保泰松
Phenylbutazone
Phenylbutazone (synthetic pyrazolone derivative)
別名: Butazolidin · Phenylbute · butadiene · fenilbutazona · phenylbutazonum
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。
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 inflammation/pain | 14 mg/kg | PO | three times daily initially | — | 🌎 NA |
| General inflammation/pain | 15-22 mg/kg | PO | q12h | — | 🌎 NA |
| Analgesia | 1-5 mg/kg | PO | q8h | — | 🌎 NA |
- General inflammation/pain: Maximum of 800 mg/day regardless of weight; titrate dose to lowest effective dose. Rarely used today.
馬
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| To reduce pain or pyrexia associated with pleuropneumonia | 2.2-4.4 mg/kg | PO or IV | q12h | first week of treatment or longer | 🌎 NA |
| General musculoskeletal inflammation | 1-2 grams per 454 kg (1000 lb.) horse IV, or 2-4 grams per 454 kg (1000 lb.) horse PO | IV or PO | daily | Limit IV administration to no more than 5 successive days | 🌎 NA |
| Adjunctive treatment of colic (to reduce endotoxic effects) | 2.2 mg/kg | PO or IV | twice daily | — | 🌎 NA |
| Adjunctive treatment of laminitis | Initial dose of 4 grams, immediately decreased to 1 to 1.5 grams | PO or IV | twice daily | — | 🌎 NA |
| Osteoarthritis | 2.2 mg/kg | PO | twice daily | — | 🌎 NA |
- General musculoskeletal inflammation: Do not exceed 4 grams/day. Use high end of dosage range initially, then titrate to lowest effective dose. Injection must be made slowly and with care.
- Adjunctive treatment of laminitis: Dose for an average adult-sized horse. Lower dose is used to keep the horse comfortable, but not relieve pain to the extent the horse moves around excessively.
- Osteoarthritis: Minimal dose to control pain.
牛
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| General inflammation/pain | 4-8 mg/kg PO or 2-5 mg/kg IV | PO or IV | — | — | 🌎 NA |
| General inflammation/pain | 10-20 mg/kg PO, then 2.5-5 mg/kg q24h or 10 mg/kg every 48 hours PO | PO | q24h or q48h | — | 🌎 NA |
- General inflammation/pain: Extralabel use prohibited in female dairy cattle 20 months of age or older.
- General inflammation/pain: Extralabel use prohibited in female dairy cattle 20 months of age or older.
豬
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| General inflammation/pain | 4 mg/kg | IV or PO | q24h | — | 🌎 NA |
| General inflammation/pain | 4-8 mg/kg PO or 2-5 mg/kg IV | PO or IV | — | — | 🌎 NA |
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
保泰松 (Phenylbutazone，俗稱 "bute") 是一種經典的非選擇性非類固醇消炎止痛藥 (NSAID)，屬於吡唑酮 (pyrazolone) 類。
臨床要點： 雖然歷史上曾廣泛應用於多種動物以發揮其強效的鎮痛、消炎和解熱作用，但在現代獸醫學中，其應用幾乎完全侷限於馬科臨床，用於控制肌肉骨骼疼痛（如蹄葉炎、骨關節炎）。
在小動物（犬貓）中，由於其引發嚴重不良反應（包括血液惡病質、肝毒性和嚴重的胃腸道潰瘍）的風險極高，已大多被更安全的 COX-2 選擇性 NSAIDs（如卡洛芬或美洛昔康）所取代。由於對人類有骨髓毒性（再生不良性貧血）的安全疑慮，本藥在經濟動物中的使用受到嚴格管制。
作用機制
Phenylbutazone acts primarily by inhibiting the cyclooxygenase (COX) enzymes (both COX-1 and COX-2), which prevents the conversion of arachidonic acid → prostaglandins and thromboxanes.
- ↓ Prostaglandins → Reduced inflammation, analgesia, and antipyresis.
- ↓ Thromboxane A2 → Decreased platelet aggregation.
Pharmacological Note: Phenylbutazone is metabolized in the liver to oxyphenbutazone, an active metabolite that contributes significantly to its prolonged efficacy (often >24 hours) despite a relatively short plasma half-life. The irreversible binding of phenylbutazone to cyclooxygenase also extends its duration of action. It also possesses mild uricosuric properties.
安全性與警告
禁忌症
- Known hypersensitivity to phenylbutazone or other NSAIDs
- History of or preexisting hematologic or bone marrow abnormalities
- Preexisting gastrointestinal ulcers
- Food-producing animals (especially female dairy cattle 20 months of age or older)
- Lactating dairy cattle
- Pre-existing gastrointestinal ulceration
- Renal impairment
- Hepatic impairment
- Hematological disorders
- Use in food-producing animals (banned in many jurisdictions)
不良反應
- Gastrointestinal and oral erosions/ulcers
- Hypoalbuminemia (especially in foals/ponies)
- Renal papillary necrosis and azotemia
- Sodium and water retention (edema)
- Blood dyscrasias (agranulocytosis, aplastic anemia)
- Hepatotoxicity
- Severe tissue necrosis and sloughing (if injected IM or SC)
- CNS stimulation and seizures (if injected intracarotid)
- Gastrointestinal ulceration and bleeding
- Bone marrow suppression (aplastic anemia, leukopenia)
注意事項
Use with extreme caution in foals and ponies due to increased incidence of hypoproteinemia and GI ulceration. Avoid in horses with known or suspected Equine Gastric Ulcer Syndrome (EGUS). Use cautiously in animals with preexisting renal disease or congestive heart failure (CHF) due to potential for sodium/water retention and decreased renal blood flow. May mask clinical signs of lameness in horses. WARNING: Do not administer injectable preparations IM or SC as it is highly irritating and causes necrosis/sloughing. Intracarotid injections may cause CNS stimulation and seizures.
