ଟାକ୍ରୋଲିମସ

ଟାକ୍ରୋଲିମସ
Clinical data
Trade names	Prograf, Advagraf, Protopic, others
Synonyms	FK-506, fujimycin
AHFS/Drugs.com	monograph
MedlinePlus	a601117
data	EU EMA: yes; US DailyMed: Tacrolimus;
Pregnancy; category	AU: C ;
Routes of; administration	Topical, by mouth, intravenous
ATC code	D11AH01 (WHO) ; L04AD02;
Legal status
Legal status	US: ℞-only ; EU: Rx-only ; ℞ (Prescription only);
Pharmacokinetic data
Bioavailability	24% (5–67%), less after eating food rich in fat
Protein binding	≥98.8%
Metabolism	Liver CYP3A4, CYP3A5
Elimination half-life	11.3 h for transplant patients (range 3.5–40.6 h)
Excretion	Mostly fecal
Identifiers
	IUPAC name (−)-(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 Number	104987-11-3 ;
PubChem CID	445643;
DrugBank	DB00864 ;
ChemSpider	393220 ;
UNII	Y5L2157C4J;
KEGG	D00107 ; C01375 ;
ChEBI	CHEBI:61049;
ChEMBL	CHEMBL269732 ;
PDB ligand	FK5 (PDBe, RCSB PDB);
ECHA InfoCard	100.155.367
Chemical and physical data
Formula	C44H69NO12
Molar mass	୮୦୪.୦୩ g·mol−1
3D model (JSmol)	Interactive image;
	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 ;
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ଟାକ୍ରୋଲିମସ ଏକ ପ୍ରକାର ଔଷଧ ଯାହା ଅଙ୍ଗ ପ୍ରତିରୋପଣ ପରେ ହେଉଥିବା ପ୍ରତ୍ୟାଖ୍ୟାନ ରୋକିବା ପାଇଁ ପାଟିରେ କିମ୍ବା ଇଞ୍ଜେକ୍ସନ୍ଦ୍ୱାରା ଦିଆଯାଏ |^[୫] ^[୬] ଔଷଧର ସ୍ତର ନିୟମିତ ଭାବେ ତଦାରଖ କରାଯିବା ଉଚିତ୍ | ^[୭] ମଧ୍ୟମରୁ ଗମ୍ଭୀର ଧରଣରୁ ଏକଜିମା କିମ୍ବା ସୋରିୟାସିସ ପାଇଁ ଏହା କ୍ରିମ ଭାବରେ ବ୍ୟବହୃତ ହୁଏ ଯେତେବେଳେ ଅନ୍ୟ ଚିକିତ୍ସା ପର୍ଯ୍ୟାପ୍ତ ନୁହେଁ | ^[୮] ^[୯]

ପାଟି କିମ୍ବା ଇଞ୍ଜେକ୍ସନ‌ଦ୍ୱାରା ନେଉଥିବା ଔଷଧର ସାଧାରଣ ପାର୍ଶ୍ୱ ପ୍ରତିକ୍ରିୟାରେ ବୃକ୍‌କ ସମସ୍ୟା, ତରଳ ଝାଡ଼ା, ବାନ୍ତି, ଉଚ୍ଚ ରକ୍ତ ପୋଟାସିୟମ୍ ଏବଂ ସଂକ୍ରମଣ ଅନ୍ତର୍ଭୁକ୍ତ | ^[୬] ଅନ୍ୟାନ୍ୟ ପାର୍ଶ୍ୱ ପ୍ରତିକ୍ରିୟାରେ ଉଚ୍ଚ ରକ୍ତ ଶର୍କରା, ସ୍ନାୟୁଗତ ସମସ୍ୟା, ଲିମ୍ଫୋମା ଏବଂ ଆନାଫାଇଲକ୍‌ସିସ ଅନ୍ତର୍ଭୁକ୍ତ ହୋଇପାରେ |^[୬] କ୍ରିମ୍ ଭାବରେ ବ୍ୟବହୃତ ହେଲେ ସାଧାରଣ ପାର୍ଶ୍ୱ ପ୍ରତିକ୍ରିୟାରେ ଗଲୁ, ମୁଣ୍ଡବିନ୍ଧା ଏବଂ ଲାଲ ଚର୍ମ ଅନ୍ତର୍ଭୁକ୍ତ | ^[୯] ଗର୍ଭାବସ୍ଥାରେ କ୍ରିମ୍ ସୁରକ୍ଷିତ କି ନାହିଁ ତାହା ଅସ୍ପଷ୍ଟ ରହିଛି। ^[୧୦] ଟାକ୍ରୋଲିମସ ହେଉଛି ଏକ କ୍ୟାଲସିନ୍ୟୁରିନ ଇନହିବିଟର | ^[୫]ଟି ଜୀବକୋଷଗୁଡ଼ିକର କାର୍ଯ୍ୟକଳାପ ହ୍ରାସ କରି ଏହା କାର୍ଯ୍ୟ କରେ ବୋଲି ବିଶ୍ୱାସ କରାଯାଏ | ^[୭]

