Hidroksizin

Hidroksizin
Nama sistematis (IUPAC)
(±)-2-(2-{4-[(4-klorofenil)-fenilmetil]piperazin-1-il}etoksi)etanol
Data klinis
Nama dagang Atarax,[1] Vistaril,[2] dll
AHFS/Drugs.com monograph
MedlinePlus a682866
Data lisensi US Daily Med:pranala
Kat. kehamilan ?
Status hukum Harus dengan resep dokter (S4) (AU) ℞-only (CA) POM (UK) ℞-only (US) ℞ Preskripsi saja
Kemungkinan
ketergantungan 		None [3]
Rute Oral, intramuskular
Data farmakokinetik
Bioavailabilitas Tinggi
Ikatan protein 93%
Metabolisme Hati
Waktu paruh Dewasa: 20 jam[4][5]
Lansia: 29,3 jam[6]
Anak-anak: 7,1 jam[4]
Ekskresi Urin, feses
Pengenal
Nomor CAS 68-88-2 YaY 10246-75-0 (pamoate)
Kode ATC N05BB01 N05BB51
PubChem CID 3658
Ligan IUPHAR 7199
DrugBank DB00557
ChemSpider 3531 YaY
UNII 30S50YM8OG YaY
KEGG D08054 YaY
ChEBI CHEBI:5818 YaY
ChEMBL CHEMBL896 YaY
Sinonim UCB-4492
Data kimia
Rumus C21H27ClN2O2 

  • InChI=1S/C21H27ClN2O2/c22-20-8-6-19(7-9-20)21(18-4-2-1-3-5-18)24-12-10-23(11-13-24)14-16-26-17-15-25/h1-9,21,25H,10-17H2 YaY
    Key:ZQDWXGKKHFNSQK-UHFFFAOYSA-N YaY

Hidroksizin merupakan obat antihistamin. Obat ini digunakan untuk mengatasi rasa gatal, gelisah, insomnia, dan mual (termasuk yang disebabkan oleh mabuk gerak). Obat ini digunakan baik melalui mulut atau disuntikan ke otot.[7]

Hidroksizin bekerja dengan cara menghalangi efek histamin.[8] Obat ini adalah antihistamin generasi pertama dalam keluarga bahan kimia piperazina.[7][9] Efek samping yang umum termasuk rasa kantuk, sakit kepala, dan mulut kering.[7][8] Efek samping yang serius mungkin termasuk perpanjangan QT.[8] Tidak jelas apakah penggunaannya selama kehamilan atau menyusui aman.[7]

Obat ini pertama kali dibuat oleh Union Chimique Belge pada tahun 1956 dan disetujui untuk dijual oleh Pfizer di Amerika Serikat pada akhir tahun itu.[7][10]

Kimia

Hidroksizin dipasok terutama sebagai garam dihidroklorida (hidroksizin hidroklorida) tetapi juga dalam jumlah yang lebih sedikit sebagai garam embonat (hidroksizin pamoat).[63][64][65] Berat molekul hidroksizin, hidroksizin dihidroklorida, dan hidroksizin pamoat masing-masing adalah 374,9 g/mol, 447,8 g/mol, dan 763,3 g/mol.[4] Karena perbedaan berat molekulnya, 1 mg hidroksizin dihidroklorida setara dengan sekitar 1,7 mg hidroksizin pamoat.[66]

Referensi

  1. ^ "Atarax: FDA-Approved Drugs". U.S. Food and Drug Administration (FDA). Diakses tanggal 25 March 2023. 
  2. ^ "Vistaril: FDA-Approved Drugs". U.S. Food and Drug Administration (FDA). Diakses tanggal 5 August 2020. 
  3. ^ Hubbard JR, Martin PR (2001). Substance Abuse in the Mentally and Physically Disabled. CRC Press. hlm. 26. ISBN 9780824744977. 
  4. ^ a b Paton DM, Webster DR (1985). "Clinical pharmacokinetics of H1-receptor antagonists (the antihistamines)". Clinical Pharmacokinetics. 10 (6): 477–497. doi:10.2165/00003088-198510060-00002. PMID 2866055. 
  5. ^ Simons FE, Simons KJ, Frith EM (January 1984). "The pharmacokinetics and antihistaminic of the H1 receptor antagonist hydroxyzine". The Journal of Allergy and Clinical Immunology. 73 (1 Pt 1): 69–75. doi:10.1016/0091-6749(84)90486-x alt=Dapat diakses gratis. PMID 6141198. 
  6. ^ Simons KJ, Watson WT, Chen XY, Simons FE (January 1989). "Pharmacokinetic and pharmacodynamic studies of the H1-receptor antagonist hydroxyzine in the elderly". Clinical Pharmacology and Therapeutics. 45 (1): 9–14. doi:10.1038/clpt.1989.2. PMID 2562944. 
  7. ^ a b c d e "Hydroxyzine Hydrochloride Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Diakses tanggal 21 November 2018. 
  8. ^ a b c British national formulary : BNF 74 (edisi ke-74). British Medical Association. 2017. hlm. X. ISBN 978-0857112989. 
  9. ^ "Hydroxyzine". United States National Library of Medicine (NLM). Diakses tanggal 4 March 2020. 
  10. ^ Shorter E (2009). Before Prozac: the troubled history of mood disorders in psychiatry. Oxford [Oxfordshire]: Oxford University Press. ISBN 9780195368741. 
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