Peringatan Keamanan

The oral LD50 in rats is 142mg/kg and 15.3mg/kg in mice.L11299 The subcutaneous LD50 in rats is 114mg/kg and 46mg/kg in mice.L11299

Patients experiencing and overdose may present with hypotension, drowsiness, lethargy, and bradycardia.L11277 Overdose should be managed by first calling local poison control. Patients may require intravenous saline to maintain blood pressure.A189805

Guanfacine

DB01018

small molecule approved investigational

Deskripsi

Guanfacine, or BS 100-141,A189838,A189841 is a selective alpha-A2 adrenergic receptor agonist initially indicated for the treatment of hypertensionL11274 but is now indicated as an extended release tablet for the treatment of ADHD.L11277 Guanfacine was first described in the literature in 1974.A189841

Guanfacine was granted FDA approval on 27 October 1986.L11274

Struktur Molekul 2D

Berat 246.093
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Guanfacine has a half life of 17 hours, but this may range from 10-30 hours.[A189796] The half life is largely independant of renal function.[A189802]
Volume Distribusi Guanfacine has a volume of distribution of 6.3L/kg.[A189796]
Klirens (Clearance) Guanfacine has a total body cleraance of 360±262mL/min and a renal clearance of 233±245mL/min in patients with normal renal function. Patients with a glomerular filtration rate (GFR) of 10-30mL/min had a total body clearance of 308±274mL/min and a renal clearance of 34±22mL/min.[A189802] Patients with a GFR of <1mL/min had a total body clearance of 257±187mL/min and a renal clearance of 18±15mL/min.[A189802]

Absorpsi

Guanfacine is 80% orally bioavailable.A189796 1mg immediate release oral guanfacine reaches a Cmax of 2.5±0.6ng/mL with a Tmax of 3.0h and an AUC of 56±15ng\*h/mL.L11277 1mg extended release oral guanfacine reaches a Cmax of 1.0±0.3ng/mL with a Tmax of 6.0h and an AUC of 32±9ng\*h/mL.L11277 In adults, a 4mg oral extended release dose reaches a Cmax of 3.58±1.39ng/mL with a Tmax of 5.5h; in children, a 2mg oral extended relsease dose reaches a Cmax of 2.6±1.03ng/mL with a Tmax of 4.98h; in adolescents, a 2mg oral extended release dose reaches a Cmax of 1.7±0.43ng/mL with a Tmax of 4.96h.A189835

Metabolisme

Guanfacine is oxidized by CYP3A4A189823 to it's main metabolite, 3-hydroxyguanfacine.A189808 3-hydroxyguanfacine is then either glucuronidated or sulphated.A189808,A189811

Rute Eliminasi

Guanfacine is 57.0±32.0% eliminated in the urine in patients with normal renal function.A189802 Patients with a glomerular filtration rate (GFR) of 10-30mL/min eliminate 14.0±9.0% of a dose in the urine, while patients with a GFR of <1mL/min eliminate 7.5±2.4% of a dose in the urine.A189802

Interaksi Makanan

2 Data
  • 1. Avoid alcohol.
  • 2. Do not take with or immediately after a high-fat meal. High fat meals increase drug exposure.

