Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C34H57N2O4 |
Molecular Weight | 557.8274 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 10 / 10 |
E/Z Centers | 0 |
Charge | 1 |
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)N5CCCCC5)[N+]6(C)CCCCC6
InChI
InChIKey=BGSZAXLLHYERSY-XQIGCQGXSA-N
InChI=1S/C34H57N2O4/c1-23(37)39-31-20-25-12-13-26-27(34(25,4)22-29(31)35-16-8-6-9-17-35)14-15-33(3)28(26)21-30(32(33)40-24(2)38)36(5)18-10-7-11-19-36/h25-32H,6-22H2,1-5H3/q+1/t25-,26+,27-,28-,29-,30-,31-,32-,33-,34-/m0/s1
Molecular Formula | C34H57N2O4 |
Molecular Weight | 557.8274 |
Charge | 1 |
Count |
|
Stereochemistry | EPIMERIC |
Additional Stereochemistry | No |
Defined Stereocenters | 10 / 10 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionSources: https://www.drugbank.ca/drugs/DB01339Curator's Comment: Description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2010/075549s009lbl.pdf
Sources: https://www.drugbank.ca/drugs/DB01339
Curator's Comment: Description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2010/075549s009lbl.pdf
Vecuronium is a neuromuscular blocking agent. Vecuronium operates by competing for the cholinoceptors at the motor end plate thereby exerting its muscle-relaxing properties which are used adjunctively to general anesthesia. Vecuronium is a bisquaternary nitrogen compound that acts by competitively binding to nicotinic cholinergic receptors. The binding of vecuronium decreases the opportunity for acetylcholine to bind to the nicotinic receptor at the postjunctional membrane of the myoneural junction. As a result, depolarization is prevented, calcium ions are not released and muscle contraction does not occur. Vecuronium is indicated as an adjunct to general anesthesia, to facilitate endotracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
8.7 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Palliative | Vecuronium bromide Approved UseVecuronium bromide is indicated as an adjunct to general anesthesia, to facilitate endotracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation. Launch Date4.52044784E11 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1200 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2875724/ |
100 μg/kg bw single, intravenous dose: 100 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered: |
VECURONIUM plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
29.5 μg × min/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2875724/ |
100 μg/kg bw single, intravenous dose: 100 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered: |
VECURONIUM plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
49.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2875724/ |
100 μg/kg bw single, intravenous dose: 100 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered: |
VECURONIUM plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
75 min |
unknown |
VECURONIUM plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
20% |
unknown |
VECURONIUM plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
5 mg single, intravenous Overdose Dose: 5 mg Route: intravenous Route: single Dose: 5 mg Sources: |
unhealthy, 2 months n = 1 Health Status: unhealthy Condition: anesthesia Age Group: 2 months Sex: M Population Size: 1 Sources: |
Disc. AE: Paralysis... AEs leading to discontinuation/dose reduction: Paralysis (1 patient) Sources: |
0.12 mg/kg single, intravenous Dose: 0.12 mg/kg Route: intravenous Route: single Dose: 0.12 mg/kg Sources: |
unhealthy, 23 - 58 years n = 20 Health Status: unhealthy Condition: 27-81% total body surface area (TBSA) burn Age Group: 23 - 58 years Sex: unknown Population Size: 20 Sources: |
|
37 mg single, intravenous Overdose Dose: 37 mg Route: intravenous Route: single Dose: 37 mg Sources: |
unhealthy, 23 months n = 1 Health Status: unhealthy Condition: Down’s syndrome had corrective cardiac surgery for an atrioventricular canal defect Age Group: 23 months Sex: unknown Population Size: 1 Sources: |
Disc. AE: Sepsis... AEs leading to discontinuation/dose reduction: Sepsis (grade 5, 1 patient) Sources: |
0.112 mg/kg single, intravenous Dose: 0.112 mg/kg Route: intravenous Route: single Dose: 0.112 mg/kg Sources: |
unknown, adult n = 1 Health Status: unknown Age Group: adult Sex: unknown Population Size: 1 Sources: |
Other AEs: Bradycardia... |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Paralysis | 1 patient Disc. AE |
5 mg single, intravenous Overdose Dose: 5 mg Route: intravenous Route: single Dose: 5 mg Sources: |
unhealthy, 2 months n = 1 Health Status: unhealthy Condition: anesthesia Age Group: 2 months Sex: M Population Size: 1 Sources: |
Sepsis | grade 5, 1 patient Disc. AE |
37 mg single, intravenous Overdose Dose: 37 mg Route: intravenous Route: single Dose: 37 mg Sources: |
unhealthy, 23 months n = 1 Health Status: unhealthy Condition: Down’s syndrome had corrective cardiac surgery for an atrioventricular canal defect Age Group: 23 months Sex: unknown Population Size: 1 Sources: |
Bradycardia | 0.112 mg/kg single, intravenous Dose: 0.112 mg/kg Route: intravenous Route: single Dose: 0.112 mg/kg Sources: |
unknown, adult n = 1 Health Status: unknown Age Group: adult Sex: unknown Population Size: 1 Sources: |
PubMed
Title | Date | PubMed |
---|---|---|
Muscle relaxants in paediatric day case surgery. | 2001 |
|
Newer neuromuscular blocking agents: how do they compare with established agents? | 2001 |
|
Acute respiratory and metabolic acidosis induced by excessive muscle contraction during spinal evoked stimulation. | 2001 Apr |
|
[Anesthetic management of the King-Denborough syndrome]. | 2001 Apr |
|
Effect of halothane on the cerebral circulation in young children: a hysteresis phenomenon. | 2001 Apr |
|
Postoperative residual block after intermediate-acting neuromuscular blocking drugs. | 2001 Apr |
|
