卡托普利
Captopril
1-[(2S)-3-mercapto-2-methylpropionyl]-L-proline (SQ-14225)
別名: Capoten · Capozide · captoprilum · SQ-14225
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 |
|---|---|---|---|---|---|
| CHF / Hypertension | 0.5-2 mg/kg PO three times daily | PO | TID | — | 🌎 NA |
| CHF / Hypertension | 0.5-2 mg/kg PO q8-12h | PO | q8-12h | — | 🌎 NA |
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| CHF / Hypertension | 1/4 to 1/2 of a 12.5 mg tablet PO q8-12h | PO | q8-12h | — | 🌎 NA |
| Dilative, restrictive or hypertrophic cardiomyopathy | 0.55-1.54 mg/kg PO q8-12h | PO | q8-12h | — | 🌎 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。
概覽
卡托普利 (Captopril) 是一種含有巰基的第一代血管張力素轉化酶 (ACE) 抑制劑。它最初是從南美蝮蛇的毒液中分離出來的胜肽衍生物。雖然作為首個上市的 ACE 抑制劑具有歷史意義，但由於其半衰期較短（通常需要每天給藥三次）且不良反應（特別是狗的胃腸道不適）發生率較高，目前在獸醫學中的應用已大部分被依那普利 (Enalapril) 和貝那普利 (Benazepril) 等較新的藥物所取代。
臨床要點：與依那普利不同，卡托普利本身即為活性藥物，不需要經過肝臟生物轉化為活性代謝物即可發揮作用。
作用機轉
Captopril acts as a competitive inhibitor of angiotensin-converting enzyme (ACE), for which it has a much higher affinity than the natural substrate, angiotensin-I.
- Angiotensin I → (blocked by ACE) → Angiotensin II (a potent vasoconstrictor).
- The reduction in Angiotensin II leads to vasodilation, decreasing total peripheral resistance, pulmonary vascular resistance, and blood pressure.
- Decreased Angiotensin II also reduces aldosterone secretion, leading to decreased sodium and water retention, while increasing plasma renin activity.
- Cardiovascular benefits in CHF include increased cardiac output, stroke volume, and exercise tolerance with little to no change in heart rate.
安全性與警告
禁忌症
- Hypersensitivity to ACE inhibitors
不良反應
- Hypotension
- Renal failure
- Hyperkalemia
- Vomiting
- Diarrhea
- Skin rashes (reported in humans, not dogs)
- Neutropenia/agranulocytosis (rare, reported in humans)
注意事項
Use with caution and under close supervision in patients with renal insufficiency; doses may need to be reduced.
Use cautiously in patients with hyponatremia or sodium depletion, coronary or cerebrovascular insufficiency, preexisting hematologic abnormalities, or collagen vascular diseases (e.g., SLE).
Patients with severe CHF should be monitored very closely upon initiation of therapy to prevent profound hypotension.
Reproductive Safety: Captopril crosses the placenta. High doses in rodents caused decreased fetal weights and increased mortality. Use during pregnancy only when potential benefits outweigh risks (FDA Category C for 1st trimester; Category D for 2nd/3rd trimesters). Enters milk at ~1% of maternal plasma concentrations.
藥物交互作用
Reduced oral absorption of captopril; separate dosing by at least two hours.
Concomitant use has caused neurologic dysfunction in human patients.
Digoxin levels may increase 15-30%; monitor serum digoxin levels.
Concomitant use may cause hypotension; titrate dosages carefully.
May reduce the clinical efficacy of captopril when used as an antihypertensive agent.
Increased risk of developing hyperkalemia.
Can decrease renal excretion of captopril, possibly enhancing clinical and toxic effects.
Concomitant use may cause additive hypotension; titrate dosages carefully.
監測
- Clinical signs of CHF (respiratory rate/effort, exercise tolerance)
- Blood pressure (especially if treating hypertension or if signs of hypotension arise)
- Serum electrolytes (monitor for hyperkalemia)
- Renal panel (Creatinine, BUN)
- Urine protein
- CBC with differential (periodic)
藥物動力學
半衰期
吸收
In dogs, ~75% of an oral dose is absorbed, but food in the GI tract reduces bioavailability by 30-40%.
分佈
Distributed to most tissues (excluding the CNS). Approximately 40% bound to plasma proteins in dogs. Crosses the placenta and enters milk.
代謝
Metabolized in the liver.
排除
More than 95% of a dose is excreted renally, both as unchanged drug (45-50%) and as metabolites. Half-life is significantly prolonged in patients with renal dysfunction.
過量
The primary concern in an overdose situation is hypotension.
- Treatment: Supportive treatment with volume expansion using normal saline is recommended to correct blood pressure.
- Toxicity thresholds: Dogs given 1.5 g/kg orally developed emesis and decreased blood pressure. Dogs receiving doses greater than 6.6 mg/kg q8h may develop renal failure.
可用產品
劑型
- Oral Tablets
- Oral Suspension (compounded)
人用標示
- Captopril Oral Tablets: 12.5 mg, 25 mg, 50 mg, & 100 mg (Capoten®, generic)
- Captopril and Hydrochlorothiazide Oral Tablets: 15mg/25mg, 15mg/50mg, 25mg/25mg, 25mg/50mg (Capozide®, generic)
各地核准狀態
暫無法規資料: 🇺🇸 US · 🇪🇺 EU · 🇬🇧 UK · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Store tablets in tight containers at temperatures not greater than 30°C. Compounded oral suspension (0.75 mg/mL in Ora-Plus/Ora-Sweet) retains >90% potency for 14 days at 5°C and 7 days at 25°C; protect from light.
飼主須知
重要提示：請在空腹時（飯前1小時或飯後2小時）給予此藥物，除非獸醫師另有指示，因為食物會顯著降低其吸收率。
- 未經獸醫師同意，請勿突然停藥或減少劑量。
- 如果寵物出現持續或嚴重的嘔吐、腹瀉，請立即聯繫您的獸醫師，因為這可能導致危險的脫水和低血壓。
- 密切觀察寵物是否有嗜睡、虛弱或病情惡化的跡象，這可能表明血壓過低或心臟病加重。
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