Details
Stereochemistry | ACHIRAL |
Molecular Formula | C10H16NO.Cl |
Molecular Weight | 201.693 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[Cl-].CC[N+](C)(C)C1=CC=CC(O)=C1
InChI
InChIKey=BXKDSDJJOVIHMX-UHFFFAOYSA-N
InChI=1S/C10H15NO.ClH/c1-4-11(2,3)9-6-5-7-10(12)8-9;/h5-8H,4H2,1-3H3;1H
Molecular Formula | C10H15NO |
Molecular Weight | 165.2322 |
Charge | 0 |
Count |
|
Stereochemistry | RACEMIC |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | ClH |
Molecular Weight | 36.461 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: http://www.rxlist.com/enlon-drug.htm
Sources: http://www.rxlist.com/enlon-drug.htm
Edrophonium is a short and rapid-acting cholinergic drug. Chemically, edrophonium is ethyl (m-hydroxyphenyl) dimethylammonium. Edrophonium is used 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. Because of its brief duration of action, it is not recommended for maintenance therapy in myasthenia gravis. It is also useful whenever a curare antagonist is needed to reverse the neuromuscular block produced by curare, tubocurarine, gallamine triethiodide or dimethyl-tubocurarine. It is not effective against decamethonium bromide and succinylcholine chloride. It may be used adjunctively in the treatment of respiratory depression caused by curare overdosage.
Originator
Sources: https://www.google.com/patents/US2647924
Curator's Comment: reference retrieved from http://www.drugfuture.com/chemdata/edrophonium-chloride.html # Hoffmann La Roche
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL220 |
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Target ID: CHEMBL1914 Sources: https://www.ncbi.nlm.nih.gov/pubmed/21397501 |
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Target ID: CHEMBL2362997 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8109771 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Diagnostic | ENLON Approved UseEnlon (edrophonium injection) ® is recommended 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. Because of its brief duration of action, it is not recommended for maintenance therapy in myasthenia gravis.
Enlon (edrophonium injection) ® is also useful whenever a curare antagonist is needed to reverse the neuromuscular block produced by curare, tubocurarine, gallamine triethiodide or dimethyl-tubocurarine. It is not effective against decamethonium bromide and succinylcholine chloride. It may be used adjunctively in the treatment of respiratory depression caused by curare overdosage. Launch Date1985 |
|||
Preventing | ENLON Approved UseEnlon (edrophonium injection) ® is recommended 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. Because of its brief duration of action, it is not recommended for maintenance therapy in myasthenia gravis.
Enlon (edrophonium injection) ® is also useful whenever a curare antagonist is needed to reverse the neuromuscular block produced by curare, tubocurarine, gallamine triethiodide or dimethyl-tubocurarine. It is not effective against decamethonium bromide and succinylcholine chloride. It may be used adjunctively in the treatment of respiratory depression caused by curare overdosage. Launch Date1985 |
T1/2
Value | Dose | Co-administered | Analyte | Population |
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84.2 min EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2169210/ |
1 mg/kg single, intravenous dose: 1 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: ATROPINE |
EDROPHONIUM plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
56.6 min EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2169210/ |
1 mg/kg single, intravenous dose: 1 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: ATROPINE |
EDROPHONIUM plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
110 min EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7224209/ |
0.5 mg/kg single, intravenous dose: 0.5 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: ATROPINE |
EDROPHONIUM blood | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
110 min EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7224209/ |
1 mg/kg single, intravenous dose: 1 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: ATROPINE |
EDROPHONIUM blood | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
PubMed
Title | Date | PubMed |
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Determination of inhibitors' potency (IC50) by a direct high-performance liquid chromatographic method on an immobilised acetylcholinesterase column. | 2001 Apr 5 |
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Electrogastrography: a non-invasive measurement of gastric function. | 2001 Apr-Jun |
|
Edrophonium antagonism of cisatracurium-induced neuromuscular block: dose requirements in children and adults. | 2001 Aug |
|
Asystole induced by edrophonium following beta blockade. | 2001 Aug 28 |
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Reversal of rocuronium with edrophonium during propofol versus sevoflurane anesthesia. | 2001 Feb |
|
A dose-response study of anticholinesterase drugs on contractile and phosphatidylinositol responses of rat trachea. | 2001 Jan |
|
[Voice disorders caused by neurological diseases]. | 2001 Jul 16-31 |
|
Thioflavin T is a fluorescent probe of the acetylcholinesterase peripheral site that reveals conformational interactions between the peripheral and acylation sites. | 2001 Jun 29 |
|
