Peringatan Keamanan

In high doses or when ingested, naphazoline can lead to central nervous system depression (which can progress to coma and death), hypothermia, bradycardia, and deathA176558. This effect is especially pronounced in children under 6 yearsA176558,A176564.

Long term use of naphazoline can lead to rhinitis medicamentosa once naphazoline is stoppedA176567. This condition is a result of norepinephrine release by naphazoline triggering a negative feedback loopA176567.

Safety and effectiveness in children under 12 has not been establishedF4214. Studies in elderly patients have yet to be performedF4214. Risk in pregnancy, breast feeding, and on overall fertility have not been established, though pregnant and breast feeding patients should consider the risk and benefit before starting naphazoline treatmentF4214.

Naphazoline

DB06711

small molecule approved investigational

Deskripsi

Naphazoline is a rapid acting imidazoline sympathomimetic vasoconstrictor of ocular or nasal artieriolesL5804,L5807. It acts to decrease congestion and is found in many over the counter (OTC) eye drops and nasal preparationsL5804,L5807.

Naphazoline was first developed in 1942 as a nasal formulation for congestionA176609.

Struktur Molekul 2D

Berat 210.2744
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Half life has not been determined but effects last for 4 to 8 hours[L5807]. Other imidazoline compounds have half lives varying from 2 to 12 hours[T530].
Volume Distribusi Distribution data for naphazoline are scarce but imidazoline compounds are distributed throughout the body, and can cross the blood-brain barrier[T530].
Klirens (Clearance) Clearance data for naphazoline is unavailable[F4214].

Absorpsi

Absorption data for naphazoline are scarce but imidazoline compounds in general are weakly basic and lipophilic, with high bioavailability from the gastrointestinal tractT530.

Metabolisme

Metabolism data for naphazoline are scarce. Imidazoline compounds undergo some hepatic metabolism but a large fraction of the dose may be excreted unchanged in the urineT530.

Rute Eliminasi

Imidazoline compounds undergo some hepatic metabolism but a large fraction of the dose may be excreted unchanged in the urineT530. Urinary excretion is higher with more acidic urineT530.

