Pancuronium

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Pancuronium chemical structure
Pancuronium
Systematic (IUPAC) name
[(2S,3S,5S,8R,9S,10S,13S,14S,16S,17R)-
17-acetyloxy-10,13-dimethyl-2,16-bis(1-methyl-
3,4,5,6-tetrahydro-2H-pyridin-1-yl)-2,3,4,5,6,7,
8,9,11,12,14,15,16,17-tetradecahydro-1H-
cyclopenta[a]phenanthren-3-yl] acetate
Identifiers
CAS number 15500-66-0
ATC code M03AC01
PubChem 441289
Chemical data
Formula C35H60N2O4 
Mol. weight 572.861 g/mol
Pharmacokinetic data
Bioavailability NA
Protein binding 77 to 91%
Metabolism Hepatic
Half life 1.5 to 2.7 hours
Excretion Renal and biliary
Therapeutic considerations
Pregnancy cat.

B2(AU) C(US)
Legal status

POM(UK) ℞-only(US)
Routes Intravenous

Pancuronium bromide is a chemical compound, used in medicine with the brand name Pavulon® (Organon International).

Contents

[edit] Mode of action

Pancuronium is a typical non-depolarising curaremimetic muscle relaxant. It acts as a competitive acetylcholine antagonist on neuromuscular junctions, displacing acetylcholine ions (hence competitive) from its post-synaptic nicotinic acetylcholine receptors. It is, unlike suxamethonium, a non-depolarising agent, which means, that it causes no spontaneous depolarisations upon association with the nicotinic receptor in neuromuscular junction, thus producing no muscle fasciculations upon administration. Pancuronium has no hormonal activity. It exerts slight vagolytic activity (i.e. diminishing activity of the vagus nerve) and no ganglioplegic (i.e., blocking ganglions) activity. Pancuronium is a very potent muscle relaxant/curaremimetic, the ED95 (i.e. a dose causing a 95% reduction in muscle activity) being only 60 µg/kg body weight administered intravenously. Usual doses for anesthesiologic muscle relaxation (e.g. for intubation and major surgery) are about 100 µg/kg IV (0.1 mg/kg IV); muscle relaxation suitable for intubation sets in about 90–120 seconds after administration of the drug. Full muscle paralysis for major surgery is achieved about 2–4 minutes post application. Clinical effects (muscle activity lower than 25% of physiological) last for about 100 minutes. The time needed for full (over 90% muscle activity) recovery after single administration is about 120–180 minutes in healthy adults, but can be protracted to more hours in poor health subjects and when concomitantly administered with other long-acting anesthetics (e.g. some opioids, barbiturates, inhalation anesthetics). The effects of pancuronium can be at least partially reversed by anticholinesterasics, such as neostigmine, pyridostigmine and edrophonium.

[edit] Uses in medicine

Pancuronium is used with general anaesthesia in surgery for muscle relaxation and as an aid to intubation or ventilation. It does not have sedative or analgesic effects.

Side effects include moderately raised heart rate and thereby arterial pressure and cardiac output, excessive salivation, apnea and respiratory depression, rashes, flushing and sweating. The muscular relaxation can be dangerous in the seriously ill and it can accumulate leading to extended weakness.

[edit] Uses in execution

It is also used as one component of a lethal injection used in capital punishment in some parts of the USA. If improperly administered it can cause sodium pentothal, commonly used as the anesthetic in the lethal injection process, to precipitate and become ineffective. Because pancuronium bromide has no analgesic effects but prevents the body from displaying pain, Amnesty International has objected to its use in lethal injections on the grounds that it "may mask the condemned prisoner's suffering during the execution" [1] and thereby lead observers to conclude that lethal injection is painless, or less cruel than other forms of execution.

[edit] Chemical details

Its empirical formula is:

C35H60Br2N2O4

Its structural name is 3α, 17β - diacetoxy - 5α - androstan - 2β, 16β - ylene bis [1 - methylpiperidinium] dibromide.

[edit] Historical notes

Pavulon® was the compound used in "Angel of Death" Efren Saldivar's killing spree [2].

[edit] References

    [edit] External links


    Muscle relaxants (M03) edit
    Peripherally acting:

    Alcuronium, Atracurium, Cisatracurium, Dimethyltubocurarine, Doxacurium chloride, Fazadinium bromide, Gallamine, Hexafluronium, Mivacurium chloride, Pancuronium, Pipecuronium bromide, Rocuronium bromide, Suxamethonium, Tubocurarine, Vecuronium
    Centrally acting:

    Baclofen, Carisoprodol, Chlormezanone, Chlorzoxazone, Cyclobenzaprine, Febarbamate, Mephenesin, Methocarbamol, Orphenadrine, Phenprobamate, Phenyramidol, Pridinol, Styramate, Tetrazepam, Thiocolchicoside, Tizanidine, Tolperisone
    Directly acting:

    Dantrolene
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