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厄貝沙坦

Irbesartan

Irbesartanum

血管張力素II受體拮抗劑 (ARB)PO狗

別名: Avalide · Aprovel · Karvea · Arbit · Cavapro · Coaproval · BMS 186295 · SR 47436 · Irbesartanum

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

5 mg/kg PO q12-24 hours.PO· q12-24h
— 🐕

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
As an alternative to ACE inhibitors for treatment of hypertension associated with renal insufficiency5 mg/kg PO q12-24 hours.POq12-24h—🌎 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

厄貝沙坦是一種​血管張力素II受體拮抗劑 (ARB)​，主要用於人類醫學以控制高血壓和糖尿病腎病變。在獸醫學中，其使用經驗目前非常有限，但可作為 ACE 抑制劑（如依那普利或貝那普利）的替代或輔助藥物，用於治療​伴隨腎功能不全的犬隻高血壓​。

​臨床要點：​ 當病患出現「ACE 逃逸現象」（即儘管使用 ACE 抑制劑，醛固酮濃度仍反彈）或無法耐受 ACE 抑制劑時，常會考慮使用 ARB。與需要肝臟轉化為活性代謝物的氯沙坦 (Losartan) 不同（犬隻對此轉化效率不佳），厄貝沙坦以其原型發揮活性，使其成為犬隻病患更可靠的選擇。

​主要特點：​

  • 可能對繼發於腎臟疾病的高血壓有用。
  • 缺乏用於犬隻心臟衰竭的充分文獻支持。
  • 由於具有致畸胎性，​嚴禁於懷孕期間使用​。

作用機轉

Irbesartan selectively and competitively blocks the AT1 (Angiotensin II Type 1) receptor in the Renin-Angiotensin-Aldosterone System (RAAS).

  • ​Pathway:​ Angiotensinogen → Angiotensin I → Angiotensin II.
  • Angiotensin II normally binds to AT1 receptors to cause potent vasoconstriction and stimulate aldosterone release.
  • By blocking the AT1 receptor, irbesartan prevents these effects, leading to vasodilation, decreased aldosterone synthesis, reduced potassium excretion, and increased sodium and water excretion.
  • ​Pharmacologic Advantage:​ It does not inhibit ACE (kininase II), so it does not interfere with bradykinin or substance P responses. Furthermore, it does not require hepatic conversion to an active metabolite, which is a significant pharmacokinetic advantage in dogs compared to losartan.

安全性與警告

禁忌症

  • Pregnancy (teratogenic)
  • Nursing/lactating animals
  • Hypotension
  • Uncorrected volume depletion
  • Uncorrected sodium depletion
  • Hypersensitivity to irbesartan

不良反應

  • Diarrhea
  • Dyspepsia (indigestion)
  • Fatigue or somnolence
  • Orthostatic hypotension
  • Dizziness

注意事項

​Important Warnings:​

  • ​Hypovolemia/Hyponatremia:​ Patients who are volume- or sodium-depleted must have these deficits corrected prior to initiating therapy to avoid acute hypotensive crises.
  • ​Pregnancy Warning:​ Irbesartan is highly teratogenic (FDA Category D). It causes fetal abnormalities (renal pelvic cavitation, hydroureter) and increased maternal death/spontaneous abortion. Discontinue immediately if pregnancy is detected.
  • ​Hypotension:​ Do not use in patients with pre-existing hypotension.

藥物交互作用

Other antihypertensive agents (e.g., amlodipine, ACE inhibitors)

Increased risk of additive hypotension. Use with caution and monitor blood pressure closely.

Diuretics

May exacerbate volume depletion and increase the risk of severe hypotension.

監測

  • Systemic blood pressure
  • Heart rate
  • Serum electrolytes (especially potassium)
  • BUN and Creatinine (renal function)
  • Clinical signs of adverse effects (GI upset, lethargy, weakness)

藥物動力學

半衰期

狗9 hours (single dose) to 21 hours (multiple doses)

吸收

In humans, absorption is rapid with a bioavailability of 60-80%. Peak levels occur in 1.5-2 hours. Bioavailability is not altered by food.

分佈

Highly protein-bound (90% in humans). Crosses the blood-brain barrier and placenta in small quantities.

代謝

Metabolized in the liver via glucuronidation and oxidation. Metabolites are inactive. Does not require conversion to an active metabolite to exert its effects.

排除

Eliminated primarily in the feces (both unchanged drug and metabolites) and to a lesser extent in the urine. Dosage adjustment is not required for renal dysfunction.

過量

​Toxicity Profile:​ Irbesartan has a wide margin of safety in acute overdose scenarios. Rats and mice have survived acute oral overdoses exceeding 2000 mg/kg.

​Clinical Signs of Overdose:​

  • Severe hypotension
  • Tachycardia (reflex) or bradycardia

​Treatment:​

  • Treatment is largely supportive and symptomatic.
  • Address hypotension with intravenous fluids and cardiovascular support as needed.
  • Contact an animal poison control center for specific guidance.

可用產品

劑型

  • Tablets

人用標示

  • Irbesartan Tablets: 75 mg, 150 mg, & 300 mg (Avapro)
  • Irbesartan 150 mg with Hydrochlorothiazide 12.5 mg Tablets (Avalide)
  • Irbesartan 300 mg with Hydrochlorothiazide 12.5 mg or 25 mg Tablets (Avalide)

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 at room temperature (15-30°C).

飼主須知

​寵物主人指引：​

  • ​給藥方式：​ 您可以將此藥物與食物一起或空腹餵食。如果您的寵物在空腹服藥後嘔吐，請嘗試在未來的劑量中加入少量零食或隨餐給予。
  • ​新興療法：​ 獸醫界對此藥物的臨床經驗目前有限。請務必密切觀察您的寵物，若發現任何異常症狀（如腹瀉、極度疲倦或虛弱），請立即向您的獸醫師報告。
  • ​懷孕警告：​ ​絕對不可用於懷孕或哺乳中的動物。​ 此藥物會導致嚴重的出生缺陷或流產。如果您懷疑寵物懷孕，請立即聯繫您的獸醫師。
  • ​監測：​ 您的獸醫師可能需要定期測量寵物的血壓並進行血液檢查，以確保藥物安全有效地發揮作用。

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