|Accession Number||DB00416 (APRD01318)|
Metocurine iodide is a benzylisoquinolinium competitive nondepolarizing neuromuscular blocking agent. It is used as an anesthesia adjunct to induce skeletal muscle relaxation and to reduce the intensity of muscle contractions in convulsive therapy Metocurine iodide has a moderate risk of inducing histamine release and has some ganglion blocking activity. Metocurine iodide can be used most advantageously if muscle twitch response to peripheral nerve stimulation is monitored to assess degree of muscle relaxation. Metocurine Iodide is no longer available on the US market.
|Product Ingredients||Not Available|
|Approved Prescription Products|
|Approved Generic Prescription Products||Not Available|
|Approved Over the Counter Products||Not Available|
|Unapproved/Other Products||Not Available|
|International Brands||Not Available|
|Brand mixtures||Not Available|
|Weight||Average: 906.6279 |
For use as an anesthesia adjunct to induce skeletal muscle relaxation and to reduce the intensity of muscle contractions in convulsive therapy.
|Structured Indications||Not Available|
Metocurine iodide is a benzylisoquinolinium competitive nondepolarizing neuromuscular blocking agent. Metocurine iodide has a moderate risk of inducing histamine release and has some ganglion blocking activity. Metocurine iodide can be used most advantageously if muscle twitch response to peripheral nerve stimulation is monitored to assess degree of muscle relaxation. As with other nondepolarizing neuromuscular blockers, the time to onset of paralysis decreases and the duration of maximum effect increases with increasing doses of metocurine iodide. Repeated administration of maintenance doses of metocurine iodide has no cumulative effect on the duration of neuromuscular block if recovery is allowed to begin prior to repeat dosing. Moreover, the time needed to recover from repeat doses does not change with additional doses. Repeat doses can therefore be administered at relatively regular intervals with predictable results.
|Mechanism of action|
Metocurine iodide antagonizes the neurotransmitter action of acetylcholine by binding competitively with cholinergic receptor sites on the motor end-plate. This antagonism is inhibited, and neuromuscular block reversed, by acetylcholinesterase inhibitors such as neostigmine, edrophonium, and pyridostigmine.
|Volume of distribution||Not Available|
35% in plasma
|Route of elimination||Not Available|
3 to 4 hours
Excessive doses can be expected to produce enhanced pharmacological effects. Overdosage may increase the risk of histamine release and cardiovascular effects, especially hypotension.
|Pharmacogenomic Effects/ADRs||Not Available|
|Food Interactions||Not Available|
Bray, M.D.; U.S. Patent 2,581,903; January 8, 1952; assigned to Eli Lilly and Company.
|General References||Not Available|
|ATC Codes||Not Available|
|AHFS Codes||Not Available|
|PDB Entries||Not Available|
|FDA label||Not Available|
|Clinical Trials||Not Available|
|Predicted ADMET features|
|Mass Spec (NIST)||Not Available|
|Description||This compound belongs to the class of chemical entities known as diarylethers. These are organic compounds containing the dialkyl ether functional group, with the formula ROR', where R and R' are aryl groups.|
|Super Class||Organic compounds|
|Class||Organic oxygen compounds|
|Sub Class||Organooxygen compounds|
|Alternative Parents||Tetrahydroisoquinolines / Anisoles / Aralkylamines / Alkyl aryl ethers / Tetraalkylammonium salts / Oxacyclic compounds / Azacyclic compounds / Organopnictogen compounds / Organic zwitterions / Organic iodide salts / Hydrocarbon derivatives|
|Substituents||Diaryl ether / Tetrahydroisoquinoline / Anisole / Alkyl aryl ether / Aralkylamine / Benzenoid / Tetraalkylammonium salt / Quaternary ammonium salt / Oxacycle / Azacycle/ Organoheterocyclic compound / Organic nitrogen compound / Organic zwitterion / Organic salt / Organic iodide salt / Organonitrogen compound / Hydrocarbon derivative / Organopnictogen compound / Amine / Aromatic heteropolycyclic compound|
|Molecular Framework||Aromatic heteropolycyclic compounds|
|External Descriptors||Not Available|
- Pharmacological action
- General Function:
- Drug binding
- Specific Function:
- After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane.
- Gene Name:
- Uniprot ID:
- Uniprot Name:
- Neuronal acetylcholine receptor subunit alpha-2
- Molecular Weight:
- 59764.82 Da
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