Peringatan Keamanan

Most common adverse reactions (?3% incidence and greater than placebo) are headache, nasopharyngitis and cough.

Aclidinium

DB08897

small molecule approved

Deskripsi

Aclidinium is an anticholinergic for the long-term management of chronic obstructive pulmonary disease (COPD). It has a much higher propensity to bind to muscarinic receptors than nicotinic receptors. FDA approved on July 24, 2012.

Struktur Molekul 2D

Berat 484.651
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Plasma half-life = 2.4 minutes (indicating that aclidinium is very rapidly hydrolyzed in plasma into its two inactive metabolites and has a low chance of causing systemic side effects). Effective half-life = 5-8 hours.
Volume Distribusi Following IV administration, the volume of distribution is 300 L
Klirens (Clearance) Total clearance, IV dose, young healthy subjects = 170 L/h (inter-individual variability of 36%)

Absorpsi

Bioavailability, healthy subjects = 6%; T max, healthy subjects = 10 minutes; Time to steady state, healthy subjects = 2 days;

Metabolisme

The major route of metabolism of aclidinium bromide is hydrolysis, which occurs both chemically and enzymatically by esterases in the plasma. Aclidinium bromide is rapidly and extensively hydrolyzed to its alcohol and dithienylglycolic acid derivatives, neither of which binds to muscarinic receptors and are pharmacologically inactive.

Rute Eliminasi

Intravenously administered radiolabelled aclidinium bromide was administered to healthy volunteers and was extensively metabolized with 1% excreted as unchanged aclidinium. Approximately 54% to 65% of the radioactivity was excreted in urine and 20% to 33% of the dose was excreted in feces. The combined results indicated that almost the entire aclidinium bromide dose was eliminated by hydrolysis. After dry powder inhalation, urinary excretion of aclidinium is about 0.09% of the dose.

