Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C35H60N2O4 |
Molecular Weight | 572.8619 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 10 / 10 |
E/Z Centers | 0 |
Charge | 2 |
SHOW SMILES / InChI
SMILES
[H][C@@]12C[C@@H]([C@H](OC(C)=O)[C@@]1(C)CC[C@@]3([H])[C@@]2([H])CC[C@@]4([H])C[C@H](OC(C)=O)[C@H](C[C@]34C)[N+]5(C)CCCCC5)[N+]6(C)CCCCC6
InChI
InChIKey=GVEAYVLWDAFXET-XGHATYIMSA-N
InChI=1S/C35H60N2O4/c1-24(38)40-32-21-26-13-14-27-28(35(26,4)23-31(32)37(6)19-11-8-12-20-37)15-16-34(3)29(27)22-30(33(34)41-25(2)39)36(5)17-9-7-10-18-36/h26-33H,7-23H2,1-6H3/q+2/t26-,27+,28-,29-,30-,31-,32-,33-,34-,35-/m0/s1
Pancuronium (trademarked as Pavulon) is an aminosteroid muscle relaxant with various medical uses. Pancuronium is a typical non-depolarizing curare-mimetic muscle relaxant. It competitively inhibits the nicotinic acetylcholine receptor at the neuromuscular junction by blocking the binding of acetylcholine. It has slight vagolytic activity, causing an increase in heart rate, but no ganglioplegic (i.e., blocking ganglions) activity. It is a very potent muscle relaxant drug, with an ED95 of only 60 µg/kg body weight. The onset of action is relatively slow compared to other similar drugs, in part due to its low dose - an intubating dose takes 3–6 minutes for full effect. 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. Pancuronium is used with general anesthesia 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 for the seriously ill and it can accumulate leading to extended weakness. Pancuronium is not preferable to long-term use in ICU-ventilated patients. Pancuronium is also used as one component of a lethal injection in the administration of the death penalty in some parts of the United States.
CNS Activity
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2362997 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17525594 |
15.0 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | PAVULON Approved UsePancuronium bromide injection is indicated as an adjunct to general anesthesia, to facilitate tracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation. Launch Date1972 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
460 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1276000 |
4 mg single, intravenous dose: 4 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
PANCURONIUM plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
600 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1276000 |
4 mg single, intravenous dose: 4 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
PANCURONIUM plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
0.761 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/789085 |
6 mg single, intravenous dose: 6 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
PANCURONIUM plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
12.46 min EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/789085 |
6 mg single, intravenous dose: 6 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
PANCURONIUM plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
0.15 mg/kg 1 times / day single, intravenous Highest studied dose Dose: 0.15 mg/kg, 1 times / day Route: intravenous Route: single Dose: 0.15 mg/kg, 1 times / day Sources: |
unhealthy, 17 years n = 1 Health Status: unhealthy Age Group: 17 years Sex: F Population Size: 1 Sources: |
PubMed
Title | Date | PubMed |
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Ultra-fast-track anesthetic technique facilitates operating room extubation in patients undergoing off-pump coronary revascularization surgery. | 2001 Apr |
|
Suramin prevents cerebellar granule cell-death induced by dequalinium. | 2001 Feb |
|
[Anesthetic experience of emergency coronary artery bypass graft operation in a patient with cardioamyloidosis]. | 2001 Jan |
|
Facilitation of fiberoptic nasotracheal intubation by simultaneous direct laryngoscopy in anesthetized patients. | 2001 Jun |
|
Anaesthetic management of baboons undergoing heterotopic porcine cardiac xenotransplantation. | 2001 May |
|
Efficacy of propofol to prevent bronchoconstriction: effects of preservative. | 2001 May |
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Influence of blood cell transfusion on the presence of propofol in blood components. | 2001 Nov-Dec |
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The kinetics of inhibition of nicotinic acetylcholine receptors by (+)-tubocurarine and pancuronium. | 2001 Oct |
|
Different patterns of mast cell activation by muscle relaxants in human skin. | 2001 Sep |
|
[Hemostatic profile of women using low-dose oral contraceptive Mercilon. (Preliminary report)]. | 2002 |
|
Increased airway resistance during xenon anaesthesia in pigs is attributed to physical properties of the gas. | 2002 Apr |
|
A study of the in vitro clinical interaction between lidocaine and premedications using rat liver microsomes. | 2002 Aug |
|
Synthesis and structure-activity relationships of neuromuscular blocking agents. | 2002 Aug |
|
Intramucosal-arterial PCO2 gap fails to reflect intestinal dysoxia in hypoxic hypoxia. | 2002 Dec |
|
A combination of intrathecal morphine and remifentanil anesthesia for fast-track cardiac anesthesia and surgery. | 2002 Dec |
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The use of neuromuscular blocking drugs in adult cardiac surgery: results of a national postal survey. | 2002 Dec |