[The influence of age on hemodynamics and the dose requirements of propofol and buprenorphine in total intravenous anesthesia combined with continuous epidural anesthesia]. | 2001 Aug |
|
Overdistension in ventilated children. | 2001 Aug |
|
Increased sensitivity to depolarization and nondepolarizing neuromuscular blocking agents in young rat hemidiaphragms. | 2001 Aug |
|
Small dose of prostaglandin E(1) increases cardiac output without altering blood volume. | 2001 Aug |
|
Lightwand intubation is associated with less hemodynamic changes than fibreoptic intubation in normotensive, but not in hypertensive patients over the age of 60. | 2001 Dec |
|
Intravenous ketamine attenuates arterial pressure changes during the induction of anaesthesia with propofol. | 2001 Feb |
|
Effect of hypothermia on the hepatic uptake and biliary excretion of vecuronium in the isolated perfused rat liver. | 2001 Feb |
|
[A case of ventricular tachycardia immediately after electroconvulsive therapy in a schinzophrenic patient]. | 2001 Jan |
|
No substitute for the intravenous route. | 2001 Jan |
|
Vaginal physiological changes in a model of sexual arousal in anesthetized rats. | 2001 Jul |
|
Post-neonatal tetanus: issues in intensive care management. | 2001 Mar |
|
[Pulmonary edema in a child following laryngospasm triggered by a laryngeal mask airway during emergence from anesthesia]. | 2001 Mar |
|
Cesarean section in a patient with syringomyelia. | 2001 May |
|
Rapacuronium and bronchospasm. | 2001 May |
|
Rapacuronium: an alternative to succinylcholine for electroconvulsive therapy. | 2001 May |
|
[Two pediatric cases of malignant hyperthermia caused by sevoflurane]. | 2001 Nov |
|
Drug wastage contributes significantly to the cost of routine anesthesia care. | 2001 Nov |
|
Use of rapacuronium in a child with spinal muscular atrophy. | 2001 Nov |
|
Severe bradycardia during epilepsy surgery. | 2001 Oct |
|
[Anesthetic management of a patient with Dyggve-Melchior-Clausen syndrome]. | 2001 Oct |
|
The bispectral index during an anaphylactic circulatory arrest. | 2001 Oct |
|
Effects of rapacuronium on respiratory function during general anesthesia: a comparison with cis-atracurium. | 2001 Oct |
|
Different patterns of mast cell activation by muscle relaxants in human skin. | 2001 Sep |
|
Tracheal lidocaine attenuates the cardiovascular response to endotracheal intubation. | 2001 Sep |
|
Nasotracheal intubation: a randomized trial of two methods. | 2002 Jan |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.drugs.com/pro/vecuronium.html
The recommended initial dose of Vecuronium is 0.08 to 0.1 mg/kg (1.4 to 1.75 times the ED90) given as an intravenous bolus injection. This dose can be expected to produce good or excellent non-emergency intubation conditions in 2.5 to 3 minutes after injection. Under balanced anesthesia, clinically required neuromuscular blockade lasts approximately 25-30 minutes, with recovery to 25% of control achieved approximately 25 to 40 minutes after injection and recovery to 95% of control achieved approximately 45-65 minutes after injection. In the presence of potent inhalation anesthetics, the neuromuscular blocking effect of Vecuronium is enhanced. If Vecuronium is first administered more than 5 minutes after the start of inhalation agent or when steady-state has been achieved, the initial Vecuronium bromide dose may be reduced by approximately 15%, i.e., 0.06 to 0.085 mg/kg.
Route of Administration:
Intravenous
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/21986576
Magnesium sulfate at the concentrations of 1, 3, and 6 umol/L markedly enhanced the inhibition of vecuronium (10 nmol/L) on adult muscle-type acetylcholine receptors expressed in HEK293 cells.
Substance Class |
Chemical
Created
by
admin
on
Edited
Wed Jul 05 23:55:53 UTC 2023
by
admin
on
Wed Jul 05 23:55:53 UTC 2023
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Record UNII |
5438723848
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Record Status |
Validated (UNII)
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Record Version |
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WHO-ATC |
M03AC03
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WHO-VATC |
QM03AC03
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WHO-ESSENTIAL MEDICINES LIST |
20
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NDF-RT |
N0000175720
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NCI_THESAURUS |
C66886
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NDF-RT |
N0000175732
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Vecuronium
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5438723848
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C87317
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5438723848
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DTXSID1044146
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71535
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86029-43-8
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4002
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DB01339
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100000087879
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39765
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Vecuronium
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SUB05084MIG
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1546399
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2811
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METABOLITE -> PARENT |
rarely detected in human plasma; recovered by T-tube in some patients
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ACTIVE MOIETY |
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Biological Half-life | PHARMACOKINETIC |
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