Peringatan Keamanan

Overdosage of intranasal or ophthalmic azelastine is unlikely to result in clinically significant adverse effects aside from increased drowsiness.L8240,L8270 If overdose does occur, employ general supportive measures. Oral ingestion of antihistamines, including non-oral formulations of azelastine, can cause serious adverse effects in children - for this reason, these products should be kept out of the reach of children. The oral LD50 in rats is 580 mg/kg.L8276

Azelastine

DB00972

small molecule approved

Deskripsi

Azelastine, a phthalazine derivative, is an antihistamine available as an intranasal spray for the treatment of allergic and vasomotor rhinitis and as an ophthalmic solution for the treatment of allergic conjunctivitis.L8240,L8270 It is a racemic mixture, though there is no noted difference in pharmacologic activity between enantiomers, and was first granted FDA approval in 1996.L8240,L8270 Azelastine is also available in combination with fluticasone propionate as a nasal spray marketed under the trade name Dymista™, which is indicated for the symptomatic treatment of seasonal allergic rhinitis in patients 6 years of age and older.L8309

Struktur Molekul 2D

Berat 381.898
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Based on intravenous and oral administration, azelastine demonstrated an elimination half-life of 22 hours.[L8240,L8270] Its primary active metabolite, desmethylazelastine, has an elimination half-life of 54 hours.[A1518]
Volume Distribusi After intravenous and oral administration, the steady-state volume of distribution is 14.5 L/kg.[A1518,L8240,L8270]
Klirens (Clearance) Based on intravenous and oral administration, azelastine demonstrated a plasma clearance of 0.5 L/h/kg.[L8240,L8270,A184232]

Absorpsi

Systemic bioavailability of azelastine hydrochloride following intranasal administration is approximately 40%, reaching Cmax within 2-3 hours.A1518 When administered at doses greater than the recommended maximum, greater than proportional increases in both Cmax and AUC were observed.

Metabolisme

Azelastine hydrochloride is oxidatively metabolized to its main, and biologically active, metabolite desmethylazelastine by the cytochrome P450 enzyme system.L8240,L8270 Though labels for azelastine state that specific CYP enzyme involvement has not been elucidated, it has been suggested that the N-demethylation of azelastine is primarily catalyzed by CYP3A4, CYP2D6, and CYP1A2.A38655

Rute Eliminasi

After an oral dose of radio-labeled azelastine hydrochloride, approximately 75% was excreted in the feces, with less than 10% as unchanged azelastine hydrochloride.A1518,L8240,L8270

Interaksi Makanan

1 Data
  • 1. Avoid alcohol. Ingesting alcohol may cause additive CNS depressant effects.

Interaksi Obat

1396 Data
Cilostazol The metabolism of Cilostazol can be decreased when combined with Azelastine.
Deferasirox The serum concentration of Azelastine can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Azelastine can be increased when it is combined with Peginterferon alfa-2b.
Teriflunomide The serum concentration of Azelastine can be decreased when it is combined with Teriflunomide.
Leflunomide The serum concentration of Azelastine can be decreased when it is combined with Leflunomide.
Metyrosine Azelastine may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Pramipexole Azelastine may increase the sedative activities of Pramipexole.
Ropinirole Azelastine may increase the sedative activities of Ropinirole.
Thalidomide Azelastine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Eliglustat The metabolism of Azelastine can be decreased when combined with Eliglustat.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Azelastine.
Fentanyl Fentanyl may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Vardenafil The metabolism of Azelastine can be decreased when combined with Vardenafil.
Lovastatin The metabolism of Azelastine can be decreased when combined with Lovastatin.
Benzylpenicilloyl polylysine Azelastine may decrease effectiveness of Benzylpenicilloyl polylysine as a diagnostic agent.
Betahistine The therapeutic efficacy of Betahistine can be decreased when used in combination with Azelastine.
Hyaluronidase (ovine) The therapeutic efficacy of Hyaluronidase (ovine) can be decreased when used in combination with Azelastine.
Hyaluronidase (human recombinant) The therapeutic efficacy of Hyaluronidase (human recombinant) can be decreased when used in combination with Azelastine.
Hyaluronidase The therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Azelastine.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Azelastine.
Mifepristone The serum concentration of Azelastine can be increased when it is combined with Mifepristone.
Atomoxetine The metabolism of Azelastine can be decreased when combined with Atomoxetine.
(R)-warfarin The metabolism of (R)-warfarin can be decreased when combined with Azelastine.
(S)-Warfarin The metabolism of (S)-Warfarin can be decreased when combined with Azelastine.
Acenocoumarol The metabolism of Acenocoumarol can be decreased when combined with Azelastine.
Warfarin The metabolism of Azelastine can be decreased when combined with Warfarin.
Tacrolimus The metabolism of Tacrolimus can be decreased when combined with Azelastine.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Azelastine.
Mirabegron The serum concentration of Azelastine can be increased when it is combined with Mirabegron.
Abiraterone The serum concentration of Azelastine can be increased when it is combined with Abiraterone.
Cyproterone acetate The metabolism of Azelastine can be increased when combined with Cyproterone acetate.
Ethanol Azelastine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Botulinum toxin type B Botulinum toxin type B may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Botulinum toxin type A Botulinum toxin type A may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Tryptophan Tryptophan may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Fluvoxamine Fluvoxamine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Baclofen Baclofen may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Lorazepam Lorazepam may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Ethchlorvynol Ethchlorvynol may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Tramadol Tramadol may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Succinylcholine Succinylcholine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Reserpine Reserpine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Citalopram Citalopram may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Eletriptan Eletriptan may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Enflurane Enflurane may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Pregabalin Pregabalin may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Temazepam Temazepam may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Reboxetine Reboxetine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Butabarbital Butabarbital may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Butalbital Butalbital may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Ziprasidone Ziprasidone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Methysergide Methysergide may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Cabergoline Cabergoline may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Phenytoin Phenytoin may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Topiramate Topiramate may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Clemastine Clemastine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Venlafaxine Venlafaxine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Etomidate Etomidate may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Morphine Morphine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Talbutal Talbutal may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Pentobarbital Pentobarbital may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Valproic acid Valproic acid may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Zolmitriptan Zolmitriptan may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Codeine Codeine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Dihydroergotamine Dihydroergotamine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Amitriptyline Amitriptyline may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Tolcapone Tolcapone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Hydromorphone Hydromorphone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Olanzapine Olanzapine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Cetirizine Cetirizine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Protriptyline Protriptyline may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Trimethadione Trimethadione may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Clobazam Clobazam may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Chlorzoxazone Chlorzoxazone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Clozapine Clozapine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Mirtazapine Mirtazapine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Meprobamate Meprobamate may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Thiethylperazine Thiethylperazine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Palonosetron Palonosetron may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Sulpiride Sulpiride may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Carisoprodol Carisoprodol may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Eszopiclone Eszopiclone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Alprazolam Alprazolam may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Dexbrompheniramine Dexbrompheniramine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Loxapine Loxapine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Remoxipride Remoxipride may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Metocurine iodide Metocurine iodide may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Secobarbital Secobarbital may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Promazine Promazine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Methocarbamol Methocarbamol may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Zolpidem Zolpidem may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Triprolidine Triprolidine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Prochlorperazine Prochlorperazine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Cyproheptadine Cyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Meperidine Meperidine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Imipramine Imipramine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Metharbital Metharbital may increase the central nervous system depressant (CNS depressant) activities of Azelastine.

