spironolactone

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Related to Berlactone: Spiractin, Spirotone, Spironolact

spironolactone

 [spi″rah-no-lak´tōn]
one of the spirolactones, a competitive antagonist of aldosterone and a potassium-sparing diuretic; used in treatment of edema, hypokalemia, primary aldosteronism, and (usually in combination with other drugs) hypertension.

spironolactone

Aldactone, Novo-Spiroton (CA)

Pharmacologic class: Aldosterone inhibitor

Therapeutic class: Potassium-sparing diuretic

Pregnancy risk category D

FDA Box Warning

• Drug induced tumors in chronic toxicity studies in rats. Use only in conditions listed under "Indications and dosages." Avoid unnecessary use.

Action

Inhibits aldosterone effects in distal renal tubule, promoting sodium and water excretion and potassium retention

Availability

Tablets: 25 mg, 50 mg, 100 mg

Indications and dosages

Edema caused by heart failure, hepatic cirrhosis, or nephrotic syndrome

Adults: As sole diuretic, initially 100 mg/day P.O. (range of 25 to 200 mg) in single or divided doses, continued for 5 or more days and then adjusted to optimal therapeutic level

Children: 1 to 3 mg/kg/day P.O. as a single dose or in divided doses

Essential hypertension

Adults: Initially, 50 to 100 mg/day P.O. as a single dose or in divided doses, continued for at least 2 weeks

Children: 1 to 2 mg/kg P.O. b.i.d.

Hypokalemia

Adults: 25 to 100 mg/day P.O.

Diagnosis and treatment of primary hyperaldosteronism

Adults: For diagnosis, 400 mg/day P.O. for 4 days in short test or for 3 to 4 weeks in long test. Resolution of hypokalemia and hypertension confirm diagnosis of primary hyperaldosteronism. Dosages of 100 to 400 mg/day P.O. may be used as a bridge to surgical therapy; in patients unsuitable for this therapy, lowest effective dosage may be used for long-term maintenance.

Off-label uses

• Acne vulgaris
• Familial male precocious puberty (given with other drugs)
• Premenstrual syndrome

Contraindications

• Anuria, acute renal insufficiency, significant impairment of renal excretory function
• Hyperkalemia

Precautions

Use cautiously in:
• hepatic dysfunction, diabetes mellitus, fluid and electrolyte imbalances, severe heart failure
• concurrent use of other potassium-sparing diuretics, such as amiloride and triamterene (avoid use)
• concurrent use of potassium supplements (avoid use with serum potassium level greater than 3.5 mEq/L)
• concurrent use of ACE inhibitors and nonsteroidal anti-inflammatory drugs (NSAIDs) (use with extreme caution)
• concurrent use of lithium (generally avoid use)
• elderly or debilitated patients
• pregnant or breastfeeding patients
• children (safety not established).

Administration

• Give single daily dose with breakfast. If two daily doses are prescribed, give second dose with food in mid-afternoon.

Adverse reactions

CNS: headache, drowsiness, lethargy, ataxia, confusion

GI: vomiting, diarrhea, cramping, gastritis, GI ulcers, GI bleeding

GU: gynecomastia, irregular menses or amenorrhea, postmenopausal bleeding, erectile dysfunction, breast cancer

Hematologic: agranulocytosis

Metabolic: hyponatremia, hyperchloremic metabolic acidosis, hyperkalemia

Skin: rash, pruritus, hirsutism, drug rash with eosinophilia and systemic symptoms (DRESS), Stevens-Johnson Syndrome, toxic epidermal necrolysis

Other: deepening of voice, drug fever, hypersensitivity (including vasculitis, anaphylactic reactions)

Interactions

Drug-drug.Angiotensin-converting enzyme inhibitors, NSAIDs, potassium-sparing diuretics, potassium supplements, other potassium-containing drugs: increased risk of hyperkalemia

Anticoagulants, heparin: reduced hypoprothrombinemic effects of these drugs

Digoxin: increased digoxin blood level

Lithium: reduced lithium renal clearance and increased risk of lithium toxicity

Salicylates: decreased diuretic effect

Drug-diagnostic tests.Blood urea nitrogen, potassium: increased levels

Digoxin assays: false digoxin elevation

Granulocytes: decreased count

Drug-food.Potassium-containing salt substitutes, potassium-rich diet: increased risk of hyperkalemia

Drug-herbs.Licorice: potassium loss

Patient monitoring

Monitor electrolyte levels (especially potassium), particularly in patients with severe heart failure. Watch for signs and symptoms of imbalances and metabolic acidosis. Interrupt or discontinue treatment for serum potassium level greater than 5 mEq/L or serum creatinine greater than 4 mg/dl.
• Monitor weight and fluid intake and output. Stay alert for indications of fluid imbalance.
• Monitor CBC with white cell differential.

