Pharmacology: Endocrine drugs Flashcards
Lispro
Rapid-acting insulin
- Binds insulin R (cell surface receptor tyrosine kinase with intrinsic activity, MAP kinase)
- Liver: incr glycogen storage
- Muscle: incr glycogen and protein synthesis, K+ uptake (**Shift K* IN!)
- Fat: incr TG storage
Aspart
Rapid-acting insulin
- Binds insulin R (receptor tyrosine kinase with intrinsic activity, MAP kinase)
- Liver: incr glycogen storage
- Muscle: incr glycogen and protein synthesis, K+ uptake (**Shift K* IN!)
- Fat: incr TG storage
Regular insulin
Short-acting insulin
- Binds insulin R (receptor tyrosine kinase with intrinsic activity, MAP kinase)
- Liver: incr glycogen storage
- Muscle: incr glycogen and protein synthesis, K+ uptake (**Shift K* IN!)
- Fat: incr TG storage
NPH
Intermediate-acting insulin
- Binds insulin R (receptor tyrosine kinase with intrinsic activity, MAP kinase)
- Liver: incr glycogen storage
- Muscle: incr glycogen and protein synthesis, K+ uptake (**Shift K* IN!)
- Fat: incr TG storage
Detemir
Long-acting insulin
- Binds insulin R (receptor tyrosine kinase with intrinsic activity, MAP kinase)
- Liver: incr glycogen storage
- Muscle: incr glycogen and protein synthesis, K+ uptake (**Shift K* IN!)
- Fat: incr TG storage
Glargine
Long-acting insulin
- Binds insulin R (receptor tyrosine kinase with intrinsic activity, MAP kinase)
- Liver: incr glycogen storage
- Muscle: incr glycogen and protein synthesis, K+ uptake (**Shift K* IN!)
- Fat: incr TG storage
Tolbutamide
First generation sulfonylurea
- Close K+ATP channel => cell depolarization => Ca2+ influx => insulin release
- Disulfiram-like effects
Chlorpropamide
First generation sulfonylurea
- Close K+ATP channel => cell depolarization => Ca2+ influx => insulin release
- Disulfiram-like effects
Glyburide
Second generation sulfonylurea
- Close K+ATP channel on pancreatic beta cells => cell depolarization => Ca2+ influx => insulin release
- Hypoglycemia
Glimepiride
Second generation sulfonylurea
- Close K+ATP channel on pancreatic beta cells => cell depolarization => Ca2+ influx => insulin release
- Hypoglycemia
Glipizide
Second generation sulfonylurea
- Close K+ATP channel on pancreatic beta cells => cell depolarization => Ca2+ influx => insulin release
- Hypoglycemia
Metformin
Biguanide
- Unk mechanism: DECR gluconeogenesis, incr glycolysis and peripheral glucose uptake/insulin sensitivity
- Lactic acidosis! *Don’t give in RF, check BUN/Cr
Pioglitazone
Glitazone/thiazolidinedione
- Bind to nuclear PPAR-gamma (peroxisome proliferator-activated receptor), in family of steroid and thyroid nuclear receptors, affects transcription
- Effects: 1) incr adiponectin, 2) incr FA transport protein, 3) incr insulin R substrate, 4) incr Glut4
- SEs: weight gain (from fluid), edema (caution in CHF), hepatotoxity (check LFTs!), heart failure.
- NO hypoglycemia
Rosiglitazone
Glitazone/thiazolidinedione
- Bind to nuclear PPAR-gamma (peroxisome proliferator-activated receptor), in family of steroid and thyroid nuclear receptors, affects transcription
- Effects: 1) incr adiponectin, 2) incr FA transport protein, 3) incr insulin R substrate, 4) incr Glut4
- SEs: weight gain, edema, hepatotoxity, heart failure.
- NO hypoglycemia
Acarbose
alpha-glucosidase inhibitor
- Inhibits intestinal brush border alpha-glucosidases
- Decreases post-prandial hypergly
Miglitol
alpha-glucosidase inhibitor
- Inhibits intestinal brush border alpha-glucosidases
- Decreases post-prandial hypergly
Pramlintide
Mimetic
- Mimics amylin (secreted with insulin): decr glucagon and inh gastric mobility
Exenatide
GLP-1 analog
- Incr insulin, decr glucagon release
GLP-1 (cAMP-coupled R)
- incretin hormone secreted by intestinal L cells in response to food intake
- decreases blood glucose by incr satiety, decr gastric emptying, incr insulin release from pancreatic beta cells
Repaglinide
Meglitinide
- Similar to sulfonylureas; bind to different spot on K+ channel
Nateglinide
Meglitinide
- Similar to sulfonylureas; bind to different spot on K+ channel
Sitagliptine
DD4 inhibitor
- DD4 normally degrades GLP-1 (an incretin hormone secreted by intestinal L cells in response to food intake–incr insulin and decr gastric motility and glucagon)
Vildagliptine
DD4 inhibitor
- DD4 normally degrades GLP-1 (an incretin hormone secreted by intestinal L cells in response to food intake–incr insulin and decr gastric motility and glucagon)
PTU vs. Methimazole
PTU: inhibits both peroxidase (thyroid) and 5’-deiodinase (peripheral T4 to T3 conversion), heptatotoxic
Methimazole: inhibits peroxidase only, possible teratogen
Levothyroxine
Hypothyroid
Perchlorate
Anion, competitively inhibits basolateral Na-I symporter on thyroid follicular cells
- Tx: Hyperthyroid
Pertechnetate
Anion, competitively inhibits basolateral Na-I symporter on thyroid follicular cells
- Tx: Hyperthyroid
Which diabetic drug requires some islet cell function?
Sulfonylureas, because they increase endogenous insulin secretion from beta cells
GH
Tx: GH deficiency, Turner’s
SST
AKA Octreotide
Tx: Acromegaly, carcinoid, gastrinoma, glucaconoma
Oxytocin
Stimulates labor, uterine contractions, milk let down; controls uterine hemorrhage
ADH (desmopressin)
Pituitary/central DI
Demeclocycline
A tetracycline, used to treat SIADH but can cause nephrogenic DI, photosensitivity, bone and teeth abnormalities
Hydroxycortisone
Glucocorticoid
Indications: Addison’s disease, immunosuppression, inflammation, asthma
SE: Iatrogenic Cushing’s; adrenal insufficiency, >3 weeks of use/more potent GCs increase risk of insufficiency after d/c
Prednisone
Glucocorticoid
Indications: Addison’s disease, immunosuppression, inflammation, asthma
SE: Iatrogenic Cushing’s; adrenal insufficiency, >3 weeks of use/more potent GCs increase risk of insufficiency after d/c
Triamcinolone
Glucocorticoid
Indications: Addison’s disease, immunosuppression, inflammation, asthma
SE: Iatrogenic Cushing’s; adrenal insufficiency, >3 weeks of use/more potent GCs increase risk of insufficiency after d/c
Dexamethasone
Glucocorticoid
Indications: Addison’s disease, immunosuppression, inflammation, asthma
SE: Iatrogenic Cushing’s; adrenal insufficiency, >3 weeks of use/more potent GCs increase risk of insufficiency after d/c
Beclomethasone
Glucocorticoid
Indications: Addison’s disease, immunosuppression, inflammation, asthma
SE: Iatrogenic Cushing’s; adrenal insufficiency, >3 weeks of use/more potent GCs increase risk of insufficiency after d/c