xamoterol

Action and Spectrum

Actions and Spectrum: 

Action: xamoterol is a selective beta-1 adrenergic receptor agonist. It specifically targets and activates the beta-1 adrenergic receptors found in the heart muscle. Activating these receptors increases the force and rate of the heart’s contractions, which can benefit certain medical conditions, particularly heart failure. 

Spectrum: The spectrum of xamoterol refers to the range of effects it has on different tissues and organs in the body. Since it is a selective beta-1 adrenergic receptor agonist, its effects are limited to the heart and cardiovascular system. By selectively targeting the beta-1 receptors in the heart, xamoterol avoids activation of beta-2 adrenergic receptors found in other tissues, such as the lungs and blood vessels. 

Drug Interaction

Adverse Reaction

Frequency not defined  

N/A 

Black Box Warning

Black Box Warning:  

None

Contraindication / Caution

Contraindication/Caution:  

Hypersensitivity: xamoterol should not be used in individuals with a known hypersensitivity or allergy to the drug or any of its components. 

Severe Bradycardia: xamoterol is a beta-adrenergic agonist that can lower heart rate. It should not be used in patients with severe bradycardia (very slow heart rate) as it could worsen the condition. 

Heart Block: xamoterol is not recommended for patients with significant heart block, It is a cardiac condition characterized by disruptions in the heart’s electrical conduction system, resulting in the occurrence of slow or irregular heartbeats. 

Cardiogenic Shock: xamoterol should be avoided in patients with cardiogenic shock, A severe type of heart failure occurs when the heart cannot effectively pump an adequate amount of blood to meet the demands of the body. 

Recent Myocardial Infarction (Heart Attack): xamoterol may be contraindicated in patients who have experienced a recent myocardial infarction (heart attack). 

Pregnancy and Breastfeeding: xamoterol’s safety during pregnancy and breastfeeding has not been well-established, The utilization of this approach should be limited to situations where the potential advantages surpass the associated risks. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: N/A 

Lactation: Excreted into human milk is unknown 

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.   

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:  

xamoterol was a beta-adrenergic agonist drug used primarily in treating heart failure. 

Pharmacodynamics:  

xamoterol acts as a selective beta-1 adrenergic receptor agonist, explicitly targeting and activating beta-1 receptors in the heart. This leads to increased cardiac contractility (the force of the heart’s contractions), heart rate (positive chronotropic effect), and cardiac output. By stimulating these receptors, xamoterol helps the heart pump more effectively, improving symptoms and quality of life in heart failure patients.  

Pharmacokinetics: 

Absorption 

xamoterol is administered orally as tablets. After ingestion, it undergoes absorption from the gastrointestinal tract into the bloodstream. The rate and extent of absorption may vary among individuals. 

Distribution 

xamoterol is distributed throughout the body, and its distribution is likely to be restricted mainly to tissues expressing beta-1 adrenergic receptors, such as the heart. The drug may also bind to plasma proteins to some extent. 

Metabolism 

xamoterol undergoes hepatic metabolism, primarily via glucuronidation. The liver metabolizes the drug into various inactive metabolites.  

Excretion and Elimination 

xamoterol and its metabolites are primarily excreted through the renal route. Some small amounts of the drug and its metabolites may be excreted through the feces. The main route of elimination for xamoterol and its metabolites is through the kidneys. They are excreted primarily in the urine. The elimination half-life of xamoterol determines the dosing frequency and can vary among individuals. 

Adminstartion

Administration:  

Dosage: The dosage of xamoterol would be determined by the prescribing physician based on the patient’s specific condition, age, weight, and other relevant factors. 

Route of administration: xamoterol was primarily administered orally tablets or capsules. The medication was typically taken with a glass of water and could be taken with or without food, depending on the doctor’s instructions. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: xamoterol 

Why do we use xamoterol?  

Heart Failure: xamoterol is used to treat mild to moderate heart failure. It works by stimulating the beta-1 receptors in the heart, increasing the heart’s pumping ability, improving cardiac output, and reducing symptoms of heart failure. 

Angina Pectoris: xamoterol may be prescribed to patients with stable angina, By increasing the heart’s pumping capacity and oxygen supply, xamoterol can help alleviate angina symptoms. 

Cardiomyopathy: xamoterol might be used in some instances of dilated cardiomyopathy, a condition where the heart’s ability to pump blood efficiently is impaired. The medication can aid in improving cardiac function and alleviating symptoms.