螺內酯
Spironolactone
別名: Aldactone · Aldactazide · Cardalis · Prilactone · espironolactona · SC-9420 · spirolactone · spironolactonum
由 VetSheet 獸醫團隊審訂更新於 2026年4月5日本內容以實證獸醫文獻為本
劑量為持牌獸醫專業人員的臨床參考。請務必對照最新藥品說明書及個別病患確認。
各物種劑量
🌎 NA — North America🌍 EU — Europe
狗
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| As a diuretic in CHF (when furosemide and ACE inhibitors alone do not control fluid accumulation) | 1-2 mg/kg PO q12h | PO | q12h | — | 🌎 NA |
| As a diuretic in CHF (with other diuretics when hypokalemia is an issue) | 2-4 mg/kg PO once daily | PO | q24h | — | 🌎 NA |
| As a diuretic in CHF (to allow further reduction of furosemide dose) | 0.5 mg/kg PO once daily to 2 mg/kg twice daily | PO | q24h to q12h | — | 🌎 NA |
| For treating ascites (using fixed dose combination with hydrochlorothiazide) | 0.5-1 mg/kg PO twice daily | PO | q12h | — | 🌎 NA |
| For treating ascites (caused by right-sided heart failure) | 1-2 mg/kg PO q12h | PO | q12h | — | 🌎 NA |
| For adjunctive treatment of hypertension | 1-2 mg/kg PO q12h | PO | q12h | — | 🌎 NA |
| For adjunctive treatment of hypertension (Step 4 drug) | 1-2 mg/kg twice daily | PO | q12h | — | 🌎 NA |
| Congestive heart failure, ascites, hyperaldosteronism | 2-4 mg/kg | PO | q24h | Continuous | 🌍 EU |
- As a diuretic in CHF (when furosemide and ACE inhibitors alone do not control fluid accumulation): Refractory CHF
- As a diuretic in CHF (to allow further reduction of furosemide dose): 0.5 mg/kg once daily for aldosterone blockage (weak diuretic effect); 2 mg/kg twice daily for stronger diuretic effect.
- For treating ascites (using fixed dose combination with hydrochlorothiazide): Empirical dosage based on the spironolactone component of Aldactazide.
- For treating ascites (caused by right-sided heart failure): Added to optimized furosemide and ACE inhibitor therapy.
- For adjunctive treatment of hypertension (Step 4 drug): For systolic >160 mmHg, diastolic >120 mmHg after enalapril/benazepril and amlodipine.
- Congestive heart failure, ascites, hyperaldosteronism: Licensed for use in combination with standard therapy for treatment of CHF caused by valvular regurgitation in dogs.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| As a diuretic in CHF (when furosemide and ACE inhibitors alone do not control fluid accumulation) | 1-2 mg/kg PO q12h | PO | q12h | — | 🌎 NA |
| As a diuretic in CHF (when serum potassium is low) | 1 mg/kg q12h PO | PO | q12h | — | 🌎 NA |
| For adjunctive treatment of hypertension | 1-2 mg/kg PO q12h | PO | q12h | — | 🌎 NA |
| For adjunctive treatment of hypertension (Step 3 drug) | 1-2 mg/kg twice daily | PO | q12h | — | 🌎 NA |
| For adjunctive treatment of primary hyperaldosteronism | 1-2 mg/kg PO twice daily | PO | q12h | — | 🌎 NA |
| Congestive heart failure, ascites, hyperaldosteronism | 2-4 mg/kg | PO | q24h | Continuous | 🌍 EU |
- As a diuretic in CHF (when furosemide and ACE inhibitors alone do not control fluid accumulation): Refractory CHF
- For adjunctive treatment of hypertension (Step 3 drug): When systolic BP >160 mmHg, diastolic >120 mmHg after amlodipine and ACE inhibitor.
- For adjunctive treatment of primary hyperaldosteronism: If potassium supplementation alone does not control clinical signs.
- Congestive heart failure, ascites, hyperaldosteronism: Severe ulcerative facial dermatitis has been reported in Maine Coon cats.
劑量為持牌獸醫專業人員的臨床參考。請務必對照最新藥品說明書及個別病患確認。
概覽
螺內酯(Spironolactone)是一種合成的醛固酮拮抗劑和保鉀利尿劑。在獸醫學中,它主要作為鬱血性心衰竭(CHF)、腹水、全身性高血壓和原發性醛固酮增多症(特別是在貓)的輔助治療藥物。
臨床重點與藥理背景:
- 醛固酮逃逸(Aldosterone Escape): 雖然與呋塞米(Furosemide)等環利尿劑相比,其直接利尿效果較弱,但螺內酯在阻斷腎素-血管張力素-醛固酮系統(RAAS)中扮演著關鍵角色。即使病患正在服用ACE抑制劑,醛固酮水平最終仍可能反彈升高(即「醛固酮逃逸」現象),而螺內酯能有效減輕此現象。
- 心肌保護作用: 在人類醫學中,螺內酯因其對心肌的抗纖維化作用而受到高度重視,有助於防止有害的心臟重塑。雖然這種益處在獸醫病患(如患有黏液瘤性二尖瓣疾病的狗)中的程度仍有爭議,但它已越來越多地被納入標準的多重藥物CHF治療方案中。
- 生物可用率: 與食物一起服用可顯著提高其吸收率。
作用機制
Spironolactone acts as a competitive antagonist at the mineralocorticoid receptor.
- Mechanism: It competitively inhibits aldosterone binding in the distal renal tubules and collecting ducts.