Interaksi Obat

1153 Data
Loxapine The therapeutic efficacy of Aclidinium can be decreased when used in combination with Loxapine.
Tramadol The risk or severity of adverse effects can be increased when Tramadol is combined with Aclidinium.
Trospium The risk or severity of adverse effects can be increased when Trospium is combined with Aclidinium.
Oxyphenonium The risk or severity of adverse effects can be increased when Oxyphenonium is combined with Aclidinium.
Benzatropine The risk or severity of adverse effects can be increased when Benzatropine is combined with Aclidinium.
Ziprasidone The risk or severity of adverse effects can be increased when Ziprasidone is combined with Aclidinium.
Disopyramide The risk or severity of adverse effects can be increased when Disopyramide is combined with Aclidinium.
Amitriptyline The risk or severity of adverse effects can be increased when Amitriptyline is combined with Aclidinium.
Ipratropium The risk or severity of adverse effects can be increased when Ipratropium is combined with Aclidinium.
Olanzapine The risk or severity of adverse effects can be increased when Olanzapine is combined with Aclidinium.
Metixene The risk or severity of adverse effects can be increased when Metixene is combined with Aclidinium.
Terfenadine The risk or severity of adverse effects can be increased when Terfenadine is combined with Aclidinium.
Buclizine The risk or severity of adverse effects can be increased when Buclizine is combined with Aclidinium.
Clozapine The risk or severity of adverse effects can be increased when Clozapine is combined with Aclidinium.
Doxylamine The risk or severity of adverse effects can be increased when Doxylamine is combined with Aclidinium.
Trihexyphenidyl The risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Aclidinium.
Oxyphencyclimine The risk or severity of adverse effects can be increased when Oxyphencyclimine is combined with Aclidinium.
Procyclidine The risk or severity of adverse effects can be increased when Procyclidine is combined with Aclidinium.
Profenamine The risk or severity of adverse effects can be increased when Profenamine is combined with Aclidinium.
Promazine The risk or severity of adverse effects can be increased when Promazine is combined with Aclidinium.
Hyoscyamine The risk or severity of adverse effects can be increased when Hyoscyamine is combined with Aclidinium.
Cyproheptadine The risk or severity of adverse effects can be increased when Cyproheptadine is combined with Aclidinium.
Imipramine The risk or severity of adverse effects can be increased when Imipramine is combined with Aclidinium.
Methscopolamine bromide The risk or severity of adverse effects can be increased when Methscopolamine bromide is combined with Aclidinium.
Chlorpromazine The risk or severity of adverse effects can be increased when Chlorpromazine is combined with Aclidinium.
Gallamine triethiodide The risk or severity of adverse effects can be increased when Gallamine triethiodide is combined with Aclidinium.
Darifenacin The risk or severity of adverse effects can be increased when Darifenacin is combined with Aclidinium.
Tridihexethyl The risk or severity of adverse effects can be increased when Tridihexethyl is combined with Aclidinium.
Triflupromazine The risk or severity of adverse effects can be increased when Triflupromazine is combined with Aclidinium.
Anisotropine methylbromide The risk or severity of adverse effects can be increased when Anisotropine methylbromide is combined with Aclidinium.
Nortriptyline The risk or severity of adverse effects can be increased when Nortriptyline is combined with Aclidinium.
Amoxapine The risk or severity of adverse effects can be increased when Amoxapine is combined with Aclidinium.
Lamotrigine Lamotrigine may decrease the excretion rate of Aclidinium which could result in a higher serum level.
Atropine The risk or severity of adverse effects can be increased when Atropine is combined with Aclidinium.
Nicardipine The risk or severity of adverse effects can be increased when Nicardipine is combined with Aclidinium.
Pirenzepine The risk or severity of adverse effects can be increased when Pirenzepine is combined with Aclidinium.
Paroxetine The risk or severity of adverse effects can be increased when Paroxetine is combined with Aclidinium.
Homatropine methylbromide The risk or severity of adverse effects can be increased when Homatropine methylbromide is combined with Aclidinium.
Rocuronium The risk or severity of adverse effects can be increased when Rocuronium is combined with Aclidinium.
Scopolamine The risk or severity of adverse effects can be increased when Scopolamine is combined with Aclidinium.
Benzquinamide The risk or severity of adverse effects can be increased when Benzquinamide is combined with Aclidinium.
Clidinium The risk or severity of adverse effects can be increased when Clidinium is combined with Aclidinium.
Propiomazine The risk or severity of adverse effects can be increased when Propiomazine is combined with Aclidinium.
Propantheline The risk or severity of adverse effects can be increased when Propantheline is combined with Aclidinium.
Dicyclomine The risk or severity of adverse effects can be increased when Dicyclomine is combined with Aclidinium.
Biperiden The risk or severity of adverse effects can be increased when Biperiden is combined with Aclidinium.
Brompheniramine The risk or severity of adverse effects can be increased when Brompheniramine is combined with Aclidinium.
Flupentixol The risk or severity of adverse effects can be increased when Flupentixol is combined with Aclidinium.
Cocaine The risk or severity of adverse effects can be increased when Cocaine is combined with Aclidinium.
Quinidine The risk or severity of adverse effects can be increased when Quinidine is combined with Aclidinium.
Maprotiline The risk or severity of adverse effects can be increased when Maprotiline is combined with Aclidinium.
Methantheline The risk or severity of adverse effects can be increased when Methantheline is combined with Aclidinium.
Cycrimine The risk or severity of adverse effects can be increased when Cycrimine is combined with Aclidinium.
Glycopyrronium The risk or severity of adverse effects can be increased when Glycopyrronium is combined with Aclidinium.
Tolterodine The risk or severity of adverse effects can be increased when Tolterodine is combined with Aclidinium.
Oxybutynin The risk or severity of adverse effects can be increased when Oxybutynin is combined with Aclidinium.
Promethazine The risk or severity of adverse effects can be increased when Promethazine is combined with Aclidinium.
Diphenhydramine The risk or severity of adverse effects can be increased when Diphenhydramine is combined with Aclidinium.
Doxacurium The risk or severity of adverse effects can be increased when Doxacurium is combined with Aclidinium.
Doxepin The risk or severity of adverse effects can be increased when Doxepin is combined with Aclidinium.
Flavoxate The risk or severity of adverse effects can be increased when Flavoxate is combined with Aclidinium.
Desipramine The risk or severity of adverse effects can be increased when Desipramine is combined with Aclidinium.
Orphenadrine The risk or severity of adverse effects can be increased when Orphenadrine is combined with Aclidinium.
Escitalopram The risk or severity of adverse effects can be increased when Escitalopram is combined with Aclidinium.
Quetiapine The risk or severity of adverse effects can be increased when Quetiapine is combined with Aclidinium.
Mivacurium The risk or severity of adverse effects can be increased when Mivacurium is combined with Aclidinium.
Diphenidol The risk or severity of adverse effects can be increased when Diphenidol is combined with Aclidinium.
Aripiprazole The risk or severity of adverse effects can be increased when Aripiprazole is combined with Aclidinium.
Chlorprothixene The risk or severity of adverse effects can be increased when Chlorprothixene is combined with Aclidinium.
Metocurine The risk or severity of adverse effects can be increased when Metocurine is combined with Aclidinium.
Pancuronium The risk or severity of adverse effects can be increased when Pancuronium is combined with Aclidinium.
Pipecuronium The risk or severity of adverse effects can be increased when Pipecuronium is combined with Aclidinium.
Methotrimeprazine The risk or severity of adverse effects can be increased when Methotrimeprazine is combined with Aclidinium.
Tiotropium The risk or severity of adverse effects can be increased when Tiotropium is combined with Aclidinium.
Solifenacin The risk or severity of adverse effects can be increased when Solifenacin is combined with Aclidinium.
Isopropamide The risk or severity of adverse effects can be increased when Isopropamide is combined with Aclidinium.
Rapacuronium The risk or severity of adverse effects can be increased when Rapacuronium is combined with Aclidinium.
Mepenzolate The risk or severity of adverse effects can be increased when Mepenzolate is combined with Aclidinium.
Pizotifen The risk or severity of adverse effects can be increased when Pizotifen is combined with Aclidinium.
Fesoterodine The risk or severity of adverse effects can be increased when Fesoterodine is combined with Aclidinium.
Hexocyclium The risk or severity of adverse effects can be increased when Hexocyclium is combined with Aclidinium.
Dimetindene The risk or severity of adverse effects can be increased when Dimetindene is combined with Aclidinium.
Dexetimide The risk or severity of adverse effects can be increased when Dexetimide is combined with Aclidinium.
Benactyzine The risk or severity of adverse effects can be increased when Benactyzine is combined with Aclidinium.
Umeclidinium The risk or severity of adverse effects can be increased when Umeclidinium is combined with Aclidinium.
Trimebutine The risk or severity of adverse effects can be increased when Trimebutine is combined with Aclidinium.
Dosulepin The risk or severity of adverse effects can be increased when Dosulepin is combined with Aclidinium.
Imidafenacin The risk or severity of adverse effects can be increased when Imidafenacin is combined with Aclidinium.
Butylscopolamine The risk or severity of adverse effects can be increased when Butylscopolamine is combined with Aclidinium.
Thonzylamine The risk or severity of adverse effects can be increased when Thonzylamine is combined with Aclidinium.
Methscopolamine The risk or severity of adverse effects can be increased when Methscopolamine is combined with Aclidinium.
Revefenacin The risk or severity of adverse effects can be increased when Revefenacin is combined with Aclidinium.
Oxitropium The risk or severity of adverse effects can be increased when Oxitropium is combined with Aclidinium.
Propiverine The risk or severity of adverse effects can be increased when Propiverine is combined with Aclidinium.
Batefenterol The risk or severity of adverse effects can be increased when Batefenterol is combined with Aclidinium.
Mebeverine The risk or severity of adverse effects can be increased when Mebeverine is combined with Aclidinium.
Tropatepine The risk or severity of adverse effects can be increased when Tropatepine is combined with Aclidinium.
Prifinium The risk or severity of adverse effects can be increased when Prifinium is combined with Aclidinium.
Piperidolate The risk or severity of adverse effects can be increased when Piperidolate is combined with Aclidinium.
Benzilone The risk or severity of adverse effects can be increased when Benzilone is combined with Aclidinium.