Interaksi Obat

1761 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Guanfacine is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Guanfacine is combined with Levodopa.
Risperidone Guanfacine may increase the hypotensive activities of Risperidone.
Ceritinib Guanfacine may increase the bradycardic activities of Ceritinib.
Ivabradine Guanfacine may increase the bradycardic activities of Ivabradine.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Guanfacine.
Alfuzosin Alfuzosin may increase the hypotensive activities of Guanfacine.
Amifostine Guanfacine may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Guanfacine.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Guanfacine.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Guanfacine.
Obinutuzumab Guanfacine may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Guanfacine.
Rituximab Guanfacine may increase the hypotensive activities of Rituximab.
Epicaptopril Epicaptopril may decrease the antihypertensive activities of Guanfacine.
Valsartan Guanfacine may decrease the antihypertensive activities of Valsartan.
Ramipril Guanfacine may decrease the antihypertensive activities of Ramipril.
Olmesartan Guanfacine may decrease the antihypertensive activities of Olmesartan.
Minoxidil Guanfacine may decrease the antihypertensive activities of Minoxidil.
Trandolapril Guanfacine may decrease the antihypertensive activities of Trandolapril.
Benazepril Guanfacine may decrease the antihypertensive activities of Benazepril.
Enalapril Guanfacine may decrease the antihypertensive activities of Enalapril.
Moexipril Guanfacine may decrease the antihypertensive activities of Moexipril.
Nitroglycerin Guanfacine may decrease the antihypertensive activities of Nitroglycerin.
Candesartan cilexetil Guanfacine may decrease the antihypertensive activities of Candesartan cilexetil.
Eprosartan Guanfacine may decrease the antihypertensive activities of Eprosartan.
Quinapril Guanfacine may decrease the antihypertensive activities of Quinapril.
Telmisartan Guanfacine may decrease the antihypertensive activities of Telmisartan.
Remikiren Guanfacine may decrease the antihypertensive activities of Remikiren.
Bethanidine Bethanidine may decrease the antihypertensive activities of Guanfacine.
Guanadrel Guanfacine may decrease the antihypertensive activities of Guanadrel.
Candoxatril Guanfacine may decrease the antihypertensive activities of Candoxatril.
Guanabenz Guanabenz may decrease the antihypertensive activities of Guanfacine.
Cryptenamine Guanfacine may decrease the antihypertensive activities of Cryptenamine.
Omapatrilat Omapatrilat may decrease the antihypertensive activities of Guanfacine.
Deserpidine Guanfacine may decrease the antihypertensive activities of Deserpidine.
Pentolinium Guanfacine may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Guanfacine may decrease the antihypertensive activities of Trimethaphan.
Bretylium Guanfacine may decrease the antihypertensive activities of Bretylium.
Rescinnamine Guanfacine may decrease the antihypertensive activities of Rescinnamine.
Captopril Guanfacine may decrease the antihypertensive activities of Captopril.
Cilazapril Guanfacine may decrease the antihypertensive activities of Cilazapril.
Saprisartan Guanfacine may decrease the antihypertensive activities of Saprisartan.
Spirapril Guanfacine may decrease the antihypertensive activities of Spirapril.
Debrisoquine Guanfacine may decrease the antihypertensive activities of Debrisoquine.
Diethylnorspermine Guanfacine may decrease the antihypertensive activities of Diethylnorspermine.
Temocapril Guanfacine may decrease the antihypertensive activities of Temocapril.
Moxonidine Guanfacine may decrease the antihypertensive activities of Moxonidine.
Rauwolfia serpentina root Guanfacine may decrease the antihypertensive activities of Rauwolfia serpentina root.
Angiotensin 1-7 Guanfacine may decrease the antihypertensive activities of Angiotensin 1-7.
Rilmenidine Guanfacine may decrease the antihypertensive activities of Rilmenidine.
Imidapril Guanfacine may decrease the antihypertensive activities of Imidapril.
BQ-123 Guanfacine may decrease the antihypertensive activities of BQ-123.
Dihydralazine Guanfacine may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Guanfacine may decrease the antihypertensive activities of Zofenopril.
Guanoxan Guanfacine may decrease the antihypertensive activities of Guanoxan.
Delapril Guanfacine may decrease the antihypertensive activities of Delapril.
Vincamine Guanfacine may decrease the antihypertensive activities of Vincamine.
Linsidomine Guanfacine may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Guanfacine may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Guanfacine may decrease the antihypertensive activities of Tolonidine.
Endralazine Guanfacine may decrease the antihypertensive activities of Endralazine.
Cadralazine Guanfacine may decrease the antihypertensive activities of Cadralazine.
Bietaserpine Guanfacine may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Guanfacine may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Guanfacine may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Guanfacine may decrease the antihypertensive activities of Guanoclor.
Candesartan Guanfacine may decrease the antihypertensive activities of Candesartan.
Tocopherylquinone Guanfacine may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Guanfacine may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Guanfacine may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Guanfacine may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Guanfacine may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Guanfacine may decrease the antihypertensive activities of Quinaprilat.
Isoxsuprine Isoxsuprine may decrease the antihypertensive activities of Guanfacine.
Dutasteride Dutasteride may decrease the antihypertensive activities of Guanfacine.
Phentermine Phentermine may decrease the antihypertensive activities of Guanfacine.
Amlodipine Guanfacine may decrease the antihypertensive activities of Amlodipine.
Nimodipine Guanfacine may decrease the antihypertensive activities of Nimodipine.
Lercanidipine Guanfacine may decrease the antihypertensive activities of Lercanidipine.
Bosentan Guanfacine may decrease the antihypertensive activities of Bosentan.
Losartan Guanfacine may decrease the antihypertensive activities of Losartan.
Felodipine Guanfacine may decrease the antihypertensive activities of Felodipine.
Irbesartan Guanfacine may decrease the antihypertensive activities of Irbesartan.
Nitrendipine Guanfacine may decrease the antihypertensive activities of Nitrendipine.
Bepridil Guanfacine may decrease the antihypertensive activities of Bepridil.
Mibefradil Guanfacine may decrease the antihypertensive activities of Mibefradil.
Sitaxentan Guanfacine may decrease the antihypertensive activities of Sitaxentan.
Ambrisentan Guanfacine may decrease the antihypertensive activities of Ambrisentan.
Pinacidil Guanfacine may decrease the antihypertensive activities of Pinacidil.
Riociguat Guanfacine may decrease the antihypertensive activities of Riociguat.
Aliskiren Guanfacine may decrease the antihypertensive activities of Aliskiren.
Manidipine Guanfacine may decrease the antihypertensive activities of Manidipine.
Selexipag Guanfacine may decrease the antihypertensive activities of Selexipag.
Naftopidil Guanfacine may decrease the antihypertensive activities of Naftopidil.
Dexniguldipine Guanfacine may decrease the antihypertensive activities of Dexniguldipine.
Finasteride Finasteride may decrease the antihypertensive activities of Guanfacine.
Indacaterol Indacaterol may decrease the antihypertensive activities of Guanfacine.
Nylidrin Nylidrin may decrease the antihypertensive activities of Guanfacine.
Siponimod Siponimod may decrease the antihypertensive activities of Guanfacine.