Target Protein

Histamine H1 receptor HRH1
Histamine H2 receptor HRH2
Phospholipase A2 PLA2G1B
Leukotriene C4 synthase LTC4S

Referensi & Sumber

Synthesis reference: Yutaka Morita, Noritoshi Koyama, Shigemitsu Ohsawa, "Methods employing stable preparation containing azelastine hydrochloride." U.S. Patent US6117864, issued December 1990.
Artikel (PubMed)
  • PMID: 19209282
    Horak F: Effectiveness of twice daily azelastine nasal spray in patients with seasonal allergic rhinitis. Ther Clin Risk Manag. 2008 Oct;4(5):1009-22.
  • PMID: 17723160
    Bernstein JA: Azelastine hydrochloride: a review of pharmacology, pharmacokinetics, clinical efficacy and tolerability. Curr Med Res Opin. 2007 Oct;23(10):2441-52.
  • PMID: 22954967
    Zha W, Shum L: Simultaneous determination of azelastine and its major metabolite desmethylazelastine in human plasma using high performance liquid chromatography-tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2012 Oct 1;906:69-74. doi: 10.1016/j.jchromb.2012.08.023. Epub 2012 Aug 24.
  • PMID: 10570018
    Nakajima M, Nakamura S, Tokudome S, Shimada N, Yamazaki H, Yokoi T: Azelastine N-demethylation by cytochrome P-450 (CYP)3A4, CYP2D6, and CYP1A2 in human liver microsomes: evaluation of approach to predict the contribution of multiple CYPs. Drug Metab Dispos. 1999 Dec;27(12):1381-91.
  • PMID: 10383922
    Nakajima M, Ohyama K, Nakamura S, Shimada N, Yamazaki H, Yokoi T: Inhibitory effects of azelastine and its metabolites on drug oxidation catalyzed by human cytochrome P-450 enzymes. Drug Metab Dispos. 1999 Jul;27(7):792-7.
  • PMID: 20856595
    Williams PB, Crandall E, Sheppard JD: Azelastine hydrochloride, a dual-acting anti-inflammatory ophthalmic solution, for treatment of allergic conjunctivitis. Clin Ophthalmol. 2010 Sep 7;4:993-1001. doi: 10.2147/opth.s13479.
  • PMID: 27885525
    Fukui H, Mizuguchi H, Nemoto H, Kitamura Y, Kashiwada Y, Takeda N: Histamine H1 Receptor Gene Expression and Drug Action of Antihistamines. Handb Exp Pharmacol. 2017;241:161-169. doi: 10.1007/164201614.
  • PMID: 11291777
    Baroody FM, Naclerio RM: Antiallergic effects of H1-receptor antagonists. Allergy. 2000;55 Suppl 64:17-27.
Menampilkan 8 dari 9 artikel.

Contoh Produk & Brand

Produk: 70 • International brands: 1
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International Brands
  • Astepro Allergy — Bayer

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