ଆପ୍ରେମିଲାଷ୍ଟ

ଆପ୍ରେମିଲାଷ୍ଟ
Clinical data
Pronunciation	/əˈprɛmɪlæst/ ə-PREM-i-last
Trade names	Otezla, Aplex, others
Synonyms	CC-10004
AHFS/Drugs.com	monograph
MedlinePlus	a614022
data	EU EMA: yes; US DailyMed: Apremilast;
Pregnancy; category	AU: B3 ; US: C (Risk not ruled out) ; ;
Routes of; administration	By mouth (tablets)
Legal status
Legal status	AU: S4 (Prescription only) ; UK: POM (Prescription only) ; US: ℞-only ; ℞ (Prescription only);
Pharmacokinetic data
Bioavailability	73%; Tmax = ~2.5 hours
Protein binding	c. 68%
Metabolism	Liver (CYP3A4, with minor contributions from CYP2A6, CYP1A2)
Metabolites	O-desmethylapremilast glucuronide (and others)
Elimination half-life	6–9 hours
Excretion	Urine (58%), faeces (39%)
Identifiers
	IUPAC name N-{2-[(1S)-1-(3-Ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl}acetamide;
ECHA InfoCard	100.234.786
Chemical and physical data
Formula	C22H24N2O7S
Molar mass	୪୬୦.୫0 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES O=S(=O)(C)C[C@H](c1ccc(OC)c(OCC)c1)N3C(=O)c2cccc(c2C3=O)NC(=O)C;
	InChI InChI=1S/C22H24N2O7S/c1-5-31-19-11-14(9-10-18(19)30-3)17(12-32(4,28)29)24-21(26)15-7-6-8-16(23-13(2)25)20(15)22(24)27/h6-11,17H,5,12H2,1-4H3,(H,23,25)/t17-/m1/s1; Key:IMOZEMNVLZVGJZ-QGZVFWFLSA-N;

ଆପ୍ରେମିଲାଷ୍ଟ, ଅନ୍ୟମାନଙ୍କ ମଧ୍ୟରେ ଏକ ବିକ୍ରୟ ନାମ ଓଟେଜଲା, ହେଉଛି ପ୍ଲେକ୍ ସୋରିଆସିସ୍, ସୋରିଆଟିକ୍ ଆର୍ଥ୍ରାଇଟିସ୍ ଏବଂ ବେସେଟ ରୋଗର ଚିକିତ୍ସା ପାଇଁ ବ୍ୟବହୃତ ଏକ ଔଷଧ । ^[୫] ^[୬] ଅନ୍ୟ ଚିକିତ୍ସା ଫଳପ୍ରଦ ହୁଏ ନାହିଁ ନ ହେଲେ ଏହା ବ୍ୟବହୃତ ହୁଏ । ^[୫] ଏହା ପାଟିରେ ଦିଆଯାଏ । ^[୭]

ସାଧାରଣ ପାର୍ଶ୍ୱ ପ୍ରତିକ୍ରିୟାରେ ତରଳ ଝାଡ଼ା, ଅଇ, ସାଧାରଣ ଥଣ୍ଡା ଏବଂ ମୁଣ୍ଡବିନ୍ଧା ହୋଇପାରେ । ^[୫] ଅନ୍ୟ ପାର୍ଶ୍ୱ ପ୍ରତିକ୍ରିୟାରେ ଅବସାଦ ଏବଂ ଓଜନ ହ୍ରାସ ହୋଇପାରେ । ^[୬] ଗର୍ଭାବସ୍ଥାରେ ନିରାପତ୍ତା ଅସ୍ପଷ୍ଟ, ଅନ୍ୟ ପ୍ରାଣୀମାନଙ୍କର କ୍ଷତି ହେବାର ପ୍ରମାଣ ରହିଛି। ^[୮] ଏହା ଏନଜାଇମ୍ ଫସଫୋଡିଏଷ୍ଟେରେଜ୍ 4 (PDE4)ର ଏକ ପ୍ରତିବନ୍ଧକ ଯାହାଦ୍ୱାରା ସାଇଟୋକିନସ ହ୍ରାସ ହୁଏ । ^[୫]

୨୦୧୪ରେ ଆମେରିକାରେ ଏବଂ ୨୦୧୫ରେ ୟୁରୋପରେ ଚିକିତ୍ସା ବ୍ୟବହାର ନିମନ୍ତେ ଆପ୍ରେମିଲାଷ୍ଟ ଅନୁମୋଦିତ ହୋଇଥିଲା । ^[୫] ^[୬] ଯୁକ୍ତରାଜ୍ୟରେ ୪ ସପ୍ତାହ ଚିକିତ୍ସା ଖର୍ଚ୍ଚ ୫୫୦ ପାଉଣ୍ଡ ।^[୭] ଯୁକ୍ତରାଷ୍ଟ୍ରରେ ଏହାର ମୂଲ୍ୟ ପ୍ରାୟ ୪,୧୦୦ ଡଲାର । ^[୯]

