Peringatan Keamanan

In rats, the oral LD50 is 680 ug/kg and the subcutaneous LD50 is 1630 ug/kg. In mice, the oral LD50 is 4700 ug/kg, the intraperitoneal LD50 is 48 mg/kg, and the subcutaneous LD50 is 34 mg/kg.L15077

Case reports have documented unintended overdose in both children and adults: overdose has led to dizziness, chest pain, headaches, myocardial infarction, stroke, visual disturbances, arrhythmia, hypertension, or hypotension.L15057 Accidental ingestion of topical solutions of imidazoline derivatives, including oxymetazoline, in children has resulted in serious adverse events requiring hospitalization, such as nausea, vomiting, lethargy, tachycardia, decreased respiration, bradycardia, hypotension, hypertension, sedation, somnolence, mydriasis, stupor, hypothermia, drooling, and coma.L15062, L15067 Possible rebound nasal congestion, irritation of nasal mucosa, and adverse systemic effects (particularly in children), including serious cardiovascular adverse events, have been reported with overdosage as well as prolonged or too frequent intranasal use of oxymetazoline.L15057 Overdose should be responded with close monitoring, supportive care, and symptomatic treatment.L15057, L15062, L15067

Oxymetazoline

DB00935

small molecule approved investigational

Deskripsi

Oxymetazoline is an imidazole derivative and a potent, direct-acting alpha (?)-adrenergic agonist with affinity to both ?1- and ?2-adrenoceptors.A215542 Oxymetazoline is available in various formulations with a wide variety of clinical implications. The topical formulation of the drug is used to treat persistent facial redness in adults.L15062 As an effective decongestant, oxymetazoline is available in over-the-counter intranasal sprays used to relieve nasal and sinus congestion caused by a wide variety of conditions, such as common cold, hay fever, and upper respiratory allergies.A215587, L15092 In dentistry, oxymetazoline and tetracaine combination intranasal spray (Kovanaze) is used for regional anesthesia during dental procedures in children and adults.L15057 In July 2020, the FDA approved the use of an ophthalmic formulation of oxymetazoline (Upneeq) in adults with acquired blepharoptosis, or ptosis, making it the first FDA-approved medical treatment for this medical condition.L15042, L15067

Struktur Molekul 2D

Berat 260.3746
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Following ocular administration in healthy adults, the mean terminal half-life was 8.3 hours, ranging from 5.6 to 13.9 hours.[L15067] The terminal half-life of oxymetazoline following nasal administration of the combination product containing tetracaine and oxymetazoline in adult subjects is approximately 5.2 hours.[L15057]
Volume Distribusi There is limited information on the volume of distribution of oxymetazoline.
Klirens (Clearance) There is limited information on the clearance rate of oxymetazoline.

Absorpsi

Imidazole derivatives such as oxymetazoline are readily absorbed across mucosal membranes, especially in children.A215542 In adult subjects with erythema associated with rosacea, the mean ± standard deviation (SD) Cmax was 60.5 ± 53.9 pg/mL and the AUC from time 0 to 24 hours (AUC0-24hr) was 895 ±798 pg x hr/mL following topical administration of first-dose oxymetazoline. Following once-daily topical applications for 28 days, the mean ± SD Cmax was 66.4 ± 67.1 pg/mL and the AUC0-24hr was 1050 ± 992 pg x hr/mL. Following twice-daily applications for 28 days, the mean ± SD Cmax was 68.8 ± 61.1 pg/mL and the AUC0-24hr was 1530 ± 922 pg x hr/mL.L15062 Following single-drop ocular administration of oxymetazoline in healthy adult subjects, the mean ± SD Cmax was 30.5 ± 12.7 pg/mL and the area under the concentration-time curve (AUCinf) was 468 ± 214 pg x hr/mL. The median Tmax was 2 hours, ranging from 0.5 to 12 hours.L15067 Following nasal administration of an 0.6 mL combination product containing tetracaine and oxymetazoline in adult subjects, the maximum concentrations of oxymetazoline were reached within approximately 10 minutes. The mean Cmax was 1.78 ng/mL and the AUC0-inf value was 4.24 ng x h/mL, with a median Tmax of 5 minutes.L15057

Metabolisme

In vitro, oxymetazoline was minimally metabolized by human liver enzymes to produce mono-oxygenated and dehydrogenated metabolites. About 95.9% of the total dose of oxymetazoline remained as an unchanged parent compound after a 120-minute incubation with human liver microsomes.L15062, L15067 When incubated in rat, rabbit, and human liver post-mitochondrial supernatant fraction from homogenized tissue (S9) fractions, oxymetazoline was more efficiently metabolized by rabbit liver S9 fractions (~65%) than by rat (~20%) or human (~10%) liver S9 fractions. At concentrations (50 ?M) at least 130-fold greater than the usual therapeutic intranasal dose (400 nM), CYP2C19 was suggested to be involved in the oxidation of oxymetazoline following intranasal administration; however, metabolites in humans have not been fully characterized up to date and remain speculated based on in vitro studies using rat and rabbit liver S9 fractions and microsomes.A17771 The O-glucuronide metabolite catalyzed by UGT1A9 has been identified in vitro.A226535, L15057

