Peringatan Keamanan

The expected signs and symptoms associated with overdosage of indacaterol are those of excessive beta-adrenergic stimulation and occurrence or exaggeration of any of the signs and symptoms, e.g., angina, hypertension or hypotension, tachycardia, with rates up to 200 bpm, arrhythmias, nervousness, headache, tremor, dry mouth, palpitation, muscle cramps, nausea, dizziness, fatigue, malaise, hypokalemia, hyperglycemia, metabolic acidosis and insomnia. As with all inhaled sympathomimetic medications, cardiac arrest and even death may be associated with an overdose of indacaterol.

Indacaterol

DB05039

small molecule approved

Deskripsi

Indacaterol is a novel, ultra-long-acting, rapid onset ?(2)-adrenoceptor agonist developed for Novartis for the once-daily management of asthma and chronic obstructive pulmonary disease. It was approved by the European Medicines Agency (EMA) on 30 November 2009 and by the FDA on 1 July 2011. It is marketed in Europe as Onbrez and in America as Arcapta Neohaler. Indacaterol is provided as its maleate salt form. Indacaterol is also a chiral molecule but only the pure R-enantiomer is dispensed.

Struktur Molekul 2D

Berat 392.4907
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Indacaterol serum concentrations declined in a multi-phasic manner with an average terminal half-life ranging from 45.5 to 126 hours. The effective half-life, calculated from the accumulation of indacaterol after repeated dosing with once daily doses between 75 mcg and 600 mcg ranged from 40 to 56 hours which is consistent with the observed time-to-steady state of approximately 12-15 days.
Volume Distribusi After intravenous infusion the volume of distribution (Vz) of indacaterol was 2,361 L to 2,557 L indicating an extensive distribution.
Klirens (Clearance) Renal clearance of indacaterol is, on average, between 0.46 and 1.2 L/h. Serum clearance of indacaterol is 18.8 L/h to 23.3 L/h.

Absorpsi

The median time to reach peak serum concentrations of indacaterol was approximately 15 minutes after single or repeated inhaled doses. Absolute bioavailability of indacaterol after an inhaled dose was on average 43-45%.

Metabolisme

After oral administration of radiolabeled indacaterol, unchanged indacaterol was the main component in serum, accounting for about one third of total drug-related AUC over 24 hours. The monohydroxylated derivative, glucuronide conjugate, and the 8-O-glucuronide were the most prominent metabolites in serum. Other metabolites identified include a diastereomer of the hydroxylated derivative, a N-glucuronide of indacaterol, and C- and N-dealkylated products. In vitro investigations indicated that UGT1A1 was the only UGT isoform that metabolized indacaterol to the phenolic O-glucuronide. CYP3A4 is the predominant isoenzyme responsible for hydroxylation of indacaterol.

Rute Eliminasi

Renal clearance plays a minor role (about 2 to 6% of systemic clearance) in the elimination of systemically available indacaterol. In a human ADME study where indacaterol was given orally, the fecal route of excretion was dominant over the urinary route. Indacaterol was excreted into human feces primarily as unchanged parent drug (54% of the dose) and, to a lesser extent, hydroxylated indacaterol metabolites (23% of the dose).