Target Protein

Muscarinic acetylcholine receptor M1 CHRM1
Muscarinic acetylcholine receptor M2 CHRM2
Muscarinic acetylcholine receptor M3 CHRM3
Muscarinic acetylcholine receptor M4 CHRM4
Muscarinic acetylcholine receptor M5 CHRM5

Referensi & Sumber

Artikel (PubMed)
  • 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.
  • PMID: 23566013
    Cazzola M, Page CP, Matera MG: Aclidinium bromide for the treatment of chronic obstructive pulmonary disease. Expert Opin Pharmacother. 2013 Jun;14(9):1205-14. doi: 10.1517/14656566.2013.789021. Epub 2013 Apr 9.
  • PMID: 23553509
    Jones P: Aclidinium bromide twice daily for the treatment of chronic obstructive pulmonary disease: a review. Adv Ther. 2013 Apr;30(4):354-68. doi: 10.1007/s12325-013-0019-2. Epub 2013 Apr 2.
  • PMID: 20332199
    Alberti J, Martinet A, Sentellas S, Salva M: Identification of the human enzymes responsible for the enzymatic hydrolysis of aclidinium bromide. Drug Metab Dispos. 2010 Jul;38(7):1202-10. doi: 10.1124/dmd.109.031724. Epub 2010 Mar 23.

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