Peringatan Keamanan

A death was reported in dogs after a single oral dose of 5 mg/kg (approximately 4500 times the maximum recommended daily inhalation dose in adults on a mg/m2 basis). As with all inhaled sympathomimetic medications, cardiac arrest and even death may be associated with an overdose. Arformoterol should not be used more often or at higher doses than recommended, or conjunction with other medications containing long-acting beta2-agonists.L43732

Arformoterol

DB01274

small molecule approved investigational

Deskripsi

Arformoterol is a bronchodilator. It works by relaxing muscles in the airways to improve breathing. Arformoterol inhalation is used to prevent bronchoconstriction in people with chronic obstructive pulmonary disease, including chronic bronchitis and emphysema. The use of arformoterol is pending revision due to safety concerns in regards to an increased risk of severe exacerbation of asthma symptoms, leading to hospitalization as well as death in some patients using long-acting beta agonists for the treatment of asthma.

Struktur Molekul 2D

Berat 344.4049
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) In COPD patients given 15 mcg inhaled arformoterol twice a day for 14 days, the mean terminal half-life of arformoterol was 26 hours.[L43732]
Volume Distribusi -
Klirens (Clearance) In healthy male subjects, the clearance of a single oral dose of arformoterol was 8.9 L/h.[L43732]

Absorpsi

In patients with COPD, the mean peak plasma concentration (Cmax) and AUC0-12h following twice daily administration for 14 days were 4.3 pg/mL and 34.5 pg.hr/mL, respectively.L43732 The time to peak plasma concentration (Tmax) was approximately 0.5 hours.L43732

Metabolisme

Arformoterol was almost entirely metabolized following oral administration of 35 mcg of radiolabeled arformoterol in eight healthy subjects. Direct conjugation of arformoterol with glucuronic acid was the major metabolic pathway. O-Desmethylation is a secondary route catalyzed by the CYP enzymes CYP2D6 and CYP2C19.

Rute Eliminasi

Following the administration of a single oral dose of arformoterol to eight healthy subjects, 63% of the administered dose was recovered in the urine and 11% in the feces within 48 hours.L43732 After 14 days, a total of 89% of the total dose had been recovered - 67% in the urine and 22% in the feces - with approximately 1% remaining unchanged in the urine.L43732

