Alcuronium
From DrugPedia: A Wikipedia for Drug discovery
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{{Drugbox | {{Drugbox | ||
| - | | IUPAC_name = | + | | IUPAC_name =4,4'-Didemethyl-4,4'-di-propenyltoxiferin-1-dichloride |
| PubChem = 10010215 | | PubChem = 10010215 | ||
| + | | CAS_number = 23214-96-2 | ||
| + | | ATC_prefix = M03 | ||
| + | | ATC_suffix = AA01 | ||
| DrugBank = | | DrugBank = | ||
| ChemSpiderID = | | ChemSpiderID = | ||
| Line 21: | Line 24: | ||
| metabolism = | | metabolism = | ||
| elimination_half-life = | | elimination_half-life = | ||
| + | | excretion = 70-90% unchanged in urine 1.3ml/kg/min t1/2 2- 4 hours | ||
}} | }} | ||
==Description== | ==Description== | ||
A non-depolarizing skeletal muscle relaxant similar to TUBOCURARINE. It is used as an anesthesia adjuvant. | A non-depolarizing skeletal muscle relaxant similar to TUBOCURARINE. It is used as an anesthesia adjuvant. | ||
| + | Alcuronium is a peripherally acting muscle relaxant in the curare alkaloid family. It is a semi-synthetic substance derived from toxiferine. | ||
| + | |||
| + | Use - Intubation and ventilation | ||
| + | |||
| + | Action - NDMB post synapthis n2 receptor | ||
| + | |||
| + | Dose .2 - .5 mg/kg ivi | ||
==General Properties== | ==General Properties== | ||
| Line 37: | Line 48: | ||
<b>*IUPAC NAME</b> | <b>*IUPAC NAME</b> | ||
| - | + | 4,4'-Didemethyl-4,4'-di-propenyltoxiferin-1-dichloride | |
<b>*Canonical Smiles</b> | <b>*Canonical Smiles</b> | ||
| Line 54: | Line 65: | ||
46.9 | 46.9 | ||
| + | |||
| + | ==Effects== | ||
| + | *Cardiovascular system - histamine release and blockage of the sympathetic ganglia including adrenal medulla could cause Hypotension | ||
| + | |||
| + | *Respiratory - apnea due to phrenic blockage but bronchoconstriction can occur from the histamine release | ||
| + | |||
| + | *Central nervous system - no effect on intraoccular pressure | ||
| + | |||
| + | *Autonomic ganglion blockade can cause decrease in gut motility | ||
| + | |||
| + | ==Kinetics== | ||
| + | *Poor oral absorption | ||
| + | |||
| + | *Distribution - 40 % protein bound Volume of Distribution .37l/kg. Does cross placenta ratio .6 | ||
| + | |||
| + | *Metabolism - not metabolized | ||
| + | |||
| + | *Excretion | ||
| + | 70 - 90% unchanged in urine 1.3ml/kg/min t1/2 2- 4 hours | ||
| + | |||
| + | ==Special points== | ||
| + | *Duration of action prolonger in states of low potassium, calcium and protein, also in states of high magnesium and acidosis. | ||
| + | *Pharmaceutically incompatible with thiopentone | ||
| + | Infusion can cause fixed dilated pupils | ||
==External Links== | ==External Links== | ||
| Line 60: | Line 95: | ||
[http://crdd.osdd.net/raghava/biadb/detail.php?id=1003 Link to BIAdb Database] | [http://crdd.osdd.net/raghava/biadb/detail.php?id=1003 Link to BIAdb Database] | ||
| + | |||
| + | * {{cite journal | author = Zahn K, Eckstein N, Tränkle C, Sadée W, Mohr K | title = Allosteric modulation of muscarinic receptor signaling: alcuronium-induced conversion of pilocarpine from an agonist into an antagonist. | journal = J Pharmacol Exp Ther | volume = 301 | issue = 2 | pages = 720–8 | year = 2002 | pmid = 11961078 | doi = 10.1124/jpet.301.2.720}} | ||
