WEEK 3- endocrine Flashcards
**MOA **
Prednisone, prednisolone, hydrocortisone, dexamethasone
Drug Class
Replaces endogenous cortisol, causes inhibition of phospholipaseA2; ↓ Cyclooxygenase (prostaglandins, leukotriene), Cytokines (Tumor necrosis factor, IL-3,4,5,13, Granulocyte-Macrophage Stimulating factor)
Glucocorticoids
Adverse Effects
Prednisone, prednisolone, hydrocortisone, dexamethasone
Acute: mood changes, hypokalemia, GI upset/ulcer, hyperglycemia. Chronic: HPA-axis suppression, muscle wasting, cushingnoid, gluconeogenesis, salt&water retention, GI ulcer, osteoporosis, psychosis, immunosuppression, thin skin, cataract, glaucoma.
MOA
Fludrocortisone
Clinical Use
Drug Class
Very potent affinity for mineralocorticoid receptor (↑ Na+/K+ATPase & ENaC expression) leads ↑ Na+ reabsorption and K+ excretion in distal tubules
Adrenal insufficiency, hypopituitarism
mineralcorticoid
Adverse Effects
Fludrocortisone
Hypertension, edema, headache, hypokalemia, weight gain.
MOA
Ketoconazole
drug class/clinical use
Inhibits cytochrome P450-dependent enzymes~cortisol synthesis
Hypercortisolism drugs/cushings
Adverse Effects
Ketoconazole
Nausea, vomiting, diarrhea and tiredness, gynecomastia
**MOA **
Mitotane
drug class/clinical use
Cytotoxic drug that suppreses ACTH secretion and reduces synthesis of cortisol.
Hypercortisol/ Inoperable adrenocortical carcinoma; Cushing’s syndromee (off label)
MOA
Metyrapone
Class/ Clinical
Decreases cortisol synthesis by inhibition of 11-hydroxylase activity
Hypercortisolism/ Cushings (off label)
Adverse Effects
Mitotane
Nausea, vomiting, diarrhea and tiredness
Adverse Effects
Metryapone
Nausea, vomiting, dizziness and sedation
MOA
Propylthiouracil (PTU)
Drug Class/Clinical Use
Inhibits both thyroid peroxidase reactions and 5’-deiodinase
HyperThryoidism
MOA
Levothyroxine (T4)
Drug class/Clinical
Activation of nuclear receptors, gene expression, and protein synthesis
Hypothyroid
Adverse Effects
Levothyroxine
Cardiovascular (tachycardia, arrhythmia, MI), CNS (headache, nervousness, insomnia, irritability, GI (diarrhea, vomiting, cramps), weight loss
Adverse Effects
Propylthiouracil (PTU)
Nausea, GI distress, hepatitis (black box warning), hypothyroidism, agranulocytosis is rare but life-threatening side effect of thiomides. PTU has higher hepatotoxicity than methimazole.
MOA
Methimazole
Drug Class/Clinical
Inhibits thyroid peroxidase reactions
Hyperthyroid drug
MOA
Somatropin
Drug class/Clinical Use
Recombinant form of human GH. Binds to GH receptors and increases production of IGF-1
GH deficiency
Adverse Affects
Somatropin
Gynecomastia, hyperglycemia, scoliosis, arthritis
**MOA **
Somatostatin analongs: Octreotide, Lanreotide, Pasireotide
Clinical Use
Agonist at somatostatin receptors; inhibits production of GH and to a lesser extent, of TSH, glucagon, insulin, and gastrin.
Acromegaly and several other hormone-secreting tumors and acute control of bleeding from esophageal varices
Adverse Affects
Somatostatin analongs: Octreotide, Lanreotide, Pasireotide
GI, gallstones, bradycardia, cardiac conduction problems, hypothyroidism, hyperglycemia
MOA
Pegvisomant
Clinical Use
Blocks GH receptors- stops activation of JAK stat Tyrosine kinase rececptro
Acromegaly; used in patients with inadequate response to surgery, radiation, or other therapies.
