Description

Simple

A medication used to treat inflammatory condition leading to weakness of the lungs.

Clinical

A long-acting bronchodilator used in the management of chronic obstructive pulmonary disease (COPD).

Overview

Tiotropium is a long-acting, antimuscarinic bronchodilator used in the management of chronic obstructive pulmonary disease (COPD) and asthma.[1,2,3,4,5] Tiotropium acts mainly on M3 muscarinic receptors located in the airways to produce smooth muscle relaxation and bronchodilation.[1,Read more

Pharmacology

Indication

Tiotropium powder for inhalation is indicated for the maintenance of bronchospasm in COPD and to prevent exacerbations of COPD.[2] A combination tiotropium and [olodaterol... Read more

Pharmacodynamic

Tiotropium is a long acting antimuscarinic that causes bronchodilation.[ Read more

Mechanism of action

Tiotropium is an antagonist of muscarinic receptors M1 to M5.[ Read more

Absorption

33% of an inhaled solution reaches systemic circulation, while oral solutions have a bioavailability of 2-3%.[ Read more

Protein binding

Tiotropium is 72% protein bound in plasma.[ Read more

Volume of distribution

The volume of distribution of tiotropium is 32L/kg.[ Read more

Clearance

The total clearance of tiotropium is 880mL/min in healthy subjects receiving 5µg daily.[ Read more

Half life

The terminal half life of tiotropium is 24 hours in patients with COPD and 44 hours in patients with asthma.[4, Read more

Route of elimination

74% of intravenous tiotropium was excreted unchanged in urine.[ Read more

Toxicity

Symptoms of overdose include altered mental status, tremors, abdominal pain, and severe constipation.[2] However, doses of up to 282µg did not lead to systemic anticholine... Read more

Adverse Effects

Contraindications

  • Route:
    • Respiratory (inhalation)
  • Dose Form:
    • Spray
  • Regions: US
  • Patient Conditions:
      • Name: Not being treated with an inhaled corticosteroid
      • Drugbank Id: DBCOND0121032
      • Name: Asthma
      • Drugbank Id: DBCOND0013565
  • Hypersensitivity:
    • true
  • Regions: US

Food Interactions

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

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine
The metabolism of Tiotropium can be decreased when combined with 1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine.
1,10-Phenanthroline
The therapeutic efficacy of Tiotropium can be decreased when used in combination with 1,10-Phenanthroline.
2,5-Dimethoxy-4-ethylamphetamine
The risk or severity of Tachycardia can be increased when Tiotropium is combined with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamine
2,5-Dimethoxy-4-ethylthioamphetamine may increase the central nervous system depressant (CNS depressant) activities of Tiotropium.
4-Bromo-2,5-dimethoxyamphetamine
4-Bromo-2,5-dimethoxyamphetamine may increase the central nervous system depressant (CNS depressant) activities of Tiotropium.
4-Methoxyamphetamine
4-Methoxyamphetamine may increase the central nervous system depressant (CNS depressant) activities of Tiotropium.
5-methoxy-N,N-dimethyltryptamine
5-methoxy-N,N-dimethyltryptamine may increase the central nervous system depressant (CNS depressant) activities of Tiotropium.
7-Nitroindazole
7-Nitroindazole may increase the central nervous system depressant (CNS depressant) activities of Tiotropium.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the central nervous system depressant (CNS depressant) activities of Tiotropium.
Abacavir
Abacavir may decrease the excretion rate of Tiotropium which could result in a higher serum level.
Abatacept
The metabolism of Tiotropium can be increased when combined with Abatacept.
Abediterol
The risk or severity of Tachycardia can be increased when Tiotropium is combined with Abediterol.
Abiraterone
The metabolism of Tiotropium can be decreased when combined with Abiraterone.
Acarbose
Acarbose may decrease the excretion rate of Tiotropium which could result in a higher serum level.
Acebutolol
The metabolism of Tiotropium can be decreased when combined with Acebutolol.
Aceclofenac
Aceclofenac may decrease the excretion rate of Tiotropium which could result in a higher serum level.
Acemetacin
Acemetacin may decrease the excretion rate of Tiotropium which could result in a higher serum level.
Acepromazine
Acepromazine may increase the central nervous system depressant (CNS depressant) activities of Tiotropium.
Aceprometazine
Aceprometazine may increase the central nervous system depressant (CNS depressant) activities of Tiotropium.
Acetaminophen
Acetaminophen may decrease the excretion rate of Tiotropium which could result in a higher serum level.
5 References
  1. 1 . 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 .PubMed: 19292598
  2. 2 . FDA Drug Approval Package: Tiotropium Bromide Powder for Inhalation Link
  3. 3 . FDA Approved Drug Products: Tiotropium and Olodaterol Metered Inhalation Spray Link
  4. 4 . FDA Approved Drug Products: Tiotropium Inhalation Spray Link
  5. 5 . FDA Approved Drug Products: Tiotropium Metered Inhalation Spray Link