| + | * {{cite journal | author = Maass A, Mohr K | title = Opposite effects of alcuronium on agonist and on antagonist binding to muscarinic receptors. | journal = Eur J Pharmacol | volume = 305 | issue = 1-3 | pages = 231–4 | year = 1996 | pmid = 8813558 | doi = 10.1016/0014-2999(96)00240-3}} | ||
| + | * {{cite journal | author = Jakubík J, Tucek S | title = Protection by alcuronium of muscarinic receptors against chemical inactivation and location of the allosteric binding site for alcuronium. | journal = J Neurochem | volume = 63 | issue = 5 | pages = 1932–40 | year = 1994 | pmid = 7931349}} | ||
| + | |||
| + | [[Category:Muscle relaxants]] | ||
Current revision
| Alcuronium
| |
| Systematic (IUPAC) name | |
| 4,4'-Didemethyl-4,4'-di-propenyltoxiferin-1-dichloride | |
| Identifiers | |
| CAS number | |
| ATC code | M03 |
| PubChem | |
| Chemical data | |
| Formula | C44H50Cl2N4O2 |
| Mol. mass | 737.7994 |
| SMILES | & |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | ? |
| Excretion | 70-90% unchanged in urine 1.3ml/kg/min t1/2 2- 4 hours |
| Therapeutic considerations | |
| Pregnancy cat. |
? |
| Legal status | |
| Routes | ? |
Contents |
[edit] Description
A non-depolarizing skeletal muscle relaxant similar to TUBOCURARINE. It is used as an anesthesia adjuvant. Alcuronium is a peripherally acting muscle relaxant in the curare alkaloid family. It is a semi-synthetic substance derived from toxiferine.
Use - Intubation and ventilation
Action - NDMB post synapthis n2 receptor
Dose .2 - .5 mg/kg ivi
[edit] General Properties
*Molecular Weight
737.7994
*Molecular Formula
C44H50Cl2N4O2
*IUPAC NAME
4,4'-Didemethyl-4,4'-di-propenyltoxiferin-1-dichloride
*Canonical Smiles
C=CC[N+]12CCC34C1CC(C(=CCO)C2)C5=CN6C7C(=CN(C53)C8=CC=CC=C48)C9CC1C7(CC[N+]1(CC9=CCO)CC=C)C1=CC=CC=C16.[Cl-].[Cl-]
*Isomeric Smiles
C=CC[N+]12CCC34C1CC(/C(=CCO)/C2)/C/5=C/N6C7/C(=CN(C53)C8=CC=CC=C48)/C9CC1C7(CC[N+]1(C/C9=C/CO)CC=C)C1=CC=CC=C16.[Cl-].[Cl-]
*XLogP
N/A
*Topological Polar Surface Area
46.9
[edit] Effects
- Cardiovascular system - histamine release and blockage of the sympathetic ganglia including adrenal medulla could cause Hypotension
- Respiratory - apnea due to phrenic blockage but bronchoconstriction can occur from the histamine release
- Central nervous system - no effect on intraoccular pressure
- Autonomic ganglion blockade can cause decrease in gut motility
[edit] Kinetics
- Poor oral absorption
- Distribution - 40 % protein bound Volume of Distribution .37l/kg. Does cross placenta ratio .6
- Metabolism - not metabolized
- Excretion
70 - 90% unchanged in urine 1.3ml/kg/min t1/2 2- 4 hours
[edit] Special points
- Duration of action prolonger in states of low potassium, calcium and protein, also in states of high magnesium and acidosis.
- Pharmaceutically incompatible with thiopentone
Infusion can cause fixed dilated pupils
[edit] External Links
- Zahn K, Eckstein N, Tränkle C, Sadée W, Mohr K (2002). "Allosteric modulation of muscarinic receptor signaling: alcuronium-induced conversion of pilocarpine from an agonist into an antagonist.". J Pharmacol Exp Ther 301 (2): 720–8. doi:. PMID 11961078.
- Maass A, Mohr K (1996). "Opposite effects of alcuronium on agonist and on antagonist binding to muscarinic receptors.". Eur J Pharmacol 305 (1-3): 231–4. doi:. PMID 8813558.
- Jakubík J, Tucek S (1994). "Protection by alcuronium of muscarinic receptors against chemical inactivation and location of the allosteric binding site for alcuronium.". J Neurochem 63 (5): 1932–40. PMID 7931349.
