Glitazones - Actos (pioglitazone ) Avandia ( rosiglitazone )
Hint - it is time to retire and join sulfonylureas in the" has been" room
I loved the mechanism of action and hated the side effects. I will outline the mechanism of action below for anyone other than me who may be interested. I was shocked to learn that ACTOS is one of the most commonly prescribed drugs in the world for treatment of Type 2 Diabetes .
I never prescribed Avandi because I did not like its effect on lipids but I did use ACTOS in a limited manor. The side effects of edema (swelling ) , weight gain and the tendency be associated with congestive heart failure in older people limited its usefulness in my patients.
Both drugs now have FDA warnings
AVANDIA for it's association with increase risk of heart disease
ACTOS with a possible like to bladder cancer.
We have better safer medications .
Mechanism of Action with " light "((embellishment to make a better story
One good thing about these two drugs is this mechanism of action that caught my attention a few years ago.A researcher using sophisticated imaging techniques was able to demonstrate the process discussed below.I am not sure if this research was confirmed by others.
Insulin connects to a insulin receptor on a cell . This signals the nucleus ( the business office ) in the cell to send a message to the Glut 4 transporters ( the Teamsters ) to go out to the surface of the cell and pick up a glucose molecule and return it to the office ( nucleus) to be used for fuel .
Type 2 diabetes
The business office in the cell ( the nucleus ) is not efficient and fails to send a memo to the Teamsters to make the trip. This results in glucose piling up on the loading dock outside the cell and an increase in blood glucose levels.
ACTOS is hired as an efficiency expert
ACTOS quickly correct the" office inefficiencies " , the correct memo gets to the "Teamsters", and
the glucose is pickup and delivered to the right address in the cell .
Have Fun , Be Smart and chose your medications carefully.
Enjoy your week end, the sun is actually visible in western Oregon.
David Calder, MD