ସିରୋଲିମସ

ସିରୋଲିମସ
Clinical data
Trade names	Rapamune
Synonyms	Rapamycin
data	EU EMA: yes; US FDA: Sirolimus;
Pregnancy; category	AU: C ; US: C (Risk not ruled out) ; ;
Routes of; administration	By mouth
Legal status
Legal status	US: ℞-only ;
Pharmacokinetic data
Bioavailability	14% (oral solution), lower with high-fat meals; 18% (tablet), higher with high-fat meals
Protein binding	92%
Metabolism	Hepatic
Elimination half-life	57–63 hours
Excretion	Mostly faecal
Identifiers
	IUPAC name (1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,26E,28E,; 30S,32S,35R)-1,18-dihydroxy-12-{(2R)-1-[(1S,3R,; 4R)-4-hydroxy-3-methoxycyclohexyl]-2-propanyl}-; 19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-; 11,36-dioxa-4-azatricyclo[30.3.1.0~4,9~]hexatria; conta-16,24,26,28-tetraene-2,3,10,14,20-pentone;
ECHA InfoCard	100.107.147
Chemical and physical data
Formula	C51H79NO13
Molar mass	୯୧୪.୧୯ g·mol−1
3D model (JSmol)	Interactive image;
Solubility in water	0.0026 mg/mL (20 °C)
	SMILES O[C@@H]1CC[C@H](C[C@H]1OC)C[C@@H](C)[C@@H]4CC(=O)[C@H](C)/C=C(\C)[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)\C=C\C=C\C=C(/C)[C@@H](OC)C[C@@H]2CC[C@@H](C)[C@@](O)(O2)C(=O)C(=O)N3CCCC[C@H]3C(=O)O4;
	InChI InChI=1S/C51H79NO13/c1-30-16-12-11-13-17-31(2)42(61-8)28-38-21-19-36(7)51(60,65-38)48(57)49(58)52-23-15-14-18-39(52)50(59)64-43(33(4)26-37-20-22-40(53)44(27-37)62-9)29-41(54)32(3)25-35(6)46(56)47(63-10)45(55)34(5)24-30/h11-13,16-17,25,30,32-34,36-40,42-44,46-47,53,56,60H,14-15,18-24,26-29H2,1-10H3/b13-11+,16-12+,31-17+,35-25+/t30-,32-,33-,34-,36-,37+,38+,39+,40-,42+,43+,44-,46-,47+,51-/m1/s1 ; Key:QFJCIRLUMZQUOT-HPLJOQBZSA-N ;
(verify)

ସିରୋଲିମସ, ଯାହାକୁ ରାପାମାଇସିନ ମଧ୍ୟ କୁହାଯାଏ, ଔଷଧ ଯାହା ମୁଖ୍ୟତଃ ଅଙ୍ଗ ପ୍ରତିରୋପଣ ପ୍ରତ୍ୟାଖ୍ୟାନ ରୋକିବା ପାଇଁ ଓ ଲୋମ୍ଫଞ୍ଜିଓଲିଓମାୟୋମାଟୋସିସ ରୋଗର ଚିକିତ୍ସା ପାଇଁ ବ୍ୟବହୃତ ହୁଏ ।^[୪] ^[୫] ବୃକ୍‌କ ପ୍ରତିରୋପଣ ପାଇଁ ଏହା ଏକ ଦ୍ୱିତୀୟ ଧାଡିର ଚିକିତ୍ସା ।^[୬] ଏହା ପାଟିରେ ଦିଆଯାଏ ।^[୪]

ସାଧାରଣ ପାର୍ଶ୍ୱ ପ୍ରତିକ୍ରିୟାରେ ସଂକ୍ରମଣ, ଜ୍ୱର, ଖରାପ କ୍ଷତ ଆରୋଗ୍ୟ, ମଧୁମେହ, ମୂତ୍ରରେ ପୁଷ୍ଟିସାର, ରାସ ଏବଂ ଫୁଲା ହୋଇପାରେ ।^[୫] ଅନ୍ୟ ପାର୍ଶ୍ୱ ପ୍ରତିକ୍ରିୟାରେ ଲିମ୍ଫୋମା, ଆନାଫାଇଲକ୍ସିସ୍, ଆଞ୍ଜିଓଇଡିମା, ବୃକ୍‌କ ସମସ୍ୟା, ଏବଂ ପ୍ରଗତିଶୀଳ ମଲ୍ଟିଫୋକାଲ୍ ଲ୍ୟୁକୋଏନସେଫାଲୋପାଥି ଅନ୍ତର୍ଭୁକ୍ତ ହୋଇପାରେ । ^[୪] ଏହା ଏକ ଏମଟଓଆର (mTOR) ପ୍ରତିବନ୍ଧକ ଏବଂଟି ଜୀବକୋଷ ଏବଂ ବି ଜୀବକୋଷଗୁଡ଼ିକର ସକ୍ରିୟତା ହ୍ରାସ କରି କାର୍ଯ୍ୟ କରେ ।^[୪]

