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36 Cards in this Set

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Treatment of Hypoadrenalism (Addison's Disease)
1) Hydrocortisone or cortisone
2) hydrocortisone or cortisone is reduced
3) A mineralocorticoid will then need to be added (fludrocortisone).
4) Prednisone or prednisolone may also be used with concurrent administration of fludrocortisone.
a potent steroid with both glucocorticoid and
mineralocorticoid activity. Used mainly for
its mineralocorticoid activity in Addison’s
disease
FLUDROCORTISONE
fludrocortisone mimics the action of ______ (increased sodium and water absorption, increased potassium excretion)
aldosterone
______ is predominant stimulus for aldosterone synthesis.
Activation of renin-angiotensin system in response to hypovolemia
Cushing’s disease, AKA pituitary _____
basophilism
_____ Syndrome - mutation of the epithelial Na channel causing uncontrolled increased activity
Liddle
glycyrrhizin and glycyrrhetic acid in _____ cause increased sensitivity to aldosterone
licorice
licorice consumption contraindicated in patients taking ____ to lower blood pressure.
"ACE" inhibitors
Initiating event of Secondary Hyperaldosteronism
decreased BP

or

decrerased circulating volume
licorice inhibs what enzyme converting cortisol to cortisone?
11betaHSDII
Genetic defects or chemical inhibition of this enzyme (licorice - ____ acid) lead to a pseudo-hyperaldosteronism state characterized by severe hypertension. Due to glucocorticoid hormone saturation of MR --> increases aldo effect.
glycyrrhizic
Benign tumor of the adrenal cortex
Unilateral
Amenable to surgical cure
causes PRIMARY HYPERALDOSTERONISM
Aldosterone producing adenoma (APA or Conn’s Tumor)
Bilateral hyperplasia of the zona glomerulosa
Treated medically
causes PRIMARY HYPERALDOSTERONISM
Idiopathic hyperaldosteronism
TREATMENT OF PRIMARY HYPERALDOSTERONISM:
APA
unilateral adrenalectomy
TREATMENT OF PRIMARY HYPERALDOSTERONISM:
IHA
medical management
Mineralocorticoid receptor (MR) blockers
Spironolactone or eplerenone
Epithelial sodium channel blockers
Amiloride or triamterene
Other antihypertensives as needed
2 Mineralocorticoid receptor antagonists drugs are available in the U.S.
spironolactone (Aldactone) and eplerenone (Inspra)
Mechanism of Action of spironolactone
competitive inhibitor of aldosterone in the collecting duct of the renal tubal.
Side Effects and Toxicity of spironolactone
hyperkalemia (monitoring is required), gynecomastia, menstrual disturbances, GI upset, rashes
Drug Interactions of spironolactone
Salicylates increase metabolism of spironolactone. Drugs that cause hyperkalemia will exacerbate spironolactone-induced hyperkalemia
Potassium-sparing diuretics that Block sodium channels
Amiloride; Trimterene
SPIRONOLACTONE - ____% is metabolized to canrenone
80%
Aldosterone analogues:

Fludrocortisone = pure ____
agonist
Eplerenone (Inspra) = selective aldosterone receptor antagonist

Spironolactone = aldosterone antagonist, not _______
selective
ACE Inhibitors: Antihypertensives

Contraindications
Bilateral renal artery stenosis
Hyperkalemia
Pregnancy
Do NSAIDs block Renin release?
Yes, by blocking PGE2 and PGI2
ACE Inhibitors: 3 groups
Sulfhydryl-containing (know this one - Captopril)

Dicarboxyl-containing

Phosphorus-containing : Prodrug
Group of Captopril, fentiapril, pivalopril, zofenopril, alacepril
Sulfhydryl-containing (know this one)

know captopril
Group of Lisinopril, ramipril
Dicarboxyl-containing
Group of Fosinopril
Phosphorus-containing : Prodrug
Why caution giving ACEi to old folks
ACE Inhibitors-Induced Acute Renal Failure
ACE breaks down bradykinin. What is effect of ACEI?
Bradykinin no broken down --> vasodilation
AT1 receptor blockers contraindications
Bilateral renal artery stenosis
Hyperkalemia
Pregnancy
AT1 receptor blockers indications
ACE inhibitor-associated cough
Diabetic nephropathy -Irbesartan, losartan
Heart failure -valsartan
Direct renin inhibitor
Aliskiren (Tekturna® )
Aliskiren (Tekturna® ) indications
Treatment of hypertension, alone or in combination with other antihypertensives
Pharmacokinetics of Tekturna
Absorption – decreased with a high fat meal
Distribution – steady state in 7-8 days
Metabolism – major enzyme appears to be CYP3A4
Excretion – ~25% appears in urine as parent drug