Rute Eliminasi

While the excretion of oxymetazoline following nasal, topical, or ophthalmic administration of oxymetazoline has not been fully characterized in humans, it is believed that the predominant route of elimination at clinically relevant concentrations of oxymetazoline is renal excretion.L15057

Interaksi Obat

786 Data
Nitroprusside Oxymetazoline may decrease the antihypertensive activities of Nitroprusside.
Fenoldopam Oxymetazoline may decrease the antihypertensive activities of Fenoldopam.
Epoprostenol Oxymetazoline may decrease the antihypertensive activities of Epoprostenol.
Enalaprilat Oxymetazoline may decrease the antihypertensive activities of Enalaprilat.
Vincamine Oxymetazoline may decrease the antihypertensive activities of Vincamine.
Atomoxetine The risk or severity of hypertension can be increased when Atomoxetine is combined with Oxymetazoline.
Linezolid The risk or severity of hypertension can be increased when Linezolid is combined with Oxymetazoline.
Benzylpenicilloyl polylysine Oxymetazoline 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 Oxymetazoline.
Cyclosporine The risk or severity of hypertension can be increased when Cyclosporine is combined with Oxymetazoline.
Icosapent The risk or severity of hypertension can be increased when Icosapent is combined with Oxymetazoline.
Eletriptan The risk or severity of hypertension can be increased when Eletriptan is combined with Oxymetazoline.
Isoetharine The risk or severity of hypertension can be increased when Isoetharine is combined with Oxymetazoline.
Mesalazine The risk or severity of hypertension can be increased when Mesalazine is combined with Oxymetazoline.
Etomidate The risk or severity of hypertension can be increased when Etomidate is combined with Oxymetazoline.
Zolmitriptan The risk or severity of hypertension can be increased when Zolmitriptan is combined with Oxymetazoline.
Indomethacin The risk or severity of hypertension can be increased when Indomethacin is combined with Oxymetazoline.
Methylphenidate The risk or severity of hypertension can be increased when Methylphenidate is combined with Oxymetazoline.
Nabumetone The risk or severity of hypertension can be increased when Nabumetone is combined with Oxymetazoline.
Ketorolac The risk or severity of hypertension can be increased when Ketorolac is combined with Oxymetazoline.
Tenoxicam The risk or severity of hypertension can be increased when Tenoxicam is combined with Oxymetazoline.
Celecoxib The risk or severity of hypertension can be increased when Celecoxib is combined with Oxymetazoline.
Buspirone The risk or severity of hypertension can be increased when Buspirone is combined with Oxymetazoline.
Tolmetin The risk or severity of hypertension can be increased when Tolmetin is combined with Oxymetazoline.
Rofecoxib The risk or severity of hypertension can be increased when Rofecoxib is combined with Oxymetazoline.
Piroxicam The risk or severity of hypertension can be increased when Piroxicam is combined with Oxymetazoline.
Doxapram The risk or severity of hypertension can be increased when Doxapram is combined with Oxymetazoline.
Atropine The risk or severity of hypertension can be increased when Atropine is combined with Oxymetazoline.
Fenoprofen The risk or severity of hypertension can be increased when Fenoprofen is combined with Oxymetazoline.
Valdecoxib The risk or severity of hypertension can be increased when Valdecoxib is combined with Oxymetazoline.
Diclofenac The risk or severity of hypertension can be increased when Diclofenac is combined with Oxymetazoline.
Sulindac The risk or severity of hypertension can be increased when Sulindac is combined with Oxymetazoline.
Dexmedetomidine The risk or severity of hypertension can be increased when Dexmedetomidine is combined with Oxymetazoline.
Sumatriptan The risk or severity of hypertension can be increased when Sumatriptan is combined with Oxymetazoline.
Sufentanil The risk or severity of hypertension can be increased when Sufentanil is combined with Oxymetazoline.
Flurbiprofen The risk or severity of hypertension can be increased when Flurbiprofen is combined with Oxymetazoline.
Etodolac The risk or severity of hypertension can be increased when Etodolac is combined with Oxymetazoline.
Isoflurane The risk or severity of hypertension can be increased when Isoflurane is combined with Oxymetazoline.
Mefenamic acid The risk or severity of hypertension can be increased when Mefenamic acid is combined with Oxymetazoline.
Naproxen The risk or severity of hypertension can be increased when Naproxen is combined with Oxymetazoline.
Sulfasalazine The risk or severity of hypertension can be increased when Sulfasalazine is combined with Oxymetazoline.
Alfentanil The risk or severity of hypertension can be increased when Alfentanil is combined with Oxymetazoline.
Phenylbutazone The risk or severity of hypertension can be increased when Phenylbutazone is combined with Oxymetazoline.
Meloxicam The risk or severity of hypertension can be increased when Meloxicam is combined with Oxymetazoline.
Propofol The risk or severity of hypertension can be increased when Propofol is combined with Oxymetazoline.
Carprofen The risk or severity of hypertension can be increased when Carprofen is combined with Oxymetazoline.
Diflunisal The risk or severity of hypertension can be increased when Diflunisal is combined with Oxymetazoline.
Remifentanil The risk or severity of hypertension can be increased when Remifentanil is combined with Oxymetazoline.
Bitolterol The risk or severity of hypertension can be increased when Bitolterol is combined with Oxymetazoline.
Almotriptan The risk or severity of hypertension can be increased when Almotriptan is combined with Oxymetazoline.
