Peringatan Keamanan

Symptoms of overdose include altered mental status, tremors, abdominal pain, and severe constipation.L7084 However, doses of up to 282µg did not lead to systemic anticholinergic effects in a trial of 6 patients.L7087,L7090,L7093
In case of overdose, stop tiotropium and being symptomatic and supportive therapy.L7084,L7087,L7090,L7093

Tiotropium

DB01409

small molecule approved

Deskripsi

Tiotropium is a long-acting, antimuscarinic bronchodilator used in the management of chronic obstructive pulmonary disease (COPD) and asthma.A180163,L7084,L7087,L7090,L7093 Tiotropium acts mainly on M3 muscarinic receptors located in the airways to produce smooth muscle relaxation and bronchodilation.A180163,L7084,L7087,L7090,L7093

Tiotropium is more specific for the subset of muscarinic receptors commonly found in the lungs than ipratropium.A180163

Tiotropium was granted FDA approval on 30 January 2004.L7084

Struktur Molekul 2D

Berat 392.512
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The terminal half life of tiotropium is 24 hours in patients with COPD and 44 hours in patients with asthma.[L7090,L7093]
Volume Distribusi The volume of distribution of tiotropium is 32L/kg.[A180163,L7084,L7087,L7090,L7093]
Klirens (Clearance) The total clearance of tiotropium is 880mL/min in healthy subjects receiving 5µg daily.[A180163,L7084] The renal clearance of tiotropium was 669mL/min.[A180163] Patients <65 years old demonstrated a clearance of 365mL/min while patients ?65 demonstrated a clearance of 271mL/min.[L7084] This decreased clearance is not associated with increased AUC or C<sub>max</sub>.[L7087,L7090,L7093]

Absorpsi

33% of an inhaled solution reaches systemic circulation, while oral solutions have a bioavailability of 2-3%.A180163,L7087,L7090,L7093 A dry powder for inhalation is 19.5% bioavailable.A180163,L7084 Tiotropium metered spray for inhalation reaches a maximum concentration in 5-7 minutes.L7087,L7090,L7093

Metabolisme

Tiotropium is not heavily metabolized in the body.L7084,L7087,L7090,L7093 74% of an intravenous dose is excreted in the urine as unchanged drug.L7084,L7087,L7090,L7093 Tiotropium is nonenzymatically cleaved to the inactive metabolites N-methylscopine and dithienylglycolic acid.L7084,L7087,L7090,L7093 In vitro experiments show cytochrome P-450 dependent oxidation and glutathione conjugation to further metabolites.L7084,L7087,L7090,L7093

Rute Eliminasi

74% of intravenous tiotropium was excreted unchanged in urine.A180163,L7084,L7087,L7090,L7093 14% of a dry powder inhalation dose was excreted unchanged in the urine.A180163 24 hour urinary excretion after 21 days of 5µg once daily inhalation in patients with COPD is 18.6% and in patients with asthma is 12.8%.L7084,L7087,L7090,L7093

