Action and Spectrum

Actions and Spectrum: 

Actions: 

• Bronchodilation: tiotropium is an anticholinergic agent that acts as a long-acting muscarinic antagonist (LAMA). It works by binding to the muscarinic receptors in the airways and inhibiting the effects of acetylcholine, a neurotransmitter that causes bronchoconstriction. By blocking these receptors, tiotropium helps relax and widen the airways, improving breathing and bronchodilation. 
• Reduction of Mucus Production: tiotropium can also reduce excessive mucus production in the airways. By inhibiting the activity of acetylcholine, it helps to decrease the secretion of mucus, thereby reducing the formation of mucus plugs and improving airflow. 

Spectrum: 

• Chronic Obstructive Pulmonary Disease (COPD): tiotropium is one of the mainstay treatments for COPD. It is used for maintenance therapy to improve lung function, reduce symptoms such as shortness of breath and cough, and prevent exacerbations (flare-ups) in patients with COPD. 
• Asthma: tiotropium is sometimes prescribed as an add-on therapy in adult patients with asthma who have inadequate control of their symptoms despite inhaled corticosteroids and long-acting beta-agonists. It helps to improve lung function and reduce symptoms in certain individuals with asthma. 
• Maintenance Treatment: tiotropium is primarily used as a maintenance treatment, taken regularly over an extended period, to manage the symptoms and prevent exacerbations in patients with COPD or asthma. It is not typically used for immediate relief of acute symptoms. 

Drug Interaction

Adverse Reaction

Frequency defined 

>10% 

Upper respiratory tract infection (41%) 

Sinusitis (11%) 

Dry mouth (16%) 

1-10% 

Abdominal pain 

Angina pectoris 

Allergic reaction 

Cataract 

Constipation 

Chest pain (nonspecific) 

Dyspepsia 

Dysphonia 

Depression 

Edema 

Epistaxis 

Hypercholesterolemia 

Hyperglycemia 

Gastroesophageal reflux 

Herpes zoster 

Infection 

Moniliasis 

Myalgia 

Laryngitis 

Leg pain 

Paresthesia 

Pharyngitis 

Skeletal pain 

Stomatitis (including ulcerative stomatitis) 

Rash 

Rhinitis 

Urinary tract infection 

Vomiting 

<1% 

Angioedema 

Supraventricular tachycardia 

Urinary retention 

Fibrillation 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindications 

Cautions 

• Narrow-angle glaucoma 
• Cardiac disease 
• Urinary retention 
• Pregnancy  
• Breastfeeding 

Pregnancy / Lactation

Pregnancy consideration:  

Few data is available regarding the usage of drug during pregnancy. Untreated asthma during pregnancy can lead to the risk of preeclampsia in infants and prematurity in infants. 

Breastfeeding warnings:  

No data is available regarding the excretion of drug in breast milk. 

Pregnancy category: 

Category A: well-controlled and satisfactory studies show no risk to the fetus in the first or later trimester. 

<b>Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: No data is available for the drug under this category. 

Pharmacology

Pharmacology: 

• Muscarinic Receptor Antagonism: tiotropium selectively binds to and antagonizes the M1 to M5 subtypes of muscarinic receptors, with a higher affinity for the M3 receptors. By inhibiting acetylcholine binding to these receptors, tiotropium prevents the activation of smooth muscle cells in the airways, leading to bronchodilation. 
• Bronchodilation: tiotropium causes relaxation of the smooth muscles lining the airways, resulting in bronchodilation. This action widens the air passages and improves airflow, relieving symptoms such as shortness of breath and wheezing. 
• Blockade of Mucus Secretion: tiotropium also inhibits mucus secretion in the airways. By blocking acetylcholine’s action, it reduces goblet cell activity and decreases mucus production, helping to reduce mucus plugging and improving the clearance of secretions. 

Pharmacodynamics: 

The primary pharmacodynamic effect of tiotropium is bronchodilation. By relaxation of smooth muscles in the airways, tiotropium helps to widen the bronchi and bronchioles, improving airflow and reducing airway resistance. This leads to improved lung function and reduced symptoms such as wheezing, shortness of breath, and cough. 

Pharmacokinetics: 

Absorption 

The bioavailability is 19.5% 

The onset of action takes place in 30 minutes 

Duration of action is greater than 24 hours 

The time to achieve peak effect is 1-4 hour 

Distribution 

Protein-bound is 72% 

Volume of distribution is 32 L/kg 

Metabolism 

Drug gets metabolized in the liver by CYP450-dependent oxidation and following glutathione conjugation. 

Elimination and Excretion 

The half-life is 5-6 days 

The rate of total body clearance is 880 mL/min 

The drug is excreted in the urine 

Adminstartion

Administration: 

Open the inhaler device according to the manufacturer’s instructions. Some inhalers require priming before the first use. Follow the priming instructions if necessary. Exhale away from the inhaler to empty your lungs as much as possible before using the inhaler. 

Hold inhaler upright with the mouthpiece pointing towards you. Ensure that the mouthpiece is clean and free from obstructions. Fix the inhaler in the lips as seal.

Slowly take deep breath through your mouth, and at the same time, press down the dose-release button on the inhaler to release the medication. After inhaling the medication, remove the inhaler from your mouth. Hold your breath for some time and then exhale slowly and gently. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: tiotropium 

Pronounced: tye-oh-troe-pee-um 

Why do we use tiotropium? 

tiotropium is primarily used as a maintenance treatment for respiratory conditions. It is taken regularly, usually once daily, to provide sustained bronchodilation and symptom control over an extended period. It treats COPD and asthma.