VetSheet

卡維地洛

Carvedilol

carvedilolum

β及α-1腎上腺素受體阻斷劑PO狗

別名: Coreg CR · Eucardic · BM-14190 · carvedilolum · Cardilol · Cardiol · Carloc · Carvil · Carvipress · Coritensil · Coropres · Dilatrend · Dilbloc · Dimitone · Divelol · Hybridil · Kredex · Querto

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

0.2 mg/kg PO twice daily initially with slow titration upwards towards a dose of 0.8 mg/kg twice dailyPO· twice daily
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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
Heart failure (adjunctive therapy)¼-½ of a 3.125 mg tablet PO twice dailyPOtwice daily—🌎 NA
Early/mild heart failure or later stages of CHF0.2 mg/kg PO twice daily initially with slow titration upwards towards a dose of 0.8 mg/kg twice dailyPOtwice daily—🌎 NA
Heart failure (target plasma concentration)0.5 mg/kg PO twice dailyPOtwice daily—🌎 NA
Dilated cardiomyopathy0.3 mg/kg PO q12hPOq12h3 months🌎 NA
Chronic heart failure / Dilated Cardiomyopathy (DCM)Start at 0.05-0.1 mg/kg, gradually increase at 2-week intervals to target dose of 0.3-0.4 mg/kgPOq12hLong-term🌍 EU
ACVIM stage B2 degenerative mitral valve disease0.3 mg/kg, increased at intervals up to 1.1 mg/kgPOq12hLong-term🌍 EU
  • Heart failure (adjunctive therapy): Usual starting dose. Start at the low end of the dosing range and gradually titrate upward carefully watching to avoid negative inotropic effects.
  • Early/mild heart failure or later stages of CHF: Beta blockers are best employed in dogs that are minimally symptomatic. Many dogs with CHF will not tolerate this upward titration.
  • Heart failure (target plasma concentration): Should result in beta-blockade, but maximum beta-blockade may require doses of >0.7-0.9 mg/kg. Because of bioavailability variations, plasma monitoring, clinical trials and uptitration protocols may be beneficial.
  • Dilated cardiomyopathy: Did not produce any significant improvements in neurohormonal activation, heart size, or owner-perceived quality of life. Doses >0.3 mg/kg q12h are likely to be required to effect changes in ventricular remodeling and function.
  • Chronic heart failure / Dilated Cardiomyopathy (DCM): Increase dose only if tolerated.
  • ACVIM stage B2 degenerative mitral valve disease: For cardiac remodelling with no signs of cardiac failure.

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

卡維地洛（Carvedilol）是一種獨特的第三代​非選擇性β受體阻斷劑​，同時具有​α-1腎上腺素受體阻斷​特性。在獸醫學中，主要被研究作為​犬擴張性心肌病 (DCM)​ 及慢性心臟衰竭的輔助治療。

  • ​雙重作用：​ 與傳統的β受體阻斷劑（如阿替洛爾）不同，卡維地洛提供額外的血管擴張作用，從而降低心臟後負荷。
  • ​具爭議性的使用：​ 其在獸醫心臟病學中的應用仍具爭議。雖然在人類心臟衰竭中已證實能降低死亡率，但在犬隻的研究中，標準劑量對於改善神經賀爾蒙活化或心室重塑的療效結果不一。
  • ​臨床要點：​ 卡維地洛具有強烈的負性肌力作用。它可能會導致晚期或症狀嚴重的心臟衰竭患畜出現急性代償失調。必須極度謹慎且緩慢地向上滴定劑量，且最好在症狀輕微的患畜中開始使用。

作用機轉

Carvedilol exerts its cardiovascular effects through multiple mechanisms:

  • ​Non-selective Beta-Adrenergic Blockade (β1 and β2):​ Heart failure leads to chronic sympathetic nervous system (SNS) activation → tachycardia, renin-angiotensin-aldosterone system (RAAS) activation, beta-receptor downregulation, and myocyte necrosis. Carvedilol blocks these receptors → reverses/diminishes SNS toxicity, reduces heart rate, and decreases myocardial oxygen demand.
  • ​Selective Alpha-1 Adrenergic Blockade:​ Blocks peripheral α1-receptors → vasodilation → reduces systemic vascular resistance and cardiac afterload.
  • ​Antioxidant Properties:​ Carvedilol and its metabolites act as potent scavengers of reactive oxygen species (ROS) and inhibit lipid peroxidation, protecting the myocardium from oxidative stress.
  • ​Antidysrhythmic Effects:​ Secondary to its beta-blocking and membrane-stabilizing properties.

安全性與警告

禁忌症

  • Class IV decompensated heart failure
  • Bronchial asthma
  • 2nd or 3rd degree AV block
  • Sick sinus syndrome (unless artificially paced)
  • Severe bradycardia
  • Cardiogenic shock
  • Hypersensitivity to the drug

不良反應

  • Inappetence
  • Lassitude (lethargy/fatigue)
  • Hypotension
  • Decompensation of heart failure (if titrated too rapidly)
  • Bronchospasm (reported in humans)
  • Mild hepatocellular injury (rare)

注意事項

​Black Box Warning Equivalent:​ Too rapid beta blockade can cause decompensation in patients with heart failure; cautious dosage titration is mandatory.

