edrophonium/atropine

Action and Spectrum

Actions and Spectrum 

edrophonium is a short-acting cholinesterase inhibitor. It works by blocking the action of the enzyme acetylcholinesterase (AChE), which is responsible for breaking down the neurotransmitter acetylcholine (ACh). atropine is an anticholinergic drug, i.e., it blocks the effects of acetylcholine at muscarinic receptors in the parasympathetic nervous system.  

Drug Interaction

Adverse Reaction

Frequency not defined  

None

Black Box Warning

Black Box Warning 

None

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• edrophonium/atropine should not be used in individuals with known hypersensitivity or allergy to these drugs or any of its components. 

Caution: 

• Caution should be exercised when using edrophonium in patients with a history of epilepsy or seizure disorders. 
• atropine should be used with caution in individuals with obstructive disorders of the gastrointestinal tract, urinary tract, or respiratory system. 
• edrophonium should be used with caution in individuals with a history of peptic ulcer disease. 
• atropine can cause tachycardia hence it should be used cautiously in individuals with heart disease. 

Pregnancy / Lactation

Pregnancy consideration: 

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  

edrophonium inhibits the activity of acetylcholinesterase (AChE), an enzyme responsible for breaking down acetylcholine. Acetylcholine is a neurotransmitter which plays a crucial role in transmitting nerve impulses in the parasympathetic nervous system. 

atropine prevents acetylcholine from exerting its effects, leading to inhibition of the parasympathetic response and dominance of the sympathetic nervous system. 

Pharmacodynamics 

The increased concentration of ACh in edrophonium enhances cholinergic transmission, leading to prolonged stimulation of cholinergic receptors. 

atropine engages with acetylcholine for binding to muscarinic receptors, which are found in tissues innervated by the parasympathetic nervous system. By covering these receptors, atropine prevents acetylcholine from activating them. 

Pharmacokinetics 

Absorption   

edrophonium/atropine when given intravenously, both are rapidly absorbed into the bloodstream. 

Distribution 

edrophonium has a relatively small volume of distribution while atropine is distributed throughout the body.  

Metabolism 

edrophonium shows minimal metabolism in the body.  

atropine undergoes metabolism in the liver, through hydrolysis and conjugation.  

Elimination and excretion 

The elimination half-life of edrophonium is around 2 to 10 minutes. It is primarily excreted unchanged in the urine. 

The half-life of atropine ranges from 2 to 4 hours. It excreted through the urine. 

Adminstartion

Administration 

edrophonium/atropine is administered through intravenously (IV).

Patient Information Leaflet

Patient information leaflet 

Generic Name: edrophonium/atropine 

Why do we use edrophonium/atropine? 

edrophonium is used for evaluating myasthenia gravis, a neuromuscular disorder characterized by muscle weakness and fatigue.  

atropine is used in management of symptomatic bradycardia, where the heart rate is too slow and causing insufficient blood flow to vital organs.