Tiotropium
Tiotropium Uses, Dosage, Side Effects, Food Interaction and all others data.
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 bronchodilation following inhalation of Tiotropium is predominantly a site-specific effect.
Tiotropium is a long acting antimuscarinic that causes bronchodilation. The effects of tiotropium last over 24 hours and there is a wide therapeutic index as overdoses are uncommon even at doses well above the recommended maximum.
| Trade Name | Tiotropium |
| Availability | Prescription only |
| Generic | Tiotropium |
| Related Drugs | Dupixent, Xolair, ProAir Digihaler, Symbicort, Breo Ellipta, Ventolin, Xopenex, Ventolin HFA, Spiriva |
| Type | |
| Formula | C19H22NO4S2 |
| Weight | Average: 392.512 Monoisotopic: 392.099024577 |
| Protein binding | Tiotropium is 72% protein bound in plasma. |
| Groups | Approved |
| Therapeutic Class | Anticholinergic bronchodilators |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Tiotropium is used for the long-term, once-daily, maintenance treatment of bronchospasm associated with chronic obstructive pulmonary disease (COPD), including chronic bronchitis and emphysema.
Tiotropium is also used to associated treatment for these conditions: Asthma, Bronchitis, Bronchoconstriction, Chronic Bronchitis, Chronic Obstructive Airways Disease Exacerbated, Chronic Obstructive Pulmonary Disease (COPD), Chronic Obstructive Respiratory Diseases, Emphysema
How Tiotropium works
Tiotropium is an antagonist of muscarinic receptors M1 to M5. Inhibition of the M3 receptor in the smooth muscle of the lungs leads to relaxation of smooth muscle and bronchodilation.
Dosage
Tiotropium dosage
Adults and adolescents 12 years and older: The recommended dosage of Tiotropium bromide is the inhalation of 2 puffsonce daily.
Side Effects
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.
Toxicity
Symptoms of overdose include altered mental status, tremors, abdominal pain, and severe constipation. However, doses of up to 282µg did not lead to systemic anticholinergic effects in a trial of 6 patients. In case of overdose, stop tiotropium and being symptomatic and supportive therapy.
Precaution
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. As a predominantly renally excreted drug, patients with moderate to severe renal impairment treated with Tiotropium should be monitored closely.
Eye pain or discomfort, blurred vision, visual halos or colored images in association with red eyes from conjunctival congestion and corneal edema may be signs of acute narrow angle glaucoma. Should any of these signs and symptoms develop, consult a physician immediately. Miotic eye drops alone are not considered to be effective treatment.
Interaction
Tiotropium has been used concomitantly with other drugs commonly used in COPD without increases in adverse drug reactions. These include sympathomimetic bronchodilators, methylxanthines, and oral and inhaled steroids. However, the co-administration of Tiotropium with other anticholinergic-containing drugs (e.g., ipratropium) has not been studied and is therefore not recommended.
Food Interaction
- Take with or without food. Food is not expected to interfere with absorption.
Tiotropium Drug Interaction
Moderate: albuterol / ipratropium, albuterol / ipratropiumUnknown: fluticasone / salmeterol, aspirin, aspirin, omega-3 polyunsaturated fatty acids, fluticasone nasal, furosemide, metoprolol, metoprolol, polyethylene glycol 3350, nitroglycerin, acetaminophen, albuterol, budesonide / formoterol, albuterol, albuterol, cyanocobalamin, ascorbic acid, cholecalciferol
Tiotropium Disease Interaction
Moderate: angioedema, anticholinergic effects, tachycardia, liver, renal dysfunction
Volume of Distribution
The volume of distribution of tiotropium is 32L/kg.
Elimination Route
33% of an inhaled solution reaches systemic circulation, while oral solutions have a bioavailability of 2-3%. A dry powder for inhalation is 19.5% bioavailable. Tiotropium metered spray for inhalation reaches a maximum concentration in 5-7 minutes.
Half Life
The terminal half life of tiotropium is 24 hours in patients with COPD and 44 hours in patients with asthma.
Clearance
The total clearance of tiotropium is 880mL/min in healthy subjects receiving 5µg daily. The renal clearance of tiotropium was 669mL/min. Patients 2 This decreased clearance is not associated with increased AUC or Cmax.
