Peringatan Keamanan

The Lowest published toxic dose (TDLo) of tetryzoline in children following oral administration is 175 mg/kg. Oral LD50 is 785 mg/kg in rats and 345 mg/kg in mice. Intraperitoneal LD50 is 122 mg/kg in rats and 110 mg/kg in mice. Subcutaneous LD50 is 500 mg/kg in rats.L32609

Overdose following accidental oral ingestion in children may lead to profound sedation, possibly accompanied by profuse sweating, hypotension, and shock. In adults, hypertension, bradycardia, drowsiness, and rebound hypotension may be observed, in addition to a shock-like syndrome with hypotension and bradycardia.L32599 In one case, cardiovascular effects persisted for 36 hours after unintentional ingestion of tetrahydrozoline.A7045 Profound sedation has occurred in adults following accidental oral ingestion due to poisoning.A231764

Overdose should be managed with supportive treatment, with the patient kept warm. Fluid maintenance therapy may be initiated if necessary. The respiratory rate dropping to 10 or below should be responded with oxygen therapy and respiratory assistance. Blood pressure should be carefully monitored to prevent a hypotensive crisis.L32599 There is no known antidote to tetryzoline overdose; however, one case report illustrates the successful use of naloxone in reversing the clinical signs and symptoms of tetryzoline overdose in a child. Naloxone has been used to revere clonidine overdose. The exact mechanism of action of naloxone as an antidote is not fully understood; however, it is understood that clonidine and tetryzoline work to inhibit central sympathetic outflow by activating alpha-2 adrenoceptors and inducing endogenous opiate release, which naloxone works to antagonize.A231779

Tetryzoline

DB06764

small molecule approved

Deskripsi

Tetryzoline, also known as tetrahydrozoline, is a derivative of imidazoline with central and peripheral alpha (?)-adrenergic properties.A231769 Available since the 1950s, tetryzoline is a selective ?1-receptor agonist A231774 that is used as an ocular and nasal decongestant. Tetryzoline is found in a wide array of over-the-counter eye drops, including the most common brand, Visine.L32579 Tetryzoline is also found in combination products with other lubricants and anti-irritants, such as povidone, polyethylene glycol 400, dextran, and zinc sulfate.L32584, L32589, L32594 It is also used in combination with other drug classes, such as antihistamines, corticosteroids, and glucocorticoids in other countries. Tetryzoline is also found in nasal spray under the trade name Tyzine, which is used for decongestion of nasal and nasopharyngeal mucosa.L32599

As it causes profound sedation in children and adults, tetryzoline is increasingly becoming scrutinized for possible drug overdose and toxicity from accidental ingestion.A7045, A231769 It has also been misused for non-therapeutic purposes as a causative drug for several cases of drug-facilitated sexual assault.A231764

Struktur Molekul 2D

Berat 200.285
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Following ocular administration of 0.05% tetryzoline, the mean serum half-life was approximately 6 hours.[A7044]
Volume Distribusi No information is available.
Klirens (Clearance) No information is available.

Absorpsi

When consumed orally, tetryzoline is rapidly absorbed from the gastrointestinal tract and can cross the blood-brain barrier.A231764 Following ocular administration of 0.05% tetryzoline, Cmax ranged from 0.068 to 0.380 ng/mL.A7044

Metabolisme

No information is available.

Rute Eliminasi

Following ocular administration of 0.05% tetryzoline, tetryzoline was detected in urine at 24 hours.A7044

Interaksi Obat

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

Target Protein

Alpha-1 adrenergic receptors ADRA1A
Alpha-2C adrenergic receptor ADRA2C
Alpha-2 adrenergic receptors ADRA2A

Referensi & Sumber

Artikel (PubMed)
  • PMID: 21972870
    Carr ME, Engebretsen KM, Ho B, Anderson CP: Tetrahydrozoline (Visine(R)) concentrations in serum and urine during therapeutic ocular dosing: a necessary first step in determining an overdose. Clin Toxicol (Phila). 2011 Nov;49(9):810-4. doi: 10.3109/15563650.2011.615064. Epub 2011 Oct 5.
  • PMID: 18259967
    Spiller H, Griffith J: Prolonged cardiovascular effects after unintentional ingestion of tetrahydrozoline. Clin Toxicol (Phila). 2008 Feb;46(2):171-2. doi: 10.1080/15563650701258070.
  • PMID: 22554870
    Stillwell ME, Saady JJ: Use of tetrahydrozoline for chemical submission. Forensic Sci Int. 2012 Sep 10;221(1-3):e12-6. doi: 10.1016/j.forsciint.2012.04.004. Epub 2012 May 1.
  • PMID: 12882493
    Daggy A, Kaplan R, Roberge R, Akhtar J: Pediatric Visine (tetrahydrozoline) ingestion: case report and review of imidazoline toxicity. Vet Hum Toxicol. 2003 Aug;45(4):210-2.
  • PMID: 32801982
    Hosten LO, Snyder C: Over-the-Counter Ocular Decongestants in the United States - Mechanisms of Action and Clinical Utility for Management of Ocular Redness. Clin Optom (Auckl). 2020 Jul 23;12:95-105. doi: 10.2147/OPTO.S259398. eCollection 2020.
  • PMID: 10389957
    Holmes JF, Berman DA: Use of naloxone to reverse symptomatic tetrahydrozoline overdose in a child. Pediatr Emerg Care. 1999 Jun;15(3):193-4. doi: 10.1097/00006565-199906000-00008.
  • 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: 7507588
    Johnson DA, Hricik JG: The pharmacology of alpha-adrenergic decongestants. Pharmacotherapy. 1993 Nov-Dec;13(6 Pt 2):110S-115S; discussion 143S-146S.

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