Interaksi Obat

1750 Data
Loxapine The therapeutic efficacy of Arformoterol can be decreased when used in combination with Loxapine.
Ramipril Arformoterol may decrease the antihypertensive activities of Ramipril.
Remikiren Arformoterol may decrease the antihypertensive activities of Remikiren.
Olmesartan Arformoterol may decrease the antihypertensive activities of Olmesartan.
Minoxidil Arformoterol may decrease the antihypertensive activities of Minoxidil.
Trandolapril Arformoterol may decrease the antihypertensive activities of Trandolapril.
Benazepril Arformoterol may decrease the antihypertensive activities of Benazepril.
Enalapril Arformoterol may decrease the antihypertensive activities of Enalapril.
Candoxatril Arformoterol may decrease the antihypertensive activities of Candoxatril.
Nitroglycerin Arformoterol may decrease the antihypertensive activities of Nitroglycerin.
Metyrosine Arformoterol may decrease the antihypertensive activities of Metyrosine.
Cryptenamine Arformoterol may decrease the antihypertensive activities of Cryptenamine.
Eprosartan Arformoterol may decrease the antihypertensive activities of Eprosartan.
Quinapril Arformoterol may decrease the antihypertensive activities of Quinapril.
Telmisartan Arformoterol may decrease the antihypertensive activities of Telmisartan.
Deserpidine Arformoterol may decrease the antihypertensive activities of Deserpidine.
Pentolinium Arformoterol may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Arformoterol may decrease the antihypertensive activities of Trimethaphan.
Cilazapril Arformoterol may decrease the antihypertensive activities of Cilazapril.
Saprisartan Arformoterol may decrease the antihypertensive activities of Saprisartan.
Spirapril Arformoterol may decrease the antihypertensive activities of Spirapril.
Ambrisentan Arformoterol may decrease the antihypertensive activities of Ambrisentan.
Diethylnorspermine Arformoterol may decrease the antihypertensive activities of Diethylnorspermine.
Pinacidil Arformoterol may decrease the antihypertensive activities of Pinacidil.
Temocapril Arformoterol may decrease the antihypertensive activities of Temocapril.
Riociguat Arformoterol may decrease the antihypertensive activities of Riociguat.
Hexamethonium Arformoterol may decrease the antihypertensive activities of Hexamethonium.
Aliskiren Arformoterol may decrease the antihypertensive activities of Aliskiren.
Rauwolfia serpentina root Arformoterol may decrease the antihypertensive activities of Rauwolfia serpentina root.
Selexipag Arformoterol may decrease the antihypertensive activities of Selexipag.
Angiotensin 1-7 Arformoterol may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril Arformoterol may decrease the antihypertensive activities of Imidapril.
BQ-123 Arformoterol may decrease the antihypertensive activities of BQ-123.
Dihydralazine Arformoterol may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Arformoterol may decrease the antihypertensive activities of Zofenopril.
Guanoxan Arformoterol may decrease the antihypertensive activities of Guanoxan.
Delapril Arformoterol may decrease the antihypertensive activities of Delapril.
Vincamine Arformoterol may decrease the antihypertensive activities of Vincamine.
Linsidomine Arformoterol may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Arformoterol may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Arformoterol may decrease the antihypertensive activities of Tolonidine.
Endralazine Arformoterol may decrease the antihypertensive activities of Endralazine.
Cadralazine Arformoterol may decrease the antihypertensive activities of Cadralazine.
Bietaserpine Arformoterol may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Arformoterol may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Arformoterol may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Arformoterol may decrease the antihypertensive activities of Guanoclor.
Dexniguldipine Arformoterol may decrease the antihypertensive activities of Dexniguldipine.
Tocopherylquinone Arformoterol may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Arformoterol may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Arformoterol may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Arformoterol may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Arformoterol may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Arformoterol may decrease the antihypertensive activities of Quinaprilat.
Captopril Arformoterol may decrease the antihypertensive activities of Captopril.
Amlodipine The metabolism of Arformoterol can be decreased when combined with Amlodipine.
Levamlodipine Arformoterol may decrease the antihypertensive activities of Levamlodipine.
Lercanidipine Arformoterol may decrease the antihypertensive activities of Lercanidipine.
Azilsartan medoxomil Arformoterol may decrease the antihypertensive activities of Azilsartan medoxomil.
Diazoxide Arformoterol may decrease the antihypertensive activities of Diazoxide.
Phentermine The risk or severity of hypertension can be increased when Phentermine is combined with Arformoterol.
Bethanidine Arformoterol may decrease the antihypertensive activities of Bethanidine.
Zolmitriptan The risk or severity of hypertension can be increased when Zolmitriptan is combined with Arformoterol.
Phenylephrine The risk or severity of hypertension can be increased when Phenylephrine is combined with Arformoterol.
Doxapram The risk or severity of hypertension can be increased when Doxapram is combined with Arformoterol.
Metaraminol The risk or severity of hypertension can be increased when Metaraminol is combined with Arformoterol.
Guanabenz Arformoterol may decrease the antihypertensive activities of Guanabenz.
Sufentanil The risk or severity of hypertension can be increased when Sufentanil is combined with Arformoterol.
Methoxamine The risk or severity of hypertension can be increased when Methoxamine is combined with Arformoterol.
Alfentanil The risk or severity of hypertension can be increased when Alfentanil is combined with Arformoterol.
Phenmetrazine The risk or severity of hypertension can be increased when Phenmetrazine is combined with Arformoterol.
Pseudoephedrine The risk or severity of hypertension can be increased when Pseudoephedrine is combined with Arformoterol.
Benzphetamine The risk or severity of hypertension can be increased when Benzphetamine is combined with Arformoterol.
Omapatrilat Arformoterol may decrease the antihypertensive activities of Omapatrilat.
Remifentanil The risk or severity of hypertension can be increased when Remifentanil is combined with Arformoterol.
Oxymetazoline The risk or severity of hypertension can be increased when Oxymetazoline is combined with Arformoterol.
Diethylpropion The risk or severity of hypertension can be increased when Diethylpropion is combined with Arformoterol.
Naratriptan The risk or severity of hypertension can be increased when Naratriptan is combined with Arformoterol.
Frovatriptan The risk or severity of hypertension can be increased when Frovatriptan is combined with Arformoterol.
Dutasteride The risk or severity of hypertension can be increased when Dutasteride is combined with Arformoterol.
Rescinnamine Arformoterol may decrease the antihypertensive activities of Rescinnamine.
Finasteride The risk or severity of hypertension can be increased when Finasteride is combined with Arformoterol.
Lisdexamfetamine The risk or severity of hypertension can be increased when Lisdexamfetamine is combined with Arformoterol.
Ephedrine The risk or severity of hypertension can be increased when Arformoterol is combined with Ephedrine.
Mephentermine The risk or severity of hypertension can be increased when Arformoterol is combined with Mephentermine.
MMDA The risk or severity of hypertension can be increased when Arformoterol is combined with MMDA.
2,5-Dimethoxy-4-ethylamphetamine The risk or severity of hypertension can be increased when Arformoterol is combined with 2,5-Dimethoxy-4-ethylamphetamine.
4-Bromo-2,5-dimethoxyamphetamine The risk or severity of hypertension can be increased when Arformoterol is combined with 4-Bromo-2,5-dimethoxyamphetamine.
Tenamfetamine The risk or severity of hypertension can be increased when Arformoterol is combined with Tenamfetamine.
Chlorphentermine The risk or severity of hypertension can be increased when Arformoterol is combined with Chlorphentermine.
Dextroamphetamine The risk or severity of hypertension can be increased when Arformoterol is combined with Dextroamphetamine.
Phendimetrazine The risk or severity of hypertension can be increased when Arformoterol is combined with Phendimetrazine.
Epicaptopril The risk or severity of hypertension can be increased when Arformoterol is combined with Epicaptopril.
Taxifolin The risk or severity of hypertension can be increased when Arformoterol is combined with Taxifolin.
1-benzylimidazole The risk or severity of hypertension can be increased when Arformoterol is combined with 1-benzylimidazole.
Flibanserin The risk or severity of hypertension can be increased when Arformoterol is combined with Flibanserin.
Amibegron The risk or severity of hypertension can be increased when Arformoterol is combined with Amibegron.
Naluzotan The risk or severity of hypertension can be increased when Arformoterol is combined with Naluzotan.
Nylidrin The risk or severity of hypertension can be increased when Arformoterol is combined with Nylidrin.
Solabegron The risk or severity of hypertension can be increased when Arformoterol is combined with Solabegron.

