Identification
- Summary
Pancuronium is a neuromuscular blocker used as an adjunct to general anesthesia to facilitate tracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation.
- Generic Name
- Pancuronium
- DrugBank Accession Number
- DB01337
- Background
A bis-quaternary steroid that is a competitive nicotinic antagonist. As a neuromuscular blocking agent it is more potent than curare but has less effect on the circulatory system and on histamine release.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Pancuronium (DB01337)
- Weight
- Average: 572.8619
Monoisotopic: 572.455308418 - Chemical Formula
- C35H60N2O4
- Synonyms
- Pancuronium
Pharmacology
- Indication
Used as a muscle relaxant during anesthesia and surgical procedures.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Therapies
- Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Pancuronium is a non-depolarising muscle relaxant similar to curare. It acts as a competitive acetylcholine antagonist on neuromuscular junctions, displacing acetylcholine (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.
- Mechanism of action
Nondepolarizing neuromuscular blocking agents inhibit neuromuscular transmission by competing with acetylcholine for the cholinergic receptors of the motor end plate, thereby reducing the response of the end plate to acetylcholine. This type of neuromuscular block is usually antagonized by anticholinesterase agents.
Target Actions Organism ANeuronal acetylcholine receptor subunit alpha-2 antagonistHumans UMuscarinic acetylcholine receptor M2 antagonistHumans UMuscarinic acetylcholine receptor M3 antagonistHumans - Absorption
Not Available
- Volume of distribution
- 241 to 280 mL/kg
- Protein binding
77 to 91%
- Metabolism
Hepatic.
- Route of elimination
Not Available
- Half-life
1.5 to 2.7 hours.
- Clearance
- Plasma cl=1.1–1.9 mL/minute/kg
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The risk or severity of CNS depression can be increased when Pancuronium is combined with 1,2-Benzodiazepine. Acebutolol Pancuronium may increase the bradycardic activities of Acebutolol. Acetazolamide The risk or severity of CNS depression can be increased when Acetazolamide is combined with Pancuronium. Acetophenazine The risk or severity of CNS depression can be increased when Acetophenazine is combined with Pancuronium. Acetylcholine The risk or severity of adverse effects can be increased when Pancuronium is combined with Acetylcholine. - Food Interactions
- No interactions found.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Pancuronium bromide U9LY9Y75X2 15500-66-0 NPIJXCQZLFKBMV-YTGGZNJNSA-L - International/Other Brands
- Mioblock / Pavulon
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Pancuronium Bromide - Liq IV 1mg/ml Solution 1 mg / mL Intravenous Sandoz Canada Incorporated 1995-12-31 Not applicable Canada 
Pancuronium Bromide - Liq IV 2mg/ml Solution 2 mg / mL Intravenous Sandoz Canada Incorporated 1996-12-31 Not applicable Canada Pancuronium Bromide 1mg/ml Solution 1 mg / mL Intravenous Hospira Healthcare Ulc 1996-10-24 2018-11-29 Canada Pancuronium Bromide 2mg/ml Solution 2 mg / mL Intravenous Hospira Healthcare Ulc 1995-12-31 2018-11-29 Canada Pavulon Inj 1mg/ml Liquid 1 mg / mL Intravenous Organon Canada Ltd Ltee 1979-12-31 1997-08-18 Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Pancuronium Bromide Injection, solution 2 mg/1mL Intravenous Teva Parenteral Medicines, Inc. 1990-08-01 2012-11-30 US 
Pancuronium Bromide Injection, solution 1 mg/1mL Intravenous Hospira, Inc. 2005-10-11 Not applicable US Pancuronium Bromide Injection, solution 2 mg/1mL Intravenous Teva Parenteral Medicines, Inc. 1990-08-01 2012-07-31 US Pancuronium Bromide Injection, solution 1 mg/1mL Intravenous Teva Parenteral Medicines, Inc. 1990-08-01 2012-11-30 US
Categories
- ATC Codes
- M03AC01 — Pancuronium
- Drug Categories
- Agents producing tachycardia
- Androstanes
- Androstanols
- Anticholinergic Agents
- Central Nervous System Depressants
- Cholinergic Agents
- Cholinesterase Inhibitors
- Fused-Ring Compounds
- Muscarinic Antagonists
- Muscle Relaxants
- Muscle Relaxants, Peripherally Acting Agents
- Musculo-Skeletal System
- Neuromuscular Agents
- Neuromuscular Blocking Agents
- Neuromuscular Nondepolarizing Blockade
- Neuromuscular-Blocking Agents (Nondepolarizing)
- Neurotransmitter Agents
- Nicotinic Antagonists
- OCT1 inhibitors
- OCT1 substrates
- Peripheral Nervous System Agents
- Steroids
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as steroid esters. These are compounds containing a steroid moiety which bears a carboxylic acid ester group.
