Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C35H60N2O4.2Br |
Molecular Weight | 732.67 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 10 / 10 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[Br-].[Br-].[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=NPIJXCQZLFKBMV-YTGGZNJNSA-L
InChI=1S/C35H60N2O4.2BrH/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;2*1H/q+2;;/p-2/t26-,27+,28-,29-,30-,31-,32-,33-,34-,35-;;/m0../s1
Molecular Formula | BrH |
Molecular Weight | 80.912 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | C35H60N2O4 |
Molecular Weight | 572.8619 |
Charge | 2 |
Count |
|
Stereochemistry | MIXED |
Additional Stereochemistry | No |
Defined Stereocenters | 10 / 10 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
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 |
---|---|---|---|---|
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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Synthesis and neuromuscular blocking activity of 16beta-piperidinosteroidal derivatives. | 2001 Feb |
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Combination propofol-ketamine anaesthesia in sick neonates. | 2001 Jan |
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Anaesthetic management of baboons undergoing heterotopic porcine cardiac xenotransplantation. | 2001 May |
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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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Characterisation of [(125)I]-apamin binding sites in rat brain membranes with HE293 cells transfected with SK channel subtypes. | 2001 Sep |
|
Thermogenesis induced by intravenous infusion of hypertonic solutions in the rat. | 2001 Sep 1 |
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A study of the in vitro clinical interaction between lidocaine and premedications using rat liver microsomes. | 2002 Aug |
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Synthesis and structure-activity relationships of neuromuscular blocking agents. | 2002 Aug |
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A combination of intrathecal morphine and remifentanil anesthesia for fast-track cardiac anesthesia and surgery. | 2002 Dec |
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Sustained firing of alpha and gamma hind limb motoneurons induced by stimulation of the pudendal nerve. | 2002 Dec |
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Comparison of a sidestream capnograph and a mainstream capnograph in mechanically ventilated dogs. | 2002 Dec 1 |
|
Vasoactive modulators during and after craniotomy: relation to postoperative hypertension. | 2002 Jul |
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Case report: Survival after deliberate strychnine self-poisoning, with toxicokinetic data. | 2002 Oct |
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Anesthetic management for a hypertensive patent ductus arteriosus (PDA) closure in a patient with surgically uncorrectable long-segment right pulmonary artery hypoplasia and a ventricular septal defect. | 2003 Dec |
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Characterization of human alpha 4 beta 2-nicotinic acetylcholine receptors stably and heterologously expressed in native nicotinic receptor-null SH-EP1 human epithelial cells. | 2003 Dec |
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Preoperative pulmonary assessment of the older adult. | 2003 Feb |
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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 |
|
Potentiation of mivacurium blockade by low dose of pancuronium: a pharmacokinetic study. | 2003 May |
|
Endotracheal intubation with a lightwand or a laryngoscope results in similar hemodynamic variations in patients with coronary artery disease. | 2003 Oct |
|
The hemodynamic and metabolic effects of shivering during acute normovolemic hemodilution. | 2003 Oct |
|
Postanesthesia care unit recovery times and neuromuscular blocking drugs: a prospective study of orthopedic surgical patients randomized to receive pancuronium or rocuronium. | 2004 Jan |
|
Electrophysiological evaluation of phrenic nerve injury during cardiac surgery--a prospective, controlled, clinical study. | 2004 Jan 14 |
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
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 15:18:49 GMT 2023
by
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on
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Record UNII |
U9LY9Y75X2
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Record Status |
Validated (UNII)
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C29696
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7884
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PANCURONIUM BROMIDE
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Related Record | Type | Details | ||
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BASIS OF STRENGTH->SUBSTANCE |
ASSAY (TITRATION)
EP
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BASIS OF STRENGTH->SUBSTANCE |
ASSAY (TITRATION)
USP
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Related Record | Type | Details | ||
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IMPURITY -> PARENT |
UNSPECIFIED
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (TLC)
USP
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IMPURITY -> PARENT |
UNSPECIFIED
EP
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PARENT -> IMPURITY |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Biological Half-life | PHARMACOKINETIC |
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Elimination PHARMACOKINETIC |
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