Interaksi Obat

1270 Data
Loxapine The therapeutic efficacy of Indacaterol can be decreased when used in combination with Loxapine.
Ranolazine The serum concentration of Indacaterol can be increased when it is combined with Ranolazine.
Valsartan Indacaterol may decrease the antihypertensive activities of Valsartan.
Ramipril Indacaterol may decrease the antihypertensive activities of Ramipril.
Remikiren Indacaterol may decrease the antihypertensive activities of Remikiren.
Olmesartan Indacaterol may decrease the antihypertensive activities of Olmesartan.
Nitroprusside Indacaterol may decrease the antihypertensive activities of Nitroprusside.
Minoxidil Indacaterol may decrease the antihypertensive activities of Minoxidil.
Fosinopril Indacaterol may decrease the antihypertensive activities of Fosinopril.
Trandolapril Indacaterol may decrease the antihypertensive activities of Trandolapril.
Benazepril Indacaterol may decrease the antihypertensive activities of Benazepril.
Candoxatril Indacaterol may decrease the antihypertensive activities of Candoxatril.
Mecamylamine Indacaterol may decrease the antihypertensive activities of Mecamylamine.
Lisinopril Indacaterol may decrease the antihypertensive activities of Lisinopril.
Nitroglycerin Indacaterol may decrease the antihypertensive activities of Nitroglycerin.
Metyrosine Indacaterol may decrease the antihypertensive activities of Metyrosine.
Cryptenamine Indacaterol may decrease the antihypertensive activities of Cryptenamine.
Perindopril Indacaterol may decrease the antihypertensive activities of Perindopril.
Fenoldopam Indacaterol may decrease the antihypertensive activities of Fenoldopam.
Eprosartan Indacaterol may decrease the antihypertensive activities of Eprosartan.
Quinapril Indacaterol may decrease the antihypertensive activities of Quinapril.
Methyldopa Indacaterol may decrease the antihypertensive activities of Methyldopa.
Deserpidine Indacaterol may decrease the antihypertensive activities of Deserpidine.
Pentolinium Indacaterol may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Indacaterol may decrease the antihypertensive activities of Trimethaphan.
Diazoxide Indacaterol may decrease the antihypertensive activities of Diazoxide.
Epoprostenol Indacaterol may decrease the antihypertensive activities of Epoprostenol.
Saprisartan Indacaterol may decrease the antihypertensive activities of Saprisartan.
Spirapril Indacaterol may decrease the antihypertensive activities of Spirapril.
Tienilic acid Indacaterol may decrease the antihypertensive activities of Tienilic acid.
Diethylnorspermine Indacaterol may decrease the antihypertensive activities of Diethylnorspermine.
Temocapril Indacaterol may decrease the antihypertensive activities of Temocapril.
Hexamethonium Indacaterol may decrease the antihypertensive activities of Hexamethonium.
Nicorandil Indacaterol may decrease the antihypertensive activities of Nicorandil.
Rauwolfia serpentina root Indacaterol may decrease the antihypertensive activities of Rauwolfia serpentina root.
Enalaprilat Indacaterol may decrease the antihypertensive activities of Enalaprilat.
Angiotensin 1-7 Indacaterol may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril Indacaterol may decrease the antihypertensive activities of Imidapril.
BQ-123 Indacaterol may decrease the antihypertensive activities of BQ-123.
Dihydralazine Indacaterol may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Indacaterol may decrease the antihypertensive activities of Zofenopril.
Guanoxan Indacaterol may decrease the antihypertensive activities of Guanoxan.
Delapril Indacaterol may decrease the antihypertensive activities of Delapril.
Vincamine Indacaterol may decrease the antihypertensive activities of Vincamine.
Linsidomine Indacaterol may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Indacaterol may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Indacaterol may decrease the antihypertensive activities of Tolonidine.
Endralazine Indacaterol may decrease the antihypertensive activities of Endralazine.
Cadralazine Indacaterol may decrease the antihypertensive activities of Cadralazine.
Bietaserpine Indacaterol may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Indacaterol may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Indacaterol may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Indacaterol may decrease the antihypertensive activities of Guanoclor.
Muzolimine Indacaterol may decrease the antihypertensive activities of Muzolimine.
Xipamide Indacaterol may decrease the antihypertensive activities of Xipamide.
Tocopherylquinone Indacaterol may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Indacaterol may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Indacaterol may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Indacaterol may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Indacaterol may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Indacaterol may decrease the antihypertensive activities of Quinaprilat.
Lercanidipine Indacaterol may decrease the antihypertensive activities of Lercanidipine.
Bosentan Indacaterol may decrease the antihypertensive activities of Bosentan.
Eplerenone Indacaterol may decrease the antihypertensive activities of Eplerenone.
Tadalafil Indacaterol may decrease the antihypertensive activities of Tadalafil.
Guanfacine Indacaterol may decrease the antihypertensive activities of Guanfacine.
Irbesartan Indacaterol may decrease the antihypertensive activities of Irbesartan.
Hydralazine Indacaterol may decrease the antihypertensive activities of Hydralazine.
Sitaxentan Indacaterol may decrease the antihypertensive activities of Sitaxentan.
Pinacidil Indacaterol may decrease the antihypertensive activities of Pinacidil.
Riociguat The serum concentration of Riociguat can be increased when it is combined with Indacaterol.
Macitentan Indacaterol may decrease the antihypertensive activities of Macitentan.
Aliskiren Indacaterol may decrease the antihypertensive activities of Aliskiren.
Manidipine Indacaterol may decrease the antihypertensive activities of Manidipine.
Naftopidil Indacaterol may decrease the antihypertensive activities of Naftopidil.
Amlodipine Indacaterol may decrease the antihypertensive activities of Amlodipine.
Nisoldipine Indacaterol may decrease the antihypertensive activities of Nisoldipine.
Clonidine Indacaterol may decrease the antihypertensive activities of Clonidine.
Enalapril Indacaterol may decrease the antihypertensive activities of Enalapril.
Candesartan cilexetil Indacaterol may decrease the antihypertensive activities of Candesartan cilexetil.
Telmisartan Indacaterol may decrease the antihypertensive activities of Telmisartan.
Captopril Indacaterol may decrease the antihypertensive activities of Captopril.
Cilazapril Indacaterol may decrease the antihypertensive activities of Cilazapril.
Debrisoquine Indacaterol may decrease the antihypertensive activities of Debrisoquine.
Candesartan Indacaterol may decrease the antihypertensive activities of Candesartan.
Levamlodipine Indacaterol may decrease the antihypertensive activities of Levamlodipine.
Azilsartan medoxomil Indacaterol may decrease the antihypertensive activities of Azilsartan medoxomil.
Desmopressin The risk or severity of hypertension can be increased when Desmopressin is combined with Indacaterol.
Icosapent The risk or severity of hypertension can be increased when Icosapent is combined with Indacaterol.
Amphetamine The risk or severity of hypertension can be increased when Amphetamine is combined with Indacaterol.
Midodrine The risk or severity of hypertension can be increased when Midodrine is combined with Indacaterol.
Bethanidine Indacaterol may decrease the antihypertensive activities of Bethanidine.
Mesalazine The risk or severity of hypertension can be increased when Mesalazine is combined with Indacaterol.
Etomidate The risk or severity of hypertension can be increased when Etomidate is combined with Indacaterol.
Zolmitriptan The risk or severity of hypertension can be increased when Zolmitriptan is combined with Indacaterol.
Phenylephrine The risk or severity of hypertension can be increased when Phenylephrine is combined with Indacaterol.
Methylphenidate The risk or severity of hypertension can be increased when Methylphenidate is combined with Indacaterol.
Nabumetone The risk or severity of hypertension can be increased when Nabumetone is combined with Indacaterol.
Ketorolac The risk or severity of hypertension can be increased when Ketorolac is combined with Indacaterol.
Tenoxicam The risk or severity of hypertension can be increased when Tenoxicam is combined with Indacaterol.

