布托啡諾
Butorphanol
Butorphanol tartrate
別名: Stadol · Torbutrol · Torbugesic · Dolorex · Equanol · Alvegesic · Butomidor · Torphasol · levo-BC-2627 · butorphanol tartrate
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
經審核的非計算證據經審核的非計算證據 (5)
僅供證據參考，不會自動計算
Chelonians/minimal sedation
TABLE 127.5. Agent: Butorphanol. Dosage: 0.2 mg/kg IM118,275. Species/Comments: Chelonians/minimal sedation.
僅供證據參考，不會自動計算
Most species/sedation; preanesthetic
TABLE 127.5. Agent: Butorphanol. Dosage: 0.4–1 mg/kg SC, IM295. Species/Comments: Most species/sedation; preanesthetic.
僅供證據參考，不會自動計算
Most species/preanesthetic
TABLE 127.5. Agent: Butorphanol. Dosage: 0.5–2 mg/kg IM, or 0.2–0.5 mg/kg IV, IO23. Species/Comments: Most species/preanesthetic.
僅供證據參考，不會自動計算
Butorphanol combinations follow; see ketamine for combinations; inadequate for analgesia
TABLE 127.5. Agent: Butorphanol. Dosage: —. Species/Comments: Butorphanol combinations follow; see ketamine for combinations; inadequate for analgesia.
僅供證據參考，不會自動計算
Lizards/administer 30 min before isoflurane for smoother, shorter induction
TABLE 127.5. Agent: Butorphanol. Dosage: 1–1.5 mg/kg SC, IM295. Species/Comments: Lizards/administer 30 min before isoflurane for smoother, shorter induction.
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
布托啡諾 (Butorphanol) 是一種合成的鴉片類部分促效劑，廣泛應用於多種動物的獸醫學中。
- 鎮痛作用：提供輕至中度的內臟鎮痛。由於其「天花板效應 (ceiling effect)」，增加劑量並不會增強鎮痛效果，因此不適用於嚴重疼痛（如大型骨科手術）。
- 鎮咳作用：對抑制犬隻的慢性非生產性咳嗽（如傳染性氣管支氣管炎、氣管塌陷）非常有效。
- 逆轉劑：能獨特地逆轉純粹的 mu-促效劑（如芬太尼、美沙酮或嗎啡）所引起的嚴重呼吸和中樞神經抑制，同時仍保留一定程度由 kappa 受體介導的鎮痛效果。
- 鎮靜作用：常與 alpha-2 促效劑（如右美托咪啶或甲苯噻嗪）及苯二氮平類藥物合併使用，以達到協同鎮靜和化學保定的效果。
臨床要點：雖然布托啡諾在小動物中是極佳的鎮咳劑和輕度鎮靜劑，但其作用時間極短（犬隻的鎮痛作用通常小於 1 小時），限制了它作為主要鎮痛劑的實用性。相反地，它在馬匹（例如治療疝痛）中是一種非常有效且常用的內臟鎮痛劑。
作用機轉
Butorphanol exerts its effects by interacting with specific opioid receptors in the central nervous system:
- Kappa (κ) and Sigma (σ) Agonist: Activation of κ-receptors in the limbic system and spinal cord provides visceral analgesia and sedation.
- Mu (μ) Antagonist: Competitively binds to and blocks μ-receptors. This antagonism is responsible for its ability to reverse pure μ-agonist drugs and is the reason for its analgesic "ceiling effect."
- Antitussive Mechanism: Directly suppresses the medullary cough center, elevating the threshold to stimuli (like CO2) without depressing respiratory center sensitivity as profoundly as pure agonists.
- Cellular Pathway: Binds to κ-receptors → inhibits adenylate cyclase → decreases intracellular cAMP → closes voltage-gated calcium channels and opens potassium channels → hyperpolarization and reduced neuronal excitability.
安全性與警告
禁忌症
- Known hypersensitivity to butorphanol
- Lower respiratory tract conditions with copious mucous production (suppressing cough prevents clearance)
- Caution in patients with head trauma, increased CSF pressure, or severe CNS dysfunction (e.g., coma)
- Caution in severe liver disease, renal insufficiency, hypothyroidism, or Addison's disease
- Caution in dogs with heartworm disease (safety not established)
不良反應
- Sedation and ataxia
- Anorexia or diarrhea (rare in small animals)
- Respiratory depression (mild compared to pure agonists)
- CNS excitement, head tossing, and increased ambulation (especially in horses at high doses or rapid IV administration)
- Decreased gastrointestinal motility and potential ileus (horses)
- Nystagmus, salivation, seizures, and hyperthermia (at massive overdoses in horses)
注意事項
MDR1 (ABCB1) Mutation Warning: Dogs with the MDR1 mutation (e.g., Collies, Australian Shepherds) may develop pronounced and prolonged sedation. Reduce the dose by 25% in heterozygous dogs and by 30-50% in homozygous mutant dogs.
