Endocrine Flashcards
Insulin, rapid acting
Uses?
Toxicity?
Lispro
Aspart
Glulisine
Uses = DM1, DM2, GDM (postpradial glucose control) Toxicity = hypoglycemia, rare hypersensitivity rxns
Action of insulin in general
Effect on liver? Muscle? Fat?
Bind insulin receptor (tyrosine kinase activity)
Liver = increase glucose stored as glycogen
muscle = increase glycogen, protein synthesis, and K uptake
Fat = increase TG storage
Insulin, short acting
Uses?
Regular
Uses = DM1, DM2, GDM, DKA (IV), hyperkalemia (+ glucose), stress hyperglycemia
Insulin, intermediate acting
NPH = Neutral Protamine Hagedorn
Uses = DM1, DM2, GDM
Insulin, long acting
Glargine
Detemir
Uses = DM1, DM2, GDM (basal glucose control)
Biguanides
Metformin
Metformin action and uses
Biguanide = MOA unknown
Decreases gluconeogenesis
Increases glycolysis and peripheral glucose uptake (insulin sensitivity)
Oral = first line therapy in type 2 DM
Can be used in patients without islet function
Metformin toxicity
GI upset
LACTIC ACIDOSIS = most serious adverse effect (contraindicated in RENAL FAILURE)
Sulfonylureas - first generation (2)
Toxicity?
Tolbutamide
Chlorpropamide
Disulfiram-like effects
Sulfonylureas - second generation (3)
Toxicity?
Glyburide
Glimepiride
Glipizide
Hypoglycemia
Sulfonylureas Action
Tolbutamide, Chlorpropamide
Glyburide, Glimepiride, Glipizide
Close K+ channel in B-cell membrane so cell depolarizes = triggers insulin release via increased Ca2+ influx
Sulfonylureas Uses and Toxicity (general)
Tolbutamide, Chlorpropamide
Glyburide, Glimepiride, Glipizide
Stimulate release of endogenous insulin in type 2 DM
Require some islet function, so useless in type 1 DM
Toxicity = risk of hypoglycemia increased in renal failure
Can sulfonylureas be used in type 1 DM?
NO - require some islet function as they stimulate endogenous insulin release
Risk of hypoglycemia while taking sulfonylureas is increased in which type of patients?
Renal failure
Glitazones/thiazolidinediones (2)
Pioglitazone
Rosiglitazone
Pioglitazone, Rosiglitazone
Action?
Uses?
Glitazones/thiazolidinediones
Increase insulin sensitivity in peripheral tissue (also increases levels of adiponectin)
Binds to PPAR-gamma nuclear transcription regulator (activated genes regulate FA storage and glucose metabolism)
Pioglitazone, Rosiglitazone
Toxicity?
Weight gain, edema
Hepatotoxicity, heart failure
a-glucosidase inhibitors (2)
Acarbose
Miglitol
Acarbose, Miglitol
Action?
Inhibit intestinal brush border a-glucosidases
Delayed sugar hydrolysis and glucose absorption = DECREASE postprandial hyperglycemia
Acarbose, Miglitol
Uses?
Toxicity?
a-glucosidase inhibitors
Uses = monotherapy in type 2 DM or in combination
Toxicity = GI disturbances
Amylin analogs
Pramlintide
Pramlintide
Action?
Use?
Toxicity?
Amylin analog (co-secreted with insulin)
Decrease gastric emptying
Decrease glucagon
Uses = Type 1 and Type 2 DM Toxicity = hypoglycemia, nausea, diarrhea
GLP-1 analogs
Exenatide
Liraglutide
Exenatide, Liraglutide
Action?
Use?
Toxicity?
GLP-1 analogs (glucagon like peptide)
Increase insulin
Decrease glucagon release
Uses = Type 2 DM Toxicity = nausea, vomiting; pancreatitis
DPP-4 inhibitors
Linagliptin
Saxagliptin
Sitagliptin
“gliptin”
Linagliptin, Saxagliptin, Sitagliptin
Action?