Salicylic acid The risk or severity of hypertension can be increased when Oxymetazoline is combined with Salicylic acid.
Salmeterol The risk or severity of hypertension can be increased when Oxymetazoline is combined with Salmeterol.
Meclofenamic acid The risk or severity of hypertension can be increased when Oxymetazoline is combined with Meclofenamic acid.
Acetylsalicylic acid The risk or severity of hypertension can be increased when Oxymetazoline is combined with Acetylsalicylic acid.
Naratriptan The risk or severity of hypertension can be increased when Oxymetazoline is combined with Naratriptan.
Rizatriptan The risk or severity of hypertension can be increased when Oxymetazoline is combined with Rizatriptan.
Oxaprozin The risk or severity of hypertension can be increased when Oxymetazoline is combined with Oxaprozin.
Frovatriptan The risk or severity of hypertension can be increased when Oxymetazoline is combined with Frovatriptan.
Albuterol The risk or severity of hypertension can be increased when Oxymetazoline is combined with Salbutamol.
Ketoprofen The risk or severity of hypertension can be increased when Oxymetazoline is combined with Ketoprofen.
Balsalazide The risk or severity of hypertension can be increased when Oxymetazoline is combined with Balsalazide.
Methoxyflurane The risk or severity of hypertension can be increased when Oxymetazoline is combined with Methoxyflurane.
Ibuprofen The risk or severity of hypertension can be increased when Oxymetazoline is combined with Ibuprofen.
Arbutamine The risk or severity of hypertension can be increased when Oxymetazoline is combined with Arbutamine.
Dutasteride The risk or severity of hypertension can be increased when Oxymetazoline is combined with Dutasteride.
Halothane The risk or severity of hypertension can be increased when Oxymetazoline is combined with Halothane.
Desflurane The risk or severity of hypertension can be increased when Oxymetazoline is combined with Desflurane.
Finasteride The risk or severity of hypertension can be increased when Oxymetazoline is combined with Finasteride.
Sevoflurane The risk or severity of hypertension can be increased when Oxymetazoline is combined with Sevoflurane.
Arformoterol The risk or severity of hypertension can be increased when Oxymetazoline is combined with Arformoterol.
Lumiracoxib The risk or severity of hypertension can be increased when Oxymetazoline is combined with Lumiracoxib.
Pirbuterol The risk or severity of hypertension can be increased when Oxymetazoline is combined with Pirbuterol.
Ephedra sinica root The risk or severity of hypertension can be increased when Oxymetazoline is combined with Ephedra sinica root.
Yohimbine The risk or severity of hypertension can be increased when Oxymetazoline is combined with Yohimbine.
Magnesium salicylate The risk or severity of hypertension can be increased when Oxymetazoline is combined with Magnesium salicylate.
Salsalate The risk or severity of hypertension can be increased when Oxymetazoline is combined with Salsalate.
Choline magnesium trisalicylate The risk or severity of hypertension can be increased when Oxymetazoline is combined with Choline magnesium trisalicylate.
Bambuterol The risk or severity of hypertension can be increased when Oxymetazoline is combined with Bambuterol.
Antrafenine The risk or severity of hypertension can be increased when Oxymetazoline is combined with Antrafenine.
Aminophenazone The risk or severity of hypertension can be increased when Oxymetazoline is combined with Aminophenazone.
Antipyrine The risk or severity of hypertension can be increased when Oxymetazoline is combined with Antipyrine.
Solifenacin The risk or severity of hypertension can be increased when Oxymetazoline is combined with Solifenacin.
Tiaprofenic acid The risk or severity of hypertension can be increased when Oxymetazoline is combined with Tiaprofenic acid.
Etoricoxib The risk or severity of hypertension can be increased when Oxymetazoline is combined with Etoricoxib.
Epicaptopril The risk or severity of hypertension can be increased when Oxymetazoline is combined with Epicaptopril.
Taxifolin The risk or severity of hypertension can be increased when Oxymetazoline is combined with Taxifolin.
Oxyphenbutazone The risk or severity of hypertension can be increased when Oxymetazoline is combined with Oxyphenbutazone.
1-benzylimidazole The risk or severity of hypertension can be increased when Oxymetazoline is combined with 1-benzylimidazole.
Nimesulide The risk or severity of hypertension can be increased when Oxymetazoline is combined with Nimesulide.
Benoxaprofen The risk or severity of hypertension can be increased when Oxymetazoline is combined with Benoxaprofen.
Metamizole The risk or severity of hypertension can be increased when Oxymetazoline is combined with Metamizole.
Zomepirac The risk or severity of hypertension can be increased when Oxymetazoline is combined with Zomepirac.
Flibanserin The risk or severity of hypertension can be increased when Oxymetazoline is combined with Flibanserin.
Indacaterol The risk or severity of hypertension can be increased when Oxymetazoline is combined with Indacaterol.
Cimicoxib The risk or severity of hypertension can be increased when Oxymetazoline is combined with Cimicoxib.
Rotigotine The risk or severity of hypertension can be increased when Oxymetazoline is combined with Rotigotine.
Amibegron The risk or severity of hypertension can be increased when Oxymetazoline is combined with Amibegron.
Naluzotan The risk or severity of hypertension can be increased when Oxymetazoline is combined with Naluzotan.
Cariprazine The risk or severity of hypertension can be increased when Oxymetazoline is combined with Cariprazine.
Solabegron The risk or severity of hypertension can be increased when Oxymetazoline is combined with Solabegron.

