Aldactone Indication:

Used primarily to treat low-renin hypertension, hypokalemia, and Conn's syndrome.

Aldactone Mechanism Of Action:

Aldactone is a specific pharmacologic antagonist of aldosterone, acting primarily through competitive binding of receptors at the aldosterone-dependent sodium-potassium exchange site in the distal convoluted renal tubule. Aldactone causes increased amounts of sodium and water to be excreted, while potassium is retained. Aldactone acts both as a diuretic and as an antihypertensive drug by this mechanism. It may be given alone or with other diuretic agents which act more proximally in the renal tubule.

Aldactone Drug Interactions:

Not Available

Aldactone Food Interactions:

Avoid alcohol.
Avoid salt substitutes containing potassium.
Take with food.

Aldactone Generic Name:

Synonyms:

  • Not Available

Drug Type:

Small Molecule; Approved

Absorption:

Fairly rapidly absorbed from the gastrointestinal tract. Food increases the bioavailability of unmetabolized spironolactone by almost 100%.

Toxicity (Overdose):

The oral LD50 of spironolactone is greater than 1,000 mg/kg in mice, rats, and rabbits. Acute overdosage of spironolactone may be manifested by drowsiness, mental confusion, maculopapular or erythematous rash, nausea, vomiting, dizziness, or diarrhea. Spironolactone has been shown to be a tumorigen in chronic toxicity studies in rats.

Protein Binding:

Spironolactone and its metabolites are more than 90% bound to plasma proteins.

Biotransformation:

Rapidly and extensively metabolized. The metabolic pathway of spironolactone is complex and can be divided into two main routes: those in which the sulfur moiety is retained and those in which the sulfur moiety is removed by dethioacetylation. Spironolactone is transformed to a reactive metabolite that can inactivate adrenal and testicular cytochrome P450 enzymes. It also has anti-androgenic activity.

Half Life:

10 minutes

Dosage Forms of Aldactone:

Tablet Oral

Chemical IUPAC Name:

S-[(7R,8R,9S,10R,13S,14S,17R)-10,13-dimethyl-3,5'-dioxospiro[2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthrene-17,2'-oxolane]-7-yl] ethanethioate

Organisms Affected:

Humans and other mammals

Aldactone to general, pharmacology

General, pharmacology..
Diuretics