagon-like peptide-1 (GLP-1) receptor agonists

Hello everyone!

Let's talk about glucagon-like peptide-1 (GLP-1) receptor agonists today!

Background on pharmacology and mechanism of action: Incretins are hormones produced by the intestinal mucosa in response to oral intake of nutrients that enhance glucose-stimulated insulin secretion and lower blood glucose levels.

Incretins also reduce insulin release when glucose levels are near normal. They also slow gastric emptying and suppress secretion of glucagon.

Two incretin hormones have been identified: glucose-dependent insulinotropic polypeptide and glucagon-like peptide 1 (GLP-1).

Administration of GLP-1 receptor agonists stimulates GLP-1 receptors, thereby increasing insulin secretion.

The GLP-1RAs are peptide-based therapies and therefore, such as insulin, require subcutaneous injection to avoid degradation by gastrointestinal enzymes.

Short-acting agents: 
Exenatide twice daily (BID)

Liraglutide (administered once daily)

Long-acting agents administered once weekly (QW):
Exenatide QW

Mnemonic: A tide of insulin is secreted after GLP1RA reaches the receptor shores. Exenatide liraglutide, etc.

Clinical use: According to the AACE/ACE and ADA diabetes treatment algorithms for glycemic control, GLP-1RAs are recommended as add-on therapy for patients who do not achieve their A1C target after 3 months of metformin therapy. GLP-1RAs also are recommended as first-line therapy as an alternative to metformin in patients who cannot tolerate or are contraindicated for metformin.

Nausea: Nausea with GLP-1RAs often occurs early in GLP-1 RA therapy and can be limited using an incremental dosing approach

Weight loss: Body weight reduction was a common effect observed in clinical trials evaluating GLP-1RAs in patients with type 2 diabetes. Weight loss in patients receiving GLP-1RAs is thought to occur as a result of slowed gastric emptying and increased satiety.
Mnemonic:  "Tide" is an anagram for "diet" - so tides cause increased satiety and reduce diet :D

Low risk of hypoglycemia: GLP-1RAs are well suited for early use in type 2 diabetes because they stimulate release of insulin and suppress glucagon secretion only when blood glucose concentrations are elevated; thus, the risk of hypoglycemia is low.

Renal function: Use with caution in patients with severe renal impairment.

Potential concerns: Development of pancreatitis and medullary thyroid carcinoma.

That's all!

More mnemonics:
GLP-1 analogues mnemonics
Mechanisms of oral hypoglycemic drugs used for diabetes mellitus mnemonic
Oral hypoglycemic drugs and weight - Weight gain or weight loss mnemonic

Glucagon-Like Peptide 1 Receptor Agonists for Type 2 Diabetes
GLP-1 receptor agonists vs. DPP-4 inhibitors for type 2 diabetes: is one approach more successful or preferable than the other?

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