Peringatan Keamanan

Patients experiencing and overdose may present with headache, hypertension, reflex bradycardia, tingling limbs, cardiac arrhythmias, and a feeling of fullness in the head.L9416,L9413,L9410 Overdose may be treated by supportive care and discontinuing phenylephrine, chronotropic medications, and vasodilators.A187370 Subcutaneous phentolamine may be used to treat tissue extravasation.A187370,L9413

Phenylephrine

DB00388

small molecule approved

Deskripsi

Phenylephrine is an alpha-1 adrenergic receptor agonist used to treat hypotension,L9416,L9410 dilate the pupil,L9413 and induce local vasoconstriction.A187370 The action of phenylephrine, or neo-synephrine, was first described in literature in the 1930s.A187376

Phenylephrine was granted FDA approval in 1939.L9413

Struktur Molekul 2D

Berat 167.205
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Intravenous phenylephrine has an effective half life of 5 minutes and an elimination half life of 2.5 hours.[A187379,L9416,L9410]
Volume Distribusi The volume of distribution of phenylephrine is 340L.[L9416,L9410]
Klirens (Clearance) Phenylephrine has an average clearance of 2100mL/min.[L9416,L9410]

Absorpsi

Phenylephrine is 38% orally bioavailable.A187379 Clinically significant systemic absorption of ophthalmic formulations is possible, especially at higher strengths and when the cornea is damaged.L9416

Metabolisme

Phenylephrine is mainly metabolized by monoamine oxidase A, monoamine oxidase B, and SULT1A3.A187382,A187385,L9416,L9410 The major metabolite is the inactive meta-hydroxymandelic acid, followed by sulfate conjugates.A187385,L9416,L9410 Phenylephrine can also be metabolized to phenylephrine glucuronide.A187385

Rute Eliminasi

86% of a dose of phenylephrine is recovered in the urineA187379 with 16% as the unmetabolized drug, 57% as the inactive meta-hydroxymendelic acid, and 8% as inactive sulfate conjugates.L9416,L9410

