Draft:Tryvio (aprocitentan)

Aprocitentan
Clinical data
Trade names	Tryvio
Other names	ACT-132577
Routes of; administration	By mouth
Drug class	Antihypertensive
ATC code	C02KN01 (WHO) ;
Legal status
Legal status	US: ℞-only;
Identifiers
	IUPAC name 5-(4-Bromophenyl)-4-[2-(5-bromopyrimidin-2-yl)oxyethoxy]-6-(sulfamoylamino)pyrimidine;
CAS Number	1103522-45-7;
PubChem CID	25099191;
IUPHAR/BPS	10070;
DrugBank	DB15059;
ChemSpider	25027753;
UNII	MZI81HV01P;
KEGG	D11441;
ChEBI	CHEBI:76609;
ChEMBL	ChEMBL2165326;
Chemical and physical data
Formula	C16H14Br2N6O4S
Molar mass	546.19 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C1=CC(=CC=C1C2=C(N=CN=C2OCCOC3=NC=C(C=N3)Br)NS(=O)(=O)N)Br;
	InChI InChI=1S/C16H14Br2N6O4S/c17-11-3-1-10(2-4-11)13-14(24-29(19,25)26)22-9-23-15(13)27-5-6-28-16-20-7-12(18)8-21-16/h1-4,7-9H,5-6H2,(H2,19,25,26)(H,22,23,24); Key:DKULOVKANLVDEA-UHFFFAOYSA-N;

Submission declined on 14 April 2024 by Wikishovel (talk).

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Declined by Wikishovel 41 days ago. Last edited by Wikishovel 41 days ago. Reviewer: Inform author.

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Tryvio (aprocitentan)[edit]

Tryvio (aktivna supstanca lijeka je aprocitentan, ACT-132577) je antagonist receptora endotelina koji se koristiti za liječenje visokog krvnog tlaka koji nije adekvatno kontroliran drugim lijekovima za visoki krvni tlak (antihipertenzivima). Uzima se oralno, u formi tablete, jedanput na dan. Koristi se u kombinaciji s drugim antihipertenzivima i ima nizak potencijal za interakcije s drugim lijekovima.^[2]

Tryvio djeluje tako da sprječava vezanje endotelina-1 (ET-1) na receptore ET_A i ET_B. Sprječavanjem vezanja ET-1, Tryvio snižava krvni tlak. Endotelin-1 je peptid kojeg proizvode različite stanica i tkiva, poput makrofaga, endotelnih i vaskularnih glatkih mišićnih stanica te stanica bubrežne moždine (medule). Povezan je s nekoliko učinaka, kao što su vazokonstrikcija (sužavanje krvnih žila), fibroza (zadebljanje i stvaranje ožiljaka na tkivu) i upala. ^[2]

FDA je odobrila Tryvio 19. ožujka 2024. godine.

Hipertenzija i endotelin-1[edit]

Endotelin-1 (ET-1) regulira krvni tlak i vaskularni tonus, tj. kontrakcije glatkih mišićnih stanica krvnih žila u stijenkama malih arterija i arteriola.^[3] Rezultat uspješne interakcijom s ET_A i ET_B receptorima su kontrakcije glatkih mišićnih stanica ^[4] koje se nalaze u stijenkama žila. Dakle, endotelin-1 ima vazokonstrikcijski učinak i često rezultira hipertenzijom. ^[5]

Hiperzenzija, tj. povišeni krvni tlak, može rezultirati komplikacijama, pogotovo ukoliko ne poduzimamo nikakve postupke prevencije ili liječenja. Hipertenzija može izazvati ozbiljno oštećenje srca. Pretjerani tlak može otvrdnuti arterije, smanjujući dotok krvi i kisika u srce. Ovaj povišeni tlak i smanjeni protok krvi mogu uzrokovati: anginu (bol u prsima), srčani udar, zatajenje srca (događa se kada srce ne može pumpati dovoljno krvi i kisika u druge vitalne tjelesne organe) te nepravilan rad srca koji može dovesti do iznenadne smrti. Hipertenzija također može prsnuti ili blokirati arterije koje opskrbljuju mozak krvlju i kisikom, uzrokujući moždani udar. Osim toga, hipertenzija može uzrokovati oštećenje bubrega, što dovodi do zatajenja bubrega.^[6]

Aprocitentan kao lijek[edit]

Aprocitentan (ACT-132577) je antagonist ET receptora koji sprječava vezanje ET-1 na receptore ET_A i ET_B. Aprocitentan uzrokuje sniženje krvnog tlaka koje je ovisno o dozi. Također, pokazalo se da ima sinergistički učinak s blokatorima renin-angiotenzinskog sustava. ^[5]

Reference[edit]

Category:Drugs acting on the cardiovascular system Category:Hypertension

^ https://www.accessdata.fda.gov/drugsatfda_docs/label/2024/217686s000lbl.pdf
^ ^a ^b "Tryvio: Uses, Dosage, Side Effects, Warnings". Drugs.com. Retrieved 2024-04-14.
^ Jackson, W.F. (2000) ‘Ion channels and vascular tone’, Hypertension, 35(1), pp. 173–178. doi:10.1161/01.hyp.35.1.173. Retrieved 2024-04-14
^ Schiffrin, E.L. (1998) ‘Endothelin and endothelin antagonists in hypertension’, Journal of Hypertension, 16(Supplement), pp. 1891–1895. doi:10.1097/00004872-199816121-00007. Retrieved 2024-04-14
^ ^a ^b Angeli, F., Verdecchia, P. and Reboldi, G. (2021) ‘Aprocitentan, a dual endothelin receptor antagonist under development for the treatment of resistant hypertension’, Cardiology and Therapy, 10(2), pp. 397–406. doi:10.1007/s40119-021-00233-7. Retrieved 2024-04-14
^ Hypertension (2023) World Health Organization. Available at: https://www.who.int/news-room/fact-sheets/detail/hypertension (Published 16th March 2023). Retrieved 2024-04-14

Category:Endothelin receptor antagonists

[Tryvio_FDA_label-1] ttps://www.accessdata.fda.gov/drugsatfda_docs/label/2024/217686s000lbl.pdf

[:0-2] "Tryvio: Uses, Dosage, Side Effects, Warnings". Drugs.com. Retrieved 2024-04-14.

[3] Jackson, W.F. (2000) ‘Ion channels and vascular tone’, Hypertension, 35(1), pp. 173–178. doi:10.1161/01.hyp.35.1.173. Retrieved 2024-04-14

[4] Schiffrin, E.L. (1998) ‘Endothelin and endothelin antagonists in hypertension’, Journal of Hypertension, 16(Supplement), pp. 1891–1895. doi:10.1097/00004872-199816121-00007. Retrieved 2024-04-14

[:1-5] Angeli, F., Verdecchia, P. and Reboldi, G. (2021) ‘Aprocitentan, a dual endothelin receptor antagonist under development for the treatment of resistant hypertension’, Cardiology and Therapy, 10(2), pp. 397–406. doi:10.1007/s40119-021-00233-7. Retrieved 2024-04-14

[6] Hypertension (2023) World Health Organization. Available at: https://www.who.int/news-room/fact-sheets/detail/hypertension (Published 16th March 2023). Retrieved 2024-04-14

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