Peringatan Keamanan

The oral LD50 of phentolamine mesylate, a salt of phentolamine, was 1250 mg/kg in rats and 1000-1100 mg/kg in mice.L48410, L48420

No deaths due to acute poisoning with phentolamine have been reported. Overdosage with phentolamine is characterized chiefly by cardiovascular disturbances, such as arrhythmias, tachycardia, hypotension, and possibly shock. Other possible signs and symptoms include excitation, headache, sweating, pupillary contraction, visual disturbances, nausea, vomiting, diarrhea, and hypoglycemia. There is no specific antidote: Treatment consists of appropriate monitoring and supportive care. A plasma expander and norepinephrine may be administered to manage decreased blood pressure.L48415, L48420

Phentolamine

DB00692

small molecule approved

Deskripsi

Phentolamine is a reversible, non-selective alpha-adrenergic blocker that induces vasodilation. While initially introduced to the market for the treatment of hypertension, this clinical use was halted due to cardiovascular and gastrointestinal adverse effects with the prolonged use of large oral doses of phentolamine.A261781, A261786 It has several therapeutic uses, including the treatment of hypertensive episodes, prevention of norepinephrine-induced extravasation, diagnosis of pheochromocytoma, reversal of soft-tissue anesthesia, and treatment of pharmacologically-induced mydriasis.L48420, L48415, L48390 Phentolamine is administered intravenously, intramuscularly, submucosally, and topically.

Struktur Molekul 2D

Berat 281.3523
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Phentolamine has a half-life of 19 minutes following intravenous administration.[L48420] The terminal elimination half-life of phentolamine was approximately two to three hours following submucosal administration.[L48415]
Volume Distribusi While there is limited information on phentolamine distribution, the drug is reported to cross the blood-brain barrier.[A261766]
Klirens (Clearance) -

Absorpsi

The peak concentrations of phentolamine are achieved within 10 to 20 minutes following submucosal administration. The Cmax was higher in children with greater weights.L48415 Following topical ocular administration of phentolamine ophthalmic solution 0.75%, the peak concentration levels were achieved between 15 minutes and one hour after dosing with the median value of 0.45 ng/mL.L48390

Metabolisme

Data metabolisme tidak tersedia.

Rute Eliminasi

Approximately 13% of a single intravenous dose appears in the urine as unchanged drug.L48420