୧୯୮୭ ମସିହାରେ ଟାକ୍ରୋଲିମସ୍ ଆବିଷ୍କୃତ ହୋଇଥିଲା ଏବଂ ୧୯୯୪ ମସିହାରେ ଯୁକ୍ତରାଷ୍ଟ୍ରରେ ଚିକିତ୍ସା ପାଇଁ ଅନୁମୋଦିତ ହୋଇଥିଲା। ^[୬] ଏହା ଏକ ସାଧାରଣ ଔଷଧ ଭାବରେ ଉପଲବ୍ଧ | ^[୧୧] ଯୁକ୍ତରାଜ୍ୟରେ ୫ ମିଗ୍ରାର ୫୦ଟି ଟାବଲେଟ ପାଇଁ ଏନଏଚଏସକୁ ୨୦୨୦ ମସିହାରେ ପ୍ରାୟ 206 ପାଉଣ୍ଡ ଖର୍ଚ୍ଚ କରିଥାଏ |^[୫] ଯୁକ୍ତରାଷ୍ଟ୍ରରେ ଏହାର 0.୧%ର ମୂଲ୍ୟ ୩୬ ଡଲାର ଥିଲା । ^[୧୨] ^[୧୩] ଏହା ପ୍ରଥମେ ଜାପାନର ଏକ ମୃତ୍ତିକା ନମୁନାରୁ ତିଆରି ହୋଇଥିଲା ଯେଉଁଥିରେ ସ୍ଟ୍ରେପ୍ଟୋମାଇସେସ ସୁକୁବେନସିସଜୀବାଣୁ ରହିଥିଲା | ^[୧୪]

ଆଧାର

↑ "Tacrolimus Use During Pregnancy". Drugs.com. 3 October 2019. Retrieved 29 April 2020.
↑ "Prograf- tacrolimus capsule, gelatin coated Prograf- tacrolimus injection, solution Prograf- tacrolimus granule, for suspension". DailyMed. Retrieved 16 July 2021.
↑ "Advagraf EPAR". European Medicines Agency. Retrieved 16 July 2021.
↑ "Protopic EPAR". European Medicines Agency. Retrieved 16 July 2021.
1 2 3 BNF 79 : March 2020. London: Royal Pharmaceutical Society. 2020. p. 868. ISBN 9780857113658.
1 2 3 4 "Tacrolimus Monograph for Professionals". Drugs.com (in ଇଂରାଜୀ). Retrieved 12 October 2020.
1 2 "Tacrolimus Monograph for Professionals". Drugs.com (in ଇଂରାଜୀ). Retrieved 12 October 2020.
↑ BNF 79 : March 2020. London: Royal Pharmaceutical Society. 2020. p. 868. ISBN 9780857113658.
1 2 "Tacrolimus topical Monograph for Professionals". Drugs.com (in ଇଂରାଜୀ). Retrieved 12 October 2020.
↑ "Tacrolimus topical (Protopic) Use During Pregnancy". Drugs.com (in ଇଂରାଜୀ). Retrieved 12 October 2020.
↑ "Tacrolimus Prices, Coupons & Savings Tips". GoodRx (in ଆମେରିକୀୟ ଇଂରାଜୀ). Retrieved 12 October 2020.
↑ "Tacrolimus Prices, Coupons & Savings Tips". GoodRx (in ଆମେରିକୀୟ ଇଂରାଜୀ). Retrieved 12 October 2020.
↑ "Tacrolimus Prices and Tacrolimus Coupons". GoodRx (in ଆମେରିକୀୟ ଇଂରାଜୀ). Retrieved 12 October 2020.
↑ Chakravarty, Dilip; Chakravarty, Dilip K.; Lee, W. C. (2010). Liver Transplantation (in ଇଂରାଜୀ). Boydell & Brewer Ltd. p. 169. ISBN 978-81-8448-770-1.

[Drugs.com_pregnancy-1] "Tacrolimus Use During Pregnancy". Drugs.com. 3 October 2019. Retrieved 29 April 2020.

[Prograf_FDA_label-2] "Prograf- tacrolimus capsule, gelatin coated Prograf- tacrolimus injection, solution Prograf- tacrolimus granule, for suspension". DailyMed. Retrieved 16 July 2021.

[3] "Advagraf EPAR". European Medicines Agency. Retrieved 16 July 2021.

[4] "Protopic EPAR". European Medicines Agency. Retrieved 16 July 2021.

[BNF79-5] 1 2 3 BNF 79 : March 2020. London: Royal Pharmaceutical Society. 2020. p. 868. ISBN 9780857113658.

[AHFS2020Oral-6] 1 2 3 4 "Tacrolimus Monograph for Professionals". Drugs.com (in ଇଂରାଜୀ). Retrieved 12 October 2020.

[autogen4-7] 1 2 "Tacrolimus Monograph for Professionals". Drugs.com (in ଇଂରାଜୀ). Retrieved 12 October 2020.

[autogen3-8] BNF 79 : March 2020. London: Royal Pharmaceutical Society. 2020. p. 868. ISBN 9780857113658.

[AHFS2020Top-9] 1 2 "Tacrolimus topical Monograph for Professionals". Drugs.com (in ଇଂରାଜୀ). Retrieved 12 October 2020.

[Preg2020Top-10] "Tacrolimus topical (Protopic) Use During Pregnancy". Drugs.com (in ଇଂରାଜୀ). Retrieved 12 October 2020.

[GX2020Oral-11] "Tacrolimus Prices, Coupons & Savings Tips". GoodRx (in ଆମେରିକୀୟ ଇଂରାଜୀ). Retrieved 12 October 2020.

[autogen2-12] "Tacrolimus Prices, Coupons & Savings Tips". GoodRx (in ଆମେରିକୀୟ ଇଂରାଜୀ). Retrieved 12 October 2020.

[GX2020Top-13] "Tacrolimus Prices and Tacrolimus Coupons". GoodRx (in ଆମେରିକୀୟ ଇଂରାଜୀ). Retrieved 12 October 2020.

[14] Chakravarty, Dilip; Chakravarty, Dilip K.; Lee, W. C. (2010). Liver Transplantation (in ଇଂରାଜୀ). Boydell & Brewer Ltd. p. 169. ISBN 978-81-8448-770-1.

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