endocrine meds

Question 1

Which medication causes lactic acidosis?

Mech. of action?

caution?

Answer 1

Increase insulin secretion

Biguanides

Metformin

Inhibit mGPD mitochondrial glycerophosphate dehydrogenase—-> inhibition of hepatic gluconeogenesis and the action of glucagon. increase glycolysis, peripheral glucose uptake ( insulin sensitivity).

GI upset/ time limited diarrhea, lactic acidosis (use with caution in renal insufficiency/ contraindicated, vitamin B12 deficiency.

Weight loss (often desired)

Question 2

Which medication cases MI and HF?

AD?

mech. of action?

Answer 2

Thiazolidinediones TZD“-glits” Pioglitazone, rosiglitazone

Activate PPAR-γ (a nuclear receptor) increase insulin sensitivity and levels of adiponectin Ž regulation of glucose metabolism and fatty acid storage (via GLUT4).

Weight gain, edema (fluid retension), HF,  risk of fractures (stealing the progenitor cells for adipocytes, therefore less osteoblasts). Bladder cancer.
Delayed onset of action (several weeks).

Rosiglitazone:  risk of MI, cardiovascular death

Question 3

Which medication causes Disulfiram like reaction or which med. causes hypoglycemia?

Mech. of action?

Answer 3

Increase insulin secretion

Sulfonylureas (1st gen)
Chlorpropamide, tolbutamide

Sulfonylureas (2nd gen)
Glipizide, glyburide

Meglitinides“-glins”
Nateglinide, repaglinide

Close K+ channels in pancreatic B cell membrane—->cell depolarizes—-> insulin release via  Ca2+ influx.

Disulfiram-like reaction with first-generation sulfonylureas only (rarely used).

Hypoglycemia ( risk in renal insufficiency), weight gain.

Question 4

Which med. causes pancreatitis/ prancreatic cancer? mech. of action?

Which medication causes urinary infectins? mech. of action

Answer 4

Increase glucose-induced insulin secretion/ incretins

GLP-1 analogs

Exenatide, liraglutide glucagon release,  gastric emptying,  glucose-dependent insulin release.

Nausea, vomiting, pancreatitis. Weight loss (often desired). satiety (often desired).

DPP-4 inhibitors“-gliptins” Linagliptin, saxagliptin, sitagliptin

Inhibit DPP-4 enzyme that deactivates GLP-1 —-> increases glucagon release,  gastric emptying. glucose-dependent insulin release.
(do not work)

Respiratory and urinary infections, weight neutral. satiety (often desired).

Question 5

Which medications cause flatulence and boating? mech. of action?

Which medications cause euglycemic DKA? other side effects? Mech. of action?

Answer 5

Decrease glucose absorption

Sodium-glucose co-transporter 2 SGLT2 inhibitors“-gliflozins” Canagliflozin, dapagliflozin, empagliflozin Block reabsorption of glucose in proximal convoluted tubule PCT.

Glucosuria (UTIs, vulvovaginal candidiasis), dehydration (orthostatic hypotension), weight loss. Use with caution in renal insufficiency ( efficacy with  GFR). Euglycemic DKA

α-glucosidase inhibitors
Acarbose, miglitol Inhibit intestinal brush-border α-glucosidases—> delayed carbohydrate hydrolysis and glucose absorption—> postprandial hyperglycemia.
GI upset, bloating.

Not recommended in renal insufficiency.

Question 6

What medication release glucagon?

Answer 6

Others

Amylin analogs

Pramlintide glucagon release,  gastric emptying.
Hypoglycemia, nausea.  satiety (often desired).