Target Protein

Alpha-2A adrenergic receptor ADRA2A
Alpha-2B adrenergic receptor ADRA2B

Referensi & Sumber

Synthesis reference: U.S. Patent 3,632,645.
Artikel (PubMed)
  • PMID: 20844694
    Cruz MP: Guanfacine Extended-Release Tablets (Intuniv), a Nonstimulant Selective Alpha(2A)-Adrenergic Receptor Agonist For Attention-Deficit/Hyperactivity Disorder. P T. 2010 Aug;35(8):448-51.
  • PMID: 6994776
    Kirch W, Kohler H, Braun W: Elimination of guanfacine in patients with normal and impaired renal function. Br J Clin Pharmacol. 1980;10 Suppl 1:33S-35S. doi: 10.1111/j.1365-2125.1980.tb04902.x.
  • PMID: 20136479
    Minns AB, Clark RF, Schneir A: Guanfacine overdose resulting in initial hypertension and subsequent delayed, persistent orthostatic hypotension. Clin Toxicol (Phila). 2010 Feb;48(2):146-8. doi: 10.3109/15563650903505174.
  • PMID: 6994775
    Kiechel JR: Pharmacokinetics and metabolism of guanfacine in man: a review. Br J Clin Pharmacol. 1980;10 Suppl 1:25S-32S. doi: 10.1111/j.1365-2125.1980.tb04901.x.
  • PMID: 6761349
    Guerret M, Julien-Larose C, Kiechel JR, Lavene D: Determination of 3-hydroxy-guanfacine in biological fluids by electron-capture gas-liquid chromatography. J Chromatogr. 1982 Dec 10;233:181-92. doi: 10.1016/s0378-4347(00)81745-4.
  • PMID: 31313320
    Inoue Y, Morita H, Nozawa K, Kanazu T: Metabolite profiling of guanfacine in plasma and urine of healthy Japanese subjects after oral administration of guanfacine extended-release tablets. Biopharm Drug Dispos. 2019 Sep;40(8):282-293. doi: 10.1002/bdd.2201. Epub 2019 Aug 7.
  • PMID: 27128830
    Martin P, Satin L, Vince BD, Padilla AF, White C, Corcoran M, Stevenson A, Ermer J: Pharmacokinetics and pharmacodynamics of guanfacine extended release in adolescents aged 13-17 years with attention-deficit/hyperactivity disorder. Clin Pharmacol Drug Dev. 2014 Jul;3(4):252-61. doi: 10.1002/cpdd.124. Epub 2014 May 17.
  • PMID: 326262
    Dubach UC, Huwyler R, Radielovic P, Singeisen M: A new centrally action antihypertensive agent guanfacine (BS 100-141). Arzneimittelforschung. 1977;27(3):674-6.
Menampilkan 8 dari 9 artikel.

Contoh Produk & Brand

Produk: 202 • International brands: 1
Produk
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  • Apo-guanfacine XR
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  • Apo-guanfacine XR
    Tablet, extended release • 2 mg • Oral • Canada • Generic • Approved
  • Apo-guanfacine XR
    Tablet, extended release • 3 mg • Oral • Canada • Generic • Approved
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International Brands
  • Estulic — Egis

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