Tiotropium

Tiotropium is a long-acting, antimuscarinic agent, which is often referred to as an anticholinergic. It has similar affinity to the subtypes of muscarinic receptors, M 1 to M 5 .

• Tiotropium bromide inhalation powder is indicated for the long-term, once-daily, maintenance treatment of bronchospasm associated with chronic obstructive pulmonary disease (COPD), including chronic bronchitis and emphysema. Tiotropium bromide inhalation powder is indicated to reduce exacerbations in COPD patients.ICD-10: J20.9, J44.9

• Tiotropium bromide inhalation powder is contraindicated in patients with a hypersensitivity to tiotropium, ipratropium, or any components of this product [see Warnings and Precautions ( 5.2 )] . In clinical trials and postmarketing experience with tiotropium bromide inhalation powder, immediate hypersensitivity reactions, including angioedema (including swelling of the lips, tongue, or throat), itching, or rash have been reported [see Warnings and Precautions ( 5.2 )] .contraindicated

For oral inhalation only. Do not swallow tiotropium bromide inhalation powder capsules, as the intended effects on the lungs will not be obtained. The contents of the tiotropium bromide inhalation powder capsules should only be used with the LupinHaler ® device [see Overdosage ( 10 )] . The recommended dosage of tiotropium bromide inhalation powder is two inhalations of the powder contents of one tiotropium bromide inhalation powder capsule, once-daily, with the LupinHaler device [see Patient Counseling Information ( 17 )]. Do not take more than one dose in 24 hours. For administration of tiotropium bromide inhalation powder, a tiotropium bromide inhalation powder capsule is placed into the center chamber of the LupinHaler device. The tiotropium bromide inhalation powder capsule is pierced by pressing and releasing the green piercing button on the side of the LupinHaler device. The tiotropium formulation is dispersed into the air stream when the patient inhales through the mouthpiece [see Patient Counseling Information ( 17 )]. No dosage adjustment is required for geriatric, hepatically-impaired, or renally-impaired patients. However, patients with moderate to severe renal impairment given tiotropium bromide inhalation powder should be monitored closely for anticholinergic effects [see Warnings and Precautions ( 5.6 ), Use in Specific Populations ( 8.5 , 8.6 , 8.7 ), and Clinical Pharmacology ( 12.3 )]. For oral inhalation only. DO NOT swallow tiotropium bromide inhalation powder capsules.

Not for acute use: Not a rescue medication ( 5.1 ) Immediate hypersensitivity reactions: Discontinue tiotropium bromide inhalation powder at once and consider alternatives if immediate hypersensitivity reactions, including angioedema, urticaria, rash, bronchospasm, or anaphylaxis, occur. Use with caution in patients with severe hypersensitivity to milk proteins. ( 5.2 ) Paradoxical bronchospasm: Discontinue tiotropium bromide inhalation powder and consider other treatments if paradoxical bronchospasm occurs ( 5.3 ) Worsening of narrow-angle glaucoma may occur. Use with caution in patients with narrow-angle glaucoma and instruct patients to consult a physician immediately if this occurs. ( 5.4 ) Worsening of urinary retention may occur. Use with caution in patients with prostatic hyperplasia or bladder-neck obstruction and instruct patients to consult a physician immediately if this occurs. ( 5.5 ) 5.1 Not for Acute Use Tiotropium bromide inhalation powder is intended as a once-daily maintenance treatment for COPD and should not be used for relief of acute symptoms, i.e., as rescue therapy for the treatment of acute episodes of bronchospasm. 5.2 Immediate Hypersensitivity Reactions Immediate hypersensitivity reactions, including urticaria, angioedema (including swelling of the lips, tongue, or throat), rash, bronchospasm, anaphylaxis, or itching, may occur after administration of tiotropium bromide inhalation powder. If such a reaction occurs, therapy with tiotropium bromide inhalation powder should be stopped at once and alternative treatments should be considered.

The following adverse reactions are described, or described in greater detail, in other sections: Immediate hypersensitivity reactions [see Warnings and Precautions ( 5.2 )] Paradoxical bronchospasm [see Warnings and Precautions ( 5.3 )] Worsening of narrow-angle glaucoma [see Warnings and Precautions ( 5.4 )] Worsening of urinary retention [see Warnings and Precautions ( 5.5 )] The most common adverse reactions (>5% incidence in the 1-year placebo- controlled trials) were upper respiratory tract infection, dry mouth, sinusitis, pharyngitis, non-specific chest pain, urinary tract infection, dyspepsia, and rhinitis ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Lupin Pharmaceuticals, Inc. at 1-800-399-2561 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, the incidence of adverse reactions observed in the clinical trials of a drug cannot be directly compared to the incidences in the clinical trials of another drug and may not reflect the incidences observed in practice. 6-Month to 1-Year Trials The data described below reflect exposure to tiotropium bromide inhalation powder in 2,663 patients. Tiotropium bromide inhalation powder was studied in two 1-year placebo-controlled trials, two 1-year active-controlled trials, and two 6-month placebo-controlled trials in patients with COPD. In these trials, 1,308 patients were treated with tiotropium bromide inhalation powder at the recommended dosage of 18 mcg once a day.