Interaksi Obat

932 Data
Valsartan Naphazoline may decrease the antihypertensive activities of Valsartan.
Ramipril Naphazoline may decrease the antihypertensive activities of Ramipril.
Reserpine Naphazoline may decrease the antihypertensive activities of Reserpine.
Remikiren Naphazoline may decrease the antihypertensive activities of Remikiren.
Torasemide Naphazoline may decrease the antihypertensive activities of Torasemide.
Isradipine Naphazoline may decrease the antihypertensive activities of Isradipine.
Olmesartan Naphazoline may decrease the antihypertensive activities of Olmesartan.
Chlorthalidone Naphazoline may decrease the antihypertensive activities of Chlorthalidone.
Nitroprusside Naphazoline may decrease the antihypertensive activities of Nitroprusside.
Diltiazem Naphazoline may decrease the antihypertensive activities of Diltiazem.
Minoxidil Naphazoline may decrease the antihypertensive activities of Minoxidil.
Treprostinil Naphazoline may decrease the antihypertensive activities of Treprostinil.
Amlodipine Naphazoline may decrease the antihypertensive activities of Amlodipine.
Nimodipine Naphazoline may decrease the antihypertensive activities of Nimodipine.
Nisoldipine Naphazoline may decrease the antihypertensive activities of Nisoldipine.
Bendroflumethiazide Naphazoline may decrease the antihypertensive activities of Bendroflumethiazide.
Fosinopril Naphazoline may decrease the antihypertensive activities of Fosinopril.
Trandolapril Naphazoline may decrease the antihypertensive activities of Trandolapril.
Metolazone Naphazoline may decrease the antihypertensive activities of Metolazone.
Lercanidipine Naphazoline may decrease the antihypertensive activities of Lercanidipine.
Benazepril Naphazoline may decrease the antihypertensive activities of Benazepril.
Bosentan Naphazoline may decrease the antihypertensive activities of Bosentan.
Enalapril Naphazoline may decrease the antihypertensive activities of Enalapril.
Cyclothiazide Naphazoline may decrease the antihypertensive activities of Cyclothiazide.
Candoxatril Naphazoline may decrease the antihypertensive activities of Candoxatril.
Mecamylamine Naphazoline may decrease the antihypertensive activities of Mecamylamine.
Losartan Naphazoline may decrease the antihypertensive activities of Losartan.
Moexipril Naphazoline may decrease the antihypertensive activities of Moexipril.
Eplerenone Naphazoline may decrease the antihypertensive activities of Eplerenone.
Lisinopril Naphazoline may decrease the antihypertensive activities of Lisinopril.
Nitroglycerin Naphazoline may decrease the antihypertensive activities of Nitroglycerin.
Metyrosine Naphazoline may decrease the antihypertensive activities of Metyrosine.
Hydroflumethiazide Naphazoline may decrease the antihypertensive activities of Hydroflumethiazide.
Cryptenamine Naphazoline may decrease the antihypertensive activities of Cryptenamine.
Perindopril Naphazoline may decrease the antihypertensive activities of Perindopril.
Candesartan cilexetil Naphazoline may decrease the antihypertensive activities of Candesartan cilexetil.
Fenoldopam Naphazoline may decrease the antihypertensive activities of Fenoldopam.
Indapamide Naphazoline may decrease the antihypertensive activities of Indapamide.
Tadalafil Naphazoline may decrease the antihypertensive activities of Tadalafil.
Eprosartan Naphazoline may decrease the antihypertensive activities of Eprosartan.
Chlorothiazide Naphazoline may decrease the antihypertensive activities of Chlorothiazide.
Quinapril Naphazoline may decrease the antihypertensive activities of Quinapril.
Telmisartan Naphazoline may decrease the antihypertensive activities of Telmisartan.
Methyldopa Naphazoline may decrease the antihypertensive activities of Methyldopa.
Hydrochlorothiazide Naphazoline may decrease the antihypertensive activities of Hydrochlorothiazide.
Trichlormethiazide Naphazoline may decrease the antihypertensive activities of Trichlormethiazide.
Irbesartan Naphazoline may decrease the antihypertensive activities of Irbesartan.
Nitrendipine Naphazoline may decrease the antihypertensive activities of Nitrendipine.
Deserpidine Naphazoline may decrease the antihypertensive activities of Deserpidine.
Pentolinium Naphazoline may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Naphazoline may decrease the antihypertensive activities of Trimethaphan.
Diazoxide Naphazoline may decrease the antihypertensive activities of Diazoxide.
Captopril Naphazoline may decrease the antihypertensive activities of Captopril.
Epoprostenol Naphazoline may decrease the antihypertensive activities of Epoprostenol.
Bepridil Naphazoline may decrease the antihypertensive activities of Bepridil.
Hydralazine Naphazoline may decrease the antihypertensive activities of Hydralazine.
Polythiazide Naphazoline may decrease the antihypertensive activities of Polythiazide.
Cilazapril Naphazoline may decrease the antihypertensive activities of Cilazapril.
Saprisartan Naphazoline may decrease the antihypertensive activities of Saprisartan.
Spirapril Naphazoline may decrease the antihypertensive activities of Spirapril.
Mibefradil Naphazoline may decrease the antihypertensive activities of Mibefradil.
Tienilic acid Naphazoline may decrease the antihypertensive activities of Tienilic acid.
Debrisoquine Naphazoline may decrease the antihypertensive activities of Debrisoquine.
Sitaxentan Naphazoline may decrease the antihypertensive activities of Sitaxentan.
Ambrisentan Naphazoline may decrease the antihypertensive activities of Ambrisentan.
Diethylnorspermine Naphazoline may decrease the antihypertensive activities of Diethylnorspermine.
Nilvadipine Naphazoline may decrease the antihypertensive activities of Nilvadipine.
Pinacidil Naphazoline may decrease the antihypertensive activities of Pinacidil.
Temocapril Naphazoline may decrease the antihypertensive activities of Temocapril.
Riociguat Naphazoline may decrease the antihypertensive activities of Riociguat.
Macitentan Naphazoline may decrease the antihypertensive activities of Macitentan.
Hexamethonium Naphazoline may decrease the antihypertensive activities of Hexamethonium.
Aliskiren Naphazoline may decrease the antihypertensive activities of Aliskiren.
Nicorandil Naphazoline may decrease the antihypertensive activities of Nicorandil.
Efonidipine Naphazoline may decrease the antihypertensive activities of Efonidipine.
Lacidipine Naphazoline may decrease the antihypertensive activities of Lacidipine.
Manidipine Naphazoline may decrease the antihypertensive activities of Manidipine.
Rauwolfia serpentina root Naphazoline may decrease the antihypertensive activities of Rauwolfia serpentina root.
Enalaprilat Naphazoline may decrease the antihypertensive activities of Enalaprilat.
Selexipag Naphazoline may decrease the antihypertensive activities of Selexipag.
Angiotensin 1-7 Naphazoline may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril Naphazoline may decrease the antihypertensive activities of Imidapril.
BQ-123 Naphazoline may decrease the antihypertensive activities of BQ-123.
Tetrahydropalmatine Naphazoline may decrease the antihypertensive activities of Tetrahydropalmatine.
Cicletanine Naphazoline may decrease the antihypertensive activities of Cicletanine.
Dihydralazine Naphazoline may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Naphazoline may decrease the antihypertensive activities of Zofenopril.
Guanoxan Naphazoline may decrease the antihypertensive activities of Guanoxan.
Delapril Naphazoline may decrease the antihypertensive activities of Delapril.
Vincamine Naphazoline may decrease the antihypertensive activities of Vincamine.
Linsidomine Naphazoline may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Naphazoline may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Naphazoline may decrease the antihypertensive activities of Tolonidine.
Endralazine Naphazoline may decrease the antihypertensive activities of Endralazine.
Cadralazine Naphazoline may decrease the antihypertensive activities of Cadralazine.
Cyclopenthiazide Naphazoline may decrease the antihypertensive activities of Cyclopenthiazide.
Bietaserpine Naphazoline may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Naphazoline may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Naphazoline may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Naphazoline may decrease the antihypertensive activities of Guanoclor.

