Drugs Week 3

Question 1

MOA of Prednisone, prednisolone, hydrocortisone, dexamethasone

Answer 1

Replaces endogenous cortisol, causes inhibition of phospholipaseA2; ↓ Cyclooxygenase (prostaglandins, leukotriene), Cytokines (Tumor necrosis factor, IL-3,4,5,13, Granulocyte-Macrophage Stimulating factor)

Question 2

Adverse effects of Prednisone, prednisolone, hydrocortisone, dexamethasone

Answer 2

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.

Question 3

Prednisone must be converted to what and where?

Answer 3

Prednisone is a prodrug and must be converted to prednisolone by the liver before it becomes active

Question 4

MOA of Fludrocortisone

Answer 4

Very potent affinity for mineralocorticoid receptor (↑ Na+/K+ATPase & ENaC expression) leads ↑ Na+ reabsorption and K+ excretion in distal tubules

Question 5

Adverse effects of Fludrocortisone

Answer 5

Hypertension, edema, headache, hypokalemia, weight gain.

Question 6

MOA of Ketoconazole

Answer 6

Inhibits cytochrome P450-dependent enzymes~cortisol synthesis

Question 7

Adverse effects of Ketoconazole

Answer 7

Nausea, vomiting, headache, impotence and hepatotoxicity

Question 8

Ketoconazole is used for what disease?

Answer 8

Cushing’s disease

Question 9

What is Mitotane
used for?

Answer 9

Inoperable adrenocortical carcinoma; Cushing’s syndromee (off label)

Question 10

MOA of Mitotane

Answer 10

Cytotoxic drug that suppreses ACTH secretion and reduces synthesis of cortisol.

Question 11

Adverse effects of Mitotane

Answer 11

Nausea, vomiting, diarrhea and tiredness

Question 12

MOA of Metyrapone

Answer 12

Decreases cortisol synthesis by inhibition of 11-hydroxylase activity

Question 13

Purpose of Metyrapone

Answer 13

Cushing’s syndrome (off label)

Question 14

Adverse effects of Metyrapone

Answer 14

Nausea, vomiting, dizziness and sedation

Question 15

MOA of Levothyroxine (T4)

Answer 15

Activation of nuclear receptors, gene expression, and protein synthesis

Question 16

Adverse effects of Levothyroxine (T4)

Answer 16

Cardiovascular (tachycardia, arrhythmia, MI), CNS (headache, nervousness, insomnia, irritability, GI (diarrhea, vomiting, cramps), weight loss

Question 17

Purpose of Propylthiouracil

Answer 17

Hyperthyroidism (Methimazole is preferred to PTU except in the 1st trimester of pregnancy and in thyroid storm)

Question 18

MOA of Propylthiouracil

Answer 18

Inhibits both thyroid peroxidase reactions and 5’-deiodinase

Question 19

Adverse effects of Propylthiouracil

Answer 19

Nausea, GI distress, hepatitis (black box warning), hypothyroidism, agranulocytosis is rare but life-threatening side effect of thiomides. PTU has higher hepatotoxicity than methimazole.

Question 20

MOA of Methimazole (hyperthyroidism)

Answer 20

Inhibits thyroid peroxidase reactions

Question 21

Adverse effects of Methimazole

Answer 21

Nausea, GI distress, hepatitis (black box warning), hypothyroidism, agranulocytosis is rare but life-threatening side effect of thiomides. Methimazole causes serious congenital defects.

Question 22

MOA of Potassium Iodide (SSKI) [aka Lugol’s solution]

Answer 22

Inhibit iodine organification and hormone release; reduce size and vascularity of thyroid gland

Question 23

Purpose of Potassium Iodide (SSKI) [aka Lugol’s solution]

Answer 23

Preparation for surgical thyroidectomy; Thyroid storm

Question 24

MOA of Propranolol

Answer 24

Inhibition of β receptors; inhibition of conversion of T4 to T3

Question 25

Adverse effects of Propranolol

Answer 25

Asthma, AV blockade, hypotension, bradycardia

Question 26

Clinical use of Propranolol

Answer 26

Thyroid storm

Question 27

MOA of Somatropin

Answer 27

Recombinant form of human GH. Binds to GH receptors and increases production of IGF-1

Question 28

Adverse effects of Somatropin

Answer 28

Gynecomastia, hyperglycemia, scoliosis, arthritis

Question 29

Clinical use of Somatropin

Answer 29

Treatment of growth failure in children with GH deficiency, short stature, turner syndrome, chronic kidney disease, short bowel syndrome, wasting in HIV infection

Question 30

MOA of Somatostatin analogs: Octreotide, Lanreotide, Pasireotide

Answer 30

Agonist at somatostatin receptors; inhibits production of GH and to a lesser extent, of TSH, glucagon, insulin, and gastrin.

Question 31

Clinical use of Somatostatin analogs: Octreotide, Lanreotide, Pasireotid

Answer 31

Acromegaly and several other hormone-secreting tumors and acute control of bleeding from esophageal varices

Question 32

Adverse effects of Somatostatin analogs: Octreotide, Lanreotide, Pasireotide

Answer 32

GI, gallstones, bradycardia, cardiac conduction problems, hypothyroidism, hyperglycemia

Question 33

MOA of Pegvisomant

Answer 33

Blocks GH receptors

Question 34

Clinical use of Pegvisomant

Answer 34

Acromegaly; used in patients with inadequate response to surgery, radiation, or other therapies.

Question 35

Adverse effects of Pegvisomant

Answer 35

Infection, pain, nausea, diarrhea, increased liver enzymes.

Question 36

What are examples of glucocorticoids?

Answer 36

Prednisone, prednisolone, hydrocortisone, dexamethasone

Question 37

What is an example of a mineralocorticoid?

Answer 37

Fludrocortisone

Question 38

Glucocorticoids

Answer 38

Prednisone, prednisolone, hydrocortisone, dexamethasone

Question 39

Mineralocorticoid

Answer 39

Fludrocortisone

Question 40

Hypercortisolism drugs:

Answer 40

Ketoconazole

Question 41

Hypercortisolism drugs:

Answer 41

Mitotane

Question 42

Hypercortisolism drugs:

Answer 42

Metyrapone

Question 43

Hypothyroid drugs:

Answer 43

Levothyroxine (T4)

Question 44

Hyperthyroid drugs:

Answer 44

Propylthiouracil

Question 45

Hyperthyroid drugs:

Answer 45

Methimazole

Question 46

Hyperthyroid drugs:

Answer 46

Potassium Iodide (SSKI) [aka Lugol's solution]

Question 47

Hyperthyroid drugs:

Answer 47

Propranolol

Question 48

Growth Hormone deficiency drugs:

Answer 48

Somatropin

Question 49

Growth Hormone excess drugs:

Answer 49

Somatostatin analogs: Octreotide, Lanreotide, Pasireotide

Question 50

Growth Hormone excess drugs:

Answer 50

Pegvisomant