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曲洛司坦

Trilostane

4-alpha, 5-alpha-Epoxy-17-beta-hydroxy-3-oxoandrostane-2-alpha-carbonitrile

腎上腺類固醇合成抑制劑PO狗貓馬

別名: Vetoryl · Modrastane · Desopan · Modrenal · WIN 24540 · Trilostanum

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

2.2-6.7 mg/kg PO once a day with foodPO· q24h
— 🐕

劑量為合格獸醫專業人員的臨床參考。請務必對照最新仿單及個別病患確認。

各物種劑量

🌎 NA — North America🌍 EU — Europe

狗

適應症劑量途徑頻次療程地區
Hyperadrenocorticism (HAC) - Label Dose2.2-6.7 mg/kg PO once a day with foodPOq24h—🌎 NA
Hyperadrenocorticism (HAC) - Alternative Protocol2-10 mg/kg PO once dailyPOq24h—🌎 NA
Hyperadrenocorticism (HAC) - Low Dose Protocol1 mg/kg PO once dailyPOq24h—🌎 NA
Alopecia X (Alaskan Malamutes)3-3.6 mg/kg PO twice a dayPOq12h4-6 months🌎 NA
Alopecia X (Miniature poodles and Pomeranians)10.85 mg/kg per day given either once a day or divided twice a dayPOq24h or q12h4-8 weeks🌎 NA
Hyperadrenocorticism2 mg/kg p.o. q24h or 1 mg/kg p.o. q12hPOq12h or q24hLifelong🌍 EU
  • Hyperadrenocorticism (HAC) - Label Dose: Adjust dose based on ACTH stimulation test 10-14 days post-initiation. May require twice daily dosing if clinical signs are not controlled for the full day.
  • Hyperadrenocorticism (HAC) - Alternative Protocol: Doses of up to 50 mg/kg/day divided twice daily have been given. Adjust based on ACTH stim test 4-6 hours post-dose.
  • Hyperadrenocorticism (HAC) - Low Dose Protocol: Recheck in 1 week. Adjust based on clinical response, UCCR, and ACTH stimulation test.
  • Alopecia X (Miniature poodles and Pomeranians): Average dose reported.
  • Hyperadrenocorticism: Give with food. Adjust dose based on monitoring.

貓

適應症劑量途徑頻次療程地區
Hyperadrenocorticism7 mg/kg/day divided and given twice dailyPOq12h—🌎 NA
Hyperadrenocorticism15 mg (total dose) PO once daily to 60 mg (total dose) PO q12hPOq24h to q12h—🌎 NA
Hyperadrenocorticism10-30 mg/cat p.o. q12-24hPOq12h to q24hLifelong🌍 EU
  • Hyperadrenocorticism: Doses of up to 60 mg per cat per day have been used.
  • Hyperadrenocorticism: Titrate dose with ACTH stimulation tests. Cats typically remain diabetic despite clinical improvement.
  • Hyperadrenocorticism: Give with food.

馬

適應症劑量途徑頻次療程地區
Equine Cushing's syndrome0.4-1 mg/kg (total dose 120-240 mg) PO once dailyPOq24h—🌎 NA

劑量為合格獸醫專業人員的臨床參考。請務必對照最新仿單及個別病患確認。

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概覽

曲洛司坦（Trilostane）是一種合成的類固醇類似物，目前是治療犬隻腦下垂體依賴型及腎上腺依賴型腎上腺皮質機能亢進（庫興氏症候群）的​標準藥物​。

與會導致腎上腺皮質壞死的舊型療法（如 Mitotane）不同，曲洛司坦能可逆地抑制類固醇生成。這使其通常更安全且效果更可預測，但仍需密切監測以防止醫源性腎上腺皮質機能低下（愛迪生氏症）。

​主要臨床用途：​

  • ​犬：​ 腦下垂體依賴型及腎上腺依賴型庫興氏症候群；X 脫毛症（Alopecia X，特別是博美犬和阿拉斯加雪橇犬）。
  • ​貓：​ 貓腦下垂體依賴型庫興氏症候群（仿單標示外使用）。
  • ​馬：​ 馬庫興氏症候群 / 腦下垂體中葉機能異常 (PPID)（仿單標示外使用，儘管 Pergolide 通常是 PPID 的第一線治療藥物）。

​臨床要點：​ 當用於患有腎上腺腫瘤的犬隻時，曲洛司坦能控制庫興氏症的臨床症狀，但​不會​使腫瘤縮小。事實上，在治療期間，腎上腺可能會因失去負回饋機制而發生代償性肥大並增加體積。

作用機轉

Trilostane acts as a competitive, reversible, and dose-dependent inhibitor of the enzyme ​3-beta hydroxysteroid dehydrogenase (3β-HSD)​.

  • ​Pathway Blockade:​ Pregnenolone → ​[3β-HSD Blocked]​ → Progesterone
  • By blocking this crucial early step in the adrenal steroidogenesis pathway, trilostane effectively reduces the downstream synthesis of cortisol, aldosterone, and adrenal androgens.
  • Because the inhibition is competitive and reversible, the suppressive effects on cortisol production wane within 10 to 20 hours, necessitating daily or twice-daily dosing.