Target Protein

D(2) dopamine receptor DRD2
Alpha-2A adrenergic receptor ADRA2A
Alpha-1A adrenergic receptor ADRA1A

Referensi & Sumber

Synthesis reference: Roy W. Bryant, Ravi Parihar, Thomas Rowe, Susan Caballa, "Methods of Making and Using Stable Pharmaceutical Compositions Comprising Ketotifen and Naphazoline." U.S. Patent US20110312998, issued December 22, 2011.
Artikel (PubMed)
  • PMID: 8067910
    Vitezic D, Rozmanic V, Franulovic J, Ahel V, Matesic D: Naphazoline nasal drops intoxication in children. Arh Hig Rada Toksikol. 1994 Mar;45(1):25-9.
  • PMID: 8276031
    Mahieu LM, Rooman RP, Goossens E: Imidazoline intoxication in children. Eur J Pediatr. 1993 Nov;152(11):944-6.
  • PMID: 16784007
    Ramey JT, Bailen E, Lockey RF: Rhinitis medicamentosa. J Investig Allergol Clin Immunol. 2006;16(3):148-55.
  • PMID: 18903384
    HAINSWORTH WC: Accidental poisoning with naphazoline (privine) hydrochloride. Am J Dis Child. 1948 Jan;75(1):76-80.
Textbook
  • ISBN: 978-0-12-420227-6
    Dalefield, Rosalind (2015). 12. In Veterinary Toxicology for Australia and New Zealand (pp. 170-171). Elsevier.

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