Target Protein

Alpha-1A adrenergic receptor ADRA1A
Alpha-2A adrenergic receptor ADRA2A
Alpha-2B adrenergic receptor ADRA2B
Alpha-2C adrenergic receptor ADRA2C
Alpha-1B adrenergic receptor ADRA1B
Alpha-1D adrenergic receptor ADRA1D
5-hydroxytryptamine receptor 1A HTR1A
5-hydroxytryptamine receptor 1B HTR1B
5-hydroxytryptamine receptor 1D HTR1D
5-hydroxytryptamine receptor 2C Htr2c

Referensi & Sumber

Artikel (PubMed)
  • PMID: 25039870
    Tobias JD, Cartabuke R, Taghon T: Oxymetazoline (Afrin(R)): maybe there is more that we need to know. Paediatr Anaesth. 2014 Aug;24(8):795-8. doi: 10.1111/pan.12399.
  • PMID: 8250339
    Sisk AL: Vasoconstrictors in local anesthesia for dentistry. Anesth Prog. 1992;39(6):187-93.
  • PMID: 14579657
    Watanabe H, Foo TH, Djazaeri B, Duncombe P, Mackay IS, Durham SR: Oxymetazoline nasal spray three times daily for four weeks in normal subjects is not associated with rebound congestion or tachyphylaxis. Rhinology. 2003 Sep;41(3):167-74.
  • PMID: 3950497
    Bende M, Loth S: Vascular effects of topical oxymetazoline on human nasal mucosa. J Laryngol Otol. 1986 Mar;100(3):285-8. doi: 10.1017/s0022215100099151.
  • 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: 21177487
    Mahajan MK, Uttamsingh V, Daniels JS, Gan LS, LeDuc BW, Williams DA: In vitro metabolism of oxymetazoline: evidence for bioactivation to a reactive metabolite. Drug Metab Dispos. 2011 Apr;39(4):693-702. doi: 10.1124/dmd.110.036004. Epub 2010 Dec 21.
  • PMID: 20669329
    Mahajan MK, Uttamsingh V, Gan LS, Leduc B, Williams DA: Identification and characterization of oxymetazoline glucuronidation in human liver microsomes: evidence for the involvement of UGT1A9. J Pharm Sci. 2011 Feb;100(2):784-93. doi: 10.1002/jps.22303.
  • PMID: 28837365
    Patel NU, Shukla S, Zaki J, Feldman SR: Oxymetazoline hydrochloride cream for facial erythema associated with rosacea. Expert Rev Clin Pharmacol. 2017 Oct;10(10):1049-1054. doi: 10.1080/17512433.2017.1370370. Epub 2017 Aug 24.
Menampilkan 8 dari 14 artikel.

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Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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