- Kingdom
- Organic compounds
- Super Class
- Lipids and lipid-like molecules
- Class
- Steroids and steroid derivatives
- Sub Class
- Steroid esters
- Direct Parent
- Steroid esters
- Alternative Parents
- Androstane steroids / Piperidines / Dicarboxylic acids and derivatives / Tetraalkylammonium salts / Carboxylic acid esters / Azacyclic compounds / Organopnictogen compounds / Organic salts / Organic oxides / Hydrocarbon derivatives show 3 more
- Substituents
- Aliphatic heteropolycyclic compound / Amine / Androstane-skeleton / Azacycle / Carbonyl group / Carboxylic acid derivative / Carboxylic acid ester / Dicarboxylic acid or derivatives / Hydrocarbon derivative / Organic cation show 12 more
- Molecular Framework
- Aliphatic heteropolycyclic compounds
- External Descriptors
- acetate ester, steroid ester (CHEBI:7907)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- J76UF062FS
- CAS number
- 16974-53-1
- InChI Key
- GVEAYVLWDAFXET-XGHATYIMSA-N
- InChI
- 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
- IUPAC Name
- 1-[(1R,2S,3aS,3bR,5aS,7S,8S,9aS,9bS,11aS)-1,7-bis(acetyloxy)-9a,11a-dimethyl-8-(1-methylpiperidin-1-ium-1-yl)-hexadecahydro-1H-cyclopenta[a]phenanthren-2-yl]-1-methylpiperidin-1-ium
- SMILES
- [H][C@@]12C[C@@H]([C@H](OC(C)=O)[C@@]1(C)CC[C@@]1([H])[C@@]2([H])CC[C@@]2([H])C[C@H](OC(C)=O)[C@H](C[C@]12C)[N+]1(C)CCCCC1)[N+]1(C)CCCCC1
References
- General References
- Not Available
- External Links
- Human Metabolome Database
- HMDB0015430
- KEGG Compound
- C07551
- PubChem Compound
- 441289
- PubChem Substance
- 46506118
- ChemSpider
- 390052
- 7883
- ChEBI
- 7907
- ChEMBL
- CHEMBL185073
- ZINC
- ZINC000004097383
- Therapeutic Targets Database
- DAP000123
- PharmGKB
- PA450771
- Guide to Pharmacology
- GtP Drug Page
- Wikipedia
- Pancuronium
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Baxter International Inc.
- Elkins-Sinn Inc.
- Hospira Inc.
- Teva Pharmaceutical Industries Ltd.
