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Drug vs. MOA
Mechanism of Action of drugs.
59
Other
Not Applicable
09/25/2012

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Term
somatotropin
Definition
Replace GH levels appropriate for age
Term
Sermorellin acetate
Definition
Replaces GHRF and acts on pituitary to secrete GH
Term
Somatomedin C
Definition
Replaces IGF-1 to promote growth/maturation in tissues
Term
Octreotide
Definition
Blockade of GH release from pituitary as well as direct decrease in insulin secretion
Term
Pegvisomant
Definition
antagonizes the GH receptors on the liver
Term
Bromocriptine and Cabergoline
Definition
decreases GH levels via unk mechanism
Term
Clomiphene
Definition
interrupts esterogen negative feedback at hypothalamus/anterior pituitary --> stimulates GnRH/GnH release
Term
Gonadorelin
Definition
Mimics natural secretion of GnRH from hypothalamus
Term
Desmopressin
Definition
Longer duration of action, increases expression of aquaporin2 for fluid reuptake --> increases ADH
Term
Demeclocycline
Definition
antagonizes the action of ADH through an unknown post receptor mechanism
Term
Conivaptan, Tolvaptin, Lixivaptan
Definition
antagonizes ADH receptor --> decreases ADH levels
Term
Metyrapone
Definition
inhibits 11 B-hydroxylase --> decrease cortisol synthesis --> increase ACTH of pituitary origin but not ectopic ACTH (lung carcinoma or CRC)
Term
Aminoglutethimide
Definition
Desmolase inhibitor (cholesterol --> pregnenolone), therefore blocks formation of ALL adrenocorticosteroids
Term
Ketoconazole
Definition
Prefentially inhibits 17 alpha hydroxylation and inhibits formulation of DHEA, Andostenedion, and Cortisol
Term
Mitotane
Definition
cytotoxic agent that acts on normal and neoplastic adrenocorticol cells to rapidly reduce adrenal steroid levels in blood
Term
Levothyroxine- T4
Definition
primary circulating TH, bound to TBG --> longer half life than T3
Term
Liothyronine T3
Definition
Increased affinity for nuclear receptor, very rapid onset of action and short duration of action
Term
Suppression of inflammation with adrenocorticosteroids
Definition
decreased autoantibody levels --> recovery of thyroid function --> increased T4 --> decreased TSH and reversal of any thyroid hyperplasia (used cautiously due to immunosuppression SE)
Term
Propylthiouracil and Methimazole
Definition
Compete with thyroglobulin for FE-O-I on thyroid peroxidase to decrease tyrosyl iodination
Term
Iodide salts
Definition
decreases TH release
Term
Beta Blockers used in hyperthyroidism
Definition
decrease sensitivity of CVS to circulating adrenergic hormones
Term
Testosterone synthesis
Definition
made in leydid cells of testes, circulated in blood via SHBG and albumin, promotes development of male genitalia, skeletal muscle and bone
Term
DHT synthesis
Definition
made insitu from testosterone via testosterone 5 alpha reductase. promotes differentiation of genitalia during developmental and maturation, spermatogenesis, hair maturation and prostate growth
Term
Finasteride and Dutasteride
Definition
competitive enzyme inhibitor at the step where testostoerone -- DHT via 5 alpha reductase 2.
Term
Terazosin, Doxazosin, tamsulosin, alfuzosin
Definition
drug induced relaxation --> increased urinary flow
Term
Leuprolide, Goserelin
Definition
decrease anterior pituitary GnH leads to decreased testicular androgen synthesis, leads to suppression of testerone dependent prostate cancer and metastases
Term
Estrogens (DES) in managing prostate cancer w/ metastasis
Definition
suppresses GnH (and decreases osteoporosis!)
