プロプラノロール
Propranolol
Propranolol Hydrochloride
別名: Inderal LA · InnoPran XL · Syprol · AY-64043 · ICI-45520 · NSC-91523 · propranololi hydrochloridum · Propranolol hydrochloride
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
監査済み v13 用量エビデンス
構造化された用量計算エビデンスHypertrophic cardiomyopathy (extra-label)
認証済み獣医師の確認が必要
- q12-24h
NA
必ず考慮する臨床コンテキスト (6)
- NOTE: Because of a high first-pass effect after oral dosing, IV dosages are ≈10% of oral dosages. Do not confuse the dosages.
- ■ This medicine can be given with or without food.
- ■ When starting this medicine, your veterinarian may start with a low dose and gradually increase it over time to see how your animal reacts to it. Do not administer more than your veterinarian prescribes.
- ■ Do not suddenly stop giving propranolol to your animal as it can make your animal’s condition worse.
- ■ Your veterinarian will need to monitor your animal closely while it is receiving this medicine. Do not miss these important follow-up visits.
- All propranolol preparations should be stored at room temperature (15°C-30°C [59°F-86°F]) and protected from light. Propranolol solutions will decompose rapidly at alkaline pH.
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。
概要
プロプラノロールは非選択的βアドレナリン受容体拮抗薬（β遮断薬）であり、獣医学では主に抗不整脈薬として使用されます。クラスII抗不整脈薬に分類されます。
- 主な用途： 上室性および心室性頻脈性不整脈（APC、VPC、心房細動など）、肥大型心筋症（HCM）、および全身性高血圧の管理。
- 内分泌疾患での用途： 猫の甲状腺機能亢進症や褐色細胞腫における交感神経過剰刺激による心血管系および神経筋肉系の症状を制御するために頻繁に使用されます。
- 行動学的な用途： 犬の状況不安や大きな音に対する恐怖症に対して適応外使用されることがあります。
臨床上のポイント： プロプラノロールは非選択的であるため、心臓と肺の両方の受容体を遮断します。猫喘息やその他の気管支痙攣性気道疾患を持つ患者には、極めて慎重に使用するか、使用を避けるべきです。
作用機序
Propranolol acts via competitive blockade of both $\beta_1$ and $\beta_2$ adrenergic receptors.
- $\beta_1$ Blockade (Cardiac): $\rightarrow$ Decreases sinus heart rate (negative chronotropy) $\rightarrow$ Depresses AV node conduction (negative dromotropy) $\rightarrow$ Decreases myocardial contractility (negative inotropy) $\rightarrow$ Ultimately reduces cardiac output and myocardial oxygen demand.
- $\beta_2$ Blockade (Pulmonary/Vascular): $\rightarrow$ Can cause bronchoconstriction and peripheral vasoconstriction.
- Additional Effects: Possesses membrane-stabilizing (quinidine-like) effects at higher doses, which alters the cardiac action potential. It lacks intrinsic sympathomimetic activity (ISA) and inhibits glycogenolysis.
安全性・警告
禁忌
- Overt heart failure
- Hypersensitivity to beta-blockers
- Greater than 1st degree heart block
- Sinus bradycardia
- Congestive heart failure (unless secondary to a tachyarrhythmia responsive to beta-blockers)
- Bronchospastic lung disease (e.g., feline asthma)
- Bradyarrhythmias
- Acute or decompensated congestive heart failure
- Concurrent administration with alpha-adrenergic agonists (e.g., adrenaline)
有害事象
- Bradycardia
- Lethargy and depression
- Impaired AV conduction
- Congestive heart failure (CHF) or worsening of heart failure
- Hypotension
- Syncope
- Diarrhea
- Hypoglycemia
- Bronchoconstriction
- AV block
- Myocardial depression
- Hypoglycaemia
- Bronchospasm
- Diarrhoea
- Peripheral vasoconstriction
注意事項
Use with Caution:
- Patients with significant renal or hepatic insufficiency.
- Patients with sinus node dysfunction.
- Labile diabetic patients (can cause or mask clinical signs of hypoglycemia).
- Digitalized or digitalis-intoxicated patients (severe bradycardia may result).
- May mask clinical signs of thyrotoxicosis.
- Withdrawal: If discontinuing the drug after chronic use, gradual withdrawal is recommended to prevent exacerbation of clinical signs.
