Endocrine- Pharmacology Flashcards
What are some rapid acting insulins?
Aspart, Glulisine, Lispro
How do rapid acting insulins work?
they bind insulin receptors (tyrosine kinase activity) and cause:
- increased glycogenogenesis in the liver
- increased TAG formation
- protein synthesis
What are the clinical uses of rapid acting insulins?
type I, II, and GDM
What are the intermediate acting insulins?
NPH
What are the long acting insulins?
Detemir, Glargine
What are the biguanides?
Metformin
How do biguanides like metformin work?
exact mechanism unknown but results in:
decreased gluconeogenesis
increased peripheral glucose uptake/intake
What are the AEs of metformin?
GI upset
lactic acidosis (contraindicated in renal insufficiency)
What are the sulfonylureas?
First gen: chlorporamide, tolbutamide
Second gen: Glimepiride, Glipizide, Glyburide
How do sulfonylureas work?
they close K+ channels in B-cell membrane so that the cel depolarizes leading to increased insulin release via Ca2+ influx
T or F. Sulfonylureas can be used for both Type I and II DM
F. Only II because it reuqires some islet function
What are the AEs of sulfonylureas?
Risk of hypoglyceia in renal failure
First gen: disulfram-like effects
Second gen: hypoglycemia
What are the glitazones/thiazolidinediones?
pioglitazone
rosiglitazone
How do the thiazolidinediones work?
they increase insulin sensitivity in peripheral tissue by binding to PPAR-y nucelar transcription regulators
What are the AEs of thiazolidinediones?
weight gain, edema
Hepatotoxicity
HF
increased risk of fracture
What are the GLP-1 analogs?
exenatide
liraglutide
How do GLP-1 analogs work and what are they used for?
they increase insulin and decrease glucagon release for tx of type II DM only
What are the AEs of GLP-1 analogs?
N/V
pancreatitis
What are the DPP-4 inhibitors?
-gliptins like linagliptin, saxagliptin
How do DPP-4 inhibitors work and what are they used for?
they increase insulin and decrease glucagon release for tx of type II DM only
What are the AEs of DDP-4 inhibitors?
mild urinary or respiratory infections
What are the amylin analogs that work for Type I and II Dm tx by decreasing gastric emptying and glucagon levels?
pramlintide
What are the SGLT-2 inhibitors that block reabsorption of glucose in the PCT?
-glifozins
What are the a-glucosidase inhibitors?
Acarbose, miglitol
How do a-glucosidase inhibitors work?
they inhibit brush border a-glucosidease that causes delayed carb hydrolysis and glucose absorption, decreasing posprandial hyperglycemia (type II only)
What is the mechanism of propylthiouracil and methimazole?
they block thyroid peroxidase, inhibiting the oxidation of iodide and the organification (coupling) of iodine, inhibiting thyroid hormone synthesis. PTU also blocks 5’-deiodinase
What are the AEs of PTU and methimazole?
skin rash
agranulocytosis
aplastic anemia
hepatotoxicity (PTU)
methimazole is a teratogen (hold until late pregnancy)
What are the main tx options for hypothyroidism?
levothyroxine (T4) and triiodothyronine (T3)
What are some ADH antagonists used in the tx of SIADH by competitvely binding to V2 receptors?
Convaptan and tolvaptan
Demeclocycline
What is an ADH analog used in the tx of central DI?
Desmopressin acetate
What are the clinical uses of giving oxytocin?
stimulating labor, uterine contractions, milk let-down, and controlling uterine-hemorrhage
What are the uses of somatostatin (octreotide)?
acromegaly
carcinoid syndrome
gastrinoma or glucagonoma
esophaeal varices
What is Cinacalcet?
it sensitizes the CaSR in the PTH gland to criculating Ca2+ to decrease the release of PTH for the tx of hypercalcemia/hyperPTHism
