麥考酚酸酯
Mycophenolate Mofetil
Mycophenolate mofetil (RS-61443)
別名: CellCept · Cellmune · Imuxgen · Munotras · Mycept · Myfortic · Refrat · RS-61443 · MMF · Mycophenolic acid (active metabolite) · MPA
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 |
|---|---|---|---|---|---|
| Immune-mediated hemolytic anemia (IMHA) | 12-17 mg/kg PO once daily or divided twice daily | PO | q12-24h | — | 🌎 NA |
| IMHA, myasthenia gravis or glomerulonephritis | 12-17 mg/kg PO once daily or divided twice daily | PO | q12-24h | — | 🌎 NA |
| Immune-mediated hemolytic anemia (IMHA) | 400-600 mg/m2 orally twice daily | PO | q12h | — | 🌎 NA |
| Adjunctive treatment of glomerulonephritis | 10-20 mg/kg PO q12h | PO | q12h | 3-4 weeks trial | 🌎 NA |
| Pemphigus foliaceous | 22-39 mg/kg/day divided into 3 daily doses | PO | q8h | — | 🌎 NA |
| Pemphigus foliaceous | 20-40 mg/kg/day PO divided q8h | PO | q8h | — | 🌎 NA |
| Aplastic anemia | 10 mg/kg PO q12h | PO | q12h | — | 🌎 NA |
| Rescue agent for generalized myasthenia gravis | 500 mg (15-20 mg/kg) diluted and given IV over 2-4 hours | IV | q24h | 13 days | 🌎 NA |
- Immune-mediated hemolytic anemia (IMHA): Given with prednisolone (at 2 mg/kg q12-24h). Dogs also received ranitidine and sucralfate in the study.
- IMHA, myasthenia gravis or glomerulonephritis: Given with prednisone (at 2.2 mg/kg q12-24h).
- Immune-mediated hemolytic anemia (IMHA): Extrapolated from human medicine. Gastrointestinal side effects are common and dose limiting.
- Adjunctive treatment of glomerulonephritis: Trial of single drug therapy for 3-4 weeks recommended.
- Pemphigus foliaceous: Success rates of approx 50%; most dogs require glucocorticoids to control signs.
- Pemphigus foliaceous: Steroid-sparing only.
- Aplastic anemia: First effects observed 2 weeks later; complete remission in approx 3 weeks.
- Rescue agent for generalized myasthenia gravis: Given daily IV until swallowing oral meds, then switched to 10-11 mg/kg PO q12h.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| IMHA | 10 mg/kg PO q12h | PO | q12h | — | 🌎 NA |
- IMHA: Use with caution due to feline glucuronidation deficiency.
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
麥考酚酸酯 (Mycophenolate mofetil, MMF) 是一種強效的免疫抑制劑，在獸醫學中越來越常被用作類固醇替代藥物，或用於治療嚴重、難治性免疫介導疾病的救援療法。
主要臨床應用包括：
- 免疫介導性溶血性貧血 (IMHA)
- 腎小球腎炎
- 重症肌無力
- 落葉型天皰瘡
- 器官移植抗排斥方案
雖然曾被建議用於炎症性腸病 (IBD)，但由於該藥物在犬隻的主要副作用為胃腸道症狀（胃炎、腹瀉和腸道發炎），因此使用上較為複雜。臨床要點： 在某些危重病例中，由於 MMF 作用相對迅速，常被優先於硫唑嘌呤 (azathioprine) 使用，但其高昂的成本和嚴重的胃腸道副作用可能成為限制因素。在貓的臨床經驗非常有限，且因貓缺乏葡萄糖醛酸結合代謝途徑，必須極度謹慎使用。
作用機制
Mycophenolate mofetil (MMF) is a prodrug that is rapidly hydrolyzed in vivo to its active form, mycophenolic acid (MPA).
- MPA non-competitively and reversibly inhibits inosine monophosphate dehydrogenase (IMPDH).
- IMPDH is the rate-limiting enzyme in the de novo synthesis of guanosine nucleotides.
- Because T-lymphocytes and B-lymphocytes are highly dependent on this de novo purine synthesis pathway (and lack the purine salvage pathways utilized by other cell types), MPA selectively inhibits their proliferative responses.
- This leads to → suppression of B-cell antibody formation and → inhibition of leukocyte recruitment to inflammatory sites and allotransplant tissues.
安全性與警告
禁忌症
- Documented hypersensitivity to mycophenolate
- Pregnancy (teratogenic effects noted in animal models)
- Caution in patients with severe renal dysfunction (dosage adjustment may be required)
- Caution in cats (deficient in glucuronidation metabolism)
- Pre-existing bone marrow suppression
- Pre-existing infections
不良反應
- Diarrhea (can be severe)
- Vomiting
- Anorexia
- Lethargy / reduced activity
- Weight loss
- Lymphopenia
- Increased rates of dermal infections
- Increased susceptibility to systemic infections
- Potential increased risk of malignancy/lymphoma
- Bone marrow suppression
- Nausea
- Diarrhoea
- Increased incidence of infections (e.g., pyoderma, Malassezia)
- Increased risk of lymphoma (reported in humans)
- Headache (reported in humans)
- Hypertension (reported in humans)
- Peripheral oedema (reported in humans)
- Confusion (reported in humans)
- Coughs (reported in humans)
- Tremors (reported in humans)
注意事項
Black Box Warning: In humans, mycophenolate carries a warning regarding a potential increased risk for lymphoma and susceptibility to infections associated with its use.
