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特布他林

Terbutaline

Terbutaline sulfate

β-腎上腺素受體激動劑POSCIMIVIntradermal

別名: Brethine · Bricanyl · Monovent · KWD-2019 · terbutaline sulphate · terbutalini sulfas · Terbutaline sulfate · Terbutalinum

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

Bradyarrhythmias (extra-label)

0.2 mg/kgPO
  • q8-12h

NA

必須同時考慮的臨床上下文 (2)
  • 1. Do not confuse mg/kg dosages with mg/dog or mg/cat.
  • 2. Terbutaline should not be administered as an IV bolus; administer slowly if IV use cannot be avoided.
formulary方案年份 2023審核 dose-audit-plumb-v13

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概覽

特布他林是一種合成的選擇性 ​β2-腎上腺素受體激動劑​,在獸醫學中主要作為支氣管擴張劑使用。它常用於輔助治療心肺疾病,如 ​貓氣喘、犬慢性支氣管炎、氣管塌陷和肺水腫​

除了呼吸道應用外,特布他林偶爾也會被標籤外使用作為 ​安胎藥​(透過放鬆子宮平滑肌來抑制早產),以及用於治療某些 ​心跳過緩​。在馬医學中,它可透過皮內注射作為診斷工具,用於定量測試無汗症。

​臨床提示:​ 雖然在標準劑量下對 β2 受體具有高度選擇性,但較高劑量可能會影響 β1 受體,導致直接的心臟刺激。周邊行管擴張引發的反射性心跳過速也是常見的臨床觀察。

作用機制

Terbutaline selectively binds to and stimulates beta-2 adrenergic receptors located predominantly in bronchial, vascular, and uterine smooth muscle.

​Mechanism Pathway:​ Beta-2 receptor activation → Stimulation of adenylyl cyclase → Increased intracellular ​cyclic AMP (cAMP)​ → Activation of ​protein kinase A (PKA)​ → Decreased intracellular calcium concentrations → Smooth muscle relaxation.

This results in significant bronchodilation and reduced airway resistance. At therapeutic doses, it has minimal affinity for beta-1 receptors (cardiac muscle) and virtually no alpha-adrenergic activity.

安全性與警告

禁忌症

  • Heart disease (especially congestive heart failure or cardiomyopathy)
  • Known hypersensitivity to terbutaline or sympathomimetic amines
  • Severe cardiac arrhythmias
  • Hypertrophic cardiomyopathy (relative contraindication)

不良反應

  • Increased heart rate (tachycardia)
  • CNS excitement (nervousness)
  • Dizziness
  • Sweating (reported in horses after parenteral injection)
  • Transient hypokalemia
  • Muscle tremors
  • Restlessness or excitement
  • Hypokalemia (with high doses or prolonged use)
  • Hypertension or hypotension

注意事項

Use with extreme caution in patients with diabetes mellitus, hyperthyroidism, hypertension, seizure disorders, or cardiac disease (especially with concurrent arrhythmias).

​Note:​ Terbutaline can cause transient hypokalemia. If an animal is susceptible to developing hypokalemia, additional serum potassium monitoring should be performed early in therapy.

藥物相互作用

Inhalation Anesthetics (e.g., halothane, isoflurane, methoxyflurane)

May predispose the patient to ventricular arrhythmias, particularly with preexisting cardiac disease; use cautiously.

Beta-Adrenergic Blocking Agents (e.g., propranolol)

May antagonize the bronchodilating and cardiovascular actions of terbutaline.

DigoxinModerate

Concurrent use with digitalis glycosides may increase the risk of cardiac arrhythmias.

Monoamine Oxidase Inhibitors (MAOIs)

May potentiate the vascular effects of terbutaline.

Other Sympathomimetics

May increase the risk of developing adverse cardiovascular effects.

Tricyclic Antidepressants

May potentiate the vascular effects of terbutaline.

Beta-blockers (e.g., propranolol)Major

Antagonize the bronchodilating effects of terbutaline

SympathomimeticsModerate

Additive cardiovascular toxicity and CNS stimulation

Inhalant anesthetics (e.g., halothane)Major

Sensitize the myocardium, increasing the risk of severe arrhythmias

Tricyclic antidepressants (TCAs) / MAOIsModerate

May potentiate vascular effects

監測

  • Clinical symptom improvement (respiratory rate/effort)
  • Auscultation of lung sounds
  • Cardiac rate and rhythm (especially if indicated for arrhythmias or if tachycardia develops)
  • Serum potassium (early in therapy if the animal is susceptible to hypokalemia)
  • Heart rate and rhythm
  • Respiratory rate and effort
  • Serum potassium levels (with prolonged or high-dose therapy)

藥物動力學

半衰期

Unknown, presumed similar to dogsApproximately 2-4 hoursMean residence time (MRT) is about 30 minutes when given IV.

吸收

In humans, 33-50% of an oral dose is absorbed. Well-absorbed following SC administration (onset within 15 mins, peak 30-60 mins). In horses, oral bioavailability is very poor (<1%).

分佈

Distributed into milk at levels approximately 1% of the oral dose given to the mother.

代謝

Metabolized in the liver to an inactive sulfate conjugate.

排除

Principally excreted unchanged in the urine (60%).

過量

Clinical signs of significant systemic overdose may include arrhythmias (bradycardia, tachycardia, heart block, extrasystoles), hypertension, fever, vomiting, mydriasis, and CNS stimulation.

​Treatment:​

  • For recent oral ingestion without significant cardiac/CNS effects: Empty gut, administer activated charcoal, and a cathartic.
  • For severe cardiac arrhythmias: A beta-blocking agent (e.g., propranolol) can be used, but caution is advised as it may precipitate severe bronchoconstriction.

可用產品

劑型

  • Injection
  • Injectable: 0.5 mg/ml solution
  • Oral: 5 mg tablets
  • Oral: 1.5 mg/5 ml syrup

人用標示

  • Terbutaline Sulfate Tablets: 2.5 mg & 5 mg (Brethine®, generic)
  • Terbutaline Injection: 1 mg/mL in 1 mL vials & 2 mL amps with 1 mL fill (Brethine®, generic)
  • Bricanyl 0.5 mg/ml injection
  • Bricanyl 5 mg tablets
  • Bricanyl 1.5 mg/5 ml syrup
  • Monovent

各地核准狀態

European Union✓ 已核准處方藥EMA

Approved for human use; used off-label in veterinary medicine under the cascade.

United Kingdom✓ 已核准處方藥 · POMVMD

Prescription Only Medicine (POM). Human products (Bricanyl, Monovent) used under the prescribing cascade.

暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU

儲存與穩定性

Tablets should be stored in tight containers at room temperature (15-30°C). Injection should be stored at room temperature (15-30°C) and protected from light. Injection is stable over a pH range of 1-7; discolored solutions should not be used.

飼主須知

  • ​用途:​ 特布他林用於打開肺部的呼吸道,使您的寵物更容易呼吸。
  • ​給藥方式:​ 請嚴格按照獸醫師的指示給藥。除非有指示,否則請勿突然停藥。
  • ​副作用:​ 您可能會注意到寵物的心跳比平時快、輕微顫抖或神經質/焦躁。這些影響通常是輕微且暫時的。
  • ​何時聯絡獸醫:​ 如果您的寵物呼吸惡化、暈倒或突然生病,請立即聯絡您的獸醫師。

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