別嘌醇
Allopurinol
1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
別名: Zyloprim · Aloprim · Zyloric · Zylapour · allopurinolum · BW-56-158 · HPP · NSC-1390 · oxypurinol (active metabolite) · alloxanthine
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 |
|---|---|---|---|---|---|
| Urate uroliths (dissolution) | 15 mg/kg PO q12h; only in conjunction with low purine foods. | PO | q12h | — | 🌎 NA |
| Urate uroliths (prevention) | 10-20 mg/kg/day | PO | Daily | — | 🌎 NA |
| Urate uroliths (dissolution and prevention) | 7-10 mg/kg PO three times daily | PO | TID | — | 🌎 NA |
| Leishmaniasis (First line treatment) | 10 mg/kg PO twice daily | PO | BID | 6-12 months | 🌎 NA |
| Leishmaniasis (Second line treatment) | 10 mg/kg PO twice daily | PO | BID | 6-12 months | 🌎 NA |
| Leishmaniasis | 20 mg/kg PO q12h | PO | q12h | 9 months | 🌎 NA |
| Leishmaniasis (Alternate protocol alone) | 10 mg/kg PO q8h or 10-20 mg/kg PO q12h | PO | q8h or q12h | 1-4 months | 🌎 NA |
| Leishmaniasis | 10 mg/kg PO twice daily | PO | BID | — | 🌎 NA |
| Leishmaniasis (with renal insufficiency) | 5 mg/kg PO twice daily | PO | BID | — | 🌎 NA |
| Leishmaniasis | 15 mg/kg PO twice daily | PO | BID | months | 🌎 NA |
| Uric acid urolithiasis (Dissolution) | 10 mg/kg p.o. q8h or 15 mg/kg p.o. q12h | PO | q8h or q12h | up to 4 weeks | 🌍 EU |
| Uric acid urolithiasis (Prevention) | 10-15 mg/kg | PO | q24h | — | 🌍 EU |
| Leishmaniosis | 10 mg/kg | PO | q12h | at least 6-12 months | 🌍 EU |
- Urate uroliths (prevention): Preferable to minimize recurrence with dietary therapy to avoid xanthine uroliths.
- Urate uroliths (dissolution and prevention): Goal is to reduce urine urate:creatinine ratio by 50%.
- Leishmaniasis (First line treatment): Used plus Meglumine antimoniate 75-100 mg/kg once daily for 4-8 weeks.
- Leishmaniasis (Second line treatment): Used plus Miltofosine 2 mg/kg PO once daily for 4 weeks OR allopurinol alone.
- Leishmaniasis: With Meglumine antimoniate (100 mg/kg/day SQ) until resolution.
- Leishmaniasis: If possible use with meglumine antimoniate, if not, use alone.
- Leishmaniosis: Use with meglumine antimonate for 1-2 months, or miltefosine for 1 month (NB: this does not result in complete parasitological cure).
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Leishmaniosis | 10-20 mg/kg | PO | q12-24h | — | 🌍 EU |
- Leishmaniosis: Has been shown to be effective (although experience is limited in this species).
鳥
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Gout (budgies and cockatiels) | Crush one 100 mg tablet into 10 mL of water. Add 20 drops of this solution to one ounce of drinking water. | PO | Continuous in water | — | 🌎 NA |
| Gout (parakeets) | Crush one 100 mg tablet into 10 mL of water. Add 20 drops of this solution to one ounce of drinking water or give 1 drop 4 times daily. | PO | Continuous or QID | — | 🌎 NA |
爬蟲類
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Elevated uric acid levels in renal disease (lizards) | 20 mg/kg PO once daily | PO | SID | — | 🌎 NA |
| Gout | 20 mg/kg PO once daily | PO | SID | — | 🌎 NA |
| Hyperuricemia (green iguanas) | 25 mg/kg PO daily | PO | SID | — | 🌎 NA |
- Gout: Suggested dosage based upon human data as dose is not established for reptiles.
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
別嘌醇 (Allopurinol) 是一種強效的黃嘌呤氧化酶抑制劑，廣泛應用於獸醫學中。
主要臨床應用包括：
- 尿酸鹽結石： 主要用於犬隻（特別是易感品種如大麥町犬）以溶解和預防尿酸結石。必須結合低嘌呤飲食使用，以防止黃嘌呤結石的形成。
- 犬利什曼原蟲症： 作為抑制利什曼原蟲的藥物。通常與葡甲胺銻 (meglumine antimoniate) 或米替福新 (miltefosine) 聯合使用進行長期管理。
- 鳥類與爬蟲類醫學： 用於控制高尿酸血症及治療鳥類和爬蟲類的痛風。
臨床提示： 由於別嘌醇會增加黃嘌呤的尿液排泄，若長期高劑量使用且未限制飲食中的嘌呤，反而可能導致黃嘌呤結石的形成。
作用機制
Allopurinol and its primary active metabolite, oxypurinol (alloxanthine), competitively inhibit the enzyme xanthine oxidase.