Elimination Route
74% of intravenous tiotropium was excreted unchanged in urine. 14% of a dry powder inhalation dose was excreted unchanged in the urine. 24 hour urinary excretion after 21 days of 5µg once daily inhalation in patients with COPD is 18.6% and in patients with asthma is 12.8%.
Pregnancy & Breastfeeding use
Pregnancy Category C. Tiotropium should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Use in Labor and Delivery: The safety and effectiveness of Tiotropium has not been studied during labor and delivery.
Nursing Mothers: Clinical data from nursing women exposed to Tiotropium are not available. caution should be exercised if administered to a nursing woman.
Contraindication
Tiotropium is contraindicated in patients with a history of hypersensitivity to atropine or its derivatives, including ipratropium, or to any component of this product.
Special Warning
Pediatric Use: The safety and effectiveness of Tiotropium in pediatric patients have not been established.
Geriatric use: No adjustment of Tiotropium dosage in geriatric patients is warranted.
Acute Overdose
High doses of Tiotropium may lead to anticholinergic signs and symptoms. Acute intoxication by inadvertent oral ingestion of Tiotropium Bromide unlikely since it is not well-absorbed systemically.
Storage Condition
The inhaler should be stored in a dry, cool place away from direct sunlight and heat. The canister should not be broken, punctured or burnt, even when apparently empty. Keep away from eyes. Keep out of reach of children.
Innovators Monograph
You find simplified version here Tiotropium
FAQ
What is Tiotropium used for?
Tiotropium is used to prevent wheezing, shortness of breath, coughing, and chest tightness in patients with chronic obstructive pulmonary disease.
How safe is Tiotropium?
Tiotropium appears to be efficacious, safe, and well tolerated in patients with asthma and COPD. Dose escalation beyond 5 μg has not been shown to improve spirometric or clinical outcomes, and in asthma, it has been associated with a small increase in adverse events.
What are the common side effects of Tiotropium?
The common side effects of Tiotropium are include:
- dry mouth
- constipation
- stomach pain
- vomiting
- indigestion
- muscle pain
- nosebleed
- runny nose
- sneezing
- painful white patches in mouth
How should Tiotropium be used?
Tiotropium is usually inhaled once a day in the morning or evening. To help you remember to inhale tiotropium, inhale it around the same time every day.
Is Tiotropium safe during pregnancy?
The manufacturer makes no recommendation regarding use during pregnancy.The limited data available on use in pregnant women are insufficient to know this drugs risks, including the risk of fetal harm or reproductive effects.
Is Tiotropium safe during breastfeeding?
The manufacturer makes no recommendation regarding use during lactation.There is no information regarding this drug on the presence in human milk, the effects on a breastfed infant, or effects on milk production.
Can I drink alcohol with Tiotropium?
Alcohol is known to interact with a number of medications, many people taking this medication are wondering whether it is safe to consume alcohol while on Tiotropium treatment.
Can I drive after taking Tiotropium ?
This Tiotropium can cause dizziness. Use extreme caution when driving a vehicle or using machinery if you take this Tiotropium.
Can Tiotropium be used in asthma?
Tiotropium is only licensed for use in asthma when delivered using the solution for inhalation device, Respimat.
When is the best time to take Tiotropium?
Tiotropium is usually inhaled once a day in the morning or evening. To help you remember to inhale Tiotropium, inhale it around the same time every day.
How long does it take Tiotropium to work?
Tiotropium may take 4 to 8 weeks before you get the full benefit of this drug.
How often should I use Tiotropium?
Tiotropium is an asthma maintenance medicine taken 1 time each day. You should take 2 puffs 1 time each day,
Does Tiotropium reduce inflammation?
Tiotropium exerts anti-inflammatory effects during resistive breathing, an experimental model of severe airway obstruction.
Does Tiotropium stop coughing?
Tiotropium can actually make the cough reflex more sensitive.
What happen If I missed Tiotropium?
If you miss doses or don’t take the drug on schedule,Your medication may not work as well or may stop working completely.Take your dose as soon as you remember. But if you remember just a few hours before your next scheduled dose, take only one dose. Never try to catch up by taking two doses at once.
What happens If I stop taking Tiotropium?
If you stop taking the drug or don’t take it at all,You may have worsened shortness of breath or other breathing problems.
What happens if I overdose?
If you take overdose or too much,You could have dangerous levels of the drug in your body. If you think you’ve taken too much of this drug, call your doctor or local poison control center.
