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36 Cards in this Set
- Front
- Back
Treatment of Hypoadrenalism (Addison's Disease)
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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. |
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a potent steroid with both glucocorticoid and
mineralocorticoid activity. Used mainly for its mineralocorticoid activity in Addison’s disease |
FLUDROCORTISONE
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fludrocortisone mimics the action of ______ (increased sodium and water absorption, increased potassium excretion)
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aldosterone
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______ is predominant stimulus for aldosterone synthesis.
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Activation of renin-angiotensin system in response to hypovolemia
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Cushing’s disease, AKA pituitary _____
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basophilism
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_____ Syndrome - mutation of the epithelial Na channel causing uncontrolled increased activity
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Liddle
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glycyrrhizin and glycyrrhetic acid in _____ cause increased sensitivity to aldosterone
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licorice
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licorice consumption contraindicated in patients taking ____ to lower blood pressure.
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"ACE" inhibitors
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Initiating event of Secondary Hyperaldosteronism
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decreased BP
or decrerased circulating volume |
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licorice inhibs what enzyme converting cortisol to cortisone?
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11betaHSDII
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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.
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glycyrrhizic
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Benign tumor of the adrenal cortex
Unilateral Amenable to surgical cure causes PRIMARY HYPERALDOSTERONISM |
Aldosterone producing adenoma (APA or Conn’s Tumor)
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Bilateral hyperplasia of the zona glomerulosa
Treated medically causes PRIMARY HYPERALDOSTERONISM |
Idiopathic hyperaldosteronism
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TREATMENT OF PRIMARY HYPERALDOSTERONISM:
APA |
unilateral adrenalectomy
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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 |
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2 Mineralocorticoid receptor antagonists drugs are available in the U.S.
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spironolactone (Aldactone) and eplerenone (Inspra)
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Mechanism of Action of spironolactone
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competitive inhibitor of aldosterone in the collecting duct of the renal tubal.
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Side Effects and Toxicity of spironolactone
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hyperkalemia (monitoring is required), gynecomastia, menstrual disturbances, GI upset, rashes
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Drug Interactions of spironolactone
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Salicylates increase metabolism of spironolactone. Drugs that cause hyperkalemia will exacerbate spironolactone-induced hyperkalemia
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Potassium-sparing diuretics that Block sodium channels
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Amiloride; Trimterene
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SPIRONOLACTONE - ____% is metabolized to canrenone
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80%
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Aldosterone analogues:
Fludrocortisone = pure ____ |
agonist
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Eplerenone (Inspra) = selective aldosterone receptor antagonist
Spironolactone = aldosterone antagonist, not _______ |
selective
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ACE Inhibitors: Antihypertensives
Contraindications |
Bilateral renal artery stenosis
Hyperkalemia Pregnancy |
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Do NSAIDs block Renin release?
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Yes, by blocking PGE2 and PGI2
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ACE Inhibitors: 3 groups
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Sulfhydryl-containing (know this one - Captopril)
Dicarboxyl-containing Phosphorus-containing : Prodrug |
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Group of Captopril, fentiapril, pivalopril, zofenopril, alacepril
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Sulfhydryl-containing (know this one)
know captopril |
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Group of Lisinopril, ramipril
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Dicarboxyl-containing
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Group of Fosinopril
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Phosphorus-containing : Prodrug
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Why caution giving ACEi to old folks
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ACE Inhibitors-Induced Acute Renal Failure
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ACE breaks down bradykinin. What is effect of ACEI?
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Bradykinin no broken down --> vasodilation
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AT1 receptor blockers contraindications
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Bilateral renal artery stenosis
Hyperkalemia Pregnancy |
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AT1 receptor blockers indications
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ACE inhibitor-associated cough
Diabetic nephropathy -Irbesartan, losartan Heart failure -valsartan |
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Direct renin inhibitor
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Aliskiren (Tekturna® )
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Aliskiren (Tekturna® ) indications
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Treatment of hypertension, alone or in combination with other antihypertensives
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Pharmacokinetics of Tekturna
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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 |