藥物相互作用
Phenylbutazone may antagonize the increased renal blood flow effects caused by furosemide.
Concurrent administration may increase the chances of hepatotoxicity developing.
Concurrent use increases the potential for adverse GI and renal reactions. (Note: 'Stacking' with ketoprofen shows synergistic toxicity).
May increase the risk of hematologic and/or renal adverse reactions.
Phenylbutazone may increase the plasma half-life of penicillin G.
Phenylbutazone could potentially displace sulfonamides from plasma proteins, increasing the risk for adverse effects.
Phenylbutazone could potentially displace warfarin from plasma proteins, increasing the risk for bleeding.
Increased risk of gastrointestinal ulceration
Increased risk of gastrointestinal ulceration and renal toxicity
Displacement from plasma proteins leading to increased free drug concentrations
監測
- Analgesic, anti-inflammatory, and antipyretic efficacy
- Complete blood counts (CBC) with chronic therapy (weekly early in therapy, biweekly later)
- Urinalysis and renal function parameters (serum creatinine/BUN) with chronic therapy
- Plasma protein determinations (especially in ponies, foals, and debilitated animals)
- Complete Blood Count (CBC)
- Renal function (BUN, Creatinine)
- Liver enzymes
- Clinical signs of GI bleeding (melena)
藥物動力學
半衰期
吸收
Absorbed from both the stomach and small intestine following oral administration.
分佈
Distributed throughout the body with highest levels attained in the liver, heart, lungs, kidneys, and blood. Plasma protein binding in horses exceeds 99%. Crosses the placenta and is excreted into milk.
代謝
Nearly completely metabolized in the liver, primarily to oxyphenbutazone (active) and gamma-hydroxyphenylbutazone.
排除
Excreted primarily in the urine. More rapidly excreted into alkaline than acidic urine. Oxyphenbutazone can be detected in horse urine up to 48 hours after a single dose.
過量
Manifestations of acute overdosage include prompt respiratory or metabolic acidosis with compensatory hyperventilation, seizures, coma, and acute hypotensive crisis.
- Systemic Effects: Clinical signs of renal failure (oliguric, proteinuria, hematuria), liver injury (hepatomegaly, jaundice), bone marrow depression, and severe GI ulceration/perforation may develop.
- Dogs: Common signs include ataxia, seizures, tachycardia, trembling, tremors, vomiting, and tachypnea. Oral LD50 is 332 mg/kg.
- Horses: Common signs include colic, anorexia, and ataxia.
Treatment: Standard overdose procedures should be followed (e.g., empty gut following oral ingestion). Institute supportive treatment as necessary. Intravenous diazepam can be used to help control seizures. Monitor fluid therapy carefully, as phenylbutazone may cause fluid retention.
可用產品
劑型
- Tablets
- Oral powder
- Oral paste
- Injection
- 100 mg tablet
- 200 mg tablet
獸醫用
- Phenylbutazone Tablets: 100 mg, 200 mg, 1 gram
- Phenylbutazone Oral Powder: 1 gram in 10 grams of powder
- Phenylbutazone Paste Oral Syringes: 6 grams or 12 grams/syringe
- Phenylbutazone Injection: 200 mg/mL in 100 mL vials
- 100 mg tablets (Currently unavailable)
- 200 mg tablets (Currently unavailable)
各地核准狀態
POM. Licensed forms for small animals are currently unavailable. Prohibited in food-producing animals.
POM-V. Licensed forms for small animals are currently unavailable. Prohibited in food-producing animals.
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Oral products should be stored in tight, child-resistant containers if possible. The injectable product should be stored in a cool place (46-56° F) or kept refrigerated.
飼主須知
給馬主人的指引：
- 「Bute」對於控制骨骼和關節疼痛非常有效。請務必完全按照獸醫師的指示給藥。
-
嚴重警告： 絕對不可將液體注射劑施打於肌肉內 (IM) 或皮下 (SC)。必須由專業人員嚴格執行靜脈注射 (IV)。若注射不當，會導致嚴重的組織壞死和脫落。
- 密切觀察是否有胃潰瘍或腎臟問題的跡象：食慾不振、腹瀉、腹痛 (疝痛) 跡象，或腿部/腹部腫脹。若出現這些情況，請立即停藥並聯絡您的獸醫師。
給狗主人的指引：
- 由於有更安全的替代藥物，現今已極少在狗身上使用此藥。如果您的狗被開立此藥，請密切觀察是否有嘔吐、排黑/柏油樣糞便或嗜睡的情況，若有發生請立即聯絡獸醫師。
經濟動物限制：
- FDA 嚴格禁止將此藥用於 20 個月齡以上的母乳牛。
- 若標示外使用於肉牛，需遵守嚴格的停藥期（例如：1 劑 = 30 天，2 劑 = 35 天）。請諮詢您的獸醫師。
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