Endocrine - Pharmacology Flashcards
Pharmacologic drug: Lispro
Rapid-acting insulin
Is regular insulin short or long acting?
Short acting
Pharmacologic drug: NPH
Intermediate acting insulin
Pharmacologic drug: Glargine
Long acting insulin
Insulin: Mechanism of Action
Binds insulin receptor (RTK activity) Increases liver glucose storage as glycogen, muscle glycogen synthesis and protein snthesis; K+ uptake Increase TG storage
Insulin: Clinical Use
Type 1 and 2 DM Gestational diabetes Life-threatening hyperkalemia Stress-induced hyperglycemia
Insulin: Toxicity
Hypoglycemia, very rarely hypersensitivity reaction
Metformin: Mechanism of Action
Biguanide Decrease gluconeogenesis, increase glycolysis, increase peripheral glucose uptake (insulin sensitivity)
Metformin: Clinical Use
First-line therapy in Type 2 DM (oral) Can be used in patients without islet function
Metformin: Toxicities
GI upset Lactic acidosis (contraindicated in renal failure)
Pharmacologic drug: Tolbutamide
1st generation sulfonylurea
Pharmacologic drug: Glyburide
Second generation sulfonylurea
Sulfonylureas: Mechanism of Action
Close K+ channel in beta-cell membrane -> increase Ca2+ influx
Sulfonylureas: Clinical Use
Stimulate release of endogenous insulin in type 2 DM Requires some islet functions (not for DMI)
Sulfonylureas: Toxicities
First generation: disulfiram-like Second generation: hypoglycemia
Pharmacologic drug: Pioglitazone
Thiazolidinedione
Thiazolidinediones: Mechanism of Action
Increase insulin sensitivity in peripheral tissue Binds to PPAR-gamma nuclear transcription regulator
Thiazolidinediones: Clinical Use
Monotherapy in type 2 DM or combined
Thiazolidinediones: Toxicities
Weight gain, edema Hepatotoxicity Heart failure
Pharmacologic drug: Acarbose
Alpha-glucosidase inhibitor
Alpha-glucosidase inhibitors: Mechanism of action
Inhibit intestinal brush-border alpha-glucosidases Delayed sugar hydrolysis and glucose absorption -> decrease postprandial hyperglycemia
Alpha-glucosidase inhibitors: Clinical Use
Monotherapy in type 2 DM or in combination
Alpha-glucosidase inhibitors: Toxicities
GI disturbances
What is the amylin analog?
Pramlintide
Amylin analog (Pramlintide): Mechanism of action
Decreases glucagon
Amylin analog (Pramlintide): Clinical use
Type 1 and 2 DM
Amylin analog (Pramlintide): Toxicities
Hypoglycemia, nausea, diarrhea
Pharmacologic drug: Exenatide
GLP-1 analog
GLP-1 analogs: Mechanism of action
increase insulin, decrease glucagon release
GLP-1 analogs: Clinical use
Type 2 DM
GLP-1 analogs: Toxicities
Nausea, vomiting, pancreatitis
Pharmacologic drugs: Linagliptin, Saxagliptin, Sitagliptin
DPP-4 inhibitors
DPP-4 inhibitors: Mechanism of action
Increases insulin, decrease glucagon release
DPP-4 inhibitors: Clinical use
Type 2 DM
DPP-4 inhibitors: Toxicities
Mild urinary or respiratory infections
Propylthiouracil, Methimazole: Mechanism of action
Block peroxidase (inhibit organification of iodide and coupling of thyroid hormone synthesis) PTU also blocks 5’-deiodinase (decrease peripheral conversion of T4 to T3)
Propylthiouracil, Methimazole: Clinical use
hyperthyroidism
Propylthiouracil, Methimazole: Toxicity
Skin rash Agranulocytosis (rare) Aplastic anemia Hepatotoxicity (PTU) Possible teratogen (methimazole)
Levothyroxine, Triiodothyronine: Mechanism of action
Thyroxine replacement
Levothyroxine, Triiodothyronine: Clinical use
Hypothyroidism, myxedema
Levothyroxine, Triiodothyronine: Toxicity
Tachycardia, heat intolerance, tremors, arrhythmias
GH: Clinical use
GH deficiencies, Turner syndrome
Somatostatin (Octreotide): Clinical use
Acromegaly, carcinoid, gastrinoma, glucagonoma, esophageal varices
Oxytocin: Clinical use
Stimulates labor, uterine contractions, milk let-down Controls uterine hemorrhage
ADH (Desmopressin): Clinical use
pituitary (central, not nephrogenic) DI
Demeclocycline: mechanism of action
ADH antagonist (member of the tetracycline family)
Demeclocycline: Clinical use
SIADH
Demeclocycline: Toxicity
Nephrogenic DI Photosensitivity Abnormalities of bone and teeth
Pharmacologic drugs: hydrocortisone, prednisone, dexamethasone, beclomethasone
Glucocorticoid
Glucocorticoids: Mechanism of action
Decrease production of leukotrienes and prostaglandins by inhibiting phospholipase A2 and expression of COX-2
Glucocorticoids: Clinical use
Addison’s disease Inflammation Immune suppression Asthma
Glucocorticoids: Toxicity
Iatrogenic Cushing’s syndrome Adrenal insufficiency when drug stopped abruptly after chronic use
Pharmacologi drug triamcinolone
Glucocorticoid
Pharmacologic drug: Aspart
Rapid-acting insulin
Pharmacologic drug: Glulisine
Rapid acting insulin
Pharmacologic drug: Chlorpropamide
First generation sulfonylurea
Pharmacologic drug: Glimepiride
Second generation sulfonylurea
Pharmacologic drug: Glipizide
2nd generation sulfonylurea
Pharmacologic drug: Rosiglitazone
2nd generation sulfonylurea
Pharmacologic drug: Miglitol
alpha-glucosidase inhibitor
Pharmacologic Drug: Liraglutide
GLP-1 analog
Pharmacologic drug: Detemir
Long acting insulin