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Pharm 20
Golan Second Edition
33
Pharmacology
Graduate
03/14/2011

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Term
Angiotensin Converting Enzyme Inhibitors
Definition
Captopril, Enelapril, Ramipril, Benazepril, Fosinopril, Moexipril, Perindopril, Quinapril, Trandolapril, Lisinopril
Term
ACE inihbitor metabolism
Definition
1) active drug to active metabolite (captopril); 2) prodrug to active metabolite (enalapril/ramipril) 3) active drug unchanged (lisinopril)
Term
ACE inhibitor information
Definition
HTN, HF, diabetic nephropathy, MI {Angioedema (black), agranulocytosis, neutropenia, cough, edema, hypotension, rash gynecomastia, hyperkalemia, proteinuria} [Angioedema, renal artery stenosis, renal failure, pregnancy] Allopurinol may precipitate hypersensitivity. Delay contractile dysfunction and diabetic nephropathy
Term
Cause of cough in ACE inhibitors
Definition
Anti-bradykinin effect
Term
Angiotensin II receptor antagonists (AT1 receptor blockers)
Definition
Candesartan, Irbesartan, Losartan, Temisartan, Valsartan. May also increase vasorelaxant AT2 receptor activity
Term
Angiotensin receptor blocker information
Definition
HTN, Diabetic Nephropathy, HF, MI, Stroke prophylaxis {Thrombocytopenia, rhabdomyolysis, angioedema, Hypotension, diarrhea, asthenia, dizziness} [Renal artery stenosis, Pregnancy] Combination with ACE inhibitors for HF survival. Good for ACEI hypersensivitity.
Term
B-type natriuretic peptides
Definition
Nesiritide
Term
Nesiritide
Definition
Acutely decompensated heart failure {Hypotension, cardiac arrhythmia, renal dysfunction, headache, confusion, somnolence, tremor, pruritus, nausea} [Cardiogenic shock, systolic < 90] decreases systemic vascular resistance. Increased risk of renal dysfunction
Term
Nesiritide MOA
Definition
Increases cGMP by binding guanylyl cyclase receptor causing smooth muscle relaxation
Term
Vasopressin Receptor 2 (V2) antagonists
Definition
Conivaptan, Lixivaptan, Tolvaptan
Term
V2 (ADH) blocker MOA
Definition
Prevents vasopressin-stimulated water resorption in apical membrane of collecting duct cells
Term
V2 (ADH) blocker information
Definition
Euvolemic hyponatremia, SIADH, HF, cirrhotic ascites, autosomal dominant polycystic kidney {atrial fibrillation, orthostatic hypotension, HTN, edema, hypokalemia, thirst, dyspepsia, headache, polyuria} [CYP450 3A4 inhibitors, hyovolemia hyponatremia]
Term
Conivaptan
Definition
IV, non-selective between V1 and V2
Term
Lixivaptan, Tolvaptan
Definition
Orally available, V2 selective V2 blockers, approval anticipated
Term
Carbonic Anhydrase Inhibitors
Definition
Acetazolamide
Term
Acetazolamide MOA
Definition
inhibit sodium and bicarbonate reabsorption at proximal-tubule cytoplasmic carbonic anhydrase II and luminal carbonic anhydrase IV
Term
Acetazolamide Information
Definition
High-altitude sickness, HP, epilepsy, glaucoma (Metabolic Acidosis, sufonamide adversia, diarrhea, weight and appetite loss, tinnitus, nausea, vomiting, paresthesia, somnolence, polyuria) [Adrenal gland failure, chronic angle-closure glaucoma, cirrhosis, hyponatremia/hypokalemia, hypoerchloremia acidosis, hepatic/renal disease]
Term
Acetazolamide Considerations
Definition
Metabolic acidosis, reduces secretion of aqueous humor, mountain sickness, alkalinize urin increasing exretion of acids like aspirin. Treatment of hyperuricemia or gout. Aspirin increases acetazolamide (CNS toxicity)
Term
Osmotic diuretics
Definition
Mannitol
Term
Mannitol
Definition
Cerebral edema, increased intraocular pressure, renal failure oliguria prophylaxis {Bhrombophlebitis, acidosis, seizure, urinary retention, pulmonary edema, hypotension, palpitations, fluid/electrolyte imbalance, diarrhea, nausea, rhinitis} [Anuria, dehydration, HF, pulmonary congestion, renal dysfunction] Vigoruos natriuresis, water loss causes hypernatremia, compartment syndrome or increased intracranial pressure
Term
Loop diuretics
Definition
Furosemide, Bumetanide, Torsemide, Ethacrynic Acid
Term
Loop Diuretics Information
Definition
HTN, Acute pulmonary edema, hypercalcemia, hyperkalemia, Edema w/ HT, cirrhosis, renal dysfunction {Hypotension, erythema multiforme, Stevens-Johnson, pancreatitis, aplastic/hemolytic anemia, leukopenia, thrombocytopenia, ototoxicity, alkalosis, hypokalemia, hyperuricemia, hypomagnesemia, hyperglycemia, spasticity, headache, glycosura} [Sulfonamides (except ethacrynic acid), Anuria, aminoglycosides]
Term
Most powerful loop diuretic
Definition
Bumetanide
Term
Loop diuretic MOA
Definition
inhibits sodium-potassium-chloride cotransporter NHCC2 in luminal membrance of thick ascending limb
Term
Thiazide Diuretics
Definition
Hydrochloro/Bendroflume/Hydroflume/Poly-thiazide, Chlorthalidone, Metolazone, Indapamide
Term
Thiazide Diuretics Information
Definition
HTN, edema states with HF, cirrhosis, renal dysfunction, corticosteroids and estrogen {arrhythmia, Stevens-Johnson, toxic epidermal necrolysis, pancreatitis, hepatotoxicity, SLE, hypotension, photosensitivity, vasculitis, hypokalemia metabolic alkalosis, hypoerglycemia, hyperuricemia, dyspepsia, headache, impotence, blurred vision, restlessness} [anuria, sulfonamide hypersensitivity, QT prolonging agents] first-line for hypertension, synergistic with loops. Diminish hypercalciuria. Paradoxical urine decrease in diabetic nephropathy
Term
Hydrochlorothiazide Complication
Definition
decreases glucose tolerance, potentially unmasking diabetes
Term
Potassium Sparing (Collecting Duct) Diuretics
Definition
Spironolactone, Eplerenone, Amiloride, Triamterene
Term
Spirololactone, Eplerenone MOA
Definition
inhibit aldosterone action preventing nuclear translocation of mineralocorticoid receptor
Term
Amiloride, Triampterene MOA
Definition
inhibit principal cell apical ENaC sodium channel
Term
Spironolactone, Eplerenone
Definition
HTN, Hypokalemia, primary aldosteronism, edema w/ HF, cirrhosis, nephrotic syndrome {Hyperkalemic metabolic acidosis, GI hemorrhage, agranulocytosis, SLE, breast cancer?, gynecomastia, dyspepsia, lethargy, abnormal menstruation, impotence, rash} [anuria, hyperkalemia, renal insufficency] Inhibit cardiac fibrosis
Term
Spironolactone (but not eplerenone)
Definition
Acne vulgatis, female hirsutism {impotence and gynecomastic more pronounced}
Term
Amiloride, Triamterene
Definition
HTN, Liddle syndrome {Hematopoietic disease, hyperkalemic metabolic acidosis, nephrotoxicity for triamterene, orthostatic hypotension, hypoerkalemia, dyspepsia, headache} [Same as aldosterone blocking diuretics]
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