Use?
Toxicity?
DPP-4 inhibitors (dipeptidyl peptidase CD26)
Increase insulin
Decrease glucagon release
Uses = Type 2 DM Toxicity = mild urinary or respiratory infections
Which two diabetic classes of drugs increase insulin and decrease glucagon release?
GLP-1 analogs (exenatide, liraglutide) “tide”
DPP-4 inhibitors (linagliptin, saxagliptin, sitagliptin) “gliptin”
Which diabetic drug can cause lactic acidosis?
Metformin
Which diabetic drug(s) can cause disulfiram-like effects
First generation sulfonylureas:
Tolbutamide
Chlorpropamide
Which diabetic drug(s) can cause weight gain/edema and hepatotoxicity/heart failure
Pioglitazone
Rosiglitazone
(Glitazones/thiazolidinediones)
Which class of diabetic drugs can cause pancreatitis?
GLP-1 analogs
Exenatide, Liraglutide
Propylthiouracil, Methimazole
Mechanism?
Block thyroid peroxidase = inhibit oxidation of iodide and organification (coupling) of iodine = inhibit thyroid hormone synthesis
Propylthiouracil also blocks 5’-deiodinase, which decreases peripheral conversion of T4 to T3
What additional function does propylthiouracil have that methimazole does not?
Propylthiouracil also blocks 5’-deiodinase, which decreases peripheral conversion of T4 to T3
Propylthiouracil, Methimazole
Uses? Which is safe in pregnancy?
Toxicity?
Uses = HYPERthyroidism
PTU used in pregnancy; Methimazole is a possible teratogen (aplasia cutis)
Toxicity = skin rash, agranulocytosis, aplastic anemia, hepatotoxicity (PTU), teratogenic (methimazole)
What is a possible teratogenic outcome of methimazole use in pregnancy?
Aplasia cutis
Levothyroxine, triiodothyronine
Mechanism?
Uses?
Thyroxine replacement
HYPOthyroidism, myxedema
Levothyroxine, triiodothyronine
Toxicity?
Tachycardia, heat intolerance, tremors, arrhythmias
Hyperthyroid symptoms
Growth hormone uses (2)
GH deficiency
Turner syndrome
Octreatide
Agent?
Uses?
Somatostatin (GHIH; growth hormone inhibitory hormone)
Acromegaly, carcinoid, gastrinoma, glucagonoma, esophageal varices
Oxytocin uses
Stimulates labor, uterine contractions, MILK LET-DOWN
controls uterine hemorrhage
ADH (DDAVP) / Desmopressin
Pituitary (central, not nephrogenic) DI
Demeclocycline
Use?
Toxicity?
ADH antagonists (tetracycline family) Use = SIAHD Toxicity = nephrogenic DI, photosensitivity, abnormalities of bone and teeth
Glucocorticoids
Hydrocortisone Prednisone Triamcinolone Dexamethasone Beclomethasone Fludrocortisone (mineralocorticoid and glucocorticoid activity)
Which steroid has both mineralocorticoid and glucocorticoid activity?
Fludrocortisone
Glucocorticoids
Mechanism?
Metabolic, catabolic, anti-inflammatory, and immunosuppressive effects mediated by interactions with glucocorticoid response elements and inhibition of transcription factors such as NF-kB
Glucocorticoids
Uses? (4)
Addison disease
Inflammation
Immune suppression
Asthma
Glucocorticoids
Toxicity?
Iatrogenic Cushing syndrome = buffalo hump, moon facies, truncal obesity, muscle wasting, thin skin, easy bruisability, osteoporosis (treat with bisphosphonates), adrenocortical atrophy, peptic ulcers, diabetes (if chronic)
Adrenal insufficiency when drug stopped abruptly after chronic use
What can occur if glucocorticoids are stopped abruptly after chronic use?
Adrenal insufficiency
