丁丙諾啡
Buprenorphine
Buprenorphine hydrochloride
別名: Buprenex · Subutex · Suboxone · Butrans · Temgesic · Simbadol · Zorbium · Bupaq · Buprecare · Buprenodale · Buprevet · Vetergesic · Buprenorphine HCl · buprenorphini hydrochloridum · CL-112302 · NIH-8805 · UM-952 · Buprenorphinum
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Analgesia during gastrointestinal stasis
須由已驗證獸醫確認
- q8–12h
必須同時考慮的臨床上下文 (1)
- Exclude emergent diagnoses (obstruction, enterotoxemia)
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
丁丙諾啡在獸醫學中是一種用途廣泛的鴉片類部分促效劑。主要用於控制小動物的輕至中度急性疼痛，並常與 α-2 促效劑及解離型麻醉劑合併用於短效保定「雞尾酒」配方中。
- 臨床要點：丁丙諾啡在標準劑量下具有「天花板效應（ceiling effect）」，意味著超過一定劑量後，可能無法產生額外的鎮痛效果，甚至在理論上可能降低鎮痛效力。
- 貓科優勢：貓的口腔 pH 值偏鹼性，這使得丁丙諾啡具有高度脂溶性，從而實現極佳的經口腔黏膜（OTM）/ 頰黏膜吸收。在貓身上，頰黏膜給藥的生物可用率幾乎與肌肉注射相當，是居家術後疼痛管理的實用途徑。
- 作用時間：與純 mu-促效劑（如吩坦尼或美沙酮）相比，其起效時間較長，但鎮痛持續時間顯著更長（通常為 6-8 小時，最長可達 12 小時）。
- 法規：本品屬於管制藥品。
作用機制
Buprenorphine exerts its analgesic effects by acting as a partial agonist at the mu (μ) opioid receptor and an antagonist at the kappa (κ) opioid receptor in the central nervous system.
- High Affinity, Slow Dissociation: It binds to the μ-receptor with an affinity approximately 30 times greater than morphine. This tight binding → prolonged duration of action.
- Receptor Competition: Because of its high affinity, it can displace pure μ-agonists from the receptor, potentially antagonizing their analgesic effects while reversing their sedative and respiratory depressant effects.
- Naloxone Resistance: Its slow dissociation from the receptor makes it notoriously difficult to fully reverse with standard doses of the opioid antagonist naloxone; high doses of naloxone or the use of doxapram may be required in cases of severe respiratory depression.
安全性與警告
禁忌症
- Known hypersensitivity to buprenorphine
不良反應
- Respiratory depression (rare but significant)
- Sedation
- Urine retention or difficulty voiding (particularly with high IV or epidural doses)
- Excitement (horses)
- Diminished gut sounds (horses)
- Vomiting (rare in cats)
注意事項
Use with caution in patients with hypothyroidism, severe renal insufficiency, adrenocortical insufficiency (Addison's), and in geriatric or severely debilitated patients. Use cautiously in patients with compromised cardiopulmonary function due to the rare risk of respiratory depression. Extreme caution is required in patients with head trauma, increased CSF pressure, or CNS dysfunction (e.g., coma). Patients with severe hepatic dysfunction may eliminate the drug more slowly. May increase bile duct pressure; use cautiously in biliary tract disease.
藥物相互作用
May be potentiated by concomitant use of buprenorphine
May decrease plasma buprenorphine levels
Case reports of humans developing respiratory/cardiovascular/CNS depression; use with caution
May cause increased CNS or respiratory depression when used with buprenorphine
Can increase plasma buprenorphine levels
Buprenorphine may potentially antagonize some analgesic effects, but may also reverse some sedative and respiratory depressant effects
Potentially can increase buprenorphine effects
Can increase plasma buprenorphine levels
Possible additive effects or increased CNS depression
May reduce analgesia associated with high dose buprenorphine
If used with buprenorphine may cause increased conjunctival changes
Potentially decrease plasma buprenorphine concentrations
May antagonize the effects of full opioid agonists, though clinical relevance is debated. If analgesia is inadequate after buprenorphine, a full mu agonist may be administered without delay.
May antagonize the effects of full opioid agonists.
Reduces the doses of other drugs required for induction and maintenance of anaesthesia.
監測
- Analgesic efficacy
- Respiratory status
- Cardiac status
藥物動力學
半衰期
吸收
Rapidly absorbed following IM injection (40-90% in humans). Sublingual bioavailability is ~55% in humans. Oral doses undergo a high first-pass effect in the GI mucosa and liver. In cats, oral transmucosal (buccal) absorption is comparable to IM or IV administration. In dogs, oral transmucosal absorption is about 50%. Subcutaneous administration may be less bioavailable.
分佈
Highly bound (96%) to plasma proteins (not albumin). Concentrates in the liver, but also found in the brain, GI tract, and placenta. Crosses the placenta and is found in maternal milk at concentrations equal to or greater than plasma. Volume of distribution in cats is approximately 8 L/kg.
代謝
Metabolized in the liver by N-dealkylation and glucuronidation.
排除
Metabolites are eliminated by biliary excretion into the feces (≈70%) and urinary excretion (≈27%). Clearance in cats is about 20 mL/kg/min.
過量
Buprenorphine has a very high index of safety (ratio of lethal dose to effective dose is at least 1000:1 in rodents). Life-threatening acute overdoses are rare in veterinary medicine, but clinical signs are common.
- Clinical Signs (Dogs): Vocalization, ataxia, hypersalivation, hypothermia, and lethargy.
- Treatment: Supportive care. In cases of acute overdose causing severe respiratory or cardiac effects, naloxone and doxapram are suggested.
Note: Due to buprenorphine's extremely high affinity for the mu-receptor, standard doses of naloxone may be ineffective; very high doses of naloxone may be required to reverse respiratory depression.
可用產品
劑型
- Sublingual tablets
- Transdermal patch
- Sublingual film/tablet with naloxone
- Compounded sustained-release injection
獸醫用
- Compounded sustained-release injectable (SC) product (zoopharm.net)
人用標示
- Buprenorphine HCl for Injection: 0.324 mg/mL (equivalent to 0.3 mg/mL buprenorphine) (Buprenex)
- Buprenorphine HCl Sublingual Tablets: 2 mg & 8 mg (Subutex)
- Buprenorphine HCl Transdermal System (Butrans)
- Buprenorphine HCl Combinations (Sublingual Tablets): 2 mg buprenorphine/0.5 mg naloxone; 8 mg buprenorphine/2 mg naloxone (Suboxone)
各地核准狀態
POM-V CD
POM-V CD SCHEDULE 3
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Store at room temperature (15-30° C). Avoid temperatures above 40° C or below freezing. Store away from bright light. Autoclaving may considerably decrease drug potency. Stable between a pH of 3.5-5.
飼主須知
丁丙諾啡是一種強效止痛藥，常讓飼主帶回家用於貓咪和小型犬。
- 給藥技巧：如果您被指示經口給予此藥物，請勿將其直接射入喉嚨。請將注射器尖端放在口腔側邊（頰囊或舌下）給藥。藥物會直接透過牙齦吸收。如果被吞下，藥物在發揮作用前就會被肝臟大量破壞。
- 準備工作：強烈建議預先將劑量抽入注射器中，以確保在家中給藥的準確性。
- 預期反應：您的寵物可能會變得有些嗜睡，或者在少數情況下會有些焦躁或發出叫聲。
- 安全性：按照指示使用時，此藥物非常安全，但它屬於管制藥品。請務必將其放在兒童和其他寵物絕對接觸不到的地方。
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