Edrophonium (by the so-called Tensilon test) is used to differentiate myasthenia gravis A neuromuscular disorder that leads to weakness of skeletal muscles.Myasthenia Gravis
What is edrophonium used to diagnose?
What is edrophonium? Edrophonium is used as part of a medical test to help diagnose a muscle disorder called myasthenia gravis. Edrophonium is sometimes used to reverse the effects of certain medications used to prevent muscle contractions during surgical procedures.
What is the generic name for edrophonium?
Generic Name: edrophonium (ED roe FOE nee um) Brand Name: Enlon, Reversol, Tensilon. Edrophonium is used as part of a medical test to help diagnose a muscle disorder called myasthenia gravis. Edrophonium is sometimes used to reverse the effects of certain medications used to prevent muscle contractions during surgical procedures.
How does edrophonium work in the body?
Mechanism of action Edrophonium works by prolonging the action acetylcholine, which is found naturally in the body. It does this by inhibiting the action of the enzyme acetylcholinesterase. Acetylcholine stimulates nicotinic and muscarinic receptors.
What is edrophonium chloride used for in MG?
Edrophonium chloride is an acetylcholinesterase inhibitor that has been used for the diagnosis of MG since the 1960s. The short duration of action of edrophonium that made it unsatisfactory as a therapeutic agent for MG makes it useful as a diagnostic agent.
Why is edrophonium used to diagnose myasthenia gravis?
The Tensilon test uses the drug Tensilon (edrophonium) to help your doctor diagnose myasthenia gravis. Tensilon prevents the breakdown of the chemical acetylcholine, a neurotransmitter that nerve cells release to stimulate your muscles.
What is edrophonium used for?
Edrophonium injection is used to help diagnose myasthenia gravis (severe muscle weakness) and may be used to help select the proper treatment for the disease. It is also used to reverse the effects of certain muscle relaxants (eg, gallamine, tubocurarine) during surgery or after an overdose of the muscle relaxant.
Why is edrophonium used after surgery?
Edrophonium is used to help the muscles work again after surgery.
What is the mechanism of action of edrophonium?
7.7Mechanism of Action Edrophonium works by prolonging the action acetylcholine, which is found naturally in the body. It does this by inhibiting the action of the enzyme acetylcholinesterase. Acetylcholine stimulates nicotinic and muscarinic receptors. When stimulated, these receptors have a range of effects.
How does the Edrophonium test work?
First, a small amount of the drug Tensilon (edrophonium chloride) is injected into your arm or hand via an IV needle. Once injected, the drug usually kicks in within 30 to 45 seconds. Your doctor will then ask you to perform a series of movements over and over again to see if the drug is working.
How does edrophonium inhibit acetylcholinesterase?
Edrophonium. Edrophonium is the only short-acting anticholinesterase available; it is a synthetic quaternary ammonium compound. The drug competes with acetylcholine and binds by a non-covalent bond to acetylcholinesterase at the anionic site.
What is edrophonium an antidote for?
Generic Name Edrophonium DrugBank Accession Number DB01010 Background. A rapid-onset, short-acting cholinesterase inhibitor used in cardiac arrhythmias and in the diagnosis of myasthenia gravis. It has also been used as an antidote to curare principles.
What is treatment for myasthenia gravis?
The first medicine used for myasthenia gravis is usually a tablet called pyridostigmine, which helps electrical signals travel between the nerves and muscles. It can reduce muscle weakness, but the effect only lasts a few hours so you'll need to take it several times a day.
Why does edrophonium improve Annie's muscle function?
Edrophonium thus increases the likelihood of a nerve signal being successfully transmitted to the muscle. It improves nerve transmission to the muscles and allows these muscles to function normally.
What type of medication is edrophonium?
What is this medicine? EDROPHONIUM (ed ruh FOH nee uhm) works on the nervous system of the body. It is used to test for muscle response and to diagnose myasthenia gravis. It is also used to check for a response to drug therapy in patients with myasthenia gravis.
How do you diagnose myasthenia gravis?
The main test for myasthenia gravis is a blood test to look for a type of antibody (produced by the immune system) that stops signals being sent between the nerves and muscles. A high level of these antibodies usually means you have myasthenia gravis.
What is the mechanism of myasthenia gravis?
Myasthenia gravis is an autoimmune disease of the neuromuscular junction (NMJ) caused by antibodies that attack components of the postsynaptic membrane, impair neuromuscular transmission, and lead to weakness and fatigue of skeletal muscle.