安全性與警告

禁忌症

  • Hypersensitivity to trilostane
  • Pregnancy (reduces progesterone synthesis)
  • Use with caution in patients with renal impairment
  • Use with caution in patients with hepatic impairment
  • Renal insufficiency
  • Hepatic insufficiency

不良反應

  • Lethargy
  • Inappetence
  • Vomiting
  • Diarrhea
  • Mild electrolyte abnormalities (hyponatremia, hyperkalemia)
  • Iatrogenic hypoadrenocorticism (Addisonian crisis)
  • Adrenal necrosis (rare but potentially fatal)
  • Mild gastrointestinal signs
  • Mild increases in serum potassium, bilirubin, and calcium
  • Clinical hypoadrenocorticism (Addisonian crisis)
  • Adrenal hyperplasia (with prolonged treatment)
  • Prolonged adrenal suppression after drug withdrawal

注意事項

Trilostane is contraindicated in pregnant dogs and should be used with caution in lactating animals. It should be used cautiously in patients with pre-existing renal or hepatic impairment.

​Important:​ Trilostane does not shrink adrenal tumors; adrenal glands may actually increase in size during therapy due to loss of negative feedback.

​Human Safety Warning:​ Trilostane is an FDA Category X drug (contraindicated in pregnancy). Pregnant women or women trying to conceive must not handle the capsules.

藥物交互作用

ACE Inhibitors (e.g., benazepril, enalapril)

Could increase risk for hyperkalemia

Aminoglutethimide

May potentiate the effects of trilostane and lead to hypoadrenocorticism

Ketoconazole

May potentiate the effects of trilostane and lead to hypoadrenocorticism

MitotaneMajor

May potentiate the effects of trilostane and lead to hypoadrenocorticism

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

Could increase risk for hyperkalemia

Potassium supplements / High potassium foods

Could increase risk for hyperkalemia

ItraconazoleModerate

Concurrent suppression of adrenal function

監測

  • Clinical signs (water intake, urination, appetite, energy level)
  • Adverse effects (vomiting, diarrhea, lethargy)
  • Serum electrolytes (Sodium and Potassium)
  • Urinalysis (Specific gravity, glucose, urine cortisol:creatinine ratio [UCCR])
  • ACTH stimulation tests (conducted 4-6 hours post-pill)
  • Clinical signs (water intake, urination, appetite, hair coat)
  • ACTH stimulation test (3 hours post-pill)
  • Pre-pill baseline cortisol
  • Serum electrolytes (potassium, calcium)
  • Liver parameters (bilirubin)

藥物動力學

吸收

In dogs, orally administered trilostane is rapidly but erratically absorbed. Peak levels occur between 1.5-2 hours post-dose. It is unknown if food significantly alters absorption, but administration with food is recommended.

代謝

Metabolized in the liver to several metabolites, including the active metabolite ketotrilostane.

排除

Drug levels return to baseline after 18 hours. Effects on cortisol production wane within 10-20 hours of dosing.

過量

Acute overdoses are unlikely to be life-threatening, and severe clinical signs are not typically expected immediately.

  • ​Monitoring:​ Assess blood pressure, hydration status, and electrolyte balance (Na/K).
  • ​Treatment:​ If the animal is stressed or showing signs of hypoadrenocorticism, consider administering exogenous corticosteroids short-term.
  • Because the drug's effects are relatively short-lived, monitoring of uncomplicated patients is usually only required for a few days post-ingestion.

可用產品

劑型

  • Oral capsules: 10 mg, 30 mg, 60 mg, 120 mg
  • Oral capsules: 5 mg (named patient basis)
  • Liquid formulation (named patient basis)

獸醫用

  • Vetoryl Oral Capsules: 10 mg, 30 mg, & 60 mg (packaged in aluminum foil blister cards)
  • Vetoryl 10 mg, 30 mg, 60 mg, 120 mg capsules

人用標示

  • Modrastane (Withdrawn from the US market in 1994)

各地核准狀態

European Union✓ 已核准處方藥EMA
🐕 Dogs

POM-V

United Kingdom✓ 已核准處方藥VMD
🐕 Dogs

POM-V

暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU

儲存與穩定性

Store commercially available trilostane capsules at room temperature in tight, light-resistant containers.

飼主須知

曲洛司坦是一種控制庫興氏症非常有效的藥物，但需要謹慎處理和監測。

​處理注意事項：​

  • ​請將藥物放在兒童和寵物接觸不到的地方。​
  • ​懷孕警告：​ 懷孕或正在備孕的婦女​絕對不可​接觸這些膠囊，因為該藥物可能會影響人類妊娠。
  • 接觸藥物後請徹底洗手。
  • 請勿打開、清空或試圖分割膠囊。

​給藥方式：​

  • 請完全依照獸醫的指示給藥，最好​隨餐給予​以促進吸收。
  • 請理解此藥物是​控制病情而非治癒疾病​。您的寵物可能需要終身服用此藥。

​需要注意的狀況：​

  • 在服藥的最初幾天，隨著寵物身體適應較低的類固醇濃度，可能會出現輕微的精神不振或食慾下降。
  • 如果您的寵物出現嚴重的精神不振、嘔吐、腹瀉、虛脫或完全拒食，請​立即停藥並聯繫您的獸醫​。這些可能是皮質醇濃度降得太低（愛迪生氏症危機）的徵兆。

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