Inhalation/Respiratory Maintenance therapy in chronic obstructive pulmonary disease
Adult: As cap for dry powder inhalation: 1 cap (18 mcg or 13 mcg) once daily via the inhaler device. As 2.5 mcg/actuation solution for inhalation: 2 puffs (5 mcg) once daily. Dosage and treatment recommendations may vary among countries and individual products (refer to specific local product guidelines).
Inhalation/Respiratory Asthma
Adult: As an add-on maintenance therapy: As 2.5 mcg/actuation solution for inhalation: 2 puffs (5 mcg) once daily. Full benefits in lung function may be apparent after several doses. Dosage and treatment recommendations may vary among countries and individual products (refer to specific local product guidelines). Child: ≥6 years As an add-on maintenance therapy: As 2.5 mcg/actuation solution for inhalation: Same as adult dose. Dosage and treatment recommendations may vary among countries and individual products (refer to specific local product guidelines).
Contraindications
Hypersensitivity to tiotropium bromide, atropine, or atropine derivatives (e.g. ipratropium bromide, oxitropium bromide).
Special Precautions
Patient with narrow-angle glaucoma; prostatic hyperplasia, bladder neck obstruction; recent MI (<6 months), heart failure (NYHA class III or IV) requiring hospitalisation within the past year, cardiac arrhythmia (which may be unstable, life-threatening, or requiring intervention in the past year). Not indicated to be used as initial or rescue treatment for acute episodes of bronchospasm. Not intended to be used as monotherapy for asthma; asthma patients are recommended to continue with the anti-inflammatory treatment (e.g. inhaled corticosteroids). Moderate to severe renal impairment. Children. Pregnancy and lactation.
This drug may cause dizziness and blurred vision, if affected, do not drive or operate machinery. Avoid accidental contact of the inhaler solution or cap powder with the eyes. Cap for dry powder inhalation: The powder contents of the cap are for inhalation only using the specific device; do not swallow the cap.
Monitoring Parameters
Monitor FEV1, peak flow, and other pulmonary function tests. Assess for signs and symptoms of narrow-angle glaucoma, urinary retention, hypersensitivity reactions, and anticholinergic adverse effects (particularly in patients with moderate to severe renal impairment).
Overdosage
Symptoms: Dry mouth, throat or nasal mucosa; high doses may result in other anticholinergic effects. Management: Symptomatic and supportive treatment.
Drug Interactions
May cause an additive effect which may result in increased anticholinergic events when used with other anticholinergic drugs.
Action
Description: Mechanism of Action: Tiotropium bromide, a quaternary ammonium derivative, is a long-acting antimuscarinic or anticholinergic agent. It has a similar affinity to subtypes 1-5 muscarinic (M1-M5) receptors. In the bronchial smooth muscles, it competitively and reversibly inhibits the action of acetylcholine at subtype 3 muscarinic (M3) receptors, thereby leading to bronchodilation. Pharmacokinetics: Absorption: Absorbed systemically from the lungs. Bioavailability: Approx 33% (solution for inhalation); 19.5% (cap for dry powder inhalation). Time to peak plasma concentration: 5-7 minutes (solution for inhalation); 7 minutes (cap for dry powder inhalation). Distribution: Volume of distribution: 32 L/kg. Plasma protein binding: 72%. Metabolism: Minimal hepatic metabolism by CYP2D6 and CYP3A4 isoenzymes. Excretion: Via urine (7% [cap for dry powder inhalation]; 18.6% in COPD patients and approx 12% in asthma patients [solution for inhalation]). Elimination half-life: Cap for dry powder inhalation: Approx 25 hours (COPD patients). Solution for inhalation: 25 hours (COPD patients); 44 hours (asthma patients).
Chemical Structure
Tiotropium bromide Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5487426, Tiotropium bromide. https://pubchem.ncbi.nlm.nih.gov/compound/Tiotropium-bromide. Accessed Apr. 26, 2024.
Storage
Cap for dry powder inhalation: Store at 25°C. Protect from extreme temperatures and moisture. Do not freeze or store capsules in the inhaler device. Solution for inhalation: Store between 15-30°C. Do not freeze.