  • ​Hepatic Insufficiency:​ Because the drug is extensively metabolized in the liver, patients with hepatic insufficiency should receive the drug with caution.
  • ​Pregnancy/Nursing:​ FDA Category C. Increased post-implantation loss seen in animal studies. Unknown if it enters canine milk, but does enter rat milk. Use with caution in nursing patients.

藥物交互作用

Beta-Blockers (other)

Use with carvedilol may cause additive effects

Calcium Channel Blockers (e.g., diltiazem, verapamil)

May rarely cause hemodynamic compromise

Cimetidine

May decrease metabolism and increase AUC of carvedilol

Clonidine

Carvedilol may potentiate the cardiovascular effects of clonidine

Cyclosporine

Carvedilol may increase cyclosporine levels

DigoxinMajor

Can increase digoxin plasma concentrations by approximately 15%

Fluoxetine, Paroxetine, Quinidine

May increase R(+)carvedilol concentrations and increase alpha-1 blocking effects (vasodilation)

Insulin / Oral Antidiabetic Agents

Carvedilol may enhance the blood glucose lowering effects of insulin or other antidiabetic agents

RifampinModerate

Can decrease carvedilol plasma concentrations by as much as 70%

Reserpine

Can cause increased bradycardia and hypotension in patients taking carvedilol

Anaesthetic agentsMajor

Enhanced hypotensive effect and myocardial depression

PhenothiazinesModerate

Enhanced hypotensive effect

Antihypertensive drugsModerate

Enhanced hypotensive effect

DiureticsModerate

Enhanced hypotensive effect

DiazepamMinor

Enhanced hypotensive effect

Calcium-channel blockersMajor

Increased risk of bradycardia, severe hypotension, heart failure, and AV block

NSAIDsModerate

May antagonize the hypotensive effect of carvedilol

InsulinModerate

May enhance the hypoglycaemic effect of insulin and mask signs of hypoglycaemia

CiclosporinMajor

Carvedilol increases plasma concentration of ciclosporin

Adrenaline (Epinephrine)Major

Contraindicated; risk of severe hypertension and bradycardia

監測

  • Clinical efficacy (improvement in heart failure signs)
  • Adverse effects (lethargy, inappetence, hypotension, worsening heart failure)
  • Plasma drug levels (Target: 50-100 nanograms/mL)

藥物動力學

半衰期

狗100 minutes

吸收

In dogs, bioavailability after oral dosing averages about 23%, but is highly variable (ranging from 3-10% in some individuals). In humans, it is rapidly and extensively absorbed but has a high first-pass effect, resulting in ~30% bioavailability.

分佈

In dogs, volume of distribution averages about 1.4 L/kg. In humans, it is extensively bound to plasma proteins (98%).

代謝

Extensively metabolized in the liver. In dogs, hydroxylation of the carbazolyl ring and glucuronidation are the predominant processes (at least 15 metabolites identified). In humans, CYP2D6 and CYP2C9 are the primary P450 isoenzymes responsible.

排除

Metabolites are primarily excreted via the bile and feces.

過量

The acute oral LD50 in healthy rats and mice is greater than 8 grams/kg.

​Clinical Signs of Overdose:​

  • Severe hypotension
  • Cardiac insufficiency
  • Bradycardia
  • Cardiogenic shock
  • Death due to cardiac arrest

​Treatment:​

  • Gut emptying protocols should be considered if ingestion was recent.
  • ​Bradycardia:​ Treat with atropine.
  • ​Cardiovascular Support:​ Support function with glucagon and sympathomimetics (e.g., dobutamine, epinephrine).
  • Contact an animal poison control center for specific information.

可用產品

劑型

  • Oral tablets
  • Extended-release oral capsules
  • Compounded oral suspension

人用標示

  • Carvedilol Oral Tablets: 3.125 mg, 6.25 mg, 12.5 mg, & 25 mg (Coreg, generic)
  • Carvedilol Extended-Release Oral Capsules: 10 mg, 20 mg, 40 mg & 80 mg as phosphate (Coreg CR)

各地核准狀態

European Union✓ 已核准處方藥EMA

POM (Prescription Only Medicine)

United Kingdom✓ 已核准處方藥VMD

POM (Prescription Only Medicine)

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

儲存與穩定性

Tablets and extended-release capsules should be stored below 30°C (86°F), protected from moisture, and dispensed in tight, light-resistant containers. Compounded oral suspensions (2 mg/mL or 10 mg/mL in simple syrup) should be stored in amber bottles at temperatures not exceeding 25°C and protected from light for up to 90 days. Shake well before administering.

飼主須知

寵物主人重要指引

  • ​嚴格遵守劑量：​ 請​完全​依照獸醫師的處方給藥。​切勿突然停藥​，除非有獸醫師的同意與指導，因為這可能會對心臟造成危險的反彈效應。
  • ​注意病情惡化跡象：​ 如果您的寵物在服藥期間病情惡化（例如：咳嗽增加、呼吸困難），請立即聯繫您的獸醫師。
  • ​監測副作用：​ 如果您的寵物出現食慾減退、嚴重疲勞或無精打采、頭暈或步態不穩（這可能表示血壓過低）的跡象，請致電您的獸醫師。
  • ​給藥方式：​ 此藥物最好與食物一起餵食，以幫助吸收並降低血壓突然下降的風險。

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