Renal drugs Flashcards
Acetazolamide (Diamox)
Proximal Tubule: Carbonic Anhydrase Inhibitor
Furosemide (Laxis)
Loop diuretic “high ceiling” (Loop of hence-thick ascending limb)
Bumeanide (Bumex)
Loop diuretic “high ceiling” (Loop of hence-thick ascending limb)
Ethacrynic Acid (Edacrin)
Loop diuretic “high ceiling” (Loop of hence-thick ascending limb)
Acetazolamid (Diamox)
Actions:
- decrease NaHCO3 reabsorption
- decrease H2O reabsorption
- metabolic acidosis
Acetazolamid (Diamox)
Clinical uses:
- acute mountain sickness
- metabolic alkalosis
- glaucoma
- urinary alkalizations
Acetazolamid (Diamox)
Toxicities:
- hyperchloremic metabolic acidosis
- renal stones
- renal potassium wasting
- drowsiness/paresthesia
Acetazolamid (Diamox)
Contraindications:
- hepatic cirrhosis
- sulfa allergies
Loop Diuretics Actions:
- inhibit the Na+/K+/2Cl- cotransporter in the thick ascending limb
- reduce NaCl, K+ and divalent cations (Ca2+ and Mg2+) reabsorption
- increase renal blood flow
- rapid response after I.V. administration
- duration of action dependent upon renal function
Loop Diuretics Clinical Uses:
- edematous conditions
- acute pulmonary edema
- acute hypercalcemia
- hyperkalemia
- acute renal failure
- anion overdose
Loop Diuretics toxicities
- dehydration
- hypokalemic metabolic alkalosis
- ototoxicity
- hyperuricemia
- hypomagnesemia
Loop diuretics contraindications:
sulfa allergy
Thiazides act
distal convoluted tubule: Na+ Cl- symport inhibitors
chlorthalidone (Hygroton)
thiazide like
indapamide (Lozol)
thiazide like
metolazone (Diulo, Zaroxolyn)
thiazide like
thiazide actions:
- inhibit the NaCl
- reabsorption in the distal convoluted tubule
- enhance Ca2+ reabsorption
thiazide clinical uses:
- hypertension
- congestive heart failure
- nephrolithiasis due to idiopathic hypercalciuria
- nephrogenic diabetes inspidus
thiazide toxicities:
- hypokalemic metabolic alkalosis and hyperuricemia
- impaired carbohydrate
- hyperlipidemia
- hyponatremia
thiazide contraindications:
sulfa allergies
Amiloride (Midamor) act
diuretics that act in the collecting tubule: Na+ channel inhibitors
Amiloride (Midamor) actions:
- inhibit the Na+ channels in the apical membrane of the collecting tubule
- reduce Na+ entry into these cells also reduces K+ excertion (K+ sparing)
Amiloride (Midamor) clinical uses:
-adjunctive treatment with thiazide or loop diuretic in CHF or hypertension
Amiloride (Midamor) toxicities:
- hyperkalemia
- hperchloremic metabolic acidosis
Amiloride (Midamor) contraindications:
- K+ supplements
- ACE inhibitors (cause retention of K+)
Triamterene (Dyrenium) actions:
- inhibit the Na+ channels in the apical membrane of the collecting tubule
- reduce Na+ entry into these cells also reduces K+ excretion (K+sparing)
Triamterene (Dyrenium) clinical uses:
-edema associated with CHF, nematic cirrhosis, nephrotic syndrome, or hyperaldosteronism
Triamterene (Dyrenium) toxicities:
- hyperkalemia
- hyperchloremic metabolic acidosis
Triamterene (Dyrenium) contraindications:
- kidney stones
- K+ supplements, ACE inhibitors
Spironlactone (Aldactone) actions:
- block actions of aldosteron
- inhibition of 5alpha-reductace
Spironlactone (Aldactone) clinical uses:
- hypertension or CHF w/other diuretics
- mineralcorticoid excess
- aldosteronism (primary or secondary resulting from CHF, hepatic cirrhosis or nephrotic syndrome)
Spironlactone (Aldactone) toxicities:
- hyperkalemia
- hyperchloremic metabolic acidosis
- gynecomastia
- impotence
- BPH
Spironlactone (Aldactone) contraindications:
- supplements, ACE inhibitors
- chronic renal insufficiency
Eplerenone (Inspra) actions:
-selective antagonisms of mineralcorticoid receptor in kidnye, heart, blood vessels, and brain
Eplerenone (Inspra) clinical uses:
- hypertension, alone or in combination
- full therapeutic effect should be observed within 4 weeks
Eplerenone (Inspra) toxicities and adverse reactions:
- hyperkalemia
- hypertriglyceridemia
Eplerenone (Inspra) contraindications:
- K+ supplements, K+ sparing diuretics, ACE inhibitors
- chronic renal insufficiency
- diabetes associated with microalbuminuria
- CYP450 3A4 inhibitors (e.g. ketoconazole)
Manitol actions:
- excreted, but not reabsorbed from the lumenal fluid (urine)
- creates osmotic resistance that limits water reabsorption in the proximal tubule and descending limb of the loop of hence
- natriuresis<diuresis
Manitol indications:
- to increase urine volume
- reduction of intracranial or intraocular pressure
Manitol toxicity:
- extracellular volume expansion
- dehydration and hypernatremia
Demeclocycline (Declomycin) actions:
- tetracycline derivative
- inhibit the effects of ADH at the collecting tubule
- reduce water reabsorption
- lithium salts have a similar effect
Demeclocycline (Declomycin) indications:
- syndrome of inappropriate ADH secretions (SIADH)
- elevated ADH
Demeclocycline (Declomycin) toxicity:
- nephrogenic diabetes insipidus
- renal failure
CA inhibitor structure: Cl-, Br-, CF3-, or NO2-
maximal diuretic activity (upper left or ring structure)
substitution with amine (-NH2) structure activity
increases natriuretic activity, but decrease CA inhibitor activity (upper right of ring structure)
H2NO2S structure activity (lower left)
unsubstituted sulfamoyl moiety required for activity
SO2NH2 structure activity (lower right)
can be replaced with electrophilic group (carboxyl, carbamoyl, etc.) increases diuretic activity and decreases CA inhibitory activity
