Peringatan Keamanan

Based on the findings of an acute toxicity study in animals, the oral LD50 of olopatadine was >1150 mg/kg in mice and >3870 mg/kg in rats.L6790 The Lowest published toxic dose via the oral route was 20 mg/kg in rat and 0.1 mg/kg in mouse.MSDS

There are no known reports on overdosage following oral, ophthalmic, or intranasal administration of olopatadine. Likely symptoms of antihistamine overdose may include drowsiness in adults and, initially, agitation and restlessness, followed by drowsiness in children. In case of suspected overdose, supportive and symptomatic treatment is recommended.L6784

Olopatadine

DB00768

small molecule approved

Deskripsi

Olopatadine is a selective histamine H1 antagonist and mast cell stabilizer that works by attenuating inflammatory and allergic reactions. It is a structural analog of doxepin, which has a minimal anti-allergic activity.L6790 Olopatadine works by blocking the effects of histamine, which is a primary inflammatory mediator that causes inflammatory and allergic reactions. An ophthalmic solution of olopatadine was approved by the FDA and European Union for the treatment of seasonal and perennial allergic conjunctivitis in 1996 and 2002, respectively.A1172 In comparison to other anti-allergenic ophthalmic medications, olopatadine displays a good comfort and tolerability profile since it does not cause perturbation of cell membranes.A179809 Olopatadine is used for the symptomatic treatment of ocular itching associated with allergic conjunctivitis in ophthalmic formulations and seasonal allergic rhinitis in intranasal formulations. It is currently marketed under several brand names, including Pazeo, Patanase, and Opatanol.

Struktur Molekul 2D

Berat 337.4122
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, the elimination half-life of olopatadine was 3.4 ± 1.2 hours. In oral pharmacokinetics study, the elimination half-life was reported to be 8 to 12 hours.[L6787]
Volume Distribusi In an open-label study consisting of healthy Chinese subjects receiving oral administration of olopatadine, the mean apparent volume of distribution was 133.83 L.[A179740]
Klirens (Clearance) In an open-label study consisting of healthy Chinese subjects receiving oral administration of olopatadine, the mean apparent oral clearance (CL/F) was 23.45 L/h.[A179740]

Absorpsi

Ocular administration of olopatadine in healthy subjects resulted in the Cmax of 1.6 ± 0.9 ng/mL, which was reached after about 2.0 hours. The AUC was 9.7 ± 4.4 ngxh/mL.L6781 The average absolute bioavaiability of intranasal olopatadine is about 57%. Following intranasal administration in healthy subjects, the Cmax of 6.0 ± 8.99 ng/mL at steady-state was reached between 30 minutes to 1 hour after twice daily intranasal administration. The average AUC was 66.0 ± 26.8 ng·h/mL. In patients with seasonal allergic rhinitis, the Cmax of 23.3 ± 6.2 ng/mL at steady-state was reached between 15 minutes and 2 hours post-dosing and the average AUC was 78.0 ± 13.9 ng·h/mL.L6784

Metabolisme

Olopatadine undergoes hepatic metabolism in a non-extensive manner.L6784,L6787 Based on oral pharmacokinetic studies, there are at least 6 circulating metabolites in human plasma.L6784 Following topical ocular application of olopatadine, olopatadine N-oxide is formed by metabolism catalyzed by flavin-containing monooxygenase (FMO) 1 and 3 L6784 and was detected in the plasma after 4 hours post-dosing in less than 10% of the total plasma in half of the patients.L6781 Mono-desmethyl olopatadine, or N-desmethyl olopatadine, is formed by CYP3A4 L6784 and may be detected in minimal levels.L6781

Rute Eliminasi

Olopatadine is mainly eliminated through urinary excretion. Following oral administration, about 70% and 17% of the total dose was recovered in the urine and feces, respectively.L6784

