Drugs Week 3 Flashcards
MOA of Prednisone, prednisolone, hydrocortisone, dexamethasone
Replaces endogenous cortisol, causes inhibition of phospholipaseA2; ↓ Cyclooxygenase (prostaglandins, leukotriene), Cytokines (Tumor necrosis factor, IL-3,4,5,13, Granulocyte-Macrophage Stimulating factor)
Adverse effects of 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.
Prednisone must be converted to what and where?
Prednisone is a prodrug and must be converted to prednisolone by the liver before it becomes active
MOA of Fludrocortisone
Very potent affinity for mineralocorticoid receptor (↑ Na+/K+ATPase & ENaC expression) leads ↑ Na+ reabsorption and K+ excretion in distal tubules
Adverse effects of Fludrocortisone
Hypertension, edema, headache, hypokalemia, weight gain.
MOA of Ketoconazole
Inhibits cytochrome P450-dependent enzymes~cortisol synthesis
Adverse effects of Ketoconazole
Nausea, vomiting, headache, impotence and hepatotoxicity
Ketoconazole is used for what disease?
Cushing’s disease
What is Mitotane
used for?
Inoperable adrenocortical carcinoma; Cushing’s syndromee (off label)
MOA of Mitotane
Cytotoxic drug that suppreses ACTH secretion and reduces synthesis of cortisol.
Adverse effects of Mitotane
Nausea, vomiting, diarrhea and tiredness
MOA of Metyrapone
Decreases cortisol synthesis by inhibition of 11-hydroxylase activity
Purpose of Metyrapone
Cushing’s syndrome (off label)
Adverse effects of Metyrapone
Nausea, vomiting, dizziness and sedation
MOA of Levothyroxine (T4)
Activation of nuclear receptors, gene expression, and protein synthesis
Adverse effects of Levothyroxine (T4)
Cardiovascular (tachycardia, arrhythmia, MI), CNS (headache, nervousness, insomnia, irritability, GI (diarrhea, vomiting, cramps), weight loss
Purpose of Propylthiouracil
Hyperthyroidism (Methimazole is preferred to PTU except in the 1st trimester of pregnancy and in thyroid storm)
MOA of Propylthiouracil
Inhibits both thyroid peroxidase reactions and 5’-deiodinase
Adverse effects of Propylthiouracil
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 of Methimazole (hyperthyroidism)
Inhibits thyroid peroxidase reactions
Adverse effects of Methimazole
Nausea, GI distress, hepatitis (black box warning), hypothyroidism, agranulocytosis is rare but life-threatening side effect of thiomides. Methimazole causes serious congenital defects.
MOA of Potassium Iodide (SSKI) [aka Lugol’s solution]
Inhibit iodine organification and hormone release; reduce size and vascularity of thyroid gland
Purpose of Potassium Iodide (SSKI) [aka Lugol’s solution]
Preparation for surgical thyroidectomy; Thyroid storm
MOA of Propranolol
Inhibition of β receptors; inhibition of conversion of T4 to T3
Adverse effects of Propranolol
Asthma, AV blockade, hypotension, bradycardia
Clinical use of Propranolol
Thyroid storm
MOA of Somatropin
Recombinant form of human GH. Binds to GH receptors and increases production of IGF-1
Adverse effects of Somatropin
Gynecomastia, hyperglycemia, scoliosis, arthritis
Clinical use of Somatropin
Treatment of growth failure in children with GH deficiency, short stature, turner syndrome, chronic kidney disease, short bowel syndrome, wasting in HIV infection
MOA of Somatostatin analogs: Octreotide, Lanreotide, Pasireotide
Agonist at somatostatin receptors; inhibits production of GH and to a lesser extent, of TSH, glucagon, insulin, and gastrin.
Clinical use of Somatostatin analogs: Octreotide, Lanreotide, Pasireotid
Acromegaly and several other hormone-secreting tumors and acute control of bleeding from esophageal varices
Adverse effects of Somatostatin analogs: Octreotide, Lanreotide, Pasireotide
GI, gallstones, bradycardia, cardiac conduction problems, hypothyroidism, hyperglycemia
MOA of Pegvisomant
Blocks GH receptors
Clinical use of Pegvisomant
Acromegaly; used in patients with inadequate response to surgery, radiation, or other therapies.
Adverse effects of Pegvisomant
Infection, pain, nausea, diarrhea, increased liver enzymes.
What are examples of glucocorticoids?
Prednisone, prednisolone, hydrocortisone, dexamethasone
What is an example of a mineralocorticoid?
Fludrocortisone
Glucocorticoids
Prednisone, prednisolone, hydrocortisone, dexamethasone
Mineralocorticoid
Fludrocortisone
Hypercortisolism drugs:
Ketoconazole
Hypercortisolism drugs:
Mitotane
Hypercortisolism drugs:
Metyrapone
Hypothyroid drugs:
Levothyroxine (T4)
Hyperthyroid drugs:
Propylthiouracil
Hyperthyroid drugs:
Methimazole
Hyperthyroid drugs:
Potassium Iodide (SSKI) [aka Lugol’s solution]
Hyperthyroid drugs:
Propranolol
Growth Hormone deficiency drugs:
Somatropin
Growth Hormone excess drugs:
Somatostatin analogs: Octreotide, Lanreotide, Pasireotide
Growth Hormone excess drugs:
Pegvisomant