Patients with moderate to severe renal impairment should be monitored closely for potential anticholinergic side effects ( 2 , 8.6 ) 8.1 Pregnancy Risk Summary The limited human data with tiotropium bromide inhalation powder use during pregnancy are insufficient to inform a drug-associated risk of adverse pregnancy-related outcomes. Based on animal reproduction studies, no structural abnormalities were observed when tiotropium was administered by inhalation to pregnant rats and rabbits during the period of organogenesis at doses 790 and 8 times, respectively, the maximum recommended human daily inhalation dose (MRHDID). Increased post-implantation loss was observed in rats and rabbits administered tiotropium at maternally toxic doses 430 times and 40 times the MRHDID, respectively [see Data]. The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.

Metabolism

Tiotropium is administered by dry powder inhalation. Some of the pharmacokinetic data described below were obtained with higher doses than recommended for therapy.

High doses of tiotropium may lead to anticholinergic signs and symptoms. However, there were no systemic anticholinergic adverse effects following a single inhaled dose of up to 282 mcg tiotropium in 6 healthy volunteers. In a study of 12 healthy volunteers, bilateral conjunctivitis and dry mouth were seen following repeated once- daily inhalation of 141 mcg of tiotropium. Treatment of overdosage consists of discontinuation of tiotropium bromide inhalation powder together with institution of appropriate symptomatic and/or supportive therapy. Accidental Ingestion Acute intoxication by inadvertent oral ingestion of tiotropium bromide inhalation powder capsules is unlikely since it is not well-absorbed systemically. A case of overdose has been reported from postmarketing experience. A female patient was reported to have inhaled 30 capsules over a 2.5 day period, and developed altered mental status, tremors, abdominal pain, and severe constipation. The patient was hospitalized, tiotropium bromide inhalation powder was discontinued, and the constipation was treated with an enema. The patient recovered and was discharged on the same day.

• Jan 30, 2004NDANDA021395Boehringer Ingelheim
• Sep 24, 2014NDANDA021936Boehringer Ingelheim
• May 21, 2015NDANDA206756Boehringer Ingelheim
• Sep 15, 2015NDANDA207070Boehringer Ingelheim
• Jun 20, 2023ANDAANDA211287Lupin

1. 1Dyspnoea25,29117%
2. 2Incorrect Route Of Drug Administration23,32716%
3. 3Asthma12,2328.1%
4. 4Drug Ineffective10,4166.9%
5. 5Cough9,9566.6%
6. 6Pneumonia9,3686.2%
7. 7Wheezing7,5855.0%
8. 8Chronic Obstructive Pulmonary Disease6,9364.6%
9. 9Product Quality Issue6,4734.3%
10. 10Fatigue6,0544.0%
11. 11Off Label Use5,6363.8%
12. 12Malaise5,0083.3%
13. 13Nausea4,4983.0%
14. 14Headache4,4813.0%
15. 15Fall4,3992.9%

Recent PubMed references pinned to Tiotropium as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

• Simultaneous quantification and aerodynamic particle size distribution analysis of tiotropium bromide and olodaterol in nebulized aerosol using UHPLC-MS/MS.
  Journal of pharmaceutical and biomedical analysis · 2026 · Dou J, Hong Y, Qian R, et al.
  PMID 41990594DOI 10.1016/j.jpba.2026.117500
• Identifying patients with mild-to-moderate COPD who require intensified initial treatment to control annualized clinically important deterioration.
  NPJ primary care respiratory medicine · 2026 · Wang Z, Zhou Y, Guan WJ, et al.
  PMID 41942485DOI 10.1038/s41533-026-00501-w
• Can tiotropium add-on inhalation revolutionize therapy in elderly asthmatic patients? A treatable traits approach towards successful aging.
  International journal of clinical pharmacology and therapeutics · 2026 · Ishiura Y, Nomura S, Ohkura N, et al.
  PMID 41841282DOI 10.5414/CP204911
• Inhaled Corticosteroids Plus Tiotropium Compared to Inhaled Corticosteroids Plus Montelukast in Children with Partly Controlled/Uncontrolled Asthma: A Non-Inferiority Trial.
  Indian journal of pediatrics · 2026 · Sengupta S, Das RR, Gulla KM, et al.
  PMID 41772161DOI 10.1007/s12098-026-06003-4
• Long-acting muscarinic antagonist versus leukotriene receptor antagonist as additional treatment in uncontrolled asthma patients used inhaled corticosteroids and long-acting β2 adrenergic agonist: a randomized phase 2 screening trial.
  Respiratory medicine and research · 2025 · Nihashi F, Furuhashi K, Niwa M, et al.
  PMID 41166913DOI 10.1016/j.resmer.2025.101191
• Lower baseline FEV1 is associated with greater FEV1 improvement after tiotropium add-on in uncontrolled asthma.
  Medicine · 2025 · Shim JS, Ahn KM, Kim MH, et al.
  PMID 41088610DOI 10.1097/MD.0000000000044912
• Comparable Clinical Outcomes with Tiotropium/Olodaterol or Fluticasone Furoate/Umeclidinium/Vilanterol in Patients with COPD and Blood Eosinophil Count ≤300 Cells/μL.
  International journal of chronic obstructive pulmonary disease · 2025 · Sethi S, Clark B, Buysman EK, et al.
  PMID 41031390DOI 10.2147/COPD.S534974
• Adverse drug events associated with tiotropium: a real-world pharmacovigilance study of FDA adverse event reporting system database.
  Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques · 2025 · Rui Y, Xin T, Chen Y, et al.
  PMID 40949724DOI 10.3389/jpps.2025.14917

