Pharmacology of diabetes Flashcards
What is the first line treatment for diabetes?
Lifestyle changes
What are the different mediations for diabetes?
-Metformin
-Dipeptidyl peptidase 4 (DPP-4) inhibitor
-Sulphonylurea
-Sodium glucose cotransporter (SGLT2) inhibitors
What is the first line medication for diabetes?
Metformin
What is AMPK?
AMP activated protein kinase
(An enzyme involved in metabolic processes)
What is the primary mechanism of action of metformin?
- Metformin activates AMPK in hepatocyte mitochondria
- This inhibits ATP production
3a. Blocks gluconeogenesis and subsequent glucose output
3b. Blocks adenylate cyclase which promotes fat oxidation - Both help to restore insulin sensitivity
What is the drug target of metformin?
AMPK in hepatocyte mitochondria
What are the main side effects of metformin?
-GI side effects
(20-30% of patients)
What are examples of GI side effects?
-Abdominal pain
-Decreased appetite
-Diarrhoea
-Vomiting
When are these side effects observed?
When very high doses are administered
How can side effects be diminished?
Slow increase in dose
What does metformin require to access tissues?
Organic cation transporter 1 (OCT-1) as metformin is highly polar
How does the characteristics of metformin allow it to have its therapeutic effect?
It is polar so accumulates in the liver
When is metformin most effective?
In the presence of endogenous insulin
What is Dipeptidyl-peptidase 4?
An enzyme which is responsible for breaking down incretin hormones
What are incretin hormones?
Gut peptides that stimulate insulin secretion when the body is in a hyperglycaemic state after food intake