VetSheet

カルベジロール

Carvedilol

carvedilolum

βおよびα1アドレナリン受容体遮断薬PO犬

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

VetSheet 獣医チームが監修更新日 2026年4月5日エビデンスに基づく獣医学リファレンス

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

用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。

動物種別用量

🌎 NA — North America🌍 EU — Europe

犬

適応用量経路頻度期間地域
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.

用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。

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概要

カルベジロールは、​α1アドレナリン受容体遮断​作用を併せ持つユニークな第3世代の​非選択的β遮断薬​です。獣医療においては、主に​犬の拡張型心筋症（DCM）​および慢性心不全の補助療法として研究されています。

  • ​二重作用：​ 従来のβ遮断薬（アテノロールなど）とは異なり、カルベジロールは追加の血管拡張作用をもたらし、心臓の後負荷を軽減します。
  • ​使用に関する議論：​ 獣医循環器学における使用は依然として議論の余地があります。ヒトの心不全では死亡率低下の利点が証明されていますが、犬の研究では、標準用量での神経体液性活性化や心室リモデリングの改善に関する有効性はまちまちです。
  • ​臨床上のポイント：​ カルベジロールは強力な陰性変力作用を持ちます。進行した、あるいは症状の重い心不全患者において急性代償不全を引き起こす可能性があります。極めて慎重かつゆっくりとした用量漸増が必要であり、症状が軽微な患者から開始するのが最適です。

作用機序

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・警告

禁忌

  • 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

有害事象

  • 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.

医薬品相互作用

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

監視

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

薬物動態

半減期

犬100 minutes

吸収

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.

分布

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.

消失

Metabolites are primarily excreted via the bile and feces.

過剰投与

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.

製品

製剤

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

ヒト用医薬品

  • 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)

規制ステータス

European Union✓ 承認済み処方箋医薬品EMA

POM (Prescription Only Medicine)

United Kingdom✓ 承認済み処方箋医薬品VMD

POM (Prescription Only Medicine)

規制データなし: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU

保管・安定性

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.

飼主向け情報

飼い主様への重要な情報

  • ​厳密な投薬：​ 獣医師の処方​通り​に正確にこの薬を与えてください。獣医師の承認と指導なしに​絶対に投薬を急に中止しないでください​。心臓に危険なリバウンド効果を引き起こす可能性があります。
  • ​症状の悪化に注意：​ この薬を服用中にペットの症状が悪化した場合（例：咳の増加、呼吸困難など）は、直ちに獣医師に連絡してください。
  • ​副作用の観察：​ ペットに食欲低下、極度の疲労や無気力、めまい、ふらつき（血圧低下を示す可能性があります）の兆候が見られた場合は、獣医師に連絡してください。
  • ​投与方法：​ 吸収を助け、急激な血圧低下のリスクを減らすため、この薬は食事と一緒に与えるのが最適です。

VetSheet医薬品リファレンスは獣医専門家の臨床意思決定支援を目的としており、専門的判断または製造業者の最新医薬品情報の代替にはなりません。