Sibutramina

Sibutramin (atas), (S)-(−)-sibutramin (bawah)
Data klinis
Nama dagang	Meridia, dll
Nama lain	BTS-54524
AHFS/Drugs.com	monograph
MedlinePlus	a601110
Kategori kehamilan	AU: C Tidak ada data pada manusia; bukti potensi teratogenik yang tidak meyakinkan dalam penelitian pada hewan
Rute pemberian	Oral
Kelas obat	Serotonin–norepinephrine reuptake inhibitor; Anoretic
Kode ATC	A08AA10 (WHO)
Status hukum
Status hukum	CA: Withdrawn from market US: Schedule IV
Data farmakokinetika
Bioavailabilitas	Penyerapan 77%, metabolisme lintas pertama yang signifikan
Pengikatan protein	97%, (94% untuk metabolit desmetilnya, M1 & M2)
Metabolisme	Hati (dimediasi CYP3A4-mediated)
Waktu paruh eliminasi	1 jam (sibutramin), 14 jam (M1) & 16 jam (M2)
Ekskresi	Urin (77%), feses (8%)
Pengenal
Nama IUPAC 1-(1-(4-klorofenil)siklobutil)-N,N,2,2-tetrametilpropan-1-amina
Nomor CAS	106650-56-0 Y 766462-77-5 (klorosibutramin)
PubChem CID	5210
IUPHAR/BPS	2586
DrugBank	DB01105 Y
ChemSpider	5021 Y
UNII	WV5EC51866
KEGG	D08513 Y
ChEMBL	ChEMBL1419 Y
CompTox Dashboard (EPA)	DTXSID1023578
ECHA InfoCard	100.130.097
Data sifat kimia dan fisik
Rumus	C17H26ClN
Massa molar	279,85 g·mol−1
Model 3D (JSmol)	Gambar interaktif
SMILES ClC1=CC=C(C2(CCC2)C(CC(C)C)N(C)C)C=C1
InChI InChI=1S/C17H26ClN/c1-13(2)12-16(19(3)4)17(10-5-11-17)14-6-8-15(18)9-7-14/h6-9,13,16H,5,10-12H2,1-4H3 Y Key:UNAANXDKBXWMLN-UHFFFAOYSA-N Y
(verify)

Sibutramin merupakan obat penekan nafsu makan yang dijual dengan merek dagang Meridia atau Reductil. Hingga tahun 2010, sibutramin dipasarkan secara luas dan diresepkan sebagai obat dalam pengobatan obesitas.^[2] Mekanisme utama obat ini adalah penghambatan pengambilan kembali serotonin dan norepinefrin pada sinapsis neuron yang menghasilkan efek penurunan asupan energi dan meningkatkan rasa kenyang.^[3]

Di banyak negara, penjualan sibutramin telah dihentikan pada tahun 2010 karena penggunaannya dikaitkan dengan peningkatan kasus penyakit kardiovaskular dan strok. Beberapa negara yang menarik sibutramin dari pasar di antaranya adalah Australia,^[4] Kanada,^[5] Cina,^[6] Uni Eropa,^[7] Hong Kong,^[8] India,^[9] Selandia Baru,^[10] Filipina,^[11] Thailand,^[12] Inggris,^[13] dan Amerika Serikat.^[14] Mulai tanggal 14 Oktober 2010, distribusi sibutramin di Indonesia telah dilarang oleh Badan Pengawas Obat dan Makanan (BPOM).^[15]

1. ^ Anvisa (2023-03-31). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (dalam bahasa Brazilian Portuguese). Diário Oficial da União (dipublikasikan 2023-04-04). Diarsipkan dari versi aslinya tanggal 2023-08-03. Diakses tanggal 2023-08-16.
2. ^ "Sibutramine (Meridia)". Encyclopedia of Obesity. 2455 Teller Road, Thousand Oaks California 91320 United States: SAGE Publications, Inc. 2008. Pemeliharaan CS1: Lokasi (link)
3. ^ Lean, M. E. J. (2001-12). "How does sibutramine work?". International Journal of Obesity (dalam bahasa Inggris). 25 (4): S8 – S11. doi:10.1038/sj.ijo.0801931. ISSN 1476-5497.
4. ^ &NA; (2010-06). "The Australian Therapeutic Goods Administration (TGA) is reviewing the safety of sibutramine". Reactions Weekly. &NA, (1304): 5. doi:10.2165/00128415-201013040-00014. ISSN 0114-9954. Pemeliharaan CS1: Banyak nama: authors list (link) Pemeliharaan CS1: Tanda baca tambahan (link)
5. ^ Health Canada Endorsed Important Safety Information on MERIDIA (Sibutramine Hydrochloride Monohydrate) Archived 2013-01-11 at the Wayback Machine: Subject: Voluntary withdrawal of Meridia (sibutramine) capsules from the Canadian market.
6. ^ "Notification of Termination of Production, Sale, and Usage of Sibutramine Preparations and Their Active Pharmaceutical Ingredient". sda.gov in People's Republic of China. October 30, 2010. Archived from the original on 2011-10-07. Retrieved 2011-05-21.
7. ^ (in German) Sibutramin-Vertrieb in der Europäischen Union ausgesetzt [1] Archived 2012-07-19 at archive.today. Abbott Laboratories in Germany. Press Release 2010-01-21. Retrieved 2010-01-27
8. ^ "De-registration of pharmaceutical products containing sibutramine" (Press release). info.gov in Hong Kong. November 2, 2010. Retrieved 2010-11-08.
9. ^ "Banned Medicines" (Press release). Ministry of Health and Family Welfare. February 10, 2011. Retrieved 2011-03-15.
10. ^ "Withdrawal of Sibutramine (Reductil) in New Zealand" (Press release). MedSafe in New Zealand. October 11, 2010. Retrieved 2012-11-06.
11. ^ "FDA warns online sellers of banned slimming pills". January 12, 2014. Archived from the original on January 15, 2014. Retrieved February 20, 2014.
12. ^ "Thai FDA reveals voluntary withdrawal of sibutramine from the Thai market" (Press release). Food and Drug Administration of Thailand. October 20, 2010. Archived from the original on 2011-05-11. Retrieved 2010-12-22.
13. ^ "Top obesity drug being suspended" (dalam bahasa Inggris (Britania)). 2010-01-22. Diakses tanggal 2024-01-06.
14. ^ Rockoff JD, Dooren JC (October 8, 2010). "Abbott Pulls Diet Drug Meridia Off US Shelves". The Wall Street Journal. Archived from the original on 11 October 2010. Retrieved 8 October 2010.
15. ^ Media, Kompas Cyber (2010-10-18). "Obat Diet Mengandung Sibutramin Dilarang". KOMPAS.com. Diakses tanggal 2024-01-06.

• Abbott Press Release on Meridia Withdrawal Diarsipkan 2011-09-27 di Wayback Machine.
• Sibutramine drug information from Merck Manual. Includes dosage information and a comprehensive list of international brand names
• U.S. Food and Drug Administration (FDA) product safety website