Interaksi Makanan

1 Data
  • 1. Take with or without food. Food is not expected to interfere with absorption.

Interaksi Obat

1417 Data
Loxapine The therapeutic efficacy of Tiotropium can be decreased when used in combination with Loxapine.
Aclidinium The risk or severity of adverse effects can be increased when Tiotropium is combined with Aclidinium.
Mianserin Mianserin may increase the anticholinergic activities of Tiotropium.
Mirabegron The risk or severity of urinary retention can be increased when Tiotropium is combined with Mirabegron.
Potassium chloride The risk or severity of gastrointestinal ulceration can be increased when Tiotropium is combined with Potassium chloride.
Pramlintide The risk or severity of reduced gastrointestinal motility can be increased when Pramlintide is combined with Tiotropium.
Secretin porcine The therapeutic efficacy of Secretin porcine can be decreased when used in combination with Tiotropium.
Tramadol The risk or severity of adverse effects can be increased when Tramadol is combined with Tiotropium.
Trospium The risk or severity of adverse effects can be increased when Trospium is combined with Tiotropium.
Oxyphenonium The risk or severity of adverse effects can be increased when Oxyphenonium is combined with Tiotropium.
Benzatropine The risk or severity of adverse effects can be increased when Benzatropine is combined with Tiotropium.
Ziprasidone The risk or severity of adverse effects can be increased when Ziprasidone is combined with Tiotropium.
Disopyramide The risk or severity of adverse effects can be increased when Disopyramide is combined with Tiotropium.
Amitriptyline The risk or severity of adverse effects can be increased when Amitriptyline is combined with Tiotropium.
Ipratropium The risk or severity of adverse effects can be increased when Ipratropium is combined with Tiotropium.
Olanzapine The risk or severity of adverse effects can be increased when Olanzapine is combined with Tiotropium.
Metixene The risk or severity of adverse effects can be increased when Metixene is combined with Tiotropium.
Terfenadine The risk or severity of adverse effects can be increased when Terfenadine is combined with Tiotropium.
Buclizine The risk or severity of adverse effects can be increased when Buclizine is combined with Tiotropium.
Clozapine The risk or severity of adverse effects can be increased when Clozapine is combined with Tiotropium.
Doxylamine The risk or severity of adverse effects can be increased when Doxylamine is combined with Tiotropium.
Trihexyphenidyl The risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Tiotropium.
Oxyphencyclimine The risk or severity of adverse effects can be increased when Oxyphencyclimine is combined with Tiotropium.
Procyclidine The risk or severity of adverse effects can be increased when Procyclidine is combined with Tiotropium.
Profenamine The risk or severity of adverse effects can be increased when Profenamine is combined with Tiotropium.
Promazine The risk or severity of adverse effects can be increased when Promazine is combined with Tiotropium.
Hyoscyamine The risk or severity of adverse effects can be increased when Hyoscyamine is combined with Tiotropium.
Cyproheptadine The risk or severity of adverse effects can be increased when Cyproheptadine is combined with Tiotropium.
Imipramine The risk or severity of adverse effects can be increased when Imipramine is combined with Tiotropium.
Methscopolamine bromide The risk or severity of adverse effects can be increased when Methscopolamine bromide is combined with Tiotropium.
Chlorpromazine The risk or severity of adverse effects can be increased when Chlorpromazine is combined with Tiotropium.
Gallamine triethiodide The risk or severity of adverse effects can be increased when Gallamine triethiodide is combined with Tiotropium.
Darifenacin The risk or severity of adverse effects can be increased when Darifenacin is combined with Tiotropium.
Tridihexethyl The risk or severity of adverse effects can be increased when Tridihexethyl is combined with Tiotropium.
Triflupromazine The risk or severity of adverse effects can be increased when Triflupromazine is combined with Tiotropium.
Anisotropine methylbromide The risk or severity of adverse effects can be increased when Anisotropine methylbromide is combined with Tiotropium.
Nortriptyline The risk or severity of adverse effects can be increased when Nortriptyline is combined with Tiotropium.
Amoxapine The risk or severity of adverse effects can be increased when Amoxapine is combined with Tiotropium.
Lamotrigine Lamotrigine may decrease the excretion rate of Tiotropium which could result in a higher serum level.
Atropine The risk or severity of adverse effects can be increased when Atropine is combined with Tiotropium.
Nicardipine The risk or severity of adverse effects can be increased when Nicardipine is combined with Tiotropium.
Pirenzepine The risk or severity of adverse effects can be increased when Pirenzepine is combined with Tiotropium.
Paroxetine The risk or severity of adverse effects can be increased when Paroxetine is combined with Tiotropium.
Homatropine methylbromide The risk or severity of adverse effects can be increased when Homatropine methylbromide is combined with Tiotropium.
Rocuronium The risk or severity of adverse effects can be increased when Rocuronium is combined with Tiotropium.
Scopolamine The risk or severity of adverse effects can be increased when Scopolamine is combined with Tiotropium.
Benzquinamide The risk or severity of adverse effects can be increased when Benzquinamide is combined with Tiotropium.
Clidinium The risk or severity of adverse effects can be increased when Clidinium is combined with Tiotropium.
Propiomazine The risk or severity of adverse effects can be increased when Propiomazine is combined with Tiotropium.
Propantheline The risk or severity of adverse effects can be increased when Propantheline is combined with Tiotropium.
Dicyclomine The risk or severity of adverse effects can be increased when Dicyclomine is combined with Tiotropium.
Biperiden The risk or severity of adverse effects can be increased when Biperiden is combined with Tiotropium.
Brompheniramine The risk or severity of adverse effects can be increased when Brompheniramine is combined with Tiotropium.
