budesonide inhaled/formoterol/glycopyrrolate inhaled

Action and Spectrum

Actions and Spectrum 

Within the respiratory system, budesonide inhaled exerts a localised anti-inflammatory action that is most pronounced in the airways. By controlling the release of inflammatory mediators and lowering the production of cytokines and other elements of the inflammatory response, it lessens inflammation.  

For the treatment of COPD and asthma, formoterol, a long-acting beta-agonist (LABA), is frequently coupled with budesonide in a single inhaler. It causes relaxation and bronchodilation by activating beta-2 adrenergic receptors in the smooth muscles of the airways.  

glycopyrrolate inhaled an anticholinergic drug, is occasionally coupled with budesonide and formoterol in a single inhaler. It functions by inhibiting the neurotransmitter acetylcholine, which causes smooth muscles, especially those in the airways, to constrict. 

Drug Interaction

Adverse Reaction

Frequency defined  

<1% 

Cataracts 

1-10% 

Muscle spasms (2.8-3.3%) 

Oral candidiasis (3%) 

Influenza (2.9%) 

Sinusitis (2.6%) 

Diarrhea (2.1%) 

Urinary tract infection (2.7%) 

Upper respiratory tract infection (5.7%) 

Back pain (3.1%) 

Cough (2.7%) 

Pneumonia (4.6%) 

Dysphonia (3.3%) 

Frequency not defined 

Tachycardia 

Hyperglycemia 

Agitation 

Angina pectoris 

Arrhythmias 

Sign or symptoms of systemic glucocorticoid steroid effects  

Dry mouth 

Chest pain 

Bronchospasm 

Abnormal behavior 

Restlessness 

Throat irritation 

Bruising 

Urinary retention 

Dizziness 

Palpitations 

Depression 

Nervousness 

Tremor 

Headache 

Nausea 

Hypersensitivity 

Anxiety 

Insomnia 

Black Box Warning

Black Box Warning 

There is no black box warning for budesonide inhaled/formoterol/glycopyrrolate inhaled drug. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• People having allergy or hypersensitivity history to budesonide inhaled/formoterol, glycopyrrolate inhaled, or any other component in the formulation should not use the combo medication. 

Caution: 

• Patients with cardiovascular diseases such hypertension (high blood pressure), arrhythmias (irregular heart rhythms), or heart disease should use the combination medication with caution.  
• The budesonide inhaled may have an impact on blood glucose levels. Those with diabetes or those who are at risk for getting it should closely check their blood glucose levels. 
• formoterol is a beta-agonist that may lower serum potassium levels when used. People with low potassium levels or those using drugs that can result in hypokalemia should exercise caution.  
• glycopyrrolate inhaled may impact intraocular pressure, so caution is advised in those with glaucoma, cataracts, or other ocular diseases. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: N/A 

Lactation: Excretion into human milk is unknown  

Pregnancy Categories:         

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:  There is no data available for the drug under this category. 

Pharmacology

Pharmacology  

budesonide inhaled that acts locally in the airways. It helps to lower airway inflammation in disorders like asthma and COPD and has strong anti-inflammatory properties.  

formoterol is a long-acting beta-agonist (LABA). The bronchial tubes relax and enlarge as a result of the stimulation of beta-2 adrenergic receptors in the smooth muscles of the airways. 

The anticholinergic drug glycopyrrolate inhaled works by inhibiting the neurotransmitter acetylcholine, which is implicated in bronchoconstriction and mucus formation. 

Pharmacodynamics 

Leukotrienes and prostaglandins are two inflammatory mediators that are inhibited from being released when budesonide inhaled interacts with inflammatory cells and airway epithelial cells. budesonide inhaled assists in lowering bronchial hyperresponsiveness, preventing mucus secretion, and improving airflow by reducing airway inflammation. 

formoterol activates receptors, which causes the smooth muscles in the bronchial tubes to relax and enlarge, improving airflow. It has a long-lasting effect that contributes to persistent bronchodilation throughout time. 

glycopyrrolate inhaled helps in bronchodilation by relaxing the smooth muscles in the airways by blocking the cholinergic receptors. Additionally, it lessens overproduction of mucus, which aids in mucus removal and enhances ventilation. 

Pharmacokinetics 

Absorption   

budesonide inhaled/formoterol/glycopyrrolate inhaled are all directly administered to the respiratory system when inhaled. The medication particles are typically released into the lungs, where the respiratory mucosa allows for absorption. Particle size, inhalation technique, and the formulation of the medication are just a few examples of the variables that might affect the rate of absorption. 

Distribution 

The body distributes budesonide inhaled/formoterol/glycopyrrolate inhaled to variable degrees. As an inhaled corticosteroid with a high affinity for glucocorticoid receptors, budesonide mainly affects the airways locally. formoterol, a beta-agonist, can bind to beta-2 adrenergic receptors in a variety of organs, including the lungs. It has a systemic distribution. As an anticholinergic, glycopyrrolate typically affects the respiratory system locally, while it can also have systemic effects. 

Metabolism 

In the liver, budesonide inhaled is extensively metabolized, largely by the cytochrome P450 enzyme CYP3A4. It is broken down into several metabolites, with 6-hydroxybudesonide being the primary one. The liver extensively metabolizes formoterol by O-demethylation and glucuronidation.  

glycopyrrolate inhaled is largely metabolized in the liver and plasma through the process of hydrolysis. 

Elimination and excretion 

The routes of elimination for the unmodified medication and its metabolites, including budesonide inhaled/formoterol/glycopyrrolate inhaled, are urine and feces. Each component’s elimination half-life can be different. budesonide inhaled has a 2-to-3-hour elimination half-life, which is quite brief.  

The elimination of half-life of formoterol is prolonged, lasting around 10 hours. The half-life of glycopyrrolate’s elimination is about 8 hours. 

Adminstartion

Administration 

The administration of budesonide inhaled/formoterol/glycopyrrolate inhaled drug involves the use of a handheld inhaler device. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: budesonide inhaled/formoterol/glycopyrrolate inhaled 

Why do we use budesonide inhaled/formoterol/glycopyrrolate inhaled? 

The budesonide inhaled/ formoterol/ glycopyrrolate inhaled medication is recommended for the ongoing management of airflow restriction in COPD patients with chronic bronchitis and emphysema.  

In patients with moderate to severe COPD, it is used to enhance lung function, lessen symptoms including breathlessness and coughing.