Peringatan Keamanan

The oral LD50 is 230 mg/kg in rats and 75 mg/kg in mice. The subcutaneous LD50 is 90 mg/kg in rats and 53 mg/kg in mice. The intraperitoneal LD50 is 43 mg/kg in rats.L31608

Xylometazoline poisoning is documented in three pediatric patients who were exposed to a drug concentration 40 times above the adequate dosage for children due to a compounding error: these patients experienced bradypnea and sinus bradycardia with supraventricular extrasystoles and were managed with fluid management.A228528

Xylometazoline

DB06694

small molecule approved investigational

Deskripsi

Xylometazoline is an imidazoline derivative A228523 with sympathomimetic and nasal decongestant activity. Xylometazoline works by binding to alpha (?)-adrenergic receptors to cause vasoconstriction of nasal blood vessels.A228508

Xylometazoline is available in over-the-counter (OTC) nasal sprays or drops to temporarily relieve nasal congestion due to cold, hay fever or other respiratory allergies. In some countries, it is available as combination products with ipratropium, domiphen, or dexpanthenol.

Struktur Molekul 2D

Berat 244.3752
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) No information is available on xylometazoline pharmacokinetics.
Volume Distribusi No information is available on xylometazoline pharmacokinetics.
Klirens (Clearance) No information is available on xylometazoline pharmacokinetics.

Absorpsi

No information is available on xylometazoline pharmacokinetics.

Metabolisme

No information is available on xylometazoline pharmacokinetics.

Rute Eliminasi

No information is available on xylometazoline pharmacokinetics.

Interaksi Obat

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

Target Protein

Alpha-2A adrenergic receptor ADRA2A
Alpha-2B adrenergic receptor ADRA2B
Alpha-1A adrenergic receptor ADRA1A
Alpha-1B adrenergic receptor ADRA1B
Alpha-1D adrenergic receptor ADRA1D
Alpha-2C adrenergic receptor ADRA2C

Referensi & Sumber

Artikel (PubMed)
  • PMID: 20030735
    Haenisch B, Walstab J, Herberhold S, Bootz F, Tschaikin M, Ramseger R, Bonisch H: Alpha-adrenoceptor agonistic activity of oxymetazoline and xylometazoline. Fundam Clin Pharmacol. 2010 Dec;24(6):729-39. doi: 10.1111/j.1472-8206.2009.00805.x.
  • PMID: 18655753
    Eccles R, Eriksson M, Garreffa S, Chen SC: The nasal decongestant effect of xylometazoline in the common cold. Am J Rhinol. 2008 Sep-Oct;22(5):491-6. doi: 10.2500/ajr.2008.22.3202. Epub 2008 Jul 24.
  • PMID: 7540314
    Graf P, Juto JE: Sustained use of xylometazoline nasal spray shortens the decongestive response and induces rebound swelling. Rhinology. 1995 Mar;33(1):14-7.
  • PMID: 12073765
    Castellano F, Mautone G: Decongestant activity of a new formulation of xylometazoline nasal spray: a double-blind, randomized versus placebo and reference drugs controlled, dose-effect study. Drugs Exp Clin Res. 2002;28(1):27-35.
  • PMID: 29109644
    Haldar R, Bajwa SS, Kaur J: Xylometazoline nasal drops induced anaphylaxis: An atypical perioperative complication. J Anaesthesiol Clin Pharmacol. 2017 Jul-Sep;33(3):399-401. doi: 10.4103/0970-9185.173331.
  • PMID: 24642023
    Musshoff F, Madea B, Woelfle J, Vlanic D: Xylometazoline poisoning: A 40-fold nasal overdose caused by a compounding error in 3 children. Forensic Sci Int. 2014 May;238:e3-5. doi: 10.1016/j.forsciint.2014.02.011. Epub 2014 Feb 20.
  • PMID: 21069518
    Eskiizmir G, Hircin Z, Ozyurt B, Unlu H: A comparative analysis of the decongestive effect of oxymetazoline and xylometazoline in healthy subjects. Eur J Clin Pharmacol. 2011 Jan;67(1):19-23. doi: 10.1007/s00228-010-0941-z. Epub 2010 Nov 11.
  • PMID: 8549644
    Westerveld GJ, Scheeren RA, Dekker I, Griffioen DH, Voss HP, Bast A: Anti-oxidant actions of oxymethazoline and xylomethazoline. Eur J Pharmacol. 1995 Sep 15;291(1):27-31. doi: 10.1016/0922-4106(95)90185-x.

Contoh Produk & Brand

Produk: 37 • International brands: 7
Produk
  • 4 Way Moisturizing Relief
    Spray • 1 mg/1mL • Nasal • US • OTC
  • Aqua Maris Fast Acting Decongestant
    Spray • 10 mg/10mL • Nasal • US • OTC
  • Aqua Maris Kids Fast Acting Decongestant
    Spray • .05 mg/10mL • Nasal • US • OTC
  • Balminil Decongest
    Solution • 0.1 % • Nasal • Canada • OTC • Approved
  • Balminil Nasal Decongestant
    Spray • 0.1 % w/v • Nasal • Canada • OTC • Approved
  • Certified Decongestant Nasal Spray .1%
    Solution; Spray • 0.1 % • Nasal • Canada • OTC • Approved
  • Cold & Allergy Relief
    Spray • 0.1 % w/v • Nasal • Canada • OTC • Approved
  • Cold & Allergy Relief With Moisturizers
    Spray • 0.1 % • Nasal • Canada • OTC • Approved
Menampilkan 8 dari 37 produk.
International Brands
  • Balminil
  • Otriven
  • Otrivin
  • Otrivine
  • Otrix
  • Xylomet
  • Xylostar — Intas

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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