醋酸可的松
Cortisone Acetate
11-dehydro-17-hydroxycorticosterone acetate
別名: acetato de cortisona · compound E acetate · acétate de cortisone · cortisoni acetas · 11-dehydro-17hydroxycorticosterone 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
狗
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Long-term treatment of hypoadrenocorticism (changeover period) | 0.5-1 mg/kg PO q12-24h | PO | q12-24h | Initial stabilization | 🌎 NA |
| Long-term treatment of hypoadrenocorticism (maintenance) | 0.5 mg/kg PO q12-24h | PO | q12-24h | Long-term | 🌎 NA |
- Long-term treatment of hypoadrenocorticism (changeover period): Used initially with a semi-selective mineralocorticoid (fludrocortisone).
- Long-term treatment of hypoadrenocorticism (maintenance): Provides adequate additional glucocorticoid supplementation once stable.
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
醋酸可的松 (Cortisone acetate) 是一種口服皮質類固醇，同時具有糖皮質素和鹽皮質素的作用。
主要臨床重點：
- 前驅藥特性：它在體內無生物活性，必須經由肝臟轉化為皮質醇 (cortisol) 才能發揮作用。
- 艾迪森氏症管理：可作為犬隻腎上腺皮質功能低下症（艾迪森氏症）口服治療中，替代培尼皮質醇 (prednisolone) 的潛在選擇。由於它同時提供糖皮質素和鹽皮質素活性，可能減少主要鹽皮質素藥物（如氟氫可的松）的劑量需求，進而降低整體治療成本。
- 爭議性：在獸醫學中並不常用，且其增加的鹽皮質素活性是否比標準培尼皮質醇療法具有顯著的臨床益處，在內分泌學家中仍有爭議。
- 安全性：當用於艾迪森氏症的生理替代劑量時，通常耐受性極佳。若使用超生理劑量，則會引發典型的皮質類固醇副作用（例如：多渴/多尿/多食、喘息、免疫抑制）。
作用機轉
Cortisone acetate is a prodrug. Upon oral absorption, it undergoes first-pass hepatic metabolism where the enzyme 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) converts it into the active hormone, cortisol.
- Glucocorticoid Action: Cortisol diffuses across cell membranes and binds to cytosolic glucocorticoid receptors (GR) → the receptor-ligand complex translocates to the nucleus → binds to glucocorticoid response elements (GREs) on DNA → alters gene transcription (transactivation of anti-inflammatory proteins and transrepression of pro-inflammatory cytokines).
- Mineralocorticoid Action: Cortisol also binds to mineralocorticoid receptors (MR) in the distal renal tubules → promotes sodium retention and potassium excretion, which is critical for patients with hypoadrenocorticism.
安全性與警告
禁忌症
- Hypersensitivity to cortisone acetate
- Systemic fungal infections (general corticosteroid contraindication)
不良反應
- Vomiting
- Inappetence
- Diarrhea
- Hypersensitivity reactions (rare)
- Polyuria/Polydipsia/Polyphagia (at supra-physiologic doses)
- Panting (at supra-physiologic doses)
- Immunosuppression (at supra-physiologic doses)
注意事項
Laboratory Interference: Cortisone cross-reacts with cortisol in the ACTH stimulation test. Baseline testing must be performed before administering cortisone (Note: Dexamethasone does not cross-react).
- Pregnancy: FDA Category C. Excessive dosages early in pregnancy may lead to teratogenic effects. Glucocorticoids are necessary for normal fetal development, but high doses should be avoided.
- Nursing: Unbound glucocorticoids enter milk. High doses or prolonged use may inhibit the growth of nursing newborns.
- Supra-physiologic Doses: If used at higher than physiologic replacement doses, standard corticosteroid precautions apply (risk of iatrogenic Cushing's, immunosuppression, GI ulceration).
藥物交互作用
Concomitant use may cause hypokalemia; risk of CHF and cardiac enlargement reported in humans.
Glucocorticoids may reduce salicylate blood levels and increase risk for GI ulceration/bleeding.
Concomitant administration may cause hypokalemia.
May potentiate the effects of hydrocortisone/glucocorticoids.
Insulin requirements may increase due to glucocorticoid-induced insulin resistance.
May alter steroid metabolism; higher doses of steroids may be needed to treat mitotane-induced adrenal insufficiency.
Increased risk of gastrointestinal ulceration and bleeding.
Virus replication may be augmented if given at immunosuppressive doses; diminished immune response to killed vaccines/toxoids.
May affect INR values; requires monitoring.
監測
- Weight, appetite, signs of edema
- Serum and/or urine electrolytes (Na+, K+)
- Total plasma proteins, albumin
- Blood glucose
- Growth and development in young animals
- ACTH stimulation test (Note: Cortisone cross-reacts with cortisol assays; must test before administration)
藥物動力學
吸收
Absorbed orally. Oral bioavailability in humans ranges widely but is approximately 50%.
分佈
Unbound glucocorticoids enter milk. Distributes widely to tissues.
代謝
Rapidly converted to the active hormone cortisol in vivo.
排除
Excreted primarily via the kidneys after hepatic metabolism.
過量
Acute ingestion is rarely a clinical problem, and severe clinical effects are unlikely with a single acute overdose. However, neuropsychiatric effects can occur. Cardiac arrhythmias and anaphylaxis are theoretically possible but very rare. Treatment is generally supportive.
可用產品
劑型
- Oral Tablets
人用標示
- Cortisone Acetate Oral Tablets: 25 mg
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
Store tablets in well-closed containers at a temperature less than 40°C, preferably at room temperature (15-30°C).
飼主須知
- 嚴格遵從醫囑：務必完全按照處方給藥。切勿突然停藥，因為這可能引發危及生命的艾迪森氏症危機。
- 副作用：觀察是否有腸胃不適的跡象（嘔吐、腹瀉、食慾不振）。如果您的寵物接受較高劑量，您可能會注意到口渴、排尿和食慾增加，以及喘息。
- 獸醫回診：按時進行所有預定的血液檢查（電解質），以確保劑量符合您寵物的需求。
- 壓力事件：如果您的寵物面臨壓力事件（手術、寄宿、生病），請聯繫您的獸醫，因為可能需要暫時增加劑量。
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