What is edrophonium an antidote for?
Generic Name Edrophonium DrugBank Accession Number DB01010 Background. A rapid-onset, short-acting cholinesterase inhibitor used in cardiac arrhythmias and in the diagnosis of myasthenia gravis. It has also been used as an antidote to curare principles.
How do you diagnose myasthenia gravis?
The main test for myasthenia gravis is a blood test to look for a type of antibody (produced by the immune system) that stops signals being sent between the nerves and muscles. A high level of these antibodies usually means you have myasthenia gravis.
What is the cause of myasthenia gravis?
Cause of myasthenia gravis Myasthenia gravis is caused by a problem with the signals sent between the nerves and the muscles. It's an autoimmune condition, which means it's the result of the immune system (the body's natural defence against infection) mistakenly attacking a healthy part of the body.
How do you administer edrophonium?
For Use as a Curare Antagonist: Enlon (edrophonium injection) ® should be administered by intravenous injection in 1 mL (10 mg) doses given slowly over a period of 30 to 45 seconds so that the onset of cholinergic reaction can be detected. This dosage may be repeated whenever necessary.
What is edrophonium used for?
Edrophonium is a medication used in the diagnosis of myasthenia gravis. It is in the acetylcholinesterase class of drugs. This activity reviews the indications, action, contraindications for edrophonium as a valuable agent in the management of myasthenia gravis.
What is the antidote for edrophonium?
Atropine is an ideal antidote for edrophonium since it has a similar onset of action as edrophonium. Atropine functions by competitively inhibiting the muscarinic receptors on structures innervated by postganglionic cholinergic nerves and inhibiting muscarinic receptors on smooth muscle. [13]
What is the best treatment for edrophonium overdose?
The treatment of an edrophonium overdose is atropine. Atropine is an ideal antidote for edrophonium since it has a similar onset of action as edrophonium.
What are the side effects of edrophonium?
The adverse effects of edrophonium occur due to the increased levels of acetylcholine binding to muscarinic acetylcholine receptors. The more serious adverse effects are cardiac arrhythmias, especially bradycardia, atrioventricular block, and cardiac arrest. The muscarinic cholinergic adverse effects also include bronchoconstriction due to airway smooth muscle contraction secondary to increased stimulation of muscarinic receptors. Other adverse effects include bronchial secretions, diarrhea, salivation, lacrimation, increased urinary frequency and urgency, and miosis. The majority of the adverse effects can be attenuated with the simultaneous administration of atropine, which functions as a muscarinic receptor antagonist to prevent the development of these cholinergic adverse effects. [11]
What is atropine used for?
Atropine is reserved for situations where serious side effects of bradycardia or bronchospasm manifest in patients receiving edrophonium. [2][9] Edrophonium is rarely utilized for the reversal of non-depolarizing NMBA after a surgical procedure.
Is edrophonium a neuromuscular blocking agent?
Edrophonium is FDA-approved for use in the reversal of non-depolarizing neuromuscular blocking agents (NMBA) after a surgical procedure. Nonetheless, neostigmine is preferably utilized instead of edrophonium in the reversal of non-depolarizing NMBA. Neostigmine has a longer duration of action, and it is 12 to 16 times more potent than edrophonium making it more effective in reversing long-acting non-depolarizing NMBA. In rare cases, when using edrophonium as a reversing agent, it is administered simultaneously with atropine to minimize the muscarinic side effects. If administering glycopyrronium with edrophonium, its administration must be a few minutes before edrophonium since it has a slower onset of action. [4][5][6]
Is Neostigmine more effective than Edrophonium?
Neostigmine has a longer duration of action, and it is 12 to 16 times more potent than edrophonium making it more effective in reversing long-acting non-depolarizing NMBA. In rare cases, when using edrophonium as a reversing agent, it is administered simultaneously with atropine to minimize the muscarinic side effects.
What is edrophonium used for?
Edrophonium. Edrophonium is a cholinesterase inhibitor used to diagnose and evaluate myasthenia gravis. A rapid-onset, short-acting cholinesterase inhibitor used in cardiac arrhythmias and in the diagnosis of myasthenia gravis. It has also been used as an antidote to curare principles.
How does edrophonium chloride work?
Mechanism of action. Edrophonium works by prolonging the action acetylcholine, which is found naturally in the body.
How long does edrophonium last?
