索他洛爾
Sotalol
d,l-sotalol hydrochloride
別名: Betapace · Sotacor · MJ-1999 · d,l-sotalol hydrochloride · sotaloli hydrochloridum · Sotalolum
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
劑量為合格獸醫專業人員的臨床參考。請務必對照最新仿單及個別病患確認。
各物種劑量
🌎 NA — North America🌍 EU — Europe
狗
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| General antiarrhythmic | 1-2 mg/kg | PO | q12h | — | 🌎 NA |
| General antiarrhythmic | 1-3 mg/kg | PO | twice daily | — | 🌎 NA |
| For ventricular tachycardia | 1-2 mg/kg | PO | twice daily | — | 🌎 NA |
| For ventricular tachyarrhythmias in Boxers in combination with mexiletine | 1.5-3 mg/kg | PO | twice daily | — | 🌎 NA |
| In Boxers | 40-80 mg (total dose) | PO | q12h | — | 🌎 NA |
| Ventricular arrhythmias | 0.5-3 mg/kg | PO | q12h | Ongoing | 🌍 EU |
| Ventricular arrhythmias (Acute/Severe) | 0.5 mg/kg given over 2 min, up to 3 times (to a total dose of 1.5 mg/kg) | IV | As needed | Acute setting | 🌍 EU |
- For ventricular tachyarrhythmias in Boxers in combination with mexiletine: Given with mexiletine (5-7.5 mg/kg PO three times daily)
- Ventricular arrhythmias: Start with lower doses if myocardial function is reduced.
- Ventricular arrhythmias (Acute/Severe): Anecdotal dosing.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| General antiarrhythmic | 2 mg/kg | PO | twice daily | — | 🌎 NA |
| For ventricular tachyarrhythmias | 2 mg/kg | PO | q12h | — | 🌎 NA |
| General antiarrhythmic | 1-2 mg/kg | PO | q12h | — | 🌎 NA |
| General antiarrhythmic | 1/8th of an 80 mg tablet (approximately 2 mg/kg) | PO | twice daily | — | 🌎 NA |
| Ventricular arrhythmias | 10-20 mg/cat | PO | q12h | Ongoing | 🌍 EU |
劑量為合格獸醫專業人員的臨床參考。請務必對照最新仿單及個別病患確認。
概覽
索他洛爾 (Sotalol) 是一種獨特的抗心律不整藥物，兼具非選擇性 β-受體阻斷劑 (第二類) 與 鉀離子通道阻斷劑 (第三類) 的特性。
- 臨床用途：在獸醫學中，主要用於治療犬貓的心室性心搏過速 (Ventricular tachycardia)，偶爾用於心房上性心搏過速。
- 目標族群：特別常被用於治療拳師犬的心室性心律不整（通常與致心律不整性右心室心肌病 ARVC 相關），以及對利多卡因 (Lidocaine) 產生抗藥性的病例。
- 藥理特點：索他洛爾是一種消旋混合物。其 d- 和 l- 異構物均具有第三類抗心律不整活性，但只有 l- 異構物具有 β-阻斷活性。其 β-阻斷效力約為普萘洛爾 (Propranolol) 的 30%。
作用機轉
Sotalol exerts a dual mechanism of action:
- Class II (Beta-Blocking) Action: Competitively antagonizes non-selective $\beta_1$ and $\beta_2$ adrenergic receptors $\rightarrow$ decreases heart rate, slows AV nodal conduction, and exerts a negative inotropic effect on the myocardium.
- Class III (Antiarrhythmic) Action: Selectively inhibits the rapid delayed rectifier potassium current ($I_{Kr}$) $\rightarrow$ prolongs the action potential duration (APD) and the effective refractory period (ERP) in both atrial and ventricular myocardium without affecting depolarization or conduction velocity.
安全性與警告
禁忌症
- Asthma or reactive airway disease
- Sinus bradycardia
- 2nd or 3rd degree AV block (unless artificially paced)
- Long QT syndromes
- Cardiogenic shock
- Uncontrolled congestive heart failure (CHF)
- Atrioventricular (AV) block
- Decompensated congestive heart failure (CHF)
- Long QT interval on ECG
不良反應
- Negative inotropism (decreased heart contractility)
- Proarrhythmia (can induce new or worsen existing arrhythmias)
- Dyspnea / Bronchospasm
- Fatigue / Lethargy
- Dizziness / Syncope exacerbation
- Nausea / Vomiting
- Bradycardia
- Hypotension
- Bradyarrhythmias
- Depression
- Diarrhoea
- Decreased cardiac output
- Precipitation of congestive heart failure
- Prolonged QT interval
- Torsades de pointes (proarrhythmic effect)
注意事項
Use with caution in patients with congestive heart failure (due to negative inotropic effects), diabetes mellitus, or hyperthyroidism (may mask clinical signs of hypoglycemia or thyrotoxicosis). Use with caution in patients with renal dysfunction; dosage intervals may need to be extended as it is renally excreted. Safety in pregnancy is not fully established (FDA Category B). Sotalol enters maternal milk at up to 5x serum concentrations; consider milk replacer for nursing animals.
