isoetharine

Action and Spectrum

Actions and spectrum: 

Action: 

• Bronchodilation: Isoetharine stimulates beta-2 adrenergic receptors in the bronchial smooth muscle. This activation leads to relaxation of the smooth muscle, resulting in bronchodilation. This effect is beneficial in the treatment of conditions such as asthma and COPD where bronchoconstriction is a key feature. 
• Relief of Bronchoconstriction: By promoting the relaxation of bronchial smooth muscle, isoetharine helps alleviate bronchoconstriction, which is a narrowing of the airways. This action facilitates increased airflow and improved breathing for individuals with respiratory conditions characterized by airway constriction. 
• Treatment of Acute Bronchospasm: Isoetharine is often used in the treatment of acute bronchospasm, providing rapid relief for individuals experiencing sudden and severe narrowing of the airways. 
• Selective Beta-2 Agonist: Isoetharine’s selectivity for beta-2 receptors makes it more specific to the bronchial smooth muscle, reducing the likelihood of unwanted cardiovascular side effects associated with beta-1 receptor stimulation. 

Spectrum: 

• Isoetharine’s spectrum of action is primarily focused on the respiratory system. It is used in the management of reversible airway obstruction due to conditions such as asthma, bronchitis, and emphysema. Isoetharine is often administered via inhalation to provide rapid and targeted relief of bronchoconstriction. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Palpitations 

elevated BP 

angina 

Tremor 

headache 

Weakness 

restlessness 

tachycardia 

chest tightness 

Dizziness 

nervousness 

insomnia 

Drowsiness 

Dry mouth 

vomiting 

Diarrhea 

Nausea 

heartburn 

Bronchospasm 

anorexia 

Black Box Warning

Black Box Warning: 

there is no specific black box warning associated with isoetharine. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity: Individuals with known allergic or hypersensitivity to isoetharine or any of its components should avoid its use. 
• Cardiovascular Conditions: Isoetharine can have cardiovascular effects, including an increase in heart rate and blood pressure. Therefore, it is contraindicated in individuals with pre-existing cardiovascular conditions such as severe hypertension, tachyarrhythmias (rapid heart rhythms), and coronary artery disease. 
• Hyperthyroidism: Individuals with overactive thyroid gland, may be at an increased risk of cardiovascular effects with beta-agonists like isoetharine. Isoetharine use may exacerbate cardiovascular symptoms in individuals with hyperthyroidism. 

Caution: 

• Diabetes: Beta-agonists like isoetharine may affect blood glucose levels. Individuals with diabetes should use isoetharine with caution, and glucose levels should be carefully monitored. Adjustments to diabetes medications may be necessary. 
• Seizure Disorders: Isoetharine may lower the seizure threshold, and caution should be exercised in individuals with a history of seizure disorders. The risk and benefits of isoetharine use should be carefully considered in such cases. 
• Pediatric and Geriatric Populations: Caution is advised when using isoetharine in pediatric and geriatric populations, as they may be more susceptible to certain side effects or variations in drug response. 

Comorbidities: 

• Allergies: Individuals with asthma may have allergies as a common comorbidity. Allergic triggers can contribute to asthma symptoms. 
• Gastroesophageal Reflux Disease (GERD): GERD is known to be more prevalent in individuals with asthma. The presence of GERD can worsen asthma symptoms. 
• Obesity: Obesity is a common comorbidity with asthma and may contribute to the severity of respiratory symptoms. 
• Anxiety and Depression: Mental health conditions are known to be associated with respiratory conditions such as asthma and COPD. 

Pregnancy / Lactation

Pregnancy consideration: pregnancy category: not assigned 

Lactation: excreted into human milk: unknown 

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

Pharmacology

Pharmacology: 

Isoetharine is a bronchodilator medication belonging to the class of beta-adrenergic agonists. Its pharmacology involves selectively stimulating beta-2 adrenergic receptors, particularly in the smooth muscle of the respiratory tract. Activation of receptors leads to the relaxation of bronchial smooth muscle, resulting in bronchodilation. This mechanism is especially beneficial in the treatment of reversible airway obstruction conditions, such as asthma and chronic obstructive pulmonary disease (COPD), where constriction of the airways is a key feature.

