umeclidinium bromide/vilanterol inhaled

Action and Spectrum

Actions and Spectrum: 

Actions: 

umeclidinium bromide selectively antagonizes the muscarinic M3 receptors in the airway smooth muscles, preventing the binding of acetylcholine and inhibiting the bronchoconstriction caused by acetylcholine. 

umeclidinium bromide produces bronchodilation by relaxing the smooth muscles in the airways, improving airflow, and reducing airway resistance. It also helps to reduce mucus production.  

vilanterol is a long-acting beta2-adrenergic agonist (LABA). It selectively stimulates the beta2-adrenergic receptors in the bronchial smooth muscles, activating adenylate cyclase and increasing intracellular cyclic adenosine monophosphate (cAMP) levels. 

Spectrum: 

The combination of umeclidinium bromide and vilanterol provides a dual broncho dilatory effect due to their distinct mechanisms of action. This combination medication offers a broader spectrum of bronchodilation compared to using either component alone. By targeting different receptors and signaling pathways, umeclidinium bromide/vilanterol can synergistically relax the smooth airway muscles, reduce airway resistance, and improve lung function in patients with COPD. 

Drug Interaction

Adverse Reaction

Frequency defined 

1-10% 

Pharyngitis (2%) 

Diarrhea (2%) 

Neck pain (1%) 

Chest pain (1%) 

Pain in extremities (2%) 

Muscle spasms (1%) 

Sinusitis (1%) 

Constipation (1%) 

Lower respiratory tract infection (1%) 

<1% 

Productive cough 

Dry mouth 

GERD 

Vomiting 

Dyspepsia 

Abdominal pain 

Musculoskeletal chest pain 

Chest discomfort 

Ventricular extrasystoles 

Supraventricular extrasystoles 

Asthenia 

Atrial fibrillation 

Myocardial infarction 

Rash 

Conjunctivitis 

Pruritus 

Black Box Warning

Contraindication / Caution

Contraindication/Caution: 

Contraindications 

• Hypersensitivity 
• Acute Narrow-angle glaucoma 
• Severe allergies 

Cautions 

Caution should be maintained in the people with 

• Diabetes 
• Asthma 
• Hypokalemia 
• Cardiac disease 
• Seizures 
• Drug Interactions 

Pregnancy / Lactation

Pregnancy consideration:  

No data is available regarding the well-controlled studies on pregnant women.  

Breastfeeding warnings:  

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

Pregnancy category: 

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

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 

umeclidinium bromide selectively antagonizes the muscarinic M3 receptors in the smooth muscles of the airways. By blocking the binding of acetylcholine to these receptors, it inhibits the bronchoconstrictive effects of acetylcholine, leading to bronchodilation. umeclidinium bromide primarily acts locally in the lungs. 

vilanterol selectively stimulates the beta2-adrenergic receptors in the smooth muscles of the airways. This stimulation activates adenylate cyclase, increasing cyclic adenosine monophosphate (cAMP) levels within the cells. Elevated cAMP levels cause relaxation of the bronchial smooth muscle, leading to bronchodilation and improved airflow. vilanterol primarily acts locally in the lungs. 

Pharmacodynamics 

The combination of umeclidinium bromide and vilanterol provides a dual bronchodilatory effect. By targeting different receptors and signaling pathways, the combination produces a synergistic effect, resulting in enhanced bronchodilation and improved lung function compared to using either component alone. 

The pharmacodynamics of umeclidinium bromide/vilanterol help alleviate symptoms associated with COPD. Promoting bronchodilation and improving airflow helps patients with COPD breathe more easily. 

Pharmacokinetics 

umeclidinium bromide: 

Absorption 

After inhalation, umeclidinium bromide is absorbed into the systemic circulation. The absolute bioavailability of umeclidinium bromide following inhalation is low, as most of the inhaled dose remains in the lungs. 

Distribution 

umeclidinium bromide has a large volume of distribution, indicating extensive distribution into the tissues. 

Metabolism 

umeclidinium bromide undergoes minimal metabolism in the liver.  

Elimination and Excretion 

umeclidinium bromide is eliminated mainly through fecal biliary excretion, with minimal renal excretion. 

vilanterol: 

Absorption 

Following inhalation, vilanterol is absorbed into the systemic circulation. The absolute bioavailability of vilanterol following inhalation is low, as most of the inhaled dose remains in the lungs. 

Distribution 

vilanterol has a large volume of distribution, indicating extensive distribution into the tissues. 

Metabolism 

Hepatic enzymes primarily metabolize vilanterol, including cytochrome P450 3A4 (CYP3A4). The main metabolic pathway involves O-dealkylation to form the inactive metabolite GW642444. 

Elimination and Excretion 

The metabolites of vilanterol are eliminated primarily through fecal excretion, with a smaller portion excreted in the urine. 

Combination Pharmacokinetics: 

When used as a fixed-dose combination, the pharmacokinetics of umeclidinium bromide and vilanterol can be influenced by each other. However, due to their low systemic bioavailability, most of the administered dose of both components remains in the lungs, where their local pharmacological effects occur. 

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

Slowly breathe deeply 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: umeclidinium/vilanterol 

Pronounced: ue-ME-kli-DIN-ee-um/vye-LAN-ter-ol  

Why do we use umeclidinium and vilanterol? 

umeclidinium/vilanterol are combined as fixed-dose medications for treating chronic obstructive pulmonary disease (COPD). 

The fixed-dose combination of umeclidinium/vilanterol simplifies the treatment regimen for patients by combining two different bronchodilators into a single inhaler.