Target Protein

Beta-2 adrenergic receptor ADRB2

Referensi & Sumber

Synthesis reference: Vaman Vaishali Haldavanekar, Mangesh Prabhu, Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, "Process for the Synthesis of Arformoterol." U.S. Patent US20110166237, issued July 07, 2011.
Artikel (PubMed)
  • PMID: 20214460
    Hanania NA, Donohue JF, Nelson H, Sciarappa K, Goodwin E, Baumgartner RA, Hanrahan JP: The safety and efficacy of arformoterol and formoterol in COPD. COPD. 2010 Feb;7(1):17-31. doi: 10.3109/15412550903499498.
  • PMID: 19124357
    Donohue JF, Hanania NA, Sciarappa KA, Goodwin E, Grogan DR, Baumgartner RA, Hanrahan JP: Arformoterol and salmeterol in the treatment of chronic obstructive pulmonary disease: a one year evaluation of safety and tolerance. Ther Adv Respir Dis. 2008 Apr;2(2):37-48. doi: 10.1177/1753465808089455.
  • PMID: 16022567
    Cazzola M, Matera MG, Lotvall J: Ultra long-acting beta 2-agonists in development for asthma and chronic obstructive pulmonary disease. Expert Opin Investig Drugs. 2005 Jul;14(7):775-83.
  • PMID: 19808130
    Panettieri RA Jr, MacIntyre N, Sims M, Kerwin E, Fogarty C, Noonan M, Claus R, Andrews WT: Comparison of the efficacy and safety of arformoterol 15 microg twice daily and arformoterol 30 microg once daily in COPD: a single-dose, multicenter, randomized, modified-blind, two-way crossover study. Clin Ther. 2009 Aug;31(8):1716-23. doi: 10.1016/j.clinthera.2009.08.012.
  • PMID: 18501650
    Kharidia J, Fogarty CM, Laforce CF, Maier G, Hsu R, Dunnington KM, Curry L, Baumgartner RA, Hanrahan JP: A pharmacokinetic/pharmacodynamic study comparing arformoterol tartrate inhalation solution and racemic formoterol dry powder inhaler in subjects with chronic obstructive pulmonary disease. Pulm Pharmacol Ther. 2008 Aug;21(4):657-62. doi: 10.1016/j.pupt.2008.03.003. Epub 2008 Apr 7.
  • PMID: 17472819
    Baumgartner RA, Hanania NA, Calhoun WJ, Sahn SA, Sciarappa K, Hanrahan JP: Nebulized arformoterol in patients with COPD: a 12-week, multicenter, randomized, double-blind, double-dummy, placebo- and active-controlled trial. Clin Ther. 2007 Feb;29(2):261-78.

Contoh Produk & Brand

Produk: 16 • International brands: 0
Produk
  • Arformoterol Tartrate
    Solution • 15 ug/2mL • Respiratory (inhalation) • US • Generic • Approved
  • Arformoterol Tartrate
    Solution • 15 ug/2mL • Respiratory (inhalation) • US • Generic • Approved
  • Arformoterol Tartrate
    Solution • 15 ug/2mL • Respiratory (inhalation) • US • Generic • Approved
  • Arformoterol tartrate
    Solution • 15 ug/2mL • Respiratory (inhalation) • US • Generic • Approved
  • Arformoterol tartrate
    Solution • 15 ug/2mL • Respiratory (inhalation) • US • Generic • Approved
  • Arformoterol tartrate
    Solution • 15 ug/2mL • Respiratory (inhalation) • US • Generic • Approved
  • Arformoterol Tartrate
    Solution • 15 ug/2mL • Respiratory (inhalation) • US • Generic • Approved
  • Arformoterol Tartrate
    Solution • 15 ug/2mL • Respiratory (inhalation) • US • Generic • Approved
Menampilkan 8 dari 16 produk.

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