普萘洛爾
Propranolol
Propranolol Hydrochloride
別名: Inderal LA · InnoPran XL · Syprol · AY-64043 · ICI-45520 · NSC-91523 · propranololi hydrochloridum · Propranolol hydrochloride
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
經審核的 v13 劑量證據
結構化劑量計算證據Hypertrophic cardiomyopathy (extra-label)
須由已驗證獸醫確認
- q12-24h
NA
必須同時考慮的臨床上下文 (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.
劑量為持牌獸醫專業人員的臨床參考。請務必對照最新藥品說明書及個別病患確認。
概覽
普萘洛爾是一種非選擇性β-腎上腺素受體阻斷劑(β-blocker),在獸醫學中主要用作抗心律不整藥物。它被歸類為第二類抗心律不整藥物。
- 主要用途: 治療心房和心室心搏過速(例如 APCs、VPCs、心房顫動)、肥厚型心肌病 (HCM) 以及全身性高血壓。
- 內分泌用途: 常用於控制貓甲狀腺機能亢進和嗜鉻細胞瘤中交感神經過度刺激所引起的心血管和神經肌肉症狀。
- 行為用途: 偶爾用於標示外用途,以治療狗的情境焦慮或對巨大聲響的恐懼症。
臨床要點: 由於普萘洛爾是非選擇性的,它會同時阻斷心臟和肺部的受體。對於患有貓氣喘或其他支氣管痙攣性呼吸道疾病的病患,應極度謹慎使用或避免使用。
作用機制
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.
安全性與警告
禁忌症
- 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)
不良反應
- 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.
藥物相互作用
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
監測
- 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)
藥物動力學
半衰期
吸收
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.
分佈
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.
排除
Less than 1% of a dose is excreted unchanged into the urine.
過量
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.
可用產品
劑型
- 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
人用標示
- 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)
各地核准狀態
Available as POM (Prescription Only Medicine)
Available as POM-V or POM (human generics like Syprol used under the cascade)
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Store all propranolol preparations at room temperature (15-30°C) and protect from light. Propranolol solutions will decompose rapidly at alkaline pH.
飼主須知
- 按時服藥是關鍵: 為了達到療效,您的寵物必須完全按照獸醫的處方服用所有劑量。未經獸醫同意,請勿突然停藥,因為這可能會對心臟造成危險的反彈效應。
- 注意事項: 如果您的寵物變得異常嗜睡、運動耐力下降、開始喘息、呼吸急促或咳嗽,或者行為或態度突然改變,請立即聯繫您的獸醫。
- 忘記服藥: 如果您忘記給藥,請在想起來時盡快補給,但絕對不要一次給予雙倍劑量。
VetSheet 藥物參考供持牌獸醫專業人員作臨床決策輔助之用,不能取代專業判斷或廠方最新藥品說明書。
