Peringatan Keamanan

In the event of an overdose, patients may experience hypotensionFDA Label. Blood pressure and heart rate should be controlled by having the patient lie down or by treating with volume expanders or if necessary vasopressorsFDA Label. Patients should be monitored for renal functionFDA Label. Because terazosin is highly protein bound, dialysis is unlikely to provide benefit to overdosing patientsFDA Label.

The oral LD50 in mice is 5500mg/kgMSDS.

Terazosin

DB01162

small molecule approved

Deskripsi

Terazosin is a quinazoline derivative alpha-1-selective adrenergic blocking agent indicated for benign prostatic hyperplasia and hypertensionFDA LabelA176831. Terazosin blocks adrenaline's action on alpha-1 adrenergic receptors, causing relaxation of smooth muscle in blood vessels and the prostateA176837.

Struktur Molekul 2D

Berat 387.4329
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Terazosin has a mean half life 12 hours though this can be as high as 14 hours in patients over 70 years and as low as 11.4 hours in patients 20 to 39 years old[FDA Label][A176831].
Volume Distribusi 25L to 30L[A176831].
Klirens (Clearance) Plasma clearance is 80mL/min and renal clearance is 10mL/min[A176831].

Absorpsi

Approximately 90%A176831.

Metabolisme

The majority of terazosin is hepatically metabolizedA176831. The metabolites recovered include 6-O-demethyl terazosin, 7-O-methyl terazosin, a piperozine derivative, and a diamine derivativeA176831.

Rute Eliminasi

Approximately 10% of the oral dose is excreted unchanged in the urine and approximately 20% is excreted in the fecesFDA LabelA176831. 40% of the total dose is eliminated in urine and 60% of the total dose is eliminated in the fecesFDA LabelA176831.

Interaksi Makanan

1 Data
  • 1. Take with or without food. A meal does not significantly affect the extent of absorption but delays Tmax by 40 minutes.