ଆଧାର

↑ "Apremilast (Otezla) Use During Pregnancy". Drugs.com. 27 September 2019. Archived from the original on 4 December 2020. Retrieved 19 April 2020.
↑ "Otezla 30 mg Film-Coated Tablets - Summary of Product Characteristics (SmPC)". (emc). 15 April 2020. Archived from the original on 15 January 2021. Retrieved 19 April 2020.
↑ ^୩.୦ ^୩.୧ ^୩.୨ ^୩.୩ ^୩.୪ "Otezla (aprelimast) dosing, indications, interactions, adverse effects, and more". Medscape Reference. WebMD. Archived from the original on 17 October 2014. Retrieved 28 March 2014.
↑ Haberfeld H, ed. (2015). Austria-Codex (in ଜର୍ମାନ). Vienna: Österreichischer Apothekerverlag.
↑ ^୫.୦ ^୫.୧ ^୫.୨ ^୫.୩ ^୫.୪ "Otezla". Archived from the original on 3 March 2020. Retrieved 15 January 2022.
↑ ^୬.୦ ^୬.୧ ^୬.୨ "DailyMed - OTEZLA- apremilast tablet, film coated". dailymed.nlm.nih.gov. Archived from the original on 15 January 2022. Retrieved 15 January 2022.
↑ ^୭.୦ ^୭.୧ BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 1165. ISBN 978-0857114105.
↑ "Apremilast (Otezla) Use During Pregnancy". Drugs.com (in ଇଂରାଜୀ). Archived from the original on 4 December 2020. Retrieved 15 January 2022.
↑ "Otezla Prices, Coupons & Patient Assistance Programs". Drugs.com (in ଇଂରାଜୀ). Archived from the original on 25 May 2016. Retrieved 15 January 2022.

[Drugs.com_pregnancy-1] "Apremilast (Otezla) Use During Pregnancy". Drugs.com. 27 September 2019. Archived from the original on 4 December 2020. Retrieved 19 April 2020.

[2] "Otezla 30 mg Film-Coated Tablets - Summary of Product Characteristics (SmPC)". (emc). 15 April 2020. Archived from the original on 15 January 2021. Retrieved 19 April 2020.

[MSR-3] ୩.୦ ^୩.୧ ^୩.୨ ^୩.୩ ^୩.୪ "Otezla (aprelimast) dosing, indications, interactions, adverse effects, and more". Medscape Reference. WebMD. Archived from the original on 17 October 2014. Retrieved 28 March 2014.

[AC-4] Haberfeld H, ed. (2015). Austria-Codex (in ଜର୍ମାନ). Vienna: Österreichischer Apothekerverlag.

[EPAR2022-5] ୫.୦ ^୫.୧ ^୫.୨ ^୫.୩ ^୫.୪ "Otezla". Archived from the original on 3 March 2020. Retrieved 15 January 2022.

[PI2022-6] ୬.୦ ^୬.୧ ^୬.୨ "DailyMed - OTEZLA- apremilast tablet, film coated". dailymed.nlm.nih.gov. Archived from the original on 15 January 2022. Retrieved 15 January 2022.

[BNF81-7] ୭.୦ ^୭.୧ BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 1165. ISBN 978-0857114105.

[AHFS2022-8] "Apremilast (Otezla) Use During Pregnancy". Drugs.com (in ଇଂରାଜୀ). Archived from the original on 4 December 2020. Retrieved 15 January 2022.

[9] "Otezla Prices, Coupons & Patient Assistance Programs". Drugs.com (in ଇଂରାଜୀ). Archived from the original on 25 May 2016. Retrieved 15 January 2022.

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Clinical data


Pronunciation	/əˈprɛmɪlæst/ ə-PREM-i-last
Trade names	Otezla, Aplex, others
Synonyms	CC-10004
AHFS/Drugs.com	monograph
MedlinePlus	a614022
data	EU EMA: yes US DailyMed: Apremilast
Pregnancy category	AU: B3 US: C (Risk not ruled out) ^[୧]
Routes of administration	By mouth (tablets)
Legal status
Legal status	AU: S4 (Prescription only) UK: POM (Prescription only) ^[୨] US: ℞-only ℞ (Prescription only)
Pharmacokinetic data
Bioavailability	73%;^[୩] T_max = ~2.5 hours
Protein binding	c. 68%^[୩]
Metabolism	Liver (CYP3A4, with minor contributions from CYP2A6, CYP1A2)^[୩]
Metabolites	O-desmethylapremilast glucuronide (and others)^[୪]
Elimination half-life	6–9 hours^[୩]
Excretion	Urine (58%), faeces (39%)^[୩]
Identifiers
IUPAC name N-{2-[(1S)-1-(3-Ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl}acetamide
ECHA InfoCard	100.234.786
Chemical and physical data
Formula	C₂₂H₂₄N₂O₇S
Molar mass	୪୬୦.୫0 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES O=S(=O)(C)C[C@H](c1ccc(OC)c(OCC)c1)N3C(=O)c2cccc(c2C3=O)NC(=O)C
InChI InChI=1S/C22H24N2O7S/c1-5-31-19-11-14(9-10-18(19)30-3)17(12-32(4,28)29)24-21(26)15-7-6-8-16(23-13(2)25)20(15)22(24)27/h6-11,17H,5,12H2,1-4H3,(H,23,25)/t17-/m1/s1 Key:IMOZEMNVLZVGJZ-QGZVFWFLSA-N