苯磺酸氨氯地平 (Amlodipine)
Amlodipine
Amlodipine besylate
別名: Norvasc · Lotrel (combination) · Caduet (combination) · Amodip · Istin · Amlodipini besilas · UK-48340-26 · UK-48340-11 · Amlodipine maleate · Amlodipine besylate · Amlodipino
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 |
|---|---|---|---|---|---|
| Adjunctive therapy for refractory heart failure (advanced mitral valve degeneration as an afterload reducer) | 0.2-0.4 mg/kg PO twice daily. Initiate therapy at 0.1 mg/kg PO twice daily and up-titrate weekly while monitoring blood pressure. | PO | q12h | — | 🌎 NA |
| Arterial vasodilator for refractory CHF secondary to mitral regurgitation | 0.1 mg/kg q12-24h initially; titrate up as needed to 0.25 mg/kg PO q12-24h | PO | q12-24h | — | 🌎 NA |
| Systemic hypertension in dogs with chronic renal disease | 0.1-0.5 mg/kg PO once daily (q24h) | PO | q24h | — | 🌎 NA |
| Systemic hypertension (2nd step drug) | 0.1 mg/kg q24h; step up to 0.2 mg/kg q24h if needed | PO | q24h | — | 🌎 NA |
| Systemic hypertension | 0.05-0.1 mg/kg (titrate upwards weekly as required, up to 0.5 mg/kg) | PO | q12-24h | Long-term | 🌍 EU |
- Adjunctive therapy for refractory heart failure (advanced mitral valve degeneration as an afterload reducer): After ACE inhibitor maintenance therapy has been established.
- Arterial vasodilator for refractory CHF secondary to mitral regurgitation: Monitor blood pressure.
- Systemic hypertension in dogs with chronic renal disease: Most often combined with an ACE inhibitor. May require weeks to months to achieve satisfactory control.
- Systemic hypertension (2nd step drug): Used after enalapril/benazepril. Each step added if after 1-2 weeks systolic BP > 160 mmHg.
- Systemic hypertension: Monitor blood pressure regularly. Consider concurrent ACE inhibitor.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Systemic hypertension (1st step drug) | 0.625 mg per cat q24h, if cat greater then 6 kg, 1.25 mg/cat q24h | PO | q24h | — | 🌎 NA |
| Systemic hypertension | 0.625-1.25 mg (total dose) PO once daily | PO | q24h | — | 🌎 NA |
| Systemic hypertension | 0.625-1.25 mg/cat | PO | q24h (may increase slowly or increase frequency to q12h if necessary) | Long-term | 🌍 EU |
- Systemic hypertension (1st step drug): Add ACE inhibitor if proteinuric.
- Systemic hypertension: Drug of choice; often successful as a single agent. Maximum effect seen within 7 days.
- Systemic hypertension: Blood pressure monitoring is essential. Appears safe even with concurrent renal failure.
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
Amlodipine 是一種二氫吡啶類鈣離子通道阻斷劑 (CCB)，在獸醫學中主要用作強效的周邊動脈血管擴張劑。
- 貓科醫學：它是治療貓全身性高血壓（通常繼發於慢性腎病、甲狀腺機能亢進或肥厚型心肌病）的黃金標準和第一線藥物。單獨使用於貓咪通常具有極佳療效。
- 犬科醫學：在狗中，它通常用作難治性充血性心衰竭 (CHF) 的輔助降低後負荷藥物，或作為第二線抗高血壓藥物。在狗單獨使用較高劑量時，可能會活化腎素-血管收縮素-醛固酮系統 (RAAS)，因此經常與 ACE 抑制劑（如 enalapril）合併使用以減輕此效應。
- 臨床要點：其作用起效相對緩慢，有助於防止急性低血壓危機，但漏服藥物可能導致血壓迅速反彈。
作用機制
Amlodipine selectively inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle by blocking L-type voltage-gated calcium channels.
- Vascular Smooth Muscle → Relaxation and vasodilation → Significant reduction in peripheral vascular resistance (afterload) → Decreased systemic blood pressure.