Interaksi Obat

699 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Terazosin is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Terazosin is combined with Levodopa.
Risperidone Terazosin may increase the hypotensive activities of Risperidone.
Amifostine Terazosin may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Terazosin.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Terazosin.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Terazosin.
Obinutuzumab Terazosin may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Terazosin.
Rituximab Terazosin may increase the hypotensive activities of Rituximab.
Desmopressin Desmopressin may decrease the antihypertensive activities of Terazosin.
Methysergide Methysergide may decrease the antihypertensive activities of Terazosin.
Atomoxetine Atomoxetine may decrease the antihypertensive activities of Terazosin.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Terazosin.
Protriptyline Protriptyline may decrease the antihypertensive activities of Terazosin.
Methylergometrine Methylergometrine may decrease the antihypertensive activities of Terazosin.
Mirtazapine Mirtazapine may decrease the antihypertensive activities of Terazosin.
Buspirone Buspirone may decrease the antihypertensive activities of Terazosin.
Doxapram Doxapram may decrease the antihypertensive activities of Terazosin.
Atropine Atropine may decrease the antihypertensive activities of Terazosin.
Lisuride Lisuride may decrease the antihypertensive activities of Terazosin.
Alfentanil Alfentanil may decrease the antihypertensive activities of Terazosin.
Fentanyl Fentanyl may decrease the antihypertensive activities of Terazosin.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Terazosin.
Almotriptan Almotriptan may decrease the antihypertensive activities of Terazosin.
Naratriptan Naratriptan may decrease the antihypertensive activities of Terazosin.
Rizatriptan Rizatriptan may decrease the antihypertensive activities of Terazosin.
Dopamine Dopamine may decrease the antihypertensive activities of Terazosin.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Terazosin.
Methoxyflurane Methoxyflurane may decrease the antihypertensive activities of Terazosin.
Ergoloid mesylate Ergoloid mesylate may decrease the antihypertensive activities of Terazosin.
Dutasteride Dutasteride may decrease the antihypertensive activities of Terazosin.
Desipramine Desipramine may decrease the antihypertensive activities of Terazosin.
Finasteride Finasteride may decrease the antihypertensive activities of Terazosin.
Yohimbine Yohimbine may decrease the antihypertensive activities of Terazosin.
Solifenacin Solifenacin may decrease the antihypertensive activities of Terazosin.
Epicaptopril Epicaptopril may decrease the antihypertensive activities of Terazosin.
1-benzylimidazole 1-benzylimidazole may decrease the antihypertensive activities of Terazosin.
Lysergic acid diethylamide Lysergic acid diethylamide may decrease the antihypertensive activities of Terazosin.
Amineptine Amineptine may decrease the antihypertensive activities of Terazosin.
Flibanserin Flibanserin may decrease the antihypertensive activities of Terazosin.
Naluzotan Naluzotan may decrease the antihypertensive activities of Terazosin.
Cariprazine Cariprazine may decrease the antihypertensive activities of Terazosin.
Mianserin Mianserin may decrease the antihypertensive activities of Terazosin.
Esmirtazapine Esmirtazapine may decrease the antihypertensive activities of Terazosin.
Vilazodone Vilazodone may decrease the antihypertensive activities of Terazosin.
Nitrous oxide Nitrous oxide may decrease the antihypertensive activities of Terazosin.
Saralasin Saralasin may decrease the antihypertensive activities of Terazosin.
Cinitapride Cinitapride may decrease the antihypertensive activities of Terazosin.
Tyramine Tyramine may decrease the antihypertensive activities of Terazosin.
Ifenprodil Ifenprodil may decrease the antihypertensive activities of Terazosin.
Dimetacrine Dimetacrine may decrease the antihypertensive activities of Terazosin.
Butriptyline Butriptyline may decrease the antihypertensive activities of Terazosin.
Cannabidiol Cannabidiol may decrease the antihypertensive activities of Terazosin.
Vortioxetine Vortioxetine may decrease the antihypertensive activities of Terazosin.
Dosulepin Dosulepin may decrease the antihypertensive activities of Terazosin.
Moxisylyte Moxisylyte may decrease the antihypertensive activities of Terazosin.
Tianeptine Tianeptine may decrease the antihypertensive activities of Terazosin.
Oxaprotiline Oxaprotiline may decrease the antihypertensive activities of Terazosin.
Dihydroergocornine Dihydroergocornine may decrease the antihypertensive activities of Terazosin.
Atipamezole Atipamezole may decrease the antihypertensive activities of Terazosin.
Tetrahydrocannabivarin Tetrahydrocannabivarin may decrease the antihypertensive activities of Terazosin.
Piclozotan Piclozotan may decrease the antihypertensive activities of Terazosin.
Siponimod Siponimod may decrease the antihypertensive activities of Terazosin.
Idazoxan Idazoxan may decrease the antihypertensive activities of Terazosin.
Opipramol Opipramol may decrease the antihypertensive activities of Terazosin.
Tramazoline Tramazoline may decrease the antihypertensive activities of Terazosin.
Amitriptylinoxide Amitriptylinoxide may decrease the antihypertensive activities of Terazosin.
Dibenzepin Dibenzepin may decrease the antihypertensive activities of Terazosin.
Quinupramine Quinupramine may decrease the antihypertensive activities of Terazosin.
Trichloroethylene Trichloroethylene may decrease the antihypertensive activities of Terazosin.
Fenozolone Fenozolone may decrease the antihypertensive activities of Terazosin.
Dihydroergocristine Dihydroergocristine may decrease the antihypertensive activities of Terazosin.
Melitracen Melitracen may decrease the antihypertensive activities of Terazosin.
Dihydroergocryptine Dihydroergocryptine may decrease the antihypertensive activities of Terazosin.
Terguride Terguride may decrease the antihypertensive activities of Terazosin.
Lofepramine Lofepramine may decrease the antihypertensive activities of Terazosin.
Xenon Xenon may decrease the antihypertensive activities of Terazosin.
Iprindole Iprindole may decrease the antihypertensive activities of Terazosin.
Buflomedil Buflomedil may decrease the antihypertensive activities of Terazosin.
Metergoline Metergoline may decrease the antihypertensive activities of Terazosin.
Diethyl ether Diethyl ether may decrease the antihypertensive activities of Terazosin.
Imipramine oxide Imipramine oxide may decrease the antihypertensive activities of Terazosin.
Mefenorex Mefenorex may decrease the antihypertensive activities of Terazosin.
5-methoxy-N,N-dimethyltryptamine 5-methoxy-N,N-dimethyltryptamine may decrease the antihypertensive activities of Terazosin.
Quinoline Yellow WS Quinoline Yellow WS may decrease the antihypertensive activities of Terazosin.
Solriamfetol Solriamfetol may decrease the antihypertensive activities of Terazosin.
Sufentanil Sufentanil may decrease the antihypertensive activities of Terazosin.
Isoflurane Isoflurane may decrease the antihypertensive activities of Terazosin.
Propofol Propofol may decrease the antihypertensive activities of Terazosin.
Remifentanil Remifentanil may decrease the antihypertensive activities of Terazosin.
Halothane Halothane may decrease the antihypertensive activities of Terazosin.
Omapatrilat Omapatrilat may decrease the antihypertensive activities of Terazosin.
Rescinnamine Rescinnamine may decrease the antihypertensive activities of Terazosin.
Desflurane Desflurane may decrease the antihypertensive activities of Terazosin.
Sevoflurane Sevoflurane may decrease the antihypertensive activities of Terazosin.
Clomipramine Clomipramine may decrease the antihypertensive activities of Terazosin.
Rotigotine Rotigotine may decrease the antihypertensive activities of Terazosin.
Cyclosporine Cyclosporine may decrease the antihypertensive activities of Terazosin.
Eletriptan Eletriptan may decrease the antihypertensive activities of Terazosin.