- Dosage Forms
Form Route Strength Solution 4.000 mg Solution Parenteral 4 mg Solution Intravenous 4 mg Injection, solution Intravenous 1 mg/1mL Injection, solution Intravenous 2 mg/1mL Solution Intravenous 1 mg / mL Solution Intravenous 2 mg / mL Injection Intravenous 4 mg/2ml Solution Intravenous 4.2 mg Injection, solution Intravenous Liquid Intravenous 1 mg / mL Liquid Intravenous 2 mg / mL Solution 2 mg/1ml - Prices
Unit description Cost Unit Pancuronium 2 mg/ml vial 2.59USD ml Pancuronium 1 mg/ml vial 0.13USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 215 °C PhysProp water solubility 5E+005 mg/L MERCK INDEX (1996) - Predicted Properties
Property Value Source Water Solubility 3.08e-06 mg/mL ALOGPS logP 1.04 ALOGPS logP -3.3 Chemaxon logS -8.3 ALOGPS pKa (Strongest Basic) -6.7 Chemaxon Physiological Charge 2 Chemaxon Hydrogen Acceptor Count 2 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 52.6 Å2 Chemaxon Rotatable Bond Count 6 Chemaxon Refractivity 185.22 m3·mol-1 Chemaxon Polarizability 69.56 Å3 Chemaxon Number of Rings 6 Chemaxon Bioavailability 1 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption - 0.8913 Blood Brain Barrier + 0.878 Caco-2 permeable + 0.5457 P-glycoprotein substrate Substrate 0.77 P-glycoprotein inhibitor I Inhibitor 0.6962 P-glycoprotein inhibitor II Inhibitor 0.6508 Renal organic cation transporter Non-inhibitor 0.6862 CYP450 2C9 substrate Non-substrate 0.8382 CYP450 2D6 substrate Non-substrate 0.7638 CYP450 3A4 substrate Substrate 0.742 CYP450 1A2 substrate Non-inhibitor 0.9045 CYP450 2C9 inhibitor Non-inhibitor 0.9229 CYP450 2D6 inhibitor Non-inhibitor 0.9231 CYP450 2C19 inhibitor Non-inhibitor 0.9026 CYP450 3A4 inhibitor Non-inhibitor 0.8309 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9368 Ames test Non AMES toxic 0.7499 Carcinogenicity Non-carcinogens 0.9265 Biodegradation Not ready biodegradable 0.8557 Rat acute toxicity 2.6653 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9021 hERG inhibition (predictor II) Non-inhibitor 0.7784
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 246.5010903 predictedDarkChem Lite v0.1.0 [M-H]- 239.6401903 predictedDarkChem Lite v0.1.0 [M-H]- 222.3792 predictedDeepCCS 1.0 (2019) [M+H]+ 246.5838903 predictedDarkChem Lite v0.1.0 [M+H]+ 240.5713903 predictedDarkChem Lite v0.1.0 [M+H]+ 224.1029 predictedDeepCCS 1.0 (2019) [M+Na]+ 245.6260903 predictedDarkChem Lite v0.1.0 [M+Na]+ 230.35663 predictedDeepCCS 1.0 (2019)
Targets
Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Drug binding
- Specific Function
- After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane.