- It has a much higher affinity for vascular smooth muscle than cardiac muscle, meaning it produces profound vasodilation with minimal negative inotropic (contractility) or chronotropic (heart rate) effects at therapeutic doses.
- Cardiac Muscle → Mildly depresses impulse formation (automaticity) and conduction velocity.
安全性與警告
禁忌症
- Patients with cardiogenic shock
- Advanced aortic stenosis (relative contraindication)
- Use with caution in patients with heart failure (due to slight negative inotropic effects)
- Use with caution in patients with hepatic dysfunction
不良反應
- Cats: Infrequent azotemia, lethargy, hypokalemia, reflex tachycardia, weight loss
- Dogs: Gingival hyperplasia (with long-term use)
- Anorexia and hypotension (early in therapy)
注意事項
Renal Considerations in Cats: There is concern that using amlodipine alone for treating hypertension in cats with renal disease may expose glomeruli to higher pressures secondary to efferent arteriolar constriction (caused by localized RAAS activation). Using an ACE inhibitor concurrently may help prevent this, though routine use of ACE inhibitors with amlodipine in cats with CKD remains somewhat controversial.
- Cardiac Disease: Use cautiously in patients with heart failure due to slight negative inotropic effects.
- Hepatic Disease: Use cautiously as the drug is extensively metabolized in the liver; half-life may be prolonged.
- Pregnancy: Fetotoxic in laboratory animals at very high doses; prolonged labor in rats. FDA Category C.
藥物相互作用
Concomitant use may cause additive hypotension.
Concomitant use may cause additive hypotension.
Concomitant use may cause additive hypotension.
May cause hypotension if used concurrently.
May alter bioavailability of amlodipine.
May impair hepatic metabolism of amlodipine, increasing circulating levels
May impair hepatic metabolism of amlodipine, increasing circulating levels
May impair hepatic metabolism of amlodipine, increasing circulating levels
May impair hepatic metabolism of amlodipine, increasing circulating levels
CYP3A4 inducer; may reduce circulating amlodipine levels
Increased risk of hypotension when combined
監測
- Systemic blood pressure (frequent monitoring during dose titration)
- Ophthalmic exam (to assess for hypertensive retinopathy/retinal detachment)
- Renal values and electrolytes (especially if combined with ACE inhibitors)
- Clinical signs of hypotension (lethargy, weakness)
藥物動力學
半衰期
吸收
Slowly but almost completely absorbed after oral administration. Bioavailability is not altered by food.
分佈
Very high plasma protein binding characteristics (approximately 93%).
代謝
Slowly but extensively metabolized to inactive compounds in the liver.
排除
Hepatic metabolism and subsequent excretion.
過量
Overdoses pose a significant risk for profound hypotension and reflex tachycardia (though bradycardia is also possible). Common clinical signs in dogs and cats include lethargy and vomiting.
Treatment:
- When possible, massive overdoses should be managed with gut emptying (emesis/lavage) and activated charcoal.
- Provide aggressive supportive treatment (IV fluids).
- Specific therapies may include beta-agonists, intravenous lipid emulsion (ILE) therapy, and intravenous calcium to counteract the calcium channel blockade.
可用產品
劑型
- Oral tablets
- Oral suspension (compounded)
人用標示
- Amlodipine Oral Tablets: 2.5 mg, 5 mg, & 10 mg (Norvasc, generic)
- Fixed-dose combination products with benazepril (Lotrel) or atorvastatin (Caduet)
各地核准狀態
Amodip is approved for cats in the EU.
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. Compounded oral suspensions (1 mg/mL in Ora-Plus/Ora-Sweet) retain >90% potency for 91 days at 5°C and 25°C, but must be protected from light.
飼主須知
- 給藥方式：可與食物一起餵食或空腹餵食。
- 切勿漏藥：高血壓被稱為「無形殺手」。漏服藥物會導致血壓迅速反彈，可能引發急性失明、癲癇或嚴重的腎臟損傷。
- 監測：需定期回診測量寵物的血壓，以確保劑量正確。
- 副作用：在開始服藥時，請注意是否有嗜睡、虛弱或食慾不振的跡象。在狗中，長期使用可能會導致牙齦過度生長（牙齦增生）。
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