Target Protein

Alpha-1A adrenergic receptor ADRA1A
Alpha-1B adrenergic receptor ADRA1B
Alpha-1D adrenergic receptor ADRA1D
Transforming growth factor beta-1 proprotein TGFB1
Voltage-gated inwardly rectifying potassium channel KCNH2 KCNH2
Voltage-gated inwardly rectifying potassium channel KCNH6 KCNH6
Voltage-gated inwardly rectifying potassium channel KCNH7 KCNH7

Referensi & Sumber

Synthesis reference: K. S. Keshava Murthy, Gamini Weeratunga, Tianhao Zhou, Bhaskar Reddy Guntoori, "Process for the manufacture of intermediates suitable to make doxazosin, terazosin, prazosin, tiodazosin and related antihypertensive medicines." U.S. Patent US5919931, issued September, 1986.
Artikel (PubMed)
  • PMID: 2872802
    Sonders RC: Pharmacokinetics of terazosin. Am J Med. 1986 May 23;80(5B):20-4.
  • PMID: 23518907
    Papadopoulos G, Vlachodimitropoulos D, Kyroudi A, Kouloukoussa M, Perrea D, Mitropoulos D: Terazosin treatment induces caspase-3 expression in the rat ventral prostate. J Clin Med Res. 2013 Apr;5(2):127-31. doi: 10.4021/jocmr1215w. Epub 2013 Feb 25.
  • PMID: 14767264
    Roehrborn CG, Schwinn DA: Alpha1-adrenergic receptors and their inhibitors in lower urinary tract symptoms and benign prostatic hyperplasia. J Urol. 2004 Mar;171(3):1029-35.
  • PMID: 10503165
    Na YJ, Guo YL, Gu FL: Clinical comparison of selective and non-selective alpha 1A-adrenoceptor antagonists for bladder outlet obstruction associated with benign prostatic hyperplasia: studies on tamsulosin and terazosin in Chinese patients. The Chinese Tamsulosin Study Group. J Med. 1998;29(5-6):289-304.
  • PMID: 11170131
    Glassman DT, Chon JK, Borkowski A, Jacobs SC, Kyprianou N: Combined effect of terazosin and finasteride on apoptosis, cell proliferation, and transforming growth factor-beta expression in benign prostatic hyperplasia. Prostate. 2001 Jan 1;46(1):45-51.

Contoh Produk & Brand

Produk: 245 • International brands: 9
Produk
  • Apo-terazosin
    Tablet • 2 mg • Oral • Canada • Generic • Approved
  • Apo-terazosin
    Tablet • 5 mg • Oral • Canada • Generic • Approved
  • Apo-terazosin
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Apo-terazosin
    Tablet • 1 mg • Oral • Canada • Generic • Approved
  • Dom-terazosin
    Tablet • 1 mg • Oral • Canada • Generic • Approved
  • Dom-terazosin
    Tablet • 2 mg • Oral • Canada • Generic • Approved
  • Dom-terazosin
    Tablet • 5 mg • Oral • Canada • Generic • Approved
  • Dom-terazosin
    Tablet • 10 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 245 produk.
International Brands
  • Blavin — Baliarda (Argentina)
  • Flumarc — Raffo (Argentina)
  • Fosfomic — Finadiet (Argentina)
  • Heitrin — Abbott (Germany; discontinued)
  • Hytrinex — Amdipharm (Sweden)
  • Itrin — Keryos (Italy)
  • Urodie — Keryos (Italy)
  • Vicard — Amdipharm (Austria)
  • Zayasel

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