카르베딜롤

베타 및 알파-1 아드레날린 수용체 차단제

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.

동물 종별 용량

Dogs

Heart failure (adjunctive therapy) · ¼-½ of a 3.125 mg tablet PO twice daily · PO · twice daily · 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 · 0.2 mg/kg PO twice daily initially with slow titration upwards towards a dose of 0.8 mg/kg twice daily · PO · twice daily · 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) · 0.5 mg/kg PO twice daily · PO · twice daily · 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 · 0.3 mg/kg PO q12h · PO · q12h · 3 months · 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) · Start at 0.05-0.1 mg/kg, gradually increase at 2-week intervals to target dose of 0.3-0.4 mg/kg · PO · q12h · Long-term · Increase dose only if tolerated.
ACVIM stage B2 degenerative mitral valve disease · 0.3 mg/kg, increased at intervals up to 1.1 mg/kg · PO · q12h · Long-term · For cardiac remodelling with no signs of cardiac failure.

용량은 면허 수의 전문가를 위한 임상 참고 자료입니다. 항상 최신 라벨과 개별 환자에 대해 확인하십시오.

투여 경로

금기

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

이상반응

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

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
Digoxin · Can increase digoxin plasma concentrations by approximately 15% · major
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
Rifampin · Can decrease carvedilol plasma concentrations by as much as 70% · moderate
Reserpine · Can cause increased bradycardia and hypotension in patients taking carvedilol
Anaesthetic agents · Enhanced hypotensive effect and myocardial depression · major
Phenothiazines · Enhanced hypotensive effect · moderate

모니터링

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

과용량

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.

VetSheet 약물 레퍼런스는 면허 수의 전문가를 위한 임상 의사결정 보조 도구이며, 전문적 판단이나 제조사의 최신 라벨을 대신하지 않습니다.