Edrophonium is a short and rapid-acting anticholinesterase drug. Its effect is manifest within 30 to 60 seconds after injection and lasts an average of 10 minutes. Edrophonium's pharmacologic action is due primarily to the inhibition or inactivation of acetylcholinesterase at sites of cholinergic transmission.
Which drug may increase the excretion rate of Edrophonium?
Trichlormethiazide may increase the excretion rate of Edrophonium which could result in a lower serum level and potentially a reduction in efficacy. Triethylenetetramine. Edrophonium may decrease the excretion rate of Triethylenetetramine which could result in a higher serum level. Triflupromazine.
Does Edrophonium lower the excretion rate of Vortioxetine?
Edrophonium may decrease the excretion rate of Vortioxetine which could result in a higher serum level. Edrophonium may decrease the excretion rate of Warfarin which could result in a higher serum level. Zaleplon may decrease the excretion rate of Edrophonium which could result in a higher serum level.
Does edrophonium lower vaborbactam?
Edrophonium may decrease the excretion rate of Vaborbactam which could result in a higher serum level. Valaciclovir may decrease the excretion rate of Edrophonium which could result in a higher serum level. Edrophonium may decrease the excretion rate of Valbenazine which could result in a higher serum level.
Does edrophonium increase serum levels?
Antihemophilic factor (recombinant), PEGylated. Edrophonium may decrease the excretion rate of Antihemophilic factor (recombinant), PEGylated which could result in a higher serum level. Antipyrine. Antipyrine may decrease the excretion rate of Edrophonium which could result in a higher serum level.
What is the purpose of edrophonium test?
Edrophonium (by the so-called Tensilon test) is used to differentiate myasthenia gravis from cholinergic crisis and Lambert-Eaton. In myasthenia gravis, the body produces autoantibodies which block, inhibit or destroy nicotinic acetylcholine receptors in the neuromuscular junction. Edrophonium—an effective acetylcholinesterase inhibitor —will ...
What is edrophonium made of?
Edrophonium, ethyl- (3-hydroxyphenyl)dim ethylammonium chloride, is made by reacting 3-dimethylaminophenol with ethyl bromide, which forms ethyl (3-hydroxyphenyl)dimethylammonium bromide, the bromine atom of which is replaced with a chlorine atom by reacting it with silver chloride, giving edrophonium.
Is edrophonium a reversible acetylcholinesterase inhibitor?
Edrophonium is a readily reversible acetylcholinesterase inhibitor. It prevents break down of the neurotransmitter acetylcho line and acts by competitive ly inhibiting the enzyme acetylcholinesterase, mainly at the neuromuscular junction. It is sold under the trade names Tensilon and Enlon (according to FDA Orange Book ).
Does edrophonium increase muscle strength?
Consequently, there will typically be not as much increase in muscle strength observed after edrophonium injection, if any with LEMS. The Tensilon test may also be used to predict if neurotoxic paralysis caused by snake envenomation is presynaptic or postsynaptic.
Does edrophonium bind to a cholinergic receptor?
It binds to a Serine-103 allosteric site, while pyridostigmine and neostigmine bind to the AchE active site for their inhibitory effects. In a cholinergic crisis, where a person has too much neuromuscular stimulation, edrophonium will make the muscle weakness worse by inducing a depolarizing block.
What is this medicine?
EDROPHONIUM (ed ruh FOH nee uhm) works on the nervous system of the body. It is used to test for muscle response and to diagnose myasthenia gravis. It is also used to check for a response to drug therapy in patients with myasthenia gravis. It can be used to reverse the effects of certain muscle relaxants used during surgery.
How should I use this medicine?
This medicine is for injection into a muscle or a vein. It is given by a health care professional in a hospital or clinic setting.
What should I watch for while using this medicine?
Your condition will be monitored carefully while you are receiving this medicine.
What side effects may I notice from receiving this medicine?
Side effects that you should report to your doctor or health care professional as soon as possible:
Where should I keep my medicine?
This drug is given in a hospital or clinic and will not be stored at home.
How does edrophonium work?
Edrophonium is a rapid-acting anticholinesterase drug of short duration that improves symptoms of myasthenia gravis by inhibiting the breakdown of ACh and increasing its concentration in the neuromuscular junction. A test dose of 0.015 mg/kg is given intravenously; if it is tolerated, the full dose of 0.15 mg/kg (up to 10 mg) is given. If measurable improvement in ocular muscle or extremity strength occurs, myasthenia gravis is likely. Because edrophonium may precipitate a cholinergic crisis (e.g., bradycardia, hypotension, vomiting, bronchospasm), atropine and resuscitation equipment should be available.
