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スピロノラクトン

Spironolactone

別名: Aldactone · Aldactazide · Cardalis · Prilactone · espironolactona · SC-9420 · spirolactone · spironolactonum

VetSheet 獣医チームが監修更新日 2026年4月5日エビデンスに基づく獣医学リファレンス

1-2 mg/kg PO q12hPO· q12h
🐕

用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。

動物種別用量

🌎 NA — North America🌍 EU — Europe

適応用量経路頻度期間地域
As a diuretic in CHF (when furosemide and ACE inhibitors alone do not control fluid accumulation)1-2 mg/kg PO q12hPOq12h🌎 NA
As a diuretic in CHF (with other diuretics when hypokalemia is an issue)2-4 mg/kg PO once dailyPOq24h🌎 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 dailyPOq24h to q12h🌎 NA
For treating ascites (using fixed dose combination with hydrochlorothiazide)0.5-1 mg/kg PO twice dailyPOq12h🌎 NA
For treating ascites (caused by right-sided heart failure)1-2 mg/kg PO q12hPOq12h🌎 NA
For adjunctive treatment of hypertension1-2 mg/kg PO q12hPOq12h🌎 NA
For adjunctive treatment of hypertension (Step 4 drug)1-2 mg/kg twice dailyPOq12h🌎 NA
Congestive heart failure, ascites, hyperaldosteronism2-4 mg/kgPOq24hContinuous🌍 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.

適応用量経路頻度期間地域
As a diuretic in CHF (when furosemide and ACE inhibitors alone do not control fluid accumulation)1-2 mg/kg PO q12hPOq12h🌎 NA
As a diuretic in CHF (when serum potassium is low)1 mg/kg q12h POPOq12h🌎 NA
For adjunctive treatment of hypertension1-2 mg/kg PO q12hPOq12h🌎 NA
For adjunctive treatment of hypertension (Step 3 drug)1-2 mg/kg twice dailyPOq12h🌎 NA
For adjunctive treatment of primary hyperaldosteronism1-2 mg/kg PO twice dailyPOq12h🌎 NA
Congestive heart failure, ascites, hyperaldosteronism2-4 mg/kgPOq24hContinuous🌍 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.

用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。

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概要

スピロノラクトンは合成​アルドステロン拮抗薬​およびカリウム保持性利尿薬です。獣医療では主に、うっ血性心不全(CHF)、腹水、全身性高血圧、および原発性アルドステロン症(特に猫)の補助治療として使用されます。

​臨床のポイントと薬理学的背景:​

  • ​アルドステロン・ブレイクスルー:​ フロセミドなどのループ利尿薬に比べて直接的な利尿効果は弱いものの、レニン・アンジオテンシン・アルドステロン系(RAAS)の阻害において重要な役割を果たします。ACE阻害薬を服用していても、最終的にアルドステロン値が再び上昇する現象(アルドステロン・ブレイクスルー)を防ぐ効果があります。
  • ​心筋保護作用:​ 人医療では、心筋の線維化を防ぎ、有害な心臓リモデリングを予防する効果が高く評価されています。獣医療(粘液腫様僧帽弁疾患の犬など)におけるこの効果の程度については議論がありますが、標準的なCHFの多剤併用プロトコルに組み込まれることが増えています。
  • ​バイオアベイラビリティ:​ 食事と一緒に投与することで吸収が大幅に向上します。

作用機序

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・警告

禁忌

  • 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

有害事象

  • 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.

医薬品相互作用

DigoxinModerate

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).

Mitotane

Spironolactone may mute the effects of mitotane if given concurrently; monitor carefully.

Neuromuscular blockers, non-depolarizing

Possible increase in neuromuscular blockade effects.

Potassium-sparing diuretics (e.g., triamterene)

Increased risk of hyperkalemia.

Potassium supplementsMajor

Increased risk of hyperkalemia.

Salicylates (e.g., Aspirin)

Spironolactone's diuretic effects may be decreased if administered concomitantly.

Thiazide diureticsModerate

Potentiates diuretic effects

Loop diureticsModerate

Potentiates diuretic effects

ACE inhibitorsModerate

Increased risk of hyperkalaemia (though generally safe to use concurrently in practice; monitor potassium)

NSAIDsMajor

Increased risk of hyperkalaemia and nephrotoxicity

CiclosporinModerate

Increased risk of hyperkalaemia

監視

  • 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)

薬物動態

半減期

Spironolactone: 1-2 hours; Canrenone (active metabolite): ~20 hours

吸収

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.

分布

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.

消失

About 70% of a dose is found in the feces and 18% in the urine.

過剰投与

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.

製品

製剤

  • 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)

動物用医薬品

  • Cardalis (compound with benazepril)
  • Prilactone

ヒト用医薬品

  • 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

規制ステータス

European Union✓ 承認済み処方箋医薬品EMA
🐕 Dogs

POM-V / POM

United Kingdom✓ 承認済み処方箋医薬品VMD
🐕 Dogs

POM-V / POM

規制データなし: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU

保管・安定性

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.

飼主向け情報

  • ​投与方法:​ 薬の体内への吸収を大幅に高めるため、​食事と一緒に​与えてください。
  • ​カリウムに関する注意:​ この薬は体内にカリウムを保持する働きがあるため、獣医師の特別な指示がない限り、​カリウムのサプリメントを与えたり、高カリウム食に変更したりしないでください​
  • ​獣医師への連絡の目安:​ 重度または持続的な嘔吐、下痢、食欲不振、または極度の疲労や虚弱が見られる場合は、獣医師にお知らせください。
  • ​猫の飼い主様へ:​ 一部の猫(特にメインクーン)では、この薬の服用中に顔の激しい痒み、かさぶた、または皮膚炎を発症することがあります。猫が顔を過剰に掻いているのに気づいた場合は、獣医師に連絡してください。

VetSheet医薬品リファレンスは獣医専門家の臨床意思決定支援を目的としており、専門的判断または製造業者の最新医薬品情報の代替にはなりません。