医薬品相互作用
May reduce oral propranolol absorption; separate doses by at least one hour
Additive myocardial depression may occur
May negate cardiac effects of beta-blockers
Concurrent use should be done with caution due to additive negative inotropic effects, particularly in patients with cardiomyopathy or CHF
May decrease the metabolism of propranolol and increase blood levels
May increase risk for hypotension
Unopposed alpha effects of epinephrine may lead to rapid increases in blood pressure and decrease in heart rate
May decrease propranolol metabolism; complete heart block reported in one human
Propranolol may prolong the hypoglycemic effects of insulin therapy
Clearance may be impaired by propranolol
Propranolol doses may need to be decreased when initiating therapy
May increase the metabolism of propranolol
May increase risk for hypotension
May have additive effects with propranolol
Effects may be enhanced with propranolol therapy
May have their actions blocked by propranolol
Effects of theophylline (bronchodilation) may be blocked by propranolol
May decrease the effects of beta blocking agents
Enhanced hypotensive effect
Enhanced hypotensive effect
Enhanced hypotensive effect
Increased risk of bradycardia, severe hypotension, heart failure, and AV block
Potentiates bradycardia
May necessitate a decrease in propranolol dose when initiating therapy
Reduces propranolol absorption
Enhances the effects of the muscle relaxants
Hepatic enzyme induction increases the rate of metabolism of propranolol
Propranolol may enhance the hypoglycaemic effect of insulin
Concurrent use is contraindicated; risk of severe hypertension and bradycardia
監視
- ECG (Electrocardiogram)
- Signs of toxicity (bradycardia, hypotension, lethargy)
- Blood pressure (especially if administering IV)
- Heart rate and rhythm (ECG)
- Signs of congestive heart failure (e.g., respiratory rate/effort)
- Blood glucose (especially in diabetic patients receiving insulin)
薬物動態
半減期
吸収
Well absorbed after oral administration, but undergoes a rapid first-pass effect through the liver, reducing systemic bioavailability to approximately 2-27% in dogs. Hyperthyroid cats may have increased bioavailability compared to normal cats.
分布
Highly lipid soluble and readily crosses the blood-brain barrier. Apparent volume of distribution is 3.3-11 L/kg in dogs. Crosses the placenta and enters milk at very low levels. Approximately 90% bound to plasma proteins in humans.
代謝
Principally metabolized by the liver. An active metabolite, 4-hydroxypropranolol, has been identified after oral administration.
消失
Less than 1% of a dose is excreted unchanged into the urine.
過剰投与
Clinical Signs: The most predominant expected signs are hypotension and bradycardia. Other possible effects include CNS depression (ranging from depressed consciousness to seizures), bronchospasm, hypoglycemia, hyperkalemia, respiratory depression, pulmonary edema, AV block, or asystole.
Treatment:
- Decontamination: If recent oral ingestion, consider emptying the gut and administering activated charcoal.
- Monitoring: Monitor ECG, blood glucose, potassium, and blood pressure.
- Cardiovascular Support: Use IV fluids and pressor agents for hypotension. Treat bradycardia with atropine; if atropine fails, cautiously administer isoproterenol. A transvenous pacemaker may be necessary.
- Heart Failure: Treat with digoxin, diuretics, oxygen, and IV aminophylline if necessary.
- Antidotal Therapy: Glucagon (5-10 mg IV; human dose) may increase heart rate and blood pressure, reducing the cardiodepressant effects of propranolol.
- Seizures: Generally respond to IV diazepam.
製品
製剤
- Oral Tablets
- Extended/Sustained-Release Capsules
- Injection
- 1 mg/ml injectable solution
- 10 mg tablet
- 40 mg tablet
- 80 mg tablet
- 160 mg tablet
- 5 mg/5 ml oral solution
- 10 mg/5 ml oral solution
- 40 mg/5 ml oral solution
- 50 mg/5 ml oral solution
ヒト用医薬品
- Propranolol HCl Oral Tablets: 10 mg, 20 mg, 40 mg, 60 mg & 80 mg
- Propranolol HCl Extended/Sustained-Release Capsules: 60 mg, 80 mg, 120 mg & 160 mg (Inderal LA, InnoPran XL)
- Propranolol for Injection: 1 mg/mL in 1 mL amps or vials (Inderal)
- Propranolol Oral Solution: 4 mg/mL & 8 mg/mL in 500 mL
- Syprol oral solution
- Propranolol tablets (10 mg, 40 mg, 80 mg, 160 mg)
- Propranolol injection (1 mg/ml)
規制ステータス
Available as POM (Prescription Only Medicine)
Available as POM-V or POM (human generics like Syprol used under the cascade)
規制データなし: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
保管・安定性
Store all propranolol preparations at room temperature (15-30°C) and protect from light. Propranolol solutions will decompose rapidly at alkaline pH.
飼主向け情報
- 継続が重要です： 効果を得るためには、獣医師の処方通りにすべての用量を投与する必要があります。心臓に危険なリバウンド効果を引き起こす可能性があるため、獣医師に相談せずに急に投薬を中止しないでください。
- 注意すべき症状： ペットが異常に無気力になったり、運動を嫌がったり、喘鳴（ゼーゼーという呼吸）を始めたり、息切れや咳が出たり、行動や態度に急な変化が見られた場合は、すぐに獣医師に連絡してください。
- 飲み忘れた場合： 飲み忘れた場合は、気づいた時点ですぐに与えてください。ただし、絶対に1回に2回分を与えないでください。
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