藥物交互作用
May prolong refractory periods; concurrent use not recommended.
Additive myocardial depression may occur.
May reduce oral sotalol absorption; separate doses by at least 2 hours.
May prolong refractory periods and QT interval; concurrent use not recommended.
May prolong QT interval.
Potential to increase hypotensive effects; additive effects on AV conduction or ventricular function. Use with caution.
May prolong QT interval.
Increased risk for rebound hypertension if clonidine is discontinued after concomitant therapy.
Potential for increased risks for proarrhythmic events.
May prolong QT interval.
Clearance of lidocaine may be impaired by sotalol.
May prolong QT interval.
May have additive hypotensive and bradycardic effects.
Actions may be blocked by sotalol.
May prolong QT interval.
Mutual antagonism; sotalol may block their actions, and they may reduce sotalol's efficacy.
Additive myocardial depression.
Additive myocardial depression.
Enhanced hypotensive effects; risk of hypokalaemia which increases risk of torsades de pointes.
Enhanced hypotensive effects.
May prolong hypoglycaemic effects of insulin therapy.
Additive negative inotropic effects; use with extreme caution in patients with systolic dysfunction or CHF.
監測
- Efficacy via Electrocardiogram (ECG)
- Adverse effects (heart rate, blood pressure, respiratory effort)
- Renal function (baseline and periodic, as drug is renally excreted)
- Blood glucose (especially in diabetic patients)
- Heart rate and rhythm (Holter ECG monitoring is highly recommended to assess efficacy and detect proarrhythmias)
- Renal function (BUN, Creatinine, SDMA)
- Serum electrolytes (especially potassium, to avoid hypokalaemia)
- Clinical signs of congestive heart failure
藥物動力學
半衰期
吸收
Bioavailability is 90-100% if given on an empty stomach. Food may reduce bioavailability by approximately 20%. Unlike propranolol, sotalol does not have any appreciable first-pass effect.
分佈
Relatively low lipid solubility and virtually no protein binding. Enters maternal milk in concentrations up to 5 times that found in serum.
代謝
Minimal to no hepatic metabolism.
排除
Elimination is almost entirely via the kidneys, and most of the drug is excreted unchanged.
過量
Overdoses may result in bradycardia, hypotension, congestive heart failure, bronchospasm, and hypoglycemia.
- Treatment: Use gut evacuation (emesis or gastric lavage) if not contraindicated and when there is a significant risk of morbidity.
- Supportive Care: Treat adverse effects symptomatically and supportively (e.g., atropine for bradycardia, fluids/vasopressors for hypotension, bronchodilators for bronchospasm).
可用產品
劑型
- Tablets
- Injection solution concentrate
- 40 mg oral tablet
- 80 mg oral tablet
- 160 mg oral tablet
- 200 mg oral tablet
- 10 mg/ml injectable solution
- 10 mg oral tablet (special reformulation)
- 30 mg oral tablet (special reformulation)
人用標示
- Sotalol HCl Tablets: 80 mg, 120 mg, 160 mg & 240 mg; Betapace® (Bayer); generic
- Sotalol Injection Solution Concentrate: 15 mg/mL in 10 mL vials; generic
- Sotacor tablets
- Sotalol generic tablets (40 mg, 80 mg, 160 mg, 200 mg)
- Sotalol generic injection (10 mg/ml)
各地核准狀態
Human registered products used under the cascade.
POM (Prescription Only Medicine). Human registered products used under the cascade.
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Store tablets at room temperature.
飼主須知
重要提示：未經獸醫師同意，請勿突然停藥或更改劑量。突然停藥可能會導致危險的心律不整反彈或血壓升高。
- 給藥方式：為了獲得最佳吸收效果，如果您的寵物能適應，建議空腹給藥。如果引起腸胃不適，可以與少量食物一起餵食。
- 觀察與監測：密切觀察您的寵物是否出現極度疲倦、虛弱、昏厥或呼吸困難的跡象。
- 溝通：如果發現寵物有嘔吐、嗜睡或呼吸問題，請立即聯繫您的獸醫師。請務必按時回診進行心電圖 (ECG) 監測，以確保藥物安全有效。
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