The 10 most recently updated of 428 ClinicalTrials.gov registrations naming Tiotropium as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• TRIple in Asthma hiGh strenGth vErsus Ics/Laba hs and tiotRopium (TRIGGER)
  Completed · Phase 3 · Interventional · 1,437 enrolled · Chiesi Farmaceutici S.p.A.
  NCT02676089updated 2026-05-29
• Description of the Ability to Learn How to Handle Inhaler Devices in COPD
  Completed · Phase 4 · Interventional · 24 enrolled · University Hospital, Bordeaux
  NCT02813200updated 2026-05-14
• Effect on Bronchodilation Response and Ventilation Heterogeneity of Different Inhalation Volumes in COPD
  Not yet recruiting · Observational · 30 enrolled · University of Milan
  NCT05381415updated 2026-05-04
• Comparative Efficacy of Once-daily LAMA/LABA Combinations Versus Tiotropium on Constant-work-rate Cycle Endurance in COPD
  Suspended · Interventional · 100 enrolled · Medical University of Bialystok
  NCT07541378updated 2026-04-21
• Effects of Tiotropium/Olodaterol on Cardio-pulmonary Exercise Capacity in Patients With Hyperinflated Chronic Obstructive Pulmonary Disease [ACHIEVE]
  Completed · Interventional · 44 enrolled · Yonsei University
  NCT04994574updated 2026-04-07
• A Clinical Study to Evaluate the Safety, Tolerability and Pharmacokinetic Profile of TQC3302 Inhalation Spray in Healthy Adult Subjects
  Recruiting · Phase 1 · Interventional · 57 enrolled · Chia Tai Tianqing Pharmaceutical (Guangzhou) Co., Ltd.
  NCT07267130updated 2026-03-10
• Tiotropium vs. Inhaled Corticosteroids in Children With Nonatopic Asthma Pilot Study (TioNAAP)
  Terminated · Phase 2 · Interventional · 11 enrolled · Nemours Children's Clinic
  NCT04990167updated 2025-12-23
• Two-period 21 Day Cross-over Study to Compare the Pharmacokinetics of Tiotropium From Two Inhalers
  Completed · Phase 1 · Interventional · 40 enrolled · Kindeva Drug Delivery
  NCT03246581updated 2025-12-04
• Airway Effects of Tiotropium in Patients With COPD
  Completed · Phase 3 · Interventional · 44 enrolled · Imperial College London
  NCT02683668updated 2025-08-29
• ANTES B+ Clinical Trial
  Terminated · Phase 4 · Interventional · 48 enrolled · Fundacio Privada Mon Clinic Barcelona
  NCT06282861updated 2025-08-14

Ranked by 2D fingerprint (Tanimoto) similarity over PubChem structures. Structural proximity only — not a claim of therapeutic equivalence.

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• TacrolimusAgents for dermatitis, excluding corticosteroids78%

Frequently asked questions

How does Tiotropium work?

Tiotropium is a long-acting, antimuscarinic agent, which is often referred to as an anticholinergic. It has similar affinity to the subtypes of muscarinic receptors, M 1 to M 5 .

What is Tiotropium used for?

According to FDA labeling, Tiotropium carries indications including: Tiotropium bromide inhalation powder is indicated for the long-term, once-daily, maintenance treatment of bronchospasm associated with chronic obstructive pulmonary disease (COPD), including chronic bronchitis and emphysema. Tiotropium bromide inhalation powder is indicated to reduce exacerbations in COPD patients.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Tiotropium?

Tiotropium is classified as Anticholinergic, Cholinergic Antagonists, Cholinergic Muscarinic Antagonists, Bronchodilation, Decreased Parasympathetic Acetylcholine Activity.

What are the brand names for Tiotropium?

Tiotropium is marketed under brand names including Spiriva, Stiolto.

What are the contraindications for Tiotropium?

Tiotropium labeling lists contraindications including: Tiotropium bromide inhalation powder is contraindicated in patients with a hypersensitivity to tiotropium, ipratropium, or any components of this product [see Warnings and Precautions ( 5.2 )] . In clinical trials and postmarketing experience with tiotropium bromide inhalation powder, immediate hypersensitivity reactions, including angioedema (including swelling of the lips, tongue, or throat), itching, or rash have been reported [see Warnings and Precautions ( 5.2 )] .. Always consult the full prescribing information and a clinician.