ଭୋରାପାକ୍ସର

ଭୋରାପାକ୍ସର
Clinical data
Trade names	Zontivity
Synonyms	SCH-530348
data	EU EMA: yes;
Pregnancy; category	US: B (No risk in non-human studies) ; ;
Routes of; administration	By mouth
Legal status
Legal status	US: ℞-only ;
Pharmacokinetic data
Bioavailability	~100%
Protein binding	≥99%
Metabolism	Liver (CYP3A4 and CYP2J2)
Elimination half-life	5–13 days
Excretion	Feces (58%), urine (25%)
Identifiers
	IUPAC name Ethyl N-[(3R,3aS,4S,4aR,7R,8aR,9aR)-4-[(E)-2-[5-(3-fluorophenyl)-2-pyridyl]vinyl]-3-methyl-1-oxo-3a,4,4a,5,6,7,8,8a,9,9a-decahydro-3H-benzo[f]isobenzofuran-7-yl]carbamate;
ECHA InfoCard	100.116.767
Chemical and physical data
Formula	C29H33FN2O4
Molar mass	୪୯୨.୫୯ g·mol−1
3D model (JSmol)	Interactive image;
Melting point	278 °C (532 °F)
	SMILES Fc1cccc(c1)c2ccc(nc2)\C=C\[C@H]4[C@H]3[C@@H](C[C@H](NC(=O)OCC)CC3)C[C@H]5C(=O)O[C@@H]([C@@H]45)C;
	InChI InChI=1S/C29H33FN2O4/c1-3-35-29(34)32-23-10-11-24-20(14-23)15-26-27(17(2)36-28(26)33)25(24)12-9-22-8-7-19(16-31-22)18-5-4-6-21(30)13-18/h4-9,12-13,16-17,20,23-27H,3,10-11,14-15H2,1-2H3,(H,32,34)/b12-9+/t17-,20+,23-,24-,25+,26-,27+/m1/s1 ; Key:ZBGXUVOIWDMMJE-QHNZEKIYSA-N ;
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ଭୋରାପାକ୍ସର (ଇଂରାଜୀ ଭାଷାରେ Vorapaxar), ଜୋନାଟିଭିଟି ଏହାର ବିକ୍ରୟ ନାମ, ହେଉଛି ଏକ ଔଷଧ ଯାହା ଆଥେରୋସ୍କ୍ଲେରୋସିସ ରୋଗୀଙ୍କଠାରେ ହୃଦଘାତ ଏବଂ ଷ୍ଟ୍ରୋକର ଆଶଙ୍କା କମାଇବା ପାଇଁ ବ୍ୟବହୃତ ହୁଏ ।^[୨] ତଥାପି ସାମଗ୍ରିକ ଉପକାର ୨୦୨୧ ସୁଦ୍ଧା ଅସ୍ପଷ୍ଟ ରହିଥିଲା ।^[୨] ଏହା ପାଟିରେ ଦିଆଯାଏ ।^[୨]

ସାଧାରଣ ପାର୍ଶ୍ୱ ପ୍ରତିକ୍ରିୟାରେ ରକ୍ତସ୍ରାବ ହୋଇପାରେ ଯେପରିକି ଖପୁରୀ ମଧ୍ୟସ୍ଥ ରକ୍ତସ୍ରାବ ମଧ୍ୟ ହୋଇପାରେ ।^[୨] ପ୍ରାକୃତିକ ଦ୍ରବ୍ୟ ହିମାବାସିନ୍ ଉପରେ ଆଧାରିତ ଏହା ଏକ ଥ୍ରୋମ୍ବିନ୍ ରିସେପ୍ଟର ( ପ୍ରୋଟିଏଜ-ଆକ୍ଟିଭେଟ୍ ଅଭିଗ୍ରାହକ ବା ରିସେପ୍ଟର, ଭାଗ-୧) ବ୍ଲକର ଅଟେ ।^[୩] ଏହା ପ୍ଲାଟେଲେଟ୍ ଏକତ୍ରୀକରଣକୁ ଅବରୋଧ କରି କାର୍ଯ୍ୟକ୍ଷମ ହୁଏ । ^[୨]