୧୯୭୨ ମସିହାରେ ସିରୋଲିମସ ପୃଥକୀକରଣ ହୋଇଥିଲା ଏବଂ ୧୯୯୯ରେ ଯୁକ୍ତରାଷ୍ଟ୍ରରେ ଏବଂ ୨୦୦୧ରେ ୟୁରୋପରେ ଚିକିତ୍ସା ପାଇଁ ଅନୁମୋଦିତ ହୋଇଥିଲା ।^[୪] ^[୭] ^[୫] ଏହା ଏକ ସାଧାରଣ ଔଷଧ ଭାବରେ ଉପଲବ୍ଧ । ଯୁକ୍ତରାଷ୍ଟ୍ରରେ ଏକ ମାସର ଚିକିତ୍ସାରେ ୨୦୨୧ ସୁଦ୍ଧା ଦିନକୁ ୨ମିଗ୍ରାର ମୂଲ୍ୟ ପ୍ରାୟ ୨୨୫ ଡଲାର ଥିଲା ।^[୮] ଯୁକ୍ତରାଜ୍ୟରେ ଏହି ରାଶି ମୂଲ୍ୟ £୧୭୨ ଖର୍ଚ୍ଚ ହୁଏ ।^[୬] ଏହା ରାପାମୁନ ନାମରେ ବିକ୍ରି ହୁଏ ।^[୪]

ଆଧାର

↑ Buck ML (2006). "Immunosuppression With Sirolimus After Solid Organ Transplantation in Children". Pediatric Pharmacotherapy. 12 (2). Archived from the original on 18 April 2020. Retrieved 11 June 2021.
↑ "Rapamycin". PubChem Compound. National Center for Biotechnology Information. Archived from the original on 16 August 2016. Retrieved 1 August 2016.
↑ Simamora P, Alvarez JM, Yalkowsky SH (February 2001). "Solubilization of rapamycin". International Journal of Pharmaceutics. 213 (1–2): 25–9. doi:10.1016/s0378-5173(00)00617-7. PMID 11165091.
↑ ^୪.୦ ^୪.୧ ^୪.୨ ^୪.୩ ^୪.୪ ^୪.୫ "Sirolimus Monograph for Professionals". Drugs.com (in ଇଂରାଜୀ). Archived from the original on 13 August 2020. Retrieved 12 October 2021."Sirolimus Monograph for Professionals". Drugs.com. Archived from the original on 13 August 2020. Retrieved 12 October 2021.
↑ ^୫.୦ ^୫.୧ ^୫.୨ "Rapamune". Archived from the original on 13 August 2021. Retrieved 12 October 2021."Rapamune".
↑ ^୬.୦ ^୬.୧ BNF (80 ed.). BMJ Group and the Pharmaceutical Press. September 2020 – March 2021. p. 886. ISBN 978-0-85711-369-6.{{cite book}}: CS1 maint: date format (link)
↑ Seto B (November 2012). "Rapamycin and mTOR: a serendipitous discovery and implications for breast cancer". Clinical and Translational Medicine. 1 (1): 29. doi:10.1186/2001-1326-1-29. PMC 3561035. PMID 23369283.{{cite journal}}: CS1 maint: unflagged free DOI (link)
↑ "Sirolimus Prices, Coupons & Savings Tips - GoodRx". GoodRx. Retrieved 12 October 2021.

[1] Buck ML (2006). "Immunosuppression With Sirolimus After Solid Organ Transplantation in Children". Pediatric Pharmacotherapy. 12 (2). Archived from the original on 18 April 2020. Retrieved 11 June 2021.

[Pubchem_Rapamycin-2] "Rapamycin". PubChem Compound. National Center for Biotechnology Information. Archived from the original on 16 August 2016. Retrieved 1 August 2016.

[3] Simamora P, Alvarez JM, Yalkowsky SH (February 2001). "Solubilization of rapamycin". International Journal of Pharmaceutics. 213 (1–2): 25–9. doi:10.1016/s0378-5173(00)00617-7. PMID 11165091.

[AHFS2021-4] ୪.୦ ^୪.୧ ^୪.୨ ^୪.୩ ^୪.୪ ^୪.୫ "Sirolimus Monograph for Professionals". Drugs.com (in ଇଂରାଜୀ). Archived from the original on 13 August 2020. Retrieved 12 October 2021."Sirolimus Monograph for Professionals". Drugs.com. Archived from the original on 13 August 2020. Retrieved 12 October 2021.

[EPAR2021-5] ୫.୦ ^୫.୧ ^୫.୨ "Rapamune". Archived from the original on 13 August 2021. Retrieved 12 October 2021."Rapamune".

[BNF80-6] ୬.୦ ^୬.୧ BNF (80 ed.). BMJ Group and the Pharmaceutical Press. September 2020 – March 2021. p. 886. ISBN 978-0-85711-369-6.{{cite book}}: CS1 maint: date format (link)

[Seto2021-7] Seto B (November 2012). "Rapamycin and mTOR: a serendipitous discovery and implications for breast cancer". Clinical and Translational Medicine. 1 (1): 29. doi:10.1186/2001-1326-1-29. PMC 3561035. PMID 23369283.{{cite journal}}: CS1 maint: unflagged free DOI (link)

[8] "Sirolimus Prices, Coupons & Savings Tips - GoodRx". GoodRx. Retrieved 12 October 2021.

[୪]

[୫]

[୬]

[୧]

[୨]

[୩]

[୭]

[୮]