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, M1 to M5. In the airways, it exhibits pharmacological effects through inhibition of M3-receptors at the smooth muscle leading to bronchodilation. The competitive and reversible nature of antagonism was shown with human and animal origin receptors and isolated organ preparations. In preclinical in vitro as well as in vivo studies, prevention of methacholine-induced bronchoconstriction effects was dose-dependent and lasted longer than 24 hours. The bronchodilation following inhalation of Tiotropium is predominantly a site-specific effect.

Tiotropium is indicated for the long-term treatment of bronchospasm associated with chronic obstructive pulmonary disease (COPD), including chronic bronchitis and emphysema.

Adult over 18 years: The recommended dose of Tiotropium Dry Powder Inhaler capsule is 18 mcg (1 capsule) once-daily, with the device.

The contents of the Tiotropium Dry Powder Inhaler capsules are only for oral inhalation and should only be used with the device.

No dosage adjustment is required for geriatric, hepatically-impaired, or renally-impaired patients. However, patients with moderate to severe renal impairment given Tiotropium capsule should be monitored closely for anticholinergic effects.

Tiotropium is contraindicated in patients with a history of hypersensitivity to atropine or its derivatives, including ipratropium, or to any component of this product.

The most commonly reported adverse drug reaction was dry mouth. Dry mouth was usually mild and often resolved during continued treatment. Other reactions reported in individual patients and consistent with possible anticholinergic effects included constipation, increased heart rate, blurred vision, glaucoma, urinary difficulty, and urinary retention.

Overdose Effects

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

As an anticholinergic drug, Tiotropium may potentially worsen symptoms and signs associated with narrow-angle glaucoma, prostatic hyperplasia or bladder-neck obstruction and should be used with caution in patients with any of these conditions.

Pregnancy & Lactation

Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women with Tiotropium. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. The safety and effectiveness of Tiotropium has not been studied during labor and delivery.