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카르베딜롤

Carvedilol

carvedilolum

베타 및 알파-1 아드레날린 수용체 차단제PO개

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

VetSheet 수의사 팀 검수업데이트 2026년 4월 5일근거 기반 수의학 참고자료

0.2 mg/kg PO twice daily initially with slow titration upwards towards a dose of 0.8 mg/kg twice dailyPO· twice daily
— 🐕

용량은 수의사 전문가를 위한 임상 참고자료입니다. 반드시 최신 약물 정보 및 개별 환자에 따라 확인하시기 바랍니다.

동물 종별 용량

🌎 NA — North America🌍 EU — Europe

개

적응증용량경로빈도기간지역
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.

용량은 수의사 전문가를 위한 임상 참고자료입니다. 반드시 최신 약물 정보 및 개별 환자에 따라 확인하시기 바랍니다.

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개요

카르베딜롤은 ​알파-1 아드레날린 차단​ 특성을 가진 독특한 3세대 ​비선택적 베타 차단제​입니다. 수의학에서는 주로 ​개 확장성 심근병증(DCM)​ 및 만성 심부전의 보조 치료제로 연구되고 있습니다.

  • ​이중 작용:​ 기존의 베타 차단제(예: 아테놀롤)와 달리 카르베딜롤은 추가적인 혈관 확장 효과를 제공하여 심장의 후부하를 감소시킵니다.
  • ​논란이 되는 사용:​ 수의 심장학에서의 사용은 여전히 논란의 여지가 있습니다. 인체 심부전에서는 사망률 감소 효과가 입증되었으나, 개를 대상으로 한 연구에서는 표준 용량 투여 시 신경호르몬 활성화나 심실 재형성 개선에 대한 효능 결과가 엇갈립니다.
  • ​임상적 핵심:​ 카르베딜롤은 강력한 음성 변력 작용을 합니다. 진행성 또는 증상이 심한 심부전 환자에서 급성 비대상성을 유발할 수 있습니다. 매우 주의 깊고 천천히 용량을 증량해야 하며, 증상이 경미한 환자에서 시작하는 것이 가장 좋습니다.

작용 기전

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.

안전성·주의사항

금기사항

  • 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

부작용

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

주의

​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.

약물 상호작용

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

모니터링

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

약동학

반감기

개100 minutes

흡수

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.

분포

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

대사

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.

배설

Metabolites are primarily excreted via the bile and feces.

과다투여

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.

제품

제형

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

인용의약품

  • 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)

규제 현황

European Union✓ 승인됨처방전의약품EMA

POM (Prescription Only Medicine)

United Kingdom✓ 승인됨처방전의약품VMD

POM (Prescription Only Medicine)

규제 데이터 없음: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU

보관·안정성

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.

보호자 정보

반려동물 보호자를 위한 중요 안내

  • ​엄격한 용량 준수:​ 수의사가 처방한 ​정확한​ 용량대로 이 약을 투여하십시오. 수의사의 승인과 지도 없이 ​갑자기 약물 투여를 중단하지 마십시오​. 심장에 위험한 반동 현상을 일으킬 수 있습니다.
  • ​증상 악화 관찰:​ 이 약을 복용하는 동안 반려동물의 상태가 악화되면(예: 기침 증가, 호흡 곤란) 즉시 수의사에게 연락하십시오.
  • ​부작용 모니터링:​ 반려동물에게 식욕 감소, 심한 피로감이나 무기력증, 어지러움 또는 비틀거림(저혈압을 의미할 수 있음)의 징후가 나타나면 수의사에게 연락하십시오.
  • ​투여 방법:​ 흡수를 돕고 갑작스러운 혈압 강하의 위험을 줄이기 위해 이 약은 음식과 함께 먹이는 것이 가장 좋습니다.

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