- Gene Name
- CHRNA2
- Uniprot ID
- Q15822
- Uniprot Name
- Neuronal acetylcholine receptor subunit alpha-2
- Molecular Weight
- 59764.82 Da
References
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Dilger JP, Vidal AM, Liu M, Mettewie C, Suzuki T, Pham A, Demazumder D: Roles of amino acids and subunits in determining the inhibition of nicotinic acetylcholine receptors by competitive antagonists. Anesthesiology. 2007 Jun;106(6):1186-95. [Article]
- Jonsson Fagerlund M, Dabrowski M, Eriksson LI: Pharmacological characteristics of the inhibition of nondepolarizing neuromuscular blocking agents at human adult muscle nicotinic acetylcholine receptor. Anesthesiology. 2009 Jun;110(6):1244-52. doi: 10.1097/ALN.0b013e31819fade3. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- G-protein coupled acetylcholine receptor activity
- Specific Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
- Gene Name
- CHRM2
- Uniprot ID
- P08172
- Uniprot Name
- Muscarinic acetylcholine receptor M2
- Molecular Weight
- 51714.605 Da
References
- Milchert M, Spassov A, Meissner K, Nedeljkov V, Lehmann C, Wendt M, Loster BW, Mazurkiewicz-Janik M, Gedrange T, Pavlovic D: Skeletal muscle relaxants inhibit rat tracheal smooth muscle tone in vitro. J Physiol Pharmacol. 2009 Dec;60 Suppl 8:5-11. [Article]
- Cembala TM, Forde SC, Appadu BL, Lambert DG: Allosteric interaction of the neuromuscular blockers vecuronium and pancuronium with recombinant human muscarinic M2 receptors. Eur J Pharmacol. 2007 Aug 13;569(1-2):37-40. Epub 2007 May 22. [Article]
- Okanlami OA, Fryer AD, Hirshman C: Interaction of nondepolarizing muscle relaxants with M2 and M3 muscarinic receptors in guinea pig lung and heart. Anesthesiology. 1996 Jan;84(1):155-61. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Receptor activity
- Specific Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
- Gene Name
- CHRM3
- Uniprot ID
- P20309
- Uniprot Name
- Muscarinic acetylcholine receptor M3
- Molecular Weight
- 66127.445 Da
References
- Milchert M, Spassov A, Meissner K, Nedeljkov V, Lehmann C, Wendt M, Loster BW, Mazurkiewicz-Janik M, Gedrange T, Pavlovic D: Skeletal muscle relaxants inhibit rat tracheal smooth muscle tone in vitro. J Physiol Pharmacol. 2009 Dec;60 Suppl 8:5-11. [Article]
- Okanlami OA, Fryer AD, Hirshman C: Interaction of nondepolarizing muscle relaxants with M2 and M3 muscarinic receptors in guinea pig lung and heart. Anesthesiology. 1996 Jan;84(1):155-61. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Identical protein binding
- Specific Function
- Esterase with broad substrate specificity. Contributes to the inactivation of the neurotransmitter acetylcholine. Can degrade neurotoxic organophosphate esters.
- Gene Name
- BCHE
- Uniprot ID
- P06276
- Uniprot Name
- Cholinesterase
- Molecular Weight
- 68417.575 Da
References
- Stovner J, Oftedal N, Holmboe J: The inhibition of cholinesterases by pancuronium. Br J Anaesth. 1975 Sep;47(9):949-54. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Secondary active organic cation transmembrane transporter activity
- Specific Function
- Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnico...
- Gene Name
- SLC22A1
- Uniprot ID
- O15245
- Uniprot Name
- Solute carrier family 22 member 1
- Molecular Weight
- 61153.345 Da
References
- Lozano E, Herraez E, Briz O, Robledo VS, Hernandez-Iglesias J, Gonzalez-Hernandez A, Marin JJ: Role of the plasma membrane transporter of organic cations OCT1 and its genetic variants in modern liver pharmacology. Biomed Res Int. 2013;2013:692071. doi: 10.1155/2013/692071. Epub 2013 Jul 31. [Article]
- van Montfoort JE, Muller M, Groothuis GM, Meijer DK, Koepsell H, Meier PJ: Comparison of "type I" and "type II" organic cation transport by organic cation transporters and organic anion-transporting polypeptides. J Pharmacol Exp Ther. 2001 Jul;298(1):110-5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Quaternary ammonium group transmembrane transporter activity
- Specific Function
- Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creat...
- Gene Name
- SLC22A2
- Uniprot ID
- O15244
- Uniprot Name
- Solute carrier family 22 member 2
- Molecular Weight
- 62579.99 Da
References
- Gorboulev V, Ulzheimer JC, Akhoundova A, Ulzheimer-Teuber I, Karbach U, Quester S, Baumann C, Lang F, Busch AE, Koepsell H: Cloning and characterization of two human polyspecific organic cation transporters. DNA Cell Biol. 1997 Jul;16(7):871-81. [Article]
Drug created at June 30, 2007 18:07 / Updated at February 20, 2024 23:54