Interaksi Obat

1 Data
Oxymetazoline The absorption of Olopatadine can be decreased when combined with Oxymetazoline.

Target Protein

Histamine H1 receptor HRH1
Histamine H2 receptor HRH2
Histamine H3 receptor HRH3
Protein S100-A1 S100A1
Protein S100-A12 S100A12
Protein S100-B S100B
Protein S100-A13 S100A13
Protein S100-A2 S100A2

Referensi & Sumber

Synthesis reference: Thomas Bader, Hans-Ulrich Bichsel, Bruno Gilomen, Imelda Meyer-Wilmes, Mark Sundermeier, "Polymorphic forms of olopatadine hydrochloride and methods for producing olopatadine and salts thereof." U.S. Patent US20070232814, issued October 04, 2007.
Artikel (PubMed)
  • PMID: 12046981
    Ohmori K, Hayashi K, Kaise T, Ohshima E, Kobayashi S, Yamazaki T, Mukouyama A: Pharmacological, pharmacokinetic and clinical properties of olopatadine hydrochloride, a new antiallergic drug. Jpn J Pharmacol. 2002 Apr;88(4):379-97.
  • PMID: 15646365
    Ohmori K, Hasegawa K, Tamura T, Miyake K, Matsubara M, Masaki S, Karasawa A, Urayama N, Horikoshi K, Kajita J, Hasegawa M, Taniguchi K, Komada T, Kawamoto Y: Properties of olopatadine hydrochloride, a new antiallergic/antihistaminic drug. Arzneimittelforschung. 2004;54(12):809-29.
  • PMID: 16197656
    Rosenwasser LJ, O'Brien T, Weyne J: Mast cell stabilization and anti-histamine effects of olopatadine ophthalmic solution: a review of pre-clinical and clinical research. Curr Med Res Opin. 2005 Sep;21(9):1377-87. doi: 10.1185/030079905X56547.
  • PMID: 30224900
    Branco ACCC, Yoshikawa FSY, Pietrobon AJ, Sato MN: Role of Histamine in Modulating the Immune Response and Inflammation. Mediators Inflamm. 2018 Aug 27;2018:9524075. doi: 10.1155/2018/9524075. eCollection 2018.
  • PMID: 19499962
    Chu NN, Chen WL, Xu HR, Li XN: Pharmacokinetics of orally administered single- and multiple-dose olopatadine in healthy Chinese subjects: an open-label study. Clin Drug Investig. 2009;29(7):451-457. doi: 10.2165/00044011-200929070-00003.
  • PMID: 20476906
    Lichtenstein SJ, Abelson MB: Pharmacology, clinical efficacy and safety of olopatadine hydrochloride. Expert Rev Clin Immunol. 2006 May;2(3):341-51. doi: 10.1586/1744666X.2.3.341.

Contoh Produk & Brand

Produk: 163 • International brands: 4
Produk
  • Act Olopatadine 0.1%
    Solution • 0.1 % w/v • Ophthalmic • Canada • Approved
  • Act Olopatadine 0.2%
    Solution • 0.2 % w/v • Ophthalmic • Canada • Approved
  • Apo-olopatadine
    Solution • 0.1 % • Ophthalmic • Canada • Generic • Approved
  • Apo-olopatadine
    Solution • 0.2 % w/v • Ophthalmic • Canada • Generic • Approved
  • Clear Eyes Once Daily Eye Allergy Itch Relief
    Solution / drops • 2 mg/1mL • Ophthalmic • US • Generic • OTC • Approved
  • CVS Eye Allergy Itch Relief Once Daily
    Solution • 2 mg/1mL • Ophthalmic • US • Generic • OTC • Approved
  • CVS Eye Allergy Itch Relief Twice Daily
    Solution / drops • 1 mg/1mL • Ophthalmic • US • Generic • OTC • Approved
  • Eye Allergy Itch and Redness Relief
    Solution / drops • 1 mg/1mL • Ophthalmic • US • Generic • OTC • Approved
Menampilkan 8 dari 163 produk.
International Brands
  • Alchek — Apex
  • Alerchek — Indoco
  • Allelock — Dae Woong
  • Patanol S — Alcon

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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