使用者:Gavin730/他克莫司

Gavin730/他克莫司
臨床資料
商品名（英語：Drug nomenclature）	Prograf, Advagraf, Protopic, others
其他名稱	FK-506, fujimycin
AHFS/Drugs.com	Monograph
MedlinePlus	a601117
核准狀況	歐 EMA: yes; 美 DailyMed: Tacrolimus;
懷孕分級	澳: C ; ;
給藥途徑	Topical, by mouth, intravenous (IV)
ATC碼	D11AH01 (WHO) ; L04AD02;
法律規範狀態
法律規範	美：處方藥（℞-only）; 處方藥（℞-only）;
藥物動力學數據
生物利用度	24% (5–67%), less after eating food rich in fat
血漿蛋白結合率	≥98.8%
藥物代謝	Hepatic CYP3A4, CYP3A5
生物半衰期	11.3 h for transplant patients (range 3.5–40.6 h)
排泄途徑	Mostly faecal
識別資訊
	IUPAC命名法 (−)-(3S,4R,5S,8R,9E,12S,14S,15R,16S,18R,26aS)-8-allyl-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-5,19-dihydroxy-3-{(E)-2-[(1R,3R,4R)-4-hydroxy-3-methylcyclohexyl]-1-methylvinyl}-14,16-dimethoxy-4,10,12,18-tetramethyl-15,19-epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclotricosane-1,7,20,21(4H,23H)-tetrone; ;
CAS號	104987-11-3
PubChem CID	445643;
DrugBank	DB00864 ;
ChemSpider	393220 ;
UNII	Y5L2157C4J;
KEGG	D00107 ; C01375 ;
ChEBI	CHEBI:61049;
ChEMBL	ChEMBL269732 ;
PDB配體ID	FK5 (PDBe, RCSB PDB);
化學資訊
化學式	C44H69NO12
摩爾質量	804.018
3D模型（JSmol（英語：JSmol））	交互式圖像;
	SMILES O=C3C(=O)N1CCCC[C@H]1C(=O)O[C@H](C(=C/[C@@H]2CC[C@@H](O)[C@H](OC)C2)/C)[C@H](C)[C@@H](O)CC(=O)[C@@H](/C=C(/C[C@@H](C[C@H](OC)[C@H]4O[C@]3(O)[C@H](C)C[C@@H]4OC)C)C)C\C=C;
	InChI InChI=1S/C44H69NO12/c1-10-13-31-19-25(2)18-26(3)20-37(54-8)40-38(55-9)22-28(5)44(52,57-40)41(49)42(50)45-17-12-11-14-32(45)43(51)56-39(29(6)34(47)24-35(31)48)27(4)21-30-15-16-33(46)36(23-30)53-7/h10,19,21,26,28-34,36-40,46-47,52H,1,11-18,20,22-24H2,2-9H3/b25-19+,27-21+/t26-,28+,29+,30-,31+,32-,33+,34-,36+,37-,38-,39+,40+,44+/m0/s1 ; Key:QJJXYPPXXYFBGM-LFZNUXCKSA-N ;

他克莫司是一種免疫抑制劑。它被用於降低器官移植後的排斥風險, 也可以被用作外用藥物來治療T細胞介導免疫產生的疾病，例如異位性皮膚炎和牛皮蘚. 它還可以用於治療骨髓移植後的虹彩炎、微小病變的惡化、木村氏症、白癜風和貓狗的乾眼症。^[2]^[3]

他克莫司可抑制鈣調磷酸酶, 從而影響白血球介素-2的產生。這種白血球介素是獲得性免疫系統中的一部分，可以促進T細胞的發育和增殖。

它是一種在1987年於一份來自日本的含有的土壤樣本中被首次發現的大環內酯^[4]。

醫療用途

器官移植

他克莫司具有和環孢素相似的免疫抑制性，但效果遠強於環孢素. 在一項研究中他克莫司與環孢素相比可以顯著降低發生急性排斥反應的概率(30.7%vs46.4%)。^[5]在肝移植的第一年中他克莫司的療效也優於環孢素。^[6]^[7]長期療效則不及環孢素。他克莫司通常作為器官移植後藥物的一種，另外還有皮質類固醇, 霉酚酸和如 [[en:basiliximab|巴利昔單抗]的白血球介素-2受體抑制劑]. Dosages are titrated to target blood levels.

潰瘍性結腸炎

近幾年他克莫司已被用於抑制潰瘍性結腸炎。儘管現在它幾乎盡在試驗中使用，但已經顯示出很好的療效。^[8]^[9]

皮炎

他克莫司可作為軟膏來治療皮膚炎特別是特異性皮炎, . 它以和類固醇相似的方式抑制炎症，效果和中效類固醇相似。他克莫司與類固醇相比具有不會引起萎縮和類固醇的其他副作用^[10]

狼瘡性腎炎

與其他藥物相比他克莫司可以降低狼瘡性腎炎嚴重感染的風險。^[11]

