シクロスポリン
Cyclosporine
Cyclosporin A
別名: Optimmune · Restasis · Atopica · Cyclavance · Modulis · Sporimmune · Cyclosporin A · Ciclosporin · Cyclosporine
VetSheet 獣医チームが監修更新日 2026年4月5日エビデンスに基づく獣医学リファレンス
監査済み v13 用量エビデンス
構造化された用量計算エビデンスAllergic dermatitis (extra-label)
認証済み獣医師の確認が必要
- q24-48h
NA
必ず考慮する臨床コンテキスト (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.
用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。
概要
シクロスポリンは、真菌から分離された高脂溶性のポリペプチド薬です。獣医眼科において、犬の乾性角結膜炎（KCS、ドライアイ）および慢性表層角膜炎（パンヌス）の治療における第一選択薬です。
涙液分泌を刺激するだけでなく、慢性炎症に伴う角膜の色素沈着や肉芽形成を軽減します。長期の局所投与でも全身性の免疫抑制の副作用を引き起こすことなく、一般的に安全に使用できます。
作用機序
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・警告
禁忌
- Feline keratoconjunctivitis sicca associated with active herpes virus infection
- Feline eosinophilic keratitis (historically, though newer evidence varies, the monograph notes it is not promising)
有害事象
- 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.
医薬品相互作用
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.
監視
- Schirmer Tear Test (STT) after 1 month of therapy, then periodically
- Fluorescein staining to monitor for corneal ulceration
- Resolution of corneal pigmentation and neovascularization
薬物動態
半減期
吸収
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.
分布
Concentrates locally in the cornea, conjunctiva, and lacrimal glands.
代謝
Hepatic (Cytochrome P450 3A4) if absorbed systemically.
消失
Primarily biliary/fecal if absorbed systemically.
過剰投与
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.
製品
製剤
- 0.2% ophthalmic ointment
- 0.05% ophthalmic emulsion
- 1% ophthalmic solution (compounded)
動物用医薬品
- Cyclosporine Ophthalmic Ointment 0.2% (Optimmune)
ヒト用医薬品
- Cyclosporine 0.05% Ophthalmic Emulsion (Restasis)
規制ステータス
POM-V classification
POM-V classification
規制データなし: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
保管・安定性
Store at room temperature away from moisture and heat. Keep the tube tightly closed.
飼主向け情報
ペットのドライアイの管理
- 忍耐が鍵です： 涙の量が劇的に改善するまでには、継続して3〜8週間使用する必要があります。途中で薬をやめないでください！
- 生涯にわたる治療： ドライアイ（KCS）は通常、生涯付き合っていく病気です。軟膏の塗布をやめると、数日以内に症状が再発する可能性が高いです。
- 使用方法： 少量の軟膏（約6mm）を直接目に塗布します。人工涙液も使用している場合は、先に人工涙液を点眼し、5〜10分待ってからシクロスポリン軟膏を塗布してください。
- 安全性： この薬は目に非常に安全であり、ステロイドのような全身性の副作用を引き起こすことはありません。
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