[Giant-cell myocarditis without a symptom of heart failure seen in a patient with myasthenia gravis and concurrent Hashimoto's disease]. | 2001 Nov |
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Regulation of GABA release by nicotinic acetylcholine receptors in the neonatal rat hippocampus. | 2001 Oct 1 |
|
Respiratory failure due to vocal cord paresis in myasthenia gravis. | 2002 |
|
Clinical, electrophysiological and immunological remissions after thymectomy in myasthenia gravis. | 2002 Apr |
|
Autosomal recessive limb girdle myasthenia in two sisters. | 2002 Dec |
|
[Seronegative myasthenia gravis]. | 2002 Jan |
|
Markedly enhanced susceptibility to experimental autoimmune myasthenia gravis in the absence of decay-accelerating factor protection. | 2002 Nov |
|
[Comparison between idiopathic achalasia and achalasia caused by Chagas' disease: a review on the publications about the subject]. | 2003 Apr-Jun |
|
Ocular myasthenia gravis associated with euthyroid ophthalmopathy. | 2003 Dec |
|
Development of generalized disease at 2 years in patients with ocular myasthenia gravis. | 2003 Feb |
|
beta-Amyloid aggregation induced by human acetylcholinesterase: inhibition studies. | 2003 Feb 1 |
|
Edrophonium effectively antagonizes neuromuscular block at the laryngeal adductors induced by rapacuronium, rocuronium and cisatracurium, but not mivacurium. | 2003 Nov |
|
[Response to thymectomy in patients with thymoma]. | 2003 Nov-Dec |
|
Interactions of edrophonium with neostigmine in the rat trachea. | 2003 Oct |
|
Antinociception of intrathecal cholinesterase inhibitors and cholinergic receptors in rats. | 2003 Oct |
|
Myasthenia gravis in childhood. | 2004 |
|
Mutation in the AChR ion channel gate underlies a fast channel congenital myasthenic syndrome. | 2004 Apr 13 |
|
Appearance of systemic lupus erythematosus in patients with myasthenia gravis following thymectomy: two case reports. | 2004 Feb |
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Response of thymectomy: clinical and pathological characteristics among seronegative and seropositive myasthenia gravis patients. | 2004 Mar |
|
A case of Lambert-Eaton myasthenic syndrome associated with atypical bronchopulmonary carcinoid tumor. | 2004 Oct |
|
Evaluation of mechanisms of azinphos-methyl resistance in the codling moth Cydia pomonella (L.). | 2004 Oct |
|
Painful sweating. | 2004 Oct 26 |
|
Pupil-sparing, painless compression of the oculomotor nerve by expanding basilar artery aneurysm: a case of ocular pseudomyasthenia. | 2004 Sep |
|
Advances in the diagnosis of neuromuscular junction disorders. | 2005 Aug |
|
Postinfectious myasthenia gravis: report of two children. | 2005 May |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: http://www.rxlist.com/enlon-drug.htm
Enlon (edrophonium injection) ® Test in the Differential Diagnosis of Myasthenia Gravis:1-8
Intravenous Dosage (Adults): A tuberculin syringe containing 1 mL (10 mg) of Enlon (edrophonium injection) ® is prepared with an intravenous needle, and 0.2 mL (2 mg) is injected intravenously within 15 to 30 seconds. The needle is left in situ. Only if no reaction occurs after 45 seconds is the remaining 0.8 mL (8 mg) injected. If a cholinergic reaction (muscarinic side effects, skeletal muscle fasciculations and increased muscle weakness) occurs after injection of 0.2 mL (2 mg), the test is discontinued and atropine sulfate, 0.4 mg to 0.5 mg, is administered intravenously. After one-half hour the test may be repeated.
Intramuscular Dosage (Adults): In adults with inaccessible veins, dosage for intramuscular injection is 1 mL (10 mg) of Enlon (edrophonium injection) ®. Subjects who demonstrate hyperreactivity to this injection (cholinergic reaction), should be retested after one-half hour with 0.2 mL (2mg) of Enlon (edrophonium injection) ® intramuscularly to rule out false-negative reactions.
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. The maximal dose for any one patient should be 4 mL (40 mg). Because of its brief effect, Enlon (edrophonium injection) ® should not be given prior to the administration of curare, tubocurarine, gallamine triethiodide or dimethyl-tubocurarine: it should be used at the time when its effect is needed. When given to counteract curare overdosage, the effect of each dose on the respiration should be carefully observed before it is repeated, and assisted ventilation should always be employed.
Route of Administration:
Other
Substance Class |
Chemical
Created
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Record UNII |
QO611KSM5P
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C47792
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EDROPHONIUM CHLORIDE
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PRIMARY | Description: A white, crystalline powder; odourless.Solubility: Soluble in 0.5 parts of water and in 5 parts of ethanol (~750 g/l) TS; practically insoluble in ether R.Category: Diagnostic agent.Storage: Edrophonium chloride should be kept in a well-closed container, protected from light.Requirements: Definition. Edrophonium chloride contains not less than 98.5% and not more than 101.0% of C10H16ClNO, calculated withreference to the dried substance. | ||
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PARENT -> SALT/SOLVATE |
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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ACTIVE MOIETY |