୨୦୧୪ ମସିହାରେ ଯୁକ୍ତରାଷ୍ଟ୍ରରେ ଡାକ୍ତରୀ ବ୍ୟବହାର ପାଇଁ ଭୋରାପାକ୍ସରକୁ ଅନୁମୋଦନ କରାଯାଇଥିଲା ।^[୨] ୨୦୧୫ରେ ୟୁରୋପରେ ଡାକ୍ତରୀ ବ୍ୟବହାର ପାଇଁ ଏହାକୁ ଅନୁମୋଦନ କରାଯାଇଥିବାବେଳେ ୨୦୧୭ରେ ଏହି ଅନୁମୋଦନ ପ୍ରତ୍ୟାହାର କରାଯାଇଥିଲା ।^[୪] ^[୫] ଯୁକ୍ତରାଷ୍ଟ୍ରରେ ୨୦୨୧ ସୁଦ୍ଧା ଏହା ପିଛା ମାସକୁ ପ୍ରାୟ ୩୭୦ ଡଲାର ଖର୍ଚ୍ଚ ହୋଇଥାଏ ^[୬]

ଆଧାର

↑ "ZONTIVITY™ (vorapaxar) Tablets 2.08 mg, for oral use. Full Prescribing Information" (PDF). Merck & Co., Inc. Initial U.S. Approval: 05/2014. Archived (PDF) from the original on 17 June 2014. Retrieved 17 June 2014.
↑ ^୨.୦ ^୨.୧ ^୨.୨ ^୨.୩ ^୨.୪ ^୨.୫ "Vorapaxar Monograph for Professionals". Drugs.com (in ଇଂରାଜୀ). Archived from the original on 24 January 2021. Retrieved 16 September 2021.
↑ Chackalamannil, S; Wang, Y; Greenlee, WJ; Hu, Z; Xia, Y; Ahn, HS; Boykow, G; Hsieh, Y; Palamanda, J (12 June 2008). "Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity". Journal of medicinal chemistry. 51 (11): 3061–4. doi:10.1021/jm800180e. PMID 18447380.
↑ "Zontivity". Archived from the original on 28 November 2020. Retrieved 16 September 2021.
↑ "Zontivity Withdrawal of the marketing authorisation in the European Union" (PDF). Archived (PDF) from the original on 3 June 2019. Retrieved 16 September 2021.
↑ "Zontivity Prices, Coupons & Savings Tips - GoodRx". GoodRx. Archived from the original on 9 August 2016. Retrieved 16 September 2021.

[zontivity-1] "ZONTIVITY™ (vorapaxar) Tablets 2.08 mg, for oral use. Full Prescribing Information" (PDF). Merck & Co., Inc. Initial U.S. Approval: 05/2014. Archived (PDF) from the original on 17 June 2014. Retrieved 17 June 2014.

[AHFS2021-2] ୨.୦ ^୨.୧ ^୨.୨ ^୨.୩ ^୨.୪ ^୨.୫ "Vorapaxar Monograph for Professionals". Drugs.com (in ଇଂରାଜୀ). Archived from the original on 24 January 2021. Retrieved 16 September 2021.

[3] Chackalamannil, S; Wang, Y; Greenlee, WJ; Hu, Z; Xia, Y; Ahn, HS; Boykow, G; Hsieh, Y; Palamanda, J (12 June 2008). "Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity". Journal of medicinal chemistry. 51 (11): 3061–4. doi:10.1021/jm800180e. PMID 18447380.

[4] "Zontivity". Archived from the original on 28 November 2020. Retrieved 16 September 2021.

[5] "Zontivity Withdrawal of the marketing authorisation in the European Union" (PDF). Archived (PDF) from the original on 3 June 2019. Retrieved 16 September 2021.

[6] "Zontivity Prices, Coupons & Savings Tips - GoodRx". GoodRx. Archived from the original on 9 August 2016. Retrieved 16 September 2021.

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