Patient teaching

• Tell patient to take daily dose with breakfast. If two daily doses are prescribed, advise him to take second dose with food in mid-afternoon.
• Advise patient to restrict intake of high-potassium foods and to avoid licorice and salt substitutes containing potassium.
• Tell male patient drug may cause breast enlargement.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, and herbs mentioned above.

spi·ro·no·lac·tone

(spī'rō-nō-lak'tōn),
A diuretic agent that blocks the renal tubular actions of aldosterone. It increases the urinary excretion of sodium and chloride, decreases the excretion of potassium and ammonium, and reduces the titratable acidity of the urine; most effectively used to potentiate the natriuretic action and reduce the potassium excretion produced by other diuretics.

spironolactone

/spir·o·no·lac·tone/ (spi″rah-no-lak´tōn) one of the spirolactones, an aldosterone inhibitor that blocks the aldosterone-dependent exchange of sodium and potassium in the distal tubule, thus increasing excretion of sodium and water and decreasing excretion of potassium; used in the treatment of edema, hypokalemia, primary aldosteronism, and hypertension.

spironolactone

(spī′rə-nō-lăk′tōn, spī-rō′-, spī-rŏn′ə-)
n.
An aldosterone antagonist and antiandrogen, C24H32O4S, that promotes diuresis and is used to treat fluid retention, androgenic syndromes in women, and hypertension.

spironolactone

[spī′rənəlak′tōn]
a potassium-sparing aldosterone antagonist diuretic.
indications It is prescribed in the treatment of primary hyperaldosteronism, edema of congestive heart failure, cirrhosis of the liver accompanied by edema, nephrotic syndrome, essential hypertension, and hypokalemia.
contraindications Anuria, acute renal insufficiency, significant impairment of renal function, or hyperkalemia prohibits its use.
adverse effects Among the most serious adverse effects are hyperkalemia, gynecomastia, mental confusion, ataxia, impotence, amenorrhea, hirsutism, and urticaria.

spironolactone

A potassium-sparing diuretic, which inhibits aldosterone, resulting in less sodium retention. See Diuretics, Potassium-sparing diuretic.

spi·ro·no·lac·tone

(spī'rō-nō-lak'tōn)
Diuretic that blocks aldosterone's renal tubular actions and increases urinary excretion of sodium and chloride.

spironolactone

A DIURETIC drug that does not lead to loss of potassium from the body. It is an antagonist of the hormone aldosterone. The drug is on the WHO official list. Brand names are Aldactone and Spiroctan.

diuretics

powerful drugs, often termed 'water tablets', that control hypertension and peripheral oedema; action of some local anaesthetics is antagonized by concomitant use of some diuretics (see Table 1), e.g. aldosterone antagonists (e.g. spironolactone); carbonic anhydrase inhibitors, e.g. acetazolamide; loop diuretics, e.g. furosemide; osmotic diuretics, e.g. mannitol; potassium-sparing diuretics, e.g. amiloride, or in combination with other diuretics; thiazide diuretics, e.g. bendroflumethiazide
Table 1: Principal drug interactions of local anaesthetic agents and other medications
Local anaesthetic agent Proprietary name Principal drug interactionsEffect of interaction
Lidocaine
Xylocaine
Antiarrhythmic agents
Antibacterial agents
Antipsychotics
Antivirals
Beta-blockers
Diuretics
Dolasetron
Ulcer-healing drugs
Increased myocardial depression
Increased risk of ventricular arrhythmias if lidocaine is given with quinpristin/dalfopristin
Increased risk of ventricular arrhythmias if lidocaine is given with any drug that prolongs the QT interval of the cardiac cycle
Plasma concentration of lidocaine increased by amprenavir, atazanavir and lopinavir
Increased myocardial depression
Increased risk of lidocaine toxicity when given with propranolol
The action of lidocaine is antagonized by the hypokalaemia caused by acetazolamide, loop diuretics or thiazide and related diuretics (i.e. a greater dose of lidocaine would be required to achieve anaesthesia)
Increased risk of ventricular arrhythmia if lidocaine is given with dolasetron
Plasma concentration of lidocaine increased when given with cimetidine; risk of lidocaine toxicity increased with cimetidine
Bupivacaine
Marcain
Levo-bupivacaine
Chirocaine
Beta-blockersIncreased risk of bupivacaine toxicity when given with propranolol
Increased risk of myocardial depression if given with other antiarrhythmic agents
Prilocaine
Citanest
Antiarrhythmic agents
Antibacterial agents
Increased risk of myocardial depression if given with antiarrhythmic agents
Increased risk of methaemoglobinaemia if given with sulphonamide antibacterial agents
Ropivacaine
Naropin
AntidepressantsMetabolism of ropivacaine is inhibited by fluvoxamine, thereby enhancing the risk of ropivacaine toxicity
Mepivacaine
Scandonest
Drug not listed in the British National Formulary

spi·ro·no·lac·tone

(spī'rō-nō-lak'tōn)
A diuretic agent that blocks the renal tubular actions of aldosterone.

spironolactone (spī´rənōlak´tōn),

n brand names: Aldactone, Spirozide;
drug class: potassium-sparing diuretic;
action: competes with aldosterone at receptor sites in distal tubule, resulting in excretion of sodium chloride and water and retention of potassium and phosphate;
uses: treatment for edema, hypertension, diuretic-induced hypokalemia, and cirrhosis of the liver with ascites.

spironolactone

a competitive antagonist of aldosterone, used as a diuretic. It increases resorption of sodium in the distal renal tubules.