- Intravenous Administration: Must be administered over at least two hours. Do NOT give as an IV bolus or via rapid IV infusion.
- Feline Patients: The active metabolite (MPA) is primarily excreted as a glucuronide metabolite. Cats are deficient in this metabolic process; use with extreme caution.
- Pregnancy: Teratogenic (increased resorptions and malformations). Avoid use during pregnancy.
- Handling: Due to teratogenic risks, tablets or capsules should not be crushed, split, or opened. Personnel and owners should wear gloves when handling.
藥物相互作用
Increased serum concentrations of acyclovir and the phenolic glucuronide of mycophenolic acid
Decreased absorption of mycophenolate; separate dosing by at least 2 hours
Potentially increased concentrations of free mycophenolic acid
Increased risk for bone marrow suppression; use together not recommended in humans
Decreased absorption of mycophenolate; separate dosing by at least 2 hours
Potentially increased serum levels of mycophenolic acid and the phenolic glucuronide of mycophenolic acid
May be less effective; avoid use
Competes for secretion, resulting in increased concentrations of either drug
Concomitant administration may decrease the absorption of mycophenolate
監測
- Clinical efficacy (resolution of immune-mediated disease signs)
- Complete Blood Count (CBC) for bone marrow suppression
- Renal and hepatic function panels
- Serum electrolytes
- Gastrointestinal effects (monitor weight, appetite, and client reports of vomiting/diarrhea)
- Complete Blood Count (CBC) to monitor for bone marrow suppression
- Gastrointestinal signs (nausea, vomiting, diarrhea)
- Signs of secondary infections (e.g., skin lesions, lethargy, fever)
藥物動力學
半衰期
吸收
Absorbed orally but with wide inter-patient and inter-dose variation. Bioavailability in dogs ranges from 54-87%. In humans, oral bioavailability averages 94%, but food reduces peak levels of MPA by up to 40%.
分佈
Volume of distribution at steady-state in dogs is approximately 5 L/kg, with wide inter-patient variability (±4.5).
代謝
Rapidly hydrolyzed in vivo to the active form, mycophenolic acid (MPA). MPA is primarily metabolized via glucuronidation (cats are deficient in this pathway).
排除
Primarily excreted in the urine, both unchanged (approx. 5%) and as the glucuronide metabolite (approx. 90%).
過量
In oral acute studies performed in mice and monkeys, no deaths occurred in dosages up to 4,000 mg/kg and 1,000 mg/kg, respectively. In small animals, acute gastrointestinal disturbances (severe vomiting, diarrhea) could be expected. Treatment should be symptomatic and supportive.
可用產品
劑型
- Oral capsules
- Oral tablets
- Lyophilized powder for injection
- 250 mg capsule
- 500 mg tablet
- 1 g/5 ml powder for oral suspension
- 180 mg tablet
- 360 mg tablet
- 500 mg powder for reconstitution and slow i.v. infusion
人用標示
- Mycophenolate Mofetil Oral Capsules: 250 mg (CellCept®)
- Mycophenolate Mofetil Oral Tablets: 500 mg (CellCept®)
- Mycophenolate Mofetil Powder for Oral Suspension: 200 mg/mL (reconstituted) (CellCept®)
- Mycophenolate Mofetil Lyophilized Powder for Injection: 500 mg in 20 mL vials (CellCept®)
- CellCept (250 mg capsule, 500 mg tablet, 1 g/5 ml oral suspension)
- Myfortic (180 mg, 360 mg tablets)
- 500 mg powder for injection
各地核准狀態
Human-approved product used off-label in veterinary medicine under the cascade. POM status.
Human-approved product used off-label in veterinary medicine under the cascade. POM status.
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Tablets and capsules: Store between 15-30°C and protect from light. Oral suspension: Store powder between 15-30°C. Once reconstituted, store at room temperature or refrigerate (do not freeze); discard unused portion after 60 days. Injectable: Store between 15-30°C. Reconstitute with 5% dextrose. Do not mix with other medications. Administer within 6 hours of dilution.
飼主須知
- 給藥方式： 建議空腹給藥。但如果出現嘔吐或食慾不振，可以嘗試與食物一起餵食以觀察是否改善。
- 處理注意事項： 由於此藥物可能導致出生缺陷，請勿壓碎、剝半或打開膠囊/錠劑。孕婦應避免接觸此藥物。給藥後請徹底洗手。
- 副作用： 腸胃不適是最常見的副作用。如果腹瀉持續、變得嚴重，或您的寵物停止進食，請立即聯繫您的獸醫師。
- 感染風險： 此藥物會抑制免疫系統。請讓您的寵物遠離生病的動物，若發現感染跡象（如嗜睡、發燒、新的皮膚病灶），請通知您的獸醫師。
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