Lecture 21 - Pharm of Adrenal Steroids

Question 1

Cortizone is the trade name for ______.

Answer 1

Cortisol

Question 2

Cortisol can inhibit the transcription of genes when it binds to a GR and this monomeric complex does not dimerize, but binds _____ _____ of other genes –> decreases transacetylase activity.

Answer 2

Transcription factor

Question 3

The reason Cortisol has cardiovascular effects is because it has a permissive effect on the activity of _______ receptors –> low or absent cortisol leads to cardiovascular collapse.

Answer 3

Adrenergic receptors

Question 4

Remember that Cortisol is increased in ______, which is actually how it was discovered.

Answer 4

Pregnancy

Question 5

Keeping in mind the mechanism by which cortisol inhibits gene transcription, ______ is one of the transcription factors Cortisol binds to do this –> anti-inflammatory effect.

Answer 5

NfKB

Question 6

_____, a G-protein coupled receptor, is upregulated by subtle drops in pH, and thus, by cortisol. It is responsible for apoptosis in lymph tissue and inhibiting transcription of cytokines in Macrophages.

Answer 6

tdag8 (T-cell death-associated gene 8)

Question 7

Cortisol has antihistamine effects by ______ mast cell membranes. How long does this action of cortisol take, and how does it compare to its action of modifying gene transcription?

Answer 7

Stabilizing

This happens within minutes, while transcription modification takes hours.

Question 8

Cortisol and its analogs are used to treat Nausea and Vomiting in ______ patients ONLY (too many side effects to treat these things in lesser disease states).

Answer 8

Cancer patients

Question 9

How does cortisol improve lung development in premature infants?

Answer 9

Cortisol given to the mother actually increases production of Surfactant in the fetal lungs.

Question 10

Cortisol inhibits ______ activity in bone, decreases intestinal absorption of ______, and increases renal excretion of _____.

So think osteoporosis!

Answer 10

Osteoblast

Ca++

Ca++

Question 11

Cortisol can form cataracts. Is this reversible? How does this compare to other side effects of cortisol?

Answer 11

No, not reversible. Most other side effects are reversible with gradual cessation of administration.

Question 12

List the following glucocorticoids in order of shortest to longest acting:

Prednisone; Hydrocortisone; Dexamethasone; Betamethasone

Remember that ______ is the one with equal GR and MR activity, while ______ has very little MR activity, and _____ and _____ have no MR activity.

Answer 12

Hydrocortisone –> 8-12hrs

Prednisone –> 18-36hrs

Beta and Dexamethasone –> 1-3 days

Hydrocortisone

Prednisone

Beta and Dexamethasone

Question 13

Which cortisol analog is used for fetal lung maturation?

Answer 13

Betamethasone

Question 14

______ is a mineralocorticoid analog used ONLY for replacement therapy of hypoaldosteronism.

Answer 14

Fludrocortisone

Question 15

_______ is an aldosterone receptor antagonist.

Answer 15

Spironolactone

Question 16

_______ is an antifungal drug that inhibits CYP17, and thus is an inhibitor of Cortisol synth at high doses. It is temporarily used for treatment in patients with tumors that overproduce cortisol.

Answer 16

Ketoconazole