- Normal Pathway: Hypoxanthine → xanthine oxidase → Xanthine → xanthine oxidase → Uric Acid
- Inhibition: By blocking this enzyme, allopurinol prevents the conversion of oxypurines to uric acid. This decreases serum and urine concentrations of uric acid, while increasing the levels of the more water-soluble precursors (hypoxanthine and xanthine).
In Leishmaniasis: Allopurinol acts as a purine analogue. Leishmania organisms mistakenly incorporate allopurinol metabolites into their RNA, which disrupts protein synthesis and inhibits parasite multiplication.
安全性與警告
禁忌症
- Known hypersensitivity to allopurinol
- Red-tailed hawks (anecdotal reports of severe toxicity)
不良反應
- Xanthine urolithiasis (especially with high doses or non-restricted diets)
- Hypersensitivity reactions (rash, erythema)
- Lethargy
- Gastrointestinal upset
- Hepatotoxicity (rare)
- Bone marrow suppression (rare)
注意事項
Prolonged high doses of allopurinol may result in xanthine uroliths; it is highly recommended to use concurrently with a low-purine diet for urolith management. Use with caution and consider dose reduction (e.g., 5 mg/kg PO twice daily) in patients with renal insufficiency.
藥物相互作用
May increase risks for hypoglycemia and hepato-renal reactions
Increased bone marrow depression may occur
Allopurinol may increase cyclosporine levels
Can increase uric acid levels, antagonizing allopurinol's effect
Allopurinol may reduce the metabolism of warfarin thereby increasing its effect
Thrombocytopenia has occurred in a few human patients when used concurrently
May increase the renal excretion of oxypurinol and thereby reduce xanthine oxidase inhibition; additive effects on blood uric acid may be beneficial
May reduce the solubility of uric acid in the urine and induce urolithiasis
Allopurinol inhibits the metabolism of azathioprine, leading to severe, potentially fatal myelosuppression.
Allopurinol inhibits the metabolism of mercaptopurine, significantly increasing toxicity risk.
Concurrent use increases the risk of cutaneous rash.
May decrease theophylline clearance, increasing the risk of toxicity.
May increase the risk of allopurinol hypersensitivity and toxicity.
Increased risk of skin rashes when used concurrently.
監測
- Urine uric acid (for urolithiasis)
- Adverse effects (rash, lethargy)
- Periodic CBC, liver and renal function tests (e.g., BUN, Creatinine, liver enzymes); especially early in therapy
藥物動力學
吸收
Rapidly absorbed following oral administration.
分佈
Widely distributed in tissue fluid; not highly bound to plasma proteins.
代謝
Rapidly oxidized to its primary active metabolite, oxypurinol (alloxanthine), which is also a xanthine oxidase inhibitor.
排除
Excreted primarily in the urine as oxypurinol and unchanged allopurinol.
過量
Information on acute overdosage in veterinary species is limited. Massive overdoses may cause gastrointestinal distress (vomiting, diarrhea). Treatment should consist of supportive care and monitoring of renal function. Adequate hydration is important to promote diuresis and excretion.
可用產品
劑型
- Oral tablets
- Powder for injection (lyophilized)
- Compounded oral suspension
人用標示
- Allopurinol Oral Tablets: 100 mg & 300 mg; Zyloprim® (Faro); generic
- Allopurinol Powder for Injection, lyophilized: 500 mg preservative-free in 30 mL vials; Aloprim® (Nabi); generic (Bedford Labs)
各地核准狀態
Approved in several EU member states specifically for canine leishmaniosis.
Used under the cascade where specific veterinary licensed products are unavailable.
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Tablets should be stored at room temperature in well-closed containers; stable in light and air. Powder for injection should be stored at 25°C (excursions permitted to 15-30°C). Once diluted to ≤6 mg/mL, store at room temperature and use within 10 hours; do not refrigerate. Compounded oral suspensions (20 mg/mL) in Ora-Plus/Ora-Sweet retain >95% potency for 60 days at 5°C and 25°C and should be protected from light.
飼主須知
重要提示： 除非獸醫師另有指示，否則請在飯後（通常約飯後1小時）給予此藥物，以減少腸胃不適。
- 飲食管理： 如果您的寵物正在接受尿酸結石治療，請嚴格遵守獸醫師處方的低嘌呤飲食。若未配合適當飲食而服用此藥，可能會導致形成另一種結石（黃嘌呤結石）。
- 何時應聯繫獸醫師： 如果您的寵物出現皮疹、異常嗜睡或看起來生病，請立即通知您的獸醫師。
- 確保您的寵物隨時有充足的新鮮飲水，以幫助沖洗泌尿系統。
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