Interaksi Obat

1014 Data
Valsartan Phenylephrine may decrease the antihypertensive activities of Valsartan.
Ramipril Phenylephrine may decrease the antihypertensive activities of Ramipril.
Reserpine Phenylephrine may decrease the antihypertensive activities of Reserpine.
Remikiren Phenylephrine may decrease the antihypertensive activities of Remikiren.
Torasemide Phenylephrine may decrease the antihypertensive activities of Torasemide.
Olmesartan Phenylephrine may decrease the antihypertensive activities of Olmesartan.
Chlorthalidone Phenylephrine may decrease the antihypertensive activities of Chlorthalidone.
Nitroprusside Phenylephrine may decrease the antihypertensive activities of Nitroprusside.
Minoxidil Phenylephrine may decrease the antihypertensive activities of Minoxidil.
Treprostinil Phenylephrine may decrease the antihypertensive activities of Treprostinil.
Bendroflumethiazide Phenylephrine may decrease the antihypertensive activities of Bendroflumethiazide.
Fosinopril Phenylephrine may decrease the antihypertensive activities of Fosinopril.
Trandolapril Phenylephrine may decrease the antihypertensive activities of Trandolapril.
Metolazone Phenylephrine may decrease the antihypertensive activities of Metolazone.
Benazepril Phenylephrine may decrease the antihypertensive activities of Benazepril.
Bosentan Phenylephrine may decrease the antihypertensive activities of Bosentan.
Enalapril Phenylephrine may decrease the antihypertensive activities of Enalapril.
Cyclothiazide Phenylephrine may decrease the antihypertensive activities of Cyclothiazide.
Candoxatril Phenylephrine may decrease the antihypertensive activities of Candoxatril.
Mecamylamine Phenylephrine may decrease the antihypertensive activities of Mecamylamine.
Losartan Phenylephrine may decrease the antihypertensive activities of Losartan.
Moexipril Phenylephrine may decrease the antihypertensive activities of Moexipril.
Eplerenone Phenylephrine may decrease the antihypertensive activities of Eplerenone.
Lisinopril Phenylephrine may decrease the antihypertensive activities of Lisinopril.
Nitroglycerin Phenylephrine may decrease the antihypertensive activities of Nitroglycerin.
Metyrosine Phenylephrine may decrease the antihypertensive activities of Metyrosine.
Hydroflumethiazide Phenylephrine may decrease the antihypertensive activities of Hydroflumethiazide.
Cryptenamine Phenylephrine may decrease the antihypertensive activities of Cryptenamine.
Perindopril Phenylephrine may decrease the antihypertensive activities of Perindopril.
Candesartan cilexetil Phenylephrine may decrease the antihypertensive activities of Candesartan cilexetil.
Fenoldopam Phenylephrine may decrease the antihypertensive activities of Fenoldopam.
Indapamide Phenylephrine may decrease the antihypertensive activities of Indapamide.
Eprosartan Phenylephrine may decrease the antihypertensive activities of Eprosartan.
Chlorothiazide Phenylephrine may decrease the antihypertensive activities of Chlorothiazide.
Quinapril Phenylephrine may decrease the antihypertensive activities of Quinapril.
Telmisartan Phenylephrine may decrease the antihypertensive activities of Telmisartan.
Methyldopa Phenylephrine may decrease the antihypertensive activities of Methyldopa.
Hydrochlorothiazide Phenylephrine may decrease the antihypertensive activities of Hydrochlorothiazide.
Trichlormethiazide Phenylephrine may decrease the antihypertensive activities of Trichlormethiazide.
Irbesartan Phenylephrine may decrease the antihypertensive activities of Irbesartan.
Deserpidine Phenylephrine may decrease the antihypertensive activities of Deserpidine.
Pentolinium Phenylephrine may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Phenylephrine may decrease the antihypertensive activities of Trimethaphan.
Diazoxide Phenylephrine may decrease the antihypertensive activities of Diazoxide.
Captopril Phenylephrine may decrease the antihypertensive activities of Captopril.
Epoprostenol Phenylephrine may decrease the antihypertensive activities of Epoprostenol.
Hydralazine Phenylephrine may decrease the antihypertensive activities of Hydralazine.
Polythiazide Phenylephrine may decrease the antihypertensive activities of Polythiazide.
Cilazapril Phenylephrine may decrease the antihypertensive activities of Cilazapril.
Saprisartan Phenylephrine may decrease the antihypertensive activities of Saprisartan.
Spirapril Phenylephrine may decrease the antihypertensive activities of Spirapril.
Tienilic acid Phenylephrine may decrease the antihypertensive activities of Tienilic acid.
Debrisoquine Phenylephrine may decrease the antihypertensive activities of Debrisoquine.
Sitaxentan Phenylephrine may decrease the antihypertensive activities of Sitaxentan.
Ambrisentan Phenylephrine may decrease the antihypertensive activities of Ambrisentan.
Diethylnorspermine Phenylephrine may decrease the antihypertensive activities of Diethylnorspermine.
Pinacidil Phenylephrine may decrease the antihypertensive activities of Pinacidil.
Temocapril Phenylephrine may decrease the antihypertensive activities of Temocapril.
Riociguat Phenylephrine may decrease the antihypertensive activities of Riociguat.
Macitentan Phenylephrine may decrease the antihypertensive activities of Macitentan.
Hexamethonium Phenylephrine may decrease the antihypertensive activities of Hexamethonium.
Aliskiren Phenylephrine may decrease the antihypertensive activities of Aliskiren.
Nicorandil Phenylephrine may decrease the antihypertensive activities of Nicorandil.
Rauwolfia serpentina root Phenylephrine may decrease the antihypertensive activities of Rauwolfia serpentina root.
Enalaprilat Phenylephrine may decrease the antihypertensive activities of Enalaprilat.
Selexipag Phenylephrine may decrease the antihypertensive activities of Selexipag.
Angiotensin 1-7 Phenylephrine may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril Phenylephrine may decrease the antihypertensive activities of Imidapril.
BQ-123 Phenylephrine may decrease the antihypertensive activities of BQ-123.
Cicletanine Phenylephrine may decrease the antihypertensive activities of Cicletanine.
Zofenopril Phenylephrine may decrease the antihypertensive activities of Zofenopril.
Guanoxan Phenylephrine may decrease the antihypertensive activities of Guanoxan.
Delapril Phenylephrine may decrease the antihypertensive activities of Delapril.
Vincamine Phenylephrine may decrease the antihypertensive activities of Vincamine.
Linsidomine Phenylephrine may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Phenylephrine may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Phenylephrine may decrease the antihypertensive activities of Tolonidine.
Endralazine Phenylephrine may decrease the antihypertensive activities of Endralazine.
Cadralazine Phenylephrine may decrease the antihypertensive activities of Cadralazine.
Cyclopenthiazide Phenylephrine may decrease the antihypertensive activities of Cyclopenthiazide.
Bietaserpine Phenylephrine may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Phenylephrine may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Phenylephrine may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Phenylephrine may decrease the antihypertensive activities of Guanoclor.
Muzolimine Phenylephrine may decrease the antihypertensive activities of Muzolimine.
Xipamide Phenylephrine may decrease the antihypertensive activities of Xipamide.
Candesartan Phenylephrine may decrease the antihypertensive activities of Candesartan.
Tocopherylquinone Phenylephrine may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Phenylephrine may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Phenylephrine may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Phenylephrine may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Phenylephrine may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Phenylephrine may decrease the antihypertensive activities of Quinaprilat.
Furosemide Phenylephrine may decrease the antihypertensive activities of Furosemide.
Levamlodipine The risk or severity of hypertension can be decreased when Levamlodipine is combined with Phenylephrine.
Buthiazide Phenylephrine may decrease the antihypertensive activities of Buthiazide.
Azilsartan medoxomil Phenylephrine may decrease the antihypertensive activities of Azilsartan medoxomil.
Atomoxetine The risk or severity of hypertension can be increased when Atomoxetine is combined with Phenylephrine.
Linezolid The risk or severity of hypertension can be increased when Linezolid is combined with Phenylephrine.
Benzylpenicilloyl polylysine Phenylephrine may decrease effectiveness of Benzylpenicilloyl polylysine as a diagnostic agent.