What is edrophonium test?
The Edrophonium Test. Edrophonium is a short-acting acetylcholinesterase inhibitor that is used only for diagnostic purposes; the half-life is so short that this medication has no therapeutic value.
How long does edrophonium last?
The effect begins within about 30–40 seconds and lasts about 8–10 minutes. Patients will usually show improvement of ptosis.
What is demecarium used for?
It is used to constrict pupils, elevate intraocular pressure in treating glaucoma, and also for alleviating atropine mydriasis.
What inhibits the breakdown of ACh?
Binding of acetylcholinesterase inhibits the breakdown of ACh, increasing the amount of neurotransmitter available to stimulate the reduced number of ACh receptors in the synaptic cleft of the neuromuscular junction.
How to administer edrophonium?
Edrophonium (Tensilon), an AChE inhibitor, administered intravenously to a suspected MG patient may transiently improve certain symptoms, providing supportive evidence for the diagnosis. For an appropriate examination, a markedly affected, easily testable and/or observable muscle should be selected (frequently the deltoid or an upper extremity extensor). Two 1-ml tuberculin syringes should be prepared: one as a placebo injection (1 ml normal saline) and one as an injection of 10 mg of edrophonium in 1 ml of solution. The placebo is usually administered first, with observation for improvement for a few minutes. The edrophonium is administered next with an initial dose of 2 mg, with observation and/or strength testing for 1 min. If no improvement is noted, the remaining 8 mg is given and the process is repeated. If no effect is noted following the second dose, the test is negative. Any symptomatic improvement in responsive patients is short lived, lasting no longer than 30 min. Ideally, the patient should not take any AChE inhibitor for at least 24 h before the test. Several cholinergic side effects may appear following intravenous edrophonium, including asystole, bradycardia, syncope nausea, and excessive lacrimation and salivation, and the examiner must be aware of these risks, which in certain patients are relative contraindications for this test. Reported sensitivities and specificities for this test are 90–95% and 80–95%, respectively, in generalized and 80–95% and 80–90% in ocular MG, but these data depend greatly on a carefully performed and judiciously interpreted examination and are subject to significant error in the hands of a careless examiner.
Which drugs contain quaternary ammonium?
Pyridostigmine, neostigmine, and edrophonium all contain a quaternary ammonium group, limiting lipid solubility and preventing passage through the blood-brain barrier. Physostigmine lacks the quaternary ammonium group enabling it to pass freely into the CNS.170 The longer-acting agents, pyridostigmine, neostigmine, and physostigmine, contain a carbamate group that forms a reversible covalent bond with acetylcholinesterase. Edrophonium, lacking a carbamate group, forms short-lived electrostatic and hydrogen bonds with acetylcholinesterase, accounting for its shorter activity.
What is edrophonium used for?
Edrophonium injection is used to help diagnose myasthenia gravis (severe muscle weakness) and may be used to help select the proper treatment for the disease. It is also used to reverse the effects of certain muscle relaxants (eg, gallamine, tubocurarine) during surgery or after an overdose of the muscle relaxant.
Who gives edrophonium?
Edrophonium is to be given only by or under the direct supervision of a doctor.
What are the medical problems with edrophonium?
Make sure you tell your doctor if you have any other medical problems, especially: Allergy to sulfites, history of— May cause severe allergic reactions. Asthma or other breathing problems, history of or.
Is edrophonium safe for children?
Appropriate studies performed to date have not demonstrated pediatric-specific problems that would limit the usefulness of edrophonium injection in children.
Can you have allergies to edrophonium?
Tell your doctor if you have ever had any unusual or allergic reaction to edrophonium or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.
Does edrophonium cause side effects?
Edrophonium side effects. Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention. Check with your doctor or nurse immediately if any of the following side effects occur:
Can edrophonium cause anaphylaxis?
Edrophonium may cause serious types of allergi c reactions, including anaphylaxis. Anaphylaxis can be life-threatening and requires immediate medical attention. Tell your doctor or nurse right away if you have itching, hoarseness, trouble breathing, trouble swallowing, or any swelling of your hands, face, mouth, or throat while you are receiving edrophonium.
Why do doctors order edrophonium?
Doctors usually order the edrophonium test when there’s suspicion that the patient has myasthenia gravis. They also use it to control the dose of anticholinesterase drugs when a diagnosis of the disease has already taken place and the patients taking these drugs as treatment.
