spironolactone
CLINICAL USE
Diuretic, aldosterone antagonist
DOSE IN NORMAL RENAL FUNCTION
25–400 mg daily
PHARMACOKINETICS
Molecular weight                           :416.6 %Protein binding                           :90 %Excreted unchanged in urine     : 0 (47–57 as metabolites) Volume of distribution (L/kg)       :No datahalf-life – normal/ESRD (hrs)      :1.3–1.4/Unchanged DOSE IN RENAL IMPAIRMENT
GFR (mL/MIN)
20 to 50     : 50% of normal dose 10 to 20     : 50% of normal dose <10           : Use with caution DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES
CAPD                :Not dialysed. Dose as in GFR <10 mL/min HD                     :Not dialysed. Dose as in GFR <10 mL/minHDF/high flux   :Unknown dialysability. Dose as in GFR <10 mL/minCAV/VVHD      :Not dialysed. Dose as in GFR 10 to 20 mL/min IMPORTANT DRUG INTERACTIONS
Potentially hazardous interactions with other drugsACE inhibitors or angiotensin-II antagonists: enhanced hypotensive effect; risk of severe hyperkalaemiaAntibacterials: avoid concomitant use with lymecyclineAntidepressants: increased risk of postural hypotension with tricyclics
Antihypertensives: enhanced hypotensive effect; increased risk of first dose hypotensive effect with post-synaptic alpha-blockersCardiac glycosides: increased digoxin concentration; possibly increased digitoxin concentrationCiclosporin: increased risk of hyperkalaemia Lithium: reduced lithium excretion NSAIDs: increased risk of hyperkalaemia (especially with indometacin); increased risk of nephrotoxicity; diuretic effect of spironolactone antagonised by aspirin Potassium salts: increased risk of hyperkalaemia Tacrolimus: increased risk of hyperkalaemia ADMINISTRATION
Reconstition
– Route
Oral Rate of Administration
–Comments
– OTHER INFORMATION
Renal patients are at an increased risk of hyperkalaemia and therefore spironolactone should be used with caution. It has active metabolites with long half-livesSmall studies have shown that doses of 25 mg of spironolactone 3 times a week can be safely used in haemodialysis patients although unknown whether that dose would be therapeutic – potassium levels should be monitored closely. Another small study used 25 mg daily but the potassium was monitored 3 times a week.
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