Isoetharine’s bronchodilatory effects enhance airflow and alleviate symptoms of bronchospasm. The medication is typically administered via inhalation, allowing for rapid and targeted action. While isoetharine has been used historically, newer bronchodilators with improved safety profiles are now more commonly prescribed. The use of isoetharine and its pharmacological effects should be carefully considered based on patient needs and the latest medical guidelines. 

Pharmacodynamics: 

• Beta-2 Adrenergic Agonism: Isoetharine is a selective beta-2 adrenergic agonist, meaning it specifically targets and stimulates beta-2 receptors in the bronchial smooth muscle. 
• Smooth Muscle Relaxation: Activation of beta-2 receptors leads to the relaxation of bronchial smooth muscle. This relaxation results in bronchodilation, widening the airways and improving airflow. 
• Inhibition of Bronchoconstriction: Isoetharine’s primary action is to counteract bronchoconstriction, a narrowing of the airways that occurs in conditions such as asthma and COPD. 
• Increased Cyclic AMP (cAMP) Production: Stimulation of beta-2 receptors activates the adenylate cyclase enzyme, leading to increased cyclic AMP (cAMP) production. Elevated cAMP levels contribute to smooth muscle relaxation and inhibit the release of mediators that promote bronchoconstriction. 
• Reduction of Mast Cell Mediators: Beta-2 receptor activation can also reduce the release of mediators from mast cells, such as histamine, which are involved in the inflammatory response and bronchoconstriction. 

Pharmacokinetics: 

• Absorption: Isoetharine is typically administered via inhalation as an aerosol or nebulized solution. Through inhalation, the drug is absorbed directly into the respiratory system, where it can exert its bronchodilatory effects. 
• Distribution: After absorption, isoetharine is distributed throughout the body via the bloodstream. Its primary site of action is the smooth muscle of the respiratory tract, where it selectively stimulates beta-2 adrenergic receptors. 
• Metabolism: Isoetharine undergoes metabolism primarily in the liver. The specific metabolic pathways and the identity of metabolites may vary. The metabolism of beta-2 agonists like isoetharine is often associated with cytochrome P450 enzymes. 
• Excretion: Metabolized isoetharine and its metabolites are excreted primarily through the kidneys. Some unchanged drug and metabolites may also be excreted in the urine. Isoetharine has a short half-life, meaning it is eliminated from the body within a relatively brief period. The specific half-life may vary among individuals.

Adminstartion

Administration: 

• Metered-Dose Inhaler (MDI): Isoetharine is available in metered-dose inhalers, which deliver a specific, measured dose of the medication with each actuation. Patients should be instructed on proper inhalation technique to ensure effective delivery to the lungs. 
• Nebulized Solution: Isoetharine can be administered as a nebulized solution using a nebulizer machine. The liquid solution is converted into a fine mist that inhales through a mask or mouthpiece. Nebulized administration is often used in individuals who may have difficulty using inhalers. 
• Dosage and Frequency: The frequency and dosage of isoetharine administration depend on the severity of the respiratory condition being treated.  
• Individualized Treatment Plan: The use of isoetharine should be part of an individualized treatment plan developed in consultation with healthcare professionals. The plan may also include other medications and strategies for managing respiratory conditions such as asthma or chronic obstructive pulmonary disease (COPD). 

Patient Information Leaflet

Patient information leaflet 

Generic Name: isoetharine 

Pronounced: (eye soe eth a reen) 

Why do we use isoetharine? 

Isoetharine is a bronchodilator medication primarily used for the short-term relief of symptoms associated with reversible airway obstruction conditions, such as asthma and chronic obstructive pulmonary disease (COPD). As a selective beta-2 adrenergic agonist, isoetharine works by stimulating beta-2 receptors in the smooth muscle of the respiratory tract, leading to bronchial smooth muscle relaxation and bronchodilation.

This results in improved airflow, alleviating symptoms like wheezing, shortness of breath, and bronchospasm. Isoetharine is typically administered via inhalation using metered-dose inhalers or nebulizers, allowing for rapid delivery to the lungs. While isoetharine has been historically used, newer bronchodilators with improved safety profiles are now more commonly prescribed.