Astemizol: Perbedaan antara revisi

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Revisi per 15 Oktober 2024 15.16 sunting Muhammad Anas Sidik (bicara \| kontrib) 25.778 suntingan ←Membuat halaman berisi '{{Drugbox \| Watchedfields = changed \| verifiedrevid = 457285684 \| IUPAC_name = 1-[(4-fluorophenyl)methyl]-''N''-[1-[2-(4-methoxyphenyl)ethyl]-4-piperidyl]benzoimidazol-2-amine \| image = Astemizole.svg \| width = 250 <!--Clinical data--> \| tradename = \| Drugs.com = {{drugs.com\|MTM\|astemizole}} \| MedlinePlus = a600034 \| pregnancy_category = C (USA) \| legal_status = Withdrawn \| routes_of_administration = Oral <!--Pharmacokinetic data--> \| bioava...' Tag: Suntingan perangkat seluler Suntingan peramban seluler Suntingan seluler lanjutan		Revisi terkini sejak 16 Oktober 2024 01.14 sunting balikkan Hysocc (bicara \| kontrib) Pengguna terkonfirmasi, Peninjau 64.020 suntingan k Menambah Kategori:Senyawa 4-metoksifenil menggunakan HotCat
(4 revisi perantara oleh satu pengguna lainnya tidak ditampilkan)
Baris 2: \| Watchedfields = changed \| verifiedrevid = 457285684 \| IUPAC_name = 1-[(4-~~fluorophenyl~~fluorofenil)~~methyl~~metil]-''N''-[1-[2-(4-~~methoxyphenyl~~metoksifenil)~~ethyl~~etil]-4-~~piperidyl~~piperidil]benzoimidazol-2-~~amine~~aminadi \| image = Astemizole.svg ~~\| image = Astemizole.svg~~ \| width = 250 Baris 10 ⟶ 9: \| Drugs.com = {{drugs.com\|MTM\|astemizole}} \| MedlinePlus = a600034 \| pregnancy_category = C ~~([[United States\|USA]])~~ \| legal_status = ~~Withdrawn~~Ditarik dari perdaran \| routes_of_administration = Oral Baris 17 ⟶ 16: \| bioavailability = \| protein_bound = ~96% \| metabolism = [[~~Hepatic~~Hati]] ([[CYP3A4]])<ref name="pmid11259984">{{cite journal \| vauthors = Matsumoto S, Yamazoe Y \| title = Involvement of multiple human cytochromes P450 in the liver microsomal metabolism of astemizole and a comparison with terfenadine \| journal = British Journal of Clinical Pharmacology \| volume = 51 \| issue = 2 \| pages = 133–142 \| date = February 2001 \| pmid = 11259984 \| pmc = 2014443 \| doi = 10.1111/j.1365-2125.2001.01292.x }}</ref> \| elimination_half-life = 24 ~~hours~~jam \| excretion = [[~~Fecal~~Feses]] <!--Identifiers--> Baris 50 ⟶ 49: }} '''Astemizol''' (kode pengembangan R43512) adalah obat [[antihistamin]] generasi kedua yang memiliki durasi kerja panjang. ~~Astemizole~~Astemizol ditemukan oleh [[Janssen ~~Pharmaceutica~~Pharmaceuticals]] pada tahun 1977. Obat ini ditarik dari pasaran secara global pada tahun 1999 karena efek samping yang jarang terjadi tetapi berpotensi fatal (perpanjangan interval QTc dan [[aritmia]] terkait akibat blokade saluran hERG).~~[2][3]~~<ref name="pmid10376921">{{cite journal \| vauthors = Zhou Z, Vorperian VR, Gong Q, Zhang S, January CT \| title = Block of HERG potassium channels by the antihistamine astemizole and its metabolites desmethylastemizole and norastemizole \| journal = Journal of Cardiovascular Electrophysiology \| volume = 10 \| issue = 6 \| pages = 836–843 \| date = June 1999 \| pmid = 10376921 \| doi = 10.1111/j.1540-8167.1999.tb00264.x \| s2cid = 25655101 }}</ref><ref>{{cite journal \| vauthors = Charles O, Onakpoya I, Benipal S, Woods H, Bali A, Aronson JK, Heneghan C, Persaud N \| display-authors = 6 \| title = Withdrawn medicines included in the essential medicines lists of 136 countries \| journal = PLOS ONE \| volume = 14 \| issue = 12 \| pages = e0225429 \| date = 2019 \| pmid = 31791048 \| pmc = 6887519 \| doi = 10.1371/journal.pone.0225429 \| doi-access = free \| bibcode = 2019PLoSO..1425429C }}</ref> ==Farmakologi== Astemizol adalah antagonis reseptor histamin H1. Obat ini memiliki efek [[antikolinergik]] dan [[antipruritik]]. Astemizol cepat diserap dari saluran pencernaan dan secara kompetitif mengikat reseptor histamin H1 di saluran pencernaan, rahim, pembuluh darah, dan otot bronkial. Hal ini menekan pembentukan [[sembap\|edema]] dan [[gatal\|pruritus]] (yang disebabkan oleh [[histamin]]). Meskipun beberapa laporan sebelumnya menyatakan bahwa astemizol tidak melewati [[sawar darah otak]], beberapa penelitian<ref>{{cite journal \| vauthors = Rojo LE, Alzate-Morales J, Saavedra IN, Davies P, Maccioni RB \| title = Selective interaction of lansoprazole and astemizole with tau polymers: potential new clinical use in diagnosis of Alzheimer's disease \| journal = Journal of Alzheimer's Disease \| volume = 19 \| issue = 2 \| pages = 573–589 \| year = 2010 \| pmid = 20110603 \| pmc = 2951486 \| doi = 10.3233/JAD-2010-1262 \| publisher = IOS Press }}</ref><ref>{{cite journal \| vauthors = Di L, Kerns EH, Fan K, McConnell OJ, Carter GT \| title = High throughput artificial membrane permeability assay for blood-brain barrier \| journal = European Journal of Medicinal Chemistry \| volume = 38 \| issue = 3 \| pages = 223–232 \| date = March 2003 \| pmid = 12667689 \| doi = 10.1016/S0223-5234(03)00012-6 }}</ref> telah menunjukkan permeabilitas tinggi dan ikatan tinggi pada lipatan protein yang terkait dengan [[Penyakit Alzheimer]]. Astemizol juga dapat bekerja pada reseptor histamin H<sub>3</sub>, sehingga menimbulkan efek samping.{{citation needed\|date=December 2013}} Astemizol juga bekerja sebagai FIASMA (penghambat fungsional sfingomielinase asam).<ref name="pmid18504571">{{cite journal \| vauthors = Kornhuber J, Muehlbacher M, Trapp S, Pechmann S, Friedl A, Reichel M, Mühle C, Terfloth L, Groemer TW, Spitzer GM, Liedl KR, Gulbins E, Tripal P \| display-authors = 6 \| title = Identification of novel functional inhibitors of acid sphingomyelinase \| journal = PLOS ONE \| volume = 6 \| issue = 8 \| pages = e23852 \| year = 2011 \| pmid = 21909365 \| pmc = 3166082 \| doi = 10.1371/journal.pone.0023852 \| doi-access = free \| bibcode = 2011PLoSO...623852K }}</ref> Astemizol telah diteliti sebagai pengobatan untuk [[Penyakit Creutzfeldt-Jakob]] (CJD).<ref>{{cite journal \| vauthors = Karapetyan YE, Sferrazza GF, Zhou M, Ottenberg G, Spicer T, Chase P, Fallahi M, Hodder P, Weissmann C, Lasmézas CI \| display-authors = 6 \| title = Unique drug screening approach for prion diseases identifies tacrolimus and astemizole as antiprion agents \| journal = Proceedings of the National Academy of Sciences of the United States of America \| volume = 110 \| issue = 17 \| pages = 7044–7049 \| date = April 2013 \| doi = 10.1073/pnas.1303510110 \| pmid = 23576755 \| pmc = 3637718 \| bibcode = 2013PNAS..110.7044K \| doi-access = free }}</ref> ==Toksisitas== Astemizol memiliki [[median dosis letal\|LD<sub>50</sub>]] oral sekitar 2052 mg/kg (pada tikus). ==Referensi== {{Reflist}} Baris 58 ⟶ 72: * [http://publications.gc.ca/collections/Collection/H30-12-21-2001E.pdf Statement on Astemizole from Health Canada] [[Kategori:Fenetilamina]] ~~[[Category:Phenethylamines]]~~ [[Kategori:Benzimidazola]] ~~[[Category:Belgian inventions]]~~ [[Kategori:Senyawa 4-fluorofenil]] ~~[[Category:Benzimidazoles]]~~ [[Kategori:Antagonis reseptor H1]] ~~[[Category:4-Fluorophenyl compounds]]~~ [[Kategori:Penghalang KCNH2]] ~~[[Category:H1 receptor antagonists]]~~ [[~~Category~~Kategori:Janssen Pharmaceutica]]▼ ~~[[Category:HERG blocker]]~~ [[Kategori:Piperidina]] ▲[[Category:Janssen Pharmaceutica]] [[Kategori:Obat yang ditarik]] ~~[[Category:4-Methoxyphenyl compounds]]~~ [[Kategori:Antihistamin]] ~~[[Category:Piperidines]]~~ [[Kategori:Senyawa 4-metoksifenil]] ~~[[Category:Withdrawn drugs]]~~