|
|
Line 44: |
Line 44: |
| | StdInChIKey = CPYGBGOXCJJJGC-GKLGUMFISA-L | | | StdInChIKey = CPYGBGOXCJJJGC-GKLGUMFISA-L |
| }} | | }} |
|
| |
| '''Alcuronium''' is a neuromuscular blocking (NMB) agent, alternatively referred to as a skeletal [[muscle relaxant]]. It is a semi-synthetic substance prepared from C-[[toxiferine]] I,<ref>{{cite journal | author = Foldes FF | title = | journal = Br. J. Anaesth | volume = 26 | issue = | pages = 394 | year = 1954 | pmid = | doi = 10.1093/bja/26.6.394}}</ref> a ''bis''-quaternary alkaloid obtained from ''Strychnos toxifera''. C-[[toxiferine]] I itself has been tested for its pharmacological action and noted to be a very long acting neuromuscular blocking agent<ref>{{cite journal | author = Waser PG | title = | journal = Helv. Physiol. Pharmacol. Acta | volume = 8 | issue = | pages = 342 | year = 1950 | pmid = | doi = }}</ref> For a formal definition of the durations of actions associated with NMB agents, see page for [[gantacurium]]. The replacement of both the ''N''-methyl groups with ''N-allyl'' moieties yielded ''N,N''-diallyl-''bis''-nortoxiferine, now recognized as alcuornium (and at one time marketed as the proprietary agent called Alloferin).
| |
|
| |
| Inclusion of the allylic functions presented an enhanced potential area of biotransformation, and thus alcuronium is observed to have a much shorter duration of neuromuscular blocking action than its parent C-toxiferine I.<ref>Martin-Smith M (1971), In: Ariens EJ (ed.), "Drug Design". Vol. 2. Academic Press. New York and London. pp.453-530.</ref> It also has a more rapid onset of action, and is ~1.5 times as potent as [[tubocurarine]].<ref name = Speight>{{cite journal | author = Speight TM, Avery GS | title = | journal = Drugs | volume = 4 | issue = | pages = 163 | year = 1972 | pmid = | doi = 10.2165/00003495-197204030-00002 }}</ref> The pharmacological action of alcuronium is readily reversed by neostigmine, and it produced little histamine release.<ref>{{cite journal | author = Thompson MA | title = | journal = Br. J. Hosp Med | volume = 23 | issue = | pages = 153 | year = 1980 | pmid = | doi = }}</ref> The major disadvantage of alcuronium is that it elicits a vagolytic effect produced by a selective atropoine-like blockade of cardiac muscarinic receptors.<ref name = Speight/><ref>{{cite journal | author = Coleman AJ, Downing JW, Leary WP, Moyes DG, Styles M. | title = The immediate cardiovascular effects of pancuronium, alcuronium and tubocurarine in man| journal = Anaesthesia | volume = 27 | issue = 4| pages = 415–22 | year = 1972 | pmid = 4264060| doi = 10.1111/j.1365-2044.1972.tb08247.x }}</ref><ref>{{cite journal | author = Hughes R, Chapple DJ. | title = | journal = Br. J. Anaesth | volume = 48 | issue = | pages = 59 | year = 1976 | pmid = | doi = 10.1093/bja/48.2.59}}</ref>
| |
|
| |
| == 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
| |
|
| |
| == Special points ==
| |
|
| |
| * Duration of action prolonged 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
| |
|
| |
| == References ==
| |
| {{Reflist}}
| |
|
| |
| * {{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 | doi = 10.1046/j.1471-4159.1994.63051932.x | 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}}
| |
| * {{cite journal | author = Proska J, Tucek S | title = Mechanisms of steric and cooperative actions of alcuronium on cardiac muscarinic acetylcholine receptors | journal = Mol Pharmacol | volume = 45 | issue = 4 | pages = 709–17 | year = 1994 | pmid = 8183250}}
| |
|
| |
| {{Muscle relaxants}}
| |
| {{Cholinergics}}
| |
|
| |
| [[Category:Muscle relaxants]]
| |
| [[Category:World Health Organization essential medicines]]
| |