indacaterol, inhaled/glycopyrrolate inhaled

Action and Spectrum

Actions and Spectrum: 

The actions and spectrum of these medications: 

indacaterol (Inhaled): 

It stimulates the beta-2 adrenergic receptors in the smooth muscles of the airways, resulting in bronchodilation. By activating these receptors, indacaterol relaxes the muscles and improves airflow, thereby relieving symptoms of COPD, such as shortness of breath and wheezing. 

By inhibiting the binding of acetylcholine, glycopyrrolate prevents smooth muscle contraction and bronchoconstriction, leading to bronchodilation. It helps relax the airway muscles and improve airflow, reducing symptoms of COPD. 

Spectrum: 

Both indacaterol and glycopyrrolate are indicated for the long-term maintenance treatment of COPD. They improve symptoms, reduce exacerbations, and enhance lung function in individuals with COPD. These medications are not intended for immediate relief of acute symptoms and should be used regularly as prescribed by a healthcare professional. 

It’s important to note that individual responses to these medications may vary, and a healthcare professional should determine the specific dosage and treatment plan based on the individual’s condition and needs.  

Drug Interaction

Adverse Reaction

Black Box Warning

Black Box Warning: 

LABAs; Long-acting beta2-adrenergic agonists increase the risk of death due to asthma. 

The safety and efficacy of glycopyrrolate and indacaterol are not established in asthmatic patients.  

Contraindication / Caution

Contraindication/Caution: 

Contraindications 

• Hypersensitivity 
• Acute Narrow-angle glaucoma 
• Severe allergies 

Cautions 

Caution should be maintained in the people with 

• Diabetes 
• Hyperthyroidism 
• Cardiac disease 
• Urinary retention 
• Pregnancy  
• Breastfeeding 

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: 

indacaterol binds to and activates beta2-adrenergic receptors in the smooth muscle cells of the airways. This leads to the stimulation of adenylate cyclase and a subsequent increase in cyclic adenosine monophosphate (cAMP) levels. Elevated cAMP levels cause relaxation of the bronchial smooth muscle, resulting in bronchodilation and improved airflow. 

glycopyrrolate competitively blocks the action of acetylcholine at muscarinic receptors in the airway smooth muscle, glands, and vagal pathways. Inhibiting the muscarinic receptors prevents the broncho-constrictive effects of acetylcholine, leading to bronchodilation. It also reduces mucus secretion. 

Pharmacodynamics: 

indacaterol is a selective beta2-adrenergic receptor agonist that acts on the smooth muscles of the airways. When inhaled, it binds to and activates the beta2-adrenergic receptors on the bronchial smooth muscle cells. This activation stimulates adenylate cyclase, an enzyme that converts adenosine triphosphate (ATP) into cyclic adenosine monophosphate (cAMP). Increased levels of cAMP lead to the relaxation of the smooth muscles in the airways, resulting in bronchodilation.  

Pharmacokinetics: 

indacaterol 

Absorption 

indacaterol is inhaled using a dry powder inhaler (DPI). After inhalation, it rapidly reaches the lungs, where it is absorbed into the systemic circulation. 

Distribution 

indacaterol binds extensively to plasma proteins, primarily albumin. It has a large volume of distribution, indicating that it is distributed extensively into tissues. 

Metabolism 

The liver mainly metabolizes indacaterol through hydroxylation via the cytochrome P450 enzyme system, primarily CYP3A4. The primary metabolites formed are indacaterol carboxylic acid and indacaterol glucuronide. 

Elimination and Excretion 

Most metabolized indacaterol is excreted in the urine, with less than 1% excreted unchanged. The elimination half-life of indacaterol is approximately 40 hours. 

glycopyrrolate: 

Absorption 

glycopyrrolate is available in both oral and inhaled formulations. When administered orally, it is well absorbed from the gastrointestinal tract. In the inhaled form, such as the DPI or metered-dose inhaler (MDI), glycopyrrolate is primarily deposited in the lungs for local action. 

Distribution 

The distribution of glycopyrrolate in the body needs to be better documented. However, it is expected to be distributed throughout the body after systemic absorption or inhalation. 

Metabolism 

glycopyrrolate undergoes limited metabolism in the liver, mainly through ester hydrolysis. The primary metabolite is N-methyl glycopyrrolate. 

Elimination and Excretion 

The elimination half-life of glycopyrrolate is approximately 2 to 3 hours. It gets excreted primarily in an unchanged form in urine, with a small portion undergoing metabolism. 

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 a while, after that exhale slowly and gently. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: indacaterol/glycopyrrolate 

Pronounced: in-da-KA-ter-ol-& glye-koe-PIR-oh-late 

Why do we use indacaterol/glycopyrrolate? 

indacaterol and glycopyrrolate are combined as fixed-dose medications for treating chronic obstructive pulmonary disease (COPD). 

The fixed-dose combination of indacaterol and glycopyrrolate simplifies the treatment regimen for patients by combining two different bronchodilators into a single inhaler.