Pharm: Metformin, thiazolidinediones, pramlintide, SGLT-2 inhibitors Flashcards
What is the first line oral agent for the management of type 2 diabetes?
Metformin (think of the student saying metaphors)
What does metformin do?
Decreases hepatic glucose output
Decreases intestinal glucose absorption
Increases peripheral glucose uptake and utilization
Metformin inhibits the enzyme, _________, to decrease hepatic gluconeogensis.
glycerophosphate dehydrogenase (mGDP)- a mitochondrial enzyme responsible for getting molecules into the gluconeogenesis pathway
(think of the girl- whom the METaphOR-weilding boy is trying to woo- who is biting a mitochondria-shaped candy)
Metformin activates __________ to exert its effect.
AMP-activated protein kinase aka AMPK- inhibits gluconeogenesis
(think of the AMPK liver bag)
Besides supressing gluconeogenesis in the liver, how does metformin help control glucose levels?
Increasing insulin sensitivity- facilitates peripheral uptake of glucose
(think of the valentines mailbox by the metformin metaphor boy- welcome INside for INsulin increasing fat and sugar uptake)
What side effects can metformin cause? And which patients do we need to be concerned about?
- lactic acidosis from blocked gluconeogenesis in liver (think of the spilled, spoiled milk).
This needs to be thought of in patients with renal failure, because metformin is just usually excreted unmodified by the kidneys and with kidney disease, metformin builds up (think of the cracked, kidney-shaped tray that the lactic acid is on).
- GI upset (like the green-faced girl about to barf at the metformin boy)
True or False: Metformin causes weight loss.
True. Modest weight reduction- unlike sulfonylureas and meglitinides (just like how metformin metaphor boy is skinny)
What is the suffix for thiadolidinediones?
-glitazone: rosiglitazone, pioglitazone (think of girl reading “ROSes are red” on the GLITter-covered card)
What is the mechanism of thiadolidinediones?
They ligands of peroxisome proliferator activated receptor gamma aka PPAR-gamma (think of the “life of the PPARy on the successful boy’s shirt)- an intracellular receptor that regulates gene transcription and increases glucose uptake and decreases glucose production
What are two of the most important genes regulated by PPARy?
- adiponectin- upregulated (think of his turtleneck)
2. GLUT4- upregulated (like the open GLUT4 mailbox)
Explain the unique relationship between the thiazolidinediones and weight gain.
Thiazodlidinediones lead to increased differentiation of adipocytes, leading to decreased serum triglyceride levels (from increased triglyceride storage) and weight gain
(think of the successful, fat boy eating doughnuts to represent fat storage: -glitazones put extra GLIT in your ZONE)
True or false: thiazolidinediones take days to weeks to become effective.
True. Because it works by increasing gene expression, it takes time.
What big side effect do you need to worry about with the thiazolidinediones (not related to weight gain)?
Peripheral edema from increase fluid retention from increased sodium retention in the renal collecting tubules (like thiazolidinedione boy’s baggy pants)
What patient population do you need to avoid giving thiazolidinediones?
Do not give to patients with CHF (like the baggy heart balloon being crushed by the boy’s chair)
The non-insulin-raising drug that acts on the peroxisome proliferator-activator receptor gamma can cause which side effect that is especially common in older women?
Osteoporosis (think of the boy’s chair, which has a femur-shaped leg that is breaking)
