布地奈德
Budesonide
別名: Entocort EC · Pulmicort · Rhinocort · Benacort · Budelin · Budenofalk · Cortiment · Budesonidum
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
這是依體表面積（mg/m²）計算的劑量；給藥前須先將體重換算為體表面積。
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
狗
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Inflammatory Bowel Disease (IBD) (Clinical Pearl) | 1 - 3 mg/m2 or 1 - 3 mg/dog | PO | q24h | Chronic management; taper to lowest effective dose | 🌍 EU |
- Inflammatory Bowel Disease (IBD) (Clinical Pearl): Do not crush or chew capsules.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Inflammatory Bowel Disease (IBD) (Clinical Pearl) | 1 mg/cat | PO | q24h | Chronic management; taper to lowest effective dose | 🌍 EU |
| Feline Asthma (Clinical Pearl) | 100 - 400 µg (1-2 puffs) | Inhalation | q12h | Chronic management | 🌍 EU |
- Inflammatory Bowel Disease (IBD) (Clinical Pearl): May be compounded if standard sizes are too large, though this alters the enteric coating.
- Feline Asthma (Clinical Pearl): Administer via a feline-specific spacer mask (e.g., AeroKat).
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
布地奈德 (Budesonide) 是一種局部作用、高效能的糖皮質激素（效力約為潑尼松龍的 15 倍），具有微弱的鹽皮質激素活性。
- 靶向釋放：口服劑型通常採用腸溶包衣（如 Entocort EC®），延遲藥物溶解直至抵達十二指腸。這使得藥物能在腸道內發揮集中的局部抗發炎作用。
- 減少全身性副作用：雖然會被吸收到門脈循環中，但布地奈德具有極高的肝臟首過代謝率。肝臟會在藥物進入全身血液循環前清除絕大部分，這大幅降低了典型全身性類固醇副作用（如多飲、多尿和多食）的風險。
- 臨床應用：在獸醫學中主要用於標示外治療犬貓的炎症性腸病 (IBD)，特別是針對無法耐受或對傳統全身性類固醇無反應的病患。
- 成本與劑型：藥物費用可能是一個限制因素；此外，由於人類用膠囊對小型獸醫病患來說通常劑量過大，此藥物經常需要透過特殊藥局重新調配成較小的劑量。
作用機轉
Budesonide diffuses across cell membranes and binds with high affinity to cytosolic glucocorticoid receptors (GR).
- The receptor-ligand complex translocates to the nucleus → binds to glucocorticoid response elements (GREs) on DNA → alters gene transcription.
- Anti-inflammatory pathway: Induces the production of lipocortin-1 (annexin-1) → inhibits phospholipase A2 → blocks the release of arachidonic acid from membrane phospholipids → decreases the synthesis of potent inflammatory mediators (prostaglandins and leukotrienes).
- Despite its high first-pass metabolism, it still causes significant suppression of the hypothalamic-pituitary-adrenal (HPA) axis.
安全性與警告
禁忌症
- Hypersensitivity to budesonide
- Patients with active GI ulcers
- Active systemic infections
- Diabetes mellitus
- Cataracts
不良反應
- Steroid hepatopathy
- HPA-axis suppression
- Hyperadrenocorticism (rare, but risk increases with hepatic dysfunction)
注意事項
Use with caution in patients with moderate to severe hepatic dysfunction, as they are more likely to develop signs of hypercorticism. Because budesonide suppresses the HPA-axis, animals undergoing stressful procedures (such as surgery) should be considered for exogenous systemic steroid administration. FDA Category C for pregnancy; demonstrated to be embryocidal and teratogenic in rats and rabbits.
藥物交互作用
May decrease the hepatic metabolism of budesonide, leading to increased systemic blood levels and a higher risk of glucocorticoid adverse effects.
May increase gastric pH, potentially causing premature dissolution of the enteric coating and reducing the drug's targeted efficacy in the intestines.
Inhibits CYP3A4, significantly increasing systemic budesonide levels and risk of toxicity
Inhibits CYP3A4, increasing systemic budesonide levels
Inhibits CYP3A4, potentially increasing budesonide levels
Increased risk of gastrointestinal ulceration and bleeding
監測
- Resolution of clinical signs of IBD (vomiting, diarrhea, weight loss)
- Liver enzymes (ALP, ALT) for potential steroid hepatopathy
- Clinical signs of hyperadrenocorticism (PU/PD/PP, panting, alopecia)
藥物動力學
半衰期
吸收
Bioavailability is 10-20% in dogs due to a high first-pass effect. In humans, food may delay absorption but does not impact the total amount absorbed.
分佈
Mean volume of distribution in humans ranges from 2.2-3.9 L/kg.
代謝
Undergoes extensive first-pass metabolism in the liver, which significantly reduces systemic bioavailability.
排除
Completely metabolized; metabolites are excreted in the feces and urine. Clearance in dogs is 2.2 L/hr/kg.
過量
Acute oral overdoses are unlikely to be of much clinical concern, though massive overdoses may warrant gut evacuation. The lethal dose in mice is reported to be 200 mg/kg.
可用產品
劑型
- Enteric-coated capsules
- Inhalation suspension
- Nasal spray
- Compounded oral formulations
人用標示
- Entocort EC® (capsules)
各地核准狀態
Human authorized products used off-label under the cascade.
Human authorized products used off-label under the cascade.
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Store at room temperature in tight, light-resistant containers. Protect from moisture.
飼主須知
重要提示：請勿將腸溶膠囊壓碎或讓寵物咀嚼。必須保持特殊的包衣完整，才能將藥物準確送達腸道。
- 給藥方式：可與食物一起或空腹餵食。如果您的寵物腸胃敏感，與食物同服可能會有幫助。
- 副作用：雖然比標準全身性類固醇（如潑尼松）少見得多，但仍需注意是否有飲水量增加、排尿量增加、食慾大增或異常喘息的情況。
- 壓力與手術注意事項：由於此藥物會抑制身體自然的壓力反應，在進行任何手術、洗牙或面臨重大壓力事件前，請務必告知獸醫師您的寵物正在服用布地奈德。他們可能需要暫時給予其他類固醇來幫助寵物度過壓力期。
- 調劑藥品：由於人類用膠囊對小型寵物來說通常劑量過大，您的獸醫師可能會將此藥物送至特殊藥局重新調配，以確保劑量準確。
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