Target Protein

Alpha-1A adrenergic receptor ADRA1A
D(2) dopamine receptor DRD2
Alpha-1B adrenergic receptor ADRA1B
Alpha-1D adrenergic receptor ADRA1D

Referensi & Sumber

Synthesis reference: Franz Dietrich Klinger, Lienhard Wolter, Wolfgang Dietrich, "Method for preparing of L-phenylephrine hydrochloride." U.S. Patent US6187956, issued February, 1976.
Artikel (PubMed)
  • PMID: 30521222
    Richards E, Maani CV: Phenylephrine .
  • PMID: 18609981
    Prescott F: CLINICAL EVALUATION OF THE PRESSOR ACTIVITY OF METHEDRINE, NEO-SYNEPHRINE, PAREDRINE, AND PHOLEDRINE. Br Heart J. 1944 Oct;6(4):214-20. doi: 10.1136/hrt.6.4.214.
  • PMID: 7507589
    Kanfer I, Dowse R, Vuma V: Pharmacokinetics of oral decongestants. Pharmacotherapy. 1993 Nov-Dec;13(6 Pt 2):116S-128S; discussion 143S-146S.
  • PMID: 31145702
    Bairam AF, Rasool MI, Alherz FA, Abunnaja MS, El Daibani AA, Gohal SA, Alatwi ES, Kurogi K, Liu MC: Impact of SULT1A3/SULT1A4 genetic polymorphisms on the sulfation of phenylephrine and salbutamol by human SULT1A3 allozymes. Pharmacogenet Genomics. 2019 Jul;29(5):99-105. doi: 10.1097/FPC.0000000000000371.
  • PMID: 26267590
    Gelotte CK, Zimmerman BA: Pharmacokinetics, safety, and cardiovascular tolerability of phenylephrine HCl 10, 20, and 30 mg after a single oral administration in healthy volunteers. Clin Drug Investig. 2015 Sep;35(9):547-58. doi: 10.1007/s40261-015-0311-9.

Contoh Produk & Brand

Produk: 6204 • International brands: 13
Produk
  • 24/7 Life Cold and Flu DayTime Severe
    Tablet, film coated • - • Oral • US • OTC
  • 4 Way Fast Acting
    Spray • 10 mg/1mL • Nasal • US • OTC
  • 4248 First Aid Kit
    Kit • - • Ophthalmic; Oral; Respiratory (inhalation); Topical • US • OTC
  • 4356 First Aid Kit
    Kit • - • Ophthalmic; Oral; Respiratory (inhalation); Topical • US • OTC
  • 4390 First Aid Kit
    Kit • - • Ophthalmic; Oral; Respiratory (inhalation); Topical • US • OTC
  • 4392 First Aid Kit
    Kit • - • Ophthalmic; Oral; Respiratory (inhalation); Topical • US • OTC
  • 7 Select Cold and Allergy Childrens
    Liquid • - • Oral • US • OTC
  • 7 Select Day Time Relief
    Solution • - • Oral • US • OTC
Menampilkan 8 dari 6204 produk.
International Brands
  • AK-Dilate
  • AK-Nefrin
  • Alconefrin
  • Mesatone
  • Minims Phenylephrine
  • Neofrin
  • Ocugestrin
  • Phenoptic
  • Phenylephrine Minims
  • Prefrin

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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