Tiotropium is a long-acting antimuscarinic bronchodilator (anticholinergic). It binds with high affinity to muscarinic receptor subtypes (M1–M5). In the airways, it primarily blocks M3 receptors on airway smooth muscle, leading to sustained bronchodilation by inhibiting acetylcholine-mediated bronchoconstriction.
Its antagonism is competitive and reversible, demonstrated in both human and animal studies. In vitro and in vivo models show dose-dependent prevention of methacholine-induced bronchoconstriction, with effects lasting over 24 hours. The bronchodilation achieved through inhalation of Tiotropium is mainly a local, site-specific effect.
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Tiotrop is indicated for the long-term maintenance treatment of bronchospasm associated with Chronic Obstructive Pulmonary Disease (COPD), including chronic bronchitis and emphysema
Adults (≥18 years): The recommended dose is 18 mcg (1 capsule) once daily, administered via the Dry Powder Inhaler device.
The capsule contents are strictly for oral inhalation only and must be used with the inhaler device.
No dosage adjustment is necessary for geriatric, hepatic, or renally impaired patients. However, those with moderate to severe renal impairment should be closely monitored for possible anticholinergic effects.
Most common: Dry mouth (generally mild, resolving with continued therapy).
Other possible effects: Constipation, tachycardia, blurred vision, glaucoma, urinary retention, and urinary difficulty.
Co-administration with cimetidine (400 mg TDS) increased AUC (0–4h) by 20% and reduced renal clearance of Tiotropium by 28%, without a significant change in Cmax or total urinary excretion.
Ranitidine (300 mg OD) did not significantly affect Tiotropium pharmacokinetics.
Hypersensitivity to Tiotropium, atropine, or its derivatives (e.g., ipratropium).
Hypersensitivity to any component of the formulation.
Pregnancy Category C: No adequate human studies available. Should be used only if the potential benefit outweighs the potential risk to the fetus.
Safety in labor and delivery has not been established.
Caution is advised during breastfeeding, as excretion in human milk is unknown.
Capsules are not for oral ingestion—use only with the inhaler device.
Store below 30°C, away from direct sunlight and heat.
Keep out of reach of children.
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