他克莫司
免疫抑制劑(鈣調磷酸酶抑制劑)
他克莫司(FK 506)是一種強效的巨環類免疫抑制劑。在獸醫學中,主要用於局部治療免疫介導性皮膚病(如肛周瘻管和異位性皮膚炎)以及眼部治療乾眼症(KCS)。由於潛在的毒性,全身性使用較不常見,但可用於嚴重的免疫介導性疾病。 **臨床提示:** 對於環孢素治療無效的乾眼症病例,他克莫司通常有效。
作用機制: Binds to the intracellular protein **FKBP-12** (FK506 binding protein) → forms a complex that inhibits **calcineurin** (a calcium-dependent phosphatase) → prevents dephosphorylation of NF-AT (nuclear factor of activated T-cells) → inhibits transcription of **IL-2** and other cytokines → profound **T-lymphocyte inhibition**.
給藥途徑
TopicalOphthalmicPO
禁忌症
- Hypersensitivity to macrolides
- Active systemic infections
- Malignancy (for systemic use)
不良反應
- Topical: local irritation, erythema, pruritus
- Ophthalmic: mild ocular irritation
- Systemic: GI upset (vomiting, diarrhea), nephrotoxicity, neurotoxicity, secondary infections
藥物相互作用
- Ketoconazole · Inhibits CYP3A metabolism, significantly increasing systemic tacrolimus levels · major
- Erythromycin · Inhibits metabolism, increasing tacrolimus levels · major
- Grapefruit juice · Increases systemic absorption and blood levels of tacrolimus · moderate
監測
- Tear production (Schirmer Tear Test) for KCS
- Resolution of skin lesions
- Whole blood trough levels (if used orally)
- Renal and hepatic function (if used orally)
過量
Systemic overdose can lead to severe nephrotoxicity, neurotoxicity (tremors, seizures), and profound immunosuppression. Treatment is supportive and symptomatic. No specific antidote exists.
VetSheet 藥物參考供持牌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方最新藥品說明書。