What is the edrophonium test?
The edrophonium test, in addition to being called the Tensilon® test, is also called the Anticude® test. These names vary because they refer to the brand name of the drug.
How is the edrophonium test performed?
First, a specialist places an intravenous needle into the patient’s arm or hand.
What is the purpose of edrophonium test for myasthenia gravis?
When a patient with myasthenia gravis undergoes the edrophonium test, the muscles are more powerful. In addition, this test also makes it possible to evaluate which is the most suitable treatment in terms of dosage.
Why do doctors prescribe myasthenia gravis?
The objective’s to study a patient’s muscular fatigue. Therefore, doctors prescribe it to diagnose and assess the response to treatment in myasthenia gravis.
Does edrophonium cause muscle stimulation?
The edrophonium test causes no breakdown of acetylcholine. An enzyme called acetylcholinesterase is responsible for this breakdown. As it’s not broken down, there is more concentration. Therefore, muscle stimulation is greater.
What is the purpose of tensilon test?
The Tensilon test uses the drug Tensilon (edrophonium) to help your doctor diagnose myasthenia gravis. Tensilon prevents the breakdown of the chemical acetylcholine, a neurotransmitter that nerve cells release to stimulate your muscles.
How does anticholinesterase work?
Anticholinesterase drugs work by preventing the breakdown of acetylcholine in people with myasthenia gravis. Labored breathing and extremely weak muscles are symptoms that your myasthenia gravis has worsened or that you’ve overdosed on the medication. The Tensilon test helps your doctor determine the right treatment.
What is the name of the anticholinesterase drug that is administered to confirm myasthenia gravis?
If it does, you may be diagnosed with myasthenia gravis. Your doctor may also administer another anticholinesterase drug, called neostigmine (Prostigmin), to confirm the diagnosis.
Identification
- Summary
1. Edrophoniumis a cholinesterase inhibitor used to diagnose and evaluate myasthenia gravis. - Brand Names
1. Enlon, Enlon-plus
Pharmacology
- Indication
1. For the differential diagnosis of myasthenia gravis and as an adjunct in the evaluation of treatment requirements in this disease. It may also be used for evaluating emergency treatment in myasthenic crises.Reduce drug development failure ratesBuild, train, & validate machine-learnin…
Interactions
- Drug Interactions information
1. This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist. - Food Interactions
1. No interactions found.
Categories
- ATC Codes
1. V04CX07 — Edrophonium
Chemical Identifiers
- UNII
1. 70FP3JLY7N - CAS number
1. 312-48-1
References
- Synthesis Reference
1. Terrell, R.C.; U.S. Patents 3,469,011; September 23, 1969 and 3,527,813; September 8,1970; both assigned to Air Reduction Company, Incorporated. - General References
1. Not Available
Properties
- State
1. Liquid
Spectra
- Mass Spec (NIST)
1. Not Available
Overview
Edrophonium is a readily reversible acetylcholinesterase inhibitor. It prevents breakdown of the neurotransmitter acetylcholine and acts by competitively inhibiting the enzyme acetylcholinesterase, mainly at the neuromuscular junction. It is sold under the trade names Tensilon and Enlon (according to FDA Orange Book).
Clinical uses
Edrophonium (by the so-called Tensilon test) is used to differentiate myasthenia gravis from cholinergic crisis and Lambert-Eaton. In myasthenia gravis, the body produces autoantibodies which block, inhibit or destroy nicotinic acetylcholine receptors in the neuromuscular junction. Edrophonium—an effective acetylcholinesterase inhibitor—will reduce the muscle weakness by blocking the enzymatic effect of acetylcholinesterase enzymes, prolonging the presence of acetyl…
Chemistry
Edrophonium, ethyl-(3-hydroxyphenyl)dimethylammonium chloride, is made by reacting 3-dimethylaminophenol with ethyl bromide, which forms ethyl(3-hydroxyphenyl)dimethylammonium bromide, the bromine atom of which is replaced with a chlorine atom by reacting it with silver chloride, giving edrophonium.
Pharmacokinetics
The drug has a brief duration of action, about 10–30 mins.
Further reading
• Brenner GM (2000). Pharmacology. Philadelphia, PA: W. B. Saunders Company. ISBN 0-7216-7757-6.
• Canadian Pharmacists Association (2000). Compendium of Pharmaceuticals and Specialties (25th ed.). Toronto, ON: Webcom. ISBN 0-919115-76-4.