ACTH and Adrenal Steriods Flashcards
1
Q
Corticotropin (ACTH), or Cosyntropin
A
Not often used to increase glucocorticoid levels because glucocorticoids are cheaper and easier to administer
- Used to diagnostically distinguish between primary (adrenal malfunction) and secondary (pituitary malfunction) adrenal insufficiency
- Adverse effects:
- allergic reactions to ACTH
- similar to those for glucocorticoid administration - CI
- Pregnancy- because adrenal androgen synthesis may be increased
2
Q
Aldosterone (Endogenous Hormone)
A
- mineralocorticoid
- Produced in the Zona Glomerulosa in response to Ang II and K+
- minor ACTH stimulation
Physiologic effects: - increase the Na and water retention
- increase K and hydrogen ions excretions
- prolonged administration can result in hypokalemia alkalosis
3
Q
Fludrocortisone
A
Glucocorticoid and mineralocorticoid
- Glucocorticoid action and mineralocorticoid action - PREDOMINATELY MINERALOCORTICOID
- effects very similar to aldosterone - Indications:
- given with glucocorticoid for replacement therapy in adrenocorticoid insufficiency
- Salt losing adrenogenital syndrome (hyperkalemia, arrythmias, dec. Na, and dehydration)
- typical tx for primary adrenal insufficiency - Oral Drug
4
Q
Hydrocortisone (cortisol)
A
Glucocorticoid and mineralocorticoid
- Glucocorticoid and mineralcorticoid
- Used for replacement therapy in pts with adrenal insufficiency (Addisons)- preferred tx for adrenal insufficiency
- Equal mineralocorticoid and glucocorticoid properties- weak anti-inflammatory drugs
- short acting
5
Q
Cortisone
A
Glucocorticoid and mineralocorticoid
Cortisone is inactive and must be converted to hydrocortisone in the liver to be active
- same as hydrocortisone, but 80% of the anti-inflammatory and Na retaining potency of hydrocortisone because of metabolic loss before the conversion
- short acting
6
Q
Predisnone, prednisolone
A
Glucocorticoid, and partial mineralocorticoid
- Have more glucocorticoid effect than mineralocorticoid- more anti-inflammatory with minor salt retaining
- Prednisone is converted to prednislone in the liver in order to be active
- prednisone Most commonly prescribed oral glucocorticoid
- intermediate duration
7
Q
Triamcinolone, methyprednisone
A
Glucocorticoid
- All glucocorticoid activity- higher anti-inflammatory with no salt retaining effects
- Most newer glucocorticoids are identical in action to these drugs
- intermediate duration
8
Q
Dexamethasone
A
Glucocorticoid
- All glucocorticoid activity- higher anti-inflammatory with no salt retaining effects
- Indications
- Preferred for cerebral edema because it can enter the CNS easily
- Used when endogenous cortisol levels have to be measured (no cross reaction)
- long acting
9
Q
Flucticasone (Flonase)
A
Glucocorticoid
- All glucocorticoid activity- higher anti-inflammatory with no salt retaining effects
- Indications
- inhaled and intranasal use - asthma and rhinitis
10
Q
Aminogluthemide
A
- inhibits all steroid synthesis- inhibits conversion of cholesterol to pregnenolone, also inhibits aromatase enzyme (inhibits estrogen synthesis
- Indictions
- used in cushing syndrome that results from a adrenal carcinoma or ectopic ACTH secreting tumor
- tx metastatic breast and prostate cancer that has not responded to tamoxifen or anti-androgen tx
* *off market! - Adverse effects
- adrenal insufficiency
- inhibits estrogen synthesis- less effect on testosterone production
- drowsiness, skin rash, nausea, agranulocytosis and leukopenia
11
Q
Ketoconazole
A
- Antifungal that also inhibits steroidogenesis at higher doses
- Inhibits 17a-hydroxylase –> dec. androgens first then cortisol (hence high dose— yeah HEENCE!)
- At even higher dose: inhibits all steroid synthesis via inhibiting conversion of cholesterol to pregnenolone 3. Indications - very high doses are used in pts with chushing before surgery or radiation
- Most effective inhibitor of sterioid biosynthesis in pts with Cushing disease
- not for long term use - Adverse Effects
- Reversible hepatotoxicity
- gynecomastia, libido dec, and impotence
12
Q
Mitotane
A
- Adrenocorticolytic- causes selective atrophy of the zona fasciculata and zona reticularis of the adrenal gland
- Binds to mitochondrial proteins and inhibits synthesis of corticosteroids
- Indications
- primary adrenal carcinoma when surgery/radiation not an option
- produce remission of cushings disease- although most will relapse - Adverse Effects
- Severe gastrointestingal distress
- Lethargy, mental confusion, skin rash, and altered hepatic function - CI
- induces hepatic enzymes, inc. metabolism of phenytoin and warfarin
13
Q
Metyrapone
A
- cushings tx category
- Selective inhibitor of 11b1-hydroxylase (the terminal enzyme in cortisol synthesis), reduces deoxycorticosterone levels leading to reduced aldosterone, 11-deoxycortisol (the cortisol precursor) is increased and maintains aldosterone function without glucocorticoid effect
- Indications
- Adrenal function tests
- short term sx - while determining cause of cushing
- can be used in pregnant women ** (only drug in this class) - Adverse Effects
- Less toxicity than mitotane
- GI disturbances, sedation, dizziness, rash, hirsutism
14
Q
Mifepristone
A
- cushing tx category
- Powerful antagonist of progesterone receptors and at higher doses glucocorticoid receptors
- Indications
- inducing abortions
- causes glucocorticoid resistance
- inoperable tx for ectopic ACTH secretion, or adrenal carcinoma that failed to respond to other drugs - CI
- abdominal pain, amenorrhea, fatigue, and gastrointestinal upset
15
Q
Spiralactone
A
- Cushing tx category
- potassium sparing diuretic by competing with aldosterone for binding sites, higher doses have anti-androgenic effects
- Indications
- Hypertension
- Primary hyperaldosteronism ( also for dx)
- decrease hirsutism in women
- tx ascites associated with cirrhosis - Adverse Effects
- hyperkalemia
- gynocomastia and impotence in men
- menstrual irregularities in women
- GI issues