Term
Sipuleucel-T
Definition
immune cells from pt are exposed to prostate cancer associated antigen (PSA) which stimulates production of antigen presenting cells that can specifically target prostate cancer cells and strengthen natural immunity (results in increased life by 4.1 months)
Term
Flutamide, Bicalutamide
Definition
androgen receptor antagonists: decreased receptor mediated effects of DHT and adrenal androgens
Term
PDE5 inhibitors (Sidenafil citrate, vardenafil, Tadafil
Definition
blockade of PDE5-> increased cGMP --> decreased Ca by promoting export outside cell or SR storage --> relaxation of corporeal arterial and sinusoidal smooth muscle --> erection
Term
Alprostadil
Definition
PGE1--> cAMP- mediated phosphorylation and decreased activity of voltage dependent calcium ion channels --> relaxation of arterial and trabercular smooth muscle
Term
Mechanisms of Insulin secretion from Beta Cells
Definition
Activation of receptor for incretions (GLP-1) can also promote insulin secretion by increase cAMP; Glucose, FA, and ketone bodies that increase ATP can stimulate insulin secretion; Calcium mediated insulin release
Term
GLUT1
Definition
predominantly found in placenta, bronchial epithelia, and pancreas
Term
GLUT2
Definition
expressed in liver, pancreatic B cells, hypothalamus, SI, and renal tubular cells
Term
GLUT3
Definition
Primarily in neurons- primary source of neuronal glucose transport. Also found in placenta
Term
GLUT4
Definition
insulin induces translocation from intracellular sites to the membrane in adipose tissue, skeletal muscle, and heart
Term
Parenteral glucagon
Definition
promotes release of somatostatin leads to decreased insulin
Term
Dizoxide
Definition
increase membrane permeability to potassium--> decreased calcium uptake via voltage gated channels --> decreased calcium mediated insulin secretion
Term
Alpha Glucosidase Inhibitors (acarabose and migitol)
Definition
synthetic oligosaccharide inhibits intestinal mucosal alpha glycosidase which blocks intestinal uptake of carbs into the blood (Therefore this will UNblock uptake!)
Term
Leptin
Definition
acts at receptors in hypothalamus to decrease appetite (mutations associated with ravenous appetite and profound obesity)
Term
Adiponectin
Definition
promotes fatty acid oxidation in muscles and suppresses hepatic glucose release
Term
Diabetic Ketoacidosis
Definition
Insulin deficiency leads to increased breakdown of TG, this results increased fatty acids in blood; fatty acids are converted to acetylCoA --> ATP in liver; overproduction --> unmetabolized hepatic actylCoA-->ketone bodies --> excess are excreted and metabolized in other tissues
Term
Metformin
Definition
Increase in GLUT1 translocation to tissue membrane; decreases hyperglycemia by dereasing hepatic glucose production and increasing glucose utilization by muscle and other non-hepatic tissues
Term
Thiazolidinediones
Definition
Requires insulin, leads to gene expression that facilitates the action of insulin
Term
Amylin Analogs (Simylin)
Definition
made in beta cells and secreted with insulin; acts on alpha cells to decreased glucagon secretion, leads to decreased hepatic flucose production, this leads to increased hepatic insulin responsiveness. Also delays gastric emptying and suppresses appetitie.
Term
Sulfonureas
Definition
Results in increased calcium --> increased insulin secretion
Term
Meglitinide analogs (repaglinide)
Definition
same mechanism as sulfonureas (increased calcium --> increased insulin secretion)
Term
Exenatide
Definition
acts on receptors on pancreatic beta cell membrane --> Gs-linked receptor lead to increased cAMP--> increased glucose induced insulin secretion
Term
Sitagliptin
Definition
delays GLP-1 breakdown
Term
Cinacalcet
Definition
increases sensitivity of calcium sensing receptors on parathyroid gland--> decreased PTH and serum calcium levels
Term
Ibandronate and Zoledronate
Definition
Inhibits bone resorption via action on osteoclasts or osteoclast precursors; indirect inrease in bone mineral density
Term
Calcitonin
Definition
antagonizes the effects of PTH; directly inhibits osteoclastic bone resorption
Term
High dose glucocorticoids
Definition
antagonizes GI absorption
Term
EDTA
Definition
calcium displaced by divalent and trivalent heavy metals forming non ionizing soluble complex that is excreted in the urine
Term
Estrogen supplementation to treat Postmenopausal Osteopenia and Osteoporosis
Definition
antagonizes action of osteoclasts --> decrease bone resorption; no increase in skeletal mass but slows loss relative to no estrogen
Term
Raloxifene
Definition
Weak estrogen agonist activity in bone -> decreases bone resorption. increase risk of thombosis in women with prior history
Term
Calcitonin in treating osteoporosis/osteopenia regardless of cause
Definition
antagonizes osteoclasts-> increases cAMP, as well as interferes with the membrane transport of phosphate and calcium; does not promote bone growth
Term
Bisphonate MOA for bone restoration
Definition
directly attaches to bone --> resist demineralization; at sites of osteoclast-medicated bone resorption they are released and internalized by osteoclasts--> cytotoxic events and decrease osteoclastic-mediated bone resorption
Term
Teriparatide or PTH
Definition
at very low levels -> new bone formation by attracting osteoblasts; at high levels --> measurable serum elvels-->bone resorption
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