Tiotropium: Formula, Presentation, Indications, Mechanism of Action, Dosage, Side Effects, Contraindications and Interactions

It is an anticholinergic quaternary ammonium derivative.

Used as a bronchodilator for the long-term treatment of chronic obstructive pulmonary disease and asthma in adults and pediatric patients 6 years of age and older.

Given once a day, it has minimal side effects for most patients with the exception of xerostomia .

Chemical formula

  • C19H22NO4S2.


Tiotropium is a tiotropium bromide inhalation powder consisting of capsules and a device.

Each hard gelatin capsule contains a dry powder consisting of 18 mcg of tiotropium (equivalent to 22.5 mcg of tiotropium bromide monohydrate) mixed with lactose (which may contain milk proteins).


It is indicated for the once daily long-term maintenance treatment of bronchospasm associated with chronic obstructive pulmonary disease, including chronic bronchitis and emphysema.

Tiotropium is indicated to reduce exacerbations in patients with chronic obstructive pulmonary disease.

The contents of the tiotropium capsules are intended for oral inhalation only, and are intended for administration only with the device that delivers an average of 10.4 mcg of tiotropium in each application.

Mechanism of action

Tiotropium is a long-acting antimuscarinic agent, often referred to as an anticholinergic.

Its action is similar to muscarinic receptors. It is an inhibitor of M3 receptors in smooth muscle and its use leads to bronchodilation.


The recommended dose of tiotropium is two inhalations of the powder content of one capsule, once a day, with the device.

Side effects

The most commonly reported adverse drug reaction was dry mouth.

The dry mouth was generally mild and often resolved during continued treatment.

Other reactions reported in individual patients and consistent with possible anticholinergic effects include constipation, tachycardia, blurred vision, glaucoma (onset or worsening), dysuria, and urinary retention.

Other adverse reactions not previously mentioned that have been reported more frequently in patients with chronic obstructive pulmonary disease treated with Tiotropium include:

  • Dehydration
  • Skin ulcer
  • Estomatitis.
  • Gingivitis.
  • Oropharyngeal candidiasis.
  • Dry Skin.
  • Skin infection
  • Swelling of the joints


Immediate hypersensitivity reactions

Immediate hypersensitivity reactions, including hives , angioedema (including swelling of the lips, tongue, or throat), rash, bronchospasm, anaphylaxis, or itching, can occur after tiotropium administration.

If such a reaction occurs, tiotropium therapy should be stopped immediately and alternative treatments should be considered.

Given the similar structural formula of atropine to tiotropium, patients with a history of hypersensitivity reactions to atropine or its derivatives should be closely monitored for tiotropium-like hypersensitivity reactions.

Tiotropium should be used with caution in patients with lactose sensitivity.

Paradoxical bronchospasm

Inhaled medications, including tiotropium, can cause paradoxical bronchospasm.

If this occurs, it should be treated immediately with a short-acting beta agonist inhaler such as albuterol.

Treatment with tiotropium should be discontinued and other treatments should be considered.

Worsening of narrow-angle glaucoma

Tiotropium should be used with caution in patients with narrow-angle glaucoma.

Be alert to the appearance of symptoms such as: pain or discomfort in the eye, blurred vision, red eyes, conjunctival congestion, visual halos or colored images, and corneal edema.

Worsening urinary retention

Tiotropium should be used with caution in patients with urinary retention. The patient may have difficulty and pain when urinating.

As a predominantly renal excreted drug, patients with moderate to severe renal impairment (creatinine clearance <60 ml / min) treated with Tiotropium should be closely monitored for anticholinergic side effects.

Tiotropium is not indicated for use in children.

The safety and effectiveness of tiotropium in pediatric patients have not been established.

Pregnancy and breastfeeding

The health and developmental benefits of breastfeeding should be considered in conjunction with the mother’s clinical need to use tiotropium against any possible adverse effects on the breastfed child or the underlying maternal condition.


Tiotropium has been used concomitantly with long-acting sympathomimetic bronchodilators (beta-agonists) methylxanthines and oral and inhaled steroids without increasing adverse reactions.

However there is the possibility of an additive interaction with concomitant anticholinergic medicinal products.

Therefore, avoid concomitant administration of tiotropium with other anticholinergic-containing medicinal products, as this may lead to increased anticholinergic adverse effects.