Pharmacology - Endocrine Flashcards
Lispro
MOA: bind insulin receptor (tyrosine kinase activity).
Rapid Acting
Use: Type 1 and 2 DM
Tox: Hypoglycemia, lipodystrophy, weight gain.
Aspart
MOA: bind insulin receptor (tyrosine kinase activity).
Rapid Acting
Use: Type 1 and 2 DM
Tox: Hypoglycemia, lipodystrophy, weight gain.
Regular insulin
MOA: bind insulin receptor (tyrosine kinase activity).
Rapid Acting
Use: Type 1 and 2 DM
Tox: Hypoglycemia, lipodystrophy, weight gain.
NPH
MOA: bind insulin receptor (tyrosine kinase activity).
intermediate acting
Use: Type 1 and 2 DM
Tox: Hypoglycemia, lipodystrophy, weight gain.
Glargine
MOA: bind insulin receptor (tyrosine kinase activity).
Long Acting
Use: Type 1 and 2 DM
Tox: Hypoglycemia, lipodystrophy, weight gain.
Detemir
MOA: bind insulin receptor (tyrosine kinase activity).
Long Acting
Use: Type 1 and 2 DM
Tox: Hypoglycemia, lipodystrophy, weight gain.
Chlorpropamide
Sulfonylurea (1st gen)
MOA: Closes K+ channel in B-cell membrane = depolarization = triggers insulin release via increase in Ca2+ influx.
Uses: type 2 DM ONLY! useless in Type 1 DM.
Tox: disulfiram
Glyburide
Sulfonylurea (2nd gen) = insulin secretagon
MOA: Closes K+ channel in B-cell membrane = depolarization = triggers insulin release via increase in Ca2+ influx.
Uses: type 2 DM ONLY! useless in Type 1 DM.
Glimepiride
Sulfonylurea (2nd gen) = insulin secretagon
MOA: Closes K+ channel in B-cell membrane = depolarization = triggers insulin release via increase in Ca2+ influx.
Uses: type 2 DM ONLY! useless in Type 1 DM.
Glipizide
Sulfonylurea (2nd gen) = insulin secretagon
MOA: Closes K+ channel in B-cell membrane = depolarization = triggers insulin release via increase in Ca2+ influx.
Uses: type 2 DM ONLY! useless in Type 1 DM.
Metformin
Biguanides.
Mechanism unknown.
Decreases gluconeogensis! Increases glycolysis and peripheral glucose uptake.
Use: both I and II DM…doesn’t involve islet cells.
TOX: lactic acidosis!!!
Pioglitazone
Glitazone.
MOA: increase insulin sensitivity. Binds PPAR-gamma, transcription regululator (in adipose/sk muscle)
Rosiglitazone
Glitazone.
MOA: increase insulin sensitivity. Binds PPAR-gamma, transcription regululator (in adipose/sk muscle).
Tox: Cardiovascular (increase risk for MI)
Acarbose
alpha-glucosidase inhibitor.
MOA: Inhibits intestinal brush border a-glucosidase.
Decreases postprandial hyperglycemia!!
Miglitol
alpha-glucosidase inhibitor.
MOA: Inhibits intestinal brush border a-glucosidase.
Decreases postprandial hyperglycemia!!
Pramlintide
Mimetic - - amyline Decrease glucagon and gastric emptying. Must decrease insulin dose by 50%. Type 2 DM Tox: nausea and diarrhea
Exenatide
GLP-1
Increase insulin and decrease glucagon release.
Type 2 DM
Tox: nausea and diarrhea
“-gliptin”
Decrease breakdown of GLP1 by inhibiting DDP-4.
Propylthiouracil
MOA: Inhibits organification of iodine and coupling of thyroid hormone synthesis.
*Propylthiouracil also DECreases conversion of T4 to T3.
Use: Hyperthyroidism.
Tox: agranulocytosis and aplastic anemia!
Safe in prego.
Methimazole
MOA: Inhibits organification of iodine and coupling of thyroid hormone synthesis.
*Propylthiouracil also DECreases conversion of T4 to T3.
Use: Hyperthyroidism.
Tox: agranulocytosis and aplastic anemia! Metallic taste.
Levothyroxine
T4 - - Thyroxine replacement
Use: Hypothyroidism, myxedema
Tox: tackycardia, heat intolerance, tremors, arrythmias.
Triiodothyrine
T3 - - Thyroxine replacement
Use: Hypothyroidism, myxedema
Tox: tackycardia, heat intolerance, tremors, arrythmias.
GH
Clinical Use:
GH deficinecy
Turner Syndrome
Octreotide
Somatostatin Analog
Uses: Acromegaly, carcinoid, gastrinoma, glucagonoma
Oxytocin
Uses:
Stimulates labor, uterine contractions, milk let down; controls uterine hemorrhage.
Desmopressin
ADH agonist
Use: central Diabetes Insipidus
Demclocyclin
ADH antagonist (member of the tetracycline family).
Use: SIADH
Tox: Nephrogenic DI
Glucocorticoids
MOA: Decrease the production of leukotrienes and prostaglandins by inhibiting phospholipase A2 and expression of COX-2.
Use: addison’s disease, inflammation, immune suppression, asthma.
Tox: Iatrogenic Cushing’s Syndrome - buffalo hump, moon fascies, thin skin, diabetes.
Adrenal insufficiency when drug suddenly stopped.
