neladenoson

Action and Spectrum

Actions and spectrum:  

It belongs to the class of selective adenosine A2A receptor agonist. 

Neladenoson works by enhancing the natural sleep-inducing effects of adenosine which stimulates its physiological action in the brain. 

Drug Interaction

Adverse Reaction

Frequency not defined  

Drowsiness  

Constipation  

Abdominal discomfort  

Diarrhea 

Headache  

Dizziness  

Nausea 

Black Box Warning

Black Box Warning: 

There is specific black box warning associated with neladenoson. 

Contraindication / Caution

Contraindication/Caution:  

The drug is contraindicated in following situations:  

Hypersensitivity 

Depressive Disorder  

History of Suicidal behavior  

Pregnancy / Lactation

Pregnancy Warnings:  

Pregnancy category: N/A  

Lactation:  

Excretion of the drug in human breast milk is unknown  

Pregnancy Categories:    

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

<b>Category B: No evidence of risk to fetus found in animal reproduction studies and there are not enough studies on pregnant women.    

Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for an effect in humans, care must be taken for potential risks in pregnant women.    

Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms, but despite potential risks may be used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category clearly outweigh risks over benefits. These category drugs should be prohibited for pregnant women.    

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

Pharmacology

Pharmacology:  

Neladenoson binds with A2A receptors, and it stimulates the release of GABA.  

It is a major inhibitory neurotransmitter which allows it to calm down brain activity. 

Pharmacodynamics:  

It inhibits glutamate release then it further reduces the brain activity and pushes towards sleep.  

Pharmacokinetics:  

Absorption:  

It is absorbed rapidly within 1 to 2 hours after oral administration.  

Distribution:  

It enters the blood brain barrier to reach target sites in the brain. 

Metabolism:  

The metabolism process occurs under hepatic pathway.  

Excretion:  

The drug is excreted by using fecal route. 

Adminstartion

Administration: 

The drug is available for oral intake.  

Patient Information Leaflet

Patient information leaflet: 

Generic Name: neladenoson  

Why do we use neladenoson?  

It is studied for its efficacy and safety in patients with chronic heart failure. 

Neladenoson is under investigation as a potential treatment for primary insomnia.