^ ^1.0 ^1.1 Tacrolimus Use During Pregnancy. Drugs.com. 3 October 2019 [29 April 2020].
^ Berdoulay A, English RV, Nadelstein B. Effect of topical 0.02% tacrolimus aqueous suspension on tear production in dogs with keratoconjunctivitis sicca. Veterinary Ophthalmology. 2005, 8 (4): 225–32. PMID 16008701. doi:10.1111/j.1463-5224.2005.00390.x.
^ Tacrolimus for Dogs and Cats.
^ Baldo A, Cafiero M, Di Caterino P, Di Costanzo L. Tacrolimus ointment in the management of atopic dermatitis. Clin Cosmet Investig Dermatol. January 2009, 2: 1–7. PMC 3047924 . PMID 21436963. doi:10.2147/ccid.s3378.
^ McCauley, Jerry. Long-Term Graft Survival In Kidney Transplant Recipients. Slide Set Series on Analyses of Immunosuppressive Therapies. Medscape. 2004-05-19 [2006-06-06].
^ Haddad EM, McAlister VC, Renouf E, Malthaner R, Kjaer MS, Gluud LL. McAlister V , 編. Cyclosporin versus tacrolimus for liver transplanted patients. The Cochrane Database of Systematic Reviews. October 2006, 4 (4): CD005161. PMID 17054241. doi:10.1002/14651858.CD005161.pub2.
^ O'Grady JG, Burroughs A, Hardy P, Elbourne D, Truesdale A. Tacrolimus versus microemulsified ciclosporin in liver transplantation: the TMC randomised controlled trial. Lancet. October 2002, 360 (9340): 1119–25. PMID 12387959. doi:10.1016/S0140-6736(02)11196-2.
^ Baumgart DC, Pintoffl JP, Sturm A, Wiedenmann B, Dignass AU. Tacrolimus is safe and effective in patients with severe steroid-refractory or steroid-dependent inflammatory bowel disease--a long-term follow-up. The American Journal of Gastroenterology. May 2006, 101 (5): 1048–56. PMID 16573777.
^ Baumgart DC, Macdonald JK, Feagan B. Baumgart DC , 編. Tacrolimus (FK506) for induction of remission in refractory ulcerative colitis. The Cochrane Database of Systematic Reviews. July 2008, 16 (3): CD007216. PMID 18646177. doi:10.1002/14651858.CD007216.
^ 引用錯誤：沒有為名為AC-Protopic的參考文獻提供內容
^ Singh JA, Hossain A, Kotb A, Wells G. Risk of serious infections with immunosuppressive drugs and glucocorticoids for lupus nephritis: a systematic review and network meta-analysis. BMC Medicine. September 2016, 14 (1): 137. PMC 5022202 . PMID 27623861. doi:10.1186/s12916-016-0673-8.

[Drugs.com_pregnancy-1] 1.0 ^1.1 Tacrolimus Use During Pregnancy. Drugs.com. 3 October 2019 [29 April 2020].

[2] Berdoulay A, English RV, Nadelstein B. Effect of topical 0.02% tacrolimus aqueous suspension on tear production in dogs with keratoconjunctivitis sicca. Veterinary Ophthalmology. 2005, 8 (4): 225–32. PMID 16008701. doi:10.1111/j.1463-5224.2005.00390.x.

[3] Tacrolimus for Dogs and Cats.

[4] Baldo A, Cafiero M, Di Caterino P, Di Costanzo L. Tacrolimus ointment in the management of atopic dermatitis. Clin Cosmet Investig Dermatol. January 2009, 2: 1–7. PMC 3047924 . PMID 21436963. doi:10.2147/ccid.s3378.

[Medscape2004-McCauley-5] McCauley, Jerry. Long-Term Graft Survival In Kidney Transplant Recipients. Slide Set Series on Analyses of Immunosuppressive Therapies. Medscape. 2004-05-19 [2006-06-06].

[6] Haddad EM, McAlister VC, Renouf E, Malthaner R, Kjaer MS, Gluud LL. McAlister V , 編. Cyclosporin versus tacrolimus for liver transplanted patients. The Cochrane Database of Systematic Reviews. October 2006, 4 (4): CD005161. PMID 17054241. doi:10.1002/14651858.CD005161.pub2.

[7] O'Grady JG, Burroughs A, Hardy P, Elbourne D, Truesdale A. Tacrolimus versus microemulsified ciclosporin in liver transplantation: the TMC randomised controlled trial. Lancet. October 2002, 360 (9340): 1119–25. PMID 12387959. doi:10.1016/S0140-6736(02)11196-2.

[8] Baumgart DC, Pintoffl JP, Sturm A, Wiedenmann B, Dignass AU. Tacrolimus is safe and effective in patients with severe steroid-refractory or steroid-dependent inflammatory bowel disease--a long-term follow-up. The American Journal of Gastroenterology. May 2006, 101 (5): 1048–56. PMID 16573777.

[9] Baumgart DC, Macdonald JK, Feagan B. Baumgart DC , 編. Tacrolimus (FK506) for induction of remission in refractory ulcerative colitis. The Cochrane Database of Systematic Reviews. July 2008, 16 (3): CD007216. PMID 18646177. doi:10.1002/14651858.CD007216.

[AC-Protopic-10] 引用錯誤：沒有為名為AC-Protopic的參考文獻提供內容

[11] Singh JA, Hossain A, Kotb A, Wells G. Risk of serious infections with immunosuppressive drugs and glucocorticoids for lupus nephritis: a systematic review and network meta-analysis. BMC Medicine. September 2016, 14 (1): 137. PMC 5022202 . PMID 27623861. doi:10.1186/s12916-016-0673-8.

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