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Potassium-sparing diuretics:

reduce Na+ reabsorption


reduce K+ secretion

These are not potent diuretics when used
alone

They are primarily used in combination
with other diuretics.






Amiloride (Midamor)

Spironolactone (Aldactone)

Triamterene (Dyrenium)
Interfere with sodium-potassium exchange in
collecting ducts and convoluted tubules

Competitively bind to aldosterone receptors
Block the reabsorption of sodium and water

Prevent potassium from being pumped into the
tubule, thus preventing its secretion





Sodium and water are excreted



These drugs are generally used in combination
with a thiazide or loop diuretic to treat
hypertension
CHF
refractory edema

They are also used to induce diuresis in clinical
situations associated with hyperaldosteronism:

adrenal hyperplasia
in the presence of aldosterone-producing
adenomas when surgery is not feasible.

these drugs are well absorbed protein bound,
and widely distributed

they are metabolized in the liver and primarily
excreted in urine

these diuretics cross the placenta and enter
breast milk
* routine use during pregnancy is not appropriate,
and they should be saved for situations in which the
mother has pathological reasons for use, not pregnancy
manifestations or complications , and the benefit to
the mother clearly outweighs the risk to the fetus.
* If one of these drugs is needed during lactation,
another method of feeding the baby should be used,
because of the potential for adverse effects on fluid and
electrolyte changes in the baby.
these drugs are contraindicated for use in
patients with allergy to the drug,hyperkalemia,
renal disease , or anuria.
are given cautiously during pregnancy and
lactation.
These agents can cause hyperkalemia,
hyperchloremic metabolic acidosis, and
arrhythmias.

Spironolactone is associated with
gynecomastia and can also cause menstrual
abnormalities in women.

These drugs are contraindicated in renal
insufficiency, especially in diabetic patients.

They are contraindicated in the presence of
other potassium-sparing diuretics and should
be used with extreme caution in individuals
taking an angiotensin-converting enzyme
(ACE) inhibitor.




Spironolactone
Act as antagonists to aldosterone, competes
with aldosterone for receptor sites in DCT

Results in decreased Na
+
reabsorption in DCT

Promotes Na
+
and water loss

Decreased Na
+
reabsorption balanced by K
+
retention at this site (and H
+
).

Used in combination with diuretic e.g..
frusomide
Triamterene and Amiloride

Similar effect to spironolactone by reducing Na
+

absorption and H
+
/K
+
secretion in DCT
Independent of aldosterone
Have little diuretic effect
Used in conjunction with diuretics
In low doses blocks entry of Na+ into tubule
cells across luminal membrane
Decrease availability of Na
+
to Na
+
-K
+
-ATPase at
basal cell membrane
Called Na
+
channel blockers

Drug Name Usual Dosage Usual Indications
amiloride (Midamor) 15 -20 mg/d PO with
monitoring of
electrolytes
All of the potassium
sparing diuretics are
indicated for the
adjunctive treatment of
edema caused by
congestive heart failure,
liver disease, or renal
disease; hypertension;
hyperkalemia; and
hyperaldosteronism;
Special considerations:
Not for use in children
Spironolactone
(Aldactone)
100 200 mg/d PO for
edema; 100 400 mg/d
PO for
hyperaldosteronism;
50 100 mg/d PO for
hypertension
Pediatric: 3.3 mg/kg per
day PO
Special considerations:
Can be used in children
with careful monitoring
of electrolytes
Triamterene (Dyrenium) 100 mg/D PO b.i.d Special considerations:
Not for use in children

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