Target Protein

Beta-2 adrenergic receptor ADRB2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 17135231
    Naline E, Trifilieff A, Fairhurst RA, Advenier C, Molimard M: Effect of indacaterol, a novel long-acting beta2-agonist, on isolated human bronchi. Eur Respir J. 2007 Mar;29(3):575-81. Epub 2006 Nov 29.
  • PMID: 22648561
    Kagan M, Dain J, Peng L, Reynolds C: Metabolism and pharmacokinetics of indacaterol in humans. Drug Metab Dispos. 2012 Sep;40(9):1712-22. doi: 10.1124/dmd.112.046151. Epub 2012 May 30.
  • PMID: 23641160
    Reid DJ, Pham NT: Emerging Therapeutic Options for the Management of COPD. Clin Med Insights Circ Respir Pulm Med. 2013 Apr 9;7:7-15. doi: 10.4137/CCRPM.S8140. Print 2013.

Contoh Produk & Brand

Produk: 101 • International brands: 4
Produk
  • Arcapta Neohaler
    Capsule • 75 ug/1 • Oral; Respiratory (inhalation) • US • Approved
  • Arcapta Neohaler
    Capsule • 75 ug/1 • Oral; Respiratory (inhalation) • US • Approved
  • Atectura Breezhaler
    Capsule • - • Respiratory (inhalation) • EU • Approved
  • Atectura Breezhaler
    Capsule • - • Respiratory (inhalation) • Canada • Approved
  • Atectura Breezhaler
    Capsule • - • Respiratory (inhalation) • Canada • Approved
  • Atectura Breezhaler
    Capsule • - • Respiratory (inhalation) • EU • Approved
  • Atectura Breezhaler
    Capsule • - • Respiratory (inhalation) • Canada • Approved
  • Atectura Breezhaler
    Capsule • - • Respiratory (inhalation) • EU • Approved
Menampilkan 8 dari 101 produk.
International Brands
  • Arcapta — Novartis
  • Hirobriz
  • Onbrez — Novartis
  • Onbrize

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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