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Responses of diencephalic nociceptive neurones to orofacial stimuli and effects of internal capsule stimulation in the rat. | 2002 Dec |
|
The detection and identification of quaternary nitrogen muscle relaxants in biological fluids and tissues by ion-trap LC-ESI-MS. | 2002 Jan-Feb |
|
Vasoactive modulators during and after craniotomy: relation to postoperative hypertension. | 2002 Jul |
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Tachyphylaxis associated with continuous cisatracurium versus pancuronium therapy. | 2002 Jul |
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Presynaptic inhibitory effects of rocuronium and SZ1677 on [3H]acetylcholine release from the mouse hemidiaphragm preparation. | 2002 Jun |
|
Intradermal cholinergic agonists induce itch-associated response via M3 muscarinic acetylcholine receptors in mice. | 2002 Mar |
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Impact of shorter-acting neuromuscular blocking agents on fast-track recovery of the cardiac surgical patient. | 2002 Mar |
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Anionic cyclophanes as potential reversal agents of muscle relaxants by chemical chelation. | 2002 Mar 11 |
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Case report: Survival after deliberate strychnine self-poisoning, with toxicokinetic data. | 2002 Oct |
|
Cost comparisons of pharmacological strategies in open-heart surgery. | 2003 |
|
Diverse range of fixed positional deformities and bone growth restraint provoked by flaccid paralysis in embryonic chicks. | 2003 Aug |
|
Mouse muscle denervation increases expression of an alpha7 nicotinic receptor with unusual pharmacology. | 2003 Feb 15 |
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Resuscitation from hemorrhagic shock: experimental model comparing normal saline, dextran, and hypertonic saline solutions. | 2003 Jul |
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Tolerance to acute isovolemic hemodilution. Effect of anesthetic depth. | 2003 Jul |
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Screening procedure for eight quaternary nitrogen muscle relaxants in blood by high-performance liquid chromatography-electrospray ionization mass spectrometry. | 2003 Jun 5 |
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[The use of muscle relaxants for routine induction of anesthesia in Germany]. | 2003 May |
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Angiotensin AT1 receptor antagonist losartan and the defence reaction in the anaesthetised rat. Effect on the carotid chemoreflex. | 2003 May |
|
The hemodynamic and metabolic effects of shivering during acute normovolemic hemodilution. | 2003 Oct |
|
Thermogenesis elicited by skin cooling in anaesthetized rats: lack of contribution of the cerebral cortex. | 2004 Mar 1 |
Patents
Sample Use Guides
Load: 0.04-0.1 mg/kg IV
Maintenance: 0.015-0.1 mg/kg IV q30-60min OR
Continuous infusion: 0.1 mg/kg/hr IV
Dose should be calculated based on ideal body weight
Monitoring of muscle twitch response to a peripheral nerve stimulator is advised
Route of Administration:
Intravenous
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/17525594
HEK293 cells were prepared for patch clamp recording by replacing the culture medium with an extracellular solution consisting of 150 mM NaCl, 5.6 mM KCl, 1.8 mM CaCl2, 1.0 mM MgCl2, and 10 mM HEPES, pH 7.3. Subsequently, 3−5 μl of polystyrene beads coated with a monoclonal antibody specific for the CD8 antigen (Dyna-beads; Dynal, Lake Success, NY) were added to the culture dish. Good expression of nAChR channels in excised patches was found for most cells having two or three beads attached. Patch pipettes, filled with a solution consisting of 140 mM KCl, 5 mM EGTA, 5 mM MgCl2, and 10 mM HEPES, pH 7.3, had resistances of 3−6 MΩ. An outside-out patch24 with a seal resistance of 5 GΩ or greater was excised from a cell and moved into position at the outflow of a HSSE-2 rapid perfusion device (ALA Scientific Instruments, Westbury, NY). The perfusion system consisted of solution reservoirs, manual switching valves, a solenoid-driven pinch valve, and two tubes inserted into the culture dish and had a time resolution of less than 100 μs. One tube contained extracellular solution without agonist (normal solution); the other contained extracellular solution with 300 μM acetylcholine (test solution). In the control protocol, the patch, initially perfused with normal solution, was exposed to a series of ten 0.25- s exposures to the test solution at 5-s intervals. Manual valves were used to connect to reservoirs containing a defined concentration of competitive antagonist (Pancuronium ) with or without acetylcholine. An equilibrium (+/+) protocol was performed by exposing the patch to acetylcholine plus antagonist for 0.25 s, with a 5-s interval of antagonist alone. After switching back to antagonist free solutions, the control protocol was repeated
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QM03AC01
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M03AC01
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C29696
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N0000175732
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ACTIVE MOIETY
METABOLITE LESS ACTIVE (PARENT)
METABOLITE LESS ACTIVE (PARENT)
METABOLITE LESS ACTIVE (PARENT)