Geriatric/Debilitated Patients: Use with caution and consider dose reductions.
Hepatic/Renal Impairment: The manufacturer advises against use in dogs with a history of liver disease. Use cautiously in renal insufficiency.
Pregnancy/Nursing: Category C (human). Safe for use if used cautiously in dogs/cats, but manufacturer does not recommend use in pregnant bitches, foals, weanlings, or breeding horses.
藥物交互作用
May cause increased CNS or respiratory depression; dosage may need to be decreased.
Could potentially decrease the metabolism of butorphanol, prolonging its effects.
Butorphanol may antagonize analgesic effects, but will also reverse sedative and respiratory depressant effects.
May cause increased conjunctival changes when used concurrently.
Could potentially decrease the metabolism of butorphanol.
Reduces the doses of other drugs required for induction and maintenance of anaesthesia
Addition of butorphanol will reduce analgesia produced from the full mu agonist; combination is not recommended for analgesia
Synergistic sedation
Synergistic sedation and analgesia
Butorphanol's mu-antagonist properties may block or partially reverse the analgesic effects of full mu-agonists. Higher doses of full mu-agonists may be required.
監測
- Analgesic and/or antitussive efficacy
- Respiratory rate and depth
- Appetite and bowel function
- CNS effects (sedation vs. excitement)
藥物動力學
半衰期
吸收
Completely absorbed in the gut when administered orally, but due to a high first-pass effect, only about 16% (1/6th) reaches systemic circulation. Completely absorbed following IM administration.
分佈
Well distributed. Highest levels found in liver, kidneys, and intestine. Approximately 80% bound to plasma proteins. Crosses the placenta (neonatal levels roughly equivalent to maternal) and distributes into maternal milk.
代謝
Metabolized in the liver, primarily by hydroxylation, as well as N-dealkylation and conjugation. Metabolites do not exhibit analgesic activity.
排除
Metabolites and parent compound are mainly excreted into the urine (only 5% unchanged). 11-14% is excreted into the bile and eliminated in feces.
過量
Acute life-threatening overdoses are unlikely (LD50 in dogs is 50 mg/kg). However, because veterinary injection comes in two highly different strengths (0.5 mg/mL and 10 mg/mL), inadvertent overdoses can occur in small animals.
Clinical Signs: CNS effects (profound sedation or excitement), cardiovascular changes, and respiratory depression.
Treatment:
- Administer intravenous naloxone immediately to reverse opioid effects.
- Provide supportive measures: IV fluids, oxygen therapy, vasopressors, and mechanical ventilation if required.
- If seizures occur and persist, use diazepam for control.
可用產品
劑型
- Veterinary Injection: 0.5 mg/mL, 2 mg/mL, 10 mg/mL
- Veterinary Tablets: 1 mg, 5 mg, 10 mg
- Human Injection: 1 mg/mL, 2 mg/mL
- Human Nasal Spray: 10 mg/mL
獸醫用
- Butorphanol Tartrate Injection: 0.5 mg/mL (Torbutrol)
- Butorphanol Tartrate Injection: 2 mg/mL (Torbugesic-SA)
- Butorphanol Tartrate Injection: 10 mg/mL (Torbugesic, Dolorex, Butorject, Torphaject, Equanol)
- Butorphanol Tartrate Tablets: 1 mg, 5 mg, and 10 mg (Torbutrol)
人用標示
- Butorphanol Tartrate Injection: 1 mg/mL, 2 mg/mL (Stadol)
- Butorphanol Nasal Spray: 10 mg/mL
各地核准狀態
Subject to specific member state controlled drug regulations.
Classified as POM-V (Prescription Only Medicine - Veterinarian).
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
The injectable product should be stored out of bright light and at room temperature; avoid freezing.
飼主須知
這是什麼藥物？ 布托啡諾是一種用於緩解咳嗽、提供輕度止痛，或在獸醫進行處置前作為鎮靜劑的藥物。
我應該預期什麼情況？
- 您的寵物可能會變得嗜睡或稍微步態不穩（搖晃）。這是正常現象，但在藥效消退前，請將牠們安置在安全、安靜的環境中（例如避免上下樓梯）。
- 如果是為了治療咳嗽而開立此藥，您應該會注意到咳嗽發作的頻率顯著減少。
重要警告：
- 請勿超過處方劑量給藥。 給予過多藥物並不會增加止痛效果，反而會增加副作用。
- 如果您寵物的咳嗽從「乾咳」變成「有痰的濕咳」，請聯繫您的獸醫師。抑制濕咳可能會導致黏液積聚在肺部。
- 如果發現寵物行為有重大改變、食慾不振，或出現嚴重的便秘/腹瀉，請向您的獸醫師報告。
VetSheet 藥物參考供合格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商最新仿單。