環孢素
Cyclosporine
Cyclosporin A
別名: Optimmune · Restasis · Atopica · Cyclavance · Modulis · Sporimmune · Cyclosporin A · Ciclosporin · Cyclosporine
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
經審核的 v13 劑量證據
結構化劑量計算證據Allergic dermatitis (extra-label)
須由已驗證獸醫確認
- q24-48h
NA
必須一併考量的臨床脈絡 (3)
- NOTE: Dosages are for cyclosporine (modified), Atopica®, Cyclavance®, Neoral®, or equivalent; these dosages are not interchangeable with Sandimmune® (or equivalent) dosages.
- ■ Consider therapeutic drug monitoring (pharmacokinetic and pharmacodynamic) to assess effectiveness of therapy, particularly when response is poor or when adverse effects occur. Therapeutic drug monitoring can also be considered when changing brands or manufacturers, especially if response to therapy changes in the individual patient. Cyclosporine blood concentrations are not typically monitored when treating atopic dermatitis 93 or inflammatory bowel disease 9 because the blood concentrations were found to not correlate with clinical efficacy, but this may be warranted in some cases. 50
- ■ This medication is considered to be a hazardous drug as defined by the National Institute for Occupational Safety and Health (NIOSH). Talk with your veterinarian or pharmacist about the use of personal protective equipment when handling this medicine.
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
環孢素是一種高脂溶性的多肽類藥物，最初從真菌中分離。在獸醫眼科中，它是治療犬乾眼症 (KCS) 和慢性表層角膜炎 (Pannus) 的基石療法。
除了刺激淚液分泌外，環孢素還能減少與慢性發炎相關的角膜色素沉著和肉芽組織增生。它在長期局部使用下通常非常安全，不會產生全身性的免疫抑制副作用。
作用機轉
Cyclosporine is a calcineurin inhibitor. It binds to cyclophilin within T-lymphocytes, inhibiting the enzyme calcineurin → prevents dephosphorylation of Nuclear Factor of Activated T-cells (NFAT) → blocks transcription of interleukin-2 (IL-2) and other inflammatory cytokines.
In the eye, this halts local inflammatory mediator production, arresting self-perpetuating lacrimal adenitis. It also acts as a prolactin analog, fitting onto lacrimal prolactin receptors to directly stimulate tear production. Furthermore, it increases conjunctival mucin stores, improving the overall quality of the tear film.
安全性與警告
禁忌症
- Feline keratoconjunctivitis sicca associated with active herpes virus infection
- Feline eosinophilic keratitis (historically, though newer evidence varies, the monograph notes it is not promising)
不良反應
- Mild ocular irritation upon application
- Aggravation of ophthalmic herpes virus infections (especially in cats)
注意事項
Important: Discontinuation of therapy usually results in the return of clinical signs of KCS within a few days.
Use with caution in the face of ulcerative keratitis, although it is generally considered safe when concurrent antibiotic therapy is administered. Compounded formulations should be avoided if an approved commercial product (Optimmune) is available and effective.
藥物交互作用
Inhibits cytochrome P450 metabolism of ciclosporin, increasing blood concentrations up to five-fold. Dose reduction (halving dose or doubling interval) is required.
Inhibits cytochrome P450 metabolism of ciclosporin, significantly increasing blood concentrations.
Competitively inhibits enzymes involved in ciclosporin metabolism, increasing serum levels.
Inhibits enzymes involved in ciclosporin metabolism, increasing serum levels.
Increased risk of nephrotoxicity; concomitant use is not recommended.
Increased risk of nephrotoxicity; concomitant use is not recommended.
Increased risk of nephrotoxicity; concomitant use is not recommended.
Increased risk of nephrotoxicity; concomitant use is not recommended.
Increased risk of hyperkalaemia.
Ciclosporin inhibits MDR1 P-glycoprotein, decreasing the efflux of macrocyclic lactones from the blood-brain barrier, potentially resulting in CNS toxicity.
監測
- Schirmer Tear Test (STT) after 1 month of therapy, then periodically
- Fluorescein staining to monitor for corneal ulceration
- Resolution of corneal pigmentation and neovascularization
藥物動力學
半衰期
吸收
Poor systemic absorption across the GI tract. When delivered topically to the eye, it reaches very low systemic concentrations. Trace levels may be detected in blood but clinical implication is uncertain.
分佈
Concentrates locally in the cornea, conjunctiva, and lacrimal glands.
代謝
Hepatic (Cytochrome P450 3A4) if absorbed systemically.
排除
Primarily biliary/fecal if absorbed systemically.
過量
Systemic toxicity has not been noted in dogs given this drug chronically via the topical ophthalmic route. Even if 100% of the ophthalmic dose were absorbed, it is well below the systemic therapeutic/toxic dose.
可用產品
劑型
- 0.2% ophthalmic ointment
- 0.05% ophthalmic emulsion
- 1% ophthalmic solution (compounded)
獸醫用
- Cyclosporine Ophthalmic Ointment 0.2% (Optimmune)
人用標示
- Cyclosporine 0.05% Ophthalmic Emulsion (Restasis)
各地核准狀態
POM-V classification
POM-V classification
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Store at room temperature away from moisture and heat. Keep the tube tightly closed.
飼主須知
管理寵物的乾眼症
- 耐心是關鍵： 持續使用 3 到 8 週後，淚液分泌才會有顯著改善。請勿提早停藥！
- 終身治療： 乾眼症通常是終身疾病。如果停止點藥，乾眼症狀可能會在幾天內復發。
- 給藥方式： 將少量（約 1/4 英寸）藥膏直接點入眼中。如果同時使用人工淚液，請先點人工淚液，等待 5-10 分鐘後再點環孢素藥膏。
- 安全性： 此藥物對眼睛非常安全，不會引起類固醇常見的全身性副作用。
VetSheet 藥物參考供合格獸醫專業人員作臨床決策輔助之用，不能取代專業判斷或廠商最新仿單。