Adrenal Drugs

Question 0

x Cortisone

Answer 0

glucocorticoid, converted to cortisol in liver (by 11BHDS1);
–> modulate gene transcription, *low MR affinity
Use: cortisol replacement (short acting)
SE: many w/ chronic use, *must taper to prevent adrenal atrophy

Question 1

Cortisol (aka Hydrocortisone)

Answer 1

short-acting Glucorticoid (GR & MR affinity),
=> modulates gene transcription.
Use: replacement Tx or emergencies (~10 mg/day)
*NOT anti-inflammatory bc MR activity
SE: many w/ chronic use, *must taper to prevent adrenal atrophy

Question 2

Side effects associated w/ glucocorticoid use

Answer 2

• Chronic use:
  Cushing’s syndrome, HTN, osteoporosis, growth retardation, cataracts/glaucoma, psychosis, myopathies
• Discontinue too quickly:
  adrenal atrophy –> insufficiency

Question 3

Prednisone (prednisolone = active metabolite)

Answer 3

intermed. acting Glucocorticoid;
low MR activity, oral only.
*4x stronger than cortisol
* hepatic activation by 11BHDS1, can’t use if liver failure.
Use: against inflammatory diseases/for immune suppression
SE: many w/ chronic use, *must taper to prevent adrenal atrophy

Question 4

Triamcinolone

Answer 4

intermed. acting Glucorticoid,
*low MR activity.
Use: against inflammatory diseases/for immune suppression
SE: many w/ chronic use, *must taper to prevent adrenal atrophy

Question 5

x Methylprednisolone

Answer 5

intermed. acting Glucocorticoid, *low MR activity;
Use: against inflammatory diseases/for immune suppression
SE: many w/ chronic use, *must taper to prevent adrenal atrophy

Question 6

Dexemethasone

also Betamethasone

Answer 6

long-acting glucorticoid, NO MR activity;
*25-50x stronger than cortisol.
Use: Dex = #1 for suppressing ACTH production,
- inflammatory diseases/for immune suppression,
- induce fetal lung surfactant (in mothers w/ preterm delivery risk)
SE: many w/ chronic use, *must taper to prevent adrenal atrophy

Question 7

Beclomethasone

also: Fluticasone, Budesonide, Mometasone

Answer 7

Inhaled glucorticoids (-> GR => modulates gene transcription)
Use: asthma, allergic rhinitis
SE: oropharyngeal candidiasis
- chronic use risk less bc inhaled/nasal spray (vs. oral)

Question 8

x Loteprednol etabonate

Answer 8

“soft” glucocorticosteroid,
Use: opthalmic anti-inflammatory
SE: many w/ chronic use, but less bc lacks C20 ketone group

Question 9

x Aldosterone

Answer 9

endogenous mineralcorticoid,

* NOT used therapeutically

Question 10

x Fludrocortisone

Answer 10

synthetic mineralcorticoid (MR & GR, but only MR activity @ therapeutic doses)
Use: replacement therapy
SE: Na+ retention, hypoK+, edema, HTN

Question 11

x Metyrapone

Answer 11

Cortisol synthesis blocker (–l 11b-hydroxylase)
Use: Dx HPA axis deficit, to treat Cushing’s syndrome
SE: nausea, HTN, hirsutism, edema

Question 12

x Mitotane

Answer 12

Adrenolytic agent (–l steroid synth enzymes)
Use: decrease size of tumors causing Cushing’s syndrome
SE: nausea, hypercholesterolemia
*only used IN hospitals (not outpt)

Question 13

x Ketoconazole

Answer 13

Steroid synthesis blocker (& antifungal agent),
Use: Tx Cushing’s syndrome after surgery/radiation fails
+/- in combo w/ Mitotane
SE: sedation, impotence, gynecomastia, hepatotoxicity (rare)
inhibits multiple P450s!!!

Question 14

x Pasireotide

Answer 14

Somatostatin analog (esp. high affinity for type 5 R)
Use: Cushing Syndrome after fail surgery or radiation

Question 15

x Etomidate

Answer 15

Cortisol synth blocker (–l 11b-hydroxylase & other enzymes)
Use: Cushing’s syndrome, acute hypercholesterolemia, anaesthesia
SE: sedating - IN-hospital use only (via IV)

Question 16

x Mifepristone

Answer 16

Progesterone R & Glucocorticoid R antagonist;
Use: Cushing’s syndrome (high dose), medical abortion
SE: hypoK+, hypothyroidism, bleeding