Interaksi Obat

702 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Phentolamine is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Phentolamine is combined with Levodopa.
Risperidone Phentolamine may increase the hypotensive activities of Risperidone.
Amifostine Phentolamine may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Phentolamine.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Phentolamine.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Phentolamine.
Obinutuzumab Phentolamine may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Phentolamine.
Rituximab Phentolamine may increase the hypotensive activities of Rituximab.
Yohimbine Yohimbine may decrease the antihypertensive activities of Phentolamine.
Epicaptopril Epicaptopril may decrease the antihypertensive activities of Phentolamine.
Siponimod Siponimod may decrease the antihypertensive activities of Phentolamine.
Valsartan Phentolamine may decrease the antihypertensive activities of Valsartan.
Ramipril Phentolamine may decrease the antihypertensive activities of Ramipril.
Olmesartan Phentolamine may decrease the antihypertensive activities of Olmesartan.
Minoxidil Phentolamine may decrease the antihypertensive activities of Minoxidil.
Trandolapril Phentolamine may decrease the antihypertensive activities of Trandolapril.
Benazepril Phentolamine may decrease the antihypertensive activities of Benazepril.
Enalapril Phentolamine may decrease the antihypertensive activities of Enalapril.
Losartan Phentolamine may decrease the antihypertensive activities of Losartan.
Moexipril Phentolamine may decrease the antihypertensive activities of Moexipril.
Remikiren Phentolamine may decrease the antihypertensive activities of Remikiren.
Guanadrel Phentolamine may decrease the antihypertensive activities of Guanadrel.
Bosentan Phentolamine may decrease the antihypertensive activities of Bosentan.
Candoxatril Phentolamine may decrease the antihypertensive activities of Candoxatril.
Nitroglycerin Phentolamine may decrease the antihypertensive activities of Nitroglycerin.
Metyrosine Phentolamine may decrease the antihypertensive activities of Metyrosine.
Cryptenamine Phentolamine may decrease the antihypertensive activities of Cryptenamine.
Candesartan cilexetil Phentolamine may decrease the antihypertensive activities of Candesartan cilexetil.
Eprosartan Phentolamine may decrease the antihypertensive activities of Eprosartan.
Quinapril Phentolamine may decrease the antihypertensive activities of Quinapril.
Omapatrilat Phentolamine may decrease the antihypertensive activities of Omapatrilat.
Telmisartan Phentolamine may decrease the antihypertensive activities of Telmisartan.
Irbesartan Phentolamine may decrease the antihypertensive activities of Irbesartan.
Deserpidine Phentolamine may decrease the antihypertensive activities of Deserpidine.
Pentolinium Phentolamine may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Phentolamine may decrease the antihypertensive activities of Trimethaphan.
Bretylium Phentolamine may decrease the antihypertensive activities of Bretylium.
Rescinnamine Phentolamine may decrease the antihypertensive activities of Rescinnamine.
Captopril Phentolamine may decrease the antihypertensive activities of Captopril.
Cilazapril Phentolamine may decrease the antihypertensive activities of Cilazapril.
Saprisartan Phentolamine may decrease the antihypertensive activities of Saprisartan.
Spirapril Phentolamine may decrease the antihypertensive activities of Spirapril.
Debrisoquine Phentolamine may decrease the antihypertensive activities of Debrisoquine.
Sitaxentan Phentolamine may decrease the antihypertensive activities of Sitaxentan.
Ambrisentan Phentolamine may decrease the antihypertensive activities of Ambrisentan.
Diethylnorspermine Phentolamine may decrease the antihypertensive activities of Diethylnorspermine.
Pinacidil Phentolamine may decrease the antihypertensive activities of Pinacidil.
Temocapril Phentolamine may decrease the antihypertensive activities of Temocapril.
Riociguat Phentolamine may decrease the antihypertensive activities of Riociguat.
Hexamethonium Phentolamine may decrease the antihypertensive activities of Hexamethonium.
Aliskiren Phentolamine may decrease the antihypertensive activities of Aliskiren.
Rauwolfia serpentina root Phentolamine may decrease the antihypertensive activities of Rauwolfia serpentina root.
Selexipag Phentolamine may decrease the antihypertensive activities of Selexipag.
Angiotensin 1-7 Phentolamine may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril Phentolamine may decrease the antihypertensive activities of Imidapril.
BQ-123 Phentolamine may decrease the antihypertensive activities of BQ-123.
Dihydralazine Phentolamine may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Phentolamine may decrease the antihypertensive activities of Zofenopril.
Guanoxan Phentolamine may decrease the antihypertensive activities of Guanoxan.
Delapril Phentolamine may decrease the antihypertensive activities of Delapril.
Vincamine Phentolamine may decrease the antihypertensive activities of Vincamine.
Linsidomine Phentolamine may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Phentolamine may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Phentolamine may decrease the antihypertensive activities of Tolonidine.
Endralazine Phentolamine may decrease the antihypertensive activities of Endralazine.
Cadralazine Phentolamine may decrease the antihypertensive activities of Cadralazine.
Bietaserpine Phentolamine may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Phentolamine may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Phentolamine may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Phentolamine may decrease the antihypertensive activities of Guanoclor.
Candesartan Phentolamine may decrease the antihypertensive activities of Candesartan.
Tocopherylquinone Phentolamine may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Phentolamine may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Phentolamine may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Phentolamine may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Phentolamine may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Phentolamine may decrease the antihypertensive activities of Quinaprilat.
Sufentanil Sufentanil may decrease the antihypertensive activities of Phentolamine.
Isoflurane Isoflurane may decrease the antihypertensive activities of Phentolamine.
Propofol Propofol may decrease the antihypertensive activities of Phentolamine.
Remifentanil Remifentanil may decrease the antihypertensive activities of Phentolamine.
Halothane Halothane may decrease the antihypertensive activities of Phentolamine.
Desflurane Desflurane may decrease the antihypertensive activities of Phentolamine.
Sevoflurane Sevoflurane may decrease the antihypertensive activities of Phentolamine.
Rotigotine Rotigotine may decrease the antihypertensive activities of Phentolamine.
Fentanyl Fentanyl may decrease the antihypertensive activities of Phentolamine.
Desipramine Desipramine may decrease the antihypertensive activities of Phentolamine.
Clomipramine Clomipramine may decrease the antihypertensive activities of Phentolamine.
Dimetacrine Dimetacrine may decrease the antihypertensive activities of Phentolamine.
Selpercatinib Selpercatinib may decrease the antihypertensive activities of Phentolamine.
Naxitamab Naxitamab may decrease the antihypertensive activities of Phentolamine.
Levamlodipine Phentolamine may decrease the antihypertensive activities of Levamlodipine.
Eletriptan Eletriptan may decrease the antihypertensive activities of Phentolamine.
Methysergide Methysergide may decrease the antihypertensive activities of Phentolamine.
Cabergoline Cabergoline may decrease the antihypertensive activities of Phentolamine.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Phentolamine.
Protriptyline Protriptyline may decrease the antihypertensive activities of Phentolamine.
Methylergometrine Methylergometrine may decrease the antihypertensive activities of Phentolamine.

