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EndocrinE ` endocrine—PhArmAcology EndocrinE ` endocrine—PhArmAcology SEcTion iii 353
Diabetes mellitus therapy (continued)
drUg clAss mechAnism AdVerse eFFects
Increase insulin sensitivity
Biguanides Inhibit mGPD inhibition of hepatic GI upset, lactic acidosis (use with caution in
Metformin gluconeogenesis and the action of glucagon. renal insufficiency), vitamin B 12 deficiency.
glycolysis, peripheral glucose uptake ( insulin Weight loss (often desired).
sensitivity).
Glitazones/ Activate PPAR-γ (a nuclear receptor) insulin Weight gain, edema, HF, risk of fractures.
thiazolidinediones sensitivity and levels of adiponectin Delayed onset of action (several weeks).
“-gliTs” regulation of glucose metabolism and fatty Rosiglitazone: risk of MI, cardiovascular
Pioglitazone, acid storage. death.
rosiglitazone
Increase insulin secretion
Sulfonylureas (1st gen) DisulFIRam-like reaction (FIRst-generation
Chlorpropamide, only).
tolbutamide Rarely used.
Sulfonylureas (2nd gen) Close K channels in pancreatic B cell Hypoglycemia ( risk in renal insufficiency),
+
Glipizide, glyburide membrane cell depolarizes insulin weight gain.
2+
Meglitinides release via Ca influx.
“-gliNs”
Nateglinide,
repaglinide
Increase glucose-induced insulin secretion
GLP-1 analogs glucagon release, gastric emptying, Nausea, vomiting, pancreatitis. Weight loss
Exenatide, liraglutide glucose-dependent insulin release. (often desired).
satiety (often desired).
DPP-4 inhibitors Inhibit DPP-4 enzyme that deactivates GLP-1 Respiratory and urinary infections, weight
“-gliPs” glucagon release, gastric emptying. neutral.
Linagliptin, saxagliptin, glucose-dependent insulin release. satiety (often desired).
sitagliptin
Decrease glucose absorption
Sodium-glucose Block reabsorption of glucose in proximal Glucosuria (UTIs, vulvovaginal candidiasis),
co-transporter 2 convoluted tubule. dehydration (orthostatic hypotension),
(SGLT2) inhibitors hyperkalemia, weight loss.
“-gliFs” Use with caution in renal insufficiency
Canagliflozin, ( efficacy with GFR).
dapagliflozin,
empagliflozin
α-glucosidase Inhibit intestinal brush-border α-glucosidases GI upset, bloating.
inhibitors delayed carbohydrate hydrolysis and glucose Not recommended in renal insufficiency.
Acarbose, miglitol absorption postprandial hyperglycemia.
Others
Amylin analogs glucagon release, gastric emptying. Hypoglycemia, nausea. satiety (often desired).
Pramlintide
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