Flupentixol The risk or severity of adverse effects can be increased when Flupentixol is combined with Tiotropium.
Cocaine The risk or severity of adverse effects can be increased when Cocaine is combined with Tiotropium.
Quinidine The risk or severity of adverse effects can be increased when Quinidine is combined with Tiotropium.
Maprotiline The risk or severity of adverse effects can be increased when Maprotiline is combined with Tiotropium.
Methantheline The risk or severity of adverse effects can be increased when Methantheline is combined with Tiotropium.
Cycrimine The risk or severity of adverse effects can be increased when Cycrimine is combined with Tiotropium.
Glycopyrronium The risk or severity of adverse effects can be increased when Glycopyrronium is combined with Tiotropium.
Tolterodine The risk or severity of adverse effects can be increased when Tolterodine is combined with Tiotropium.
Oxybutynin The risk or severity of adverse effects can be increased when Oxybutynin is combined with Tiotropium.
Promethazine The risk or severity of adverse effects can be increased when Promethazine is combined with Tiotropium.
Diphenhydramine The risk or severity of adverse effects can be increased when Diphenhydramine is combined with Tiotropium.
Doxacurium The risk or severity of adverse effects can be increased when Doxacurium is combined with Tiotropium.
Doxepin The risk or severity of adverse effects can be increased when Doxepin is combined with Tiotropium.
Flavoxate The risk or severity of adverse effects can be increased when Flavoxate is combined with Tiotropium.
Desipramine The risk or severity of adverse effects can be increased when Desipramine is combined with Tiotropium.
Orphenadrine The risk or severity of adverse effects can be increased when Orphenadrine is combined with Tiotropium.
Escitalopram The risk or severity of adverse effects can be increased when Escitalopram is combined with Tiotropium.
Quetiapine The risk or severity of adverse effects can be increased when Quetiapine is combined with Tiotropium.
Mivacurium The risk or severity of adverse effects can be increased when Mivacurium is combined with Tiotropium.
Diphenidol The risk or severity of adverse effects can be increased when Diphenidol is combined with Tiotropium.
Aripiprazole The risk or severity of adverse effects can be increased when Aripiprazole is combined with Tiotropium.
Chlorprothixene The risk or severity of adverse effects can be increased when Chlorprothixene is combined with Tiotropium.
Metocurine The risk or severity of adverse effects can be increased when Metocurine is combined with Tiotropium.
Pancuronium The risk or severity of adverse effects can be increased when Pancuronium is combined with Tiotropium.
Pipecuronium The risk or severity of adverse effects can be increased when Pipecuronium is combined with Tiotropium.
Methotrimeprazine The risk or severity of adverse effects can be increased when Methotrimeprazine is combined with Tiotropium.
Solifenacin The risk or severity of adverse effects can be increased when Solifenacin is combined with Tiotropium.
Isopropamide The risk or severity of adverse effects can be increased when Isopropamide is combined with Tiotropium.
Rapacuronium The risk or severity of adverse effects can be increased when Rapacuronium is combined with Tiotropium.
Mepenzolate The risk or severity of adverse effects can be increased when Mepenzolate is combined with Tiotropium.
Pizotifen The risk or severity of adverse effects can be increased when Pizotifen is combined with Tiotropium.
Fesoterodine The risk or severity of adverse effects can be increased when Fesoterodine is combined with Tiotropium.
Hexocyclium The risk or severity of adverse effects can be increased when Hexocyclium is combined with Tiotropium.
Dimetindene The risk or severity of adverse effects can be increased when Dimetindene is combined with Tiotropium.
Dexetimide The risk or severity of adverse effects can be increased when Dexetimide is combined with Tiotropium.
Benactyzine The risk or severity of adverse effects can be increased when Benactyzine is combined with Tiotropium.
Umeclidinium The risk or severity of adverse effects can be increased when Umeclidinium is combined with Tiotropium.
Trimebutine The risk or severity of adverse effects can be increased when Trimebutine is combined with Tiotropium.
Dosulepin The risk or severity of adverse effects can be increased when Dosulepin is combined with Tiotropium.
Imidafenacin The risk or severity of adverse effects can be increased when Imidafenacin is combined with Tiotropium.
Butylscopolamine The risk or severity of adverse effects can be increased when Butylscopolamine is combined with Tiotropium.
Thonzylamine The risk or severity of adverse effects can be increased when Thonzylamine is combined with Tiotropium.
Methscopolamine The risk or severity of adverse effects can be increased when Methscopolamine is combined with Tiotropium.
Revefenacin The risk or severity of adverse effects can be increased when Revefenacin is combined with Tiotropium.
Oxitropium The risk or severity of adverse effects can be increased when Oxitropium is combined with Tiotropium.
Propiverine The risk or severity of adverse effects can be increased when Propiverine is combined with Tiotropium.
Batefenterol The risk or severity of adverse effects can be increased when Batefenterol is combined with Tiotropium.

Target Protein

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

Referensi & Sumber

Synthesis reference: Rolf Banholzer, "Crystalline tiotropium bromide monohydrate, processes for the preparation thereof, and pharmaceutical compositions." U.S. Patent US20020169321, issued November 14, 2002.
Artikel (PubMed)
  • PMID: 19292598
    Price D, Sharma A, Cerasoli F: Biochemical properties, pharmacokinetics and pharmacological response of tiotropium in chronic obstructive pulmonary disease patients. Expert Opin Drug Metab Toxicol. 2009 Apr;5(4):417-24. doi: 10.1517/17425250902828337 .

Contoh Produk & Brand

Produk: 14 • International brands: 0
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Menampilkan 8 dari 14 produk.

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