- Pathway: Blockade of the receptor → prevents the synthesis of aldosterone-induced proteins (such as Na+/K+ ATPase and epithelial sodium channels) → decreases sodium and chloride reabsorption while decreasing potassium, ammonium, and phosphate excretion.
- Result: Mild diuresis with potassium retention. It does not affect carbonic anhydrase or proximal renal transport mechanisms.
安全性與警告
禁忌症
- Hyperkalemia
- Addison's disease (hypoadrenocorticism)
- Anuria
- Acute renal failure
- Significant renal impairment
- Hyperkalaemia
- Hyponatraemia
- Concurrent use with NSAIDs in animals with renal insufficiency
- Pregnancy
- Lactation
- Animals intended for breeding
不良反應
- Facial dermatitis (notably reported in Maine Coon cats)
- Hyperkalemia
- Hyponatremia
- Dehydration
- Increased BUN and mild acidosis (in patients with renal impairment)
- Gastrointestinal distress (vomiting, anorexia)
- CNS effects (lethargy, ataxia)
- Endocrine changes (anti-androgenic effects, e.g., gynecomastia in humans, feminization of male fetuses)
- Hyponatraemia
- Hyperkalaemia
- Reversible prostatic atrophy (in entire male dogs)
- Severe ulcerative facial dermatitis (in Maine Coon cats)
- Hepatotoxicity (reported in humans)
注意事項
Hepatic & Renal Caution: Use cautiously in patients with hepatic disease (though often used to treat ascites). Use in patients with renal impairment may lead to hyperkalemia.
Reproductive Safety: FDA Category D for pregnancy. Spironolactone and its active metabolites cross the placenta and can cause feminization of male fetuses. Canrenone (active metabolite) is excreted in breast milk; use with caution in nursing animals.
藥物相互作用
Spironolactone may increase the half-life of digoxin; enhanced monitoring of digoxin serum levels is warranted. May also cause falsely elevated digoxin values if using a radioimmune assay (RIA).
Spironolactone may mute the effects of mitotane if given concurrently; monitor carefully.
Possible increase in neuromuscular blockade effects.
Increased risk of hyperkalemia.
Increased risk of hyperkalemia.
Spironolactone's diuretic effects may be decreased if administered concomitantly.
Potentiates diuretic effects
Potentiates diuretic effects
Increased risk of hyperkalaemia (though generally safe to use concurrently in practice; monitor potassium)
Increased risk of hyperkalaemia and nephrotoxicity
Increased risk of hyperkalaemia
監測
- Serum electrolytes (especially potassium and sodium)
- BUN and creatinine
- Hydration status
- Blood pressure (if indicated)
- Clinical signs of edema/ascites
- Patient weight
- Serum potassium
- Serum sodium
- Renal function (BUN, Creatinine)
- Digoxin levels (if used concurrently)
藥物動力學
半衰期
吸收
In fasted dogs, oral bioavailability is approximately 50%, but increases up to 90% when given with food. In humans, it is >90% bioavailable with peak levels reached within 1-2 hours.
分佈
Spironolactone and its active metabolite, canrenone, are both about 98% bound to plasma proteins. Both cross the placenta, and canrenone is detected in breast milk.
代謝
Rapidly metabolized to several metabolites, including the active metabolite canrenone, which possesses diuretic activity.
排除
About 70% of a dose is found in the feces and 18% in the urine.
過量
Information on acute overdosage of spironolactone in veterinary patients is limited.
- Management: Should an acute overdose occur, follow general guidelines for diuretic overdose (e.g., furosemide or chlorothiazide).
- Treatment: Empty the stomach if ingestion was recent. Provide supportive care, monitor hydration status, and closely evaluate serum electrolytes (especially potassium and sodium).
- Contact an animal poison control center for further guidance.
可用產品
劑型
- Oral tablets
- Oral suspension (compounded)
- 10 mg tablet
- 40 mg tablet
- 50 mg tablet
- 80 mg tablet
- 100 mg tablet
- Compound preparations with benazepril (e.g., 2.5mg/20mg, 5mg/40mg, 10mg/80mg)
獸醫用
- Cardalis (compound with benazepril)
- Prilactone
人用標示
- Spironolactone Oral Tablets: 25 mg, 50 mg & 100 mg; Aldactone® (Searle); generic
- Spironolactone/Hydrochlorothiazide Oral Tablets: 25 mg/25 mg & 50 mg/50 mg; Aldactazide® (Searle); generic
- Spironolactone generics
各地核准狀態
POM-V / POM
POM-V / POM
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Store tablets at room temperature in tight, light-resistant containers. An extemporaneously prepared oral suspension using pulverized tablets and cherry syrup is reportedly stable for at least one month when refrigerated.
飼主須知
- 給藥方式: 請將此藥物與食物一起餵食,這能大幅提高藥物在體內的吸收率。
- 鉀離子警告: 因為此藥物會幫助身體保留鉀離子,請勿給予您的寵物額外的鉀補充劑或改用高鉀飲食,除非獸醫師特別指示。
- 何時該聯繫獸醫師: 如果您的寵物出現嚴重或持續的嘔吐、腹瀉、食慾不振,或極度疲倦/虛弱,請立即通知您的獸醫師。
- 貓咪飼主請注意: 少部分貓咪(特別是緬因貓)在服用此藥期間可能會出現嚴重的臉部搔癢、結痂或皮膚炎。如果您發現貓咪過度抓臉,請聯繫您的獸醫師。
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