Target Protein

Alpha-1 adrenergic receptors ADRA1A
D(2) dopamine receptor DRD2
Alpha-2 adrenergic receptors ADRA2A
ATP-sensitive inward rectifier potassium channel 11 KCNJ11

Referensi & Sumber

Artikel (PubMed)
  • PMID: 949032
    Gould L, Reddy CV: Phentolamine. Am Heart J. 1976 Sep;92(3):397-402. doi: 10.1016/s0002-8703(76)80121-4.
  • PMID: 1848966
    Raja SN, Treede RD, Davis KD, Campbell JN: Systemic alpha-adrenergic blockade with phentolamine: a diagnostic test for sympathetically maintained pain. Anesthesiology. 1991 Apr;74(4):691-8. doi: 10.1097/00000542-199104000-00012.
  • PMID: 9326676
    Proks P, Ashcroft FM: Phentolamine block of KATP channels is mediated by Kir6.2. Proc Natl Acad Sci U S A. 1997 Oct 14;94(21):11716-20. doi: 10.1073/pnas.94.21.11716.
  • PMID: 12879109
    Brock G: Oral phentolamine (Vasomax). Drugs Today (Barc). 2000 Feb-Mar;36(2-3):121-4. doi: 10.1358/dot.2000.36.2-3.568785.

Contoh Produk & Brand

Produk: 15 • International brands: 3
Produk
  • OraVerse
    Injection, solution • 0.4 mg/1.7mL • Submucosal • US • Approved
  • Oraverse
    Injection, solution • 0.235 mg/1mL • Submucosal • US • Approved
  • Oraverse
    Solution • 0.4 mg / 1.7 mL • Submucosal • Canada • Approved
  • Phentolamine Mesylate
    Injection, powder, for solution • 5 mg/1mL • Intramuscular; Intravenous • US • Generic • Approved
  • Phentolamine Mesylate
    Injection, powder, for solution • 5 mg/1mL • Intramuscular; Intravenous • US • Generic • Approved
  • Phentolamine Mesylate
    Powder • 1 g/1g • Not applicable • US
  • Phentolamine Mesylate
    Injection • 5 mg/1mL • Intramuscular; Intravenous; Parenteral • US
  • Phentolamine Mesylate
    Powder • 1 g/1g • Not applicable • US
Menampilkan 8 dari 15 produk.
International Brands
  • Regitin — Novartis
  • Regitina — Novartis
  • Vigamed — Grupo Cimed

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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