醋酸異氟潑尼龍
Isoflupredone Acetate
9alpha-fluoroprednisolone acetate
別名: Predef 2X · U-6013 · 9alpha-fluoroprednisolone acetate
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。
各物種劑量
🌎 NA — North America🌍 EU — Europe
馬
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Labeled systemic indications | 5-20 mg (total dose) | IM | repeated as necessary | — | 🌎 NA |
| Intrasynovial administration | 5-20 mg or more | Intrasynovial | — | — | 🌎 NA |
| Intraarticular administration | 4-20 mg | Intraarticular | — | — | 🌎 NA |
| Treatment of 'heaves' (RAO) | 10-14 mg (total dose) | IM | once daily | — | 🌎 NA |
| Treatment of recurrent airway obstruction (RAO) | 0.03 mg/kg | IM | once daily | 14 days | 🌎 NA |
- Intrasynovial administration: depending on the size of the joint cavity
- Intraarticular administration: has a short to medium duration of action
- Treatment of 'heaves' (RAO): for a horse weighing between 450-500 kg
- Treatment of recurrent airway obstruction (RAO): Patients developed significant decreases in serum potassium
牛
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Labeled systemic indications | 10-20 mg (total dose) | IM | repeated in 12 to 24 hours if indicated | — | 🌎 NA |
- Labeled systemic indications: according to the size of the animal and severity of the condition
豬
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Labeled systemic indications | 5 mg (total dose) | IM | — | — | 🌎 NA |
- Labeled systemic indications: for a 300 lb. animal. Adjust dose proportionally for a smaller or larger animal.
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
醋酸異氟潑尼龍 (Isoflupredone acetate) 是一種強效的含氟合成糖皮質素，主要於大型動物（牛、馬和豬）醫學中使用。
- 效力：其抗發炊效力約為氫化可的松的 17 倍，潑尼松龍的 10 倍。其糖皮質素活性評估為氫化可的松的 50 倍。
- 臨床應用：常用於其顯著的抗發炊和免疫抑制作用。標示適應症包括牛酮體症的輔助治療、肌肉骨骼發炊、急性過敏反應、伴隨嚴重毒性的嚴重感染，以及馬匹的復發性呼吸道阻塞 (RAO)。
- 臨床珍珠：與地塞米松或倍他米松不同，異氟潑尼龍較不易引發早產，但在懷孕後期仍應避免使用。值得注意的是，它保留了顯著的礦物皮質素活性，使患者極易出現低血鉀，即使在乳牛中僅使用單一劑量也可能發生。
作用機轉
Isoflupredone exerts its effects via classic genomic and non-genomic steroid pathways:
- Anti-inflammatory (Glucocorticoid Receptor - GR): Binds to cytosolic GR → translocates to the nucleus → induces transcription of lipocortin-1 (annexin A1). Lipocortin-1 inhibits phospholipase A2, thereby blocking the release of arachidonic acid and halting the production of inflammatory prostaglandins and leukotrienes. It also transrepresses pro-inflammatory transcription factors like NF-κB and AP-1.
- Mineralocorticoid Effects (Mineralocorticoid Receptor - MR): Binds to MR in the distal renal tubules → upregulates Na+/K+ ATPase and ENaC channels → promotes sodium retention and potassium excretion (leading to hypokalemia).
- Metabolic: Stimulates hepatic gluconeogenesis (useful in bovine ketosis) and decreases peripheral glucose utilization.
安全性與警告
禁忌症
- Systemic fungal infections (unless used for Addison's replacement)
- Idiopathic thrombocytopenia (when administered IM)
- Hypersensitivity to the compound
- Downer cows or animals susceptible to hypokalemia
- Calves to be processed into veal
- Late stages of pregnancy (relative contraindication)
不良反應
- Hypokalemia (even with single doses)
- Reduced milk production
- Delayed wound healing
- Gastrointestinal ulceration
- Increased infection rates
- Diabetes mellitus exacerbation / hyperglycemia
- Pancreatitis
- Hepatopathy
- Renal dysfunction
- Osteoporosis
- Laminitis (horses)
- Hypothyroidism
- Hyperlipidemia
- Decreased growth in young animals
- Premature parturition with retained placenta (if used in late pregnancy)
注意事項
Use with extreme caution in patients with active GI ulcers or those susceptible to them. Use cautiously in patients with diabetes mellitus. Because it can cause hypokalemia, it should not be used in downer cows or animals susceptible to the effects of hypokalemia. Chronic use in young, growing animals must be undertaken cautiously, as decreased growth may occur. Avoid using during pregnancy as it may induce premature parturition with retained placenta.
藥物交互作用
Increased chance of digitalis toxicity may occur should hypokalemia develop; diligent monitoring of potassium and digitalis glycoside levels is recommended
Administered concomitantly with glucocorticoids may cause hypokalemia
Glucocorticoids may reduce salicylate blood levels
With glucocorticoids may increase the risk of gastrointestinal ulceration
A diminished immune response may occur; patients receiving immunosuppressive dosages should generally not receive live attenuated-virus vaccines
監測
- Efficacy and adverse effects
- Serum potassium (highly recommended due to hypokalemia risk)
- Renal and liver function
- CBC
- Blood glucose
- Serum electrolytes
- ACTH stimulation tests (to determine HPA axis suppression)
- Thyroid hormone monitoring (if use is prolonged)
藥物動力學
代謝
Gluconeogenic activity persists for 48 hours after dosing in cattle.
過量
A single overdose of isoflupredone is unlikely to cause harmful effects. Should clinical signs require intervention, use supportive treatment. Chronic usage of glucocorticoids can lead to serious adverse effects, generally manifested as signs of hyperadrenocorticism.
可用產品
劑型
- Aqueous suspension for injection (2 mg/mL)
獸醫用
- Isoflupredone acetate 2 mg/mL aqueous suspension for injection in 10 mL and 100 mL vials; Predef 2x (Pfizer)
各地核准狀態
暫無法規資料: 🇺🇸 US · 🇪🇺 EU · 🇬🇧 UK · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
The injection should be stored at controlled room temperature 20°-25°C.
飼主須知
重要提示：這是一種強效類固醇藥物，必須完全按照獸醫的指示使用。
- 乳牛：請注意，投藥後牛奶產量可能會暫時下降。
- 馬與豬：觀察是否有虛弱、肌肉顫抖或嗜睡的跡象，這些可能是血鉀過低（低血鉀症）的表現。
- 一般監測：注意是否有口渴增加、排尿增加或食慾改變的情況。
- 如果您在家中自行給藥，請嚴格遵守獸醫的指示。如果已經長期使用此藥，請勿在未諮詢獸醫的情況下突然停藥。
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